Thiadiazines Patents (Class 544/8)
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Publication number: 20030225270Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (I), (II), (Ia) and (Ib) further defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel compounds.Type: ApplicationFiled: April 24, 2003Publication date: December 4, 2003Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Michel Jose Emmanuel, Eugene R. Hickey, Weimin Liu, Denice Mary Spero, Sanxing Sun, David S. Thomson, Yancey David Ward, Erick Richard Roush Young
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Publication number: 20030199689Abstract: The present invention relates to compounds of formula I, 1Type: ApplicationFiled: November 21, 2002Publication date: October 23, 2003Inventors: Marc Nazare, Melanie Essrich, David William Will, Hans Matter, Kurt Ritter, Volkmar Wehner
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Patent number: 6635634Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.Type: GrantFiled: February 14, 2002Date of Patent: October 21, 2003Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
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Publication number: 20030176692Abstract: Described is a process for the preparation of a particulate tetrahydro-3,5-dimethyl-1,3,5-thiadiazine-2-thione product by combining a first aqueous solution comprising methylammonium N-methyldithiocarbamate with a second aqueous solution comprising formaldehyde, followed by separation and drying of the resulting solid, which comprises combining the first and the second aqueous solutions in such a way that the ratio between the concentrations of dithiocarbamate functions and of formaldehyde is essentially constant in the reaction mixture over time during the duration of the reaction.Type: ApplicationFiled: February 6, 2003Publication date: September 18, 2003Inventors: Heinz Isak, Norbert Sendhoff, Franz Schutz, Jorg Therre, Michael Drogemuller, Dirk Franke, Manfred Munzinger, Alexander Weck, Kirsten Burkart
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Publication number: 20030139397Abstract: Compounds of Formula (I), and their N-oxides and agriculturally suitable salts, are disclosed which are useful as arthropodicides wherein A is H; E is H or C1-C3 alkyl; or A and E can be taken together to form —CH2—, —CH2CH2—, —O—, —S—, —S(O)—, —S(O)2—, —NR8—, —OCH2—, —SCH2—, —N(R8)CH2—, substituted —CH2— and substituted —CH2CH2—, the substituents independently selected from 1-2 halogen and 1-2 methyl; W is N or CR4;X is CR5R6, O, S, NR7 or a direct bond, provided that when W is N, then X is other than a direct bond; Y is H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C3 alkylsulfonyl, C3-C6 cycloalkyl, C3-C6 cycloalkylalkyl, NR9R10, N═CR11R12, OR7, COR13, CO2R14 or C1-C6 alkyl substituted by at least one group selected from halogen, C1-C3 alkoxy, CN, NO2, S(O)1R15, COR13, CO2R14 and optionally substituted phenyl; Z is O or S; and R2, R3, R4, R5, R6, R7, R8, R9Type: ApplicationFiled: August 28, 2002Publication date: July 24, 2003Inventor: David Walter Piotrowski
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Publication number: 20030130122Abstract: Substituted aryl ether derived compounds represented by the general structure (1) are described.Type: ApplicationFiled: December 5, 2001Publication date: July 10, 2003Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Sandeep Gupta, Masamitsu Tsukamoto, Mark Read
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Patent number: 6579982Abstract: The present invention relates to pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein X, Y, Ar1, Z, R1, R2 and R3 are as defined in the specification, and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.Type: GrantFiled: August 9, 2000Date of Patent: June 17, 2003Assignee: Pfizer Inc.Inventor: Julian Blagg
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Publication number: 20030092680Abstract: Compounds of formula (I) or pesticidally acceptable salts thereof, compositions containing them and methods of use.Type: ApplicationFiled: September 11, 2002Publication date: May 15, 2003Inventor: Tai-Teh Wu
