JP2008526724A5 - - Google Patents
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- Publication number
- JP2008526724A5 JP2008526724A5 JP2007548904A JP2007548904A JP2008526724A5 JP 2008526724 A5 JP2008526724 A5 JP 2008526724A5 JP 2007548904 A JP2007548904 A JP 2007548904A JP 2007548904 A JP2007548904 A JP 2007548904A JP 2008526724 A5 JP2008526724 A5 JP 2008526724A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- pharmaceutically acceptable
- cycloalkyl
- substituted
- heteroaryl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 125000000217 alkyl group Chemical group 0.000 claims 44
- 150000001875 compounds Chemical class 0.000 claims 26
- 150000003839 salts Chemical class 0.000 claims 22
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 18
- 125000000623 heterocyclic group Chemical group 0.000 claims 18
- 125000003118 aryl group Chemical group 0.000 claims 16
- 125000000753 cycloalkyl group Chemical group 0.000 claims 16
- 125000005843 halogen group Chemical group 0.000 claims 15
- 125000001072 heteroaryl group Chemical group 0.000 claims 14
- 239000001257 hydrogen Substances 0.000 claims 14
- 229910052739 hydrogen Inorganic materials 0.000 claims 14
- 150000002431 hydrogen Chemical class 0.000 claims 11
- 125000001424 substituent group Chemical group 0.000 claims 11
- 125000003342 alkenyl group Chemical group 0.000 claims 10
- 125000000304 alkynyl group Chemical group 0.000 claims 10
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 9
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 7
- 125000001309 chloro group Chemical group Cl* 0.000 claims 7
- 229910052731 fluorine Inorganic materials 0.000 claims 7
- 239000011737 fluorine Substances 0.000 claims 7
- 125000002877 alkyl aryl group Chemical group 0.000 claims 6
- 239000003937 drug carrier Substances 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 5
- 125000005213 alkyl heteroaryl group Chemical group 0.000 claims 5
- 125000004122 cyclic group Chemical group 0.000 claims 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 4
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- JBXUWTJKJKKFAZ-UHFFFAOYSA-N 4-[3-(piperidin-4-ylmethyl)phenyl]pyridine Chemical compound C=1C=CC(C=2C=CN=CC=2)=CC=1CC1CCNCC1 JBXUWTJKJKKFAZ-UHFFFAOYSA-N 0.000 claims 1
- 102100031933 Adhesion G protein-coupled receptor F5 Human genes 0.000 claims 1
- 208000002705 Glucose Intolerance Diseases 0.000 claims 1
- 101000775045 Homo sapiens Adhesion G protein-coupled receptor F5 Proteins 0.000 claims 1
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 1
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 208000006575 hypertriglyceridemia Diseases 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- -1 or optionally OR 6 Chemical group 0.000 claims 1
- 201000009104 prediabetes syndrome Diseases 0.000 claims 1
- 125000004307 pyrazin-2-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 claims 1
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims 1
- 125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 claims 1
- 230000036186 satiety Effects 0.000 claims 1
- 235000019627 satiety Nutrition 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- UDPYUAHSZFGRJO-UHFFFAOYSA-N tert-butyl 4-[(3-pyridin-4-ylphenyl)methyl]piperidine-1-carboxylate Chemical compound C1CN(C(=O)OC(C)(C)C)CCC1CC1=CC=CC(C=2C=CN=CC=2)=C1 UDPYUAHSZFGRJO-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0428514.4A GB0428514D0 (en) | 2004-12-31 | 2004-12-31 | Compounds |
| GB0428514.4 | 2004-12-31 | ||
