AR083873A1 - Derivados de acido amino-fenil-pentanoico sustituidos como inhibidores de nep - Google Patents

Derivados de acido amino-fenil-pentanoico sustituidos como inhibidores de nep

Info

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
Application number
ARP110104250A
Other languages
English (en)
Original Assignee
Novartis Ag
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of AR083873A1 publication Critical patent/AR083873A1/es

Links

Classifications

    • 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
    • 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 
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/16—Emollients or protectives, e.g. against radiation
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A61P25/10—Antiepileptics; Anticonvulsants for petit-mal
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
    • 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
    • A61P9/06—Antiarrhythmics
    • 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
    • A61P9/08—Vasodilators for multiple indications
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Psychiatry (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Reproductive Health (AREA)
  • Vascular Medicine (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Toxicology (AREA)
  • Gynecology & Obstetrics (AREA)

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.
ARP110104250A 2010-11-16 2011-11-14 Derivados de acido amino-fenil-pentanoico sustituidos como inhibidores de nep AR083873A1 (es)

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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2008290567B2 (en) 2007-08-17 2011-05-12 Novartis Ag Cyclic depsipeptides
MX354476B (es) 2010-12-15 2018-03-07 Theravance Inc Inhibidores de neprilisina.
SI2651896T1 (sl) 2010-12-15 2015-11-30 Theravance Biopharma R&D Ip, Llc Inhibitorji neprilizina
US8449890B2 (en) 2011-02-17 2013-05-28 Theravance, Inc. Neprilysin inhibitors
MX342212B (es) 2011-02-17 2016-09-20 Theravance Inc Inhibidores de neprilisina.
CA2835216A1 (en) 2011-05-31 2012-12-06 Theravance, Inc. Neprilysin inhibitors
EP2714648B1 (en) 2011-05-31 2017-08-16 Theravance Biopharma R&D IP, LLC Neprilysin inhibitors
WO2012166390A1 (en) 2011-05-31 2012-12-06 Theravance, Inc. Neprilysin inhibitors
TWI560172B (en) 2011-11-02 2016-12-01 Theravance Biopharma R&D Ip Llc Neprilysin inhibitors
CN104350052B (zh) 2012-05-31 2017-05-31 施万生物制药研发Ip有限责任公司 一氧化氮供体脑啡肽酶抑制剂
ME02698B (me) 2012-06-08 2017-10-20 Theravance Biopharma R&D Ip Llc Inhibitori neprilizina
US8871792B2 (en) 2012-06-08 2014-10-28 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
ES2634218T3 (es) 2013-03-05 2017-09-27 Theravance Biopharma R&D Ip, Llc Inhibidores de neprilisina
US9585882B2 (en) 2014-01-30 2017-03-07 Theravance Biopharma R&D Ip, Llc Neprilysin inhibitors
JP2017507921A (ja) 2014-01-30 2017-03-23 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
MY189770A (en) * 2014-12-24 2022-03-04 Lg Chemical Ltd Biaryl derivative as gpr120 agonists
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
MY187899A (en) 2015-02-11 2021-10-27 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
JP6714009B2 (ja) 2015-02-19 2020-06-24 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 （２ｒ，４ｒ）−５−（５’−クロロ−２’−フルオロビフェニル−４−イル）−２−ヒドロキシ−４−［（５−メチルオキサゾール−２−カルボニル）アミノ］ペンタン酸
KR20220035991A (ko) 2016-03-08 2022-03-22 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 (2s,4r)-5-(5'-클로로-2'-플루오로-[1,1'-비페닐]-4-일)-2-(에톡시메틸)-4-(3-히드록시이속사졸-5-카르복사미도)-2-메틸펜탄산 결정 및 그 용도
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
CN113166204A (zh) 2018-11-27 2021-07-23 诺华股份有限公司 作为治疗代谢障碍的蛋白质原转换酶枯草杆菌蛋白酶/kexin 9型（PCSK9）抑制剂的环状肽
CN113166101A (zh) 2018-11-27 2021-07-23 诺华股份有限公司 作为治疗代谢障碍的蛋白质原转换酶枯草杆菌蛋白酶/kexin 9型（PCSK9）抑制剂的环状五聚体化合物
WO2023084449A1 (en) 2021-11-12 2023-05-19 Novartis Ag Diaminocyclopentylpyridine derivatives for the treatment of a disease or disorder