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Patent number: 6555534Abstract: The use of 4,4-methylenebis (tetrahydro-1,2-4-thiadiazine-1,1 -dioxide) in the eradication and control of the microorganism Helicobacter pylori in humans is disclosed.Type: GrantFiled: March 10, 1999Date of Patent: April 29, 2003Assignee: Medpointe Healthcare Inc.Inventor: James C. Costin
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Publication number: 20030064980Abstract: Compound represented by the structural formula 1Type: ApplicationFiled: June 6, 2002Publication date: April 3, 2003Inventors: Neng-Yang Shih, Ho-Jane Shue, Gregory A. Reichard, Sunil Paliwal, David J. Blythin, John J. Piwinski, Dong Xiao, Xiao Chen
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Patent number: 6500818Abstract: Compounds having the following formula wherein L, M, R2, R3, R4, R5, R6, R7, X1 and X2 are as defined in the specification, pharmaceutically-acceptable salt thereof, useful for treating depression, anxiety, asthma, rheumatoid arthritis, Alzheimer's disease, cancer, schizophrenia, oedema, allergic rhinitis, inflammation, pain, gastrointestinal-hypermotility, emesis, Huntington's disease, psychoses, hypertension, migraine, bladder hypermotility, or urticaria, compositions including such compounds and processes for making such compounds.Type: GrantFiled: March 30, 2001Date of Patent: December 31, 2002Assignee: Astrazeneca ABInventors: Peter Robert Bernstein, Robert Frank Dedinas, Cyrus John Ohnmacht, Keith Russell
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Patent number: 6495547Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein Alk1 is C1-6alkanediyl optionally substituted with hydroxy, C1-4alkyloxy or C1-4alkylcarbonyloxy; —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical; R4 is hydrogen or C1-6alkyl; A is a bivalent radical of formula —NR6—Alk2— (b-1), or —Npiperidinyl-(CH2)m (b-2) wherein m is 0 or 1; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen.Type: GrantFiled: August 18, 2000Date of Patent: December 17, 2002Assignee: Janssen Pharmaceutica, N.V.Inventors: Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren, Marc Francis Josephine Schroven, Marcel Frans Leopold De Bruyn
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Patent number: 6495546Abstract: Propanolamine derivatives represented by the following formula (I): These derivatives may be &bgr;3 agonists and exert sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic and anti-urinary incontinence and anti-pollakiuria activities. Pharmaceutical compositions containing such propanolamine derivatives, methods for the prevention and/or treatment diseases using these propanolamine derivatives, and processes for their preparation are also described.Type: GrantFiled: November 22, 2000Date of Patent: December 17, 2002Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
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Publication number: 20020173492Abstract: Compounds of formula (I) or pesticidally acceptable salts thereof, compositions containing them and methods of use.Type: ApplicationFiled: February 1, 2002Publication date: November 21, 2002Inventor: Tai-Teh Wu
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Publication number: 20020123491Abstract: Compound represented by the structural formula 1Type: ApplicationFiled: December 14, 2000Publication date: September 5, 2002Inventors: Neng-Yang Shih, Ho-Jane Shue, Gregory A. Reichard, Sunil Paliwal, David J. Blythin, John J. Piwinski, Dong Xiao, Xiao Chen
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Patent number: 6423718Abstract: The present invention relates to 4,4-disubstituted-3,4-dihydro-2(1H)-quinazolinones of formula I: or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.Type: GrantFiled: August 2, 2000Date of Patent: July 23, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Jeffrey W. Corbett, Soo S. Ko
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Publication number: 20020058809Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (I), (II), (Ia) and (Ib) further defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel compounds.Type: ApplicationFiled: November 2, 2001Publication date: May 16, 2002Inventors: Michel Jose Emmanuel, Eugene R. Hickey, Weimin Liu, Denice Mary Spero, Sanxing Sun, David S. Thomson, Yancey David Ward, Erick Richard Roush Young
