Polycyclo Ring System Patents (Class 564/308)
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Patent number: 5576353Abstract: R(+)-N-propargyl-1-aminoindan, its preparation and use and pharmaceutical compositions containing it. The novel compound was found to be useful for the treatment of human patients for Parkinson's disease, memory disorders, dementia of the Alzheimer type (DAT), depression and the hyperactive syndrome.Type: GrantFiled: June 2, 1995Date of Patent: November 19, 1996Assignees: Teva Pharmaceutical Industries Ltd., Technion Research and Development Foundation, Ltd.Inventors: Moussa B. H. Youdim, John P. M. Finberg, Ruth Levy, Haim Yellin
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Patent number: 5569669Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which R.sub.1, R.sub.2, R.sub.2', R.sub.2", R.sub.2'", R.sub.3 and n are as defined in the description, an optical isomer, and an addition salt thereof with a pharmaceutically-acceptable acid or base,and medicinal product containing the same useful for treating a mammal afflicted with a disorder associated to 5-HT.sub.1A or 5-HT.sub.2C receptors.Type: GrantFiled: March 10, 1995Date of Patent: October 29, 1996Assignee: Adir et CompagnieInventors: G erald Guillaumet, Marie-Claude Viaud, Pierre Renard, G erard Adam, Daniel-Henri Caignard, B eatrice Guardiola-Lemaitre, Marie-Claire Rettori
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Patent number: 5545755Abstract: This invention is therapeutically useful 2-aminotetralins and pharmaceutically acceptable acid addition salts thereof of the formula ##STR1## R, R.sub.1 to R.sub.5 and p are as defined in the specification, these compounds are useful to treat central nervous system disorders, hypertension, diabetes, sexual impotency and to control appetite.Type: GrantFiled: January 18, 1995Date of Patent: August 13, 1996Assignee: The Upjohn CompanyInventors: Chiu-Hong Lin, Susanne R. Haadsma-Svensson, Montford F. Piercey, Arthur G. Romero, William H. Darlington
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Patent number: 5532415Abstract: The subject invention provides R(+)-N-propargyl-1-aminoindan and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions containing same. The subject invention also provides methods of treating a subject afflicted with Parkinson's disease, a memory disorder, dementia, depression, hyperactive syndrome, an affective illness, a neurodegenerative disease, a neurotoxic injury, brain ischemia, a head trauma injury, a spinal trauma injury, schizophrenia, an attention deficit disorder, multiple sclerosis, or withdrawal symptoms, using R(+)-N-propargyl-1-aminoindan or the pharmaceutically acceptable salt of the subject invention. The subject invention further provides a method of preventing nerve damage in a subject. Finally, the subject invention provides methods of preparing R(+)-N-propargyl-1-aminoindan, a salt thereof, and racemic N-propargyl-1-aminoindan.Type: GrantFiled: March 28, 1995Date of Patent: July 2, 1996Assignees: Teva Pharmaceutical Industries Ltd., Technion Research and Development Foundation Ltd.Inventors: Moussa B. H. Youdim, John P. M. Finberg, Ruth Levy, Jeffrey Sterling, David Lerner, Tirtsah Berger-Paskin, Haim Yellin, Alex Veinberg
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Patent number: 5475137Abstract: An electrophotographic photoconductor is composed of an electroconductive substrate and a photoconductive layer formed thereon including a m-phenylenediamine derivative of formula (I): ##STR1## wherein Ar represents a non-condensed polycyclic hydrocarbon group other than a phenyl group, or a condensed polycyclic hydrocarbon group having not more than 18 carbon atoms; and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each represent hydrogen, a halogen atom, a cyano group, a nitro group, an alkyl group, an alkoxyl group, an aryl group, an aryloxy group, an alkylmercapto group, a group represented by ##STR2## in which R.sup.6 and R.sup.7 each represent hydrogen, an alkyl group, or an aryl group, an alkylenedioxy group or an alkylenedithio group. Novel m-phenylenediamine derivatives for use in the electrophotoconductor and intermediates for producing the m-phenylenediamine derivatives, and methods of those derivatives are disclosed.Type: GrantFiled: April 7, 1994Date of Patent: December 12, 1995Assignee: Ricoh Company, Ltd.Inventors: Tomoyuki Shimada, Masaomi Sasaki, Tamotsu Aruga, Hiroshi Adachi
