CA2728767A1 - Alkynyl alcohols as kinase inhibitors - Google Patents

Alkynyl alcohols as kinase inhibitors Download PDF

Info

Publication number
CA2728767A1
CA2728767A1 CA2728767A CA2728767A CA2728767A1 CA 2728767 A1 CA2728767 A1 CA 2728767A1 CA 2728767 A CA2728767 A CA 2728767A CA 2728767 A CA2728767 A CA 2728767A CA 2728767 A1 CA2728767 A1 CA 2728767A1
Authority
CA
Canada
Prior art keywords
alkylene
bromo
valance
allowed
mmol
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.)
Abandoned
Application number
CA2728767A
Other languages
English (en)
French (fr)
Inventor
Guoqing Chen
Timothy David Cushing
Benjamin Fisher
Xiao He
Kexue Li
Zhihong Li
Lawrence R. Mcgee
Vatee Pattaropong
Paul Faulder
Jennifer L. Seganish
Youngsook Shin
Zhulun Wang
Wen Liu
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.)
Amgen Inc
Original Assignee
Amgen Inc
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 Amgen Inc filed Critical Amgen Inc
Publication of CA2728767A1 publication Critical patent/CA2728767A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • 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
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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
    • C07D233/88—Nitrogen atoms, e.g. allantoin
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D403/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/08—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a carbon chain containing alicyclic 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • C07D471/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/06—Peri-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/16—Peri-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/10—Spiro-condensed systems

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Otolaryngology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Hospice & Palliative Care (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Pyridine Compounds (AREA)
CA2728767A 2008-06-26 2009-06-26 Alkynyl alcohols as kinase inhibitors Abandoned CA2728767A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US13324908P 2008-06-26 2008-06-26
US61/133,249 2008-06-26
PCT/US2009/003803 WO2009158011A1 (en) 2008-06-26 2009-06-26 Alkynyl alcohols as kinase inhibitors

Publications (1)

Publication Number Publication Date
CA2728767A1 true CA2728767A1 (en) 2009-12-30

Family

ID=41090264

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2728767A Abandoned CA2728767A1 (en) 2008-06-26 2009-06-26 Alkynyl alcohols as kinase inhibitors

Country Status (7)

Country Link
US (1) US20110086834A1 (cg-RX-API-DMAC10.html)
EP (1) EP2315751A1 (cg-RX-API-DMAC10.html)
JP (1) JP2011525915A (cg-RX-API-DMAC10.html)
AU (1) AU2009263037B2 (cg-RX-API-DMAC10.html)
CA (1) CA2728767A1 (cg-RX-API-DMAC10.html)
MX (1) MX2010013920A (cg-RX-API-DMAC10.html)
WO (1) WO2009158011A1 (cg-RX-API-DMAC10.html)

