Ring Nitrogen Is Shared By Two Cyclos Patents (Class 544/282)
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Patent number: 6057325Abstract: This invention concerns the compounds of formula ##STR1## the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Alk is C.sub.1-6 alkanediyl; R.sup.1 is hydrogen, C.sub.1-6 alkyl, aryl or aryl C.sub.1-6 alkyl; R.sup.2, R.sup.3 and R.sup.4 are each independently selected from hydrogen, halo, hydroxy, nitro, cyano, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, trifluoromethyl, C.sub.1-6 alkylthio, mercapto, amino, mono- and di(C.sub.1-6 alkyl)amino, carboxyl, C.sub.1-6 alkyloxycarbonyl or C.sub.1-6 alkylcarbonyl; R.sup.5 is hydrogen, C.sub.1-6 alkyl, phenyl or phenylC.sub.1-6 alkyl; R.sup.6 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylthio, or a radical of formula --NR.sup.8 R.sup.9, wherein R.sup.8 and R.sup.9 are each independently selected from hydrogen, C.sub.1-6 alkyl, phenyl or phenylC.sub.1-6 alkyl; R.sup.7 is hydrogen or C.sub.1-6 alkyl; or R.sup.6 and R.sup.7 taken together may form a bivalent radical of formula --R.sup.6 --R.sup.Type: GrantFiled: November 9, 1998Date of Patent: May 2, 2000Assignee: Janssen Pharmaceutia, N.V.Inventors: Ludo Edmond Josephine Kennis, Josephus Carolus Mertens
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Patent number: 6028073Abstract: N-substitued 3-azabicyclo[3.2.0]heptane derivatives of formula (I) ##STR1## in which R.sup.1, R.sup.2, A, X, Y and Z have the meanings given in the description, their method of preparation and their use as pharmacological agents.Type: GrantFiled: September 18, 1998Date of Patent: February 22, 2000Assignee: BASF AktiengesellschaftInventors: Gerd Steiner, Rainer Munschauer, Thomas Hoger, Liliane Unger, Hans-Jurgen Teschendorf
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Patent number: 5998333Abstract: Pyrimidinone derivatives of the general formula: ##STR1## wherein R.sup.1 is hydrogen or alkyl; R.sup.2 is haloalkyl; R.sup.3 is nitrogen or CH; G is optionally substituted ethylene, trimethylene, or vinylene; and Q is selected from several heterocyclic-condensed phenyl groups, are useful as the active ingredients of herbicides because of their excellent herbicidal activity.Type: GrantFiled: September 4, 1998Date of Patent: December 7, 1999Assignee: Sumitomo Chemical Company, Ltd.Inventors: Takashi Komori, Hisayuki Hoshi
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Patent number: 5939415Abstract: The present invention relates to heterocyclic compounds with the formula ##STR1## in which R.sup.1 to R.sup.7, B, a, and X have the meanings indicated in the specification. These compounds can be used for the treatment of diseases of the rheumatic variety and for the prevention of allergically-induced diseases.Type: GrantFiled: March 28, 1997Date of Patent: August 17, 1999Assignee: Merckle GmbHInventors: Stefan Laufer, Hans Gunther Striegel, Gerd Dannhardt
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Patent number: 5922869Abstract: The process for the preparation of bicyclic amidines of the general formula: ##STR1## wherein A is selected from the group consisting of --CR.sup.1 R.sup.2 --CR.sup.3 R.sup.4 --CR.sup.5 R.sup.6 --, --CR.sup.1 R.sup.2 --CR.sup.3 R.sup.4 --CR.sup.5 R.sup.6 --CR.sup.7 R.sup.8 -- and --CR.sup.1 R.sup.2 --CR.sup.3 R.sup.4 --CR.sup.5 R.sup.6 --CR.sup.7 R.sup.8 --CR.sup.9 R.sup.10 --, wherein the substituents in A are in each case numbered starting from the nitrogen atom, and B is selected from the group consisting of --CR.sup.11 R.sup.12 --CR.sup.13 R.sup.14 --, --CR.sup.11 R.sup.12 --CR.sup.15 R.sup.16 --CR.sup.13 R.sup.14 -- and --CR.sup.11 R.sup.12 --CR.sup.15 R.sup.16 --CR.sup.17 R.sup.18 --CR.sup.13 R.sup.14 --, and R.sup.1, R.sup.2 and R.sup.11 to R.sup.14 are, in each case independently of one another, hydrogen, C.sub.1 -C.sub.4 -alkyl, aryl, or are C.sub.1 -C.sub.4 -alkyl which is substituted with hydroxyl, amino, C.sub.1 -C.sub.4 -alkylamino or mercapto, and R.sup.3 to R.sup.10 and R.sup.15 to R.sup.Type: GrantFiled: October 3, 1997Date of Patent: July 13, 1999Assignee: Lonza Ltd.Inventors: Oleg Werbitzky, Ulrich Daum, Rachel Bregy
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Patent number: 5919788Abstract: The present invention concerns the compounds of formula ##STR1## the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein the dashed line designates an optional bond; R.sup.1 and R.sup.2 are each independently hydrogen, halogen, C.sub.1-6 alkyl or C.sub.1-6 alkyloxy; R.sup.3 and R.sup.4 are each independently hydrogen, C.sub.1-6 alkyl, phenyl or phenyl substituted with one, two or three substituents selected from halo, hydroxy, nitro, cyano, trifluoromethyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylthio, mercapto, amino, mono- and di(C.sub.1-6 alkyl)-amino, carboxyl, C.sub.1-6 alkyloxycarbonyl and C.sub.1-6 alkylcarbonyl; Alk is C.sub.1-4 alkanediyl; D is a pyrimidinone, piperidone or a benzimidozolidinone; having antipsychotic activity; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: June 27, 1997Date of Patent: July 6, 1999Assignee: Janssen Pharmaceutica, N.V.Inventors: Jan Vandenberk, Ludo Edmond Josephine Kennis, Josephus Carolus Mertens
