[go: up one dir, main page]

ES2654395T3 - Análogos de amilorida espirocíclicos como bloqueantes de ENaC - Google Patents

Análogos de amilorida espirocíclicos como bloqueantes de ENaC Download PDF

Info

Publication number
ES2654395T3
ES2654395T3 ES11184004.7T ES11184004T ES2654395T3 ES 2654395 T3 ES2654395 T3 ES 2654395T3 ES 11184004 T ES11184004 T ES 11184004T ES 2654395 T3 ES2654395 T3 ES 2654395T3
Authority
ES
Spain
Prior art keywords
spirocyclic
amiloride analogs
enac blockers
image
image2 image3
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
ES11184004.7T
Other languages
English (en)
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
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Novartis AG
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
Application granted granted Critical
Publication of ES2654395T3 publication Critical patent/ES2654395T3/es
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/12Heterocyclic 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
    • C07D471/20Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/26Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32Nitrogen atom
    • C07D473/34Nitrogen atom attached in position 6, e.g. adenine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/10Spiro-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Ophthalmology & Optometry (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 que se selecciona de **(Ver fórmulas)** o solvatos, hidratos o sales farmacéuticamente aceptables de los mismos.

Description

imagen1
imagen2
imagen3
imagen4
imagen5
imagen6
imagen7
imagen8
imagen9
imagen10
imagen11
imagen12
imagen13
imagen14
imagen15
imagen16
imagen17
imagen18
imagen19
imagen20
imagen21
imagen22
imagen23
imagen24
imagen25
imagen26
imagen27
imagen28

Claims (1)

  1. imagen1
    imagen2
    imagen3
    imagen4
    imagen5
    imagen6
    imagen7
    imagen8
    imagen9
    imagen10
    imagen11
    imagen12
    imagen13
    imagen14
    imagen15
    imagen16
    imagen17
    imagen18
    imagen19
    imagen20
    imagen21
    imagen22
    imagen23
    imagen24
    imagen25
    imagen26
    imagen27
    imagen28
    imagen29
    imagen30
    imagen31
    imagen32
    imagen33
    imagen34
    imagen35
    imagen36
    imagen37
    imagen38
ES11184004.7T 2007-12-10 2008-12-09 Análogos de amilorida espirocíclicos como bloqueantes de ENaC Active ES2654395T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP07122739 2007-12-10
EP07122739 2007-12-10

Publications (1)

Publication Number Publication Date
ES2654395T3 true ES2654395T3 (es) 2018-02-13

Family

ID=39322745

Family Applications (2)

Application Number Title Priority Date Filing Date
ES08860731.2T Active ES2602331T3 (es) 2007-12-10 2008-12-09 Pirazin-carboxamidas de tipo amilorida como bloqueantes de ENaC
ES11184004.7T Active ES2654395T3 (es) 2007-12-10 2008-12-09 Análogos de amilorida espirocíclicos como bloqueantes de ENaC

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ES08860731.2T Active ES2602331T3 (es) 2007-12-10 2008-12-09 Pirazin-carboxamidas de tipo amilorida como bloqueantes de ENaC