Families Citing this family (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20120117905A (ko) 2010-01-28 2012-10-24 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 프로테아좀 활성을 향상시키는 조성물 및 방법
JP2014500277A (ja) 2010-12-09 2014-01-09 アムジエン・インコーポレーテツド Ｐｉｍ阻害剤としての二環式化合物
AR085908A1 (es) * 2011-03-16 2013-11-06 Hoffmann La Roche DERIVADOS DE 3-BUTIN-2-OL Y DE CARBONITRILO CON ACTIVIDAD INHIBIDORA DE LA QUINASA INDUCTORA DE NF-kB (NIK)
WO2012129338A1 (en) 2011-03-22 2012-09-27 Amgen Inc. Azole compounds as pim inhibitors
WO2012135697A2 (en) * 2011-03-30 2012-10-04 H. Lee Moffitt Cancer Center & Research Institute Inc. Novel rho kinase inhibitors and methods of use
TR201906779T4 (tr) 2011-05-12 2019-05-21 Proteostasis Therapeutics Inc Proteostaz regülatörleri.
EP2551670A1 (en) 2011-07-27 2013-01-30 Merck Patent GmbH NIK inhibitors cell-based assay
US8921576B2 (en) 2011-10-19 2014-12-30 Kowa Company, Ltd. Spiroindoline compound, and medicinal agent comprising same
AR089999A1 (es) * 2012-02-17 2014-10-01 Hoffmann La Roche Compuestos triciclicos y metodos para el uso de los mismos
WO2014116228A1 (en) 2013-01-25 2014-07-31 President And Fellows Of Harvard College Usp14 inhibitors for treating or preventing viral infections
TWI663166B (zh) * 2013-04-24 2019-06-21 健生藥品公司 新化合物
WO2015025026A1 (en) * 2013-08-22 2015-02-26 F. Hoffmann-La Roche Ag Alkynyl alcohols and methods of use
JP2016533385A (ja) * 2013-08-22 2016-10-27 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ アルキニルアルコール及び使用方法
TWI704146B (zh) * 2013-09-26 2020-09-11 比利時商健生藥品公司 用作ＮＩＫ抑制劑之新的1-(４-嘧啶基)-１Ｈ-吡唑並[３,２-ｃ]吡啶衍生物
TWI627173B (zh) * 2013-09-26 2018-06-21 比利時商健生藥品公司 作為ＮＩＫ抑制劑的新穎３－（１Ｈ－吡唑－４－基）－１Ｈ－吡咯并［２，３－ｃ］吡啶衍生物
WO2015073528A1 (en) 2013-11-12 2015-05-21 Proteostasis Therapeutics, Inc. Proteasome activity enhancing compounds
WO2015150097A1 (en) 2014-04-04 2015-10-08 Iomet Pharma Ltd Indole derivatives for use in medicine
KR101551313B1 (ko) * 2014-07-28 2015-09-09 충남대학교산학협력단 신규한 인덴 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 망막 질환의 예방 또는 치료용 약학적 조성물
EA033237B1 (ru) * 2014-10-23 2019-09-30 Янссен Фармацевтика Нв Новые производные пиразолопиримидина в качестве ингибиторов nik, фармацевтическая композиция и лекарственное средство, содержащее ее
WO2016062792A1 (en) * 2014-10-23 2016-04-28 Janssen Pharmaceutica Nv New compounds as nik inhibitors
JP6616411B2 (ja) 2014-10-23 2019-12-04 ヤンセン ファーマシューティカ エヌ．ベー． 新規な、ｎｉｋ阻害剤としてのピラゾール誘導体
AU2015334914B2 (en) * 2014-10-23 2019-09-19 Janssen Pharmaceutica Nv New thienopyrimidine derivatives as NIK inhibitors
WO2016135163A1 (en) * 2015-02-25 2016-09-01 F. Hoffmann-La Roche Ag Alkynyl alcohols and methods of use
CN107614503B (zh) * 2015-04-29 2020-03-10 广东众生药业股份有限公司 稠环或三环芳基嘧啶化合物用作激酶抑制剂
HRP20200133T1 (hr) 2016-01-22 2020-05-15 Janssen Pharmaceutica Nv Novi supstituirani derivati cijanoindolina kao inhibitori nik
EP3405464B1 (en) 2016-01-22 2019-12-04 Janssen Pharmaceutica NV New 6-membered heteroaromatic substituted cyanoindoline derivatives as nik inhibitors
CN105769871A (zh) * 2016-03-03 2016-07-20 东北师范大学 Nik蛋白激酶抑制剂作为制备治疗肝病的药物的应用
EA037358B1 (ru) * 2016-03-10 2021-03-17 Янссен Фармасьютика Нв Новые замещённые производные цианиндолина в качестве nik-ингибиторов
WO2018002219A1 (en) * 2016-06-30 2018-01-04 Janssen Pharmaceutica Nv Cyanoindoline derivatives as nik inhibitors
EP3478675B1 (en) * 2016-06-30 2020-04-22 Janssen Pharmaceutica NV Heteroaromatic derivatives as nik inhibitors
CN109863142B (zh) * 2016-08-24 2022-06-10 豪夫迈·罗氏有限公司 2-氮杂双环[3.1.0]己烷-3-酮衍生物及使用方法
JP7140751B2 (ja) * 2016-08-24 2022-09-21 エフ．ホフマン－ラ ロシュ アーゲー ２－アザビシクロ［３．１．０］ヘキサン－３－オン誘導体及び使用方法
US10858319B2 (en) 2016-10-03 2020-12-08 Iomet Pharma Ltd. Indole derivatives for use in medicine
CN110769830A (zh) 2017-05-12 2020-02-07 马瓦隆治疗有限公司 作为ii组代谢型谷氨酸受体的别构调节剂的取代的杂环化合物
CN109810110B (zh) * 2017-11-22 2023-01-24 中国科学院上海药物研究所 一种具有2-氨基嘧啶结构的化合物，其制备方法和用途
US11149011B2 (en) 2018-03-20 2021-10-19 Plexxikon Inc. Compounds and methods for IDO and TDO modulation, and indications therefor
CR20210587A (es) 2019-05-31 2022-02-11 Janssen Pharmaceutica Nv Inhibidores de molécula pequeña de quinasa inductora de nf-kb
EP3782702A1 (en) * 2019-08-21 2021-02-24 AC BioScience SA Compounds and use thereof for the treatment of infectious diseases and cancer
JP2023530271A (ja) * 2020-06-12 2023-07-14 バーテックス ファーマシューティカルズ インコーポレイテッド Ａｐｏｌ１の阻害剤及びこれを使用する方法
CN113831325A (zh) * 2020-06-23 2021-12-24 沈阳药科大学 新型吲哚类衍生物及其制备方法和应用
CN111960983A (zh) * 2020-08-31 2020-11-20 南通大学 一种n-甲基-3-(1-甲基吡咯烷-3-基)丙-1-胺及其合成方法
CN112194609B (zh) * 2020-10-22 2022-11-04 西北农林科技大学 3,3-二取代氧化吲哚类化合物及其制备方法与用途
CN112174938A (zh) * 2020-10-27 2021-01-05 浙江工业大学 4-吲哚-2-氨基嘧啶类化合物及其应用
CN115215861B (zh) * 2021-04-16 2024-03-15 上海翊石医药科技有限公司 一种芳杂环取代的炔烃类化合物及其制备方法和用途

