EA200300286A1 - Агонисты активируемых пероксисомальным пролифератором рецепторов - Google Patents
Агонисты активируемых пероксисомальным пролифератором рецепторовInfo
- Publication number
- EA200300286A1 EA200300286A1 EA200300286A EA200300286A EA200300286A1 EA 200300286 A1 EA200300286 A1 EA 200300286A1 EA 200300286 A EA200300286 A EA 200300286A EA 200300286 A EA200300286 A EA 200300286A EA 200300286 A1 EA200300286 A1 EA 200300286A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- alkyl
- unsubstituted
- substituted
- haloalkyl
- agonists
- Prior art date
Links
- 230000000858 peroxisomal effect Effects 0.000 title abstract 2
- 239000000556 agonist Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- -1 thiophene-2,5-diyl Chemical group 0.000 abstract 3
- 125000001188 haloalkyl group Chemical group 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 125000005493 quinolyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000003107 substituted aryl group Chemical group 0.000 abstract 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 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
- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- 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
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
-
- 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
-
- 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
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
- C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D263/32—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring 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
- C07D413/06—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
-
- 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
- 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
- C07D413/12—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 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
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Child & Adolescent Psychology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pyridine Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Настоящее изобретение относится к соединениям, представленным следующей структурной формулой (I):и их фармацевтически приемлемым солям, сольватам и гидратам, где n равно 2, 3 или 4 и W представляет CH, CH(OH), C(O) или O; R1 представляет незамещенный или замещенный арил, гетероарил, циклоалкил, гетероциклоалкил, арилалкил, гетероарилалкил, циклоалкилалкил или т-бутил; R2 представляет H, алкил, галогеналкил или фенил; Y представляет незамещенный или замещенный тиофен-2,5-диил или фенилен; R3 представляет алкил или галогеналкил; R4 представляет замещенный или незамещенный фенил, нафтил, 1,2,3,4-тетрагидронафтил, хинолил, пиридил или бензо[1,3]диоксол-5-ильную группу; и R5 представляет H, алкил или аминоалкил; которые используют для модулирования рецептора, активируемого пероксисомальным пролифератором, в частности для лечения сахарного диабета.Международная заявка была опубликована вместе с отчетом о международном поиске.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US22723400P | 2000-08-23 | 2000-08-23 | |
PCT/US2001/022616 WO2002016331A1 (en) | 2000-08-23 | 2001-08-23 | Oxazolyl-arylpropionic acid derivatives and their use as ppar agonists |
Publications (1)
Publication Number | Publication Date |
---|---|
EA200300286A1 true EA200300286A1 (ru) | 2003-08-28 |
Family
ID=22852309
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA200300286A EA200300286A1 (ru) | 2000-08-23 | 2001-08-23 | Агонисты активируемых пероксисомальным пролифератором рецепторов |
Country Status (26)
Country | Link |
---|---|
US (2) | US6930120B2 (ru) |
EP (1) | EP1313716B1 (ru) |
JP (1) | JP2004506721A (ru) |
KR (1) | KR20030027054A (ru) |
CN (1) | CN1471517A (ru) |
AT (1) | ATE361283T1 (ru) |
AU (1) | AU2001284659A1 (ru) |
BR (1) | BR0113409A (ru) |
CA (1) | CA2418104A1 (ru) |
CY (1) | CY1107679T1 (ru) |
CZ (1) | CZ2003482A3 (ru) |
DE (1) | DE60128239T2 (ru) |