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
KR101578235B1 (ko) * 2007-12-10 2015-12-16 노파르티스 아게 유기 화합물
TWI432198B (zh) 2008-02-26 2014-04-01 Parion Sciences Inc 多芳香族鈉通道阻斷劑
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
UA104601C2 (uk) 2008-10-23 2014-02-25 Вертекс Фармасьютікалз, Інкорпорейтед Модулятори регулятора трансмембранної провідності при муковісцидозі
PT2433940E (pt) 2009-04-28 2014-12-12 Chugai Pharmaceutical Co Ltd 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
AU2010310449A1 (en) * 2009-10-22 2012-05-03 Vertex Pharmaceuticals Incorporated Compositions for treatment of cystic fibrosis and other chronic diseases
BR112012009584A2 (pt) 2009-10-23 2019-09-24 Vertex Pharma formas sólidas de n-(4-(7-azabiciclo[2.2.1]heptan-7-il)-2-(trifluorometil)fenil)-4-oxo-5-(trifluorometil)-1,4-di-hidroquinolina-3-carboxamida
RU2553989C2 (ru) 2009-10-23 2015-06-20 Вертекс Фармасьютикалз Инкорпорейтед Способ получения модуляторов регулятора трансмембранной проводимости кистозного фиброза
AR081920A1 (es) 2010-05-20 2012-10-31 Vertex Pharma Procesos de produccion de moduladores del regulador de conductancia transmembrana de fibrosis quistica
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
EP2760821B1 (en) 2011-09-02 2017-10-11 Novartis AG Choline salt of an anti-inflammatory substituted cyclobutenedione compound
WO2013064451A1 (en) * 2011-11-02 2013-05-10 Boehringer Ingelheim International Gmbh Novel process for the preparation of acylguanidines and acylthioureas
KR102006612B1 (ko) 2011-11-02 2019-08-02 베링거 인겔하임 인터내셔날 게엠베하 헤테로사이클릭 화합물, 상기 화합물을 포함하는 약제, 이의 용도, 및 이의 제조 방법
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
WO2013158121A1 (en) 2012-04-20 2013-10-24 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
SMT202500078T1 (it) 2012-11-02 2025-03-12 Vertex Pharma Composizioni farmaceutiche per il trattamento di malattie mediate da cftr
CN104854106B (zh) 2012-12-10 2017-07-04 中外制药株式会社 乙内酰脲衍生物
WO2014099673A1 (en) 2012-12-17 2014-06-26 Parion Sciences, Inc. 3,5-diamino-6-chloro-n-(n-(4-phenylbutyl)carbamimidoyl) pyrazine-2- carboxamide compounds
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
US9593084B2 (en) 2012-12-17 2017-03-14 Parion Sciences, Inc. Chloro-pyrazine carboxamide derivatives with epithelial sodium channel blocking activity
CN105189478B (zh) 2013-01-07 2019-10-22 南加州大学 脱氧尿苷三磷酸酶抑制剂
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
AU2014284268A1 (en) 2013-07-02 2016-01-07 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
US9790214B2 (en) 2014-01-03 2017-10-17 University Of Southern California Heteroatom containing deoxyuridine triphosphatase inhibitors
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
BR112017007224A2 (pt) 2014-10-08 2018-03-06 Spyryx Biosciences Inc inibidores de canais de sódio, de peptídeo, aperfeiçoados
MX2017005663A (es) 2014-10-31 2018-03-01 Abbvie Sarl Tetrahidropiranos sustituidos y metodo de uso.
WO2016113170A1 (en) * 2015-01-12 2016-07-21 Boehringer Ingelheim International Gmbh Substituted benzimidazolium compounds useful in the treatment of respiratory diseases
US20180002312A1 (en) * 2015-01-12 2018-01-04 Boehringer Ingelheim International Gmbh Tetra- and pentasubstituted benzimidazolium compounds useful in the treatment of respiratory diseases
