JP2005507932A5 - - Google Patents
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- Publication number
- JP2005507932A5 JP2005507932A5 JP2003539676A JP2003539676A JP2005507932A5 JP 2005507932 A5 JP2005507932 A5 JP 2005507932A5 JP 2003539676 A JP2003539676 A JP 2003539676A JP 2003539676 A JP2003539676 A JP 2003539676A JP 2005507932 A5 JP2005507932 A5 JP 2005507932A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- represents hydrogen
- pharmaceutically acceptable
- formula
- 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.)
- Withdrawn
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- 229910052739 hydrogen Inorganic materials 0.000 claims 65
- 239000001257 hydrogen Substances 0.000 claims 65
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 64
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 63
- 150000002148 esters Chemical class 0.000 claims 39
- 150000003839 salts Chemical class 0.000 claims 39
- 150000001875 compounds Chemical class 0.000 claims 32
- 239000008194 pharmaceutical composition Substances 0.000 claims 25
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 23
- 125000001424 substituent group Chemical group 0.000 claims 21
- 239000003937 drug carrier Substances 0.000 claims 20
- 229910052736 halogen Inorganic materials 0.000 claims 16
- 150000002367 halogens Chemical group 0.000 claims 16
- 229940079593 drug Drugs 0.000 claims 15
- 239000003814 drug Substances 0.000 claims 15
- 125000000623 heterocyclic group Chemical group 0.000 claims 14
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims 12
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 12
- 125000004104 aryloxy group Chemical group 0.000 claims 11
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 11
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 11
- 229910052717 sulfur Inorganic materials 0.000 claims 11
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 10
- 125000000217 alkyl group Chemical group 0.000 claims 10
- 239000003472 antidiabetic agent Substances 0.000 claims 10
- 125000004093 cyano group Chemical group *C#N 0.000 claims 10
- 229940126904 hypoglycaemic agent Drugs 0.000 claims 10
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims 10
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 10
- 229910052760 oxygen Inorganic materials 0.000 claims 10
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 9
- 125000004432 carbon atom Chemical group C* 0.000 claims 8
- 125000005842 heteroatom Chemical group 0.000 claims 8
- 229910052757 nitrogen Inorganic materials 0.000 claims 8
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 8
- 125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 claims 6
- 125000003545 alkoxy group Chemical group 0.000 claims 6
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 6
- HSINOMROUCMIEA-FGVHQWLLSA-N (2s,4r)-4-[(3r,5s,6r,7r,8s,9s,10s,13r,14s,17r)-6-ethyl-3,7-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-17-yl]-2-methylpentanoic acid Chemical compound C([C@@]12C)C[C@@H](O)C[C@H]1[C@@H](CC)[C@@H](O)[C@@H]1[C@@H]2CC[C@]2(C)[C@@H]([C@H](C)C[C@H](C)C(O)=O)CC[C@H]21 HSINOMROUCMIEA-FGVHQWLLSA-N 0.000 claims 5
