Benzothiazoles (including Hydrogenated) Patents (Class 544/135)
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Patent number: 5633248Abstract: A compound of the formula: ##STR1## wherein Ar.sup.1 and Ar.sup.2 independently represent an optionally substituted aromatic group; P and Q independently represent a divalent aliphatic hydrocarbon group having at least 2 carbon atoms and optionally having either oxygen or sulfur in the carbon chain; R.sup.1 and R.sup.3 independently represent --CO--R, --CONH--R (R represents a hydrocarbon group or a heterocyclic group) or a hydrocarbon group; R.sup.2 and R.sup.4 independently represent hydrogen or an alkyl group; R.sup.2 and R.sup.4 independently represent hydrogen or an alkyl group; R.sup.1 and R.sup.2 or R.sup.3 and R.sup.4, taken together with the adjacent nitrogen atom, may form a nitrogen-containing heterocyclic group; and j represents 0 or 1, or a salt thereof, has excellent GnRH-receptor antagonizing activity and is useful as a prophylactic and therapeutic agent for hormone-dependent and other diseases.Type: GrantFiled: November 21, 1995Date of Patent: May 27, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Kaneyoshi Kato, Yoshihiro Sugiura, Koichi Kato
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Patent number: 5629326Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: May 13, 1997Assignee: Hoechst-Marion-Roussel, Inc.Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
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Patent number: 5624927Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: April 29, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
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Patent number: 5614543Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: March 25, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau, Edward J. Glamkowski, Yulin Chiang, Grover C. Helsley
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Patent number: 5612343Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: March 18, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
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Patent number: 5602158Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents, the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: February 11, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
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Patent number: 5602159Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: February 11, 1997Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
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Patent number: 5594144Abstract: The present invention provides novel tropolone derivatives of the formula I ##STR1## wherein R.sub.10 is a substituted or unsubstituted piperazinyl or benzothiazolidinyl group, and pharamaceutical compositions thereof. These compounds are useful for the prevention and treatment of ischemic diseases, including cerebrovascular diseases and cardiovascular diseases.Type: GrantFiled: May 18, 1995Date of Patent: January 14, 1997Assignee: The Upjohn CompanyInventors: Noriie Itoh, Mineo Kunihara, Hiroshi Kushida, William W. McWhorter, Syunji Nomura, Kazunori Ozawa, Mikio Taniguchi, Kazuo Tsuzuki
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Patent number: 5589495Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents, the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: December 31, 1996Assignee: Hoechst Marion Roussel, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
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Patent number: 5583146Abstract: Heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein n, R, R.sup.1, R.sup.2, R.sup.3, G, G.sub.x, R.sup.6', Ra, Xa, R.sup.6, Rb, R.sub.3, p, Q, A and R.sup.4 are as defined herein.Type: GrantFiled: January 17, 1995Date of Patent: December 10, 1996Assignee: Bristol-Myers Squibb CompanyInventors: Spencer D. Kimball, Jagabandhu Das, Wan F. Lau, Steven E. Hall, Wen-Ching Han
