CN105960404B - 布鲁顿氏酪氨酸激酶的抑制剂 - Google Patents

布鲁顿氏酪氨酸激酶的抑制剂 Download PDF

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Publication number
CN105960404B
CN105960404B CN201480074736.1A CN201480074736A CN105960404B CN 105960404 B CN105960404 B CN 105960404B CN 201480074736 A CN201480074736 A CN 201480074736A CN 105960404 B CN105960404 B CN 105960404B
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amino
carboxamide
phenyl
pyrazine
piperidin
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CN105960404A (zh
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兆忠·J·贾
威廉姆·D·托马斯
陈伟
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Pharmacyclics LLC
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Pharmacyclics LLC
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • 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
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
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    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
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    • 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
    • A—HUMAN NECESSITIES
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
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    • A61P19/00—Drugs for skeletal disorders
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    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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    • 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
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  • Rheumatology (AREA)
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  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Transplantation (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201480074736.1A 2013-12-05 2014-12-03 布鲁顿氏酪氨酸激酶的抑制剂 Expired - Fee Related CN105960404B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361912483P 2013-12-05 2013-12-05
US61/912,483 2013-12-05
PCT/US2014/068434 WO2015084998A1 (en) 2013-12-05 2014-12-03 Inhibitors of bruton's tyrosine kinase

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CN105960404A CN105960404A (zh) 2016-09-21
CN105960404B true CN105960404B (zh) 2019-09-03

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US (5) US9382246B2 (enExample)
EP (1) EP3077388A1 (enExample)
JP (3) JP6345786B2 (enExample)
KR (1) KR20160093675A (enExample)
CN (1) CN105960404B (enExample)
AR (1) AR099367A1 (enExample)
AU (3) AU2014360446A1 (enExample)
BR (1) BR112016012728A2 (enExample)
CA (1) CA2932609A1 (enExample)
MX (2) MX375752B (enExample)
TW (2) TWI708771B (enExample)
WO (1) WO2015084998A1 (enExample)

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2014360446A1 (en) * 2013-12-05 2016-06-09 Pharmacyclics, Llc Inhibitors of Bruton's tyrosine kinase
MA42623A (fr) * 2015-06-02 2018-06-20 Pharmacyclics Llc Inhibiteurs de la tyrosine kinase de bruton
US10954216B2 (en) 2016-12-27 2021-03-23 Riken BMP-signal-inhibiting compound
CN107382836A (zh) * 2017-08-04 2017-11-24 吴赣药业（苏州）有限公司 一种1‑(4‑氨基苯基)‑1h‑吡啶‑2‑酮的制备方法
CN107445981B (zh) * 2017-08-25 2018-06-22 牡丹江医学院 一种用于防治宫颈炎的活性化合物
KR102702228B1 (ko) * 2017-11-21 2024-09-02 브리스톨-마이어스 스큅 컴퍼니 술폰 피리딘 알킬 아미드-치환된 헤테로아릴 화합물
AU2019232437A1 (en) 2018-03-07 2020-10-08 Bayer Aktiengesellschaft Identification and use of ERK5 inhibitors
KR102545594B1 (ko) 2018-07-31 2023-06-21 록쏘 온콜로지, 인코포레이티드 (s)-5-아미노-3-(4-((5-플루오로-2-메톡시벤즈아미도)메틸)페닐)-1-(1,1,1-트리플루오로프로판-2-일)-1h-피라졸-4-카르복스아미드의 분무-건조된 분산물 및 제제
