AR035608A1 - Derivados de urea y uretano, las preparaciones farmaceuticas que los contienen, el uso de estos derivados para la preparacion de un medicamento, un procedimiento para su preparacion, y las sustancias de partida empleadas en este procedimiento - Google Patents

Derivados de urea y uretano, las preparaciones farmaceuticas que los contienen, el uso de estos derivados para la preparacion de un medicamento, un procedimiento para su preparacion, y las sustancias de partida empleadas en este procedimiento

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Publication number
AR035608A1
AR035608A1 ARP010105796A ARP010105796A AR035608A1 AR 035608 A1 AR035608 A1 AR 035608A1 AR P010105796 A ARP010105796 A AR P010105796A AR P010105796 A ARP010105796 A AR P010105796A AR 035608 A1 AR035608 A1 AR 035608A1
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AR
Argentina
Prior art keywords
nhr7
procedure
hal
cycloalkyl
preparation
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Application number
ARP010105796A
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English (en)
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Merck Patent Gmbh
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Publication date
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Publication of AR035608A1 publication Critical patent/AR035608A1/es

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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
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P35/00—Antineoplastic agents
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P41/00—Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution
    • A—HUMAN NECESSITIES
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    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00—Drugs for disorders of the cardiovascular system
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • C07D235/30—Nitrogen atoms not forming part of a nitro radical

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Cardiology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Surgery (AREA)
  • Virology (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Derivados de urea y uretano de fórmula (1) donde: X es O ó NR5, Y es -N(R5)R4, -C(=NR7)-NHR7 o -c(=NR9)-NHR7; B es H o un resto de fórmula (2); R es H, A, cicloalquilo, Ar, arilalquilo o Pol; R1 es OR o N(R)2; R2 y R3 son cada uno, independientemente entre sí, H, A, Hal, NO2, OR, N(R)2, CN, CO-R, SO3R, SO2R, NH-C(O)A o SR; R4 es H, R7, -C(=NR7)-NHR7, -C(=NR9)-NHR7, -C(=CH-NO2)-NHR7 o Het; R5 y R5' son cada uno, independientemente entre sí, H o A, R6 es Hal o NO2; R7 es H, -C(O)R8, -C(O)-Ar, R8, COOR8, COO-(CH2)o-Ar, SO2-Ar, SO2R8 o SO2-Het; R8 es A o cicloalquilo; R9 es CN o NO2; A es alquilo C1-8, donde los grupos alquilo pueden ser monosustituidos o polisustituidos por R6 y/o sus cadenas de carbono alquilo pueden ser interrumpidas por -O-; Ar es fenilo, naftilo, antrilo o bifenililo, cada uno de los cuales es insustituido o monosustituido, disustituido o trisustituido por A, OH, OA, CN, NO2 o Hal; cicloalquilo es cicloalquilo C3-15; Hal es F, Cl, Br o I; Het es un radical heterocíclico, monocíclico o bicíclico saturado, parcialmente insaturado o totalmente insaturado con entre 5 y 10 miembros en el anillo, donde pueden estar presentes 1 ó 2 átomos de N y/o 1 ó 2 átomos de S u O, y el radical heterocíclico puede ser monosustituido o disustituido por =O, A, NO2, NHCOA o NHA; Pol es una fase sólida sin ningún grupo funcional terminal; n y m son cada uno, independientemente entre sí, 1, 2, 3, 4, 5, ó 6; o es 1, 2, 3 ó 4; p es 1, 2, 3, 4 ó 5; y sus sales y solvatos aceptables para uso fisiológico. Estos compuestos actúan como inhibidores de integrina, inhibiendo especialmente las interacciones de los receptores de integrina avb1 ó avb6 con ligandos. También se describe un procedimiento para la preparación de los compuestos de fórmula (1) y las sustancias de partida para dicho procedimiento, las preparaciones farmacéuticas que contienen los compuestos de fórmula (1) y el uso de estos últimos para preparar un medicamento destinado a combatir la trombosis, el infarto cardíaco, las afecciones coronarias, la arteriosclerosis, la inflamación, los tumores, la osteoporosis, las infecciones y la restenosis post-angioplastia y los procesos patológicos mantenidos o propagados por angiogénesis.
ARP010105796A 2000-12-18 2001-12-14 Derivados de urea y uretano, las preparaciones farmaceuticas que los contienen, el uso de estos derivados para la preparacion de un medicamento, un procedimiento para su preparacion, y las sustancias de partida empleadas en este procedimiento AR035608A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE10063173A DE10063173A1 (de) 2000-12-18 2000-12-18 Harnstoff- und Urethanderivate

Publications (1)

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AR035608A1 true AR035608A1 (es) 2004-06-16

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ID=7667710

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ARP010105796A AR035608A1 (es) 2000-12-18 2001-12-14 Derivados de urea y uretano, las preparaciones farmaceuticas que los contienen, el uso de estos derivados para la preparacion de un medicamento, un procedimiento para su preparacion, y las sustancias de partida empleadas en este procedimiento

Country Status (23)

Country Link
US (1) US7135587B2 (es)
EP (1) EP1343764B1 (es)
JP (1) JP4216071B2 (es)
KR (1) KR20030063432A (es)
CN (1) CN1481364A (es)
AR (1) AR035608A1 (es)
AT (1) ATE274497T1 (es)
AU (1) AU2002217078A1 (es)
BR (1) BR0116202A (es)
CA (1) CA2431974C (es)
CZ (1) CZ20031775A3 (es)
DE (2) DE10063173A1 (es)
DK (1) DK1343764T3 (es)
ES (1) ES2227063T3 (es)
HU (1) HUP0302753A3 (es)
MX (1) MXPA03005431A (es)
NO (1) NO20032754L (es)
PL (1) PL361745A1 (es)
PT (1) PT1343764E (es)
RU (1) RU2003121015A (es)
SK (1) SK8182003A3 (es)
WO (1) WO2002050039A1 (es)
ZA (1) ZA200305550B (es)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10204789A1 (de) * 2002-02-06 2003-08-14 Merck Patent Gmbh Inhibitoren des Integrins alpha¶v¶beta6
EP2287199B1 (en) 2002-03-13 2017-08-02 Biogen MA Inc. Anti-alpha V beta 6 antibodies
PL1667668T3 (pl) * 2003-10-01 2008-10-31 Merck Patent Gmbh Antagoniści integryny alfavbeta3 oraz alfavbeta6 jako czynniki przeciwzwłóknieniowe
CN104072614B (zh) 2005-07-08 2017-04-26 生物基因Ma公司 抗-αvβ6 抗体及其用途
SG173364A1 (en) 2006-07-10 2011-08-29 Biogen Idec Inc Compositions and methods for inhibiting growth of smad4-deficient cancers
AU2007354317A1 (en) * 2006-10-19 2008-12-04 Biogen Idec Ma Inc. Treatment and prevention of chronic asthma using antagonists of integrin alphaVbeta6
AT509266B1 (de) * 2009-12-28 2014-07-15 Tech Universität Wien Substituierte pyridine und pyrimidine
CN102353728B (zh) * 2011-06-29 2013-03-27 中国食品发酵工业研究院 一种黄酒生产过程质量控制快速检测方法
WO2014144466A1 (en) 2013-03-15 2014-09-18 Biogen Idec Ma Inc. Anti-alpha v beta 6 antibodies and uses thereof
US10035860B2 (en) 2013-03-15 2018-07-31 Biogen Ma Inc. Anti-alpha V beta 6 antibodies and uses thereof
WO2017068090A1 (en) 2015-10-23 2017-04-27 Vifor (International) Ag Novel ferroportin inhibitors
JOP20180036A1 (ar) 2017-04-18 2019-01-30 Vifor Int Ag أملاح لمثبطات فروبورتين جديدة

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6306840B1 (en) 1995-01-23 2001-10-23 Biogen, Inc. Cell adhesion inhibitors
KR20010087125A (ko) * 1998-04-16 2001-09-15 데이비드 비. 맥윌리암스 인테그린 수용체에 대한 인테그린의 결합을 억제하는 화합물
GB9909409D0 (en) * 1999-04-24 1999-06-23 Zeneca Ltd Chemical compounds
DE19939980A1 (de) * 1999-08-24 2001-03-01 Merck Patent Gmbh Inhibitoren des Integrins alphavbeta¶3¶

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Publication number Publication date
PT1343764E (pt) 2005-01-31
CA2431974C (en) 2010-08-17
ES2227063T3 (es) 2005-04-01
JP2004516282A (ja) 2004-06-03
KR20030063432A (ko) 2003-07-28
RU2003121015A (ru) 2005-02-10
MXPA03005431A (es) 2003-09-10
DE60105192T2 (de) 2005-09-08
EP1343764A1 (en) 2003-09-17
US20040063644A1 (en) 2004-04-01
DK1343764T3 (da) 2004-12-06
DE10063173A1 (de) 2002-06-20
HUP0302753A3 (en) 2005-03-29
HUP0302753A2 (hu) 2003-12-29
NO20032754D0 (no) 2003-06-17
NO20032754L (no) 2003-06-17
ATE274497T1 (de) 2004-09-15
JP4216071B2 (ja) 2009-01-28
CN1481364A (zh) 2004-03-10
US7135587B2 (en) 2006-11-14
EP1343764B1 (en) 2004-08-25
DE60105192D1 (de) 2004-09-30
CZ20031775A3 (cs) 2003-09-17
BR0116202A (pt) 2003-12-23
PL361745A1 (en) 2004-10-04
ZA200305550B (en) 2004-10-18
AU2002217078A1 (en) 2002-07-01
WO2002050039A1 (en) 2002-06-27
SK8182003A3 (en) 2003-10-07
CA2431974A1 (en) 2002-06-27

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