EA013084B1 - Модуляторы метаболизма и лечение связанных с ним нарушений - Google Patents
Модуляторы метаболизма и лечение связанных с ним нарушений Download PDFInfo
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- EA013084B1 EA013084B1 EA200800834A EA200800834A EA013084B1 EA 013084 B1 EA013084 B1 EA 013084B1 EA 200800834 A EA200800834 A EA 200800834A EA 200800834 A EA200800834 A EA 200800834A EA 013084 B1 EA013084 B1 EA 013084B1
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- Eurasian Patent Office
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- pharmaceutically acceptable
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Classifications
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- 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
- C07D401/14—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 three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
- A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Diabetes (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Steroid Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US71801505P | 2005-09-16 | 2005-09-16 | |
| PCT/US2006/035651 WO2007035355A2 (en) | 2005-09-16 | 2006-09-14 | Modulators of metabolism and the treatment of disorders related thereto |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA200800834A1 EA200800834A1 (ru) | 2008-08-29 |
| EA013084B1 true EA013084B1 (ru) | 2010-02-26 |
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|---|---|---|---|
| EA200800834A EA013084B1 (ru) | 2005-09-16 | 2006-09-14 | Модуляторы метаболизма и лечение связанных с ним нарушений |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US20100160359A1 (https=) |
| EP (1) | EP1931654B1 (https=) |
| JP (1) | JP2009508861A (https=) |
| KR (1) | KR20080044296A (https=) |
| CN (1) | CN101263135A (https=) |
| AT (1) | ATE429430T1 (https=) |
| AU (1) | AU2006292620A1 (https=) |
| BR (1) | BRPI0616245A2 (https=) |
| CA (1) | CA2619093A1 (https=) |
| DE (1) | DE602006006461D1 (https=) |
| DK (1) | DK1931654T3 (https=) |
| EA (1) | EA013084B1 (https=) |
| EC (1) | ECSP088281A (https=) |
| ES (1) | ES2326391T3 (https=) |
| GE (1) | GEP20104966B (https=) |
| IL (1) | IL189490A0 (https=) |
| MA (1) | MA29860B1 (https=) |
| MX (1) | MX2008003634A (https=) |
| NI (1) | NI200800078A (https=) |
| NO (1) | NO20081810L (https=) |
| NZ (1) | NZ565898A (https=) |
| RS (1) | RS20080112A (https=) |
| TN (1) | TNSN08097A1 (https=) |
| WO (1) | WO2007035355A2 (https=) |
| ZA (1) | ZA200801704B (https=) |
Families Citing this family (75)
| Publication number | Priority date | Publication date | Assignee | Title |
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| US7407955B2 (en) | 2002-08-21 | 2008-08-05 | Boehringer Ingelheim Pharma Gmbh & Co., Kg | 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions |
| MXPA05007485A (es) | 2003-01-14 | 2006-01-30 | Arena Pharm Inc | Derivados de arilo y heteroarilo 1,2,3-trisubstituidos como moduladores del metabolismo y la profilaxis y tratamiento de trastornos relacionados con ello tales como diabetes e hiperglicemia. |
| US7501426B2 (en) | 2004-02-18 | 2009-03-10 | Boehringer Ingelheim International Gmbh | 8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions |
| DE102004054054A1 (de) | 2004-11-05 | 2006-05-11 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Verfahren zur Herstellung chiraler 8-(3-Amino-piperidin-1-yl)-xanthine |
