CN101421256A - 蛋白酪氨酸磷酸酶的噻二唑烷酮抑制剂 - Google Patents

蛋白酪氨酸磷酸酶的噻二唑烷酮抑制剂 Download PDF

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Publication number
CN101421256A
CN101421256A CNA2007800120054A CN200780012005A CN101421256A CN 101421256 A CN101421256 A CN 101421256A CN A2007800120054 A CNA2007800120054 A CN A2007800120054A CN 200780012005 A CN200780012005 A CN 200780012005A CN 101421256 A CN101421256 A CN 101421256A
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hydroxy
thiadiazolidin
phenyl
trioxo
substituted
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Chinese (zh)
Inventor
A·诺伊贝特
D·巴恩斯
郭英信
中岛胜正
G·R·贝伯恩尼茨
G·M·科波拉
L·克尔曼
M·H·塞拉诺-武
T·施塔姆斯
S·W·托皮欧
T·R·维达那达
J·R·韦尔林
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Novartis AG
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Novartis AG
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Publication of CN101421256A publication Critical patent/CN101421256A/zh
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/10—1,2,5-Thiadiazoles; Hydrogenated 1,2,5-thiadiazoles
    • 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
    • A61K31/41—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
    • A61K31/433—Thidiazoles
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
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    • 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
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    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • 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
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • 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
    • C07D417/10—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 carbon chain containing aromatic rings

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  • Health & Medical Sciences (AREA)
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  • Biomedical Technology (AREA)
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  • Orthopedic Medicine & Surgery (AREA)
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  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Child & Adolescent Psychology (AREA)
  • Epidemiology (AREA)
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  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
CNA2007800120054A 2006-03-31 2007-03-29 蛋白酪氨酸磷酸酶的噻二唑烷酮抑制剂 Pending CN101421256A (zh)

Applications Claiming Priority (2)

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US78850206P 2006-03-31 2006-03-31
US60/788,502 2006-03-31

Publications (1)

Publication Number Publication Date
CN101421256A true CN101421256A (zh) 2009-04-29

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CNA2007800120054A Pending CN101421256A (zh) 2006-03-31 2007-03-29 蛋白酪氨酸磷酸酶的噻二唑烷酮抑制剂

Country Status (11)

Country Link
US (1) US8084448B2 (https=)
EP (1) EP2038267A2 (https=)
JP (1) JP2009532379A (https=)
KR (1) KR20080110882A (https=)
CN (1) CN101421256A (https=)
AU (1) AU2007233251A1 (https=)
BR (1) BRPI0710182A2 (https=)
CA (1) CA2647472A1 (https=)
MX (1) MX2008012598A (https=)
RU (1) RU2008143053A (https=)
WO (1) WO2007115058A2 (https=)

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102659539A (zh) * 2012-05-15 2012-09-12 北京化工大学 一种由α,β-不饱和酰氯制备二氢查尔酮类化合物的方法
CN102884047A (zh) * 2009-12-04 2013-01-16 大正制药株式会社 2-吡啶酮化合物
CN116283467A (zh) * 2023-01-18 2023-06-23 四川大学 一种合成二芳基烷基甲烷的方法
CN117658947A (zh) * 2022-09-06 2024-03-08 杭州中美华东制药有限公司 蛋白酪氨酸磷酸酶抑制作用的5-(取代芳基)-1,2,5-噻二唑啉-3-酮类化合物
CN119220146A (zh) * 2024-10-24 2024-12-31 山东三佳聚合高分子材料有限公司 一种新型隔热保温涂料
WO2025077572A1 (zh) * 2023-10-13 2025-04-17 华东师范大学 一种用于前药给药系统的可裂解连接体化合物及其制备和应用
WO2026037253A1 (zh) * 2024-08-10 2026-02-19 杭州英创医药科技有限公司 作为ptpn抑制剂的化合物

