CN103717593B - 调节激酶的组合物和方法 - Google Patents

调节激酶的组合物和方法 Download PDF

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CN103717593B
CN103717593B CN201280028167.8A CN201280028167A CN103717593B CN 103717593 B CN103717593 B CN 103717593B CN 201280028167 A CN201280028167 A CN 201280028167A CN 103717593 B CN103717593 B CN 103717593B
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cancer
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CN103717593A (zh
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奥伦·M·贝克尔
艾泰·布洛赫
埃弗拉特·本-泽埃夫
爱丽娜·谢特里特
阿韦海·雅科温
莎伦·格则勒
韦雷德·比哈尔
亚历山大·加森
尼利·舒茨
西玛·米瑞拉什维利
加利·戈兰
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Dynamix Pharmaceuticals Ltd
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    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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
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    • 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
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    • C07D491/22—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 four or more hetero rings
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  • Transplantation (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN201280028167.8A 2011-06-07 2012-06-07 调节激酶的组合物和方法 Active CN103717593B (zh)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201161520256P 2011-06-07 2011-06-07
US61/520,256 2011-06-07
US201161562700P 2011-11-22 2011-11-22
US61/562,700 2011-11-22
US201261640139P 2012-04-30 2012-04-30
US61/640,139 2012-04-30
PCT/IB2012/001987 WO2012172438A2 (en) 2011-06-07 2012-06-07 Compositions and methods for modulating a kinase

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CN103717593A CN103717593A (zh) 2014-04-09
CN103717593B true CN103717593B (zh) 2016-07-06

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Families Citing this family (12)

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Publication number Priority date Publication date Assignee Title
US10954567B2 (en) 2012-07-24 2021-03-23 Pharmacyclics Llc Mutations associated with resistance to inhibitors of Bruton's Tyrosine Kinase (BTK)
AU2016368257C1 (en) * 2015-12-07 2019-12-05 Suzhou Sinovent Pharmaceuticals Co., Ltd. Five-membered heterocyclic amides wnt pathway inhibitor
CN107056754B (zh) * 2015-12-07 2020-12-04 苏州信诺维医药科技有限公司 内嵌脲类结构的wnt通路抑制剂
KR20210016545A (ko) 2018-05-29 2021-02-16 오메로스 코포레이션 Masp-2 억제제 및 사용 방법
US20220372135A1 (en) 2019-09-27 2022-11-24 Disc Medicine, Inc. Methods for treating myelofibrosis and related conditions
CN115103709A (zh) 2019-12-04 2022-09-23 奥默罗斯公司 Masp-2抑制剂和使用方法
WO2021146903A1 (zh) * 2020-01-21 2021-07-29 苏州信诺维医药科技股份有限公司 一种含氮化合物的晶型
IL297437A (en) 2020-05-13 2022-12-01 Disc Medicine Inc Anti-hemojuvelin (hjv) antibodies for treating myelofibrosis
AU2022280871A1 (en) * 2021-05-26 2023-12-07 Emory University Jak inhibitors for managing conditions in patients with down's syndrome or other trisomy
CA3233636A1 (en) * 2021-09-29 2023-04-06 Repare Therapeutics Inc. N-(5-substituted-[(1,3,4-thiadiazolyl) or (thiazolyl)])(substituted)carboxamide compounds and use thereof for inhibiting human polymerase theta
CN120344522A (zh) * 2022-09-29 2025-07-18 修复治疗公司 N-(5-取代的-[(1,3,4-噻二唑基)或(1,3-噻唑基)](取代的)甲酰胺化合物、药物组合物以及制备酰胺化合物的方法及其用途
EP4620949A1 (en) * 2024-03-18 2025-09-24 Eberhard Karls Universität Tübingen (Medizinische Fakultät) Ackr3 modulators for cardiovascular or antiplatelet therapy

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0259085A1 (en) * 1986-08-29 1988-03-09 Pfizer Inc. 2-Guanidino-4-arylthiazoles for treatment of peptic ulcers
WO2000033841A1 (en) * 1998-12-07 2000-06-15 Smithkline Beecham Corporation Myt1 kinase inhibitors
CN1735611A (zh) * 2003-01-02 2006-02-15 霍夫曼-拉罗奇有限公司 新cb1受体反激动剂
CN101528738A (zh) * 2006-09-01 2009-09-09 沃泰克斯药物股份有限公司 可用作磷脂酰肌醇3-激酶抑制剂的5-（2-呋喃基）-1，3-噻唑衍生物

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4642903A (en) 1985-03-26 1987-02-17 R. P. Scherer Corporation Freeze-dried foam dosage form
US4855326A (en) 1987-04-20 1989-08-08 Fuisz Pharmaceutical Ltd. Rapidly dissoluble medicinal dosage unit and method of manufacture
TW311136B (enExample) * 1990-11-30 1997-07-21 Otsuka Pharma Co Ltd
US5578322A (en) 1990-11-30 1996-11-26 Yamanouchi Pharmaceutical Co., Ltd. Quick release coated preparation
US5518730A (en) 1992-06-03 1996-05-21 Fuisz Technologies Ltd. Biodegradable controlled release flash flow melt-spun delivery system
US5380473A (en) 1992-10-23 1995-01-10 Fuisz Technologies Ltd. Process for making shearform matrix
ATE208615T1 (de) 1993-07-09 2001-11-15 Scherer Corp R P Verfahren zur herstellung von gefriergetrockneten arzneistoffdosierungsformen
US5616344A (en) 1994-06-14 1997-04-01 Fuisz Technologies Ltd. Apparatus and process for strengthening low density compression dosage units and product therefrom
US5895664A (en) 1993-09-10 1999-04-20 Fuisz Technologies Ltd. Process for forming quickly dispersing comestible unit and product therefrom
US5622719A (en) 1993-09-10 1997-04-22 Fuisz Technologies Ltd. Process and apparatus for making rapidly dissolving dosage units and product therefrom
US5607697A (en) 1995-06-07 1997-03-04 Cima Labs, Incorporated Taste masking microparticles for oral dosage forms
WO1998036738A1 (en) 1997-02-20 1998-08-27 Therics, Inc. Dosage form exhibiting rapid disperse properties, methods of use and process for the manufacture of same
US6277406B1 (en) 1997-10-08 2001-08-21 Fuisz Technologies Ltd. Easily processed tablet compositions
ATE414079T1 (de) * 2000-03-01 2008-11-15 Janssen Pharmaceutica Nv 2,4-disubstituierte thiazolyl derivate

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0259085A1 (en) * 1986-08-29 1988-03-09 Pfizer Inc. 2-Guanidino-4-arylthiazoles for treatment of peptic ulcers
WO2000033841A1 (en) * 1998-12-07 2000-06-15 Smithkline Beecham Corporation Myt1 kinase inhibitors
CN1735611A (zh) * 2003-01-02 2006-02-15 霍夫曼-拉罗奇有限公司 新cb1受体反激动剂
CN101528738A (zh) * 2006-09-01 2009-09-09 沃泰克斯药物股份有限公司 可用作磷脂酰肌醇3-激酶抑制剂的5-（2-呋喃基）-1，3-噻唑衍生物

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Integrative computational protocol for the discovery of inhibitors of the Helicobacter pylori nickel response regulator (NikR);Aldo Segura-Cabrera，等;《J. Mol. Model》;20110301;第17卷;第3075–3084页 *
RN：1225040-09-4;CHEMICAL ABSTRACTS SERVICE;《STN REGISTRY》;20100525 *

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