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

Info

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
Authority
CU
Cuba
Prior art keywords
sodium channel
epitelial
pirazin
carboxamide
derivatives
Prior art date
Application number
CU20100118A
Other languages
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.)
Filing date
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

Links

Classifications

    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Communicable Diseases (AREA)
  • Pain & Pain Management (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)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Processing Or Creating Images (AREA)
  • Image Analysis (AREA)
  • Image Processing (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) EP2444120B1 (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) ES2654395T3 (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
CL2008003651A1 (es) * 2007-12-10 2009-06-19 Novartis Ag Compuestos derivados de 3,5-diamino-6-cloropirazinamida sustituida; composicion farmaceutica; combinacion farmaceutica; y uso en el tratamiento de una condición inflamatoria o alergica, en particular una enfermedad inflamatoria u obstructiva de las vias respiratorias.
WO2009139948A1 (en) 2008-02-26 2009-11-19 Johnson Michael R Poly aromatic sodium channel blockers
UA103198C2 (en) 2008-08-04 2013-09-25 Новартис Аг Squaramide derivatives as cxcr2 antagonists
EP2421532A4 (en) * 2008-10-02 2012-07-04 Univ Johns Hopkins SPIPERON DERIVATIVES AND METHOD FOR THE TREATMENT OF ILLNESSES
NZ592685A (en) 2008-10-23 2013-04-26 Vertex Pharma Modulators of cystic fibrosis transmembrane conductance regulator
ES2525353T3 (es) 2009-04-28 2014-12-22 Chugai Seiyaku Kabushiki Kaisha Derivado de espiroimidazolona
US9549967B2 (en) 2009-05-29 2017-01-24 The University Of North Carolina At Chapel Hill Regulation of sodium channels by PLUNC proteins
US20110098311A1 (en) * 2009-10-22 2011-04-28 Vertex Pharmaceuticals Incorported Compositions for treatment of cystic fibrosis and other chronic diseases
CN102648182A (zh) 2009-10-23 2012-08-22 沃泰克斯药物股份有限公司 用于制备囊性纤维化跨膜传导调节因子的调节剂的方法
WO2011050220A1 (en) 2009-10-23 2011-04-28 Vertex Pharmaceuticals Incorporated Solid forms of n-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide
TW201202250A (en) 2010-05-20 2012-01-16 Vertex Pharma Processes for producing modulators of cystic fibrosis transmembrane conductance regulator
US8372845B2 (en) * 2010-09-17 2013-02-12 Novartis Ag Pyrazine derivatives as enac blockers
US9050339B2 (en) 2010-09-17 2015-06-09 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
ES2655942T3 (es) 2011-09-02 2018-02-22 Novartis Ag Sal de colina de un compuesto anti-inflamatorio de ciclobutenodiona sustituida
CA2854221A1 (en) 2011-11-02 2013-05-10 Boehringer Ingelheim International Gmbh Novel process for the preparation of acylguanidines and acylthioureas
WO2013064450A1 (en) 2011-11-02 2013-05-10 Boehringer Ingelheim International Gmbh Heterocyclic compounds, medicaments containing said compounds, use thereof and processes for the preparation thereof
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
AU2012377446A1 (en) 2012-04-20 2014-10-23 Vertex Pharmaceuticals Incorporated Solid forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
WO2014044849A1 (en) * 2012-09-24 2014-03-27 Boehringer Ingelheim International Gmbh Heterocyclic compounds, medicaments containing said compounds, use thereof and processes for the preparation thereof