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Patent number: 5908844Abstract: Compounds of the formula I ##STR1## where B, R.sup.1, R.sup.2, n, R.sup.3, A, X, Y and Z have the meanings stated in the description, and their preparation are described. The novel ompounds are suitable for controlling diseases.Type: GrantFiled: May 6, 1996Date of Patent: June 1, 1999Assignee: BASF AktiengesellschaftInventors: Gerd Steiner, Rainer Munschauer, Liliane Unger, Hans-Jurgen Teschendorf, Thomas Hoger
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Patent number: 5854239Abstract: The present invention relates to diazabicyclic compounds and, specifically, to compounds of the formula ##STR1## wherein A, G, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 are as defined in the specification. The compounds of formula I are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.Type: GrantFiled: June 20, 1996Date of Patent: December 29, 1998Assignee: Pfizer Inc.Inventors: Harry R. Howard, Kevin D. Shenk
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Patent number: 5753664Abstract: A novel compound of the formula:A--Z--Ar.sup.1 1'CO--Ar.sup.2wherein A is a condensed pyrimidinone or condensed pyridazinone ring; Ar.sup.1 and Ar.sup.2 are independently a ring; Z is a divalent group, or a salt thereof which have an excellent antitumor activity.Type: GrantFiled: March 13, 1996Date of Patent: May 19, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Tetsuya Aono, Shogo Marui, Fumio Itoh, Masuo Yamaoka, Masafumi Nakao
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Patent number: 5723605Abstract: The process for the preparation of bicyclic amidines of the general formula: ##STR1## wherein A is selected from the group consisting of --CR.sup.1 R.sup.2 --CR.sup.3 R.sup.4 --CR.sup.5 R.sup.6 --, --CR.sup.1 R.sup.2 --CR.sup.3 R.sup.4 --CR.sup.5 R.sup.6 --CR.sup.7 R.sup.8 -- and --CR.sup.1 R.sup.2 --CR.sup.3 R.sup.4 --CR.sup.5 R.sup.6 --CR.sup.7 R.sup.8 --CR.sup.9 R.sup.10 --, wherein the substituents in A are in each case numbered starting from the nitrogen atom, and B is selected from the group consisting of --CR.sup.11 R.sup.12 --CR.sup.13 R.sup.14 --, --CR.sup.11 R.sup.12 --CR.sup.15 R.sup.16 --CR.sup.13 R.sup.14 -- and --CR.sup.11 R.sup.12 --CR.sup.15 R.sup.16 --CR.sup.17 R.sup.18 --CR.sup.13 R.sup.14 --, and R.sup.1, R.sup.2 and R.sup.11 to R.sup.14 are, in each case independently of one another, hydrogen, C.sub.1 -C.sub.4 -alkyl, aryl, or are C.sub.1 -C.sub.4 -alkyl which is substituted with hydroxyl, amino, C.sub.1 -C.sub.4 -alkylamino or mercapto, and R.sup.3 to R.sup.10 and R.sup.15 to R.sup.Type: GrantFiled: November 10, 1994Date of Patent: March 3, 1998Assignee: Lonza Ltd.Inventors: Oleg Werbitzky, Ulrich Daum, Rachel Bregy
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Patent number: 5723410Abstract: This invention relates to certain herbicidal pyrrolesulfonylureas, compositions thereof and a method for their use as herbicides or plant growth regulants.Type: GrantFiled: August 2, 1996Date of Patent: March 3, 1998Assignee: E. I. du Pont de Nemours and CompanyInventors: William Thomas Zimmerman, Bruce Anthony Lockett, John Cuomo
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Patent number: 5688799Abstract: The present invention is concerned with novel compounds having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof and the stereochemically isomeric forms thereof, whereinAlk represents C.sub.1-4 alkanediyl;D is a bicyclic heterocycle of formula ##STR2## wherein each R.sup.1 independently is C.sub.2-6 alkenyl; C.sub.2-6 alkynyl; C.sub.3-6 cycloalkyl optionally substituted with C.sub.1-4 alkyl; C.sub.1-19 alkyl optionally substituted with C.sub.3-6 cycloalkyl, halo, C.sub.1-6 alkyloxy or cyano; and each R.sup.2 independently is hydrogen or C.sub.1-4 alkyl. Novel compounds; compositions; processes for preparing novel compounds and intermediates are described.Type: GrantFiled: March 3, 1996Date of Patent: November 18, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Jan Vandenberk, Ludo Edmond Josephine Kennis
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Process for the manufacture of 5-dichloroacetyl-3,3,6-trimethyl-9-oxo-1,5-diazabicyclo?4.3.0! nonane