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Patent number: 6344453Abstract: Insecticidal heterocyclic compounds of the formula 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 halogen atom or C1-4 alkyl group, Z represents a three-membered straight chain, each member being selected from the group consisting of CH2—, O, S and N—R2 with at least one of said three members being O, S or N—R2, E represents CH2, O, S or N—R2, wherein R2 represents a hydrogen atom, a C1-4 alkyl group, a C1-4 alkoxy group or the group wherein R3 represents a hydrogen atom or halogen atom, X represents CH or N, Y represents a nitro group or cyano group, and R1 represents a hydrogen atom or methyl group.Type: GrantFiled: April 19, 1999Date of Patent: February 5, 2002Inventors: Kozo Shiokawa, Shinichi Tsuboi, Koichi Moriya, Katsuhiko Shibuya
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Patent number: 6326368Abstract: The present invention provides novel compounds, and pharmaceutical compositions thereof, and methods of using same in the treatment of affective disorders, anxiety, depression, post-traumatic stress disorders, eating disorders, supranuclear palsey, irritable bowl syndrome, immune supression, Alzheimer's disease, gastrointestinal diseases, anorexia nervosa, drug and alcohol withdrawal symptoms, drug addiction, inflammatory disorders, or fertility problems. The novel compounds provided by this invention are those of formula: wherein R1, R3, R5, Q, Z, Y, V, X and X′ are as defined herein.Type: GrantFiled: March 13, 1997Date of Patent: December 4, 2001Assignee: DuPont Pharmaceuticals CompanyInventors: Robert John Chorvat, Parthasarathi Rajagopalan
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Patent number: 6313111Abstract: Substitued 6H-1,3,4-thiadiazin-2-amines of the following general formula: wherein Ar is phenyl optionally substituted with one or more chloro, bromo atoms, C1-C4 alkoxy, or C1-C4 alkyl groups; and represents a morpholino, thimomorpholino, piperidino, pyrrolidino, or hexamethylenimino moieties, the pharmaceutically acceptable salts thereof and the use of them anasethetic, cardiovascular and hypometabolic agents and pharmaceutical compositions containing them.Type: GrantFiled: December 8, 1998Date of Patent: November 6, 2001Assignees: The Procter & Gamble Company, Nauchno-Tekhnologicheskoe Predpriyatie “Ligand” (Tovarischestvo S Ogranichennoi Otvetstvennostiju)Inventors: Oleg Nikolaevich Chupakhin, Larisa Petrovna Sidorova, Emma Afanasievna Tarakhty, Antonina Petrovna Novikova, Natalya Mikhailovna Perova, Valentin Antonovich Vinogradov, Michiel Franciscus van Ginkel
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Patent number: 6265398Abstract: The present invention relates to novel substituted pyridines/pyrimidines of the formula I where A is CH or N; X is NH, O or S(O)q where q is 0, 1 or 2; Y1, Y2 and Y3 independently of one another are a group of the formula —O—, —CO—, —CNR6—, —S(O)r— or —N(O)lR6— where l is 0 or 1 and where r is 0, 1 or 2, or a group of the formula CR7R8, or Y1 or Y3 replace a direct bond; Z is a direct bond, NR9, O, S(O)s where s is 0, 1 or 2, OSO2, SO2O, NR10SO2, SO2NR11, SiR12R13 or where U is a direct bond, NR14 or O; W is oxygen or sulfur; V is a direct bond, NR15 or oxygen; m and n and 0, 1, 2, 3 or 4; where the radicals R1 to R15 have the meaning given in the description, to processes for their preparation, to their use as pesticides, fungicides and ovicides and to their use as veterinary medicaments.Type: GrantFiled: October 23, 1998Date of Patent: July 24, 2001Assignee: Hoechst Schering AgrEvo GmbHInventors: Ralf Braun, Wolfgang Schaper, Herbert Stark, Rainer Preuss, Werner Knauf, Ulrich Sanft, Manfred Kern, Werner Bonin
