GB1078852A

GB1078852A – Alkanolamine derivatives
– Google Patents

GB1078852A – Alkanolamine derivatives
– Google Patents
Alkanolamine derivatives

Info

Publication number
GB1078852A

GB1078852A
GB39774/64A
GB3977464A
GB1078852A
GB 1078852 A
GB1078852 A
GB 1078852A
GB 39774/64 A
GB39774/64 A
GB 39774/64A
GB 3977464 A
GB3977464 A
GB 3977464A
GB 1078852 A
GB1078852 A
GB 1078852A
Authority
GB
United Kingdom
Prior art keywords
radical
compounds
general formula
addition salts
starting materials
Prior art date
1964-09-30
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
GB39774/64A
Inventor
Ralph Howe
Leslie Harold Smith
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.)

Imperial Chemical Industries Ltd

Original Assignee
Imperial Chemical Industries Ltd
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.)
1964-09-30
Filing date
1964-09-30
Publication date
1967-08-09

1964-09-30
Application filed by Imperial Chemical Industries Ltd
filed
Critical
Imperial Chemical Industries Ltd

1964-09-30
Priority to GB39774/64A
priority
Critical
patent/GB1078852A/en

1965-09-17
Priority to US488252A
priority
patent/US3408387A/en

1965-09-24
Priority to AT873365A
priority
patent/AT261582B/en

1965-09-24
Priority to AT239367A
priority
patent/AT261586B/en

1965-09-27
Priority to CH1329165A
priority
patent/CH466317A/en

1965-09-27
Priority to CH967068A
priority
patent/CH504407A/en

1965-09-29
Priority to BR173584/65A
priority
patent/BR6573584D0/en

1965-09-29
Priority to SE12618/65A
priority
patent/SE313061B/xx

1965-09-30
Priority to BE670364A
priority
patent/BE670364A/xx

1965-09-30
Priority to FR33270A
priority
patent/FR1458635A/en

1965-09-30
Priority to JP40059684A
priority
patent/JPS5031136B1/ja

1965-09-30
Priority to DE1493887A
priority
patent/DE1493887C3/en

1965-09-30
Priority to ES0318019A
priority
patent/ES318019A1/en

1965-09-30
Priority to NL6512676A
priority
patent/NL6512676A/xx

1965-09-30
Priority to DK504665AA
priority
patent/DK113295B/en

1965-12-29
Priority to FR44136A
priority
patent/FR5662M/fr

1966-12-23
Priority to DK668366AA
priority
patent/DK122879B/en

1967-08-09
Publication of GB1078852A
publication
Critical
patent/GB1078852A/en

1967-09-14
Priority to JP6759060A
priority
patent/JPS514978B1/ja

1968-09-06
Priority to FR165406A
priority
patent/FR96559E/en

1968-09-06
Priority to CH1341068A
priority
patent/CH518260A/en

1968-09-16
Priority to ES358534A
priority
patent/ES358534A2/en

1968-09-26
Priority to CH1694570A
priority
patent/CH516515A/en

1968-09-26
Priority to CH1438468A
priority
patent/CH516509A/en

1968-09-27
Priority to FR167977A
priority
patent/FR96560E/en

Status
Expired
legal-status
Critical
Current

Links

Espacenet

Global Dossier

Discuss

Classifications

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

A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline

C—CHEMISTRY; METALLURGY

C07—ORGANIC CHEMISTRY

C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS

C07C233/00—Carboxylic acid amides

C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms

C07C233/16—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms

C—CHEMISTRY; METALLURGY

C07—ORGANIC CHEMISTRY

C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS

C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups

C—CHEMISTRY; METALLURGY

C07—ORGANIC CHEMISTRY

C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS

C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups

C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings

Abstract

Novel compounds of the general formula (wherein R2 represents an alkyl radical optionally carrying one or more hydroxy, alkoxy or aryloxy substituents, an aralkyl radical optionally carrying one or more halogen or alkoxy substituents, or a cycloalkyl or alkenyl radical, R3 represents H or an alkyl radical, R4 represents an acyl radical (including sulphonyl), and the ring A may optionally be further substituted by one or more alkyl radicals, or by the radical -CH = CH-CH = CH- to complete a naphthalene ring) are prepared by reacting a compound of the general formula (wherein X represents the group or the group -CH.OH.CH2Halogen), or