Patent number: 5677452Abstract: The manufacture of 5-dichloroacetyl-3,3,6-trimethyl-9-oxo-1,5-diazabicyclo?4.3.0!-nonane I by the reaction of 3,3,6-trimethyl-9-oxo-1,5-diaza-bicyclo?4.3.0!nonane II with dichloroacetyl chloride in the presence of a solvent and a base, whereina) this reaction is carried out in a two-phase system comprising a virtually water-insoluble organic solvent and water, and sodium or potassium hydroxide acting as the base is metered in at a rate corresponding to the rate of consumption of the dichloroacetyl chloride such that the aqueous phase exhibits a pH of from 7 to 9, andb) the resulting product is separated.Type: GrantFiled: October 24, 1996Date of Patent: October 14, 1997Assignee: BASF AktiengesellschaftInventors: Gernot Reissenweber, Winfried Richarz, Knut Koob -
Patent number: 5661107Abstract: Compounds of the formula ##STR1## wherein m represents 1 or 2, X represents O, S, CH.sub.2 or substituted CH.sub.2, R.sub.1 -R.sub.4 represent hydrogen or substituted or unsubstituted hydrocarbon groups, and Q represents a substituted phenyl group. These compounds are useful as herbicides and are active in small doses with high selectivity between useful plants and weeds.Type: GrantFiled: April 13, 1995Date of Patent: August 26, 1997Assignee: Degussa AktiengesellschaftInventors: Matthias Schafer, Karlheinz Drauz
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Patent number: 5658916Abstract: The agent is the compound 3-{2-[4-(6-fluoro-benzo[d]isoxazol-3-yl)-3,6-dihydro-2H-pyridin-1-yl]-ethy l}-2-methyl-6,7,8,9-tetrahydropyrido [1,2-a]pyrimidin-4-one having the formula (I) ##STR1## and pharmaceutically acceptable salts thereof; the process is based on the reduction of a selected pyridin salt by means of a metal borohydride; its preferred application is as an antipsychotic agent.Type: GrantFiled: October 12, 1995Date of Patent: August 19, 1997Assignee: Vita-Invest, S.A.Inventors: Jose Maria Caldero Ges, Joan Huguet Clotet, Francisco Marquillas Olondriz, Pere Dalmases Barjoan, Anna Bosch Rovira, Joan Roca Acin, Juan Carlos Del Castillo Nieto
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Patent number: 5622956Abstract: Nitro-substituted heterocyclic compounds of the formula (I) ##STR1## wherein R is hydrogen or alkyl,Z is an optionally substituted aryl or optionally substituted heterocyclic group containing at least one atom selected from N, O and S,A is optionally substituted ethylene or optionally substituted trimethylene, andB stands for 2 or 3 members of a heterocyclic ring which is formed, together with the adjacent C-atom and N-atom and at least one of said members may represent a hetero atom and may be optionally substituted, provided that when B stands for 3 members, two of which are carbon atoms and the other one is a nitrogen atom which is located in the middle of the three members, then at least one of said two carbon atoms must be substituted by a keto group. Such compounds being useful as insecticides.Type: GrantFiled: June 5, 1995Date of Patent: April 22, 1997Assignee: Nihon Bayer Agrochem K.K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shoko Sasaki, Koichi Moriya, Yumi Hattori, Katsuhiko Shibuya
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Patent number: 5614469Abstract: Substituted N-pyridinyl[1,2,4]triazolo[1,5-c]-pyrimidine-2-sulfonamide compounds, such as N-(2-fluoro-4-methyl)-7-fluoro-5-methoxy[1,2,4]triazolo[1,5-c]pyrimidine-2 -sulfonamide, were prepared bycondensation of a 2-chlorosulfonyl[1,2,4]triazolo[1,5-c]pyrimidine compound, such as 2-chlorosulfonyl-7-fluoro-5-methoxy[1,2,4]triazolo[1,5-c]pyrimidine, with a substituted 3-aminopyridine compound, such as 3-amino-2-fluoro-4-methylpyridine, and found to possess herbicidal utility.Type: GrantFiled: June 6, 1995Date of Patent: March 25, 1997Assignee: DowElancoInventors: Kim E. Arndt, William A. Kleschick, Walter Reifschneider, Beth A. Swisher, Robert J. Ehr, John J. Jachetta, John C. Van Heertum
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Patent number: 5612346Abstract: A compound which is a pamoate acid addition salt of risperidone, compositions comprising the same and processes for preparing said compound and compositions.Type: GrantFiled: September 22, 1995Date of Patent: March 18, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Jean L. Mesens, Jozef Peeters
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Patent number: 5610157Abstract: N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives, their N-oxide forms and pharmaceutically acceptable salts having gastrointestinal motility stimulating properties, compositions containing these compounds as active ingredient and methods of treating warm-blooded animals suffering from the decreased peristalsis of the gastrointestinal system.Type: GrantFiled: April 13, 1995Date of Patent: March 11, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Georges H. P. Van Daele, Frans M. A. Van den Keybus
