CU23967B1 - Derivados de pirazin-2-carboxamida para tratar enfermedades mediadas por el bloqueo del canal de sodio epitelial - Google Patents

Derivados de pirazin-2-carboxamida para tratar enfermedades mediadas por el bloqueo del canal de sodio epitelial

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Publication number
CU23967B1
CU23967B1 CU20100118A CU20100118A CU23967B1 CU 23967 B1 CU23967 B1 CU 23967B1 CU 20100118 A CU20100118 A CU 20100118A CU 20100118 A CU20100118 A CU 20100118A CU 23967 B1 CU23967 B1 CU 23967B1
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CU
Cuba
Prior art keywords
sodium channel
epitelial
pirazin
carboxamide
derivatives
Prior art date
Application number
CU20100118A
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English (en)
Other versions
CU20100118A7 (es
Inventor
Gurdip Bhalay
Emma Budd
Graham Charles Bloomfield
Stephen Paul Collingwood
Andrew Dunstan
Lee Edwards
Peter Gedeck
Catherine Howsham
Peter Hunt
Thomas Anthony Hunt
Paul Oakley
Nichola Smith
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.)
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Publication date
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of CU20100118A7 publication Critical patent/CU20100118A7/es
Publication of CU23967B1 publication Critical patent/CU23967B1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • 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
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/20—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10—Spiro-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Processing Or Creating Images (AREA)
  • Image Analysis (AREA)
  • Image Processing (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

Un compuesto de la fórmula I en forma libre o de sal o de solvato, en donde R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 y R11 tienen los significados indicados en la memoria descriptiva, es útil para el tratamiento de enfermedades que respondan al bloqueo del canal de sodio epitelial. También se describen composiciones farmacéuticas que contienen los compuestos, y procesos para la preparación de los compuestos. Las enfermedades que responden al bloqueo del canal de sodio epitelial (ENaC) son condiciones inflamatorias o alérgicas seleccionadas de: fibrosis quística, discinesia ciliar primaria, bronquitis crónica, enfermedad pulmonar obstructiva crónica, asma, infecciones del tracto respiratorio, carcinoma pulmonar, xerostomía y queratoconjuntivitis.
CU20100118A 2007-12-10 2010-06-10 Derivados de pirazin-2-carboxamida para tratar enfermedades mediadas por el bloqueo del canal de sodio epitelial CU23967B1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP07122739 2007-12-10
PCT/EP2008/067110 WO2009074575A2 (en) 2007-12-10 2008-12-09 Organic compounds

Publications (2)

Publication Number Publication Date
CU20100118A7 CU20100118A7 (es) 2011-10-14
CU23967B1 true CU23967B1 (es) 2013-12-27

Family

ID=39322745

Family Applications (1)

Application Number Title Priority Date Filing Date
CU20100118A CU23967B1 (es) 2007-12-10 2010-06-10 Derivados de pirazin-2-carboxamida para tratar enfermedades mediadas por el bloqueo del canal de sodio epitelial

Country Status (30)

Country Link
US (5) US8039472B2 (es)
EP (3) EP2231280B1 (es)
JP (1) JP5455922B2 (es)
KR (1) KR101578235B1 (es)
CN (1) CN101939054B (es)
AR (1) AR069637A1 (es)
AU (1) AU2008334629B2 (es)
BR (1) BRPI0820669A2 (es)
CA (1) CA2707857C (es)
CL (1) CL2008003651A1 (es)
CO (1) CO6310968A2 (es)
CR (1) CR11470A (es)
CU (1) CU23967B1 (es)
EA (1) EA017919B1 (es)
EC (1) ECSP10010242A (es)
ES (2) ES2602331T3 (es)
HN (1) HN2010001165A (es)
IL (1) IL206165A0 (es)
MA (1) MA31894B1 (es)
MX (1) MX2010006421A (es)
MY (1) MY152955A (es)
NZ (1) NZ585789A (es)
PE (1) PE20091096A1 (es)
PL (1) PL2444120T3 (es)
PT (1) PT2444120T (es)
TN (1) TN2010000256A1 (es)
TW (1) TWI439462B (es)
UA (1) UA104997C2 (es)
WO (1) WO2009074575A2 (es)
ZA (1) ZA201003837B (es)

Families Citing this family (90)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6858615B2 (en) 2002-02-19 2005-02-22 Parion Sciences, Inc. Phenyl guanidine sodium channel blockers
US8354427B2 (en) 2004-06-24 2013-01-15 Vertex Pharmaceutical Incorporated Modulators of ATP-binding cassette transporters
PL2444120T3 (pl) * 2007-12-10 2018-02-28 Novartis Ag Spirocyklicze analogi amiloridu jako blokery ENac
MX344703B (es) 2008-02-26 2017-01-03 Parion Sciences Inc Bloqueadores de canal de sodio poliaromaticos.
