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

    • 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
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non 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
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (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) CN105001218B (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 (22)

* 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
US8883819B2 (en) 2011-09-01 2014-11-11 Irm Llc Bicyclic heterocycle derivatives for the treatment of pulmonary arterial hypertension
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
KR20210102887A (ko) 2018-11-14 2021-08-20 알타반트 사이언시스 게엠베하 말초 세로토닌과 관련된 질병 또는 장애를 치료하기 위한 트립토판 하이드록실라제 1 (tph1)의 결정질 스피로사이클릭 화합물 억제제
CN115315421B (zh) * 2019-12-13 2024-12-03 日本新药株式会社 作为pdgf受体激酶抑制剂的化合物和组合物
MX2022016581A (es) 2020-06-19 2023-02-01 Univ Yale Polimeros de poli(amina-co-ester) con grupos de extremo modificado y liberacion pulmonar mejorada.
US20220031633A1 (en) * 2020-07-28 2022-02-03 Yale University Poly(amine-co-ester) polymeric particles for selective pulmonary delivery
WO2022136509A1 (en) 2020-12-23 2022-06-30 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
WO2023247593A1 (en) 2022-06-22 2023-12-28 Actelion Pharmaceuticals Ltd Pyrrolopyridine 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
WO2023247595A1 (en) 2022-06-22 2023-12-28 Actelion Pharmaceuticals Ltd Pyrazolopyrazine 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
EP4626884A1 (en) 2022-11-30 2025-10-08 Blueprint Medicines Corporation N-phenyl-pyrazolo[1,5-a]pyridine-3-carboxamide derivatives as wild type c-kit kinase inhibitors for the treatment of urticaria

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 (fr) 1992-03-13 1993-09-16 Tokyo Tanabe Company Limited Nouveau derive de carbostyrile
WO1993019750A1 (en) 1992-04-02 1993-10-14 Smithkline Beecham Corporation Compounds useful for treating allergic or inflammatory diseases
CA2133439C (en) 1992-04-02 2005-07-26 Siegfried Benjamin Christensen, Iv Compounds useful for treating allergic and inflammatory diseases
US5605923A (en) 1992-04-02 1997-02-25 Smithkline Beecham Corporation Compounds useful for treating inflammatory diseases and inhibiting production of tumor necrosis factor
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
SK287878B6 (sk) 1996-02-21 2012-02-03 Schering Corporation Powdered medication inhaler
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
EP1040108B1 (en) 1997-12-19 2004-02-25 Schering Aktiengesellschaft Ortho-anthranilamide derivatives as anti-coagulants
US6362371B1 (en) 1998-06-08 2002-03-26 Advanced Medicine, Inc. β2- adrenergic receptor agonists
WO2000000531A1 (en) 1998-06-30 2000-01-06 The Dow Chemical Company Polymer polyols and a process for the production thereof
DE19834047A1 (de) 1998-07-29 2000-02-03 Bayer Ag Substituierte Pyrazolderivate
DE19834044A1 (de) 1998-07-29 2000-02-03 Bayer Ag Neue substituierte Pyrazolderivate
ID27652A (id) 1998-08-04 2001-04-19 Astrazeneca Ab Turunan amida yang digunakan sebagai inhibitor produksi sitokina
JP2002539187A (ja) 1999-03-17 2002-11-19 アストラゼネカ アクチボラグ アミド誘導体
GB9913083D0 (en) 1999-06-04 1999-08-04 Novartis Ag Organic compounds
TR200103214T2 (tr) 1999-05-04 2002-03-21 Schering Corporation CCR5 antagonistleri olarak yararlì piperazin trevleri.
EP1175402B1 (en) 1999-05-04 2005-07-20 Schering Corporation Piperidine 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.
CZ302882B6 (cs) 1999-08-21 2012-01-04 Nycomed Gmbh Farmaceutický prostredek
DE19943634A1 (de) 1999-09-13 2001-04-12 Bayer Ag Neuartige Dicarbonsäurederivate mit pharmazeutischen Eigenschaften
DE19943635A1 (de) 1999-09-13 2001-03-15 Bayer Ag Neuartige Aminodicarbonsäurederivate 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
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.
