AR034692A1 - Inhibidores de la integrina alfavbeta3, un procedimiento para su preparacion, los medicamentos a base de estos compuestos, las composiciones farmaceuticas que los contienen y el uso de los mismos para preparar un medicamento destinado a combatir enfermedades que se basan en la expresion y funcion pa - Google Patents

Inhibidores de la integrina alfavbeta3, un procedimiento para su preparacion, los medicamentos a base de estos compuestos, las composiciones farmaceuticas que los contienen y el uso de los mismos para preparar un medicamento destinado a combatir enfermedades que se basan en la expresion y funcion pa

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Publication number
AR034692A1
AR034692A1 ARP000104353A ARP000104353A AR034692A1 AR 034692 A1 AR034692 A1 AR 034692A1 AR P000104353 A ARP000104353 A AR P000104353A AR P000104353 A ARP000104353 A AR P000104353A AR 034692 A1 AR034692 A1 AR 034692A1
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AR
Argentina
Prior art keywords
substituted
compounds
unsubstituted
inhibitors
ocf3
Prior art date
Application number
ARP000104353A
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English (en)
Inventor
Goodman Simon Dr
Schad Oliver Dr
Jonczyk Alfred Dr
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Merck Patent Gmbh
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Publication date
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Publication of AR034692A1 publication Critical patent/AR034692A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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
    • C07D213/72Nitrogen atoms
    • C07D213/74Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4402Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)

Abstract

Se describen inhibidores de la integrina alfavbeta3 de fórmula (1): X-Y-Z-R1-CH2-R2(R4)-CH2-CO-R5, en donde: X significa H2N-C(=NH)-, H2N-C(=NH)-NH, A-C(=NH)-NH-, Het1- ó Het1-NH-, donde los grupos amino primarios también pueden estar provistos con grupos protectores de amino convencionales; Y significa -(CH2)n, ó un compuesto de fórmula (2) donde 1, 2, 3 ó 4 grupo metileno pueden estar reemplazados por N, O y/o S; Z está ausente o significa -O-, -NH-, -NA-, -CH(OH)-, -CH(OA)-, -CHA-, -CA2- ó -S-; R1 significa fenileno no sustituido o sustituido 1, 2 ó 3 veces con F, Cl, Br, A, OA, OCF3 ó CN; R2 significa N, CH ó CA; R3 significa H, F, Cl, Br, A, OA ó OCF3; R4 significa fenilo, naftilo o Het2 no sustituido o sustituido una o varias veces con A, arilo ó CF3; R5 significa OH, OA, NH2, NHA ó NA2; Het1 significa un heterociclo de 1 ó 2 núcleos con 1 a 4 átomos de N, que puede estar no sustituido o sustituido 1-2 veces con NH2; Het2 significa un heterociclo aromático de 1 ó 2 núcleos con 1 a 3 átomos de N, O y/o S, que puede estar no sustituido o sustituido 1 ó 2 veces con F, Cl, Br, A, OA, SA, OCF3, -CO-A, CN, COOA, CONH2, CONHA, CONA2 ó NO2; Arilo significa fenilo no sustituido o sustituido 1, 2 ó 3 veces con Hal, A u OA; A significa alquilo C1-12; n significa de 1 a 12; m y o independientemente entre sí significan de 1 a 12; así como sus sales y solvatos fisiológicamente inofensivos. Estos compuestos inhiben especialmente las interacciones de los receptores alfav con los ligando, siendo especialmente efectivos como ligandos de la integrina alfavbeta3. También se describe un procedimiento para preparar los compuestos de fórmula (1), los medicamentos a base de estos compuestos, las composiciones farmacéuticas que los contienen y el uso de los mismos para la preparación de un medicamento para combatir las enfermedades que se basan en la expresión y la función patológica de receptores de integrina alfavbeta3, en particular, para combatir la trombosis, el infarto de miocardio, las enfermedades cardíacas coronarias, la arteriosclerosis, los tumores, la osteoporosis, la fibrosis, las inflamaciones, las infecciones, lapsoriasis, así como para influir sobre los procesos de curación de heridas.
ARP000104353A 1999-08-24 2000-08-23 Inhibidores de la integrina alfavbeta3, un procedimiento para su preparacion, los medicamentos a base de estos compuestos, las composiciones farmaceuticas que los contienen y el uso de los mismos para preparar un medicamento destinado a combatir enfermedades que se basan en la expresion y funcion pa AR034692A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE19939980A DE19939980A1 (de) 1999-08-24 1999-08-24 Inhibitoren des Integrins alphavbeta¶3¶

Publications (1)

