JP2011529072A5 - - Google Patents
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- Publication number
- JP2011529072A5 JP2011529072A5 JP2011520189A JP2011520189A JP2011529072A5 JP 2011529072 A5 JP2011529072 A5 JP 2011529072A5 JP 2011520189 A JP2011520189 A JP 2011520189A JP 2011520189 A JP2011520189 A JP 2011520189A JP 2011529072 A5 JP2011529072 A5 JP 2011529072A5
- Authority
- JP
- Japan
- Prior art keywords
- alkylene
- alkyl
- cooh
- cycloalkyl
- nhc
- 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.)
- Pending
Links
- 125000000217 alkyl group Chemical group 0.000 claims description 169
- 125000002947 alkylene group Chemical group 0.000 claims description 111
- 150000001875 compounds Chemical class 0.000 claims description 65
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 58
- 125000005275 alkylenearyl group Chemical group 0.000 claims description 56
- 125000003118 aryl group Chemical group 0.000 claims description 27
- 125000005218 alkyleneheteroaryl group Chemical group 0.000 claims description 24
- 125000004299 tetrazol-5-yl group Chemical group [H]N1N=NC(*)=N1 0.000 claims description 19
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 14
- 125000005843 halogen group Chemical group 0.000 claims description 14
- 125000001153 fluoro group Chemical group F* 0.000 claims description 12
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims description 12
- 239000003814 drug Substances 0.000 claims description 10
- 125000000304 alkynyl group Chemical group 0.000 claims description 8
- 229910052799 carbon Inorganic materials 0.000 claims description 8
- 125000004432 carbon atom Chemical group C* 0.000 claims description 8
- -1 alkylene morpholine Chemical compound 0.000 claims description 7
- 125000003342 alkenyl group Chemical group 0.000 claims description 6
- 125000001072 heteroaryl group Chemical group 0.000 claims description 6
- 206010019280 Heart failures Diseases 0.000 claims description 4
- 206010020772 Hypertension Diseases 0.000 claims description 4
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 4
- 125000002993 cycloalkylene group Chemical group 0.000 claims description 4
- 239000002792 enkephalinase inhibitor Substances 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 4
- 125000004076 pyridyl group Chemical group 0.000 claims description 4
- 150000003839 salts Chemical class 0.000 claims description 4
- 125000001424 substituent group Chemical group 0.000 claims description 4
- 150000003852 triazoles Chemical class 0.000 claims description 4
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Natural products C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims description 3
- 239000002333 angiotensin II receptor antagonist Substances 0.000 claims description 3
- 238000004519 manufacturing process Methods 0.000 claims description 3
- 229940124597 therapeutic agent Drugs 0.000 claims description 3
- UUUHXMGGBIUAPW-UHFFFAOYSA-N 1-[1-[2-[[5-amino-2-[[1-[5-(diaminomethylideneamino)-2-[[1-[3-(1h-indol-3-yl)-2-[(5-oxopyrrolidine-2-carbonyl)amino]propanoyl]pyrrolidine-2-carbonyl]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoyl]amino]-3-methylpentanoyl]pyrrolidine-2-carbon Chemical compound C1CCC(C(=O)N2C(CCC2)C(O)=O)N1C(=O)C(C(C)CC)NC(=O)C(CCC(N)=O)NC(=O)C1CCCN1C(=O)C(CCCN=C(N)N)NC(=O)C1CCCN1C(=O)C(CC=1C2=CC=CC=C2NC=1)NC(=O)C1CCC(=O)N1 UUUHXMGGBIUAPW-UHFFFAOYSA-N 0.000 claims description 2