WO2016113167A1 (en) * 2015-01-12 2016-07-21 Boehringer Ingelheim International Gmbh Substituted benzimidazolium compounds useful in the treatment of respiratory diseases
BR112017026132A2 (pt) 2015-06-02 2018-08-28 AbbVie S.à.r.l. piridinas substituídas e métodos de uso
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
WO2017006270A1 (en) 2015-07-08 2017-01-12 University Of Southern California Deoxyuridine triphosphatase inhibitors
US10544105B2 (en) 2015-07-08 2020-01-28 Cv6 Therapeutics (Ni) Limited Deoxyuridine triphosphatase inhibitors containing cyclopropano linkage
US10570100B2 (en) 2015-07-08 2020-02-25 University Of Southern California Deoxyuridine triphosphatase inhibitors containing amino sulfonyl linkage
US10570098B2 (en) 2015-07-08 2020-02-25 Cv6 Therapeutics (Ni) Limited Hydantoin containing 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
WO2017060874A1 (en) 2015-10-09 2017-04-13 Abbvie S.Á.R.L N-sulfonylated pyrazolo[3,4-b]pyridin-6-carboxamides and method of use
EP3359539A1 (en) 2015-10-09 2018-08-15 AbbVie S.À.R.L. Substituted pyrazolo[3,4-b]pyridin-6-carboxylic acids and their use
US10402062B2 (en) * 2016-04-16 2019-09-03 Apple Inc. Organized timeline
EP3448842A1 (en) 2016-04-26 2019-03-06 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
US10399940B2 (en) 2016-10-07 2019-09-03 Abbvie S.Á.R.L. Substituted pyrrolidines and methods of use
US9981910B2 (en) 2016-10-07 2018-05-29 Abbvie S.Á.R.L. Substituted pyrrolidines and methods of use
GB201619694D0 (en) 2016-11-22 2017-01-04 Entpr Therapeutics Ltd Compounds
WO2018098209A1 (en) 2016-11-23 2018-05-31 Cv6 Therapeutics (Ni) Limited Amino sulfonyl compounds
US11014924B2 (en) 2016-11-23 2021-05-25 Cv6 Therapeutics (Ni) Limited Hydantoin containing deoxyuridine triphosphatase inhibitors
WO2018098206A1 (en) 2016-11-23 2018-05-31 Cv6 Therapeutics (Ni) Limited Hydantoin containing deoxyuridine triphosphatase inhibitors
WO2018098208A1 (en) 2016-11-23 2018-05-31 Cv6 Therapeutics (Ni) Limited Nitrogen ring linked deoxyuridine triphosphatase inhibitors
US11174271B2 (en) 2016-11-23 2021-11-16 Cv6 Therapeutics (Ni) Limited 6-membered uracil isosteres
WO2018116185A1 (en) 2016-12-20 2018-06-28 AbbVie S.à.r.l. Deuterated cftr modulators and methods of use
US11247984B2 (en) 2017-01-05 2022-02-15 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
WO2018175302A1 (en) 2017-03-20 2018-09-27 Sienna Biopharmaceuticals, Inc. Polymer conjugates targeting c-src with reduced exposure
EP3600440A1 (en) 2017-03-20 2020-02-05 Sienna Biopharmaceuticals, Inc. Reduced exposure conjugates modulating therapeutic targets
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
JP2022518778A (ja) * 2019-01-28 2022-03-16 フラットリー ディスカバリー ラブ,エルエルシー 嚢胞性線維症の治療のための化合物および方法
US11345691B2 (en) 2019-06-03 2022-05-31 AbbVie Global Enterprises Ltd. 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
IL292965A (en) 2019-11-12 2022-07-01 Genzyme Corp 6-membered heteroarylaminosulfonamides and methods of use
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
EP4274828A1 (en) 2021-01-06 2023-11-15 AbbVie Global Enterprises Ltd. Modulators of the cystic fibrosis transmembrane conductance regulator protein and methods of use
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
