JP2015505298A5 - - Google Patents
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- Publication number
- JP2015505298A5 JP2015505298A5 JP2014540076A JP2014540076A JP2015505298A5 JP 2015505298 A5 JP2015505298 A5 JP 2015505298A5 JP 2014540076 A JP2014540076 A JP 2014540076A JP 2014540076 A JP2014540076 A JP 2014540076A JP 2015505298 A5 JP2015505298 A5 JP 2015505298A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- alkylene
- chloro
- pharmaceutically acceptable
- fluoro
- 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
- 0 CCC(O1)=C(*)OC1=O Chemical compound CCC(O1)=C(*)OC1=O 0.000 description 4
- XJVDIMLQFRPIMP-UHFFFAOYSA-N CC(c1c2cccc1)OC2=O Chemical compound CC(c1c2cccc1)OC2=O XJVDIMLQFRPIMP-UHFFFAOYSA-N 0.000 description 1
- RFXBCGVZEJEYGG-UHFFFAOYSA-N Cc1ccc(CCC2)c2c1 Chemical compound Cc1ccc(CCC2)c2c1 RFXBCGVZEJEYGG-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161554625P | 2011-11-02 | 2011-11-02 | |
| US61/554,625 | 2011-11-02 | ||
| PCT/US2012/063036 WO2013067163A1 (en) | 2011-11-02 | 2012-11-01 | Neprilysin inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015505298A JP2015505298A (ja) | 2015-02-19 |
| JP2015505298A5 true JP2015505298A5 (https=) | 2015-11-12 |
| JP5944010B2 JP5944010B2 (ja) | 2016-07-05 |
Family
ID=47146772
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014540076A Expired - Fee Related JP5944010B2 (ja) | 2011-11-02 | 2012-11-01 | ネプリライシン阻害剤 |
Country Status (31)
| Country | Link |
|---|---|
| US (7) | US8691868B2 (https=) |
| EP (1) | EP2773335B1 (https=) |
| JP (1) | JP5944010B2 (https=) |
| KR (1) | KR102013200B1 (https=) |
| CN (1) | CN103906509B (https=) |
| AR (1) | AR088618A1 (https=) |
| AU (1) | AU2012332422B2 (https=) |
| BR (1) | BR112014010576B8 (https=) |
| CA (1) | CA2850953C (https=) |
| CO (1) | CO6940421A2 (https=) |
| CY (1) | CY1118909T1 (https=) |
| DK (1) | DK2773335T3 (https=) |
| ES (1) | ES2625628T3 (https=) |
| HR (1) | HRP20170646T1 (https=) |
| HU (1) | HUE034647T2 (https=) |
| IL (1) | IL232038A (https=) |
| LT (1) | LT2773335T (https=) |
| ME (1) | ME02726B (https=) |
| MX (1) | MX343753B (https=) |
| MY (1) | MY165087A (https=) |
| PH (1) | PH12014500987A1 (https=) |
| PL (1) | PL2773335T3 (https=) |
| PT (1) | PT2773335T (https=) |
| RS (1) | RS55947B1 (https=) |
| RU (1) | RU2629930C2 (https=) |
| SG (2) | SG11201401894XA (https=) |
| SI (1) | SI2773335T1 (https=) |
| SM (1) | SMT201700257T1 (https=) |
| TW (1) | TWI560172B (https=) |
| WO (1) | WO2013067163A1 (https=) |
| ZA (1) | ZA201402636B (https=) |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2548887T3 (es) | 2010-12-15 | 2015-10-21 | Theravance Biopharma R&D Ip, Llc | Inhibidores de neprilisina |
| US8586536B2 (en) | 2010-12-15 | 2013-11-19 | Theravance, Inc. | Neprilysin inhibitors |
| KR101854874B1 (ko) | 2011-02-17 | 2018-05-04 | 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 | 네프릴리신 억제제로서 치환된 아미노부티릭 유도체 |
| JP5959066B2 (ja) | 2011-02-17 | 2016-08-02 | セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー | ネプリライシン阻害剤としての置換アミノ酪酸誘導体 |
