At 2-position And At 4- Or 6-position Patents (Class 544/323)
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Publication number: 20030216406Abstract: Compounds of formula (I), wherein R1, p, R2, q, R3 and R4 are defined within, and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described are processes for their preparation and their use as medicaments, particularly medicaments for producing a cell cycle inhibitory (anti-cell-proliferation) effect in a warm-blooded animal, such as man.Type: ApplicationFiled: January 7, 2003Publication date: November 20, 2003Inventors: Andrew Peter Thomas, Nicholas John Newcombe, David William Heaton
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Patent number: 6645965Abstract: Nitric acid salts with medicines having an antihypertensive activity.Type: GrantFiled: December 12, 2000Date of Patent: November 11, 2003Assignee: Nicox S.A.Inventor: Piero Del Soldato
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Patent number: 6646125Abstract: The present invention relates to a process for the preparation of a carbocyclic purine nucleoside analogue of formula (I), its salts and pharmaceutically acceptable derivatives thereof which comprises hydrolysing a compound of formula (IV) wherein P is a protecting group, in the presence of an acid, condensing the product of formula (V) formed in situ in the presence of a base with a compound of formula (VI) followed by in situ ring closure of the resulting intermediate.Type: GrantFiled: April 25, 2000Date of Patent: November 11, 2003Assignee: SmithKline Beecham CorporationInventors: Martin Francis Jones, Christopher John Wallis
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Publication number: 20030199534Abstract: The invention relates to inhibitors of kinases, compositions comprising the inhibitors, and methods of using the inhibitors and inhibitor compositions. The inhibitors and compositions comprising them are useful for treating disease or disease symptoms. The invention also provides for methods of making kinase inhibitor compounds, methods of inhibiting kinase activity, and methods for treating disease or disease symptoms.Type: ApplicationFiled: January 28, 2003Publication date: October 23, 2003Applicant: Amgen Inc.Inventors: David M. Armistead, Jean E. Bemis, Lucian V. DiPietro, Stephanie D. Geuns-Meyer, Gregory J. Habgood, Joseph L. Kim, Joseph J. Nunes, Vinod F. Patel, Leticia M. Toledo-Sherman
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Publication number: 20030181474Abstract: Pyrimidine derivatives of formula (I) wherein Q1, Q2, G and R1 are as defined within; and pharmaceutically acceptable salts and in vivo hydrolysable esters thereof are described. Processes for their manufacture, pharmaceutical compositions and their use as cyclin-dependent serine/threonine kinase (CDK) and focal adhesion kinase (FAK) inhibitors are also described.Type: ApplicationFiled: August 5, 2002Publication date: September 25, 2003Inventors: Elizabeth Janet Pease, Emma Jane Williams, Robert Hugh Bradbury, Stuart Eric Pearson
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Publication number: 20030171359Abstract: The present invention relates to trisubstituted pyrimidines of formula (I) 1Type: ApplicationFiled: October 16, 2002Publication date: September 11, 2003Applicant: Boehringer Ingelheim Pharma KGInventors: Georg Dahmann, Frank Himmelsbach, Bernd Krist, Martin Lenter, Alexander Pautsch, Gisela Schnapp, Martin Steegmaier, Helmut Wittneben, Anthony S. Prokopowicz, Walter Spevak, Andreas Schoops, Steffen Steurer
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Publication number: 20030162802Abstract: Pyrimidine phosphodiesterase 7 (PDE 7) inhibitors of the following formula 1Type: ApplicationFiled: June 17, 2002Publication date: August 28, 2003Inventors: Junqing Guo, Joseph Barbosa, William John Pitts, Marianne Carlsen, Claude Quesnelle, Marco Dodier
