JP2008513516A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2008513516A5 JP2008513516A5 JP2007532685A JP2007532685A JP2008513516A5 JP 2008513516 A5 JP2008513516 A5 JP 2008513516A5 JP 2007532685 A JP2007532685 A JP 2007532685A JP 2007532685 A JP2007532685 A JP 2007532685A JP 2008513516 A5 JP2008513516 A5 JP 2008513516A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- hydrogen
- independently
- heteroaryl
- group
- 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
- 229910052739 hydrogen Inorganic materials 0.000 claims 42
- 239000001257 hydrogen Substances 0.000 claims 42
- 125000000217 alkyl group Chemical group 0.000 claims 32
- 125000001072 heteroaryl group Chemical group 0.000 claims 28
- 125000003118 aryl group Chemical group 0.000 claims 22
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 21
- 125000000753 cycloalkyl group Chemical group 0.000 claims 20
- 150000002431 hydrogen Chemical class 0.000 claims 20
- 125000000623 heterocyclic group Chemical group 0.000 claims 19
- 125000003710 aryl alkyl group Chemical group 0.000 claims 16
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 16
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 16
- 150000001875 compounds Chemical class 0.000 claims 15
- 125000006710 (C2-C12) alkenyl group Chemical group 0.000 claims 11
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 11
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 11
- 125000005020 hydroxyalkenyl group Chemical group 0.000 claims 11
- 239000008194 pharmaceutical composition Substances 0.000 claims 11
- 125000004642 (C1-C12) alkoxy group Chemical group 0.000 claims 9
- 125000001309 chloro group Chemical group Cl* 0.000 claims 9
- 125000001153 fluoro group Chemical group F* 0.000 claims 9
- 125000003367 polycyclic group Chemical group 0.000 claims 8
- 201000010099 disease Diseases 0.000 claims 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 6
- 125000001188 haloalkyl group Chemical group 0.000 claims 5
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 5
- 239000000203 mixture Substances 0.000 claims 4
- 125000004043 oxo group Chemical group O=* 0.000 claims 4
- 239000000651 prodrug Substances 0.000 claims 4
- 229940002612 prodrug Drugs 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 101000631826 Homo sapiens Stearoyl-CoA desaturase Proteins 0.000 claims 3
- 102000055981 human SCD1 Human genes 0.000 claims 3
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 3
- 208000004930 Fatty Liver Diseases 0.000 claims 2
- 108010087894 Fatty acid desaturases Proteins 0.000 claims 2
- 206010019708 Hepatic steatosis Diseases 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- 102000016553 Stearoyl-CoA Desaturase Human genes 0.000 claims 2
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 2
- 208000010706 fatty liver disease Diseases 0.000 claims 2
- UMBGSUJPSPGPHI-UHFFFAOYSA-N n-hexyl-2-[4-[5-(hexylamino)-2-(trifluoromethyl)benzoyl]piperazin-1-yl]pyridine-4-carboxamide Chemical compound CCCCCCNC(=O)C1=CC=NC(N2CCN(CC2)C(=O)C=2C(=CC=C(NCCCCCC)C=2)C(F)(F)F)=C1 UMBGSUJPSPGPHI-UHFFFAOYSA-N 0.000 claims 2
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 2
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 231100000240 steatosis hepatitis Toxicity 0.000 claims 2
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims 1
- FOQJPBGZVXAKHY-UHFFFAOYSA-N 5-[4-[5-fluoro-2-(trifluoromethyl)benzoyl]piperazin-1-yl]-n-hexylpyridine-3-carboxamide Chemical compound CCCCCCNC(=O)C1=CN=CC(N2CCN(CC2)C(=O)C=2C(=CC=C(F)C=2)C(F)(F)F)=C1 FOQJPBGZVXAKHY-UHFFFAOYSA-N 0.000 claims 1
- RMERVNJHRNPULI-UHFFFAOYSA-N 5-[4-[5-fluoro-2-(trifluoromethyl)benzoyl]piperazin-1-yl]-n-pentylpyridine-3-carboxamide Chemical compound CCCCCNC(=O)C1=CN=CC(N2CCN(CC2)C(=O)C=2C(=CC=C(F)C=2)C(F)(F)F)=C1 RMERVNJHRNPULI-UHFFFAOYSA-N 0.000 claims 1
- 208000032928 Dyslipidaemia Diseases 0.000 claims 1
- 208000002705 Glucose Intolerance Diseases 0.000 claims 1
- 206010022489 Insulin Resistance Diseases 0.000 claims 1
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 125000005349 heteroarylcycloalkyl group Chemical group 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- URFPCEMFTXGVTB-UHFFFAOYSA-N n-(3-cyclopropylpropyl)-2-[4-[5-fluoro-2-(trifluoromethyl)benzoyl]piperazin-1-yl]pyridine-4-carboxamide Chemical compound FC1=CC=C(C(F)(F)F)C(C(=O)N2CCN(CC2)C=2N=CC=C(C=2)C(=O)NCCCC2CC2)=C1 URFPCEMFTXGVTB-UHFFFAOYSA-N 0.000 claims 1