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Patent number: 6255303Abstract: The compounds of formula (I) in which R1, R2, R3, R4, R5, X and Y have the meanings as given in the description are novel effective bronchial therapeutica.Type: GrantFiled: September 13, 2000Date of Patent: July 3, 2001Assignee: Byk Gulden Lomberg Chemische Fabrik GmbHInventors: Geert Jan Sterk, Margaretha van der Mey
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Patent number: 6232309Abstract: Insecticidal heterocyclic compounds of the formula: 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 halogen atom or C1-4 alkyl group, Z represents a three-membered straight chain, each member being selected from the group consisting of CH2—, O, S and N—R2 with at least one of said three members being O, S or N—R2; E represents CH2, O, S or N—R2, wherein R2 represents a hydrogen atom, a C1-4 alkyl group, a C1-4 alkoxy group or the group wherein R3 represents a hydrogen atom or halogen atom, X represents CH or N, Y represents a nitro group or cyano group, and R1 represents a hydrogen atom or methyl group.Type: GrantFiled: May 22, 2000Date of Patent: May 15, 2001Assignee: Nihon Bayer Agrochem K.K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Koichi Moriya, Katsuhiko Shibuya
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Patent number: 6197766Abstract: Insecticidal dihydrooxadiazine compounds having the formula: wherein X is O, N or S; R is a substituted or unsubstituted phenyl or C4-C5 heterocyclic group; R2, R3, R4, and R5 are one of the following: a) R2, R3, and R4 are, independently, hydrogen, alkyl, alkoxy, or furanyl; and R5 is nitro, cyano, alkyl, dialkylamino, alkylthio, alkoxy, haloalkoxy, phenoxy, phenylthio, or alkoxycarbonyl, wherein R3 and R5 together can form a ring; or b) R3, R4, and R5 are hydrogen; and R2 is alkylthio, alkylsulfinyl, alkylsulfonyl, nitroalkoxy, hydroxy, dialkoxyphosphinyl, cyano, acyloxy, alkoxy, haloalkoxy, cycloalkyl, or alkenyl; or R2 is a substituted or unsubstituted phenyl, phenylthio, phenylsulfinyl, phenylsulfonyl, pyrazolyl, furanyl, thienyl, phenylalkoxy, or benzoyloxy; and R6 is hydrogen, alkyl, alkylthio, alkoxyalkyl, acyl, benzyl, or alkoxycarbonyl.Type: GrantFiled: January 11, 1999Date of Patent: March 6, 2001Assignees: Uniroyal Chemical Company, Inc. and Uniroyal Chemical Co., Uniroyal Chemical Cie.Inventors: Sheldon Bernard Park, Anupama Mishra, Mark Achiel Dekeyser, Paul Thomas McDonald
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Patent number: 6177428Abstract: Disclosed are nitrosated and/or nitrosylated phosphodiesterase inhibitors having the formula NOn-PDE inhibitor where n is 1 or 2. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides a composition comprising a therapeutically effective amount of an phosphodiesterase inhibitor (PDE inhibitor), which can optionally be substituted with at least one NO or NO2 moiety, and one to ten fold molar excess of a compound that donates, transfers or releases nitrogen monoxide as a charged species, i.e., nitrosonium (NO+) or nitroxyl (NO−), or as the neutral species, nitric oxide (NO•) or which stimulates endogenous EDRF production. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides methods for treating sexual dysfunctions in males and females.Type: GrantFiled: February 10, 1999Date of Patent: January 23, 2001Assignee: NitroMed, Inc.Inventors: David S. Garvey, Inigo Saenz de Tejada
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Patent number: 6133277Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein Alk.sup.1 is C.sub.1-6 alkanediyl optionally substituted with hydroxy, C.sub.1-4 alkyloxy or C.sub.1-4 alkylcarbonyloxy; --Z.sup.1 --Z.sup.2 -- is a bivalent radical; R.sup.1, R.sup.2 and R.sup.3 are each independently selected from hydrogen, C.sub.1-6 alkyl, hydroxy, halo and the like; or when R.sup.1 and R.sup.2 are on adjacent carbon atoms, R.sup.1 and R.sup.2 taken together may form a bivalent radical; R.sup.4 is hydrogen or C.sub.1-6 alkyl; A is a bivalent radical of formula --NR.sup.6 --Alk.sup.2 -- (b-1), or --Npiperidinyl--(CH.sub.2).sub.m (b-2) wherein m is 0 or 1; R.sup.5 is a radical of formula ##STR1## wherein n is 1 or 2; p.sup.1 is 0, and p.sup.2 is 1 or 2; or p.sup.1 is 1 or 2, and p.sup.2 is 0; X is oxygen, sulfur or .dbd.NR.sup.9 ; Y is oxygen or sulfur; R.sup.7 is hydrogen, C.sub.1-6 alkyl, C.sub.Type: GrantFiled: November 16, 1998Date of Patent: October 17, 2000Assignee: Janssen Pharmaceutica N.V.Inventors: Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren, Marc Francis Josephine Schroven, Marcel Frans Leopold De Bruyn