Family Cites Families (74)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2951135A1 (de) 1979-12-19 1981-06-25 Hoechst Ag, 6230 Frankfurt Sulfonylharnstoffe, verfahren zu ihrer herstellung, pharmazeutische praeparate auf basis dieser verbindungen und ihre verwendung
PT72878B (en) 1980-04-24 1983-03-29 Merck & Co Inc Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents
US4617307A (en) 1984-06-20 1986-10-14 Ciba-Geigy Corporation Substituted imidazo[1,5-A]pyridine derivatives as aromatase inhibitors
US4889861A (en) 1982-12-21 1989-12-26 Ciba-Geigy Corp. Substituted imidazo[1,5-a]pyridine derivatives and other substituted bicyclic derivatives and their use as aromatase inhibitors
FI77669C (fi) 1983-04-13 1989-04-10 Ciba Geigy Ag 20-spiroxaner och analoger, som innehaoller en oeppen ring e, foerfarande foer deras framstaellning samt dessa innehaollande farmaceutiska preparat.
DE3347565A1 (de) 1983-12-30 1985-07-11 Thomae Gmbh Dr K Neue phenylessigsaeurederivate, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung
JPS6354321A (ja) 1985-03-27 1988-03-08 Ajinomoto Co Inc 血糖降下剤
US5118666A (en) 1986-05-05 1992-06-02 The General Hospital Corporation Insulinotropic hormone
US5120712A (en) 1986-05-05 1992-06-09 The General Hospital Corporation Insulinotropic hormone
EP0512042B1 (en) 1990-01-24 1998-04-08 BUCKLEY, Douglas I. Glp-1 analogs useful for diabetes treatment
AU654331B2 (en) 1991-03-30 1994-11-03 Kissei Pharmaceutical Co. Ltd. Succinic acid compounds
RU2086544C1 (ru) 1991-06-13 1997-08-10 Хоффманн-Ля Рош АГ Бензолсульфонамидные производные пиримидина или их соли, фармацевтическая композиция для лечения заболеваний, связанных с активностью эндотелина
SG43036A1 (en) 1991-06-21 1997-10-17 Thomae Gmbh Dr K (S) (+) -2-ethoxy-4-[N-[1-(2-piperidino-phenyl)-3-methyl- 1-buthyl]aminocarbony methyl] - benzoic a cid
ES2100291T3 (es) 1991-07-30 1997-06-16 Ajinomoto Kk Cristales de n-(trans-4-isopropilciclohexilcarbonil)-d-fenilalanina y metodos para prepararlos.
JP3130938B2 (ja) * 1991-10-22 2001-01-31 オーストリア・タバクヴェルケ・アクチエンゲゼルシャフトヴォマー・オーシュターライヒッシェ・タバコレジー シガレットフィルター
WO1993011782A1 (en) 1991-12-19 1993-06-24 Southwest Foundation For Biomedical Research Cetp inhibitor polypeptide, antibodies against the synthetic polypeptide and prophylactic and therapeutic anti-atherosclerosis treatments
US5217996A (en) 1992-01-22 1993-06-08 Ciba-Geigy Corporation Biaryl substituted 4-amino-butyric acid amides
IL111785A0 (en) 1993-12-03 1995-01-24 Ferring Bv Dp-iv inhibitors and pharmaceutical compositions containing them
US5705483A (en) 1993-12-09 1998-01-06 Eli Lilly And Company Glucagon-like insulinotropic peptides, compositions and methods
US5512549A (en) 1994-10-18 1996-04-30 Eli Lilly And Company Glucagon-like insulinotropic peptide analogs, compositions, and methods of use
TW313568B (es) 1994-12-20 1997-08-21 Hoffmann La Roche
US5710171A (en) 1995-05-24 1998-01-20 Merck & Co., Inc. Bisphenyl inhibitors of farnesyl-protein transferase
US5886022A (en) * 1995-06-05 1999-03-23 Bayer Corporation Substituted cycloalkanecarboxylic acid derivatives as matrix metalloprotease inhibitors
