JP2014505734A5 - - Google Patents
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- Publication number
- JP2014505734A5 JP2014505734A5 JP2013554588A JP2013554588A JP2014505734A5 JP 2014505734 A5 JP2014505734 A5 JP 2014505734A5 JP 2013554588 A JP2013554588 A JP 2013554588A JP 2013554588 A JP2013554588 A JP 2013554588A JP 2014505734 A5 JP2014505734 A5 JP 2014505734A5
- Authority
- JP
- Japan
- Prior art keywords
- alkylene
- alkyl
- compound according
- halo
- benzyl
- 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 C*(*)c1ccc(CCC2)c2c1 Chemical compound C*(*)c1ccc(CCC2)c2c1 0.000 description 14
- BCIXCJIKSNDNBL-UHFFFAOYSA-N C=CC(c1ccccc11)OC1=O Chemical compound C=CC(c1ccccc11)OC1=O BCIXCJIKSNDNBL-UHFFFAOYSA-N 0.000 description 5
- IQOHNGIVDVCZEF-UHFFFAOYSA-N C1C2C(CCC3)C3C2C1 Chemical compound C1C2C(CCC3)C3C2C1 IQOHNGIVDVCZEF-UHFFFAOYSA-N 0.000 description 2
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161443828P | 2011-02-17 | 2011-02-17 | |
| US61/443,828 | 2011-02-17 | ||
| PCT/US2012/025369 WO2012154249A1 (en) | 2011-02-17 | 2012-02-16 | Substituted aminobutyric derivatives as neprilysin inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015246947A Division JP2016094453A (ja) | 2011-02-17 | 2015-12-18 | ネプリライシン阻害剤としての置換アミノ酪酸誘導体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014505734A JP2014505734A (ja) | 2014-03-06 |
| JP2014505734A5 true JP2014505734A5 (OSRAM) | 2015-04-02 |
| JP5959066B2 JP5959066B2 (ja) | 2016-08-02 |
Family
ID=45814662
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013554588A Expired - Fee Related JP5959066B2 (ja) | 2011-02-17 | 2012-02-16 | ネプリライシン阻害剤としての置換アミノ酪酸誘導体 |
| JP2015246947A Withdrawn JP2016094453A (ja) | 2011-02-17 | 2015-12-18 | ネプリライシン阻害剤としての置換アミノ酪酸誘導体 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015246947A Withdrawn JP2016094453A (ja) | 2011-02-17 | 2015-12-18 | ネプリライシン阻害剤としての置換アミノ酪酸誘導体 |
Country Status (5)
| Country | Link |
|---|---|
| US (5) | US8449890B2 (OSRAM) |
| EP (1) | EP2675792B1 (OSRAM) |
| JP (2) | JP5959066B2 (OSRAM) |
| ES (1) | ES2564275T3 (OSRAM) |
| WO (1) | WO2012154249A1 (OSRAM) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2435402B1 (en) | 2009-05-28 | 2016-04-13 | Novartis AG | Substituted aminobutyric derivatives as neprilysin inhibitors |
| KR101892611B1 (ko) | 2010-12-15 | 2018-08-28 | 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 | 네프릴리신 억제제 |
| RS54348B1 (sr) | 2010-12-15 | 2016-02-29 | Theravance Biopharma R&D Ip, Llc | Inhibitori neprilizina |
| CN103380119B (zh) | 2011-02-17 | 2016-02-17 | 施万生物制药研发Ip有限责任公司 | 作为脑啡肽酶抑制剂的经取代的氨基丁酸衍生物 |
| WO2012154249A1 (en) | 2011-02-17 | 2012-11-15 | Theravance, Inc. | Substituted aminobutyric derivatives as neprilysin inhibitors |
| EP2714660B1 (en) | 2011-05-31 | 2018-09-26 | Theravance Biopharma R&D IP, LLC | Neprilysin inhibitors |
| JP5959074B2 (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 |
| CA2871292A1 (en) | 2012-05-31 | 2013-12-05 | Theravance Biopharma R&D Ip, Llc | Nitric oxide donor neprilysin inhibitors |
| CA2873328A1 (en) | 2012-06-08 | 2013-12-12 | Theravance Biopharma R&D Ip, Llc | Neprilysin inhibitors |
| MX356260B (es) | 2012-06-08 | 2018-05-21 | Theravance Biopharma R&D Ip Llc | Inhibidores de la neprilisina. |
| CN104520277B (zh) | 2012-08-08 | 2018-01-19 | 施万生物制药研发Ip有限责任公司 | 脑啡肽酶抑制剂 |
| 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 |
| HRP20171097T1 (hr) | 2013-03-05 | 2017-10-06 | Theravance Biopharma R&D Ip, Llc | Inhibitori neprilizina |
| JP2017504625A (ja) | 2014-01-30 | 2017-02-09 | 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５−ビフェニル−４−ヘテロアリールカルボニルアミノ−ペンタン酸誘導体 |
| SG11201605965UA (en) * | 2014-01-30 | 2016-08-30 | Theravance Biopharma R&D Ip Llc | Neprilysin inhibitors |
| JP6766055B2 (ja) | 2015-02-11 | 2020-10-07 | 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（２ｓ，４ｒ）−５−（５’−クロロ−２’−フルオロビフェニル−４−イル）−４−（エトキシオキサリルアミノ）−２−ヒドロキシメチル−２−メチルペンタン酸 |
| HRP20210040T1 (hr) | 2015-02-19 | 2021-04-02 | Theravance Biopharma R&D Ip, Llc | (2r,4r)-5-(5′-klor-2’-fluorbifenil-4-il)-2-hidroksi-4-[(5-metiloksazol-2-karbonil)amino]pentanska kiselina |