LT3470063T (lt) 2012-11-02 2025-02-10 Vertex Pharmaceuticals Incorporated Farmacinės kompozicijos, skirtos cftr nulemtų ligų gydymui
CA2892621C (en) 2012-12-10 2021-02-16 Chugai Seiyaku Kabushiki Kaisha Hydantoin derivative
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
SG10201708931XA (en) 2012-12-17 2017-12-28 Parion Sciences Inc Chloro-pyrazine carboxamide derivatives useful for the treatment of diseases favoured by insufficient mucosal hydration
RU2018138195A (ru) 2012-12-17 2018-12-18 Пэрион Сайенсиз, Инк. Соединения 3,5-диамино-6-хлор-n-(n-(4- фенилбутил)карбамимидоил)пиразин-2-карбоксамида
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
WO2014177469A1 (en) * 2013-04-30 2014-11-06 Boehringer Ingelheim International Gmbh,M Diaminopyrazine compounds, medicaments containing said compounds, use thereof and processes for the preparation thereof
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
US9656972B2 (en) 2013-07-02 2017-05-23 The California Institute For Biomedical Research Compounds for treatment of cystic fibrosis
US9102633B2 (en) 2013-12-13 2015-08-11 Parion Sciences, Inc. Arylalkyl- and aryloxyalkyl-substituted epithelial sodium channel blocking compounds
JP6513095B2 (ja) 2014-01-03 2019-05-15 ユニバーシティ オブ サザン カリフォルニア ヘテロ原子含有デオキシウリジントリホスファターゼ阻害剤
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
MX2017004653A (es) * 2014-10-08 2017-10-16 Univ North Carolina Chapel Hill Inhibidores peptidicos de canales de sodio mejorados.
JP6615213B2 (ja) 2014-10-31 2019-12-04 アッヴィ・エス・ア・エール・エル 置換テトラヒドロピランおよび使用方法
EP3245202B1 (en) * 2015-01-12 2020-03-11 Boehringer Ingelheim International GmbH Tetrasubstituted benzimidazolium compounds useful in the treatment of respiratory diseases
JP6667538B2 (ja) * 2015-01-12 2020-03-18 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
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
KR20180029204A (ko) 2015-06-02 2018-03-20 애브비 에스.에이.알.엘. 치환된 피리딘 및 사용 방법
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
PT3319939T (pt) 2015-07-08 2025-03-05 Cv6 Therapeutics Ni Ltd Inibidores de desoxiuridina-trifosfatase contendo hidantoína
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
US10130622B2 (en) 2015-10-09 2018-11-20 Abbvie S.Á.R.L. Compounds for treatment of cystic fibrosis
AU2016333855A1 (en) 2015-10-09 2018-04-26 AbbVie S.à.r.l. Substituted pyrazolo[3,4-b]pyridin-6-carboxylic acids and their use
RU2724345C2 (ru) 2015-10-09 2020-06-23 Галапагос Нв N-СУЛЬФОНИЛИРОВАННЫЕ ПИРАЗОЛО[3,4-b]ПИРИДИН-6-КАРБОКСАМИДЫ И СПОСОБ ИХ ПРИМЕНЕНИЯ
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
US11014924B2 (en) 2016-11-23 2021-05-25 Cv6 Therapeutics (Ni) Limited Hydantoin containing deoxyuridine triphosphatase inhibitors
WO2018098204A1 (en) 2016-11-23 2018-05-31 Cv6 Therapeutics (Ni) Limited 6-membered uracil isosteres
US11168059B2 (en) 2016-11-23 2021-11-09 Cv6 Therapeutics (Ni) Limited Amino sulfonyl compounds
US10829457B2 (en) 2016-11-23 2020-11-10 Cv6 Therapeutics (Ni) Limited Nitrogen ring linked deoxyuridine triphosphatase inhibitors
US10858344B2 (en) 2016-11-23 2020-12-08 Cv6 Therapeutics (Ni) Limited Hydantoin containing deoxyuridine triphosphatase inhibitors
EP3558982A1 (en) 2016-12-20 2019-10-30 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
TW202115014A (zh) 2019-07-12 2021-04-16 美商奧佛麥德公司 用於治療囊腫纖維化之化合物
EP4058434A1 (en) 2019-11-12 2022-09-21 Genzyme Corporation 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