Family Cites Families (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK429884A (da) * 1983-10-07 1985-04-08 Hoffmann La Roche Heterocycliske forbindelser
GB8714537D0 (en) * 1987-06-22 1987-07-29 Ici Plc Pyrazine derivatives
DE3877459T2 (de) * 1987-08-20 1993-05-13 Ici Plc Pyrimidinderivate.
GB9016783D0 (en) * 1989-09-01 1990-09-12 Ici Plc Agrochemical compositions
UA64690C2 (en) * 1993-07-21 2004-03-15 Yamanouty Farmaceutical Co Ltd A condensed benzadepine derivative, an intermediate compound for preparing thereof and a pharmaceutical composition
CA2183655C (en) * 1994-02-23 2001-03-06 Lee D. Arnold 4-polycyclic amino-substituted quinazoline derivatives
US6063930A (en) * 1996-04-03 2000-05-16 Merck & Co., Inc. Substituted imidazole compounds useful as farnesyl-protein transferase inhibitors
ZA986729B (en) * 1997-07-29 1999-02-02 Warner Lambert Co Irreversible inhibitors of tyrosine kinases
GB9716446D0 (en) * 1997-08-05 1997-10-08 Agrevo Uk Ltd Fungicides
CN1161333C (zh) * 1998-08-20 2004-08-11 住友制药株式会社 作为生长激素释放剂的2-羟基吲哚衍生物
UA71945C2 (en) * 1999-01-27 2005-01-17 Pfizer Prod Inc Substituted bicyclic derivatives being used as anticancer agents
JP2002053561A (ja) * 1999-12-08 2002-02-19 Sumitomo Chem Co Ltd ジフルオロメチルトリアゾロン化合物、その用途およびその製造中間体
US6313310B1 (en) * 1999-12-15 2001-11-06 Hoffmann-La Roche Inc. 4-and 5-alkynyloxindoles and 4-and 5-alkenyloxindoles
US20020019527A1 (en) * 2000-04-27 2002-02-14 Wei-Bo Wang Substituted phenyl farnesyltransferase inhibitors
US7211595B2 (en) * 2000-11-30 2007-05-01 Abbott Laboratories Farnesyltransferase inhibitors
US20020115640A1 (en) * 2000-11-30 2002-08-22 Claiborne Akiyo K. Farnesyltransferase inhibitors
US6504034B2 (en) * 2001-01-23 2003-01-07 Hoffmann-La Roche Inc. Naphthostyrils
GB0123589D0 (en) * 2001-10-01 2001-11-21 Syngenta Participations Ag Organic compounds
SI1501808T1 (sl) * 2002-04-26 2008-10-31 Lilly Co Eli Antagonisti tahikininskega receptorja
AU2003230829B8 (en) * 2002-04-26 2008-12-11 Eli Lilly And Company Triazole derivatives as tachykinin receptor antagonists
US20030216441A1 (en) * 2002-05-10 2003-11-20 Gwaltney Stephen L. Farnesyltransferase inhibitors
DE10229762A1 (de) * 2002-07-03 2004-01-22 Aventis Pharma Deutschland Gmbh Pyrazoloisoquinolinenderivaten zur Inhibierung von NFkappaB-induzierende Kinase
US20050035498A1 (en) * 2003-08-13 2005-02-17 Stevens Randal Alan Methods of making a negative hearing aid mold
PE20060426A1 (es) * 2004-06-02 2006-06-28 Schering Corp DERIVADOS DE ACIDO TARTARICO COMO INHIBIDORES DE MMPs, ADAMs, TACE Y TNF-alfa
US20070167426A1 (en) * 2004-06-02 2007-07-19 Schering Corporation Compounds for the treatment of inflammatory disorders and microbial diseases
US7829727B2 (en) * 2005-11-16 2010-11-09 Xerox Corporation Device containing compound having indolocarbazole moiety and divalent linkage
US7396852B2 (en) * 2005-11-16 2008-07-08 Xerox Corporation Compound having indolocarbazole moiety and divalent linkage
KR101195351B1 (ko) * 2004-06-17 2012-10-29 인피니티 디스커버리, 인코포레이티드 Ｂｃｌ 단백질과 결합 파트너와의 상호작용을 억제하는화합물 및 방법
JP2008519850A (ja) * 2004-11-10 2008-06-12 シンタ ファーマシューティカルズ コーポレーション Ｉｌ−１２調節化合物
US20060174937A1 (en) * 2005-02-09 2006-08-10 Zhang-Lin Zhou High performance organic materials for solar cells
TW200736260A (en) * 2005-11-10 2007-10-01 Smithkline Beecham Corp Inhibitors of Akt activity
EP1954286A2 (en) * 2005-11-10 2008-08-13 SmithKline Beecham Corporation Inhibitors of akt activity
WO2007058852A2 (en) * 2005-11-10 2007-05-24 Smithkline Beecham Corporation Inhibitors of akt activity
EP2121613A2 (en) * 2007-01-31 2009-11-25 Vertex Pharmaceuticals, Inc. 2-aminopyridine derivatives useful as kinase inhibitors
US8343966B2 (en) * 2008-01-11 2013-01-01 Novartis Ag Organic compounds

