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CR20140099A - Derivados de heterociclos bicíclicos para el tratamiento de la hipertensión arterial pulmonar - Google Patents

Derivados de heterociclos bicíclicos para el tratamiento de la hipertensión arterial pulmonar

Info

Publication number
CR20140099A
CR20140099A CR20140099A CR20140099A CR20140099A CR 20140099 A CR20140099 A CR 20140099A CR 20140099 A CR20140099 A CR 20140099A CR 20140099 A CR20140099 A CR 20140099A CR 20140099 A CR20140099 A CR 20140099A
Authority
CR
Costa Rica
Prior art keywords
derivatives
bicyclic
heterocicles
treatment
arterial hypertension
Prior art date
Application number
CR20140099A
Other languages
English (en)
Inventor
Ian Bruce
Sylvie Chamoin
Stephen Paul Collingwood
Pascal Furet
Vikki Furminger
Sarah Lewis
Jon Christopher Loren
Valentina Molteni
Alex Michael Saunders
Duncan Shaw
Lilya Sviridenko
Christopher Thomson
Vince Yeh
Diana Janus
Ryan West
Original Assignee
Novartis Ag
Irm Llc
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=47018333&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CR20140099(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag, Irm Llc filed Critical Novartis Ag
Publication of CR20140099A publication Critical patent/CR20140099A/es

Links

Classifications

    • 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
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4738Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Derivados de heterociclos bicíclicos de la fórmula I útiles en la inhibición de la actividad biológica mediada por el receptor PDGF.5 (I) en donde A es ó ; y R1, R1a, R2, R3, R4, R5, R6 y X son como se definen en la presente.
CR20140099A 2011-09-01 2014-02-27 Derivados de heterociclos bicíclicos para el tratamiento de la hipertensión arterial pulmonar CR20140099A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161530049P 2011-09-01 2011-09-01
US201261680119P 2012-08-06 2012-08-06

Publications (1)

Publication Number Publication Date
CR20140099A true CR20140099A (es) 2014-06-25

Family

ID=47018333

Family Applications (1)

Application Number Title Priority Date Filing Date
CR20140099A CR20140099A (es) 2011-09-01 2014-02-27 Derivados de heterociclos bicíclicos para el tratamiento de la hipertensión arterial pulmonar

Country Status (28)

