AR048334A1 - Tetrahidrocarbazoles y sus derivados; metodos para su preparacion, composiciones farmaceuticas que los contienen y su uso en la fabricacion de medicamentos para el tratamiento y prevencion de enfermedades moduladas por agonistas de los receptores hepaticos lxralfa y/o lxrbeta. - Google Patents
Tetrahidrocarbazoles y sus derivados; metodos para su preparacion, composiciones farmaceuticas que los contienen y su uso en la fabricacion de medicamentos para el tratamiento y prevencion de enfermedades moduladas por agonistas de los receptores hepaticos lxralfa y/o lxrbeta.Info
- Publication number
- AR048334A1 AR048334A1 ARP050101164A ARP050101164A AR048334A1 AR 048334 A1 AR048334 A1 AR 048334A1 AR P050101164 A ARP050101164 A AR P050101164A AR P050101164 A ARP050101164 A AR P050101164A AR 048334 A1 AR048334 A1 AR 048334A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- halogen
- heteroaryl
- aryl
- Prior art date
Links
- 201000010099 disease Diseases 0.000 title abstract 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title abstract 4
- 238000000034 method Methods 0.000 title abstract 3
- 239000000556 agonist Substances 0.000 title abstract 2
- 238000011282 treatment Methods 0.000 title abstract 2
- 239000003814 drug Substances 0.000 title 1
- 230000002440 hepatic effect Effects 0.000 title 1
- 238000004519 manufacturing process Methods 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 230000002265 prevention Effects 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 17
- 229910052736 halogen Inorganic materials 0.000 abstract 7
- 150000002367 halogens Chemical group 0.000 abstract 7
- 150000001875 compounds Chemical class 0.000 abstract 6
- 125000002877 alkyl aryl group Chemical group 0.000 abstract 5
- 125000003118 aryl group Chemical group 0.000 abstract 4
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 abstract 4
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 4
- 125000005213 alkyl heteroaryl group Chemical group 0.000 abstract 3
- 125000001072 heteroaryl group Chemical group 0.000 abstract 3
- 208000024827 Alzheimer disease Diseases 0.000 abstract 2
- 235000012000 cholesterol Nutrition 0.000 abstract 2
- 150000002148 esters Chemical class 0.000 abstract 2
- -1 low HDL cholesterol Chemical compound 0.000 abstract 2
- 125000003386 piperidinyl group Chemical group 0.000 abstract 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- XKLNOVWDVMWTOB-UHFFFAOYSA-N 2,3,4,9-tetrahydro-1h-carbazole Chemical class N1C2=CC=CC=C2C2=C1CCCC2 XKLNOVWDVMWTOB-UHFFFAOYSA-N 0.000 abstract 1
- 206010008635 Cholestasis Diseases 0.000 abstract 1
- 208000032928 Dyslipidaemia Diseases 0.000 abstract 1
- 206010016654 Fibrosis Diseases 0.000 abstract 1
- 238000008214 LDL Cholesterol Methods 0.000 abstract 1
- 208000017170 Lipid metabolism disease Diseases 0.000 abstract 1
- 208000001145 Metabolic Syndrome Diseases 0.000 abstract 1
- 206010033645 Pancreatitis Diseases 0.000 abstract 1
- 206010040047 Sepsis Diseases 0.000 abstract 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000005115 alkyl carbamoyl group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 230000003143 atherosclerotic effect Effects 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 1
- 230000007870 cholestasis Effects 0.000 abstract 1
