GB1211258A - Amines - Google Patents

Amines

Info

Publication number
GB1211258A
GB1211258A GB5295/68A GB529568A GB1211258A GB 1211258 A GB1211258 A GB 1211258A GB 5295/68 A GB5295/68 A GB 5295/68A GB 529568 A GB529568 A GB 529568A GB 1211258 A GB1211258 A GB 1211258A
Authority
GB
United Kingdom
Prior art keywords
halogen
optionally substituted
formula
alkyl
compound
Prior art date
Legal status (The legal status 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 status listed.)
Expired
Application number
GB5295/68A
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
CH Boehringer Sohn AG and Co KG
Boehringer Ingelheim GmbH
Original Assignee
CH Boehringer Sohn AG and Co KG
Boehringer Ingelheim 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 CH Boehringer Sohn AG and Co KG, Boehringer Ingelheim GmbH filed Critical CH Boehringer Sohn AG and Co KG
Publication of GB1211258A publication Critical patent/GB1211258A/en
Expired legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D337/00—Heterocyclic compounds containing rings of more than six members having one sulfur atom as the only ring hetero atom
    • C07D337/02—Seven-membered rings
    • C07D337/06—Seven-membered rings condensed with carbocyclic rings or ring systems
    • C07D337/08—Seven-membered rings condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D313/00—Heterocyclic compounds containing rings of more than six members having one oxygen atom as the only ring hetero atom
    • C07D313/02—Seven-membered rings
    • C07D313/06—Seven-membered rings condensed with carbocyclic rings or ring systems
    • C07D313/08—Seven-membered rings condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • 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

Abstract

1,211,258. Amines. BOEHRINGER INGELHEIM G.m.b.H. 1 Feb., 1968 [1 Feb., 1967; 2 June, 1967; 19 July, 1967], No. 5295/68. Heading C2C. Racemic and optically active cis, trans and cis-trans compounds of the general Formula (I) (R 1,2 = H, halogen, Me, OMe, CF 3 , CN, OH or R 1+2 together with the adjacent ring = naphthalene, indane, tetrahydronaphthalene, benz-1,3-dioxole or benzodioxane ring system; R 3 = H, Me, Et, Ph optionally substituted by at least one methyl group; R 4 = H, Me, Et, Ph optionally substituted by halogen, Me, OMe; R 5 = H, C 1-3 alkyl, PhCH 2 optionally substituted by halogen and/or C 1-3 alkyl; R 6 = H, C 1-3 alkyl or -NR 5 R 6 = pyrrolidino, piperidino, morpholino or 5-6 membered ring containing a further nitrogen atom optionally N-substituted by Me, Et, Ph optionally substituted by at least one halogen and/or Me and/or Et; X = O, S, CH 2 provided that when X = O and R 1,2 = 7- and 8-Me, at least one of R 3-6 is not H and when X = S at least one of R 1-6 is not H) and their acid addition salts are prepared by (a) reacting a compound of the Formula (II) with a reducing agent whereby the ketonic oxyten atom is converted to an OH group with simultaneous introduction of R 3 , (b) alkylating or benzylating a compound of the Formula (I) in which R 5,6 = H, or (c) hydrolysing or hydrogenolysing a compound of the Formula (IV) (R<SP>1</SP> = protecting group), optionally followed in each case by salt formation and/or separation of the racemates of the cis and trans isomers and in the latter case by resolution. The above compounds are antidepressants and anticonvulsants, and may be administered in the form of pharmaceutical preparations containing them in association with a carrier.
GB5295/68A 1967-02-01 1968-02-01 Amines Expired GB1211258A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DEB0090994 1967-02-01

Publications (1)

Publication Number Publication Date
GB1211258A true GB1211258A (en) 1970-11-04

Family

ID=6985591

Family Applications (1)

Application Number Title Priority Date Filing Date
GB5295/68A Expired GB1211258A (en) 1967-02-01 1968-02-01 Amines

Country Status (4)

Country Link
CH (1) CH513111A (en)
DE (1) DE1593760A1 (en)
FR (2) FR1603343A (en)
GB (1) GB1211258A (en)

