Abstract

The present invention relates to compounds of general formula (I), wherein: X is selected from a group consisting of H; OH; SH; CF3; F; Cl; Br; I; C1 to C6 alkyl; C1 to C6 alkyloxy; C1 to C6 alkylthio; NH2; C1 to C6 alkylamino; di(C1 to C6 alkyl)amino; NO2; COOH; Y is selected from a group consisting of nitrogen; carbon, which can optionally be substituted with OH or F; oxygen; N-oxide; Z atoms are independently selected from the group consisting of carbon and nitrogen, whereas R is only present when the valence of Z allows it; and whereas at least one Z is carbon; and whereas n=0 or 1; L is covalent bond or —C(O)—; R are independently selected from the group consisting of H; C1 to C6 alkyl; C1 to C6 alkyloxy; C6 to C10 aryloxy; benzyloxy; C1 to C6 alkylthio; C6 to C10 arylthio; F; Cl; Br; I; OH; SH; NH2; C1 to C6 alkylamino; di(C1 to C6 alkyl)amino; C1 to C6 acylamino; di(C1 to C6 acyl)amino; C6 to C10 arylamino; di(C6 to C10 aryl)amino; CN; OH; nitro; COORn, C(O)NHRn, C(O)N(Rn)2, wherein Rn is independently H or C1 to C10 alkyl or C6 to C10 aryl; or neighboring two R together with neighboring two Z form a six-membered ring, optionally substituted with one or more substituents independently selected from the group consisting of OH, SH, CF3, F, Cl, Br, I, C1 to C6 alkyl, C1 to C6 alkyloxy, C1 to C6 alkylthio, NH2, C1 to C6 alkylamino, di(C1 to C6 alkyl)amino, NO2, COOH, COORn, C(O)NHRn, C(O)N(Rn)2, wherein Rn is independently H or C1 to C10 alkyl or C6 to C10 aryl; or X and the neighboring carbon, Z and R form a six-membered ring, optionally substituted with one or more substituents independently selected from the group consisting of OH, SH, CF3, F, Cl, Br, I, C1 to C6 alkyl, C1 to C6 alkyloxy, C1 to C6 alkylthio, NH2, C1 to C6 alkylamino, di(C1 to C6 alkyl)amino, NO2, COOH, COORn, C(O)NHRn, C(O)N(Rn)2, wherein Rn is independently H or C1 to C10 alkyl or C6 to C10 aryl; R1 is selected from the group consisting of H; —(C1 to C6 alkyl); benzyl, which can be optionally substituted independently with one or more substituents selected from nitro, OH; —(C1 to C2 alkylen)COOH, the alkylen of which can optionally be substituted with C1 to C6 alkyl; —CH2P(O)(OH)2; —CH2P(O)(OH)(C1 to C6 alkyl); The present invention relates to compounds of general formula (I), wherein: X is selected from a group consisting of H; OH; SH; CF3; F; Cl; Br; I; C1 to C6 alkyl; C1 to C6 alkyloxy; C1 to C6 alkylthio; NH2; C1 to C6 alkylamino; di(C1 to C6 alkyl)amino; NO2; COOH; Y is selected from a group consisting of nitrogen; carbon, which can optionally be substituted with OH or F; oxygen; N-oxide; Z atoms are independently selected from the group consisting of carbon and nitrogen, whereas R is only present when the valence of Z allows it; and whereas at least one Z is carbon; and whereas n=0 or 1; L is covalent bond or —C(O)—; R are independently selected from the group consisting of H; C1 to C6 alkyl; C1 to C6 alkyloxy; C6 to C10 aryloxy; benzyloxy; C1 to C6 alkylthio; C6 to C10 arylthio; F; Cl; Br; I; OH; SH; NH2; C1 to C6 alkylamino; di(C1 to C6 alkyl)amino; C1 to C6 acylamino; di(C1 to C6 acyl)amino; C6 to C10 arylamino; di(C6 to C10 aryl)amino; CN; OH; nitro; COORn, C(O)NHRn, C(O)N(Rn)2, wherein Rn is independently H or C1 to C10 alkyl or C6 to C10 aryl; or neighboring two R together with neighboring two Z form a six-membered ring, optionally substituted with one or more substituents independently selected from the group consisting of OH, SH, CF3, F, Cl, Br, I, C1 to C6 alkyl, C1 to C6 alkyloxy, C1 to C6 alkylthio, NH2, C1 to C6 alkylamino, di(C1 to C6 alkyl)amino, NO2, COOH, COORn, C(O)NHRn, C(O)N(Rn)2, wherein Rn is independently H or C1 to C10 alkyl or C6 to C10 aryl; or X and the neighboring carbon, Z and R form a six-membered ring, optionally substituted with one or more substituents independently selected from the group consisting of OH, SH, CF3, F, Cl, Br, I, C1 to C6 alkyl, C1 to C6 alkyloxy, C1 to C6 alkylthio, NH2, C1 to C6 alkylamino, di(C1 to C6 alkyl)amino, NO2, COOH, COORn, C(O)NHRn, C(O)N(Rn)2, wherein Rn is independently H or C1 to C10 alkyl or C6 to C10 aryl; R1 is selected from the group consisting of H; —(C1 to C6 alkyl); benzyl, which can be optionally substituted independently with one or more substituents selected from nitro, OH; —(C1 to C2 alkylen)COOH, the alkylen of which can optionally be substituted with C1 to C6 alkyl; —CH2P(O)(OH)2; —CH2P(O)(OH)(C1 to C6 alkyl); The present invention relates to compounds of general formula (I), wherein: X is selected from a group consisting of H; OH; SH; CF3; F; Cl; Br; I; C1 to C6 alkyl; C1 to C6 alkyloxy; C1 to C6 alkylthio; NH2; C1 to C6 alkylamino; di(C1 to C6 alkyl)amino; NO2; COOH; Y is selected from a group consisting of nitrogen; carbon, which can optionally be substituted with OH or F; oxygen; N-oxide; Z atoms are independently selected from the group consisting of carbon and nitrogen, whereas R is only present when the valence of Z allows it; and whereas at least one Z is carbon; and whereas n=0 or 1; L is covalent bond or —C(O)—; R are independently selected from the group consisting of H; C1 to C6 alkyl; C1 to C6 alkyloxy; C6 to C10 aryloxy; benzyloxy; C1 to C6 alkylthio; C6 to C10 arylthio; F; Cl; Br; I; OH; SH; NH2; C1 to C6 alkylamino; di(C1 to C6 alkyl)amino; C1 to C6 acylamino; di(C1 to C6 acyl)amino; C6 to C10 arylamino; di(C6 to C10 aryl)amino; CN; OH; nitro; COORn, C(O)NHRn, C(O)N(Rn)2, wherein Rn is independently H or C1 to C10 alkyl or C6 to C10 aryl; or neighboring two R together with neighboring two Z form a six-membered ring, optionally substituted with one or more substituents independently selected from the group consisting of OH, SH, CF3, F, Cl, Br, I, C1 to C6 alkyl, C1 to C6 alkyloxy, C1 to C6 alkylthio, NH2, C1 to C6 alkylamino, di(C1 to C6 alkyl)amino, NO2, COOH, COORn, C(O)NHRn, C(O)N(Rn)2, wherein Rn is independently H or C1 to C10 alkyl or C6 to C10 aryl; or X and the neighboring carbon, Z and R form a six-membered ring, optionally substituted with one or more substituents independently selected from the group consisting of OH, SH, CF3, F, Cl, Br, I, C1 to C6 alkyl, C1 to C6 alkyloxy, C1 to C6 alkylthio, NH2, C1 to C6 alkylamino, di(C1 to C6 alkyl)amino, NO2, COOH, COORn, C(O)NHRn, C(O)N(Rn)2, wherein Rn is independently H or C1 to C10 alkyl or C6 to C10 aryl; R1 is selected from the group consisting of H; —(C1 to C6 alkyl); benzyl, which can be optionally substituted independently with one or more substituents selected from nitro, OH; —(C1 to C2 alkylen)COOH, the alkylen of which can optionally be substituted with C1 to C6 alkyl; —CH2P(O)(OH)2; —CH2P(O)(OH)(C1 to C6 alkyl); for chromatographic separation of rare earth elements and/or s-, p-, d-metals, as well as to the method of the separation of rare earth elements.

IPC Classes  ?

• B01D 15/08 - Selective adsorption, e.g. chromatography
• C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C22B 59/00 - Obtaining rare earth metals

Abstract

The invention relates to small molecule inhibitors of formula (I) targeting the nsp14 protein of SARS- CoV-2 and other coronaviruses, for use as antiviral agents directly targeting viral proteins.

IPC Classes  ?

• C07H 19/14 - Pyrrolo-pyrimidine radicals
• C07H 19/23 - Heterocyclic radicals containing two or more heterocyclic rings condensed among themselves or condensed with a common carbocyclic ring system, not provided for in groups
• A61P 31/14 - Antivirals for RNA viruses

Abstract

The present invention relates to compounds of general formula (I) for use as complexing agents. The invention further relates to the coordination compounds thereof, peptide conjugates, method of their preparation and use thereof. The present invention relates to compounds of general formula (I) for use as complexing agents. The invention further relates to the coordination compounds thereof, peptide conjugates, method of their preparation and use thereof.

IPC Classes  ?

• G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids
• C07B 59/00 - Introduction of isotopes of elements into organic compounds
• G01N 1/40 - Concentrating samples
• G01N 33/60 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving labelled substances involving radioactive labelled substances

Abstract

The present invention relates to a crosslinked polymer material detectable by radiological imaging (radiography or radiology), in particular X-ray imaging, radiography, computed tomography, sciascopy, sciagraphy, comprising a biocompatible polymeric backbone comprising primary groups, linker groups, and radiodense imaging groups; wherein at least part of the primary groups are covalently bonded to the linker groups; and wherein at least part of the imaging groups are covalently bonded to each other and/or to one or more of the linker groups. The present invention further relates to a method to prepare said crosslinked polymer material, and uses of said crosslinked polymer material in biomedical applications such as biofabrication, tissue engineering, and medical devices.

IPC Classes  ?

• A61K 49/04 - X-ray contrast preparations
• A61L 26/00 - Chemical aspects of, or use of materials for, liquid bandages
• A61L 27/22 - Polypeptides or derivatives thereof
• A61L 27/52 - Hydrogels or hydrocolloids
• A61L 15/00 - Chemical aspects of, or use of materials for, bandages, dressings or absorbent pads

Abstract

The present disclosure provides deoxyribozymes that generate fluorescent or chromogeneic products by catalyzing the transfer of a phosphate from a substrate. Kits comprising any of the deoxyribozymes described herein are also provided by the present disclosure. The present disclosure also provides methods for identifying such deoxyribozymes. Oligonucleotide sensors that utilize the deoxyribozymes described herein and are capable of generating a fluorescent or chromogeneic product only in the presence of a specific ligand (e.g., a particular target nucleic acid sequence) are also provided by the present disclosure, as well as methods of using the same to detect the presence of a target nucleic acid sequence. The present disclosure further provides sensors that utilize the deoxyribozymes described herein to detect RNase activity or to detect DNase activity.

IPC Classes  ?

