JP2014503534A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2014503534A5 JP2014503534A5 JP2013544730A JP2013544730A JP2014503534A5 JP 2014503534 A5 JP2014503534 A5 JP 2014503534A5 JP 2013544730 A JP2013544730 A JP 2013544730A JP 2013544730 A JP2013544730 A JP 2013544730A JP 2014503534 A5 JP2014503534 A5 JP 2014503534A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- alkylene
- halo
- phenyl
- och
- 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 CNCC(O1)=C(*)OC1=O Chemical compound CNCC(O1)=C(*)OC1=O 0.000 description 4
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US42318010P | 2010-12-15 | 2010-12-15 | |
| US61/423,180 | 2010-12-15 | ||
| PCT/US2011/064829 WO2012082853A1 (en) | 2010-12-15 | 2011-12-14 | Neprilysin inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015186389A Division JP2016028089A (ja) | 2010-12-15 | 2015-09-24 | ネプリライシン阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014503534A JP2014503534A (ja) | 2014-02-13 |
| JP2014503534A5 true JP2014503534A5 (enExample) | 2014-11-20 |
| JP5944921B2 JP5944921B2 (ja) | 2016-07-05 |
Family
ID=45478501
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013544730A Expired - Fee Related JP5944921B2 (ja) | 2010-12-15 | 2011-12-14 | ネプリライシン阻害剤 |
| JP2015186389A Withdrawn JP2016028089A (ja) | 2010-12-15 | 2015-09-24 | ネプリライシン阻害剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015186389A Withdrawn JP2016028089A (ja) | 2010-12-15 | 2015-09-24 | ネプリライシン阻害剤 |
Country Status (28)
| Country | Link |
|---|---|
| US (9) | US8586536B2 (enExample) |
| EP (1) | EP2651896B1 (enExample) |
| JP (2) | JP5944921B2 (enExample) |
| KR (1) | KR101892500B1 (enExample) |
| CN (2) | CN103261164B (enExample) |
| AU (1) | AU2011343899B2 (enExample) |
| BR (1) | BR112013016595B1 (enExample) |
| CA (1) | CA2817368C (enExample) |
| CO (1) | CO6741228A2 (enExample) |
| DK (1) | DK2651896T3 (enExample) |
| ES (1) | ES2550324T3 (enExample) |
| HR (1) | HRP20151115T1 (enExample) |
| HU (1) | HUE028051T2 (enExample) |
| IL (1) | IL226327A (enExample) |
| ME (1) | ME02295B (enExample) |
| MX (1) | MX2013006805A (enExample) |
| MY (1) | MY170935A (enExample) |
| NZ (1) | NZ610983A (enExample) |
| PH (1) | PH12013501240A1 (enExample) |
| PL (1) | PL2651896T3 (enExample) |
| PT (1) | PT2651896E (enExample) |
| RS (1) | RS54348B1 (enExample) |
| RU (1) | RU2622288C2 (enExample) |
| SG (2) | SG190432A1 (enExample) |
| SI (1) | SI2651896T1 (enExample) |
| SM (1) | SMT201500271B (enExample) |
| WO (1) | WO2012082853A1 (enExample) |
| ZA (1) | ZA201304205B (enExample) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2763565A1 (en) | 2009-05-28 | 2010-12-02 | Novartis Ag | Substituted aminobutyric derivatives as neprilysin inhibitors |
| SI2651896T1 (sl) | 2010-12-15 | 2015-11-30 | Theravance Biopharma R&D Ip, Llc | Inhibitorji neprilizina |
