Plural Carbocyclic Rings Bonded Directly To The Same Acyclic Carbon Patents (Class 544/396)
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Patent number: 4883797Abstract: Derivatives of piperazine having the general formula ##STR1## wherein R.sub.1 is benzhydryl or cinnamyl and R.sub.2 is selected from the group consisting of ##STR2## --(CH.sub.2).sub.3 --R.sub.8, --CH.sub.2 NHR.sub.9, --CH.sub.2 NH.sub.2 and --COR.sub.10 ; wherein R.sub.3 is hydrogen, chloromethyl, (4-benzhydryl-1-piperazinyl) methyl, 4-morpholinylmethyl or 1-piperidinylmethyl, R.sub.4 is hydrogen, chloromethyl or carbethoxy, R.sub.5 and R.sub.6 taken together are an oxygen atom or the radical --O--(CH.sub.2).sub.2 --O--, R.sub.7 is methyl, phenyl or 2-thienyl, R.sub.8 is 4-morpholinyl, 1-piperidinyl or 4-benzhydryl-1-piperazinyl, R.sub.9 is 2-oxo-1- (pyrrolidinyl) acetyl, 2-hydroxybenzoyl or 4-sulfamoylbenzoyl, R.sub.10 is 2-oxo-1-(pyrrolidinyl)methyl or 4-sulfamoylphenyl and X is oxygen or NH; as well as methods for making the same and their use in a pharmaceutical composition is proposed. The compounds have cardiovascular properties and increasing effects on cerebral flow.Type: GrantFiled: January 7, 1988Date of Patent: November 28, 1989Assignee: Ferrer Internacional, S.A.Inventors: Rafael Foguet, Jose A. Ortiz, Santiago Gubert, Manuel M. Raga, Aurelio Sacristan
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Patent number: 4882331Abstract: The invention relates to 1-[(1,1-diphenyl)-1-alkenyl]piperazine derivatives corresponding to general formula I: ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5, which are identical or different, represent a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkenyl group, a lower alkoxy group or the trifluoromethyl group; n is an integer between 1 and 3; m is an integer from 0 to 3; Z represents a hydrogen atom, a lower alkyl group or an aryl group of the formula: ##STR2## in which R.sub.6 has the same meaning as R.sub.1, R.sub.2, R.sub.3 or R.sub.4 ; and A is an oxygen atom or a group ##STR3## and to their pharmaceutically acceptable salts. Application: pharmeutical compositions with antidepressant properties.Type: GrantFiled: April 11, 1988Date of Patent: November 21, 1989Assignee: Les Laboratoires MeramInventors: Andre Buzas, Roland Ollivier
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Patent number: 4880808Abstract: A method of improving sleep in warm-blooded animals suffering from sleep disorders, which method comprises the administration of particular N-aryl-piperazinealkanamide derivatives and compositions containing the same. Novel N-aryl-piperazinealkanamide derivatives.Type: GrantFiled: March 9, 1988Date of Patent: November 14, 1989Assignee: Janssen Pharmaceutica N.V.Inventors: Georges H. P. Van Daele, Freddy F. Vlaeminck, Marc G. C. Verdonck
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Patent number: 4859673Abstract: Novel amide derivatives are disclosed. As examples of said amide derivatives are mentioned 1-[2-(5-(3-methoxy-4-benzyloxyphenyl)-2,4-pentadienoyl)aminoethyl]-4-diphe nylmethoxypiperidine, 1-[2-(5-(3-methoxy-4-pentadienoyl)aminoethyl]-4-diphenylmethoxypiperidine and 1-[2-(5-(3-methoxy-4-ethoxymethoxyphenyl)-2,4-pentadienoyl)aminoethyl]-4-d iphenylmethoxypiperidine. These amide derivatives are useful as antiallergic agents.Type: GrantFiled: April 23, 1987Date of Patent: August 22, 1989Assignee: Terumo Kabushiki KaishaInventors: Makoto Takai, Kazuhiro Omori, Takahiro Kumonaka, Shinji Ozawa, Toshio Wakabayashi
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Patent number: 4797489Abstract: The compounds ##STR1## wherein R.sup.1 is 1-adamantyl, 3-methyl-1-adamantyl, 9-fluorenyl or 1-fluorenyl;n is 0 or 1;m is 1, 2, 3, 4 or 5; andX is ##STR2## where R.sup.2 is phenyl, benzyl, pyridinyl, pyrimidinyl, pyrazinyl or substituted phenyl or benzyl in which the substituent is alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, halo, cyano, nitro or trifluoromethyl, ##STR3## where R.sup.3 is hydrogen, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, halo, cyano or nitro;or pharmaceutically acceptable salts thereof are useful antidepressant and/or anxiolytic agents.Type: GrantFiled: December 2, 1987Date of Patent: January 10, 1989Assignee: American Home Products Corp.Inventors: Magid A. Abou-Gharbia, Gary P. Stack, John P. Yardley
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Patent number: 4795752Abstract: Novel amide derivatives are disclosed. As examples of said amide derivatives are mentioned 1-[2-[5-(3-methoxy-4-ethoxycarbonyloxyphenyl)-2,4-pentadienoyl]-aminoethyl ]-4-benzhydroxypiperidine, 1-[2-[3-(3-methoxy-4-ethoxycarbonyloxyphenyl)-2-propenoyl]aminoethyl]-4-be nzhydroxypiperidine, 1-[3-[5-(3-methoxy-4-ethoxycarbonyloxyphenyl)-2,4-pentadienoyl]aminopropyl ]-4-benzhydrylpiperazine and the like. These amide derivatives are useful as antiallergic agents.Type: GrantFiled: December 8, 1986Date of Patent: January 3, 1989Assignee: Terumo Kabushiki KaishaInventors: Shin Hattori, Makoto Takai, Kazuhiro Omori, Shinji Ozawa, Toshio Wakabayashi
