CN104010636B - 三环化合物、包含它们的组合物及其用途 - Google Patents

三环化合物、包含它们的组合物及其用途 Download PDF

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Publication number
CN104010636B
CN104010636B CN201280060159.1A CN201280060159A CN104010636B CN 104010636 B CN104010636 B CN 104010636B CN 201280060159 A CN201280060159 A CN 201280060159A CN 104010636 B CN104010636 B CN 104010636B
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branched
straight
fat
adipose tissue
compound
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Chinese (zh)
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CN104010636A (zh
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什姆埃尔·本-萨松
阿里·达冈
莎伦·佩莱斯
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Yissum Research Development Co of Hebrew University of Jerusalem
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Yissum Research Development Co of Hebrew University of Jerusalem
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/80—[b, c]- or [b, d]-condensed
    • C07D209/82—Carbazoles; Hydrogenated carbazoles
    • C07D209/86—Carbazoles; Hydrogenated carbazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the ring system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/80—[b, c]- or [b, d]-condensed
    • C07D209/82—Carbazoles; Hydrogenated carbazoles
    • C07D209/88—Carbazoles; Hydrogenated carbazoles 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 carbon atoms of the ring system
    • 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
    • A61K31/13—Amines
    • A61K31/14—Quaternary ammonium compounds, e.g. edrophonium, choline
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Reproductive Health (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Medicinal Preparation (AREA)
  • Indole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN201280060159.1A 2011-11-15 2012-11-15 三环化合物、包含它们的组合物及其用途 Active CN104010636B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201161559964P 2011-11-15 2011-11-15
US61/559,964 2011-11-15
US201261603508P 2012-02-27 2012-02-27
US61/603,508 2012-02-27
PCT/IL2012/050461 WO2013072915A1 (en) 2011-11-15 2012-11-15 Tricyclic compounds, compositions comprising them and uses thereof

Publications (2)

Publication Number Publication Date
CN104010636A CN104010636A (zh) 2014-08-27
CN104010636B true CN104010636B (zh) 2017-04-12

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Country Status (25)

Country Link
US (1) US9447040B2 (OSRAM)
EP (1) EP2802320B1 (OSRAM)
JP (1) JP6087367B2 (OSRAM)
KR (1) KR101986272B1 (OSRAM)
CN (1) CN104010636B (OSRAM)
AU (1) AU2012338362B2 (OSRAM)
BR (1) BR112014011641B1 (OSRAM)
CA (1) CA2855759C (OSRAM)
CL (1) CL2014001278A1 (OSRAM)
CO (1) CO7020909A2 (OSRAM)
DK (1) DK2802320T3 (OSRAM)
ES (1) ES2729713T3 (OSRAM)
HR (1) HRP20190927T1 (OSRAM)
HU (1) HUE043827T2 (OSRAM)
IN (1) IN2014CN03610A (OSRAM)
MX (1) MX347570B (OSRAM)
PE (1) PE20141940A1 (OSRAM)
PH (1) PH12014501061B1 (OSRAM)
PL (1) PL2802320T3 (OSRAM)
PT (1) PT2802320T (OSRAM)
RU (1) RU2624446C9 (OSRAM)
SG (1) SG11201402258UA (OSRAM)
SI (1) SI2802320T1 (OSRAM)
WO (1) WO2013072915A1 (OSRAM)
ZA (1) ZA201404065B (OSRAM)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016020919A1 (en) 2014-08-07 2016-02-11 Raziel Therapeutics Ltd. Compositions comprising tricyclic compounds, and uses thereof
ES2924728T3 (es) 2015-06-15 2022-10-10 Raziel Therapeutics Ltd Derivados de carbazol para el tratamiento de enfermedades fibróticas, así como de síntomas y afecciones relacionados con las mismas
AU2020347539A1 (en) * 2019-09-15 2022-03-31 Raziel Therapeutics Ltd. Compositions for the treatment of solid tumors
IL295014B1 (en) * 2020-01-28 2026-05-01 Raziel Therapeutics Ltd A pharmaceutical preparation containing 5-(-6,3-dibromo-H9-carbazol-9-yl)-N,N,N-trimethylpentan-1-iminium or the pharmaceutical salt is suitable for use in the treatment of angiolipoma
US20240041827A1 (en) * 2020-09-16 2024-02-08 Raziel Therapeutics Ltd. Compositions for the treatment of fat related conditions and disorders
IL301325A (en) * 2020-09-16 2023-05-01 Raziel Therapeutics Ltd Compositions and methods for the treatment of lipid-related disorders
AU2022270984A1 (en) * 2021-05-06 2023-11-23 Raziel Therapeutics Ltd. Crystalline carbazole derivative
IL310051A (en) * 2021-07-28 2024-03-01 Raziel Therapeutics Ltd Compositions and methods for treating lipoma pain
CN115073374B (zh) * 2022-06-14 2023-10-27 五邑大学 一种α-葡萄糖苷酶抑制剂及其制备方法和应用
AU2023378681A1 (en) * 2022-11-07 2025-05-15 Raziel Therapeutics Ltd. Crystalline carbazole derivative and methods of making thereof

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2676966A (en) * 1951-04-04 1954-04-27 Searle & Co Quaternary salts of 9-carbazolealkylamines and 10-acridanalkylamines and methods forpreparing same
US2930798A (en) * 1956-08-03 1960-03-29 Clin Byla Ets 3-alkanoyl 1-tertiary-amino-alkyl indol oximes and production thereof

Family Cites Families (21)

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US2590125A (en) * 1952-03-25 Quaternary-ammonium alkyl
US2676971A (en) * 1951-04-21 1954-04-27 Searle & Co Quaternary ammonium derivatives of aminoalkylxanthenes and aminoalkylthiaxanthenes
GB832568A (en) * 1956-08-03 1960-04-13 Clin Byla Ets Heterocyclic compounds and production thereof
FR1186832A (fr) * 1956-08-03 1959-09-02 Etablissements Clin-Byla Composés hétérocycliques dérivés du pyrrol et des benzopyrrols et leur fabrication
GB866418A (en) * 1958-01-25 1961-04-26 Bayer Ag Phenoxazine derivatives
US3836587A (en) * 1969-11-17 1974-09-17 American Cyanamid Co Organo phosphonium salts
AR205331A1 (es) * 1972-07-24 1976-04-30 Hoffmann La Roche Procedimiento para la preparacion de carbazoles
FR2691459B1 (fr) * 1992-05-25 1995-06-09 Adir Nouveaux derives de la phenothiazine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent.
AU5644396A (en) 1995-05-05 1996-11-21 Novo Nordisk A/S Novel heterocyclic chemistry
US6440961B1 (en) * 1997-10-27 2002-08-27 Dr. Reddy's Research Foundation Tricyclic compounds and their use in medicine: process for their preparation and pharmaceutical compositions containing them
EP1094063A1 (en) 1999-10-18 2001-04-25 Applied Research Systems ARS Holding N.V. 9-(Piperazinylalkyl)carbazoles as Bax-modulators
GB9925880D0 (en) 1999-11-01 1999-12-29 British Tech Group Int B-Carboline derivatives
US6933313B2 (en) * 2001-03-28 2005-08-23 Eli Lilly And Company Substituted carbazoles as inhibitors of sPLA2
WO2003027084A1 (en) * 2001-09-25 2003-04-03 Dr. Reddy's Laboratories Ltd. Improved process for the preparation of optically active phenoxazine derivatives as antidiabetic agents
US7428091B2 (en) * 2004-11-15 2008-09-23 Gentex Corporation Electrochromic compounds and associated media and devices
WO2007079239A2 (en) 2005-12-30 2007-07-12 Acadia Pharmaceuticals Inc. Bicyclic nitrogen compounds as modulators of ghrelin receptor and uses thereof
US20090317372A1 (en) 2008-06-20 2009-12-24 Zoltan Kiss Small molecules for the reduction of high blood glucose level
UA107652C2 (en) * 2008-10-06 2015-02-10 Incuron Llc Carbazole compounds and therapeutic uses of the compounds
US8362277B2 (en) * 2009-01-09 2013-01-29 Board Of Regents Of The University Of Texas System Pro-neurogenic compounds
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Patent Citations (2)

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US2676966A (en) * 1951-04-04 1954-04-27 Searle & Co Quaternary salts of 9-carbazolealkylamines and 10-acridanalkylamines and methods forpreparing same
US2930798A (en) * 1956-08-03 1960-03-29 Clin Byla Ets 3-alkanoyl 1-tertiary-amino-alkyl indol oximes and production thereof

Non-Patent Citations (1)

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Title
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Also Published As

Publication number Publication date
RU2624446C9 (ru) 2018-04-04
HRP20190927T1 (hr) 2019-08-23
DK2802320T3 (da) 2019-05-27
PE20141940A1 (es) 2014-12-18
CO7020909A2 (es) 2014-08-11
US9447040B2 (en) 2016-09-20
AU2012338362B2 (en) 2017-05-18
PH12014501061B1 (en) 2018-12-12
CL2014001278A1 (es) 2014-12-26
SG11201402258UA (en) 2014-06-27
EP2802320B1 (en) 2019-02-20
JP2014533264A (ja) 2014-12-11
JP6087367B2 (ja) 2017-03-01
RU2014119711A (ru) 2015-12-27
MX2014005765A (es) 2015-09-23
KR20140099492A (ko) 2014-08-12
PL2802320T3 (pl) 2019-09-30
HUE043827T2 (hu) 2019-09-30
BR112014011641A2 (pt) 2017-05-02
IN2014CN03610A (OSRAM) 2015-10-09
EP2802320A4 (en) 2015-08-12
BR112014011641B1 (pt) 2020-10-27
EP2802320A1 (en) 2014-11-19
WO2013072915A1 (en) 2013-05-23
CA2855759A1 (en) 2013-05-23
US20140329877A1 (en) 2014-11-06
KR101986272B1 (ko) 2019-06-05
CA2855759C (en) 2020-03-10
SI2802320T1 (sl) 2019-08-30
ES2729713T3 (es) 2019-11-05
ZA201404065B (en) 2015-11-25
PH12014501061A1 (en) 2014-06-23
MX347570B (es) 2017-05-02
RU2624446C2 (ru) 2017-07-04
PT2802320T (pt) 2019-06-17
CN104010636A (zh) 2014-08-27
AU2012338362A1 (en) 2014-05-29

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