BR122023024103A2 (pt) * 2018-10-15 2024-02-20 Nurix Therapeutics, Inc. Compostos bifuncionais para degradação de btk por meio da via de proteossoma de ubiquitina, composição farmacêutica compreendendo os mesmos, e seus usos
AU2019364336B2 (en) 2018-10-22 2023-11-16 Alumis Inc. TYK2 inhibitors and uses thereof
AU2020242287A1 (en) 2019-03-21 2021-09-02 INSERM (Institut National de la Santé et de la Recherche Médicale) A Dbait molecule in combination with kinase inhibitor for the treatment of cancer
BR112021019722A2 (pt) 2019-04-09 2021-12-14 Nurix Therapeutics Inc Compostos de piperidina 3-substituídos para inibição de cbl-b, e uso de inibidor de cbl-b em combinação com vacina contra câncer e/ou vírus oncolítico
EP3969447A1 (en) 2019-05-17 2022-03-23 Nurix Therapeutics, Inc. Cyano cyclobutyl compounds for cbl-b inhibition and uses thereof
EP3972963A1 (en) 2019-05-21 2022-03-30 Bayer Aktiengesellschaft Identification and use of kras inhibitors
CN110066259A (zh) * 2019-05-22 2019-07-30 南京合巨药业有限公司 一种n-环戊基-1,1-二氧代-4-硫代吗啉甲酰胺的合成方法
JP2022538174A (ja) 2019-06-26 2022-08-31 ニューリックス セラピューティクス，インコーポレイテッド Ｃｂｌ－ｂ阻害のための置換ベンジル－トリアゾール化合物、及びそのさらなる使用
WO2021061870A1 (en) 2019-09-24 2021-04-01 Nurix Therapeutics, Inc. Cbl inhibitors and compositions for expansion of immune cells
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
CN111018842B (zh) * 2019-12-04 2021-02-12 宜春市人民医院 一种唑代嘧啶衍生物、其药物组合物和在抗肿瘤中的应用
ES3033520T3 (en) * 2019-12-04 2025-08-05 Nurix Therapeutics Inc Bifunctional compounds for degrading btk via ubiquitin proteosome pathway
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
WO2022032484A1 (zh) * 2020-08-11 2022-02-17 北京诺诚健华医药科技有限公司 哒嗪-3-甲酰胺类化合物、其制备方法及其在医药学上的应用
WO2022071772A1 (ko) * 2020-09-29 2022-04-07 (주)메디톡스 단백질 키나제 저해제 및 그의 용도
KR20230167407A (ko) 2021-04-08 2023-12-08 누릭스 테라퓨틱스 인코포레이티드 Cbl-b 억제제 화합물을 이용한 조합 요법
AU2022303441A1 (en) * 2021-07-01 2024-01-25 Hangzhou Healzen Therapeutics Co., Ltd. Bruton's tyrosine kinase and mutant degrader, composition and application thereof
IL312357A (en) 2021-10-26 2024-06-01 Nurix Therapeutics Inc Piperidinylpyrazine-carboxamide compounds for the treatment and prevention of cancer and to restore BTK
WO2023088477A1 (zh) * 2021-11-22 2023-05-25 杭州和正医药有限公司 一种可降解btk激酶的多功能化合物、组合物及应用
CN114349707B (zh) * 2022-01-20 2024-01-09 中国医学科学院医药生物技术研究所 一种n-取代脲类化合物及其制备方法和应用
CN115417827B (zh) * 2022-09-30 2023-05-26 中国药科大学 6-氨基-1,3,5-三嗪类化合物及其合成方法和应用
WO2024129395A1 (en) * 2022-12-16 2024-06-20 Gwynant Therapeutics, Inc. Btk inhibitors

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102083800A (zh) * 2008-06-27 2011-06-01 阿维拉制药公司 杂芳基化合物和其用途
WO2013047813A1 (ja) * 2011-09-30 2013-04-04 大鵬薬品工業株式会社 １，２，４－トリアジン－６－カルボキサミド誘導体
US20130131040A1 (en) * 2011-11-23 2013-05-23 Portola Pharmaceuticals, Inc. Pyrazine kinase inhibitors
WO2013108754A1 (ja) * 2012-01-17 2013-07-25 アステラス製薬株式会社 ピラジンカルボキサミド化合物

Family Cites Families (115)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3993073A (en) 1969-04-01 1976-11-23 Alza Corporation Novel drug delivery device
US3598122A (en) 1969-04-01 1971-08-10 Alza Corp Bandage for administering drugs
US3598123A (en) 1969-04-01 1971-08-10 Alza Corp Bandage for administering drugs
US3710795A (en) 1970-09-29 1973-01-16 Alza Corp Drug-delivery device with stretched, rate-controlling membrane
US4069307A (en) 1970-10-01 1978-01-17 Alza Corporation Drug-delivery device comprising certain polymeric materials for controlled release of drug