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Patent number: 5463051Abstract: Disclosed are a process and intermediates of the formulae ##STR1## wherein X.sup.- is halide, BF.sub.4.sup.-, R.sup.3 SO.sub.3.sup.-, wherein R.sup.3 is C.sub.1 -C.sub.6 alkyl, CF.sub.3, C.sub.1 -C.sub.6 alkylphenyl or phenyl, and Q is a group of the formula ##STR2## wherein R is C.sub.1 -C.sub.6 alkyl; useful for preparing benzazepine intermediates of the formula ##STR3## These benzazepine intermediates are useful for preparing benzazepines having activity as selective D1 receptor antagonists.Type: GrantFiled: September 27, 1993Date of Patent: October 31, 1995Assignee: Schering CorporationInventors: Donald Hou, Richard W. Draper, Gary M. Lee, Janet L. Mas, Ingrid Mergelsberg
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Patent number: 5461147Abstract: Disclosed are a process and intermediates of the formula ##STR1## wherein R is --CH.sub.3 or --C(O)--OR.sup.1, and R.sup.1 is C.sub.1 -C.sub.6 alkyl or --CH.sub.2 C.sub.6 H.sub.5 ; or the formula ##STR2## wherein: R.sup.2 is H or OH, R is --C(O)OR.sup.1 and R.sup.1 is C.sub.1 -C.sub.6 alkyl or --CH.sub.2 C.sub.6 H.sub.5, or where R.sup.2 is H, R can also be CH.sub.3 ; for preparing benzazepine intermediates of the formula ##STR3## The benzazepine intermediates are useful for preparing benzazepines having activity as selective D1 receptor antagonists.Type: GrantFiled: September 27, 1993Date of Patent: October 24, 1995Assignee: Schering CorporationInventors: Donald Hou, Richard W. Draper, Gary M. Lee, Janet L. Mas
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Patent number: 5459275Abstract: An electrophotographic photoconductor comprises an electroconductive substrate and a photoconductive layer formed thereon comprising as an effective component at least one pyrenylamine derivative of formula (I): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, W, j, k, l, m and n are specifically defined in the specification. Furthermore, a novel pyrenylamine derivative for use in the above electrophotographic photoconductor, an aldehyde compound, which is an intermediate for producing the pyrenylamine derivative, and methods of preparing the pyrenylamine derivative and the aldehyde compound are disclosed.Type: GrantFiled: June 15, 1994Date of Patent: October 17, 1995Assignee: Ricoh Company, Ltd.Inventors: Chiaki Tanaka, Masaomi Sasaki, Tamotsu Aruga, Tomoyuki Shimida, Hiroshi Adachi
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Patent number: 5457133Abstract: R(+)-N-propargyl-1-aminoindan, its preparation and use and pharmaceutical compositions containing it. The novel compound was found to be useful for the treatment of human patients for Parkinson's disease, memory disorders, dementia of the Alzheimer type (DAT), depression and the hyperactive syndrome.Type: GrantFiled: February 17, 1994Date of Patent: October 10, 1995Assignees: Teva Pharmaceutical Industries Ltd., Technion Research and Development Foundation Ltd.Inventors: Moussa B. H. Youdim, John P. M. Finberg, Ruth Levy, Jeffrey Sterling, David Lerner, Tirtsah Berger-Paskin, Haim Yellin
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Patent number: 5457232Abstract: A pyrenylamine derivative having an unsaturated bond of formula (I), which can be employed as an organic photoconductive material for use in electrophotography: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, W, l, m, n, j and k are specifically defined in the specification, an aldehyde compound of formula (II), which is an intermediate for preparing the pyrenylamine derivative: ##STR2## and methods of producing the pyrenylamine derivative and the aldehyde compound are disclosed.Type: GrantFiled: September 9, 1994Date of Patent: October 10, 1995Assignee: Ricoh Company, Ltd.Inventors: Chiaki Tanaka, Masaomi Sasaki, Tamotsu Aruga, Tomoyuki Shimada, Hiroshi Adachi
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Patent number: 5453446Abstract: R(+)-N-p-opargyl-1-aminoindan, its preparation and use and pharmaceutical compositions containing it. The novel compound was found to be useful for the treatment of human patients for Parkinson's disease, memory disorders, dementia of the Alzheimer type (DAT), depression and the hyperactive syndrome.Type: GrantFiled: June 7, 1994Date of Patent: September 26, 1995Assignees: Teva Pharmaceutical Industries, Ltd., Technion Research and Development Foundation Ltd.Inventors: Moussa B. H. Youdim, John P. M. Finberg, Ruth Levy, Jeffrey Sterling, David Lerner, Tirtsah Berger-Paskin, Haim Yellin
