ZA201805840B - 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 - Google Patents
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 thereofInfo
- Publication number
- ZA201805840B ZA201805840B ZA2018/05840A ZA201805840A ZA201805840B ZA 201805840 B ZA201805840 B ZA 201805840B ZA 2018/05840 A ZA2018/05840 A ZA 2018/05840A ZA 201805840 A ZA201805840 A ZA 201805840A ZA 201805840 B ZA201805840 B ZA 201805840B
- Authority
- ZA
- South Africa
- Prior art keywords
- hydroxyisoxazole
- carboxamido
- ethoxymethyl
- biphenyl
- fluoro
- Prior art date
Links
- IFWBKJFCPSEDNJ-CJAUYULYSA-N (2s,4r)-5-[4-(5-chloro-2-fluorophenyl)phenyl]-2-(ethoxymethyl)-2-methyl-4-[(3-oxo-1,2-oxazole-5-carbonyl)amino]pentanoic acid Chemical compound C([C@H](C[C@@](C)(COCC)C(O)=O)NC(=O)C=1ONC(=O)C=1)C(C=C1)=CC=C1C1=CC(Cl)=CC=C1F IFWBKJFCPSEDNJ-CJAUYULYSA-N 0.000 title 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
- C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
- C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
- C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D261/18—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4816—Wall or shell material
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Physiology (AREA)
- Nutrition Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662305393P | 2016-03-08 | 2016-03-08 | |
| US201662346336P | 2016-06-06 | 2016-06-06 | |
| PCT/US2017/021172 WO2017156009A1 (en) | 2016-03-08 | 2017-03-07 | 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 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA201805840B true ZA201805840B (en) | 2019-07-31 |
Family
ID=58387911
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA2018/05840A ZA201805840B (en) | 2016-03-08 | 2018-08-30 | 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 |
Country Status (30)
| Country | Link |
|---|---|
| US (6) | US10100021B2 (enExample) |
| EP (1) | EP3408260B1 (enExample) |
| JP (2) | JP7306828B2 (enExample) |
| KR (2) | KR20220035991A (enExample) |
| CN (1) | CN108779084A (enExample) |
| AU (1) | AU2017229466C1 (enExample) |
| CA (1) | CA3015505C (enExample) |
| CL (1) | CL2018002539A1 (enExample) |
| CO (1) | CO2018010568A2 (enExample) |
| CY (1) | CY1124397T1 (enExample) |
| DK (1) | DK3408260T3 (enExample) |
| ES (1) | ES2880123T3 (enExample) |
| HR (1) | HRP20211169T1 (enExample) |
| HU (1) | HUE055546T2 (enExample) |
| IL (1) | IL261244B (enExample) |
| LT (1) | LT3408260T (enExample) |
| MX (1) | MX377177B (enExample) |
| MY (1) | MY198185A (enExample) |
| PH (1) | PH12018501876A1 (enExample) |
| PL (1) | PL3408260T3 (enExample) |
| PT (1) | PT3408260T (enExample) |
| RS (1) | RS62172B1 (enExample) |
| RU (1) | RU2756223C2 (enExample) |
| SA (1) | SA518392325B1 (enExample) |
| SG (1) | SG11201807591VA (enExample) |
| SI (1) | SI3408260T1 (enExample) |
| SM (1) | SMT202100434T1 (enExample) |
| TW (1) | TWI731943B (enExample) |
| WO (1) | WO2017156009A1 (enExample) |
| ZA (1) | ZA201805840B (enExample) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| WO2021052441A1 (zh) | 2019-09-20 | 2021-03-25 | 深圳信立泰药业股份有限公司 | 血管紧张素ii受体拮抗剂代谢产物与nep抑制剂的复合物治疗心衰的用途 |
| KR102485499B1 (ko) * | 2022-07-15 | 2023-01-09 | 오가노이드사이언스 주식회사 | 신장 질환의 치료 또는 예방용 조성물 |
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| 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 |
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| 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 |