Cited By (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0116373A1 (en) * 1983-02-15 1984-08-22 Merrell Dow Pharmaceuticals Inc. 2H-(1) benzoxepino(5,4-b)-1,4-oxazine derivatives
EP0116372A1 (en) * 1983-02-15 1984-08-22 Merrell Dow Pharmaceuticals Inc. 2H-(1) benzoxepino (5,4-b)-1,4 oxazine derivatives
FR2600332A1 (en) * 1986-06-19 1987-12-24 Squibb & Sons Inc P-AMINOPHENOLS AND DERIVATIVES WITH THERAPEUTIC ACTION
US4845094A (en) * 1986-06-20 1989-07-04 Suntory Limited 2-phenylbenzoxepin derivative
WO1997033882A1 (en) * 1996-03-11 1997-09-18 G.D. Searle And Co. Novel benzothiepines having activity as inhibitors of ileal bile acid transport and taurocholate uptake
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
AU723123B2 (en) * 1996-03-11 2000-08-17 G.D. Searle & Co. Novel 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
EP0781278B1 (en) * 1994-09-13 2001-03-14 Monsanto Company Novel 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
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
US6458851B1 (en) 1998-12-23 2002-10-01 G. D. Searle, Llc Combinations of ileal bile acid transport inhibitors and cholesteryl ester transfer protein inhibitors for cardiovascular indications
US6458850B1 (en) 1998-12-23 2002-10-01 G.D. Searle, Llc Combinations of cholesteryl ester transfer protein inhibitors and fibric acid derivatives for cardiovascular indications
US6462091B1 (en) 1998-12-23 2002-10-08 G.D. Searle & Co. Combinations of cholesteryl ester transfer protein inhibitors and HMG coA reductase inhibitors for cardiovascular indications
US6489366B1 (en) 1998-12-23 2002-12-03 G. D. Searle, Llc Combinations of cholesteryl ester transfer protein inhibitors and nicotinic acid derivatives for cardiovascular indications
US6562860B1 (en) 1998-12-23 2003-05-13 G. D. Searle & Co. Combinations of ileal bile acid transport inhibitors and bile acid sequestering agents 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
US6586434B2 (en) 2000-03-10 2003-07-01 G.D. Searle, Llc Method for the preparation of tetrahydrobenzothiepines
US6638969B1 (en) 1998-12-23 2003-10-28 G.D. Searle, Llc Combinations of ileal bile acid transport inhibitors and fibric acid derivatives for cardiovascular indications
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
US6642269B2 (en) 1998-06-10 2003-11-04 Aventis Pharma Deutschland Gmbh Benzothiepine 1,1-dioxide derivatives, a process for their preparation, pharmaceuticals comprising these compounds, and their use
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
EP1440972A1 (en) * 1996-03-11 2004-07-28 G.D. Searle &amp; Co. Novel benzothiepines having pharmaceutical activity.
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
US10512657B2 (en) 2011-10-28 2019-12-24 Lumena Pharmaceutials Llc Bile acid recycling inhibitors for treatment of pediatric cholestatic liver diseases

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2353519A1 (en) * 1975-12-08 1977-12-30 Roussel Uclaf Amino dihydro or tetrahydro benzocycloheptenes - useful as antidepressants
DE2931398A1 (en) 1979-08-02 1981-02-26 Kali Chemie Pharma Gmbh NEW 1-BENZOXEPIN-5 (2H) -ON DERIVATIVES AND THEIR SALTS, METHODS AND INTERMEDIATE PRODUCTS FOR THE PRODUCTION THEREOF AND MEDICINAL PRODUCTS CONTAINING THESE COMPOUNDS
DE2931399A1 (en) * 1979-08-02 1981-02-26 Kali Chemie Pharma Gmbh NEW 3-AMINO-1-BENZOXEPINE DERIVATIVES AND THEIR SALTS, METHOD FOR THE PRODUCTION THEREOF AND MEDICINAL PRODUCTS CONTAINING THESE COMPOUNDS
DE3440296A1 (en) * 1984-11-05 1986-05-15 Kali-Chemie Pharma Gmbh, 3000 Hannover 3-AMINO-2,3-DIHYDRO-1-BENZOXEPINE COMPOUNDS AND METHOD FOR THE PRODUCTION THEREOF, AND MEDICINAL PRODUCTS CONTAINING THESE COMPOUNDS
FR2698873B1 (en) * 1992-12-07 1995-02-24 Lipha Benzocycloheptenes, benzoxepines and benzothiepins activators of potassium channels, preparation process, pharmaceutical composition containing them.

