JP5959541B2 - Trk阻害剤としてのピラゾロ[1,5−a]ピリジン - Google Patents

Trk阻害剤としてのピラゾロ[1,5−a]ピリジン Download PDF

Info

Publication number
JP5959541B2
JP5959541B2 JP2013555571A JP2013555571A JP5959541B2 JP 5959541 B2 JP5959541 B2 JP 5959541B2 JP 2013555571 A JP2013555571 A JP 2013555571A JP 2013555571 A JP2013555571 A JP 2013555571A JP 5959541 B2 JP5959541 B2 JP 5959541B2
Authority
JP
Japan
Prior art keywords
formula
compound
fluorophenyl
cancer
independently selected
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.)
Expired - Fee Related
Application number
JP2013555571A
Other languages
English (en)
Japanese (ja)
Other versions
JP2014506599A5 (enExample
JP2014506599A (ja
Inventor
バレンティナ・モルテニ
ファン・イ
ジョン・ローレン
ジェフリー・エム・スミス
ブレントン・ティ・フラット
Original Assignee
ノバルティス アーゲー
ノバルティス アーゲー
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=45815979&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=JP5959541(B2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by ノバルティス アーゲー, ノバルティス アーゲー filed Critical ノバルティス アーゲー
Publication of JP2014506599A publication Critical patent/JP2014506599A/ja
Publication of JP2014506599A5 publication Critical patent/JP2014506599A5/ja
Application granted granted Critical
Publication of JP5959541B2 publication Critical patent/JP5959541B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • 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
    • 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • C07D207/09Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2013555571A 2011-02-25 2012-02-23 Trk阻害剤としてのピラゾロ[1,5−a]ピリジン Expired - Fee Related JP5959541B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161446572P 2011-02-25 2011-02-25
US61/446,572 2011-02-25
PCT/US2012/026377 WO2012116217A1 (en) 2011-02-25 2012-02-23 Compounds and compositions as trk inhibitors

Publications (3)

Publication Number Publication Date
JP2014506599A JP2014506599A (ja) 2014-03-17
JP2014506599A5 JP2014506599A5 (enExample) 2015-03-19
JP5959541B2 true JP5959541B2 (ja) 2016-08-02

Family

ID=45815979

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2013555571A Expired - Fee Related JP5959541B2 (ja) 2011-02-25 2012-02-23 Trk阻害剤としてのピラゾロ[1,5−a]ピリジン

Country Status (28)

Country Link
US (1) US9102671B2 (enExample)
EP (1) EP2678338B1 (enExample)
JP (1) JP5959541B2 (enExample)
KR (1) KR20140014184A (enExample)
CN (1) CN103492384B (enExample)
AP (1) AP2013007103A0 (enExample)
AU (1) AU2012220572A1 (enExample)
BR (1) BR112013021638A2 (enExample)
CA (1) CA2828219A1 (enExample)
CL (1) CL2013002430A1 (enExample)
CO (1) CO6751270A2 (enExample)
CR (1) CR20130410A (enExample)
CU (1) CU20130115A7 (enExample)
DO (1) DOP2013000192A (enExample)
EA (1) EA201391230A1 (enExample)
ES (1) ES2551592T3 (enExample)
GE (1) GEP20156285B (enExample)
GT (1) GT201300209A (enExample)
IL (1) IL227987A0 (enExample)
MA (1) MA34969B1 (enExample)
MX (1) MX2013009767A (enExample)
NI (1) NI201300073A (enExample)
PE (1) PE20140378A1 (enExample)
PH (1) PH12013501758A1 (enExample)
SG (1) SG192795A1 (enExample)
TN (1) TN2013000348A1 (enExample)
WO (1) WO2012116217A1 (enExample)
ZA (1) ZA201306221B (enExample)