a mixture of such compounds in which X has both meanings, with an amine R2NH2, or, when R2 is not an a -arylalkyl radical, by hydrogenolysis of a corresponding compound containing an a -arylalkyl radical in place of the H atom attached to the side-chain N atom. The resulting alkanolamine derivatives may be converted into acid addition salts, and these may be treated with an acylating agent to esterify the hydroxy group in the 2-position of the propanol side-chain, or the free alkanolamines or their acid addition salts may be reacted with aldehydes R5.CHO to form oxazolidines of the general formula (wherein R5 represents H or an alkyl radical) or acid-addition salts thereof. Starting materials.-Compounds of the second general formula above are prepared by reacting the corresponding phenols with an epihalohydrin. The N-(a -arylalkyl)-amino starting materials for the alternative process are prepared by acylating the corresponding compounds containing a substituent R3NH- instead of R3R4N- in the ring A. Other starting materials and intermediates described are: 1 – (2 – and 4 – nitrophenoxy) – 3 – (N – benzylisopropylamino) – 2 – propanol (as hydrochlorides), and the corresponding aminophenoxy compounds. Pharmaceutical compositions, e.g. tablets, capsules, solutions, suspensions, emulsions or dispersible powders, having b -adrenergic blocking activity, comprise one or more of the free or esterified alkanolamines or the oxazolidines, or the acid addition salts thereof, in association with a pharmaceutically acceptable diluent or carrier.

GB39774/64A
1964-09-30
1964-09-30
Alkanolamine derivatives

Expired

GB1078852A
(en)

Priority Applications (24)

Application Number
Priority Date
Filing Date
Title

GB39774/64A

GB1078852A
(en)

1964-09-30
1964-09-30
Alkanolamine derivatives

US488252A

US3408387A
(en)

1964-09-30
1965-09-17
Amidoaroxyalkanolamines

AT873365A

AT261582B
(en)

1964-09-30
1965-09-24

Process for the preparation of new alkanolamine derivatives and their acid addition salts

AT239367A

AT261586B
(en)

1964-09-30
1965-09-24

Process for the preparation of new alkanolamine derivatives and their acid addition salts

CH1329165A

CH466317A
(en)

1964-09-30
1965-09-27

Process for the preparation of alkanolamine derivatives

CH967068A

CH504407A
(en)

1964-09-30
1965-09-27

Process for the preparation of alkanolamine derivatives

BR173584/65A

BR6573584D0
(en)

1964-09-30
1965-09-29

PROCESS FOR THE PREPARATION OF ALKANOLAMINE DERIVATIVES

SE12618/65A

SE313061B
(en)

1964-09-30
1965-09-29

JP40059684A

JPS5031136B1
(en)

1964-09-30
1965-09-30

DK504665AA

DK113295B
(en)

1964-09-30
1965-09-30

Process for the preparation of alkanolamine derivatives or acid addition salts thereof.

FR33270A

FR1458635A
(en)

1964-09-30
1965-09-30

Manufacturing process for new alkanolamines and their derivatives

BE670364A

BE670364A
(en)

1964-09-30
1965-09-30

DE1493887A

DE1493887C3
(en)

1964-09-30
1965-09-30

Alkanolamine derivatives, processes for their preparation and pharmaceuticals containing them

ES0318019A

ES318019A1
(en)

1964-09-30
1965-09-30
Amidoaroxyalkanolamines

NL6512676A

NL6512676A
(en)

1964-09-30
1965-09-30

FR44136A

FR5662M
(en)

1964-09-30
1965-12-29

DK668366AA

DK122879B
(en)

1964-09-30
1966-12-23

Analogous process for the preparation of alkanolamine derivatives or acid addition salts thereof.

JP6759060A

JPS514978B1
(en)

1964-09-30
1967-09-14

CH1341068A

CH518260A
(en)

1964-09-30
1968-09-06
Alkanolamine derivs beta-adrenergic blocking agents

FR165406A

FR96559E
(en)

1964-09-30
1968-09-06

Process for the manufacture of new alkanolamines and their derivatives.

ES358534A

ES358534A2
(en)

1964-09-30
1968-09-16
Procedure for the manufacture of alcanolamine derivatives (Machine-translation by Google Translate, not legally binding)

CH1694570A

CH516515A
(en)

1964-09-30
1968-09-26
Alkanolamine derivatives b-adrenergic blocking agents

CH1438468A

CH516509A
(en)

1964-09-30
1968-09-26
Alkanolamine derivatives b-adrenergic blocking agents

FR167977A

FR96560E
(en)

1964-09-30
1968-09-27

Process for the manufacture of new alkanolamines and their derivatives.