Also Published As

Publication number Publication date
JP2011525915A (ja) 2011-09-29
US20110086834A1 (en) 2011-04-14
AU2009263037B2 (en) 2011-10-06
MX2010013920A (es) 2011-02-21
WO2009158011A1 (en) 2009-12-30
AU2009263037A1 (en) 2009-12-30
EP2315751A1 (en) 2011-05-04

Similar Documents

Publication Publication Date Title
AU2009263037B2 (en) Alkynyl alcohols as kinase inhibitors
JP7086395B2 (ja) 置換インドールＭｃｌ－１阻害剤
AU2013344886B2 (en) Bicyclic urea, thiourea, guanidine and cyanoguanidine compounds useful for the treatment of pain
US7696229B2 (en) Compounds having 5-HT6 receptor affinity
JP2022050469A (ja) リガンド依存性の標的タンパク質分解のための単官能性中間体
CA3029305C (en) 2-(piperidin-1-yl)-pyrimidin-4(3h)-ones useful as tankyrase inhibitors
KR20200092420A (ko) 피페리딘 cxcr7 수용체 조절제
JP2026010047A (ja) タンパク質の動員および／または分解を調節する化合物
MX2013012243A (es) Compuestos heterociclicos biciclicos y sus usos en terapia.
NZ569087A (en) Polycyclic indazole derivatives that are ERK inhibitors
JP6305510B2 (ja) ヤヌスキナーゼ阻害剤としての非環式シアノエチルピラゾロピリドン
AU2005266461A1 (en) Heterocycle-substituted cyclic urea derivatives, preparation thereof and pharmaceutical use thereof as kinase inhibitors
CN101595107A (zh) 能提高p53活性的有取代哌啶及其用途
CA2643066A1 (en) Pyrazole compounds
JP7336506B2 (ja) 置換トリアゾロキノキサリン誘導体
AU2008256859A1 (en) 4' substituted compounds having 5-HT6 receptor affinity
AU2008216032A1 (en) 6 ' substituted indole and indazole derivatives having 5-HT6 receptor affinity
WO2019062657A1 (zh) 氮杂环类衍生物、其制备方法及其医药用途
CN101321726A (zh) 新型稠合吡咯衍生物

Legal Events

Date Code Title Description
EEER Examination request
FZDE Discontinued

Effective date: 20131105