- ZILVNHNSYBNLSZ-UHFFFAOYSA-N 2-(diaminomethylideneamino)guanidine Chemical compound NC(N)=NNC(N)=N ZILVNHNSYBNLSZ-UHFFFAOYSA-N 0.000 claims 5
- ILPUOPPYSQEBNJ-UHFFFAOYSA-N 2-methyl-2-phenoxypropanoic acid Chemical class OC(=O)C(C)(C)OC1=CC=CC=C1 ILPUOPPYSQEBNJ-UHFFFAOYSA-N 0.000 claims 5
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims 5
- 206010020772 Hypertension Diseases 0.000 claims 5
- 102000004877 Insulin Human genes 0.000 claims 5
- 108090001061 Insulin Proteins 0.000 claims 5
- 229940122199 Insulin secretagogue Drugs 0.000 claims 5
- 229940100389 Sulfonylurea Drugs 0.000 claims 5
- 238000010521 absorption reaction Methods 0.000 claims 5
- 239000000048 adrenergic agonist Substances 0.000 claims 5
- 229940126157 adrenergic receptor agonist Drugs 0.000 claims 5
- 239000003613 bile acid Substances 0.000 claims 5
- 239000011230 binding agent Substances 0.000 claims 5
- 239000003795 chemical substances by application Substances 0.000 claims 5
- 229940125753 fibrate Drugs 0.000 claims 5
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims 5
- 229940125396 insulin Drugs 0.000 claims 5
- 230000008991 intestinal motility Effects 0.000 claims 5
- 230000004130 lipolysis Effects 0.000 claims 5
- 239000000203 mixture Substances 0.000 claims 5
- 230000036186 satiety Effects 0.000 claims 5
- 235000019627 satiety Nutrition 0.000 claims 5
- YROXIXLRRCOBKF-UHFFFAOYSA-N sulfonylurea Chemical class OC(=N)N=S(=O)=O YROXIXLRRCOBKF-UHFFFAOYSA-N 0.000 claims 5
- 230000035924 thermogenesis Effects 0.000 claims 5
- 239000003316 glycosidase inhibitor Substances 0.000 claims 4
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims 2
- 125000002837 carbocyclic group Chemical group 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 229940077274 Alpha glucosidase inhibitor Drugs 0.000 claims 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims 1
- -1 benzyloxycarbonylamino Chemical group 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 229910052708 sodium Inorganic materials 0.000 claims 1
- 239000011734 sodium Substances 0.000 claims 1
- 0 C*C(CCC*1)C1C1CC1 Chemical compound C*C(CCC*1)C1C1CC1 0.000 description 4
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US32923601P | 2001-10-12 | 2001-10-12 | |
| PCT/US2002/032895 WO2003037332A1 (en) | 2001-10-12 | 2002-10-15 | Phenyl substituted 5-membered nitrogen containing heterocycles for the treatment of obesity |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005507932A JP2005507932A (ja) | 2005-03-24 |
| JP2005507932A5 true JP2005507932A5 (https=) | 2006-01-05 |
Family
ID=23284480
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003539676A Withdrawn JP2005507932A (ja) | 2001-10-12 | 2002-10-15 | 肥満の処置のためのフェニル置換５−員窒素含有複素環 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US20050014805A1 (https=) |
| EP (1) | EP1435951B1 (https=) |
| JP (1) | JP2005507932A (https=) |
| CA (1) | CA2463441A1 (https=) |
| DE (1) | DE60208815T2 (https=) |
| ES (1) | ES2256560T3 (https=) |
| MX (1) | MXPA04002931A (https=) |
| WO (1) | WO2003037332A1 (https=) |