EP4396176A1 (en) 2021-09-03 2024-07-10 Genzyme Corporation Indole compounds and uses thereof in the treatement of cystic fibrosis
EP4396179A1 (en) 2021-09-03 2024-07-10 Genzyme Corporation Indole compounds and methods of use
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
WO2024054845A1 (en) 2022-09-07 2024-03-14 Sionna Therapeutics Macrocycic compounds, compositions, and methods of using thereof
AU2023338225A1 (en) 2022-09-07 2025-03-20 Genzyme Corporation 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
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
US3328404A (en) * 1966-08-25 1967-06-27 Merck & Co Inc Derivatives of pyrazine
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
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
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
SK279958B6 (sk) 1992-04-02 1999-06-11 Smithkline Beecham Corporation Zlúčeniny s protialergickým a protizápalovým účink
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
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
PT1175402E (pt) 1999-05-04 2005-11-30 Schering Corp Derivados da piperidina uteis como antagonistas ccr5
CA2371583C (en) 1999-05-04 2005-09-13 Schering Corporation Piperazine derivatives useful as ccr5 antagonists
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.
HU229439B1 (hu) 1999-08-21 2013-12-30 Takeda Gmbh Roflumilast és salmeterol szinergetikus kombinációja
OA11558A (en) 1999-12-08 2004-06-03 Advanced Medicine Inc Beta 2-adrenergic receptor agonists.
PL362868A1 (en) 2000-04-27 2004-11-02 Boehringer Ingelheim Pharma Gmbh & Co.Kg Novel, slow-acting betamimetics, a method for their production and their use as medicaments
IL153707A0 (en) 2000-06-27 2003-07-06 S A L V A T Lab Sa Carbamates derived from arylalkylamines
GB0015876D0 (en) 2000-06-28 2000-08-23 Novartis Ag Organic compounds
DE10038639A1 (de) 2000-07-28 2002-02-21 Schering Ag Nichtsteroidale Entzündungshemmer
CZ304043B6 (cs) 2000-08-05 2013-09-04 Glaxo Group Limited Estery steroidních thiokyselin
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
AU2002228015B2 (en) 2000-12-22 2007-08-23 Almirall, S.A. Quinuclidine carbamate derivatives and their use as M3 antagonists
CA2433128C (en) 2000-12-28 2010-05-25 Almirall Prodesfarma Ag Novel quinuclidine derivatives and medicinal compositions containing the same
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
WO2002076933A1 (en) 2001-03-22 2002-10-03 Glaxo Group Limited Formailide derivatives as beta2-adrenoreceptor agonists
US7291608B2 (en) 2001-04-30 2007-11-06 Glaxo Group Limited Anti-inflammatory 17.β.-carbothioate ester derivatives of androstane with a cyclic ester group in position 17.α
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
BRPI0212455B8 (pt) 2001-09-14 2021-05-25 Glaxo Group Ltd composto derivado de fenetanolamina para o tratamento de doenças respiratórias, formulação farmacêutica, combinação, e, uso do mesmo
HUP0401849A3 (en) 2001-10-17 2007-05-02 Ucb Sa Quinuclidine derivatives, processes for preparing them and their uses as m2 and/or m3 muscarinic receptor inhibitors
GB0125259D0 (en) 2001-10-20 2001-12-12 Glaxo Group Ltd Novel compounds
MY130622A (en) 2001-11-05 2007-07-31 Novartis Ag Naphthyridine derivatives, their preparation and their use as phosphodiesterase isoenzyme 4 (pde4) inhibitors