DE19616486C5 (de) 1996-04-25 2016-06-30 Royalty Pharma Collection Trust Verfahren zur Senkung des Blutglukosespiegels in Säugern
TW492957B (en) 1996-11-07 2002-07-01 Novartis Ag N-substituted 2-cyanopyrrolidnes
US6197786B1 (en) 1998-09-17 2001-03-06 Pfizer Inc 4-Carboxyamino-2-substituted-1,2,3,4-tetrahydroquinolines
GT199900147A (es) 1998-09-17 1999-09-06 1, 2, 3, 4- tetrahidroquinolinas 2-sustituidas 4-amino sustituidas.
CO5150173A1 (es) 1998-12-10 2002-04-29 Novartis Ag Compuestos n-(glicilo sustituido)-2-cianopirrolidinas inhibidores de peptidasa de dipeptidilo-iv (dpp-iv) los cuales son efectivos en el tratamiento de condiciones mediadas por la inhibicion de dpp-iv
JP4070357B2 (ja) 1999-06-03 2008-04-02 花王株式会社 皮膚外用剤
US6683113B2 (en) 1999-09-23 2004-01-27 Pharmacia Corporation (R)-chiral halogenated substituted N,N-Bis-benzyl aminioalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity
WO2001076574A2 (en) 2000-04-12 2001-10-18 Novartis Ag Novel medical use of aldosterone synthase inhibitors alone or in combination with at1-receptor antagonists
AU1339302A (en) 2000-10-20 2002-05-06 Biocryst Pharm Inc Biaryl compounds as serine protease inhibitors
BRPI0306907B8 (pt) 2002-01-17 2021-05-25 Novartis Ag composição farmacêutica, que compreende valsartan e inibidor de nep ou seus sais
CN100404535C (zh) 2002-08-07 2008-07-23 诺瓦提斯公司 用作治疗醛固酮介导的病症的药物的有机化合物
EP1565463B1 (en) 2002-11-18 2008-06-11 Novartis AG Imidazo[1,5a] pyridine derivatives and methods for treating aldosterone mediated diseases
CA2514733A1 (en) 2003-02-28 2004-09-16 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
JP2006525364A (ja) 2003-04-30 2006-11-09 ジ インスチチュート フォー ファーマシューティカル ディスカバリー、エルエルシー 置換アミノカルボン酸
PT1732933E (pt) 2004-03-26 2008-10-20 Lilly Co Eli Compostos para o tratamento da dislipidémia
UA90269C2 (ru) 2004-04-02 2010-04-26 Мицубиси Танабе Фарма Корпорейшн Тетрагидрохинолиновые производные и способ их получения
US20080076794A1 (en) 2004-05-28 2008-03-27 Peter Herold Heterocyclic Compounds And Their Use As Aldosterone Synthase Inhibitors
TW200612947A (en) 2004-05-28 2006-05-01 Speedel Experimenta Ag Organic compounds
CN1997643A (zh) 2004-05-28 2007-07-11 斯皮德尔实验股份公司 杂环化合物及其作为醛固酮合酶抑制剂的应用
WO2006005726A2 (en) 2004-07-09 2006-01-19 Speedel Experimenta Ag Heterocyclic compounds
WO2006083924A1 (en) * 2005-02-02 2006-08-10 Vitae Pharmaceuticals, Inc. 1-acylamino-2-hydroxy-3-amino-w-arylalkanes as renin inhibitors
MY146830A (en) 2005-02-11 2012-09-28 Novartis Ag Combination of organic compounds
TW200716634A (en) 2005-05-31 2007-05-01 Speedel Experimenta Ag Heterocyclic spiro-compounds
TW200716105A (en) 2005-05-31 2007-05-01 Speedel Experimenta Ag Imidazole compounds
TW200716636A (en) 2005-05-31 2007-05-01 Speedel Experimenta Ag Heterocyclic spiro-compounds
GT200600381A (es) 2005-08-25 2007-03-28 Compuestos organicos
WO2007045663A2 (en) 2005-10-19 2007-04-26 Novartis Ag Combination of an ati receptor antagonist and a np inhibitor fro treating ia hypertension and heartfailure
WO2007056324A2 (en) 2005-11-08 2007-05-18 Novartis Ag Combination of an angiotensin ii receptor blocker, a calcium channel blocker and another active agent