WO2022150173A1 (en) 2021-01-06 2022-07-14 AbbVie Global Enterprises Ltd. Modulators of the cystic fibrosis transmembrane conductance regulator protein and methods of use
WO2022150174A1 (en) 2021-01-06 2022-07-14 AbbVie Global Enterprises Ltd. Modulators of the cystic fibrosis transmembrane conductance regulator protein and methods of use
CA3230259A1 (en) 2021-09-03 2023-03-09 Junkai Liao 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
KR20250091331A (ko) 2022-09-07 2025-06-20 시오나 테라퓨틱스 인크. 거대환식 화합물, 조성물, 및 이의 사용 방법
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
NL6707564A (es) * 1966-08-25 1968-02-26
IL27897A (en) * 1966-08-25 1972-02-29 Merck & Co Inc Preparation of pyrazinoalguanides and pyrazinoamidoguanidines
US3432502A (en) * 1966-08-25 1969-03-11 Merck & Co Inc Preparation of pyrazinoylguanidine and pyrazinamidoguanidine products
US3328404A (en) * 1966-08-25 1967-06-27 Merck & Co Inc Derivatives of pyrazine
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
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
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
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
JP3251587B2 (ja) 1992-04-02 2002-01-28 スミスクライン・ビーチャム・コーポレイション 炎症疾患の治療および腫瘍壊死因子の産生阻害に有用な化合物
US5552438A (en) 1992-04-02 1996-09-03 Smithkline Beecham Corporation Compounds useful for treating allergic and inflammatory diseases
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
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
WO1999016766A1 (en) 1997-10-01 1999-04-08 Kyowa Hakko Kogyo Co., Ltd. Benzodioxole derivatives
US6541669B1 (en) 1998-06-08 2003-04-01 Theravance, Inc. β2-adrenergic receptor agonists
BR9815931A (pt) 1998-06-30 2001-02-20 Dow Chemical Co Polióis poliméricos, um processo para sua produção, e espuma de poliuretanoobtida
GB9913083D0 (en) 1999-06-04 1999-08-04 Novartis Ag Organic compounds
KR100439357B1 (ko) 1999-05-04 2004-07-07 쉐링 코포레이션 Ｃｃｒ５ 길항제로서 유용한 피페리딘 유도체
SK287418B6 (sk) 1999-05-04 2010-09-07 Schering Corporation Farmaceutický prípravok s obsahom CCR5 antagonistov a súprava s obsahom tohto prípravku
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.
CA2715683A1 (en) 1999-08-21 2001-03-01 Nycomed Gmbh Synergistic combination
OA11558A (en) 1999-12-08 2004-06-03 Advanced Medicine Inc Beta 2-adrenergic receptor agonists.
SK15382002A3 (sk) 2000-04-27 2003-03-04 Boehringer Ingelheim Pharma Kg Betamimetiká, farmaceutický prostriedok s ich obsahom a ich použitie
KR100751981B1 (ko) 2000-06-27 2007-08-28 라보라토리오스 살바트, 에스.에이. 아릴알킬아민으로부터 유도된 카바메이트
GB0015876D0 (en) 2000-06-28 2000-08-23 Novartis Ag Organic compounds
DE10038639A1 (de) 2000-07-28 2002-02-21 Schering Ag Nichtsteroidale Entzündungshemmer
SI1775305T1 (sl) 2000-08-05 2015-01-30 Glaxo Group Limited S-fluorometil ester 6alfa,9alfa-difluoro-17alfa-((2-furanilkarboksil)oksi)- 11beta-hidroksi-16alfa-metil-3-okso-androst-1,4-dien-17-karbotiojske kisline kot protivnetno sredstvo
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
NZ526580A (en) 2000-12-22 2005-04-29 Almirall Prodesfarma Ag Quinuclidine carbamate derivatives and their use as M3 antagonists
DE60121813T2 (de) 2000-12-28 2007-09-20 Almirall Ag Neue chinuclidinderivate und medizinische zusammensetzungen, die diese verbindungen enthalten
GB0103630D0 (en) 2001-02-14 2001-03-28 Glaxo Group Ltd Chemical compounds
US7144908B2 (en) 2001-03-08 2006-12-05 Glaxo Group Limited Agonists of beta-adrenoceptors
ES2296923T3 (es) 2001-03-22 2008-05-01 Glaxo Group Limited Derivados formanilidas como agonistas del adrenorreceptor beta2.