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Patent number: 5569655Abstract: Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.Type: GrantFiled: July 29, 1994Date of Patent: October 29, 1996Assignee: Sterling Winthrop Inc.Inventors: John A. Dority, Jr., William G. Earley, Virendra Kumar, John P. Mallamo, Matthew S. Miller, Chakrapani Subramanyam
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Patent number: 5561146Abstract: Thrombin inhibitors are provided which have the formula ##STR1## wherein Z is a thrombin inhibitor substructure containing distal and proximal binding site residues; andR.sup.1 is cyano, hydroxyl, alkoxy, amino, aminoalkyl or nitro.Type: GrantFiled: October 14, 1994Date of Patent: October 1, 1996Assignee: Bristol-Myers Squibb CompanyInventors: Kyoung S. Kim, Spencer D. Kimball, Jagabandhu Das, Edwin J. Iwanowicz, Wen-Ching Han
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Patent number: 5512569Abstract: The invention relates to the compounds of formula (I): ##STR1## in which R.sub.1 and R.sup.2 are as defined in the description, the optical isomers thereof,and an addition salt thereof with a pharmaceutically-acceptable acid or base, and medicinal product useful for treating a mammal afflicted with a disease associated with sigma receptors.Type: GrantFiled: March 21, 1995Date of Patent: April 30, 1996Assignee: Adir et CompagnieInventors: Hamid A. Mansour, Thierry Taverne, Raymond Houssin, Isabelle Lesieur, Patrick Depreux, Geard Adam, Daniel-Henri Caignard, Pierre Renard, Marie-Claire Rettori
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Patent number: 5512589Abstract: A compound having the formula: ##STR1## wherein Ar, R.sup.4 and R.sup.5 are defined herein have pharmaceutical utility as proteolytic enzyme inhibitors.Type: GrantFiled: September 3, 1993Date of Patent: April 30, 1996Assignee: Sterling Winthrop Inc.Inventors: Richard P. Dunlap, Neil W. Boaz, Albert J. Mura, Virendra Kumar, Chakrapani Subramanyam, Ranjit C. Desai, Dennis J. Hlasta, Manohar T. Saindane, Malcolm R. Bell, John J. Court, Robert P. Farrell
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Patent number: 5494908Abstract: This application relates to compounds of the formula ##STR1## wherein R.sup.1, X, Y and n are as defined in the specification; and pharmaceutically acceptable addition salts thereof and optical and geometric isomers or racemic mixtures thereof; which compounds are useful for the treatment of various memory dysfunctions characterized by a decreased cholinergic function such as Alzheimer's disease. Compounds of this invention also inhibit monoamine oxidase and hence are useful as antidepressants.Type: GrantFiled: November 12, 1993Date of Patent: February 27, 1996Assignee: Hoechst-Roussel Pharmaceutical IncorporatedInventors: Gerard J. O'Malley, Mark G. Palermo
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Patent number: 5488062Abstract: 4-R.sup.4 -R.sup.5 -2-Saccharinylmethyl heterocyclic carboxylates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 -R.sup.5 -2-halomethylsaccharin with either a heterocyclic carboxylic acid in the presence of an acid-acceptor or the alkali metal salt of a heterocyclic carboxylic acid.Type: GrantFiled: August 9, 1994Date of Patent: January 30, 1996Assignee: Sterling Winthrop Inc.Inventors: Richard P. Dunlap, Dennis J. Hlasta, Ranjit C. Desai, Lee H. Latimer, Chakrapani Subramanyam, John J. Court, Malcolm R. Bell, Virendra Kumar
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Patent number: 5464852Abstract: Compounds having the structural formula ##STR1## wherein L is N, O or SO.sub.n wherein n is 0, 1 or 2;L--R.sup.1 is a leaving group, H--L--R.sup.1 is the conjugate acid thereof and,when L is N, H--L--R.sup.1 has a pK.sub.a value less than or equal to 6, when L is O, H--L--R.sup.1 has a pK.sub.a value less than or equal to to 8, and when L is SO.sub.n, H--L--R.sup.1 has a pK.sub.a value less than or equal to 5;R.sup.2 is primary or secondary alkyl of two to four carbon atoms, primary alkylamino of one to three carbon atoms, primary alkylmethylamino of two to four carbon atoms, diethylamino or primary alkoxy of one to three carbon atoms; andR.sup.Type: GrantFiled: August 11, 1994Date of Patent: November 7, 1995Assignee: Sterling Winthrop Inc.Inventors: Richard P. Dunlap, Albert J. Mura, Dennis J. Hlasta, Ranjit C. Desai, Lee H. Latimer, Chakrapani Subramanyam
