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AR016437A1 - Derivados de acilguanidina como inhibidores de resorcion osea y como antagonistas del receptor vitronectina, procedimiento para su preparacion ypreparacion farmaceutica que los comprenden - Google Patents

Derivados de acilguanidina como inhibidores de resorcion osea y como antagonistas del receptor vitronectina, procedimiento para su preparacion ypreparacion farmaceutica que los comprenden

Info

Publication number
AR016437A1
AR016437A1 ARP980106446A ARP980106446A AR016437A1 AR 016437 A1 AR016437 A1 AR 016437A1 AR P980106446 A ARP980106446 A AR P980106446A AR P980106446 A ARP980106446 A AR P980106446A AR 016437 A1 AR016437 A1 AR 016437A1
Authority
AR
Argentina
Prior art keywords
alkyl
aryl
radical
unsubstituted
substituted
Prior art date
Application number
ARP980106446A
Other languages
English (en)
Original Assignee
Hoechst Marion Roussel Deutchland Gmbh
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 Hoechst Marion Roussel Deutchland Gmbh filed Critical Hoechst Marion Roussel Deutchland Gmbh
Publication of AR016437A1 publication Critical patent/AR016437A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C279/00Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C279/20Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups containing any of the groups, X being a hetero atom, Y being any atom, e.g. acylguanidines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • A61K31/155Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41681,3-Diazoles having a nitrogen attached in position 2, e.g. clonidine
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/28Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D233/44Nitrogen atoms not forming part of a nitro radical
    • C07D233/48Nitrogen atoms not forming part of a nitro radical with acyclic hydrocarbon or substituted acyclic hydrocarbon radicals, attached to said nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/06Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D239/08Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms directly attached in position 2
    • C07D239/12Nitrogen atoms not forming part of a nitro radical
    • C07D239/16Nitrogen atoms not forming part of a nitro radical acylated on said nitrogen atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Indole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Derivados de acilguanidinas, que comprenden un compuesto de la formula (I) donde, R1 y R2 independientemente uno de otro son hidrogeno o alquilo C1-6 quees insustituido o sustituido por R3, siempre y cuando R1 y R2 no sean ambos hidrogeno al mismo tiempo, o donde los radicales R1 y R2 juntos son un radicalalquileno C2-9, bivalente saturado o insaturado, que es insustituido o es sustituido por uno o más grupos del grupo formado por halogeno, alquilo C1-6, alcoxiC1-6, arilo C6-14, arilo C6-14-alquilo C1-6, heteroarilo C5-14, heteroarilo C5-14-alquilo C1-6, cicloalquilo C3-12, cicloalquilo C3-12-alquilo C1-6 y oxo,donde un anillo saturado o insaturado de 5 a 7 miembros, que es insustituido o sustituido por R3 y que es un anillo carbocíclico oun anillo heterocíclico quecontiene uno o dos átomos de nitrogeno anulares que pueden estar fusionados a un enlace carbono-carbono en el radical alquileno C2-9; R3 es alquilo C1-8,alcoxi C1-8, arilo C5-14, arilo C5-14-alquilo C1-4, halogeno, trifluormetilo, hidroxilo, nitro o amino; R4 es hidrogeno, alquilo (C1-6)-CO-O-alquilo C1-4 oalquilo C1-6, que es insustituido o sustituido por un radical del grupo formado por hidroxilo, alcoxi C1-4, alquilo (C1-4)-S(O)2-, NR7R7 y N+R7R7R7 Q-,donde R7, R7 yR7 independientemente uno del otro, son hidrogeno, alquilo C1-6, arilo C5-14, o arilo C5-14-alquilo C1-6 y Q- es un anion fisiologicamentetolerable, o donde R4 es uno de los radicales del grupo (II), donde los enlaces, via los cuales los radicales se unen, se indican mediante guiones; R5 esalquilo C1-8, arilo C6-14-alquilo c1-6 o heteroarilo C5-14-alquilo C1-6, donde el radical arilo o el radical heteroarilo es insustituido o sustituido por uno,dos o tres radicales R3; R6 es hidrogeno, alquilo(C1-6)-O-CO-, hidroxilo, alquilo (C1-6)-O-CO-O o nitro; A es Ch2, O, S o NH; m es 1, 2 o 3; n es 0 o 1; entodas sus formas estereoisoméricas y mezclas de los mismos en todas las proporciones y sus sales fisiologicamente tolerables y sus prodrogas. Los compuestos dela formula (I) son ingredientes activos farmacéuticamente valiosos. Los mismos son antagonistas del receptor vitronectina e inhibidores de la resorcion osea
ARP980106446A 1997-12-19 1998-12-17 Derivados de acilguanidina como inhibidores de resorcion osea y como antagonistas del receptor vitronectina, procedimiento para su preparacion ypreparacion farmaceutica que los comprenden AR016437A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP97122520A EP0933367A1 (en) 1997-12-19 1997-12-19 Novel acylguanidine derivates as inhibitors of bone resorption and as vitronectin receptor antagonists

Publications (1)

Publication Number Publication Date
AR016437A1 true AR016437A1 (es) 2001-07-04

Family

ID=8227841

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP980106446A AR016437A1 (es) 1997-12-19 1998-12-17 Derivados de acilguanidina como inhibidores de resorcion osea y como antagonistas del receptor vitronectina, procedimiento para su preparacion ypreparacion farmaceutica que los comprenden

Country Status (33)