Publication Number Publication Date
AR034692A1 true AR034692A1 (es) 2004-03-17

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ID=7919342

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ARP000104353A AR034692A1 (es) 1999-08-24 2000-08-23 Inhibidores de la integrina alfavbeta3, un procedimiento para su preparacion, los medicamentos a base de estos compuestos, las composiciones farmaceuticas que los contienen y el uso de los mismos para preparar un medicamento destinado a combatir enfermedades que se basan en la expresion y funcion pa

Country Status (19)

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US (1) US6645991B1 (es)
EP (1) EP1206455A1 (es)
JP (1) JP2003507457A (es)
KR (1) KR20020086849A (es)
CN (1) CN1370146A (es)
AR (1) AR034692A1 (es)
AU (1) AU6992500A (es)
BR (1) BR0013502A (es)
CA (1) CA2382561A1 (es)
CZ (1) CZ2002525A3 (es)
DE (1) DE19939980A1 (es)
HK (1) HK1049667A1 (es)
HU (1) HUP0203212A3 (es)
MX (1) MXPA02001862A (es)
NO (1) NO20020885L (es)
PL (1) PL352987A1 (es)
SK (1) SK2272002A3 (es)
WO (1) WO2001014337A1 (es)
ZA (1) ZA200202284B (es)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0008696D0 (en) 2000-04-07 2000-05-31 Merck Sharp & Dohme Therapeutic agents
US6900232B2 (en) 2000-06-15 2005-05-31 Pharmacia Corporation Cycloalkyl alkanoic acids as integrin receptor antagonists
US6531494B1 (en) 2001-08-29 2003-03-11 Pharmacia Corporation Gem-substituted αvβ3 antagonists
DE10063173A1 (de) * 2000-12-18 2002-06-20 Merck Patent Gmbh Harnstoff- und Urethanderivate
AU783516B2 (en) 2001-04-30 2005-11-03 Warner-Lambert Company Methods, kits and compositions for using pyrrole derivatives
WO2003034995A2 (en) * 2001-10-22 2003-05-01 The Scripps Research Institute Integrin targeting compounds
MXPA05013637A (es) * 2003-08-13 2006-02-24 Chiron Corp Inhibidores gsk-3 y usos de los mismos.
WO2005117954A2 (en) 2004-06-04 2005-12-15 The Scripps Research Institute Compositions and methods for treatment of neovascular diseases
WO2006111925A2 (en) * 2005-04-18 2006-10-26 Sloan-Kettering Institute For Cancer Research Inhibition of tumorigenesis by inhibition of a6b4 integrin

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5234936A (en) * 1991-10-24 1993-08-10 American Home Products Corporation Pyrimidocycloalkanes as a ii antagonists
US5654322A (en) * 1992-08-11 1997-08-05 Wakunaga Seiyaku Kabushiki Kaisha Biphenylmethane derivatives and pharmaceuticals containing the same
EP0628559B1 (en) * 1993-06-10 2002-04-03 Beiersdorf-Lilly GmbH Pyrimidine compounds and their use as pharmaceuticals
CN1209063A (zh) 1995-12-29 1999-02-24 史密丝克莱恩比彻姆公司 玻连蛋白受体拮抗剂
JP2000506538A (ja) * 1996-03-29 2000-05-30 ジー.ディー.サール アンド カンパニー メタ―置換フェニレン誘導体
WO1997036882A1 (en) 1996-04-03 1997-10-09 Takeda Chemical Industries, Ltd. Oxazole derivatives, their production and use
EA200000921A1 (ru) 1998-03-10 2001-04-23 Смитклайн Бичам Корпорейшн Антагонисты рецептора витронектина
IL145401A0 (en) 1999-03-24 2002-06-30 Anormed Inc Chemokine receptor binding heterocyclic compounds

Also Published As

Publication number Publication date
ZA200202284B (en) 2003-08-27
WO2001014337A1 (de) 2001-03-01
HK1049667A1 (zh) 2003-05-23
EP1206455A1 (de) 2002-05-22
AU6992500A (en) 2001-03-19
HUP0203212A2 (hu) 2003-02-28
NO20020885D0 (no) 2002-02-22
CA2382561A1 (en) 2001-03-01
CZ2002525A3 (cs) 2002-05-15
SK2272002A3 (en) 2002-06-04
DE19939980A1 (de) 2001-03-01
KR20020086849A (ko) 2002-11-20
PL352987A1 (en) 2003-09-22
US6645991B1 (en) 2003-11-11
MXPA02001862A (es) 2002-10-23
CN1370146A (zh) 2002-09-18
NO20020885L (no) 2002-02-22
JP2003507457A (ja) 2003-02-25
HUP0203212A3 (en) 2005-02-28
BR0013502A (pt) 2002-05-07

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