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Patent number: 4792553Abstract: Novel dienyl derivatives are disclosed. As examples of said diene derivative are mentioned 1-benzhydryl-4-(5-phenyl-2,4-pentadienyl)piperazine, 1-(4,4'-difluorobenzhydryl)-4-(5-phenyl-2,4-pentadienyl)piperazine, 1-benzhydryl-4-(5-(3,4,5-trimethoxyphenyl)-2,4-pentadienyl)piperazine, 1-(4,4'-difluorobenzhydryl)-4-(5-(2,4-dimethoxyphenyl)-2,4-pentadienyl)pip erazine, 1-benzhydryl-4-(5-(2,3,4-trimethoxyphenyl)-2,4-pentadienyl)piperazine, 1-(4,4'-difluorobenzhydryl)-4-(5-(2,3,4-trimethoxyphenyl)-2,4-pentadienyl) piperazine and the like. These dienyl derivatives are useful as vasodilators.Type: GrantFiled: February 3, 1987Date of Patent: December 20, 1988Assignee: Terumo Kabushiki KaishaInventors: Shin Hattori, Makoto Takai, Toshio Wakabayashi, Yasusi Suwabe, Syozo Miyaoka
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Patent number: 4766116Abstract: A diaryl butyric acid derivative having the general formula: ##STR1## wherein R.sup.1 represents a hydrogen atom, an alkyl group having 1 to 3 carbon atoms, or an acyl group having 2 to 4 carbon atoms; R.sup.2 represents an alkyl group having 1 to 3 carbon atoms; andX represents a variety of substituents.This diaryl butyric acid derivative or the pharmaceutically acceptable salt thereof can be prepared by reacting a benzoxepin derivative having the general formula: ##STR2## wherein R.sup.2 is the same as defined above with an amine or alcohol derivative having the general formula;X--Hwherein X is the same as defined above in the presence of an acid catalyst at room temperature or at an elevated temperature and, optionally, further reading the reaction product with an alkylation agent having 1 to 3 carbon atoms or an acylation agent having 2 to 4 carbon atoms.Type: GrantFiled: December 19, 1985Date of Patent: August 23, 1988Assignee: Suntory LimitedInventors: Toshio Tatsuoka, Kenji Suzuki, Kayoko Imao, Kunihiro Sumoto
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Patent number: 4757074Abstract: The present invention provides compounds of the formula (I): ##STR1## or salts, esters or amide derivatives thereof, wherein R.sub.1 is --CO.sub.2 H, --CH.dbd.CH--CO.sub.2 H, --(CH.sub.2).sub.n CO.sub.2 H, or --O--(CH.sub.2).sub.n CO.sub.2 H (n=1 to 4); R.sub.2 is C.sub.1.varies. alkyl or benzyl which is optionally substituted by a C.sub.1-4 alkyl group or groups; R.sub.3 is C.sub.1-4 alkoxy, C.sub.1-4 alkyl or halogen. Also provided are pharmaceutical formulations containing the compounds of the formula (I) and methods for the preparation of the compounds. The above mentioned compounds have antihistaminic activity.Type: GrantFiled: February 24, 1986Date of Patent: July 12, 1988Assignee: Burroughs Wellcome Co.Inventors: Geoffrey G. Coker, John W. A. Findlay
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Patent number: 4703048Abstract: A 1-benzhydryl-4-cinnamylpiperazine derivative represented by the following formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom or a methoxy group, and R.sup.2 represents a hydrogen or fluorine atom, or a pharmaceutically acceptable acid addition salt thereof. The compound (I) is prepared by selectively reducing the corresponding 1-benzhydryl-4-cinnamoylpiperazine derivative and optionally converting the product into its acid addition salt. The compound (I) is useful for treatment of cerebrovascular disease in a human.Type: GrantFiled: December 31, 1985Date of Patent: October 27, 1987Assignee: Kanebo Ltd.Inventors: Hiroshi Ohtaka, Toshiro Kanazawa, Keizo Ito, Goro Tsukamoto
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Patent number: 4686220Abstract: This disclosure describes certain substituted piperazine-1,4-naphthalenediones useful as anti-asthmatic agents.Type: GrantFiled: December 19, 1985Date of Patent: August 11, 1987Assignee: American Cyanamid CompanyInventors: Jeffrey B. Medwid, Lawrence W. Torley, Andrew S. Tomcufcik