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Patent number: 5420351Abstract: An aromatic diamine compound represented by formula (1): ##STR1## wherein R.sub.1 and R.sub.2, which may be the same or different, are each a hydrogen atom or a lower alkyl group; and an aromatic diamine compound useful as an intermediate for the synthesis of the above compound (1), represented by formula (2): ##STR2## The compound (1) alleviates the problems of the prior art, and is unlikely to cause crystallization by heat and has a melting point and a glass transition temperature both higher than those of conventional compounds.Type: GrantFiled: November 7, 1994Date of Patent: May 30, 1995Assignee: Nisshinbo Industries, Inc.Inventors: Osamu Suzuki, Hirohiko Yokomizo, Takeshi Arai, Namiko Nakajima
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Patent number: 5403950Abstract: An electrophotographic photoconductor is composed of an electroconductive substrate and a photoconductive layer formed thereon, the photoconductive layer includes a dipyrenylamine derivative of formula (I): ##STR1## wherein R represents an alkyl group with 1 to 12 carbon atoms, which may have a substituent, or an aryl group which may have a substituent. Novel dipyrenylamine derivatives of formula (I), in which R is -ph-(R.sup.4)n, wherein, ph is a phenyl group, R.sup.4 is hydrogen, an unsubstituted or substituted alkyl group having 1 to 12 carbon atoms, an unsubstituted or substituted alkoxyl group having 1 to 12 carbon atoms, n is an integer of 1 to 5, and when n is 2 to 5, R.sup.4 may be the same or different, which are for use in the photoconductive layer of the electrophotographic photoconductor, are synthesized.Type: GrantFiled: May 13, 1994Date of Patent: April 4, 1995Assignee: Ricoh Company, Ltd.Inventors: Tomoyuki Shimada, Masaomi Sasaki, Tamotsu Aruga, Hiroshi Adachi
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Patent number: 5395846Abstract: This invention relates to a class of novel amino bi- and tri-carbocyclic alkane compounds having bis-aryl substitution which exhibit squalene synthase inhibition properties. The bi- and tri-carbocyclic alkane ring contains an amino group and the ring is further linked or bridged to two mono- and/or bicyclic rings. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.Type: GrantFiled: June 25, 1993Date of Patent: March 7, 1995Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: Robert L. Morris, Kent W. Neuenschwander, Keith S. Learn, Anthony C. Scotese
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Patent number: 5387612Abstract: R(+)-N-propargyl-1-aminoindan, its preparation and use and pharmaceutical compositions containing it. The novel compound was found to be useful for the treatment of human patients for Parkinson's disease, memory disorders, dementia of the Alzheimer type (DAT), depression and the hyperactive syndrome.Type: GrantFiled: May 18, 1993Date of Patent: February 7, 1995Assignees: Teva Pharmaceutical Industries Ltd., Technion Research and Development Foundation Ltd.Inventors: Mussa B. H. Youdim, John P. M. Finberg, Ruth Levy, Jeffrey Sterling, David Lerner, Tirtsah Berger-Paskin, Haim Yellin
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Patent number: 5367051Abstract: Fullerene-functionalized amine-containing polymers and polymerizable monomers are disclosed characterized by high temperature stability, i.e., capable of withstanding a temperature of at least about 300.degree. C., and in some instances as high as 650.degree. C., when in polymerized form. The fullerene groups are bonded to the polymers through the amine groups on the polymer. In some instances enhanced mechanical properties also result and, in the case of cross-linked polymers, a composite can be formed from such materials which is structurally reinforced at the molecular level, with the fullerene groups acting as the molecular level structural reinforcement.Type: GrantFiled: July 22, 1993Date of Patent: November 22, 1994Assignee: SRI InternationalInventors: Subhash C. Narang, Susanna C. Ventura, Sivapackia Ganapathiappan, Tilak R. Bhardwaj, Asutosh Nigam
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Patent number: 5344985Abstract: A pyrenylamine derivative having an unsaturated bond of formula (I), which can be employed as an organic photoconductive material for use in electrophotography: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, W, l, m, n j and k are specifically defined the specification, an aldehyde compound of formula (II), which is an intermediate for preparing the pyrenylamine derivative: ##STR2## and methods of producing the pyrenylamine derivative and the aldehyde compound are disclosed.Type: GrantFiled: December 23, 1992Date of Patent: September 6, 1994Assignee: Ricoh Company, Ltd.Inventors: Chiaki Tanaka, Masaomi Sasaki, Tamotsu Aruga, Tomoyuki Shimada, Hiroshi Adachi
