FR2321890A1 - Hypotensive amino-quinazoline derivs. - with substd. piperidine or piperazine substit. - Google Patents

Hypotensive amino-quinazoline derivs. - with substd. piperidine or piperazine substit.

Info

Publication number
FR2321890A1
FR2321890A1 FR7526228A FR7526228A FR2321890A1 FR 2321890 A1 FR2321890 A1 FR 2321890A1 FR 7526228 A FR7526228 A FR 7526228A FR 7526228 A FR7526228 A FR 7526228A FR 2321890 A1 FR2321890 A1 FR 2321890A1
Authority
FR
France
Prior art keywords
substd
piperidine
amino
piperazine
substit
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.)
Granted
Application number
FR7526228A
Other languages
French (fr)
Other versions
FR2321890B1 (en
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.)
Synthelabo SA
Original Assignee
Synthelabo SA
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 Synthelabo SA filed Critical Synthelabo SA
Priority to FR7526228A priority Critical patent/FR2321890A1/en
Publication of FR2321890A1 publication Critical patent/FR2321890A1/en
Application granted granted Critical
Publication of FR2321890B1 publication Critical patent/FR2321890B1/fr
Granted legal-status Critical Current

Links

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
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/40—Acylated substituent nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/26—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
    • C07D211/56—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
    • C07D211/56—Nitrogen atoms
    • C07D211/58—Nitrogen atoms attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/20—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
    • C07D295/205—Radicals derived from carbonic acid

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Quinazoline derivs. of formula (I) and their pharmaceutically acceptable acid addition salts are new. In (I) -N is a piperidine or piperazine nucleus substd. in posn. 3 or 4 by R; R is -(CH2)n-(R1)-COR2, -NR1R3 or -CO2-CH2R4; R1 is H or 1-3C alkyl; R2 is -OR1, phenyl or furyl; n is 0 or 1; R3 is 1-3 C alkyl or R4 is 3-6C cycloalkyl; provided that -N R contains is not 2 N atoms. (I) are hypotensives for human or veterinary use, for treatment of all forms of essential and secondary hypertension. Toxicity is low and activity is comparable with that of dihydrolazine. LD50, rat, p.o., is typically >1 g/kg c.f. 0.44 g/kg for dihydralazine. Daily doses are e.g. 10-400 mg p.o. in units of 5-50 mg or 100 mg parenterally. A typical cpd. is 1-(4-amino-5,6-dimethoxyquinazol-2- )-4-(ethoxycarbonylamino)pip- eridine.
FR7526228A 1975-08-26 1975-08-26 Hypotensive amino-quinazoline derivs. - with substd. piperidine or piperazine substit. Granted FR2321890A1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
FR7526228A FR2321890A1 (en) 1975-08-26 1975-08-26 Hypotensive amino-quinazoline derivs. - with substd. piperidine or piperazine substit.

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
FR7526228A FR2321890A1 (en) 1975-08-26 1975-08-26 Hypotensive amino-quinazoline derivs. - with substd. piperidine or piperazine substit.

Publications (2)

Publication Number Publication Date
FR2321890A1 true FR2321890A1 (en) 1977-03-25
FR2321890B1 FR2321890B1 (en) 1979-09-14

Family

ID=9159340

Family Applications (1)

Application Number Title Priority Date Filing Date
FR7526228A Granted FR2321890A1 (en) 1975-08-26 1975-08-26 Hypotensive amino-quinazoline derivs. - with substd. piperidine or piperazine substit.

Country Status (1)

Country Link
FR (1) FR2321890A1 (en)

Cited By (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2919800A1 (en) * 1978-05-18 1979-11-22 Pfizer 4-AMINO-2-PIPERIDINOQUINAZOLINE DERIVATIVES, METHOD FOR THE PRODUCTION THEREOF AND MEDICINAL PRODUCTS CONTAINING SUCH DERIVATIVES
EP0009465A1 (en) * 1978-09-20 1980-04-02 Ciba-Geigy Ag N-(1-(4-amino-2-quinazolinyl)-3 or 4-piperidyl lactames, process for their preparation and pharmaceutical compositions containing them
EP0034471A1 (en) * 1980-02-19 1981-08-26 Orion-Yhtymä Oy Piperidinoquinazolines and a process for the preparation thereof
US4309541A (en) * 1978-09-20 1982-01-05 Ciba-Geigy Corporation Piperidinyl-lactams
WO1997020820A1 (en) * 1995-12-01 1997-06-12 Novartis Ag Heteroaryl compounds
US5675006A (en) * 1992-08-31 1997-10-07 Brantford Chemicals Inc. Methods of making ureas and guanidines, including, terazosin, prazosin, doxazosin, tiodazosin, trimazosin, quinazosin, and bunazosin (exemplary of 2- substituted quinazoline compounds), and meobentine, and bethanidine and intermediates therefor
WO2002048124A2 (en) * 2000-12-15 2002-06-20 F. Hoffmann-La Roche Ag Piperazine derivatives
WO2005000305A1 (en) * 2003-06-20 2005-01-06 Eli Lilly And Company 3-aminopiperidines and 3-aminoquinuclidines as inhibitors of monoamine uptake
WO2009107571A1 (en) * 2008-02-27 2009-09-03 住友化学株式会社 Method for optical resolution of alkylpiperidin-3-yl carbamate and intermediate therefor
WO2009119700A1 (en) * 2008-03-26 2009-10-01 住友化学株式会社 Manufacturing method for a piperidine-3-ylcarbamate compound and optical resolution method therefor
JP2009256337A (en) * 2008-03-26 2009-11-05 Sumitomo Chemical Co Ltd Method for producing piperidin-3-ylcarbamate compound
CN107814792A (en) * 2016-09-14 2018-03-20 中国科学院上海药物研究所 A kind of quinazoline derivant, its composition and purposes

