CO6540001A2 - Derivados del ácido carbamoil-metil-amino -acçetico sustituido como inhibidores de nep novedosos. - Google Patents

Derivados del ácido carbamoil-metil-amino -acçetico sustituido como inhibidores de nep novedosos.

Info

Publication number
CO6540001A2
CO6540001A2 CO12076695A CO12076695A CO6540001A2 CO 6540001 A2 CO6540001 A2 CO 6540001A2 CO 12076695 A CO12076695 A CO 12076695A CO 12076695 A CO12076695 A CO 12076695A CO 6540001 A2 CO6540001 A2 CO 6540001A2
Authority
CO
Colombia
Prior art keywords
novelable
acçetico
carbamoil
metil
nep
Prior art date
Application number
CO12076695A
Other languages
English (en)
Inventor
Yuki Iwaki
Toshio Kawanami
Gary Michael Ksander
Muneto Mogi
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 CO6540001A2 publication Critical patent/CO6540001A2/es

Links

Classifications

    • 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
    • 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
    • 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
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • 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
    • A61P15/06—Antiabortive agents; Labour repressants
    • 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
    • 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
    • A61P25/18—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
    • A61P3/02—Nutrients, e.g. vitamins, minerals
    • 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
    • A61P3/08—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
    • A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium 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
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/28—Antiandrogens
    • 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
    • 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
    • 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
    • A61P9/10—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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
    • C07D231/38—Nitrogen atoms
    • C07D231/40—Acylated on said nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D257/04—Five-membered rings
    • C07D257/06—Five-membered rings with nitrogen atoms directly attached to the ring carbon atom
    • 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
    • C07D261/14—Nitrogen atoms

Abstract

La presente invención proporciona un compuesto de la fórmula Io una sal farmacéuticamente aceptable del mismo, en donde R1, R2, R3, R4, R6, A1, A2, X1, s y m se definen en la presente. La invención también se refiere a un método para la elaboración de los compuestos de la invención, y a sus usos terapéuticos. La presente invención proporciona además una combinación de agentes farmacológicamente activos y una composición farmacéutica.
CO12076695A 2009-11-20 2012-05-10 Derivados del ácido carbamoil-metil-amino -acçetico sustituido como inhibidores de nep novedosos. CO6540001A2 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US26313709P 2009-11-20 2009-11-20
US35991410P 2010-06-30 2010-06-30

Publications (1)

Publication Number Publication Date
CO6540001A2 true CO6540001A2 (es) 2012-10-16

Family

ID=43431937

Family Applications (1)

Application Number Title Priority Date Filing Date
CO12076695A CO6540001A2 (es) 2009-11-20 2012-05-10 Derivados del ácido carbamoil-metil-amino -acçetico sustituido como inhibidores de nep novedosos.

Country Status (37)