| DE102005035891A1 (de) | 2005-07-30 | 2007-02-08 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | 8-(3-Amino-piperidin-1-yl)-xanthine, deren Herstellung und deren Verwendung als Arzneimittel |
| PE20110235A1 (es) | 2006-05-04 | 2011-04-14 | Boehringer Ingelheim Int | Combinaciones farmaceuticas que comprenden linagliptina y metmorfina |
| EP1852108A1 (en) | 2006-05-04 | 2007-11-07 | Boehringer Ingelheim Pharma GmbH & Co.KG | DPP IV inhibitor formulations |
| KR101452915B1 (ko) | 2006-05-04 | 2014-10-21 | 베링거 인겔하임 인터내셔날 게엠베하 | 다형태 |
| JP2010500300A (ja) | 2006-08-08 | 2010-01-07 | サノフィ−アベンティス | アリールアミノアリール−アルキル−置換イミダゾリジン−２，４−ジオン、それらの製造法、それらの化合物を含有する薬剤、およびそれらの使用 |
| US7638541B2 (en) | 2006-12-28 | 2009-12-29 | Metabolex Inc. | 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine |
| AU2008279447A1 (en) | 2007-07-19 | 2009-01-29 | Metabolex, Inc. | N-azacyclic substituted pyrrole, pyrazole, imidazole, triazole and tetrazole derivatives as agonists of the RUP3 or GPR119 receptor for the treatment of diabetes and metabolic disorders |
| EP2025674A1 (de) | 2007-08-15 | 2009-02-18 | sanofi-aventis | Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
| RU2443699C2 (ru) | 2007-09-20 | 2012-02-27 | Айрм Ллк | Соединения и композиции в качестве модуляторов активности gpr119 |
| CN101910151A (zh) | 2007-10-22 | 2010-12-08 | 先灵公司 | 双环杂环衍生物及其作为gpr119活性调节剂的用途 |
| PE20091730A1 (es) | 2008-04-03 | 2009-12-10 | Boehringer Ingelheim Int | Formulaciones que comprenden un inhibidor de dpp4 |
| EP2108960A1 (en) | 2008-04-07 | 2009-10-14 | Arena Pharmaceuticals, Inc. | Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditons modulated by PYY |
| MX2010013876A (es) * | 2008-06-20 | 2011-03-04 | Metabolex Inc | Agonistas de arilo grpr119 y sus usos . |
| WO2010003624A2 (en) | 2008-07-09 | 2010-01-14 | Sanofi-Aventis | Heterocyclic compounds, processes for their preparation, medicaments comprising these compounds, and the use thereof |
| US8822480B2 (en) | 2008-07-16 | 2014-09-02 | Merck Sharp & Dohme Corp. | Bicyclic heterocycle derivatives and use thereof as GPR119 modulators |
| UY32030A (es) | 2008-08-06 | 2010-03-26 | Boehringer Ingelheim Int | "tratamiento para diabetes en pacientes inapropiados para terapia con metformina" |
| KR20190016601A (ko) | 2008-08-06 | 2019-02-18 | 베링거 인겔하임 인터내셔날 게엠베하 | 메트포르민 요법이 부적합한 환자에서의 당뇨병 치료 |
| CA2736421A1 (en) | 2008-09-10 | 2010-03-18 | Boehringer Ingelheim International Gmbh | Combination therapy for the treatment of diabetes and related conditions |
| US20200155558A1 (en) | 2018-11-20 | 2020-05-21 | Boehringer Ingelheim International Gmbh | Treatment for diabetes in patients with insufficient glycemic control despite therapy with an oral antidiabetic drug |
| WO2010068601A1 (en) | 2008-12-08 | 2010-06-17 | Sanofi-Aventis | A crystalline heteroaromatic fluoroglycoside hydrate, processes for making, methods of use and pharmaceutical compositions thereof |
| WO2010075273A1 (en) | 2008-12-23 | 2010-07-01 | Schering Corporation | Bicyclic heterocycle derivatives and methods of use thereof |
| JP2012512848A (ja) | 2008-12-23 | 2012-06-07 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 有機化合物の塩の形態 |
| TW201036975A (en) | 2009-01-07 | 2010-10-16 | Boehringer Ingelheim Int | Treatment for diabetes in patients with inadequate glycemic control despite metformin therapy |