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Patent number: 6124302Abstract: The present invention relates to 4,4-disubstituted-3,4-dihydro-2(1H)-quinazolinones of formula I: ##STR1## or steroisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent, wherein:R.sup.1 is C.sub.1-3 alkyl substituted with 1-7 halogen;R.sup.2 is optionally substituted C.sub.1-5 alkyl, optionally substituted C.sub.2-5 alkenyl, or optionally substituted C.sub.2-5 alkynyl;R.sup.3, at each occurrence, is independently selected from C.sub.1-4 alkyl, OH, C.sub.1-4 alkoxy, F, Cl, Br, I, NR.sup.5 R.sup.5a, NO.sub.2, CN, C(O)R.sup.6, NHC(O)R.sup.7, and NHC(O)NR.sup.5 R.sup.5a ;R.sup.5 and R.sup.5a are independently selected from H and C.sub.1-3 alkyl;R.sup.6 is selected from H, OH, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, and NR.sup.5 R.sup.5a ;R.sup.Type: GrantFiled: April 8, 1998Date of Patent: September 26, 2000Assignee: DuPont PharmaceuticalsInventors: Jeffrey W. Corbett, Soo S. Ko
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Patent number: 6117867Abstract: Substituted 6-R-1,3,4-thiadiazin-2-amines of the following general formula: ##STR1## wherein Ar is phenyl or phenyl optionally substituted with one or more chloro, bromo atoms, C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.4 alkyl groups; R.sup.1 and R.sup.2 are each independently hydrogen atom or C.sub.1 -C.sub.4 alkyl moiety; and R.sup.3 and R.sup.4 are independently selected from C.sub.1 -C.sub.4 alkyl groups and pharmaceutically acceptable salts thereof, the use of them as anaesthetics, cardiovascular and hypometabolic agents and pharmaceutical compositions containing them.Type: GrantFiled: August 18, 1998Date of Patent: September 12, 2000Assignees: Procter & Gamble Company, Nauchno-Tekhnologicheskoepredpriyatie "Ligand"(Tovarischestvo S Organichennol Otvetstvennostju)Inventors: Oleg Nikolaevich Chupakhin, Larisa Petrovna Sidorova, Emma Afanasievna Tarakhty, Antonina Petrovna Novikova, Natalya Mikhailovna Perova, Valentin Antonovich Vinogradov, Michiel Franciscus van Ginkel
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Patent number: 6107301Abstract: The present invention provides novel compounds, compounds and pharmaceutical compositions thereof, and methods of using same in the treatment of affective disorders, anxiety, depression, post-traumatic stress disorders, eating disorders, supranuclear palsy, irritable bowel syndrome, immune suppression, Alzheimer's disease, gastrointestinal diseases, anorexia nervosa, drug and alcohol withdrawal symptoms, drug addiction, inflammatory disorders, or fertility problems. The novel compounds provided by this invention are those of formula: ##STR1## wherein R.sup.1, R.sup.3, R.sup.4, R.sup.5, Z, Y, V, X, X', J, K, L, and M are as defined herein.Type: GrantFiled: August 5, 1997Date of Patent: August 22, 2000Assignee: Dupont Pharmaceuticals CompanyInventors: Paul Edward Aldrich, Argyrios Georgios Arvanitis, Rajagopal Bakthavatchalam, James Peter Beck, Robert Scott Cheeseman, Robert John Chorvat, Paul Joseph Gilligan, Carl Nicholas Hodge, Zelda Rakowitz Wasserman
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Patent number: 6048824Abstract: Compounds of formula (I), wherein A is an unsubstituted or substituted aromatic or non-aromatic, monocyclic or bicyclic heterocyclic radical wherein a ring nitrogen atom may have been replaced by a group ##STR2## R.sub.1 is hydrogen or C.sub.1 -C.sub.3 alkyl; R.sub.2 is hydrogen or C.sub.1 -C.sub.3 alkyl; R.sub.3 is hydrogen, an unsubstituted or substituted C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl C.sub.2 -C.sub.6 alkenyl or C.sub.2 -C.sub.6 alkynyl group, or C(.dbd.O)--R.sub.5, R.sub.5 is C.sub.1 -C.sub.4 alkyl C.sub.1 -C.sub.4 alkoxy, an unsubstituted or substituted phenyl, phenoxy or benzyloxy group, or N(R.sub.6).sub.2, each R.sub.6, independently of the other, is hydrogen, C.sub.1 -C.sub.4 alkyl or unsubstituted or substituted phenyl, X is CH--NO.sub.2, N--CN or N--NO.sub.2 and n is from 1 to 3, in free form or in salt form, and, where appropriate, tautomers of those compounds and the salts thereof, can be used as agrochemical active ingredients and can be prepared in a manner known per se.Type: GrantFiled: November 22, 1995Date of Patent: April 11, 2000Assignee: Novartis CorporationInventors: Peter Maienfisch, Jozef Gonda, Olivier Jacob, Laurenz Gsell