- 239000005541 ACE inhibitor Substances 0.000 claims description 2
- 108060003345 Adrenergic Receptor Proteins 0.000 claims description 2
- 102000017910 Adrenergic receptor Human genes 0.000 claims description 2
- 102000015427 Angiotensins Human genes 0.000 claims description 2
- 108010064733 Angiotensins Proteins 0.000 claims description 2
- 229940127291 Calcium channel antagonist Drugs 0.000 claims description 2
- 229940122783 Endothelin converting-enzyme inhibitor Drugs 0.000 claims description 2
- 229940118365 Endothelin receptor antagonist Drugs 0.000 claims description 2
- 102000004270 Peptidyl-Dipeptidase A Human genes 0.000 claims description 2
- 108090000882 Peptidyl-Dipeptidase A Proteins 0.000 claims description 2
- 239000002170 aldosterone antagonist Substances 0.000 claims description 2
- 229940083712 aldosterone antagonist Drugs 0.000 claims description 2
- 125000004419 alkynylene group Chemical group 0.000 claims description 2
- 150000001413 amino acids Chemical group 0.000 claims description 2
- 229940127003 anti-diabetic drug Drugs 0.000 claims description 2
- 230000003178 anti-diabetic effect Effects 0.000 claims description 2
- 239000003472 antidiabetic agent Substances 0.000 claims description 2
- 230000015572 biosynthetic process Effects 0.000 claims description 2
- 239000000480 calcium channel blocker Substances 0.000 claims description 2
- 238000006243 chemical reaction Methods 0.000 claims description 2
- 239000003795 chemical substances by application Substances 0.000 claims description 2
- KNHUKKLJHYUCFP-UHFFFAOYSA-N clofibrate Chemical compound CCOC(=O)C(C)(C)OC1=CC=C(Cl)C=C1 KNHUKKLJHYUCFP-UHFFFAOYSA-N 0.000 claims description 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 2
- 239000002934 diuretic Substances 0.000 claims description 2
- 229940030606 diuretics Drugs 0.000 claims description 2
- 229940079593 drug Drugs 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 239000002857 endothelin converting enzyme inhibitor Substances 0.000 claims description 2
- 239000002308 endothelin receptor antagonist Substances 0.000 claims description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 2
- 125000006289 hydroxybenzyl group Chemical group 0.000 claims description 2
- 125000000814 indol-3-yl group Chemical group [H]C1=C([H])C([H])=C2N([H])C([H])=C([*])C2=C1[H] 0.000 claims description 2
- 239000003112 inhibitor Substances 0.000 claims description 2
- 238000000034 method Methods 0.000 claims description 2
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims description 2
- 229940094443 oxytocics prostaglandins Drugs 0.000 claims description 2
- 125000006245 phosphate protecting group Chemical group 0.000 claims description 2
- 150000003180 prostaglandins Chemical class 0.000 claims description 2
- 239000002461 renin inhibitor Substances 0.000 claims description 2
- 229940086526 renin-inhibitors Drugs 0.000 claims description 2
- 125000000565 sulfonamide group Chemical group 0.000 claims description 2
- 238000003786 synthesis reaction Methods 0.000 claims description 2