UA103198C2 (en) 2008-08-04 2013-09-25 Новартис Аг Squaramide derivatives as cxcr2 antagonists
US8664237B2 (en) * 2008-10-02 2014-03-04 The Johns Hopkins University Spiperone derivatives and methods of treating disorders
SI2349263T1 (sl) 2008-10-23 2014-09-30 Vertex Pharmaceuticals Incorporated Modulatorji cistiäśno-fibroznega transmembranskega regulatorja prevodnosti
SI2433940T1 (sl) 2009-04-28 2015-01-30 Chugai Seiyaku Kabushiki Kaisha Spiroimidazolonski derivat
WO2010138794A2 (en) 2009-05-29 2010-12-02 The University Of North Carolina At Chapel Hill Regulation of sodium channels by plunc proteins
CA2777245A1 (en) * 2009-10-22 2011-04-28 Vertex Pharmaceuticals Incorporated Compositions for treatment of cystic fibrosis and other chronic diseases
CN102666546B (zh) 2009-10-23 2015-09-09 沃泰克斯药物股份有限公司 N-(4-(7-氮杂双环[2.2.1]庚-7-基)-2-(三氟甲基)苯基)-4-氧代-5-(三氟甲基)-1,4-二氢喹啉-3-甲酰胺的固体形式
NZ600172A (en) 2009-10-23 2014-07-25 Vertex Pharma Process for preparing modulators of cystic fibrosis transmembrane conductance regulator
WO2011146886A1 (en) 2010-05-20 2011-11-24 Vertex Pharmaceuticals Incorporated Processes for producing modulators of cystic fibrosis transmembrane conductance regulator
US9050339B2 (en) 2010-09-17 2015-06-09 Novartis Ag Pyrazine derivatives as ENaC blockers
US8372845B2 (en) * 2010-09-17 2013-02-12 Novartis Ag Pyrazine derivatives as enac blockers
AR086745A1 (es) 2011-06-27 2014-01-22 Parion Sciences Inc 3,5-diamino-6-cloro-n-(n-(4-(4-(2-(hexil(2,3,4,5,6-pentahidroxihexil)amino)etoxi)fenil)butil)carbamimidoil)pirazina-2-carboxamida
SI2760821T1 (en) 2011-09-02 2018-02-28 Novartis Ag A salt salt of an anti-inflammatory substituted cyclobutenedione compound
MX2014005165A (es) 2011-11-02 2014-05-28 Boehringer Ingelheim Int Proceso novedoso para la preparacion de acilguanidinas y aciltioureas.
EA025158B9 (ru) 2011-11-02 2018-03-30 Бёрингер Ингельхайм Интернациональ Гмбх Гетероциклические соединения, лекарственные средства, содержащие указанные соединения, их применение и способы их получения
US8809340B2 (en) 2012-03-19 2014-08-19 Novartis Ag Crystalline form
WO2013155406A1 (en) * 2012-04-12 2013-10-17 The Chinese University Of Hong Kong Contragestion and treating inflammation by modulating sodium channel activity in the epithelium
EP2838882A1 (en) 2012-04-20 2015-02-25 Vertex Pharmaceuticals Incorporated Solid forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
EP2897940B1 (en) * 2012-09-24 2019-05-01 Boehringer Ingelheim International GmbH Heterocyclic compounds, medicaments containing said compounds, use thereof and processes for the preparation thereof
HUE070382T2 (hu) 2012-11-02 2025-06-28 Vertex Pharma Gyógyászati készítmények CFTR közvetített betegségek kezelésére
ES2663797T3 (es) 2012-12-10 2018-04-17 Chugai Seiyaku Kabushiki Kaisha Derivados de hidantoína
ES2674665T3 (es) 2012-12-17 2018-07-03 Parion Sciences, Inc. Compuestos de 3,5-diamino-6-cloro-N-(N-(4-fenilbutilo)carbamimidoilo)-pirazina-2-carboxamida
HUE032891T2 (hu) 2012-12-17 2017-11-28 Parion Sciences Inc Klórpirazin-karboxamid-származékok nem kielégítõ nyálkahártya-hidratáció által elõsegített megbetegedések kezelésére
BR112015014178A2 (pt) 2012-12-17 2017-07-11 Parion Sciences Inc compostos de 3,5-diamino-6-cloro-n-(n-(4-fenilbutil)carbamimidoil) pirazina-2- carboxamida
CA2914178C (en) 2013-01-07 2023-06-13 University Of Southern California Deoxyuridine triphosphatase inhibitors
DE202013000888U1 (de) 2013-01-29 2014-05-05 WKW Erbslöh Automotive GmbH Vorrichtung zur Abdeckung eines in Längsrichtung eines Kraftfahrzeuges verlaufenden Dachkanals
EP2970468B1 (en) 2013-03-13 2021-07-07 Novartis AG Notch2 binding molecules for treating respiratory diseases
JP6353032B2 (ja) * 2013-04-30 2018-07-04 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ジアミノピラジン化合物、前記化合物を含有する医薬、その使用、およびその調製方法
EP2815749A1 (en) 2013-06-20 2014-12-24 IP Gesellschaft für Management mbH Solid form of 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione having specified X-ray diffraction pattern
KR20160054460A (ko) 2013-07-02 2016-05-16 더 캘리포니아 인스티튜트 포 바이오메디칼 리써치 낭성 섬유증의 치료를 위한 화합물
US9102633B2 (en) 2013-12-13 2015-08-11 Parion Sciences, Inc. Arylalkyl- and aryloxyalkyl-substituted epithelial sodium channel blocking compounds
CN106061952B (zh) 2014-01-03 2022-01-28 南加州大学 含有杂原子的脱氧尿苷三磷酸酶抑制剂
UY36034A (es) 2014-03-18 2015-09-30 Astrazeneca Ab Derivados de 3,5-diamino-6-cloro-pirazina-2-carboxamida y sales farmaceuticamente aceptables de estos