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Patent number: 5385923Abstract: 4-R.sup.4 --R.sup.5 -2-Saccharinylmethyl aryl and aryloxy acetates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 --R.sup.5 -2-halomethylsaccharin with an aryl or aryloxyacetic acid in the presence of an acid-acceptor.Type: GrantFiled: August 20, 1993Date of Patent: January 31, 1995Assignee: Sterling Winthrop Inc.Inventors: Lee H. Latimer, Richard P. Dunlap
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Patent number: 5380737Abstract: Compounds having the structural formula ##STR1## wherein L is N, O or SO.sub.n wherein n is 0, 1 or 2;L-R.sup.1 is a leaving group, H-L-R.sup.1 is the conjugate acid thereof and, when L is N, H-L-R.sup.1 has a pK.sub.a value less than or equal to 6, when L is O, H-L-R.sup.1 has a pK.sub.a value less than or equal to to 8, and when L is SO.sub.n, H-L-R.sup.1 has a pK.sub.a value less than or equal to 5;R.sup.2 is primary or secondary alkyl of two to four carbon atoms, primary alkylamino of one to three carbon atoms, primary alkylmethylamino of two to four carbon atoms, diethylamino or primary alkoxy of one to three carbon atoms; andR.sup.Type: GrantFiled: August 27, 1993Date of Patent: January 10, 1995Assignee: Sterling Winthrop Inc.Inventors: Richard P. Dunlap, Albert A. Mura, Dennis J. Hlasta, Ranjit C. Desai, Lee H. Latimer, Chakrapani Subramanyam
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Patent number: 5378720Abstract: 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: May 25, 1993Date of Patent: January 3, 1995Assignee: Sterling Winthrop Inc.Inventors: Dennis J. Hlasta, James H. Ackerman, Albert J. Mura, Ranjit C. Desai
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Patent number: 5330997Abstract: Certain 1H-indazole-3-acetic acid derivatives, and their pharmaceutically-acceptable esters and salts, are inhibitors of the aldose reductase enzyme, and so are useful in the treatment of diabetic complications.Type: GrantFiled: February 24, 1993Date of Patent: July 19, 1994Assignee: Pfizer Inc.Inventors: Banavara L. Mylari, William J. Zembrowski
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Patent number: 5322843Abstract: Compounds of general formula (I): ##STR1## wherein R, X, A, B and p are defined in the description. Medicinal products useful for treating sleep disorders comprising the same.Type: GrantFiled: April 28, 1993Date of Patent: June 21, 1994Assignee: Adir et CompagnieInventors: Said Yous, Isabelle Lesieur, Patrick Depreux, Daniel H. Caignard, Beatrice Guardiola, Gerard Adam, Pierre Renard
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Patent number: 5314889Abstract: A 2-Acylaminothiazole of formula: ##STR1## in which R.sub.1 is H, an alkyl or a substituted alkyl; R.sub.IV is a cycloalkyl, an aromatic group such as phenyl or a heterocyclic group which are unsubstituted or substituted; R.sub.V is a substituted alkyl, a substituted carboxy such as an ester or an amide; or R.sub.IV and R.sub.V together represent a phenoxyalkylene group which may be substituted on the phenyl; and Z is a heterocyclic e.g. indolyl group; or a salt of compound (I).Type: GrantFiled: May 29, 1992Date of Patent: May 24, 1994Assignee: Elf SanofiInventors: Robert Boigegrain, Roger Brodin, Danielle Gully, Jean-Charles Molimard, Dominique Olliero
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Patent number: 5306818Abstract: 4-R.sup.4 -R.sup.5 -Saccharinylmethyl aryl carboxylates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 -R.sup.5 -2-halomethylsaccharin with an arylcarboxylic acid in the presence of an acid-acceptor.Type: GrantFiled: October 23, 1992Date of Patent: April 26, 1994Assignee: Sterling Winthrop Inc.Inventors: Chakrapani Subramanyam, Malcolm R. Bell