- RWRDLPDLKQPQOW-UHFFFAOYSA-N tetrahydropyrrole Substances C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims description 2
- 125000003831 tetrazolyl group Chemical group 0.000 claims description 2
- 150000003573 thiols Chemical group 0.000 claims description 2
- 230000001732 thrombotic effect Effects 0.000 claims description 2
- 239000002536 vasopressin receptor antagonist Substances 0.000 claims description 2
- 0 CC(O1)=C(*)OC1=O Chemical compound CC(O1)=C(*)OC1=O 0.000 description 6
- 102000003729 Neprilysin Human genes 0.000 description 2
- 108090000028 Neprilysin Proteins 0.000 description 2
- USWHHEHQZJHOIJ-UHFFFAOYSA-N C=CC(N1)=NOC1=O Chemical compound C=CC(N1)=NOC1=O USWHHEHQZJHOIJ-UHFFFAOYSA-N 0.000 description 1
- CNCSLGBAVUHDCG-UHFFFAOYSA-N CC1=CCC(CCC2)C2C#C1 Chemical compound CC1=CCC(CCC2)C2C#C1 CNCSLGBAVUHDCG-UHFFFAOYSA-N 0.000 description 1
- ZBDCLLBKPFZSSM-UHFFFAOYSA-N CCC(C(C)=C=C)C(N1)=NOC1=O Chemical compound CCC(C(C)=C=C)C(N1)=NOC1=O ZBDCLLBKPFZSSM-UHFFFAOYSA-N 0.000 description 1
- XJVDIMLQFRPIMP-ZCFIWIBFSA-N C[C@H](c1c2cccc1)OC2=O Chemical compound C[C@H](c1c2cccc1)OC2=O XJVDIMLQFRPIMP-ZCFIWIBFSA-N 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 239000000400 angiotensin II type 1 receptor blocker Substances 0.000 description 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US13580608P | 2008-07-24 | 2008-07-24 | |
| US61/135,806 | 2008-07-24 | ||
| PCT/US2009/051507 WO2010011821A2 (en) | 2008-07-24 | 2009-07-23 | Dual-acting antihypertensive agents |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2011529072A JP2011529072A (ja) | 2011-12-01 |
| JP2011529072A5 true JP2011529072A5 (OSRAM) | 2012-06-28 |
Family
ID=41353864
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011520189A Pending JP2011529072A (ja) | 2008-07-24 | 2009-07-23 | 二重作用血圧降下薬 |
Country Status (4)
| Country | Link |
|---|---|
| US (4) | US7863309B2 (OSRAM) |
| EP (1) | EP2334651A2 (OSRAM) |
| JP (1) | JP2011529072A (OSRAM) |
| WO (1) | WO2010011821A2 (OSRAM) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW200838501A (en) | 2007-02-02 | 2008-10-01 | Theravance Inc | Dual-acting antihypertensive agents |
| TWI448284B (zh) | 2007-04-24 | 2014-08-11 | Theravance Inc | 雙效抗高血壓劑 |
| TWI406850B (zh) | 2007-06-05 | 2013-09-01 | Theravance Inc | 雙效苯并咪唑抗高血壓劑 |
| EP2200975A1 (en) | 2007-09-07 | 2010-06-30 | Theravance, Inc. | Dual-acting antihypertensive agents |
| EP2225210B1 (en) | 2007-12-11 | 2012-04-25 | Theravance, Inc. | Dual-acting benzoimidazole derivative and their use as antihypertensive agents |
| US7989484B2 (en) * | 2008-04-29 | 2011-08-02 | Theravance, Inc. | Dual-acting antihypertensive agents |
| WO2010011821A2 (en) * | 2008-07-24 | 2010-01-28 | Theravance, Inc. | Dual-acting antihypertensive agents |
| EP2435402B1 (en) | 2009-05-28 | 2016-04-13 | Novartis AG | Substituted aminobutyric derivatives as neprilysin inhibitors |
| BRPI1011657A2 (pt) | 2009-05-28 | 2019-04-16 | Novartis Ag | derivados aminopropiônicos substituídos como inibidores de neprilisina |
| EP2451782B1 (en) | 2009-07-07 | 2016-11-09 | Theravance Biopharma R&D IP, LLC | Dual-acting pyrazole antihypertensive agents |
| US8372984B2 (en) | 2009-07-22 | 2013-02-12 | Theravance, Inc. | Dual-acting oxazole antihypertensive agents |