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| 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 |
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| US8993631B2 (en) | 2010-11-16 | 2015-03-31 | Novartis Ag | Method of treating contrast-induced nephropathy |
| 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 |
| 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 |
| 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 |
| KR101811549B1 (ko) * | 2013-06-19 | 2017-12-26 | 에프. 호프만-라 로슈 아게 | 인돌린-2-온 또는 피롤로-피리딘/피리미딘-2-온 유도체 |
| MX2016009760A (es) * | 2014-01-30 | 2016-11-08 | Theravance Biopharma R&D Ip Llc | Inhibidores de neprilisina. |
| 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 |
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2017
- 2017-03-07 TW TW106107450A patent/TWI731943B/zh active
- 2017-03-07 DK DK17712605.9T patent/DK3408260T3/da active
- 2017-03-07 RU RU2018135072A patent/RU2756223C2/ru active
- 2017-03-07 RS RS20210963A patent/RS62172B1/sr unknown
- 2017-03-07 WO PCT/US2017/021172 patent/WO2017156009A1/en not_active Ceased
- 2017-03-07 SG SG11201807591VA patent/SG11201807591VA/en unknown
- 2017-03-07 MY MYPI2018702868A patent/MY198185A/en unknown
- 2017-03-07 MX MX2018010727A patent/MX377177B/es active IP Right Grant
- 2017-03-07 HR HRP20211169TT patent/HRP20211169T1/hr unknown
- 2017-03-07 LT LTEP17712605.9T patent/LT3408260T/lt unknown
- 2017-03-07 SI SI201730845T patent/SI3408260T1/sl unknown
- 2017-03-07 KR KR1020227008251A patent/KR20220035991A/ko not_active Ceased
- 2017-03-07 JP JP2018546864A patent/JP7306828B2/ja active Active
- 2017-03-07 PL PL17712605T patent/PL3408260T3/pl unknown
- 2017-03-07 HU HUE17712605A patent/HUE055546T2/hu unknown
- 2017-03-07 SM SM20210434T patent/SMT202100434T1/it unknown
- 2017-03-07 PT PT177126059T patent/PT3408260T/pt unknown
- 2017-03-07 US US15/452,333 patent/US10100021B2/en active Active
- 2017-03-07 AU AU2017229466A patent/AU2017229466C1/en active Active
- 2017-03-07 CA CA3015505A patent/CA3015505C/en active Active
- 2017-03-07 CN CN201780016076.5A patent/CN108779084A/zh active Pending
- 2017-03-07 ES ES17712605T patent/ES2880123T3/es active Active
- 2017-03-07 KR KR1020187028757A patent/KR20180114225A/ko not_active Ceased
- 2017-03-07 EP EP17712605.9A patent/EP3408260B1/en active Active
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2018
- 2018-08-20 IL IL261244A patent/IL261244B/en unknown
- 2018-08-30 ZA ZA2018/05840A patent/ZA201805840B/en unknown
- 2018-09-02 SA SA518392325A patent/SA518392325B1/ar unknown
- 2018-09-03 PH PH12018501876A patent/PH12018501876A1/en unknown
- 2018-09-05 CL CL2018002539A patent/CL2018002539A1/es unknown
- 2018-09-10 US US16/125,991 patent/US10472335B2/en active Active
- 2018-10-02 CO CONC2018/0010568A patent/CO2018010568A2/es unknown
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2019
- 2019-09-25 US US16/582,051 patent/US10752599B2/en active Active
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2020
- 2020-07-14 US US16/928,206 patent/US11230536B2/en active Active
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2021
- 2021-07-30 CY CY20211100685T patent/CY1124397T1/el unknown
- 2021-10-29 JP JP2021177448A patent/JP2022017433A/ja active Pending
- 2021-12-14 US US17/550,564 patent/US11718591B2/en active Active
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2024
- 2024-02-15 US US18/442,885 patent/US12351561B2/en active Active
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