CN1426401A (zh) 2000-04-27 2003-06-25 贝林格尔英格海姆法玛公司 新的长效倍他米美类药物(betamimetics)其制备方法,及其作为药物组合物的用途
AU2001266100B9 (en) 2000-06-27 2005-10-06 Laboratorios S.A.L.V.A.T., S.A. 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
PT1305329E (pt) 2000-08-05 2007-12-24 Glaxo Group Ltd Éster s-fluorometílico do ácido 6.alfa.,9.alfa.-difluoro- 17.alfa.-(2-furanilcarboxil)oxi-11.beta.-hidroxi-16.alfa.-metil- 3-oxo-androsta-1,4-dieno-17-carbotióico como um agente antiinflamatório
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
NZ526580A (en) 2000-12-22 2005-04-29 Almirall Prodesfarma Ag Quinuclidine carbamate derivatives and their use as M3 antagonists
WO2002053564A2 (en) 2000-12-28 2002-07-11 Almirall Prodesfarma Ag Quinuclidine derivatives and their use as m3 antagonists
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
DE10110749A1 (de) 2001-03-07 2002-09-12 Bayer Ag Substituierte Aminodicarbonsäurederivate
DE10110750A1 (de) 2001-03-07 2002-09-12 Bayer Ag Neuartige Aminodicarbonsäurederivate mit pharmazeutischen Eigenschaften
JP2004526720A (ja) 2001-03-08 2004-09-02 グラクソ　グループ　リミテッド βアドレナリン受容体のアゴニスト
ATE381537T1 (de) 2001-03-22 2008-01-15 Glaxo Group Ltd Formanilid-derivative als beta2-adrenorezeptor- agonisten
MY137522A (en) 2001-04-30 2009-02-27 Glaxo Group Ltd Novel anti-inflammatory androstane derivatives.
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.
DK2327767T3 (en) 2001-06-21 2015-07-27 Basf Enzymes Llc nitrilases
RU2312854C2 (ru) 2001-09-14 2007-12-20 Глаксо Груп Лимитед Производные фенэтаноламина для лечения респираторных заболеваний
KR20050030169A (ko) 2001-10-17 2005-03-29 유씨비 소시에떼아노님 퀴누클리딘 유도체, 이의 제조 방법 및 ｍ2 및/또는 ｍ3무스카린 수용체 억제제로서의 이의 용도
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
WO2003042160A1 (en) 2001-11-13 2003-05-22 Theravance, Inc. Aryl aniline beta-2 adrenergic receptor agonists
TWI249515B (en) 2001-11-13 2006-02-21 Theravance Inc Aryl aniline beta2 adrenergic receptor agonists
AU2002356759A1 (en) 2001-12-01 2003-06-17 Glaxo Group Limited 17.alpha. -cyclic esters of 16-methylpregnan-3,20-dione as anti-inflammatory agents
RS52522B (sr) 2001-12-20 2013-04-30 Chiesi Farmaceutici S.P.A. Derivati 1-alkil-1-azoniabiciklo/2.2.2./oktan karbamata i njihova upotreba kao antagonista muskarinskih receptora
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
GB0204719D0 (en) 2002-02-28 2002-04-17 Glaxo Group Ltd Medicinal compounds
AU2003220190A1 (en) 2002-03-13 2003-09-29 Pharmacia & Upjohn Company Llc Pyrazolo(1,5-a)pyridine derivatives as neurotransmitter modulators
US7268152B2 (en) 2002-03-26 2007-09-11 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
HRP20040887A2 (en) 2002-03-26 2005-04-30 Boehringer Ingelheim Pharmaceuticals Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
ATE496620T1 (de) 2002-04-11 2011-02-15 Merck Sharp & Dohme 1h-benzo(f)indazol-5-yl-derivate als selektive glucocorticoid-rezeptor-modulatoren
ES2206021B1 (es) 2002-04-16 2005-08-01 Almirall Prodesfarma, S.A. Nuevos derivados de pirrolidinio.