EP2932966A1 (en) 2014-04-16 2015-10-21 Novartis AG Gamma secretase inhibitors for treating respiratory diseases
EP3153166B1 (en) 2014-06-09 2022-08-03 Chugai Seiyaku Kabushiki Kaisha Hydantoin derivative-containing pharmaceutical composition
EP3204029A4 (en) 2014-10-08 2018-07-11 The University of North Carolina at Chapel Hill Improved peptide inhibitors of sodium channels
CA2966023A1 (en) 2014-10-31 2016-05-06 Abbvie S.A.R.L. Substituted tetrahydropyrans and method of use
US9932324B2 (en) * 2015-01-12 2018-04-03 Boehringer Ingelheim International Gmbh Substituted benzimidazolium compounds useful in the treatment of respiratory diseases
EP3245202B1 (en) * 2015-01-12 2020-03-11 Boehringer Ingelheim International GmbH Tetrasubstituted benzimidazolium compounds useful in the treatment of respiratory diseases
JP6671378B2 (ja) * 2015-01-12 2020-03-25 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 呼吸器系疾患の治療に有用な置換ベンズイミダゾリウム化合物
EP3303294A1 (en) 2015-06-02 2018-04-11 Abbvie S.a.r.l. Substituted pyridines and method of use
FR3038605B1 (fr) * 2015-07-06 2018-08-24 Universite Amiens Picardie Jules Verne Diamines primaires vicinales associees a des motifs chelateurs de metaux et/ou de radicaux libres, actives contre les stress carbonyle et oxydant et leur utilisation
US10544105B2 (en) 2015-07-08 2020-01-28 Cv6 Therapeutics (Ni) Limited Deoxyuridine triphosphatase inhibitors containing cyclopropano linkage
WO2017006282A1 (en) 2015-07-08 2017-01-12 Cv6 Therapeutics (Ni) Limited Hydantoin containing deoxyuridine triphosphatase inhibitors
WO2017006271A1 (en) 2015-07-08 2017-01-12 University Of Southern California Deoxyuridine triphosphatase inhibitors containing amino sulfonyl linkage
WO2017006270A1 (en) 2015-07-08 2017-01-12 University Of Southern California Deoxyuridine triphosphatase inhibitors
US9840513B2 (en) 2015-07-16 2017-12-12 Abbvie S.Á.R.L. Substituted tricyclics and method of use
CN108431002A (zh) 2015-10-09 2018-08-21 艾伯维公司 取代的吡唑并[3，4-b]吡啶-6-甲酸及其用途
BR112018007165A2 (pt) 2015-10-09 2019-01-22 AbbVie S.à.r.l. novos compostos para tratamento da fibrose cística
CN108513574B (zh) 2015-10-09 2021-01-05 艾伯维公司 N-磺酰化吡唑并[3，4-b]吡啶-6-甲酰胺和使用方法
US10372306B2 (en) * 2016-04-16 2019-08-06 Apple Inc. Organized timeline
AU2017256172A1 (en) 2016-04-26 2018-09-06 AbbVie S.à.r.l. Modulators of cystic fibrosis transmembrane conductance regulator protein
US10138227B2 (en) 2016-06-03 2018-11-27 Abbvie S.Á.R.L. Heteroaryl substituted pyridines and methods of use
GB201610854D0 (en) 2016-06-21 2016-08-03 Entpr Therapeutics Ltd Compounds
US9981910B2 (en) 2016-10-07 2018-05-29 Abbvie S.Á.R.L. Substituted pyrrolidines and methods of use
US10399940B2 (en) 2016-10-07 2019-09-03 Abbvie S.Á.R.L. Substituted pyrrolidines and methods of use
GB201619694D0 (en) 2016-11-22 2017-01-04 Entpr Therapeutics Ltd Compounds
WO2018098208A1 (en) 2016-11-23 2018-05-31 Cv6 Therapeutics (Ni) Limited Nitrogen ring linked deoxyuridine triphosphatase inhibitors
WO2018098207A1 (en) 2016-11-23 2018-05-31 Cv6 Therapeutics (Ni) Limited Hydantoin containing deoxyuridine triphosphatase inhibitors
US11174271B2 (en) 2016-11-23 2021-11-16 Cv6 Therapeutics (Ni) Limited 6-membered uracil isosteres
US10858344B2 (en) 2016-11-23 2020-12-08 Cv6 Therapeutics (Ni) Limited Hydantoin containing deoxyuridine triphosphatase inhibitors
WO2018098209A1 (en) 2016-11-23 2018-05-31 Cv6 Therapeutics (Ni) Limited Amino sulfonyl compounds
US20200123137A1 (en) 2016-12-20 2020-04-23 AbbVie S.à.r.l. Deuterated cftr modulators and methods of use
WO2018128720A1 (en) 2017-01-05 2018-07-12 Cv6 Therapeutics (Ni) Limited Uracil containing compounds
TW201831471A (zh) 2017-02-24 2018-09-01 盧森堡商艾伯維公司 囊腫纖化症跨膜傳導調節蛋白的調節劑及其使用方法
WO2018175340A1 (en) 2017-03-20 2018-09-27 Sienna Biopharmaceuticals, Inc. Reduced exposure conjugates modulating therapeutic targets
WO2018175302A1 (en) 2017-03-20 2018-09-27 Sienna Biopharmaceuticals, Inc. Polymer conjugates targeting c-src with reduced exposure
US10988454B2 (en) 2017-09-14 2021-04-27 Abbvie Overseas S.À.R.L. Modulators of the cystic fibrosis transmembrane conductance regulator protein and methods of use
GB201717051D0 (en) 2017-10-17 2017-11-29 Enterprise Therapeutics Ltd Compounds
WO2019193062A1 (en) 2018-04-03 2019-10-10 Abbvie S.Á.R.L Substituted pyrrolidines and their use