| JP5657518B2 (ja) | 2009-02-18 | 2015-01-21 | 武田薬品工業株式会社 | 縮合複素環化合物 |
| AR076024A1 (es) | 2009-04-03 | 2011-05-11 | Schering Corp | Derivados de heterociclos biciclicos puenteados y metodos de uso de los mismos |
| EP2414348B1 (en) | 2009-04-03 | 2013-11-20 | Merck Sharp & Dohme Corp. | Bicyclic piperidine and piperazine derivatives as gpcr modulators for the treatment of obesity, diabetes and other metabolic disorders |
| US8481731B2 (en) | 2009-06-24 | 2013-07-09 | Boehringer Ingelheim International Gmbh | Compounds, pharmaceutical composition and methods relating thereto |
| EA201200046A1 (ru) | 2009-06-24 | 2012-08-30 | Бёрингер Ингельхайм Интернациональ Гмбх | Новые соединения, фармацевтическая композиция и связанные с ними способы |
| MX2012001729A (es) | 2009-08-26 | 2012-06-13 | Sanofi Sa | Nuevos hidratos cristalinos de fluoroglicosido heteroaromatico, productos farmaceuticos que comprenden estos compuestos, y su empleo. |
| US8410127B2 (en) | 2009-10-01 | 2013-04-02 | Metabolex, Inc. | Substituted tetrazol-1-yl-phenoxymethyl-thiazol-2-yl-piperidinyl-pyrimidine salts |
| US20120232073A1 (en) | 2009-11-23 | 2012-09-13 | Santhosh Francis Neelamkavil | Fused bicyclic pyrimidine derivatives and methods of use thereof |
| KR20240090632A (ko) | 2009-11-27 | 2024-06-21 | 베링거 인겔하임 인터내셔날 게엠베하 | 리나글립틴과 같은 ｄｐｐ－ｉｖ 억제제를 사용한 유전자형 검사된 당뇨병 환자의 치료 |
| SG10201906876PA (en) | 2010-01-27 | 2019-09-27 | Arena Pharm Inc | Processes for the preparation of (r)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid and salts thereof |
| WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
| JP2013522279A (ja) | 2010-03-18 | 2013-06-13 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 糖尿病及び関連状態の治療で用いるｇｐｒ１１９作動薬とｄｄｐ−ｉｖ阻害薬リナグリプチンの組合せ |
| CA3070513C (en) | 2010-05-05 | 2023-01-03 | Boehringer Ingelheim International Gmbh | A dpp-4 inhibitor for use in treatment of skin-alterations or necrosis |
| WO2011157827A1 (de) | 2010-06-18 | 2011-12-22 | Sanofi | Azolopyridin-3-on-derivate als inhibitoren von lipasen und phospholipasen |
| US8530413B2 (en) | 2010-06-21 | 2013-09-10 | Sanofi | Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments |
| CN109674753A (zh) | 2010-06-23 | 2019-04-26 | 希玛贝治疗股份有限公司 | 固态分散体 |
| KR20130093012A (ko) | 2010-06-24 | 2013-08-21 | 베링거 인겔하임 인터내셔날 게엠베하 | 당뇨병 요법 |
| TW201215387A (en) | 2010-07-05 | 2012-04-16 | Sanofi Aventis | Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament |
| TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments |
| TW201221505A (en) | 2010-07-05 | 2012-06-01 | Sanofi Sa | Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament |
| WO2012025811A1 (en) | 2010-08-23 | 2012-03-01 | Lupin Limited | Indolylpyrimidines as modulators of gpr119 |
| PH12013500547A1 (en) | 2010-09-22 | 2013-06-10 | Arena Pharm Inc | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| KR101563793B1 (ko) * | 2010-10-08 | 2015-10-27 | 카딜라 핼쓰캐어 리미티드 | 신규한 ｇｐｒ 119 작용물질 |
| AR083878A1 (es) | 2010-11-15 | 2013-03-27 | Boehringer Ingelheim Int | Terapia antidiabetica vasoprotectora y cardioprotectora, linagliptina, metodo de tratamiento |
| US9000175B2 (en) | 2010-11-26 | 2015-04-07 | Lupin Limited | Bicyclic GPR119 modulators |
| WO2012120052A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Mit carbozyklen oder heterozyklen substituierte oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung |
| US8828995B2 (en) | 2011-03-08 | 2014-09-09 | Sanofi | Branched oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof |
| US8871758B2 (en) | 2011-03-08 | 2014-10-28 | Sanofi | Tetrasubstituted oxathiazine derivatives, method for producing them, their use as medicine and drug containing said derivatives and the use thereof |
| EP2683699B1 (de) | 2011-03-08 | 2015-06-24 | Sanofi | Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| EP2683705B1 (de) | 2011-03-08 | 2015-04-22 | Sanofi | Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| KR101913619B1 (ko) | 2011-06-09 | 2018-12-28 | 리젠 파마슈티컬스 소시에떼 아노님 | Gpr-119의 조절제로서의 신규한 화합물 |
| DK2731947T3 (en) | 2011-07-15 | 2019-04-23 | Boehringer Ingelheim Int | SUBSTITUTED DIMERIC QUINAZOLINE DERIVATIVE, PREPARATION AND USE thereof IN PHARMACEUTICAL COMPOSITIONS FOR TREATMENT OF TYPE I AND TYPE II DIABETES |
| WO2013037390A1 (en) | 2011-09-12 | 2013-03-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| EP2567959B1 (en) | 2011-09-12 | 2014-04-16 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| EP2760862B1 (en) | 2011-09-27 | 2015-10-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| US9555001B2 (en) | 2012-03-07 | 2017-01-31 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition and uses thereof |
| WO2013171166A1 (en) | 2012-05-14 | 2013-11-21 | Boehringer Ingelheim International Gmbh | A xanthine derivative as dpp-4 inhibitor for use in the treatment of sirs and/or sepsis |
| WO2013171167A1 (en) | 2012-05-14 | 2013-11-21 | Boehringer Ingelheim International Gmbh | A xanthine derivative as dpp -4 inhibitor for use in the treatment of podocytes related disorders and/or nephrotic syndrome |
| WO2013174767A1 (en) | 2012-05-24 | 2013-11-28 | Boehringer Ingelheim International Gmbh | A xanthine derivative as dpp -4 inhibitor for use in modifying food intake and regulating food preference |
| WO2014014816A2 (en) * | 2012-07-17 | 2014-01-23 | Ngm Biopharmaceuticals, Inc. | Methods of treating glucose metabolism disorders |
| EP3110449B1 (en) | 2014-02-28 | 2023-06-28 | Boehringer Ingelheim International GmbH | Medical use of a dpp-4 inhibitor |
| MX386419B (es) | 2015-01-06 | 2025-03-18 | Arena Pharm Inc | Metodos de condiciones de tratamiento relacionadas con el receptor s1p1. |
| EP3939965A1 (en) | 2015-06-22 | 2022-01-19 | Arena Pharmaceuticals, Inc. | Crystalline l-arginine salt of (r)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid for use in sipi receptor-associated disorders |
| EP4233840A3 (en) | 2016-06-10 | 2023-10-18 | Boehringer Ingelheim International GmbH | Combinations of linagliptin and metformin |
| AU2017305392A1 (en) | 2016-08-03 | 2019-02-21 | Cymabay Therapeutics, Inc. | Oxymethylene aryl compounds for treating inflammatory gastrointestinal diseases or gastrointestinal conditions |
| MA47504A (fr) | 2017-02-16 | 2019-12-25 | Arena Pharm Inc | Composés et méthodes de traitement de l'angiocholite biliaire primitive |
| ES2987794T3 (es) | 2018-06-06 | 2024-11-18 | Arena Pharm Inc | Procedimientos de tratamiento de afecciones relacionadas con el receptor S1P1 |
| KR102919209B1 (ko) | 2018-08-10 | 2026-01-28 | 다이아핀 테라퓨틱스, 엘엘씨 | 트리-펩타이드 그리고 대사, 심장혈관 및 염증성 장애의 치료 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005007647A1 (en) * | 2003-07-11 | 2005-01-27 | Arena Pharmaceuticals, Inc. | Trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto |
| WO2005121121A2 (en) * | 2004-06-04 | 2005-12-22 | Arena Pharmaceuticals, Inc. | Substituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto |
| WO2006070208A1 (en) * | 2004-12-31 | 2006-07-06 | Prosidion Ltd. | Pyridine, pyrimidine and pyrazine derivatives as gpcr agonists |
Family Cites Families (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CH478817A (de) * | 1965-10-22 | 1969-09-30 | Ciba Geigy | Verfahren zur Herstellung neuer N,N'-Di-(pyrimidyl-(4)-aminoalkyl)-diazacycloalkanen |
| CA961052A (en) * | 1967-01-12 | 1975-01-14 | Max Schellenbaum | N-2-ethylhexyl-n'-aryl ureas and preparation containing them |
| US3608087A (en) * | 1968-06-21 | 1971-09-21 | Merck & Co Inc | Feed compositions |
| US3887329A (en) * | 1969-05-05 | 1975-06-03 | Ciba Geigy Ag | Hexamethyl phosphotriamide-dye compositions |
| US3686238A (en) * | 1970-01-19 | 1972-08-22 | Syntex Corp | Glycerol esterified with 2-naphthyl-acetic acids and fatty acids |
| US3852434A (en) * | 1970-09-11 | 1974-12-03 | Merck & Co Inc | Potentiation of ({31 ) cis-1,2-epoxypropyl)phosphonic acid and analogues thereof |
| US3690834A (en) * | 1971-01-11 | 1972-09-12 | Syva Co | Ligand determination with spin labeled compounds by receptor displacement |
| US3966744A (en) * | 1971-01-11 | 1976-06-29 | Syva Company | Spin labeled compounds |
| DE2106585A1 (de) * | 1971-02-11 | 1972-08-24 | Farbenfabriken Bayer Ag, 5090 Leverkusen | Aminothiodiazole und Thiodiazol-Azofarbstoffe |
| US3966764A (en) * | 1972-07-10 | 1976-06-29 | Syva Company | Ligand determination of spin labeled compounds by receptor displacement-amphetamine analogs |
| US3849420A (en) * | 1972-10-20 | 1974-11-19 | Dow Chemical Co | Bis-(alkylthio-and alkylsulfonyl)-pentachloroquinolines |
| CH574206A5 (https=) * | 1972-11-16 | 1976-04-15 | Ciba Geigy Ag | |
| DE2340569C2 (de) * | 1973-08-10 | 1982-12-02 | Bayer Ag, 5090 Leverkusen | Azofarbstoffe |
| AT340933B (de) * | 1973-08-20 | 1978-01-10 | Thomae Gmbh Dr K | Verfahren zur herstellung neuer pyrimidinderivate und ihrer saureadditionssalze |
| US4101541A (en) * | 1973-12-21 | 1978-07-18 | Ciba-Geigy Corporation | 3-Cyano-1,2,4-thiadiazolyl-5-czo dyestuffs |
| FR2306697A1 (fr) * | 1975-04-10 | 1976-11-05 | Sogeras | Nouvelles pyrimidines utilisables comme medicaments antidiabetiques et hypocholesterolemiants |
| DE2731264A1 (de) * | 1977-07-11 | 1979-02-01 | Boehringer Mannheim Gmbh | Neue 1-acyl-2-cyanaziridine, verfahren zu deren herstellung und diese verbindungen enthaltende pharmazeutische zubereitungen |
| JPS6038696B2 (ja) * | 1977-12-09 | 1985-09-02 | コニカ株式会社 | ハロゲン化銀カラ−写真感光材料 |
| US4242507A (en) * | 1978-02-23 | 1980-12-30 | Fujisawa Pharmaceutical Co., Ltd. | Sulfonic acid esters |
| DE2831580C2 (de) * | 1978-07-18 | 1980-09-18 | Boehringer Mannheim Gmbh, 6800 Mannheim | Verfahren und Reagens zur Bestimmung von Glycerin |
| DE2906603A1 (de) * | 1979-02-21 | 1980-09-04 | Boehringer Mannheim Gmbh | N-substituierte aziridin-2-carbonsaeurederivate, verfahren zu deren herstellung sowie diese substanzen enthaltende arzneimittel |
| DOP1981004033A (es) * | 1980-12-23 | 1990-12-29 | Ciba Geigy Ag | Procedimiento para proteger plantas de cultivo de la accion fitotoxica de herbicidas. |
| DE3334455A1 (de) * | 1983-03-04 | 1984-09-06 | Bayer Ag, 5090 Leverkusen | Guanidin - derivate |