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Patent number: 5599815Abstract: Compounds represented by the formula (I) and pharmacologically acceptable salts thereof: ##STR1## These compounds have little extrapyramidal effect and thus are effective as an anti-psychotic agent having few side effects.Type: GrantFiled: December 20, 1994Date of Patent: February 4, 1997Assignee: Meiji Seika Kabushiki KaishaInventors: Yoshimasa Fukuda, Toshiro Sasaki, Yuuko Nakatani, Yasuyuki Ichimaru, Taiichiro Imanishi
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Patent number: 5576432Abstract: A process of preparing a dihydropyrimidine compound of the structure (I): ##STR1## wherein R.sup.1 and R.sup.2 are bonded together to form an aromatic or heterocyclic ring, which may be substituted or unsubstituted, or are individually selected from the group consisting of hydrogen, or a substituted or unsubstituted aliphatic, carbocyclic, or heterocyclic group;R.sup.3, R.sup.4 and R.sup.5 are individually selected from the group consisting of hydrogen or a substituted or unsubstituted aliphatic, carbocyclic or heterocyclic group; andX represents the atoms necessary to form a 5 or 6 membered heterocyclic ring, and is selected from the group consisting of oxygen, sulfur, selenium, ##STR2## wherein R.sup.6, R.sup.7, and R.sup.8 are individually selected from the group consisting of a substituted or unsubstituted aliphatic, carbocyclic or heterocyclic group; comprising combining a compound (A) of the structure: ##STR3## wherein X, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, and R.sup.Type: GrantFiled: December 23, 1994Date of Patent: November 19, 1996Assignee: Eastman Kodak CompanyInventors: Roger Lok, Antony J. Williams
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Patent number: 5532243Abstract: There are provided nitrogen-containing bicyclic compounds, pharmaceutical compositions containing these compounds and methods of using these compounds to treat physiological or drug-induced psychosis or diskinesia in a mammal.Type: GrantFiled: February 14, 1992Date of Patent: July 2, 1996Assignee: The DuPont Merck Pharmaceutical CompanyInventor: Paul J. Gilligan
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Patent number: 5512576Abstract: 2-Substituted 1,2,5-thiadiazolidin-3-one 1,1-dioxides, pharmaceutical compositions containing them and methods for the treatment of degenerative diseases utilizing them.Type: GrantFiled: December 2, 1994Date of Patent: April 30, 1996Assignee: Sterling Winthrop Inc.Inventors: Ranjit C. Desai, Dennis J. Hlasta
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Patent number: 5482943Abstract: Novel 2,9-disubstituted-4H-pyrido[1,2-a]pyrimidin-4-ones having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, whereinAlk represents C.sub.1-4 alkanediyl,D is a bicyclic heterocycle of formula ##STR2## wherein R.sup.1 represents C.sub.1-4 alkyl, hydroxyC.sub.1-4 alkyl, carboxaldehyde, carboxyl, C.sub.1-10 alkylcarbonyloxyC.sub.1-4 alkyl; each R.sup.2 represents hydrogen or C.sub.1-4 alkyl; R.sup.3 represents C.sub.1-4 alkyl, hydroxyC.sub.1-4 alkyl or methyl substituted with phenyl, 5-methyl-2-furanyl or 3-pyridinyl; and R.sup.4 represents C.sub.1-3 alkyl, phenyl, 5-methyl-2-furanyl or 3-pyridinyl.Type: GrantFiled: March 28, 1991Date of Patent: January 9, 1996Assignee: Janssen Pharmaceutica N.V.Inventors: Ludo E. J. Kennis, Jan Vandenberk, Albertus H. M. T. Van Heertum
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Patent number: 5475105Abstract: Abstract of the Disclosure: Compounds of the formula I ##STR1## where R.sup.1, R.sup.2, n , R.sup.3, A, X, Y and Z have the meanings stated in the description, and the preparation thereof are described. The novel compounds are suitable for controlling diseases , i.e., as neuroleptics, antidepressants, sedatives, hypnotics, CNS protectives or muscle relaxants.Type: GrantFiled: December 16, 1994Date of Patent: December 12, 1995Assignee: BASF AktiengesellschaftInventors: Gerd Steiner, Liiane Unger, Berthold Behl, Hans-Juergen Teschendorf, Rainer Munschauer