- -1 nitro, hydroxy Chemical group 0.000 claims 1
- 201000009104 prediabetes syndrome Diseases 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US61164704P | 2004-09-20 | 2004-09-20 | |
| US60/611,647 | 2004-09-20 | ||
| PCT/US2005/034136 WO2006034446A2 (en) | 2004-09-20 | 2005-09-20 | Pyridine derivatives for inhibiting human stearoyl-coa-desaturase |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2008513516A JP2008513516A (ja) | 2008-05-01 |
| JP2008513516A5 true JP2008513516A5 (https=) | 2008-10-23 |
| JP4958787B2 JP4958787B2 (ja) | 2012-06-20 |
Family
ID=36035771
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007532685A Expired - Fee Related JP4958787B2 (ja) | 2004-09-20 | 2005-09-20 | ヒトステアロイル−CoAデサチュラーゼを阻害するためのピリジン誘導体 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US20080167321A1 (https=) |
| EP (2) | EP1827438B2 (https=) |
| JP (1) | JP4958787B2 (https=) |
| CN (1) | CN101090724A (https=) |
| AR (1) | AR051095A1 (https=) |
| AT (1) | ATE494895T1 (https=) |
| AU (1) | AU2005286653A1 (https=) |
| BR (1) | BRPI0515499A (https=) |
| CA (1) | CA2580860A1 (https=) |
| DE (1) | DE602005025924D1 (https=) |
| ES (1) | ES2359840T5 (https=) |
| MX (1) | MX2007003330A (https=) |
| TW (1) | TW200626153A (https=) |
| WO (1) | WO2006034446A2 (https=) |
Families Citing this family (80)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7517884B2 (en) | 1998-03-30 | 2009-04-14 | Kalypsys Inc. | Sulfonyl-substituted bicyclic compounds as modulators of PPAR |
| US20050119251A1 (en) * | 2001-12-21 | 2005-06-02 | Jian-Min Fu | Nicotinamide derivatives and their use as therapeutic agents |
| 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. |
| 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 |
| RS20060018A (sr) | 2003-07-14 | 2007-12-31 | Arena Pharmaceuticals Inc., | Derivati spojenih arila i heteroarila kao modulatori metabolizma u profilaksi i lečenju sa njima povezanih stanja |
| AU2005286647A1 (en) | 2004-09-20 | 2006-03-30 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors |
| AU2005286790A1 (en) | 2004-09-20 | 2006-03-30 | Xenon Pharmaceuticals Inc. | Bicyclic heterocyclic derivatives and their use as inhibitors of stearoyl-CoA-desaturase (SCD) |
| MX2007003318A (es) | 2004-09-20 | 2007-05-18 | Xenon Pharmaceuticals Inc | Derivados heterociclicos y su uso como agentes terapeuticos. |
| BRPI0515500A (pt) * | 2004-09-20 | 2008-07-29 | Xenon Pharmaceuticals Inc | derivados piridazina para inibição de estearoil-coa-desaturase |
| BRPI0515482A (pt) | 2004-09-20 | 2008-07-22 | Xenon Pharmaceuticals Inc | derivados heterocìclicos e seus usos como agentes terapêuticos |
| AU2005286728A1 (en) | 2004-09-20 | 2006-03-30 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives and their use as mediators of stearoyl-CoA desaturase |
| CN101084211A (zh) * | 2004-09-20 | 2007-12-05 | 泽农医药公司 | 杂环衍生物及其作为治疗剂的用途 |
| MX2007003332A (es) | 2004-09-20 | 2007-06-05 | Xenon Pharmaceuticals Inc | Derivados heterociclicos y su uso como inhibidores de estearoil-coa-desaturasa. |
| CA2585172C (en) | 2004-10-29 | 2014-08-12 | Kalypsys, Inc. | Sulfonyl-substituted bicyclic compounds as modulators of ppar |
| 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 |
| WO2007044085A2 (en) * | 2005-05-19 | 2007-04-19 | Xenon Pharmaceuticals Inc. | Heteroaryl compounds and their uses as therapeutic agents |
| CA2618646A1 (en) | 2005-06-03 | 2007-11-15 | Xenon Pharmaceuticals Inc. | Aminothiazole derivatives as human stearoyl-coa desaturase inhibitors |
| HUE040020T2 (hu) | 2005-10-25 | 2019-02-28 | Kalypsys Inc | PPAR modulátorok sói és eljárások metabolikus betegségek kezelésére |
| CN100463691C (zh) * | 2005-11-03 | 2009-02-25 | 贵州中际药业有限公司 | 一种止咳凝胶的制备方法 |
| WO2007092435A2 (en) | 2006-02-07 | 2007-08-16 | Wyeth | 11-beta hsd1 inhibitors |
| PE20080176A1 (es) | 2006-03-31 | 2008-04-25 | Glaxo Group Ltd | Compuestos de arilpiperazina sulfonamida como agonista de los receptores de secretagogos de la hormona de crecimiento (ghs) |
| WO2007143597A2 (en) | 2006-06-05 | 2007-12-13 | Novartis Ag | Organic compounds |