• C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides

Abstract

The present invention relates to novel compounds, to said compounds for use as a medicine, more in particular for the prevention or treatment of diseases mediated by activity of cGAS, yet more in particular for the prevention or treatment of inflammation conditions or cancer. The present invention also relates to a method for the prevention or treatment of said diseases comprising the use of the novel compounds. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the novel compounds as well as to said compositions or preparations for use as a medicine, more preferably for the prevention or treatment of diseases mediated by activity of cGAS, yet more in particular for the prevention or treatment of inflammation conditions or cancer. The present invention also relates to processes for the preparation of said compounds.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 17/06 - Antipsoriatics
• A61P 25/16 - Anti-Parkinson drugs
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 35/00 - Antineoplastic agents
• A61P 37/00 - Drugs for immunological or allergic disorders
• A61P 37/02 - Immunomodulators

Abstract

The present invention relates to 4-amino-2,6-bis(phenylmethylen)cyclohexanones of general formula I wherein R1, R2, R3and R4are independently selected from the group comprising a hydrogen atom, a hydroxy group, a C1-C3 alkoxy group, a trifluoromethoxy group, and a difluoromethoxy group; and R5and R6are independently selected from the group consisting of a C1-C3 alkyl and a hydrogen atom, or R5is a hydrogen atom and R6is an acyl or thioacyl group of general formula II or a sulfonic group of general formula III wherein X is O or S; R7is selected from a group consisting of R8and NH-R8, wherein R822n222nn-(C1-C3 alkyl), C6-C12 aryl, five- to nine-membered heteroaryl, (C6-C12)aryl-(C1-C3)alkyl-, five- to seven-membered heteroaryl-(C1-C3)alkyl-, five- to seven- membered heteroaryl-O-(C1-C3)alkyl-, (C1-C3 alkyl)O-C(O)-(C1-C3)alkyl-, wherein n is 1, 2, 3, 4 or 5, wherein substituent R8222C(=O)-(C1-C3 alkoxy), NHR9, wherein R9is selected from C1–C3 alkyl and NR1022, wherein R10are independently selected from C1-C3 alkyl or both R10together are formed by C2-C5 alkylene, with the proviso that at least one of the substituents R1and R2is not a hydrogen atom, and at least one of the substituents R3and R4 is not a hydrogen atom; and their pharmaceutically acceptable salts, addition salts and solvates. Said compounds are suitable for the treatment of proteinopathies, viral diseases, and diseases directly related to elevated levels of ferroptosis, such as stroke, rhabdomyolysis, non-alcoholic steatohepatitis, acute pancreatitis, and psoriasis.

IPC Classes  ?

• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 31/12 - Antivirals
• C07C 225/20 - Compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly-bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of the carbon skeleton
• C07C 233/32 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by doubly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a ring other than a six-membered aromatic ring
• C07C 233/61 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by doubly-bound oxygen atoms
• C07C 235/14 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
• C07C 237/04 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
• C07C 237/30 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having the nitrogen atom of the carboxamide group bound to hydrogen atoms or to acyclic carbon atoms
• C07C 275/26 - Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of rings other than six-membered aromatic rings
• C07C 275/34 - Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by singly-bound oxygen atoms having nitrogen atoms of urea groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
• C07C 307/08 - Diamides of sulfuric acids having nitrogen atoms of the sulfamide groups bound to carbon atoms of rings other than six-membered aromatic rings
• C07C 311/07 - Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
• C07C 311/14 - Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of rings other than six-membered aromatic rings
• C07C 311/29 - Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring

Abstract

The present invention relates to the use of bis(phenylmethylene)cycloalkanones and heterocyclic analogues thereof in human and veterinary medicine, for the treatment of diseases caused by the presence or elevated levels of metastable proteins in the cell, imbalances in protein homeostasis and proteotoxic stress, in general proteinopathy, in particular their use in the treatment of neurodegenerative diseases, such as amyotrophic lateral sclerosis (ALS), Parkinson's disease (PD), Alzheimer's disease (AD), Kennedy's disease (KD), Huntington's disease (HD), Creutzfeldt-Jakob disease (CJD), spinocerebellar ataxia (SCA), dentatorubral- pallidoluysian atrophy, transthyretin familial amyloid polyneuropathy, systemic amyloidosis, organ- confined amyloidosis, cystic fibrosis, and diabetes. Furthermore, the invention provides novel bis(phenylmethylene)cycloalkanones.

IPC Classes  ?

• A61K 31/122 - Ketones having the oxygen atom directly attached to a ring, e.g. quinones, vitamin K1, anthralin
• A61K 31/351 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
• A61K 31/382 - Heterocyclic compounds having sulfur as a ring hetero atom having six-membered rings, e.g. thioxanthenes
• A61K 31/45 - Non-condensed piperidines, e.g. piperocaine having oxo groups directly attached to the heterocyclic ring, e.g. cycloheximide
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics

Abstract

The invention provides 7-substituted 7-deazaadenine-containing 2′,3′-cyclic dinucleotides of general formula I, wherein R is selected from the group comprising C1-C5 alkyl; C6-C16 aryl, optionally substituted by at least one substituent selected from C6-C16 aryl or (C6-C16 aryloxy) C1-C5 alkyl; C4-C12 heteroaryl, comprising at least one O atom; C4-C12 heteroaryl, comprising at least one S atom, and pharmaceutically acceptable salts thereof. The compounds according to the invention show strong activation of protein STING (stimulator of interferon genes) and, consequently, stimulation of the signal transduction pathway that induces interferons and other cytokines/chemokines. (I) The invention provides 7-substituted 7-deazaadenine-containing 2′,3′-cyclic dinucleotides of general formula I, wherein R is selected from the group comprising C1-C5 alkyl; C6-C16 aryl, optionally substituted by at least one substituent selected from C6-C16 aryl or (C6-C16 aryloxy) C1-C5 alkyl; C4-C12 heteroaryl, comprising at least one O atom; C4-C12 heteroaryl, comprising at least one S atom, and pharmaceutically acceptable salts thereof. The compounds according to the invention show strong activation of protein STING (stimulator of interferon genes) and, consequently, stimulation of the signal transduction pathway that induces interferons and other cytokines/chemokines. (I)

IPC Classes  ?

• C07H 21/02 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical
• A61K 31/7084 - Compounds having two nucleosides or nucleotides, e.g. nicotinamide-adenine dinucleotide, flavine-adenine dinucleotide

Abstract

The present invention relates to a lipidoid of general formula I, wherein X is selected from —C(═O)NH—, —C(═O)O—, —C(═S)O—, —C(═O)S—, —C(═S)S—, —C(═O)NHNH—, —CH2—, —O—, —OC(═O)—, —S—, —SC(═O)—, —NH—, —NHNH—, —NHC(═O)—, —NHNHC(═O)—, —C═C—, —CH═CH—, a five-membered heterocycle containing at least 2 nitrogen atoms, —CH2C(═O)NH—, —CH2C(═S)O—, —CH2C(═S)S—, —CH2C(═O)NHNH—, —N═CH—, —CH═N—, —NH—N═CH—, and —CH═N—NH—; Y is alkylene C2-C10 chain; R1 is selected from alkyl C1-C46, alkenyl C2-C46, alkynyl C2-C46; Z is selected from H, —OH, —CH3, —CH2OH, —NH2, —C(═O)NH2, —CONH(CH2)2OH, —CON[(CH2)2OH]2, —CONHCH(CH2OH)2, —CONHCH2CH(—OH)CH2OH, —CONH(CH2)2C(═O)NH2, —CON[CH2C(═O)NH2]2, —CONH(CH2)2NHC(═O)NH2, —CONH(CH2)3—N+(CH3)2—(CH2)2—SO3—, —CONH(CH2)3—N+(CH3)2—(CH2)2—COO−, —COO(CH2)2—O—P(═O)(O—)—O(CH2)2—N+(CH3)3, —N+(CH3)2—(CH2)3—SO3—, —N+(CH3)2—(CH2)2—COO−, formula (II), and formula (III), wherein R2 is independently selected from hydrogen and —CH3; E is independently selected from O and S atoms; n is an integer within the range of from 1 to 5; and T is selected from —X—Y—N(R1)2, —C(═O)O(C1-C3 alkyl), —C(═O)OCH2CH2OH, formula (IV), formula (V), formula (VI), —C(═O)OH, —CONH(CH2)2OH, —CON[(CH2)2OH]2, —CONHCH(CH2OH)2, CONH(CH2)2C(═O)NH2, —CON[CH2C(═O)NH2]2, —CONHCH[C(═O)NH2]2, —CONH(CH2)2NHC(═O)NH2, —C(═O)NH2, —CONH(CH2)3—N+(CH3)2—(CH2)2—SO3—, —CONH(CH2)3—N+(CH3)2—(CH2)2—COO−, —NH2, —NHC(═O)CH3, —COO(CH2)2—O—P(═O)(O—)—O(CH2)2—N+(CH3)3, —OH, —O(C1-C3 alkyl), —NHC(═O)NH(CH3), —NHC(═S)N(CH3)2, —NHC(═S)NH(CH3), —NHC(═N—CN)NH2, —NHC(═N—CN)NH(CH3), —NHC(═N—CN)N(CH3)2, —NHC[═N—S(═O)2NH2]NH2, —N+(CH3)2—(CH2)3—SO3—, —N+(CH3)2—(CH2)2—COO−, wherein R2, E and n are as defined above; and/or if Z is —OH or —CH2OH, and T is —C(═O)OH, then Z together with T and three carbon atoms between them may form a cyclic lactone containing 4 to 5 carbon atoms; and pharmaceutically acceptable salts, addition salts and solvates thereof. This lipidoid is useful as a transfection agent. The invention further describes transfection reagents, transfection particles containing this lipidoid, and their use. The present invention relates to a lipidoid of general formula I, wherein X is selected from —C(═O)NH—, —C(═O)O—, —C(═S)O—, —C(═O)S—, —C(═S)S—, —C(═O)NHNH—, —CH2—, —O—, —OC(═O)—, —S—, —SC(═O)—, —NH—, —NHNH—, —NHC(═O)—, —NHNHC(═O)—, —C═C—, —CH═CH—, a five-membered heterocycle containing at least 2 nitrogen atoms, —CH2C(═O)NH—, —CH2C(═S)O—, —CH2C(═S)S—, —CH2C(═O)NHNH—, —N═CH—, —CH═N—, —NH—N═CH—, and —CH═N—NH—; Y is alkylene C2-C10 chain; R1 is selected from alkyl C1-C46, alkenyl C2-C46, alkynyl C2-C46; Z is selected from H, —OH, —CH3, —CH2OH, —NH2, —C(═O)NH2, —CONH(CH2)2OH, —CON[(CH2)2OH]2, —CONHCH(CH2OH)2, —CONHCH2CH(—OH)CH2OH, —CONH(CH2)2C(═O)NH2, —CON[CH2C(═O)NH2]2, —CONH(CH2)2NHC(═O)NH2, —CONH(CH2)3—N+(CH3)2—(CH2)2—SO3—, —CONH(CH2)3—N+(CH3)2—(CH2)2—COO−, —COO(CH2)2—O—P(═O)(O—)—O(CH2)2—N+(CH3)3, —N+(CH3)2—(CH2)3—SO3—, —N+(CH3)2—(CH2)2—COO−, formula (II), and formula (III), wherein R2 is independently selected from hydrogen and —CH3; E is independently selected from O and S atoms; n is an integer within the range of from 1 to 5; and T is selected from —X—Y—N(R1)2, —C(═O)O(C1-C3 alkyl), —C(═O)OCH2CH2OH, formula (IV), formula (V), formula (VI), —C(═O)OH, —CONH(CH2)2OH, —CON[(CH2)2OH]2, —CONHCH(CH2OH)2, CONH(CH2)2C(═O)NH2, —CON[CH2C(═O)NH2]2, —CONHCH[C(═O)NH2]2, —CONH(CH2)2NHC(═O)NH2, —C(═O)NH2, —CONH(CH2)3—N+(CH3)2—(CH2)2—SO3—, —CONH(CH2)3—N+(CH3)2—(CH2)2—COO−, —NH2, —NHC(═O)CH3, —COO(CH2)2—O—P(═O)(O—)—O(CH2)2—N+(CH3)3, —OH, —O(C1-C3 alkyl), —NHC(═O)NH(CH3), —NHC(═S)N(CH3)2, —NHC(═S)NH(CH3), —NHC(═N—CN)NH2, —NHC(═N—CN)NH(CH3), —NHC(═N—CN)N(CH3)2, —NHC[═N—S(═O)2NH2]NH2, —N+(CH3)2—(CH2)3—SO3—, —N+(CH3)2—(CH2)2—COO−, wherein R2, E and n are as defined above; and/or if Z is —OH or —CH2OH, and T is —C(═O)OH, then Z together with T and three carbon atoms between them may form a cyclic lactone containing 4 to 5 carbon atoms; and pharmaceutically acceptable salts, addition salts and solvates thereof. This lipidoid is useful as a transfection agent. The invention further describes transfection reagents, transfection particles containing this lipidoid, and their use.