Country Link
US (2) US8883819B2 (es)
EP (1) EP2751108B1 (es)
JP (1) JP5815870B2 (es)
KR (1) KR101687082B1 (es)
CN (2) CN104024252B (es)
AP (1) AP3818A (es)
AR (1) AR087755A1 (es)
AU (1) AU2012303674B2 (es)
BR (1) BR112014004631B1 (es)
CA (1) CA2845753C (es)
CL (1) CL2014000459A1 (es)
CO (1) CO6900139A2 (es)
CR (1) CR20140099A (es)
EA (1) EA024068B1 (es)
ES (1) ES2585048T3 (es)
IL (1) IL231228A0 (es)
MA (1) MA35364B1 (es)
MX (1) MX360316B (es)
PE (1) PE20141674A1 (es)
PH (1) PH12014500407A1 (es)
PL (1) PL2751108T3 (es)
PT (1) PT2751108T (es)
SG (1) SG11201400253YA (es)
TN (1) TN2014000067A1 (es)
TW (1) TW201313718A (es)
UY (1) UY34305A (es)
WO (1) WO2013030802A1 (es)
ZA (1) ZA201401294B (es)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2685903B2 (ja) 1989-07-05 1997-12-08 アルプス電気株式会社 磁気ヘッド支持装置
UY34305A (es) * 2011-09-01 2013-04-30 Novartis Ag Derivados de heterociclos bicíclicos para el tratamiento de la hipertensión arterial pulmonar
US9073921B2 (en) 2013-03-01 2015-07-07 Novartis Ag Salt forms of bicyclic heterocyclic derivatives
UA119247C2 (uk) 2013-09-06 2019-05-27 РОЙВЕНТ САЙЕНСИЗ ҐмбГ Спіроциклічні сполуки як інгібітори триптофангідроксилази
WO2015089137A1 (en) 2013-12-11 2015-06-18 Karos Pharmaceuticals, Inc. Acylguanidines as tryptophan hydroxylase inhibitors
CN105524058B (zh) 2014-10-21 2018-03-27 广州艾格生物科技有限公司 吡唑并[1,5‑a]吡啶类化合物及其应用
WO2016109501A1 (en) 2014-12-30 2016-07-07 Karos Pharmaceuticals, Inc. Amide compounds as tryptophan hydroxylase inhibitors
US9611201B2 (en) 2015-03-05 2017-04-04 Karos Pharmaceuticals, Inc. Processes for preparing (R)-1-(5-chloro-[1,1′-biphenyl]-2-yl)-2,2,2-trifluoroethanol and 1-(5-chloro-[1,1′-biphenyl]-2-yl)-2,2,2-trifluoroethanone
GB201801355D0 (en) * 2018-01-26 2018-03-14 Enterprise Therapeutics Ltd Compounds
CN113227093A (zh) 2018-11-14 2021-08-06 阿尔塔万特科学公司 结晶螺环化合物、包含该化合物的剂型、用于疾病治疗的方法和再结晶方法
AU2020403681A1 (en) * 2019-12-13 2022-06-30 Nippon Shinyaku Co., Ltd. Compound and composition as pdgf receptor kinase inhibitor
US20220031633A1 (en) * 2020-07-28 2022-02-03 Yale University Poly(amine-co-ester) polymeric particles for selective pulmonary delivery
US20240109917A1 (en) 2020-12-23 2024-04-04 Actelion Pharmaceuticals Ltd Pyrazolothiazole carboxamides and their uses as pdgfr inhibitors
TW202313053A (zh) 2021-07-30 2023-04-01 瑞士商艾克泰聯製藥有限公司 吡唑并嘧啶及其作為pdgfr抑制劑之用途
CN113912530A (zh) * 2021-11-10 2022-01-11 山东汇海医药化工有限公司 一种4-aa中间体废液的处理方法
WO2023247590A1 (en) 2022-06-22 2023-12-28 Actelion Pharmaceuticals Ltd Triazolopyridine and benzoisoxazole carboxamides and their uses as pdgfr inhibitors
WO2023247595A1 (en) 2022-06-22 2023-12-28 Actelion Pharmaceuticals Ltd Pyrazolopyrazine carboxamides and their uses as pdgfr inhibitors
WO2023247596A1 (en) 2022-06-22 2023-12-28 Actelion Pharmaceuticals Ltd Pyrazolothiazole carboxamides and their uses as pdgfr inhibitors
WO2023247593A1 (en) 2022-06-22 2023-12-28 Actelion Pharmaceuticals Ltd Pyrrolopyridine carboxamides and their uses as pdgfr inhibitors
WO2024104968A1 (en) 2022-11-14 2024-05-23 Actelion Pharmaceuticals Ltd Pyrazolopyrrolopyridazines and their uses as pdgfr inhibitors