Country Link
US (4) US8222286B2 (es)
EP (2) EP2735561B1 (es)
JP (2) JP5543609B2 (es)
KR (1) KR101460421B1 (es)
CN (1) CN102666493B (es)
AR (1) AR079061A1 (es)
AU (1) AU2010320930B2 (es)
BR (1) BR112012011977A2 (es)
CA (1) CA2780150C (es)
CL (1) CL2012001298A1 (es)
CO (1) CO6540001A2 (es)
CR (1) CR20120237A (es)
DK (1) DK2501683T3 (es)
EA (1) EA021479B1 (es)
EC (1) ECSP12011978A (es)
ES (2) ES2481890T3 (es)
GT (1) GT201200153A (es)
HK (1) HK1170475A1 (es)
HN (1) HN2012001037A (es)
HR (1) HRP20140691T1 (es)
IL (1) IL219314A0 (es)
IN (1) IN2012DN02465A (es)
JO (1) JO2967B1 (es)
MA (1) MA33886B1 (es)
MX (1) MX2012005813A (es)
MY (1) MY158299A (es)
NZ (1) NZ599136A (es)
PE (1) PE20121311A1 (es)
PL (1) PL2501683T3 (es)
PT (1) PT2501683E (es)
RS (1) RS53422B (es)
SI (1) SI2501683T1 (es)
TN (1) TN2012000125A1 (es)
TW (1) TWI481598B (es)
UY (1) UY33044A (es)
WO (1) WO2011061271A1 (es)
ZA (1) ZA201202018B (es)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102448928B (zh) 2009-05-28 2014-10-01 诺华股份有限公司 作为中性溶酶(neprilysin)抑制剂的取代的氨基丁酸衍生物
ES2602902T3 (es) 2009-05-28 2017-02-22 Novartis Ag Derivados aminopropiónicos sustituidos como inhibidores de neprilisina
JO2967B1 (en) * 2009-11-20 2016-03-15 نوفارتس ايه جي Acetic acid derivatives of carbamoyl methyl amino are substituted as new NEP inhibitors
US8993631B2 (en) * 2010-11-16 2015-03-31 Novartis Ag Method of treating contrast-induced nephropathy
WO2012082857A1 (en) 2010-12-15 2012-06-21 Theravance, Inc. Neprilysin inhibitors
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
CA2825737C (en) 2011-02-17 2018-11-13 Theravance, Inc. Substituted aminobutyric derivatives as neprilysin inhibitors
CN103582630B (zh) 2011-05-31 2016-08-17 施万生物制药研发Ip有限责任公司 脑啡肽酶抑制剂
CA2835216A1 (en) 2011-05-31 2012-12-06 Theravance, Inc. Neprilysin inhibitors
JP5885832B2 (ja) 2011-05-31 2016-03-16 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
EP2855464B1 (en) 2012-05-31 2016-10-26 Theravance Biopharma R&D IP, LLC Nitric oxide donor neprilysin inhibitors
NZ723772A (en) 2012-06-08 2017-06-30 Theravance Biopharma R&D Ip Llc Neprilysin inhibitors
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
EP2882716B9 (en) 2012-08-08 2018-12-26 Theravance Biopharma R&D IP, LLC Neprilysin inhibitors
UY35144A (es) 2012-11-20 2014-06-30 Novartis Ag Miméticos lineales sintéticos de apelina para el tratamiento de insuficiencia cardiaca
PE20151666A1 (es) 2013-02-14 2015-11-19 Novartis Ag Derivados sustituidos del acido bisfenil butanoico fosfonico como inhibidores de la nep
MX2015010434A (es) * 2013-02-14 2015-10-05 Novartis Ag Derivados de acido bisfenil-butanoico sustituido como inhibidores de la endopeptidasa neutra (nep), con una mayor eficacia in vivo.
SI2964616T1 (sl) 2013-03-05 2017-08-31 Theravance Biopharma R&D Ip, Llc Zaviralci neprilizina
TW201536814A (zh) 2013-07-25 2015-10-01 Novartis Ag 用於治療心臟衰竭之合成環狀多肽
MX2016001021A (es) 2013-07-25 2016-08-03 Novartis Ag Bioconjugados de polipeptidos de apelina sinteticos.
RU2016135057A (ru) 2014-01-30 2018-03-12 ТЕРЕВАНС БАЙОФАРМА Ар энд Ди АйПи, ЭлЭлСи Производные 5-бифенил-4-гетероарилкарбониламинопентановой кислоты в качестве ингибиторов неприлизина
US9593110B2 (en) 2014-01-30 2017-03-14 Theravence Biopharma R&D IP, LLC Neprilysin inhibitors
BR112017014194A2 (pt) 2015-01-23 2018-01-09 Novartis Ag conjugados de ácido graxo de apelina sintéticos com meia-vida melhorada
CN107257785B (zh) 2015-02-11 2020-07-07 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(2s,4r)-5-(5’-氯-2’-氟联苯-4-基)-4-(乙氧基草酰基氨基)-2-羟甲基-2-甲基戊酸
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
CN108779084A (zh) 2016-03-08 2018-11-09 施万生物制药研发Ip有限责任公司 结晶型(2s,4r)-5-(5′-氯-2′-氟-[1,1′-联苯]-4-基)-2-(乙氧基甲基)-4-(3-羟基异恶唑-5-甲酰氨基)-2-甲基戊酸和其用途
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
JP2022507958A (ja) 2018-11-27 2022-01-18 ノバルティス アーゲー 代謝障害の治療用のプロタンパク質転換酵素サブチリシン／ケキシン９型（ｐｃｓｋ９）阻害薬としての環状四量体化合物
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
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
WO2020254553A1 (en) 2019-06-19 2020-12-24 Nmd Pharma A/S Compounds for the treatment of neuromuscular disorders
WO2023084449A1 (en) 2021-11-12 2023-05-19 Novartis Ag Diaminocyclopentylpyridine derivatives for the treatment of a disease or disorder