| MX2009002019A (es) | 2006-08-24 | 2009-03-09 | Novartis Ag | Derivados de 2-(pirazin-2-il)-tiazol y 2-(1h-pirazol-3-il)-tiazol asi como compuestos relacionados como inhibidores de la estearoil-coa-desaturasa (scd) para el tratamiento de trastornos metabolicos, cardiovasculares, y otros. |
| WO2008029266A1 (en) * | 2006-09-08 | 2008-03-13 | Glenmark Pharmaceuticals S.A. | Stearoyl coa desaturase inhibitors |
| DE102006042143A1 (de) * | 2006-09-08 | 2008-03-27 | Bayer Healthcare Aktiengesellschaft | Neue substituierte Bipyridin-Derivate und ihre Verwendung |
| DE102006044696A1 (de) | 2006-09-22 | 2008-03-27 | Bayer Healthcare Ag | 3-Cyano-5-thiazaheteroaryl-dihydropyridine und ihre Verwendung |
| DE102006056740A1 (de) | 2006-12-01 | 2008-06-05 | Bayer Healthcare Ag | Cyclisch substituierte 3,5-Dicyano-2-thiopyridine und ihre Verwendung |
| DE102006056739A1 (de) | 2006-12-01 | 2008-06-05 | Bayer Healthcare Ag | Substituierte 4-Amino-3,5-dicyano-2-thiopyridine und ihre Verwendung |
| KR101490723B1 (ko) | 2006-12-14 | 2015-02-06 | 신젠타 파티서페이션즈 아게 | 신규한 제초제로서의 4-페닐-피란-3,5-디온, 4-페닐-티오피란-3,5-디온 및 사이클로헥산트리온 |
| WO2008091863A1 (en) | 2007-01-23 | 2008-07-31 | Kalypsys, Inc. | Sulfonyl-substituted bicyclic compounds as ppar modulators for the treatment of non-alcoholic steatohepatitis |
| US8575167B2 (en) | 2007-02-06 | 2013-11-05 | Takeda Pharmaceutical Company Limited | Spiro compounds having stearoyl-CoA desaturase action |
| CL2008000467A1 (es) | 2007-02-14 | 2008-08-22 | Janssen Pharmaceutica Nv | Compuestos derivados de 2-aminopirimidina, moduladores del receptor histamina h4; su procedimiento de preparacion; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar un trastorno inflamatorio seleccionado de alegia, asma |
| CA2685266C (en) * | 2007-04-27 | 2014-01-28 | Purdue Pharma L.P. | Trpv1 antagonists and uses thereof for the treatment of prevention of pain, ui and ulcer, ibd, or ibs in an animal |
| GB0710223D0 (en) | 2007-05-29 | 2007-07-11 | Syngenta Ltd | Novel Herbicides |
| WO2008157844A1 (en) * | 2007-06-21 | 2008-12-24 | Forest Laboratories Holdings Limited | Novel piperazine derivatives as inhibitors of stearoyl-coa desaturase |
| GB0712653D0 (en) | 2007-06-28 | 2007-08-08 | Syngenta Ltd | Novel herbicides |
| DE102007035367A1 (de) | 2007-07-27 | 2009-01-29 | Bayer Healthcare Ag | Substituierte Aryloxazole und ihre Verwendung |
| DE102007036076A1 (de) | 2007-08-01 | 2009-02-05 | Bayer Healthcare Aktiengesellschaft | Dipeptoid-Produgs und ihre Verwendung |
| US8895761B2 (en) | 2007-12-13 | 2014-11-25 | Syngenta Limited | 4-phenylpyrane-3,5-diones, 4-phenylthiopyrane-3,5-diones and 2-phenylcyclohexane-1,3,5-triones as herbicides |
| DE102007061764A1 (de) * | 2007-12-20 | 2009-06-25 | Bayer Healthcare Ag | Anellierte Cyanopyridine und ihre Verwendung |
| DE102007061763A1 (de) * | 2007-12-20 | 2009-06-25 | Bayer Healthcare Ag | Substituierte azabicyclische Verbindungen und ihre Verwendung |
| DE102008013587A1 (de) * | 2008-03-11 | 2009-09-17 | Bayer Schering Pharma Aktiengesellschaft | Heteroaryl-substituierte Dicyanopyridine und ihre Verwendung |
| RU2010142937A (ru) * | 2008-03-20 | 2012-04-27 | Форест Лабораториес Холдингс Лимитед (Bm) | НОВЫЕ ПРОИЗВОДНЫЕ ПИПЕРИДИНА В КАЧЕСТВЕ ИНГИБИТОРОВ СТЕАРОИЛ-КоА ДЕСАТУРАЗЫ |
| WO2009143992A1 (de) * | 2008-05-29 | 2009-12-03 | Bayer Schering Pharma Aktiengesellschaft | 2-alkoxy-substituierte dicyanopyridine und ihre verwendung |
| US9187426B2 (en) * | 2008-06-27 | 2015-11-17 | Novartis Ag | Organic compounds |
| DE102008062567A1 (de) | 2008-12-16 | 2010-06-17 | Bayer Schering Pharma Aktiengesellschaft | Dipeptoid-Prodrugs und ihre Verwendung |
| US20100160323A1 (en) * | 2008-12-23 | 2010-06-24 | Alexander Bischoff | NOVEL PIPERAZINE DERIVATIVES AS INHIBITORS OF STEAROYL-CoA DESATURASE |
| GB0900641D0 (en) | 2009-01-15 | 2009-02-25 | Syngenta Ltd | Novel herbicides |
| GB0901086D0 (en) | 2009-01-22 | 2009-03-11 | Syngenta Ltd | Novel herbicides |
| DE102009006602A1 (de) * | 2009-01-29 | 2010-08-05 | Bayer Schering Pharma Aktiengesellschaft | Alkylamino-substituierte Dicyanopyridine und deren Aminosäureester-Prodrugs |
| GB0901834D0 (en) | 2009-02-04 | 2009-03-11 | Syngenta Ltd | Novel herbicides |
| GB0901835D0 (en) | 2009-02-04 | 2009-03-11 | Syngenta Ltd | Novel herbicides |
| EP2398809B1 (en) | 2009-02-17 | 2015-07-08 | Merck Canada Inc. | Novel spiro compounds useful as inhibitors of stearoyl-coenzyme a delta-9 desaturase |