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
AR056888A1 (es) 2005-12-09 2007-10-31 Speedel Experimenta Ag Derivados de heterociclil imidazol
MX2008012387A (es) * 2006-03-29 2008-10-09 Novartis Ag Inhibidores selectivos de mmp basados en hidroxamato.
EP2009080A4 (en) 2006-04-04 2010-05-26 Taiyo Nippon Sanso Corp PROCESS FOR SEPARATION OF METHANE, METHANE SEPARATOR AND METHANE USE SYSTEM
TW200808812A (en) 2006-04-12 2008-02-16 Speedel Experimenta Ag Imidazo compounds
TW200808813A (en) 2006-04-12 2008-02-16 Speedel Experimenta Ag Imidazo compounds
EP1886695A1 (en) 2006-06-27 2008-02-13 Speedel Experimenta AG Pharmaceutical combination of an aldosterone synthase inhibitor and a glucocorticoid receptor antagonist or a cortisol synthesis inhibitor or a corticotropin releasing factor antagonist
MX2009000646A (es) 2006-07-20 2009-01-29 Novartis Ag Derivados de amino-piperidina como inhibidores de la proteina de transferencia de colesteril-ester (cetp).
EP2057163A1 (en) 2006-08-25 2009-05-13 Novartis AG Fused imidazole derivatives for the treatment of disorders mediated by aldosterone synthase and/or 11-beta-hydroxylase and/or aromatase
EP1903027A1 (en) 2006-09-13 2008-03-26 Novartis AG Process for preparing biaryl substituted 4-amino-butyric acid or derivatives thereof and their use in the production of NEP inhibitors
BRPI0721290A2 (pt) 2006-12-18 2014-03-25 Novartis Ag Compostos orgânicos
EP2121652A1 (en) 2006-12-18 2009-11-25 Novartis AG 4-imidazolyl-1,2,3,4-tetrahydroquinoline derivatives and their use as aldosterone/11-beta-hydroxylase inhibitors
WO2008076336A2 (en) 2006-12-18 2008-06-26 Novartis Ag Imidazoles as aldosterone synthase inhibitors
AR064842A1 (es) 2007-01-12 2009-04-29 Mazzucco Gavieiro Maria Belen Pirrolidin-2-onas, y su uso en la preparacion de inhibidores de nep
TW200904416A (en) 2007-03-29 2009-02-01 Speedel Experimenta Ag Heterocyclic spiro-compounds
EP2207775B1 (en) 2007-11-05 2012-03-21 Novartis AG 4-benzylamino-1-carboxyacyl-piperidine derivatives as cetp inhibitors useful for the treatment of diseases such as hyperlipidemia or arteriosclerosis
SI3067043T1 (sl) 2007-11-06 2023-04-28 Novartis Ag Farmacevtski sestavki na osnovi superstruktur antagonista/blokatorja angiotenzinskega receptorja (ARB) in zaviralca nevtralne endopeptidaze (NEP)
EP2229356B1 (en) 2007-12-03 2011-10-12 Novartis AG 1,2-disubstituted-4-benzylamino-pyrrolidine derivatives as cetp inhibitors useful for the treatment of diseases such as hyperli pidemia or arteriosclerosis
PE20091364A1 (es) 2008-01-17 2009-10-13 Novartis Ag Proceso para la preparacion de inhibidores de nep
AR072297A1 (es) 2008-06-27 2010-08-18 Novartis Ag Derivados de indol-2-il-piridin-3-ilo, composicion farmaceutica que los comprende y su uso en medicamentos para el tratamiento de enfermedades mediadas por la sintasa aldosterona.
JP5659224B2 (ja) 2009-05-15 2015-01-28 ノバルティス アーゲー アルドステロンシンターゼ阻害剤としてのアリールピリジン
SG176010A1 (en) * 2009-05-28 2011-12-29 Novartis Ag Substituted aminobutyric derivatives as neprilysin inhibitors
AU2010251967B9 (en) * 2009-05-28 2014-04-03 Novartis Ag Substituted aminopropionic derivatives as neprilysin inhibitors

