AR049497A1 - Derivados indolicos como moduladores del receptor x del higado; composiciones farmaceuticas y metodos de preparacion - Google Patents
Derivados indolicos como moduladores del receptor x del higado; composiciones farmaceuticas y metodos de preparacionInfo
- Publication number
- AR049497A1 AR049497A1 ARP050101717A ARP050101717A AR049497A1 AR 049497 A1 AR049497 A1 AR 049497A1 AR P050101717 A ARP050101717 A AR P050101717A AR P050101717 A ARP050101717 A AR P050101717A AR 049497 A1 AR049497 A1 AR 049497A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- hydrogen
- aryl
- hydroxy
- carbon
- Prior art date
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Classifications
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- 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
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- 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
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- 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]
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- 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
- A61P3/06—Antihyperlipidemics
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- 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
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- 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
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- 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
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- 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
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
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- 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
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/12—Radicals substituted by oxygen atoms
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- 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
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
-
- 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
- C07D401/06—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
-
- 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
- C07D403/06—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 carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—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
- C07D409/06—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 carbon chain containing only aliphatic carbon atoms
-
- 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
- C07D413/10—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 aromatic 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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Rheumatology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Urology & Nephrology (AREA)
- Cardiology (AREA)
- Pain & Pain Management (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychiatry (AREA)
- Gastroenterology & Hepatology (AREA)
- Dermatology (AREA)
- Indole Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Los compuestos pertenecen a la categoría de derivados de indol utilizados como antidiabéticos y antihiperlipidémicos por su accion moduladora del receptor X del hígado. Procedimientos de obtencion de los mismos. Composiciones farmacéuticas que los contienen. Reivindicacion 1: Compuestos de formula (1), en donde: R1 es hidrogeno, alquilo, halogeno, formilo, hidroxialquilo o trifluorometilo; R2 es hidrogeno, alquilo, alquenilo, alquinilo, ciano o halogeno; R3 es hidrogeno o alquilo; R4 es hidrogeno, alquilo, hidroxi o alcoxi; R5 y R6 son independientemente seleccionados