Families Citing this family (55)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2464461T3 (es) 2008-09-22 2014-06-02 Array Biopharma, Inc. Compuestos de imidazo[1,2B]piridazina sustituidos como inhibidores de la TRK cinasa
MX2011004204A (es) 2008-10-22 2011-08-12 Array Biopharma Inc Compuestos pirazolo [1,5-a] pirimidina sustituida como inhibidores de cinasa trk.
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
CN102971322B (zh) 2010-05-20 2016-02-17 阵列生物制药公司 作为trk激酶抑制剂的大环化合物
WO2013088257A1 (en) 2011-12-12 2013-06-20 Dr. Reddy's Laboratories Ltd. Substituted heterocyclic compounds as tropomyosin receptor kinase a (trka) inhibitors
US10407509B2 (en) 2013-07-30 2019-09-10 Blueprint Medicines Corporation NTRK2 fusions
EA201890061A3 (ru) * 2013-12-26 2018-09-28 Игнита, Инк. Производные пиразоло[1,5-a]пиридина и способы их применения
EP3102555B1 (en) * 2014-02-05 2021-05-12 VM Oncology LLC Compositions of compounds and uses thereof
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
CA2967951C (en) 2014-11-16 2023-11-07 Array Biopharma, Inc. Crystalline form of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate
CN104529815B (zh) * 2014-12-04 2016-08-24 宁波欧迅化学新材料技术有限公司 合成2,4-二硝基苯氧胺的方法
US20180177792A1 (en) * 2015-05-29 2018-06-28 Ignyta, Inc. Compositions and methods for treating patients with rtk mutant cells
US20180140604A1 (en) 2015-06-01 2018-05-24 Loxo Oncology, Inc. Methods of diagnosing and treating cancer
CN108349969B (zh) 2015-07-16 2022-05-10 阵列生物制药公司 作为RET激酶抑制剂的取代的吡唑并[1,5-a]吡啶化合物
WO2017075107A1 (en) 2015-10-26 2017-05-04 Nanda Nisha Point mutations in trk inhibitor-resistant cancer and methods relating to the same
DK3439662T3 (da) 2016-04-04 2024-09-02 Loxo Oncology Inc Væskeformige formuleringer af (s)-n-(5-((r)-2-(2,5-difluorphenyl)-pyrrolidin-1-yl)-pyrazol[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidin-1-carboxamid
PL3439663T3 (pl) 2016-04-04 2024-11-18 Loxo Oncology, Inc. Sposoby leczenia nowotworów wieku dziecięcego
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
US11214571B2 (en) 2016-05-18 2022-01-04 Array Biopharma Inc. Process for the preparation of (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide and salts thereof
CN109843889B (zh) 2016-08-01 2022-03-15 阿普廷伊克斯股份有限公司 螺-内酰胺nmda调节剂和使用其的方法
BR112019001768A2 (pt) 2016-08-01 2019-06-11 Aptinyx Inc moduladores do receptor de spiro-lactamas nmda e usos dos mesmos
SG11201900558RA (en) 2016-08-01 2019-02-27 Aptinyx Inc Spiro-lactam nmda receptor modulators and uses thereof
JOP20190077A1 (ar) 2016-10-10 2019-04-09 Array Biopharma Inc مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret
TWI704148B (zh) 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
CN108003161B (zh) * 2016-10-28 2020-10-09 正大天晴药业集团股份有限公司 神经营养因子酪氨酸激酶受体抑制剂
EP3533796B1 (en) 2016-10-28 2021-09-29 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Amino pyrazolopyrimidine compound used as neurotrophic factor tyrosine kinase receptor inhibitor
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
ES2948194T3 (es) 2017-01-18 2023-09-01 Array Biopharma Inc Compuestos de pirazolo[1,5-a]pirazina sustituida como inhibidores de la cinasa RET
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
CN113735881A (zh) 2017-08-23 2021-12-03 正大天晴药业集团股份有限公司 含有氨基吡唑并嘧啶的大环化合物及其药物组合物和用途
TWI812649B (zh) 2017-10-10 2023-08-21 美商絡速藥業公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物
TWI791053B (zh) 2017-10-10 2023-02-01 美商亞雷生物製藥股份有限公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物
WO2019084285A1 (en) 2017-10-26 2019-05-02 Qian Zhao FORMULATIONS OF A MACROCYCLIC TRK KINASE INHIBITOR
CN111971286B (zh) 2018-01-18 2023-04-14 阿雷生物药品公司 作为RET激酶抑制剂的取代的吡咯并[2,3-d]嘧啶化合物
US11472802B2 (en) 2018-01-18 2022-10-18 Array Biopharma Inc. Substituted pyrazolyl[4,3-c]pyridine compounds as RET kinase inhibitors
CN111630054B (zh) 2018-01-18 2023-05-09 奥瑞生物药品公司 作为RET激酶抑制剂的取代的吡唑并[3,4-d]嘧啶化合物
MA52218A (fr) 2018-03-29 2021-02-17 Loxo Oncology Inc Traitement de cancers associés à trk
CN117281803A (zh) 2018-07-31 2023-12-26 罗索肿瘤学公司 喷雾干燥的分散体和制剂
WO2020055672A1 (en) 2018-09-10 2020-03-19 Array Biopharma Inc. Fused heterocyclic compounds as ret kinase inhibitors
CN111171019A (zh) * 2018-11-13 2020-05-19 上海轶诺药业有限公司 一类五元并六元杂环化合物及其作为蛋白受体激酶抑制剂的用途
EP3898626A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
EP3898615A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
WO2020187291A1 (zh) 2019-03-19 2020-09-24 华中师范大学 吡唑并嘧啶化合物和药物组合物及其应用
CN114364798A (zh) 2019-03-21 2022-04-15 欧恩科斯欧公司 用于治疗癌症的Dbait分子与激酶抑制剂的组合
KR102731401B1 (ko) 2019-05-08 2024-11-15 티와이케이 메디슨즈, 인코포레이티드 키나아제 억제제로 사용되는 화합물 및 이의 응용
CN110804059B (zh) * 2019-09-30 2024-03-12 郑州泰基鸿诺医药股份有限公司 氨基甲酸酯类化合物、药物组合物及其应用
CN110643672A (zh) * 2019-10-15 2020-01-03 西安交通大学 高表达TrkB作为新型靶点在抑制胰腺癌转移方面的医药用途
US20220401436A1 (en) 2019-11-08 2022-12-22 INSERM (Institute National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
CN112979654B (zh) * 2019-12-16 2024-03-19 赛诺哈勃药业(成都)有限公司 杂芳基稠环化合物、其制备方法及应用
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
MX2022008930A (es) * 2020-01-22 2022-10-18 Benevolentai Bio Ltd Composiciones farmaceuticas y sus usos.
CN112779518B (zh) * 2020-12-17 2022-07-22 东北师范大学 一种高发光强度的薄膜、制备方法及其用途
CN112645955B (zh) * 2020-12-24 2022-11-04 四川国康药业有限公司 一种[1,2,4]三唑并[4,3-b]哒嗪类化合物及其制备方法和用途
CN112979646B (zh) * 2021-03-08 2022-01-14 北京富龙康泰生物技术有限公司 一种咪唑并吡啶类衍生物