- 231100000359 cholestasis Toxicity 0.000 abstract 1
- 230000003920 cognitive function Effects 0.000 abstract 1
- 206010009887 colitis Diseases 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 125000005117 dialkylcarbamoyl group Chemical group 0.000 abstract 1
- 230000004761 fibrosis Effects 0.000 abstract 1
- 230000001771 impaired effect Effects 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 230000002757 inflammatory effect Effects 0.000 abstract 1
- 150000002632 lipids Chemical class 0.000 abstract 1
- 210000004185 liver Anatomy 0.000 abstract 1
- 102000004311 liver X receptors Human genes 0.000 abstract 1
- 108090000865 liver X receptors Proteins 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 230000001131 transforming effect Effects 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/10—Antimycotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/56—Ring systems containing three or more rings
- C07D209/58—[b]- or [c]-condensed
- C07D209/70—[b]- or [c]-condensed containing carbocyclic rings other than six-membered
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/56—Ring systems containing three or more rings
- C07D209/80—[b, c]- or [b, d]-condensed
- C07D209/82—Carbazoles; Hydrogenated carbazoles
- C07D209/86—Carbazoles; Hydrogenated carbazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the ring system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/56—Ring systems containing three or more rings
- C07D209/80—[b, c]- or [b, d]-condensed
- C07D209/82—Carbazoles; Hydrogenated carbazoles
- C07D209/88—Carbazoles; Hydrogenated carbazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—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
- C07D401/02—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
- C07D401/12—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Neurology (AREA)
- Communicable Diseases (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Oncology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Rheumatology (AREA)
- Emergency Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Child & Adolescent Psychology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Endocrinology (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Indole Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Tetrahidrocarbazoles y sus derivados, los compuestos son utiles para el tratamiento y profiláxis de enfermedades que son moduladas por agonistas LXRalfa y/o LXRbeta, indluyendo niveles incrementados de lípidos y colesterol, particuilarmente bajo colesterol-HDL, alto colesterol-LDL, enfermedades ateroscleroticas, diabetes, particularmente diabetes mellitus no-insulino dependiente, síndrome metabolico, dislipidemia, enfermedad de Alzheimer, sepsis, enfermedades inflamatorias tales como colitis, pancreatitis, colestasis/fibrosis del hígado, y enfermedades que tienen un componente inflamatorio tales como enfermedad de Alzheimer o funcion cognitiva deteriorada/mejorable. Reivindicacion 1: Compuestos de la formula (1) en donde n es un numero entero seleccionado de 0 a 3; R1 es independientemente seleccionado del grupo que consiste en halogeno, -CN, -NO2, -SO2Me, alquilo inferior, trifluorometoxilo, -OR11,m piperidinilo, pirrolidinilo, y -N(R11)(R11), en donde R11 es