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Patent number: 5296496Abstract: 4-R.sub.1 -R.sub.2 -R.sub.3 -2-Saccharinylmethyl and 4,7-C-4,5,6,7-tetrahydro-2-saccharinylmethyl phosphates, phosphonates and phosphinates of formulas I and IIA respectively herein, useful in the treatment of degenerative diseases, and compositions containing them, methods for using them to treat degenerative diseases, and processes for their preparation by reaction of the corresponding 2-halomethylsaccharins with a phosphate, phosphonate or phosphinic acid of formula III herein in the presence of an acid-acceptor.Type: GrantFiled: December 8, 1992Date of Patent: March 22, 1994Assignee: Sterling Winthrop Inc.Inventors: Ranjit C. Desai, John J. Court, Dennis J. Hlasta
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Patent number: 5288744Abstract: Aromatic heterocyclic derivatives have the formula ##STR1## wherein R.sub.1 represents (i)--CH.sub.3, (ii)--CH.sub.2 OH or (iii) ##STR2## wherein R.sub.3 represents hydrogen, --OR.sub.4 wherein R.sub.4 represents hydrogen, alkyl having 1-20 carbon atoms or mono- or polyhydroxyalkyl or R.sub.3 represents ##STR3## wherein r' and r" represent hydrogen, lower alkyl or together form a heterocycle, R.sub.2 represents hydrogen or --CH.sub.3 and Ar represents ##STR4## wherein Z is O or S, ##STR5## wherein R.sub.5 is lower alkyl or ##STR6## wherein R.sub.6 is hydrogen or alkyl having 1-10 carbon atoms and R.sub.7 represents alkyl having 4-12 carbon atoms or cycloalkyl, Y is CH or a nitrogen atom and X represents oxygen, sulfur or --N--R.sub.8 when R.sub.8 represents hydrogen, lower alkyl or lower alkoxycarbonyl, with the proviso that (i) when Y is CH and X is oxygen or sulfur Ar is other than C and (ii) when Y is nitrogen and X is oxygen, Ar is other than (C) or (D) in which R.sub.Type: GrantFiled: June 18, 1992Date of Patent: February 22, 1994Assignee: Centre International De Recherches Dermatologiques (C.I.R.D.)Inventors: Braham Shroot, Jacques Eustache, Jean-Michel Bernardon
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Patent number: 5260295Abstract: Aromatic heterocyclic derivatives have the formula ##STR1## wherein R.sub.1 represents (i)--CH.sub.3, (ii)--CH.sub.2 OH or (iii) ##STR2## wherein R.sub.3 represents hydrogen, --OR.sub.4 wherein R.sub.4 represents hydrogen, alkyl having 1-20 carbon atoms or mono- or polyhydroxyalkyl or R.sub.3 represents ##STR3## wherein r' and r" represent hydrogen, lower alkyl or together form a heterocycle, R.sub.2 represents hydrogen or --CH.sub.3 and Ar represents ##STR4## wherein R.sub.6 is hydrogen or alkyl having 1-10 carbon atoms and R.sub.7 represents alkyl having 4-12 carbon atoms or cycloalkyl, Y is CH or a nitrogen atom and X represents oxygen, sulfur or --N--R.sub.8 when R.sub.8 represents hydrogen, lower alkyl or lower alkoxycarbonyl, with the proviso that (i) when Y is CH and X is oxygen or sulfur Ar is other than C and (ii) when Y is nitrogen and X is oxygen, Ar is other than (C) or (D) in which R.sub.6 is alkyl having 1-4 carbon atoms and R.sub.7 is branched alkyl having 4-12 atoms.Type: GrantFiled: May 7, 1991Date of Patent: November 9, 1993Assignee: Centre International de Recherches Dermatologiques (C.I.R.D.)Inventors: Braham Shroot, Jacques Eustache, Jean-Michel Bernardon
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Benzazole derivatives, processes for their preparation containing such compounds and the use thereof
Patent number: 5246927Abstract: The invention relates to new benzazole derivatives of the formula I ##STR1## wherein X is oxygen or sulphur, R.sub.1 is lower alkyl, lower alkenyl or cycloalkyl, R.sub.2 and R.sub.3 independently of one another are each hydrogen, lower alkyl or cycloalkyl radicals or taken together are a substituted or unsubstituted bivalent hydrocarbon residue of aliphatic character in which the carbon atoms of the chain may be interrupted by a heteroatom, R.sub.4 is either a group ##STR2## wherein R.sub.5 and R.sub.6 independently of one another are lower alkyl or cycloalkyl radicals, optionally substituted, or taken together R.sub.5 and R.sub.6 are a substituted or unsubstituted bivalent hydrocarbon residue of aliphatic character in which the carbon atoms of the chain may be interrupted by a heteroatom, or, R.sub.4 is a group ##STR3## where R.sub.7 is a lower alkyl group, and their salts and N-oxides. The products are useful as anthelmintic effective agents. The products can be prepared to methods known per se.Type: GrantFiled: October 6, 1992Date of Patent: September 21, 1993Assignee: Ciba-Geigy CorporationInventor: Vittal R. Rao -