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Patent number: 4675319Abstract: Novel piperazine derivatives having the general formula: ##STR1## wherein R is hydrogen or lower alkyl, A is straight or branched chain lower alkyl, and R.sub.1 and R.sub.2 are each hydrogen, amino, alkylamino, dialkylamino, mono- or di(hydroxyalkyl)amino, morpholino, pyrrolidino, piperidino, N-alkylpiperazino, 1,3-dithiolan-2-ylidenamino, or N-alkylureido, with the proviso that at least one of R.sub.1 and R.sub.2 is other than hydrogen, or the isomeric mixtures, individual enantiomers or pharmaceutically acceptable acid addition salts thereof, are therapeutically useful antianaphylactic and antibronchospastic agents.Type: GrantFiled: June 9, 1986Date of Patent: June 23, 1987Assignee: Recordati S. A. Chemical and Pharmaceutical CompanyInventors: Dante Nardi, Amedeo Leonardi, Gianni Motta, Pietro Cazzulani
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Patent number: 4663325Abstract: A 1-benzyl-4-benzhydrylpiperazine derivative represented by the following general formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom or a methoxy group, andR.sup.2 represents a hydrogen or fluorine atom,or a pharmaceutically acceptable acid addition salt thereof.The 1-benzyl-4-benzhydrylpiperazine derivative or an acid addition salt thereof is prepared by reductively condensing a benzaldehyde derivative with a fluorobenzhydrylpiperazine, or condensing a benzyl halide derivative with a fluorobenzhydrylpiperazine optionally in the presence of an acid acceptor, or condensing a benzylpiperazine with a fluorobenzhydryl halide derivative and, optionally converting the product to its acid addition salt.The 1-benzyl-4-benzhydrylpiperazine derivative is useful for improving a cerebrovascular disease.Type: GrantFiled: March 25, 1985Date of Patent: May 5, 1987Assignee: Kanebo Ltd.Inventors: Hiroshi Ohtaka, Toshiro Kanazawa, Keizo Ito, Goro Tsukamoto
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Patent number: 4663456Abstract: The .beta.-carbolines N-substituted in 2-position with a piperidinyl alkyl group are antipsychotic agents and anxiolytic agents with minimal extrapyramidal side effects, useful in the treatment of psychological disorders such as paranoia and schizophrania as well as general states of anxiety.Type: GrantFiled: September 16, 1985Date of Patent: May 5, 1987Assignee: American Home Products CorporationInventor: Magid A. Abou-Gharbia
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Patent number: 4638003Abstract: N-substituted derivatives of 1-(4'-alkylthiophenyl)-2-amino-1,3-propanediol, their salts with pharmaceutically acceptable organic and inorganic acids, processes for preparing them, pharmaceutical compositions containing them and intermediates useful in the preparation thereof.The novel derivatives according to this invention are endowed with calcium antagonist activity and are useful as antiarrhythmic and vasodilating agents.Type: GrantFiled: August 1, 1984Date of Patent: January 20, 1987Assignee: Zambon S.p.A.Inventors: Dario Chiarino, Angelo Carenzi, Davide Della Bella, Mario Fantucci
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Patent number: 4632940Abstract: N-substituted derivatives of 1-(4'-alkylsulfonylphenyl)-2-amino-1,3-propanediol, their salts with pharmaceutically acceptable organic and inorganic acids, processes for preparing them, pharmaceutical compositions containing them and intermediates useful in the preparation thereof.The novel derivatives according to this invention are endowed with local anesthetic activity.Type: GrantFiled: August 3, 1984Date of Patent: December 30, 1986Assignee: Zambon S.p.A.Inventors: Dario Chiarino, Angelo Carenzi, Davide Della Bella, Mario Fantucci
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Patent number: 4619944Abstract: Provided are antihypertensive compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are hydrogen, alkyl, alkenyl, alkynyl, phenyl-alkyl, or cycloalkyl, and may be the same or different,m is an integer from 0 to 2 inclusive,n is an integer from 0 to 4 inclusive,M is alkenyl, alkynyl, cycloalkyl, cycloalkyl-alkyl, polycycloalkyl, polycycloalkyl-alkyl, aryl, aralkyl, heteroaryl, heteroaryl-alkyl, hetero-cycloalkyl, hetero-cycloalkyl-alkyl, fused aryl-cycloalkyl, fused aryl-cycloalkyl-alkyl, fused heteroaryl-cycloalkyl, fused heteroaryl-cycloalkyl-alkyl, alkoxyalkyl, alkylthioalkyl, alkylamino-alkyl, or dialkylaminoalkyl.Y is hydroxy, alkoxy, amino, or substituted amino, aminoalkanoyl, aryloxy, aminoalkoxy, or hydroxyalkoxy, andR.sub.7 is alkyl, aryl, aralkyl, cycloalkyl, cycloalkyl-alkyl, heterocyclic, --CO--SR, --CS--SR, ##STR2## CH.sub.2 CO.sub.2 R, --CHM--CO.sub.2 R, --CH.sub.2 --CO--SR, --CN, ##STR3## --CO--NH--CH.sub.2 CO.sub.2 R, ##STR4## or --CO--CO.sub.Type: GrantFiled: February 19, 1985Date of Patent: October 28, 1986Assignee: USV Pharmaceutical CorporationInventors: Raymond D. Youssefyeh, Howard Jones