Family Cites Families (197)

* 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
GB8334494D0 (en) 1983-12-24 1984-02-01 Tanabe Seiyaku Co Carbostyril derivatives
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
GB8916480D0 (en) 1989-07-19 1989-09-06 Glaxo Group Ltd Chemical process
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
US5451700A (en) 1991-06-11 1995-09-19 Ciba-Geigy Corporation Amidino compounds, their manufacture and methods of treatment
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
US5605923A (en) 1992-04-02 1997-02-25 Smithkline Beecham Corporation Compounds useful for treating inflammatory diseases and inhibiting production of tumor necrosis factor
SK279958B6 (sk) 1992-04-02 1999-06-11 Smithkline Beecham Corporation Zlúčeniny s protialergickým a protizápalovým účink
GB9301000D0 (en) 1993-01-20 1993-03-10 Glaxo Group Ltd Chemical compounds
GB9414193D0 (en) 1994-07-14 1994-08-31 Glaxo Group Ltd Compounds
GB9414208D0 (en) 1994-07-14 1994-08-31 Glaxo Group Ltd Compounds
GB9622386D0 (en) 1996-10-28 1997-01-08 Sandoz Ltd Organic compounds
TW528755B (en) 1996-12-24 2003-04-21 Glaxo Group Ltd 2-(purin-9-yl)-tetrahydrofuran-3,4-diol derivatives
AU9281298A (en) 1997-10-01 1999-04-23 Kyowa Hakko Kogyo Co. Ltd. Benzodioxole derivatives
GB9723566D0 (en) 1997-11-08 1998-01-07 Glaxo Group Ltd Chemical compounds
GB9723589D0 (en) 1997-11-08 1998-01-07 Glaxo Group Ltd Chemical compounds
GB9723590D0 (en) 1997-11-08 1998-01-07 Glaxo Group Ltd Chemical compounds
YU44900A (sh) 1998-01-31 2003-01-31 Glaxo Group Limited Derivati 2-(purin-9-il)tetrahidrofuran-3,4-diola
PE20000270A1 (es) 1998-02-14 2000-05-20 Glaxo Group Ltd Derivados de 2-(purin-9-il)-tetrahidrofuran-3,4-diol
US6362371B1 (en) 1998-06-08 2002-03-26 Advanced Medicine, Inc. β2- adrenergic receptor agonists
GB9813535D0 (en) 1998-06-23 1998-08-19 Glaxo Group Ltd Chemical compounds
EE200000768A (et) 1998-06-23 2002-04-15 Glaxo Group Limited 2-(puriin-9-üül)tetrahüdrofuraan-3,4-diooli derivaadid
GB9813565D0 (en) 1998-06-23 1998-08-19 Glaxo Group Ltd Chemical compounds
GB9813540D0 (en) 1998-06-23 1998-08-19 Glaxo Group Ltd Chemical compounds
DE69827673T2 (de) 1998-06-30 2005-04-21 Dow Global Technologies Inc Polymerpolyole und ein verfahren zu ihrer darstellung
ES2264826T3 (es) 1998-10-16 2007-01-16 Pfizer Inc. Derivados de adenina.
GB9913083D0 (en) 1999-06-04 1999-08-04 Novartis Ag Organic compounds
YU25500A (sh) 1999-05-11 2003-08-29 Pfizer Products Inc. Postupak za sintezu analoga nukleozida
US6683115B2 (en) 1999-06-02 2004-01-27 Theravance, Inc. β2-adrenergic receptor agonists
GB9913932D0 (en) 1999-06-15 1999-08-18 Pfizer Ltd Purine derivatives
US6322771B1 (en) 1999-06-18 2001-11-27 University Of Virginia Patent Foundation Induction of pharmacological stress with adenosine receptor agonists
ES2165768B1 (es) 1999-07-14 2003-04-01 Almirall Prodesfarma Sa Nuevos derivados de quinuclidina y composiciones farmaceuticas que los contienen.
CA2715683A1 (en) 1999-08-21 2001-03-01 Nycomed Gmbh Synergistic combination
CO5180581A1 (es) 1999-09-30 2002-07-30 Pfizer Prod Inc Compuestos para el tratamiento de la isquemia ciones farmaceuticas que los contienen para el tratamiento de la isquemia
GB9924361D0 (en) 1999-10-14 1999-12-15 Pfizer Ltd Purine derivatives
GB9924363D0 (en) 1999-10-14 1999-12-15 Pfizer Central Res Purine derivatives
OA11558A (en) 1999-12-08 2004-06-03 Advanced Medicine Inc Beta 2-adrenergic receptor agonists.
GB0003960D0 (en) 2000-02-18 2000-04-12 Pfizer Ltd Purine derivatives
NZ522677A (en) 2000-04-27 2004-10-29 Boehringer Ingelheim Pharma Novel, slow-acting betamimetics, a method for their production and their use as medicaments
TWI227240B (en) 2000-06-06 2005-02-01 Pfizer 2-aminocarbonyl-9H-purine derivatives
GB0015727D0 (en) 2000-06-27 2000-08-16 Pfizer Ltd Purine derivatives