DE60318193T2 (de) 2002-04-25 2008-12-04 Glaxo Group Ltd., Greenford Phenethanolaminderivate
DE10220570A1 (de) 2002-05-08 2003-11-20 Bayer Ag Carbamat-substituierte Pyrazolopyridine
EP1507754A1 (en) 2002-05-28 2005-02-23 Theravance, Inc. Alkoxy aryl beta-2 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
AU2003243870B2 (en) 2002-06-25 2008-11-20 Merck Frosst Canada Ltd 8-(biaryl) quinoline PDE4 inhibitors
WO2004005258A1 (en) 2002-07-02 2004-01-15 Merck Frosst Canada & Co. Di-aryl-substituted-ethane pyridone pde4 inhibitors
ES2204295B1 (es) 2002-07-02 2005-08-01 Almirall Prodesfarma, S.A. Nuevos derivados de quinuclidina-amida.
AU2003281355A1 (en) 2002-07-08 2004-01-23 Pfizer Products Inc. Modulators of the glucocorticoid receptor
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
WO2004018449A1 (en) 2002-08-10 2004-03-04 Altana Pharma Ag Piperidine-derivatives as pde4 inhibitors
CA2494643A1 (en) 2002-08-10 2004-03-04 Altana Pharma Ag Piperidine-n-oxide-derivatives
DE60313472T2 (de) 2002-08-10 2008-01-24 Nycomed Gmbh Pyrrolidindion-substituierte piperidin-phthalazone als pde4-inhibitoren
EP1556369A1 (en) 2002-08-10 2005-07-27 ALTANA Pharma AG Pyridazinone-derivatives as pde4 inhibitors
JP2005537312A (ja) 2002-08-17 2005-12-08 アルタナ　ファルマ　アクチエンゲゼルシャフト 新規のフェナントリジン
US20060113968A1 (en) 2002-08-17 2006-06-01 Altana Pharma Ag Novel benzonaphthyridines
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
SE0202483D0 (sv) 2002-08-21 2002-08-21 Astrazeneca Ab Chemical compounds
WO2004018422A1 (en) 2002-08-23 2004-03-04 Ranbaxy Laboratories Limited Fluoro and sulphonylamino containing 3,6-disubstituted azabicyclo (3.1.0) hexane derivatives as muscarinic receptor antagonists
ATE353217T1 (de) 2002-08-29 2007-02-15 Altana Pharma Ag 3-hydroxy-6-phenylphenanthridine als pde-4 inhibitoren
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
EP1539141B1 (en) 2002-08-29 2010-07-14 Boehringer Ingelheim Pharmaceuticals Inc. 3-(sulfonamidoethyl)-indole derivatives for use as glucocorticoid mimetics in the treatment of inflammatory, allergic and proliferative diseases
GB0220730D0 (en) 2002-09-06 2002-10-16 Glaxo Group Ltd Medicinal compounds
BR0314304A (pt) 2002-09-18 2005-07-26 Ono Pharmaceutical Co Drogas e derivados de triazapiro[5.5]undecano compreendendo o mesmo como o ingrediente ativo
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
ATE378336T1 (de) 2002-09-19 2007-11-15 Schering Corp Imidazopyridine als hemmstoffe cyclin abhängiger kinasen
US7151104B2 (en) 2002-09-19 2006-12-19 Schering Corporation Pyrazolopyridines as cyclin dependent kinase inhibitors
EP1542996A4 (en) 2002-09-20 2009-11-18 Merck & Co Inc OCTAHYDRO-2H-NAPHTOc1,2-F INDOL-4-CARBONSUUREAMIDE DERIVATIVES AS SELECTIVE MODULATORS OF THE GLUCOCORTICOID RECEPTOR
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
EP1440966A1 (en) 2003-01-10 2004-07-28 Pfizer Limited Indole derivatives useful for the treatment of diseases
OA12938A (en) 2002-10-11 2006-10-13 Pfizer Indole derivatives as beta-2 agonists.