| PCT/GB2005/050266 WO2006070208A1 (en) | 2004-12-31 | 2005-12-30 | Pyridine, pyrimidine and pyrazine derivatives as gpcr agonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2008526724A JP2008526724A (ja) | 2008-07-24 |
| JP2008526724A5 true JP2008526724A5 (enExample) | 2008-12-04 |
| JP4916452B2 JP4916452B2 (ja) | 2012-04-11 |
Family
ID=34179041
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007548904A Expired - Fee Related JP4916452B2 (ja) | 2004-12-31 | 2005-12-30 | Ｇｐｃｒ作動薬としてのピリジン、ピリミジン、およびピラジンの誘導体 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US8173807B2 (enExample) |
| EP (1) | EP1838698B1 (enExample) |
| JP (1) | JP4916452B2 (enExample) |
| AT (1) | ATE479677T1 (enExample) |
| DE (1) | DE602005023343D1 (enExample) |
| ES (1) | ES2350729T3 (enExample) |
| GB (1) | GB0428514D0 (enExample) |
| SI (1) | SI1838698T1 (enExample) |
| WO (1) | WO2006070208A1 (enExample) |
Families Citing this family (56)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RS20050532A (sr) | 2003-01-14 | 2007-12-31 | Arena Pharmaceuticals Inc., | Derivati 1,2,3-trisupstituisanog arila i heteroarila kao modulatori metabolizma za profilaksu i tretman poremećaja povezanih sa njim, kao što su dijebetes i hiperglikemija |
| AR045047A1 (es) | 2003-07-11 | 2005-10-12 | Arena Pharm Inc | Derivados arilo y heteroarilo trisustituidos como moduladores del metabolismo y de la profilaxis y tratamiento de desordenes relacionados con los mismos |
| AU2006264649A1 (en) * | 2005-06-30 | 2007-01-11 | Prosidion Limited | GPCR agonists |
| BRPI0616245A2 (pt) * | 2005-09-16 | 2011-06-14 | Arena Pharm Inc | modulador de metabolismo, seus usos, composiÇço farmaceutica compreendendo o mesmo, bem como mÉtodo para produÇço da referida composiÇço |
| PE20071221A1 (es) | 2006-04-11 | 2007-12-14 | Arena Pharm Inc | Agonistas del receptor gpr119 en metodos para aumentar la masa osea y para tratar la osteoporosis y otras afecciones caracterizadas por masa osea baja, y la terapia combinada relacionada a estos agonistas |
| NZ571110A (en) | 2006-04-11 | 2011-03-31 | Arena Pharm Inc | Methods of using GPR119 receptor to identify Glucose-dependent Insulinotropic Peptide (GIP) secretagogue compounds useful for increasing bone mass in an individual |
| WO2008076243A2 (en) | 2006-12-14 | 2008-06-26 | Merck & Co., Inc. | Acyl bipiperidinyl compounds, compositions containing such compounds and methods of treatment |
| EA016507B1 (ru) * | 2007-01-04 | 2012-05-30 | Прозидион Лимитед | Пиперидиновые агонисты gpcr |
| CL2008000018A1 (es) | 2007-01-04 | 2008-08-01 | Prosidion Ltd | Compuestos derivados de heterociclos de nitrogeno y oxigeno, agonistas de gpcr; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento de la obesidad, diabetes, sindrome metabolico, hiperlipidemia, toleranci |
| GB0700122D0 (en) | 2007-01-04 | 2007-02-14 | Prosidion Ltd | GPCR agonists |
| EP2114933B1 (en) | 2007-01-04 | 2011-09-07 | Prosidion Ltd | Piperidine gpcr agonists |
| PE20081849A1 (es) | 2007-01-04 | 2009-01-26 | Prosidion Ltd | Derivados de piperidin-4-il-propoxi-benzamida como agonistas de gpcr |
| JP2010539152A (ja) | 2007-09-10 | 2010-12-16 | プロシディオン・リミテッド | 代謝障害の治療のための化合物 |
| ES2499018T3 (es) | 2007-09-20 | 2014-09-26 | Irm Llc | Compuestos y composiciones como moduladores de la actividad de GPR119 |
| GB0720390D0 (en) | 2007-10-18 | 2007-11-28 | Prosidion Ltd | G-Protein coupled receptor agonists |
| GB0720389D0 (en) | 2007-10-18 | 2008-11-12 | Prosidion Ltd | G-Protein Coupled Receptor Agonists |
| WO2009106561A1 (en) * | 2008-02-27 | 2009-09-03 | Biovitrum Ab (Publ) | Pyrazine compounds for treating gpr119 related disorders |
| WO2009106565A1 (en) * | 2008-02-27 | 2009-09-03 | Biovitrum Ab (Publ) | Agonists of gpr119 |