| DE102009031058A1 (de) * | 2009-06-30 | 2011-01-27 | Clariant International Ltd. | Kontinuierliches Verfahren zur Herstellung von Amiden aromatischer Carbonsäuren |
| EP2459568A4 (en) | 2009-07-28 | 2013-02-27 | Merck Frosst Canada Ltd | NEW SPIRO COMPOUNDS AS AN INHIBITORS OF STEAROYL COENZYME A DELTA 9 DESATURASE |
| EP2475367A1 (en) | 2009-09-10 | 2012-07-18 | Centre National De La Recherche Scientifique | NOVEL INHIBITORS OF STEAROYL-CoA-DESATURASE-1 AND THEIR USES |
| WO2011103091A1 (en) | 2010-02-18 | 2011-08-25 | Transtech Pharma, Inc. | Phenyl-heteroaryl derivatives and methods of use thereof |
| DE102010030688A1 (de) | 2010-06-30 | 2012-01-05 | Bayer Schering Pharma Aktiengesellschaft | Substituierte Dicyanopyridine und ihre Verwendung |
| US20120058983A1 (en) | 2010-09-02 | 2012-03-08 | Bayer Pharma Aktiengesellschaft | Adenosine A1 agonists for the treatment of glaucoma and ocular hypertension |
| EP3323818A1 (en) | 2010-09-22 | 2018-05-23 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| JP5951625B2 (ja) | 2010-11-24 | 2016-07-13 | ザ・トラスティーズ・オブ・コランビア・ユニバーシティー・イン・ザ・シティー・オブ・ニューヨークThe Trustees Of Columbia University In The City Of New York | 加齢性黄斑変性症およびシュタルガルト病の処置のための非レチノイドrbp4アンタゴニスト |
| PE20141531A1 (es) | 2011-06-22 | 2014-10-23 | Purdue Pharma Lp | Antagonistas de trpv1 que incluyen sustituyentes dihidroxi y sus usos |
| US9358250B2 (en) | 2011-10-15 | 2016-06-07 | Genentech, Inc. | Methods of using SCD1 antagonists |
| US9333202B2 (en) | 2012-05-01 | 2016-05-10 | The Trustees Of Columbia University In The City Of New York | Non-retinoid antagonists for treatment of age-related macular degeneration and stargardt disease |
| MX2014014174A (es) | 2012-05-22 | 2015-07-06 | Hoffmann La Roche | Inhibidores selectivos de celulas no diferenciadas. |
| EP3495357B1 (en) | 2013-03-14 | 2021-05-05 | The Trustees of Columbia University in the City of New York | 4-phenylpiperidines, their preparation and use |
| US9944644B2 (en) | 2013-03-14 | 2018-04-17 | The Trustees Of Columbia University In The City Of New York | Octahydropyrrolopyrroles their preparation and use |
| US9938291B2 (en) | 2013-03-14 | 2018-04-10 | The Trustess Of Columbia University In The City Of New York | N-alkyl-2-phenoxyethanamines, their preparation and use |
| WO2014152018A1 (en) | 2013-03-14 | 2014-09-25 | The Trustees Of Columbia University In The City Of New York | Octahydrocyclopentapyrroles, their preparation and use |
| SG11201608943VA (en) | 2014-04-30 | 2016-11-29 | Univ Columbia | Substituted 4-phenylpiperidines, their preparaiton and use |
| PL3242666T3 (pl) | 2015-01-06 | 2025-02-17 | Arena Pharmaceuticals, Inc. | Związek do zastosowania w leczeniu dolegliwości związanych z receptorem s1p1 |
| BR112017027656B1 (pt) | 2015-06-22 | 2023-12-05 | Arena Pharmaceuticals, Inc. | Hábito cristalino de placa livre de sal de l-arginina de ácido (r)-2-(7-(4- ciclopentil-3-(trifluorometil)benzilóxi)- 1,2,3,4-tetra-hidrociclo-penta[b]indol-3- il)acético, composição farmacêutica que o compreende, seus usos e método de preparação do mesmo |
| JP2019533022A (ja) | 2016-10-24 | 2019-11-14 | ユマニティ セラピューティクス,インコーポレーテッド | 化合物及びその使用 |
| EP3566055B1 (en) | 2017-01-06 | 2025-03-12 | Janssen Pharmaceutica NV | Scd inhibitor for the treatment of neurological disorders |
| MX2019009841A (es) | 2017-02-16 | 2020-01-30 | Arena Pharm Inc | Compuestos y metodos para el tratamiento de la colangitis biliar primaria. |
| CA3083000A1 (en) | 2017-10-24 | 2019-05-02 | Yumanity Therapeutics, Inc. | Compounds and uses thereof |
| WO2019183587A1 (en) | 2018-03-23 | 2019-09-26 | Yumanity Therapeutics, Inc. | Compounds and uses thereof |
| CA3102136A1 (en) | 2018-06-06 | 2019-12-12 | Arena Pharmaceuticals, Inc. | Methods of treating conditions related to the s1p1 receptor |
| WO2020154571A1 (en) | 2019-01-24 | 2020-07-30 | Yumanity Therapeutics, Inc. | Compounds and uses thereof |
| EA202192047A1 (ru) | 2019-11-13 | 2021-12-08 | Юманити Терапьютикс, Инк. | Соединения и их применение |
Family Cites Families (109)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2985657A (en) * | 1959-10-12 | 1961-05-23 | Paul A J Janssen | 1-(aroylalkyl)-4-heterocyclylpiperazines |
| US3830924A (en) * | 1966-12-23 | 1974-08-20 | American Cyanamid Co | Substituted nitroimidazolyl-thiadiazoles as growth promoting agents |
