CN100506815C - 选择性结合整联蛋白的哌啶化合物 - Google Patents

选择性结合整联蛋白的哌啶化合物 Download PDF

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Publication number
CN100506815C
CN100506815C CNB038240904A CN03824090A CN100506815C CN 100506815 C CN100506815 C CN 100506815C CN B038240904 A CNB038240904 A CN B038240904A CN 03824090 A CN03824090 A CN 03824090A CN 100506815 C CN100506815 C CN 100506815C
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alkyl
base
compound
structural formula
tetrahydrochysene
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Expired - Fee Related
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CNB038240904A
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English (en)
Chinese (zh)
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CN1688572A (zh
Inventor
B·德科尔特
W·A·金尼
B·E·玛利亚诺夫
S·高希
L·刘
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Janssen Pharmaceutica NV
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Janssen Pharmaceutica NV
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • 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
    • 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
    • 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
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • 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
    • 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
    • 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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Vascular Medicine (AREA)
  • Surgery (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Materials For Medical Uses (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CNB038240904A 2002-08-16 2003-08-15 选择性结合整联蛋白的哌啶化合物 Expired - Fee Related CN100506815C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US40423902P 2002-08-16 2002-08-16
US60/404,239 2002-08-16

Publications (2)

Publication Number Publication Date
CN1688572A CN1688572A (zh) 2005-10-26
CN100506815C true CN100506815C (zh) 2009-07-01

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CNB038240904A Expired - Fee Related CN100506815C (zh) 2002-08-16 2003-08-15 选择性结合整联蛋白的哌啶化合物

Country Status (24)

Country Link
US (1) US20040077684A1 (https=)
EP (1) EP1539739B1 (https=)
JP (1) JP4554364B2 (https=)
KR (1) KR20050031464A (https=)
CN (1) CN100506815C (https=)
AR (1) AR041010A1 (https=)
AT (1) ATE489378T1 (https=)
AU (2) AU2003259891A1 (https=)
BR (1) BR0313534A (https=)
CA (1) CA2496127C (https=)
CR (1) CR7692A (https=)
CY (1) CY1111194T1 (https=)
DE (1) DE60335118D1 (https=)
DK (1) DK1539739T3 (https=)
ES (1) ES2355139T3 (https=)
IL (1) IL166534A (https=)
MX (1) MXPA05001859A (https=)
NO (1) NO332036B1 (https=)
PL (1) PL219749B1 (https=)
PT (1) PT1539739E (https=)
RU (1) RU2333210C2 (https=)
SI (1) SI1539739T1 (https=)
UA (1) UA83467C2 (https=)
WO (1) WO2004020435A1 (https=)