AU2003298094A1 (en) 2002-10-22 2004-05-13 Glaxo Group Limited Medicinal arylethanolamine compounds
US7238725B2 (en) 2002-10-23 2007-07-03 Glenmark Pharmaceuticals Ltd. Tricyclic compounds useful for the treatment of inflammatory and allergic disorders: process for their preparation and pharmaceutical compositions containing them
EP1556342B1 (en) 2002-10-28 2008-03-26 Glaxo Group Limited 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
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
JP4606408B2 (ja) 2003-01-21 2011-01-05 メルク・シャープ・エンド・ドーム・コーポレイション 選択的グルココルチコイド受容体調節物質としての１７−カルバモイルオキシコルチゾル誘導体
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
CA2514733A1 (en) 2003-02-28 2004-09-16 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, 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
BRPI0408420A (pt) 2003-04-03 2006-03-21 Merck Patent Gmbh compostos de carbonila
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
CA2545711A1 (en) 2003-11-13 2005-06-02 Ambit Biosciences Corporation Urea derivatives as kinase modulators
KR100807920B1 (ko) 2003-12-23 2008-02-27 화이자 인코포레이티드 신규한 퀴놀린 유도체
EP1720855A4 (en) 2004-03-02 2008-12-17 Smithkline Beecham Corp HEMMER OF ACT ACTIVITY
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
CA2589773A1 (en) 2004-12-22 2006-06-29 Astrazeneca Ab Pyridine carboxamide derivatives for use as anticancer agents
TW200635899A (en) 2004-12-22 2006-10-16 Astrazeneca Ab Chemical compounds
CN101106990B (zh) 2005-01-26 2010-12-08 Irm责任有限公司 用作蛋白激酶抑制剂的化合物和组合物
MY147647A (en) 2005-03-21 2012-12-31 S Bio Pte Ltd Imidazo [1,2-a] pyridine derivatives : preparation and pharmaceutical applications
GB0507575D0 (en) 2005-04-14 2005-05-18 Novartis Ag Organic compounds
CN101208338B (zh) * 2005-07-29 2010-12-29 霍夫曼-拉罗奇有限公司 氮杂苯并咪唑衍生物，它们的制备以及作为抗癌剂的应用
US7754717B2 (en) 2005-08-15 2010-07-13 Amgen Inc. Bis-aryl amide compounds and methods of use
EP1931641B1 (en) 2005-09-09 2010-08-25 Schering Corporation NOVEL 4-CYANO, 4-AMINO, AND 4-AMINOMETHYL DERIVATIVES OF PYRAZOLO[1,5-a]PYRIDINES, PYRAZOLO[1,5-c]PYRIMIDINES AND 2H-INDAZOLE COMPOUNDS AND 5-CYANO, 5-AMINO, AND 5-AMINOMETHYL DERIVATIVES OF IMIDAZO[1,2-a]PYRIDINES, AND IMIDAZO[1,5-a]PYRAZINES COMPOUNDS AS CYCLIN DEPENDENT KINASE INHI
AU2006322187A1 (en) 2005-12-08 2007-06-14 Novartis Ag Pyrazolo[1,5-a]pyridine-3-carboxylic acids as EphB and VEGFR2 kinase inhibitors
KR20070077468A (ko) * 2006-01-23 2007-07-26 크리스탈지노믹스(주) 단백질 키나아제 활성을 저해하는 이미다조피리딘 유도체,이의 제조방법 및 이를 함유하는 약학 조성물
GB0604937D0 (en) 2006-03-10 2006-04-19 Novartis Ag Organic compounds
US8097617B2 (en) 2006-03-31 2012-01-17 Novartis Ag Organic compounds
US20080015193A1 (en) 2006-06-20 2008-01-17 Mendoza Jose S Certain azoles exhibiting ATP-utilizing enzyme inhibitory activity, compositions, and uses thereof
PE20080403A1 (es) 2006-07-14 2008-04-25 Amgen Inc Derivados heterociclicos fusionados y metodos de uso
MX2009002010A (es) * 2006-09-06 2009-03-05 Hoffmann La Roche Derivados de heteroarilo como inhibidores de la proteina cinasa.