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Patent number: 4618611Abstract: The invention relates to new aminopropanol derivatives of the formula (I) ##STR1## wherein R.sub.1 is halogen, trihalomethyl, alkoxy having from one to 3 carbon atoms or alkyl having from one to 3 carbon atoms,R.sub.2 is alkyl having from one to 3 carbon atoms, andR.sub.3 is cycloalkyl having from 3 to 6 carbon atoms, orR.sub.2 and R.sub.3 together with the nitrogen they are attached to form an up to 8 membered ring optionally containing oxygen or a further nitrogen as an additional hetero atom, and optionally substituted with alkyl having from one to 4 carbon atoms or benzyl,and acid addition and quaternary ammonium salts thereof.According to another aspect of the invention there are provided processes for the preparation of these compounds.The new compounds are suitable for the treatment of acute ethanolic intoxication. Pharmaceutical compositions containing them are also within the scope of the invention.Type: GrantFiled: December 27, 1983Date of Patent: October 21, 1986Assignee: Richter Gedeon Vegyeszeti Gyar RtInventors: Edit Toth, Jozsef Torley, Gyorgy Fekete, Laszlo Szporny, Laszlo Vereczkey, Eva Palosi, Imre Klebovich, Pal Vittay, Sandor Gorog, Istvan Hajdu
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Patent number: 4603134Abstract: A piperazine derivative is disclosed of formula (I): ##STR1## and the non-toxic addition salts thereof, along with a process for preparation, pharmaceutical composition, and method of treating conditions characterized by histamine activity.Type: GrantFiled: January 11, 1985Date of Patent: July 29, 1986Assignee: Ferrer International, S.A.Inventors: Rafael Foguet, Santiago Gubert, Manuel Raga, Aurelio Sacristan, Jose A. Ortiz
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Patent number: 4591590Abstract: The present invention relates to novel benzhydrylpiperazine derivatives having anti-allergic activities, the preparation of these derivatives, pharmaceutical compositions comprising the same, and to a method of using these compounds therapeutically in the treatment of allergic symptoms in human beings and animals.These benzhydrylpiperazine derivatives have the follow formula: ##STR1## wherein A is a lower alkylene, Z is a benzhydryl optionally substituted with halogen, andR.sup.1 is amino, aryl, pyridyl, acyl or acylamino, in which the aryl group and pyridyl group are substituted with nitro, amino or acyl amino groups, provided that Z is benzhydryl substituted with a halogen, when R.sup.1 is an amino group.Type: GrantFiled: December 21, 1983Date of Patent: May 27, 1986Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Ikuo Ueda, Daizo Morino, Koichi Takimoto
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Patent number: 4590274Abstract: Antihypertensive piperazineethylidenebenzocycloalkanes are provided. These compounds have the formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are independently C.sub.1 -C.sub.6 alkyl, hydrogen, C.sub.1 -C.sub.6 alkoxy, hydroxy, or halo, or R.sub.1 and R.sub.2 or R.sub.2 and R.sub.3 together can form a methylenedioxy bridge;R.sub.4 is H or C.sub.1 -C.sub.6 alkyl;n is 0, 1 or 2;m is 0, 1, 2 or 3; andAr.sub.1 and Ar.sub.2 are independently phenyl optionally substituted with one or two of halogen, hydroxy, or C.sub.1 -C.sub.6 alkoxy groups,or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 3, 1985Date of Patent: May 20, 1986Assignee: E. I. Du Pont de Nemours and CompanyInventor: Anthony J. Cocuzza
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Patent number: 4528194Abstract: A piperazine derivative of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or a lower alkyl group; R.sup.2 is a hydroxyl group, an aralkyloxy group, a lower alkoxy group containing 1-5 carbon atoms or a lower alkenyloxy group containing 3-5 carbon atoms; R.sup.3 is a hydrogen atom, or an aralkyloxy group, a lower alkoxy group containing 1-5 carbon atoms or a lower alkenyloxy group containing 3-5 carbon atoms; and R.sup.4 is a hydrogen atom or a lower alkoxy group containing 1-5 carbon atoms, provided that R.sup.2 is a group other than the lower alkoxy group containing 1-5 carbon atoms when both R.sup.3 and R.sup.4 are hydrogen atoms; or a pharmaceutically acceptable salt is effectively useful as a cerebral circulation-improving agent.Type: GrantFiled: July 12, 1983Date of Patent: July 9, 1985Assignee: Nippon Chemiphar Co., Ltd.Inventor: Mitsuo Masaki