| CN103261168B (zh) | 2010-12-15 | 2015-08-05 | 施万生物制药研发Ip有限责任公司 | 脑啡肽酶抑制剂 |
| AU2012217615B2 (en) | 2011-02-17 | 2016-09-29 | Theravance Biopharma R&D Ip, Llc | Substituted aminobutyric derivatives as neprilysin inhibitors |
| US8449890B2 (en) * | 2011-02-17 | 2013-05-28 | Theravance, Inc. | Neprilysin inhibitors |
| ES2653215T3 (es) | 2011-05-31 | 2018-02-06 | Theravance Biopharma R&D Ip, Llc | Inhibidores de neprilisina |
| ES2699773T3 (es) | 2011-05-31 | 2019-02-12 | Theravance Biopharma R&D Ip Llc | Inhibidores de neprilisina |
| WO2013059215A1 (en) * | 2011-10-17 | 2013-04-25 | Biotheryx, Inc. | Substituted biaryl alkyl amides |
| TWI560172B (en) | 2011-11-02 | 2016-12-01 | Theravance Biopharma R&D Ip Llc | Neprilysin inhibitors |
| CA2871292A1 (en) | 2012-05-31 | 2013-12-05 | Theravance Biopharma R&D Ip, Llc | Nitric oxide donor neprilysin inhibitors |
| LT2864292T (lt) | 2012-06-08 | 2017-07-10 | Theravance Biopharma R&D Ip, Llc | Neprilizino inhibitoriai |
| ES2710932T3 (es) | 2012-06-08 | 2019-04-29 | Theravance Biopharma R&D Ip Llc | Inhibidores de neprilisina |
| US9126956B2 (en) | 2012-08-08 | 2015-09-08 | Theravance Biopharma R&D Ip, Llc | Neprilysin inhibitors |
| US8796305B2 (en) * | 2012-11-05 | 2014-08-05 | Bayer Pharma Aktiengesellschaft | Carboxy-substituted imidazo[1,2-a]pyridinecarboxamides and their use |
| WO2014126972A1 (en) | 2013-02-14 | 2014-08-21 | Novartis Ag | Substituted bisphenyl butanoic acid derivatives as nep inhibitors with improved in vivo efficacy |
| SG11201506018PA (en) | 2013-02-14 | 2015-08-28 | Novartis Ag | Substituted bisphenyl butanoic phosphonic acid derivatives as nep (neutral endopeptidase) inhibitors |
| HUE034210T2 (hu) * | 2013-03-05 | 2018-02-28 | Theravance Biopharma R&D Ip Llc | Neprilizininhibitorok |
| MX2016009760A (es) | 2014-01-30 | 2016-11-08 | Theravance Biopharma R&D Ip Llc | Inhibidores de neprilisina. |
| EP3099668B1 (en) | 2014-01-30 | 2022-05-04 | Theravance Biopharma R&D IP, LLC | 5-biphenyl-4-heteroarylcarbonylamino-pentanoic acid derivatives as neprilysin inhibitors |
| MX385777B (es) * | 2014-12-24 | 2025-03-04 | Lg Chemical Ltd | Derivado de biarilo como agonista de gpr120. |
| WO2016130650A1 (en) | 2015-02-11 | 2016-08-18 | Theravance Biopharma R&D Ip, Llc | (2s, 4r)-5-(5'-chloro-2'-fluorobiphenyl-4-yl)-2-ethoxyoxalylamino)-2-hydroxymethyl-2-methylpentanoic acid as neprilysin inhibitor |
| RU2715241C2 (ru) | 2015-02-19 | 2020-02-26 | ТЕРЕВАНС БАЙОФАРМА Ар энд Ди АйПи, ЭлЭлСи | (2r,4r)-5-(5′-хлор-2′-фторбифенил-4-ил)-2-гидрокси-4-[(5-метилоксазол-2-карбонил)амино]пентановая кислота |
| TWI731943B (zh) | 2016-03-08 | 2021-07-01 | 美商施萬生物製藥研發Ｉｐ有限責任公司 | 結晶型（2s，4r）－5－（5’－氯－2’－氟－［1，1’－聯苯］－4－基）－2－（乙氧基甲基）－4－（3－羥基異㗁唑－5－甲醯胺基）－2－甲基戊酸及其用途 |