| ES2653215T3 (es) | 2011-05-31 | 2018-02-06 | Theravance Biopharma R&D Ip, Llc | Inhibidores de neprilisina |
| CN202237001U (zh) * | 2011-07-01 | 2012-05-30 | 龙泰兴业有限公司 | 具防护围网的跳床结构 |
| TWI560172B (en) | 2011-11-02 | 2016-12-01 | Theravance Biopharma R&D Ip Llc | Neprilysin inhibitors |
| US8905898B2 (en) * | 2012-03-09 | 2014-12-09 | Samuel Chen | Trampoline enclosure net |
| ES2609810T3 (es) * | 2012-05-31 | 2017-04-24 | Theravance Biopharma R&D Ip, Llc | Inhibidores de neprilisina donadores de óxido nítrico |
| MX356260B (es) | 2012-06-08 | 2018-05-21 | Theravance Biopharma R&D Ip Llc | Inhibidores de la neprilisina. |
| CN104470521B (zh) | 2012-06-08 | 2017-04-12 | 施万生物制药研发Ip有限责任公司 | 脑啡肽酶抑制剂 |
| MX366149B (es) | 2012-08-08 | 2019-06-28 | Theravance Biopharma R&D Ip Llc | Inhibidores de neprilisina. |
| CA2902456A1 (en) | 2013-03-05 | 2014-09-12 | Theravance Biopharma R&D Ip, Llc | Neprilysin inhibitors |
| WO2015116786A1 (en) * | 2014-01-30 | 2015-08-06 | Theravance Biopharma R&D Ip, Llc | Neprilysin inhibitors |
| US9585882B2 (en) | 2014-01-30 | 2017-03-07 | Theravance Biopharma R&D Ip, Llc | Neprilysin inhibitors |
| WO2015154673A1 (en) * | 2014-04-10 | 2015-10-15 | Zhaoyin Wang | Novel prodrugs and combinations for treatment of hypertension and cardiovascular diseases |
| CN106458857A (zh) * | 2014-08-27 | 2017-02-22 | 上海翰森生物医药科技有限公司 | AHU‑377结晶型游离酸、半钙盐、α﹣苯乙胺盐及其制备方法和应用 |
| WO2016086798A1 (zh) * | 2014-12-03 | 2016-06-09 | 上海翰森生物医药科技有限公司 | Nep抑制剂结晶型游离酸、钙盐多晶型及其制备方法和应用 |
| KR102640906B1 (ko) * | 2015-02-11 | 2024-02-27 | 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 | 네프릴리신 저해제로서 (2s,4r)-5-(5''-클로로-2''-플루오로비페닐-4-일)-4-(에톡시옥살릴아미노)-2-히드록시메틸-2-메틸펜타노익산 |
| CN107250119B (zh) | 2015-02-19 | 2020-09-22 | 施万生物制药研发Ip有限责任公司 | (2r,4r)-5-(5′-氯-2′-氟联苯-4-基)-2-羟基-4-[(5-甲基恶唑-2-羰基)氨基]戊酸 |
| CN105330569A (zh) * | 2015-09-11 | 2016-02-17 | 天台宜生生化科技有限公司 | 一种(r)-2-(n-叔丁氧羰基氨基)联苯丙醇的制备方法 |
| CN106310270A (zh) * | 2015-12-18 | 2017-01-11 | 深圳奥萨制药有限公司 | 血管紧张素转化酶抑制剂与脑啡肽酶抑制剂的药物组合物 |
| CN106310271A (zh) * | 2016-01-27 | 2017-01-11 | 深圳奥萨制药有限公司 | 一种治疗慢性心力衰竭的药物组合物 |
| CN109362222B (zh) * | 2016-02-05 | 2021-03-19 | 益方生物科技(上海)股份有限公司 | 选择性雌激素受体降解物及其用途 |
| SMT202100434T1 (it) | 2016-03-08 | 2021-09-14 | Theravance Biopharma R&D Ip Llc | Acido (2s,4r)-5-(5’-cloro-2-fluoro-[1,1’-bifenil]-4-il)-2-(etossimetil)-4-(3-idrossiisossazol-5-carbossammido)-2-metilpentanoico cristallino e suoi usi |
| UY38072A (es) | 2018-02-07 | 2019-10-01 | Novartis Ag | Compuestos derivados de éster butanoico sustituido con bisfenilo como inhibidores de nep, composiciones y combinaciones de los mismos |
| MX2020013785A (es) * | 2018-07-03 | 2021-03-25 | Jiangsu Hengrui Medicine Co | Derivado de la pirido-pirimidina, metodo de preparacion del mismo y uso medico del mismo. |
| US20230089867A1 (en) | 2018-11-27 | 2023-03-23 | Novartis Ag | Cyclic pentamer compounds as proprotein convertase subtilisin/kexin type 9 (pcsk9) inhibitors for the treatment of metabolic disorder |