IPC Classes  ?

• A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseasesGene therapy
• A61K 8/42 - Amides
• A61K 9/127 - Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
• A61K 9/51 - Nanocapsules
• C07C 233/62 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
• C07C 237/10 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms not being part of nitro or nitroso groups
• C07D 207/12 - Oxygen or sulfur atoms
• C07D 311/00 - Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
• C12N 15/88 - Introduction of foreign genetic material using processes not otherwise provided for, e.g. co-transformation using microencapsulation, e.g. using liposome vesicle

Abstract

The present disclosure provides prodrugs of 6-diazo-5-oxo-L-norleucine (DON) for use in treating or preventing a disease, disorder, or condition in which the inhibition of glutamine-utilizing enzymes provides a benefit.

IPC Classes  ?

• C07C 245/18 - Diazo compounds, i.e. compounds having the free valencies of N2 groups attached to the same carbon atom having diazo groups bound to acyclic carbon atoms of a carbon skeleton the carbon skeleton being further substituted by carboxyl groups
• A61K 31/655 - Azo (—N=N—), diazo (=N2), azoxy (N—O—N or N(=O)—N), azido (—N3) or diazoamino (—N=N—N) compounds
• C07D 209/20 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals substituted additionally by nitrogen atoms, e.g. tryptophane
• C07D 213/56 - Amides
• C07D 233/06 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to ring carbon atoms
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 471/18 - Bridged systems

Abstract

The present invention relates to self-phosphorylating deoxyribozymes containing or consisting of the nucleotide sequence: 5′-X1X2X3AX4X5-R1-X6X7X8X9X10-bp1-helix1-R2-helix2-bp2-X11TGACX12TGGGAX13-helix3-X14-R3-3′ (SEQ ID NO. 1) wherein X1 is G or T; X2 is G or T; X3 is A or C; X4 is G or T; X5 is A or T; X6 is G or T or A; X7 is A or C or G or T; X8 is A or G or T; X9 is T or C or A or G; X10 is A or T or G; X11 is G or A; X12 is T or C or G; X13 is T or G or C; X14 is G or A or C or T; R1 represents a nucleotide sequence containing 3 to 30 nucleotides; R2 represents a nucleotide sequence containing 3 to 30 nucleotides; R3 represents a nucleotide sequence containing 0 to 30 nucleotides; bp1 and bp2 are nucleotides selected from G, A, C, T, which together form a base pair; helix1, helix2, and helix3 each independently denotes a nucleotide sequence preferably containing 4 or more nucleotides, wherein helix1, helix2, and helix3 together form a triple helical structure. The deoxyribozymes of the present invention may be used for detection of chemiluminescent substrates, or for detection of analytes (ligands) based on chemiluminescent reaction of the substrates catalyzed by the deoxyribozymes.

IPC Classes  ?

• C12Q 1/6823 - Release of bound markers
• C12N 15/11 - DNA or RNA fragmentsModified forms thereof

Abstract

2232n322P(=O)(OH)Ph; Z is H or A; for preparation of a multimodal PET/MRI contrast agents. The invention also relates to Gd(III) complexes of compound of general formula (I), wherein R is 18F, as multimodal PET/MRI contrast agents.

IPC Classes  ?

• A61K 49/00 - Preparations for testing in vivo
• A61K 49/10 - Organic compounds
• C07B 59/00 - Introduction of isotopes of elements into organic compounds
• A61K 51/04 - Organic compounds
• C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

IPC Classes  ?

• C07K 14/435 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals

Abstract

: The present invention relates to a protein derived from the extracellular domain of the surface protein ISG65 (invariant surface glycoprotein 65 (Tbg.972.2.1600)) of the human parasite Trypanosoma brucei gambiense. The ISG65-derived protein is useful in the treatment of complement dysregulation diseases. In one aspect, the present invention provides a novel thermostable mutant of ISG65.

IPC Classes  ?

• C07K 14/435 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals

Abstract

Surface modified particles have a core, an inner shell and an outer shell. The core is formed of silica or is hollow, the inner shell is formed by a layer of metal, and the outer shell is formed by a biocompatible polymer brush. The particles allow for direct optical detection of biomolecules such as nucleic acids, proteins, polysaccharides and glycoproteins in biological samples.

IPC Classes  ?

• G01N 33/58 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving labelled substances
• B82Y 15/00 - Nanotechnology for interacting, sensing or actuating, e.g. quantum dots as markers in protein assays or molecular motors

Abstract

The present invention related to the use of compounds of general formula (I) for separations of rare earth elements (lanthanides) by precipitation, wherein R is selected from the group consisting of H; —CH2COOH; R2, R3, R4, R5 and R6 areindependently selected from the group consisting of H; OH; —NO2; —COOH; phenyl; and/or R2 and R3 or R3 and R4 or R4 and R5 or R5 and R6 The invention further relates to a method of separation of rare earth elements by precipitation. together with two neighbouring carbon atoms of the aromatic ring form a six-membered aromatic ring. The present invention related to the use of compounds of general formula (I) for separations of rare earth elements (lanthanides) by precipitation, wherein R is selected from the group consisting of H; —CH2COOH; R2, R3, R4, R5 and R6 areindependently selected from the group consisting of H; OH; —NO2; —COOH; phenyl; and/or R2 and R3 or R3 and R4 or R4 and R5 or R5 and R6 The invention further relates to a method of separation of rare earth elements by precipitation. together with two neighbouring carbon atoms of the aromatic ring form a six-membered aromatic ring.

IPC Classes  ?

• B01D 9/00 - Crystallisation
• C01F 17/13 - Preparation or treatment, e.g. separation or purification by using ion exchange resins, e.g. chelate resins
• C07D 257/02 - Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
• C22B 59/00 - Obtaining rare earth metals
• B01D 15/32 - Bonded phase chromatography, e.g. with normal bonded phase, reversed phase or hydrophobic interaction
• B01D 61/14 - UltrafiltrationMicrofiltration

Abstract

The subject of the present invention is a lipidoid of general formula (I), wherein X, Y, Z and R are as defined in the claims. This lipidoid is useful as a transfection agent. The invention further describes transfection agents, transfection particles containing this lipidoid, and their use. The subject of the present invention is a lipidoid of general formula (I), wherein X, Y, Z and R are as defined in the claims. This lipidoid is useful as a transfection agent. The invention further describes transfection agents, transfection particles containing this lipidoid, and their use.

IPC Classes  ?

• C07C 233/62 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
• A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseasesGene therapy
• A61K 9/51 - Nanocapsules
• C12N 15/11 - DNA or RNA fragmentsModified forms thereof
• A61P 43/00 - Drugs for specific purposes, not provided for in groups

Abstract

Quinolinecarboxamide compounds of general formula I exceed the previously known FAP inhibitors in affinity and inhibitory effect. These agents can be used to specifically target tumours for diagnostic and therapeutic purposes, or for laboratory purposes in the study of endogenous FAP expression.

IPC Classes  ?

• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• A61P 35/00 - Antineoplastic agents
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

Abstract

A protein-based probe for detecting the presence of one of two distinct states of a target membrane-associated molecule by means of polarization microscopy is disclosed. The probe contains an anchoring moiety consisting of at least one lipidated peptide and/or at least one transmembrane α-helical peptide, a peptide linker moiety having the length of at least 5 amino acids, wherein at least 50% of the amino acids forming the linker are selected from glycine, serine, and threonine, a fluorescent moiety, and an affinity binding moiety capable of binding the target membrane-associated molecule. The moieties are arranged in the order a-b-c-d or d-c-b-a in the direction from the N-terminus to the C-terminus. Methods of detecting presence or absence of the target molecule, detecting activated or inactive forms of the target molecule, and detecting the activation of the target molecule are also described.

IPC Classes  ?

• G01N 33/50 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing
• G01N 33/58 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving labelled substances
• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals

Abstract

The invention relates to antimicrobial peptides derived from the human protein ameloblastin, intended for therapeutic and biotechnological use, in particular for application onto layers, so-called biofilms, to prevent the growth of specific strains of bacterial microflora, to prevent or remove infectious agents from the surface of joint, dental and bone replacements and to prevent infection of orthopaedic implants.

IPC Classes  ?

• A61P 1/02 - Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
• A61K 38/10 - Peptides having 12 to 20 amino acids
• A61P 31/04 - Antibacterial agents
• C07K 7/08 - Linear peptides containing only normal peptide links having 12 to 20 amino acids
• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals

Abstract

in vitroin vivoin vivo.

IPC Classes  ?

• A61P 3/04 - AnorexiantsAntiobesity agents
• A61K 38/00 - Medicinal preparations containing peptides
• C07K 14/475 - Growth factorsGrowth regulators

Abstract

The present invention relates to compounds of general formula (I) for use as complexing agents. The invention further relates to the coordination compounds thereof, peptide conjugates, method of their preparation and use thereof.

IPC Classes  ?

• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• A61K 49/08 - Nuclear magnetic resonance [NMR] contrast preparationsMagnetic resonance imaging [MRI] contrast preparations characterised by the carrier
• A61K 49/12 - Macromolecular compounds
• C07D 471/22 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups in which the condensed systems contains four or more hetero rings
• C07F 9/6524 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having four or more nitrogen atoms as the only ring hetero atoms
• C07K 7/06 - Linear peptides containing only normal peptide links having 5 to 11 amino acids
• C07F 3/04 - Calcium compounds
• C07F 3/06 - Zinc compounds
• C07F 3/08 - Cadmium compounds
• C07F 7/24 - Lead compounds

Abstract

The present invention relates to compounds of general formula (I) for use as complexing agents. The invention further relates to the coordination compounds thereof, peptide conjugates, method of their preparation and use thereof.

IPC Classes  ?

• A61K 49/08 - Nuclear magnetic resonance [NMR] contrast preparationsMagnetic resonance imaging [MRI] contrast preparations characterised by the carrier
• A61K 49/12 - Macromolecular compounds
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 471/22 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups in which the condensed systems contains four or more hetero rings
• C07F 3/04 - Calcium compounds
• C07F 3/06 - Zinc compounds
• C07F 3/08 - Cadmium compounds
• C07F 7/24 - Lead compounds
• C07F 9/6524 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having four or more nitrogen atoms as the only ring hetero atoms
• C07K 7/06 - Linear peptides containing only normal peptide links having 5 to 11 amino acids

Abstract

The invention provides 7-substituted 7-deazaadenine-containing 2',3'-cyclic dinucleotides of general formula I, wherein R is selected from the group comprising C1-C5 alkyl; C6-C16 aryl, optionally substituted by at least one substituent selected from C6-C16 aryl or (C6-C16 aryloxy)C1-C5 alkyl; C4-C12 heteroaryl, comprising at least one O atom; C4-C12 heteroaryl, comprising at least one S atom, and pharmaceutically acceptable salts thereof. The compounds according to the invention show strong activation of protein STING (stimulator of interferon genes) and, consequently, stimulation of the signal transduction pathway that induces interferons and other cytokines/chemokines. (I)

IPC Classes  ?

• A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
• C07H 21/02 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical

Abstract

The invention provides 7-substituted 7-deazaadenine-containing 2',3'-cyclic dinucleotides of general formula I, wherein R is selected from the group comprising C1-C5 alkyl; C6-C16 aryl, optionally substituted by at least one substituent selected from C6-C16 aryl or (C6-C16 aryloxy)C1-C5 alkyl; C4-C12 heteroaryl, comprising at least one O atom; C4-C12 heteroaryl, comprising at least one S atom, and pharmaceutically acceptable salts thereof. The compounds according to the invention show strong activation of protein STING (stimulator of interferon genes) and, consequently, stimulation of the signal transduction pathway that induces interferons and other cytokines/chemokines. (I)

IPC Classes  ?