| 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 |
| 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 |
| WO2020110008A1 (en) | 2018-11-27 | 2020-06-04 | Novartis Ag | Cyclic pentamer compounds as proprotein convertase subtilisin/kexin type 9 (pcsk9) inhibitors for the treatment of metabolic disorder |
| 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 |
| CN112592294B (zh) * | 2020-12-22 | 2022-05-13 | 江苏阿尔法药业股份有限公司 | 一种沙库巴曲药物中间体的合成方法 |
| WO2023084449A1 (en) | 2021-11-12 | 2023-05-19 | Novartis Ag | Diaminocyclopentylpyridine derivatives for the treatment of a disease or disorder |
| 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 |
Family Cites Families (52)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| GB2090595B (en) * | 1978-11-25 | 1983-05-11 | Nippon Kayaku Kk | Threo-3-amino-2-hydroxybutanoylacetice acid derivatives |
| IL58849A (en) | 1978-12-11 | 1983-03-31 | Merck & Co Inc | Carboxyalkyl dipeptides and derivatives thereof,their preparation and pharmaceutical compositions containing them |
| JPS5615257A (en) | 1979-07-17 | 1981-02-14 | Nippon Hidorajin Kogyo Kk | Preparation of methylhydrazine |
| 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 |
| CN1008092B (zh) * | 1983-10-03 | 1990-05-23 | E·R·斯奎布父子公司 | 脑啡肽酶抑制剂的制备方法 |
| 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 |
| CA2058797A1 (en) * | 1991-02-01 | 1992-08-02 | Michael John Broadhurst | Amino acid derivatives |
| US5155100A (en) | 1991-05-01 | 1992-10-13 | Ciba-Geigy Corporation | Phosphono/biaryl substituted dipeptide derivatives |
| US5294632A (en) | 1991-05-01 | 1994-03-15 | Ciba-Geigy Corporation | Phosphono/biaryl substituted dipetide 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 |
| BR0314898A (pt) * | 2002-11-19 | 2005-08-02 | Galderma Res & Dev | Compostos, composição cosmética, uso cosmético de uma composição, uso de um composto e composição farmacêutica |
| CN1566065A (zh) * | 2003-06-27 | 2005-01-19 | 中国医学科学院药物研究所 | α位杂原子取代的γ芳基丁本酮酸衍生物及其制法和其药物组合物与用途 |
| WO2006027680A1 (en) | 2004-09-10 | 2006-03-16 | Pfizer Limited | 3-(1-carbamoylcyclohexyl) propionic acid derivatives as inhibitors of neutral endopeptidase enzyme |
| KR20070110847A (ko) * | 2005-02-10 | 2007-11-20 | 메디비르 아베 | Ｈｉｖ 프로테아제 억제제 |
| 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 |
| ES2602566T3 (es) * | 2007-01-12 | 2017-02-21 | Novartis Ag | Proceso para preparar ácido 5-bifenil-4-amino-2-metil pentanoico |
| TWI448284B (zh) | 2007-04-24 | 2014-08-11 | Theravance Inc | 雙效抗高血壓劑 |
| AR070176A1 (es) | 2008-01-17 | 2010-03-17 | Novartis Ag | Procesos de sintesis de inhibidores de nep, compuestos intermediarios y uso de los mismos en la sintesis |
| CA2763565A1 (en) | 2009-05-28 | 2010-12-02 | Novartis Ag | Substituted aminobutyric derivatives as neprilysin inhibitors |
