HRP20030889B1 - Karboksilnom kiselinom supstituirani derivati oksazola u primjeni kao ppar-alfa i -gama aktivatori u liječenju dijabetesa - Google Patents
Karboksilnom kiselinom supstituirani derivati oksazola u primjeni kao ppar-alfa i -gama aktivatori u liječenju dijabetesaInfo
- Publication number
- HRP20030889B1 HRP20030889B1 HR20030889A HRP20030889A HRP20030889B1 HR P20030889 B1 HRP20030889 B1 HR P20030889B1 HR 20030889 A HR20030889 A HR 20030889A HR P20030889 A HRP20030889 A HR P20030889A HR P20030889 B1 HRP20030889 B1 HR P20030889B1
- Authority
- HR
- Croatia
- Prior art keywords
- alkyl
- alkoxy
- hydroxy
- halogen
- phenyl
- Prior art date
Links
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
- C07D413/12—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
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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
-
- 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
- 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
- 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
- C07D413/14—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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Spojevi, naznačeni time, da se biraju iz skupine spojeva prikazanih formulom I: u kojojR1 predstavlja aril ili heteroaril; R2, R3, R4 i R6 su međusobno nezavisno vodik, hidroksi, C2-8-alkenil, halogen, C1-7-alkil ili C1-7-alkoksi, u kojima najmanje jedan od R2, R3, R4 i R6 ne predstavlja vodik, ili R3 i R4 su međusobno vezani tako da tvore prsten zajedno sa atomom ugljika na koji su vezani, a R3 i R4 zajedno predstavljaju -CH=CH-S-, -S-CH=CH-, -CH=CH-O-, -O-CH=CH-, -CH=CH-CH=CH-, -(CH2)3-5-, -O-(CH2)2-3- ili -(CH2)2-3-O- i gdje R2 i R6 su u skladu s prethodno navedenom definicijom; R5 predstavlja C1-7-alkoksi, C2-5-alkeniloksi, R7 predstavlja vodik ili C1-7-alkil; R8 predstavlja vodik ili C1-7-alkil; R9 predstavlja vodik ili C1-7-alkil; R10 predstavlja aril; n je 1, 2 ili 3; gdje veza između ugljikova atoma Ca i ugljikova atoma Cb predstavlja ugljik ugljik jednostruku ili dvostruku vezu; i njihove farmaceutski prihvatljive soli i estere; gdje je: "aril" fenilna ili naftilna grupa koja može po izboru biti mono- ili višestruko supstituirana halogenom, hidroksi, CN, CF3, NO2, NH2, N(H, C1-7-alkil), N (C1-7-alkil) 2, karboksi, aminokarbonil, C1-7-alkil, C1-7alkoksi, fenil i/ili feniloksi; "heteroaril" je aromatski 5- ili 6-člani prsten koji može sadržavati 1,2 ili 3 atoma odabrana iz duškove, kisikove i/ili sumporne ili bicikličke aromatske grupe koja sadrži dva 5- ili 6-člana prstena, u kojima jedan ili oba prstena mogu sadržavati 1, 2 ili 3 atoma odabrana iz dušika, kisika ili sumpora, koja heteroarilna grupa može opcionalno biti mono-ili višestruko supstituirana halogenom, hidroksi, CN, CF3, NO2, NH2, N(H, C1-7-alkilom), N (C1-7-alkil)2, karboksi, aminokarbonilom, C1-7-alkilom, C1-7-alkoksi, fenilom i/ili feniloksi; alkilne ili C1-7-alkilne grupe mogu biti supstituirane s halogenom, hidroksi, C1-7-alkoksi, C1-7-alkoksi-karbonilom, NH2, N(H, C1-7-alkilom) i/ili N (C1-7-alkilom)2.Patent sadrži još 21 patentni zahtjev.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP01111745 | 2001-05-15 | ||