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Patent number: 5475000Abstract: 4-oxo-4H-pyrido[1,2-a]-pyrimidines are disclosed of the formula ##STR1## wherein R is a C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-6 alkynyl, C.sub.3-7 cycloalkyl, --(CH.sub.2).sub.n --COOR.sup.3 wherein R.sup.3 is C.sub.1 to C.sub.4 alkyl and n is 0 or 1 or a C.sub.7-8 aralkyl group, optionally substituted by one or more halogen atom(s), or by a nitro-group, R.sup.1 is a hydrogen atom or a C.sub.1-4 alkyl group, and salts thereof, as well as a process for their preparation, and pharmaceutical compositions containing them. These compounds are therapeutically useful as gastroprotectives in the treatment and prevention of ulcer.Type: GrantFiled: February 10, 1994Date of Patent: December 12, 1995Assignee: Chinoin Gyogyszer-es Vegyeszeti Termekek Gyara Rt.Inventors: Istvan Hermecz, Jozsef Knoll, Judit Sipos, Klara Gyires, Agnes Horvath, Lelle Vasvari, Laszlo Tardos, Maria Balogh, Zoltan Kapui, Ilona Papp
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Patent number: 5466701Abstract: Compounds having the structural formula ##STR1## which inhibit the enzymatic activity of proteolytic enzymes, and processes for preparation thereof, method of use thereof in treatment of degenerative diseases and pharmaceutical compositions thereof are disclosed.Type: GrantFiled: June 22, 1994Date of Patent: November 14, 1995Assignee: Sterling Winthrop Inc.Inventors: Dennis J. Hlasta, James H. Ackerman, Albert J. Mura, Ranjit C. Desai
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Patent number: 5397767Abstract: A class of 6-arylpyrimidines which is useful in the control of weeds is of the general formulae: ##STR1## wherein R.sup.2 is selected from hydrogen, halo, substituted or unsubstituted alkyl, haloalkyl, polyhaloalkyl, haloalkenyl, polyhaloalkenyl, haloalkynyl, polyhaloalkynyl, alkenyl, alkynyl, alkoxy, alkylthio, alkoxycarbonylalkyl, cyano, alkoxyalkyl, alkoxycarbonyl, cycloalkyl, aralkyl, alkylamino, dialkylamino, or dialkylaminocarbonyl group; R.sup.3 is an alkyl, alkenyl, alkynyl, or haloalkyl group; R.sup.5 is an alkyl, alkenyl, alkynyl, alkenynyl, or alkoxyalkyl, group; R.sup.6 is an aryl group (e.g. aromatic ring); and X is oxygen or sulfur. R.sup.2 and R.sup.3 may form a fused ring.Type: GrantFiled: March 4, 1994Date of Patent: March 14, 1995Assignee: Rohm and Haas CompanyInventor: Colin M. Tice
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Patent number: 5387588Abstract: The present invention relates to novel 4-oxo-4H-pyrido[1,2-a]pyrimidine-3-carboxamide derivatives of the general formula (I) and the acid addition salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the general formula (I) ##STR1## R stands for a C.sub.1-12 alkyl group optionally substituted by a C.sub.1-4 alkoxycarbonyl group; a C.sub.3-9 cycloalkyl, adamantyl or optionally substituted phenyl group;R.sup.1 means hydrogen or a C.sub.1-4 alkyl group; orR and R.sup.1 together form a --(CH.sub.2).sub.n -- chain, wherein n is 4, 5 or 6;R.sup.2 stands for hydrogen, a C.sub.1-4 alkyl group or halogen;R.sup.3 represents hydrogen or a C.sub.1-4 alkyl group; andm is 0 or 1.The compounds of the general formula (I) possess a gastroprotective effect and are useful for the prevention and therapy of ulcers of the stomach and the small intestine.Type: GrantFiled: June 21, 1993Date of Patent: February 7, 1995Assignee: Chinoin Gyogyszer- es Vegyeszeti Termekek Gyara Rt.Inventors: Istvan Hermecz, Jozsef Knoll, Lelle Vasvari nee Debreczy, Klara Gyires, Judit Sipos, Agnes Horvath, Laszlo Tardos, Maria Blaogh
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Patent number: 5344933Abstract: An azomethine dye is disclosed, represented by the general formula (I), (II) or (III): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each independently represents a hydrogen atom or nonmetallic atom group; X represents --OH or --NR.sup.5 R.sup.6 ; R.sup.5 and R.sup.6 each independently represents a hydrogen atom, alkyl group, aryl group or heterocyclic group; R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11, R.sup.12 and R.sup.13 each independently represents a hydrogen atom or nonmetallic atom group; and R.sup.1 and R.sup.2, and/or R.sup.2 and R.sup.5, and/or R.sup.5 and R.sup.6, and/or R.sup.6 and R.sup.3, and/or R.sup.3 and R.sup.4, and/or R.sup.7 and R.sup.8, and/or R.sup.9 and R.sup.10, and/or R.sup.11 and R.sup.12, and/or R.sup.12 and R.sup.13 may be connected to each other to form a cyclic structure.Type: GrantFiled: September 10, 1992Date of Patent: September 6, 1994Assignee: Fuji Photo Film Co., Ltd.Inventors: Hisashi Mikoshiba, Katsuyoshi Yamakawa, Kozo Sato, Koushin Matsuoka
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Patent number: 5324729Abstract: Substituted pyrimidines, pyrimidinones and pyridopyrimidines of formula (I) are as angiotensin II antagonists useful in the treatment of hypertension, ocular hypertension and certain CNS ailments: ##STR1## wherein K is --N(R.sup.8a)--C(.dbd.M) or --N.dbd.C(R.sup.8b) where M is O or NR.sup.22.Type: GrantFiled: July 31, 1992Date of Patent: June 28, 1994Assignee: Merck & Co., Inc.Inventors: Eric E. Allen, William J. Greenlee, Malcolm MacCoss, Arthur A. Patchett