| PL2435409T3 (pl) | 2009-05-28 | 2015-01-30 | Novartis Ag | Podstawione pochodne aminopropionowe jako inhibitory neprylizyny |
| JO2967B1 (en) | 2009-11-20 | 2016-03-15 | نوفارتس ايه جي | Acetic acid derivatives of carbamoyl methyl amino are substituted as new NEP inhibitors |
| ES2550485T3 (es) | 2010-01-22 | 2015-11-10 | Novartis Ag | Intermedios de inhibidores de la endopeptidasa neutra y método de preparación de los mismos |
| US8993631B2 (en) | 2010-11-16 | 2015-03-31 | Novartis Ag | Method of treating contrast-induced nephropathy |
| US8673974B2 (en) | 2010-11-16 | 2014-03-18 | Novartis Ag | Substituted amino bisphenyl pentanoic acid derivatives as NEP inhibitors |
| CN103261168B (zh) | 2010-12-15 | 2015-08-05 | 施万生物制药研发Ip有限责任公司 | 脑啡肽酶抑制剂 |
| SI2651896T1 (sl) | 2010-12-15 | 2015-11-30 | Theravance Biopharma R&D Ip, Llc | Inhibitorji neprilizina |
| AU2012217615B2 (en) | 2011-02-17 | 2016-09-29 | Theravance Biopharma R&D Ip, Llc | Substituted aminobutyric derivatives as neprilysin inhibitors |
| US8449890B2 (en) | 2011-02-17 | 2013-05-28 | Theravance, Inc. | Neprilysin inhibitors |
| CA2835281A1 (en) | 2011-05-31 | 2012-12-06 | Theravance, Inc. | Neprilysin inhibitors |
| ES2699773T3 (es) | 2011-05-31 | 2019-02-12 | Theravance Biopharma R&D Ip Llc | Inhibidores de neprilisina |
| ES2653215T3 (es) | 2011-05-31 | 2018-02-06 | Theravance Biopharma R&D Ip, Llc | Inhibidores de neprilisina |
| TWI560172B (en) | 2011-11-02 | 2016-12-01 | Theravance Biopharma R&D Ip Llc | Neprilysin inhibitors |
| CA2871292A1 (en) | 2012-05-31 | 2013-12-05 | Theravance Biopharma R&D Ip, Llc | Nitric oxide donor neprilysin inhibitors |
| ES2710932T3 (es) | 2012-06-08 | 2019-04-29 | Theravance Biopharma R&D Ip Llc | Inhibidores de neprilisina |
| LT2864292T (lt) | 2012-06-08 | 2017-07-10 | Theravance Biopharma R&D Ip, Llc | Neprilizino inhibitoriai |
| US9126956B2 (en) | 2012-08-08 | 2015-09-08 | Theravance Biopharma R&D Ip, Llc | Neprilysin inhibitors |
-
2011
- 2011-12-14 SI SI201130630T patent/SI2651896T1/sl unknown
- 2011-12-14 BR BR112013016595-2A patent/BR112013016595B1/pt not_active IP Right Cessation
- 2011-12-14 ES ES11808444.1T patent/ES2550324T3/es active Active
- 2011-12-14 KR KR1020137017560A patent/KR101892500B1/ko not_active Expired - Fee Related
- 2011-12-14 CA CA2817368A patent/CA2817368C/en active Active
- 2011-12-14 AU AU2011343899A patent/AU2011343899B2/en not_active Ceased
- 2011-12-14 JP JP2013544730A patent/JP5944921B2/ja not_active Expired - Fee Related
- 2011-12-14 RU RU2013132533A patent/RU2622288C2/ru active
- 2011-12-14 MX MX2013006805A patent/MX2013006805A/es active IP Right Grant
- 2011-12-14 HR HRP20151115TT patent/HRP20151115T1/hr unknown
- 2011-12-14 DK DK11808444.1T patent/DK2651896T3/en active
- 2011-12-14 HU HUE11808444A patent/HUE028051T2/hu unknown