Applications Claiming Priority (1)

Application Number
Priority Date
Filing Date
Title

GB39774/64A

GB1078852A
(en)

1964-09-30
1964-09-30
Alkanolamine derivatives

Publications (1)

Publication Number
Publication Date

GB1078852A
true

GB1078852A
(en)

1967-08-09

Family
ID=10411417
Family Applications (1)

Application Number
Title
Priority Date
Filing Date

GB39774/64A
Expired

GB1078852A
(en)

1964-09-30
1964-09-30
Alkanolamine derivatives

Country Status (13)

Country
Link

US
(1)

US3408387A
(en)

JP
(2)

JPS5031136B1
(en)

AT
(2)

AT261582B
(en)

BE
(1)

BE670364A
(en)

BR
(1)

BR6573584D0
(en)

CH
(1)

CH504407A
(en)

DE
(1)

DE1493887C3
(en)

DK
(2)

DK113295B
(en)

ES
(2)

ES318019A1
(en)

FR
(1)

FR5662M
(en)

GB
(1)

GB1078852A
(en)

NL
(1)

NL6512676A
(en)

SE
(1)

SE313061B
(en)

Cited By (2)

* Cited by examiner, † Cited by third party

Publication number
Priority date
Publication date
Assignee
Title

JPS4911836A
(en)

*

1972-05-15
1974-02-01

US3934032A
(en)

*

1969-02-21
1976-01-20
Imperial Chemical Industries Limited
Alkanolamine derivatives for treating hypertension

Families Citing this family (30)

* Cited by examiner, † Cited by third party

Publication number
Priority date
Publication date
Assignee
Title

US3857952A
(en)

*

1967-12-22
1974-12-31
May & Baker Ltd
Certain benzene derivatives useful in treating cardiac disorders

ZA6808345B
(en)

*

1967-12-22

May & Baker Ltd
Benzene derivatives

GB1269775A
(en)

*

1968-07-18
1972-04-06
Ici Ltd
Alkanolamine derivatives

DE1957706C3
(en)

*

1968-11-18
1978-06-29
Pfizer Corp., Colon (Panama)

Nuclear-substituted 3-phenoxy-1-phenoxyalkylamino-propan-2-ols and drugs based on them

US3873618A
(en)

*

1969-07-18
1975-03-25
Ici Ltd
1-{8 4-(4-Acetamidophenyl)phenoxy{9 -3-isopropyl-2-propanol

US4038313A
(en)

*

1970-01-08
1977-07-26
Ciba-Geigy Corporation
Cycloalkylureido phenoxy propanolamines

US4120978A
(en)

*

1970-01-08
1978-10-17
Ciba-Geigy Corporation
Pharmaceutical composition for inhibiting and blocking cardioselective beta-receptors

US3864398A
(en)

*

1972-05-01
1975-02-04
Teikoku Hormone Mfg Co Ltd
Process for the preparation of acylamino alkanol derivatives

FR2330383A1
(en)

*

1975-11-06
1977-06-03
Synthelabo

NEW PHENOL SUBSTITUTE ETHERS, THEIR SALTS, THEIR PREPARATION AND THE MEDICINAL PRODUCTS CONTAINING THEM

US4064125A
(en)

*

1976-10-29
1977-12-20
E. R. Squibb And Sons, Inc.
Substituted amides having antiinflammatory activity

US4177280A
(en)

*

1978-07-03
1979-12-04
Syntex (U.S.A.) Inc.
Bicyclo[3.1.0]hexyl-substituted carbonylaminophenoxy cardiovascular agents

DE2948056A1
(en)

*

1979-11-29
1981-06-04
Boehringer Mannheim Gmbh, 6800 Mannheim

NEW AMINOPROPANOL DERIVATIVES, METHOD FOR THE PRODUCTION THEREOF AND MEDICINAL PRODUCTS CONTAINING THESE COMPOUNDS

US4342783A
(en)

*

1980-06-30
1982-08-03
Synthelabo
Anti-glaucoma agent

DE3640829A1
(en)

*

1986-11-28
1988-06-09
Boehringer Ingelheim Kg

NEW 1-ARYLOXY-3-AMINO-2-PROPANOLS, THEIR PRODUCTION AND USE

MXPA05001958A
(en)

2002-08-19
2005-04-28
Pfizer Prod Inc
Combination therapy for hyperproliferative diseases.

US20060063803A1
(en)

*

2004-09-23
2006-03-23
Pfizer Inc
4-Amino substituted-2-substituted-1,2,3,4-tetrahydroquinoline compounds

GT200600381A
(en)

2005-08-25
2007-03-28

ORGANIC COMPOUNDS

US7741317B2
(en)

2005-10-21
2010-06-22
Bristol-Myers Squibb Company
LXR modulators

US7888376B2
(en)

2005-11-23
2011-02-15
Bristol-Myers Squibb Company
Heterocyclic CETP inhibitors

JP5498168B2
(en)

2006-12-01
2014-05-21
ブリストル−マイヤーズ スクイブ カンパニー

N-((3-Benzyl) -2,2- (bis-phenyl) -propan-1-amine derivatives as CETP inhibitors for the treatment of atherosclerosis and cardiovascular disease

US20100120694A1
(en)