independientemente seleccionado de alquilo inferior y H; X1, X2, X3, y X4 son independientemente seleccionados de N y C, con la condicion de que no más de dos de X1, X2, X3, y X4 puedan ser N a la vez, y cuando dos de X1, X2, X3, y X4 son N, n es 0, 1 o 2; k es un numero entero de 0 a 1; R2 es H; R3 es H, alquilo, o halogeno; R4 es arilo, heteroarilo, alquilarilo o alquilheteroarilo, estando todos opcionalmente sustituidos con 1 a 5 sustituyentes seleccionados independientemente del grupo que contiene halogeno, alquilo, -OR41, alquinilo inferior, y NR42R43, en donde R41es alquilo inferior o -H, R42 y R43 independientemente de cada uno son H o alquilo, o NR42R43 es piperidinilo o pirrolidinilo, oR4 es alquilo; R5 es seleccionado del grupo que consiste en el grupo de formulas (2) estando dichos arilo y heteroarilo opcionalmente sustituidos en una o más posiciones con uno o más sustituyentes independinetemente seleccionados del grupo que consiste en H, halogeno, alquilo inferior y (CH2)vR53, en donde R51 se selecciona del grupo que consiste en H, alquilo, alquenilo inferior y alquilarilo, estando dicho alquilarilo opcionalmente sustituido en una o más posiciones con uno o más alquilos inferiores, -CN, halogeno, -COOR54, y - CH2OR54, en donde R54 es alquilo o -H; R52 es alquilo inferior o -H; R53 es H, alquiolo, cicloalquilo, COOR55, -N(R55)(R56), -CH2OH, -CN, CF3, -CONH2, -CH2OR55 o -CONR55R56, en donde R55 es independientemente seleccionado del grupo que consiste en alquilo, -H, -C(O)-arilo, -C(O)-alquilo, o -C(O)-heteroarilo, y R56 se selecciona el grupo que consiste en H, alquilo, C(O)CF3, -C(O)-arilo, -C(O)-alquilo, -C(O)-heteroarilo, alquilarilo y alquilheteroarilo, y en donde dicho arilo, heteroarilo, alquilarilo y alquil-heteroarilo son opcionalmente sustituidos en una o más posiciones con uno o más de alquilo, -CN, halogeno, -COOR57, y -CH2OR57, en donde R57 es alquilo inferior o -H, o R55 y R56 junto con el átomo al que están unidos forman un anillo; o R53 es arilo que puede opcionalmente estar sustituido con benciloxilo, carboxilo, alcoxilo inferior carbonilo, hidroxi-alquilo inferior, halogeno, carbamoilo, alquilo inferior-carbamoilo, dialquilo inferior-carbamoilo, m es un numero entero seleccionado de 0 a 2; v es un numero entero seleccionado de 0 a 4; y sales aceptables farmacéuticamente y/o ésteres aceptables farmacéuticamente de los mismos. Reivindicacion 35: Un proceso para la elaboracion de un compuesto de la formula (1) de acuerdo con cualquiera de las reivindicaciones 1 a 34, proceso que comprende losm pasos de hacer reaccionar un compuesto de la formula (3) en donde R2, R3, R4, R5 y k tienen el significado dado en cualquiera de las reivindicaciones 1 a 31, con un compuesto de la formula (4) en donde R1, n, X1, X2, X3, y X4 tienen el significado dado en cualquiera de las reivindicaciones 1 a 31, y transformar opcionalmente el compuesto de la formula (1) en uan sal farmacéuticamente aceptable y/o un éster farmacéutuicamente aceptable.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP04101252 | 2004-03-26 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR048334A1 true AR048334A1 (es) | 2006-04-19 |
Family
ID=34963176