Family Cites Families (177)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1219606A (en) 1968-07-15 1971-01-20 Rech S Et D Applic Scient Soge Quinuclidinol derivatives and preparation thereof
IT1016489B (it) 1974-03-18 1977-05-30 Isf Spa Inalatore
ZA81219B (en) 1980-01-23 1982-01-27 Schering Corp Imidazo (1,2-a) pyridines ,process for their preparation and pharmaceutical compositions containing them
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
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
GB9816837D0 (en) 1998-08-04 1998-09-30 Zeneca Ltd Amide derivatives
WO1993018007A1 (en) 1992-03-13 1993-09-16 Tokyo Tanabe Company Limited Novel carbostyril derivative
AU3924993A (en) 1992-04-02 1993-11-08 Smithkline Beecham Corporation Compounds useful for treating inflammatory diseases and inhibiting production of tumor necrosis factor
US5552438A (en) 1992-04-02 1996-09-03 Smithkline Beecham Corporation Compounds useful for treating allergic and inflammatory diseases
WO1993019750A1 (en) 1992-04-02 1993-10-14 Smithkline Beecham Corporation Compounds useful for treating allergic or inflammatory diseases
US6596260B1 (en) 1993-08-27 2003-07-22 Novartis Corporation Aerosol container and a method for storage and administration of a predetermined amount of a pharmaceutically active aerosol
PT995457E (pt) 1995-12-07 2004-07-30 Jago Res Ag Bocal para um inalador para a distribuicao reiterada doseadamente de um po farmacologicamente seco
ES2172763T3 (es) 1996-02-21 2002-10-01 Schering Corp Inhalador de medicamento en polvo.
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 (fr) 1997-10-01 1999-04-08 Kyowa Hakko Kogyo Co., Ltd. Derives de benzodioxole
DK1040108T3 (da) 1997-12-19 2004-05-24 Schering Ag Orthoanthranilamidderivater som antikoagulanter
US6541669B1 (en) 1998-06-08 2003-04-01 Theravance, Inc. β2-adrenergic receptor agonists
AU8180398A (en) 1998-06-30 2000-01-17 Dow Global Technologies Inc. Polymer polyols and a process for the production thereof
DE19834044A1 (de) 1998-07-29 2000-02-03 Bayer Ag Neue substituierte Pyrazolderivate
DE19834047A1 (de) 1998-07-29 2000-02-03 Bayer Ag Substituierte Pyrazolderivate
RU2216541C2 (ru) 1998-08-04 2003-11-20 Астразенека Аб Производные бензамида, способ их получения и фармацевтическая композиция на их основе
SK13132001A3 (sk) 1999-03-17 2002-02-05 Astrazeneca Ab Amidové deriváty, spôsob ich prípravy, farmaceutická kompozícia, ktorá ich obsahuje, a ich použitie
GB9913083D0 (en) 1999-06-04 1999-08-04 Novartis Ag Organic compounds
CN1151131C (zh) 1999-05-04 2004-05-26 先灵公司 用作ccr5拮抗剂的哌啶衍生物
ES2244437T3 (es) 1999-05-04 2005-12-16 Schering Corporation Derivados de piperazina utiles como antagonistas de ccr5.
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.
EA006685B1 (ru) 1999-08-21 2006-02-24 Алтана Фарма Аг Синергетическая композиция
DE19943634A1 (de) 1999-09-13 2001-04-12 Bayer Ag Neuartige Dicarbonsäurederivate mit pharmazeutischen Eigenschaften
DE19943636A1 (de) 1999-09-13 2001-03-15 Bayer Ag Neuartige Dicarbonsäurederivate mit pharmazeutischen Eigenschaften
DE19943639A1 (de) 1999-09-13 2001-03-15 Bayer Ag Dicarbonsäurederivate mit neuartigen pharmazeutischen Eigenschaften