KR100831534B1 (ko) 2001-04-30 2008-05-22 글락소 그룹 리미티드 17.알파 위치에 시클릭 에스테르기를 지닌 항염증성의안드로스탄의 17.베타.-카르보티오에이트 에스테르 유도체
ES2307751T3 (es) 2001-06-12 2008-12-01 Glaxo Group Limited Nuevos esteres heterociclicos centi-inflamatorios 17 alfa de derivados 17 beta de carbotioato de androstano.
DK2327765T3 (en) 2001-06-21 2015-07-13 Basf Enzymes Llc nitrilases
KR20090057477A (ko) 2001-09-14 2009-06-05 글락소 그룹 리미티드 호흡기 질환 치료용 펜에탄올아민 유도체
CN1571787A (zh) 2001-10-17 2005-01-26 Ucb公司 奎宁环衍生物、制备它们的方法和它们作为m2和/或m3毒蕈碱受体抑制剂的用途
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
TWI249515B (en) 2001-11-13 2006-02-21 Theravance Inc Aryl aniline beta2 adrenergic receptor agonists
US6653323B2 (en) 2001-11-13 2003-11-25 Theravance, Inc. Aryl aniline β2 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
JP4505227B2 (ja) 2001-12-20 2010-07-21 キエシ・フアルマチエウテイチ・ソチエタ・ペル・アチオニ １−アルキル−１−アゾニアビシクロ［２．２．２］オクタンカルバメート誘導体およびムスカリンレセプターアンタゴニストとしてのそれらの使用
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
CA2478156C (en) 2002-03-26 2011-02-15 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
WO2003082787A1 (en) 2002-03-26 2003-10-09 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
EP1496892B1 (en) 2002-04-11 2011-01-26 Merck Sharp & Dohme Corp. 1h-benzo(f)indazol-5-yl derivatives as selective glucocorticoid receptor modulators
ES2206021B1 (es) 2002-04-16 2005-08-01 Almirall Prodesfarma, S.A. Nuevos derivados de pirrolidinio.
JP2005523920A (ja) 2002-04-25 2005-08-11 グラクソ　グループ　リミテッド フェネタノールアミン誘導体
WO2003099764A1 (en) 2002-05-28 2003-12-04 Theravance, Inc. ALKOXY ARYL β2 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
ATE356808T1 (de) 2002-06-25 2007-04-15 Merck Frosst Canada Ltd 8-(biaryl)chinolin-pde4-inhibitoren
AU2003281219A1 (en) 2002-07-02 2004-01-23 Bernard Cote Di-aryl-substituted-ethane pyridone pde4 inhibitors
ES2204295B1 (es) 2002-07-02 2005-08-01 Almirall Prodesfarma, S.A. Nuevos derivados de quinuclidina-amida.