| JO2967B1 (en) | 2009-11-20 | 2016-03-15 | نوفارتس ايه جي | Acetic acid derivatives of carbamoyl methyl amino are substituted as new NEP inhibitors |
| EP2526095A1 (en) | 2010-01-19 | 2012-11-28 | Theravance, Inc. | Dual-acting thiophene, pyrrole, thiazole and furan antihypertensive agents |
| EP3391890B1 (en) * | 2010-06-29 | 2021-08-25 | Merck Sharp & Dohme Corp. | Posaconazole intravenous solution formulations stabilized by substituted beta-cyclodextrin |
| BR112013018898B1 (pt) | 2011-01-27 | 2021-10-05 | Neuren Pharmaceuticals Limited | Uso de ácido glicil-l-2-metilprolil-l-glutâmico e análogos do mesmo para o tratamento de transtornos do espectro do autismo |
| US8686184B2 (en) * | 2011-05-31 | 2014-04-01 | Theravance, Inc. | Neprilysin inhibitors |
| EP2714660B1 (en) * | 2011-05-31 | 2018-09-26 | Theravance Biopharma R&D IP, LLC | Neprilysin inhibitors |
| WO2013014204A2 (en) | 2011-07-26 | 2013-01-31 | Sanofi | 3-heteroaroylamino-propionic acid derivatives and their use as pharmaceuticals |
| SG11201506018PA (en) | 2013-02-14 | 2015-08-28 | Novartis Ag | Substituted bisphenyl butanoic phosphonic acid derivatives as nep (neutral endopeptidase) inhibitors |
| KR20150119107A (ko) | 2013-02-14 | 2015-10-23 | 노파르티스 아게 | 개선된 생체내 효능을 갖는 nep 억제제로서의 치환된 비스페닐 부탄산 유도체 |
| TW201822637A (zh) | 2016-11-07 | 2018-07-01 | 德商拜耳廠股份有限公司 | 用於控制動物害蟲的經取代磺醯胺類 |
| TW202146416A (zh) | 2019-12-11 | 2021-12-16 | 德商拜耳廠股份有限公司 | 吡唑并三𠯤 |
| AU2021231312A1 (en) | 2020-03-06 | 2022-08-25 | Bayer Aktiengesellschaft | Imidazotriazines acting on cancer via inhibition of CDK12 |
| CN111978257A (zh) * | 2020-08-26 | 2020-11-24 | 武汉药明康德新药开发有限公司 | 含有醛基和羧基的1-甲基芳烃-1h-咪唑系列化合物的合成方法 |
| WO2022120442A1 (en) * | 2020-12-10 | 2022-06-16 | Aché Laboratórios Farmacêuticos S.A. | Codrugs of angiotensin ii type 1 receptor antagonists and neprilysin inhibitors |
| US20250066370A1 (en) | 2022-01-11 | 2025-02-27 | Deutsches Krebsforschungszentrum | Bicyclic triazine derivatives for the treatment of cancer |
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| DK113716B (da) * | 1960-07-30 | 1969-04-21 | Takeda Chemical Industries Ltd | Fremgangsmåde til fremstilling af 1-[pyrimidinyl-(2)]-guanazolforbindelser eller salte deraf. |
| FR2480747A1 (fr) | 1980-04-17 | 1981-10-23 | Roques Bernard | Derives d'acides amines et leur application therapeutique |
| US4610816A (en) | 1980-12-18 | 1986-09-09 | Schering Corporation | Substituted dipeptides as inhibitors of enkephalinases |
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| KR880007441A (ko) | 1986-12-11 | 1988-08-27 | 알렌 제이.스피겔 | 스피로-치환된 글루타르아미드 이뇨제 |
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| DE3928177A1 (de) | 1989-04-08 | 1991-02-28 | Thomae Gmbh Dr K | Benzimidazole, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung |
| ATE113281T1 (de) | 1989-08-02 | 1994-11-15 | Takeda Chemical Industries Ltd | Pyrazol-derivate, verfahren zu deren herstellung und anwendung. |
| CA2032289A1 (en) | 1989-12-29 | 1991-06-30 | Joseph A. Finkelstein | Substituted 5-(alkyl) carboxamide imidazoles |
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| JP4842463B2 (ja) | 2001-08-03 | 2011-12-21 | 株式会社ポーラファルマ | 新規ビフェニルウレイド誘導体及びこれを有効成分とする医薬 |