DE19943635A1 (de) 1999-09-13 2001-03-15 Bayer Ag Neuartige Aminodicarbonsäurederivate mit pharmazeutischen Eigenschaften
ES2316383T3 (es) 1999-09-17 2009-04-16 Millennium Pharmaceuticals, Inc. Benzamidas e inhibidores relacionados del factor xa.
GB9924092D0 (en) 1999-10-13 1999-12-15 Zeneca Ltd Pyrimidine derivatives
OA11558A (en) 1999-12-08 2004-06-03 Advanced Medicine Inc Beta 2-adrenergic receptor agonists.
HRP20020845A2 (en) 2000-04-27 2003-10-31 Boehringer Ingelheim Pharma Novel, slow-acting betamimetics, a method for their production and their use as medicaments
DK1300407T4 (da) 2000-06-27 2011-09-05 S A L V A T Lab Sa Carbamater afledt af arylalkylaminer
GB0015876D0 (en) 2000-06-28 2000-08-23 Novartis Ag Organic compounds
DE10038639A1 (de) 2000-07-28 2002-02-21 Schering Ag Nichtsteroidale Entzündungshemmer
JP2004505990A (ja) 2000-08-05 2004-02-26 グラクソ グループ リミテッド 抗炎症剤としての17β−カルボチオエート−17α−アリールカルボニルオキシルオキシアンドロスタン誘導体
GB0028383D0 (en) 2000-11-21 2001-01-03 Novartis Ag Organic compounds
AR031176A1 (es) 2000-11-22 2003-09-10 Bayer Ag Nuevos derivados de pirazolpiridina sustituidos con piridina
ATE305468T1 (de) 2000-12-22 2005-10-15 Almirall Prodesfarma Ag Chinuclidincarbamat derivate und deren verwendung als m3 antagonisten
PL363807A1 (en) 2000-12-28 2004-11-29 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
SE0100567D0 (sv) 2001-02-20 2001-02-20 Astrazeneca Ab Compounds
SE0100568D0 (sv) 2001-02-20 2001-02-20 Astrazeneca Ab Compounds
DE10110750A1 (de) 2001-03-07 2002-09-12 Bayer Ag Neuartige Aminodicarbonsäurederivate mit pharmazeutischen Eigenschaften
DE10110749A1 (de) 2001-03-07 2002-09-12 Bayer Ag Substituierte Aminodicarbonsäurederivate
US7144908B2 (en) 2001-03-08 2006-12-05 Glaxo Group Limited Agonists of beta-adrenoceptors
US7045658B2 (en) 2001-03-22 2006-05-16 Glaxo Group Limited Formailide derivatives as beta2-adrenoreceptor agonists
ES2314052T3 (es) 2001-04-30 2009-03-16 Glaxo Group Limited Derivados de ester de 17beta-carbotioato de androstano con un grupo ester ciclico en la posicion 17alfa.
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
EP2039762A3 (en) 2001-06-21 2009-07-29 Verenium Corporation Nitralases
EP2042168B1 (en) 2001-09-14 2013-10-23 Glaxo Group Limited Inhalation formulation comprising phenethanolamine derivatives for the treatment of respiratory diseases
US7361668B2 (en) 2001-10-17 2008-04-22 Ucb, S.A. 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
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
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
RS52522B (en) 2001-12-20 2013-04-30 Chiesi Farmaceutici S.P.A. 1-ALKYL-1-AZONIABICYCLE DERIVATIVES / 2.2.2. / OCTAN CARBAMATE AND THEIR USE AS AN ANTAGONIST OF MUSCAR RECEPTORS
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
GB0204719D0 (en) 2002-02-28 2002-04-17 Glaxo Group Ltd Medicinal compounds
WO2003078435A1 (en) 2002-03-13 2003-09-25 Pharmacia & Upjohn Company Llc Pyrazolo(1,5-a)pyridine derivatives as neurotransmitter modulators
UA80120C2 (en) 2002-03-26 2007-08-27 Boehringer Ingelheim Pharma Glucocorticoid mimetics, pharmaceutical composition based thereon
WO2003082787A1 (en) 2002-03-26 2003-10-09 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