| UY38485A (es) | 2018-11-27 | 2020-06-30 | Novartis Ag | Compuestos tetrámeros cíclicos como inhibidores de proproteína convertasa subtilisina/kexina tipo 9 (pcsk9), método de tratamiento, uso y su preparación |
| JP7657151B2 (ja) | 2018-11-27 | 2025-04-04 | ノバルティス アーゲー | 代謝性障害の処置のためのプロタンパク質コンバターゼスブチリシン／ケキシン９型（ｐｃｓｋ９）阻害剤としての環状ペプチド |
| CN112107568B (zh) * | 2019-06-19 | 2022-03-25 | 北京龙嘉博创医药科技有限公司 | 二芳基酰胺类化合物及其应用 |
| WO2022123592A1 (en) * | 2020-12-08 | 2022-06-16 | Alkem Laboratories Ltd | Stable pharmaceutical composition of azilsartan medoxomil or pharmaceutical acceptable salt and processes for preparing thereof |
| WO2023084449A1 (en) | 2021-11-12 | 2023-05-19 | Novartis Ag | Diaminocyclopentylpyridine derivatives for the treatment of a disease or disorder |
| CN115340472B (zh) * | 2022-09-19 | 2024-05-07 | 合肥工业大学 | 一种谷氨酸衍生物及其合成方法和应用 |
| CN119306633B (zh) * | 2024-09-24 | 2025-04-25 | 深圳市第二人民医院(深圳市转化医学研究院) | 一种β3-氨基酸衍生物的合成方法 |
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| US4189604A (en) | 1975-07-22 | 1980-02-19 | Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai | Bestatin |
| US4206232A (en) | 1976-05-10 | 1980-06-03 | E. R. Squibb & Sons, Inc. | Relieving hypertension with carboxyalkylacylamino acids |
| IL58849A (en) | 1978-12-11 | 1983-03-31 | Merck & Co Inc | Carboxyalkyl dipeptides and derivatives thereof,their preparation and pharmaceutical compositions containing them |
| FR2480747A1 (fr) | 1980-04-17 | 1981-10-23 | Roques Bernard | Derives d'acides amines et leur application therapeutique |
| US4906615A (en) | 1980-12-18 | 1990-03-06 | Schering Corporation | Substituted dipeptides as inhibitors of enkephalinases |
| US4722810A (en) | 1984-08-16 | 1988-02-02 | E. R. Squibb & Sons, Inc. | Enkephalinase inhibitors |
| US4939261A (en) | 1984-06-08 | 1990-07-03 | Ciba-Geigy Corporation | N-substituted butyramide derivatives useful for treatment of conditions responsive to inhibition of enkephalinase |
| EP0225292A3 (en) | 1985-12-06 | 1988-11-30 | Ciba-Geigy Ag | Certain n-substituted butyramide derivatives |
| US4929641B1 (en) | 1988-05-11 | 1994-08-30 | Schering Corp | Mercapto-acylamino acid antihypertensives |
| KR880007441A (ko) | 1986-12-11 | 1988-08-27 | 알렌 제이.스피겔 | 스피로-치환된 글루타르아미드 이뇨제 |
| FR2623498B1 (fr) | 1987-11-24 | 1990-04-06 | Bioprojet Soc Civ | Nouveaux composes enantiomeres derives d'amino-acides, leur procede de preparation et leurs applications therapeutiques |
| GB8820844D0 (en) | 1988-09-05 | 1988-10-05 | Pfizer Ltd | Therapeutic agents |
| US5599951A (en) | 1989-09-15 | 1997-02-04 | Societe Civile Bioprojet | Amino acid derivatives, the process for their preparation and their applications to therapy |
| US5294632A (en) | 1991-05-01 | 1994-03-15 | Ciba-Geigy Corporation | Phosphono/biaryl substituted dipetide derivatives |
| US5155100A (en) | 1991-05-01 | 1992-10-13 | Ciba-Geigy Corporation | Phosphono/biaryl substituted dipeptide derivatives |
| US5217996A (en) | 1992-01-22 | 1993-06-08 | Ciba-Geigy Corporation | Biaryl substituted 4-amino-butyric acid amides |