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Patent number: 4525358Abstract: New 2-[4-(diphenylmethyl)-1-piperazinyl]-acetic acids, their amides and their salts, processes for the preparation thereof and therapeutic compositions. These compounds have the formula ##STR1## wherein Y=--OH or --NH.sub.2 ; X and X'=H, halogen, alkoxy or trifluoromethyl; m=1 or 2 and n=1 or 2.The amides of the 2-[4-(diphenylmethyl)-1-piperazinyl]-acetic acids are prepared either by reacting a 1-(diphenylmethyl)-piperazine with an omegahaloacetamide, or by reacting an alkali metal salt of an omega-[4-(diphenylmethyl)-1-piperazinyl]-alkanol with a 2-haloacetamide, or yet by reacting ammonia with a halide or alkyl ester of a 2-[4-(diphenylmethyl)-1-piperazinyl]-acetic acid, whereas the 2-[4-(diphenylmethyl)-1-piperazinyl]-acetic acids are prepared by hydrolyzing the corresponding amide or lower alkyl ester.These compounds have in particular an antiallergic, spasmolytic and antihistaminic activity.Type: GrantFiled: May 17, 1983Date of Patent: June 25, 1985Assignee: UCB Pharmaceuticals, Inc.Inventors: Eugene Baltes, Jean de Lannoy, Ludovic Rodriguez
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Patent number: 4504663Abstract: The present invention concerns novel heterocyclic aminoalcoyl derivatives having the formula: ##STR1## wherein n=1, 2 or 3; A represents a nitrogen atom or the CH group, X=CH.sub.2 or CH.sub.2 O; R represents a phenyl nucleus possibly substituted; NR.sub.1 R.sub.2 =amino, methylamino, N,N-dialkylamino or an heterocyclic radical; and R.sub.3 =H, halogen, alkyl, alkyloxy or methoxy.These derivatives are useful as drugs, especially as analgesics and antidepressants.Type: GrantFiled: November 15, 1983Date of Patent: March 12, 1985Assignee: Delalande S.A.Inventors: Gerard H. Moinet, Philippe L. Dostert, Guy R. Bourgery
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Patent number: 4504481Abstract: The invention relates to new benzhydrylpiperazine derivatives of the formula (I) ##STR1## wherein n is 2 or 3, and acid addition salts thereof. According to another aspect of the invention there are provided processes for the preparation of these compounds.The compounds of the formula (I) are pharmacologically active. More particularly, they inhibit the microsomal monooxigenase enzyme system of liver. Pharmaceutical compositions containing them as active ingredient are also within the scope of the invention.Type: GrantFiled: December 27, 1983Date of Patent: March 12, 1985Assignee: Richter Gedeon Vegyeszeti Gyar Rt.Inventors: Edit Toth, Jozsef Torley, Eva Palosi, Szabolcs Szeberenyi, Laszlo Szporny, Sandor Gorog, Istvan Hajdu
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Patent number: 4490548Abstract: Processes for preparing dihydro-prostacyclin analogs, which are 9-deoxy-5,9-cyclic ethers of prostaglandin F.sub.1 .alpha.-type compounds, illustrated, for example, by a compound of the formula ##STR1## wherein .about. indicates alpha or beta configuration; including the products and intermediates produced therein, said products having pharmacological utility.Type: GrantFiled: March 26, 1979Date of Patent: December 25, 1984Assignee: The Upjohn CompanyInventor: Roy A. Johnson
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Patent number: 4482549Abstract: Compounds are described of the formula ##STR1## in which --COR.sup.1 is a complex ester or thioester group,W is alkylene,X is cis or trans --CH.dbd.CH or --CH.sub.2 CH.sub.2 --,n is 1 or 2,Y is a saturated heterocyclic amino group having 5-8 ring members, andR.sup.2 is unsubstituted or substituted phenylalkyl, thienzlalkyl, naphthylalkyl or cinnamyl, and their salts and solvates.These compounds inhibit blood platelet aggregation and bronchoconstriction and may be formulated for use as antithrombotic and antiasthmatic agents.Type: GrantFiled: February 8, 1984Date of Patent: November 13, 1984Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, Norman F. Hayes, John Bradshaw, Malcolm Carter, Alan Wadsworth
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Patent number: 4431851Abstract: The present invention concerns compounds of the formula ##STR1## wherein n=1, 2 or 3; and R' represents phenyl or orthofluorophenyl. Said compounds are used as intermediates in the preparation of heterocyclic aminoalkyl derivatives which are useful as analgesics and antidepressants.Type: GrantFiled: March 8, 1983Date of Patent: February 14, 1984Assignee: Delalande S.A.Inventors: Gerard H. Moinet, Philippe L. Dostert, Guy R. Bourgery
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Patent number: 4410521Abstract: Compounds are described of the formula ##STR1## in which --COR.sup.1 is a complex ester or thioester group,W is alkylene,X is cis or trans --CH.dbd.CH or --CH.sub.2 CH.sub.2 --,n is 1 or 2,Y is a saturated heterocyclic amino group having 5-8 ring members, andR.sup.2 is unsubstituted or substituted phenylalkyl, thienylalkyl, naphthylalkyl or cinnamyl,and their salts and solvates.These compounds inhibit blood platelet aggregation and bronchoconstruction and may be formulated for use as antithrombotic and antiasthmatic agents.Type: GrantFiled: September 16, 1982Date of Patent: October 18, 1983Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, Norman F. Hayes, John Bradshaw, Malcolm Carter