2008-06-04
2010-05-13
Synergy Pharmaceuticals, Inc.
Agonists of Guanylate Cyclase Useful for the Treatment of Gastrointestinal Disorders, Inflammation, Cancer and Other Disorders

CA3089569A1
(en)

2007-06-04
2008-12-11
Synergy Pharmaceuticals Inc.
Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders

US8969514B2
(en)

2007-06-04
2015-03-03
Synergy Pharmaceuticals, Inc.
Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases

AU2009270833B2
(en)

2008-07-16
2015-02-19
Bausch Health Ireland Limited
Agonists of guanylate cyclase useful for the treatment of gastrointestinal, inflammation, cancer and other disorders

US9616097B2
(en)

2010-09-15
2017-04-11
Synergy Pharmaceuticals, Inc.
Formulations of guanylate cyclase C agonists and methods of use

EP2968439A2
(en)

2013-03-15
2016-01-20
Synergy Pharmaceuticals Inc.
Compositions useful for the treatment of gastrointestinal disorders

WO2014151206A1
(en)

2013-03-15
2014-09-25
Synergy Pharmaceuticals Inc.
Agonists of guanylate cyclase and their uses

SG11201507496UA
(en)

2013-04-17
2015-11-27
Pfizer
N-piperidin-3-ylbenzamide derivatives for treating cardiovascular diseases

JP6606491B2
(en)

2013-06-05
2019-11-13
シナジー ファーマシューティカルズ インコーポレイテッド

Ultra high purity agonist of guanylate cyclase C, method for producing and using the same

WO2016055901A1
(en)

2014-10-08
2016-04-14
Pfizer Inc.
Substituted amide compounds

Family Cites Families (1)

* Cited by examiner, † Cited by third party

Publication number
Priority date
Publication date
Assignee
Title

GB922600A
(en)

*

1960-05-06
1963-04-03
Crookes Lab Ltd
Ortho-tertiary-butyl phenolethers

1964

1964-09-30
GB
GB39774/64A
patent/GB1078852A/en
not_active
Expired

1965

1965-09-17
US
US488252A
patent/US3408387A/en
not_active
Expired – Lifetime

1965-09-24
AT
AT873365A
patent/AT261582B/en
active

1965-09-24
AT
AT239367A
patent/AT261586B/en
active

1965-09-27
CH
CH967068A
patent/CH504407A/en
not_active
IP Right Cessation

1965-09-29
BR
BR173584/65A
patent/BR6573584D0/en
unknown

1965-09-29
SE
SE12618/65A
patent/SE313061B/xx
unknown

1965-09-30
NL
NL6512676A
patent/NL6512676A/xx
unknown

1965-09-30
BE
BE670364A
patent/BE670364A/xx
unknown

1965-09-30
DE
DE1493887A
patent/DE1493887C3/en
not_active
Expired

1965-09-30
DK
DK504665AA
patent/DK113295B/en
unknown

1965-09-30
ES
ES0318019A
patent/ES318019A1/en
not_active
Expired

1965-09-30
JP
JP40059684A
patent/JPS5031136B1/ja
active
Pending

1965-12-29
FR
FR44136A
patent/FR5662M/fr
not_active
Expired

1966

1966-12-23
DK
DK668366AA
patent/DK122879B/en
unknown

1967

1967-09-14
JP
JP6759060A
patent/JPS514978B1/ja
active
Pending

1968

1968-09-16
ES
ES358534A
patent/ES358534A2/en
not_active
Expired

Cited By (3)

* Cited by examiner, † Cited by third party

Publication number
Priority date
Publication date
Assignee
Title

US3934032A
(en)

*

1969-02-21
1976-01-20
Imperial Chemical Industries Limited
Alkanolamine derivatives for treating hypertension

JPS4911836A
(en)

*

1972-05-15
1974-02-01

JPS5323826B2
(en)

*

1972-05-15
1978-07-17

Also Published As

Publication number
Publication date

DE1493887C3
(en)

1978-06-15

CH504407A
(en)

1971-03-15

AT261582B
(en)

1968-05-10

NL6512676A
(en)

1966-03-31

ES358534A2
(en)

1970-07-01

JPS5031136B1
(en)

1975-10-07

DK113295B
(en)

1969-03-10

DK122879B
(en)

1972-04-24

DE1493887A1
(en)

1972-06-15

BR6573584D0
(en)

1973-08-02

JPS514978B1
(en)

1976-02-16

DE1493887B2
(en)

1977-08-25

FR5662M
(en)

1968-01-02

AT261586B
(en)

1968-05-10

SE313061B
(en)

1969-08-04

BE670364A
(en)

1966-03-30

US3408387A
(en)

1968-10-29

ES318019A1
(en)

1966-07-01

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