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Patent number: 6046329Abstract: Compounds of formula I, in which the substituents and symbols have the meanings indicated in the description, R5-HT.sub.1A -agonists and .alpha..sub.1 -adrenoceptor blockers. Compositions containing these compounds as active ingredients are useful for treating those diseases which can be treated by 5-HT.sub.1A agonists or by .alpha..sub.1 -adrenoreceptor blockers.Type: GrantFiled: June 6, 1997Date of Patent: April 4, 2000Assignee: Byk Gulden Lomberg Chemische Fabrik GmbHInventors: Wolfgang Prusse, Wolf-Rudiger Ulrich
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Patent number: 6028068Abstract: Substituted 6H-1,3,4-thiadiazin-2-amines of the following general formula: ##STR1## wherein ##STR2## represents a morpholino, thiomorpholino, piperidino, pyrrolidino, or hexamethyienimino moiety, and pharmaceutically acceptable salts thereof which are used as anaesthetics, cardiovascular and hypometabolic agents, and the pharmaceutical compositions containing them.Type: GrantFiled: January 21, 1999Date of Patent: February 22, 2000Assignees: The Procter & Gamble Company, Nauchno-Tekhnologicheskoe Predpriyatie "Ligand"(Tovarischestvo S Ogranichennoi Otvetstvennostju)Inventors: Oleg Nikolaevich Chupakhin, Larisa Petrovna Sidorova, Emma Afanasievna Tarakhty, Antonina Petrovna Novikova, Natalya Mikhailovna Perova, Valentin Antonovich Vinogradov
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Patent number: 6025354Abstract: Arylalkyl-thiadiazinone derivatives of the formula I ##STR1## and physiologically unobjectionable salts thereof in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and Q have the meanings given in claim 1, exhibit phosphodiesterase IV inhibition and can be used for the therapy of asthmatic disorders.Type: GrantFiled: January 20, 1998Date of Patent: February 15, 2000Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Rochus Jonas, Michael Wolf, Michael Klockow
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Patent number: 6020335Abstract: An (N-(pyridinylmethyl)-heterocyclic)ylideneamine compound of the formula ##STR1## wherein R.sup.3, A, and B are as described below, and its pharmaceutically acceptable salts and prodrugs. Compounds of the formula I and their pharmaceutically acceptable salts and prodrugs are useful in the treatment of addictive disorders, such as the use of tobacco or other nicotine containing products, neurological and mental disorders such as senile dementia of the Alzheimer's type, Parkinson's disease, attentional hyperactivity disorder, anxiety, obesity, Tourette's Syndrome and ulcerative colitis.Type: GrantFiled: November 4, 1997Date of Patent: February 1, 2000Assignee: Pfizer IncInventors: Arthur A. Nagel, Steven W. Goldstein, Stanley Jung, Peter H. Dorff
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Patent number: 6011034Abstract: Insecticidal dihydrooxadiazine compounds having the formula: ##STR1## wherein X is O or S; R is a substituted or unsubstituted phenyl or heterocyclic group; R.sup.1 is halogen, haloalkyl or haloalkoxy; R.sup.2, R.sup.3 , and R.sup.4 are, independently, hydrogen, alkyl or alkoxy; R.sup.5 is nitro, cyano, alkoxy, alkyl, haloalkoxy, dialkylamino, alkylthio, phenoxy, phenylthio, or alkoxycarbonyl; R.sup.6 is hydrogen, alkyl, alkylthio, alkoxyalkyl, alkoxycarbonyl, acyl, or benzyl, wherein R.sup.3 and R.sup.5 together can form a ring.Type: GrantFiled: February 12, 1998Date of Patent: January 4, 2000Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Co./CIE.Inventors: Anupama Mishra, Mark Achiel Dekeyser, Paul Thomas McDonald