CA2668190A1 (en) 2006-11-03 2008-05-15 Irm Llc Compounds and compositions as protein kinase inhibitors
KR101532256B1 (ko) 2006-11-22 2015-06-29 인사이트 코포레이션 키나제 억제제로서의 이미다조트리아진 및 이미다조피리미딘
MX2009006704A (es) 2006-12-22 2009-06-30 Astex Therapeutics Ltd Derivados de amina triciclicos como inhibidores de proteina de tirosina cinasa.
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
JP5539864B2 (ja) 2007-06-12 2014-07-02 アカオゲン，インコーポレーテッド 抗菌剤
MX2010000617A (es) 2007-07-17 2010-05-17 Plexxikon Inc Compuestos y metodos para modulacion de cinasa, e indicaciones de estos.
US8217064B2 (en) 2007-12-20 2012-07-10 Envivo Pharmaceuticals, Inc. Tetrasubstituted benzenes
US20100324086A1 (en) 2008-02-19 2010-12-23 Novasaid Ab Compounds and methods
EA019507B1 (ru) 2008-05-13 2014-04-30 Айрм Ллк Конденсированные азотсодержащие гетероциклы и содержащие их композиции в качестве ингибиторов киназы
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
GEP201706639B (en) 2009-08-17 2017-03-27 Intellikine Llc Heterocyclic compounds and uses thereof
WO2011050245A1 (en) 2009-10-23 2011-04-28 Yangbo Feng Bicyclic heteroaryls as kinase inhibitors
US9180127B2 (en) 2009-12-29 2015-11-10 Dana-Farber Cancer Institute, Inc. Type II Raf kinase inhibitors
WO2011156655A2 (en) 2010-06-09 2011-12-15 Receptos, Inc. Novel glp-1 receptor stabilizers and modulators
MA34373B1 (fr) 2010-07-14 2013-07-03 Novartis Ag Composés hétérocycliques agonistes du récepteur ip
JP2013538798A (ja) * 2010-08-03 2013-10-17 グラフィニティ ファーマシューティカルズ ゲーエムベーハー アフィニティクロマトグラフィーによる抗体およびＦｃ融合タンパク質精製のためのリガンド
KR101477156B1 (ko) 2010-08-25 2014-12-29 (주)네오팜 신규한 헤테로고리 화합물 및 이를 이용한 염증성 질환 치료용 조성물
US8883819B2 (en) * 2011-09-01 2014-11-11 Irm Llc Bicyclic heterocycle derivatives for the treatment of pulmonary arterial hypertension
US9199981B2 (en) 2011-09-01 2015-12-01 Novartis Ag Compounds and compositions as C-kit kinase inhibitors

Also Published As

Publication number Publication date
CN104024252A (zh) 2014-09-03
PL2751108T3 (pl) 2016-11-30
CA2845753C (en) 2021-04-20
EP2751108A1 (en) 2014-07-09
PT2751108T (pt) 2016-08-04
IL231228A0 (en) 2014-04-30
PE20141674A1 (es) 2014-11-14
MA35364B1 (fr) 2014-08-01
CL2014000459A1 (es) 2014-09-05
US8883819B2 (en) 2014-11-11
CN105001218B (zh) 2017-04-12
ZA201401294B (en) 2015-06-24
WO2013030802A1 (en) 2013-03-07
TN2014000067A1 (en) 2015-07-01
SG11201400253YA (en) 2014-03-28
PH12014500407A1 (en) 2017-04-07
AU2012303674A1 (en) 2014-03-13
US20130237519A1 (en) 2013-09-12
AR087755A1 (es) 2014-04-16
CN104024252B (zh) 2015-08-26
CA2845753A1 (en) 2013-03-07
EA024068B1 (ru) 2016-08-31
NZ621436A (en) 2015-10-30
AP2014007539A0 (en) 2014-03-31
US20150025059A1 (en) 2015-01-22
EA201490543A1 (ru) 2014-07-30
ES2585048T3 (es) 2016-10-03
CO6900139A2 (es) 2014-03-20