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Patent number: 6600044Abstract: A process for the preparation of 1,3-oxathiolane nucleoside analogues in predominantly the cis-form, from mixture of cis-/trans-1,3-oxathiolane nucleosides or their protected derivatives thereof, comprising: (i) treatment of the cis-/trans-1,3-oxathiolane nucleosides (or protected derivatives thereof) with a pyrimidine base (or it derivatives thereof) and an acid, (ii) adding a suitable acid to the obtained cis-/trans-mixture of isomers, (iii) selective crystallization of the desired cis-isomer salt from a solvent or combination of solvents, and (iv) treatment of the predominantly cis-isomer salt with a suitable base to offer the free 1,3-oxathiolane nucleosides, and thereafter optionally repeating steps (i) to (iv) inclusive.Type: GrantFiled: June 18, 2001Date of Patent: July 29, 2003Assignee: Brantford Chemicals Inc.Inventors: K. S. Keshava Murthy, Gurijala V. Reddy, Zhi-xian Wang, Chandrawansha B. W. Senanayake
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Publication number: 20030134838Abstract: The present invention relates to trisubstituted pyrimidines of formula 1Type: ApplicationFiled: October 16, 2002Publication date: July 17, 2003Applicant: Boehringer Ingelheim Pharma KGInventors: Klaus Bornemann, Hans Briem, Cornelia Dorner-Clossek, Katja Fechteler, Klaus Fuchs, Frank Himmelsbach, Klaus Klinder, Markus Kostka
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Patent number: 6593326Abstract: A pyrimidine derivative of formula (I): wherein: R1 is an optional substituent as defined within; Rx is selected from halo, hydroxy, nitro, amino, cyano, mercapto, carboxy, sulphamoyl, formamido, ureido or carbamoyl or a group of formula (Ib): A—B—C— as defined within; Q1 and Q2 are independently selected from aryl, a 5- or 6-membered monocyclic moiety; and a 9- or 10-membered bicyclic heterocyclic moiety; and one or both of Q1 and Q2 bears on any available carbon atom one substituent of formula (Ia) as defined within; and Q1 and Q2 are optionally further substituted; or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof; are useful as anti-cancer agents; and processes for their manufacture and pharmaceutical compositions containing them are described.Type: GrantFiled: August 23, 2001Date of Patent: July 15, 2003Assignee: AstraZeneca ABInventors: Robert H Bradbury, Gloria A Breault, Philip J Jewbury, Janet E Pease
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Patent number: 6583148Abstract: The present invention relates to novel derivatives of a series of substituted pyrimidines, to pharmaceutical compositions which contain them, to methods for their preparation and to their use in therapy, particularly in the treatment of neurodegenerative or other neurological disorders of the central and peripheral systems.Type: GrantFiled: April 8, 1999Date of Patent: June 24, 2003Assignee: Krenitsky Pharmaceuticals, Inc.Inventors: James L. Kelley, Thomas A. Krenitsky, Lilia M. Beauchamp
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Publication number: 20030114472Abstract: This invention concerns the use of compounds of formula 1Type: ApplicationFiled: November 1, 1999Publication date: June 19, 2003Inventors: BART DE CORTE, MARC RENE DE JONGE, JAN HEERES, CHIH YUNG HO, PAUL ADRIAAN JAN JANSSEN, ROBERT W. KAVASH, LUCIEN MARIA HENRICUS KOYMANS, MICHAEL JOSEPH KUKLA, DONALD WILLIAM LUDOVICI, KOEN JEANNE ALFONS VAN AKEN
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Publication number: 20030105323Abstract: 1.Type: ApplicationFiled: August 19, 2002Publication date: June 5, 2003Applicant: SUMITOMO PHARMACEUTICALS COMPANY LIMITEDInventors: Hitoshi Fujita, Fujio Antoku, Norio Fujiwara, Kiyotaka Iwai, Hiroshi Tanaka, Hajime Kawakami
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Publication number: 20030083317Abstract: This invention concerns the use of the compounds of formula 1Type: ApplicationFiled: June 28, 2002Publication date: May 1, 2003Inventors: Koenraad Jozef Lodewijk Marcel Andries, Bart De Corte, Marc Rene De Jonge, Jan Heeres, Chih Yung Ho, Marcel August Constant Janssen, Paul Adriaan Jan Janssen, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken
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Patent number: 6525200Abstract: Multicyclic aromatic compounds useful as complexing agents having the general formula: Methods of complexing and quantitating a component in a sample such as urea or guanidine are also disclosed.Type: GrantFiled: August 10, 2000Date of Patent: February 25, 2003Assignee: Roche Diagnostics CorporationInventors: Alisher B. Khasanov, Thomas W. Bell
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Publication number: 20030032647Abstract: An aromatic nitrogen-containing 6-membered cyclic compound of the formula (I): 1Type: ApplicationFiled: August 10, 2001Publication date: February 13, 2003Inventors: Koichiro Yamada, Kenji Matsuki, Kenji Omori, Kohei Kikkawa
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Patent number: 6518425Abstract: Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include efficient methods for the preparation of the 1,3-oxathiolane ring and subsequent condensation of the 1,3-oxathiolane with a pyrimidine or purine base. Using the processes described herein, the compounds can be provided as isolated enantiomers.Type: GrantFiled: May 15, 2000Date of Patent: February 11, 2003Assignees: Emory University, Triangle Pharmaceuticals, Inc.Inventors: George R. Painter, Dennis C. Liotta, Merrick R. Almond, Darryl G. Cleary, Josè D. Soria, Marcos Sznaidman
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Patent number: 6511659Abstract: Hair growth-/hair loss-affecting cosmetic/therapeutic compositions contain an effective amount of at least one 2-amino-4-alkylaminopyrimidine 3-oxide having the structural formula (I): in which R1 is an alkyl radical having from 5 to 20 carbon atoms, and Z is either a hydrogen atom or a radical —OR2, wherein R2 is an alkyl radical having from 1 to 12 carbon atoms, or an acyl derivative or acid addition salt thereof.Type: GrantFiled: June 6, 2001Date of Patent: January 28, 2003Assignee: Societe L'Oreal S.A.Inventors: Yann Mahe, Jean-François Michelet, Patrick Pichaud, Jean-Baptiste Galey
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Publication number: 20030004174Abstract: The invention relates to inhibitors of kinases, compositions comprising the inhibitors, and methods of using the inhibitors and inhibitor compositions. The inhibitors and compositions comprising them are useful for treating disease or disease symptoms. The invention also provides for methods of making kinase inhibitor compounds, methods of inhibiting kinase activity, and methods for treating disease or disease symptoms.Type: ApplicationFiled: February 16, 2001Publication date: January 2, 2003Inventors: David M. Armistead, Jean E. Bemis, Lucian V. DiPietro, Stephanie D. Geuns-Meyer, Gregory J. Habgood, Joseph L. Kim, Joseph J. Nunes, Vinod F. Patel, Leticia M. Toledo-Sherman
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Patent number: 6500952Abstract: The invention relates to the preparation of compounds (I) in which A=H or acyl and R1, R21, R3, R, n, X, Y and Z are as defined in claim 1 by halogenation and rearrangement of compounds (II) (optionally salt) to give compounds (III) a) ammonolysis of (III) to (IV), reduction of the nitro group and reaction with carbamate (salts) (VI) of the formula Ar—OCO—N(M)—Het, where Ar=phenyl, M=H or cation and Het=heterocycle from formula (I), to give compounds (I) (A=H), or b) ammonolysis of (III) to (IV), reaction with carbamate (salt) (VI) and reduction of resulting compounds (VII) at the NO2 group to give compounds (I) (A=H), or c) reaction of (III) with cyanates and amines (VIII) of the formula HNR3—Het and reduction of the resulting compound (VII) at the NO2 group to give compounds (I) (A=H) and optional acylation if A is to be other than H.Type: GrantFiled: September 18, 2000Date of Patent: December 31, 2002Assignee: Hoechst Schering AgrEvo GmbHInventors: Gerhard Schnabel, Jan Vermehren, Lothar Willms