| ZA848275B (en) * | 1983-12-28 | 1985-08-28 | Degussa | New piridine-2-ethers or pyridine-2-thioethers having a nitrogen-containing cycloaliphatic ring |
| DE3601196A1 (de) * | 1986-01-17 | 1987-07-23 | Merck Patent Gmbh | 1,4-dihydropyridine |
| US5364865A (en) * | 1992-12-30 | 1994-11-15 | Sterling Winthrop Inc. | Phenoxy- and phenoxyalkyl-piperidines as antiviral agents |
| TW530047B (en) * | 1994-06-08 | 2003-05-01 | Pfizer | Corticotropin releasing factor antagonists |
| FI970967A7 (fi) * | 1994-09-09 | 1997-03-07 | Nippon Shinyaku Co Ltd | Heterosyklinen johdannainen ja lääkeaine |
| US5691364A (en) * | 1995-03-10 | 1997-11-25 | Berlex Laboratories, Inc. | Benzamidine derivatives and their use as anti-coagulants |
| US6956047B1 (en) * | 1995-06-06 | 2005-10-18 | Pfizer Inc. | Corticotropin releasing factor antagonists |
| US6403599B1 (en) * | 1995-11-08 | 2002-06-11 | Pfizer Inc | Corticotropin releasing factor antagonists |
| US5849759A (en) * | 1995-12-08 | 1998-12-15 | Berlex Laboratories, Inc. | Naphthyl-substituted benzimidazole derivatives as anti-coagulants |
| US5948786A (en) * | 1996-04-12 | 1999-09-07 | Sumitomo Pharmaceuticals Company, Limited | Piperidinylpyrimidine derivatives |
| AR008789A1 (es) * | 1996-07-31 | 2000-02-23 | Bayer Corp | Piridinas y bifenilos substituidos |
| US6008234A (en) * | 1996-09-12 | 1999-12-28 | Berlex Laboratories, Inc. | Benzamidine derivatives substituted by cyclic amino acid and cyclic hydroxy acid derivatives and their use as anti-coagulants |
| US6187777B1 (en) * | 1998-02-06 | 2001-02-13 | Amgen Inc. | Compounds and methods which modulate feeding behavior and related diseases |
| US6239126B1 (en) * | 1998-12-17 | 2001-05-29 | American Home Products Corporation | Arylpiperidine and aryl-1,2,5,6-tetra-hydropyridine urea derivatives |
| US6414002B1 (en) * | 1999-09-22 | 2002-07-02 | Bristol-Myers Squibb Company | Substituted acid derivatives useful as antidiabetic and antiobesity agents and method |
| US6598801B1 (en) * | 2000-11-17 | 2003-07-29 | General Electric Company | Methods and apparatus for injecting water into gas turbine engines |
| US6545016B1 (en) * | 2000-12-08 | 2003-04-08 | 3M Innovative Properties Company | Amide substituted imidazopyridines |
| US6545017B1 (en) * | 2000-12-08 | 2003-04-08 | 3M Innovative Properties Company | Urea substituted imidazopyridines |
| US6525064B1 (en) * | 2000-12-08 | 2003-02-25 | 3M Innovative Properties Company | Sulfonamido substituted imidazopyridines |
| MXPA05007485A (es) * | 2003-01-14 | 2006-01-30 | Arena Pharm Inc | Derivados de arilo y heteroarilo 1,2,3-trisubstituidos como moduladores del metabolismo y la profilaxis y tratamiento de trastornos relacionados con ello tales como diabetes e hiperglicemia. |
| ES2316964T3 (es) * | 2003-02-24 | 2009-04-16 | Arena Pharmaceuticals, Inc. | Fenil-y piridilpipereidinia-derivados como moduladores del metabolismo de la glucosa. |
| US7083933B1 (en) * | 2003-05-09 | 2006-08-01 | Prosidion Limited | Methods for identification of modulators of OSGPR116 activity |
| US7132426B2 (en) * | 2003-07-14 | 2006-11-07 | Arena Pharmaceuticals, Inc. | Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto |
| MY148521A (en) * | 2005-01-10 | 2013-04-30 | Arena Pharm Inc | Substituted pyridinyl and pyrimidinyl derivatives as modulators of metabolism and the treatment of disorders related thereto |