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Patent number: 5298658Abstract: A photographic element is detailed which provides for improved resolution by decreasing the blue and ultraviolet radiation typically associated with internal scatter and print-through. These and other improvements are provided in a photographic element comprising a support having thereon at least one hydrophilic colloid layer, and a radiation sensitive silver halide emulsion layer present as a portion of the colloid layer or in a separate layer wherein the emulsion contains a dye of the formula: ##STR1## wherein: A=counterion chosen from the set consisting of lithium, sodium, potassium, ammonium and alkylammonium andZ is a linking group.Type: GrantFiled: December 20, 1991Date of Patent: March 29, 1994Assignee: E. I. Du Pont de Nemours and CompanyInventor: Dietrich M. Fabricius
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Patent number: 5294619Abstract: A series of novel N-alkyl or oxyalkyl arylpiperidine derivatives have been prepared, including their pharmaceutically acceptable acid addition salts, wherein the N-alkyl or oxyalkyl side chain is further substituted by certain aryl or heterocyclic ring groups. These particular compounds are useful in therapy as neuroleptic agents for the control of various psychotic disorders. Typical and preferred member compounds include 4-{{4-{2-[4-(2-methoxyphenyl)-1-piperidinyl]ethyl}phenyl}}thiazole-2-amine , 4-{{4-{4-[4-(2-methoxyphenyl)-1-piperidinyl]-n-butyl}phenyl}}thiazole-2-a mine, 3-{4-[4-(2-methoxyphenyl)-1-piperidinyl]-n-butyl}-1,8,8-trimethyl-3-azabic yclo[3.2.1]octane-2,4-dione, 5-{2-[4-(2-methoxyphenyl)-1-piperidinyl]ethyl}oxindole and 3-{2-[4-(1-naphthyl)-1-piperidinyl]ethyl}-2-methyl-4H-pyrido[1,2-a]pyrimid ine-4-one, respectively. Methods for preparing all these compounds from known starting materials are provided.Type: GrantFiled: July 29, 1992Date of Patent: March 15, 1994Assignee: Pfizer Inc.Inventor: Arthur A. Nagel
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Patent number: 5290779Abstract: Nitro-substituted heterocyclic compounds of the formula (I) ##STR1## wherein R is hydrogen or alkyl,Z is an optionally substituted aryl or optionally substituted heterocyclic groun containing at least one atom selected from N, O and S,A is optionally substituted ethylene or optionally substituted trimethylene, andB stands for 2 or 3 members of a heterocyclic ring which is formed, together with the adjacent C-atom and N-aom and at least one of said members may represent a hetero atom and may be optionally substituted, provided that when B stands for 3 members, two of which are carbon atoms and the other one is a nitrogen atom which is located in the middle of the three members, then at least one of said two carbon atoms must be substituted by a xeto group. Such compounds being useful as insecticides.Type: GrantFiled: December 30, 1992Date of Patent: March 1, 1994Assignee: Nihon Bayer Agrochem K.K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shoko Sasaki, Koichi Moriya, Yumi Hattori, Katsuhiko Shibuya
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Patent number: 5272150Abstract: Hydroxyalkylfuranyl derivatives, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof having antiallergic properties, compositions containing the same and methods of treating warm-blooded animals suffering from allergic diseases.Type: GrantFiled: February 26, 1992Date of Patent: December 21, 1993Assignee: Janssen Pharmaceutica N.V.Inventors: Frans E. Janssens, Gaston S. M. Diels, Joseph E. Leenaerts
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Patent number: 5258380Abstract: (4-Piperidinylmethyl and -hetero)purines having antihistaminic properties and being useful agents in the treatment of allergic diseases.Type: GrantFiled: June 21, 1991Date of Patent: November 2, 1993Assignee: Janssen Pharmaceutica N.V.Inventors: Frans E. Janssens, Gaston S. M. Diels
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Patent number: 5254688Abstract: A pyrido[1,2-a]pyrimidine derivative which is useful as an antiallergic agent can be produced from a 2-aminopyridine derivative or a hydrazoic acid salt thereof by a one-pot and substantially one-step process.Type: GrantFiled: June 19, 1991Date of Patent: October 19, 1993Assignee: Wako Pure Chemical Industries, Ltd.Inventors: Atsunori Sano, Motoshige Sumino, Masami Ishihara, Kazuo Maruhashi