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
JP2002114788A (ja) * 2000-08-03 2002-04-16 Banyu Pharmaceut Co Ltd カルバペネム誘導体の製造方法及び合成中間体
EP1305329B2 (en) 2000-08-05 2015-03-18 Glaxo Group Limited 6.alpha.,9.alpha.-difluoro-17.alpha.-(2-furanylcarboxyl)oxy-11.beta.-hydroxy-16.alpha.-methyl-3-oxo-androst-1,4-diene-17-carbothioic acid s-fluoromethyl ester as an anti-inflammatory agent
GB0022695D0 (en) 2000-09-15 2000-11-01 Pfizer Ltd Purine Derivatives
GB0028383D0 (en) 2000-11-21 2001-01-03 Novartis Ag Organic compounds
WO2002051841A1 (en) 2000-12-22 2002-07-04 Almirall Prodesfarma Ag Quinuclidine carbamate derivatives and their use as m3 antagonists
HUP0303524A3 (en) 2000-12-28 2008-03-28 Almirall Ag Novel quinuclidine derivatives, process for their preparation and medicinal compositions containing the same and their use
GB0103630D0 (en) 2001-02-14 2001-03-28 Glaxo Group Ltd Chemical compounds
EP1366025B1 (en) 2001-03-08 2007-06-27 Glaxo Group Limited Agonists of beta-adrenoreceptors
EP1241176A1 (en) 2001-03-16 2002-09-18 Pfizer Products Inc. Purine derivatives for the treatment of ischemia
WO2002076933A1 (en) 2001-03-22 2002-10-03 Glaxo Group Limited Formailide derivatives as beta2-adrenoreceptor agonists
EP2039700A2 (en) 2001-04-30 2009-03-25 Glaxo Group Limited Novel anti-inflammatory androstane derivatives
IL158774A0 (en) 2001-05-25 2004-05-12 Pfizer An adenosine a2a receptor agonist and an anticholinergic agent in combination for treating obstructive airways diseases
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
DK2327767T3 (en) 2001-06-21 2015-07-27 Basf Enzymes Llc nitrilases
DE60230425D1 (de) 2001-09-14 2009-01-29 Glaxo Group Ltd Phenethanolamin-derivate zur behandlung von erkrankungen der atemwege
WO2003033495A1 (en) 2001-10-17 2003-04-24 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
IL161867A0 (en) 2001-11-09 2005-11-20 Cv Therapeutics Inc A2b adenosine receptor antagonists
US6653323B2 (en) 2001-11-13 2003-11-25 Theravance, Inc. Aryl aniline β2 adrenergic receptor agonists
TWI249515B (en) 2001-11-13 2006-02-21 Theravance Inc Aryl aniline beta2 adrenergic receptor agonists
AU2002356759A1 (en) 2001-12-01 2003-06-17 Glaxo Group Limited 17.alpha. -cyclic esters of 16-methylpregnan-3,20-dione as anti-inflammatory agents
US7452904B2 (en) 2001-12-20 2008-11-18 Chiesi Farmaceutici S.P.A. 1-alkyl-1-azoniabicyclo' 2.2.2 octane carbamate derivatives and their use as muscarinic receptor antagonists
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
WO2004078163A2 (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
GB0204719D0 (en) 2002-02-28 2002-04-17 Glaxo Group Ltd Medicinal compounds
US7268152B2 (en) 2002-03-26 2007-09-11 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
DE60318188T2 (de) 2002-03-26 2008-12-11 Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield Glucocorticoid-mimetika, deren herstellung, pharmazeutische zusammensetzungen und verwendung
WO2003086408A1 (en) 2002-04-10 2003-10-23 University Of Virginia Patent Foundation Use of a2a adenosine receptor agonists for the treatment of inflammatory diseases
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
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
EP1517895B1 (en) 2002-06-25 2007-03-14 Merck Frosst Canada Ltd. 8-(biaryl) quinoline pde4 inhibitors
ES2204295B1 (es) 2002-07-02 2005-08-01 Almirall Prodesfarma, S.A. Nuevos derivados de quinuclidina-amida.
WO2004005258A1 (en) 2002-07-02 2004-01-15 Merck Frosst Canada & Co. Di-aryl-substituted-ethane pyridone pde4 inhibitors
MXPA05000345A (es) 2002-07-08 2005-03-31 Pfizer Prod Inc Moduladores del receptor 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
WO2004018450A1 (en) 2002-08-10 2004-03-04 Altana Pharma Ag Piperidine-n-oxide-derivatives
RS51445B (sr) 2002-08-10 2011-04-30 Nycomed Gmbh. Pirolidindion supstituisan piperidin-ftalazonima kao inhibitorima pde4
