GB1374345A

GB1374345A – 2,4,5-trisubstituted oxazoles
– Google Patents

GB1374345A – 2,4,5-trisubstituted oxazoles
– Google Patents
2,4,5-trisubstituted oxazoles

Info

Publication number
GB1374345A

GB1374345A
GB5396672A
GB5396672A
GB1374345A
GB 1374345 A
GB1374345 A
GB 1374345A
GB 5396672 A
GB5396672 A
GB 5396672A
GB 5396672 A
GB5396672 A
GB 5396672A
GB 1374345 A
GB1374345 A
GB 1374345A
Authority
GB
United Kingdom
Prior art keywords
alkyl
methyl
aryl
acid chloride
oxazolecarboxylic acid
Prior art date
1972-08-07
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
GB5396672A
Inventor
G Tarzia
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.)

Gruppo Lepetit SpA

Original Assignee
Gruppo Lepetit SpA
Lepetit SpA
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.)
1972-08-07
Filing date
1972-12-14
Publication date
1974-11-20

1972-12-14
Application filed by Gruppo Lepetit SpA, Lepetit SpA
filed
Critical
Gruppo Lepetit SpA

1974-11-20
Publication of GB1374345A
publication
Critical
patent/GB1374345A/en

Status
Expired
legal-status
Critical
Current

Links

Espacenet

Global Dossier

Discuss

Classifications

C—CHEMISTRY; METALLURGY

C07—ORGANIC CHEMISTRY

C07D—HETEROCYCLIC COMPOUNDS

C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings

C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings

C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members

C07D263/34—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms

C—CHEMISTRY; METALLURGY

C07—ORGANIC CHEMISTRY

C07D—HETEROCYCLIC COMPOUNDS

C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings

C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings

C07D263/04—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members

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

A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole

A61K31/42—Oxazoles

A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione

Abstract

1374345 Oxazole derivatives GRUPPO LEPETIT SpA 14 Dec 1972 [7 Aug 1972] 53966/72 Heading C2C Novel oxazole derivatives of the formula wherein A is cyclohexyl, thienyl or phenyl optionally substituted by one or more halogen atoms, or C 1-6 alkyl, halo-C 1-6 alkyl, C 1-6 alkoxy, NO 2 , CN, NH 2 , carbamoyl, sulphamoyl or carboxy radicals, and one of the radicals R 1 and R 2 is C 1-6 alkyl and the other is CON(R 3 )R 4 , wherein R 3 is H, C 1-6 alkyl, C 2-6 alkenyl, cycloalkyl, aryl, aryl-C 1-6 alkyl, hydroxy-C 1-6 alkyl, acyloxy-C 1-6 alkyl, OH, NH 2 , C 1-6 alkylideneamino, cycloalkylideneamino, or aralkylideneamino, and R 2 is H, C 1-6 alkyl, C 2-6 alkenyl, cycloalkyl, aryl, aryl-C 1-6 alkyl, hydroxy- C 1-6 alkyl or acyloxy-C 1-6 alkyl, or R 3 and R 4 , together with the N atom to which they are attached form a 5 to 7 membered saturated heterocyclic ring optionally containing further N, O or S atoms, are prepared by reacting the appropriate C 1-6 alkyl 4-(or 5-)-oxazolecarboxylates or 4- (or 5-)-oxazolecarboxylic acid halides with amines of the formula Alternatively compound in which R 3 is C 1-6 alkylideneamino, cycloalkylideneamino or aralkylideneamino may be obtained by reacting compound in which R 3 is NH 2 with the corresponding aldehydes or ketones, and those in which R 3 and/or R 4 is acyloxy-C 1-6 alkyl by acylating the corresponding hydroxy compounds. Ethyl 2 – phenyl – 4 – methyl – 5 – oxasolecarboxylate, 5 – methyl – 2 – phenyl – 4 – oxazolecarboxylic acid chloride, ethyl 5 – methyl – 2 – (2- thienyl) – 4 – oxazolecarboxylate, ethyl 5 – methyl- 2 – (4 – fluorophenyl) 4 – oxazolecarboxylate, 2- (4 – hclorophenyl) – 5 – methyl – 4- oxazolecarboxylic acid chloride, 5 – methyl – 2 – (p – tolyl) – 4- oxazolecarboxylic acid chloride, and 2-cyclohexyl 5 – methyl – 4 – oxazolecarboxylic acid chloride are obtained by known methods. Pharmaceutical compositions, having antiinflammatory and analgesic activities, contain the above novel compounds together with pharmaceutically acceptable carriers.