GB201808093D0 (en) 2018-05-18 2018-07-04 Enterprise Therapeutics Ltd Compounds
CN113613649A (zh) * 2019-01-28 2021-11-05 弗拉特利发现实验室有限责任公司 用于治疗囊肿状纤维化的化合物及其治疗方法
EP3747882A1 (en) 2019-06-03 2020-12-09 AbbVie Overseas S.à r.l. Prodrug modulators of the cystic fibrosis transmembrane conductance regulator protein and methods of use
US11236067B2 (en) 2019-07-12 2022-02-01 Orphomed, Inc. Compound for treating cystic fibrosis
PH12022551138A1 (en) 2019-11-12 2023-07-17 Genzyme Corp 6-membered heteroarylaminosulfonamides for treating diseases and conditions mediated by deficient cftr activity
WO2021113809A1 (en) 2019-12-05 2021-06-10 Genzyme Corporation Arylamides and methods of use thereof
WO2021113806A1 (en) 2019-12-05 2021-06-10 Genzyme Corporation Arylamides and methods of use thereof
US20220213041A1 (en) 2021-01-06 2022-07-07 AbbVie Global Enterprises Ltd. Modulators of the Cystic Fibrosis Transmembrane Conductance Regulator Protein and Methods of Use
US20220211692A1 (en) 2021-01-06 2022-07-07 AbbVie Global Enterprises Ltd. Modulators of the Cystic Fibrosis Transmembrane Conductance Regulator Protein and Methods of Use
IL311038A (en) 2021-09-03 2024-04-01 Genzyme Corp Indole compounds and methods of use
EP4396176A1 (en) 2021-09-03 2024-07-10 Genzyme Corporation Indole compounds and uses thereof in the treatement of cystic fibrosis
CN113880735A (zh) * 2021-11-08 2022-01-04 湖北九宁化学科技有限公司 一种双氟磺酰二乙胺锂的制备方法
EP4583972A1 (en) 2022-09-07 2025-07-16 Sionna Therapeutics Inc. Macrocyclic compounds, compositions, and methods of using thereof
WO2024054851A1 (en) 2022-09-07 2024-03-14 Sionna Therapeutics Macrocyclic compounds, compositions and methods of using thereof
WO2024054845A1 (en) 2022-09-07 2024-03-14 Sionna Therapeutics Macrocycic compounds, compositions, and methods of using thereof
WO2025132358A1 (en) 2023-12-21 2025-06-26 Galapagos Nv Novel compounds and pharmaceutical compositions thereof for the treatment of infectious diseases

Family Cites Families (141)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3432502A (en) * 1966-08-25 1969-03-11 Merck & Co Inc Preparation of pyrazinoylguanidine and pyrazinamidoguanidine products
IL27897A (en) * 1966-08-25 1972-02-29 Merck & Co Inc Preparation of pyrazinoalguanides and pyrazinoamidoguanidines
US3328404A (en) * 1966-08-25 1967-06-27 Merck & Co Inc Derivatives of pyrazine
NL6707564A (es) * 1966-08-25 1968-02-26
GB1219606A (en) 1968-07-15 1971-01-20 Rech S Et D Applic Scient Soge Quinuclidinol derivatives and preparation thereof
US3503972A (en) * 1968-11-04 1970-03-31 Merck & Co Inc Alkyl n-amidino (or guanidino)-pyrazinimidates
US3577418A (en) * 1969-02-12 1971-05-04 Merck & Co Inc Pyrazinamide derivatives and processes for their preparation
US3573306A (en) 1969-03-05 1971-03-30 Merck & Co Inc Process for preparation of n-substituted 3,5-diamino-6-halopyrazinamides
US4085211A (en) * 1975-12-15 1978-04-18 Merck & Co., Inc. Pyrazinecarboxamides and processes for preparing same
US4246406A (en) 1979-03-27 1981-01-20 Merck & Co., Inc. Heterocyclic substituted pyrazinoylguanidines
US4277602A (en) * 1980-07-02 1981-07-07 Merck & Co., Inc. 3-Amino-5-substituted-6-halo-N-(3,4-dihydro-6-substituted-1,3,5-truazin-2-yl)2-pyrazinecarboxamides
US4272537A (en) * 1980-07-02 1981-06-09 Merck & Co., Inc. 3-Amino-5-substituted-6-halo-N-(4,4-disubstituted-6-substituted-1,3,5-triazin-2-yl)-2-pyrazinecarboxamides
JPS6235216A (ja) 1985-08-09 1987-02-16 Noritoshi Nakabachi 不均質物質層の層厚非破壊測定方法および装置
EP0300431A3 (en) 1987-07-22 1990-06-27 Neorx Corporation Method of radiolabeling chelating compounds comprising sulfur atoms with metal radionuclides
GB8923590D0 (en) 1989-10-19 1989-12-06 Pfizer Ltd Antimuscarinic bronchodilators
PT100441A (pt) 1991-05-02 1993-09-30 Smithkline Beecham Corp Pirrolidinonas, seu processo de preparacao, composicoes farmaceuticas que as contem e uso
WO1993018007A1 (fr) 1992-03-13 1993-09-16 Tokyo Tanabe Company Limited Nouveau derive de carbostyrile
NZ251092A (en) 1992-04-02 1996-12-20 Smithkline Beecham Corp 4-cyano-cyclohexane derivatives; medicaments; used in treating asthma
JP3192424B2 (ja) 1992-04-02 2001-07-30 スミスクライン・ビーチャム・コーポレイション アレルギーまたは炎症疾患の治療用化合物
WO1993019751A1 (en) 1992-04-02 1993-10-14 Smithkline Beecham Corporation Compounds useful for treating inflammatory diseases and inhibiting production of tumor necrosis factor
EP0620222A3 (en) 1993-04-14 1995-04-12 Lilly Co Eli Tetrahydro-beta-carbolines.
