A plurality of particles of tasquinimod in free base form or as a pharmaceutically acceptable salt, the particles having a D(v,0.9) of at most 30 μm and a D(v,0.5) of at most 15 μm. A pharmaceutical composition comprising the particles and preferably one or more pharmaceutically acceptable excipients. A pharmaceutical dosage unit. The particles, composition and dosage unit are useful in the treatment of cancer.
Disclosed is a method for treating an ocular inflammatory disease (OID), e. g., uveitis conjunctivitis, comprising periodic administration of a therapeutically effective amount of laquinimod or a pharmaceutically acceptable salt thereof. Also provided is a pharmaceutical composition comprising laquinimod or a pharmaceutically acceptable salt thereof for use in treating a subject suffering from an OID, uveitis, bacterial conjunctivitis, viral conjunctivitis, an inflammation of the orbital tissue, the lacrimal apparatus, the eyelid, the cornea, the retina or the optic pathway. This application also provides a method for treating a subject suffering from an autoimmune disease-associated ocular inflammation comprising periodic ocular administration to the subject a therapeutically effective amount of laquinimod or a pharmaceutically acceptable salt, and an ocular pharmaceutical composition comprising laquinimod or a pharmaceutically acceptable salt thereof for use in treating an autoimmune disease-associated ocular inflammation.
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
4.
QUINOLINE CARBOXAMIDES FOR USE IN THE TREATMENT OF MPN
BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM (USA)
ACTIVE BIOTECH AB (Sweden)
Inventor
Bhalla, Kapil
Eriksson, Helena
Tuvesson, Helen
Abstract
Described herein is certain quinoline carboxamides for use in the treatment of a myeloproliferative neoplasm (MPN). The quinoline carboxamides may more specifically be used in the treatment of advanced stages of MPN, including accelerated-phase MPN and secondary acute myeloid leukemia, i.e., acute myeloid leukemia evolving from an antecedent myeloproliferative neoplasm (post-MPN AML), optionally in combination with a further compound selected from a Janus kinase (JAK) inhibitor, a bromodomain and extra-terminal motif protein (BET) inhibitor, a B-cell lymphoma 2 (Bcl-2) inhibitor, and combinations thereof. Also included are pharmaceutical combinations of the quinoline carboxamides and second agents such as a BET inhibitor or a Bcl-2 inhibitor. Further included are certain quinoline carboxamides for use in combination with a BET inhibitor or a Bcl-2 inhibitor, in the treatment of a myeloproliferative neoplasm (MPN).
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
A plurality of particles of tasquinimod in free base form or as a pharmaceutically acceptable salt, said particles having a D(v, 0.9) of at most 30 pm and a D(v, 0.5) of at most 15 μm. A pharmaceutical composition comprising said particles and preferably one or more pharmaceutically acceptable excipients. A pharmaceutical dosage unit. The particles, composition and dosage unit are useful in the treatment of cancer.
A pharmaceutical composition containing tasquinimod or a pharmaceutically salt of tasquinimod, a method for assessment thereof and a process for its manufacture. The use in therapy of a pharmaceutical composition containing tasquinimod or a pharmaceutically acceptable salt of tasquinimod. The compound 3,3′-methylenebis(4-hydroxy-5-methoxy-1-methylquinoline-2(1H)-one) and its use in a method for assessing a pharmaceutical composition containing tasquinimod or a pharmaceutically acceptable salt of tasquinimod.
A pharmaceutical formulation comprising laquinimod or a pharmaceutically acceptable salt thereof as active ingredient, a pharmaceutically acceptable viscosity agent, a pharmaceutically acceptable tonicity adjusting agent, a pharmaceutically acceptable humectant, a pharmaceutically acceptable antioxidant, and a pharmaceutically acceptable pH regulating agent. The formulation is suitable for the treatment of ocular diseases by ocular administration, preferably topical ocular administration.
The present invention concerns a combination comprising tasquinimod, or a pharmaceutically acceptable salt thereof, and a PD-1 and/or PD-L1 inhibitor, for use as a medicament. It also concerns a pharmaceutical composition comprising tasquinimod, or a pharmaceutically acceptable salt thereof, and PD-1 and/or PD-L1 inhibitor.