a partir de hidrogeno, alquilo, arilalquilo, heteroarilalquilo, hidroxialquilo, alcoxicarbonilo, arilo y heteroarilo; A es arilo o heterociclilo, en donde arilo y heterociclilo son opcionalmente sustituidos con 1 a 3 sustituyentes independientemente seleccionados a partir de alquilo, halogeno, amino, hidroxialquilo, arilo, ariloxi, alcoxi, arilalquilo, arilalquenilo, alcoxicarbonilamino, aminocarboniloxi, carboxi, alcoxicarbonilo, alcoxicarbonilalquilo, aminoalquilo, trifluorometilo, arilalquilaminocarbonilo, alcoxicarbonilalquilaminocarbonilo, indolilalquilaminocarbonilo, morfolinilcarbonilo, aminocarbonilo, aminocarbonilalquilo, aminocarbonilalcoxi, alcoxicarbonilalcoxi, piridinilalquilaminocarbonilo, alquiloxicarbonilalquilarilo, alquiloxicarbonilalcoxiarilo, carboxialquilarilo, carboxialcoxiarilo, aminocarbonilalquilarilo, aminocarbonilalcoxiarilo, aminocarbonilamino, aminocarboniloxi, aminocarboniloxiarilo, carboxialquilo, carboxialcoxi, cicloalquilaminocarbonilo, morfolinilcarboniloxiarilo, morfolinilcarbonilarilo, arilalcoxiarilo, aminocarbonilarilo, pirrolidinilcarboniloxiarilo, pirrolidinilcarbonilarilo, piperidinilcarbonilarilo, piperidinilcarboniloxiarilo; hidroxialquilarilo, hidroxi(carboxi)alquilarilo, hidroxi(alcoxicarbonil)alquilarilo, hidroxi(aminocarbonil)alquilarilo y piridinilo; m es 0, 1, 2 o 3; n es 0 o 1; p es 0, 1, 2 o 3; con la condicion que la suma de m, n y p es 1, 2, 3 o 4; y, en donde el compuesto no es 2-(1-bencil-2,3-dihidro-1H-indol-5-il)-1,1,1,3,3,3-hexafluoro-propan-2-ol; y, en donde el enlace entre los átomos de carbono Ca y Cb es un carbono-carbono simple o doble enlace y en el caso que el enlace Ca y Cb sea un doble enlace carbono-carbono R3 y R4 están ausentes; y sales farmacéuticamente aceptables y ésteres farmacéuticamente aceptables de éstos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP04101889 | 2004-05-03 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR049497A1 true AR049497A1 (es) | 2006-08-09 |
Family
ID=34970495
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP050101717A AR049497A1 (es) | 2004-05-03 | 2005-04-29 | Derivados indolicos como moduladores del receptor x del higado; composiciones farmaceuticas y metodos de preparacion |
Country Status (26)
| Country | Link |
|---|---|
| US (2) | US7173048B2 (es) |
| EP (1) | EP1756096B1 (es) |
| JP (1) | JP4682192B2 (es) |
| KR (1) | KR100893449B1 (es) |
| CN (1) | CN1950365A (es) |
| AR (1) | AR049497A1 (es) |
| AT (1) | ATE439357T1 (es) |
| AU (1) | AU2005238176B2 (es) |
| BR (1) | BRPI0510599A (es) |
| CA (1) | CA2564563C (es) |
| DE (1) | DE602005015962D1 (es) |
| DK (1) | DK1756096T3 (es) |
| ES (1) | ES2329489T3 (es) |
| HR (1) | HRP20090533T1 (es) |
| IL (1) | IL178767A0 (es) |
| MX (1) | MXPA06012683A (es) |
| MY (1) | MY139571A (es) |
| NO (1) | NO20065503L (es) |
| NZ (1) | NZ550447A (es) |
| PL (1) | PL1756096T3 (es) |
| PT (1) | PT1756096E (es) |
| RU (1) | RU2368612C2 (es) |
| SI (1) | SI1756096T1 (es) |
| TW (1) | TWI287537B (es) |
| WO (1) | WO2005105791A1 (es) |
| ZA (1) | ZA200608886B (es) |
Families Citing this family (44)
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| US7790745B2 (en) | 2005-10-21 | 2010-09-07 | Bristol-Myers Squibb Company | Tetrahydroisoquinoline LXR Modulators |
| US7741317B2 (en) | 2005-10-21 | 2010-06-22 | Bristol-Myers Squibb Company | LXR modulators |
| US20070225285A1 (en) * | 2005-11-04 | 2007-09-27 | Amira Pharmaceuticals, Inc. | 5-lipoxygenase-activating protein (flap) inhibitors |
| US20070244128A1 (en) * | 2005-11-04 | 2007-10-18 | Amira Pharmaceuticals, Inc. | 5-lipoxygenase-activating protein (flap) inhibitors |