• C07H 21/02 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical
• A61P 35/00 - Antineoplastic agents
• A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin

Abstract

The present invention relates to a lipidoid of general formula I, wherein X is selected from -C(=O)NH-, -C(=O)O-, -C(=S)O-, -C(=O)S-, -C(=S)S-, -C(=O)NHNH-, -CH2-, -O-, -OC(=O)-, -S-, -SC(=O)-, -NH-, -NHNH-, -NHC(=O)-, -NHNHC(=O)-, -C?C-, -CH=CH-, a five-membered heterocycle containing at least 2 nitrogen atoms, -CH2C(=O)NH-, -CH2C(=S)O-, -CH2C(=S)S-, -CH2C(=O)NHNH-, -N=CH-, -CH=N-, -NH-N=CH-, and -CH=N-NH-; Y is alkylene C2-C10 chain; R1 is selected from alkyl C1-C46, alkenyl C2-C46, alkynyl C2-C46; Z is selected from H, -OH, -CH3, -CH2OH, -NH2, -C(=O)NH2, -CONH(CH2)2OH, -CON[(CH2)2OH]2, -CONHCH(CH2OH)2, -CONHCH2CH(-OH)CH2OH, -CONH(CH2)2C(=O)NH2, -CON[CH2C(=O)NH2]2, -CONH(CH2)2NHC(=O)NH2, -CONH(CH2)3-N+(CH3)2-(CH2)2-SO3?, -CONH(CH2)3-N+(CH3)2-(CH2)2-COO?, -COO(CH2)2-O-P(=O)(O?)-O(CH2)2-N+(CH3)3, -N+(CH3)2-(CH2)3-SO3?, -N+(CH3)2-(CH2)2-COO-, formula (II), and formula (III), wherein R2 is independently selected from hydrogen and -CH3; E is independently selected from O and S atoms; n is an integer within the range of from 1 to 5; and T is selected from -X-Y-N(R1)2, -C(=O)O(C1-C3 alkyl), -C(=O)OCH2CH2OH, formula (IV), formula (V), formula (VI), -C(=O)OH, -CONH(CH2)2OH, -CON[(CH2)2OH]2, -CONHCH(CH2OH)2, CONH(CH2)2C(=O)NH2, -CON[CH2C(=O)NH2]2, -CONHCH[C(=O)NH2]2, -CONH(CH2)2NHC(=O)NH2, -C(=O)NH2, -CONH(CH2)3-N+(CH3)2-(CH2)2-SO3?, -CONH(CH2)3-N+(CH3)2-(CH2)2-COO?, -NH2, -NHC(=O)CH3, -COO(CH2)2-O-P(=O)(O?)-O(CH2)2-N+(CH3)3, -OH, -O(C1-C3 alkyl), -NHC(=O)NH(CH3), -NHC(=S)N(CH3)2, -NHC(=S)NH(CH3), -NHC(=N-CN)NH2, -NHC(=N-CN)NH(CH3), -NHC(=N-CN)N(CH3)2, -NHC[=N-S(=O)2NH2]NH2, -N+(CH3)2-(CH2)3-SO3?, -N+(CH3)2-(CH2)2-COO?, wherein R2, E and n are as defined above; and/or if Z is -OH or -CH2OH, and T is -C(=O)OH, then Z together with T and three carbon atoms between them may form a cyclic lactone containing 4 to 5 carbon atoms; and pharmaceutically acceptable salts, addition salts and solvates thereof. This lipidoid is useful as a transfection agent. The invention further describes transfection reagents, transfection particles containing this lipidoid, and their use.

IPC Classes  ?

• C07C 233/62 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
• C07C 237/10 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms not being part of nitro or nitroso groups
• C07D 295/185 - Radicals derived from carboxylic acids from aliphatic carboxylic acids
• C07D 313/20 - Eight-membered rings condensed with carbocyclic rings or ring systems

Abstract

Lipophosphonoxins of general formula I, diastereomers and mixtures of diastereomers of compounds of general formula I and their pharmaceutically acceptable salts and hydrates as antibacterial agents, forming an active ingredient in pharmaceutical compositions for the treatment of resistant bacterial infections, disinfectants and/or selective culture media is disclosed.

IPC Classes  ?

• C07F 9/40 - Esters thereof

Abstract

2222221010 chain; R11462462463222222222222222222222233222322222222333223332222-COO-, formula (II), and formula (III), wherein R23nn is an integer within the range of from 1 to 5; and T is selected from -X-Y-N(R12132222222222222222222222332223233222232222331333232332222323332222-COO–, wherein R2n22OH, and T is -C(=O)OH, then Z together with T and three carbon atoms between them may form a cyclic lactone containing 4 to 5 carbon atoms; and pharmaceutically acceptable salts, addition salts and solvates thereof. This lipidoid is useful as a transfection agent. The invention further describes transfection reagents, transfection particles containing this lipidoid, and their use.

IPC Classes  ?

• C07C 233/62 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
• C07C 237/10 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms not being part of nitro or nitroso groups
• C07D 295/185 - Radicals derived from carboxylic acids from aliphatic carboxylic acids
• C07D 313/20 - Eight-membered rings condensed with carbocyclic rings or ring systems
• A61K 47/00 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient

Abstract

Glutamine antagonists and their use for treating oncological, immunological, and neurological diseases are disclosed. Also disclosed are methods for treating an oncological, immunological, infectious or neurological disease or disorder, the method comprising administering to a subject in need of treatment thereof a therapeutically effective amount of a glutamine antagonist of the disclosure or the pharmaceutical composition thereof. Also disclosed are methods of enhancing the effects of an immune checkpoint inhibitor, enabling a subject to respond to an immune checkpoint inhibitor, or enabling the toxicity or the dose or number of treatments with an immune checkpoint inhibitor to be reduced, comprising administering to a subject in need of treatment thereof a therapeutically effective amount of a glutamine antagonist of the disclosure or the pharmaceutical composition thereof, and an immune checkpoint inhibitor. Also disclosed are methods for treating an oncological, immunological, infectious or neurological disease or disorder that is refractory to checkpoint inhibitor therapy, the method comprising administering to a subject in need thereof, and having the refractory disease or disorder, a therapeutically effective amount of a glutamine antagonist of the disclosure or the pharmaceutical composition thereof.

IPC Classes  ?

• C07C 271/22 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
• A61P 35/00 - Antineoplastic agents
• C07C 245/18 - Diazo compounds, i.e. compounds having the free valencies of N2 groups attached to the same carbon atom having diazo groups bound to acyclic carbon atoms of a carbon skeleton the carbon skeleton being further substituted by carboxyl groups
• C07D 209/20 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals substituted additionally by nitrogen atoms, e.g. tryptophane

Abstract

Derivatives of human insulin that have a higher resistance to fibrillation caused by elevated temperature in comparison with human insulin are described. The derivatives of human insulin retain full biological activity. The derivatives can be useful for application in sampling devices destined for the treatment of diabetes.

IPC Classes  ?

• C07K 14/62 - Insulins
• A61P 3/00 - Drugs for disorders of the metabolism
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics

Abstract

The invention relates to a novel antibody binding to the RBD of the Spike protein of the SARS-CoV-2. The antibody recognizes a conservative conformational epitope of the Spike RBD protein, inhibits Spike RBD – ACE2 binding, and inhibits viral infection in Virus Neutralization Test (VNT). The inhibition of the viral infection was observed for the wild-type SARS-CoV-2 (variant B.1.) as well as for the variants of concern alpha (B.1.1.7), beta (B.1.351), gamma (P.1), delta (B.1.617.2) and omicron (B.1.1.529) of the SARS-CoV-2. The invention further provides the method for detecting and quantifying protective antibodies recognizing the SARS-CoV-2 Spike protein using the novel antibody.

IPC Classes  ?

• C07K 16/10 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from viruses from RNA viruses
• A61P 31/14 - Antivirals for RNA viruses
• G01N 33/577 - ImmunoassayBiospecific binding assayMaterials therefor involving monoclonal antibodies

Abstract

The present disclosure provides prodrugs of 6-diazo-5-oxo-L-norleucine (DON) for use in treating or preventing a disease, disorder, or condition in which the inhibition of glutamineutilizing enzymes provides a benefit.

IPC Classes  ?

• C07C 245/20 - Diazonium compounds

Abstract

A catheter that has a catheter tube everting inside-out during the process of catheterization is disclosed. The catheter tube has a plurality of longitudinal protrusions extending from the first end of the catheter tube through at least a portion of the catheter tube, and forming an angle of 0 degrees to 45 degrees with respect to the longitudinal axis of the catheter tube and facing radially inwards, and provides for dilating a circumference of the catheter tube upon everting the catheter tube inside-out from the first end of the catheter tube.

IPC Classes  ?

• A61M 25/01 - Introducing, guiding, advancing, emplacing or holding catheters
• B29C 48/00 - Extrusion moulding, i.e. expressing the moulding material through a die or nozzle which imparts the desired formApparatus therefor
• B29C 48/09 - Articles with cross-sections having partially or fully enclosed cavities, e.g. pipes or channels
• B29C 48/21 - Articles comprising two or more components, e.g. co-extruded layers the components being layers the layers being joined at their surfaces
• A61M 25/00 - CathetersHollow probes
• B29D 23/00 - Producing tubular articles

Abstract

The present invention relates to self-phosphorylating deoxyribozymes containing or consisting of the nucleotide sequence: 5´-X1X2X3AX4X5-R1-X6X7X8X9X10-bp1-helix1-R2-helix2-bp2-X11TGACX12TGGGAX13-helix3-X14-R3-3´ (SEQ ID NO. 1) wherein X1 is G or T; X2 is G or T; X3 is A or C; X4 is G or T; X5 is A or T; X6 is G or T or A; X7 is A or C or G or T; X8 is A or G or T; X9 is T or C or A or G; X10 is A or T or G; X11 is G or A; X12 is T or C or G; X13 is T or G or C; X14 is G or A or C or T; R1 represents a nucleotide sequence containing 3 to 30 nucleotides; R2 represents a nucleotide sequence containing 3 to 30 nucleotides; R3 represents a nucleotide sequence containing 0 to 30 nucleotides; bp1 and bp2 are nucleotides selected from G, A, C, T, which together form a base pair; helix1, helix2, and helix3 each independently denotes a nucleotide sequence preferably containing 4 or more nucleotides, wherein helix1, helix2, and helix3 together form a triple helical structure. The deoxyribozymes of the present invention may be used for detection of chemiluminescent substrates, or for detection of analytes (ligands) based on chemiluminescent reaction of the substrates catalyzed by the deoxyribozymes.

IPC Classes  ?

• C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
• C12N 15/115 - Aptamers, i.e. nucleic acids binding a target molecule specifically and with high affinity without hybridising therewith
• C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids

Abstract

The present invention relates to self-phosphorylating deoxyribozymes containing or consisting of the nucleotide sequence: 5´-X1X2X3AX4X5-R1-X6X7X8X9X10-bp1-helix1-R2-helix2-bp2-X11TGACX12TGGGAX13-helix3-X14-R3-3´ (SEQ ID NO. 1) wherein X1is G or T; X2is G or T; X3is A or C; X4is G or T; X5is A or T; X6is G or T or A; X7is A or C or G or T; X8is A or G or T; X9is T or C or A or G; X10is A or T or G; X11is G or A; X12is T or C or G; X13is T or G or C; X14is G or A or C or T; R1represents a nucleotide sequence containing 3 to 30 nucleotides; R2represents a nucleotide sequence containing 3 to 30 nucleotides; R3 represents a nucleotide sequence containing 0 to 30 nucleotides; bp1 and bp2 are nucleotides selected from G, A, C, T, which together form a base pair; helix1, helix2, and helix3 each independently denotes a nucleotide sequence preferably containing 4 or more nucleotides, wherein helix1, helix2, and helix3 together form a triple helical structure. The deoxyribozymes of the present invention may be used for detection of chemiluminescent substrates, or for detection of analytes (ligands) based on chemiluminescent reaction of the substrates catalyzed by the deoxyribozymes.

IPC Classes  ?