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Patent number: 5322962Abstract: Disclosed are a novel aromatic diamine; a polymide comprising 1,3-bis(3-aminobenzoyl)benzene or 4,4'-bis(3-aminobenzoyl)biphenyl as a diamine component and having recurring structural units represented by the formula (III): ##STR1## wherein R is a tetravalent radical selected from the group consisting of an aliphatic radical having from 2 to 27 carbon atoms, alicyclic radical, monoaromatic radical, condensed polyaromatic radical, and noncondensed aromatic radical connected each other with a direct bond or a bridge member, and X is a divalent radical of ##STR2## and a polyimide having a terminal aromatic group which is essentially unsubstituted or substituted with a radical having no reactivity with amines or dicarboxylic acid anhydrides or a composition comprising said polyimide.Type: GrantFiled: May 12, 1993Date of Patent: June 21, 1994Assignee: Mitsui Toatsu Chemicals, Inc.Inventors: Shoji Tamai, Keizaburo Yamaguchi, Yuko Ishihara, Saburo Kawashima, Hideaki Oikawa, Toshiyuki Kataoka, Akihiro Yamaguchi
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Patent number: 5298661Abstract: Charge transporting materials having general formula (I): ##STR1## R.sup.1 represents hydrogen; an unsubstituted or substituted alkyl group; an alkoxyl group having 1 to 4 carbon atoms; a thioalkoxyl group having 1 to 4 carbon atoms; an aryloxy group; an aralkyl group; a nitro group; an unsubstituted or substituted aryl group; a halogen; an amino group; an unsubstituted or substituted dialkylamino group; R.sup.2 represents hydrogen; an unsubstituted or substituted alkyl group; an alkoxyl group having 1 to 4 carbon atoms; or a halogen; R.sup.3 represents hydrogen; an alkyl group having 1 to 4 carbon atoms; an alkoxyl group having 1 to 4 carbon atoms; a halogen; a dialkylamino group; an amino group; a thioalkoxyl group having 1 to 4 carbon atoms; an aryloxy group; a methylenedioxy group; an aralkyl group; or an unsubstituted or substituted aryl group; R.sup.Type: GrantFiled: June 18, 1993Date of Patent: March 29, 1994Assignee: Ricoh Company, Ltd.Inventors: Tomoyuki Shimada, Masaomi Sasaki, Tamotsu Aruga
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Patent number: 5294732Abstract: The present invention is directed to polysubstituted fullerene moieties having a plurality of substituents thereon wherein the substituents are selected from the group consisting of hydroxy in combination with hydroxy, amino, oxide, nitro, organocarboxy, amide and mixtures thereof.Type: GrantFiled: December 23, 1992Date of Patent: March 15, 1994Assignee: Exxon Research & Engineering Co.Inventors: Long Y. Chiang, Ravindra B. Upasanti, John W. Swirczewski
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Patent number: 5250733Abstract: Benzylideneindene compounds, which are useful not only as the photoconductive material for electrophotography, but also as a charge transporting material employed in a function-separating type photoconductor in which an organic or inorganic pigment is used as a charge generating material, and an electrophotographic photoconductor containing at least one of the above benzylideneindene compounds in a photoconductive layer thereof, are disclosed.Type: GrantFiled: February 19, 1992Date of Patent: October 5, 1993Assignee: Ricoh Company, Ltd.Inventors: Tamotsu Aruga, Masaomi Sasaki, Mitsuru Hashimoto
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Patent number: 5248686Abstract: The invention relates to substituted arylamines and heteroarylamines, their preparation process and the pharmaceutical composition containing them. Said substituted amine is in accordance with the formula: ##STR1## in which R.sup.1 and R.sup.2 are optionally substituted alkyl radicals or form with N an optionally substituted piperazine or piperidine cycle, R.sup.3 and R.sup.4 represent a hydrogen atom or an organic radical, Y represents CR.sup.6 or N and R.sup.5 is an optionally substituted benzothiophenyl, benzofuranyl or naphthyl radical.These amines can be used in pharmaceutical compositions for the treatment of nervous depression or for stimulating vigilance.Type: GrantFiled: May 12, 1992Date of Patent: September 28, 1993Assignee: Centre National de la Recherche ScientifiqueInventors: Jean-Marc Kamenka, Alain Privat, Robert Chicheportiche, Jean Costentin
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Patent number: 5248699Abstract: This invention relates to a novel crystalline polymorphic form of sertraline hydrochloride, (1S-cis)-4-(3,4-dichlorophenyl)-1,2,3,4 -tetrahydro-N-methyl-1-naphthalenamine hydrochloride, and to a method for preparing it.Type: GrantFiled: August 13, 1992Date of Patent: September 28, 1993Assignee: Pfizer Inc.Inventors: Robert J. Sysko, Douglas J. M. Allen