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP050101164A AR048334A1 (es) | 2004-03-26 | 2005-03-23 | Tetrahidrocarbazoles y sus derivados; metodos para su preparacion, composiciones farmaceuticas que los contienen y su uso en la fabricacion de medicamentos para el tratamiento y prevencion de enfermedades moduladas por agonistas de los receptores hepaticos lxralfa y/o lxrbeta. |
Country Status (26)
| Country | Link |
|---|---|
| US (2) | US20050215577A1 (es) |
| EP (1) | EP1732892B1 (es) |
| JP (1) | JP4705630B2 (es) |
| KR (1) | KR100803478B1 (es) |
| CN (1) | CN1938273B (es) |
| AR (1) | AR048334A1 (es) |
| AT (1) | ATE408599T1 (es) |
| AU (1) | AU2005225524B2 (es) |
| BR (1) | BRPI0509275A (es) |
| CA (1) | CA2560700A1 (es) |
| DE (1) | DE602005009811D1 (es) |
| DK (1) | DK1732892T3 (es) |
| ES (1) | ES2314633T3 (es) |
| HR (1) | HRP20080651T3 (es) |
| IL (1) | IL177704A (es) |
| MX (1) | MXPA06010815A (es) |
| MY (1) | MY140874A (es) |
| NO (1) | NO20064820L (es) |
| NZ (1) | NZ549396A (es) |
| PL (1) | PL1732892T3 (es) |
| PT (1) | PT1732892E (es) |
| RU (1) | RU2382770C2 (es) |
| SI (1) | SI1732892T1 (es) |
| TW (1) | TW200539870A (es) |
| WO (1) | WO2005092856A1 (es) |
| ZA (1) | ZA200607491B (es) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8168666B2 (en) | 2006-11-30 | 2012-05-01 | Kowa Company, Ltd. | Substituted carbinol compound |
| FR2913886B1 (fr) | 2007-03-22 | 2012-03-02 | Guerbet Sa | Utilisation de nanoparticules metalliques dans le diagnostique de la maladie d'alzheimer |
| WO2009107387A1 (ja) | 2008-02-29 | 2009-09-03 | 興和株式会社 | ２－オキソクロメン誘導体 |
| CN101970479A (zh) * | 2008-03-17 | 2011-02-09 | 弗·哈夫曼-拉罗切有限公司 | Lxr配体结合结构域(lxr lbd)晶体 |
| JP5511080B2 (ja) * | 2008-03-31 | 2014-06-04 | 興和株式会社 | １，３−ジヒドロイソベンゾフラン誘導体 |
| EP2272843A4 (en) | 2008-04-30 | 2011-07-20 | Kowa Co | quinoline |
| US8153634B2 (en) * | 2008-05-29 | 2012-04-10 | Kowa Company, Ltd. | Carbinol derivatives having cyclic linker |
| FR2938537B1 (fr) | 2008-11-14 | 2012-10-26 | Sanofi Aventis | Derives de carbamates d'alkyl-heterocycles, leur preparation et leur application en therapeutique. |
| US8551985B2 (en) * | 2009-04-29 | 2013-10-08 | Kowa Company, Ltd. | Carbinol derivatives having heterocyclic linker |
| EP2623499B1 (en) | 2010-10-01 | 2015-04-22 | Taisho Pharmaceutical Co., Ltd | 1,2,4-triazolone derivative |
| DE102011055815A1 (de) | 2011-11-29 | 2013-05-29 | Aicuris Gmbh & Co. Kg | Carboxamid-substituierte Heteroaryl-Pyrazole und ihre Verwendung |
| CN107674071B (zh) * | 2012-05-11 | 2021-12-31 | 同步制药公司 | 作为隐花色素调节剂的含有咔唑的磺酰胺类 |
| DE102012016908A1 (de) | 2012-08-17 | 2014-02-20 | Aicuris Gmbh & Co. Kg | Tris-(Hetero)Aryl-Pyrazole und ihre Verwendung |
| SG11201507459YA (en) | 2013-03-15 | 2015-10-29 | Epigen Biosciences Inc | Heterocyclic compounds useful in the treatment of disease |
| CN103910659B (zh) * | 2013-11-04 | 2016-05-11 | 迈克斯(如东)化工有限公司 | 2-硝基-4-甲磺酰基苯甲酸的精制方法及其中间体 |
| US9556150B2 (en) | 2013-12-13 | 2017-01-31 | Hoffmann-La Roche Inc. | Inhibitors of bruton's tyrosine kinase |
| WO2015106164A1 (en) | 2014-01-10 | 2015-07-16 | Rgenix, Inc. | Lxr agonists and uses thereof |
| TWI690521B (zh) | 2014-04-07 | 2020-04-11 | 美商同步製藥公司 | 作為隱花色素調節劑之含有咔唑之醯胺類、胺基甲酸酯類及脲類 |
| WO2017023916A1 (en) | 2015-08-05 | 2017-02-09 | Georgetown University | Small molecule androgen receptor inhibitors and methods of use thereof |