EP0702004A2 (de) 1994-09-15 1996-03-20 Ciba-Geigy Ag 2,9-Diamino- und 2-amino-8-carbamoyl-4-hydroxy-alkansäureamid-derivative
GB9622386D0 (en) 1996-10-28 1997-01-08 Sandoz Ltd Organic compounds
US6166037A (en) 1997-08-28 2000-12-26 Merck & Co., Inc. Pyrrolidine and piperidine modulators of chemokine receptor activity
AU9281298A (en) 1997-10-01 1999-04-23 Kyowa Hakko Kogyo Co. Ltd. Benzodioxole derivatives
US6541669B1 (en) 1998-06-08 2003-04-01 Theravance, Inc. β2-adrenergic receptor agonists
CN1146616C (zh) 1998-06-30 2004-04-21 陶氏环球技术公司 聚合物多元醇及其生产方法
GB9913083D0 (en) 1999-06-04 1999-08-04 Novartis Ag Organic compounds
ATE299865T1 (de) 1999-05-04 2005-08-15 Schering Corp Piperazinderivate verwendbar als ccr5 antagonisten
JP3894729B2 (ja) 1999-05-04 2007-03-22 シェーリング コーポレイション Ｃｃｒ５アンタゴニストとして有用なピペラジン誘導体
US6683115B2 (en) 1999-06-02 2004-01-27 Theravance, Inc. β2-adrenergic receptor agonists
ES2165768B1 (es) 1999-07-14 2003-04-01 Almirall Prodesfarma Sa Nuevos derivados de quinuclidina y composiciones farmaceuticas que los contienen.
SK287231B6 (sk) 1999-08-21 2010-04-07 Nycomed Gmbh Liečivo zahŕňajúce PDE inhibítor a agonistu beta2 adrenoreceptora
OA11558A (en) 1999-12-08 2004-06-03 Advanced Medicine Inc Beta 2-adrenergic receptor agonists.
BR0110331A (pt) 2000-04-27 2003-01-07 Boehringer Ingelheim Pharma Substâncias que mimetizam beta que têm uma atividade de longa duração, processos para prepará-las e o uso das mesmas como medicamentos
US6916828B2 (en) 2000-06-27 2005-07-12 Laboratorios S.A.L.V.A.T., S.A. Carbamates derivatived from arylakylamines
GB0015876D0 (en) 2000-06-28 2000-08-23 Novartis Ag Organic compounds
DE10038639A1 (de) 2000-07-28 2002-02-21 Schering Ag Nichtsteroidale Entzündungshemmer
JP4436041B2 (ja) 2000-08-05 2010-03-24 グラクソ グループ リミテッド 抗炎症剤としての６α，９α−ジフルオロ−１７α−［（２−フラニルカルボキシル）オキシ］−１１β−ヒドロキシ−１６α−メチル−３−オキソ−アンドロスト−１，４−ジエン−１７−チオカルボン酸Ｓ−フルオロメチルエステル
DE10056400A1 (de) 2000-11-14 2002-05-23 Merck Patent Gmbh Galenische Formulierung
GB0028383D0 (en) 2000-11-21 2001-01-03 Novartis Ag Organic compounds
RU2296762C2 (ru) 2000-12-22 2007-04-10 Альмиралль Продесфарма Аг Карбаматы хинуклидина, способы их получения и фармацевтическая композиция на их основе
DK1353919T3 (da) 2000-12-28 2006-11-20 Almirall Prodesfarma Ag Hidtil ukendte quinuclidinderivater og medicinale sammensætninger indeholdende samme
GB0103630D0 (en) 2001-02-14 2001-03-28 Glaxo Group Ltd Chemical compounds
ATE365720T1 (de) 2001-03-08 2007-07-15 Glaxo Group Ltd Agonisten von beta-adrenorezeptoren
ATE381537T1 (de) 2001-03-22 2008-01-15 Glaxo Group Ltd Formanilid-derivative als beta2-adrenorezeptor- agonisten
BR0209271A (pt) 2001-04-30 2004-06-15 Glaxo Group Ltd Composto, uso de um composto composição farmacêutica, formulação em aerossol farmacêutica, método para o tratamento de um paciente humano ou animal com uma condição inflamatória e/ou alérgica, e, processo para a preparação de um composto
JP2005500290A (ja) 2001-06-12 2005-01-06 グラクソ　グループ　リミテッド 抗炎症性の、１７β−カルボチオアートアンドロスタン誘導体である１７α複素環エステル
CA2445046C (en) 2001-06-21 2009-11-24 Diversa Corporation Nitrilases