-
2006
- 2006-09-14 BR BRPI0616245-2A patent/BRPI0616245A2/pt not_active IP Right Cessation
- 2006-09-14 NZ NZ565898A patent/NZ565898A/en not_active IP Right Cessation
- 2006-09-14 AU AU2006292620A patent/AU2006292620A1/en not_active Withdrawn
- 2006-09-14 EP EP06803504A patent/EP1931654B1/en active Active
- 2006-09-14 RS RSP-2008/0112A patent/RS20080112A/sr unknown
- 2006-09-14 DE DE602006006461T patent/DE602006006461D1/de active Active
- 2006-09-14 MX MX2008003634A patent/MX2008003634A/es unknown
- 2006-09-14 WO PCT/US2006/035651 patent/WO2007035355A2/en not_active Ceased
- 2006-09-14 ES ES06803504T patent/ES2326391T3/es active Active
- 2006-09-14 US US11/992,024 patent/US20100160359A1/en not_active Abandoned
- 2006-09-14 KR KR1020087006329A patent/KR20080044296A/ko not_active Withdrawn
- 2006-09-14 GE GEAP200610642A patent/GEP20104966B/en unknown
- 2006-09-14 CN CNA2006800339067A patent/CN101263135A/zh not_active Withdrawn
- 2006-09-14 JP JP2008531275A patent/JP2009508861A/ja not_active Withdrawn
- 2006-09-14 DK DK06803504T patent/DK1931654T3/da active
- 2006-09-14 CA CA002619093A patent/CA2619093A1/en not_active Withdrawn
- 2006-09-14 NI NI200800078A patent/NI200800078A/es unknown
- 2006-09-14 EA EA200800834A patent/EA013084B1/ru not_active IP Right Cessation
- 2006-09-14 AT AT06803504T patent/ATE429430T1/de not_active IP Right Cessation
-
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- 2008-02-21 ZA ZA200801704A patent/ZA200801704B/xx unknown
- 2008-02-28 TN TNP2008000097A patent/TNSN08097A1/en unknown
- 2008-03-14 EC EC2008008281A patent/ECSP088281A/es unknown
- 2008-04-14 MA MA30834A patent/MA29860B1/fr unknown
- 2008-04-14 NO NO20081810A patent/NO20081810L/no not_active Application Discontinuation
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005007647A1 (en) * | 2003-07-11 | 2005-01-27 | Arena Pharmaceuticals, Inc. | Trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto |
| WO2005121121A2 (en) * | 2004-06-04 | 2005-12-22 | Arena Pharmaceuticals, Inc. | Substituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto |
| WO2006070208A1 (en) * | 2004-12-31 | 2006-07-06 | Prosidion Ltd. | Pyridine, pyrimidine and pyrazine derivatives as gpcr agonists |
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| GEP20104966B (en) | 2010-04-26 |
| EP1931654B1 (en) | 2009-04-22 |
| ES2326391T3 (es) | 2009-10-08 |
| DK1931654T3 (da) | 2009-07-27 |
| WO2007035355A2 (en) | 2007-03-29 |
| MX2008003634A (es) | 2009-10-08 |
| JP2009508861A (ja) | 2009-03-05 |
| ZA200801704B (en) | 2008-11-26 |
| ECSP088281A (es) | 2008-04-28 |
| CA2619093A1 (en) | 2007-03-29 |
| NI200800078A (es) | 2009-03-03 |
| IL189490A0 (en) | 2008-08-07 |
| EA200800834A1 (ru) | 2008-08-29 |
| ATE429430T1 (de) | 2009-05-15 |
| BRPI0616245A2 (pt) | 2011-06-14 |
| US20100160359A1 (en) | 2010-06-24 |
| WO2007035355A3 (en) | 2007-06-21 |
| HK1112908A1 (en) | 2008-09-19 |
| CN101263135A (zh) | 2008-09-10 |
| DE602006006461D1 (de) | 2009-06-04 |
| NO20081810L (no) | 2008-04-14 |
| RS20080112A (sr) | 2009-05-06 |
| KR20080044296A (ko) | 2008-05-20 |
| EP1931654A2 (en) | 2008-06-18 |
| AU2006292620A1 (en) | 2007-03-29 |
| NZ565898A (en) | 2010-07-30 |
| TNSN08097A1 (en) | 2009-07-14 |
| MA29860B1 (fr) | 2008-10-03 |
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