US3731683A (en) 1971-06-04 1973-05-08 Alza Corp Bandage for the controlled metering of topical drugs to the skin
US3996934A (en) 1971-08-09 1976-12-14 Alza Corporation Medical bandage
US3742951A (en) 1971-08-09 1973-07-03 Alza Corp Bandage for controlled release of vasodilators
BE795384A (fr) 1972-02-14 1973-08-13 Ici Ltd Pansements
US3921636A (en) 1973-01-15 1975-11-25 Alza Corp Novel drug delivery device
US3993072A (en) 1974-08-28 1976-11-23 Alza Corporation Microporous drug delivery device
US4151273A (en) 1974-10-31 1979-04-24 The Regents Of The University Of California Increasing the absorption rate of insoluble drugs
US3972995A (en) 1975-04-14 1976-08-03 American Home Products Corporation Dosage form
US4077407A (en) 1975-11-24 1978-03-07 Alza Corporation Osmotic devices having composite walls
US4031894A (en) 1975-12-08 1977-06-28 Alza Corporation Bandage for transdermally administering scopolamine to prevent nausea
US4060084A (en) 1976-09-07 1977-11-29 Alza Corporation Method and therapeutic system for providing chemotherapy transdermally
US4201211A (en) 1977-07-12 1980-05-06 Alza Corporation Therapeutic system for administering clonidine transdermally
JPS5562012A (en) 1978-11-06 1980-05-10 Teijin Ltd Slow-releasing preparation
US4230105A (en) 1978-11-13 1980-10-28 Merck & Co., Inc. Transdermal delivery of drugs
US4229447A (en) 1979-06-04 1980-10-21 American Home Products Corporation Intraoral methods of using benzodiazepines
CA1146866A (en) 1979-07-05 1983-05-24 Yamanouchi Pharmaceutical Co. Ltd. Process for the production of sustained release pharmaceutical composition of solid medical material
US4291015A (en) 1979-08-14 1981-09-22 Key Pharmaceuticals, Inc. Polymeric diffusion matrix containing a vasodilator
US4327725A (en) 1980-11-25 1982-05-04 Alza Corporation Osmotic device with hydrogel driving member
US5116817A (en) 1982-12-10 1992-05-26 Syntex (U.S.A.) Inc. LHRH preparations for intranasal administration
US4476116A (en) 1982-12-10 1984-10-09 Syntex (U.S.A.) Inc. Polypeptides/chelating agent nasal compositions having enhanced peptide absorption
US4596795A (en) 1984-04-25 1986-06-24 The United States Of America As Represented By The Secretary, Dept. Of Health & Human Services Administration of sex hormones in the form of hydrophilic cyclodextrin derivatives
US4624848A (en) 1984-05-10 1986-11-25 Ciba-Geigy Corporation Active agent containing hydrogel devices wherein the active agent concentration profile contains a sigmoidal concentration gradient for improved constant release, their manufacture and use
GB8518301D0 (en) 1985-07-19 1985-08-29 Fujisawa Pharmaceutical Co Hydrodynamically explosive systems
JPH0778017B2 (ja) 1985-12-28 1995-08-23 住友製薬株式会社 パルス的かつ持続放出性製剤
US4755386A (en) 1986-01-22 1988-07-05 Schering Corporation Buccal formulation
US5312325A (en) 1987-05-28 1994-05-17 Drug Delivery Systems Inc Pulsating transdermal drug delivery system
US4968509A (en) 1987-07-27 1990-11-06 Mcneilab, Inc. Oral sustained release acetaminophen formulation and process
US5052558A (en) 1987-12-23 1991-10-01 Entravision, Inc. Packaged pharmaceutical product
US5033252A (en) 1987-12-23 1991-07-23 Entravision, Inc. Method of packaging and sterilizing a pharmaceutical product
IL92966A (en) 1989-01-12 1995-07-31 Pfizer Dispensing devices powered by hydrogel
US5739136A (en) 1989-10-17 1998-04-14 Ellinwood, Jr.; Everett H. Intraoral dosing method of administering medicaments