CA2494650A1 (en) 2002-08-10 2004-03-04 Altana Pharma Ag Pyridazinone-derivatives as pde4 inhibitors
AU2003255376A1 (en) 2002-08-10 2004-03-11 Altana Pharma Ag Piperidine-derivatives as pde4 inhibitors
AU2003263216A1 (en) 2002-08-17 2004-03-11 Nycomed Gmbh Benzonaphthyridines with PDE 3/4 inhibiting activity
PL374014A1 (en) 2002-08-17 2005-09-19 Altana Pharma Ag Novel phenanthridines having pde 3/4 inhibiting properties
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
EP1534675B1 (en) 2002-08-23 2009-02-25 Ranbaxy Laboratories, Ltd. Fluoro and sulphonylamino containing 3,6-disubstituted azabicyclo¬3.1.0 hexane derivatives as muscarinic receptor antagonists
BR0313923A (pt) 2002-08-29 2005-07-12 Boehringer Ingelheim Pharma Derivados de 3-(sulfonamidoetil)-indol para uso como miméticos de glicocorticóide no tratamento de doenças inflamatórias, alérgicas e proliferativas
EP1536798B1 (en) 2002-08-29 2007-02-07 ALTANA Pharma AG 3-hydroxy-6-phenylphenanthridines as pde-4 inhibitors
ATE348616T1 (de) 2002-08-29 2007-01-15 Altana Pharma Ag 2-hydroxy-6-phenylphenanthridine als pde-4-hemmer
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
AU2003270783C1 (en) 2002-09-20 2010-05-20 Merck Sharp & Dohme Corp. Octahydro-2-H-naphtho[1,2-F] indole-4-carboxamide derivatives as selective glucocorticoid receptor modulators
JP2004107299A (ja) 2002-09-20 2004-04-08 Japan Energy Corp 新規1−置換ウラシル誘導体及びアレルギー性疾患の治療剤
DE10246374A1 (de) 2002-10-04 2004-04-15 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Betamimetika mit verlängerter Wirkungsdauer, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
EP1440966A1 (en) 2003-01-10 2004-07-28 Pfizer Limited Indole derivatives useful for the treatment of diseases
KR20050047552A (ko) 2002-10-11 2005-05-20 화이자 인코포레이티드 베타-2 작용제로서의 인돌 유도체
EP1554264B1 (en) 2002-10-22 2007-08-08 Glaxo Group Limited Medicinal arylethanolamine compounds
PL376769A1 (pl) 2002-10-23 2006-01-09 Glenmark Pharmaceuticals Ltd. Nowe związki tricykliczne użyteczne w leczeniu chorób zapalnych i alergicznych, sposób ich wytwarzania i kompozycje farmaceutyczne je zawierające
GB0225030D0 (en) 2002-10-28 2002-12-04 Glaxo Group Ltd Medicinal compounds
ATE390407T1 (de) 2002-10-28 2008-04-15 Glaxo Group Ltd Phenethanolamin-derivate zur behandlung von atemwegserkrankungen
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
DE10253426B4 (de) 2002-11-15 2005-09-22 Elbion Ag Neue Hydroxyindole, deren Verwendung als Inhibitoren der Phosphodiesterase 4 und Verfahren zu deren Herstellung
DE10253282A1 (de) 2002-11-15 2004-05-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Arzneimittel zur Behandlung von chronisch obstruktiver Lungenerkrankung
DE10253220A1 (de) 2002-11-15 2004-05-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Dihydroxy-Methyl-Phenyl-Derivate, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
DE10261874A1 (de) 2002-12-20 2004-07-08 Schering Ag Nichtsteroidale Entzündungshemmer
DE60317102T3 (de) 2003-01-09 2010-02-18 Astellas Pharma Inc. Pyrrolopyridazinderivate
CA2512987C (en) 2003-01-21 2011-06-14 Merck & Co., Inc. 17-carbamoyloxy cortisol derivatives as selective glucocorticoid receptor modulators
PE20040950A1 (es) 2003-02-14 2005-01-01 Theravance Inc DERIVADOS DE BIFENILO COMO AGONISTAS DE LOS RECEPTORES ADRENERGICOS ß2 Y COMO ANTAGONISTAS DE LOS RECEPTORES MUSCARINICOS
EP1460064A1 (en) 2003-03-14 2004-09-22 Pfizer Limited Indole-2-carboxamide derivatives useful as beta-2 agonists
US7317102B2 (en) 2003-04-01 2008-01-08 Theravance, Inc. Diarylmethyl and related compounds
PL1613315T3 (pl) 2003-04-04 2009-07-31 Novartis Ag Pochodne chinolino-2-onu do leczenia chorób dróg oddechowych
AR044134A1 (es) 2003-05-02 2005-08-24 Novartis Ag Derivados de quinuclidina, metodo de preparacion y composiciones farmaceuticas.