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
WO2003048181A1 (en) 2001-12-01 2003-06-12 Glaxo Group Limited 17.alpha. -cyclic esters of 16-methylpregnan-3,20-dione as anti-inflammatory agents
EA006505B1 (ru) 2001-12-20 2005-12-29 Лабораториос С.А.Л.В.А.Т.,С.А. Производные карбамата 1-алкил-1-азониабицикло[2.2.2]октана и их применение в качестве антагонистов мускаринового рецептора
WO2003072592A1 (en) 2002-01-15 2003-09-04 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
WO2003082787A1 (en) 2002-03-26 2003-10-09 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
EA008830B1 (ru) 2002-03-26 2007-08-31 Бёрингер Ингельхайм Фармасьютиклз, Инк. Миметики глюкокортикоидов, способы их получения, фармацевтические композиции и их применение
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.
EP1497261B1 (en) 2002-04-25 2007-12-19 Glaxo Group Limited Phenethanolamine derivatives
JP2005527618A (ja) 2002-05-28 2005-09-15 セラヴァンス インコーポレーテッド アルコキシアリールβ2アドレナリン作動性レセプターアゴニスト
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
WO2004000814A1 (en) 2002-06-25 2003-12-31 Merck Frosst Canada & Co. 8-(biaryl) quinoline pde4 inhibitors
US20060004056A1 (en) 2002-07-02 2006-01-05 Bernard Cote Di-aryl-substituted-ethan pyridone pde4 inhibitors
ES2204295B1 (es) 2002-07-02 2005-08-01 Almirall Prodesfarma, S.A. Nuevos derivados de quinuclidina-amida.
DK1521733T3 (da) 2002-07-08 2014-10-13 Pfizer Prod Inc Modulatorer af glucocorticoid receptoren
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
AU2003260371A1 (en) 2002-08-10 2004-03-11 Altana Pharma Ag Piperidine-n-oxide-derivatives
WO2004018457A1 (en) 2002-08-10 2004-03-04 Altana Pharma Ag Pyrrolidinedione substituted piperidine-phthalazones as pde4 inhibitors
JP2005538138A (ja) 2002-08-10 2005-12-15 アルタナ ファルマ アクチエンゲゼルシャフト Pde4インヒビターとしてのピリダジノン誘導体
JP2005537313A (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 新規のベンゾナフチリジン
WO2004018431A2 (en) 2002-08-17 2004-03-04 Altana Pharma Ag Novel phenanthridines
SE0202483D0 (sv) 2002-08-21 2002-08-21 Astrazeneca Ab Chemical compounds
CA2496175A1 (en) 2002-08-21 2004-03-04 Boehringer Ingelheim Pharmaceuticals, Inc. Substituted hihydroquinolines as glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
DE60231341D1 (de) 2002-08-23 2009-04-09 Ranbaxy Lab Ltd Fluor- und sulfonylaminohaltige, 3,6-disubstituierptorantagonisten
NZ538932A (en) 2002-08-29 2007-04-27 Boehringer Ingelheim Pharma 3-(sulfonamidoethyl)-indole derivatives for use as glucocorticoid mimetics in the treatment of inflammatory, allergic and proliferative disease
ES2281658T3 (es) 2002-08-29 2007-10-01 Nycomed Gmbh 3-hidroxi-6-fenilfenantridinas como inhibidores de pde-4.
WO2004019944A1 (en) 2002-08-29 2004-03-11 Altana Pharma Ag 2-hydroxy-6-phenylphenanthridines as pde-4 inhibitors
GB0220730D0 (en) 2002-09-06 2002-10-16 Glaxo Group Ltd Medicinal compounds
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
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
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
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
BR0315234A (pt) 2002-10-11 2005-08-23 Pfizer 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
WO2004037807A2 (en) 2002-10-22 2004-05-06 Glaxo Group Limited Medicinal arylethanolamine compounds
