AR083873A1 - Derivados de acido amino-fenil-pentanoico sustituidos como inhibidores de nep - Google Patents
Derivados de acido amino-fenil-pentanoico sustituidos como inhibidores de nepInfo
- Publication number
- AR083873A1 AR083873A1 ARP110104250A ARP110104250A AR083873A1 AR 083873 A1 AR083873 A1 AR 083873A1 AR P110104250 A ARP110104250 A AR P110104250A AR P110104250 A ARP110104250 A AR P110104250A AR 083873 A1 AR083873 A1 AR 083873A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- phenyl
- amino
- acid derivatives
- pentanoic acid
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
- C07C235/70—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton
- C07C235/72—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms
- C07C235/74—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of a saturated carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
- C07C235/70—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton
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- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
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- 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
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/216—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Diabetes (AREA)
- Hematology (AREA)
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- Neurology (AREA)
- Neurosurgery (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pain & Pain Management (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Dermatology (AREA)
- Urology & Nephrology (AREA)
- Pulmonology (AREA)
- Ophthalmology & Optometry (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Hospice & Palliative Care (AREA)
- Oncology (AREA)
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- Emergency Medicine (AREA)
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Abstract
Reivindicación 1: Un compuesto de la fórmula (1), en donde: X y X1 son independientemente OH, -O-alquilo C1-7, NRaRb, -NHS(O)2-alquilo C1-7 o -NHS(O)2-bencilo, en donde Ra y Rb, por cada presentación, son independientemente H o alquilo C1-7; R1 es H o alquilo C1-6; R2 por cada presentación, es independientemente alcoxilo C1-6, hidroxilo, halógeno, alquilo C1-6, ciano o halo-alquilo C1-6; A1 es un alquileno C1-4 lineal; R3 por cada presentación, es independientemente halógeno, hidroxilo, alcoxilo C1-7, halógeno, alquilo C1-7, o halo-alquilo C1-7; o n es un entero de 1 a 5; s es 0 o un entero de 1 a 4; o una sal farmacéuticamente aceptable del mismo.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US41416310P | 2010-11-16 | 2010-11-16 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR083873A1 true AR083873A1 (es) | 2013-03-27 |
Family
ID=45093705
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP110104250A AR083873A1 (es) | 2010-11-16 | 2011-11-14 | Derivados de acido amino-fenil-pentanoico sustituidos como inhibidores de nep |
Country Status (14)
Country | Link |
---|---|
US (1) | US8673974B2 (es) |
EP (1) | EP2640690A1 (es) |
JP (1) | JP5872575B2 (es) |
KR (1) | KR101951492B1 (es) |
CN (1) | CN103201257B (es) |
AR (1) | AR083873A1 (es) |
AU (1) | AU2011331294B2 (es) |
BR (1) | BR112013011580A2 (es) |
CA (1) | CA2817114A1 (es) |
EA (1) | EA021537B1 (es) |
MX (1) | MX2013005533A (es) |
TW (1) | TW201305089A (es) |
UY (1) | UY33731A (es) |
WO (1) | WO2012065956A1 (es) |
Families Citing this family (26)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP2183273B1 (en) | 2007-08-17 | 2017-04-05 | Novartis AG | Cyclic depsipeptides |
US8586536B2 (en) | 2010-12-15 | 2013-11-19 | Theravance, Inc. | Neprilysin inhibitors |
AU2011343903B2 (en) | 2010-12-15 | 2016-06-30 | Theravance Biopharma R&D Ip, Llc | Neprilysin inhibitors |
US8449890B2 (en) | 2011-02-17 | 2013-05-28 | Theravance, Inc. | Neprilysin inhibitors |
RU2604522C2 (ru) | 2011-02-17 | 2016-12-10 | ТЕРЕВАНС БАЙОФАРМА Ар энд Ди АйПи,ЭлЭлСи | Замещенные аминомасляные производные в качестве ингибиторов неприлизина |