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UA94921C2 (en) 2005-12-08 2011-06-25 Новартис Аг 1-orthofluorophenyl substituted 1, 2, 5-thiazolidinedione derivatives as ptp-as inhibitors
CA2629819A1 (en) * 2005-12-08 2007-06-14 Novartis Ag 1,2,5-thiazolidine derivatives useful for treating conditions mediated by protein tyrosine phosphatases (ptpase)
CA2630448A1 (en) * 2005-12-08 2007-06-14 Novartis Ag 1,1,3-trioxo-1,2,5-thiadiazolidines and their use as ptp-ases inhibitors
UA94724C2 (en) * 2005-12-08 2011-06-10 Новартис Аг Thiadiazolidinone derivatives as antidiabetic agents
EP2025674A1 (de) 2007-08-15 2009-02-18 sanofi-aventis Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
WO2011107494A1 (de) 2010-03-03 2011-09-09 Sanofi Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung
EP2582709B1 (de) 2010-06-18 2018-01-24 Sanofi Azolopyridin-3-on-derivate als inhibitoren von lipasen und phospholipasen
US8530413B2 (en) 2010-06-21 2013-09-10 Sanofi Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments
TW201215388A (en) 2010-07-05 2012-04-16 Sanofi Sa (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments
TW201215387A (en) 2010-07-05 2012-04-16 Sanofi Aventis Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament
TW201221505A (en) 2010-07-05 2012-06-01 Sanofi Sa Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament
JP5809157B2 (ja) * 2010-10-08 2015-11-10 持田製薬株式会社 環状アミド誘導体
EP2683704B1 (de) 2011-03-08 2014-12-17 Sanofi Verzweigte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
WO2012120056A1 (de) 2011-03-08 2012-09-13 Sanofi Tetrasubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
US8828994B2 (en) 2011-03-08 2014-09-09 Sanofi Di- and tri-substituted oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof
EP2683699B1 (de) 2011-03-08 2015-06-24 Sanofi Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
EP2766349B1 (de) 2011-03-08 2016-06-01 Sanofi Mit carbozyklen oder heterozyklen substituierte oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung
JPWO2012147516A1 (ja) * 2011-04-28 2014-07-28 持田製薬株式会社 環状アミド誘導体
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WO2013045413A1 (en) 2011-09-27 2013-04-04 Sanofi 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
US9216988B2 (en) * 2011-12-22 2015-12-22 Genentech, Inc. Benzyl sulfonamide derivatives as RORc modulators
WO2014081718A1 (en) 2012-11-20 2014-05-30 Genentech, Inc. Aminopyrimidine compounds as inhibitors of t790m containing egfr mutants
WO2017165139A1 (en) 2016-03-25 2017-09-28 St. Jude Children's Research Hospital 1,4,5-substituted 1,2,3-triazole analogues as antagonists of the pregnane x receptor
AU2019200683B2 (en) * 2018-02-01 2024-05-30 The University Of Sydney Anti-cancer compounds
EA202092305A1 (ru) * 2018-03-27 2020-12-07 Нейропор Терапиз, Инк. Соединения в качестве модуляторов сигнализации tlr2
BR112020026086A2 (pt) * 2018-06-21 2021-03-23 Calico Life Sciences Llc inibidores da proteína tirosina fosfatase e métodos de uso destes
WO2020035019A1 (zh) 2018-08-17 2020-02-20 浙江海正药业股份有限公司 吲唑胺类衍生物及其制备方法和其在医药上的用途
IL286373B2 (en) * 2019-03-14 2026-03-01 Calico Life Sciences Llc Protein tyrosine phosphate inhibitor compounds and uses thereof
EP4073242A4 (en) 2019-12-12 2024-01-03 Kumquat Biosciences Inc. Compositions and methods for potentiating immune activity
PE20241474A1 (es) * 2021-11-23 2024-07-17 Kumquat Biosciences Inc Compuestos que contienen heteroatomos y usos de estos
PE20250780A1 (es) * 2022-02-02 2025-03-14 Nerio Therapeutics Inc Inhibidores de proteina tirosina fosfatasa y usos de estos
JP2025513882A (ja) * 2022-04-14 2025-04-30 ネリオ セラピューティクス，インク． タンパク質チロシンホスファターゼ阻害剤およびその使用
EP4522594A4 (en) * 2022-05-13 2026-04-22 Mondego Bio Lda A Limited Liability Company By Quotas Soc Por Quotas PTPN2 INHIBITORS
AR131413A1 (es) * 2022-12-21 2025-03-19 Bristol Myers Squibb Co Inhibidores de la proteína tirosina fosfatasa, composiciones y métodos de uso
PE20252789A1 (es) 2023-05-24 2025-12-22 Kumquat Biosciences Inc Compuestos heterociclicos y usos de estos
US20260008777A1 (en) * 2024-07-08 2026-01-08 Bristol-Myers Squibb Company Inhibitors of protein tyrosine phosphatase, compositions, and methods of use
US20260092058A1 (en) 2024-09-30 2026-04-02 St. Jude Children's Research Hospital, Inc. Small Molecule Degraders and Fluorescent Probes of PXR