US5017381A (en) 1990-05-02 1991-05-21 Alza Corporation Multi-unit pulsatile delivery system
US5633009A (en) 1990-11-28 1997-05-27 Sano Corporation Transdermal administration of azapirones
JP2527107B2 (ja) 1991-04-16 1996-08-21 日本新薬株式会社 固体分散体の製造方法
US5229135A (en) 1991-11-22 1993-07-20 Prographarm Laboratories Sustained release diltiazem formulation
CZ282760B6 (cs) 1991-11-22 1997-09-17 Procter And Gamble Pharmaceuticals, Inc. Risedronátové prostředky se zpožděným uvolňováním
US5340591A (en) 1992-01-24 1994-08-23 Fujisawa Pharmaceutical Co., Ltd. Method of producing a solid dispersion of the sparingly water-soluble drug, nilvadipine
US5461140A (en) 1992-04-30 1995-10-24 Pharmaceutical Delivery Systems Bioerodible polymers for solid controlled release pharmaceutical compositions
US5260068A (en) 1992-05-04 1993-11-09 Anda Sr Pharmaceuticals Inc. Multiparticulate pulsatile drug delivery system
US5281420A (en) 1992-05-19 1994-01-25 The Procter & Gamble Company Solid dispersion compositions of tebufelone
US5323907A (en) 1992-06-23 1994-06-28 Multi-Comp, Inc. Child resistant package assembly for dispensing pharmaceutical medications
AU4198793A (en) 1992-07-24 1994-01-27 Takeda Chemical Industries Ltd. Microparticle preparation and production thereof
US5700485A (en) 1992-09-10 1997-12-23 Children's Medical Center Corporation Prolonged nerve blockade by the combination of local anesthetic and glucocorticoid
EP0665010B1 (en) 1992-10-16 2002-09-11 Nippon Shinyaku Company, Limited Method of manufacturing wax matrices
US5260069A (en) 1992-11-27 1993-11-09 Anda Sr Pharmaceuticals Inc. Pulsatile particles drug delivery system
US5686105A (en) 1993-10-19 1997-11-11 The Procter & Gamble Company Pharmaceutical dosage form with multiple enteric polymer coatings for colonic delivery
US6326469B1 (en) 1994-04-22 2001-12-04 Sugen, Inc. Megakaryocytic protein tyrosine kinases
US5665378A (en) 1994-09-30 1997-09-09 Davis; Roosevelt Transdermal therapeutic formulation
US5567441A (en) 1995-03-24 1996-10-22 Andrx Pharmaceuticals Inc. Diltiazem controlled release formulation
JPH11505258A (ja) 1995-05-17 1999-05-18 セダーシナイ メディカル センター 小腸における消化および吸収を改善させる脂肪酸を含む組成物
SE9502244D0 (sv) 1995-06-20 1995-06-20 Bioglan Ab A composition and a process for the preparation thereof
US5837284A (en) 1995-12-04 1998-11-17 Mehta; Atul M. Delivery of multiple doses of medications
US5858401A (en) 1996-01-22 1999-01-12 Sidmak Laboratories, Inc. Pharmaceutical composition for cyclosporines
US6929801B2 (en) 1996-02-19 2005-08-16 Acrux Dds Pty Ltd Transdermal delivery of antiparkinson agents
US6923983B2 (en) 1996-02-19 2005-08-02 Acrux Dds Pty Ltd Transdermal delivery of hormones
US6458373B1 (en) 1997-01-07 2002-10-01 Sonus Pharmaceuticals, Inc. Emulsion vehicle for poorly soluble drugs
US5840329A (en) 1997-05-15 1998-11-24 Bioadvances Llc Pulsatile drug delivery system
US6391452B1 (en) 1997-07-18 2002-05-21 Bayer Corporation Compositions for nasal drug delivery, methods of making same, and methods of removing residual solvent from pharmaceutical preparations
JP4135318B2 (ja) 1997-12-15 2008-08-20 アステラス製薬株式会社 新規なピリミジン−５−カルボキサミド誘導体
US5869090A (en) 1998-01-20 1999-02-09 Rosenbaum; Jerry Transdermal delivery of dehydroepiandrosterone
US6946144B1 (en) 1998-07-08 2005-09-20 Oryxe Transdermal delivery system
ES2307482T3 (es) 1999-02-10 2008-12-01 Pfizer Products Inc. Dispersiones farmaceuticas solidas.
