PE20121311A1 - Derivados del acido carbamoil-metil-amino-acetico sustituido como inhibidores de nep novedosos - Google Patents

Derivados del acido carbamoil-metil-amino-acetico sustituido como inhibidores de nep novedosos

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Publication number
PE20121311A1
PE20121311A1 PE2012000661A PE2012000661A PE20121311A1 PE 20121311 A1 PE20121311 A1 PE 20121311A1 PE 2012000661 A PE2012000661 A PE 2012000661A PE 2012000661 A PE2012000661 A PE 2012000661A PE 20121311 A1 PE20121311 A1 PE 20121311A1
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PE
Peru
Prior art keywords
amino
alkyl
ethyl
nep
carbamoyl
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PE2012000661A
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English (en)
Inventor
Yuki Iwaki
Toshio Kawanami
Gary Michael Ksander
Muneto Mogi
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Novartis Ag
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Publication date
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of PE20121311A1 publication Critical patent/PE20121311A1/es

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Abstract

REFERIDA A UN COMPUESTO DERIVADO DE ACIDO CARBAMOIL-METIL-AMINO-ACETICO DE FORMULA (I'), DONDE X1 ES OH, O-ALQUILO C1-C7, NHS(O)2-ALQUILO C1-C7, ENTRE OTROS; R1 ES H, ALQUILO C1-C6, ARILO C6-C10-ALQUILO C1-C6, ENTRE OTROS; R2 ES ALCOXILO C1-C6, OH, HALOGENO, ALQUILO C1-C6, ENTRE OTROS; A2 ES O O NR5; R4 Y R5 SON H O ALQUILO C1-C6; A1 ES UN ENLACE O ALQUILENO C1-C3; R3 ES ARILO C6-C10, HETEROARILO DE 5 O 6 MIEMBROS, ENTRE OTROS; R6 ES HALOGENO, OH, ALCOXILO C1-C7, HALOGENO, ENTRE OTROS; m ES UN ENTERO DE 0 A 5; s ES UN ENTERO DE 0 A 4. SON COMPUESTOS PREFERIDOS: TERBUTIL-ESTER DEL ACIDO (S)-2-[(S)-2-(2',5'-DICLORO-BIFENIL-4-IL)-1-(1H-TETRAZOL-5-ILCARBAMOIL)-ETIL-AMINO]-PROPIONICO, ETIL-ESTER DEL ACIDO (S)-3-BENCILOXI-2-[(S)-2-(3'-CLORO-BIFENIL-4-IL)-1-(1H-TETRAZOL-5-IL-CARBAMOIL)-ETIL-AMINO]-PROPIONICO, TERBUTIL-ESTER DEL ACIDO (S)-2-[(R)-2-(2',5'-DICLORO-BIFENIL-4-IL)-1-(1H-TETRAZOL-5-IL-CARBAMOIL)-ETIL-AMINO]-PROPIONICO, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA ENDOPEPTIDASA NEUTRA (NEP) Y SON UTILES EN EL TRATAMIENTO DE HIPERTENSION, INSUFICIENCIA CARDIACA CONGESTIVA, SINDROME NEFROTICO, FIBROSIS RENAL, ENTRE OTROS
PE2012000661A 2009-11-20 2010-11-18 Derivados del acido carbamoil-metil-amino-acetico sustituido como inhibidores de nep novedosos PE20121311A1 (es)

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US26313709P 2009-11-20 2009-11-20
US35991410P 2010-06-30 2010-06-30

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PE20121311A1 true PE20121311A1 (es) 2012-10-12