DE60317918T2 (de) 2002-10-23 2009-01-29 Glenmark Pharmaceuticals Ltd. Tricyclische verbindungen zur behandlung von entzündlichen und allergischen erkrankungen verfahren zu deren herstellung und sie enthaltende pharmazeutische zusammensetzungen
NZ539676A (en) 2002-10-28 2006-10-27 Glaxo Group Ltd Phenethanolamine derivative for the treatment of respiratory diseases
GB0225030D0 (en) 2002-10-28 2002-12-04 Glaxo Group Ltd Medicinal compounds
GB0225287D0 (en) 2002-10-30 2002-12-11 Glaxo Group Ltd Novel compounds
GB0225535D0 (en) 2002-11-01 2002-12-11 Glaxo Group Ltd Medicinal compounds
GB0225540D0 (en) 2002-11-01 2002-12-11 Glaxo Group Ltd Medicinal compounds
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
DE10253282A1 (de) 2002-11-15 2004-05-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Arzneimittel zur Behandlung von chronisch obstruktiver Lungenerkrankung
DE10261874A1 (de) 2002-12-20 2004-07-08 Schering Ag Nichtsteroidale Entzündungshemmer
WO2004066920A2 (en) 2003-01-21 2004-08-12 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
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
ATE440825T1 (de) 2003-06-06 2009-09-15 Vertex Pharma Pyrimidin-derivate zur verwendung als modulatoren von atp-bindende kassette transportern
AU2004245174A1 (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
CA2539016A1 (en) 2003-09-17 2005-03-24 Novartis Ag Organic compounds
US7598412B2 (en) 2003-10-08 2009-10-06 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
US7541466B2 (en) 2003-12-23 2009-06-02 Genzyme Corporation Tetrahydroisoquinoline derivatives for treating protein trafficking diseases
ES2631362T3 (es) 2004-01-30 2017-08-30 Vertex Pharmaceuticals Incorporated Moduladores de transportadores de casete de unión 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
EP1865949B1 (en) 2005-03-11 2012-11-14 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
JP2008538107A (ja) 2005-03-18 2008-10-09 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア 変異型cftrプロセシングの修正において活性を有する化合物及びその用途
ATE533749T1 (de) 2005-05-24 2011-12-15 Vertex Pharma Modulatoren von atp-bindenden kassettentransportern
EP1912983B1 (en) 2005-08-11 2011-06-08 Vertex Pharmaceuticals, Inc. Modulators of cystic fibrosis transmembrane conductance regulator
NL2000284C2 (nl) 2005-11-04 2007-09-28 Pfizer Ltd Pyrazine-derivaten.
GB0526240D0 (en) * 2005-12-22 2006-02-01 Novartis Ag Organic compounds
GB0526244D0 (en) 2005-12-22 2006-02-01 Novartis Ag Organic compounds
EP1976528A2 (en) 2005-12-29 2008-10-08 Janssen Pharmaceutica, N.V. Prokineticin 2 receptor antagonists
MX2009006472A (es) 2006-12-14 2009-06-26 Janssen Pharmaceutica Nv Procedimiento para la preparacion de derivados benzamida piperacinilo y diazepanilo.
US8450348B2 (en) 2007-02-21 2013-05-28 Forma Tm, Llc Derivatives of squaric acid with anti-proliferative activity
WO2009074333A1 (en) 2007-12-10 2009-06-18 Synthon B.V. Synthesis of paliperidone
KR101578235B1 (ko) 2007-12-10 2015-12-16 노파르티스 아게 유기 화합물
EP2341052A4 (en) 2008-09-05 2011-10-12 Shionogi & Co RING-CONDENSED MORPHOLINE DERIVATIVITY WITH PI3K-INHIBITING EFFECT
WO2011059839A1 (en) 2009-10-29 2011-05-19 Sirtris Pharmaceuticals, Inc. Bicyclic pyridines and analogs as sirtuin modulators
TR201810944T4 (tr) 2013-10-25 2018-08-27 Novartis Ag Fgfr4 inhibitörleri olarak halka-füzyonlu bisiklik piridil türevleri.