US7268147B2 (en) 2003-05-15 2007-09-11 Pfizer Inc Compounds useful for the treatment of diseases
EP1477167A1 (en) 2003-05-15 2004-11-17 Pfizer Limited [(2-hydroxy-2-(4-hydroxy-3-hydroxymethylphenyl)-ethylamino)-propyl] phenyl derivatives as beta2 agonists
TWI328009B (en) 2003-05-21 2010-08-01 Glaxo Group Ltd Quinoline derivatives as phosphodiesterase inhibitors
JP4616264B2 (ja) 2003-05-28 2011-01-19 セラヴァンス, インコーポレーテッド ムスカリン性レセプターアンタゴニストとしてのアザビシクロアルカン化合物
GB0312832D0 (en) 2003-06-04 2003-07-09 Pfizer Ltd 2-amino-pyridine derivatives useful for the treatment of diseases
BRPI0410660A (pt) 2003-06-04 2006-06-20 Pfizer derivados de 2-amino-piridina como agonistas de adrenoreceptor ß2
JP2006527207A (ja) 2003-06-11 2006-11-30 メルク フロスト カナダ リミテツド 7−(1,3−チアゾール−2−イル)チオ−クマリン誘導体およびそれのロイコトリエン生合成阻害薬としての使用
WO2004111044A1 (en) 2003-06-17 2004-12-23 Glenmark Pharmaceuticals Ltd. Tricyclic compounds useful for the treatment of inflammatory and allergic disorders:process for their preparation
GB0316290D0 (en) 2003-07-11 2003-08-13 Glaxo Group Ltd Novel compounds
ITMI20031451A1 (it) 2003-07-16 2005-01-17 Zambon Spa Derivati diidro-ftalazinici inibitori della fosfodiesterasi 4
EP1658271A1 (en) 2003-07-31 2006-05-24 ALTANA Pharma AG Novel 6-phenylphenanthridines
CA2533635A1 (en) 2003-07-31 2005-02-10 Altana Pharma Ag Novel 6-phenylphenantridines
EP1664026B1 (en) * 2003-08-15 2009-01-21 Merck & Co., Inc. Mitotic kinesin inhibitors
GB0322722D0 (en) 2003-09-27 2003-10-29 Glaxo Group Ltd Compounds
GB0322726D0 (en) 2003-09-27 2003-10-29 Glaxo Group Ltd Compounds
WO2005033121A2 (en) 2003-10-03 2005-04-14 King Pharmaceuticals Research & Development, Inc. Synthesis of 2-aralkyloxyadenosines, 2-alkoxyadenosines, and their analogs
GB0323701D0 (en) 2003-10-09 2003-11-12 Glaxo Group Ltd Formulations
GB0324654D0 (en) 2003-10-22 2003-11-26 Glaxo Group Ltd Medicinal compounds
GB0324886D0 (en) 2003-10-24 2003-11-26 Glaxo Group Ltd Medicinal compounds
GB0329182D0 (en) 2003-12-17 2004-01-21 Glaxo Group Ltd Chemical compounds
US20050133417A1 (en) 2003-12-19 2005-06-23 Bhan Opinder K. Systems, methods, and catalysts for producing a crude product
JP2005187357A (ja) 2003-12-25 2005-07-14 Nippon Suisan Kaisha Ltd 選択的なβ2受容体アゴニスト活性を有するベンゾチアゾロン誘導体の製造方法
DE102004001413A1 (de) 2004-01-09 2005-08-18 Boehringer Ingelheim Pharma Gmbh & Co. Kg 3-Hydroxymethyl-4-Hydroxy-Phenyl-Derivate zur Behandlung von chronisch obstruktiver Lungenerkrankung
TW200531692A (en) 2004-01-12 2005-10-01 Theravance Inc Aryl aniline derivatives as β2 adrenergic receptor agonists
DK1708992T3 (da) 2004-01-22 2007-11-05 Pfizer Sulfonamidderivater til behandling af sygdomme
AU2005214153B2 (en) 2004-01-22 2008-09-18 Pfizer Inc. Sulfonamide derivatives for the treatment of diseases
DE102004003428A1 (de) 2004-01-23 2005-08-11 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue langwirksame Beta-2-Agonisten, und deren Verwendung als Arzneimittel
GB0402797D0 (en) 2004-02-09 2004-03-10 Novartis Ag Organic compounds
US7320990B2 (en) 2004-02-13 2008-01-22 Theravance, Inc. Crystalline form of a biphenyl compound
JP4916317B2 (ja) 2004-02-14 2012-04-11 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規持続作用性β−2−アゴニスト及び薬剤としてのその使用
CA2558391A1 (en) 2004-03-10 2005-09-22 Altana Pharma Ag Novel amido-substituted hydroxy-6-phenylphenanthridines and their use as pde4 inhibitors
KR20060124783A (ko) 2004-03-10 2006-12-05 알타나 파마 아게 신규 티오-함유 히드록시-6-페닐페난트리딘 및 pde4억제제로서의 이의 용도
EP1574501A1 (en) 2004-03-11 2005-09-14 Pfizer Limited Quinolinone derivatives, pharmaceutical compositions containing them and their use
US20070225308A1 (en) 2004-03-15 2007-09-27 Kyowa Hakko Kogyo Co.,Ltd. 2-Amino Quinazoline Derivative
US7671068B2 (en) 2004-03-17 2010-03-02 Nycomed Gmbh N-(alkoxyalkyl) carbamoyl-substituted 6-phenyl-benzonaphthyridine derivatives and their use as PDE ¾ inhibitors