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Patent number: 6448403Abstract: A compound of formula (VI) A process for the preparation of a compound of formula (VI): comprising: reacting a compound of formula (III): with an amine of formula R3NH2.Type: GrantFiled: July 31, 1996Date of Patent: September 10, 2002Assignee: SmithKline Beecham CorporationInventors: Susan Mary Daluge, Michael Tolar Martin
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Patent number: 6440975Abstract: The invention relates to amino acid derivatives of the formula I where the radicals have the meanings stated in the description, and to the use thereof as drugs.Type: GrantFiled: March 31, 1998Date of Patent: August 27, 2002Assignee: Abbott LaboratoriesInventors: Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Hartmut Riechers, Liliane Unger, Manfred Raschack
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Patent number: 6440986Abstract: This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR4 or N; n is 0 to 4; Q is hydrogen or —NR1R2; R1 and R2 are selected from hydrogen, hydroxy, C1-12alkyl, C1-12alkyloxy, C1-12alkylcarbonyl, C1-12alkyloxycarbonyl, aryl, amino, mono- or di(C1-12alkyl)amino, mono- or di(C1-12alkyl)aminocarbonyl wherein each C1-12alkyl may optionally be substituted; or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-12alkyl)aminoC1-4alkylidene; R3 is hydrogen, aryl, C1-6alkylcarbonyl, optionally substituted C1-6alkyl, C1-6alkyloxycarbonyl,; and R4 is hydroxy, halo, optionally substituted C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy; R5 is hydrogen or C1-4alkyl; L is optionally substituted C1-10alkyl, C3-10alkenyl, C3-10alkynyl, C3-7cycloalkyl; or L is —X1—R6 orType: GrantFiled: December 27, 2000Date of Patent: August 27, 2002Assignee: Janssen Pharmaceutica, N.V.Inventors: Koenraad Jozef Lodewijk Marcel Andries, Bart De Corte, Marc René De Jonge, Jan Heeres, Chih Yung Ho, Marcel August Constant Janssen, Paul Adriaan Jan Janssen, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken
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Patent number: 6432963Abstract: Pyrimidine-5-carboxamide derivatives represented by a general formula (I) or salts thereof [wherein each symbol has the following meaning; X: O, S, NR1, CO, NR1CO, CONR1, C═N—OR1 or a bond, Y: a lower alkylene group which may be substituted by OR1 or —NHR1, or a bond, Z: O, NR2 or a bond, A: H, or a lower alkyl which may have a substituent, a —CO-lower alkyl which may have a substituent, an aryl which may have a substituent, a heteroaryl which may have a substituent, a cycloalkyl which may have a substituent or a nitrogen-containing saturated heterocyclic group which may have a substituent, B: an aryl which may have a substituent or a heteroaryl group which may have a substituent, R1, R2: H, a lower alkyl or a —CO-lower alkyl group].Type: GrantFiled: June 15, 2000Date of Patent: August 13, 2002Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Hiroyuki Hisamichi, Ryo Naito, Souichirou Kawazoe, Akira Toyoshima, Kazuhito Tanabe, Eiichi Nakai, Atsushi Ichikawa, Akiko Orita, Makoto Takeuchi
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Patent number: 6433170Abstract: The invention relates to a novel method for producing 4-[(2′,5′-diamino-6′-halopyrimidine-4′-yl)amino]-cyclopent-2-enylmethanols of general formula (I), wherein X represents a halogen atom. According to the inventive method amino-4,6-halopyrimidine of general formula (II), wherein X has the aforementioned meaning, is reacted with a 4-aminocyclopent-2-enylmethanol of formula (III) or with a salt thereof in the presence of a base in a polar protic solvent.Type: GrantFiled: June 17, 2001Date of Patent: August 13, 2002Assignee: Lonza GroupInventors: Walter Brieden, Elie Saikali