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
9.
TASQUINIMOD OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF FOR USE IN THE TREATMENT OF MYELODYSPLASTIC SYNDROME
A combination comprising tasquinimod, or a pharmaceutically acceptable salt thereof, and at least one further compound selected from a proteasome inhibitor, an immunomodulatory imide, and an antibody, for use as a in the treatment of multiple myeloma. A kit comprising tasquinimod and a package insert with instructions for using tasquinimod in combination with at least one further compound selected from a proteasome inhibitor, an immunomodulatory imide, and an antibody, to treat multiple myeloma in an individual. Tasquinimod for use in the treatment of multiple myeloma, in combination with a further compound selected from a proteasome inhibitor, an immunomodulatory imide, and an antibody.
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 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/573 - 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 substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
The present invention relates to compounds for treatment of a disease or disorder associated with excessive vascularisation of the eye, such as for instance corneal neovascularisation, neovascularisation of the iris, neovascularisation of the ciliary body, corneal pannus, choroidal neovascularisation, retinal neovascularisation, wet age-related macular degeneration, proliferative diabetic retinopathy, retinopathy of prematurity, and ischemic retinopathy.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 47/68 - 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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A pharmaceutical composition containing tasquinimod or a pharmaceutically salt of tasquinimod, a method for assessment thereof and a process for its manufacture. The use in therapy of a pharmaceutical composition containing tasquinimod or a pharmaceutically acceptable salt of tasquinimod. The compound 3,3'-methylenebis(4-hydroxy-5-methoxy-1- methylquinoline-2(1H)-one) and its use in a method for assessing a pharmaceutical composition containing tasquinimod or a pharmaceutically acceptable salt of tasquinimod.
C07D 215/56 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3 with oxygen atoms in position 4
A pharmaceutical composition containing tasquinimod or a pharmaceutically salt of tasquinimod, a method for assessment thereof and a process for its manufacture. The use in therapy of a pharmaceutical composition containing tasquinimod or a pharmaceutically acceptable salt of tasquinimod. The compound 3,3'-methylenebis(4-hydroxy-5-methoxy-1- methylquinoline-2(1H)-one) and its use in a method for assessing a pharmaceutical composition containing tasquinimod or a pharmaceutically acceptable salt of tasquinimod.
C07D 215/56 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3 with oxygen atoms in position 4
14.
A PLURALITY OF TASQUINIMOD PARTICLES AND USE THEREOF
A plurality of particles of tasquinimod in free base form or as a pharmaceutically acceptable salt, said particles having a D(v,0.9) of at most 30 pm and a D(v,0.5) of at most 15 μm. A pharmaceutical composition comprising said particles and preferably one or more pharmaceutically acceptable excipients. A pharmaceutical dosage unit. The particles, composition and dosage unit are useful in the treatment of cancer.
A plurality of particles of tasquinimod in free base form or as a pharmaceutically acceptable salt, said particles having a D(v,0.9) of at most 30 pm and a D(v,0.5) of at most 15 ?m. A pharmaceutical composition comprising said particles and preferably one or more pharmaceutically acceptable excipients. A pharmaceutical dosage unit. The particles, composition and dosage unit are useful in the treatment of cancer.
A pharmaceutical formulation comprising laquinimod or a pharmaceutically acceptable salt thereof as active ingredient, a pharmaceutically acceptable viscosity agent, a pharmaceutically acceptable tonicity adjusting agent, a pharmaceutically acceptable humectant, a pharmaceutically acceptable antioxidant, and a pharmaceutically acceptable pH regulating agent. The formulation is suitable for the treatment of ocular diseases by ocular administration, preferably topical ocular administration.
A61K 47/44 - Oils, fats or waxes according to two or more groups of Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
A pharmaceutical formulation comprising laquinimod or a pharmaceutically acceptable salt thereof as active ingredient, a pharmaceutically acceptable viscosity agent, a pharmaceutically acceptable tonicity adjusting agent, a pharmaceutically acceptable humectant, a pharmaceutically acceptable antioxidant, and a pharmaceutically acceptable pH regulating agent. The formulation is suitable for the treatment of ocular diseases by ocular administration, preferably topical ocular administration.