Country Link
US (1) US6492356B1 (es)
EP (2) EP0933367A1 (es)
JP (1) JP2001526271A (es)
KR (1) KR20010033281A (es)
CN (1) CN1205191C (es)
AP (1) AP2000001842A0 (es)
AR (1) AR016437A1 (es)
AT (1) ATE228112T1 (es)
AU (1) AU753109B2 (es)
BG (1) BG64754B1 (es)
BR (1) BR9814308A (es)
CA (1) CA2312712A1 (es)
CU (1) CU23032A3 (es)
DE (1) DE69809594T2 (es)
DK (1) DK1042301T3 (es)
EA (1) EA002921B1 (es)
ES (1) ES2186251T3 (es)
HR (1) HRP20000412A2 (es)
HU (1) HUP0104912A3 (es)
ID (1) ID26248A (es)
IL (1) IL136858A0 (es)
MY (1) MY122269A (es)
NO (1) NO317420B1 (es)
NZ (1) NZ504954A (es)
PL (1) PL341216A1 (es)
PT (1) PT1042301E (es)
SI (1) SI1042301T1 (es)
SK (1) SK9032000A3 (es)
TR (1) TR200001964T2 (es)
TW (1) TW446705B (es)
WO (1) WO1999032457A1 (es)
YU (1) YU39000A (es)
ZA (1) ZA9811571B (es)

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GB9805655D0 (en) 1998-03-16 1998-05-13 Celltech Therapeutics Ltd Chemical compounds
US6521626B1 (en) 1998-03-24 2003-02-18 Celltech R&D Limited Thiocarboxamide derivatives
GB9814414D0 (en) 1998-07-03 1998-09-02 Celltech Therapeutics Ltd Chemical compounds
AU747784B2 (en) * 1998-07-29 2002-05-23 Merck & Co., Inc. Integrin receptor antagonists
GB9821061D0 (en) 1998-09-28 1998-11-18 Celltech Therapeutics Ltd Chemical compounds
GB9826174D0 (en) 1998-11-30 1999-01-20 Celltech Therapeutics Ltd Chemical compounds
EP1028114A1 (en) 1999-02-13 2000-08-16 Aventis Pharma Deutschland GmbH Novel guanidine derivatives as inhibitors of cell adhesion
US6518283B1 (en) 1999-05-28 2003-02-11 Celltech R&D Limited Squaric acid derivatives
EP1065207A1 (en) 1999-07-02 2001-01-03 Aventis Pharma Deutschland GmbH Naphthyridine derivatives, processes for their preparation, their use, and pharmaceutical compositions comprising them
EP1070707A1 (en) * 1999-07-21 2001-01-24 Aventis Pharma Deutschland GmbH 1,4,5,6-tetrahydropyrimidine derivative as a vitronectin inhibitor
US6534513B1 (en) 1999-09-29 2003-03-18 Celltech R&D Limited Phenylalkanoic acid derivatives
US6849639B2 (en) 1999-12-14 2005-02-01 Amgen Inc. Integrin inhibitors and their methods of use
US6455539B2 (en) 1999-12-23 2002-09-24 Celltech R&D Limited Squaric acid derivates
JP2003531141A (ja) 2000-04-17 2003-10-21 セルテック アール アンド ディ リミテッド エナミン誘導体
FR2808798A1 (fr) * 2000-05-09 2001-11-16 Hoechst Marion Roussel Inc Nouveaux derives antagonistes du recepteur de la vitronectine
US6403608B1 (en) 2000-05-30 2002-06-11 Celltech R&D, Ltd. 3-Substituted isoquinolin-1-yl derivatives
US6545013B2 (en) 2000-05-30 2003-04-08 Celltech R&D Limited 2,7-naphthyridine derivatives
WO2002004426A1 (en) 2000-07-07 2002-01-17 Celltech R & D Limited Squaric acid derivatives containing a bicyclic heteroaromatic ring as integrin antagonists
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FR2870541B1 (fr) * 2004-05-18 2006-07-14 Proskelia Sas Derives de pyrimidines antigonistes du recepteur de la vitronectine
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Also Published As

Publication number Publication date
AU2270099A (en) 1999-07-12
JP2001526271A (ja) 2001-12-18
EP1042301A1 (en) 2000-10-11
AP2000001842A0 (en) 2000-06-30
HRP20000412A2 (en) 2000-10-31
EP1042301B1 (en) 2002-11-20
BG64754B1 (bg) 2006-02-28
DE69809594T2 (de) 2003-04-24
HUP0104912A1 (hu) 2002-07-29
DE69809594D1 (de) 2003-01-02
NO317420B1 (no) 2004-10-25
BG104544A (en) 2001-03-30
PL341216A1 (en) 2001-03-26
MY122269A (en) 2006-03-31
HK1034974A1 (en) 2001-11-09
US6492356B1 (en) 2002-12-10
ID26248A (id) 2000-12-07
EA002921B1 (ru) 2002-10-31
WO1999032457A1 (en) 1999-07-01
TW446705B (en) 2001-07-21
HUP0104912A3 (en) 2002-09-30
CU23032A3 (es) 2005-03-22
NO20003118D0 (no) 2000-06-16
KR20010033281A (ko) 2001-04-25
ATE228112T1 (de) 2002-12-15
CA2312712A1 (en) 1999-07-01
AU753109B2 (en) 2002-10-10
NO20003118L (no) 2000-08-21
CN1205191C (zh) 2005-06-08
EP0933367A1 (en) 1999-08-04
ES2186251T3 (es) 2003-05-01
IL136858A0 (en) 2001-06-14
CN1284950A (zh) 2001-02-21
SK9032000A3 (en) 2001-04-09
ZA9811571B (en) 1999-06-21
SI1042301T1 (en) 2003-04-30
PT1042301E (pt) 2003-04-30
BR9814308A (pt) 2000-10-10
NZ504954A (en) 2002-05-31
TR200001964T2 (tr) 2000-11-21
DK1042301T3 (da) 2003-03-17
YU39000A (sh) 2002-11-15
EA200000682A1 (ru) 2000-12-25

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