JP4503436B2 (ja) 2002-07-08 2010-07-14 ファイザー・プロダクツ・インク 糖質コルチコイド受容体のモジュレーター
GB0217225D0 (en) 2002-07-25 2002-09-04 Glaxo Group Ltd Medicinal compounds
PE20050130A1 (es) 2002-08-09 2005-03-29 Novartis Ag Compuestos organicos
EP1556369A1 (en) 2002-08-10 2005-07-27 ALTANA Pharma AG Pyridazinone-derivatives as pde4 inhibitors
BR0313330A (pt) 2002-08-10 2005-06-14 Altana Pharma Ag Piperidina-ftalazonas substituìdas com pirrolidinadiona como inibidores de pde4
US20060166995A1 (en) 2002-08-10 2006-07-27 Altana Pharma Ag Piperidine-n-oxide-derivatives
WO2004018449A1 (en) 2002-08-10 2004-03-04 Altana Pharma Ag Piperidine-derivatives as pde4 inhibitors
RS20050117A (sr) 2002-08-17 2007-06-04 Altana Pharma Ag., Novi benzonaftiridini
CA2495597A1 (en) 2002-08-17 2004-03-04 Altana Pharma Ag Novel phenanthridines
JP2006504678A (ja) 2002-08-21 2006-02-09 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
SE0202483D0 (sv) 2002-08-21 2002-08-21 Astrazeneca Ab Chemical compounds
EP1534675B1 (en) 2002-08-23 2009-02-25 Ranbaxy Laboratories, Ltd. Fluoro and sulphonylamino containing 3,6-disubstituted azabicyclo¬3.1.0 hexane derivatives as muscarinic receptor antagonists
JP4587294B2 (ja) 2002-08-29 2010-11-24 ニコメッド ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｐｄｅ４インヒビターとしての２−ヒドロキシ−６−フェニルフェナントリジン
WO2004019935A1 (en) 2002-08-29 2004-03-11 Boehringer Ingelheim Pharmaceuticals, Inc. -3 (sulfonamidoethyl) -indole derivaties for use as glucocorticoid mimetics in the treatment of inflammatory, allergic and proliferative diseases
ATE353217T1 (de) 2002-08-29 2007-02-15 Altana Pharma Ag 3-hydroxy-6-phenylphenanthridine als pde-4 inhibitoren
GB0220730D0 (en) 2002-09-06 2002-10-16 Glaxo Group Ltd Medicinal compounds
CA2497903A1 (en) 2002-09-18 2004-04-01 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
AU2003270783C1 (en) 2002-09-20 2010-05-20 Merck Sharp & Dohme Corp. Octahydro-2-H-naphtho[1,2-F] indole-4-carboxamide derivatives as selective glucocorticoid receptor modulators
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
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
ES2302938T3 (es) 2002-10-11 2008-08-01 Pfizer Inc. Derivados de indol como agonistas beta-2.
EP1440966A1 (en) 2003-01-10 2004-07-28 Pfizer Limited Indole derivatives useful for the treatment of diseases
EP1554264B1 (en) 2002-10-22 2007-08-08 Glaxo Group Limited Medicinal arylethanolamine compounds
EA010408B1 (ru) 2002-10-23 2008-08-29 Гленмарк Фармасьютикалс Лтд. Трициклические соединения для лечения воспалительных и аллергических нарушений, способы их приготовления и содержащие их фармацевтические составы
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
DE10253426B4 (de) 2002-11-15 2005-09-22 Elbion Ag Neue Hydroxyindole, deren Verwendung als Inhibitoren der Phosphodiesterase 4 und Verfahren zu deren Herstellung
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
DE10261874A1 (de) 2002-12-20 2004-07-08 Schering Ag Nichtsteroidale Entzündungshemmer
CA2512987C (en) 2003-01-21 2011-06-14 Merck & Co., Inc. 17-carbamoyloxy cortisol derivatives as selective glucocorticoid receptor modulators
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
WO2004080972A1 (en) 2003-03-12 2004-09-23 Vertex Pharmaceuticals Incorporated Pirazole 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
US7696244B2 (en) 2003-05-16 2010-04-13 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
WO2004108765A2 (en) 2003-06-10 2004-12-16 Ace Biosciences A/S Extracellular aspergillus polypeptides
ZA200602755B (en) 2003-09-06 2007-06-27 Vertex Pharma Modulators of ATP-binding cassette transporters
WO2005026134A1 (en) 2003-09-17 2005-03-24 Novartis Ag Organic compounds
MXPA06004005A (es) 2003-10-08 2006-06-28 Vertex Pharma Moduladores de transportadores con casete de union con atp.