SI1425001T1 (sl) 2001-09-14 2009-04-30 Glaxo Group Ltd Glaxo Welcome Fenetanolaminski derivati za zdravljenje respiratornih bolezni
BR0212983A (pt) 2001-10-17 2004-10-13 Ucb Sa Composto, uso do composto, e, intermediários de sìntese
GB0125259D0 (en) 2001-10-20 2001-12-12 Glaxo Group Ltd Novel compounds
AR037517A1 (es) 2001-11-05 2004-11-17 Novartis Ag Derivados de naftiridinas, un proceso para su preparacion, composicion farmaceutica y el uso de los mismos para la preparacion de un medicamento para el tratamiento de una enfermedad inflamatoria
US6653323B2 (en) 2001-11-13 2003-11-25 Theravance, Inc. Aryl aniline β2 adrenergic receptor agonists
TWI249515B (en) 2001-11-13 2006-02-21 Theravance Inc Aryl aniline beta2 adrenergic receptor agonists
AU2002356759A1 (en) 2001-12-01 2003-06-17 Glaxo Group Limited 17.alpha. -cyclic esters of 16-methylpregnan-3,20-dione as anti-inflammatory agents
CN1832948B (zh) 2001-12-20 2011-06-15 基耶西药品股份公司 1-烷基-1-氮*双环[2.2.2]辛烷氨基甲酸酯衍生物及其用作蕈毒碱受体拮抗剂的用途
AU2003202044A1 (en) 2002-01-15 2003-09-09 Glaxo Group Limited 17.alpha-cycloalkyl/cycloylkenyl esters of alkyl-or haloalkyl-androst-4-en-3-on-11.beta.,17.alpha.-diol 17.beta.-carboxylates as anti-inflammatory agents
AU2003201693A1 (en) 2002-01-21 2003-09-02 Glaxo Group Limited Non-aromatic 17.alpha.-esters of androstane-17.beta.-carboxylate esters as anti-inflammatory agents
GB0202216D0 (en) 2002-01-31 2002-03-20 Glaxo Group Ltd Novel compounds
US6858615B2 (en) * 2002-02-19 2005-02-22 Parion Sciences, Inc. Phenyl guanidine sodium channel blockers
GB0204719D0 (en) 2002-02-28 2002-04-17 Glaxo Group Ltd Medicinal compounds
JP2005521717A (ja) 2002-03-26 2005-07-21 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド グルココルチコイドミメチックス、その製造方法、その医薬組成物、及び使用
JP4324480B2 (ja) 2002-03-26 2009-09-02 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド グルココルチコイドミメティクス、その製法、医薬組成物、及び使用
ATE496620T1 (de) 2002-04-11 2011-02-15 Merck Sharp & Dohme 1h-benzo(f)indazol-5-yl-derivate als selektive glucocorticoid-rezeptor-modulatoren
ES2206021B1 (es) 2002-04-16 2005-08-01 Almirall Prodesfarma, S.A. Nuevos derivados de pirrolidinio.
DE60318193T2 (de) 2002-04-25 2008-12-04 Glaxo Group Ltd., Greenford Phenethanolaminderivate
AU2003239880A1 (en) 2002-05-28 2003-12-12 Theravance, Inc. ALKOXY ARYL Beta2 ADRENERGIC RECEPTOR AGONISTS
US7186864B2 (en) 2002-05-29 2007-03-06 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
ES2201907B1 (es) 2002-05-29 2005-06-01 Almirall Prodesfarma, S.A. Nuevos derivados de indolilpiperidina como potentes agentes antihistaminicos y antialergicos.
DE10224888A1 (de) 2002-06-05 2003-12-24 Merck Patent Gmbh Pyridazinderivate
US7074806B2 (en) 2002-06-06 2006-07-11 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
DE10225574A1 (de) 2002-06-10 2003-12-18 Merck Patent Gmbh Aryloxime
DE10227269A1 (de) 2002-06-19 2004-01-08 Merck Patent Gmbh Thiazolderivate
CA2490043A1 (en) 2002-06-25 2003-12-31 Merck Frosst Canada & Co. 8-(biaryl) quinoline pde4 inhibitors
CA2490097A1 (en) 2002-07-02 2004-01-15 Merck Frosst Canada & Co. Di-aryl-substituted-ethane pyridone pde4 inhibitors
ES2204295B1 (es) 2002-07-02 2005-08-01 Almirall Prodesfarma, S.A. Nuevos derivados de quinuclidina-amida.