GB5396672A
1972-08-07
1972-12-14
2,4,5-trisubstituted oxazoles

Expired

GB1374345A
(en)

Applications Claiming Priority (1)

Application Number
Priority Date
Filing Date
Title

IT2795872

1972-08-07

Publications (1)

Publication Number
Publication Date

GB1374345A
true

GB1374345A
(en)

1974-11-20

Family
ID=11222675
Family Applications (1)

Application Number
Title
Priority Date
Filing Date

GB5396672A
Expired

GB1374345A
(en)

1972-08-07
1972-12-14
2,4,5-trisubstituted oxazoles

Country Status (23)

Country
Link

JP
(1)

JPS5030619B2
(en)

KR
(1)

KR780000069B1
(en)

AR
(1)

AR200007A1
(en)

AT
(1)

AT322551B
(en)

AU
(1)

AU477231B2
(en)

BE
(1)

BE794096A
(en)

CH
(1)

CH544105A
(en)

CS
(1)

CS177127B2
(en)

DD
(1)

DD106387A5
(en)

DE
(1)

DE2301030A1
(en)

ES
(1)

ES417638A1
(en)

FR
(1)

FR2195430B1
(en)

GB
(1)

GB1374345A
(en)

HU
(1)

HU164781B
(en)

IE
(1)

IE36941B1
(en)

IL
(1)

IL40904A
(en)

LU
(1)

LU66643A1
(en)

NL
(1)

NL149797B
(en)

NO
(1)

NO137550C
(en)

RO
(1)

RO63442A
(en)

SE
(1)

SE376236B
(en)

SU
(1)

SU511003A3
(en)

ZA
(1)

ZA728259B
(en)

Cited By (4)

* Cited by examiner, † Cited by third party

Publication number
Priority date
Publication date
Assignee
Title

US8378095B2
(en)

2007-05-10
2013-02-19
Saruem Limited
Oxazole tyrosine kinase inhibitors

US9133180B2
(en)

2012-02-06
2015-09-15
Sareum Limited
Aurora and FLT3 kinases modulators

US10882829B2
(en)

2012-03-02
2021-01-05
Sareum Limited
Pharmaceutical compounds

US11154539B2
(en)

2016-10-21
2021-10-26
Sareum Limited
Pharmaceutical compounds

Families Citing this family (7)

* Cited by examiner, † Cited by third party

Publication number
Priority date
Publication date
Assignee
Title

DD112905A5
(en)

*

1971-09-02
1975-05-12
Snam Progetti

US4110256A
(en)

*

1976-06-22
1978-08-29
Nippon Soken, Inc.
Catalyst for reforming fuel and method for producing same

JPS59125900U
(en)

*

1983-02-10
1984-08-24
マルヤス機械株式会社

assembly line equipment

DE3425118A1
(en)

*

1984-07-07
1986-01-16
Boehringer Mannheim Gmbh, 6800 Mannheim

NEW REDOX INDICATORS

JPS6133499U
(en)

*

1984-07-30
1986-02-28
中西金属工業株式会社

Pallets for manufacturing electrical products

JP2829451B2
(en)

*

1990-11-30
1998-11-25
大塚製薬株式会社

Active oxygen suppressant

US8946231B2
(en)

2009-03-23
2015-02-03
Merck Sharp & Dohme Corp.
P2X3, receptor antagonists for treatment of pain

Family Cites Families (1)

* Cited by examiner, † Cited by third party

Publication number
Priority date
Publication date
Assignee
Title

GB1226548A
(en)