A61K 47/44 - Oils, fats or waxes according to two or more groups of Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
Disclosed is a method for treating an ocular inflammatory disease (OID), e.g., uveitis or conjunctivitis, comprising periodic administration of a therapeutically effective amount of laquinimod or a pharmaceutically acceptable salt thereof. Also provided is a pharmaceutical composition comprising laquinimod or a pharmaceutically acceptable salt thereof for use in treating a subject suffering from an OID, uveitis, bacterial conjunctivitis, viral conjunctivitis, an inflammation of the orbital tissue, the lacrimal apparatus, the eyelid, the cornea, the retina or the optic pathway. This application also provides a method for treating a subject suffering from an autoimmune disease-associated ocular inflammation comprising periodic ocular administration to the subject a therapeutically effective amount of laquinimod or a pharmaceutically acceptable salt, and an ocular pharmaceutical composition comprising laquinimod or a pharmaceutically acceptable salt thereof for use in treating an autoimmune disease-associated ocular inflammation.
The present invention relates to compounds for treatment of a disease or disorder associated with excessive vascularisation of the eye, such as for instance corneal neovascularisation, neovascularisation of the iris, neovascularisation of the ciliary body, corneal pannus, choroidal neovascularisation, retinal neovascularisation, wet age-related macular degeneration, proliferative diabetic retinopathy, retinopathy of prematurity, and ischemic retinopathy.
A61K 47/68 - 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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
C07K 16/22 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against growth factors
A combination comprising tasquinimod, or a pharmaceutically acceptable salt thereof, and at least one further compound selected from a proteasome inhibitor, an immunomodulatory imide, and an antibody, for use as a in the treatment of multiple myeloma. A kit comprising tasquinimod and a package insert with instructions for using tasquinimod in combination with at least one further compound selected from a proteasome inhibitor, an immunomodulatory imide, and an antibody, to treat multiple myeloma in an individual. Tasquinimod for use in the treatment of multiple myeloma, in combination with a further compound selected from a proteasome inhibitor, an immunomodulatory imide, and an antibody.
A61K 31/00 - Medicinal preparations containing organic active ingredients
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
23.
TASQUINIMOD OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF FOR USE IN COMBINATION THERAPY
A combination comprising tasquinimod, or a pharmaceutically acceptable salt thereof, and at least one further compound selected from a proteasome inhibitor, an immunomodulatory imide, and an antibody, for use as a in the treatment of multiple myeloma. A kit comprising tasquinimod and a package insert with instructions for using tasquinimod in combination with at least one further compound selected from a proteasome inhibitor, an immunomodulatory imide, and an antibody, to treat multiple myeloma in an individual. Tasquinimod for use in the treatment of multiple myeloma, in combination with a further compound selected from a proteasome inhibitor, an immunomodulatory imide, and an antibody.
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 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
24.
COMPOUNDS FOR TREATMENT OF EYE DISEASES ASSOCIATED WITH EXCESSIVE VASCULARISATION
The present invention relates to compounds for treatment of a disease or disorder associated with excessive vascularisation of the eye, such as for instance corneal neovascularisation, neovascularisation of the iris, neovascularisation of the ciliary body, corneal pannus, choroidal neovascularisation, retinal neovascularisation, wet age- related macular degeneration, proliferative diabetic retinopathy, retinopathy of prematurity, and ischemic retinopathy.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
25.
COMPOUNDS FOR TREATMENT OF EYE DISEASES ASSOCIATED WITH EXCESSIVE VASCULARISATION
The present invention relates to compounds for treatment of a disease or disorder associated with excessive vascularisation of the eye, such as for instance corneal neovascularisation, neovascularisation of the iris, neovascularisation of the ciliary body, corneal pannus, choroidal neovascularisation, retinal neovascularisation, wet age- related macular degeneration, proliferative diabetic retinopathy, retinopathy of prematurity, and ischemic retinopathy.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
01 - Chemical and biological materials for industrial, scientific and agricultural use
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Chemicals for use in industry and science; Chemical products for biotechnological purposes [industrial]; Chemical substances for use in the biotechnological industry; Passivating agents; Reagents for research purposes; Reagents for industrial purposes; Reagents for chemical analyses. Pharmaceutical preparations; Vaccines; Medicinal preparations for the treatment of infectious diseases; Pharmaceutical products for the treatment of infectious diseases; Elixirs [pharmaceutical preparations].