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US20040224986A1 (en) * 2002-08-16 2004-11-11 Bart De Corte Piperidinyl targeting compounds that selectively bind integrins
US7351711B2 (en) 2003-07-31 2008-04-01 Janssen Pharmaceutical, N.V. Tricyclic indanyls as integrin inhibitors
AU2005229015C1 (en) * 2004-04-02 2013-01-17 The Regents Of The University Of California Methods and compositions for treating and preventing disease associated with alphaVbeta5 integrin
EP1830902A2 (en) * 2004-12-30 2007-09-12 Cinvention Ag Combination comprising an agent providing a signal, an implant material and a drug
EP1833512A1 (en) * 2005-01-06 2007-09-19 GE Healthcare AS Optical imaging
US8372399B2 (en) * 2006-08-31 2013-02-12 Cardiac Pacemakers, Inc. Bispecific antibodies and agents to enhance stem cell homing
US20080058922A1 (en) * 2006-08-31 2008-03-06 Cardiac Pacemakers, Inc. Methods and devices employing vap-1 inhibitors
US8636995B2 (en) * 2006-08-31 2014-01-28 Cardiac Pacemakers, Inc. Methods and devices to regulate stem cell homing
SI2178858T1 (sl) * 2007-08-02 2012-03-30 Recordati Ireland Ltd Nove heterociklične spojine kot mGlu antagonisti
WO2009058314A1 (en) 2007-10-30 2009-05-07 Janssen Pharmaceutica, N.V. Enantioselective process for preparing a substituted alkanoic acid
EP2730282A1 (en) * 2007-11-08 2014-05-14 The General Hospital Corporation Methods and compositions for the treatment of proteinuric diseases
EP2456460A4 (en) 2009-07-24 2013-02-20 Univ California METHOD AND COMPOSITIONS FOR TREATING AND PREVENTING DISEASES ASSOCIATED WITH AVB5 INTEGRIN
SI3050878T1 (sl) 2013-09-24 2022-01-31 Fujifilm Corporation Nova dušik-vsebujoča spojina ali njena sol ali kovinski kompleks le-te
EP3512839A4 (en) 2016-09-18 2020-03-25 H. Lee Moffitt Cancer Center And Research Institute, Inc. AGAINST INTERACTION OF YAP1 WITH YCT1 INHIBITORS
BR112019009245A2 (pt) * 2016-11-08 2019-07-16 Bristol-Myers Squibb Company azol amidas e aminas como inibidores de alfav integrina
HRP20210228T1 (hr) * 2016-11-08 2021-03-19 Bristol-Myers Squibb Company Amidi pirola kao inhibitori alfa v integrina
MA52117A (fr) * 2017-02-28 2022-04-06 Morphic Therapeutic Inc Inhibiteurs de l'intégrine (alpha-v) (bêta-6)
MX394210B (es) 2017-02-28 2025-03-04 Morphic Therapeutic Inc INHIBIDORES DE INTEGRINA AVß6.
BR112020018642A2 (pt) 2018-03-14 2020-12-29 H. Lee Moffitt Cancer Center And Research Institute, Inc. Composto da fórmula i, composição farmacêutica, método de tratamento de câncer em um sujeito em necessidade, método de eliminação de uma célula tumoral em um sujeito
WO2020047208A1 (en) 2018-08-29 2020-03-05 Morphic Therapeutic, Inc. Inhibitors of (alpha-v)(beta-6) integrin
WO2020047239A1 (en) 2018-08-29 2020-03-05 Morphic Therapeutic, Inc. INHIBITING αV β6 INTEGRIN
SI3844162T1 (sl) 2018-08-29 2025-06-30 Morphic Therapeutic, Inc. Zaviralci integrina alfa v beta6
WO2025067433A1 (zh) * 2023-09-28 2025-04-03 云合智药（苏州）生物科技有限公司 靶向整合素的化合物及其在RNAi剂中的应用

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US4289772A (en) * 1977-06-03 1981-09-15 Pfizer Inc. 1-Piperidinophthalazines as cardiac stimulants
US5340798A (en) * 1992-10-14 1994-08-23 Merck & Co., Inc. Fibrinogen receptor antagonists
US6211191B1 (en) * 1997-12-17 2001-04-03 Merck & Co., Inc. Integrin receptor antagonists

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US4289772A (en) * 1977-06-03 1981-09-15 Pfizer Inc. 1-Piperidinophthalazines as cardiac stimulants
US5340798A (en) * 1992-10-14 1994-08-23 Merck & Co., Inc. Fibrinogen receptor antagonists
US6211191B1 (en) * 1997-12-17 2001-04-03 Merck & Co., Inc. Integrin receptor antagonists

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PL375562A1 (en) 2005-11-28
EP1539739B1 (en) 2010-11-24
AR041010A1 (es) 2005-04-27
EP1539739A1 (en) 2005-06-15
KR20050031464A (ko) 2005-04-06
BR0313534A (pt) 2005-07-12
JP2005539049A (ja) 2005-12-22
CA2496127C (en) 2012-05-29
AU2010236002B2 (en) 2012-05-03
PT1539739E (pt) 2011-01-05
AU2010236002A1 (en) 2010-11-11
NO332036B1 (no) 2012-06-04
RU2333210C2 (ru) 2008-09-10
AU2003259891A1 (en) 2004-03-19
CN1688572A (zh) 2005-10-26
UA83467C2 (uk) 2008-07-25
RU2005104115A (ru) 2005-08-27
ES2355139T3 (es) 2011-03-23
WO2004020435A1 (en) 2004-03-11
IL166534A (en) 2012-05-31
IL166534A0 (en) 2006-01-15
SI1539739T1 (sl) 2011-04-29
PL219749B1 (pl) 2015-07-31
MXPA05001859A (es) 2005-06-03
CY1111194T1 (el) 2015-06-11
NO20051273L (no) 2005-05-10
ATE489378T1 (de) 2010-12-15
DK1539739T3 (da) 2011-03-07
CR7692A (es) 2009-01-14
DE60335118D1 (de) 2011-01-05
US20040077684A1 (en) 2004-04-22
JP4554364B2 (ja) 2010-09-29
CA2496127A1 (en) 2005-02-16

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