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Patent number: 5254556Abstract: The invention relates to C.sub.2-20 alkanoic acid esters of 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6, 7,8,9-tetrahydro-9-hydroxy-2 -methyl-4H-pyrido[1,2-a]pyrimidin-4-one, pharmaceutically acceptable acid addition salts thereof, and enantiomeric forms thereof, which are useful in the treatment of warm-blooded animals suffering from psychotic diseases.Type: GrantFiled: August 19, 1992Date of Patent: October 19, 1993Assignee: Janssen Pharmaceutica N.V.Inventors: Cornelus G. M. Janssen, Alfonsus G. Knaeps, Ludo E. J. Kennis, Jan Vandenberk
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Patent number: 5252572Abstract: The present invention relates to novel 4-oxo-4H-pyrido[1,2-a]pyrimidine-3-carboxamide derivatives of the general formula (I) and the acid addition salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the general formula (I) ##STR1## R stands for a C.sub.1-12 alkyl group optionally substituted by a C.sub.1-4 alkoxycarbonyl group; a C.sub.3-9 cycloalkyl, adamantyl or optionally substituted phenyl group;R.sup.1 means hydrogen or a C.sub.1-4 alkyl group; orR and R.sup.1 together form a --(CH.sub.2).sub.n -- chain, wherein n is 4, 5 or 6;R.sup.2 stands for hydrogen, a C.sub.1-4 alkyl group or halogen;R.sup.3 represents hydrogen or a C.sub.1-4 alkyl group; andm is 0 or 1.The compounds of the general formula (I) possess a gastroprotective effect and are useful for the prevention and therapy of ulcers of the stomach and the small intestine.Type: GrantFiled: June 23, 1992Date of Patent: October 12, 1993Assignee: Chinoin Gyogyszer- Es Vegyeszeti Termekek Gyara Rt.Inventors: Istvan Hermecz, Jozsef Knoll, Lelle Vasvari nee Debreczy, Klara Gyires, Judit Sipos, Agnes Horvath, Laszlo Tardos, Maria Blaogh
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Patent number: 5196425Abstract: 3-Piperidinyl-indazole derivatives and their pharmaceutically acceptable acid addition salts being useful antagonists of neurotransmitters; pharmaceutical compositions containing the same and a method of treating warm-blooded animals suffering from diseases associated with the release of said neutrotransmitters.Type: GrantFiled: July 17, 1989Date of Patent: March 23, 1993Assignee: Janssen Pharmaceutica N.V.Inventors: Jan Vandenberk, Ludo E. J. Kennis, Albertus H. M. T. Van Heertum
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Patent number: 5185335Abstract: Piperidine derivatives of formula ##STR1## wherein A is a radical of formula ##STR2## wherein one or two hydrogen atoms in said radicals (a-1) to (a-3) may be replaced by a C.sub.1-6 alkyl radical;R.sup.1 is hydrogen or halo; R.sup.2 is hydrogen, amino, mono or di(C.sub.1-6 alkyl)amino or C.sub.1-6 alkylcarbonylamino; R.sup.3 is hydrogen or C.sub.1-6 alkyl; L is C.sub.3-6 cycloalkyl, C.sub.5-6 cycloalkanone, C.sub.3-6 alkenyl optionally substituted with aryl, or L is a radical of formula ##STR3## the N-oxide forms, addition salts and stereochemically isomeric forms thereof, said compounds having gastrointestinal motility stimulating properties. Pharmaceutical compositions containing these compounds as active ingredient, and a method of preparing said compounds and pharmaceutical compositions.Type: GrantFiled: February 4, 1991Date of Patent: February 9, 1993Assignee: Janssen Pharmaceutica N.V.Inventors: Georges H. P. Van Daele, Jean-Paul R. M. A. Bosmans, Michel A. J. De Cleyn
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Patent number: 5158952Abstract: The present invention relates to novel 3-piperidinyl-1,2-benzisoxazoles having long-acting antipsychotic properties and which are useful in the treatment of warm-blooded animals suffering from psychotic diseases. Methods of preparing said compounds and compositions containing the same.Type: GrantFiled: October 17, 1989Date of Patent: October 27, 1992Assignee: Janssen Pharmaceutica N.V.Inventors: Cornelus G. M. Janssen, Alfonsus G. Knaeps, Ludo E. J. Kennis, Jan Vandenberk
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Patent number: 5158951Abstract: The present invention relates to novel 4-oxo-4H-pyrido[1,2-a]pyrimidine -3-carbonamide derivatives of the general formula (I) and the acid addition salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the general formula (I) ##STR1## wherein: R stands for a C.sub.1-12 alkyl group optionally substituted by a C.sub.1-4 alkoxycarbonyl group; a C.sub.3-9 cycloalkyl, adamantyl or optionally substituted phenyl group;R.sup.1 means hydrogen or a C.sub.1-4 alkyl group; orR and R.sup.1 together form a --(CH.sub.2).sub.n -- chain, wherein n is 4, 5 or 6;R.sup.2 stands for hydrogen, a C.sub.1-4 alkyl group or halogen;R.sup.3 repesents hydrogen or a C.sub.1-4 alkyl group; andm is 0 or 1.The compounds of the general formula (I) possess a gastroprotective effect and are useful for the prevention and therapy of ulcers of the stomach and the small intestine.Type: GrantFiled: February 6, 1989Date of Patent: October 27, 1992Assignee: Chinoin Gyogyszer- es Vegyeszeti Termekek Gyar Rt.Inventors: Istvan Hermecz, Jozsef Knoll, Lelle Vasvari nee Debreczy, Klara Gyires, Judit Sipos, Agnes Horvath, Laszlo Tardos, Maria Blaogh
