ATE534637T1 - 5-substituierte 1,1-dioxo- 1,2,5 thiazolidin-3- onderivate als ptpase 1b hemmer - Google Patents

5-substituierte 1,1-dioxo- 1,2,5 thiazolidin-3- onderivate als ptpase 1b hemmer

Info

Publication number
ATE534637T1
ATE534637T1 AT03720412T AT03720412T ATE534637T1 AT E534637 T1 ATE534637 T1 AT E534637T1 AT 03720412 T AT03720412 T AT 03720412T AT 03720412 T AT03720412 T AT 03720412T AT E534637 T1 ATE534637 T1 AT E534637T1
Authority
AT
Austria
Prior art keywords
compounds
employed
formula
inhibitors
ptpase
Prior art date
Application number
AT03720412T
Other languages
English (en)
Inventor
Gary Coppola
John Davies
Charles Jewell
Yu-Chin Li
James Wareing
Donald Sperbeck
Travis Stams
Sidney Topiol
Isidoros Vlattas
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Application granted granted Critical
Publication of ATE534637T1 publication Critical patent/ATE534637T1/de

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    • C—CHEMISTRY; METALLURGY
    • 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
    • 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
    • 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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • 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
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • 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
    • C07D417/06—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 only aliphatic carbon atoms
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Oncology (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Emergency Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
AT03720412T 2002-04-03 2003-04-02 5-substituierte 1,1-dioxo- 1,2,5 thiazolidin-3- onderivate als ptpase 1b hemmer ATE534637T1 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US36977902P 2002-04-03 2002-04-03
US36993002P 2002-04-03 2002-04-03
PCT/EP2003/003466 WO2003082841A1 (en) 2002-04-03 2003-04-02 5-substituted 1,1-dioxo-`1,2,5!thiazolidine-3-one derivatives as ptpase 1b inhibitors

Publications (1)

Publication Number Publication Date
ATE534637T1 true ATE534637T1 (de) 2011-12-15

Family

ID=28678287

Family Applications (1)

Application Number Title Priority Date Filing Date
AT03720412T ATE534637T1 (de) 2002-04-03 2003-04-02 5-substituierte 1,1-dioxo- 1,2,5 thiazolidin-3- onderivate als ptpase 1b hemmer

Country Status (19)

Country Link
US (3) US20040023974A1 (de)
EP (2) EP2341049A1 (de)
JP (2) JP2005535568A (de)
KR (1) KR100868587B1 (de)
CN (1) CN1646508A (de)
AT (1) ATE534637T1 (de)
AU (1) AU2003224030B2 (de)
BR (1) BR0308974A (de)
CA (1) CA2480562C (de)
CO (1) CO5611132A2 (de)
ES (1) ES2378146T3 (de)
IL (2) IL164262A0 (de)
MX (1) MXPA04009633A (de)
NO (1) NO20044745L (de)
NZ (1) NZ535545A (de)
PL (1) PL372848A1 (de)
PT (1) PT1492780E (de)
RU (1) RU2349589C2 (de)
WO (1) WO2003082841A1 (de)