| AT340933B (de) * | 1973-08-20 | 1978-01-10 | Thomae Gmbh Dr K | Verfahren zur herstellung neuer pyrimidinderivate und ihrer saureadditionssalze |
| US4247551A (en) * | 1979-09-17 | 1981-01-27 | Gruppo Lepetit S.P.A. | N-Pyrrolyl-pyridazineamines and their use as antihypertensive agents |
| FI70411C (fi) * | 1980-12-29 | 1986-09-19 | Pfizer | Foerfarande foer framstaellning av nya antihypertensiva 4-amino-6,7-dimetoxi-2-piperazinokinazolin derivat |
| US4439606A (en) * | 1982-05-06 | 1984-03-27 | American Cyanamid Company | Antiatherosclerotic 1-piperazinecarbonyl compounds |
| DE3827599A1 (de) * | 1988-08-13 | 1990-02-15 | Hoechst Ag | Verwendung von optisch aktiven tetrahydrofuran-2-carbonsaeureestern als dotierstoffe in fluessigkristallmischungen, diese enthaltende fluessigkristallmischungen und neue optisch aktive tetrahydrofuran-2-carbonsaeureester |
| US5166147A (en) * | 1990-07-09 | 1992-11-24 | The Du Pont Merck Pharmaceutical Company | 4-heteroaryl-and 4-aryl-1,4-dihydropyridine, derivatives with calcium agonist and alpha1 -antagonist activity |
| EP0471201A1 (de) * | 1990-07-21 | 1992-02-19 | Hoechst Aktiengesellschaft | Neue Oxazolidinon-Derivate und ihre Verwendung als Dotierstoffe in Flüssigkristallmischungen |
| EP0520292A1 (de) * | 1991-06-19 | 1992-12-30 | Hoechst Aktiengesellschaft | Chirale Azetidinon-Derivate und ihre Verwendung als Dotierstoffe in Flüssigkristallmischungen |
| DE4124942A1 (de) * | 1991-07-27 | 1993-01-28 | Thomae Gmbh Dr K | 5-gliedrige heterocyclen, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneimittel |
| JPH05345780A (ja) * | 1991-12-24 | 1993-12-27 | Kumiai Chem Ind Co Ltd | ピリミジンまたはトリアジン誘導体及び除草剤 |
| DE4236106A1 (de) * | 1992-10-26 | 1994-04-28 | Hoechst Ag | Azaaromatische Verbindungen, Verfahren zu ihrer Herstellung und ihre Verwendung in flüssigkristallinen Mischungen |
| US5494908A (en) * | 1992-11-23 | 1996-02-27 | Hoechst-Roussel Pharmaceutical Incorporated | Substituted 3-(aminoalkylamino)-1,2-benzisoxazoles and related compounds |
| BR9407799A (pt) | 1993-10-12 | 1997-05-06 | Du Pont Merck Pharma | Composição de matéria método de tratamento e composição farmaceutica |
| US5547605A (en) * | 1993-12-15 | 1996-08-20 | Hoechst Aktiengesellschaft | 2-Aryloxytetrafluoropropionic esters, process for their preparation, and their use in liquid-crystalline mixtures |
| US5637592A (en) * | 1994-07-12 | 1997-06-10 | Janssen Pharmaceutica N.V. | Acyl derivatives of azolones |
| US5571811A (en) * | 1994-07-12 | 1996-11-05 | Janssen Pharmaceutica N.V. | Sulfonamide derivatives of azolones |
| US5668148A (en) * | 1995-04-20 | 1997-09-16 | Merck & Co., Inc. | Alpha1a adrenergic receptor antagonists |
| DE19517051A1 (de) * | 1995-05-10 | 1996-11-14 | Hoechst Ag | 1-Fluor-6,7-dihydro-5H-isochinolin-8-on-Derivate und ihre Verwendung in flüssigkristallinen Mischungen |
| DE19517038A1 (de) * | 1995-05-10 | 1996-11-14 | Hoechst Ag | 1,8-Difluorisochinolinderivate und ihre Verwendung in flüssigkristallinen Mischungen |
| DE19517060A1 (de) * | 1995-05-10 | 1996-11-14 | Hoechst Ag | 1-Fluorisochinolinderivate und ihre Verwendung in flüssigkristallinen Mischungen |
| DE19517025A1 (de) * | 1995-05-10 | 1996-11-14 | Hoechst Ag | Trifluortetrahydroisochinolin-Derivate und ihre Verwendung in flüssigkristallinen Mischungen |
| DE19517056A1 (de) * | 1995-05-10 | 1996-11-14 | Hoechst Ag | 1-Fluor-5,6,7,8-tetrahydroisochinolin-Derivate und ihre Verwendung in flüssigkristallinen Mischungen |
| ZA969622B (en) * | 1995-12-13 | 1998-05-15 | Upjohn Co | Oxazolidinone antibacterial agents having a six-membered heteroaromatic ring. |
| MY117098A (en) * | 1996-01-15 | 2004-05-31 | Janssen Pharmaceutica Nv | Angiogenesis inhibiting pyridazinamines |
| DE19614204A1 (de) * | 1996-04-10 | 1997-10-16 | Thomae Gmbh Dr K | Carbonsäurederivate, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung |
| DE59707681D1 (de) * | 1996-10-28 | 2002-08-14 | Rolic Ag Zug | Vernetzbare, photoaktive Silanderivate |
| ZA98376B (en) * | 1997-01-23 | 1998-07-23 | Hoffmann La Roche | Sulfamide-metalloprotease inhibitors |
| ES2125206B1 (es) * | 1997-07-21 | 1999-11-16 | Esteve Labor Dr | Derivados de acil-piperazinil-pirimidinas, su preparacion y su aplicacion como medicamentos. |