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Patent number: 5962437Abstract: A method of treating viral infections, and in particular HIV-1, hepatitis B virus and herpes viruses, is disclosed. The method comprising administering to a subject in need of such treatment an infection-combating amount of a phospholipid or phospholipid derivative.Type: GrantFiled: May 2, 1997Date of Patent: October 5, 1999Assignee: Wake Forest UniversityInventors: Louis S. Kucera, Susan L. Morris-Natschke, Khalid S. Ishaq
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Patent number: 5922748Abstract: Compounds of formula (I) ##STR1## wherein R and R.sup.1 are hydrogen, C.sub.1-4 alkyl or are linked to form a ring,A is a cycloalkyl or alkyl-cycloalkyl group,n is an integer from 0 to 3,W is an optionally substituted 5-or 6-membered heterocyclic ring; or W is an optionally substituted aryl, heteroaryl, aryloxy or thiophenoxy group; orW is a group --SO.sub.2 NR.sup.6 R.sup.7 --NHC(O)R.sup.6 R.sup.7 or --C(O)NHR.sup.6 R.sup.7 ; are useful in treating clinical conditions for which a "5-HT.sub.1 -like" receptor agonist is indicated.Type: GrantFiled: January 20, 1998Date of Patent: July 13, 1999Assignee: Glaxo Wellcome Inc.Inventors: Robert Charles Glen, David Lawrence Selwood, Graeme Richard Martin, Christopher James Foster
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Patent number: 5889183Abstract: A novel process for the preparation of taurylamide or its acid addition salts and the compounds taurolidine or taurultam obtainable therefrom, in which cysteamine or cystamine, in particular in the form of acid addition salts, is used as a starting material and in which the key intermediate is the compound .beta.-aminoethanesulphonylazide, in particular in the form of a water-soluble acid addition salt.Type: GrantFiled: August 13, 1997Date of Patent: March 30, 1999Inventors: Claus Herdeis, Christian Edwin Weis
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Patent number: 5883090Abstract: This invention relates to pyridizinone derivatives of formula I ##STR1## wherein the various substituents are defined in the specification, and salts thereof, which have useful pharmacological properties, in particular endothelin receptor-antagonistic properties. The compounds are thus useful for the treatment of illnesses associated with endothelin activities, such as hypertension, cardiac insufficiency, coronary heart disease, renal, cerebral and myocardial ischaemia, renal insufficiency, cerebral infarct, subarachnoid haemorrhage, arteriosclerosis pulmonary high blood pressure, inflammations, asthma, prostate hyperplasia, endotoxic shock and in complications after the administration of immunosuppressants which produce renal vasoconstriction.Type: GrantFiled: June 6, 1997Date of Patent: March 16, 1999Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Dieter Dorsch, Mathias Osswald, Werner Mederski, Claudia Wilm, Claus Jochen Schmitges, Maria Christadler
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Patent number: 5859008Abstract: Arylalkyl diazinone derivatives of the formula I ##STR1## and their physiologically acceptable salts, in whichR.sup.1, R.sup.2, R.sup.3, R.sup.4, B, Q and X have the meanings indicated in claim 1, exhibit phosphodiesterase IV inhibition and can be employed for the treatment of inflammatory processes and also of allergies, asthma and autoimmune disorders.Type: GrantFiled: September 13, 1996Date of Patent: January 12, 1999Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Rochus Jonas, Michael Wolf, Norbert Beier
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Patent number: 5824677Abstract: Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocyle. R.sub.3 may be either hydrogen or C.sub.13. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.Type: GrantFiled: June 7, 1995Date of Patent: October 20, 1998Assignee: Cell Therapeutics, Inc.Inventors: J. Peter Klein, Gail E. Underiner, Anil M. Kumar