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Publication number: 20020099207Abstract: The invention relates to compounds of the formula 1Type: ApplicationFiled: October 15, 2001Publication date: July 25, 2002Inventor: Heinz Stadler
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Patent number: 6417141Abstract: The invention relates to novel aminouracils of the general formula (I) in which, Q, R1, R2, R3, R4, R5, R6 and R7 are each as defined in the description, to their use as herbicides and to novel intermediates.Type: GrantFiled: January 21, 1998Date of Patent: July 9, 2002Assignee: Bayer AktiengesellschaftInventors: Roland Andree, Mark Wilhelm Drewes, Otto Schallner, Markus Dollinger, Hans-Joachim Santel
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Patent number: 6417359Abstract: A compound having the formula: wherein X′ is nitrogen or carbon bonded to a substituent species characterized as having a sigma m value greater than 0, less than 0 or 0; X is nitrogen or carbon bonded to a substituent species characterized as having a sigma m value greater than 0, less than 0, but not equal to 0; A, A′ and A″ are individually substituent species characterized as having a sigma m value greater than 0, less than 0 or 0; Z′ is a substituent other than hydrogen; j is an integer from 0 to 5; and the wavy line in the structure indicates that the compound can exist in the form of an enantiomer or a diasteromer; Z″ is hydrogen or a substituent other than hydrogen; Y is C═O, C(OH)R′ or C—A, where R′ is hydrogen or lower alkyl.Type: GrantFiled: April 27, 2000Date of Patent: July 9, 2002Assignee: Targacept, Inc.Inventors: Peter Anthony Crooks, Haeil Park, Balwinder Singh Bhatti, William Scott Caldwell, Gary Maurice Dull
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Patent number: 6410482Abstract: (Het)Arylsulfonylureas having an imino function, their preparation, and their use as herbicides and plant growth regulators Compounds of the formula (I) and salts thereof in which A is a (hetero)aromatic or heterocyclic bridge linked to the group SO2 by a direct bond, or via O, S, NH, CH2 or via alkylated NH or alkylated methylene, B is a group having an imino-containing fragment N═C—N, N═C—S, N═C—O or N═C—C which is linked to A by one of the nitrogen atoms of the fragment, R═H or an aliphatic radical, W═O or S and X, Y and Z are as defined in claim 1 are suitable as herbicides and plant growth regulators. The preparation is carried out for example similarly to known processes via novel intermediates of the formula (XII) (cf.Type: GrantFiled: May 13, 1997Date of Patent: June 25, 2002Assignee: Hoechst Schering AgrEvo GmbHInventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
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Publication number: 20020072521Abstract: Arylpyrimidine compounds are provided that can act as selective modulators of CRF receptors. These compounds are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided.Type: ApplicationFiled: March 16, 2001Publication date: June 13, 2002Inventors: Taeyoung Yoon, Stephane DeLombaert, Kevin J. Hodgetts, Dario Doller
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Publication number: 20020052495Abstract: Carboxylic acid derivatives 1Type: ApplicationFiled: December 27, 2000Publication date: May 2, 2002Inventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Stefan Muller, Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Wolfgang Wernet, Liliane Unger, Manfred Raschack
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Publication number: 20020052386Abstract: The invention relates to inhibitors of kinases, compositions comprising the inhibitors, and methods of using the inhibitors and inhibitor compositions. The inhibitors and compositions comprising them are useful for treating disease or disease symptoms. The invention also provides for methods of making kinase inhibitor compounds, methods of inhibiting kinase activity, and methods for treating disease or disease symptoms.Type: ApplicationFiled: February 16, 2001Publication date: May 2, 2002Inventors: David M. Armistead, Jean E. Bemis, Lucian V. DiPietro, Stephanie D. Geuns-Meyer, Gregory J. Habgood, Joseph L. Kim, Joseph J. Nunes, Vinod F. Patel, Leticia M. Toledo-Sherman