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3511836A (en) * 1967-12-13 1970-05-12 Pfizer & Co C 2,4,6,7-tetra substituted quinazolines

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3511836A (en) * 1967-12-13 1970-05-12 Pfizer & Co C 2,4,6,7-tetra substituted quinazolines

Cited By (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2919800A1 (en) * 1978-05-18 1979-11-22 Pfizer 4-AMINO-2-PIPERIDINOQUINAZOLINE DERIVATIVES, METHOD FOR THE PRODUCTION THEREOF AND MEDICINAL PRODUCTS CONTAINING SUCH DERIVATIVES
EP0009465A1 (en) * 1978-09-20 1980-04-02 Ciba-Geigy Ag N-(1-(4-amino-2-quinazolinyl)-3 or 4-piperidyl lactames, process for their preparation and pharmaceutical compositions containing them
US4309541A (en) * 1978-09-20 1982-01-05 Ciba-Geigy Corporation Piperidinyl-lactams
EP0034471A1 (en) * 1980-02-19 1981-08-26 Orion-Yhtymä Oy Piperidinoquinazolines and a process for the preparation thereof
US5675006A (en) * 1992-08-31 1997-10-07 Brantford Chemicals Inc. Methods of making ureas and guanidines, including, terazosin, prazosin, doxazosin, tiodazosin, trimazosin, quinazosin, and bunazosin (exemplary of 2- substituted quinazoline compounds), and meobentine, and bethanidine and intermediates therefor
US5686612A (en) * 1992-08-31 1997-11-11 Brantford Chemicals Inc. Methods of making ureas and guanidines, including terazosin, prazosin, doxazosin, tiodazosin, trimazosin, quinazosin, and bunazosin (exemplary of 2-substituted quinazoline compounds), and meobentine, and bethanidine and intermediates thereof
US6080860A (en) * 1992-08-31 2000-06-27 Brantford Chemicalss Inc. Methods of making ureas and guanidines including, terazosin, prazosin, doxazosin, tiodazosin, trimazosin, quinazosin and bunazosin (exemplary of 2-substituted quinazoline compounds), and meobentine, and bethanidine and intermediates therefor
WO1997020820A1 (en) * 1995-12-01 1997-06-12 Novartis Ag Heteroaryl compounds
US7022707B2 (en) 2000-12-15 2006-04-04 Hoffman-La Roche Inc. Piperazine derivatives
WO2002048124A2 (en) * 2000-12-15 2002-06-20 F. Hoffmann-La Roche Ag Piperazine derivatives
WO2002048124A3 (en) * 2000-12-15 2003-06-05 Hoffmann La Roche Piperazine derivatives
WO2005000305A1 (en) * 2003-06-20 2005-01-06 Eli Lilly And Company 3-aminopiperidines and 3-aminoquinuclidines as inhibitors of monoamine uptake
US7432280B2 (en) 2003-06-20 2008-10-07 Eli Lilly And Company 3-aminopiperidines and 3-aminoquinuclidines as inhibitors of monoamine uptake
WO2009107571A1 (en) * 2008-02-27 2009-09-03 住友化学株式会社 Method for optical resolution of alkylpiperidin-3-yl carbamate and intermediate therefor
JP2009227665A (en) * 2008-02-27 2009-10-08 Sumitomo Chemical Co Ltd Method for optical resolution of alkylpiperidin-3-yl carbamate and intermediate therefor
WO2009119700A1 (en) * 2008-03-26 2009-10-01 住友化学株式会社 Manufacturing method for a piperidine-3-ylcarbamate compound and optical resolution method therefor
JP2009256298A (en) * 2008-03-26 2009-11-05 Sumitomo Chemical Co Ltd Optical resolution method for piperidin-3-ylcarbamate compound, and its intermediate
JP2009256337A (en) * 2008-03-26 2009-11-05 Sumitomo Chemical Co Ltd Method for producing piperidin-3-ylcarbamate compound
CN107814792A (en) * 2016-09-14 2018-03-20 中国科学院上海药物研究所 A kind of quinazoline derivant, its composition and purposes
CN107814792B (en) * 2016-09-14 2021-08-10 中国科学院上海药物研究所 Quinazoline derivative, composition and application thereof

Also Published As

Publication number Publication date
FR2321890B1 (en) 1979-09-14

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