The present invention relates to compound of general formula (I): wherein the variables take the various meanings, pharmaceutical compositions containing them and their use in medicine, particularly in cancer such as Glioblastoma. The compounds have shown to be useful in therapy as modulators of TAP73 and sternness- and invasiveness-related genes. The compounds may be isolated from the fermentation broth of a fungal strain of Chaetomium sp., or are derivatives thereof. The strain of Chaetomium sp. HT-GU-SUES-904 with accession number CECT 20840 is also claimed.
Compounds of general formula
Compounds of general formula
Compounds of general formula
wherein
the wavy bond ˜ is either a double bond or the epoxide,
Compounds of general formula
wherein
the wavy bond ˜ is either a double bond or the epoxide,
Compounds of general formula
wherein
the wavy bond ˜ is either a double bond or the epoxide,
or pharmaceutically acceptable salts, solvates, tautomers, or stereoisomers thereof, for use in the treatment of diseases associated with oxidative stress.
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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 39/06 - Free radical scavengers or antioxidants
C12P 17/18 - Preparation of heterocyclic carbon compounds with only O, N, S, Se, or Te as ring hetero atoms containing at least two hetero rings condensed among themselves or condensed with a common carbocyclic ring system, e.g. rifamycin
3.
MACROCYCLES WITH ANTIOXIDANT AND NEUROPROTECTIVE ACTIVITIES
Compounds of general formula wherein the wavy bond ~ is either a double bond or the epoxide, or pharmaceutically acceptable salts, solvates, tautomers, or stereoisomers thereof, for use in the treatment of diseases associated with oxidative stress.
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
A61P 25/14 - Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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 39/06 - Free radical scavengers or antioxidants
C07D 491/044 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
C07D 491/153 - Ortho-condensed systems the condensed system containing two rings with oxygen as ring hetero atom and one ring with nitrogen as ring hetero atom
Compounds of general formula wherein the wavy bond ~ is either a double bond or the epoxide, or pharmaceutically acceptable salts, solvates, tautomers, or stereoisomers thereof, for use in the treatment of diseases associated with oxidative stress.
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 9/00 - Medicinal preparations characterised by special physical form
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 39/06 - Free radical scavengers or antioxidants
5.
COMPOUNDS FOR THE TREATMENT OF NF-KB–RELATED DISEASES OR DISORDERS
The invention relates to a family of fungal compounds which are inhibitors of NF-κB inducing kinase and are thus useful in the treatment of NF-κB-related diseasesor disorderssuch asinflammatory or autoimmune diseasesor disorders.
A61K 31/403 - 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 carbocyclic rings, e.g. carbazole
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
Tolypocladium albumChaunopycnis albaTolypocladium albumTolypocladium album strain is capable of producing terpendoles A, C, I, J, K, N. O and P through fermentation and does not produce nalanthalide.
The invention refers to compounds of general formula (I) wherein the variables take the various meanings, pharmaceutical compositions containing them and their use in medicine: The compounds have shown to be useful in therapy as angiogenesis inhibitors. The compounds are isolated from the fermentation broth of a fungal strain Paraconiothyrium sp., or are derivatives thereof.
C07D 209/70 - [b]- or [c]-condensed containing carbocyclic rings other than six-membered
A61K 31/403 - 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 carbocyclic rings, e.g. carbazole
Compounds of general formula (I), or a pharmaceutically acceptable salt or stereoisomer thereof; a process for preparing compounds of formula (I) and their use in the treatment of cancer and bacterial infections.
Compounds of general formula (I) wherein the R1, R2, R3 and R4 groups are each independently selected from the group consisting of hydrogen, acyl, alkyl, alkenyl, alkynyl, aryl, aralkyl, -CONH2, alkali metal, and sugar and X1, X2 groups are each independently selected from the group consisting of hydrogen and halogen, or a pharmaceutically acceptable salt, solvate, tautomer or stereoisomer thereof, a method of producing them, and their use for the treatment of cancer, Alzheimer's disease, Parkinson's disease, frontoparietal dementia, corticobasal degeneration, Pick's disease, cerebrovascular accidents, peripheral neuropathies, brain, spinal cord trauma, atherosclerosis, balloon injury induced restenosis, pulmonary fibrosis, and liver fibrosis, graft versus host disease (GvHD), transplant rejection, rheumatoid arthritis, inflammatory bowel disease, multiple sclerosis, asthma, psoriasis, human multiple myeloma, T cell acute lymphoblastic leukemia and Hodgkin's disease, as protein kinase inhibitors.
A61K 31/335 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
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 9/00 - Drugs for disorders of the cardiovascular system
A61P 35/02 - Antineoplastic agents specific for leukemia
Compounds of general formula (Ia) or (Ib) or (Ic) or (Id), wherein the R groups are each independently selected from the group consisting of hydrogen, acyl, alkyl, alkenyl, alkynyl, aryl, -CONH2, alkali metal, and sugar, and their use for the treatment of cancers.