• C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
• C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids
• C12N 15/115 - Aptamers, i.e. nucleic acids binding a target molecule specifically and with high affinity without hybridising therewith

Abstract

2COOH; for chromatographic separation of rare earth elements and/or s-, p- and d-block metals, as well as to the method of the separation of rare earth elements.

IPC Classes  ?

• C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• B01D 15/42 - Selective adsorption, e.g. chromatography characterised by the development mode, e.g. by displacement or by elution
• C07B 59/00 - Introduction of isotopes of elements into organic compounds
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07F 9/6524 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having four or more nitrogen atoms as the only ring hetero atoms

Abstract

3 is independently selected from H; (C1-C6)alkyl.

IPC Classes  ?

• A61K 49/10 - Organic compounds
• A61K 49/14 - Peptides, e.g. proteins
• C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• C07F 5/00 - Compounds containing elements of Groups 3 or 13 of the Periodic Table
• C07K 5/078 - Dipeptides the first amino acid being heterocyclic, e.g. Pro, His, Trp

Abstract

A structurally novel class of heterocyclic compounds of general formula I wherein L1 is heteroaryl and L2 is heteroaryl or aryl is disclosed. The novel compounds are useful in a method of prevention or treatment of a condition that is mediated by the action, or by loss of action of Constitutive androstane receptor (CAR) receptor or its endogenous ligands. The present invention provides the novel compounds for medicinal use as well as pharmaceutical composition containing the compounds.

IPC Classes  ?

• C07D 513/04 - Ortho-condensed systems
• A61P 3/00 - Drugs for disorders of the metabolism
• C07D 471/04 - Ortho-condensed systems
• C07D 487/04 - Ortho-condensed systems

Abstract

A method for functionalization of an aromatic amino acid or a nucleobase with a fluoroalkyl-containing moiety RF, wherein the aromatic amino acid is reacted in the presence of at least one reductant with at least one hypervalent iodine fluoroalkyl reagent carrying the fluoroalkyl-containing moiety RF is disclosed. Novel hypervalent iodine fluoroalkyl reagents is also disclosed.

IPC Classes  ?

• C07K 1/107 - General processes for the preparation of peptides by chemical modification of precursor peptides
• C07B 39/00 - Halogenation
• C07C 43/225 - Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring containing halogen
• C07C 69/02 - Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen
• C07C 217/60 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by singly-bound oxygen atoms linked by carbon chains having two carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
• C07C 227/16 - Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof by reactions not involving the amino or carboxyl groups
• C07C 247/04 - Compounds containing azido groups with azido groups bound to acyclic carbon atoms of a carbon skeleton being saturated
• C07C 309/58 - Carboxylic acid groups or esters thereof
• C07D 209/16 - Tryptamines
• C07D 233/64 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
• C07H 1/00 - Processes for the preparation of sugar derivatives

Abstract

3α5β-steroid compounds of general formula I is disclosed. These compounds are useful in the treatment of epilepsy or comorbidities associated with epilepsy or conditions associated with convulsions, such as seizures associated with hypoxia, seizures associated with traumatic brain damage, seizures associated with intoxication, pathological changes caused by hyperexcitation, or in treatment of conditions accompanying epilepsy, such as affective disorders, depression, post-traumatic stress disorder (PTSD) and stress-related diseases, anxiety, schizophrenia and psychotic disorders, related ischemic CNS damage, neurodegenerative changes and disorders, multiple sclerosis. The compounds of general formula I also show age-specific efficacy.

IPC Classes  ?

• C07J 43/00 - Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
• A61P 25/08 - AntiepilepticsAnticonvulsants
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
• C07J 41/00 - Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring

Abstract

The present invention relates to the use of compounds of general formula (I) for separations of rare earth elements (lanthanides) by precipitation, wherein R1 is selected from the group consisting of H; -CH2COOH; R2, R3, R4, R5 and R6 are independently selected from the group consisting of H; OH; -NO2; -COOH; phenyl; and/or R2 and R3 or R3 and R4 or R4 and R5 or R5 and R6 together with two neighbouring carbon atoms of the aromatic ring form a six-membered aromatic ring. The invention further relates to a method of separation of rare earth elements by precipitation.

IPC Classes  ?

• C01F 17/13 - Preparation or treatment, e.g. separation or purification by using ion exchange resins, e.g. chelate resins
• C01F 17/271 - Chlorides

Abstract

The present invention relates to the use of compounds of general formula (I) for separations of rare earth elements (lanthanides) by precipitation, wherein R1is selected from the group consisting of H; -CH2COOH; R2, R3, R4, R5and R6are independently selected from the group consisting of H; OH; -NO2; -COOH; phenyl; and/or R2and R3or R3and R4or R4and R5or R5and R6 together with two neighbouring carbon atoms of the aromatic ring form a six-membered aromatic ring. The invention further relates to a method of separation of rare earth elements by precipitation.

IPC Classes  ?

• C01F 17/13 - Preparation or treatment, e.g. separation or purification by using ion exchange resins, e.g. chelate resins
• C01F 17/271 - Chlorides

Abstract

The invention provides surface-modified particles comprising a core, an inner shell and an outer shell, wherein the core is formed of silica or is hollow, the inner shell is formed by a layer of metal and the outer shell is formed by a biocompatible polymer brush. The particles allow for direct optical detection of biomolecules such as nucleic acids, proteins, polysaccharides and glycoproteins in biological samples.

IPC Classes  ?

• G01N 33/543 - ImmunoassayBiospecific binding assayMaterials therefor with an insoluble carrier for immobilising immunochemicals
• G01N 33/553 - Metal or metal coated

Abstract

The invention provides surface-modified particles comprising a core, an inner shell and an outer shell, wherein the core is formed of silica or is hollow, the inner shell is formed by a layer of metal and the outer shell is formed by a biocompatible polymer brush. The particles allow for direct optical detection of biomolecules such as nucleic acids, proteins, polysaccharides and glycoproteins in biological samples.

IPC Classes  ?

• G01N 33/543 - ImmunoassayBiospecific binding assayMaterials therefor with an insoluble carrier for immobilising immunochemicals
• G01N 33/553 - Metal or metal coated

Abstract

The subject of the present invention is a lipidoid of general formula (I), wherein X, Y, Z and R are as defined in the claims. This lipidoid is useful as a transfection agent. The invention further describes transfection agents, transfection particles containing this lipidoid, and their use.

IPC Classes  ?

• C07C 219/12 - Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the hydroxy groups esterified by a carboxylic acid having the esterifying carboxyl group bound to a carbon atom of a ring other than a six-membered aromatic ring
• C07C 233/62 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups

Abstract

The subject of the present invention is a lipidoid of general formula (I), wherein X, Y, Z and R are as defined in the claims. This lipidoid is useful as a transfection agent. The invention further describes transfection agents, transfection particles containing this lipidoid, and their use.

IPC Classes  ?

• C07C 219/12 - Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the hydroxy groups esterified by a carboxylic acid having the esterifying carboxyl group bound to a carbon atom of a ring other than a six-membered aromatic ring
• C07C 233/62 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups

Abstract

This invention provides quinolinecarboxamide compounds of general formula I which inhibit fibroblast activation protein (FAB) and target tumours for diagnostic or therapeutic purposes.

IPC Classes  ?

• A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
• A61P 35/00 - Antineoplastic agents
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07K 5/062 - Dipeptides the side chain of the first amino acid being acyclic, e.g. Gly, Ala

Abstract

This invention provides quinolinecarboxamide compounds of general formula I which by far exceed the previously known TAP inhibitors in affinity and inhibitory effect. These agents can be used to specifically target tumours for diagnostic and therapeutic purposes, or for laboratory purposes in the study of endogenous TAP expression.

IPC Classes  ?

• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• A61P 35/00 - Antineoplastic agents
• A61K 51/04 - Organic compounds
• C07K 5/062 - Dipeptides the side chain of the first amino acid being acyclic, e.g. Gly, Ala

Abstract

The present invention relates to a process for ion irradiation of a particulate substrate containing the steps of embedding particulate substrate in a solid matrix having 10B atoms, and exposing the matrix obtained in the previous step to a neutron flux to give irradiated particulate substrate. The process is extremely effective and amenable to large scale and is particularly suitable for producing irradiated nanodiamonds and irradiated SiC particles.

IPC Classes  ?

• B01J 19/08 - Processes employing the direct application of electric or wave energy, or particle radiationApparatus therefor
• C01B 32/28 - After-treatment, e.g. purification, irradiation, separation or recovery
• C01B 32/956 - Silicon carbide

Abstract

A catheter that has a catheter tube everting inside-out during the process of catheterization. The catheter tube has a plurality of longitudinal protrusions extending from the first end of the catheter tube through at least a portion of the catheter tube, and forming an angle of 0 degrees to 45 degrees with respect to the longitudinal axis of the catheter tube and facing radially inwards, and provides for dilating a circumference of the catheter tube upon everting the catheter tube inside-out from the first end of the catheter tube.

IPC Classes  ?

• A61M 25/01 - Introducing, guiding, advancing, emplacing or holding catheters
• A61M 25/00 - CathetersHollow probes
• B29C 48/21 - Articles comprising two or more components, e.g. co-extruded layers the components being layers the layers being joined at their surfaces
• B29D 23/00 - Producing tubular articles
• B29C 48/00 - Extrusion moulding, i.e. expressing the moulding material through a die or nozzle which imparts the desired formApparatus therefor
• B29C 48/09 - Articles with cross-sections having partially or fully enclosed cavities, e.g. pipes or channels
• A61F 2/966 - Instruments specially adapted for placement or removal of stents or stent-grafts having an outer sleeve with relative longitudinal movement between outer sleeve and prosthesis, e.g. using a push rod
• A61F 2/962 - Instruments specially adapted for placement or removal of stents or stent-grafts having an outer sleeve
• A61F 2/82 - Devices providing patency to, or preventing collapsing of, tubular structures of the body, e.g. stents
• B33Y 80/00 - Products made by additive manufacturing

Abstract

3 is selected from a group which contains compounds of general formulas II and III.

IPC Classes  ?

• C07H 19/10 - Pyrimidine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
• A61P 31/04 - Antibacterial agents
• A01N 57/24 - Biocides, pest repellants or attractants, or plant growth regulators containing organic phosphorus compounds having phosphorus-to-carbon bonds containing heterocyclic radicals
• A61K 31/7072 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine

Abstract

Described herein are lipophosphonoxins of general formula I, diastereomers and mixtures of diastereomers of compounds of general formula I and their pharmaceutically acceptable salts and hydrates as antibacterial agents, forming an active ingredient in pharmaceutical compositions for the treatment of resistant bacterial infections, disinfectants and/or selective culture media.

IPC Classes  ?

• A61K 31/683 - Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
• A61K 31/685 - Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
• A61P 31/04 - Antibacterial agents
• C07F 9/40 - Esters thereof

Abstract

Described herein are lipophosphonoxins of general formula I, diastereomers and mixtures of diastereomers of compounds of general formula I and their pharmaceutically acceptable salts and hydrates as antibacterial agents, forming an active ingredient in pharmaceutical compositions for the treatment of resistant bacterial infections, disinfectants and/or selective culture media.

IPC Classes  ?

• A61P 31/04 - Antibacterial agents
• A61K 31/663 - Compounds having two or more phosphorus acid groups or esters thereof, e.g. clodronic acid, pamidronic acid
• C07F 9/40 - Esters thereof

Abstract

The present invention relates to new compounds of general formula I, their synthesis, their pharmaceutically acceptable salts, and their use in treatment of T-cell acute lymphoblastic leukemia and lymphoma.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• A61P 35/02 - Antineoplastic agents specific for leukemia
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings

Abstract

Nanodiamonds having a positive ζ-potential of at least 1 mV for use in sequestration of at least one FGF family member in organisms in vivo and in vitro. It has been found that nanodiamonds with a positive ζ-potential show an extremely strong and selective binding to FGF family members, thus leading to their usability in the treatment of diseases related to aberrant FGF-FGFR signalling and/or interaction.

IPC Classes  ?