| US8399666B2 (en) * | 2005-11-04 | 2013-03-19 | Panmira Pharmaceuticals, Llc | 5-lipoxygenase-activating protein (FLAP) inhibitors |
| US20070219206A1 (en) * | 2005-11-04 | 2007-09-20 | Amira Pharmaceuticals, Inc. | 5-lipoxygenase-activating protein (flap) inhibitors |
| GB2431927B (en) * | 2005-11-04 | 2010-03-17 | Amira Pharmaceuticals Inc | 5-Lipoxygenase-activating protein (FLAP) inhibitors |
| US7977359B2 (en) * | 2005-11-04 | 2011-07-12 | Amira Pharmaceuticals, Inc. | 5-lipdxygenase-activating protein (FLAP) inhibitors |
| PL2054049T3 (pl) | 2006-08-24 | 2016-11-30 | Podstawione acyloanilidy i sposoby ich stosowania | |
| WO2008042571A2 (en) | 2006-09-29 | 2008-04-10 | Smithkline Beecham Corporation | Substituted indole compounds |
| EP2094643B1 (en) | 2006-12-01 | 2012-02-29 | Bristol-Myers Squibb Company | N-((3-benzyl)-2,2-(bis-phenyl)-propan-1-amine derivatives as cetp inhibitors for the treatment of atherosclerosis and cardiovascular diseases |
| PE20090213A1 (es) * | 2007-05-04 | 2009-02-28 | Bristol Myers Squibb Co | Agonistas del receptor acoplado a la proteina g gpr119 [6,5]-biciclicos |
| PE20090222A1 (es) * | 2007-05-04 | 2009-03-27 | Bristol Myers Squibb Co | Compuestos [6,6] y [6,7]-biciclicos como agonistas del receptor acoplado a la proteina g gpr119 |
| US8003796B2 (en) * | 2007-07-17 | 2011-08-23 | Bristol-Myers Squibb Company | Pyridone GPR119 G protein-coupled receptor agonists |
| KR100918814B1 (ko) * | 2007-10-04 | 2009-09-25 | 건국대학교 산학협력단 | 인쇄방법을 이용한 세라믹 전자부품 고속제조방법 |
| TW200920369A (en) * | 2007-10-26 | 2009-05-16 | Amira Pharmaceuticals Inc | 5-lipoxygenase activating protein (flap) inhibitor |
| WO2009115212A1 (en) * | 2008-03-17 | 2009-09-24 | F. Hoffmann-La Roche Ag | Lxr ligand binding domain (lxr lbd) crystals |
| KR20160129109A (ko) * | 2008-05-23 | 2016-11-08 | 아미라 파마슈티칼스 인코포레이티드 | 5-리폭시게나아제 활성화 단백질 억제제 |
| TW201006821A (en) | 2008-07-16 | 2010-02-16 | Bristol Myers Squibb Co | Pyridone and pyridazone analogues as GPR119 modulators |
| US8546431B2 (en) | 2008-10-01 | 2013-10-01 | Panmira Pharmaceuticals, Llc | 5-lipoxygenase-activating protein (FLAP) inhibitors |
| SG184168A1 (en) | 2010-04-08 | 2012-10-30 | Bristol Myers Squibb Co | Pyrimidinylpiperidinyloxypyridinone analogues as gpr119 modulators |
| CN102971311B (zh) | 2010-05-06 | 2015-07-08 | 百时美施贵宝公司 | 作为gpr119调节剂的二环杂芳基化合物 |
| WO2011140161A1 (en) | 2010-05-06 | 2011-11-10 | Bristol-Myers Squibb Company | Benzofuranyl analogues as gpr119 modulators |
| KR20140009291A (ko) * | 2011-01-20 | 2014-01-22 | 머크 샤프 앤드 돔 코포레이션 | 미네랄로코르티코이드 수용체 길항제 |
| US9174965B2 (en) | 2012-05-16 | 2015-11-03 | Bristol-Myers Squibb Company | Pyrimidinylpiperidinyloxypyridone analogues as GPR119 modulators |
| US9744149B2 (en) | 2012-07-13 | 2017-08-29 | Gtx, Inc. | Method of treating androgen receptor (AR)-positive breast cancers with selective androgen receptor modulator (SARMs) |
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| US10987334B2 (en) | 2012-07-13 | 2021-04-27 | University Of Tennessee Research Foundation | Method of treating ER mutant expressing breast cancers with selective androgen receptor modulators (SARMs) |
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| KR102122941B1 (ko) | 2012-07-13 | 2020-06-15 | 지티엑스, 인코포레이티드 | 선택적 안드로겐 수용체 조절자(sarms)를 이용한 안드로겐 수용체(ar) 양성 유방암의 치료 방법 |
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2005
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- 2005-04-26 DE DE602005015962T patent/DE602005015962D1/de active Active
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2006
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