Patent number: 5234924Abstract: Compound of general formula (I): ##STR1## where R.sub.1, R.sub.2, R.sub.3, n and X are defined in the description. Medicinal products.Type: GrantFiled: December 5, 1991Date of Patent: August 10, 1993Assignee: Adir et CompagnieInventors: Thierry Taverne, Isabelle Lesieur, Patrick Depreux, Daniel H. Caignard, Beatrice Guardiola, Gerard Adam, Pierre Renard
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Patent number: 5225548Abstract: Indophenol dyes of the formula ##STR1## where X is nitrogen or the radical CH,Q is a five-membered heterocyclic radical, andK is a radical of an aniline, aminonaphthalene, aminoquinoline or aminothiazole derivative, andthe radical A can be benzofused,are useful for thermal transfer processes.Type: GrantFiled: September 20, 1991Date of Patent: July 6, 1993Assignee: BASF AktiengesellschaftInventors: Volker Bach, Karl-Heinz Etzbach, Ruediger Sens
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Patent number: 5101034Abstract: A process for the preparation of a heteroaryloxyacetamide of the formula ##STR1## in which R is a 5 membered heterocycle which may be benzo-fused, andR.sup.1 and R.sup.2 each independently is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl, halogenoalkyl, alkoxyalkyl, alkoxy, aralkyl or aryl, orR.sup.1 and R.sup.2, together with the nitrogen atom to which they are bonded, form a heterocycle,which comprises reacting a sulphonylated heteroaromatic of the formulaR--SO.sub.2 --R'in whichR' is lower alkyl or benzyl,with an .alpha.-oxyacetamide of the formula ##STR2## in which R" is hydrogen or acyl,in the presence of an inorganic base as an acid acceptor and of solvent as a diluent at a temperature of about -50.degree. C. to +150.degree. C. The products are known herbicides.Type: GrantFiled: March 7, 1991Date of Patent: March 31, 1992Assignee: Bayer AktiengesellschaftInventors: Thomas Schmidt, Hans-Joachim Diehr
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Patent number: 5055466Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are inhibitors of renin and therefore useful as cardiovascular agents.Type: GrantFiled: December 14, 1989Date of Patent: October 8, 1991Assignee: E. R. Squibb & Sons, Inc.Inventors: Harold N. Weller, III, Denis E. Ryono
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Patent number: 5034524Abstract: Insecticidal heterocyclic compounds of the formula ##STR1## wherein A represents a five-membered or six-membered heteroaryl group containing one to three hetero atoms selected from the group consisting of S, O and N, said heteroaryl group being unsubstituted or substituted by a hologen atom or C.sub.1-4 alkyl group, Z represents a three-membered straight chain, each member being selected from the group consisting of CH.sub.2 -, O, S and N-R.sup.2 with at least one of said three members being O, S or N-R.sup.2, E represents CH.sub.2, O, S or N-R.sup.2, wherein R.sup.2 represents a hydrogen atom, a C.sub.1-4 alkyl group, a C.sub.1-4 alkoxy group or the group ##STR2## wherein R.sup.3 represents a hydrogen atom or halogen atom, X represents CH or N, Y represents a nitro group or cyano group, and R.sup.1 represents a hydrogen atom or methyl group.Type: GrantFiled: November 7, 1990Date of Patent: July 23, 1991Assignee: Nihon Tokushu Noyaku Seizo K.K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Koichi Moriya, Yumi Hattori, Ikuro Honda, Katsuhiko Shibuya
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Patent number: 5007952Abstract: Herbicidally active pyrroles of the formula ##STR1## wherein R.sup.1 represents C.sub.1-4 alkyl, or one R.sup.1 together with the other R.sup.1 forms tetramethylene or butenylene,X represents hydrogen or halogen,Y represents O or S,n represents 0 or 1,R.sup.2 represents hydrogen or an organic radical.Type: GrantFiled: November 9, 1989Date of Patent: April 16, 1991Assignee: Nihon Tokushu Noyaku Seizo K.K.Inventors: Toyohiko Kume, Toshio Goto, Atsumi Kamochi, Akihiko Yanagi, Hiroshi Miyauchi, Tadao Asami