• A61K 33/44 - Elemental carbon, e.g. charcoal, carbon black
• A61K 9/14 - Particulate form, e.g. powders
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• C07K 14/50 - Fibroblast growth factor [FGF]

Abstract

Substituted pyridopyrrolopyrimidine ribonucleosides of general formula I, wherein R is as described in the independent claim, preferably R is selected from the group comprising thiophen-3-yl, furan-2-yl, furan-3-yl, benzofuran-2-yl, methylsulfanyl, methoxy, amino, dimethylamino, methyl; and pharmaceutically acceptable salt thereof, their optical isomers and mixtures of such optical isomers. Compounds according to the invention show strong cytostatic and cytotoxic effects on cell lines of tumor origin in a wide variety of diseases including tumors of different histogenetic origin.

IPC Classes  ?

• C07H 19/23 - Heterocyclic radicals containing two or more heterocyclic rings condensed among themselves or condensed with a common carbocyclic ring system, not provided for in groups
• A61P 35/04 - Antineoplastic agents specific for metastasis

Abstract

The present invention relates to cyclen based cornpounds of general forrnula (I), wherein X is nitrogen and Y, Z are -CH-, or X, Z are -CH- and Y is nitrogen, or X, Y are -CH- and Z is nitrogen; R¹ is independently selected from H; COOH; benzyloxycarbonyl; fluorenylrnethyloxycarbonyl; tert-butoxycarbonyl; methylcarbonyl; trifluoromethylcarbonyl; benzyl; triphenylmethyl; tosyl; mesyl; benzyloxymethyl; phenylsulfonyl; ethoxycarbonyl;2,2,2-trichloroethyloxycarbonyl; methoxycarbonyl; methoxyrnethyloxycarbonyl; R² is selected from H; methylcarbonyl; tert-butyldimethylsilyl; (C1-C4)alkyl, which can be linear or branched, and which can optionally be substituted with CH₃0-, CH₃S-; oxacyclohexyl; allyl; tert-butyldiphenylsilyl; tert-butylcarbonyl; phenylcarbonyl; nitrobenzyl; benzyloxymethyl, which can optionally be substituted with CH₃0-, -N0₂; fluorenylmethyloxycarbonyl; trichlorocarbonyl; trifluorocarbonyl; benzyl; tosyl; mesyl; phenylsulfonyl; allylsulphonyl; ethoxycarbonyl; 2,2,2-trichloroethyloxycarbonyl; methoxycarbonyl; rnethoxymethyloxycarbonyl; R³ is independently selected from H; (C1-C6)alkyl, which can be linear or branched, and which can optionally be substituted with -CH₃,-C1, -F, -CN, tosyl, triisopropylsilyl, CH₃0-, CH₃S-; (C5-C6)cycloalkyl, which can optionally be substituted with -CH₃, -C1, -F, -CN; (C6-0.0)aryl, which can optionally be substituted with -CH₃, -C1, -F, -CN; allyl, propargyl; fluorenylmethyl; benzoylmethyl; phenyloxymethyl; oxacyclopentyl; 2-oxo-1,2-diphenylethyl; with the proviso that where R¹ is bound to nitrogen, then R¹ is not COOH; with the proviso that where R¹ is bound to -CH-, then R¹ is independently H or COOH; and with the proviso that one R¹ is COOH, and with the proviso that one-CH-R¹ group is -CH₂-. The invention further relates to its coordination compounds, peptides and pharmaceutical preparations, as well as to the rnedical use thereof.

IPC Classes  ?

• C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings

Abstract

The present invention relates to cyclen based compounds of general formula (I), wherein X is nitrogen and Y, Z are –CH-, or X, Z are –CH- and Y is nitrogen, or X, Y are –CH- and Z is nitrogen; R1is independently selected from H; COOH; benzyloxycarbonyl; fluorenylmethyloxycarbonyl; tert-butoxycarbonyl; methylcarbonyl; trifluoromethylcarbonyl; benzyl; triphenylmethyl; tosyl; mesyl; benzyloxymethyl; phenylsulfonyl; ethoxycarbonyl; 2,2,2-trichloroethyloxycarbonyl; methoxycarbonyl; methoxymethyloxycarbonyl; R233322; fluorenylmethyloxycarbonyl; trichlorocarbonyl; trifluorocarbonyl; benzyl; tosyl; mesyl; phenylsulfonyl; allylsulphonyl; ethoxycarbonyl; 2,2,2-trichloroethyloxycarbonyl; methoxycarbonyl; methoxymethyloxycarbonyl; R3333333, -C1, -F, -CN; allyl, propargyl; fluorenylmethyl; benzoylmethyl; phenyloxymethyl; oxacyclopentyl; 2-oxo-1,2-diphenylethyl; with the proviso that where R1is bound to nitrogen, then R1is not COOH; with the proviso that where R1is bound to –CH-, then R1is independently H or COOH; and with the proviso that one R1is COOH, and with the proviso that one –CH-R122-. The invention further relates to its coordination compounds, peptides and pharmaceutical preparations, as well as to the medical use thereof.

IPC Classes  ?

• C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• C07F 5/00 - Compounds containing elements of Groups 3 or 13 of the Periodic Table
• C07K 5/00 - Peptides having up to four amino acids in a fully defined sequenceDerivatives thereof
• A61K 49/06 - Nuclear magnetic resonance [NMR] contrast preparationsMagnetic resonance imaging [MRI] contrast preparations

Abstract

1 66, alkyl; halogen (F, Cl, Br or I); Y is selected from a group consisting of nitrogen; N-oxide; Z1, Z2, Zmm22222-2-; A, Amm22222nn is 1 or 2; R1, R2, R31616 610166102161616166 10610n,nn2n11061010 aryl; and/or neighboring two of R1, R2, R33161 61621616 2nnn2n110610nn is 2 and all of Z1, Z2, Zm22-22COOH; for chromatographic separation of rare earth elements and/or s-, p- and d-block metals, as well as to the method of the separation of rare earth elements.

IPC Classes  ?

• C07B 59/00 - Introduction of isotopes of elements into organic compounds
• C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system

Abstract

The present invention provides a method for functionalization of an aromatic amino acid or a nucleobase with a fluoroalkyl-containing moiety RF, wherein the aromatic amino acid is reacted in the presence of at least one reductant with at least one hypervalent iodine fluoroalkyl reagent carrying said floroalkyl-containing moiety RF. The invention further provides novel hypervalent iodine fluoroalkyl reagents.

IPC Classes  ?

• C07D 347/00 - Heterocyclic compounds containing rings having halogen atoms as ring hetero atoms

Abstract

The present invention provides a structurally novel class of heterocyclic compounds of general formula I The novel compounds are useful in the prevention or treatment of a condition which is mediated by the action, or by loss of action, of Constitutive androstane receptor (CAR) or its endogenous ligands. The present invention thus provides the novel compounds for medicinal use, as well as pharmaceutical composition containing said compounds.

IPC Classes  ?

• A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
• A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
• C07D 471/04 - Ortho-condensed systems
• C07D 513/04 - Ortho-condensed systems

Abstract

The present invention provides a structurally novel class of heterocyclic compounds of general formula I wherein L1 is heteroaryl and L2 is heteroaryl or aryl. The novel compounds are useful in a method of prevention or treatment of a condition which is mediated by the action, or by loss of action, of Constitutive androstane receptor (CAR) receptor or its endogenous ligands. The present invention thus provides the novel compounds for medicinal use, as well as pharmaceutical composition containing said compounds. (I)

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• C07D 513/04 - Ortho-condensed systems
• A61K 31/429 - Thiazoles condensed with heterocyclic ring systems
• A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
• A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
• A61P 3/00 - Drugs for disorders of the metabolism

Abstract

The invention provides 3a5ßsteroid compounds of general formula I. These compounds are useful in the treatment of epilepsy or comorbidities associated with epilepsy or conditions associated with convulsions, such as seizures associated with hypoxia; seizures associated with traumatic brain damage; seizures associated with intoxication; pathological changes caused by hyperexcitation; or in treatment of conditions accompanying epilepsy, such as affective disorders, depression, post-traumatic stress disorder (PTSD) and stress-related diseases, anxiety, schizophrenia and psychotic disorders, related ischemic CNS damage, neurodegenerative changes and disorders, multiple sclerosis. The compounds of general formula I also show age-specific efficacy.

IPC Classes  ?

• A61K 31/56 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids
• A61K 31/57 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
• A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 25/08 - AntiepilepticsAnticonvulsants
• C07J 41/00 - Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
• C07J 43/00 - Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton

Abstract

The invention provides 3α5β–steroid compounds of general formula I. These compounds are useful in the treatment of epilepsy or comorbidities associated with epilepsy or conditions associated with convulsions, such as seizures associated with hypoxia; seizures associated with traumatic brain damage; seizures associated with intoxication; pathological changes caused by hyperexcitation; or in treatment of conditions accompanying epilepsy, such as affective disorders, depression, post-traumatic stress disorder (PTSD) and stress-related diseases, anxiety, schizophrenia and psychotic disorders, related ischemic CNS damage, neurodegenerative changes and disorders, multiple sclerosis. The compounds of general formula I also show age-specific efficacy.

IPC Classes  ?

• C07J 41/00 - Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
• C07J 43/00 - Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
• A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
• A61K 31/57 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
• A61K 31/56 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 25/08 - AntiepilepticsAnticonvulsants

Abstract

3COO— or Cl— and m=1-2. Preparation and use of compounds of general formula 6 and 13 as carriers of nucleoside triphosphates across the cell membranes for the purpose of incorporation of modified nucleoside triphosphates into cellular DNA or RNA. Use of compounds of general formula 6 and 13 as carriers of nucleoside triphosphates across the cell membrane for determining the virostatic activities of modified nucleoside triphosphates. Use of compounds of general formula 6 and 13 as carriers of modified nucleoside triphosphates across the cell membrane for determining cell proliferation and S phase of the cell cycle.

IPC Classes  ?

• C08B 37/16 - CyclodextrinDerivatives thereof
• A61K 47/40 - CyclodextrinsDerivatives thereof
• G01N 33/483 - Physical analysis of biological material

Abstract

The present invention relates to compounds of general formula (I) for chromatographic separation of rare earth elements and/or s-, p-, d-metals, as well as to the method of the separation of rare earth elements.

IPC Classes  ?

• B01D 15/08 - Selective adsorption, e.g. chromatography
• C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C22B 59/00 - Obtaining rare earth metals

Abstract

2. In concentrations lowering production of this factor by 50%, these compounds have no negative effect on the cell viability and they are not cytotoxic. Furthermore, the method of production of the compounds of the general formula I is provided. A pharmaceutical composition comprising the polysubstituted pyrimidines according to the invention and the use of these compounds for the treatment of the inflammatory diseases are also provided.

IPC Classes  ?

• A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• C07D 239/42 - One nitrogen atom

Abstract

Compounds useful for the treatment of malaria, cancer, Parkinson's disease, diabetes, and bacterial infection.

IPC Classes  ?

• C07K 5/02 - Peptides having up to four amino acids in a fully defined sequenceDerivatives thereof containing at least one abnormal peptide link
• A61P 33/06 - Antimalarials
• A61K 38/08 - Peptides having 5 to 11 amino acids
• A61K 38/00 - Medicinal preparations containing peptides

Abstract

The present invention relates to a process for ion irradiation of a particulate substrate, comprising the steps of: embedding particulate substrate in a solid matrix comprising 10B atoms; and exposing the matrix obtained in the previous step to a neutron flux; to give irradiated particulate substrate. The process of the invention is extremely effective and amenable to large scale. It is particularly suitable for producing irradiated nanodiamonds and irradiated SiC particles.

IPC Classes  ?

• C01B 32/28 - After-treatment, e.g. purification, irradiation, separation or recovery
• C01B 32/956 - Silicon carbide

Abstract

2, which is a hydrophilic linker selected from a group comprising β-alanine, γ-aminobutyric acid or γ-glutamic acid; for use in the treatment and prevention of diseases, which are Alzheimer's disease (AD), Parkinson's disease (PD), cognitive impairment no dementia (CIND), brain trauma, and neurodegenerative changes and disorders.