| EE04588B1 (et) * | 1997-10-27 | 2006-02-15 | Neurosearch A/S | Heteroarüüldiasatsükloalkaanid kui atsetüülkoliini nikotiinretseptorite kolinergilised ligandid, nende kasutamine ravimitena ning neid sisaldav farmatseutiline kompositsioon |
| CN1329614A (zh) * | 1998-10-21 | 2002-01-02 | 武田药品工业株式会社 | 稠合的哒嗪衍生物、它们的制备方法和用途 |
| AU2319100A (en) | 1999-01-28 | 2000-08-18 | Nippon Shinyaku Co. Ltd. | Amide derivatives and drug compositions |
| CA2369103A1 (en) * | 1999-04-09 | 2000-10-19 | Meiji Seika Kaisha, Ltd. | Nitrogen-containing heterocyclic compounds and benamide compounds and drugs containing the same |
| FR2792314B1 (fr) * | 1999-04-15 | 2001-06-01 | Adir | Nouveaux composes aminotriazoles, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| DE19934799B4 (de) * | 1999-07-28 | 2008-01-24 | Az Electronic Materials (Germany) Gmbh | Chiral-smektische Flüssigkristallmischung und ihre Verwendung in Aktivmatrix-Displays mit hohen Kontrastwerten |
| US6127382A (en) * | 1999-08-16 | 2000-10-03 | Allergan Sales, Inc. | Amines substituted with a tetrahydroquinolinyl group an aryl or heteroaryl group and an alkyl group, having retinoid-like biological activity |
| US6677452B1 (en) * | 1999-09-30 | 2004-01-13 | Lion Bioscience Ag | Pyridine carboxamide or sulfonamide derivatives and combinatorial libraries thereof |
| HUP0204272A3 (en) | 2000-01-18 | 2005-03-29 | Pfizer Prod Inc | Corticotropin releasing factor antagonists, pharmaceutical compositions containing them and their use |
| WO2001054503A1 (en) | 2000-01-28 | 2001-08-02 | Akkadix Corporation | Methods for killing nematodes and nematode eggs using 4-phenoxy-6-aminopyrimidine derivatives |
| WO2001062954A2 (en) * | 2000-02-24 | 2001-08-30 | Xenon Genetics, Inc. | Stearoyl-coa desaturase to identify triglyceride reducing therapeutic agents |
| AU2001241128A1 (en) | 2000-03-14 | 2001-09-24 | Fujisawa Pharmaceutical Co. Ltd. | Novel amide compounds |
| US20020045613A1 (en) * | 2000-04-27 | 2002-04-18 | Heinz Pauls | 1-aroyl-piperidinyl benzamidines |
| GB0010757D0 (en) * | 2000-05-05 | 2000-06-28 | Astrazeneca Ab | Chemical compounds |
| GB0013383D0 (en) | 2000-06-01 | 2000-07-26 | Glaxo Group Ltd | Therapeutic benzamide derivatives |
| EP1301484A2 (en) * | 2000-07-20 | 2003-04-16 | Neurogen Corporation | Capsaicin receptor ligands |
| DE60130771T2 (de) * | 2000-07-27 | 2008-07-17 | Eli Lilly And Co., Indianapolis | Substituierte heterocyclische amide |
| EP1309594B1 (fr) * | 2000-08-08 | 2004-12-15 | Sanofi-Aventis | Derives de benzimidazole, leur preparation et leur application en therapeutique |
| ATE402262T1 (de) | 2000-09-26 | 2008-08-15 | Xenon Pharmaceuticals Inc | Verfahren und zusammensetzungen, die eine stearoyl-coa desuturase-hscd5 verwenden |
| US20020137755A1 (en) | 2000-12-04 | 2002-09-26 | Bilodeau Mark T. | Tyrosine kinase inhibitors |
| DE10060412A1 (de) * | 2000-12-05 | 2002-06-06 | Bayer Ag | DELTA1-Pyrroline |
| JP2004521892A (ja) | 2000-12-20 | 2004-07-22 | メルク エンド カムパニー インコーポレーテッド | (ハロ−ベンゾカルボニル)複素環縮合フェニル系p38キナーゼ阻害剤 |
| KR20030082990A (ko) * | 2001-03-15 | 2003-10-23 | 아스트라제네카 아베 | 메탈로프로테이나제 억제제 |
| FR2823209B1 (fr) * | 2001-04-04 | 2003-12-12 | Fournier Lab Sa | Nouvelles thiohydantoines et leur utilisation en therapeutique |
| US6911447B2 (en) * | 2001-04-25 | 2005-06-28 | The Procter & Gamble Company | Melanocortin receptor ligands |
| BR0209292B1 (pt) | 2001-04-30 | 2014-04-29 | Ciba Sc Holding Ag | Composto de complexo de metal, agente de lavagem, limpeza, desinfecção ou alvejamento, e preparação sólida |
| WO2002096867A2 (en) * | 2001-05-30 | 2002-12-05 | Lg Biomedical Institute | Inhibitors of protein kinase for the treatment of disease |
| DK1397351T3 (da) | 2001-06-01 | 2010-01-18 | Hoffmann La Roche | Pyrimidin-, triazin- og pyrazinderivater som glutamatreceptorer |
| DE60230266D1 (de) * | 2001-06-15 | 2009-01-22 | Astellas Pharma Inc | Phenylpyridincarbonyl piperazinderivate |
| US7115607B2 (en) * | 2001-07-25 | 2006-10-03 | Amgen Inc. | Substituted piperazinyl amides and methods of use |
| FR2829926B1 (fr) * | 2001-09-26 | 2004-10-01 | Oreal | Composition pour la teinture des fibres keratiniques comprenant un colorant diazoique dicationique particulier |
| US6916812B2 (en) * | 2001-10-09 | 2005-07-12 | Bristol-Myers Squibb Company | Alpha-aminoamide derivatives as melanocortin agonists |
