ECSP055631A - ANTRANILAMIDOPIRIMIDINAS THAT INHIBIT VEGFR-2 AND VEGFR-3 - Google Patents

ANTRANILAMIDOPIRIMIDINAS THAT INHIBIT VEGFR-2 AND VEGFR-3

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Publication number
ECSP055631A
ECSP055631A EC2005005631A ECSP055631A ECSP055631A EC SP055631 A ECSP055631 A EC SP055631A EC 2005005631 A EC2005005631 A EC 2005005631A EC SP055631 A ECSP055631 A EC SP055631A EC SP055631 A ECSP055631 A EC SP055631A
Authority
EC
Ecuador
Prior art keywords
vegfr
diseases
compounds
inhibit
cases
Prior art date
Application number
EC2005005631A
Other languages
Spanish (es)
Inventor
Andreas Menrad
Ludwig Zorn
Andreas Huth
Martin Krueger
Stuart Ince
Karl-Heinz Thierauch
Martin Haberey
Stump Holger Hess
Original Assignee
Schering 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
Priority claimed from DE10235690A external-priority patent/DE10235690A1/en
Priority claimed from DE10328036A external-priority patent/DE10328036A1/en
Application filed by Schering Ag filed Critical Schering Ag
Publication of ECSP055631A publication Critical patent/ECSP055631A/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic 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
    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
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    • A61P9/08—Vasodilators for multiple indications
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    • A—HUMAN NECESSITIES
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    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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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    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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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    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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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    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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Abstract

Se describen antranilamidopiridinamidas que inhiben VEGFR-2 y VEGFR-3, su preparación y su uso como medicamento para el tratamiento de enfermedades originadas por angiogénesis persistente y productos intermedios para la preparación de los compuestos. Los compuestos de la invención se pueden usar en casos de crecimiento de tumores o metástasis, psoriasis, sarcoma de Kaposi, restenosis, como p. ej. restenosis inducida por stent, endometriosis, enfermedad de Crohn, mal de Hodgkins, leucemia, artritis, tal como artritis reumatoide, hemangioma, angiofibroma, enfermedades oculares tales como retinopatía diabética, glaucoma neovascular, enfermedades renales como glomeronefritis, nefropatía diabética, nefroesclerosis maligna, síndromes microangiopáticos trómbicos, rechazos de transplantes y glomerulopatía, enfermedades fibróticas como cirrosis hepática, enfermedades proliferativas de células mesangiales, arterioesclerosis, lesiones del tejido nervioso para inhibir la reoclusión de vasos después de tratamiento de catéter de balón hinchable, en casos de prótesis vasculares o después de colocar dispositivos mecánicos para mantener abiertos los vasos, como p. ej. stents, como inmunosupresor, para la curación de heridas sin cicatriz, para léntigo senil y dermatitis de contacto. Tales compuestos también pueden ser usados como inhibidores de VEGFR-3 en la angiogénesis linfática.Anthranilamidopyridinamides that inhibit VEGFR-2 and VEGFR-3, their preparation and their use as a medicament for the treatment of diseases caused by persistent angiogenesis and intermediates for the preparation of the compounds are described. The compounds of the invention can be used in cases of tumor growth or metastasis, psoriasis, Kaposi's sarcoma, restenosis, such as e.g. ex. stent-induced restenosis, endometriosis, Crohn's disease, Hodgkins disease, leukemia, arthritis, such as rheumatoid arthritis, hemangioma, angiofibroma, eye diseases such as diabetic retinopathy, neovascular glaucoma, kidney diseases such as glomeronephritis, diabetic nephropathy, nephrosclerosis, malignant syndromes trombic microangiopathic, transplant rejection and glomerulopathy, fibrotic diseases such as liver cirrhosis, proliferative diseases of mesangial cells, arteriosclerosis, nerve tissue lesions to inhibit reocclusion of vessels after inflatable balloon catheter treatment, in cases of vascular prostheses or after place mechanical devices to keep the vessels open, such as p. ex. stents, as an immunosuppressant, for healing wounds without a scar, for senile lentigo and contact dermatitis. Such compounds can also be used as VEGFR-3 inhibitors in lymphatic angiogenesis.