C07C 49/743 - Unsaturated compounds containing a keto group being part of a ring containing hydroxy groups having unsaturation outside the rings, e.g. humulones, lupulones
C07C 69/007 - Esters of unsaturated alcohols having the esterified hydroxy group bound to an acyclic carbon atom
C07C 271/12 - 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 hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
C07D 263/52 - Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
C12P 15/00 - Preparation of compounds containing at least three condensed carbocyclic rings
C12P 17/14 - Nitrogen or oxygen as hetero atom and at least one other diverse hetero ring atom in the same ring
A61K 31/27 - Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, e.g. meprobamate, carbachol, neostigmine
A61K 31/22 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
A61K 31/122 - Ketones having the oxygen atom directly attached to a ring, e.g. quinones, vitamin K1, anthralin
A61K 31/423 - Oxazoles condensed with carbocyclic rings
05 - Pharmaceutical, veterinary and sanitary products
35 - Advertising and business services
42 - Scientific, technological and industrial services, research and design
Goods & Services
Compounds obtained by fermentation for the production of medicines; ferments for pharmaceutical, medical and/or veterinary purposes; Pharmaceutical preparations for medical and veterinary purposes; chemico-pharmaceutical preparations; active pharmacological and/or pharmaceutical ingredients; micro-organisms for medical and veterinary purposes. Sales promotion (for others); retailing, wholesaling and selling on-line and/or via global computer networks and/or global communication networks of active pharmacological ingredients, biotechnological and biological preparations, ingredients and compounds, microorganisms, compounds with biological activity, bioactive compounds, compounds obtained by fermentation, ferments and fermentation extracts, pharmaceutical, veterinary and medical preparations and ingredients, natural preparations, compounds and ingredients, chemicals and microbiological preparations for industrial, technological, medical, scientific or other purposes; on-line trading services; business management and exploitation; assistance in the commercial or operational management of an industrial or commercial business; advisory services and consultancy for businesses; business administration; office functions; company and organisation consulting; advertising; on-line advertising on a computer network; direct mail advertising (tracts, prospectuses, printed matter, samples); computerized on-line ordering services; advertising; on-line advertising on a computer network; direct mail advertising (tracts, prospectuses, printed matter, samples); marketing services; business consultancy, advice and information; market and market research and studies; commercial representation; services of import-export and representation; exclusive sales of preparations, ingredients and compounds relating to the marine microbiology and chemistry of natural products, biotechnological and biological preparations, ingredients and compounds, microorganisms, compounds with biological activity, bioactive compounds, compounds obtained by fermentation, ferments and fermentation extracts, pharmaceutical, veterinary and medical preparations and ingredients, natural preparations, compounds and ingredients, natural compounds isolated from microorganisms, chemicals and microbiological preparations for industrial, technological, medical, scientific or other purposes; presentation of goods on any communication media, for retail purposes; auctioneering; organisation of exhibitions and trade fairs for commercial purposes; business consultancy, information, advice and management for businesses in the field of biotechnology and/or applications thereof; public relations; management of clean rooms and chemical libraries; management of database on natural microbial products. Scientific and technological services and research and design relating thereto; industrial analysis and research services; design and development of computer hardware and software; research , development , design and analysis of scientific, technological, bioscientific and biotechnological projects in the field of human and animal health, industrial applications of microbiology, biofuels, aquaculture, biopesticides, foods, cosmetics, phytopharmacology, oenology, environmental or others; scientific and technological services, research and development in the field of biotechnology, marine microbiology and chemistry of natural products, and industrial applications thereof; biotechnology and industrial applications thereof; scientific, technological and biotechnological services, research, development and design of compounds of microbial origin for human and animal health; evaluation of biological activities; research, development, design, analysis and application of biotechnological solutions; scientific, technological and biotechnological services, research, development and design relating to active pharmacological and/or pharmaceutical ingredients, and compounds obtained by fermentation for the production of medicines and/or pharmaceutical preparations; research and development services concerning new products; research and development of microorganisms for the development of bioactive compounds and industrial applications; scientific and biotechnological services, research and development carried out in chemical processing plants, fermentation plants; scientific and biotechnological services, research and development carried out in clean rooms and chemical libraries, and rental thereof; information, consultancy, evaluations, tests, reports, surveys, analysis and advice in relation to the aforesaid services.
12.
TERPENES WITH ANTIFUNGAL ACTIVITY AGAINST MALASSEZIA YEASTS
The present invention relates to the use of some terpenes, for example chlovalicin, ovalicin or fumagillin, as antifungal against Malassezia species and to their use in the manufacture of medicaments for the treatment of human skin diseases caused by these Malassezia species, such as pityriasis versicolor, seborrheic dermatitis, dandruff, atopic dermatitis, psoriasis, confluent and reticulated papillomatosis, onychomycosis, and transient acantholytic dermatosis.
A61K 31/336 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having three-membered rings, e.g. oxirane, fumagillin
The present invention relates to the use of Collismycin and derivatives thereof as inhibitors of oxidative stress in cells and their use for the preparation of medicaments for the treatment and/or prevention of oxidative stress-induced diseases or conditions, especially neurodegenerative diseases, such as Alzheimer´s Disease and Parkinson's Disease.