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Patent number: 4970318Abstract: Acyl derivatives of 2-aminobenzothiazole and alkylated analogs thereof as antitumor agents.Type: GrantFiled: April 12, 1989Date of Patent: November 13, 1990Assignee: Pfizer Inc.Inventors: Rodney C. Schnur, Anton F. J. Fliri
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Patent number: 4959379Abstract: Fungicidal 7-substituted 2-carboxamido-benzothiazole 3-oxides of the formula ##STR1## in which n stands for the numbers 0, 1, 2 or 3,R.sup.1 stands for hydrogen or optionally substituted alkyl,R.sup.2 stands for hydrogen, hydroxyl, ureido or for an optionally substituted radical from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkinyl, alkoxy, alkenyloxy, aralkoxy, aralkyl, aryl, heterocyclyl and heterocyclylakyl, orR.sup.1 and R.sup.2 together stand for an alkylene chain which is optionally substituted and optionally interrupted by hetero atoms,R.sup.3 stands for halogen, alkyl or halogenoalkyl andR.sup.4 stands for halogen, alkyl or halogenoalykl.The intermediates of the formula ##STR2## are also new.Type: GrantFiled: March 21, 1989Date of Patent: September 25, 1990Assignee: Bayer AktiengesellschaftInventors: Klaus Wagner, Gerd Hanssler
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Patent number: 4886812Abstract: This invention relates to new tetrahydrobenzthiazoles of general formula ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the above mentioned phenyl nucleic may each be substituted by 1 or 2 halogen atoms,R.sub.2 represents a hydrogen atom or an alkyl group,R.sub.3 represents a hydrogen atom, an alkyl group a cycloalkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the phenyl nucleus may be substituted by fluorine, chlorine or bromine atoms,R.sub.4 represents a hydrogen atom, an alkyl group, an alkyl or alkenyl group, orR.sub.3 and R.sub.4 together with the nitrogen atom between them represent a pyrrolidino, piperidino, hexamethyleneimino or morpholino group, the enantiomers and the acid addition salts thereof.The compounds of general formula I above in which one of the groups R.sub.1 or R.sub.3 or both groups R.sub.1 and R.sub.Type: GrantFiled: October 12, 1988Date of Patent: December 12, 1989Assignee: Dr. Karl Thomae GmbHInventors: Gerhart Griss, deceased, Claus Schneider, Rudolf Hurnaus, Walter Kobinger, Ludwig Pichler, Rudolf Bauer, Joachim Mierau, Dieter Hinzen, Gunter Schingnitz
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Patent number: 4845098Abstract: Fungicidal saccharine salts of substituted hydroxypropylamines of the formula ##STR1## in which R.sup.1 is optionally substituted phenyl, phenoxy, phenylthio, phenylalkyl, phenoxyalkyl, or phenylthioalkyl, or optionally substituted cyclohexyl, cylohexyloxy, cyclohexylalkyl, cyclohexyloxyalkyl or cyclohexylthioalkyl,R.sup.2 is hydrogen or methyl,R.sup.3 is methyl or ethyl, andR.sup.4 and R.sup.5 each independently is alkyl or alkenyl, orR.sup.4 and R.sup.5, together with the nitrogen atom to which they are bonded, are an optionally substituted saturated heterocyclic radical which can optionally contain further hetero atoms.Type: GrantFiled: November 5, 1987Date of Patent: July 4, 1989Assignee: Bayer AktiengesellschaftInventors: Wolfgang Kramer, Joachim Weissmuller, Paul Reinecke, Gerd Hanssler
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Patent number: 4831032Abstract: The present invention provides benzimidazoles of the general formula: ##STR1## wherein R.sub.1, X, A, and R.sub.2 are as defined in the specification. The present invention also provides processes for the preparation of these new benzimidazoles and pharmaceutical compositions containing them, as well as intermediates for the preparation thereof.The new benzimidazoles are useful to treat heart or circulatory diseases which respond to a lowering of blood pressure, a positive inotropic action and/or an improvement in microcirculation.Type: GrantFiled: July 3, 1986Date of Patent: May 16, 1989Assignee: Boehringer Mannheim GmbHInventors: Wolfgang von der Saal, Alfred Mertens, Herbert Berger, Bernd Muller-Beckmann, Klaus Strein