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Patent number: 4409213Abstract: Prostanoid compounds are described having the formula: ##STR1## where A is a cyclopentane ring, which is substituted by oxo and/or hydroxy or etherified hydroxy and may be saturated or unsaturated; X is --CH.dbd.CH-- or --(CH.sub.2).sub.2 --; R is alkyl having a terminal --COOH or ester group; and Y is amino or substituted amino, particularly heterocyclic amino.The compounds have bronchodilator activity and/or inhibit blood platelet aggregation.The preparation and pharmaceutical formulation of the compounds is also described.Type: GrantFiled: November 10, 1982Date of Patent: October 11, 1983Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Harry Finch, Roger F. Newton, Christopher J. Wallis
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Patent number: 4397855Abstract: New 4-(substituted-.alpha., .alpha.-dimethyl-1-piperazine pentanoic acids and derivatives which are useful as anti-arteriosclerotic agents are disclosed. These compounds elevate the high density lipoprotein fraction of cholesterol, and also lower the low density lipoprotein fraction of cholesterol.Type: GrantFiled: June 26, 1981Date of Patent: August 9, 1983Assignee: Warner-Lambert CompanyInventor: Ila Sircar
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Patent number: 4381266Abstract: Anhydride compounds of the formula ##STR1## wherein A is an optionally substituted amino-phenyl or optionally substituted 3-indolyl radical, Hal represents halogen, Z represents hydrogen, alkyl of 1 to 4 carbon atoms or an optionally substituted phenyl radical and n is 1 to 4; these anhydrides are particularly useful as starting materials for the manufacture of halogenated 3-aryl-3-indolyl-phthalides or fluoran derivatives.Type: GrantFiled: December 22, 1980Date of Patent: April 26, 1983Assignee: Ciba-Geigy CorporationInventors: Robert Garner, Michael J. Whitehead
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Patent number: 4340756Abstract: Novel halophenyl and loweralkyl substituted halophenyl polyamines are useful antimicrobial agents, as well as algae inhibitors. They are especially useful because of their low toxicity, and as such are advantageously included as the active agent in surgical scrubs, antibacterial soaps, as preservatives in cosmetic preparations, and the like.Type: GrantFiled: February 4, 1981Date of Patent: July 20, 1982Assignee: Merck & Co., Inc.Inventors: Richard A. Dybas, Nathaniel Grier, Bruce E. Witzel
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Patent number: 4265891Abstract: Prostanoid compounds are described having the formula: ##STR1## where A is a cyclopentane ring, which is substituted by oxo and/or hydroxy or etherified hydroxy and may be saturated or unsaturated; X is --CH.dbd.CH-- or --(CH.sub.2).sub.2 --; R is alkyl having a terminal --COOH or ester grup; and Y is amino or substituted amino, particularly heterocyclic amino.The compounds have bronchodilator activity and/or inhibit blood platelet aggregation.The preparation and pharmaceutical formulation of the compounds is also described.Type: GrantFiled: July 10, 1979Date of Patent: May 5, 1981Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Harry Finch, Roger F. Newton, Christopher J. Wallis
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Patent number: 4260760Abstract: Novel diphenyl and loweralkyl substituted diphenyl polyamines are useful antimicrobial agents, as well as algae inhibitors. They are especially useful because of their low toxicity, and as such are advantageously included as the active agent in surgical scrubs, antibacterial soaps, as preservatives in cosmetic preparations, and the like. They also can be used for topical treatment of dermatological conditions having a bacterial origin or implication such as Acne vulgaris.Type: GrantFiled: March 12, 1979Date of Patent: April 7, 1981Assignee: Merck & Co., Inc.Inventors: Richard A. Dybas, Nathaniel Grier, Bruce E. Witzel
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Patent number: 4243806Abstract: Novel 5-[4-(diarylmethyl)-1-piperazinylalkyl]benzimidazole derivatives having antiallergic and antihistaminic properties.Type: GrantFiled: June 13, 1979Date of Patent: January 6, 1981Assignee: Janssen Pharmaceutica N.V.Inventors: Alfons H. M. Raeymaekers, Josephus L. H. Van Gelder, Gustaaf M. Boeckx, Lodewijk L. Van Hemeldonck