| JP7025022B2 (ja) | 2016-01-11 | 2022-02-24 | ザ ロックフェラー ユニバーシティー | 骨髄系由来抑制細胞関連障害の治療のための方法 |
| JP2021504315A (ja) | 2017-11-21 | 2021-02-15 | ルジェニクス，インコーポレーテッド | 多形及びその使用 |
| US20200085810A1 (en) | 2018-07-26 | 2020-03-19 | Hoffmann-La Roche Inc. | Compounds for use in treating kidney disorders |
| US11174220B2 (en) | 2019-12-13 | 2021-11-16 | Inspirna, Inc. | Metal salts and uses thereof |
| CN111518002B (zh) * | 2020-05-21 | 2022-06-21 | 南京林业大学 | 一种硫醚类化合物及其制备方法、医药中间体及其应用 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100500654C (zh) * | 2001-12-14 | 2009-06-17 | 赞塔里斯有限公司 | 作为g-蛋白偶联受体(gpcr)的配体的四氢咔唑衍生物 |
| AU2003222667A1 (en) * | 2002-04-23 | 2003-11-10 | Chugai Seiyaku Kabushiki Kaisha | 1,3-thiazoles as lxr modulators in the treatment of cardiovascular diseases |
| AU2003223684A1 (en) * | 2002-04-23 | 2003-11-10 | Chugai Seiyaku Kabushiki Kaisha | Lxr modulators for the treatment of cardiovascular diseases |
| TWI329111B (en) * | 2002-05-24 | 2010-08-21 | X Ceptor Therapeutics Inc | Azepinoindole and pyridoindole derivatives as pharmaceutical agents |
| CA2486651A1 (en) * | 2002-05-24 | 2003-12-04 | Pharmacia Corporation | Sulfone liver x-receptor modulators |
| EP1534696A4 (en) * | 2002-07-25 | 2010-04-07 | Merck Sharp & Dohme | THERAPEUTIC COMPOUNDS FOR THE TREATMENT OF DYSLIPIDO MINIIDES |
-
2005
- 2005-03-17 DE DE602005009811T patent/DE602005009811D1/de not_active Expired - Lifetime
- 2005-03-17 AT AT05716171T patent/ATE408599T1/de active
- 2005-03-17 AU AU2005225524A patent/AU2005225524B2/en not_active Ceased
- 2005-03-17 MX MXPA06010815A patent/MXPA06010815A/es active IP Right Grant
- 2005-03-17 CA CA002560700A patent/CA2560700A1/en not_active Abandoned
- 2005-03-17 SI SI200530469T patent/SI1732892T1/sl unknown
- 2005-03-17 PL PL05716171T patent/PL1732892T3/pl unknown
- 2005-03-17 BR BRPI0509275-2A patent/BRPI0509275A/pt not_active IP Right Cessation
- 2005-03-17 RU RU2006137655/04A patent/RU2382770C2/ru not_active IP Right Cessation
- 2005-03-17 DK DK05716171T patent/DK1732892T3/da active
- 2005-03-17 WO PCT/EP2005/002869 patent/WO2005092856A1/en not_active Ceased
- 2005-03-17 PT PT05716171T patent/PT1732892E/pt unknown
- 2005-03-17 KR KR1020067019738A patent/KR100803478B1/ko not_active Expired - Fee Related
- 2005-03-17 JP JP2007504315A patent/JP4705630B2/ja not_active Expired - Fee Related
- 2005-03-17 CN CN200580009767XA patent/CN1938273B/zh not_active Expired - Fee Related
- 2005-03-17 EP EP05716171A patent/EP1732892B1/en not_active Expired - Lifetime
- 2005-03-17 NZ NZ549396A patent/NZ549396A/en not_active IP Right Cessation
- 2005-03-17 HR HR20080651T patent/HRP20080651T3/xx unknown
- 2005-03-17 ES ES05716171T patent/ES2314633T3/es not_active Expired - Lifetime
- 2005-03-22 TW TW094108789A patent/TW200539870A/zh unknown
- 2005-03-23 AR ARP050101164A patent/AR048334A1/es active IP Right Grant
- 2005-03-23 US US11/088,065 patent/US20050215577A1/en not_active Abandoned
- 2005-03-24 MY MYPI20051291A patent/MY140874A/en unknown
-
2006
- 2006-08-24 IL IL177704A patent/IL177704A/en not_active IP Right Cessation
- 2006-09-07 ZA ZA200607491A patent/ZA200607491B/en unknown
- 2006-10-24 NO NO20064820A patent/NO20064820L/no not_active Application Discontinuation
-
2010