27.
Imidazo[2,1-B]thiazole and 5,6-dihydroimidazo[2,1-B]thiazole derivatives useful as S100-inhibitors
A compound of formula (I) or a pharmaceutically acceptable salt thereof. The compound is useful for use in the treatment of cancer, an inflammatory disorder, an autoimmunity disorder or a neurodegenerative disorder.
A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
C07D 215/22 - Oxygen atoms attached in position 2 or 4
29.
N-(heteroaryl)-sulfonamide derivatives useful as S100-inhibitors
A compound of formula (I), or a pharmaceutically acceptable salt thereof and a pharmaceutical composition comprising the compound. The compound is an inhibitor of interactions between SI 00A9 and interaction partners such as RAGE, TLR4 and EMMPRIN and as such is useful in the treatment of disorders such as cancer, autoimmune disorders, inflammatory disorders and neurodegenerative disorders.
C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
C07D 213/76 - Nitrogen atoms to which a second hetero atom is attached
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
C07D 239/47 - One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
30.
Quinoline carboxamides for use in the treatment of leukemia
A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
C07D 215/22 - Oxygen atoms attached in position 2 or 4
A compound of formula (I) or a pharmaceutically acceptable salt thereof and a pharmaceutical composition comprising the compound. The compound is an inhibitor of interactions between S100A9 and interaction partners such as RAGE, TLR4 and EMMPRIN and as such is useful in the treatment of disorders such as cancer, autoimmune disorders, inflammatory disorders and neurodegenerative disorders.
A compound of formula (I), or a pharmaceutically acceptable salt thereof and a pharmaceutical composition comprising the compound. The compound is an inhibitor of interactions between S100A9 and interaction partners such as RAGE, TLR4 and EMMPRIN and as such is useful in the treatment of disorders such as cancer, autoimmune disorders, inflammatory disorders and neurodegenerative disorders.
C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
C07D 213/76 - Nitrogen atoms to which a second hetero atom is attached
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
C07D 239/47 - One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
36.
QUINOLINE CARBOXAMIDES FOR USE IN THE TREATMENT OF MULTIPLE MYELOMA
A compound of formula (I) or a pharmaceutically acceptable salt thereof. The compound is useful for use in the treatment of cancer, an inflammatory disorder,an autoimmunity disorder or a neurodegenerative disorder.
A61K 31/429 - Thiazoles condensed with heterocyclic ring systems
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]
A compound of formula (I) or a pharmaceutically acceptable salt thereof and a pharmaceutical composition comprising the compound. The compound is an inhibitor of interactions between S100A9 and interaction partners such as RAGE, TLR4 and EMMPRIN and as such is useful in the treatment of disorders such as cancer, autoimmune disorders, inflammatory disorders and neurodegenerative disorders.
A compound of formula (I), or a pharmaceutically acceptable salt thereof and a pharmaceutical composition comprising the compound. The compound is an inhibitor of interactions between S100A9 and interaction partners such as RAGE, TLR4 and EMMPRIN and as such is useful in the treatment of disorders such as cancer, autoimmune disorders, inflammatory disorders and neurodegenerative disorders.
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 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
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
41.
Laquinimod for treatment of GABA mediated disorders
This invention provides a method of treating a subject suffering from a GABA related disorder comprising periodically administering to the subject an effective amount of laquinimod or pharmaceutically acceptable salt thereof in an amount effective to treat the subject.