| PCT/EP2002/004962 WO2002092084A1 (en) | 2001-05-15 | 2002-05-06 | Carboxylic acid substituted oxazole derivatives for use as ppar-alpha and -gamma activators in the treatment of diabetes |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HRP20030889A2 HRP20030889A2 (en) | 2005-08-31 |
| HRP20030889B1 true HRP20030889B1 (hr) | 2011-10-31 |
Family
ID=8177436
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HR20030889A HRP20030889B1 (hr) | 2001-05-15 | 2002-05-06 | Karboksilnom kiselinom supstituirani derivati oksazola u primjeni kao ppar-alfa i -gama aktivatori u liječenju dijabetesa |
Country Status (38)
| Country | Link |
|---|---|
| US (1) | US6642389B2 (hr) |
| EP (1) | EP1392295B1 (hr) |
| JP (2) | JP4330883B2 (hr) |
| KR (1) | KR100654516B1 (hr) |
| CN (1) | CN100356917C (hr) |
| AR (1) | AR035892A1 (hr) |
| AT (1) | ATE327753T1 (hr) |
| AU (1) | AU2002342244B2 (hr) |
| BG (1) | BG66316B1 (hr) |
| BR (1) | BRPI0209821B1 (hr) |
| CA (1) | CA2445145C (hr) |
| CY (1) | CY1105160T1 (hr) |
| CZ (1) | CZ20033037A3 (hr) |
| DE (1) | DE60211891T2 (hr) |
| DK (1) | DK1392295T3 (hr) |
| EC (1) | ECSP034848A (hr) |
| EG (1) | EG25755A (hr) |
| ES (1) | ES2264482T3 (hr) |
| GT (1) | GT200200085A (hr) |
| HR (1) | HRP20030889B1 (hr) |
| HU (1) | HU230224B1 (hr) |
| IL (2) | IL158589A0 (hr) |
| JO (1) | JO2282B1 (hr) |
| MA (1) | MA27025A1 (hr) |
| ME (1) | ME01310B (hr) |
| MX (1) | MXPA03010435A (hr) |
| MY (1) | MY136761A (hr) |
| NO (1) | NO333833B1 (hr) |
| NZ (1) | NZ529033A (hr) |
| PA (1) | PA8544901A1 (hr) |
| PE (1) | PE20021152A1 (hr) |
| PL (1) | PL208074B1 (hr) |
| PT (1) | PT1392295E (hr) |
| RU (1) | RU2278859C2 (hr) |
| SI (1) | SI1392295T1 (hr) |
| SK (1) | SK287842B6 (hr) |
| WO (1) | WO2002092084A1 (hr) |
| ZA (1) | ZA200308538B (hr) |
Families Citing this family (50)
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|---|---|---|---|---|
| US7041691B1 (en) | 1999-06-30 | 2006-05-09 | Amgen Inc. | Compounds for the modulation of PPARγ activity |
| CN1238347C (zh) * | 2000-05-26 | 2006-01-25 | 日本新药株式会社 | 杂环衍生物 |
| US20030171399A1 (en) | 2000-06-28 | 2003-09-11 | Tularik Inc. | Quinolinyl and benzothiazolyl modulators |
| MXPA03010435A (es) * | 2001-05-15 | 2004-03-09 | Hoffmann La Roche | Derivados de oxazol acido carboxilico sustituidos para uso como activadores de proliferacion del peroximosa(ppar-alfa y gama) en el tratamiento de diabetes. |
| US7456184B2 (en) * | 2003-05-01 | 2008-11-25 | Palatin Technologies Inc. | Melanocortin receptor-specific compounds |
| US7718802B2 (en) | 2001-08-10 | 2010-05-18 | Palatin Technologies, Inc. | Substituted melanocortin receptor-specific piperazine compounds |
| AU2002331064B2 (en) * | 2001-08-10 | 2007-08-23 | Palatin Technologies, Inc. | Peptidomimetics of biologically active metallopeptides |
| US7732451B2 (en) * | 2001-08-10 | 2010-06-08 | Palatin Technologies, Inc. | Naphthalene-containing melanocortin receptor-specific small molecule |
| US7655658B2 (en) * | 2001-08-10 | 2010-02-02 | Palatin Technologies, Inc. | Thieno [2,3-D]pyrimidine-2,4-dione melanocortin-specific compounds |
| JP2005528346A (ja) | 2002-02-25 | 2005-09-22 | イーライ・リリー・アンド・カンパニー | ペルオキシソーム増殖因子活性化受容体調節物質 |
