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

Info

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
Authority
CN
China
Prior art keywords
amino
carboxamide
phenyl
pyrazine
piperidin
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
CN201480074736.1A
Other languages
English (en)
Chinese (zh)
Other versions
CN105960404A (zh
Inventor
兆忠·J·贾
威廉姆·D·托马斯
陈伟
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Pharmacyclics LLC
Original Assignee
Pharmacyclics 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
Application filed by Pharmacyclics LLC filed Critical Pharmacyclics LLC
Publication of CN105960404A publication Critical patent/CN105960404A/zh
Application granted granted Critical
Publication of CN105960404B publication Critical patent/CN105960404B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • 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
    • 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
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • 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
    • A61K31/40—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
    • 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
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/53—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (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

Publications (2)

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

Family

ID=52302318

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201480074736.1A Expired - Fee Related CN105960404B (zh) 2013-12-05 2014-12-03 布鲁顿氏酪氨酸激酶的抑制剂

Country Status (12)

Country Link
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 (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3077388A1 (en) * 2013-12-05 2016-10-12 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
WO2018124001A1 (ja) 2016-12-27 2018-07-05 国立研究開発法人理化学研究所 Ｂｍｐシグナル阻害化合物
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
IL274816B2 (en) * 2017-11-21 2023-12-01 Bristol Myers Squibb Co Sulfone pyridine alkyl amide-substituted heteroaryl compounds
WO2019170543A1 (en) 2018-03-07 2019-09-12 Bayer Aktiengesellschaft Identification and use of erk5 inhibitors
CA3224985C (en) 2018-07-31 2025-11-18 Loxo Oncology, Inc. SPRAY-DRIED DISPERSIONS, FORMULATIONS AND POLYMORPHIES OF (S)-5-AMINO-3-(4-((5-FLUORO-2-METHOXYBENZAMIDO)METHYL)PHENYL)(1,1,1-TRIFLUOROPROPANE-2-YL)-1H-PYRAZOLE-4-CARBOXAMIDE
CN113412259B (zh) 2018-10-15 2024-07-16 紐力克斯治疗公司 通过泛素蛋白酶体途径降解btk的双官能化合物
HRP20250048T1 (hr) 2018-10-22 2025-03-28 Alumis Inc. Inhibitori tyk2 i njihova uporaba
WO2020167518A1 (en) 2019-02-13 2020-08-20 Nurix Therapeutics, Inc. Bifunctional compounds for degrading btk via ubiquitin proteosome pathway
EP3942045A1 (en) 2019-03-21 2022-01-26 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
AU2020272937B2 (en) 2019-04-09 2024-09-26 Nurix Therapeutics, Inc. 3-substituted piperidine compounds for Cbl-b inhibition, and use of a Cbl-b inhibitor in combination with a cancer vaccine and/or oncolytic virus
JP7587528B2 (ja) 2019-05-17 2024-11-20 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阻害のためのシアノシクロブチル化合物及びその使用
US20220227729A1 (en) 2019-05-21 2022-07-21 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
CA3144450A1 (en) 2019-06-26 2020-12-30 Nurix Therapeutics, Inc. Substituted benzyl-triazole compounds for cbl-b inhibition, and further uses thereof
US12121540B2 (en) 2019-09-24 2024-10-22 Nurix Therapeutics, Inc. CBL inhibitors and compositions for use in adoptive cell therapy
EP4054579A1 (en) 2019-11-08 2022-09-14 Institut National de la Santé et de la Recherche Médicale (INSERM) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
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
MX2022006672A (es) * 2019-12-04 2022-08-08 Nurix Therapeutics Inc Compuestos bifuncionales para la degradacion de btk a traves de la via de proteosomas de ubiquitina.
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
MX2023011883A (es) 2021-04-08 2023-11-09 Nurix Therapeutics Inc Terapias combinadas con compuestos inhibidores de cbl-b.
CA3223769A1 (en) * 2021-07-01 2023-01-05 Xinglu ZHOU Bruton's tyrosine kinase and mutant degrader, composition and application thereof
WO2023076303A1 (en) 2021-10-26 2023-05-04 Nurix Therapeutics, Inc. Piperidinylpyrazine-carboxamide compounds for treating and preventing cancer and for degrading 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
US3598122A (en) 1969-04-01 1971-08-10 Alza Corp Bandage for administering drugs
US3993073A (en) 1969-04-01 1976-11-23 Alza Corporation Novel drug delivery device
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
US3742951A (en) 1971-08-09 1973-07-03 Alza Corp Bandage for controlled release of vasodilators
US3996934A (en) 1971-08-09 1976-12-14 Alza Corporation Medical bandage
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
DE3684446D1 (de) 1985-12-28 1992-04-23 Sumitomo Pharma Arzneimittel mit verzoegerter stossweiser freisetzung.