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Patent number: 5153206Abstract: A series of novel N-alkyl or oxyalkyl arylpiperidine derivatives have been prepared, including their pharmaceutically acceptable acid addition salts, wherein the N-alkyl or oxyalkyl side chain is further substituted by certain aryl or heterocyclic ring groups. These particular compounds are useful in therapy as neuroleptic agents for the control of various psychotic disorders. Typical and preferred member compounds include 4-{{4-{2-[4-(2-methoxyphenyl)-1-piperidinyl]ethyl}phenyl}}thiazole-2-amine , 4-{{4-{4-[4-(2-methoxyphenyl)-1-piperidinyl]-n-butyl}phenyl}}thiazole-2-a mine, 3-{4-[4-(2-methoxyphenyl)-1-piperidinyl]-n-butyl}-1,8,8-trimethyl-3-azabic yclo[3.2.1]octane-2,4-dione, 5-{2-[4-(2-methoxyphenyl)-1-piperidinyl]ethyl}oxindole and 3-{2-[4-(1-naphthyl)-1-piperidinyl]ethyl}-2-methyl-4H-pyrido[1,2-a]pyrimid ine-4-one, respectively. Methods for preparing all these compounds from known starting materials are provided.Type: GrantFiled: July 26, 1990Date of Patent: October 6, 1992Assignee: Pfizer Inc.Inventor: Arthur A. Nagel
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Patent number: 5151424Abstract: [(Bicyclic heterocyclyl)methyl and -hetero] substituted hexahydro-1H-azepines and pyrrolidines and their pharmaceutically acceptable acid addition salts having anti-histaminic properties, compositions containing the same, and methods of treating allergic diseases in warm-blooded animals.Type: GrantFiled: September 9, 1991Date of Patent: September 29, 1992Assignee: Janssen Pharmaceutica N.V.Inventors: Frans E. Janssens, Gaston S. M. Diels, Geert M. E. Pille
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Patent number: 5081243Abstract: 3-Tetrazolylpyrido[1,2-a]pyrimidin-4-one derivatives useful as an antiallergy agent are produced by reacting a cyano derivative of pyrido[1,2-a]pyrimidin-4-one compound with (i) hydrazoic acid, followed by hydrolysis, or with (ii) a salt of hydrazoic acid, reacting the resulting product with an acid or a base, followed by hydrolysis.Type: GrantFiled: February 22, 1990Date of Patent: January 14, 1992Assignees: Wako Pure Chemical Industries, Ltd., Tokyo, Tanabe Co., Ltd.Inventors: Atsunori Sano, Masami Ishihara, Jun Yoshihara, Hiroyoshi Nawa
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Patent number: 5075315Abstract: Novel hexahydro-2H-indeno[1,2-c]pyridines and their pharmaceutically acceptable acid addition salts having useful antipsychotic properties.Type: GrantFiled: May 17, 1990Date of Patent: December 24, 1991Assignee: McNeilab, Inc.Inventor: Chris R. Rasmussen
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Patent number: 5068235Abstract: The present invention provides a diazabicycloalkane derivative which has the following formula and is useful as medicaments for treating senile dementia, i.e., as cerebral function improving agents and cerebral metabolism activators or anoxic brain damage protectives ##STR1## wherein R.sup.1 is phenyl group, thiazolyl group or furyl group, the phenyl group may have lower alkoxy, lower alkyl or halogen atom as a substituent, R.sup.2 is oxygen atom or sulfur atom, m is 3 or 4, n is 1 or 2.Type: GrantFiled: August 16, 1990Date of Patent: November 26, 1991Assignee: Taiho Pharmaceutical Company, LimitedInventors: Etsuo Hasegawa, Akihiro Kawaguchi, Makoto Kajitani, Mitsugi Yasumoto, Nobuo Kasahara, Junji Yamamoto
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Patent number: 5017212Abstract: A compound of the general formula: ##STR1## wherein Q is a condensed heterocyclic group having an N atom in the bridgehead which may be substituted, W is O or S, R.sub.1 and R.sub.2 each are an alkyl group, an alkoxy group or halogen and Z is CH or N, and a salt thereof, which is useful as a herbicide.Type: GrantFiled: March 17, 1987Date of Patent: May 21, 1991Assignee: Takeda Chemical Industries, Ltd.Inventors: Yasuo Ishida, Kazunari Ohta, Tatsuo Nakahama, Harutoshi Yoshikawa
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Patent number: 5015740Abstract: 3-Piperazinyl-1,2-benzazoles and their pharmaceutically acceptable acid addition salts having useful antipsychotic properties and being useful in the treatment of a variety of disorders in which serotonin and/or dopamine release is of predominant importance.Type: GrantFiled: June 11, 1990Date of Patent: May 14, 1991Assignee: Janssen Pharmaceutica N.V.Inventors: Ludo E. J. Kennis, Jan Vandenberk, Josephus C. Mertens