| EP2146210A1 (en) | 2008-04-07 | 2010-01-20 | Arena Pharmaceuticals, Inc. | Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditions modulated by PYY |
| JP2011520809A (ja) * | 2008-05-05 | 2011-07-21 | アムジエン・インコーポレーテツド | γセクレターゼモジュレーターとしての尿素化合物 |
| ES2403120T3 (es) | 2008-12-24 | 2013-05-14 | Cadila Healthcare Limited | Nuevos derivados de oxima |
| GB0904284D0 (en) | 2009-03-12 | 2009-04-22 | Prosidion Ltd | Compounds for the treatment of metabolic disorders |
| GB0904287D0 (en) | 2009-03-12 | 2009-04-22 | Prosidion Ltd | Compounds for the treatment of metabolic disorders |
| GB0904285D0 (en) | 2009-03-12 | 2009-04-22 | Prosidion Ltd | Compounds for the treatment of metabolic disorders |
| US8293729B2 (en) | 2009-06-24 | 2012-10-23 | Boehringer Ingelheim International Gmbh | Compounds, pharmaceutical composition and methods relating thereto |
| US8481731B2 (en) | 2009-06-24 | 2013-07-09 | Boehringer Ingelheim International Gmbh | Compounds, pharmaceutical composition and methods relating thereto |
| 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 |
| GB201006167D0 (en) | 2010-04-14 | 2010-05-26 | Prosidion Ltd | Compounds for the treatment of metabolic disorders |
| GB201006166D0 (en) | 2010-04-14 | 2010-05-26 | Prosidion Ltd | Compounds for the treatment of metabolic disorders |
| TW201209054A (en) | 2010-05-28 | 2012-03-01 | Prosidion Ltd | Novel compounds |
| WO2012025811A1 (en) | 2010-08-23 | 2012-03-01 | Lupin Limited | Indolylpyrimidines as modulators of gpr119 |
| CN103221410B (zh) | 2010-09-22 | 2017-09-15 | 艾尼纳制药公司 | Gpr119受体调节剂和对与其相关的障碍的治疗 |
| SG188547A1 (en) | 2010-10-08 | 2013-04-30 | Cadila Healthcare Ltd | Novel gpr 119 agonists |
| GB201114389D0 (en) | 2011-08-22 | 2011-10-05 | Prosidion Ltd | Novel compounds |
| AR083904A1 (es) | 2010-11-18 | 2013-04-10 | Prosidion Ltd | Derivados de 1,4-pirrolidinas disustituidos y 3-il-aminas y sus usos en el tratamiento de desordenes metabolicos |
| US9000175B2 (en) | 2010-11-26 | 2015-04-07 | Lupin Limited | Bicyclic GPR119 modulators |
| US9133187B2 (en) | 2011-02-28 | 2015-09-15 | Array Biopharma Inc. | Serine/threonine kinase inhibitors |
| ES2552989T3 (es) | 2011-08-04 | 2015-12-03 | Array Biopharma, Inc. | Compuestos de quinazolina como inhibidores de la cinasa de serina / treonina |
| PE20150666A1 (es) | 2012-03-01 | 2015-05-06 | Array Biopharma Inc | Inhibidores de serina/treonina cinasa |
| EP2877464B1 (en) | 2012-07-24 | 2016-08-24 | Boehringer Ingelheim International GmbH | N-cyclopropyl-n-piperidinyl-amide derivatives and their use as gpr119 modulators |
| CA2882750A1 (en) | 2012-08-27 | 2014-03-06 | Jim Blake | Serine/threonine kinase inhibitors for the treatment of hyperproliferative|diseases |
| CA3002540C (en) | 2015-01-06 | 2023-11-07 | Arena Pharmaceuticals, Inc. | Use of (r)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid for treating conditions related to the s1p1 receptor |
| JP6838744B2 (ja) | 2015-06-22 | 2021-03-03 | アリーナ ファーマシューティカルズ， インコーポレイテッド | Ｓ１Ｐ１レセプター関連障害における使用のための（Ｒ）−２−（７−（４−シクロペンチル−３−（トリフルオロメチル）ベンジルオキシ）−１，２，３，４−テトラヒドロシクロペンタ［ｂ］インドール−３−イル）酢酸（化合物１）の結晶性Ｌ−アルギニン塩 |
| CN110520124A (zh) | 2017-02-16 | 2019-11-29 | 艾尼纳制药公司 | 用于治疗原发性胆汁性胆管炎的化合物和方法 |
| JP7397011B2 (ja) | 2018-06-06 | 2023-12-12 | アリーナ ファーマシューティカルズ， インコーポレイテッド | Ｓ１ｐ１受容体に関連する状態を治療する方法 |
| US11066404B2 (en) | 2018-10-11 | 2021-07-20 | Incyte Corporation | Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors |
| WO2020168197A1 (en) | 2019-02-15 | 2020-08-20 | Incyte Corporation | Pyrrolo[2,3-d]pyrimidinone compounds as cdk2 inhibitors |