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
US5033252A (en) 1987-12-23 1991-07-23 Entravision, Inc. Method of packaging and sterilizing a pharmaceutical product
US5052558A (en) 1987-12-23 1991-10-01 Entravision, Inc. Packaged 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
AU1537292A (en) 1991-04-16 1992-11-17 Nippon Shinyaku Co. Ltd. Method of manufacturing solid dispersion
AU661080B2 (en) 1991-11-22 1995-07-13 Warner Chilcott Company, Llc Risedronate delayed-release compositions
US5229135A (en) 1991-11-22 1993-07-20 Prographarm Laboratories Sustained release diltiazem formulation
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
KR100291362B1 (ko) 1992-10-16 2001-09-17 니뽄 신야쿠 가부시키가이샤 왁스매트릭스의제법
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
EP0827402A2 (en) 1995-05-17 1998-03-11 Cedars-Sinai Medical Center Compositions containing fatty acids for improving digestion and absorption in the small intestine
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
AU1507199A (en) 1997-12-15 1999-07-05 Yamanouchi Pharmaceutical Co., Ltd. Novel pyrimidine-5-carboxamide derivatives
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
EP1027886B1 (en) 1999-02-10 2008-07-09 Pfizer Products Inc. Pharmaceutical solid dispersions
US6395300B1 (en) 1999-05-27 2002-05-28 Acusphere, Inc. Porous drug matrices and methods of manufacture thereof
AU5107900A (en) 1999-06-09 2000-12-28 Yamanouchi Pharmaceutical Co., Ltd. Novel heterocyclic carboxamide derivatives
AU5108000A (en) 1999-06-10 2001-01-02 Yamanouchi Pharmaceutical Co., Ltd. Novel nitrogen-contaiing heterocyclic derivatives or salts thereof
DE60014372T2 (de) 1999-06-25 2006-02-02 The Governors Of The University Of Alberta, Edmonton Polypeptid-enthaltende zusammensetzungen, hergestellt durch verwendung von matrizen in gestalt eines coiled-coil und deren gebrauch
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
NZ537155A (en) 2002-05-23 2006-09-29 Cytopia Pty Ltd Protein kinase inhibitors
EP1518855B1 (en) 2002-06-28 2011-10-26 Astellas Pharma Inc. Diaminopyrimidinecarboxa mide derivative
WO2006099075A2 (en) 2005-03-10 2006-09-21 Cgi Pharmaceuticals, Inc. Certain substituted amides, method of making, and method of use thereof
CA2657260A1 (en) 2006-07-21 2008-01-24 Novartis Ag 2, 4 -di (arylaminio) -pyrimidine-5-carboxamide compounds as jak kinases inhibitors
WO2008024978A2 (en) 2006-08-24 2008-02-28 Serenex, Inc. Tetrahydroindolone and tetrahydroindazolone derivatives
US20080076800A1 (en) 2006-08-24 2008-03-27 Huang Kenneth H Benzene, Pyridine, and Pyridazine Derivatives
JP2010502751A (ja) 2006-09-11 2010-01-28 シージーアイ ファーマシューティカルズ，インコーポレイティド キナーゼ阻害物質、およびキナーゼ阻害物質の使用および同定方法
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
KR20100132550A (ko) 2008-04-16 2010-12-17 포톨라 파마슈티컬스, 인코포레이티드 ｓｙｋ 또는 ＪＡＫ 키나제 억제제로서의 ２,６－디아미노-피리미딘－５－일－카르복스아미드
JP5705720B2 (ja) 2008-04-16 2015-04-22 ポートラ ファーマシューティカルズ， インコーポレイテッド Ｓｙｋまたはｊａｋキナーゼ阻害剤としての２，６−ジアミノ−ピリミジン−５−イル−カルボキサミド
JP2011518219A (ja) 2008-04-22 2011-06-23 ポートラ ファーマシューティカルズ， インコーポレイテッド タンパク質キナーゼの阻害剤
JP5529852B2 (ja) 2008-05-06 2014-06-25 ジリード コネティカット，インコーポレイティド 置換アミド、その製造法及びＢｔｋインヒビターとしての使用
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
US8367689B2 (en) 2009-05-06 2013-02-05 Portola Pharmaceuticals, Inc. Inhibitors of JAK
JP5364159B2 (ja) 2009-05-08 2013-12-11 アステラス製薬株式会社 ジアミノへテロ環カルボキサミド化合物
WO2010144345A1 (en) 2009-06-08 2010-12-16 Abraxis Bioscience, Llc 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
KR101789129B1 (ko) 2010-06-30 2017-11-20 후지필름 가부시키가이샤 신규 니코틴아미드 유도체 또는 그 염
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
EP2635557A2 (en) 2010-11-01 2013-09-11 Portola Pharmaceuticals, Inc. Nicotinamides as jak kinase modulators
US20130317029A1 (en) 2010-11-01 2013-11-28 Portola Pharmaceuticals, Inc. Oxypyrimidines as syk modulators
CA2816219C (en) 2010-11-01 2019-10-29 Portola Pharmaceuticals, Inc. Nicotinamides as syk modulators
EP2665711A1 (en) 2011-01-21 2013-11-27 Abbvie Inc. Picolinamide inhibitors of kinases
HRP20240097T1 (hr) 2011-04-22 2024-03-29 Signal Pharmaceuticals, Llc Supstituirani diaminokarboksamid i diaminokarbonitril pirimidini, njihovi pripravci i postupci liječenja s njima
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
EP2782580A4 (en) 2011-11-23 2015-10-07 Portola Pharm Inc SELECTIVE INHIBITORS OF KINASES
CA2861202C (en) 2011-12-28 2018-03-13 Fujifilm Corporation Nicotinamide derivatives or salt thereof having syk-inhibitory activity
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
US9676756B2 (en) 2012-10-08 2017-06-13 Portola Pharmaceuticals, 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
US9561228B2 (en) 2013-02-08 2017-02-07 Celgene Avilomics Research, Inc. ERK inhibitors and uses thereof
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
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
CN104262328B (zh) 2013-09-18 2016-09-07 北京韩美药品有限公司 抑制btk和/或jak3激酶活性的化合物
EP3077388A1 (en) * 2013-12-05 2016-10-12 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