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Patent number: 5232915Abstract: 9.alpha.-Hydroxy-19,11.beta.-bridged steroids of general formula I ##STR1## are described. The more detailed meaning of A, B, R.sup.1, R.sup.2, G, Z, R.sup.4 --Y and R.sup.4' --Y' follows from the description. The steroids of general formula I have antigestagen and/or antiglucocorticoidal action and can be used for the production of pharmaceutical agents.Type: GrantFiled: January 14, 1992Date of Patent: August 3, 1993Assignee: Schering AktiengesellschaftInventors: Eckhard Ottow, Gunter Neef, Rudolf Wiechert, Walter Elger, Sybille Beier, Karl-Heinrich Fritzemeier
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Patent number: 5233090Abstract: [2,2]paracyclophane compounds having formula (I): ##STR1## wherein R.sup.1 and R.sup.2 independently represent an alkyl group having 1 to 4 carbon atoms, which may have a substituent, or an aryl group which may have a substituent, provided that R.sup.1 and R.sup.2 may not be a methyl group at the same time, and methods of producing the same are disclosed. These compounds are useful as an effective photoconductive component for an electrophotographic photoconductor which is composed of an electroconductive support and a photoconductive layer formed thereon.Type: GrantFiled: November 6, 1991Date of Patent: August 3, 1993Assignee: Ricoh Company, Ltd.Inventors: Tomoyuki Shimada, Masaomi Sasaki, Tamotsu Aruga
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Patent number: 5228898Abstract: This invention relates to substituted bicycloheptadione derivatives with high herbicidal activity which are represented by general formula (I) ##STR1## (where R.sup.1 is a lower alkyl group, a phenyl group which may be substituted, an aralkyl group which may be substituted, or a heterocyclic group which may be substituted;R.sup.2 is, same or different, a halogen, an alkoxy group, an alkylthio group, an alkylsulfonyl group, an alkyl group, an alkoxyalkyl group, or an alkoxylcarbonyl group, and n is 0 to 4;R.sup.3 and R.sup.4 are, same or different, hydrogen or a lower alkyl group).Type: GrantFiled: February 3, 1992Date of Patent: July 20, 1993Assignee: Nippon Soda Co., Ltd.Inventors: Akiyoshi Ueda, Shigemi Suga, Hiroyuki Adachi, Toshio Aihara, Kazuyuki Tomida, Hideki Yamagishi, Hideo Hosaka
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Patent number: 5225595Abstract: Sulfonyl compounds of the formula ##STR1## where Ar is the radical of a benzene or naphthalene ring,R.sup.1 and R.sup.2 are each hydrogen, substituted or unsubstituted C.sub.1 -C.sub.4 -alkyl, substituted or unsubstituted phenyl, C.sub.1 -C.sub.4 -alkoxy, carboxyl, C.sub.1 -C.sub.4 -alkoxycarbonyl, cyano, halogen or hydroxysulfonyl,R.sup.3 is nitro, amino, C.sub.1 -C.sub.4 -alkanoylamino or benzoylamino, andR.sup.4 is a radical of the formula ##STR2## where X.sup.1, X.sup.2 and X.sup.3 are each hydrogen, substituted or unsubstituted C.sub.1 -C.sub.4 -alkyl or substituted or unsubstituted phenyl, andX.sup.4 is a group which is detachable under alkaline conditions,either in the free form or in the form of their salts, are useful for synthesizing reactive dyes.Type: GrantFiled: November 4, 1992Date of Patent: July 6, 1993Assignee: BASF AktiengesellschaftInventors: Bernd Siegel, Claus Marschner, Manfred Patsch
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Patent number: 5202486Abstract: Tetrahydronaphthaleneamine derivatives having the formula ##STR1## wherein R, R', R.sub.1 and R.sub.2 are as defined herein, are novel calcium channel blockers.Type: GrantFiled: July 31, 1990Date of Patent: April 13, 1993Assignee: E. R. Squibb & Sons, Inc.Inventors: Joel C. Barrish, Steven H. Spergel
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Patent number: 5198134Abstract: N-Allyl and N-methylene-thio substituted naphthalene-1,8- or -1,5-diamine compounds are very effective antioxidant stabilizers for organic material subject to oxidative or thermal degradation, particularly for lubricant compositions.Type: GrantFiled: October 28, 1991Date of Patent: March 30, 1993Assignee: Ciba-Geigy CorporationInventors: David H. Steinberg, John J. Luzzi
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Patent number: 5196583Abstract: The invention provides a novel class of propargyl compounds represented by the formula: ##STR1## wherein R is an C.sub.1 -C.sub.20 alkyl group, C.sub.1 -C.sub.20 alkylene group, C.sub.1 -C.sub.20 alkylene group interrupted by --NH-- group(s), C.sub.6 -C.sub.7 alicyclic group and an aromatic group; R.sub.1 comprises 1-100% --CH.sub.2 --C.tbd.CH group and 99-0% hydrogen atom and n is an integer of 1 to 4, and preparation thereof.These compounds are useful as coating material or sealer or rim-injection molding material.Type: GrantFiled: December 4, 1990Date of Patent: March 23, 1993Assignee: Nippon Paint Co., Ltd.Inventors: Mitsuo Yamada, Kei Aoki