EP1577292A1 (en) 2004-03-17 2005-09-21 Pfizer Limited Phenylaminoethanol derivatives as beta2 receptor agonists
US7244728B2 (en) 2004-03-17 2007-07-17 Boehringer Ingelheim International Gmbh Long acting betamimetics for the treatment of respiratory diseases
WO2005090287A2 (en) 2004-03-17 2005-09-29 Pfizer Limited Phenylethanolamine derivatives as beta-2 agonists
ATE432278T1 (de) 2004-03-23 2009-06-15 Pfizer Verbindungen zur behandlung von krankheiten
US20050215542A1 (en) 2004-03-23 2005-09-29 Pfizer Inc Compounds for the treatment of diseases
WO2005092860A1 (en) 2004-03-23 2005-10-06 Pfizer Limited Compounds for the treatment of diseases
AP2315A (en) 2004-03-23 2011-11-04 Pfizer Formamide derivatives useful as adrenoceptor.
BRPI0509382A (pt) 2004-04-02 2007-09-18 Glaxo Group Ltd processo para a preparação de um sal monocloridrato de composto, monocloridrato cristalino, processo para obter monocloridrato cristalino, método para a profilaxia ou o tratamento de uma condição clìnica em um mamìfero, uso de monocloridrato cristalino, formulação farmacêutica, e, combinação
US20050239778A1 (en) 2004-04-22 2005-10-27 Boehringer Ingelheim International Gmbh Novel medicament combinations for the treatment of respiratory diseases
DE102004019539A1 (de) 2004-04-22 2005-11-10 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Arzneimittel zur Behandlung von Atemwegserkrankungen
US7307076B2 (en) 2004-05-13 2007-12-11 Boehringer Ingelheim International Gmbh Beta agonists for the treatment of respiratory diseases
US7745621B2 (en) 2004-05-14 2010-06-29 Boehringer Ingelheim International Gmbh Long acting bronchodilators for the treatment of respiratory diseases
US20050256115A1 (en) 2004-05-14 2005-11-17 Boehringer Ingelheim International Gmbh Aerosol formulation for the inhalation of beta-agonists
PE20060426A1 (es) * 2004-06-02 2006-06-28 Schering Corp DERIVADOS DE ACIDO TARTARICO COMO INHIBIDORES DE MMPs, ADAMs, TACE Y TNF-alfa
WO2005121065A2 (en) 2004-06-03 2005-12-22 Theravance, Inc. DIAMINE β2 ADRENERGIC RECEPTOR AGONISTS
WO2006014704A1 (en) 2004-07-21 2006-02-09 Theravance, Inc. DIARYL ETHER β2 ADRENERGIC RECEPTOR AGONISTS
GB0416397D0 (en) 2004-07-22 2004-08-25 Glaxo Group Ltd Pharmaceutical formulations
WO2006023460A2 (en) 2004-08-16 2006-03-02 Theravance, Inc. COMPOUNDS HAVING β2 ADRENERGIC RECEPTOR AGONIST AND MUSCARINIC RECEPTOR ANTAGONIST ACTIVITY
US7838597B2 (en) 2004-08-20 2010-11-23 Sekisui Specialty Chemicals America, Llc Fluid loss concentrate for hydraulic cement
EP1786762A2 (en) 2004-09-10 2007-05-23 Theravance, Inc. Amidine substituted aryl aniline compounds
GB0424284D0 (en) 2004-11-02 2004-12-01 Novartis Ag Organic compounds
GB0426164D0 (en) 2004-11-29 2004-12-29 Novartis Ag Organic compounds
WO2006074897A1 (en) 2005-01-11 2006-07-20 Glaxo Group Limited Cinnamate salts of a beta-2 adrenergic agonist
ATE412647T1 (de) * 2005-05-13 2008-11-15 Lilly Co Eli Substituierte n-arylpyrrolidine als selektive modulatoren des androgenrezeptors
PT2206707E (pt) * 2007-10-24 2014-09-25 Astellas Pharma Inc Composto de azolcarboxamida ou um seu sal
JP5492194B2 (ja) * 2008-05-13 2014-05-14 アイアールエム・リミテッド・ライアビリティ・カンパニー キナーゼ阻害剤としての縮合窒素含有ヘテロ環およびその組成物
ES2612731T3 (es) * 2008-08-19 2017-05-18 Janssen Pharmaceutica Nv Antagonistas de receptores al frío de mentol
MX2011004204A (es) 2008-10-22 2011-08-12 Array Biopharma Inc Compuestos pirazolo [1,5-a] pirimidina sustituida como inhibidores de cinasa trk.
TW201022233A (en) * 2008-11-04 2010-06-16 Organon Nv (Pyrrolidin-2-yl)phenyl derivatives
WO2010117787A2 (en) * 2009-03-30 2010-10-14 The Brigham And Women's Hospital, Inc. Inhibiting eph b-3 kinase
AR077468A1 (es) * 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
US8637516B2 (en) 2010-09-09 2014-01-28 Irm Llc Compounds and compositions as TRK inhibitors