| US7468390B2 (en) | 2002-01-17 | 2008-12-23 | Novartis Ag | Methods of treatment and pharmaceutical composition |
| US20060046978A1 (en) | 2004-08-31 | 2006-03-02 | Morphochem Ag | Novel compounds that inhibit dipeptidyl peptidase (DPP-IV) and neprilysin (NEP) and/or angiotensin converting enzyme (ACE) |
| WO2006027680A1 (en) | 2004-09-10 | 2006-03-16 | Pfizer Limited | 3-(1-carbamoylcyclohexyl) propionic acid derivatives as inhibitors of neutral endopeptidase enzyme |
| MY146830A (en) | 2005-02-11 | 2012-09-28 | Novartis Ag | Combination of organic compounds |
| WO2007045663A2 (en) | 2005-10-19 | 2007-04-26 | Novartis Ag | Combination of an ati receptor antagonist and a np inhibitor fro treating ia hypertension and heartfailure |
| AR057882A1 (es) * | 2005-11-09 | 2007-12-26 | Novartis Ag | Compuestos de accion doble de bloqueadores del receptor de angiotensina e inhibidores de endopeptidasa neutra |
| WO2007106708A2 (en) | 2006-03-10 | 2007-09-20 | Novartis Ag | Combinations of the angiotensin ii antagonist valsartan and the nep inhibitor daglutril |
| WO2007109456A2 (en) | 2006-03-16 | 2007-09-27 | Pharmacopeia, Inc. | Substituted biphenyl isoxazole sulfonamides as dual angiotensin endothelin receptor antagonists |
| TW200838501A (en) | 2007-02-02 | 2008-10-01 | Theravance Inc | Dual-acting antihypertensive agents |
| TWI448284B (zh) * | 2007-04-24 | 2014-08-11 | Theravance Inc | 雙效抗高血壓劑 |
| WO2008142576A2 (en) | 2007-05-24 | 2008-11-27 | Eldrug S.A. | 1,(3,)5-substituted imidazoles, their use in the treatment of hypertension and methods for their preparation |
| TWI406850B (zh) | 2007-06-05 | 2013-09-01 | Theravance Inc | 雙效苯并咪唑抗高血壓劑 |
| EP2200975A1 (en) | 2007-09-07 | 2010-06-30 | Theravance, Inc. | Dual-acting antihypertensive agents |
| EP2225210B1 (en) | 2007-12-11 | 2012-04-25 | Theravance, Inc. | Dual-acting benzoimidazole derivative and their use as antihypertensive agents |
| US7989484B2 (en) | 2008-04-29 | 2011-08-02 | Theravance, Inc. | Dual-acting antihypertensive agents |
| TW201006832A (en) * | 2008-07-15 | 2010-02-16 | Novartis Ag | Organic compounds |
| WO2010011821A2 (en) * | 2008-07-24 | 2010-01-28 | Theravance, Inc. | Dual-acting antihypertensive agents |
| EP2451782B1 (en) | 2009-07-07 | 2016-11-09 | Theravance Biopharma R&D IP, LLC | Dual-acting pyrazole antihypertensive agents |
| US8372984B2 (en) | 2009-07-22 | 2013-02-12 | Theravance, Inc. | Dual-acting oxazole antihypertensive agents |
| EP2526095A1 (en) | 2010-01-19 | 2012-11-28 | Theravance, Inc. | Dual-acting thiophene, pyrrole, thiazole and furan antihypertensive agents |
-
2009
- 2009-07-23 WO PCT/US2009/051507 patent/WO2010011821A2/en not_active Ceased
- 2009-07-23 US US12/507,995 patent/US7863309B2/en not_active Expired - Fee Related
- 2009-07-23 EP EP09790756A patent/EP2334651A2/en not_active Withdrawn
- 2009-07-23 JP JP2011520189A patent/JP2011529072A/ja active Pending
-
2010
- 2010-11-18 US US12/949,114 patent/US8080572B2/en not_active Expired - Fee Related
-
2011
- 2011-11-17 US US13/298,493 patent/US8338418B2/en not_active Expired - Fee Related
-
2012
- 2012-11-20 US US13/682,005 patent/US8865755B2/en not_active Expired - Fee Related
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