WO2003086294A2 (en) 2002-04-11 2003-10-23 Merck & Co., Inc. 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.
AU2003222841A1 (en) 2002-04-25 2003-11-10 Glaxo Group Limited Phenethanolamine derivatives
DE10220570A1 (de) 2002-05-08 2003-11-20 Bayer Ag Carbamat-substituierte Pyrazolopyridine
AU2003239880A1 (en) 2002-05-28 2003-12-12 Theravance, Inc. ALKOXY ARYL Beta2 ADRENERGIC RECEPTOR AGONISTS
ES2201907B1 (es) 2002-05-29 2005-06-01 Almirall Prodesfarma, S.A. Nuevos derivados de indolilpiperidina como potentes agentes antihistaminicos y antialergicos.
US7186864B2 (en) 2002-05-29 2007-03-06 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
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
ES2204295B1 (es) 2002-07-02 2005-08-01 Almirall Prodesfarma, S.A. Nuevos derivados de quinuclidina-amida.
AU2003281219A1 (en) 2002-07-02 2004-01-23 Bernard Cote Di-aryl-substituted-ethane pyridone pde4 inhibitors
PT1521733E (pt) 2002-07-08 2014-10-29 Pfizer Prod Inc Moduladores do recetor de glucocorticoides
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
HRP20050198A2 (hr) 2002-08-10 2006-04-30 Altana Pharma Ag Piperidin-piridazoni i ftalazoni kao inhibitori pde4
EP1542987A1 (en) 2002-08-10 2005-06-22 ALTANA Pharma AG Piperidine-n-oxide-derivatives
AU2003255376A1 (en) 2002-08-10 2004-03-11 Altana Pharma Ag Piperidine-derivatives as pde4 inhibitors
CA2494650A1 (en) 2002-08-10 2004-03-04 Altana Pharma Ag Pyridazinone-derivatives as pde4 inhibitors
PL374014A1 (en) 2002-08-17 2005-09-19 Altana Pharma Ag Novel phenanthridines having pde 3/4 inhibiting properties
US20060113968A1 (en) 2002-08-17 2006-06-01 Altana Pharma Ag Novel benzonaphthyridines
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
ATE423769T1 (de) 2002-08-23 2009-03-15 Ranbaxy Lab Ltd Fluor- und sulfonylaminohaltige, 3,6- disubstituierte azabicyclo 3.1.0 hexanderivate als muscarinrezeptorantagonisten
PL375513A1 (en) 2002-08-29 2005-11-28 Boehringer Ingelheim Pharmaceuticals, Inc. 3-(sulfonamidoethyl)-indole derivatives for use as glucocorticoid mimetics in the treatment of inflammatory, allergic and proliferative diseases
DE60311662T2 (de) 2002-08-29 2007-10-25 Altana Pharma Ag 3-hydroxy-6-phenylphenanthridine als pde-4 inhibitoren
EP1539164B1 (en) 2002-08-29 2006-12-20 ALTANA Pharma AG 2-hydroxy-6-phenylphenanthridines as pde-4 inhibitors
GB0220730D0 (en) 2002-09-06 2002-10-16 Glaxo Group Ltd Medicinal compounds
TW200413372A (en) 2002-09-18 2004-08-01 Ono Pharmaceutical Co Derivatives of triazaspiro [5.5] undecane and medicants using such derivatives as effective 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
MY136840A (en) 2002-09-19 2008-11-28 Schering Corp Pyrazolopyridines as cyclin dependent kinase inhibitors
CA2499639C (en) 2002-09-19 2011-11-08 Schering Corporation Imidazopyridines as cyclin dependent kinase inhibitors
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
PL376396A1 (en) 2002-10-11 2005-12-27 Pfizer Inc. Indole derivatives as beta-2 agonists
EP1440966A1 (en) 2003-01-10 2004-07-28 Pfizer Limited Indole derivatives useful for the treatment of diseases
JP2006506373A (ja) 2002-10-22 2006-02-23 グラクソ グループ リミテッド 医薬アリールエタノールアミン化合物