Also Published As

Publication number Publication date
EA201391230A1 (ru) 2014-01-30
CR20130410A (es) 2013-10-17
CO6751270A2 (es) 2013-09-16
CN103492384A (zh) 2014-01-01
SG192795A1 (en) 2013-09-30
PE20140378A1 (es) 2014-03-28
GT201300209A (es) 2015-06-02
GEP20156285B (en) 2015-05-11
BR112013021638A2 (pt) 2016-08-02
IL227987A0 (en) 2013-09-30
CN103492384B (zh) 2016-05-11
JP2014506599A (ja) 2014-03-17
MA34969B1 (fr) 2014-03-01
ES2551592T3 (es) 2015-11-20
AU2012220572A1 (en) 2013-08-29
ZA201306221B (en) 2014-04-30
EP2678338A1 (en) 2014-01-01
DOP2013000192A (es) 2014-01-31
US9102671B2 (en) 2015-08-11
CA2828219A1 (en) 2012-08-30
KR20140014184A (ko) 2014-02-05
CU20130115A7 (es) 2013-12-27
MX2013009767A (es) 2013-10-01
AP2013007103A0 (en) 2013-09-30
WO2012116217A1 (en) 2012-08-30
CL2013002430A1 (es) 2013-11-29
PH12013501758A1 (en) 2013-10-14
EP2678338B1 (en) 2015-09-09
US20130331397A1 (en) 2013-12-12
TN2013000348A1 (en) 2015-01-20
NI201300073A (es) 2013-12-17

Similar Documents

Publication Publication Date Title
JP5959541B2 (ja) Trk阻害剤としてのピラゾロ[1,5−a]ピリジン
US8637516B2 (en) Compounds and compositions as TRK inhibitors
JP7248256B2 (ja) Jakキナーゼ阻害剤及びその調製方法、並びにその医薬分野での使用
EP2124951B1 (en) 5-cyan0-4- (pyrrolo[2, 3b]pyridine-3-yl) -pyrimidine derivatives useful as protein kinase inhibitors
JP7297776B2 (ja) ピペリジニル-3-(アリールオキシ)プロパンアミド及びプロパノエート
EA039783B1 (ru) ПРОИЗВОДНЫЕ ТИРОЗИНАМИДА В КАЧЕСТВЕ ИНГИБИТОРОВ Rho-КИНАЗЫ
WO2012034095A1 (en) Compounds and compositions as trk inhibitors
KR20160086930A (ko) 피롤로피롤론 유도체 및 bet 억제제로서의 그의 용도
WO2016100349A2 (en) Bicyclic azaheterocyclic compounds as nr2b nmda receptor antagonists
AU2021249112A1 (en) N-heteroarylalkyl-2-(heterocyclyl and heterocyclylmethyl) acetamide derivatives as SSTR4 agonists
JP7551607B2 (ja) アデノシン受容体アンタゴニストとしての5-アザインダゾール誘導体
TW202417458A (zh) 調節her2的化合物及方法
US12428403B2 (en) N-(heterocyclyl and heterocyclylalkyl)-3-benzylpyridin-2-amine derivatives as SSTR4 agonists

Legal Events

Date Code Title Description
RD04 Notification of resignation of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7424

Effective date: 20141215

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20150127

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20150127

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20150924

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20151020

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20151216

A711 Notification of change in applicant

Free format text: JAPANESE INTERMEDIATE CODE: A711

Effective date: 20160301

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20160607

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20160621

R150 Certificate of patent or registration of utility model

Ref document number: 5959541

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

LAPS Cancellation because of no payment of annual fees