| EP1537091B1 (en) * | 2002-08-30 | 2010-10-06 | F. Hoffmann-La Roche AG | Novel 2-arylthiazole compounds as pparalpha and ppargamma agonists |
| TWI343915B (en) | 2002-10-07 | 2011-06-21 | Hoffmann La Roche | Chirale ppar agonists |
| CN1738807A (zh) * | 2002-11-15 | 2006-02-22 | 卡地拉健康护理有限公司 | 取代的芳烷基衍生物 |
| ATE405560T1 (de) | 2002-11-25 | 2008-09-15 | Hoffmann La Roche | Indolderivaten |
| US7268157B2 (en) * | 2002-11-26 | 2007-09-11 | Shenzhen Chipscreen Biosciences, Ltd. | Substituted arylalcanoic acid derivatives as PPAR pan agonists with potent antihyperglycemic and antihyperlipidemic activity |
| FR2849849B1 (fr) * | 2003-01-13 | 2006-08-04 | Merck Sante Sas | Nouveaux acides carboxyliques et derives pour le traitement et la prevention du diabete et des dyslipemies |
| US7727991B2 (en) | 2003-05-01 | 2010-06-01 | Palatin Technologies, Inc. | Substituted melanocortin receptor-specific single acyl piperazine compounds |
| US7968548B2 (en) * | 2003-05-01 | 2011-06-28 | Palatin Technologies, Inc. | Melanocortin receptor-specific piperazine compounds with diamine groups |
| US7727990B2 (en) | 2003-05-01 | 2010-06-01 | Palatin Technologies, Inc. | Melanocortin receptor-specific piperazine and keto-piperazine compounds |
| US7262303B2 (en) * | 2003-09-29 | 2007-08-28 | Hoffman-La Roche Inc. | Process for the production of chiral propionic acid derivatives |
| US7223761B2 (en) | 2003-10-03 | 2007-05-29 | Amgen Inc. | Salts and polymorphs of a potent antidiabetic compound |
| KR20080042188A (ko) * | 2003-11-05 | 2008-05-14 | 에프. 호프만-라 로슈 아게 | Ｐｐａｒ 작용제로서 페닐 유도체 |
| BRPI0416284A (pt) | 2003-11-05 | 2007-01-23 | Hoffmann La Roche | compostos, processo para a manufatura dos mesmos, composições farmacêuticas que os contêm, método para o tratamento e/ou prevenção de enfermidades que são moduladas por agonistas ppar(delta) e/ou ppar(alfa) e sua utilização |
| WO2005056536A1 (en) * | 2003-12-10 | 2005-06-23 | Ranbaxy Laboratories Limited | Antidiabetic agents which exhibit activity against ppar |
| US7709484B1 (en) | 2004-04-19 | 2010-05-04 | Palatin Technologies, Inc. | Substituted melanocortin receptor-specific piperazine compounds |
| PT1756096E (pt) | 2004-05-03 | 2009-10-16 | Hoffmann La Roche | Derivados de indolilo como moduladores do receptor x do fígado |
| CN100344618C (zh) * | 2004-05-24 | 2007-10-24 | 北京摩力克科技有限公司 | 作为hPPARα和hPPARγ激动剂的N－芳丙烯酰基取代的酪氨酸衍生物 |
| CN100436430C (zh) * | 2004-05-24 | 2008-11-26 | 北京摩力克科技有限公司 | 作为hPPARα和hPPARγ激动剂的烷酰基取代的酪氨酸衍生物 |
| WO2006108491A1 (en) * | 2005-04-11 | 2006-10-19 | Dsm Fine Chemicals Austria Nfg Gmbh & Co Kg | Improved process for preparing oxazole nitriles |
| US20060241073A1 (en) * | 2005-04-20 | 2006-10-26 | Wanders Ronaldus J A | Means and methods for counteracting fatty acid accumulation |
| US7834017B2 (en) | 2006-08-11 | 2010-11-16 | Palatin Technologies, Inc. | Diamine-containing, tetra-substituted piperazine compounds having identical 1- and 4-substituents |
| KR100847780B1 (ko) * | 2006-10-26 | 2008-07-23 | 재단법인서울대학교산학협력재단 | 2-에톡시프로피온산 유도체 또는 이의 약학적으로허용가능한 염, 이의 제조방법 및 이를 유효성분으로함유하는 당뇨병 예방 및 치료제 |
| GB2460784A (en) * | 2007-03-07 | 2009-12-16 | Dong A Pharmtech Co Ltd | Novel phenylpropionic acid derivatives as peroxisome proliferator-activated gamma receptor modulators,method of the same,and pharmaceutical composition |