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Patent number: 5177248Abstract: The present invention is directed toward the preparation of novel polysubstituted fullerenes. The method of forming polysubstituted fullerenes comprises contacting a fullerene with an electrophilic reagent selected from the group consisting of nitronium ion and organic peracid, provided that when the electrophilic reagent is nitronium ion, the fullerene is subsequently contacted with a nucleophilic reagent.Type: GrantFiled: October 28, 1991Date of Patent: January 5, 1993Assignee: Exxon Research and Engineering CompanyInventors: Long Y. Chiang, Ravindra B. Upasani, John W. Swirczewski
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Patent number: 5153228Abstract: 9-Amino-2-phenylbicyclo-[3.3.1]nonanes and 9-amino-2-phenylbicyclo[3.3.1]non-2-enes of the formula I ##STR1## where R.sup.1 and R.sup.2 are identical or different and each is hydrogen, halogen, alkyl, alkoxy, dialkylamino, trifluoromethyl, hydroxyl, alkylthio, alkylsulfonyl or nitro, R.sup.3 and R.sup.4 are identical or different and each is hydrogen, alkyl or 1 to 5 or alkenyl or alkynyl of 2 to 5 carbon atoms, or benzyl, it also being possible for R.sup.3 and R.sup.4 together to form a saturated chain which contains from three to seven carbon atoms and can be substituted by phenyl, and where is a single or double bond, are used for producing drugs which act, in particular, on the central nervous system.Type: GrantFiled: June 11, 1991Date of Patent: October 6, 1992Assignee: BASF AktiengesellschaftInventors: Rainer Schlecker, Hans P. Hofmann, Laszlo Szabo
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Patent number: 5132313Abstract: The present invention relates to novel NMDA receptor antagonists and methods for their use. The present invention also provided pharmaceutical compositions comprising such NMDA receptor antagonists.Type: GrantFiled: October 26, 1989Date of Patent: July 21, 1992Assignee: University of PittsburghInventors: Alan P. Kozikowski, Yuan-Ping Pang
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Patent number: 5124483Abstract: Aromatic diamines, such as toluenediamine, are alkylated in the ortho position by heating the diamine in the presence of an aluminum alloy, aluminium chloride and, optionally, zinc, and then reacting with an alkene at elevated temperatures and pressures.Type: GrantFiled: September 13, 1990Date of Patent: June 23, 1992Assignee: The Dow Chemical CompanyInventors: Guo-shuh J. Lee, V. Rao Durvasula, George E. Hartwell, Kirk D. Anderson, Louis N. Moreno, Nirad N. Shah
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Patent number: 5116865Abstract: 15,16-Seco-19-nor progestins are provided which display elevated progestational activity with a minimum of ancillary hormonal activity. Processes for the preparation of the novel progestins are provided as are methods of use. A preferred method of use is in the suppression of ovulation in the human female.Type: GrantFiled: January 28, 1991Date of Patent: May 26, 1992Inventors: Richard H. Peters, Masato Tanabe
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Patent number: 5082970Abstract: A novel process for converting trans-isomeric N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthaleneamine to cis-isomeric N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthaleneamine is disclosed. The process involves contacting trans-isomeric N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthaleneamine, or a mixture of same with up to about an equal part by weight of the corresponding cis-isomer, with a basic equilibration agent like potassium tert.-butoxide in a reaction-inert polar organic solvent to ultimately afford a cis/trans-mixture wherein the amount of cis-amine present in said mixture achieves a constant value of about 2:1 on a weight-by-weight basis. The aforesaid resultant mixture is useful as an intermediate product that ultimately leads to pure cis-(1S) (4S)-N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthaleneamine (sertraline), which is a known antidepressant agent.Type: GrantFiled: March 6, 1991Date of Patent: January 21, 1992Assignee: Pfizer Inc.Inventor: Tamim F. Braish