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Patent number: 4826836Abstract: Fungicidally active novel saccharine salts of aminomethyl heterocyclic compounds of the formula ##STR1## in which R represents optionally substituted cycloalkyl, optionally substituted aryl or optionally substituted thienyl,R.sup.1 represents hydrogen or alkyl,R.sup.2 represents alkyl,R.sup.3 represents alkyl andR.sup.4 represents alkyl, alkenyl or alkinyl, orR.sup.3 and R.sup.4, together with the nitrogen atom to which they are bonded, represent an optionally substituted saturated heterocyclic radical which can contain further hetero atoms,X represents oxygen or sulphur,Y represents oxygen, sulphur or the methylene group,m represents 0 or 1 andn represents 0 or 1.Type: GrantFiled: November 5, 1987Date of Patent: May 2, 1989Assignee: Bayer AktiengesellschaftInventors: Joachim Weissmuller, Wolfgang Kramer, Paul Reinecke, Gerd Hanssler
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Patent number: 4824844Abstract: Fungicidally active saccharine salts of substituted amines of the formula ##STR1## in which A represents in each case optionally substituted cyclohexyl, cyclohexenyl or phenyl,R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen or alkyl,R.sup.3 and R.sup.4 independently of one another represent alkyl or, together with the nitrogen atom to which they are bonded, represent an optionally substituted saturated heterocyclic radical which can contain further hetero atoms andn represents the number 0 or 1.Type: GrantFiled: November 5, 1987Date of Patent: April 25, 1989Assignee: Bayer AktiengesellschaftInventors: Joachim Weissmuller, Paul Reinecke, Gerd Hanssler
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Patent number: 4801707Abstract: Benzothiazole sulphene amides are obtained from dibenzothiazolyl disulphide and water-soluble amines in the absence of an oxidizing agent and in the presence of aqueous alkali in a high yield and with very good stability in storage by placing the amine solution in water and simultaneously adding dibenzothiazolyl disulphide and aqueous alkali from separate storage vessels.Type: GrantFiled: December 24, 1986Date of Patent: January 31, 1989Assignee: Bayer AktiengesellschaftInventors: Alfredo Wust, Tony Van Osselaer
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Patent number: 4777168Abstract: A class of bicyclic benzo-oxy heterocyclic ether and thioether compounds exhibiting parmacological activity, including anti-secretory and anti-ulcerogenic activity, pharaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.Type: GrantFiled: January 7, 1988Date of Patent: October 11, 1988Assignee: Rorer Pharmaceutical CorporationInventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt, Kent W. Neuenschwander
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Patent number: 4769200Abstract: In order to compound organic materials which are crystalline under standard conditions, these materials, in the pulverulent and/or molten state, are processed in a self-purging, twin-screw extruder in which the screws rotate in the same direction, ejected through one or more narrow passages into a low pressure zone, cooled and comminuted to give particles. In order to improve the pourability and shelf life, the materials are completely crystallized by the time they reach the end of the screws, and are heated during discharge through the narrow passage, in order to form a melt film. Dust-free granules havig a smooth surface can be produced in this manner.Type: GrantFiled: June 20, 1986Date of Patent: September 6, 1988Assignee: BASF AktiengesellschaftInventors: Leopold Hupfer, Juergen Paetsch, Johann Hotz, Heino Thiele, Hans D. Zettler