| US5508272A (en) | 1993-06-15 | 1996-04-16 | Bristol-Myers Squibb Company | Compounds containing a fused bicycle ring and processes therefor |
| DE19510566A1 (de) | 1995-03-23 | 1996-09-26 | Kali Chemie Pharma Gmbh | Benzazepin-, Benzoxazepin- und Benzothiazepin-N-essigsäurederivate sowie Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel |
| AU5687396A (en) | 1995-04-21 | 1996-11-07 | Novarits Ag | N-aroylamino acid amides as endothelin inhibitors |
| US6660756B2 (en) | 2001-03-28 | 2003-12-09 | Pfizer Inc. | N-phenpropylcyclopentyl-substituted glutaramide derivatives as inhibitors of neutral endopeptidase |
| GB0119305D0 (en) | 2001-04-12 | 2001-10-03 | Aventis Pharma Gmbh | Mercaptoacetylamide derivatives,a process for their preparation and their use |
| WO2006027680A1 (en) | 2004-09-10 | 2006-03-16 | Pfizer Limited | 3-(1-carbamoylcyclohexyl) propionic acid derivatives as inhibitors of neutral endopeptidase enzyme |
| 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 |
| KR101580067B1 (ko) * | 2007-01-12 | 2015-12-23 | 노파르티스 아게 | 5-바이페닐-4-아미노-2-메틸 펜탄산의 제조 방법 |
| TWI448284B (zh) | 2007-04-24 | 2014-08-11 | Theravance Inc | 雙效抗高血壓劑 |
| PE20091364A1 (es) | 2008-01-17 | 2009-10-13 | Novartis Ag | Proceso para la preparacion de inhibidores de nep |
| US20100247606A1 (en) * | 2009-03-25 | 2010-09-30 | Allergan, Inc. | Intraocular sustained release drug delivery systems and methods for treating ocular conditions |
| EP2435402B1 (en) * | 2009-05-28 | 2016-04-13 | Novartis AG | Substituted aminobutyric derivatives as neprilysin inhibitors |
| CN103896796B (zh) * | 2009-05-28 | 2016-04-27 | 诺华股份有限公司 | 作为脑啡肽酶抑制剂的取代的氨基丙酸衍生物 |
| JO2967B1 (en) | 2009-11-20 | 2016-03-15 | نوفارتس ايه جي | Acetic acid derivatives of carbamoyl methyl amino are substituted as new NEP inhibitors |
| KR101463670B1 (ko) | 2010-01-22 | 2014-11-19 | 노파르티스 아게 | 중성 엔도펩티다제 억제제의 중간체 및 그의 제조 방법 |
| US8673974B2 (en) | 2010-11-16 | 2014-03-18 | Novartis Ag | Substituted amino bisphenyl pentanoic acid derivatives as NEP inhibitors |
| US8993631B2 (en) | 2010-11-16 | 2015-03-31 | Novartis Ag | Method of treating contrast-induced nephropathy |
| US8586536B2 (en) * | 2010-12-15 | 2013-11-19 | Theravance, Inc. | Neprilysin inhibitors |
| ES2548887T3 (es) | 2010-12-15 | 2015-10-21 | Theravance Biopharma R&D Ip, Llc | Inhibidores de neprilisina |
| KR101854874B1 (ko) * | 2011-02-17 | 2018-05-04 | 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 | 네프릴리신 억제제로서 치환된 아미노부티릭 유도체 |
| JP5959066B2 (ja) | 2011-02-17 | 2016-08-02 | セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー | ネプリライシン阻害剤としての置換アミノ酪酸誘導体 |
| ES2653215T3 (es) | 2011-05-31 | 2018-02-06 | Theravance Biopharma R&D Ip, Llc | Inhibidores de neprilisina |
| WO2012166389A1 (en) | 2011-05-31 | 2012-12-06 | Theravance, Inc. | Neprilysin inhibitors |
| JP5959075B2 (ja) | 2011-05-31 | 2016-08-02 | セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー | ネプリライシン阻害剤 |
| TWI560172B (en) | 2011-11-02 | 2016-12-01 | Theravance Biopharma R&D Ip Llc | Neprilysin inhibitors |