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GB0225986D0 (en) * 2002-11-07 2002-12-11 Astrazeneca Ab Chemical compounds
GB0227813D0 (en) * 2002-11-29 2003-01-08 Astrazeneca Ab Chemical compounds
US7432292B2 (en) * 2002-12-30 2008-10-07 Vertex Pharmaceuticals Incorporated Sulfhydantoins as phosphate isosteres
WO2004071448A2 (en) * 2003-02-12 2004-08-26 Transtech Pharma Inc. Substituted azole derivatives as inhibitors of protein tyrosine phosphatases
JP2006518738A (ja) * 2003-02-12 2006-08-17 トランス　テック　ファーマ，インコーポレイテッド 治療薬としての置換アゾール誘導体
US7141596B2 (en) 2003-10-08 2006-11-28 Incyte Corporation Inhibitors of proteins that bind phosphorylated molecules
US20050187277A1 (en) * 2004-02-12 2005-08-25 Mjalli Adnan M. Substituted azole derivatives, compositions, and methods of use
AU2006265653A1 (en) * 2005-07-01 2007-01-11 Novartis Ag Combination of a renin inhibitor and an insulin secretion enhancer or an insulin sensitizer
BRPI0619547A2 (pt) * 2005-12-08 2011-10-04 Novartis Ag 1,1,3-trioxo-1,2,5-tiadiazolidinas, composição farmacêutica e uso das mesmas
UA94921C2 (en) * 2005-12-08 2011-06-25 Новартис Аг 1-orthofluorophenyl substituted 1, 2, 5-thiazolidinedione derivatives as ptp-as inhibitors
KR20080074970A (ko) * 2005-12-08 2008-08-13 노파르티스 아게 단백질 티로신 포스파타제 (ｐｔｐａｓｅ)에 의해 매개되는질병의 치료에 유용한 1,2,5-티아졸리딘 유도체
UA94724C2 (en) * 2005-12-08 2011-06-10 Новартис Аг Thiadiazolidinone derivatives as antidiabetic agents
EA019879B1 (ru) 2005-12-29 2014-07-30 Лексикон Фармасьютикалз, Инк. Полициклические производные аминокислот, содержащая их фармацевтическая композиция и способ лечения, использующий эти производные
AU2007211319B9 (en) 2006-01-30 2012-05-31 Vtv Therapeutics Llc Substituted imidazole derivatives and their use as PTPase inhibitors
AU2007233251A1 (en) * 2006-03-31 2007-10-11 Novartis Ag Thiadiazolidinone inhibitors of PTPase
WO2008067527A1 (en) * 2006-12-01 2008-06-05 Novartis Ag Inhibitors of protein tyrosine phosphatase for the treatment of muscle atrophy and related disorders
AR066820A1 (es) * 2007-06-04 2009-09-16 Novartis Ag Compuestos de tiadiazolidin-3 ona
JP5856064B2 (ja) * 2009-11-17 2016-02-09 ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン 治療特性を有する１，４−ベンゾジアゼピン−２，５−ジオンおよび関連化合物
AU2011306397A1 (en) 2010-09-24 2013-05-02 Ranbaxy Laboratories Limited Matrix metalloproteinase inhibitors
JP5809157B2 (ja) * 2010-10-08 2015-11-10 持田製薬株式会社 環状アミド誘導体
EP2716636A4 (de) 2011-04-28 2014-11-26 Mochida Pharm Co Ltd Zyklische amidderivate
BR112015023571A2 (pt) * 2013-03-15 2017-07-18 Hoffmann La Roche derivados de sulfamato e sulfamida de arila como moduladores rorc
KR102533477B1 (ko) * 2018-06-21 2023-05-18 칼리코 라이프 사이언시스 엘엘씨 단백질 타이로신 포스파타아제 억제제 및 그의 사용 방법
EP4073242A4 (de) 2019-12-12 2024-01-03 Kumquat Biosciences Inc. Zusammensetzungen und verfahren zur potenzierung der immunaktivität
US12540147B2 (en) * 2020-05-15 2026-02-03 Tokuyama Corporation Method for purifying organic compound and method for producing organic compound
CN117279913A (zh) * 2021-03-11 2023-12-22 金橘生物科技公司 杂环化合物及其用途
US20250041272A1 (en) * 2021-11-03 2025-02-06 The University Of North Carolina At Chapel Hill Compositions and methods for treating cancer via ptp1b inhibition
AU2023269777A1 (en) * 2022-05-13 2024-11-28 Mondego Bio, Lda. Ptpn2 inhibitors
WO2024067802A1 (zh) * 2022-09-30 2024-04-04 深圳众格生物科技有限公司 蛋白酪氨酸磷酸酶抑制剂及其制备方法和医药用途
WO2024141015A1 (en) * 2022-12-30 2024-07-04 Insilico Medicine Ip Limited Protein tyrosine phosphatase inhibitors and uses thereof
EP4720059A1 (de) 2023-05-24 2026-04-08 Kumquat Biosciences Inc. Heterocyclische verbindungen und verwendungen davon
US12427124B1 (en) 2024-04-10 2025-09-30 Maxymune Therapeutics, Inc. Phenylalanine-based LAT1 inhibitors and uses thereof

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FR2764889B1 (fr) * 1997-06-20 2000-09-01 Sod Conseils Rech Applic Nouveaux derives du 2-(iminomethyl)amino-phenyle, leur preparation, leur application a titre de medicaments et les compositions pharmaceutiques les contenant
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JP2002506073A (ja) 1998-03-12 2002-02-26 ノボ ノルディスク アクティーゼルスカブ プロテイン・チロシン・ホスファターゼ（ＰＴＰａｓｅｓ）のモジュレーター
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ATE321052T1 (de) 2000-07-07 2006-04-15 Novo Nordisk As Modulatoren von protein tyrosin phosphatasen (ptpasen)

Also Published As

Publication number Publication date
ES2378146T3 (es) 2012-04-09
NZ535545A (en) 2007-06-29
AU2003224030A1 (en) 2003-10-13
KR20050008669A (ko) 2005-01-21
JP2010043130A (ja) 2010-02-25
JP2005535568A (ja) 2005-11-24
EP1492780A1 (de) 2005-01-05
EP2341049A1 (de) 2011-07-06
RU2349589C2 (ru) 2009-03-20
US7291635B2 (en) 2007-11-06
IL164316A0 (en) 2005-12-18
NO20044745L (no) 2004-12-14
US20050090502A1 (en) 2005-04-28
BR0308974A (pt) 2005-02-15
US20080139576A1 (en) 2008-06-12
CN1646508A (zh) 2005-07-27
CA2480562C (en) 2011-02-15
CA2480562A1 (en) 2003-10-09
IL164262A0 (en) 2005-12-18
PL372848A1 (en) 2005-08-08
WO2003082841A1 (en) 2003-10-09
KR100868587B1 (ko) 2008-11-12
US20040023974A1 (en) 2004-02-05
AU2003224030B2 (en) 2007-11-01
PT1492780E (pt) 2012-04-11
CO5611132A2 (es) 2006-02-28
RU2004132206A (ru) 2005-07-20
MXPA04009633A (es) 2005-01-11
EP1492780B1 (de) 2011-11-23

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