Family Cites Families (133)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1182125A (en) 1978-11-25 1985-02-05 Hamao Umezawa Process for producing threo-3-amino-2- hydroxybutanoyl-aminoacetic acids, as well as novel intermediates therefor and process for producing them
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
IT1148006B (it) 1980-04-11 1986-11-26 Wellcome Found Ammidi dotate di proprieta' farmaceutiche e loro preparazione
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
IE53315B1 (en) * 1980-12-18 1988-10-12 Schering Corp Substituted dipeptides,processes for their preparation and pharmaceutical compositions containing them and their use in the inhibition of enkephalinase
US4721726A (en) * 1980-12-18 1988-01-26 Schering Corporation Substituted dipeptides as inhibitors of enkephalinases
US4610816A (en) * 1980-12-18 1986-09-09 Schering Corporation Substituted dipeptides as inhibitors of enkephalinases
JPS5865260A (ja) 1981-10-13 1983-04-18 Microbial Chem Res Found ３−アミノ−２−ヒドロキシ−４−フエニル酪酸誘導体および医薬組成物
FR2518088B1 (fr) 1981-12-16 1987-11-27 Roques Bernard Nouveaux derives d'aminoacides, et leur application therapeutique
NZ201001A (en) * 1982-06-17 1986-02-21 Schering Corp Substituted dipeptide derivatives and method of preparation
EP0103077B1 (en) 1982-06-17 1988-05-18 Schering Corporation Substituted dipeptides, methods for their production, pharmaceutical compositions containing them, method for making such pharmaceutical compositions
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
US4617307A (en) 1984-06-20 1986-10-14 Ciba-Geigy Corporation Substituted imidazo[1,5-A]pyridine derivatives as aromatase inhibitors
DK31784A (da) 1983-01-28 1984-07-29 Schering Corp Phosphorholdige amidforbindelser, farmaceutiske kompositioner indeholdende disse, og fremgangsmaader til forbindelsernes fremstilling
US4559332A (en) 1983-04-13 1985-12-17 Ciba Geigy Corporation 20-Spiroxanes and analogues having an open ring E, processes for their manufacture, and pharmaceutical preparations thereof
EP0136883B1 (en) 1983-10-03 1987-11-25 E.R. Squibb & Sons, Inc. Enkephalinase inhibitors
DE3347565A1 (de) 1983-12-30 1985-07-11 Thomae Gmbh Dr K Neue phenylessigsaeurederivate, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung
JPS60248659A (ja) * 1984-05-25 1985-12-09 Microbial Chem Res Found ３−〔ｎ−（メルカプトアシル）〕アミノ−４−アリ−ル酪酸誘導体及びそれを有効成分とする鎮痛剤
JPS6354321A (ja) 1985-03-27 1988-03-08 Ajinomoto Co Inc 血糖降下剤
FR2597865B1 (fr) 1986-04-29 1990-11-09 Roussel Uclaf Nouveaux derives d'un acide benzyl alkyl carboxylique substitue par un radical 4-pyridinyl aminocarbonyle, leur procede de preparation, les nouveaux intermediaires obtenus, leur application a titre de medicaments et les compositions pharmaceutiques les renfermant
US5120712A (en) 1986-05-05 1992-06-09 The General Hospital Corporation Insulinotropic hormone