IPC Classes  ?

• A61K 38/22 - Hormones
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

Abstract

5. Compounds of the invention may be used for diagnosis and possibly also for the treatment of estrogen-dependent diseases.

IPC Classes  ?

• A61K 31/566 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol having an oxo group in position 17, e.g. oestrone
• C07J 1/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, not substituted in position 17 beta by a carbon atom, e.g. oestrane, androstane

Abstract

in vivo in vivo and in vitro. It has been found that nanodiamonds with a positive ζ-potential show an extremely strong and selective binding to FGF family members, thus leading to their usability in the treatment of diseases related to aberrant FGF-FGFR signalling and/or interaction.

IPC Classes  ?

• A61K 33/44 - Elemental carbon, e.g. charcoal, carbon black
• A61P 35/00 - Antineoplastic agents
• A61K 9/14 - Particulate form, e.g. powders

Abstract

Substituted pyridopyrrolopyrimidine ribonucleosides of general formula I, wherein R is as described in the independent claim, preferably R is selected from the group comprising thiophen-3-yl, furan-2-yl, furan-3-yl, benzofuran-2-yl, methylsulfanyl, methoxy, amino, dimethylamino, methyl; and pharmaceutically acceptable salt thereof, their optical isomers and mixtures of such optical isomers. Compounds according to the invention show strong cytostatic and cytotoxic effects on cell lines of tumor origin in a wide variety of diseases including tumors of different histogenetic origin.

IPC Classes  ?

• A61K 31/7052 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
• A61P 35/00 - Antineoplastic agents
• C07H 19/23 - Heterocyclic radicals containing two or more heterocyclic rings condensed among themselves or condensed with a common carbocyclic ring system, not provided for in groups

Abstract

Substituted pyridopyrrolopyrimidine ribonucleosides of general formula I, wherein R is as described in the independent claim, preferably R is selected from the group comprising thiophen-3-yl, furan-2-yl, furan-3-yl, benzofuran-2-yl, methylsulfanyl, methoxy, amino, dimethylamino, methyl; and pharmaceutically acceptable salt thereof, their optical isomers and mixtures of such optical isomers. Compounds according to the invention show strong cytostatic and cytotoxic effects on cell lines of tumor origin in a wide variety of diseases including tumors of different histogenetic origin.

IPC Classes  ?

• C07H 19/23 - Heterocyclic radicals containing two or more heterocyclic rings condensed among themselves or condensed with a common carbocyclic ring system, not provided for in groups
• A61K 31/7052 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
• A61P 35/00 - Antineoplastic agents

Abstract

A catheter that has a catheter tube everting inside-out during the process of catheterization. The catheter tube has a plurality of longitudinal protrusions extending from the first end of the catheter tube through at least a portion of the catheter tube, and forming an angle of 0 degrees to 45 degrees with respect to the longitudinal axis of the catheter tube and facing radially inwards, and provides for dilating a circumference of the catheter tube upon everting the catheter tube inside-out from the first end of the catheter tube.

IPC Classes  ?

• A61M 25/00 - CathetersHollow probes
• A61M 25/01 - Introducing, guiding, advancing, emplacing or holding catheters
• B29C 48/00 - Extrusion moulding, i.e. expressing the moulding material through a die or nozzle which imparts the desired formApparatus therefor
• B29C 48/09 - Articles with cross-sections having partially or fully enclosed cavities, e.g. pipes or channels
• B29C 48/21 - Articles comprising two or more components, e.g. co-extruded layers the components being layers the layers being joined at their surfaces
• B29D 23/00 - Producing tubular articles
• A61F 2/966 - Instruments specially adapted for placement or removal of stents or stent-grafts having an outer sleeve with relative longitudinal movement between outer sleeve and prosthesis, e.g. using a push rod
• A61F 2/962 - Instruments specially adapted for placement or removal of stents or stent-grafts having an outer sleeve
• A61F 2/82 - Devices providing patency to, or preventing collapsing of, tubular structures of the body, e.g. stents
• B33Y 80/00 - Products made by additive manufacturing

Abstract

The present invention relates to compounds of general formula (I) for chromatographic separation of rare earth elements and/or s-, p-, d- metals, as well as to the method of the separation of rare earth elements.

IPC Classes  ?

• B01D 15/08 - Selective adsorption, e.g. chromatography
• C07D 257/02 - Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
• C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Abstract

The present invention relates to compounds of general formula (I) for chromatographic separation of rare earth elements and/or s-, p-, d- metals, as well as to the method of the separation of rare earth elements.

IPC Classes  ?

• C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
• C07D 257/02 - Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
• B01D 15/08 - Selective adsorption, e.g. chromatography

Abstract

The present invention provides steroidal compounds for the treatment of mental and neurological disorders by targeted rectification of defects caused by a mutation occurring in the membrane region of a human N-methyl-D-aspartate receptor subunit by potentiation of the effects of the said receptor.

IPC Classes  ?

• A61K 31/00 - Medicinal preparations containing organic active ingredients
• A61K 31/56 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids
• A61K 31/568 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstane, testosterone
• A61K 31/57 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

Abstract

−.

IPC Classes  ?

• C07D 249/04 - 1,2,3-TriazolesHydrogenated 1,2,3-triazoles
• C07C 19/08 - Acyclic saturated compounds containing halogen atoms containing fluorine
• C07C 247/04 - Compounds containing azido groups with azido groups bound to acyclic carbon atoms of a carbon skeleton being saturated
• A01N 43/647 - TriazolesHydrogenated triazoles
• B01J 31/18 - Catalysts comprising hydrides, coordination complexes or organic compounds containing coordination complexes containing nitrogen, phosphorus, arsenic or antimony
• B01J 31/04 - Catalysts comprising hydrides, coordination complexes or organic compounds containing organic compounds or metal hydrides containing carboxylic acids or their salts
• C07C 323/48 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton having at least one of the nitrogen atoms, not being part of nitro or nitroso groups, further bound to other hetero atoms to nitrogen atoms
• A61K 31/655 - Azo (—N=N—), diazo (=N2), azoxy (N—O—N or N(=O)—N), azido (—N3) or diazoamino (—N=N—N) compounds

Abstract

Substituted heteropentadieno-pyrrolopyrimidine ribonucleosides of general formula I, where R is selected from the group comprising furan-2-yl, furan-3-yl, benzofuran-2-yl, methylsulfanyl, methoxy, amino, dimethylamino, methyl or chloro, and pharmaceutically acceptable salt thereof, their optical isomers and mixtures of such optical isomers.

IPC Classes  ?

• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
• A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
• A61K 31/341 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
• C07D 487/16 - Peri-condensed systems
• C07D 487/14 - Ortho-condensed systems
• C07D 491/14 - Ortho-condensed systems
• C07D 491/16 - Peri-condensed systems
• C07H 19/23 - Heterocyclic radicals containing two or more heterocyclic rings condensed among themselves or condensed with a common carbocyclic ring system, not provided for in groups
• A61P 35/02 - Antineoplastic agents specific for leukemia
• C07H 19/24 - Heterocyclic radicals containing oxygen or sulfur as ring hetero atom

Abstract

Glutamine antagonists and their use for treating oncological, immunological, and neurological diseases are disclosed. Also disclosed are methods for treating an oncological, immunological, infectious or neurological disease or disorder, the method comprising administering to a subject in need of treatment thereof a therapeutically effective amount of a glutamine antagonist of the disclosure or the pharmaceutical composition thereof. Also disclosed are methods of enhancing the effects of an immune checkpoint inhibitor, enabling a subject to respond to an immune checkpoint inhibitor, or enabling the toxicity or the dose or number of treatments with an immune checkpoint inhibitor to be reduced, comprising administering to a subject in need of treatment thereof a therapeutically effective amount of a glutamine antagonist of the disclosure or the pharmaceutical composition thereof, and an immune checkpoint inhibitor. Also disclosed are methods for treating an oncological, immunological, infectious or neurological disease or disorder that is refractory to checkpoint inhibitor therapy, the method comprising administering to a subject in need thereof, and having the refractory disease or disorder, a therapeutically effective amount of a glutamine antagonist of the disclosure or the pharmaceutical composition thereof.

IPC Classes  ?

• C07C 251/76 - Hydrazones having doubly-bound carbon atoms of hydrazone groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of a saturated carbon skeleton
• C07D 209/10 - IndolesHydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
• C07K 5/06 - Dipeptides

Abstract

A macromolecular water-soluble conjugates based on synthetic copolymers to which at least one affinity tag, at least one imaging probe and at least one targeting ligand are bound via covalent bonds. The macromolecular conjugate may be used in identification, visualization, quantification or isolation of proteins and/or cells.

IPC Classes  ?

• A61K 9/00 - Medicinal preparations characterised by special physical form
• G01N 33/534 - Production of labelled immunochemicals with radioactive label
• C08F 220/58 - Amides containing oxygen in addition to the carbonamido oxygen
• G01N 33/531 - Production of immunochemical test materials
• G01N 33/532 - Production of labelled immunochemicals
• G01N 33/533 - Production of labelled immunochemicals with fluorescent label
• A61K 49/00 - Preparations for testing in vivo
• A61K 47/58 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. poly[meth]acrylate, polyacrylamide, polystyrene, polyvinylpyrrolidone, polyvinylalcohol or polystyrene sulfonic acid resin

Abstract

Title: Chemical Compounds The present invention relates to compounds of formula I (I) wherein R1, R2, R3, R4, R5, R6, R7 and W are as described in the claims. Said compounds are useful in particular in the treatment of a condition selected from malaria, cancer, Parkinson's disease, diabetes, and bacterial infection.

IPC Classes  ?

• C07K 7/06 - Linear peptides containing only normal peptide links having 5 to 11 amino acids
• C07K 5/097 - Tripeptides the first amino acid being heterocyclic, e.g. Pro, His, Trp, e.g. thyroliberin, melanostatin
• C07K 5/103 - Tetrapeptides the side chain of the first amino acid being acyclic, e.g. Gly, Ala
• C07K 5/09 - Tripeptides the side chain of the first amino acid containing more amino groups than carboxyl groups, or derivatives thereof, e.g. Lys, Arg
• A61K 38/05 - Dipeptides
• A61K 38/06 - Tripeptides
• A61K 38/07 - Tetrapeptides
• A61K 38/08 - Peptides having 5 to 11 amino acids

Abstract

The invention describes the pyrimidine-based compounds of the general formula I. Described compounds lower the production of the prostaglandin E2. In concentrations lowering production of this factor by 50%, these compounds have no negative effect on the cell viability and they are not cytotoxic. Furthermore, the method of production of the compounds of the general formula I is provided. A pharmaceutical composition comprising the polysubstituted pyrimidines according to the invention and the use of these compounds for the treatment of the inflammatory diseases are also provided.

IPC Classes  ?

• C07D 239/42 - One nitrogen atom
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim

Abstract

Synthetic antimicrobial peptides and their use for treatment or prevention of infectious diseases of bones or surrounding infected tissues and/or to prevent or eliminate the infectious agent from joint and bone replacements and sealants, and for the prevention of infectious complications after implantation of joint replacements and after osteosynthesis.

IPC Classes  ?

• A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
• C07K 7/08 - Linear peptides containing only normal peptide links having 12 to 20 amino acids
• C07K 14/435 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans

Abstract

The present invention relates to a catheter, which comprises a catheter tube everting inside-out during the process of catheterization. A catheter tube comprises a plurality of longitudinal protrusions extending from the first end of the catheter tube through at least a portion of the catheter tube, and forming an angle of 0 degrees to 45 degrees with respect to the longitudinal axis of the catheter tube and facing radially inwards, and means for dilating a circumference of the catheter tube upon everting the catheter tube inside-out from the first end of the catheter tube. The longitudinal protrusions ensure the axial reinforcement of the catheter tube, which prevents the tube from collapsing and bending under the axial force and the resistance of the fold and of the friction between the everted portion and the corresponding underlying portion of the tube. The dilating means dilate the circumference of the catheter tube in the everted region, thus reducing the resistance of the fold and of the friction between the everted portion and the corresponding underlying portion of the tube.