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Patent number: 5747489Abstract: Arylalkyl-thiadiazinone derivatives of the formula I ##STR1## and physiologically unobjectionable salts thereof in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and Q have the meanings given in claim 1, exhibit phosphodiesterase IV inhibition and can be used for the therapy of asthmatic disorders.Type: GrantFiled: January 26, 1996Date of Patent: May 5, 1998Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Rochus Jonas, Michael Wolf, Michael Klockow
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Patent number: 5714499Abstract: The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.Type: GrantFiled: June 17, 1994Date of Patent: February 3, 1998Assignee: Corvas International, Inc.Inventors: Joseph E. Semple, Odile E. Levy, Ruth F. Nutt, William C. Ripka
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Patent number: 5705500Abstract: Selected sulfonylalkanoylamino hydroxyethylamine sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: June 7, 1995Date of Patent: January 6, 1998Assignee: G.D. Searle & Co.Inventors: Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, Joseph J. McDonald
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Patent number: 5705497Abstract: 3-Alkoxycarbonyl thiadiazinones of the formula I ##STR1## and physiologically unobjectionable salts thereof, in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, Q and n have the meanings described herein, exhibit a positively inotropic action and can be employed for the therapy of cardiac insufficiency.Type: GrantFiled: January 11, 1996Date of Patent: January 6, 1998Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Rochus Jonas, Inge Lues, Norbert Beier, Klaus-Otto Minck
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Patent number: 5659031Abstract: There is provided a 1-(3-heterocyclylphenyl)-s-triazine-2,4,6-oxo or thiotrione compound having the structural formula I ##STR1## Further provided are a composition and a method comprising that compound for the control of undesirable plant species.Type: GrantFiled: June 2, 1995Date of Patent: August 19, 1997Assignee: American Cyanamid CompanyInventors: Alvin Donald Crews, Jr., Gary Mitchell Karp, Mark Christopher Manfredi, Michael Anthony Guaciaro
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Patent number: 5641783Abstract: Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocycle. R.sub.3 may be either hydrogen or C.sub.1-3. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.Type: GrantFiled: September 8, 1994Date of Patent: June 24, 1997Assignee: Cell Therapeutics, Inc.Inventors: J. Peter Klein, Gail E. Underiner, Anil M. Kumar
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Patent number: 5633371Abstract: Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein, the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adenosylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuronal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.Formula Ia above embraces not only compounds which form part of the invention, but also known compounds: the compounds which form part of the invention can be prepared according to known methods.Type: GrantFiled: September 15, 1995Date of Patent: May 27, 1997Assignee: Hoffmann-La Roche Inc.Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mos e Da Prada, Gerhard Z urcher
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Patent number: 5616579Abstract: Compounds of formula (I): ##STR1## [wherein: R.sup.1 is a cyclic amino group, or a dialkylamino group; R.sup.2 a group of formula --NHCHR.sup.3 R.sup.4 wherein R.sup.3 and R.sup.4 are each alkyl aryl or aralkyl, or together form a cycloalkyl group, or R.sup.2 is an aromatic heterocyclic group, or a group of formula --B--S(O).sub.m --R.sup.5 wherein R.sup.5 is a substituted alkyl group, or an aromatic heterocyclic group; B is an alkylene or alkylidene group; m is 0, 1 or 2; A is a group of formula --CH.dbd.CH-- or --(CH.sub.2).sub.n --, where n is 1, 2 or 3]; and salts thereof have valuable anti-ulcer activity.Type: GrantFiled: March 22, 1993Date of Patent: April 1, 1997Assignee: Sankyo Company, LimitedInventors: Hiroshi Fukumi, Mitsuo Sugiyama, Keiichi Tabata, Koichi Kojima
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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