US5118666A (en) 1986-05-05 1992-06-02 The General Hospital Corporation Insulinotropic hormone
FR2605004B1 (fr) 1986-09-25 1989-01-13 Centre Nat Rech Scient Nouveaux derives d'amino-acides, leur procede de preparation et composition pharmaceutiques les contenant
CA1337400C (en) 1987-06-08 1995-10-24 Norma G. Delaney Inhibitors of neutral endopeptidase
EP0429537A4 (en) * 1988-08-18 1991-08-21 California Biotechnology, Inc. Atrial natriuretic peptide clearance inhibitors
FR2651229B1 (fr) 1989-08-24 1991-12-13 Inst Nat Sante Rech Med Nouveaux derives d'amino-acides, leur procede de preparation et leur application therapeutique.
FR2652087B1 (fr) * 1989-09-15 1993-10-15 Bioprojet Ste Civile Derives d'amino-acides, leur procede de preparation et leurs applications therapeutiques.
US5407960A (en) 1989-12-22 1995-04-18 Schering Corporation Mercaptocycloacyl aminoacid endopeptidase inhibitors
ATE164852T1 (de) 1990-01-24 1998-04-15 Douglas I Buckley Glp-1-analoga verwendbar in der diabetesbehandlung
US5223516A (en) * 1990-03-22 1993-06-29 E. R. Squibb & Sons, Inc. 3,3,3-trifluoro-2-mercaptomethyl-N-tetrazolyl substituted propanamides and method of using same
US5200426A (en) * 1990-08-14 1993-04-06 Board Of Regents, The University Of Texas Inhibitors of neutral endopeptidase/CALLA as chemotherapeutic agents
JPH04149166A (ja) 1990-10-12 1992-05-22 Nippon Kayaku Co Ltd 新規ケト酸アミド誘導体
CA2058797A1 (en) 1991-02-01 1992-08-02 Michael John Broadhurst Amino acid derivatives
AU654331B2 (en) 1991-03-30 1994-11-03 Kissei Pharmaceutical Co. Ltd. Succinic acid compounds
US5294632A (en) * 1991-05-01 1994-03-15 Ciba-Geigy Corporation Phosphono/biaryl substituted dipetide derivatives
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
AU660930B2 (en) 1991-06-21 1995-07-13 Novo Nordisk A/S (S)(+)-2-ethoxy-4-(N-(1-(2-piperidinophenyl)-3-methyl-1- butyl)aminocarbonylmethyl)benzoic acid
GB9114006D0 (en) 1991-06-28 1991-08-14 Fujisawa Pharmaceutical Co New propionamide derivatives,processes for the preparation thereof and pharmaceutical composition comprising the same
ES2100291T3 (es) 1991-07-30 1997-06-16 Ajinomoto Kk Cristales de n-(trans-4-isopropilciclohexilcarbonil)-d-fenilalanina y metodos para prepararlos.
EP0533130A1 (de) 1991-09-19 1993-03-24 Hoechst Aktiengesellschaft 2-Hydroxymethylpyridine, die entsprechenden Pyridin-N-oxide und ihre Derivate, Verfahren zu ihrer Herstellung sowie deren Verwendung
CA2078759C (en) 1991-09-27 2003-09-16 Alan M. Warshawsky Novel carboxyalkyl derivatives useful as inhibitors of enkephalinase and ace
US5273990A (en) * 1992-09-03 1993-12-28 Ciba-Geigy Corporation Phosphono substituted tetrazole derivatives
US5250522A (en) * 1992-10-09 1993-10-05 Ciba-Geigy Corporation Phosphono/biaryl substituted amino acid derivatives
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
JPH06234630A (ja) 1992-12-17 1994-08-23 Tanabe Seiyaku Co Ltd 中性メタロエンドペプチダーゼ阻害剤