SI1521733T1 (sl) 2002-07-08 2014-10-30 Pfizer Products Inc. Modulatorji glukokortikoidnega receptorja
GB0217225D0 (en) 2002-07-25 2002-09-04 Glaxo Group Ltd Medicinal compounds
AR040962A1 (es) 2002-08-09 2005-04-27 Novartis Ag Compuestos derivados de tiazol 1,3-2-ona, composicion farmaceutica y proceso de preparacion del compuesto
AU2003255376A1 (en) 2002-08-10 2004-03-11 Altana Pharma Ag Piperidine-derivatives as pde4 inhibitors
WO2004018457A1 (en) 2002-08-10 2004-03-04 Altana Pharma Ag Pyrrolidinedione substituted piperidine-phthalazones as pde4 inhibitors
WO2004018451A1 (en) 2002-08-10 2004-03-04 Altana Pharma Ag Pyridazinone-derivatives as pde4 inhibitors
PL373597A1 (en) 2002-08-10 2005-09-05 Altana Pharma Ag Piperidine-n-oxide-derivatives
JP2005537312A (ja) 2002-08-17 2005-12-08 アルタナ　ファルマ　アクチエンゲゼルシャフト 新規のフェナントリジン
HRP20050227A2 (en) 2002-08-17 2006-06-30 Altana Pharma Ag Novel benzonaphthyridines
SE0202483D0 (sv) 2002-08-21 2002-08-21 Astrazeneca Ab Chemical compounds
AU2003259747A1 (en) 2002-08-21 2004-03-11 Boehringer Ingelheim Pharmaceuticals, Inc. Substituted hihydroquinolines as glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
CN1688544A (zh) 2002-08-23 2005-10-26 兰贝克赛实验室有限公司 作为蕈毒碱受体拮抗剂的含氟代和磺酰氨基的3,6－二取代的氮杂双环(3.1.0)己烷衍生物
HRP20050185A2 (en) 2002-08-29 2006-05-31 Boehringer Ingelheim Pharmaceuticals Inc. -3 (sulfonamidoethyl)-indole derivatives for use as glucocorticoid mimetics in the treatment of inflammatory, allergic and proliferative diseases
US7329676B2 (en) 2002-08-29 2008-02-12 Nycomed Gmbh 2-hydroxy-6-phenylphenanthridines as PDE-4 inhibitors
US7423046B2 (en) 2002-08-29 2008-09-09 Nycomed Gmbh 3-hydroxy-6-phenylphenanthridines as pde-4 inhibitors
GB0220730D0 (en) 2002-09-06 2002-10-16 Glaxo Group Ltd Medicinal compounds
PL376154A1 (en) 2002-09-18 2005-12-27 Ono Pharmaceutical Co, Ltd. Triazaspiro[5.5]undecane derivatives and drugs comprising the same as the active ingredient
JP2006096662A (ja) 2002-09-18 2006-04-13 Sumitomo Pharmaceut Co Ltd 新規６−置換ウラシル誘導体及びアレルギー性疾患の治療剤
JP2004107299A (ja) 2002-09-20 2004-04-08 Japan Energy Corp 新規１−置換ウラシル誘導体及びアレルギー性疾患の治療剤
CA2499150A1 (en) 2002-09-20 2004-04-01 Merck & Co., Inc. Octahydro-2-h-naphtho[1,2-f] indole-4-carboxamide derivatives as selective glucocorticoid receptor modulators
DE10246374A1 (de) 2002-10-04 2004-04-15 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Betamimetika mit verlängerter Wirkungsdauer, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
KR20050047552A (ko) 2002-10-11 2005-05-20 화이자 인코포레이티드 베타-2 작용제로서의 인돌 유도체
EP1440966A1 (en) 2003-01-10 2004-07-28 Pfizer Limited Indole derivatives useful for the treatment of diseases
AU2003298094A1 (en) 2002-10-22 2004-05-13 Glaxo Group Limited Medicinal arylethanolamine compounds
US7238725B2 (en) 2002-10-23 2007-07-03 Glenmark Pharmaceuticals Ltd. Tricyclic compounds useful for the treatment of inflammatory and allergic disorders: process for their preparation and pharmaceutical compositions containing them
GB0225030D0 (en) 2002-10-28 2002-12-04 Glaxo Group Ltd Medicinal compounds
EP1556342B1 (en) 2002-10-28 2008-03-26 Glaxo Group Limited Phenethanolamine derivative for the treatment of respiratory diseases
GB0225287D0 (en) 2002-10-30 2002-12-11 Glaxo Group Ltd Novel compounds
GB0225540D0 (en) 2002-11-01 2002-12-11 Glaxo Group Ltd Medicinal compounds
GB0225535D0 (en) 2002-11-01 2002-12-11 Glaxo Group Ltd Medicinal compounds
DE10253282A1 (de) 2002-11-15 2004-05-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Arzneimittel zur Behandlung von chronisch obstruktiver Lungenerkrankung
DE10253220A1 (de) 2002-11-15 2004-05-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Dihydroxy-Methyl-Phenyl-Derivate, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
DE10253426B4 (de) 2002-11-15 2005-09-22 Elbion Ag Neue Hydroxyindole, deren Verwendung als Inhibitoren der Phosphodiesterase 4 und Verfahren zu deren Herstellung
DE10261874A1 (de) 2002-12-20 2004-07-08 Schering Ag Nichtsteroidale Entzündungshemmer
EP1587818A4 (en) 2003-01-21 2010-10-13 Merck Sharp & Dohme 17-CARBOMOYLOXYCORTISOL DERIVATIVES AS SELECTIVE MODULATORS OF THE GLUCOCORTICOID RECEPTOR
PE20040950A1 (es) 2003-02-14 2005-01-01 Theravance Inc DERIVADOS DE BIFENILO COMO AGONISTAS DE LOS RECEPTORES ADRENERGICOS ß2 Y COMO ANTAGONISTAS DE LOS RECEPTORES MUSCARINICOS
US20050113423A1 (en) 2003-03-12 2005-05-26 Vangoor Frederick F. Modulators of ATP-binding cassette transporters
EP1460064A1 (en) 2003-03-14 2004-09-22 Pfizer Limited Indole-2-carboxamide derivatives useful as beta-2 agonists
WO2004110352A2 (en) 2003-05-16 2004-12-23 The Regents Of The University Of California Compounds having activity in increasing ion transport by mutant-cftr and uses thereof
GB0312832D0 (en) 2003-06-04 2003-07-09 Pfizer Ltd 2-amino-pyridine derivatives useful for the treatment of diseases
EP1646615B1 (en) 2003-06-06 2009-08-26 Vertex Pharmaceuticals Incorporated Pyrimidine derivatives as modulators of atp-binding cassette transporters
JP2007535897A (ja) 2003-06-10 2007-12-13 エース バイオサイエンシズ エー／エス 細胞外コウジカビポリペプチド
KR20060088537A (ko) 2003-09-06 2006-08-04 버텍스 파마슈티칼스 인코포레이티드 Ａｔｐ-결합 카세트 수송체의 조절자
CA2539016A1 (en) 2003-09-17 2005-03-24 Novartis Ag Organic compounds
CN1886393A (zh) 2003-10-08 2006-12-27 沃泰克斯药物股份有限公司 含有环烷基或吡喃基基团的atp－结合弹夹转运蛋白的调控剂
US7541466B2 (en) 2003-12-23 2009-06-02 Genzyme Corporation Tetrahydroisoquinoline derivatives for treating protein trafficking diseases
MXPA06008606A (es) 2004-01-30 2007-04-13 Vertex Pharma Moduladores de transportadores con casete de union a atp.