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Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2010251967B9 (en) * 2009-05-28 2014-04-03 Novartis Ag Substituted aminopropionic derivatives as neprilysin inhibitors
EA201101672A1 (ru) 2009-05-28 2012-06-29 Новартис Аг Замещенные производные аминомасляной кислоты в качестве ингибиторов неприлизина
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
CA2817368C (en) 2010-12-15 2019-12-31 Theravance, Inc. Neprilysin inhibitors
AR084290A1 (es) 2010-12-15 2013-05-08 Theravance Inc Inhibidores de neprilisina, metodos para su preparacion e intermediarios utilizados en los mismos, composiciones farmaceuticas que los comprenden y su uso en la fabricacion de medicamentos para tratar enfermedades mediadas por la inhibicion de nep
US8449890B2 (en) 2011-02-17 2013-05-28 Theravance, Inc. Neprilysin inhibitors
ES2582640T3 (es) 2011-02-17 2016-09-14 Theravance Biopharma R&D Ip, Llc Derivados aminobutíricos sustituidos como inhibidores de neprilisina
CN103748070B (zh) 2011-05-31 2015-06-24 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
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
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
PT2864292T (pt) 2012-06-08 2017-07-10 Theravance Biopharma R&D Ip Llc Inibidores de neprisilina
US8871792B2 (en) 2012-06-08 2014-10-28 Theravance Biopharma R&D Ip, Llc Neprilysin inhibitors
US9126956B2 (en) 2012-08-08 2015-09-08 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
JP6301371B2 (ja) * 2013-02-14 2018-04-11 ノバルティス アーゲー インビボ効力が改善されたｎｅｐ阻害剤としての置換ビスフェニルブタン酸誘導体
CA2902456A1 (en) 2013-03-05 2014-09-12 Theravance Biopharma R&D Ip, Llc Neprilysin inhibitors
PE20160991A1 (es) 2013-07-25 2016-10-15 Novartis Ag Bioconjugados de polipeptidos de apelina sintetica
CN105612172A (zh) 2013-07-25 2016-05-25 诺华股份有限公司 用于治疗心力衰竭的环状多肽
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
MX2016009760A (es) 2014-01-30 2016-11-08 Theravance Biopharma R&D Ip Llc Inhibidores de neprilisina.
BR112017014194A2 (pt) 2015-01-23 2018-01-09 Novartis Ag conjugados de ácido graxo de apelina sintéticos com meia-vida melhorada
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
HUE052732T2 (hu) 2015-02-19 2021-05-28 Theravance Biopharma R&D Ip Llc (2R,4R)-5-(5'-klór-2'-fluorbifenil-4-il)-2-hidroxi-4-[(5-metiloxazol-2-karbonil)amino]pentánsav
CA3015505C (en) 2016-03-08 2024-03-05 Theravance Biopharma R&D Ip, Llc Crystalline (2s,4r)-5-(5'-chloro-2'-fluoro-[1,1'-biphenyl]-4-yl)-2-(ethoxymethyl)-4-(3-hydroxyisoxazole-5-carboxamido)-2-methylpentanoic acid and uses thereof
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
EP3887363A1 (en) 2018-11-27 2021-10-06 Novartis AG Cyclic pentamer compounds as proprotein convertase subtilisin/kexin type 9 (pcsk9) inhibitors for the treatment of metabolic disorder
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
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
NL188162C (nl) 1978-11-25 1992-04-16 Nippon Kayaku Kk Werkwijze voor het bereiden van een bestatinederivaat.
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
GB2074571B (en) 1980-04-11 1984-02-15 Wellcome Found Alpha-benzyl-substituted amides
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
US4610816A (en) * 1980-12-18 1986-09-09 Schering Corporation Substituted dipeptides as inhibitors of enkephalinases
US4721726A (en) * 1980-12-18 1988-01-26 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
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