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.
AU2005251745A1 (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
EP2363128B1 (en) 2005-03-11 2016-02-17 Vertex Pharmaceuticals Incorporated Indole modulators of ATP-binding cassette transporters
CA2600869A1 (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
EP1891018B1 (en) 2005-05-24 2011-11-16 Vertex Pharmaceuticals, Inc. Modulators of atp-binding cassette transporters
ATE512145T1 (de) 2005-08-11 2011-06-15 Vertex Pharma Modulatoren des cystic fibrosis transmembrane conductance regulators
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
CA2635845A1 (en) 2005-12-29 2007-07-12 Janssen Pharmaceutica N.V. Prokineticin 2 receptor antagonists
SI2121636T1 (sl) 2006-12-14 2017-06-30 Janssen Pharmaceutica N.V. Postopek za pripravo derivatov piperazinila in diazepanil benzamida
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
CL2008003651A1 (es) * 2007-12-10 2009-06-19 Novartis Ag Compuestos derivados de 3,5-diamino-6-cloropirazinamida sustituida; composicion farmaceutica; combinacion farmaceutica; y uso en el tratamiento de una condición inflamatoria o alergica, en particular una enfermedad inflamatoria u obstructiva de las vias respiratorias.
US20110172217A1 (en) 2008-09-05 2011-07-14 Shionogi & Co., Ltd. Ring-fused morpholine derivative having pi3k-inhibiting activity
MX2012004995A (es) 2009-10-29 2012-10-03 Sirtris Pharmaceuticals Inc Piridinas biciclicas y analogos como moduladores de sirtuina.
TN2016000115A1 (en) 2013-10-25 2017-07-05 Novartis Ag Ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors.

Also Published As

Publication number Publication date
CU20100118A7 (es) 2011-10-14
EP2231280A2 (en) 2010-09-29
AU2008334629A1 (en) 2009-06-18
AU2008334629B2 (en) 2012-04-12
ES2654395T3 (es) 2018-02-13
ECSP10010242A (es) 2010-08-31
ES2602331T3 (es) 2017-02-20
TWI439462B (zh) 2014-06-01
JP2011506386A (ja) 2011-03-03
JP5455922B2 (ja) 2014-03-26
TN2010000256A1 (en) 2011-11-11
EA017919B1 (ru) 2013-04-30
US20100130506A1 (en) 2010-05-27
NZ585789A (en) 2012-03-30
WO2009074575A2 (en) 2009-06-18
US20130012500A1 (en) 2013-01-10
ZA201003837B (en) 2011-03-30
WO2009074575A3 (en) 2009-08-13
US9643983B2 (en) 2017-05-09
CA2707857C (en) 2016-09-13
EA201000886A1 (ru) 2011-02-28
MA31894B1 (fr) 2010-12-01
HN2010001165A (es) 2012-11-12
PE20091096A1 (es) 2009-08-25
US9139586B2 (en) 2015-09-22
KR20100098682A (ko) 2010-09-08
PL2444120T3 (pl) 2018-02-28
AR069637A1 (es) 2010-02-10
MX2010006421A (es) 2010-06-25
US20110237572A1 (en) 2011-09-29
US8039472B2 (en) 2011-10-18
CO6310968A2 (es) 2011-08-22
CN101939054B (zh) 2014-10-29
TW200930717A (en) 2009-07-16
CN101939054A (zh) 2011-01-05
EP2444120B1 (en) 2017-09-27
MY152955A (en) 2014-12-15
KR101578235B1 (ko) 2015-12-16
CR11470A (es) 2010-07-09
US8697687B2 (en) 2014-04-15
UA104997C2 (uk) 2014-04-10
EP2231280B1 (en) 2016-08-10
PT2444120T (pt) 2018-01-03
IL206165A0 (en) 2010-12-30
US20140171421A1 (en) 2014-06-19