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Patent number: 4216216Abstract: Compounds of general formula ##STR1## are disclosed wherein appropriate substituents for R.sup.1, R.sup.2 to R.sup.5, R.sup.6, A, Q, X, and Z are defined for these novel hexahydropyrimidines. Procedures for the preparation of these compounds are also given. Because of the highly effective serotonin antagonistic activity in combination with a strong inhibiting effect on thrombocyte aggregation and good compatibility these compounds are effective in treating migraine. Additionally, the compounds also exhibit an anti-histamine activity, cause an increase in erythrocyte fluidity, a psychotropic activity, a weak bradykinin antagonism and hypotensive effects.Type: GrantFiled: June 15, 1978Date of Patent: August 5, 1980Assignee: Hoechst AktiengesellschaftInventors: Rolf-Ortwin Weber, Hiristo Anagnostopulos, Ulrich Gebert
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Patent number: 4209523Abstract: The invention provides new acetohydroxamic acid derivatives, having interesting properties on the central nervous system, of the formula: R.sub.1 R.sub.2 R.sub.3 C--CO--NHOH, in which R.sub.2 and R.sub.3 are each hydrogen or C.sub.1-6 alkyl, and R.sub.1 is C.sub.1-6 alkyl Z.sub.1 Z.sub.2 N (where Z.sub.1 and Z.sub.2 are each phenyl, substituted phenyl, or cycloalkyl), substituted hydantoinyl, benzhydroxylcarboxamido, Z.sub.3 CH.sub.2 -- (where Z.sub.3 =optionally substituted aryl), Z.sub.4 --A-- (where Z.sub.4 is optionally substituted phenyl or naphthyl, and A is --NH--, --N(C.sub.1-4 alkyl)--, --N(C.sub.5-6 cycloalkyl)--, --NHCO--, --N(C.sub.1-4 alkyl)CO--, --N(C.sub.5-6 cycloalkyl)CO--, --CONH--, --CON(C.sub.1-4 alkyl)--, --CON(C.sub.5-6 cycloalkyl)--, --NHCONH--, --N(C.sub.5 H.sub.6)CONH--, or --N(substituted phenyl)CONH--, optionally substituted benzimidazolyl, or an optionally substituted tricyclic radical, and their metal and acid addition salts.Type: GrantFiled: August 4, 1978Date of Patent: June 24, 1980Assignee: Laboratoire L. LafonInventor: Louis Lafon
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Patent number: 4209524Abstract: The invention provides new acetohydroxamic acid derivatives, having interesting properties on the central nervous system, of the formula: R.sub.1 R.sub.2 R.sub.3 C--CO--NHOH, in which R.sub.2 and R.sub.3 are each hydrogen or C.sub.1-6 alkyl, and R.sub.1 is C.sub.1-6 alkyl Z.sub.1 Z.sub.2 N (where Z.sub.1 and Z.sub.2 are each phenyl, substituted phenyl, or cycloalkyl), substituted hydantoinyl, benzhydroxylcarboxamido, Z.sub.3 CH.sub.2 --(where Z.sub.3 =optionally substituted aryl), Z.sub.4 --A-- (where Z.sub.4 is optionally substituted phenyl or naphthyl, and A is --NH--, --N(C.sub.1-4 alkyl)--, --N(C.sub.5-6 cycloalkyl)--, --NHCO--, --N(C.sub.1-4 alkyl(CO--, --N(C.sub.5-6 cycloalkyl)CO--, --CONH--, --CON(C.sub.1-4 alkyl)--, --CON(C.sub.5-6 cycloalkyl)-, --NHCONH--, --N(C.sub.5 H.sub.6)CONH--, or --N(substituted phenyl)CONH--, optionally substituted benzimidazolyl, or an optionally substituted tricyclic radical, and their metal and acid addition salts.Type: GrantFiled: August 4, 1978Date of Patent: June 24, 1980Assignee: Laboratoire L. LafonInventor: Louis Lafon
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Patent number: 4199582Abstract: Novel 1,2-dihydronaphthalene derivatives of the formula ##STR1## wherein A is a di-lower alkylamino group or a 5- to 7-membered cyclic amino group which may contain one oxygen atom and n is 2 or 3, and its salts have excellent pharmacological activities such as vasodilator, hypotensive and cerebral blood flow increasing actions.Type: GrantFiled: July 26, 1978Date of Patent: April 22, 1980Assignee: Takeda Chemical Industries, Ltd.Inventors: Yoshikazu Oka, Katsumi Itoh, Minoru Hirata
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Patent number: 4179505Abstract: Novel 5-[4-(diarylmethyl)-1-piperazinylalkyl]benzimidazole derivatives having antiallergic and antihistaminic properties.Type: GrantFiled: January 4, 1978Date of Patent: December 18, 1979Assignee: Janssen Pharmaceutica N.V.Inventors: Alfons H. M. Raeymaekers, Josephus L. H. Van Gelder, Gustaaf M. Boeckx, Lodewijk L. Van Hemeldonck
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Patent number: 4177290Abstract: Novel acetamide derivatives have been discovered to have useful pharmaceutical activity on the central nervous system. They may be prepared by reacting the corresponding ester or acid halide with the appropriately substituted amine.Type: GrantFiled: March 9, 1978Date of Patent: December 4, 1979Assignee: Laboratoire L. LafonInventor: Louis Lafon