| US6824707B2 (en) * | 2001-10-23 | 2004-11-30 | Clariant International Ltd. | Active matrix liquid crystal device and smectic liquid crystal mixture |
| EP1452525A4 (en) * | 2001-10-30 | 2005-01-26 | Nippon Shinyaku Co Ltd | AMIDE DERIVATIVES AND CORRESPONDING MEDICAMENTS |
| US6620811B2 (en) * | 2001-11-19 | 2003-09-16 | Hoffmann-La Roche Inc. | Isonicotin- and nicotinamide derivatives of benzothiazoles |
| CA2468159A1 (en) * | 2001-11-27 | 2003-06-05 | Merck & Co., Inc. | 4-aminoquinoline compounds |
| US20050038035A1 (en) | 2001-11-28 | 2005-02-17 | Hisashi Takasugi | Heterocyclic amide compounds as apolipoprotein b inhibitors |
| US20050119251A1 (en) * | 2001-12-21 | 2005-06-02 | Jian-Min Fu | Nicotinamide derivatives and their use as therapeutic agents |
| US7390813B1 (en) * | 2001-12-21 | 2008-06-24 | Xenon Pharmaceuticals Inc. | Pyridylpiperazines and aminonicotinamides and their use as therapeutic agents |
| US20030166932A1 (en) * | 2002-01-04 | 2003-09-04 | Beard Richard L. | Amines substituted with a dihydronaphthalenyl, chromenyl, or thiochromenyl group, an aryl or heteroaryl group and an alkyl group, having retinoid-like biological activity |
| JP4120586B2 (ja) * | 2002-01-18 | 2008-07-16 | アステラス製薬株式会社 | 2−アシルアミノチアゾール誘導体又はその塩 |
| EP1474401A2 (en) * | 2002-02-05 | 2004-11-10 | Novo Nordisk A/S | Novel aryl- and heteroarylpiperazines |
| MXPA04008797A (es) | 2002-03-13 | 2004-11-26 | Janssen Pharmaceutica Nv | Inhibidores de histona desacetilasa. |
| AU2003222786A1 (en) | 2002-04-18 | 2003-10-27 | Ucb, S.A. | Chemical compounds with dual activity, processes for their preparation and pharmaceutical compositions |
| EP1531822B1 (en) | 2002-06-12 | 2009-08-05 | ChemoCentryx Inc | 1-aryl-4-substituted piperazine derivatives for use as ccr1 antagonists for the treatment of inflammation and immune disorders |
| DE10226943A1 (de) | 2002-06-17 | 2004-01-08 | Bayer Ag | Phenylaminopyrimidine und ihre Verwendung |
| SE0201976D0 (sv) | 2002-06-24 | 2002-06-24 | Astrazeneca Ab | Novel compounds |
| JPWO2004011430A1 (ja) † | 2002-07-25 | 2005-11-24 | アステラス製薬株式会社 | ナトリウムチャネル阻害剤 |
| AR041191A1 (es) * | 2002-08-08 | 2005-05-04 | Amgen Inc | Ligandos del receptor vanilloide y su uso en tratamientos |
| US20040097492A1 (en) * | 2002-11-01 | 2004-05-20 | Pratt John K | Anti-infective agents |
| EP1571146A4 (en) | 2002-12-10 | 2010-09-01 | Ono Pharmaceutical Co | NITROGENIC HETEROCYCLIC COMPOUNDS AND THEIR MEDICAL USE |
| 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. |
| US6861422B2 (en) * | 2003-02-26 | 2005-03-01 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions |
| US20050014753A1 (en) | 2003-04-04 | 2005-01-20 | Irm Llc | Novel compounds and compositions as protein kinase inhibitors |
| PE20050226A1 (es) * | 2003-06-04 | 2005-05-18 | Aventis Pharma Sa | Productos aril-heteroaromaticos y composiciones que los contienen |
| FR2857966A1 (fr) * | 2003-07-24 | 2005-01-28 | Aventis Pharma Sa | Produits aryl-heteroaromatiques, compositions les contenant et utilisation |
| WO2005009976A1 (en) * | 2003-07-29 | 2005-02-03 | Novo Nordisk A/S | Pyridazinyl- piperazines and their use as histamine h3 receptor ligands |
| MXPA06001202A (es) * | 2003-07-29 | 2006-08-31 | Xenon Pharmaceuticals Inc | Derivados piridilo y su uso como agentes terapeuticos. |
| PL1648874T3 (pl) * | 2003-07-30 | 2012-04-30 | Xenon Pharmaceuticals Inc | Pochodne piperazyny i ich zastosowanie jako środków leczniczych |
| US7456180B2 (en) * | 2003-07-30 | 2008-11-25 | Xenon Pharmaceuticals Inc. | Piperazine derivatives and their use as therapeutic agents |
| US7754711B2 (en) * | 2003-07-30 | 2010-07-13 | Xenon Pharmaceuticals Inc. | Pyridazine derivatives and their use as therapeutic agents |
| CA2533900A1 (en) * | 2003-07-30 | 2005-02-10 | Xenon Pharmaceuticals Inc. | Pyridyl derivatives and their use as therapeutic agents |
| RS53252B (sr) * | 2003-08-11 | 2014-08-29 | F.Hoffmann-La Roche Ag. | Piperazin sa or-supstituisanom fenil grupom i njihova upotreba kao inhibitora glyt1 |
| KR101222364B1 (ko) | 2003-08-25 | 2013-01-15 | 트로비스 파마슈티칼스 엘엘씨 | 치환된 8-헤테로아릴 크산틴 |
| WO2005023261A1 (en) * | 2003-09-09 | 2005-03-17 | F. Hoffmann-La Roche Ag | 1-benzoyl-piperazine derivatives as glycine uptake inhibitors for the treatment of psychoses |