US8513244B2 (en) | 2011-05-31 | 2013-08-20 | Theravance, Inc. | Neprilysin inhibitors |
EP2714660B1 (en) | 2011-05-31 | 2018-09-26 | Theravance Biopharma R&D IP, LLC | Neprilysin inhibitors |
ES2642883T3 (es) | 2011-05-31 | 2017-11-20 | 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 |
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 |
LT2882716T (lt) | 2012-08-08 | 2017-02-10 | Theravance Biopharma R&D Ip, Llc | Neprilizino inhibitoriai |
SI2964616T1 (sl) | 2013-03-05 | 2017-08-31 | Theravance Biopharma R&D Ip, Llc | Zaviralci neprilizina |
KR20160113291A (ko) | 2014-01-30 | 2016-09-28 | 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 | 네프리리신 저해제 |
AU2015211041B2 (en) | 2014-01-30 | 2018-11-08 | Theravance Biopharma R&D Ip, Llc | 5-biphenyl-4-heteroarylcarbonylamino-pentanoic acid derivatives as neprilysin inhibitors |
US11261186B2 (en) | 2014-12-24 | 2022-03-01 | Lg Chem. Ltd. | Biaryl derivative as GPR120 agonist |
CN104557600B (zh) * | 2015-01-26 | 2016-05-04 | 苏州明锐医药科技有限公司 | 沙库比曲的制备方法 |
AU2016219362B2 (en) | 2015-02-11 | 2019-11-14 | Theravance Biopharma R&D Ip, Llc | (2S,4R)-5-(5'-chloro-2'-fluorobiphenyl-4-yl)-4-(ethoxyoxalylamino)-2-hydroxymethyl-2-methylpentanoic acid as neprilysin inhibitor |
EP3259255B1 (en) | 2015-02-19 | 2020-10-21 | Theravance Biopharma R&D IP, LLC | (2r,4r)-5-(5'-chloro-2'-fluorobiphenyl-4-yl)-2-hydroxy-4-[(5-methyloxazole-2-carbonyl)amino]pentanoic acid |
SG11201807591VA (en) | 2016-03-08 | 2018-10-30 | 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 |
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 |
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 |
EP3887388A1 (en) | 2018-11-27 | 2021-10-06 | Novartis AG | Cyclic peptides as proprotein convertase subtilisin/kexin type 9 (pcsk9) inhibitors for the treatment of metabolic disorders |
WO2023084449A1 (en) | 2021-11-12 | 2023-05-19 | Novartis Ag | Diaminocyclopentylpyridine derivatives for the treatment of a disease or disorder |
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-
2011
- 2011-11-11 US US13/294,262 patent/US8673974B2/en active Active
- 2011-11-14 CN CN201180053783.4A patent/CN103201257B/zh not_active Expired - Fee Related
- 2011-11-14 KR KR1020137015361A patent/KR101951492B1/ko active IP Right Grant
- 2011-11-14 CA CA2817114A patent/CA2817114A1/en not_active Abandoned
- 2011-11-14 MX MX2013005533A patent/MX2013005533A/es active IP Right Grant
- 2011-11-14 JP JP2013539219A patent/JP5872575B2/ja not_active Expired - Fee Related
- 2011-11-14 AU AU2011331294A patent/AU2011331294B2/en not_active Ceased
- 2011-11-14 AR ARP110104250A patent/AR083873A1/es not_active Application Discontinuation
- 2011-11-14 UY UY0001033731A patent/UY33731A/es not_active Application Discontinuation
- 2011-11-14 BR BR112013011580A patent/BR112013011580A2/pt not_active Application Discontinuation
- 2011-11-14 EP EP11790902.8A patent/EP2640690A1/en not_active Withdrawn
- 2011-11-14 WO PCT/EP2011/070080 patent/WO2012065956A1/en active Application Filing
- 2011-11-14 EA EA201390723A patent/EA021537B1/ru not_active IP Right Cessation
- 2011-11-15 TW TW100141702A patent/TW201305089A/zh unknown
Also Published As
Publication number | Publication date |
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MX2013005533A (es) | 2013-07-03 |
AU2011331294B2 (en) | 2015-11-05 |
JP2014501720A (ja) | 2014-01-23 |
EA201390723A1 (ru) | 2013-09-30 |
AU2011331294A1 (en) | 2013-05-02 |
JP5872575B2 (ja) | 2016-03-01 |
KR101951492B1 (ko) | 2019-02-22 |
BR112013011580A2 (pt) | 2016-08-09 |
KR20130116288A (ko) | 2013-10-23 |
US8673974B2 (en) | 2014-03-18 |
CA2817114A1 (en) | 2012-05-24 |
US20120122977A1 (en) | 2012-05-17 |
CN103201257B (zh) | 2016-01-20 |
EP2640690A1 (en) | 2013-09-25 |
EA021537B1 (ru) | 2015-07-30 |
TW201305089A (zh) | 2013-02-01 |
CN103201257A (zh) | 2013-07-10 |
UY33731A (es) | 2012-06-29 |
WO2012065956A1 (en) | 2012-05-24 |
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