- 2010-05-06 US US12/774,779 patent/US7906546B2/en not_active Expired - Fee Related
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR048334A1 (es) | Tetrahidrocarbazoles y sus derivados; metodos para su preparacion, composiciones farmaceuticas que los contienen y su uso en la fabricacion de medicamentos para el tratamiento y prevencion de enfermedades moduladas por agonistas de los receptores hepaticos lxralfa y/o lxrbeta. | |
| ES2655669T3 (es) | Derivados de piridinona y pirimidinona como inhibidores del factor XIa | |
| JP6213564B2 (ja) | キノリン誘導体 | |
| CN101460476B (zh) | 有机化合物 | |
| HRP20230052T1 (hr) | Spojevi derivata 1,3,4-oksadiazol sulfonamida kao inhibitori histonske deacetilaze 6, i farmaceutski pripravak koji ih sadrži | |
| AR058901A1 (es) | Compuestos derivados de hidantoina, utiles para el tratamiento de trastornos inflamatorios y composicion farmaceutica que los comprende | |
| HRP20241656T1 (hr) | Derivat nitrila koji djeluje kao inhibitor dipeptidil peptidaze 1 i njegova upotreba | |
| AR074622A1 (es) | Derivados de acido ciclopentanocarboxilico condensados sustituidos con acilamino y su uso como productos farmaceuticos | |
| CO6341548A2 (es) | Nuevos lipidos que contienen azufre para el uso como suplemento alimenticio o como medicamento | |
| AR048537A1 (es) | Derivados de nucleosidos para tratar infecciones por virus de hepatitis c. | |
| RU2011108024A (ru) | 3-азабицикло(3.1.0) гексильные производные в качестве модуляторов метаботропных глутаматных рецепторов | |
| AR071857A1 (es) | Derivados de indazol sustituidos con fenilo y benzodioxinilo, una composicion farmaceutica que los comprende y su uso en la fabricacion de un medicamento para el tratamiento de enfermedades mediadas por el receptor de glucocorticoides. | |
| HRP20151425T1 (hr) | Inhibitori indazola wnt signalnog puta i njihove terapeutske uporabe | |
| ES2564010T3 (es) | Composición farmacéutica para tratar o prevenir el glaucoma | |
| AR039219A1 (es) | Compuestos imidazo-sustituidos | |
| MA37405A1 (fr) | Composés hétérocyclyle | |
| AR035612A1 (es) | 4-(piperidin-4-ilmetil)benzamidas, o sus sales, esteres o solvatos, composiciones farmaceuticas que los comprenden, usos de los mismos para preparar medicamentos, y un kit para utilizar en el tratamiento de una enfermedad cognitiva o neurodegenerativa | |
| JP2016511753A5 (es) | ||
| RU2017117559A (ru) | Бензопроизводные с шестичленным кольцом в качестве ингибитора dpp-4 и их применение | |
| MA39165A1 (fr) | Dérivés de benzimidazole-proline pour leurs utilisations dans le traitement du syndrome des etats crepusculaires | |
| HRP20161237T1 (hr) | Antimalarijski agensi | |
| AR110241A1 (es) | Ácidos indanilaminopiridil-ciclopropano-carboxílicos, composiciones farmacéuticas y usos de los mismos | |
| AR040724A1 (es) | Compuesto de imidazopiridina, composicion farmaceutica que lo comprende y su uso para la fabricacion de un medicamento | |
| AR077534A1 (es) | Derivados de isoxazol, un proceso para su obtencion, composiciones farmaceuticas que los contienen y su uso en el tratamiento de enfermedades relacionadas con el receptor gaba aalfa5 | |
| AR086481A1 (es) | COMBINACION DE UN INHIBIDOR DE CINASA DE FOSFATIDIL-INOSITOL-3 (PI3K), Y UN INHIBIDOR DE mTOR |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration |