ATE177742T1 - Benzocycloheptine, benzoxepine und benzothiepine - Google Patents

Benzocycloheptine, benzoxepine und benzothiepine

Info

Publication number
ATE177742T1
ATE177742T1 AT94902708T AT94902708T ATE177742T1 AT E177742 T1 ATE177742 T1 AT E177742T1 AT 94902708 T AT94902708 T AT 94902708T AT 94902708 T AT94902708 T AT 94902708T AT E177742 T1 ATE177742 T1 AT E177742T1
Authority
AT
Austria
Prior art keywords
pct
group
sec
bond
compounds
Prior art date
Application number
AT94902708T
Other languages
English (en)
Inventor
Jean-Jacques Berthelon
Michel Brunet
Marc Noblet
Philippe Durbin
Daniel Guerrier
Charly
Trong Luong
Original Assignee
Merck Patent 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 Merck Patent Gmbh filed Critical Merck Patent Gmbh
Application granted granted Critical
Publication of ATE177742T1 publication Critical patent/ATE177742T1/de

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Classifications

    • 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
    • C07D213/24—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 substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
    • C07D213/30—Oxygen atoms
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P9/08—Vasodilators for multiple indications
    • 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
    • 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
    • C07D213/24—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 substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/57—Nitriles
    • 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
    • C07D213/89—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 with hetero atoms directly attached to the ring nitrogen atom
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04—Ortho-condensed systems
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Neurology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Vascular Medicine (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Biomedical Technology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Epoxy Resins (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
AT94902708T 1992-12-07 1993-12-07 Benzocycloheptine, benzoxepine und benzothiepine ATE177742T1 (de)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
FR9214720A FR2698873B1 (fr) 1992-12-07 1992-12-07 Benzocycloheptènes, benzoxépines et benzothiépines activateurs des canaux potassiques, procédé de préparation, composition pharmaceutique les contenant.

Publications (1)

Publication Number Publication Date
ATE177742T1 true ATE177742T1 (de) 1999-04-15

Family

ID=9436308

Family Applications (1)

Application Number Title Priority Date Filing Date
AT94902708T ATE177742T1 (de) 1992-12-07 1993-12-07 Benzocycloheptine, benzoxepine und benzothiepine

Country Status (29)

Country Link
US (2) US5602152A (de)
EP (1) EP0626954B1 (de)
JP (1) JPH07503977A (de)
KR (1) KR100236810B1 (de)
CN (1) CN1050127C (de)
AT (1) ATE177742T1 (de)
AU (1) AU680856B2 (de)
CA (1) CA2129642A1 (de)
CZ (1) CZ184894A3 (de)
DE (1) DE69324001T2 (de)
DK (1) DK0626954T3 (de)
ES (1) ES2132373T3 (de)
FI (1) FI943646A (de)
FR (1) FR2698873B1 (de)
GR (1) GR3030514T3 (de)
HU (1) HUT67852A (de)
IL (1) IL107891A0 (de)
LT (1) LT3167B (de)
LV (1) LV10451B (de)
NO (1) NO942914L (de)
NZ (1) NZ258896A (de)
PL (1) PL174246B1 (de)
RO (1) RO113040B1 (de)
RU (1) RU2127268C1 (de)
SI (1) SI9300632A (de)
SK (1) SK93994A3 (de)
TW (1) TW276255B (de)
WO (1) WO1994013658A2 (de)
ZA (1) ZA939127B (de)

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US6642268B2 (en) 1994-09-13 2003-11-04 G.D. Searle & Co. Combination therapy employing ileal bile acid transport inhibiting benzothipines and HMG Co-A reductase inhibitors
US5994391A (en) * 1994-09-13 1999-11-30 G.D. Searle And Company Benzothiepines having activity as inhibitors of ileal bile acid transport and taurocholate uptake
US6107494A (en) * 1994-09-13 2000-08-22 G.D. Searle And Company Substituted 5-aryl-benzothiepines having activity as inhibitors of ileal bile acid transport and taurocholate uptake
US6262277B1 (en) 1994-09-13 2001-07-17 G.D. Searle And Company Intermediates and processes for the preparation of benzothiepines having activity as inhibitors of ileal bile acid transport and taurocholate uptake
DK0781278T3 (da) * 1994-09-13 2001-04-17 Monsanto Co Nye benzothiepiner, som har aktivitet som inhibitorer af ileal galdsyretransport og taurocholatoptagelse
US6268392B1 (en) 1994-09-13 2001-07-31 G. D. Searle & Co. Combination therapy employing ileal bile acid transport inhibiting benzothiepines and HMG Co-A reductase inhibitors
US5952326A (en) * 1997-12-10 1999-09-14 Pfizer Inc. Tetralin and chroman derivatives useful in the treatment of asthma, arthritis and related diseases
US6221897B1 (en) 1998-06-10 2001-04-24 Aventis Pharma Deutschland Gmbh Benzothiepine 1,1-dioxide derivatives, a process for their preparation, pharmaceuticals comprising these compounds, and their use
WO2000038721A1 (en) * 1998-12-23 2000-07-06 G.D. Searle Llc Combinations of cholesteryl ester transfer protein inhibitors and nicotinic acid derivatives for cardiovascular indications
ES2200587T3 (es) 1998-12-23 2004-03-01 G.D. Searle Llc Combinaciones de inhibidors del transporte de acidos biliares del ileon e inhibidores de la proteina de transferencia de colesteril ester para indicaciones cardiovasculares.
EP1140187B1 (de) * 1998-12-23 2003-09-03 G.D. Searle LLC. Kombinationen einem ibat inhibitor und einem mtp inhibitor für kardiovaskuläre indikationen
AU2157400A (en) 1998-12-23 2000-07-31 G.D. Searle & Co. Combinations of cholesteryl ester transfer protein inhibitors and hmg coa reductase inhibitors for cardiovascular indications
US6569905B1 (en) 1998-12-23 2003-05-27 G.D. Searle, Llc Combinations of cholesteryl ester transfer protein inhibitors and bile acid sequestering agents for cardiovascular indications
JP2002533414A (ja) 1998-12-23 2002-10-08 ジー．ディー．サール エルエルシー 心臓血管に適用するための回腸胆汁酸輸送阻害剤および胆汁酸隔離剤の組み合わせ
DE69907960T2 (de) * 1998-12-23 2004-02-26 G.D. Searle Llc, Chicago Kombinationen von ileumgallensäuretransports inhibitoren und fibronsäure derivaten für kardiovaskuläre indikationen
EA009466B1 (ru) 1998-12-23 2007-12-28 Джи.Ди. Сирл Ллс Ингибитор белка, переносящего эфир холестерила
EP1286984A2 (de) 2000-03-10 2003-03-05 Pharmacia Corporation Verfahren zur herstellung von tetrahydrobenzothiepinen
WO2001068096A2 (en) * 2000-03-10 2001-09-20 Pharmacia Corporation Combination therapy for the prophylaxis and treatment of hyperlipidemic conditions and disorders
US20040077625A1 (en) * 2001-07-25 2004-04-22 Tremont Samuel J. Novel 1,4-benzothiazepine and 1,5-benzothiazepine compounds as inhibitors of apical sodium codependent bile acid transport abd taurocholate uptake
US6740663B2 (en) * 2001-11-02 2004-05-25 G.D. Searle, Llc Mono- and di-fluorinated benzothiepine compounds as inhibitors of apical sodium co-dependent bile acid transport (ASBT) and taurocholate uptake
US6852753B2 (en) 2002-01-17 2005-02-08 Pharmacia Corporation Alkyl/aryl hydroxy or keto thiepine compounds as inhibitors of apical sodium co-dependent bile acid transport (ASBT) and taurocholate uptake
CN104023727B (zh) 2011-10-28 2017-04-05 鲁美纳医药公司 用于治疗小儿胆汁淤积性肝病的胆汁酸再循环抑制剂
US20150057452A1 (en) 2012-04-04 2015-02-26 Catylix, Inc. Selective androgen receptor modulators

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DE1593760A1 (de) * 1967-02-01 1972-06-08 Boehringer Sohn Ingelheim Verfahren zur Herstellung neuer Benz-epinderivate
US3444176A (en) * 1967-04-28 1969-05-13 Mcneilab Inc Certain 4-diloweralkylamino-lower alkyl - 5 - pyridyl (or phenyl)-2,3-dihydro - 1 - benzothiepins and derivatives thereof
AU8402275A (en) * 1974-08-26 1977-02-17 Takeda Chemical Industries Ltd Benzocycloheptene derivatives
US4066663A (en) * 1976-07-01 1978-01-03 Syntex (U.S.A.) Inc. 6,11-Dihydrodibenzo-[b. e.]-thiepin-11-one-3-aldehyde and 3-acetal derivatives
DE3274350D1 (en) 1981-09-25 1987-01-08 Beecham Group Plc Pharmaceutically active benzopyran compounds
US4416687A (en) * 1982-02-01 1983-11-22 Monsanto Company 3,5-Bis (trifluoromethyl)phenoxy carboxylic acids and derivatives thereof
PH22343A (en) * 1983-02-15 1988-08-12 Merrell Dow Pharma 2h-(1) benzoxepino (5,4-b) 1,4-oxazine derivatives
AU597671B2 (en) * 1986-06-20 1990-06-07 Suntory Limited 2-Phenylbenzoxepin derivative
DE3726261A1 (de) 1986-12-23 1988-07-07 Merck Patent Gmbh Chromanderivate
US4971982A (en) 1987-07-06 1990-11-20 Hoffmann-La Roche Inc. Benzopyran derivatives
GB8812765D0 (en) * 1988-05-28 1988-06-29 Beecham Group Plc Novel compounds
DE3831697A1 (de) * 1988-09-17 1990-03-22 Hoechst Ag 2,3,4,5-tetrahydro-1-benzoxepine, verfahren zu ihrer herstellung, ihre verwendung sowie pharmazeutische praeparate auf basis dieser verbindungen
DE3922392A1 (de) * 1989-07-07 1991-01-17 Merck Patent Gmbh Chromanderivate
JP3018386B2 (ja) * 1990-01-24 2000-03-13 吉富製薬株式会社 光学活性なベンゾチエピノピリダジン化合物の製造法

Also Published As

Publication number Publication date
CN1050127C (zh) 2000-03-08
NO942914D0 (de) 1994-08-05
PL304719A1 (en) 1995-01-09
KR100236810B1 (ko) 2000-02-01
RO113040B1 (ro) 1998-03-30
HU9402302D0 (en) 1994-10-28
LT3167B (en) 1995-02-27
FI943646A0 (fi) 1994-08-05
JPH07503977A (ja) 1995-04-27
AU680856B2 (en) 1997-08-14
DE69324001T2 (de) 1999-10-07
NZ258896A (en) 1996-03-26
RU2127268C1 (ru) 1999-03-10
TW276255B (de) 1996-05-21
DK0626954T3 (da) 1999-10-11
SI9300632A (en) 1994-09-30
CN1097752A (zh) 1995-01-25
US5602152A (en) 1997-02-11
US5652252A (en) 1997-07-29
CA2129642A1 (en) 1994-06-23
NO942914L (no) 1994-08-05
FR2698873A1 (fr) 1994-06-10
LTIP1525A (en) 1994-07-15
RU94040853A (ru) 1996-07-10
ZA939127B (en) 1994-08-05
IL107891A0 (en) 1994-04-12
DE69324001D1 (de) 1999-04-22
PL174246B1 (pl) 1998-07-31
LV10451B (en) 1995-12-20
HUT67852A (en) 1995-05-29
EP0626954A1 (de) 1994-12-07
FI943646A (fi) 1994-08-05
GR3030514T3 (en) 1999-10-29
LV10451A (lv) 1995-02-20
CZ184894A3 (en) 1995-02-15
EP0626954B1 (de) 1999-03-17
WO1994013658A3 (en) 1994-08-04
KR950700278A (ko) 1995-01-16
FR2698873B1 (fr) 1995-02-24
AU5697594A (en) 1994-07-04
ES2132373T3 (es) 1999-08-16
WO1994013658A2 (en) 1994-06-23
SK93994A3 (en) 1995-04-12

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Legal Events

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UEP Publication of translation of european patent specification
REN Ceased due to non-payment of the annual fee