EC2005005631A 2002-07-31 2005-02-24 ANTRANILAMIDOPIRIMIDINAS THAT INHIBIT VEGFR-2 AND VEGFR-3 ECSP055631A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE10235690A DE10235690A1 (en) 2002-07-31 2002-07-31 New N-benzyl-anthranilic acid (hetero)arylamide derivatives and analogs, are tyrosine kinase KDR and FLT inhibitors and angiogenesis inhibitors, useful e.g. for treating tumors, psoriasis or restenosis
DE10328036A DE10328036A1 (en) 2003-06-19 2003-06-19 New N-benzyl-anthranilic acid (hetero)arylamide derivatives and analogs, are tyrosine kinase KDR and FLT inhibitors and angiogenesis inhibitors, useful e.g. for treating tumors, psoriasis or restenosis

Publications (1)

Publication Number Publication Date
ECSP055631A true ECSP055631A (en) 2005-04-18

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EC2005005631A ECSP055631A (en) 2002-07-31 2005-02-24 ANTRANILAMIDOPIRIMIDINAS THAT INHIBIT VEGFR-2 AND VEGFR-3

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EP (1) EP1594841A1 (en)
JP (2) JP4777648B2 (en)
KR (1) KR20050026535A (en)
CN (1) CN1671666A (en)
AU (1) AU2003281855A1 (en)
BR (1) BR0313122A (en)
CA (1) CA2493026C (en)
CO (1) CO5720998A2 (en)
CR (1) CR7673A (en)
EC (1) ECSP055631A (en)
HR (1) HRP20050187A2 (en)
IL (1) IL166377A0 (en)
MX (1) MXPA04012948A (en)
NO (1) NO20051035L (en)
PL (1) PL374610A1 (en)
RS (1) RS20050084A (en)
RU (1) RU2005105683A (en)
WO (1) WO2004013102A1 (en)

Families Citing this family (37)