| TW202100520A (zh) | 2019-03-05 | 2021-01-01 | 美商英塞特公司 | 作為cdk2 抑制劑之吡唑基嘧啶基胺化合物 |
| US11919904B2 (en) | 2019-03-29 | 2024-03-05 | Incyte Corporation | Sulfonylamide compounds as CDK2 inhibitors |
| WO2020223558A1 (en) | 2019-05-01 | 2020-11-05 | Incyte Corporation | Tricyclic amine compounds as cdk2 inhibitors |
| WO2020223469A1 (en) | 2019-05-01 | 2020-11-05 | Incyte Corporation | N-(1-(methylsulfonyl)piperidin-4-yl)-4,5-di hydro-1h-imidazo[4,5-h]quinazolin-8-amine derivatives and related compounds as cyclin-dependent kinase 2 (cdk2) inhibitors for treating cancer |
| WO2021030537A1 (en) | 2019-08-14 | 2021-02-18 | Incyte Corporation | Imidazolyl pyrimidinylamine compounds as cdk2 inhibitors |
| CR20220170A (es) | 2019-10-11 | 2022-10-10 | Incyte Corp | Aminas bicíclicas como inhibidoras de la cdk2 |
| US11981671B2 (en) | 2021-06-21 | 2024-05-14 | Incyte Corporation | Bicyclic pyrazolyl amines as CDK2 inhibitors |
| US11976073B2 (en) | 2021-12-10 | 2024-05-07 | Incyte Corporation | Bicyclic amines as CDK2 inhibitors |
| CN122055358A (zh) * | 2024-09-04 | 2026-05-15 | 四川大学 | 一种gpr65小分子调节剂及其制备方法和应用 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5629325A (en) * | 1996-06-06 | 1997-05-13 | Abbott Laboratories | 3-pyridyloxymethyl heterocyclic ether compounds useful in controlling chemical synaptic transmission |
| AU6309698A (en) * | 1997-03-12 | 1998-09-29 | Banyu Pharmaceutical Co., Ltd. | Drugs containing aminopyridine derivatives as the active ingredient |
| GB0014022D0 (en) * | 2000-06-08 | 2000-08-02 | Novartis Ag | Organic compounds |
| US20030022891A1 (en) * | 2000-12-01 | 2003-01-30 | Anandan Palani | MCH antagonists and their use in the treatment of obesity |
| ATE341327T1 (de) | 2001-02-28 | 2006-10-15 | Merck & Co Inc | Acylierte piperidin-derivate als melanocortin-4- rezeptor-agonisten |
| CA2439152C (en) | 2001-02-28 | 2008-06-17 | Merck & Co., Inc. | Acylated piperidine derivatives as melanocortin-4 receptor agonists |
| AU2002340010A1 (en) * | 2001-09-26 | 2003-04-07 | Bayer Corporation | Substituted 3-pyridyl indoles and indazoles as c17,20 lyase inhibitors |
| TWI330183B (enExample) * | 2001-10-22 | 2010-09-11 | Eisai R&D Man Co Ltd | |
| GB0203778D0 (en) * | 2002-02-18 | 2002-04-03 | Glaxo Group Ltd | Compounds |
| SE0203654D0 (sv) * | 2002-12-09 | 2002-12-09 | Astrazeneca Ab | New compounds |
| RS20050532A (sr) * | 2003-01-14 | 2007-12-31 | Arena Pharmaceuticals Inc., | Derivati 1,2,3-trisupstituisanog arila i heteroarila kao modulatori metabolizma za profilaksu i tretman poremećaja povezanih sa njim, kao što su dijebetes i hiperglikemija |
| EP1644365A2 (en) * | 2003-07-02 | 2006-04-12 | Biofocus Discovery Ltd | Pyrazine and pyridine derivatives as rho kinase inhibitors |
| US8207147B2 (en) * | 2003-12-24 | 2012-06-26 | Prosidion Limited | Heterocyclic derivatives as GPCR receptor agonists |
-
2004
- 2004-12-31 GB GBGB0428514.4A patent/GB0428514D0/en not_active Ceased
-
2005
- 2005-12-30 EP EP05821785A patent/EP1838698B1/en not_active Expired - Lifetime
- 2005-12-30 WO PCT/GB2005/050266 patent/WO2006070208A1/en not_active Ceased
- 2005-12-30 US US11/794,641 patent/US8173807B2/en not_active Expired - Fee Related
- 2005-12-30 DE DE602005023343T patent/DE602005023343D1/de not_active Expired - Lifetime
- 2005-12-30 ES ES05821785T patent/ES2350729T3/es not_active Expired - Lifetime
- 2005-12-30 AT AT05821785T patent/ATE479677T1/de not_active IP Right Cessation
- 2005-12-30 SI SI200531147T patent/SI1838698T1/sl unknown
- 2005-12-30 JP JP2007548904A patent/JP4916452B2/ja not_active Expired - Fee Related
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