DK (1) | DK1313716T3 (ru) |
EA (1) | EA200300286A1 (ru) |
EC (1) | ECSP034504A (ru) |
ES (1) | ES2286137T3 (ru) |
HU (1) | HUP0300857A3 (ru) |
IL (1) | IL154110A0 (ru) |
MX (1) | MXPA03001558A (ru) |
NO (1) | NO20030729L (ru) |
NZ (1) | NZ523804A (ru) |
PL (1) | PL360744A1 (ru) |
PT (1) | PT1313716E (ru) |
SK (1) | SK1872003A3 (ru) |
WO (1) | WO2002016331A1 (ru) |
ZA (1) | ZA200300570B (ru) |
Families Citing this family (18)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE60131001T2 (de) | 2000-08-23 | 2008-07-17 | Eli Lilly And Co., Indianapolis | Oxazolylarylpropionsäure derivate und ihre verwendung als ppar agonisten |
EP1313715B1 (en) | 2000-08-23 | 2007-08-01 | Eli Lilly And Company | Oxazolyl-aryloxyacetic acid derivatives and their use as ppar agonists |
IL158589A0 (en) * | 2001-05-15 | 2004-05-12 | Hoffmann La Roche | Carboxylic acid substituted oxazole derivatives for use as ppar-alpha and -gamma activators in the treatment of diabetes |
KR100459917B1 (ko) * | 2001-12-14 | 2004-12-03 | (주)바이오뉴트리젠 | 페놀릭산 유도체 및 이를 포함하는 혈중 지질 농도 관련질환의 예방 및 치료용 조성물 |
US6867224B2 (en) | 2002-03-07 | 2005-03-15 | Warner-Lambert Company | Compounds that modulate PPAR activity and methods of preparation |
US6833380B2 (en) | 2002-03-07 | 2004-12-21 | Warner-Lambert Company, Llc | Compounds that modulate PPAR activity and methods of preparation |
EP1519925B1 (en) | 2002-07-03 | 2007-09-12 | F. Hoffmann-La Roche Ag | Oxazole derivatives and their use as insulin sensitizers |
KR100736955B1 (ko) | 2002-08-30 | 2007-07-09 | 에프. 호프만-라 로슈 아게 | Ppar알파 및 ppar감마 작용제로서의 신규한 2-아릴티아졸 화합물 |
WO2004024726A1 (en) | 2002-09-12 | 2004-03-25 | F. Hoffmann-La Roche Ag | N-substituted-1h-indol-5-propionic acid compounds as ppar agonists useful for the treatment of diabetes |
TWI343915B (en) * | 2002-10-07 | 2011-06-21 | Hoffmann La Roche | Chirale ppar agonists |
WO2004041275A1 (en) * | 2002-11-08 | 2004-05-21 | F. Hoffmann-La Roche Ag | Substituted 4-alkoxyoxazol derivatives as ppar agonists |
RU2315767C2 (ru) | 2002-11-25 | 2008-01-27 | Ф.Хоффманн-Ля Рош Аг | Индолилпроизводные, способ их получения, фармацевтическая композиция, способ лечения и/или профилактики заболеваний |
DE10308355A1 (de) * | 2003-02-27 | 2004-12-23 | Aventis Pharma Deutschland Gmbh | Aryl-cycloalkyl substituierte Alkansäurederivate, Verfahren zu ihrer Herstellung und ihre Anwendung als Arzneimittel |
US7244763B2 (en) | 2003-04-17 | 2007-07-17 | Warner Lambert Company Llc | Compounds that modulate PPAR activity and methods of preparation |
US20070293423A1 (en) * | 2003-08-20 | 2007-12-20 | Eli Lilly And Company | Compounds, Methods and Formulations for the Oral Delivery of a Glucagon-Like Peptide (Glp)-1 Compound or a Melanocortin-4 Receptor (Mc4) Agonist Peptide |
US7662771B2 (en) * | 2003-08-20 | 2010-02-16 | Emisphere Technologies, Inc. | Compounds, methods and formulations for the oral delivery of a glucagon-like peptide (GLP)-1 compound or a melanocortin-4 receptor (MC4) agonist peptide |
WO2005100318A1 (en) * | 2004-04-14 | 2005-10-27 | Ranbaxy Laboratories Limited | Alkanoic acids and their esters as antidiabetic agents |
JPWO2006057448A1 (ja) * | 2004-11-26 | 2008-06-05 | 武田薬品工業株式会社 | アリールアルカン酸誘導体 |
Family Cites Families (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5089514A (en) | 1990-06-14 | 1992-02-18 | Pfizer Inc. | 3-coxazolyl [phenyl, chromanyl or benzofuranyl]-2-hydroxypropionic acid derivatives and analogs as hypoglycemic agents |
US5232945A (en) | 1992-07-20 | 1993-08-03 | Pfizer Inc. | 3-aryl-2-hydroxypropionic acid derivatives and analogs as antihypertensives |
US6062509A (en) | 1994-12-23 | 2000-05-16 | Hexcel Corporation | Retrofit centerline luggage bin assemblies compatible with existing aircraft bin supports |
US5902726A (en) | 1994-12-23 | 1999-05-11 | Glaxo Wellcome Inc. | Activators of the nuclear orphan receptor peroxisome proliferator-activated receptor gamma |
DE69723680T9 (de) | 1996-02-02 | 2004-11-04 | Merck & Co., Inc. | Antidiabetische mittel |