| ES2390620T3 (es) * | 2008-03-10 | 2012-11-14 | Nestec S.A. | Ácidos dicarboxílicos de cadena mediana y sus derivados y trastornos metabólicos |
| WO2009140163A1 (en) * | 2008-05-15 | 2009-11-19 | Merck & Co., Inc. | Oxazolobenzimidazole derivatives |
| CA2747309C (en) | 2008-12-23 | 2023-09-26 | F. Hoffmann-La Roche Ag | Structured testing method for diagnostic or therapy support of a patient with a chronic disease and devices thereof |
| AU2010206249B2 (en) * | 2009-01-23 | 2015-07-09 | F. Hoffmann-La Roche Ag | Pharmaceutical composition comprising aleglitazar |
| CN101805337B (zh) * | 2009-02-13 | 2012-05-23 | 天津药物研究院 | 一类含脯氨酸和异恶唑骨架的化合物、其制备方法和用途 |
| US8450496B2 (en) * | 2009-03-24 | 2013-05-28 | Hoffman-La Roche Inc. | Process for the preparation of propionic acid derivatives |
| SI2585452T1 (sl) | 2009-12-07 | 2015-12-31 | F. Hoffmann-La Roche Ag | Postopek za pripravo derivatov propionske kisline |
| CN102351852B (zh) * | 2011-08-23 | 2014-06-18 | 上海交通大学 | 苯并呋喃类化合物及其制备方法、用途 |
| WO2013181384A1 (en) | 2012-05-31 | 2013-12-05 | Ratiopharm Gmbh | Solid state forms of aleglitazar sodium |
| EP2895469B1 (en) * | 2012-09-12 | 2017-10-18 | F. Hoffmann-La Roche AG | Solid forms of (s)-2-methoxy-3-{4-[2-(5-methyl-2-phenyl-oxazol-4-yl)-ethoxy]-benzo[b]thiophen-7-yl}-propionic acid and of salts thereof |
| CN109588042A (zh) | 2015-11-18 | 2019-04-05 | 豪夫迈·罗氏有限公司 | 用于治疗糖尿病肾病的阿格列扎 |
| EP3478297A1 (en) | 2016-06-30 | 2019-05-08 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and pharmaceutical compositions for the treatment of cardiomyopathies |
| WO2020156683A1 (en) | 2019-02-01 | 2020-08-06 | F. Hoffmann-La Roche Ag | Aleglitazar for use in the treatment or prevention of major adverse cardiac events |
| WO2020201263A1 (en) | 2019-04-01 | 2020-10-08 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and pharmaceutical compositions for the treatment and prevention of cardiac remodeling |
| KR20240047401A (ko) * | 2021-08-13 | 2024-04-12 | 알레번드 파마슈티칼스 (홍콩) 리미티드 | 중수소화 화합물 |
| EP4615433A1 (en) | 2022-11-08 | 2025-09-17 | Genfit | Ppar-alpha/gamma agonist for use in the treatment of liver failure |
| CN118480034B (zh) * | 2023-02-13 | 2025-02-11 | 礼邦医药(香港)有限公司 | 氘代化合物的晶型或盐 |
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2002
- 2002-05-06 MX MXPA03010435A patent/MXPA03010435A/es active IP Right Grant
- 2002-05-06 KR KR1020037014816A patent/KR100654516B1/ko not_active Expired - Fee Related
- 2002-05-06 IL IL15858902A patent/IL158589A0/xx unknown
- 2002-05-06 NZ NZ529033A patent/NZ529033A/en not_active IP Right Cessation
- 2002-05-06 HU HU0400992A patent/HU230224B1/hu not_active IP Right Cessation
- 2002-05-06 JP JP2002589001A patent/JP4330883B2/ja not_active Expired - Fee Related
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Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2000008002A1 (en) * | 1998-08-07 | 2000-02-17 | Glaxo Group Limited | SUBSTITUTED OXAZOLES AND THIAZOLES DERIVATIVES AS hPPAR GAMMA AND hPPAR ALPHA ACTIVATORS |
| WO2002016331A1 (en) * | 2000-08-23 | 2002-02-28 | Eli Lilly And Company | Oxazolyl-arylpropionic acid derivatives and their use as ppar agonists |
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