The subject invention provides a pharmaceutical composition comprising N-ethyl-N-phenyl-1,2,-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide or the salt thereof; a pharmaceutically acceptable carrier; and not more than 0.5% w/w relative to N-ethyl-N-phenyl-1,2,-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide of 2-Chloro-6-(1-ethyl-N-methyl-2-oxoindoline-3-carboxamido)benzoic acid, 1H,3H-spiro[5-chloro-1-methylquinoline-2,4-dione-3,3′-[1]ethylindolin-[2]-one], or 5-Chloro-N-ethyl-3-hydroxy-1-methyl-2,4-dioxo-N-phenyl-1,2,3,4-tetrahydro-quinoline-3-carboxamide.
A61K 31/438 - 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 the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
43.
N-ethyl-N-phenyl-1,2-dihydro-4,5-di-hydroxy-1-methyl-2-oxo-3-quinolinecarboxamide, preparation and uses thereof
The subject invention provides a pharmaceutical composition containing laquinimod or a pharmaceutically acceptable salt thereof, and a compound of N-ethyl-N-phenyl-1,2-dihydro-4,5-di-hydroxy-1-methyl-2-oxo-3-quinolinecarboxamide or a salt thereof.
C07D 215/56 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3 with oxygen atoms in position 4
This application provides for a method of treating a human patient afflicted with anti-TNFα refractory Crohn's disease, of treating a human patient afflicted with non-fibrostenotic Crohn's disease, and of treating a human patient whose Crohn's disease had not been surgically treated, the method comprising periodically administering to the patient an amount of laquinimod or pharmaceutically acceptable salt thereof effective to treat the patient. This application also provides for a method of inducing or maintaining clinical remission in a human patient afflicted with Crohn's disease comprising periodically administering to the patient an amount of laquinimod effective to induce or maintain clinical remission in the patient, which amount of laquinimod is less than 0.5 mg/day.
A method for preparing a compound of formula (I) by reacting the appropriate alkyl ester and an aniline derivative, in a refluxing mixture containing an aliphatic solvent or a mixture of aliphatic solvents having a boiling point in the range of 68-191° C.; condensing vapors of the refluxing mixture; treating the condensed vapors with an alcohol scavenging agent or a mixture of alcohol scavenging agents; and returning the condensed vapors back to the reaction mixture.
C07D 215/56 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3 with oxygen atoms in position 4
Deuterium-enriched 4-hydroxy-5-methoxy-N,1-dimethyl-2-oxo-N-[(4-trifluoromethyl)- phenyl]-1,2-dihydroquinoline-3-carboxamide, having a deuterium enrichment in the amide-N methyl group of at least 70%; or a salt thereof with a pharmaceutically acceptable organic or inorganic cation; and a method of preparing said compounds. The compounds are useful in therapy, e.g. for the treatment of a malignant hyperproliferative disorder or an autoimmune disease.
The invention relates to a pharmaceutical composition comprising a pharmaceutically acceptable salt of N-ethyl-N-phenyl-1,2,-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide, N-methylglucamine, and a pharmaceutically acceptable carrier.
A method for preparing a compound of formula (I) by reacting the appropriate alkyl ester and an aniline derivative, in a refluxing mixture containing an aliphatic solvent or a mixture of aliphatic solvents having a boiling point in the range of 68-191 °C; condensing vapors of the refluxing mixture; treating the condensed vapors with an alcohol scavenging agent or a mixture of alcohol scavenging agents; and returning the condensed vapors back to the reaction mixture.
C07D 215/56 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3 with oxygen atoms in position 4
49.
Solid state forms of laquinimod and its sodium salt
Provided herein is a novel crystalline form of laquinimod, process for the preparation, pharmaceutical compositions, and method of treating thereof. Provided also herein are novel amorphous and polymorphic forms of laquinimod sodium, process for the preparation, pharmaceutical compositions, and method of treating thereof.
The present invention relates to a novel method for the production of 2- amino-6-ethylbenzoic acid wherein7-amino-3-methylphtalide or 7-amino-3- hydroxy-3-methylphtalide is reduced to 2-amino-6-ethylbenzoic acid in water or in a mixture of a water miscible solvent and water at a pH of 7 or higher using a hydrogenation catalyst selected from Raney nickel and palladium based catalysts and using a hydrogen source selected from the group consisting of hydrogen gas, formic acid derivatives and cyclohexen. The invention also relates to 2-amino-6-ethylbenzoic acid produced with this method, and to use of such 2-amino-6-ethylbenzoic acid in the production of paquinimod.