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Patent number: 6372758Abstract: A sulfamato hydroxamic acid compound that, inter alia, inhibits matrix metalloprotease (mmp) activity is disclosed as are a process for preparing the same, intermediate compounds useful in those syntheses, and a treatment process that comprises administering a contemplated sulfamato hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: June 19, 2001Date of Patent: April 16, 2002Assignee: G. D. Searle & CompanyInventors: Gary A DeCrescenzo, Joseph G Rico, Terri Boehm, Jeffery N Carroll, Darren J Kassab, Deborah A Mischke, Shashidhar Rao
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Publication number: 20020035109Abstract: This invention is directed to benzamidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-,states characterized by thrombotic activity.Type: ApplicationFiled: August 7, 2001Publication date: March 21, 2002Applicant: Berlex Laboratories, Inc.Inventors: Brad O. Buckman, David D. Davey, William J. Guilford, Michael M. Morrissey, Howard P. Ng, Gary B. Phillips, Shung C. Wu, Wei Xu
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Publication number: 20020032206Abstract: Patients susceptible to or suffering from central nervous system disorders are treated by administering effective amounts of aryl substituted aliphatic amine compounds, aryl substituted olefinic amine compounds or aryl substituted acetylenic amine compounds. A representative compound is (E)-N-methyl-5-(3-pyridinyl)-4-penten-2-amine.Type: ApplicationFiled: October 9, 2001Publication date: March 14, 2002Inventors: William Scott Caldwell, Gary Maurice Dull, Garyland Page Dobson
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Publication number: 20020032199Abstract: Amino-pyrimidine and amino-triazine derivatives having 5-HT7 antagonist activity for the treatment of sleeping disorders, depression, schizophrenia, anxiety, obsessive compulsive disorders, circadian rhythm disorders, ocular disorders and/or centrally and peripherally mediated hypertension are provided.Type: ApplicationFiled: April 24, 2001Publication date: March 14, 2002Inventors: Michael A. Poss, Ashok V. Purandare, Ronald J. Mattson, Li-Qiang Sun
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Patent number: 6342503Abstract: 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'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, R4, R5, Z, Y, V, X, X′, J, K, L, and M are as defined herein.Type: GrantFiled: January 7, 1998Date of Patent: January 29, 2002Assignee: DuPont Pharmaceuticals CompanyInventors: Paul Edward Aldrich, Argyrios Georgios Arvanitis, Robert Scott Cheeseman, Robert John Chorvat, Thomas Eugene Christos, Paul Joseph Gilligan, Dimitri Emil Grigoriadis, Carl Nicholas Hodge, Paul John Krenitsky, Everett Latham Scholfield, Sang William Tam, Zelda Rakowitz Wasserman
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Publication number: 20020009748Abstract: Mixtures of chemical compounds are provided having antibacterial and other utility. The mixtures are formed, preferably in solution phase, from the reaction of a purine or pyrimiding heterocyclic scaffold with a set of related chemical substituients, optionally through employment of a tether moiety. Libraries formed in accordance with the invention have utility per se and are articles of commerce. They can be used to screen for pesticides, drugs and other biologically active compounds.Type: ApplicationFiled: May 13, 1998Publication date: January 24, 2002Inventor: PHILLIP DAN COOK