AU6267894A (en) 1993-03-02 1994-09-26 G.D. Searle & Co. N-acyl beta amino acid derivatives useful as platelet aggregation inhibitors
JP3576193B2 (ja) 1993-12-03 2004-10-13 第一製薬株式会社 ビフェニルメチル置換バレリルアミド誘導体
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
US5517996A (en) * 1994-04-21 1996-05-21 Hitachi Medical Corporation Ultrasonic diagnostic apparatus
IT1270261B (it) 1994-06-21 1997-04-29 Zambon Spa Derivati peptidici ad attivita' inibitrice delle metallopeptidasi
US5512549A (en) 1994-10-18 1996-04-30 Eli Lilly And Company Glucagon-like insulinotropic peptide analogs, compositions, and methods of use
CN1055681C (zh) * 1994-11-04 2000-08-23 参天制药株式会社 带有羟基的新1,3－二烷基脲衍生物
WO1996018606A1 (fr) * 1994-12-14 1996-06-20 Santen Pharmaceutical Co., Ltd. Nouveaux derives 1,3-dialkyluree
TW313568B (es) 1994-12-20 1997-08-21 Hoffmann La Roche
US5550119A (en) * 1995-03-02 1996-08-27 Ciba-Geigy Corporation Phosphono substituted tetrazole derivatives as ECE inhibitors
US5703092A (en) * 1995-04-18 1997-12-30 The Dupont Merck Pharmaceutical Company Hydroxamic acid compounds as metalloprotease and TNF inhibitors
US5710171A (en) * 1995-05-24 1998-01-20 Merck & Co., Inc. Bisphenyl inhibitors of farnesyl-protein transferase
DE122010000020I1 (de) 1996-04-25 2010-07-08 Prosidion Ltd Verfahren zur Senkung des Blutglukosespiegels in Säugern
IL118657A0 (en) 1996-06-14 1996-10-16 Arad Dorit Inhibitors for picornavirus proteases
EP0927156A1 (en) 1996-09-04 1999-07-07 Warner-Lambert Company Biphenyl butyric acids and their derivatives as inhibitors of matrix metalloproteinases
FR2755135B1 (fr) 1996-10-25 2002-12-27 Inst Nat Sante Rech Med Nouveaux derives d'(alpha-aminophosphino)peptides, leur procede de preparation et les compositions qui les contiennent
TW492957B (en) 1996-11-07 2002-07-01 Novartis Ag N-substituted 2-cyanopyrrolidnes
AU726585B2 (en) 1997-05-29 2000-11-09 Merck & Co., Inc. Biarylalkanoic acids as cell adhesion inhibitors
AU1411499A (en) 1997-11-20 1999-06-15 Merck & Co., Inc. Para-aminomethylaryl carboxamide derivatives
AU1463499A (en) 1997-11-21 1999-06-15 Merck & Co., Inc. Substituted pyrrole derivatives as cell adhesion inhibitors
ATE267168T1 (de) 1997-11-24 2004-06-15 Merck & Co Inc Beta-alanin-derivate als zell-adhäsions- inhibitoren
MY153569A (en) 1998-01-20 2015-02-27 Mitsubishi Tanabe Pharma Corp Inhibitors of ?4 mediated cell adhesion
US6169103B1 (en) * 1998-03-03 2001-01-02 Warner-Lambert Fluorine-substituted biphenyl butyric acids and their derivatives as inhibitors of matrix metalloproteinases
GT199900147A (es) 1998-09-17 1999-09-06 1, 2, 3, 4- tetrahidroquinolinas 2-sustituidas 4-amino sustituidas.
US6197786B1 (en) 1998-09-17 2001-03-06 Pfizer Inc 4-Carboxyamino-2-substituted-1,2,3,4-tetrahydroquinolines
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
GB2354440A (en) 1999-07-20 2001-03-28 Merck & Co Inc Aryl amides as cell adhesion inhibitors