Also Published As

Publication number Publication date
EP2640690A1 (en) 2013-09-25
CA2817114A1 (en) 2012-05-24
BR112013011580A2 (pt) 2016-08-09
KR101951492B1 (ko) 2019-02-22
AU2011331294A1 (en) 2013-05-02
AU2011331294B2 (en) 2015-11-05
JP5872575B2 (ja) 2016-03-01
JP2014501720A (ja) 2014-01-23
US20120122977A1 (en) 2012-05-17
US8673974B2 (en) 2014-03-18
TW201305089A (zh) 2013-02-01
CN103201257A (zh) 2013-07-10
KR20130116288A (ko) 2013-10-23
WO2012065956A1 (en) 2012-05-24
UY33731A (es) 2012-06-29
EA021537B1 (ru) 2015-07-30
CN103201257B (zh) 2016-01-20
MX2013005533A (es) 2013-07-03
EA201390723A1 (ru) 2013-09-30

Similar Documents

Publication Publication Date Title
AR083873A1 (es) Derivados de acido amino-fenil-pentanoico sustituidos como inhibidores de nep
CY1120682T1 (el) Ενωσεις για την προστασια κυτταρων
AR060489A1 (es) Derivados del acido benzoazepin - oxi- acetico como agonistas de ppar - delta usados para aumentar hdl- c, reducir ldl-c y reducir colesterol
MA34389B1 (fr) Nouvelles aminopyrazoloquinazolines
UA111626C2 (uk) Похідні дигідрохінолін-2-ону
BR112014010407A2 (pt) compostos de azetidina, composições e seu uso como inibidores de hidrolase de epóxido solúvel
BR112013001335A2 (pt) processo de preparo de derivados de amino-benzoil-benzofurano
MX2013000295A (es) Procedimiento de preparacion de un inhibidor especifico de la trombina.
BR112013031405A2 (pt) piridopirazinas substituídas como novos inibidores de syk
BR112014010644A2 (pt) novos derivados de aril-quinolina
JO3143B1 (ar) مركبات تتراهيدرو بيرولو ثيازين
FR2952933B1 (fr) Precurseurs biscarbonates, leur procede de preparation et leurs utilisations
IN2014DN00144A (es)
UA111868C2 (uk) Спосіб одержання естерів (5-фтор-2-метил-3-хінолін-2-ілметиліндол-1-іл)-оцтової кислоти
BR112013015604A2 (pt) novo derivado de isoquinolina substituído
TR201902752T4 (tr) Oftalmik formülasyon.
IN2014MN00850A (es)
MX2013000294A (es) Intermedios y procedimiento de preparación de un inhibidor específico de la trombina.
MX343077B (es) Nuevo derivado de octahidrotienoquinolina, composicion farmaceutica que comprende el derivado, y uso de los mismos.
MY164880A (en) Process for the preparation of isoxazolyl-methoxy-nicotinic acids
MX2010009926A (es) Nuevo proceso para la preparacion de derivados de acido ciclohexancarboxilico.
MX2013005966A (es) Nuevos compuestos de benzofurano.
SE1100784A1 (sv) Ny fosfatförening
AR077332A1 (es) Procesos para la alquilacion de pirazoles
MX2013009386A (es) Nuevos compuestos de azaespirodecanona.

Legal Events

Date Code Title Description
FA Abandonment or withdrawal