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Patent number: 4762840Abstract: Novel pyrimido[2,1-b]benzothiazoles of the formula ##STR1## wherein R and R.sub.3 are individually selected from the group consisting of hydrogen and alkyl of 1 to 6 carbon atoms or taken together with the carbon to which they are attached form a cycloalkyl of 3 to 6 carbon atoms, R.sub.1 is selected from the group consisting of hydroxy, alkoxy of 1 to 12 carbon atoms, cycloalkyl of 7 to 12 carbon atoms, and ##STR2## R.sub.5 and R.sub.6 are individually selected from the group consisting of hydrogen and alkyl of 1 to 6 carbon atoms or taken together with the nitrogen form piperidino or morpholino, R.sub.Type: GrantFiled: July 31, 1986Date of Patent: August 9, 1988Assignee: Roussel UclafInventors: David A. Rowlands, Julian M. C. Golec, Saroop S. Matharu, Peter W. Hairsine
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Patent number: 4760057Abstract: This invention relates to novel (acyloxyalkoxy)carbonyl derivatives as bioreversible prodrug moieties for primary and secondary amine functions in drugs having a primary or secondary amine function thereon. Hydrolytic enzymes are used to trigger the regeneration of the parent amine drug of the carbamate prodrug moiety. The case also contains pharmaceutical composition, method of treatment and process claims.Type: GrantFiled: April 22, 1985Date of Patent: July 26, 1988Assignee: Merck & Co., Inc.Inventor: Jose Alexander
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Patent number: 4751301Abstract: Benzothiazolesulphenamides can be prepared in high yield and purity from dibenzothiazolyl disulphide and a primary or secondary amine in the absence of an oxidizing agent in a water-immiscible organic solvent and in the presence of aqueous alkali by presenting a solution of the amine in the organic solvent and adding dibenzothiazolyl disulphide and aqueous alkali either simultaneously or in succession.Type: GrantFiled: April 28, 1986Date of Patent: June 14, 1988Assignee: Bayer AktiengesellschaftInventors: Alfredo Wust, Tony van Osselaer
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Patent number: 4748182Abstract: This invention relates to aromatic 2-aminoalkyl derivatives of 1,2-benzoisothiazol-3(2H)one-1,1-dioxides, processes for the preparation of same, and to their use as anxiolytic and antihypertensive agents.Type: GrantFiled: March 5, 1986Date of Patent: May 31, 1988Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Marcel Hibert, Maurice W. Gittos
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Patent number: 4731374Abstract: This invention relates to new tetrahydrobenzthiazoles of general formula ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group, an alkenyl or alkynylk group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the above mentioned phenyl nuclei may each be substituted by 1 or 2 halogen atoms,R.sub.2 represents a hydrogen atom or an alkyl group,R.sub.3 represents a hydrogen atom, an alkyl group a cycloalkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the phenyl nucleus may be substituted by flurorine, chlorine or bromine atoms,R.sub.4 represents a hydrogen atom, an alkyl group, an alkyl or alkenyl group, orR.sub.3 and R.sub.4 together with the nitrogen atom between them represent a pyrrolidino, piperidino, hexamethyleneimino or morpholino group, the enantiomers and the acid addition salts thereof.The compounds of general formula I above in which one of the groups R.sub.1 or R.sub.3 or both groups R.sub.1 and R.sub.Type: GrantFiled: December 19, 1985Date of Patent: March 15, 1988Assignee: Dr. Karl Thomae GmbHInventors: Gerhart Griss, deceased, Rudolf Hurnaus, Walter Kobinger, Ludwig Pichler, Rudolf Bauer, Joachim Mierau, Dieter Hinzen, Gunter Schingnitz
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Patent number: 4705861Abstract: Benzothiazole derivatives of the formula ##STR1## with the substituent meanings mentioned in the description, are starting compounds for the preparation of new azo dyestuffs. Some methods of preparing the new benzothiazole derivatives are described.Type: GrantFiled: November 14, 1985Date of Patent: November 10, 1987Assignee: Bayer AktiengesellschaftInventors: Hauke Furstenwerth, Karl H. Schundehutte