US6677341B2 (en) 1999-09-23 2004-01-13 Pharmacia Corporation (R)-Chiral halogenated substituted heteroaryl benzyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity
US6509330B2 (en) * 2000-02-17 2003-01-21 Bristol-Myers Squibb Company Hydroxamic acid containing compounds useful as ACE inhibitors and/or NEP inhibotors
SK14612002A3 (sk) 2000-04-12 2003-05-02 Novartis Ag Farmaceutická kompozícia obsahujúca inhibítor aldosterónsyntázy prípadne v kombinácii s antagonistom AT1-receptora a jej použitie
DE60138658D1 (de) 2000-09-29 2009-06-18 Topotarget Uk Ltd Carbaminsäurederivate enthaltend eine Amidgruppe zur Behandlung von Malaria
CA2472399C (en) 2002-01-17 2012-02-21 Novartis Ag Pharmaceutical compositions comprising valsartan and nep inhibitors
JP4233353B2 (ja) 2002-02-27 2009-03-04 田辺三菱製薬株式会社 医薬組成物
US20040063761A1 (en) * 2002-08-06 2004-04-01 Kuduk Scott D. 2-(biarylalkyl)amino-3-(fluoroalkanoylamino)pyridine derivatives
EP1537114B8 (en) 2002-08-07 2007-10-03 Novartis AG Organic compounds as agents for the treatment of aldosterone mediated conditions
EP1565463B1 (en) 2002-11-18 2008-06-11 Novartis AG Imidazo[1,5a] pyridine derivatives and methods for treating aldosterone mediated diseases
US20040142379A1 (en) 2003-01-16 2004-07-22 Carlsberg Research Laboratory Affinity fishing for ligands and proteins receptors
JP2007524596A (ja) 2003-02-28 2007-08-30 トランスフォーム・ファーマシューティカルズ・インコーポレイテッド 共結晶医薬組成物
MXPA05011537A (es) 2003-04-30 2006-01-23 Inst For Pharm Discovery Inc Acidos aminocaboxilicos sustituidos.
WO2005012270A2 (en) 2003-07-29 2005-02-10 Rib-X Pharmaceuticals, Inc. Biaryl heterocyclic amines, amides, and sulfur-containing compounds and methods of making and using the same
WO2005014534A1 (en) 2003-08-08 2005-02-17 Transtech Pharma, Inc. Aryl and heteroaryl compounds, compositions, and methods of use
KR20070007112A (ko) 2004-03-26 2007-01-12 일라이 릴리 앤드 캄파니 이상지혈증 치료를 위한 화합물 및 방법
UA90269C2 (ru) 2004-04-02 2010-04-26 Мицубиси Танабе Фарма Корпорейшн Тетрагидрохинолиновые производные и способ их получения
JP2008500997A (ja) 2004-05-28 2008-01-17 シュペーデル・エクスペリメンタ・アーゲー アロマターゼ阻害剤としての二環式の窒素含有複素環
BRPI0510412A (pt) 2004-05-28 2007-10-23 Speedel Experimenta Ag compostos orgánicos
JP2008500998A (ja) 2004-05-28 2008-01-17 シュペーデル・エクスペリメンタ・アーゲー 複素環式化合物およびアルドステロンシンターゼ阻害薬としてのそれらの使用
AR049711A1 (es) 2004-07-09 2006-08-30 Speedel Experimenta Ag Compuestos heterociclicos condensados como inhibidores de la aldosterona sintasa; composiciones farmaceuticas que los contienen y su uso en la preparacion de un medicamento para el tratamiento o prevencion de enfermedades relacionadas con el hiperaldosterismo y por una liberacion excesiva de cortiso
US20070265345A1 (en) 2004-07-27 2007-11-15 Smithkline Beecham Corporation Novel Biphenyl Compounds And Their Use
WO2006015885A1 (en) 2004-08-13 2006-02-16 University College Dublin, National University Of Ireland, Dublin Amino acid dehydrogenase-derived biocatalysts