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Patent number: 5068435Abstract: This invention relates to a process for producing ring alkylated aromatic amines. In the process an aromatic amine is reacted with an olefin using gamma alumina as a catalyst. Under the conditions of the process the catalyst is extremely active and with amines that are capable of alkylation at the ortho and para positions, high selectivity to the ortho alkylated isomer can be achieved.The catalyst is also effective for producing unsymmetrical disubstituted alkyl aromatic amines, e.g., ethyl or propyl toluidine where one ortho position is substituted with a methyl group and the other substituted with an ethyl or propyl group.Type: GrantFiled: March 25, 1988Date of Patent: November 26, 1991Assignee: Air Products and Chemicals, Inc.Inventors: William F. Burgoyne, Jr., Dale D. Dixon
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Patent number: 5047590Abstract: Compounds having formula (I), which are useful as starting or intermediate materials for preparing organic photoconductive materials, or as organic photoconductive materials: ##STR1## wherein R.sup.1 is a nitro group, an amino group or a diphenylamino group which may have a substituent; and R.sup.2 is hydrogen or an alkyl group having 1 to 6 carbon atoms, and methods of preparing the above compounds are disclosed.Type: GrantFiled: May 29, 1990Date of Patent: September 10, 1991Assignee: Ricoh Company, Ltd.Inventors: Tomoyuki Shimada, Masaomi Sasaki, Tamotsu Aruga
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Patent number: 4999441Abstract: Tetrakis(dialkylamino)aromatics Ia to Ic ##STR1## where the radicals A may be identical or different and are n-C.sub.1 -C.sub.6 -alkyl and the radicals R may be identical or different and are hydrogen or C.sub.1 -C.sub.6 -alkyl, and their charge transfer complexes with electron acceptors, and the preparation of Ia to Ic from the corresponding N-unsubstituted amines by alkylation with A'--CHO (where A'.dbd.H or N-C.sub.1 -C.sub.5 -alkyl) and reduction with NaBH.sub.3 CN.The charge transfer complexes of Ia and Ic are used to prepare electrically conductive polymers.Type: GrantFiled: April 17, 1989Date of Patent: March 12, 1991Assignee: Max-Planck-Gesellschaft zur Foerderung der Wissenschaften e.V.Inventors: Heinz A. Staab, Karin Elbl
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Patent number: 4996316Abstract: A process for the preparation of tertiary N,N-dimethylamines by the reaction of primary amines, formaldehyde, and hydrogen under pressure and at elevated temperature in the presence of a nickel-containing hydrogenation catalyst in the liquid phase. The hydrogenation catalyst is suspended in a solvent, the nickel concentration is 0.1 to 10% by weight, based on the primary amine. The starting materials are separate from each other, brought to 80.degree. to 150.degree. C. and 1 to 15 MPa and fed into the catalyst suspension simultaneously with stirring and reacted in one step to form the tertiary N,N-dimethylamines.Type: GrantFiled: December 24, 1988Date of Patent: February 26, 1991Assignee: Hoechst AktiengesellschaftInventors: Jurgen Weber, Detlef Kampmann, Claus Kniep
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Patent number: 4992563Abstract: This invention relates to several intermediates useful in preparing thromboxane A.sub.2 inhibiting (.+-.)7-[3.alpha.-[1-[[(phenylamino)-thioxomethyl]hydrazono]ethyl]-1.alpha ., 4.alpha.-bicyclo[2.2.1]hept-2.beta.-yl]-heptenoic acids and useful derivatives thereof from (.+-.)octahydro-1.alpha.-methyl-3a.alpha., 7a.alpha.-4.alpha.,7.alpha.-methano-2H-inden-2-ones.Type: GrantFiled: December 13, 1988Date of Patent: February 12, 1991Assignee: National Research Development CorporationInventors: Robert B. Garland, Masateru Miyano
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Patent number: 4978386Abstract: 2-(3-substituted phenyl)-3-amino-2-cyclopentenone derivatives. The compounds generally exhibit both pre-emergence and post-emergence phytotoxicity and are useful as herbicides and also at low dosages as plant growth regulating agents.Type: GrantFiled: October 31, 1985Date of Patent: December 18, 1990Assignee: Chevron Research CompanyInventor: Carl E. Ward
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Patent number: 4978789Abstract: A process for producing an alkenyl substituted aromatic compound having the general formula (I): ##STR1## wherein Ar represents an aromatic ring, R.sup.1 represents an alkenyl group having 2 to 8 carbon atoms, p is 1, 2, or 3 provided that R.sup.1 may be the same or different when p is 2 or 3, R.sup.2 represents an alkyl group having 1 to 8 carbon atoms, q is 0, 1, or 2 provided that R.sup.2 may be the same or different when q is 2, X represents --OH or --NR.sup.3 R.sup.4 wherein R.sup.3 and R.sup.4 independently represent hydrogen or an alkyl group having 1 to 2 carbon atoms, n is 1 or 2, provided that the sum of p and q is 1, 2, or 3 comprising the step of catalytically dehydrogenating an alkyl substituted aromatic compound having the general formula (III): ##STR2## wherein R.sup.5 represents an alkyl group having 2 to 8 carbon atoms and Ar, R.sup.2, X, p, q, and n are the same as defined above, n is 1 or 2, provided that R.sup.Type: GrantFiled: July 10, 1989Date of Patent: December 18, 1990Inventors: Katsuo Taniguchi, Shigeki Fujikawa, Yoshito Kurano