WO2004037805A1 (en) 2002-10-23 2004-05-06 Glenmark Pharmaceuticals Ltd. Novel 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
PT1556342E (pt) 2002-10-28 2008-04-28 Glaxo Group Ltd Derivado de fenetanolamina para o tratamento de doenças respiratórias
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
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
DE10253282A1 (de) 2002-11-15 2004-05-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Arzneimittel zur Behandlung von chronisch obstruktiver Lungenerkrankung
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
TWI299664B (en) 2003-01-06 2008-08-11 Osi Pharm Inc (2-carboxamido)(3-amino)thiophene compounds
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
EP1631260A2 (en) 2003-02-28 2006-03-08 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
EP1460064A1 (en) 2003-03-14 2004-09-22 Pfizer Limited Indole-2-carboxamide derivatives useful as beta-2 agonists
PL377633A1 (pl) 2003-04-03 2006-02-06 Merck Patent Gmbh Związki karbonylowe
EP1479680A1 (en) 2003-05-19 2004-11-24 Aventis Pharma Deutschland GmbH Azaindole derivatives as Factor Xa inhibitors
GB0312832D0 (en) 2003-06-04 2003-07-09 Pfizer Ltd 2-amino-pyridine derivatives useful for the treatment of diseases
AU2004245174A1 (en) 2003-06-10 2004-12-16 Ace Biosciences A/S Extracellular Aspergillus polypeptides
US7144907B2 (en) 2003-09-03 2006-12-05 Array Biopharma Inc. Heterocyclic inhibitors of MEK and methods of use thereof
GB2407042B (en) 2003-10-17 2007-10-24 Vectura Ltd Inhaler
GB0325956D0 (en) 2003-11-06 2003-12-10 Addex Pharmaceuticals Sa Novel compounds
WO2005048953A2 (en) 2003-11-13 2005-06-02 Ambit Biosciences Corporation Amide derivatives as kinase modulators
EA009994B1 (ru) 2003-12-23 2008-06-30 Пфайзер Инк. Новые хинолиновые производные
JP2007526324A (ja) 2004-03-02 2007-09-13 スミスクライン・ビーチャム・コーポレイション Akt活性のある阻害剤
GB0410712D0 (en) 2004-05-13 2004-06-16 Novartis Ag Organic compounds
DE102004045796A1 (de) 2004-09-22 2006-03-23 Merck Patent Gmbh Arzneimittel enthaltend Carbonylverbindungen sowie deren Verwendung
AR053992A1 (es) 2004-12-22 2007-05-30 Astrazeneca Ab Compuestos quimicos con actividad anticancerosa, un procedimiento para su preparacion, su uso en la preparacion de medicamentos y composicion farmaceutica.
WO2006067446A1 (en) 2004-12-22 2006-06-29 Astrazeneca Ab Pyridine carboxamide derivatives for use as anticancer agents
KR100919905B1 (ko) 2005-01-26 2009-10-06 아이알엠 엘엘씨 단백질 키나제 억제제로서의 화합물 및 조성물
AU2006225355B2 (en) 2005-03-21 2010-12-09 Helsinn Healthcare Sa Imidazo(1,2-a)pyridine derivatives: preparation and pharmaceutical applications
GB0507575D0 (en) 2005-04-14 2005-05-18 Novartis Ag Organic compounds
DE602006020295D1 (de) * 2005-07-29 2011-04-07 Hoffmann La Roche Azabenzimidalzolderivate, ihre herstellung und ihre verwendung als antikrebsmittel
US7754717B2 (en) 2005-08-15 2010-07-13 Amgen Inc. Bis-aryl amide compounds and methods of use
CN101300233A (zh) 2005-09-09 2008-11-05 先灵公司 氮杂稠合的细胞周期蛋白依赖性激酶抑制剂
RU2008127263A (ru) 2005-12-08 2010-01-20 Новартис АГ (CH) ПИРАЗОЛ [1,5-a] ПИРИДИН-3-КАРБОНОВЫЕ КИСЛОТЫ В КАЧЕСТВЕ ИНГИБИТОРОВ EphB-И VEGFR2-КИНАЗЫ
WO2007083978A1 (en) * 2006-01-23 2007-07-26 Crystalgenomics, Inc. Imidazopyridine derivatives inhibiting protein kinase activity, method for the preparation thereof and pharmaceutical composition containing same