EP1814869A2 (en) 2004-11-18 2007-08-08 The Institutes for Pharmaceutical Discovery, LLC Substituted amino acids as protein tyrosine phosphatase inhibitors
WO2006069096A1 (en) 2004-12-20 2006-06-29 Pharmacyclics, Inc. Silanol derivatives as inhibitors of histone deacetylase
MY146830A (en) * 2005-02-11 2012-09-28 Novartis Ag Combination of organic 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
TW200716634A (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
KR20080066776A (ko) 2005-11-08 2008-07-16 노파르티스 아게 안지오텐신 ⅱ 수용체 봉쇄제, 칼슘 채널 봉쇄제 및 다른활성 약제의 조합물
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
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
JP2009537521A (ja) 2006-05-15 2009-10-29 アイアールエム・リミテッド・ライアビリティ・カンパニー テレフタラメート化合物および組成物、ならびにｈｉｖインテグラーゼ阻害剤としてのそれらの使用
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
CA2660701A1 (en) 2006-08-25 2008-03-06 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
MX2009006630A (es) 2006-12-18 2009-06-30 Novartis Ag Derivados de 4-imidazolil-1,2,3,4-tetrahidro-quinola y su uso como inhibidores de aldosterona / 11-beta-hidroxilasa.
JP2010513482A (ja) 2006-12-18 2010-04-30 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イミダゾール類
JP2010513560A (ja) 2006-12-18 2010-04-30 ノバルティス アーゲー １−置換イミダゾール誘導体およびアルドステロン合成阻害剤としてのその使用
RU2530900C2 (ru) 2007-01-12 2014-10-20 Новартис Аг Способ получения 5-бифенил-4-амино-2-метилпентановой кислоты
TW200838501A (en) * 2007-02-02 2008-10-01 Theravance Inc Dual-acting antihypertensive agents
ATE484507T1 (de) 2007-03-29 2010-10-15 Novartis Ag Heterocyclische spiroverbindungen
TWI448284B (zh) * 2007-04-24 2014-08-11 Theravance Inc 雙效抗高血壓劑
CA2723671C (en) 2007-05-10 2018-06-19 R & D Biopharmaceuticals Gmbh Tubulysine derivatives
TWI406850B (zh) 2007-06-05 2013-09-01 Theravance Inc 雙效苯并咪唑抗高血壓劑
SI2217205T1 (sl) 2007-11-06 2015-10-30 Novartis Ag Farmacevtske sestave na podlagi superstruktur zaviralca/blokatorja angiotenzinskih receptorjev (arb) in inhibitorja nevtralne endopeptidaze (nep)
US8212052B2 (en) 2007-12-11 2012-07-03 Theravance, Inc. Dual-acting benzoimidazole antihypertensive agents
EP2070928A1 (en) 2007-12-12 2009-06-17 NERVIANO MEDICAL SCIENCES S.r.l. 7-azaindol-3-ylacrylamides active as kinase inhibitors
PE20091364A1 (es) 2008-01-17 2009-10-13 Novartis Ag Proceso para la preparacion de inhibidores de nep
WO2010011821A2 (en) 2008-07-24 2010-01-28 Theravance, Inc. Dual-acting antihypertensive agents
CN102448928B (zh) * 2009-05-28 2014-10-01 诺华股份有限公司 作为中性溶酶(neprilysin)抑制剂的取代的氨基丁酸衍生物
ES2602902T3 (es) * 2009-05-28 2017-02-22 Novartis Ag Derivados aminopropiónicos sustituidos como inhibidores de neprilisina
AU2010297892B2 (en) 2009-09-23 2014-02-06 Novartis Ag Process for manufacture of N-acylbphenyl alanine
JO2967B1 (en) * 2009-11-20 2016-03-15 نوفارتس ايه جي Acetic acid derivatives of carbamoyl methyl amino are substituted as new NEP inhibitors