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Patent number: 4960815Type: GrantFiled: January 17, 1990Date of Patent: October 2, 1990Assignee: Warner-Lambert CompanyInventor: Walter H. Moos
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Patent number: 4921526Abstract: Substituted benzoyl-bicycloalkyl-1,1,3-diones and related compounds, intermediates therefor, synthesis thereof, and the use of said diones for the control of weeds.Type: GrantFiled: November 27, 1987Date of Patent: May 1, 1990Assignee: Sandoz Ltd.Inventors: Shy-Fuh Lee, Gary W. Luehr, Carol R. Scott, Werner Trueb
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Patent number: 4906662Abstract: Disclosed are phenol derivatives of the formula ##STR1## wherein R.sup.1 is a substituted phenyl group, R.sup.2 and R.sup.3 are C.sub.1 -C.sub.6 alkyl group and of the formula ##STR2## wherein R.sup.8, R.sup.9 and R.sup.10 are C.sub.1 -C.sub.6 alkyl and the like and A is H, C.sub.1 -C.sub.6 alkylsulfonyl and the like substituents. These compounds and some related compounds have anti-inflammatory activity and lipoxygenase inhibitory activity.Type: GrantFiled: January 27, 1987Date of Patent: March 6, 1990Assignee: Otsuka Pharmaceutical Factory, Inc.Inventors: Kinji Hashimoto, Kiyoto Goto, Ken-ichi Kanai, Yoshiaki Tsuda
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Patent number: 4880802Abstract: For treatment of disorders of the central nervous system, the cardiovascular system or the intestinal tract, the new substituted basic 2-aminotetralins of the formula ##STR1## in which R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen, alkyl or acyl, andR.sup.3 represents quinuclidine or a group of the formula --(CH.sub.2).sub.a --R.sup.4, --CH.sub.2 --CH.dbd.CH--(CH.sub.2).sub.b --R.sup.4, --CH.sub.2 --C.tbd.(CH.sub.2).sub.b --R.sup.4, ##STR2## wherein a denotes a number from 1 to 10,b denotes a number 0, 1, 2, 3 or 4,d denotes a number 2 or 3, andX denotes oxygen, sulphur, or NR.sup.5,and their salts.Type: GrantFiled: December 8, 1987Date of Patent: November 14, 1989Assignee: Bayer AktiengesellschaftInventors: Rudolf Schohe, Thomas Glaser, Jorg Traber, George S. Allen
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Patent number: 4866208Abstract: Novel meta phenylenediamines are provided having one or two particular benzyl radicals as substituents along with other optional substituents on the aromatic diamine ring and optionally substituents on the benzyl aromatic ring.The diamines are sterically hindered and thereby have lower amine reactivity as compared with the unsubstituted diamines.The diamines are useful as curing agents for epoxy resins and find particular utility as extenders in the formation of novel polyurethane-polyurea polymers.Type: GrantFiled: August 15, 1988Date of Patent: September 12, 1989Assignee: The Dow Chemical CompanyInventor: Kwok K. Sun
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Patent number: 4835224Abstract: Polyamines are produced by hydrolyzing an isocyanate compound in the presence of at least one of a selected group of catalysts and a water miscible polar organic solvent in substantially homogeneous phase at 40.degree.-170.degree. C. The catalyst employed is selected from potassium hydroxide, rubidium hydroxide, cesium hydroxide, potassium alcoholates, rubidium alcoholates, cesium alcoholates, potassium carboxylates, rubidium carboxylates and cesium carboxylates. These polyamines are useful in the production of polyurethane(urea)s.Type: GrantFiled: March 24, 1988Date of Patent: May 30, 1989Assignee: Bayer AktiengesellschaftInventors: Andreas Ruckes, Werner Rasshofer, Klaus Konig, Richard Kopp
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Patent number: 4806687Abstract: Ortho-alkylanilines are prepared by catalytic hydrodesulfurization of ortho-aminobenzyl sulfides using a cobalt-molybdenum oxide catalyst. For example, 2-methyl-6-trifluoromethylaniline is prepared by catalytic hydrodesulfurization of 3-trifluoromethyl-2-aminobenzyl sulfides. The substituted anilines prepared by the method of this invention are useful as intermediates in the synthesis of compounds shown to have herbicidal activity.Type: GrantFiled: September 30, 1987Date of Patent: February 21, 1989Assignee: Monsanto CompanyInventors: Terry M. Balthazor, Samuel J. Tremont