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)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Genetics & Genomics (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Emergency Medicine (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Urology & Nephrology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Child & Adolescent Psychology (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) EP1492780B1 (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
AU2003300447B2 (en) * 2002-12-30 2009-09-03 Vertex Pharmaceuticals Incorporated Sulfhydantoins as phosphate isosteres for use as phosphatase inhibitors in the treatment of cancer and autoimmune disorders
US20040186151A1 (en) * 2003-02-12 2004-09-23 Mjalli Adnan M.M. Substituted azole derivatives as therapeutic agents
AU2004210711B2 (en) * 2003-02-12 2010-07-08 Transtech Pharma, Inc. Substituted azole derivatives as therapeutic agents
WO2005035551A2 (en) 2003-10-08 2005-04-21 Incyte Corporation Inhibitors of proteins that bind phosphorylated molecules
WO2005080346A1 (en) * 2004-02-12 2005-09-01 Transtech Pharma, Inc. Substituted azole derivatives, compositions, and methods of use
BRPI0612582A2 (pt) * 2005-07-01 2010-11-23 Novartis Ag combinação de compostos orgánicos
UA94921C2 (en) * 2005-12-08 2011-06-25 Новартис Аг 1-orthofluorophenyl substituted 1, 2, 5-thiazolidinedione derivatives as ptp-as inhibitors
RU2008127253A (ru) * 2005-12-08 2010-01-20 Новартис АГ (CH) 1,1,3-триоксо-1,2,5-тиадиазолидины и их применение в качестве ингибиторов птфаз
EP1963294B1 (de) * 2005-12-08 2012-10-10 Novartis AG 1,2,5-thiazolidin-derivate zur behandlung von durch protein-tyrosin- phosphatase (ptpase) hervorgerufenen erkrankungen
UA94724C2 (en) * 2005-12-08 2011-06-10 Новартис Аг Thiadiazolidinone derivatives as antidiabetic agents
WO2007089335A2 (en) * 2005-12-29 2007-08-09 Lexicon Pharmaceutical Inc. Multicyclic amino acid derivatives and methods of their use
EP1991544B1 (de) * 2006-01-30 2018-08-15 vTv Therapeutics LLC Substituierte imidazol- derivate und ihre verwendung als ptpase inhibitoren
JP2009532379A (ja) * 2006-03-31 2009-09-10 ノバルティス アクチエンゲゼルシャフト ＰＴＰａｓｅのチアジアゾリジノン阻害剤
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
SG188644A1 (en) 2010-09-24 2013-05-31 Ranbaxy Lab Ltd Matrix metalloproteinase inhibitors
AU2011313191A1 (en) * 2010-10-08 2013-05-02 Mochida Pharmaceutical Co., Ltd. Cyclic amide derivative
JPWO2012147516A1 (ja) * 2011-04-28 2014-07-28 持田製薬株式会社 環状アミド誘導体
CN105121404A (zh) * 2013-03-15 2015-12-02 豪夫迈·罗氏有限公司 作为RORc调节剂的芳基磺酰胺和氨基磺酸衍生物
TWI888352B (zh) * 2018-06-21 2025-07-01 美商嘉來克生命科學有限責任公司 蛋白質酪胺酸磷酸酯酶抑制劑及其使用方法
AU2020401376A1 (en) 2019-12-12 2022-06-30 Kumquat Biosciences Inc. Compositions and methods for potentiating immune activity
WO2021230280A1 (ja) * 2020-05-15 2021-11-18 株式会社トクヤマ 有機化合物の精製方法及び有機化合物の製造方法
EP4305030A4 (de) * 2021-03-11 2025-05-21 Kumquat Biosciences Inc. Heterocyclen und verwendungen davon
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
KR20250011138A (ko) * 2022-05-13 2025-01-21 네스 테라퓨틱스 인코포레이티드 Ptpn2 저해제
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
WO2024243441A1 (en) 2023-05-24 2024-11-28 Kumquat Biosciences Inc. Heterocyclic compounds and uses thereof
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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WO1999046244A1 (en) 1998-03-12 1999-09-16 Novo Nordisk A/S Modulators of protein tyrosine phosphatases (ptpases)
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
WO1999046236A1 (en) 1998-03-12 1999-09-16 Novo Nordisk A/S Modulators of protein tyrosine phosphatases (ptpases)
EP1214325B1 (de) * 1999-09-10 2005-11-09 Novo Nordisk A/S Modulatoren der protein tyrosin phosphatase (ptpases)
EP1214324B1 (de) 1999-09-10 2006-06-14 Novo Nordisk A/S Modulatoren der protein tyrosin phosphatase (ptpases)
WO2002004459A1 (en) 2000-07-07 2002-01-17 Novo Nordisk A/S Modulators of protein tyrosine phosphatases (ptpases)
AU2001268951A1 (en) 2000-07-07 2002-01-21 Novo-Nordisk A/S Modulators of protein tyrosine phosphatases (ptpases)

Also Published As

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

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