Cited By (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0116372A1 (en) * 1983-02-15 1984-08-22 Merrell Dow Pharmaceuticals Inc. 2H-(1) benzoxepino (5,4-b)-1,4 oxazine derivatives
EP0116373A1 (en) * 1983-02-15 1984-08-22 Merrell Dow Pharmaceuticals Inc. 2H-(1) benzoxepino(5,4-b)-1,4-oxazine derivatives
FR2600332A1 (en) * 1986-06-19 1987-12-24 Squibb & Sons Inc P-AMINOPHENOLS AND DERIVATIVES WITH THERAPEUTIC ACTION
US4845094A (en) * 1986-06-20 1989-07-04 Suntory Limited 2-phenylbenzoxepin derivative
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
US6943189B2 (en) 1994-09-13 2005-09-13 G.D. Searle & Co. Combination therapy employing ileal bile acid transport inhibiting benzothiepines 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
EP0781278B1 (en) * 1994-09-13 2001-03-14 Monsanto Company Novel 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
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
US6420417B1 (en) 1994-09-13 2002-07-16 G. D. Searle & Co. Combination therapy employing ileal bile acid transport inhibiting benzothiepines and HMG Co-A reductase inhibitors
EP1440972A1 (en) * 1996-03-11 2004-07-28 G.D. Searle &amp; Co. Novel benzothiepines having pharmaceutical activity.
CN1110494C (en) * 1996-03-11 2003-06-04 G·D·瑟尔公司 Novel benzothiepines having activity as inhibitors of ileal bile acid transport and taurocholate uptake
WO1997033882A1 (en) * 1996-03-11 1997-09-18 G.D. Searle And Co. Novel benzothiepines having activity as inhibitors of ileal bile acid transport and taurocholate uptake
AU723123B2 (en) * 1996-03-11 2000-08-17 G.D. Searle & Co. Novel benzothiepines having activity as inhibitors of ileal bile acid transport and taurocholate uptake
US7019023B2 (en) 1998-06-10 2006-03-28 Aventis Pharma Deutschland Gmbh Benzothiepine 1, 1-dioxide derivatives, a process for their preparation, pharmaceuticals comprising these compounds, and their use
US6642269B2 (en) 1998-06-10 2003-11-04 Aventis Pharma Deutschland Gmbh Benzothiepine 1,1-dioxide derivatives, a process for their preparation, pharmaceuticals comprising these compounds, and their use
US6458851B1 (en) 1998-12-23 2002-10-01 G. D. Searle, Llc Combinations of ileal bile acid transport inhibitors and cholesteryl ester transfer protein inhibitors for cardiovascular indications
US6462091B1 (en) 1998-12-23 2002-10-08 G.D. Searle & Co. Combinations of cholesteryl ester transfer protein inhibitors and HMG coA reductase inhibitors for cardiovascular indications
US6638969B1 (en) 1998-12-23 2003-10-28 G.D. Searle, Llc Combinations of ileal bile acid transport inhibitors and fibric acid derivatives for cardiovascular indications
US6458850B1 (en) 1998-12-23 2002-10-01 G.D. Searle, Llc Combinations of cholesteryl ester transfer protein inhibitors and fibric acid derivatives 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
US6489366B1 (en) 1998-12-23 2002-12-03 G. D. Searle, Llc Combinations of cholesteryl ester transfer protein inhibitors and nicotinic acid derivatives for cardiovascular indications
US6562860B1 (en) 1998-12-23 2003-05-13 G. D. Searle & Co. Combinations of ileal bile acid transport inhibitors and bile acid sequestering agents for cardiovascular indications
US6890958B2 (en) 1998-12-23 2005-05-10 G.D. Searle, Llc Combinations of cholesteryl ester transfer protein inhibitors and nicotinic acid derivatives for cardiovascular indications
US6586434B2 (en) 2000-03-10 2003-07-01 G.D. Searle, Llc Method for the preparation of tetrahydrobenzothiepines
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
US10512657B2 (en) 2011-10-28 2019-12-24 Lumena Pharmaceutials Llc Bile acid recycling inhibitors for treatment of pediatric cholestatic liver diseases
US11229661B2 (en) 2011-10-28 2022-01-25 Shire Human Genetic Therapies, Inc. Bile acid recycling inhibitors for treatment of pediatric cholestatic liver diseases
US11376251B2 (en) 2011-10-28 2022-07-05 Shire Human Genetic Therapies, Inc. Bile acid recycling inhibitors for treatment of pediatric cholestatic liver diseases

Also Published As

Publication number Publication date
CH513111A (en) 1971-09-30
FR8052M (en) 1970-06-29
DE1593760A1 (en) 1972-06-08
FR1603343A (en) 1971-04-05

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Legal Events

Date Code Title Description
PS Patent sealed
PLNP Patent lapsed through nonpayment of renewal fees