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EP1594497B1 (en) * 2002-12-30 2009-05-27 Vertex Pharmaceuticals Incorporated Sulfhydantoins as phosphate isosteres for use as phosphatase inhibitors in the treatment of cancer and autoimmune disorders
UA94921C2 (en) * 2005-12-08 2011-06-25 Новартис Аг 1-orthofluorophenyl substituted 1, 2, 5-thiazolidinedione derivatives as ptp-as inhibitors
CA2630448A1 (en) * 2005-12-08 2007-06-14 Novartis Ag 1,1,3-trioxo-1,2,5-thiadiazolidines and their use as ptp-ases inhibitors
CA2629819A1 (en) * 2005-12-08 2007-06-14 Novartis Ag 1,2,5-thiazolidine derivatives useful for treating conditions mediated by protein tyrosine phosphatases (ptpase)

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102884047A (zh) * 2009-12-04 2013-01-16 大正制药株式会社 2-吡啶酮化合物
CN102884047B (zh) * 2009-12-04 2015-11-25 日产化学工业株式会社 2-吡啶酮化合物
CN102659539A (zh) * 2012-05-15 2012-09-12 北京化工大学 一种由α,β-不饱和酰氯制备二氢查尔酮类化合物的方法
CN117658947A (zh) * 2022-09-06 2024-03-08 杭州中美华东制药有限公司 蛋白酪氨酸磷酸酶抑制作用的5-(取代芳基)-1,2,5-噻二唑啉-3-酮类化合物
CN117658947B (zh) * 2022-09-06 2026-03-06 杭州中美华东制药有限公司 蛋白酪氨酸磷酸酶抑制作用的5-(取代芳基)-1,2,5-噻二唑啉-3-酮类化合物
CN116283467A (zh) * 2023-01-18 2023-06-23 四川大学 一种合成二芳基烷基甲烷的方法
CN116283467B (zh) * 2023-01-18 2024-06-11 四川大学 一种合成二芳基烷基甲烷的方法
WO2025077572A1 (zh) * 2023-10-13 2025-04-17 华东师范大学 一种用于前药给药系统的可裂解连接体化合物及其制备和应用
WO2026037253A1 (zh) * 2024-08-10 2026-02-19 杭州英创医药科技有限公司 作为ptpn抑制剂的化合物
CN119220146A (zh) * 2024-10-24 2024-12-31 山东三佳聚合高分子材料有限公司 一种新型隔热保温涂料

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WO2007115058A2 (en) 2007-10-11
WO2007115058A3 (en) 2008-03-20
US8084448B2 (en) 2011-12-27
BRPI0710182A2 (pt) 2012-08-07
KR20080110882A (ko) 2008-12-19
AU2007233251A1 (en) 2007-10-11
RU2008143053A (ru) 2010-05-10
CA2647472A1 (en) 2007-10-11
US20090181928A1 (en) 2009-07-16
EP2038267A2 (en) 2009-03-25
MX2008012598A (es) 2008-10-10
JP2009532379A (ja) 2009-09-10

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Application publication date: 20090429