HUP0102612A2 - Modulators of protein tyrosine phosphatases - Google Patents

Modulators of protein tyrosine phosphatases

Info

Publication number
HUP0102612A2
HUP0102612A2 HU0102612A HUP0102612A HUP0102612A2 HU P0102612 A2 HUP0102612 A2 HU P0102612A2 HU 0102612 A HU0102612 A HU 0102612A HU P0102612 A HUP0102612 A HU P0102612A HU P0102612 A2 HUP0102612 A2 HU P0102612A2
Authority
HU
Hungary
Prior art keywords
diseases
protein tyrosine
tyrosine phosphatases
ptpases
compounds according
Prior art date
Application number
HU0102612A
Other languages
Hungarian (hu)
Inventor
Henrik Sune Andersen
Frank Urban Axe
Farid Bakir
Sven Branner
Yu Ge
Daniel Dale Holsworth
Lars Fogh Iversen
Claus Bekker Jeppesen
Lone Jeppesen
Todd Kevin Jones
Luke Milburn Judge
Niels Peter Hundahl Moller
Ole Hvilsted Olsen
Lutz Stefan Richter
Wiliam Charles Ripka
Jing Su
Roy Teruyuki Uyeda
Josef Vagner
Original Assignee
Novo Nordisk A/S
Ontogen Corporation
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 Novo Nordisk A/S, Ontogen Corporation filed Critical Novo Nordisk A/S
Publication of HUP0102612A2 publication Critical patent/HUP0102612A2/en

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    • C07C235/84Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
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    • C07D213/60Heterocyclic 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
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12Heterocyclic 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 three hetero rings
    • C07D495/14Ortho-condensed systems

Abstract

A találmány tárgyát a fehérje-tirozinfoszfatázokat modulálóvegyületek, valamint ezeket tartalmazó gyógyászati készítményekképezik. A találmány szerinti vegyületek három kritériumnak felelnekmeg: (1) az (I) általános képlet alá tartozik, ahol a képletben R1, R2és R4 jelentése bármely kémiai csoport vagy ezek kombinációja; (2)foszfotirozin felismerő egység ligandumaként viselkedik, előnyösen SH2doménokat tartalmazó fehérjék vagy egy vagy több PTPázok inhibitoravagy modulátora; és (3) móltömege 2500 Dalton vagy ennél kisebb. Atalálmány szerinti vegyületek hatásosan modulálják vagy gátolják akülönböző PTPázokat, és ezért számos betegség kezelésére adhatók. Ezenbetegségek közül említik meg az I és II-típusú diabetest, az autoimmunbetegségeket, osteoporosist, a burjánzásos betegségeket, Alzheimer-kórt, skizofréniát, valamint a fertőzéses betegségeket. ÓThe subject of the invention is compounds that modulate protein tyrosine phosphatases, as well as medicinal preparations containing them. The compounds according to the invention meet three criteria: (1) belong to the general formula (I), where R1, R2 and R4 in the formula are any chemical group or their combination; (2) acts as a ligand for a phosphotyrosine recognition unit, preferably an inhibitor or modulator of proteins containing SH2 domains or one or more PTPases; and (3) has a molecular weight of 2500 Daltons or less. The compounds according to the invention effectively modulate or inhibit various PTPases and can therefore be used to treat many diseases. Among these diseases, type I and II diabetes, autoimmune diseases, osteoporosis, proliferative diseases, Alzheimer's disease, schizophrenia, and infectious diseases are mentioned. HE