US6395300B1 (en) 1999-05-27 2002-05-28 Acusphere, Inc. Porous drug matrices and methods of manufacture thereof
ATE288420T1 (de) 1999-06-09 2005-02-15 Yamanouchi Pharma Co Ltd Neuartige heterocyclische carboxamid-derivate
WO2000076980A1 (en) 1999-06-10 2000-12-21 Yamanouchi Pharmaceutical Co., Ltd. Novel nitrogen-contaiing heterocyclic derivatives or salts thereof
WO2001000010A1 (en) 1999-06-25 2001-01-04 Kondejewski Leslie H Polypeptide compositions formed using a coiled-coil template and methods of use
US6465014B1 (en) 2001-03-21 2002-10-15 Isp Investments Inc. pH-dependent sustained release, drug-delivery composition
US6960563B2 (en) 2001-08-31 2005-11-01 Morton Grove Pharmaceuticals, Inc. Spontaneous emulsions containing cyclosporine
US7122550B2 (en) 2002-05-23 2006-10-17 Cytopia Pty Ltd Protein kinase inhibitors
AU2003244098A1 (en) 2002-06-28 2004-01-19 Yamanouchi Pharmaceutical Co., Ltd. Diaminopyrimidinecarboxa mide derivative
CA2601628C (en) 2005-03-10 2014-05-13 Cgi Pharmaceuticals, Inc. Certain substituted amides, method of making, and method of use thereof
EP2046759A1 (en) 2006-07-21 2009-04-15 Novartis AG 2, 4 -di (arylaminio) -pyrimidine-5-carboxamide compounds as jak kinases inhibitors
WO2008024963A1 (en) 2006-08-24 2008-02-28 Serenex, Inc. Benzene, pyridine, and pyridazine derivatives
WO2008024978A2 (en) 2006-08-24 2008-02-28 Serenex, Inc. Tetrahydroindolone and tetrahydroindazolone derivatives
EP2068849A2 (en) 2006-09-11 2009-06-17 CGI Pharmaceuticals, Inc. Kinase inhibitors, and methods of using and identifying kinase inhibitors
CL2008002793A1 (es) 2007-09-20 2009-09-04 Cgi Pharmaceuticals Inc Compuestos derivados de amidas sustituidas, inhibidores de la actividad de btk; composicion farmaceutica que los comprende; utiles en el tratamiento del cancer, trastornos oseos, enfermedades autoinmunes, entre otras
WO2009114470A2 (en) 2008-03-10 2009-09-17 Curis, Inc. Tetrahydroindole and tetrahdyroindazole as hsp90 inhibitors containing a zinc binding moiety
FR2928645A1 (fr) 2008-03-14 2009-09-18 Sanofi Aventis Sa Nouveaux derives de carbazole inhibiteurs d'hsp90, compositions les contenant et utilisation
MY155639A (en) 2008-04-16 2015-11-13 Portola Pharm Inc 2, 6-diamino-pyrimidin-5-yl-carboxamides as syk or jak kinases inhibitors
KR20100132550A (ko) 2008-04-16 2010-12-17 포톨라 파마슈티컬스, 인코포레이티드 ｓｙｋ 또는 ＪＡＫ 키나제 억제제로서의 ２,６－디아미노-피리미딘－５－일－카르복스아미드
US8258144B2 (en) 2008-04-22 2012-09-04 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
WO2009137596A1 (en) 2008-05-06 2009-11-12 Cgi Pharmaceuticals, Inc. Substituted amides, method of making, and use as btk inhibitors
JPWO2010058846A1 (ja) 2008-11-21 2012-04-19 アステラス製薬株式会社 ４，６−ジアミノニコチンアミド化合物
KR20100097077A (ko) 2009-02-25 2010-09-02 주식회사 중외제약 Ｈｓｐ90에 대한 억제 효능을 갖는 피리디논 유도체
AR076550A1 (es) 2009-05-06 2011-06-22 Portola Pharm Inc Inhibidores de la janus tirosina kinasa (jak)