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Patent number: 6331506Abstract: Disubstituted methylidenehydrazinophenylsulfonylureas, processes for their preparation and their use as herbicides and plant growth regulators Compounds of the formula (I) and salts thereof in which R1 to R6, W, X, Y, Z are as defined in claim 1 and the group R2R3C is a carbon atom which is subsituted by at least one electron-withdrawing radical R2 or R3 are suitable as herbicides and plant growth regulators. They can be prepared in accordance with known processes via intermediates, some of which are novel.Type: GrantFiled: September 16, 1998Date of Patent: December 18, 2001Assignee: Hoechst Schering AgrEvo GmbHInventors: Heinz Kehne, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
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Patent number: 6329323Abstract: This invention relates to aminosulfonylureas possessing a high herbicidal activity, a process for their preparation and their application to control control weeds in agriculture. Aminosulfonylureas of this invention have the following formula (I): wherein R, R1, R2, R3, R4, R5, and R6 are described in the specification.Type: GrantFiled: October 21, 1999Date of Patent: December 11, 2001Assignee: Isagro Ricerca S.r.l.Inventors: Franco Bettarini, Sergio Massimini, Giovanni Meazza, Giampaolo Zanardi, Domenico Portoso, Ernesto Signorini
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Patent number: 6326375Abstract: Spiro compounds of the general formula (I): wherein Ar1 represents an optionally substituted aryl or heteroaryl; n represents 0 or 1; T, U, V and W each represent a nitrogen atom or an optionally substituted methine group, wherein at least two of which represent said methine group; X represents nitrogen; Y represents an optionally substituted imino or oxygen atom, which exhibit neuropeptide Y receptor (NPY) antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders, central nervous system disorders, metobolic diseases and the like.Type: GrantFiled: August 18, 2000Date of Patent: December 4, 2001Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Takehiro Fukami, Akio Kanatani, Akane Ishihara, Yasuyuki Ishii, Toshiyuki Takahashi, Yuji Haga, Toshihiro Sakamoto, Takahiro Itoh
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Publication number: 20010044444Abstract: Hair growth-/hair loss-affecting cosmetic/therapeutic compositions contain an effective amount of at least one 2-amino-4-alkylaminopyrimidine 3-oxide having the structural formula (I): 1Type: ApplicationFiled: June 6, 2001Publication date: November 22, 2001Inventors: Yann Mahe, Jean-Francois Michelet, Patrick Pichaud, Jean-Baptiste Galey
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Publication number: 20010031868Abstract: A novel process is described for the preparation of N-(amino-4,6-dihalopyrimidine)formamides of the formula 1Type: ApplicationFiled: May 31, 2001Publication date: October 18, 2001Inventors: Elie Saikali, Walter Brieden
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Patent number: 6291468Abstract: Hair growth-/hair loss-affecting cosmetic/therapeutic compositions contain an effective amount of at least one 2-amino-4-alkylaminopyrimidine 3-oxide having the structural formula (I): in which R1 is an alkyl radical having from 5 to 20 carbon atoms, and Z is either a hydrogen atom or a radical —OR2, wherein R2 is an alkyl radical having from 1 to 12 carbon atoms, or an acyl derivative or acid addition salt thereof.Type: GrantFiled: July 23, 1999Date of Patent: September 18, 2001Assignee: Societe L'Oreal S.A.Inventors: Yann Mahe, Jean-Fran{tilde under (c)}ois Michelet, Patrick Pichaud, Jean-Baptiste Galey