GB9604242D0 (en) * | 1996-02-28 | 1996-05-01 | Glaxo Wellcome Inc | Chemical compounds |
EP0930299A1 (en) * | 1996-08-19 | 1999-07-21 | Japan Tobacco Inc. | Propionic acid derivatives and applications thereof |
KR100620337B1 (ko) | 1998-03-10 | 2006-09-13 | 오노 야꾸힝 고교 가부시키가이샤 | 카르복실산 유도체와 그 유도체를 유효 성분으로서함유하는 약제 |
ES2204684T3 (es) | 1999-08-27 | 2004-05-01 | Eli Lilly And Company | Derivados de biaril-oxa(tia)zol y su uso como modulares de ppar. |
JP4316787B2 (ja) | 2000-01-11 | 2009-08-19 | 壽製薬株式会社 | エーテル又はアミド誘導体、その製法並びにそれを含有する糖尿病治療剤、 |
EP1313715B1 (en) | 2000-08-23 | 2007-08-01 | Eli Lilly And Company | Oxazolyl-aryloxyacetic acid derivatives and their use as ppar agonists |
DE60131001T2 (de) | 2000-08-23 | 2008-07-17 | Eli Lilly And Co., Indianapolis | Oxazolylarylpropionsäure derivate und ihre verwendung als ppar agonisten |
-
2001
- 2001-08-23 BR BR0113409-4A patent/BR0113409A/pt not_active IP Right Cessation
- 2001-08-23 DE DE60128239T patent/DE60128239T2/de not_active Expired - Lifetime
- 2001-08-23 WO PCT/US2001/022616 patent/WO2002016331A1/en active IP Right Grant
- 2001-08-23 ES ES01963733T patent/ES2286137T3/es not_active Expired - Lifetime
- 2001-08-23 AU AU2001284659A patent/AU2001284659A1/en not_active Abandoned
- 2001-08-23 KR KR10-2003-7002472A patent/KR20030027054A/ko not_active Application Discontinuation
- 2001-08-23 IL IL15411001A patent/IL154110A0/xx unknown
- 2001-08-23 CA CA002418104A patent/CA2418104A1/en not_active Abandoned
- 2001-08-23 PT PT01963733T patent/PT1313716E/pt unknown
- 2001-08-23 US US10/343,476 patent/US6930120B2/en not_active Expired - Fee Related
- 2001-08-23 EA EA200300286A patent/EA200300286A1/ru unknown
- 2001-08-23 MX MXPA03001558A patent/MXPA03001558A/es unknown
- 2001-08-23 AT AT01963733T patent/ATE361283T1/de not_active IP Right Cessation
- 2001-08-23 CZ CZ2003482A patent/CZ2003482A3/cs unknown
- 2001-08-23 DK DK01963733T patent/DK1313716T3/da active
- 2001-08-23 NZ NZ523804A patent/NZ523804A/en unknown
- 2001-08-23 PL PL01360744A patent/PL360744A1/xx not_active Application Discontinuation
- 2001-08-23 EP EP01963733A patent/EP1313716B1/en not_active Expired - Lifetime
- 2001-08-23 HU HU0300857A patent/HUP0300857A3/hu unknown
- 2001-08-23 JP JP2002521432A patent/JP2004506721A/ja not_active Withdrawn
- 2001-08-23 SK SK187-2003A patent/SK1872003A3/sk not_active Application Discontinuation
- 2001-08-23 CN CNA018177387A patent/CN1471517A/zh active Pending
-
2003
- 2003-01-21 ZA ZA200300570A patent/ZA200300570B/en unknown
- 2003-02-14 NO NO20030729A patent/NO20030729L/no not_active Application Discontinuation
- 2003-03-06 EC EC2003004504A patent/ECSP034504A/es unknown
-
2005
- 2005-02-09 US US11/054,226 patent/US7345070B2/en not_active Expired - Fee Related
-
2007
- 2007-06-19 CY CY20071100810T patent/CY1107679T1/el unknown
Also Published As
Publication number | Publication date |
---|---|
HUP0300857A3 (en) | 2007-03-28 |
DE60128239D1 (de) | 2007-06-14 |
ECSP034504A (es) | 2003-04-25 |
EP1313716A1 (en) | 2003-05-28 |
KR20030027054A (ko) | 2003-04-03 |
HUP0300857A2 (hu) | 2003-10-28 |
NO20030729L (no) | 2003-04-02 |
ES2286137T3 (es) | 2007-12-01 |
NZ523804A (en) | 2004-09-24 |
BR0113409A (pt) | 2003-07-01 |
DK1313716T3 (da) | 2007-08-27 |
WO2002016331A1 (en) | 2002-02-28 |
SK1872003A3 (en) | 2003-07-01 |
US20050245584A1 (en) | 2005-11-03 |
ATE361283T1 (de) | 2007-05-15 |
CY1107679T1 (el) | 2013-04-18 |
US7345070B2 (en) | 2008-03-18 |
JP2004506721A (ja) | 2004-03-04 |
PT1313716E (pt) | 2007-07-11 |
PL360744A1 (en) | 2004-09-20 |
NO20030729D0 (no) | 2003-02-14 |
IL154110A0 (en) | 2003-07-31 |
US20040097590A1 (en) | 2004-05-20 |
ZA200300570B (en) | 2004-04-21 |
DE60128239T2 (de) | 2008-01-10 |
MXPA03001558A (es) | 2003-06-06 |
CN1471517A (zh) | 2004-01-28 |
EP1313716B1 (en) | 2007-05-02 |
US6930120B2 (en) | 2005-08-16 |
AU2001284659A1 (en) | 2002-03-04 |
CZ2003482A3 (cs) | 2003-05-14 |
CA2418104A1 (en) | 2002-02-28 |
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