EP3009428B1 (en) * 2009-05-08 2018-02-21 Astellas Pharma Inc. Diamino heterocyclic carboxamide compound
US20130023497A1 (en) 2009-06-08 2013-01-24 Chunlin Tao Triazine Derivatives and their Therapeutical Applications
JP2012529535A (ja) * 2009-06-12 2012-11-22 ブリストル−マイヤーズ スクイブ カンパニー キナーゼモジュレーターとして有用なニコチンアミド化合物
CN102311389A (zh) 2010-06-29 2012-01-11 王小龙 一种氮芳香取代吡唑衍生物、及其合成和抗癌应用
PH12012502572A1 (en) 2010-06-30 2022-03-30 Fujifilm Corp Novel nicotinamide derivative or salt thereof
JP2014005206A (ja) * 2010-10-22 2014-01-16 Astellas Pharma Inc アリールアミノヘテロ環カルボキサミド化合物
CA2816219C (en) 2010-11-01 2019-10-29 Portola Pharmaceuticals, Inc. Nicotinamides as syk modulators
EP2975027A1 (en) 2010-11-01 2016-01-20 Portola Pharmaceuticals, Inc. Nicotinamides as jak kinase modulators
US20130317029A1 (en) 2010-11-01 2013-11-28 Portola Pharmaceuticals, Inc. Oxypyrimidines as syk modulators
CN103380117A (zh) 2011-01-21 2013-10-30 Abbvie公司 激酶的吡啶酰胺抑制剂
PE20140502A1 (es) 2011-04-22 2014-05-02 Signal Pharm Llc Pirimidinas sustituidas de diaminocarboxamida y diaminocarbonitrilo, composiciones de las mismas y metodos de tratamiento con las mismas
EP2548877A1 (en) 2011-07-19 2013-01-23 MSD Oss B.V. 4-(5-Membered fused pyridinyl)benzamides as BTK-inhibitors
WO2013054351A1 (en) 2011-08-08 2013-04-18 Cadila Healthcare Limited Heterocyclic compounds
US20140323418A1 (en) 2011-11-23 2014-10-30 Portola Pharmaceuticals, Inc. Selective kinase inhibitors
JP5868168B2 (ja) 2011-12-28 2016-02-24 富士フイルム株式会社 新規なニコチンアミド誘導体またはその塩
US20140113931A1 (en) 2012-06-22 2014-04-24 Portola Pharmaceuticals, Inc. Substituted picolinamide kinase inhibitors
US9040530B2 (en) * 2012-06-22 2015-05-26 Portola Pharmaceuticals, Inc. 1,2,4-triazine-6-carboxamide kinase inhibitors
CN103664878A (zh) 2012-09-12 2014-03-26 山东亨利医药科技有限责任公司 杂芳环及其衍生物类酪氨酸激酶抑制剂
EP2903970A4 (en) 2012-10-08 2016-11-30 Portola Pharm Inc SUBSTITUTED PYRIMIDINYL KINASE INHIBITORS
WO2014111031A1 (zh) 2013-01-17 2014-07-24 四川恒康发展有限责任公司 三嗪化合物、其药用盐、异构体或水合物及其药物组合物
WO2014124230A2 (en) 2013-02-08 2014-08-14 Celgene Avilomics Research, Inc. Erk inhibitors and uses thereof
JP2016113366A (ja) 2013-03-29 2016-06-23 大鵬薬品工業株式会社 アセトアミド基を有する１，２，４−トリアジン−６−カルボキサミド誘導体
JP2014198693A (ja) * 2013-03-29 2014-10-23 大鵬薬品工業株式会社 免疫疾患の予防及び／又は治療剤
WO2015039613A1 (zh) 2013-09-18 2015-03-26 北京韩美药品有限公司 抑制btk和/或jak3激酶活性的化合物
AU2014360446A1 (en) * 2013-12-05 2016-06-09 Pharmacyclics, Llc Inhibitors of Bruton's tyrosine kinase

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102083800A (zh) * 2008-06-27 2011-06-01 阿维拉制药公司 杂芳基化合物和其用途
WO2013047813A1 (ja) * 2011-09-30 2013-04-04 大鵬薬品工業株式会社 １，２，４－トリアジン－６－カルボキサミド誘導体
US20130131040A1 (en) * 2011-11-23 2013-05-23 Portola Pharmaceuticals, Inc. Pyrazine kinase inhibitors
WO2013108754A1 (ja) * 2012-01-17 2013-07-25 アステラス製薬株式会社 ピラジンカルボキサミド化合物

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