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Patent number: 6288060Abstract: Pyrimidines and triazines of formula (I) wherein R is C1-6alkyl, amino, mono- or diC1-6alkylamino; R1 is hydrogen, C1-6alkyl, C3-6alkenyl, hydroxyC1-6alkyl or C1-6alkyloxy-C1-6alkyl; R2 is C1-6alkyl, mono- or diC3-6cycloalkylmethyl, phenylmethyl, substituted phenylmethyl, C1-6alkyloxy-C1-6alkyl, hydroxyC1-6alkyl, C1-6alkyloxycarbonylC1-6alkyl, C3-6alkenyl; or R1 and R2 taken together with the nitrogen to which they are attached may form a pyrrolidinyl, morpholinyl or piperidinyl group; X is N or CR3; R3 is hydrogen or C1-6alkyl; R4 is phenyl or substituted phenyl; A is or —CR7R8— wherein R5 and R6 each independently are hydrogen or C1-4alkyl; R7 is hydrogen or OH, R8 is hydrogen or C1-6alkyl; having CRF receptor antagonistic properties; pharmaceutical compositions containing these compounds as active ingredients; methods of treating disorders related to hypersecretion of CRF such as depression, anxiety, substance abuse, by administering an effective amountType: GrantFiled: April 15, 1998Date of Patent: September 11, 2001Assignees: Neurocrine Biosciences, Inc., Janssen Pharmaceutia, N.V.Inventors: Thomas R. Webb, Terence J. Moran, James R. McCarthy
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Patent number: 6281219Abstract: The present invention provides compounds of Formula I methods for their preparation and their use as acaricidal and insecticidal agents.Type: GrantFiled: July 12, 1999Date of Patent: August 28, 2001Assignee: American Cyanamid Co.Inventors: Salvatore John Cuccia, William Wakefield Wood, Brian Lee Buckwalter, John Francis Chiarello, Linda Barbara Fleming
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Patent number: 6274588Abstract: The invention provides compounds of the formula wherein R1 is hydrogen or halogen; R2 is hydrogen, halogen, lower alkyl or lower alkoxy; R1 and R2 may together be —CH═CH—CH═CH—, wherein R1 and R2 together with the two carbon ring atoms to which they are attached form a fused ring; R3 is halogen, trifluoromethyl, lower alkyl or lower alkoxy; R4/R4′ are each independently hydrogen or lower alkyl; R5 is lower alkyl, lower alkoxy, amino, phenyl, hydroxy-lower alkyl, cyano-lower alkyl, carbamoyl-lower alkyl, pyridyl, pyrimidyl, —(CH2)n-piperazinyl, which is optionally substituted by one or two lower alkyl groups or by hydroxy-lower alkyl, —(CH2)n-morpholinyl, —(CH2)n-piperidinyl, —(CH2)n+1-imidazolyl, lower alkyl-sulfanyl, lower alkyl-sulfonyl, benzylamino, —NH—(CH2)n+1N(R4″)2, —(CH2)n+1N(R4″)2, —O—(CH2)n+1-morpholinyl, —O—(CH2)n+1-piperidinyl or —O&Type: GrantFiled: May 22, 2000Date of Patent: August 14, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Michael Bös, Guido Galley, Thierry Godel, Torsten Hoffmann, Walter Hunkeler, Patrick Schnider, Heinz Stadler
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Publication number: 20010011094Abstract: This invention concerns the use of the compounds of formula 1Type: ApplicationFiled: December 27, 2000Publication date: August 2, 2001Inventors: Koenraad Jozef Lodewijk Marcel Andries, Bart De Corte, Marc Rene De Jonge, Jan Heeres, Chih Yung Ho, Marcel August Constant Janssen, Paul Adriaan Jan Janssen, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken
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Patent number: 6255316Abstract: The present invention relates to several new, polymorphous crystal forms of Dicyclanil, and hydrates and solvates thereof, as well as the preparation thereof. In particular, the invention relates to substantially pure crystal forms of Dicyclanil, having characteristic lattice structures, which are effective for the control of insects and ectoparasites.Type: GrantFiled: February 22, 2000Date of Patent: July 3, 2001Assignee: Novartis Animal Health US, Inc.Inventors: Erwin Marti, Walter Oechslein, André Joseph Geoffroy
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Patent number: 6245773Abstract: This invention is directed to dihydropyrimidine compounds of the following formula: which are selective antagonists for human &agr;1A receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia and for the treatment of any disease where antagonism of the &agr;1A receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: May 16, 1997Date of Patent: June 12, 2001Assignee: Synaptic Pharmaceutical CorporationInventors: Wai C. Wong, Bharat Lagu, Dhanapalan Nagarathnam, Mohammad R. Marzabadi, Charles Gluchowski