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DK47498 1998-04-03
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DK47698 1998-04-03
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US8291298P 1998-04-24 1998-04-24
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US8811598P 1998-06-05 1998-06-05
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DKPA199801385 1998-10-28
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Families Citing this family (55)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6262044B1 (en) 1998-03-12 2001-07-17 Novo Nordisk A/S Modulators of protein tyrosine phosphatases (PTPASES)
DE19946301A1 (en) 1998-04-02 2001-04-19 Asta Medica Ag Antitumor agents and angiogenesis inhibitors having low neurotoxicity, comprise indole-3-glyoxylamide derivatives, are effective against resistant and metastasis-forming carcinomas
DE19814838C2 (en) 1998-04-02 2001-01-18 Asta Medica Ag Indolyl-3-glyoxylic acid derivatives with anti-tumor effects
CA2365945A1 (en) * 1999-04-09 2000-10-19 Max-Planck-Institute For Biochemistry Products and methods for treating ptp lar related diseases
US7115624B1 (en) 1999-09-10 2006-10-03 Novo Nordisk A/S Method of inhibiting protein tyrosine phosphatase 1B and/or T-cell protein tyrosine phosphatase 4 and/or other PTPases with an Asp residue at position 48
US6410556B1 (en) 1999-09-10 2002-06-25 Novo Nordisk A/S Modulators of protein tyrosine phosphateses (PTPases)
US7019026B1 (en) 1999-09-10 2006-03-28 Novo Nordisk A/S Modulators of Protein Tyrosine Phosphatases (PTPases)
EP1214060A2 (en) * 1999-09-10 2002-06-19 Novo Nordisk A/S Method of inhibiting protein tyrosine phosphatase 1b and/or t-cell protein tyrosine phosphatase and/or other ptpases with an asp residue at position 48
JP2003509429A (en) * 1999-09-10 2003-03-11 ノボ ノルディスク アクティーゼルスカブ Modulator of protein tyrosine phosphatase (PTPase)
TWI269654B (en) * 1999-09-28 2007-01-01 Baxter Healthcare Sa N-substituted indole-3-glyoxylamide compounds having anti-tumor action
DE60132723T2 (en) 2000-01-21 2009-01-29 Novartis Pharma Ag Compositions consisting of dipeptidyl peptidase IV inhibitors and antidiabetics
US6867299B2 (en) 2000-02-24 2005-03-15 Hoffmann-La Roche Inc. Oxamide IMPDH inhibitors
CA2452445C (en) * 2000-06-29 2011-02-15 North Shore-Long Island Jewish Health System Modulators of cellular proliferation and angiogenesis, methods for use and identification thereof
US6613903B2 (en) 2000-07-07 2003-09-02 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)
ATE321052T1 (en) * 2000-07-07 2006-04-15 Novo Nordisk As MODULATORS OF PROTEIN TYROSINE PHOSPHATASES (PTPASES)
DE10038709A1 (en) * 2000-08-09 2002-02-28 Aventis Pharma Gmbh Substituted and unsubstituted benzooxathiazoles and compounds derived from them
US20020169157A1 (en) * 2000-08-29 2002-11-14 Gang Liu Selective protein tyrosine phosphatatase inhibitors
US6627767B2 (en) 2000-08-29 2003-09-30 Abbott Laboratories Amino(oxo) acetic acid protein tyrosine phosphatase inhibitors
US6972340B2 (en) 2000-08-29 2005-12-06 Abbott Laboratories Selective protein tyrosine phosphatatase inhibitors
US6569853B1 (en) 2000-11-06 2003-05-27 Combinatorx, Incorporated Combinations of chlorpromazine and pentamidine for the treatment of neoplastic disorders
US20020116729A1 (en) * 2000-12-06 2002-08-22 Allen Keith D. Transgenic mice containing NTTP1 phosphatase gene disruptions
US20020152493A1 (en) * 2000-12-06 2002-10-17 Allen Keith D. Transgenic mice containing PTP36 tyrosine phosphatase gene disruptions
US20100074949A1 (en) 2008-08-13 2010-03-25 William Rowe Pharmaceutical composition and administration thereof
EP1404682B1 (en) * 2001-06-29 2005-09-14 Novo Nordisk A/S Method of inhibiting ptp 1b and/or t-cell ptp and/or other ptpases with an asp residue at position 48