| US7399765B2 (en) * | 2003-09-19 | 2008-07-15 | Abbott Laboratories | Substituted diazabicycloalkane derivatives |
| US20050192286A1 (en) | 2003-10-22 | 2005-09-01 | Neurocrine Biosciences, Inc. | Ligands of melanocortin receptors and compositions and methods related thereto |
| US20050124660A1 (en) * | 2003-10-27 | 2005-06-09 | Jochen Antel | Novel medical uses of compounds showing CB1-antagonistic activity and combination treatment involving said compounds |
| US20050219211A1 (en) * | 2004-03-31 | 2005-10-06 | Kotzin Michael D | Method and apparatus for content management and control |
| US7345043B2 (en) * | 2004-04-01 | 2008-03-18 | Miikana Therapeutics | Inhibitors of histone deacetylase |
| AR048523A1 (es) * | 2004-04-07 | 2006-05-03 | Kalypsys Inc | Compuestos con estructura de aril sulfonamida y sulfonilo como moduladores de ppar y metodos para tratar trastornos metabolicos |
| AU2005286728A1 (en) * | 2004-09-20 | 2006-03-30 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives and their use as mediators of stearoyl-CoA desaturase |
| BRPI0515482A (pt) * | 2004-09-20 | 2008-07-22 | Xenon Pharmaceuticals Inc | derivados heterocìclicos e seus usos como agentes terapêuticos |
| CN101084211A (zh) * | 2004-09-20 | 2007-12-05 | 泽农医药公司 | 杂环衍生物及其作为治疗剂的用途 |
| MX2007003332A (es) * | 2004-09-20 | 2007-06-05 | Xenon Pharmaceuticals Inc | Derivados heterociclicos y su uso como inhibidores de estearoil-coa-desaturasa. |
| AU2005286647A1 (en) * | 2004-09-20 | 2006-03-30 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors |
| BRPI0515500A (pt) * | 2004-09-20 | 2008-07-29 | Xenon Pharmaceuticals Inc | derivados piridazina para inibição de estearoil-coa-desaturase |
| AU2005286790A1 (en) * | 2004-09-20 | 2006-03-30 | Xenon Pharmaceuticals Inc. | Bicyclic heterocyclic derivatives and their use as inhibitors of stearoyl-CoA-desaturase (SCD) |
| MX2007003318A (es) * | 2004-09-20 | 2007-05-18 | Xenon Pharmaceuticals Inc | Derivados heterociclicos y su uso como agentes terapeuticos. |
-
2005
- 2005-09-20 EP EP05810510.7A patent/EP1827438B2/en not_active Expired - Lifetime
- 2005-09-20 CA CA002580860A patent/CA2580860A1/en not_active Abandoned
- 2005-09-20 AT AT05810510T patent/ATE494895T1/de not_active IP Right Cessation
- 2005-09-20 TW TW094132565A patent/TW200626153A/zh unknown
- 2005-09-20 US US11/575,645 patent/US20080167321A1/en not_active Abandoned
- 2005-09-20 BR BRPI0515499-5A patent/BRPI0515499A/pt not_active IP Right Cessation
- 2005-09-20 AU AU2005286653A patent/AU2005286653A1/en not_active Abandoned
- 2005-09-20 EP EP10012999A patent/EP2316457A1/en not_active Withdrawn
- 2005-09-20 CN CNA2005800397373A patent/CN101090724A/zh active Pending
- 2005-09-20 DE DE602005025924T patent/DE602005025924D1/de not_active Expired - Lifetime
- 2005-09-20 MX MX2007003330A patent/MX2007003330A/es unknown
- 2005-09-20 AR ARP050103910A patent/AR051095A1/es unknown
- 2005-09-20 ES ES05810510.7T patent/ES2359840T5/es not_active Expired - Lifetime
- 2005-09-20 WO PCT/US2005/034136 patent/WO2006034446A2/en not_active Ceased
- 2005-09-20 JP JP2007532685A patent/JP4958787B2/ja not_active Expired - Fee Related
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2008513516A5 (https=) | ||
| JP2008513498A5 (https=) | ||
| JP2008513504A5 (https=) | ||
| JP2008513506A5 (https=) | ||
| JP2008513515A5 (https=) | ||
| JP2008513499A5 (https=) | ||
| JP5966014B2 (ja) | 新規トリフルオロメチル−オキサジアゾール誘導体および疾患の処置におけるその使用 | |
| JP2008513496A5 (https=) | ||
| CN105142635B (zh) | 有用于治疗疾病的杂环化合物 | |
| RU2006105717A (ru) | Производные пиперазина и их применение в качестве терапевтических агентов | |
| JP2007500720A5 (https=) | ||
| RS61064B1 (sr) | Modulatori proteina jezgra hepatitisa b | |
| JP2017533968A5 (https=) | ||
| JP2020502092A5 (https=) | ||
| JP2017524005A5 (https=) | ||
| JP2019532079A5 (https=) | ||
| CN1152870A (zh) | 杂环化合物作为多巴胺d3配位体的用途 | |
| JP2009533410A5 (https=) | ||
| JP2005526723A5 (https=) | ||
| PE20080360A1 (es) | Derivados 4-bencilftalazinona 2-sustituidos como antagonistas de histaminas h1 y h3 | |
| JPH11193281A (ja) | アデノシンa3受容体拮抗剤およびチアゾール化合物 | |
| RU2006134020A (ru) | Конденсированные производные пиразола | |
| TWI691475B (zh) | Urat1抑制劑 | |
| JP2011523945A5 (https=) | ||
| NO20091596L (no) | Benzoylamino-heterocykliske forbindelser som Glucokinase-(GLK)-activatorer |