Families Citing this family (57)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2002319627A1 (en) | 2001-07-20 | 2003-03-03 | Merck And Co., Inc. | Substituted imidazoles as cannabinoid receptor modulators |
| JP3813152B2 (ja) | 2002-03-12 | 2006-08-23 | メルク エンド カムパニー インコーポレーテッド | 置換アミド類 |
| WO2004058727A1 (en) * | 2002-12-20 | 2004-07-15 | Bayer Pharmaceuticals Corporation | Substituted 3,5-dihydro-4h-imidazol-4-ones for the treatment of obesity |
| US7772188B2 (en) | 2003-01-28 | 2010-08-10 | Ironwood Pharmaceuticals, Inc. | Methods and compositions for the treatment of gastrointestinal disorders |
| CA2514363A1 (en) * | 2003-02-12 | 2004-08-26 | Transtech Pharma, Inc. | Substituted azole derivatives as therapeutic agents |
| MXPA05011922A (es) * | 2003-05-07 | 2006-02-17 | Pfizer Prod Inc | Ligandos del receptor de cannabinoides y sus usos. |
| AR046078A1 (es) | 2003-08-06 | 2005-11-23 | Senomyx Inc | Nuevos sabores, modificadores de sabores, sustancias gustativas, mejoradores de gusto, sustancias gustativas y/o mejoradoras del gusto umani o dulce y uso de los mismos. |
| ES2349195T3 (es) | 2004-01-28 | 2010-12-28 | F. Hoffmann-La Roche Ag | Espiro-benzodioxoles y su uso como antagonistas de cb1. |
| CA2551909C (en) * | 2004-02-12 | 2011-10-11 | Transtech Pharma, Inc. | Substituted azole derivatives, compositions, and methods of use |
| WO2005090340A1 (ja) * | 2004-03-22 | 2005-09-29 | Banyu Pharmaceutical Co., Ltd. | ピペリジン－１－カルボキサミド誘導体 |
| EP1734963A4 (en) | 2004-04-02 | 2008-06-18 | Merck & Co Inc | METHOD FOR TREATING PEOPLE WITH METABOLIC AND ANTHROPOMETRIC DISORDER |
| AU2005236055B2 (en) * | 2004-04-20 | 2011-10-06 | Transtech Pharma, Llc | Substituted thiazole and pyrimidine derivatives as melanocortin receptor modulators |
| JP4675969B2 (ja) | 2004-11-09 | 2011-04-27 | エフ．ホフマン−ラ ロシュ アーゲー | ジベンゾスベロン誘導体 |
| JP4734346B2 (ja) | 2005-02-04 | 2011-07-27 | セノミックス インコーポレイテッド | 連結ヘテロアリール部分を含む化合物、ならびに食用組成物のための新規なうまみフレーバー改変剤、味物質および味覚増強剤としての使用 |
| WO2006089076A2 (en) | 2005-02-18 | 2006-08-24 | Neurogen Corporation | Thiazole amides, imidazole amides and related analogues |
| CA2607953A1 (en) | 2005-05-09 | 2006-11-16 | Tap Pharmaceutical Products, Inc. | Methods for treating nephrolithiasis |
| TW200715993A (en) | 2005-06-15 | 2007-05-01 | Senomyx Inc | Bis-aromatic amides and their uses as sweet flavor modifiers, tastants, and taste enhancers |
| EP1940397A4 (en) * | 2005-08-03 | 2010-01-20 | Takeda Pharmaceuticals North A | METHOD FOR TREATING HYPERTONIA |
| WO2007052843A1 (ja) * | 2005-11-04 | 2007-05-10 | Takeda Pharmaceutical Company Limited | 複素環アミド化合物およびその用途 |
| NZ569329A (en) | 2006-01-30 | 2011-09-30 | Transtech Pharma Inc | Substituted imidazole derivatives and their use as PTPase inhibitors |
| ES2640453T3 (es) | 2006-04-21 | 2017-11-03 | Senomyx, Inc. | Procesos para preparar composiciones saborizantes sólidas |
| US8969514B2 (en) | 2007-06-04 | 2015-03-03 | Synergy Pharmaceuticals, Inc. | Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases |
| MX354786B (es) | 2007-06-04 | 2018-03-21 | Synergy Pharmaceuticals Inc | Agonistas de guanilato ciclasa utiles para el tratamiento de trastornos gastrointestinales, inflamacion, cancer y otros trastornos. |
| CA2691662A1 (en) * | 2007-07-02 | 2009-01-08 | F. Hoffmann-La Roche Ag | Imidazole derivatives as ccr2 receptor antagonists |
| ES2408384T3 (es) * | 2007-07-27 | 2013-06-20 | Bristol-Myers Squibb Company | Nuevos activadores de glucoquinasa y procedimientos de uso de los mismos |
| ES2522968T3 (es) | 2008-06-04 | 2014-11-19 | Synergy Pharmaceuticals Inc. | Agonistas de guanilato ciclasa útiles para el tratamiento de trastornos gastrointestinales, inflamación, cáncer y otros trastornos |
| US9447049B2 (en) | 2010-03-01 | 2016-09-20 | University Of Tennessee Research Foundation | Compounds for treatment of cancer |
| US9029408B2 (en) | 2008-06-16 | 2015-05-12 | Gtx, Inc. | Compounds for treatment of cancer |
| US8822513B2 (en) | 2010-03-01 | 2014-09-02 | Gtx, Inc. | Compounds for treatment of cancer |
| MX2010014066A (es) | 2008-06-16 | 2011-06-01 | Univ Tennessee Res Foundation | Compuestos para el tratamiento del cancer. |
| AU2009270833B2 (en) | 2008-07-16 | 2015-02-19 | Bausch Health Ireland Limited | Agonists of guanylate cyclase useful for the treatment of gastrointestinal, inflammation, cancer and other disorders |
| US8563742B2 (en) * | 2008-08-29 | 2013-10-22 | High Point Pharmaceuticals, Llc | Substituted aminothiazole derivatives, pharmaceutical compositions, and methods of use |
| EP2348857B1 (en) | 2008-10-22 | 2016-02-24 | Merck Sharp & Dohme Corp. | Novel cyclic benzimidazole derivatives useful anti-diabetic agents |
| US8329914B2 (en) | 2008-10-31 | 2012-12-11 | Merck Sharp & Dohme Corp | Cyclic benzimidazole derivatives useful as anti-diabetic agents |
| JP2013520502A (ja) | 2010-02-25 | 2013-06-06 | メルク・シャープ・エンド・ドーム・コーポレイション | 有用な抗糖尿病薬である新規な環状ベンズイミダゾール誘導体 |
| JP5879273B2 (ja) | 2010-03-01 | 2016-03-08 | ジーティーエックス・インコーポレイテッド | 癌を処置するための化合物 |
| SG10201505997TA (en) | 2010-08-05 | 2015-09-29 | Amgen Inc | Benzimidazole And Azabenzimidazole Compounds That Inhibit Anaplastic Lymphoma Kinase |
| AU2011299153B2 (en) | 2010-09-10 | 2014-10-30 | Takeda Pharmaceuticals U.S.A., Inc. | Methods for concomitant treatment of theophylline and febuxostat |
| US9616097B2 (en) | 2010-09-15 | 2017-04-11 | Synergy Pharmaceuticals, Inc. | Formulations of guanylate cyclase C agonists and methods of use |
| SG192941A1 (en) | 2011-02-25 | 2013-09-30 | Merck Sharp & Dohme | Novel cyclic azabenzimidazole derivatives useful as anti-diabetic agents |
| RU2015106909A (ru) | 2012-08-02 | 2016-09-27 | Мерк Шарп И Доум Корп. | Антидиабетические трициклические соединения |
| KR20150118158A (ko) | 2013-02-22 | 2015-10-21 | 머크 샤프 앤드 돔 코포레이션 | 항당뇨병 비시클릭 화합물 |
| MX2015011438A (es) * | 2013-03-13 | 2016-02-03 | Hoffmann La Roche | Procedimiento para preparar compuestos benzoxazepina. |
| WO2014139388A1 (en) | 2013-03-14 | 2014-09-18 | Merck Sharp & Dohme Corp. | Novel indole derivatives useful as anti-diabetic agents |
| AU2014235215A1 (en) | 2013-03-15 | 2015-10-01 | Synergy Pharmaceuticals Inc. | Agonists of guanylate cyclase and their uses |