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Publication number Priority date Publication date Assignee Title
US7615565B2 (en) 2002-07-31 2009-11-10 Bayer Schering Pharma Aktiengesellschaft VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridines
GB0229022D0 (en) * 2002-12-12 2003-01-15 Novartis Ag Organic Compounds
EP2397462A3 (en) 2003-01-14 2012-04-04 Cytokinetics, Inc. Compounds, compositions and methods of treatment for heart failure
DE102004009238A1 (en) * 2004-02-26 2005-09-08 Merck Patent Gmbh New aryl amide compounds are kinase inhibitors useful for the treatment and/or prophylaxis of e.g. tumors, psoriasis, rheumatoid arthritis, contact dermatitis, inflammations, endometriosis, scar and benign prostatic hyperplasia
EP2862859B1 (en) 2004-06-17 2018-07-25 Cytokinetics, Inc. Compounds, compositions and methods
US7176222B2 (en) 2004-07-27 2007-02-13 Cytokinetics, Inc. Syntheses of ureas
EP1655295A1 (en) * 2004-11-03 2006-05-10 Schering Aktiengesellschaft Anthranilamide pyridinureas as VEGF receptor kinase inhibitors
EP1655297A1 (en) * 2004-11-03 2006-05-10 Schering Aktiengesellschaft Nicotinamide pyridinureas as vascular endothelial growth factor (VEGF) receptor kinase inhibitors
US7906533B2 (en) 2004-11-03 2011-03-15 Bayer Schering Pharma Ag Nicotinamide pyridinureas as vascular endothelial growth factor (VEGF) receptor kinase inhibitors
EP1657241A1 (en) * 2004-11-03 2006-05-17 Schering Aktiengesellschaft Novel anthranilamide pyridinureas as VEGF receptor kinase inhibitors
KR20060071812A (en) * 2004-12-22 2006-06-27 주식회사 엘지생명과학 Novel 3-(2-amino-6-pyridinyl)-4-hydroxyphenyl amine derivatives
JPWO2006070878A1 (en) * 2004-12-28 2008-06-12 アステラス製薬株式会社 Carboxylic acid derivative or salt thereof
US7538223B2 (en) 2005-08-04 2009-05-26 Cytokinetics, Inc. Compounds, compositions and methods
US7825120B2 (en) 2005-12-15 2010-11-02 Cytokinetics, Inc. Certain substituted ((piperazin-1-ylmethyl)benzyl)ureas
AR058347A1 (en) 2005-12-15 2008-01-30 Cytokinetics Inc ENTITIES CHEMIES COMPOSITIONS AND METHODS
US7718657B2 (en) 2005-12-16 2010-05-18 Cytokinetics, Inc. Certain indanyl urea modulators of the cardiac sarcomere
US7989455B2 (en) 2005-12-19 2011-08-02 Cytokinetics, Inc. Compounds, compositions and methods
EP1975166A1 (en) * 2007-03-30 2008-10-01 Bayer Schering Pharma AG Synthesis of anthranilamides
EP2008658A1 (en) * 2007-06-28 2008-12-31 Bayer Schering Pharma Aktiengesellschaft Synergistic combination of anthranilamide pyridinureas and benzamide derivatives
US9187426B2 (en) 2008-06-27 2015-11-17 Novartis Ag Organic compounds
US8350026B2 (en) * 2008-08-27 2013-01-08 Leo Pharma A/S VEGF-2 receptor and protein tyrosine kinase inhibitors and pharmaceutical use thereof
CN101676267B (en) 2008-09-16 2012-12-26 江苏恒瑞医药股份有限公司 N-4-(1-cyan cyclopentyl) phenyl-2-(4-picolyl) amidogen-3-pyridinecarboxamide salt
US8886334B2 (en) 2008-10-07 2014-11-11 Mc10, Inc. Systems, methods, and devices using stretchable or flexible electronics for medical applications
EP2349440B1 (en) 2008-10-07 2019-08-21 Mc10, Inc. Catheter balloon having stretchable integrated circuitry and sensor array
US8097926B2 (en) 2008-10-07 2012-01-17 Mc10, Inc. Systems, methods, and devices having stretchable integrated circuitry for sensing and delivering therapy
US8372726B2 (en) 2008-10-07 2013-02-12 Mc10, Inc. Methods and applications of non-planar imaging arrays
US8389862B2 (en) 2008-10-07 2013-03-05 Mc10, Inc. Extremely stretchable electronics
WO2011041727A1 (en) 2009-10-01 2011-04-07 Mc10, Inc. Protective cases with integrated electronics
JP2014523633A (en) 2011-05-27 2014-09-11 エムシー１０ インコーポレイテッド Electronic, optical and / or mechanical devices and systems and methods of manufacturing these devices and systems
US9171794B2 (en) 2012-10-09 2015-10-27 Mc10, Inc. Embedding thin chips in polymer
CN104086484B (en) * 2014-07-08 2016-05-25 上海宣创生物科技有限公司 Mesylate solvate crystal of nicotinamide derivative and its preparation method and application
CN105541708A (en) * 2014-10-28 2016-05-04 华东理工常熟研究院有限公司 New crystal form of apatinib sulfate
CN105622499A (en) * 2014-10-28 2016-06-01 华东理工常熟研究院有限公司 New crystal of apatinib sulfate
CN105622498A (en) * 2014-10-28 2016-06-01 华东理工常熟研究院有限公司 New crystal of apatinib sulfate
JO3705B1 (en) 2014-11-26 2021-01-31 Bayer Pharma AG Novel substituted indazoles, processes for preparation thereof, pharmaceutical preparations comprising them and use thereof for production of medicaments
WO2017207481A1 (en) * 2016-06-01 2017-12-07 Bayer Animal Health Gmbh Substituted indazoles ueful for treatment and prevention of allergic and/or inflammatory diseases in animals
CN106496107A (en) * 2016-08-31 2017-03-15 浙江永宁药业股份有限公司 VEGFR inhibitor 2 and preparation method thereof

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9824579D0 (en) * 1998-11-10 1999-01-06 Novartis Ag Organic compounds
GB0001930D0 (en) * 2000-01-27 2000-03-22 Novartis Ag Organic compounds
DE10023486C1 (en) * 2000-05-09 2002-03-14 Schering Ag Ortho substituted anthranilic acid amides and their use as medicines
DE10023485A1 (en) * 2000-05-09 2001-11-22 Schering Ag New 2-((heteroaralkyl)-amino)-benzamide derivatives, are vascular endothelial growth factor (VEGF) receptors, KDR kinase and FLT kinase inhibitors useful for e.g. treating tumors, psoriasis, arthritis or renal diseases
US20020147198A1 (en) * 2001-01-12 2002-10-10 Guoqing Chen Substituted arylamine derivatives and methods of use
US6878714B2 (en) * 2001-01-12 2005-04-12 Amgen Inc. Substituted alkylamine derivatives and methods of use
US6995162B2 (en) * 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
US20030134836A1 (en) * 2001-01-12 2003-07-17 Amgen Inc. Substituted arylamine derivatives and methods of use
US20040254185A1 (en) * 2001-05-08 2004-12-16 Alexander Ernst Selective anthranilamide pyridine amides as inhibitors of vegfr-2 and vegfr-3
AU2002350217A1 (en) * 2001-12-04 2003-06-17 Bristol-Myers Squibb Company Glycinamides as factor xa inhibitors

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