EP2751108B1 (en) 2016-04-27
TW201313718A (zh) 2013-04-01
CN105001218A (zh) 2015-10-28
BR112014004631A2 (pt) 2017-03-14
AU2012303674B2 (en) 2015-11-26
MX2014002499A (es) 2014-05-30
JP5815870B2 (ja) 2015-11-17
JP2014527544A (ja) 2014-10-16
US9751876B2 (en) 2017-09-05
MX360316B (es) 2018-10-29
KR101687082B1 (ko) 2016-12-15
BR112014004631B1 (pt) 2020-02-11
UY34305A (es) 2013-04-30
HK1196126A1 (zh) 2015-03-20
AP3818A (en) 2016-09-30
KR20140059272A (ko) 2014-05-15

Similar Documents

Publication Publication Date Title
CR20140099A (es) Derivados de heterociclos bicíclicos para el tratamiento de la hipertensión arterial pulmonar
CO6311079A2 (es) Derivados de aminodihidrotiazina como inhibidores de la enzima bace para el tratamiento de la enfermedad de alzheimer
CR20140084A (es) Derivados de 2-amino-4-(piridin-2-il)-5,6-dihidro-4h-1,3-oxazina y su uso como inhibidores de bace-1 y/o bace-2
DOP2013000027A (es) Derivados de tetrahidro-pirido-pirimidina
CU24083B1 (es) Derivados de oxazina útiles como inhibidores de bace para el tratamiento de trastornos neurológicos
UY33943A (es) Derivados espirocíclicos de isoxazolina como agentes antiparasitarios.
UY32628A (es) Inhibidores de la replicación del virus de la inmunodeficiencia humana
CR20110001A (es) Compuesto heterocíclico y uso del mismo
UY34352A (es) 3-pirimidin-4-il-oxazolidin-2-onas como inhibidores de la idh mutante
MX339899B (es) Compuestos de triazolopiridina como inhibidores de pim cinasa.
CR20110620A (es) Derivados de n-(hetero)aril-pirrolidina de pirazo-4-il-pirrolo[2,3-d]pirimidinas y pirrol-3-il-pirrolo[2,3-d]pirimidinas como ihnibidores de la quinasa janus
CO7071122A2 (es) 1,3-oxazinas como inhibidores de la bace1 y/o de la bace2
CO6390057A2 (es) Indazoles oxazol sustituidos como inhibidores de pi3-quinasa
NZ601024A (en) Arylethynyl derivatives
SV2010003662A (es) Derivados de azetidina y ciclobutano como inhibidores de jak ref. x-19081
UY34067A (es) Compuestos de pirrolidinil urea pirrolidinil tiourea como inhibidores de cinasa trka
ECSP088210A (es) Bencimidazoles sustituidos y métodos de preparación
PE20121617A1 (es) Derivados de oxazina como inhibidores de bace
CR20140111A (es) Heterociclilaminas como inhibidores de pi3k
CR20140161A (es) Benzilindazoles sustituidos para uso como inhibidores de la quinasa bub1 en el tratamiento de enfermedades hiperproliferativas
CU20140072A7 (es) Derivados de dihidro-oxazina y dihidro-pirido-oxazina
UY31538A1 (es) Inhibidores de la polimerasa virica
UY33993A (es) Análogo macrocíclico de la sangliferina y su método de producción
CU20140022A7 (es) Derivados de heterociclos bicíclicos para el tratamiento de la hipertensión arterial pulmonar
ECSP11011150A (es) Derivados de arilciclopropilacetamida útiles como activadores de glucoquinasa