EP2444120A1 (en) 2012-04-25
CA2707857A1 (en) 2009-06-18
US20160068546A1 (en) 2016-03-10
BRPI0820669A2 (pt) 2020-08-04
CL2008003651A1 (es) 2009-06-19
EP2520574A1 (en) 2012-11-07

Similar Documents

Publication Publication Date Title
CU23967B1 (es) Derivados de pirazin-2-carboxamida para tratar enfermedades mediadas por el bloqueo del canal de sodio epitelial
CY1122860T1 (el) 3,5-διαμινο-6-χλωρο-ν-(ν-(4-(4-(2-(εξυλ(2,3,4,5,6-πενταϋδροξυεξυλ)αμινο)αιθοξυ)φαινυλ)βουτυλ)καρβαμιμιδοϋλ)πυραζινο-2-καρβοξαμιδιο
EA200900178A1 (ru) Конденсированные гетероциклические производные и их применение
CR11490A (es) Derivados de Piridina
EA200601350A1 (ru) Азотсодержащие гетероциклические производные и их фармацевтические применения
MX2009004289A (es) Compuestos triciclicos como inhibidores de metaloproteinasas matriciales.
CL2008001898A1 (es) Compuestos derivados de pirazinona, inhibidores de p38; proceso de preparacion de estos; composicion farmaceutica que los comprende; combinacion farmaceutica que los comprende; uso para tratar enferemedades pulmonares obstructivas cronicas y asma.
ATE524450T1 (de) 5-phenyl-isoxazol-3-carboxamid-derivate als trpv1-modulatoren
HRP20110201T1 (hr) Spojevi i sastavi kao inhibitori proteaze kanalizirane aktivacije
ATE440834T1 (de) Substituierte arylaminderivate und verwendungsverfahren
CY1112703T1 (el) Υποκατεστημενες πιπεριδινο-διϋδρο-θειενο-πυριμιδινες
EA201001772A1 (ru) Производные 3,5-диамино-6-хлорпиразин-2-карбоновой кислоты и их применение в качестве блокаторов эпителиальных натриевых каналов для лечения заболеваний дыхательных путей
CO2023015149A2 (es) Derivados de piridina con sustituyentes cíclicos ligados a n como inhibidores de cgas
EA201000120A1 (ru) Фармацевтические композиции, содержащие холиновые соли янтарной кислоты, для интраназального введения
EA025158B1 (ru) Гетероциклические соединения, лекарственные средства, содержащие указанные соединения, их применение и способы их получения
EA200870302A1 (ru) 1,3-диоксанкарбоновые кислоты
MEP42908A (en) Substituted 4-phenyltetrahydroisoquinolines, method for the production thereof, the use of the same as medicaments, and medicament containing such compounds
DK2061452T3 (da) Anvendelse af koffeinsyre og derivater deraf mod cancer
CA2796826A1 (en) Bifunctional quinoline derivatives
JOP20250101A1 (ar) مشتقات بنز إيميدازول حلقية كمثبطات cGAS
NZ709199A (en) Arylalkyl-and aryloxyalkyl-substituted epithelial sodium channel blocking compounds
MX2022016497A (es) Derivados heterociclicos, composiciones farmaceuticas y su uso en el tratamiento, mejora o prevencion de la enfermedad fibrotica.
EA201100502A1 (ru) Гликозидные производные и их применения
UY31896A (es) Derivados de 5-(4-metanosulfonil-fenil)-tiazol para el tratamiento de enfermedades inflamatorias agudas y crónicas
PE20070828A1 (es) Composicion farmaceutica que contiene una sal de glicopirronio

Legal Events

Date Code Title Description
FG Grant of patent
FD Lapse (for not paying fees)