WO2005120497A2 (en) 2004-06-04 2005-12-22 The Regents Of The University Of California Compounds having activity in increasing ion transport by mutant-cftr and uses thereof
US20060199828A1 (en) 2005-03-04 2006-09-07 Georg Jaeschke Pyrazine-2-carboxyamide derivatives
JP5385605B2 (ja) 2005-03-11 2014-01-08 バーテックス ファーマシューティカルズ インコーポレイテッド Ａｔｐ結合カセットトランスポーターのモジュレーター
WO2006101740A2 (en) 2005-03-18 2006-09-28 The Regents Of The University Of California Compounds having activity in correcting mutant-cftr processing and uses thereof
AU2006251624A1 (en) 2005-05-24 2006-11-30 Vertex Pharmaceuticals Incorporated Modulators of ATP-Binding cassette transporters
KR20080053297A (ko) 2005-08-11 2008-06-12 버텍스 파마슈티칼스 인코포레이티드 낭포성 섬유종 트랜스막 전도도 조정자의 조절자
NL2000284C2 (nl) 2005-11-04 2007-09-28 Pfizer Ltd Pyrazine-derivaten.
GB0526244D0 (en) 2005-12-22 2006-02-01 Novartis Ag Organic compounds
GB0526240D0 (en) * 2005-12-22 2006-02-01 Novartis Ag Organic compounds
CN101405002A (zh) 2005-12-29 2009-04-08 詹森药业有限公司 激肽原2受体拮抗剂
EA200970583A1 (ru) 2006-12-14 2009-12-30 Янссен Фармацевтика Н.В. Способ получения пиперазиниловых и диазепаниловых производных бензамида
US8450348B2 (en) 2007-02-21 2013-05-28 Forma Tm, Llc Derivatives of squaric acid with anti-proliferative activity
AR069621A1 (es) 2007-12-10 2010-02-03 Synthon Bv Sintesis de paliperidona
PL2444120T3 (pl) * 2007-12-10 2018-02-28 Novartis Ag Spirocyklicze analogi amiloridu jako blokery ENac
JPWO2010027002A1 (ja) 2008-09-05 2012-02-02 塩野義製薬株式会社 Ｐｉ３ｋ阻害活性を有する縮環モルホリン誘導体
IN2012DN03799A (es) 2009-10-29 2015-08-28 Sirtris Pharmaceuticals Inc
JP6203954B2 (ja) 2013-10-25 2017-09-27 ノバルティス アーゲー Ｆｇｆｒ４阻害剤としての縮環二環式ピリジル誘導体

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CN101939054A (zh) 2011-01-05
CO6310968A2 (es) 2011-08-22
US8039472B2 (en) 2011-10-18
ECSP10010242A (es) 2010-08-31
PT2444120T (pt) 2018-01-03
US9139586B2 (en) 2015-09-22
EP2231280A2 (en) 2010-09-29
WO2009074575A2 (en) 2009-06-18
MY152955A (en) 2014-12-15
JP2011506386A (ja) 2011-03-03
PE20091096A1 (es) 2009-08-25
CA2707857A1 (en) 2009-06-18
US20160068546A1 (en) 2016-03-10
CU20100118A7 (es) 2011-10-14
ES2654395T3 (es) 2018-02-13
AU2008334629B2 (en) 2012-04-12
NZ585789A (en) 2012-03-30
JP5455922B2 (ja) 2014-03-26
EP2444120A1 (en) 2012-04-25
TWI439462B (zh) 2014-06-01
KR20100098682A (ko) 2010-09-08
CL2008003651A1 (es) 2009-06-19
US20140171421A1 (en) 2014-06-19
TW200930717A (en) 2009-07-16
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CN101939054B (zh) 2014-10-29
AU2008334629A1 (en) 2009-06-18
AR069637A1 (es) 2010-02-10
IL206165A0 (en) 2010-12-30
MA31894B1 (fr) 2010-12-01
US8697687B2 (en) 2014-04-15
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US9643983B2 (en) 2017-05-09
US20130012500A1 (en) 2013-01-10
HN2010001165A (es) 2012-11-12
BRPI0820669A2 (pt) 2020-08-04
EP2444120B1 (en) 2017-09-27
TN2010000256A1 (en) 2011-11-11
PL2444120T3 (pl) 2018-02-28
UA104997C2 (uk) 2014-04-10
EA017919B1 (ru) 2013-04-30
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