IPC Classes  ?

• A61M 25/01 - Introducing, guiding, advancing, emplacing or holding catheters

Abstract

The present invention relates to a catheter, which comprises a catheter tube everting inside-out during the process of catheterization. A catheter tube comprises a plurality of longitudinal protrusions extending from the first end of the catheter tube through at least a portion of the catheter tube, and forming an angle of 0 degrees to 45 degrees with respect to the longitudinal axis of the catheter tube and facing radially inwards, and means for dilating a circumference of the catheter tube upon everting the catheter tube inside-out from the first end of the catheter tube. The longitudinal protrusions ensure the axial reinforcement of the catheter tube, which prevents the tube from collapsing and bending under the axial force and the resistance of the fold and of the friction between the everted portion and the corresponding underlying portion of the tube. The dilating means dilate the circumference of the catheter tube in the everted region, thus reducing the resistance of the fold and of the friction between the everted portion and the corresponding underlying portion of the tube.

IPC Classes  ?

• A61M 25/01 - Introducing, guiding, advancing, emplacing or holding catheters

Abstract

The present invention relates to a catheter, which comprises a catheter tube everting inside-out during the process of catheterization. A catheter tube comprises a plurality of longitudinal protrusions extending from the first end of the catheter tube through at least a portion of the catheter tube, and forming an angle of 0 degrees to 45 degrees with respect to the longitudinal axis of the catheter tube and facing radially inwards, and means for dilating a circumference of the catheter tube upon everting the catheter tube inside-out from the first end of the catheter tube. The longitudinal protrusions ensure the axial reinforcement of the catheter tube, which prevents the tube from collapsing and bending under the axial force and the resistance of the fold and of the friction between the everted portion and the corresponding underlying portion of the tube. The dilating means dilate the circumference of the catheter tube in the everted region, thus reducing the resistance of the fold and of the friction between the everted portion and the corresponding underlying portion of the tube.

IPC Classes  ?

• A61M 25/01 - Introducing, guiding, advancing, emplacing or holding catheters

Abstract

Substituted heteropentadieno-pyrrolopyrimidine ribonucleosides of general formula (I), where R is selected from the group comprising furan-2-yl, furan-3-yl, benzofuran-2-yl, methylsulfanyl, methoxy, amino, dimethylamino, methyl or chloro, and pharmaceutically acceptable salt thereof, their optical isomers and mixtures of such optical isomers. Compounds according to the invention show strong cytostatic and cytotoxic effects on cell lines in a wide variety of diseases including tumors of various histogenic origin.

IPC Classes  ?

• A61K 31/7064 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
• A61P 35/00 - Antineoplastic agents
• A61P 35/02 - Antineoplastic agents specific for leukemia
• C07H 19/23 - Heterocyclic radicals containing two or more heterocyclic rings condensed among themselves or condensed with a common carbocyclic ring system, not provided for in groups

Abstract

Substituted heteropentadieno-pyrrolopyrimidine ribonucleosides of general formula (I), where R is selected from the group comprising furan-2-yl, furan-3-yl, benzofuran-2-yl, methylsulfanyl, methoxy, amino, dimethylamino, methyl or chloro, and pharmaceutically acceptable salt thereof, their optical isomers and mixtures of such optical isomers. Compounds according to the invention show strong cytostatic and cytotoxic effects on cell lines in a wide variety of diseases including tumors of various histogenic origin.

IPC Classes  ?

• C07H 19/23 - Heterocyclic radicals containing two or more heterocyclic rings condensed among themselves or condensed with a common carbocyclic ring system, not provided for in groups
• A61K 31/7064 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
• A61P 35/00 - Antineoplastic agents
• A61P 35/02 - Antineoplastic agents specific for leukemia

Abstract

Synthetic macromolecular conjugate for selective interaction with proteins has a synthetic copolymer, and at least one binding group and at least one further group selected from an affinity tag and an imaging probe, and at least one binding group and at least one further group being bound via covalent bond to the synthetic copolymer. The macromolecular conjugate is suitable in particular for identification, visualization, quantification or isolation of proteins and/or cells.

IPC Classes  ?

• A61K 9/00 - Medicinal preparations characterised by special physical form
• G01N 33/532 - Production of labelled immunochemicals
• G01N 33/531 - Production of immunochemical test materials
• G01N 33/533 - Production of labelled immunochemicals with fluorescent label
• G01N 33/534 - Production of labelled immunochemicals with radioactive label
• C08F 8/30 - Introducing nitrogen atoms or nitrogen-containing groups
• G01N 33/58 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving labelled substances

Abstract

Substituted thienopyrrolopyrimidine ribonucleosides for therapeutic use The invention provides a new group of substituted thienopyrrolopyrimidine ribonucleosides of general formula I, wherein R is defined in the claims. The compounds of this invention show strong cytostatic and cytotoxic activities preferably against cancer cell lines of broad spectrum of diseases including tumors of various histogenetic origin.

IPC Classes  ?

• C07H 19/24 - Heterocyclic radicals containing oxygen or sulfur as ring hetero atom
• A61K 31/7042 - Compounds having saccharide radicals and heterocyclic rings
• A61P 35/00 - Antineoplastic agents

Abstract

15β-substituted derivatives of estrone of general formula I wherein R1, R2, R3, R4, R5 are independently selected from the group consisting of: C1-C4 alkyl, C1-C4 alkoxy, C1-C4 halogenalkyl, halogen, COOR6 wherein R6 is C1-C4 alkyl; H, OH; optionally, R3, R4 and R5 are each formed by a hydrogen atom, while R1 and R2 together form an aryl group, preferably naphthyl; wherein the aromatic ring in position C-15 can be mono-, di-, tri-, tetra- and penta- substituted with substituents R1-R5. Compounds of the invention may be used for diagnosis and possibly also for the treatment of estrogen-dependent diseases.

IPC Classes  ?

• C07J 1/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, not substituted in position 17 beta by a carbon atom, e.g. oestrane, androstane
• A61K 31/566 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol having an oxo group in position 17, e.g. oestrone
• A61P 5/32 - Antioestrogens

Abstract

Lipophosphonoxins of general Formula I are described here, wherein R1 is C8-C22, preferably C10-C18 and more preferably C12-C16 alkyl, or hexadecyloxypropyl, tetradecyloxypropyl, tetradecyloxyethyl or hexadecyloxyethyl, R2 is uracil, thymine, or cytosine, R3 is selected from a group which contains compounds of general formulas II and III, wherein R4 is H, CH2OH or CH2NH2, R5 is H, OH or NH2, R6 is H, OH or NH2, R7 is H, CH2OH or CH2NH2, wherein at least one of the groups R5 and R6 must be NH2 or one of the groups R4 and R7 must be CH2NH2. R8 is H, CH2OH or CH2NH2, R9 is H, OH or NH2, R10 is H, OH or NH2, R11 is H, OH or NH2, R12 is H, CH2OH or CH2NH2, wherein at least one of the groups R9, R10 and R11 must be NH2 or one of the groups R8 a R12 must be CH2NH2. R13 is NH2 or NH-CH(NH2)NH, R14 is NH2 or NH-CH(NH2)NH, R15 is NH2 or NH-CH(NH2)NH, R16 is NH2 or NH-CH(NH2)NH. Further, diastereomers and mixtures of diastereomers of compounds of general formula I and the corresponding pharmaceutically acceptable salts and/or hydrates are described. The compounds of general formula I are useful as antibacterial agents or active ingredients in disinfectants, and/or of selective in vitro culture media.

IPC Classes  ?

• A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
• A61P 31/04 - Antibacterial agents
• C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system

Abstract

Lipophosphonoxins of general Formula I are described here, wherein R1 is C8-C22, preferably C10-C18 and more preferably C12-C16 alkyl, or hexadecyloxypropyl, tetradecyloxypropyl, tetradecyloxyethyl or hexadecyloxyethyl, R2 is uracil, thymine, or cytosine, R3 is selected from a group which contains compounds of general formulas II and III, wherein R4 is H, CH2OH or CH2NH2, R5 is H, OH or NH2, R6 is H, OH or NH2, R7 is H, CH2OH or CH2NH2, wherein at least one of the groups R5 and R6 must be NH2 or one of the groups R4 and R7 must be CH2NH2. R8 is H, CH2OH or CH2NH2, R9 is H, OH or NH2, R10 is H, OH or NH2, R11 is H, OH or NH2, R12 is H, CH2OH or CH2NH2, wherein at least one of the groups R9, R10 and R11 must be NH2 or one of the groups R8 a R12 must be CH2NH2. R13 is NH2 or NH-CH(NH2)NH, R14 is NH2 or NH-CH(NH2)NH, R15 is NH2 or NH-CH(NH2)NH, R16 is NH2 or NH-CH(NH2)NH. Further, diastereomers and mixtures of diastereomers of compounds of general formula I and the corresponding pharmaceutically acceptable salts and/or hydrates are described. The compounds of general formula I are useful as antibacterial agents or active ingredients in disinfectants, and/or of selective in vitro culture media.

IPC Classes  ?

• C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
• A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
• A61P 31/04 - Antibacterial agents

Abstract

Compounds of general formulae6 and 13 where X is -NH-C(NH2)=N+H2 or -N+H3, Y is a linear oligomer consisting of arginine units terminated with an aminodimethylenamide unit (-Arg)n-NH-(CH2)2-NH2, where n = 6-10, or arginine-aminocaproic units (-Arg-Aca)n- NH2, where n = 6 to 10, A- = CF3COO- or C1- and m = 1-2. Preparation and use of compounds of general formula 6 and 13 as carriers of nucleoside triphosphates across the cell membranes for the purpose of incorporation of modified nucleoside triphosphates into the cellular DNA or RNA. Use of compounds of general formula 6 and 13 as carriers of nucleoside triphosphates across the cell membrane for the purpose of determining the virostatic activities of modified nucleoside triphosphates. Use of compounds of general formula 6 and 13 as carriers of modified nucleoside triphosphates across the cell membrane for the purpose of determining cell proliferation and S phase of the cell cycle.

IPC Classes  ?

• C08L 5/16 - CyclodextrinDerivatives thereof
• C08B 37/16 - CyclodextrinDerivatives thereof
• C07H 19/10 - Pyrimidine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids
• C07H 19/20 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids

Abstract

Amphiphilic compounds with tetradecahydrophenanthrene skeleton and their enantiomers, exhibiting neuroprotective effects, their use in methods of treatment of neuropsychiatric disorders associated with an imbalance in glutamatergic neurotransmitter system, such as ischemic damage of CNS, neurodegenerative changes and disorders of CNS, affective disorders, depression, post-traumatic stress disorder and diseases related to stress, anxiety, schizophrenia and psychotic disorders, pain, addiction, multiple sclerosis, epilepsy, glioma, and a pharmaceutical composition containing compound.

IPC Classes  ?

• C07D 213/18 - Salts thereof
• C07J 43/00 - Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
• C07J 53/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by condensation with carbocyclic rings or by formation of an additional ring by means of a direct link between two ring carbon atoms
• C07J 9/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
• C07J 41/00 - Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
• C07C 305/20 - Esters of sulfuric acids having oxygen atoms of sulfate groups bound to carbon atoms of rings other than six-membered aromatic rings
• C07C 59/80 - Unsaturated compounds containing keto groups containing rings other than six-membered aromatic rings

Abstract

− independently represent anions of pharmaceutically acceptable salts.

IPC Classes  ?

• C07D 471/22 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups in which the condensed systems contains four or more hetero rings
• A61K 31/475 - QuinolinesIsoquinolines having an indole ring, e.g. yohimbine, reserpine, strychnine, vinblastine
• A61P 35/00 - Antineoplastic agents

IPC Classes  ?

• A61K 31/223 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of alpha-amino acids
• A61K 31/27 - Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, e.g. meprobamate, carbachol, neostigmine
• A61K 31/404 - Indoles, e.g. pindolol
• A61P 35/00 - Antineoplastic agents