Also Published As

Publication number Publication date
BR112016012728A2 (pt) 2020-08-11
AU2019202507A1 (en) 2019-05-02
US9382246B2 (en) 2016-07-05
MX2020010412A (es) 2020-10-28
TWI708771B (zh) 2020-11-01
US20190100505A1 (en) 2019-04-04
MX2016007111A (es) 2016-08-11
TWI672294B (zh) 2019-09-21
US20160355498A1 (en) 2016-12-08
MX375752B (es) 2025-03-06
US20180030027A1 (en) 2018-02-01
CA2932609A1 (en) 2015-06-11
TW201607937A (zh) 2016-03-01
AU2019202507B2 (en) 2020-08-13
AU2014360446A1 (en) 2016-06-09
JP2020121988A (ja) 2020-08-13
AR099367A1 (es) 2016-07-20
CN105960404A (zh) 2016-09-21
JP6689314B2 (ja) 2020-04-28
AU2020267189A1 (en) 2020-12-03
JP6345786B2 (ja) 2018-06-20
JP2016539152A (ja) 2016-12-15
US20200079754A1 (en) 2020-03-12
WO2015084998A1 (en) 2015-06-11
JP2018158926A (ja) 2018-10-11
EP3077388A1 (en) 2016-10-12
KR20160093675A (ko) 2016-08-08
US20150158865A1 (en) 2015-06-11
US9656988B2 (en) 2017-05-23
TW201938549A (zh) 2019-10-01

Similar Documents

Publication Publication Date Title
JP6689314B2 (ja) ブルトン型チロシンキナーゼの阻害剤
CN104640861B (zh) 作为激酶抑制剂的嘌呤酮化合物
US9624224B2 (en) Inhibitors of Bruton's tyrosine kinase
TWI522359B (zh) 做爲激酶抑制劑之吡咯并嘧啶化合物
JP6458018B2 (ja) キナーゼ阻害剤としてのプリノン化合物
WO2017205762A1 (en) Inhibitors of interleukin-1 receptor-associated kinase
CA3125353A1 (en) Inhibitors of menin-mll interaction
US20250353854A1 (en) Fused pyrimidine compounds as inhibitors of menin

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant
CF01 Termination of patent right due to non-payment of annual fee
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20190903

Termination date: 20211203