NZ201001A (en) * 1982-06-17 1986-02-21 Schering Corp Substituted dipeptide derivatives and method of preparation
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
PH22224A (en) 1983-01-28 1988-07-01 Schering Corp Phosphorus containing amide compounds and pharmaceutical compositions containing them
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
JP2848411B2 (ja) 1988-08-18 1999-01-20 サイオス インコーポレイテッド 心房性ナトリウム利尿ペプチドクリアランス阻害剤
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
ES2113879T3 (es) 1990-01-24 1998-05-16 Douglas I Buckley Analogos de glp-1 utiles para el tratamiento de diabetes.
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
PL170210B1 (pl) 1991-06-21 1996-11-29 Thomae Gmbh Dr K Sposób wytwarzania nowego kwasu (S)(+)-2-etoksy-4-/N-/1-(2-piperydynofenylo)-3-metylo- 1-butyloaminokarbonylometylo/-benzoesowego i jego soli PL
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
EP0618803A4 (en) 1991-12-19 1995-03-22 Southwest Found Biomed Res POLYPEPTIDE INHIBITING PROTEIN TRANSFER TO CHOLESTERYL ESTERS, ANTIBODIES AGAINST SYNTHETIC POLYPEPTIDE AND ANTI-ATHEROSCLEROSIS PROPHYLACTIC AND THERAPEUTIC 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
WO1994020457A1 (en) 1993-03-02 1994-09-15 G.D. Searle & Co. N-acyl beta amino acid derivatives useful as platelet aggregation inhibitors
IL111785A0 (en) 1993-12-03 1995-01-24 Ferring Bv Dp-iv inhibitors and pharmaceutical compositions containing them
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
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
KR100376150B1 (ko) * 1994-11-04 2003-11-01 산텐 세이야꾸 가부시키가이샤 히드록시기를함유하는1,3-디알킬우레아유도체
EP0798291B1 (en) * 1994-12-14 2002-09-11 Santen Pharmaceutical Co., Ltd. Novel 1,3-dialkylurea derivatives
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
DE19616486C5 (de) 1996-04-25 2016-06-30 Royalty Pharma Collection Trust Verfahren zur Senkung des Blutglukosespiegels in Säugern
IL118657A0 (en) 1996-06-14 1996-10-16 Arad Dorit Inhibitors for picornavirus proteases
WO1998009940A1 (en) 1996-09-04 1998-03-12 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
WO1998053817A1 (en) 1997-05-29 1998-12-03 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
DE69824037T2 (de) 1997-11-24 2005-06-02 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
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
GB2354440A (en) 1999-07-20 2001-03-28 Merck & Co Inc Aryl amides as cell adhesion inhibitors
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
US6509330B2 (en) * 2000-02-17 2003-01-21 Bristol-Myers Squibb Company Hydroxamic acid containing compounds useful as ACE inhibitors and/or NEP inhibotors
CA2405895A1 (en) 2000-04-12 2001-10-18 Ronald Edward Steele Combination of organic compounds
DK1335898T3 (da) 2000-09-29 2006-04-03 Topotarget Uk Ltd Carbaminsyreforbindelser omfattende en amidbinding som HDAC-inhibitorer
BRPI0306907B8 (pt) 2002-01-17 2021-05-25 Novartis Ag composição farmacêutica, que compreende valsartan e inibidor de nep ou seus sais
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
ATE335744T1 (de) 2002-08-07 2006-09-15 Novartis Pharma Gmbh Organische verbindungen als mittel zur behandlung von aldosteronbedingten zuständen
PT1565463E (pt) 2002-11-18 2008-09-10 Novartis Ag Derivados de imidazo[1,5-a]piridina e métodos para tratar doenças mediadas pela aldosterona
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