| CA3015505C (en) | 2016-03-08 | 2024-03-05 | Theravance Biopharma R&D Ip, Llc | Crystalline (2s,4r)-5-(5'-chloro-2'-fluoro-[1,1'-biphenyl]-4-yl)-2-(ethoxymethyl)-4-(3-hydroxyisoxazole-5-carboxamido)-2-methylpentanoic acid and uses thereof |
| CN106905348B (zh) * | 2017-02-13 | 2018-12-04 | 牡丹江医学院 | 一种预防和治疗急性肾损伤的药物及其制备方法和用途 |
| JP7411414B2 (ja) * | 2017-12-15 | 2024-01-11 | 中外製薬株式会社 | ペプチドの製造方法、及び塩基の処理方法 |
| CN111630005A (zh) | 2018-01-03 | 2020-09-04 | 埃科莱布美国股份有限公司 | 作为腐蚀抑制剂的苯并三唑衍生物 |
| 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 |
Family Cites Families (49)
| 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 |
| 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 |
| IL97219A (en) * | 1990-02-19 | 1995-12-08 | Ciba Geigy Ag | Biphenyl substituted aliphatic amino compounds process for their preparation and pharmaceutical compositions containing them |
| 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 |
| CA2218716A1 (en) | 1995-04-21 | 1996-10-24 | Novartis Ag | N-aroylamino acid amides as endothelin inhibitors |
| MXPA02011750A (es) * | 2000-06-14 | 2003-03-27 | Warner Lambert Co | Bencenos 1,2,4-trisubstituidos como inhibidores de 15-lipoxigenasa. |
| US20050054836A1 (en) | 2000-11-09 | 2005-03-10 | Cold Spring Harbor Laboratory | Chimeric molecules to modulate gene expression |
| 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 |
| SG185318A1 (en) | 2007-01-12 | 2012-11-29 | Novartis Ag | Process for preparing 5-biphenyl-4-amino-2-methyl pentanoic acid |
| 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 |
| BRPI1011657A2 (pt) * | 2009-05-28 | 2019-04-16 | Novartis Ag | derivados aminopropiônicos substituídos como inibidores de neprilisina |
| EP2435402B1 (en) * | 2009-05-28 | 2016-04-13 | Novartis AG | Substituted aminobutyric derivatives as neprilysin inhibitors |
| JO2967B1 (en) | 2009-11-20 | 2016-03-15 | نوفارتس ايه جي | Acetic acid derivatives of carbamoyl methyl amino are substituted as new NEP inhibitors |
| CN104262228B (zh) | 2010-01-22 | 2017-01-18 | 诺华股份有限公司 | 中性内肽酶抑制剂中间体和其制备方法 |
| 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 |
| KR101892611B1 (ko) * | 2010-12-15 | 2018-08-28 | 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 | 네프릴리신 억제제 |
| RS54348B1 (sr) * | 2010-12-15 | 2016-02-29 | Theravance Biopharma R&D Ip, Llc | Inhibitori neprilizina |
| CN103380119B (zh) | 2011-02-17 | 2016-02-17 | 施万生物制药研发Ip有限责任公司 | 作为脑啡肽酶抑制剂的经取代的氨基丁酸衍生物 |
| WO2012154249A1 (en) | 2011-02-17 | 2012-11-15 | Theravance, Inc. | Substituted aminobutyric derivatives as neprilysin inhibitors |
| EP2714660B1 (en) | 2011-05-31 | 2018-09-26 | Theravance Biopharma R&D IP, LLC | Neprilysin inhibitors |
| US8686184B2 (en) | 2011-05-31 | 2014-04-01 | Theravance, Inc. | Neprilysin inhibitors |
| JP5959074B2 (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 |
| CA2871292A1 (en) | 2012-05-31 | 2013-12-05 | Theravance Biopharma R&D Ip, Llc | Nitric oxide donor neprilysin inhibitors |
| MX356260B (es) | 2012-06-08 | 2018-05-21 | Theravance Biopharma R&D Ip Llc | Inhibidores de la neprilisina. |
| CA2873328A1 (en) | 2012-06-08 | 2013-12-12 | Theravance Biopharma R&D Ip, Llc | Neprilysin inhibitors |
| CN104520277B (zh) | 2012-08-08 | 2018-01-19 | 施万生物制药研发Ip有限责任公司 | 脑啡肽酶抑制剂 |
| HRP20171097T1 (hr) | 2013-03-05 | 2017-10-06 | Theravance Biopharma R&D Ip, Llc | Inhibitori neprilizina |
-
2012
- 2012-02-16 WO PCT/US2012/025369 patent/WO2012154249A1/en not_active Ceased
- 2012-02-16 US US13/398,027 patent/US8449890B2/en not_active Expired - Fee Related
- 2012-02-16 ES ES12708195.8T patent/ES2564275T3/es active Active
- 2012-02-16 JP JP2013554588A patent/JP5959066B2/ja not_active Expired - Fee Related
- 2012-02-16 EP EP12708195.8A patent/EP2675792B1/en active Active
-
2013
- 2013-04-24 US US13/869,174 patent/US8846913B2/en active Active
-
2014
- 2014-08-15 US US14/460,567 patent/US9487514B2/en not_active Expired - Fee Related
-
2015
- 2015-12-18 JP JP2015246947A patent/JP2016094453A/ja not_active Withdrawn
-
2016
- 2016-09-20 US US15/270,187 patent/US9725448B2/en not_active Expired - Fee Related
-
2017
- 2017-06-30 US US15/638,733 patent/US20180051023A1/en not_active Abandoned
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