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Patent number: 4172094Abstract: Novel diphenyl and loweralkyl substituted diphenyl polyamines are useful antimicrobial agents, as well as algae inhibitors. They are especially useful because of their low toxicity, and as such are advantageously included as the active agent in surgical scrubs, antibacterial soaps, as preservatives in cosmetic preparations, and the like. They also can be used for topical treatment of dermatological conditions having a bacterial origin or implication such as Acne vulgaris.Type: GrantFiled: December 3, 1976Date of Patent: October 23, 1979Assignee: Merck & Co., Inc.Inventors: Richard A. Dybas, Nathaniel Grier, Bruce E. Witzel
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Patent number: 4160099Abstract: Labile quaternary ammonium salts of the following formula (I) and (II) are provided: ##STR1## wherein ##STR2## represents a tertiary aliphatic amine; wherein ##STR3## represents an unsaturated amine; wherein R represents a member selected from the group consisting of a hydrogen atom, a C.sub.1 -C.sub.8 open chain or cyclo alkyl group, a C.sub.1 -C.sub.8 alkoxyalkyl group, a C.sub.1 -C.sub.8 acyloxyalkyl group, a C.sub.1 -C.sub.8 haloalkyl group, a C.sub.1 -C.sub.8 carboxyalkyl group, a C.sub.2 -C.sub.8 alkenylphenyl group, an aryl group, and a substituted aryl group, whose substituents are selected from the group consisting of a halogen atom, an O-lower alkyl (C.sub.1 -C.sub.4) group, an O-acyl group, a nitro group, a carboxyl group, and a carboethoxy group; wherein R.sub.1 which may be the same or different, represents any member defined by R above with the proviso that R.sub.Type: GrantFiled: September 20, 1976Date of Patent: July 3, 1979Assignee: Interx Research CorporationInventor: Nicolae S. Bodor
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Patent number: 4148897Abstract: Novel 1,2-dihydronaphthalene derivatives of the formula ##STR1## wherein R.sup.1 and R.sup.2, independently of each other, are hydrogen, nitro, amino, halogen, or hydroxyl which may be protected, and R.sup.3 is a piperazinyl or morpholino group which may be substituted by lower alkyl, aralkyl, carboxylic acid-derived acyl, lower alkoxycarbonyl-lower alkyl or cycloaminocarbonyl-lower alkyl, and its salts have excellent pharmacological activities such as vasodilator and cerebral blood flow increasing activities.Type: GrantFiled: April 20, 1977Date of Patent: April 10, 1979Assignee: Takeda Chemical Industries, Ltd.Inventors: Yoshikazu Oka, Katsumi Itoh, Akio Miyake, Minoru Hirata
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Patent number: 4140770Abstract: Processes for preparing benzoylethers, their acid additive salts and their quaternary ammonium salts are disclosed. These compounds have useful pharmacodynamic properties.Type: GrantFiled: April 12, 1977Date of Patent: February 20, 1979Assignee: A. Nattermann & Cie. GmbHInventors: Gudrun Repplinger, Hans Betzing
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Patent number: 4122186Abstract: The invention provides new acetohydroxamic acid derivatives, having interesting properties on the central nervous system, of the formula: R.sub.1 R.sub.2 R.sub.3 C-CO-NHOH, in which R.sub.2 and R.sub.3 are each hydrogen or C.sub.1-6 alkyl, and R.sub.1 is C.sub.1-6 alkyl Z.sub.1 Z.sub.2 N (where Z.sub.1 and Z.sub.2 are each phenyl, substituted phenyl, or cycloalkyl), substituted hydantoinyl, benzhydroxylcarboxamido, Z.sub.3 CH.sub.2 -- (where Z.sub.3 = optionally substituted aryl), Z.sub.4 -A- (where Z.sub.4 is optionally substituted phenyl or naphthyl, and A is --NH--, --N(C.sub.1-4 alkyl)--, --N(C.sub.5-6 cycloalkyl)--, --NHCO--, --N(C.sub.1-4 alkyl)CO--, --N(C.sub.5-6 cycloalkyl)CO--, --CONH--, --CON(C.sub.1-4 alkyl)--, --CON(C.sub.5-6 cycloalkyl)--, --NHCONH--, --N(C.sub.5 H.sub.6)CONH--, or --N(substituted phenyl)CONH--, optionally substituted benzimidazolyl, or an optionally substituted tricyclic radical, and their metal and acid addition salts.Type: GrantFiled: March 17, 1977Date of Patent: October 24, 1978Assignee: Laboratoire L. LafonInventor: Louis Lafon
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Patent number: 4113972Abstract: 1,1-Diphenyl-2-hydroxy-3-aminopropane derivatives are useful for their psychotropic activity and, in particular are useful as antidepressants.Type: GrantFiled: June 21, 1976Date of Patent: September 12, 1978Assignee: Beecham Group LimitedInventor: Judith Ann Clark
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Patent number: 4088763Abstract: Alkylenedioxy piperazine compounds of the formula ##STR1## and salts thereof with physiologically tolerated acids, useful for the treatment of vascular and cardiac diseases, are disclosed, as are methods for making the compounds and pharmaceutical compositions containing the compounds.Type: GrantFiled: January 19, 1977Date of Patent: May 9, 1978Assignee: Knoll A.G. Chemische FabrikenInventors: Richard Cyrus, Manfred Raschack