| ES2609810T3 (es) | 2012-05-31 | 2017-04-24 | Theravance Biopharma R&D Ip, Llc | Inhibidores de neprilisina donadores de óxido nítrico |
| MX356260B (es) | 2012-06-08 | 2018-05-21 | Theravance Biopharma R&D Ip Llc | Inhibidores de la neprilisina. |
| CN104470521B (zh) | 2012-06-08 | 2017-04-12 | 施万生物制药研发Ip有限责任公司 | 脑啡肽酶抑制剂 |
| MX366149B (es) | 2012-08-08 | 2019-06-28 | Theravance Biopharma R&D Ip Llc | Inhibidores de neprilisina. |
-
2012
- 2012-10-18 TW TW101138516A patent/TWI560172B/zh not_active IP Right Cessation
- 2012-11-01 ES ES12783830.8T patent/ES2625628T3/es active Active
- 2012-11-01 US US13/666,538 patent/US8691868B2/en active Active
- 2012-11-01 CA CA2850953A patent/CA2850953C/en active Active
- 2012-11-01 ME MEP-2017-100A patent/ME02726B/me unknown
- 2012-11-01 CN CN201280053488.3A patent/CN103906509B/zh not_active Expired - Fee Related
- 2012-11-01 RS RS20170428A patent/RS55947B1/sr unknown
- 2012-11-01 WO PCT/US2012/063036 patent/WO2013067163A1/en not_active Ceased
- 2012-11-01 SM SM20170257T patent/SMT201700257T1/it unknown
- 2012-11-01 AR ARP120104101A patent/AR088618A1/es active IP Right Grant
- 2012-11-01 RU RU2014122109A patent/RU2629930C2/ru active
- 2012-11-01 DK DK12783830.8T patent/DK2773335T3/en active
- 2012-11-01 SG SG11201401894XA patent/SG11201401894XA/en unknown
- 2012-11-01 HR HRP20170646TT patent/HRP20170646T1/hr unknown
- 2012-11-01 HU HUE12783830A patent/HUE034647T2/hu unknown
- 2012-11-01 SG SG10201509182YA patent/SG10201509182YA/en unknown
- 2012-11-01 MY MYPI2014000853A patent/MY165087A/en unknown
- 2012-11-01 LT LTEP12783830.8T patent/LT2773335T/lt unknown
- 2012-11-01 SI SI201230972A patent/SI2773335T1/sl unknown
- 2012-11-01 AU AU2012332422A patent/AU2012332422B2/en not_active Ceased
- 2012-11-01 KR KR1020147014997A patent/KR102013200B1/ko active Active
- 2012-11-01 EP EP12783830.8A patent/EP2773335B1/en active Active
- 2012-11-01 PT PT127838308T patent/PT2773335T/pt unknown
- 2012-11-01 PH PH1/2014/500987A patent/PH12014500987A1/en unknown
- 2012-11-01 JP JP2014540076A patent/JP5944010B2/ja not_active Expired - Fee Related
- 2012-11-01 PL PL12783830T patent/PL2773335T3/pl unknown
- 2012-11-01 BR BR112014010576A patent/BR112014010576B8/pt not_active IP Right Cessation
- 2012-11-01 MX MX2014005339A patent/MX343753B/es active IP Right Grant
-
2014
- 2014-02-14 US US14/180,479 patent/US9150500B2/en active Active
- 2014-04-09 IL IL232038A patent/IL232038A/en active IP Right Grant
- 2014-04-10 ZA ZA2014/02636A patent/ZA201402636B/en unknown
- 2014-04-23 CO CO14086639A patent/CO6940421A2/es active IP Right Grant
-
2015
- 2015-08-28 US US14/838,842 patent/US9682052B2/en not_active Expired - Fee Related
-
2017
- 2017-05-12 US US15/593,833 patent/US10123984B2/en active Active
- 2017-05-26 CY CY20171100548T patent/CY1118909T1/el unknown
-
2018
- 2018-10-05 US US16/153,299 patent/US10744104B2/en active Active
-
2020
- 2020-07-08 US US16/923,396 patent/US11547687B2/en active Active
-
2022
- 2022-11-18 US US17/990,329 patent/US12016835B2/en active Active
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