- 2011-12-14 NZ NZ610983A patent/NZ610983A/en not_active IP Right Cessation
- 2011-12-14 EP EP11808444.1A patent/EP2651896B1/en active Active
- 2011-12-14 PH PH1/2013/501240A patent/PH12013501240A1/en unknown
- 2011-12-14 CN CN201180060335.7A patent/CN103261164B/zh not_active Expired - Fee Related
- 2011-12-14 CN CN201510423997.6A patent/CN105061314A/zh active Pending
- 2011-12-14 SG SG2013041181A patent/SG190432A1/en unknown
- 2011-12-14 ME MEP-2015-180A patent/ME02295B/me unknown
- 2011-12-14 MY MYPI2013001624A patent/MY170935A/en unknown
- 2011-12-14 PL PL11808444T patent/PL2651896T3/pl unknown
- 2011-12-14 RS RS20150708A patent/RS54348B1/sr unknown
- 2011-12-14 WO PCT/US2011/064829 patent/WO2012082853A1/en not_active Ceased
- 2011-12-14 US US13/325,425 patent/US8586536B2/en not_active Expired - Fee Related
- 2011-12-14 PT PT118084441T patent/PT2651896E/pt unknown
- 2011-12-14 SG SG10201510244TA patent/SG10201510244TA/en unknown
-
2013
- 2013-05-13 IL IL226327A patent/IL226327A/en active IP Right Grant
- 2013-06-07 ZA ZA2013/04205A patent/ZA201304205B/en unknown
- 2013-06-12 CO CO13140628A patent/CO6741228A2/es unknown
- 2013-10-10 US US14/050,733 patent/US9120747B2/en active Active
-
2015
- 2015-07-16 US US14/800,966 patent/US9388145B2/en active Active
- 2015-09-24 JP JP2015186389A patent/JP2016028089A/ja not_active Withdrawn
- 2015-10-29 SM SM201500271T patent/SMT201500271B/it unknown
-
2016
- 2016-06-06 US US15/173,870 patent/US9688692B2/en not_active Expired - Fee Related
-
2017
- 2017-05-19 US US15/599,769 patent/US9845332B2/en not_active Expired - Fee Related
- 2017-11-08 US US15/806,680 patent/US10336773B2/en active Active
-
2019
- 2019-05-13 US US16/410,361 patent/US10759813B2/en active Active
-
2020
- 2020-07-23 US US16/947,214 patent/US11261197B2/en not_active Expired - Fee Related
-
2022
- 2022-01-19 US US17/579,457 patent/US11851443B2/en active Active
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2013545811A5 (enExample) | ||
| JP2014515401A5 (enExample) | ||
| JP2014528903A5 (enExample) | ||
| JP2014515402A5 (enExample) | ||
| JP5944921B2 (ja) | ネプリライシン阻害剤 | |
| TWI583671B (zh) | 腦啡肽酶抑制劑 | |
| JP5959065B2 (ja) | ネプリライシン阻害剤としての置換アミノ酪酸誘導体 | |
| JP5944922B2 (ja) | ネプリライシン阻害剤 | |
| JP5944010B2 (ja) | ネプリライシン阻害剤 | |
| JP5959066B2 (ja) | ネプリライシン阻害剤としての置換アミノ酪酸誘導体 | |
| ES2710932T3 (es) | Inhibidores de neprilisina | |
| JP5959074B2 (ja) | ネプリライシン阻害剤 | |
| CN101675036B (zh) | 双效苯并咪唑抗高血压药 | |
| JP5959075B2 (ja) | ネプリライシン阻害剤 | |
| ES2718239T3 (es) | Inhibidores de neprilisina | |
| JP2018203761A (ja) | ネプリライシン阻害剤 | |
| JP2014508755A5 (enExample) | ||
| JP2017105817A (ja) | ネプリライシン阻害剤 | |
| JP2014505734A5 (enExample) | ||
| AU2016220348B2 (en) | (2R,4R)-5-(5'-chloro-2'-fluorobiphenyl-4-yl)-2-hydroxy-4-[(5-methyloxazole-2-carbonyl)amino]pentanoic acid |