C07C 227/18 - 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 involving amino or carboxyl groups, e.g. hydrolysis of esters or amides, by formation of halides, salts or esters
C07C 229/56 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring with amino and carboxyl groups bound in ortho- position
51.
Treatment of BDNF-related disorders using laquinimod
This application provides for a method of increasing brain-derived neurotrophic factor (BDNF) serum level in a human subject comprising periodically administering to the subject an amount of laquinimod or pharmaceutically acceptable salt thereof effective to increase BDNF serum level in the human subject. The method can further comprise periodically administering to the subject an amount of a second BDNF-increasing agent. This application also provides for a method for treating a human subject suffering from a BDNF-related disease comprising periodically administering laquinimod or a pharmaceutically acceptable salt thereof in an amount effective to treat the human subject. This application additionally provides for use of laquinimod in the manufacture of a medicament for increasing BDNF serum level in a human subject. This application further provides for a pharmaceutical composition comprising an amount of laquinimod effective for use in increasing BDNF serum level in a human subject. This application also provides for a pharmaceutical preparation comprising an amount of laquinimod and an amount of a second BDNF-increasing agent effective for use in increasing BDNF serum level in a human subject.
This application provides for a method of treating a subject suffering from Crohn's disease, the method comprising periodically administering to the subject an amount of laquinimod or pharmaceutically acceptable salt thereof effective to treat the subject. This application provides for use of laquinimod in the manufacture of a medicament for treating a subject suffering from Crohn's disease. This application also provides for a pharmaceutical composition comprising laquinimod for use in treating a subject suffering from Crohn's disease.
The subject invention provides a pharmaceutical composition comprising N-ethyl-N-phenyl-1,2,-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide or the salt thereof; a pharmaceutically acceptable carrier; and not more than 0.5% w/w relative to N-ethyl-N-phenyl-1,2,-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide of 2-Chloro-6-(1-ethyl-N-methyl-2-oxoindoline-3-carboxamido)benzoic acid, 1H,3H-spiro[5-chloro-1-methylquinoline-2,4-dione-3,3′-[1]ethylindolin-[2]-one], or 5-Chloro-N-ethyl-3-hydroxy-1-methyl-2,4-dioxo-N-phenyl-1,2,3,4-tetrahydro-quinoline-3-carboxamide.
A method of identifying a compound for use in therapy which modulates the interaction of SlOO A9 with a ligand comprising: - determining whether a candidate compound is capable of modulating the interaction of SlOO A9 with RAGE or the interaction of SlOO A9 with a TLR (Toll like receptor), or - determining whether a candidate compound is capable of binding to S100A9 in a manner which disrupts binding of SlOO A9 with RAGE or the binding of S100A9 with a TLR, to thereby identify whether the compound may be used in therapy.
The invention relates to a pharmaceutical composition comprising a pharmaceutically acceptable salt of N-ethyl-N-phenyl-1,2,-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide, N-methylglucamine, and a pharmaceutically acceptable carrier.
The present invention relates to methods of treating mammals affected by, for example, a hyperproliferative disease such as cancer, by administering a tumor~ targeted superantigen and a chemotherapeutic agent, whereby the administration of the tumor-targeted superantigen and chemotherapeutic agent reduce the antibody re~sponse and enhance the T cell response. The superantigen, wild-type or modified, is fused to a target-seeking moiety, such as an antibody or an antibody active fragment. The combined administration of a superantigen and a chemotherapeutic agent pro~vides enhanced therapeutic effects in a treated animal.
C07K 14/31 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from bacteria from Micrococcaceae (F) from Staphylococcus (G)
01 - Chemical and biological materials for industrial, scientific and agricultural use
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Chemicals used in industry and science, in particular chemical preparations for biochemical and laboratory use and biotechnological production; reagents. Pharmaceutical preparations, in particular vaccines and preparations for treating infectious diseases.