Also Published As

Publication number Publication date
NZ599136A (en) 2013-07-26
CL2012001298A1 (es) 2012-10-05
HK1170475A1 (en) 2013-03-01
HRP20140691T1 (hr) 2014-10-24
US20120202862A1 (en) 2012-08-09
SI2501683T1 (sl) 2014-07-31
EA021479B1 (ru) 2015-06-30
MA33886B1 (fr) 2013-01-02
PT2501683E (pt) 2014-07-24
RS53422B (en) 2014-12-31
US20140088165A1 (en) 2014-03-27
EP2735561A1 (en) 2014-05-28
PE20121311A1 (es) 2012-10-12
EA201200763A1 (ru) 2012-12-28
JP2014167015A (ja) 2014-09-11
TW201121949A (en) 2011-07-01
EP2501683A1 (en) 2012-09-26
IL219314A0 (en) 2012-06-28
ZA201202018B (en) 2012-11-28
PL2501683T3 (pl) 2014-09-30
JO2967B1 (en) 2016-03-15
US8877786B2 (en) 2014-11-04
JP5543609B2 (ja) 2014-07-09
US20110124695A1 (en) 2011-05-26
CA2780150C (en) 2017-10-17
KR20120084327A (ko) 2012-07-27
CR20120237A (es) 2012-06-07
KR101460421B1 (ko) 2014-11-10
CA2780150A1 (en) 2011-05-26
EP2735561B1 (en) 2016-07-20
CN102666493B (zh) 2015-09-23
UY33044A (es) 2011-06-30
JP2013510835A (ja) 2013-03-28
US20130096168A1 (en) 2013-04-18
HN2012001037A (es) 2015-08-10
TN2012000125A1 (en) 2013-09-19
CN102666493A (zh) 2012-09-12
AR079061A1 (es) 2011-12-21
ES2598961T3 (es) 2017-01-30
US8222286B2 (en) 2012-07-17
GT201200153A (es) 2014-12-30
WO2011061271A1 (en) 2011-05-26
ES2481890T3 (es) 2014-07-31
EP2501683B1 (en) 2014-04-23
AU2010320930B2 (en) 2014-05-15
MX2012005813A (es) 2012-06-12
BR112012011977A2 (pt) 2020-09-08
DK2501683T3 (da) 2014-06-30
MY158299A (en) 2016-09-30
TWI481598B (zh) 2015-04-21
AU2010320930A1 (en) 2012-04-12
ECSP12011978A (es) 2012-07-31
US8642635B2 (en) 2014-02-04
US8377978B2 (en) 2013-02-19
IN2012DN02465A (es) 2015-08-21

Similar Documents

Publication Publication Date Title
CO6540001A2 (es) Derivados del ácido carbamoil-metil-amino -acçetico sustituido como inhibidores de nep novedosos.
UY33731A (es) ?derivados de ácido amino-fenil-pentanoico sustituidos como inhibidores de nep?
UY32660A (es) Derivados aminobutricos sustituidos como inhibidores de neprilisina
CO6470847A2 (es) Derivados amino-propiónicos sustituidos como inhibidores de neprilisina
ECSP11011526A (es) Aril-piridinas como inhibidoras de sintasa de aldosterona
CR20140032A (es) Compuestos de tetrahidropirido-piridina y tetrahidropirido-pirimidina y su uso como modulares de receptores de c5a
CU20130082A7 (es) 1,2 oxazol-8-azabiciclo[3,2,1]octano 8 il como moduladores de fxr
UY33536A (es) INHIBIDORES BICÍCLICOS DE ACETIL-CoA-CARBOXILASA Y USOS DE LOS MISMOS
UY33075A (es) Derivados de ciclohexano y usos de los mismos
CR20150419A (es) Derivados sustituidos del ácido bisfenil butanóico fosfónico como inhibidores de la nep
UY32977A (es) Novedosos compuestos como inhibidores de la caseina quinasa
BR112014027359A2 (pt) moduladores da série de reação complementar e usos dos mesmos
CO6781541A2 (es) Derivados glucósidos y usos de los mismos
EA201101621A1 (ru) Производные бензоксазолона в качестве ингибиторов альдостеронсинтазы
EA201391524A1 (ru) Производные гликозида и их применение
UY33348A (es) Compuestos de furopiridina y usos de los mismos
UY35323A (es) Derivados sustituidos del ácido bisfenil butanóico como inhibidores de la nep con una mejorada efic acia in vivo
BR112013028197A2 (pt) compostos de benzofurano-piperidina
CU20120074A7 (es) Derivados del ácido carbamoil-metil-amino-acético sustituido como inhibidores de nep novedosos
UY33857A (es) Compuestos de tiofeno 2,3,5-trisustituidos y usos de los mismos.
AR078424A1 (es) Derivados de dihidroimidazoquinolina con actividad inhibitoria de tafia, composiciones farmaceuticas que los contienen y su uso como agentes terapeuticos o profilacticos para enfermedades tromboticas
CU23681B7 (es) Derivados de triazolopirazina