FR2829766A1 (en) * 2001-09-14 2003-03-21 Lipha Composition useful in the treatment of pathologies associated with e.g. hyperglycemia, diabetes, dyslipidemia, obesity, arterial hypertension, neuropathies, and nephropathies, comprises oxamate derivatives
US7521473B2 (en) 2004-02-25 2009-04-21 Wyeth Inhibitors of protein tyrosine phosphatase 1B
PL1773816T3 (en) 2004-06-24 2015-06-30 Vertex Pharma Modulators of ATP-binding cassette transporters
ES2393768T3 (en) 2005-05-26 2012-12-27 Neuron Systems, Inc Quinoline derivative for the treatment of retinal diseases
PT1931350E (en) 2005-09-14 2014-02-12 Takeda Pharmaceutical Administration of dipeptidyl peptidase inhibitors
LT1993360T (en) 2005-12-28 2017-06-12 Vertex Pharmaceuticals Incorporated Solid forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
CA2984994C (en) 2009-03-20 2020-03-31 Vertex Pharmaceuticals Incorporated Process for making modulators of cystic fibrosis transmembrane conductance regulator
WO2011041293A1 (en) 2009-09-30 2011-04-07 Takeda Pharmaceutical Company Limited Pyrazolo [1, 5-a] pyrimidine derivatives as apoptosis signal-regulating kinase 1 inhibitors
RU2557059C2 (en) 2009-12-04 2015-07-20 Суновион Фармасьютикалз, Инк. Polycyclic compound and methods of their application
CA2782015C (en) 2009-12-11 2020-08-25 Neuron Systems, Inc. Topical ophthalmic compositions and methods for the treatment of macular degeneration
US8802695B2 (en) 2010-02-03 2014-08-12 Takeda Pharmaceutical Company Limited Apoptosis signal-regulating kinase 1 inhibitors
AU2013226076B2 (en) 2012-02-27 2017-11-16 Vertex Pharmaceuticals Incorporated Pharmaceutical composition and administration thereof
CA2896032A1 (en) 2012-12-20 2014-06-26 Aldeyra Therapeutics, Inc. Peri-carbinols
CA2898631C (en) 2013-01-23 2023-06-13 Aldeyra Therapeutics, Inc. Toxic aldehyde related diseases and treatment
JP6266023B2 (en) 2013-01-25 2018-01-24 アルデイラ セラピューティクス, インコーポレイテッド A new trap in the treatment of macular degeneration
JP6425724B2 (en) 2013-08-08 2018-11-21 ガラパゴス・ナムローゼ・フェンノートシャップGalapagos N.V. Thieno [2,3-C] pyrans as CFTR Modulators
MX370450B (en) 2014-10-07 2019-12-13 Vertex Pharma Co-crystals of modulators of cystic fibrosis transmembrane conductance regulator.
EP3337486B1 (en) 2015-08-21 2024-04-03 Aldeyra Therapeutics, Inc. Deuterated compounds and uses thereof
MX2018013472A (en) 2016-05-09 2019-02-28 Aldeyra Therapeutics Inc Combination treatment of ocular inflammatory disorders and diseases.
EP3494119A4 (en) 2016-07-29 2020-03-25 Sunovion Pharmaceuticals Inc. Compounds and compositions and uses thereof
EP3490607A4 (en) 2016-07-29 2020-04-08 Sunovion Pharmaceuticals Inc. Compounds and compositions and uses thereof
WO2018151861A1 (en) 2017-02-16 2018-08-23 Sunovion Pharamaceuticials Inc. Methods of treating schizophrenia
CN110431130A (en) 2017-03-16 2019-11-08 奥尔德拉医疗公司 Multi-crystalline compounds and its purposes
EP3661929B1 (en) 2017-08-02 2021-07-14 Sunovion Pharmaceuticals Inc. Isochroman compounds and uses thereof
EP3694500A4 (en) 2017-10-10 2021-06-30 Aldeyra Therapeutics, Inc. Treatment of inflammatory disorders
WO2019120484A1 (en) * 2017-12-19 2019-06-27 Wacker Chemie Ag Method for producing siloxanes comprising oxamido ester groups
MX2020008537A (en) 2018-02-16 2021-01-08 Sunovion Pharmaceuticals Inc Salts, crystal forms, and production methods thereof.
CN112714762A (en) 2018-08-06 2021-04-27 奥尔德拉医疗公司 Polymorphic compounds and uses thereof
CA3130849A1 (en) 2019-03-14 2020-09-17 Sunovion Pharmaceuticals Inc. Salts of a isochromanyl compound and crystalline forms, processes for preparing, therapeutic uses, and pharmaceutical compositions thereof
WO2021211489A1 (en) 2020-04-14 2021-10-21 Sunovion Pharmaceuticals Inc. (s)-(4,5-dihydro-7h-thieno[2,3-c]pyran-7-yl)-n-methylmethanamine for treating neurological and psychiatric disorders

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0831795A2 (en) * 1995-06-07 1998-04-01 Sugen, Inc. Phosphatase inhibitors

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