http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-1393161-A
Outgoing Links
Predicate | Object |
---|---|
assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_2e5edd48190cba3fa70dd3975efd9831 |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D495-04 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D495-04 |
filingDate | 1972-05-03-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationDate | 1975-05-07-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | GB-1393161-A |
titleOfInvention | Thieno 3,2-d pyrimidines |
abstract | 1393161 Derivatives of thieno-[3,2-d]pyrimidine DR KARL THOMAE GmbH 3 May 1972 [4 May 1971 26 July 1971 29 March 1972] 20584/72 Heading C2C The invention comprises compounds of formula and their acid addition salts, wherein R 1 and R 2 each represents an unsubstituted piperazino group or a piperazino group substituted in the 4- position by a benzyl or hydroxyalkyl group or by an alkyl group containing 1 to 4 carbon atoms; or a 1,4-diazacycloheptano, morpholino, thiomorpholino, thiomorpholino-1 -oxide, thiomorpholino-1,1-dioxide, hexahydro-1,4-thiazepino or hexahydro-1,4-thiazepino-1-oxide group, the carbon atoms of the afore-mentioned heterocyclic groups being unsubstituted or substituted by one or two alkyl groups containing 1 to 4 carbon atoms; or a dialkanolamino, methylmercaptoethyimethylamino or methylsulfinylethylmethylamino group; and R 3 and R 4 each represents a hydrogen or halogen atom, a phenyl or nitro group or an alkyl group with 1 to 4 carbon atoms; with the provisos that (a) if R 3 and R 4 both represent hydrogen atoms then at least one of R 1 and R 2 represents a piperazino group substituted in the 4-position by a benzyl or hydroxyalkyl group, a 1,4-diazacycloheptano, thiomorpholino, thiomorpholino-1-oxide, thiomorpholino-1,1-dioxide, hexahydro-1,4-thiazepino or hexahydro-1,4-thiazepino-l-oxide group, the carbon atoms of the afore-mentioned heterocyclic groups being unsubstituted or substituted by one or two alkyl groups containing 1 to 4 carbon atoms, or a methylmercaptoethylmethylamino or methylsulfinylethylmethylamino group; and (b) if R 3 represents a hydrogen atom or a methyl group, R 4 represents a hydrogen atom or a methyl or phenyl group, and R 2 represents a morpholino group either unsubstituted or substituted in either or both of the 3- or 5-positions by a methyl group, then R 1 does not represent a piperazino group or a 1,4-diazacycloheptano group. These compounds are prepared in examples by (a) reacting with the appropriate base (HR, or HR 2 ) a precursor having the above formula except that one of R 1 and R 2 is (e.g.) halogen, or MeS(#O) 0-2 , (b) (where one of R 1 and R 2 is piperazino) hydrolysing a corresponding (4- carboethoxypiperazino)-thienopyrimidine, or (c) (where the desired product contains an S-oxide or dioxide group) oxidizing the corresponding S- heterocyclic-containing compound. Intermediates otherwise prepared are 2-chloro- 4 - morpholino - 6 - nitrothieno - [3,2 - d]- pyrimidine, and thieno-[3,2-d]pyrimidines substituted as follows:# 7-Br-2,4-(HO) 2 ; 6- and 7-Cl-2,4-(HO) 2 ; 7-Br-2,4-C12; 2,4,6- and 2,4,7- Cl 3 ; 2,4,6,7-C1 4 ; 6- and 7-NO 2 -2,4-(HO) 2 ; 6- and 7-NO 2 -2,4-Cl 2 . Therapeutic compositions for oral, parenteral or rectal administration comprise compounds of the above formula, which have antithrombotic activity, and in particular inhibit platelet aggregation and adhesiveness, and in some cases also lower the blood pressure. |
isCitedBy | http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-7872003-B2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-8293735-B2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-8101607-B2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-8324206-B2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2011130654-A1 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2014130923-A2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-8993563-B2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-8946217-B2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-8685968-B2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-8450315-B2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-7776856-B2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-9487533-B2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-9943519-B2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-7781433-B2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-2518074-A1 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2010138589-A1 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-7888352-B2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-8153629-B2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-7750002-B2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2012088254-A1 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2009042607-A1 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-8383620-B2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2010105008-A2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-7846929-B2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-8802670-B2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-8987260-B2 |
priorityDate | 1971-05-04-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 52.