GB0604937D0 (en) 2006-03-10 2006-04-19 Novartis Ag Organic compounds
MX2008012617A (es) 2006-03-31 2008-10-10 Novartis Ag Compuestos organicos.
WO2007149395A2 (en) 2006-06-20 2007-12-27 Amphora Discovery Corporation 2,5-substituted oxazole derivatives as protein kinase inhibitors for the treatment of cancer
PE20080403A1 (es) 2006-07-14 2008-04-25 Amgen Inc Derivados heterociclicos fusionados y metodos de uso
CN101511828A (zh) * 2006-09-06 2009-08-19 霍夫曼-拉罗奇有限公司 作为蛋白激酶抑制剂的杂芳基衍生物
US20100048539A1 (en) 2006-11-03 2010-02-25 Irm Llc Compounds and compositions as protein kinase inhibitors
RS57741B1 (sr) 2006-11-22 2018-12-31 Incyte Holdings Corp Imidazotriazini i imidazopirimidini kao inhibitori kinaze
CA2672213C (en) 2006-12-22 2016-02-16 Astex Therapeutics Limited Bicyclic amine derivatives as protein tyrosine kinase inhibitors
ES2449482T3 (es) 2007-01-09 2014-03-19 Amgen Inc. Derivados de bis-aril-amida útiles para el tratamiento de cáncer
WO2008134553A1 (en) 2007-04-26 2008-11-06 Xenon Pharmaceuticals Inc. Methods of using bicyclic compounds in treating sodium channel-mediated diseases
WO2008144253A1 (en) 2007-05-14 2008-11-27 Irm Llc Protein kinase inhibitors and methods for using thereof
CA2689514C (en) 2007-06-05 2015-09-29 Takeda Pharmaceutical Company Limited Heterobicyclic compounds as kinase inhibitors
CA2691987C (en) 2007-06-12 2016-08-16 Achaogen, Inc. Antibacterial agents
WO2009012283A1 (en) 2007-07-17 2009-01-22 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
RU2527177C2 (ru) 2007-12-20 2014-08-27 Энвиво Фармасьютикалз, Инк. Четырехзамещенные бензолы
US20100324086A1 (en) 2008-02-19 2010-12-23 Novasaid Ab Compounds and methods
AU2009246687B2 (en) 2008-05-13 2012-08-09 Irm Llc Fused nitrogen containing heterocycles and compositions thereof as kinase inhibitors
WO2010017047A1 (en) 2008-08-05 2010-02-11 Merck & Co., Inc. Therapeutic compounds
EP2210891A1 (en) 2009-01-26 2010-07-28 Domain Therapeutics New adenosine receptor ligands and uses thereof
WO2010088000A2 (en) 2009-02-02 2010-08-05 Angion Biomedica Corp. Antifibrotic compounds and uses thereof
TR201900259T4 (tr) 2009-08-17 2019-02-21 Intellikine Llc Heterosiklik Bileşikler Ve Bunların Kullanımları
WO2011050245A1 (en) 2009-10-23 2011-04-28 Yangbo Feng Bicyclic heteroaryls as kinase inhibitors
EP2937345B1 (en) 2009-12-29 2018-03-21 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
EP2579888A2 (en) 2010-06-09 2013-04-17 Receptos, Inc. Novel glp-1 receptor stabilizers and modulators
WO2012007539A1 (en) 2010-07-14 2012-01-19 Novartis Ag Ip receptor agonist heterocyclic compounds
EP2601208B1 (en) * 2010-08-03 2015-02-11 Graffinity Pharmaceuticals GmbH LIGANDS FOR ANTIBODY AND Fc-FUSION PROTEIN PURIFICATION BY AFFINITY CHROMATOGRAPHY
KR101477156B1 (ko) 2010-08-25 2014-12-29 (주)네오팜 신규한 헤테로고리 화합물 및 이를 이용한 염증성 질환 치료용 조성물
US9199981B2 (en) 2011-09-01 2015-12-01 Novartis Ag Compounds and compositions as C-kit kinase inhibitors
UY34305A (es) 2011-09-01 2013-04-30 Novartis Ag Derivados de heterociclos bicíclicos para el tratamiento de la hipertensión arterial pulmonar

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