*

1967-06-14
1971-03-31
Wyeth John & Brother Ltd

0

BE
BE794096D
patent/BE794096A/en
unknown

1972

1972-05-29
RO
RO7200074945A
patent/RO63442A/en
unknown

1972-11-09
NO
NO4068/72A
patent/NO137550C/en
unknown

1972-11-14
SE
SE7214772A
patent/SE376236B/xx
unknown

1972-11-22
ZA
ZA728259A
patent/ZA728259B/en
unknown

1972-11-22
IL
IL40904A
patent/IL40904A/en
unknown

1972-11-27
CH
CH1723972A
patent/CH544105A/en
not_active
IP Right Cessation

1972-12-04
IE
IE1677/72A
patent/IE36941B1/en
unknown

1972-12-13
LU
LU66643A
patent/LU66643A1/xx
unknown

1972-12-14
GB
GB5396672A
patent/GB1374345A/en
not_active
Expired

1972-12-29
HU
HULE673A
patent/HU164781B/hu
unknown

1973

1973-01-02
AT
AT3673A
patent/AT322551B/en
not_active
IP Right Cessation

1973-01-10
DE
DE2301030A
patent/DE2301030A1/en
active
Pending

1973-01-10
NL
NL737300326A
patent/NL149797B/en
unknown

1973-01-18
AR
AR246173A
patent/AR200007A1/en
active

1973-01-19
FR
FR7301948A
patent/FR2195430B1/fr
not_active
Expired

1973-01-25
JP
JP48010642A
patent/JPS5030619B2/ja
not_active
Expired

1973-04-16
CS
CS2724A
patent/CS177127B2/cs
unknown

1973-06-15
AU
AU56982/73A
patent/AU477231B2/en
not_active
Expired

1973-07-20
DD
DD172403A
patent/DD106387A5/xx
unknown

1973-08-06
SU
SU1942243A
patent/SU511003A3/en
active

1973-08-07
ES
ES417638A
patent/ES417638A1/en
not_active
Expired

1973-08-07
KR
KR7301283A
patent/KR780000069B1/en
active

Cited By (7)

* Cited by examiner, † Cited by third party

Publication number
Priority date
Publication date
Assignee
Title

US8378095B2
(en)

2007-05-10
2013-02-19
Saruem Limited
Oxazole tyrosine kinase inhibitors

US8921544B2
(en)

2007-05-10
2014-12-30
Sareum Limited
Oxazole tyrosine kinase inhibitors

US9187465B2
(en)

2007-05-10
2015-11-17
Sareum Limited
Oxazole tyrosine kinase inhibitors

US9133180B2
(en)

2012-02-06
2015-09-15
Sareum Limited
Aurora and FLT3 kinases modulators

US10882829B2
(en)

2012-03-02
2021-01-05
Sareum Limited
Pharmaceutical compounds

US11673870B2
(en)

2012-03-02
2023-06-13
Sareum Limited
Pharmaceutical compounds

US11154539B2
(en)

2016-10-21
2021-10-26
Sareum Limited
Pharmaceutical compounds

Also Published As

Publication number
Publication date

NO137550C
(en)

1978-03-15

LU66643A1
(en)

1973-02-14

CH544105A
(en)

1973-11-15

SU511003A3
(en)

1976-04-15

AU5698273A
(en)

1974-12-19

JPS5030619B2
(en)

1975-10-02

IL40904A0
(en)

1973-01-30

AT322551B
(en)

1975-05-26

CS177127B2
(en)

1977-07-29

KR780000069B1
(en)

1978-03-30

DD106387A5
(en)

1974-06-12

HU164781B
(en)

1974-04-11

RO63442A
(en)

1978-07-15

NL149797B
(en)

1976-06-15

BE794096A
(en)

1973-05-16

DE2301030A1
(en)

1974-02-28

NL7300326A
(en)

1974-02-11

SE376236B
(en)

1975-05-12

JPS4945067A
(en)

1974-04-27

IL40904A
(en)

1975-12-31

FR2195430B1
(en)

1976-04-09

AU477231B2
(en)

1976-10-21

NO137550B
(en)

1977-12-05

FR2195430A1
(en)

1974-03-08

IE36941B1
(en)

1977-03-30

AR200007A1
(en)

1974-10-15

ES417638A1
(en)

1976-02-01

ZA728259B
(en)

1973-07-25

IE36941L
(en)

1974-02-07

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Legal Events

Date
Code
Title
Description

1975-04-03
PS
Patent sealed [section 19, patents act 1949]

1980-07-30
PCNP
Patent ceased through non-payment of renewal fee

Download PDF in English

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