| AU2014235209B2 (en) | 2013-03-15 | 2018-06-14 | Bausch Health Ireland Limited | Guanylate cyclase receptor agonists combined with other drugs |
| BR112015030326A2 (pt) | 2013-06-05 | 2017-08-29 | Synergy Pharmaceuticals Inc | Agonistas ultrapuros de guanilato ciclase c, método de fabricar e usar os mesmos |
| WO2015051496A1 (en) | 2013-10-08 | 2015-04-16 | Merck Sharp & Dohme Corp. | Antidiabetic tricyclic compounds |
| HRP20200016T1 (hr) * | 2014-10-30 | 2020-03-20 | Janssen Pharmaceutica Nv | Amidno supstituirani tiazoli kao modulatori rorgamat |
| US10544124B2 (en) * | 2016-02-11 | 2020-01-28 | Bayer Cropscience Aktiengesellschaft | Substituted 2-(het)arylimidazolylcarboxyamides as pesticides |
| TW201803869A (zh) | 2016-04-27 | 2018-02-01 | 健生藥品公司 | 作為ＲＯＲγＴ調節劑之６－胺基吡啶－３－基噻唑 |
| US11072602B2 (en) | 2016-12-06 | 2021-07-27 | Merck Sharp & Dohme Corp. | Antidiabetic heterocyclic compounds |
| EP3807261B1 (en) | 2018-06-18 | 2022-07-13 | Janssen Pharmaceutica NV | Pyridinyl pyrazoles as modulators of roryt |
| JP2021528398A (ja) | 2018-06-18 | 2021-10-21 | ヤンセン ファーマシューティカ エヌ．ベー． | ＲＯＲγＴのモジュレーターとしての６−アミノピリジン−３−イルピラゾール |
| ES2929140T3 (es) | 2018-06-18 | 2022-11-25 | Janssen Pharmaceutica Nv | Imidazoles sustituidos con fenilo y piridinilo como moduladores de RORgammat |
| JP2021528405A (ja) | 2018-06-18 | 2021-10-21 | ヤンセン ファーマシューティカ エヌ．ベー． | ＲＯＲγｔのモジュレータとしてのアミド置換チアゾール |
| CN111333636B (zh) * | 2020-04-10 | 2021-12-17 | 福建太平洋制药有限公司 | 噻唑酰胺类衍生物及其在抗肿瘤药物中的应用 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US69849A (en) * | 1867-10-15 | sheppaed | ||
| EP0959885A4 (en) * | 1996-11-20 | 2002-07-17 | Merck & Co Inc | TRIARYL SUBSTITUTED IMIDAZOLES AND METHODS OF USE |
| JP2001506997A (ja) * | 1996-12-16 | 2001-05-29 | オントジエン・コーポレイシヨン | ホスホチロシン認識ユニットを有する蛋白質の修飾物質 |
| ID22273A (id) * | 1997-01-28 | 1999-09-23 | Merck & Co Inc | TIAZOL BENZENASULFONAMIDA SEBAGAI AGONIS β UNTUK PENGOBATAN DIABETES DAN OBESITAS |
| FR2763337B1 (fr) * | 1997-05-13 | 1999-08-20 | Sanofi Sa | Nouveaux derives du triazole, un procede pour leur preparation et compositions pharmaceutiques les contenant |
| AU778393B2 (en) * | 1999-05-12 | 2004-12-02 | Ortho-Mcneil Pharmaceutical, Inc. | Pyrazole carboxamides useful for the treatment of obesity and other disorders |
| PE20011010A1 (es) * | 1999-12-02 | 2001-10-18 | Glaxo Group Ltd | Oxazoles y tiazoles sustituidos como agonista del receptor activado por el proliferador de peroxisomas humano |
-
2002
- 2002-10-15 JP JP2003539676A patent/JP2005507932A/ja not_active Withdrawn
- 2002-10-15 ES ES02782159T patent/ES2256560T3/es not_active Expired - Lifetime
- 2002-10-15 DE DE60208815T patent/DE60208815T2/de not_active Expired - Fee Related
- 2002-10-15 MX MXPA04002931A patent/MXPA04002931A/es active IP Right Grant
- 2002-10-15 US US10/490,826 patent/US20050014805A1/en not_active Abandoned
- 2002-10-15 WO PCT/US2002/032895 patent/WO2003037332A1/en not_active Ceased
- 2002-10-15 CA CA002463441A patent/CA2463441A1/en not_active Abandoned
- 2002-10-15 EP EP02782159A patent/EP1435951B1/en not_active Expired - Lifetime
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