Also Published As

Publication number Publication date
EP2231280A2 (en) 2010-09-29
ES2602331T3 (es) 2017-02-20
AR069637A1 (es) 2010-02-10
BRPI0820669A2 (pt) 2020-08-04
NZ585789A (en) 2012-03-30
CU20100118A7 (es) 2011-10-14
MY152955A (en) 2014-12-15
US20140171421A1 (en) 2014-06-19
CL2008003651A1 (es) 2009-06-19
EP2231280B1 (en) 2016-08-10
PL2444120T3 (pl) 2018-02-28
KR101578235B1 (ko) 2015-12-16
AU2008334629B2 (en) 2012-04-12
US8697687B2 (en) 2014-04-15
JP2011506386A (ja) 2011-03-03
US20130012500A1 (en) 2013-01-10
MX2010006421A (es) 2010-06-25
MA31894B1 (fr) 2010-12-01
CO6310968A2 (es) 2011-08-22
TN2010000256A1 (en) 2011-11-11
ZA201003837B (en) 2011-03-30
PT2444120T (pt) 2018-01-03
US20160068546A1 (en) 2016-03-10
EP2520574A1 (en) 2012-11-07
CA2707857C (en) 2016-09-13
US9139586B2 (en) 2015-09-22
UA104997C2 (uk) 2014-04-10
JP5455922B2 (ja) 2014-03-26
US20100130506A1 (en) 2010-05-27
US8039472B2 (en) 2011-10-18
KR20100098682A (ko) 2010-09-08
EA201000886A1 (ru) 2011-02-28
EP2444120B1 (en) 2017-09-27
WO2009074575A2 (en) 2009-06-18
CN101939054B (zh) 2014-10-29
CA2707857A1 (en) 2009-06-18
TWI439462B (zh) 2014-06-01
HN2010001165A (es) 2012-11-12
AU2008334629A1 (en) 2009-06-18
PE20091096A1 (es) 2009-08-25
CU23967B1 (es) 2013-12-27
IL206165A0 (en) 2010-12-30
US20110237572A1 (en) 2011-09-29
CN101939054A (zh) 2011-01-05
EA017919B1 (ru) 2013-04-30
EP2444120A1 (en) 2012-04-25
US9643983B2 (en) 2017-05-09
WO2009074575A3 (en) 2009-08-13
CR11470A (es) 2010-07-09
TW200930717A (en) 2009-07-16
ECSP10010242A (es) 2010-08-31

Similar Documents

Publication Publication Date Title
ES2654395T3 (es) Análogos de amilorida espirocíclicos como bloqueantes de ENaC
ES2548578T3 (es) Monosebacato de un derivado de pirazol
ECSP109922A (es) Compuestos de pirazol y su uso como inhibidores raf
CY1112705T1 (el) Συντηγμενες κυκλικες ενωσεις
DOP2009000039A (es) COMPUESTOS DE PIRIDO (2,3-D) PIRIMIDINONA Y SU USO COMO INHIBIDORES DE P13-Ka
AR062211A1 (es) Derivados de 6-carboxi-normorfinano. composiciones farmaceuticas
CR11750A (es) Pirimidin-5-carboxamidas sustituidas 281
AR112787A2 (es) Compuestos 1,5-difenil-penta-1,4-dien-3-ona
UY31940A (es) Derivados sustituido del 4,5-(sustituido-piridin-3-il)-1-metil-1h-indol, sus sales farmacéuticamente aceptables, polimorfos, rotámeros, pro-fármacos, anantiómeros, hidratos, solvatos del mismo, composiciones conteniéndolos y aplicaciones
ES2308299T3 (es) Tiadiazoles como ligandos de receptores de cxc-y cc-quimioquinas.
UA113643C2 (xx) N-цикліламіди як нематоциди
ECSP10010415A (es) Compuestos novedosos que son inhibidores de erk
CO6220968A2 (es) Inhibidores heterociclicos de la aspartil proteasa
DOP2011000123A (es) Nuevos compuestos halosustituidos
CR20120130A (es) Compuestos de benzoxepina inhibidores de la pi3k y métodos de uso
ES2657549T3 (es) Piridopirazinas sustituidas como nuevos inhibidores de SYK
EA201070246A1 (ru) Циклические аминные соединения
CR20110474A (es) Derivados de benzofurano
UY34075A (es) ?compuestos insecticidas a base de derivados de ariltioacetamida
UA107919C2 (en) Anti-wrinkle means
MX391647B (es) Derivados heterociclicos de seis miembros y composicion farmaceutica que los comprende.
CR20110062A (es) Nuevos derivados de acilaminobenzamida
IN2014CN04960A (es)
EA200970372A1 (ru) Ингибитор развития болезни альцгеймера, содержащий гетероциклическое соединение
MX2013006811A (es) Compuestos, composiciones y articulos fotocromaticos.