EA200501715A1 (ru) 2003-04-30 2006-06-30 ДЗЕ ИНСТИТЬЮТС ФОР ФАРМАСЬЮТИКАЛ ДИСКАВЕРИ, ЭлЭлСи Замещённые аминокарбоновые кислоты в качестве ингибиторов протеинтирозинфосфатазы-1в
US20070197541A1 (en) 2003-07-29 2007-08-23 Oyelere Adegboyega K Biaryl heterocyclic amines,amides, and sulfur-containing compounds and methods of making and using the same
US7501538B2 (en) 2003-08-08 2009-03-10 Transtech Pharma, Inc. Aryl and heteroaryl compounds, compositions and methods of use
US20070208003A1 (en) 2004-03-26 2007-09-06 Bell Michael G Compounds and methods for treating dyslipidemia
UA90269C2 (ru) 2004-04-02 2010-04-26 Мицубиси Танабе Фарма Корпорейшн Тетрагидрохинолиновые производные и способ их получения
EP1765777A2 (en) 2004-05-28 2007-03-28 Speedel Experimenta AG Bicyclic, nitrogen-containing heterocycles as aromatase inhibitors
AR049388A1 (es) 2004-05-28 2006-07-26 Speedel Experimenta Ag Heterociclos como inhibidores de aldosterona sintasa
CA2568164A1 (en) 2004-05-28 2005-12-15 Speedel Experimenta Ag Heterocyclic compounds and their use as aldosterone synthase inhibitors
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
EP1778214A4 (en) 2004-07-27 2010-04-14 Glaxosmithkline Llc NEW 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
TW200804378A (en) 2005-12-09 2008-01-16 Speedel Experimenta Ag Organic compounds
WO2007116908A1 (ja) 2006-04-04 2007-10-18 Taiyo Nippon Sanso Corporation メタン分離方法、メタン分離装置及びメタン利用システム
TW200808813A (en) 2006-04-12 2008-02-16 Speedel Experimenta Ag Imidazo compounds
TW200808812A (en) 2006-04-12 2008-02-16 Speedel Experimenta Ag Imidazo compounds
AU2007333021A1 (en) 2006-05-15 2008-06-19 Irm Llc Terephthalamate compounds and compositions, and their use as HIV integrase inhibitors
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
RU2009110442A (ru) 2006-08-25 2010-09-27 Новартис АГ (CH) Конденсированные производные имидазола для лечения нарушений, опосредованных альдостеронсинтазой, и/или 11-бета-гидроксилазой, и/или ароматазой
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
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
CN101578272A (zh) 2006-12-18 2009-11-11 诺瓦提斯公司 1-取代的咪唑衍生物和它们作为醛固酮合酶抑制剂的用途
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
MY153432A (en) 2007-01-12 2015-02-13 Novartis Ag Process for preparing 5-biphenyl-4-amino-2-methyl pentanoic acid
TW200838501A (en) * 2007-02-02 2008-10-01 Theravance Inc Dual-acting antihypertensive agents
RU2009139811A (ru) 2007-03-29 2011-05-10 Новартис АГ (CH) Гетероциклические спиросоединения
TWI448284B (zh) * 2007-04-24 2014-08-11 Theravance Inc 雙效抗高血壓劑
ES2463693T3 (es) 2007-05-10 2014-05-29 R & D Biopharmaceuticals Gmbh Derivados de tubulisina
TWI406850B (zh) 2007-06-05 2013-09-01 Theravance Inc 雙效苯并咪唑抗高血壓劑
JP5653218B2 (ja) 2007-11-06 2015-01-14 ノバルティス アーゲー アンジオテンシン受容体アンタゴニスト／ブロッカーおよび中性エンドペプチダーゼ（ｎｅｐ）阻害剤の超構造に基づく二作用性医薬組成物
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
EP2334651A2 (en) 2008-07-24 2011-06-22 Theravance, Inc. Dual-acting antihypertensive agents
EA201101672A1 (ru) * 2009-05-28 2012-06-29 Новартис Аг Замещенные производные аминомасляной кислоты в качестве ингибиторов неприлизина
AU2010251967B9 (en) * 2009-05-28 2014-04-03 Novartis Ag Substituted aminopropionic derivatives as neprilysin inhibitors
CA2772681C (en) 2009-09-23 2017-01-03 Zhejiang Jiuzhou Pharmaceutical Co., Ltd. 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

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TN2012000125A1 (en) 2013-09-19
ECSP12011978A (es) 2012-07-31
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