Sulfur Attached Indirectly To The Diazine Ring By Nonionic Bonding (e.g., Thiamines, Etc.) Patents (Class 544/327)
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Patent number: 7115599Abstract: This invention relates to compounds of the formula in which R1, R2, and R3 are as defined in the claims, to a process for preparing such compounds, to pharmaceutical compositions containing such compounds, and to methods of using such compounds for treatment of hypertension and sexual dysfunction.Type: GrantFiled: November 12, 2001Date of Patent: October 3, 2006Assignee: Bayer AktiengesellschaftInventors: Johannes-Peter Stasch, Achim Feurer, Stefan Weigand, Elke Stahl, Dietmar Flubacher, Cristina Alonso-Alija, Frank Wunder, Dieter Lang, Klaus Dembowsky, Alexander Straub, Elisabeth Perzborn
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Patent number: 7105523Abstract: This invention relates to compounds of the formula wherein R1 is H or a di-C1-6-alkylaminocarbonyl raical, and R2 is a radical of the formula —O—C(X)—NR3R4 wherein X is O or S. A process for preparing such compounds, pharmaceutical compositions containing them, and methods for using them in treatment of hypertension are also disclosed and claimed.Type: GrantFiled: November 9, 2001Date of Patent: September 12, 2006Assignee: Bayer AktiengeselischaftInventors: Johannes-Peter Stasch, Achim Feurer, Stefan Weigand, Elke Stahl, Dietmar Flubacher, Cristina Alonso-Alija, Frank Wunder, Dieter Lang, Klaus Dembowsky, Alexander Straub, Elisabeth Perzborn
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Patent number: 7067522Abstract: 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: GrantFiled: November 24, 2004Date of Patent: June 27, 2006Assignee: AstraZeneca ABInventors: Elizabeth Janet Pease, Emma Jane Williams, Robert Hugh Bradbury, Stuart Eric Pearson
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Patent number: 7034019Abstract: The present invention concerns compounds of formula (A1)(A2)N—R1 (I),the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and stereochemically isomeric forms thereof, wherein R1 is substituted C1-6alkyl; —S(?O)—R8; —S(?O)2—R8; C7-12alkylcarbonyl; optionally substituted C1-6alkyloxycarbonylC1-6alkylcarbonyl; with R8 being C1-6alkyl, aryl1 or Het1; (A1)(A2)N— is the covalently bonded form of the corresponding intermediate of formula (A1)(A2)N—H, which is a HIV replication inhibiting pyrimidine of formulaType: GrantFiled: May 3, 2001Date of Patent: April 25, 2006Assignee: Janssen Pharmaceutica N.V.Inventors: Michael Joseph Kukla, Donald William Ludovici, Robert William Kavash, Bart Lieven Daniel De Corte, Jan Heeres, Paul Adriaan Jan Janssen, Lucien Maria Henricus Koymans, Marc René de Jonge, Koen Jeanne Alfons Van Aken, Alain Krief
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Patent number: 7005433Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: GrantFiled: December 29, 2003Date of Patent: February 28, 2006Assignee: Elan Pharmaceuticals, Inc.Inventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Darren B. Dressen, Francine S. Grant, Christopher Semko, Ying-Zi Xu
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Patent number: 6995262Abstract: The invention relates to a novel polymethine dyes containing at least one acylsulfonamido group of the formula (I) in which n, Y, A and R have the meaning given in the claims, and at least one compound of the formulae (a) to (n) given in the claims. The polymethine dyes according to the invention are suitable for use as dyes and/or labels, in particular for staining or labeling biomolecules.Type: GrantFiled: July 24, 2000Date of Patent: February 7, 2006Assignee: Bayer CropScience AGInventors: Geert Deroover, Michael Missfeldt, Lydia Simon
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Patent number: 6953802Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: GrantFiled: July 20, 2001Date of Patent: October 11, 2005Assignees: Elan Pharmaceuticals, Inc., WyethInventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Grant, Christopher Semko, Ying-Zi Xu
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Patent number: 6919342Abstract: The invention relates to triazole compounds of the general formula I wherein R1 is hydrogen or methyl, and R2 is C3-C4 alkyl or C1-C2 fluoroalkyl, as well as the physiologically tolerated acid addition salts of these compounds. The invention also relates to a pharmaceutical composition that comprises at least one triazole compound of the formula I and/or at least one physiologically tolerated acid addition salt thereof, and further to a method for treating disorders that respond beneficially to dopamine D3 receptor antagonists or dopamine D3 agonists, said method comprising administering an effective amount of at least one triazole compound or physiologically tolerated acid addition salt of the formula I to a subject in need thereof.Type: GrantFiled: June 4, 2004Date of Patent: July 19, 2005Assignee: Abbott GmbH & Co. KGInventors: Andreas Haupt, Roland Grandel, Wilfried Braje, Hervé Geneste, Karla Drescher, Dorothea Starck, Hans-Jürgen Teschendorf
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Patent number: 6919345Abstract: This invention relates to pyrazol pyridine derivatives of formula (I) wherein R1 is a radical of the formula ?O—SO2—R3 in which R3 is optionally substituted C1—6—alkyl, optionally substituted C3—8—cycloalkyl, or optionally substituted phenyl; R2 is H, optionally substituted C1—6—alkyl —CO—or optionally substituted C1—6—alkyl—SO2— ; as well as salts, stereoisomers, tautomers, and hydrates thereof. Pharmaceutical compositions containing these materials and methods of using them in medical treatment are also described and claimed.Type: GrantFiled: April 30, 2002Date of Patent: July 19, 2005Assignee: Bayer AktiengesellschaftInventors: Johannes-Peter Stasch, Achim Feurer, Stefan Weigand, Elke Stahl, Dietmar Flubacher, Cristina Alonso-Alija, Frank Wunder, Dieter Lang, Klaus Dembowsky, Alexander Straub, Elisabeth Perzborn
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Patent number: 6864254Abstract: An inhibitor for 20-hydroxyeicosatetraenoic acid production which comprises as the active ingredient a specific hydroxyformamidine derivative or a pharmacologically acceptable salt thereof. It is useful especially as a remedy for kidney diseases, cerebrovascular diseases, or circulatory diseases. The novel hydroxyformamidine derivative or pharmacologically acceptable salt thereof is also provided.Type: GrantFiled: November 1, 2000Date of Patent: March 8, 2005Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Kobayashi, Hideaki Amada
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Patent number: 6846828Abstract: Aminopyrimidine and aminopyridine (I) compounds, compositions and methods useful in the treatment of inflammatory, metabolic or malignant conditions, are provided herein.Type: GrantFiled: November 6, 2002Date of Patent: January 25, 2005Assignee: Roche Palo Alto LLCInventors: Ronald Charles Hawley, Sharada Shenvi Labadie, Eric Brian Sjogren, Francisco Xavier Talamas
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Patent number: 6844347Abstract: The invention relates to compounds of formula I, in which R1, R2, R3 and R4 have the meanings given in the claims. Said compounds are valuable active ingredients for the treatment and prophylaxis of diseases, for example of cardiovascular diseases such as hypertension, angina pectoris, heart failure, thrombosis or atherosclerosis. The compounds of the formula I are able to modulate the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the treatment and prophylaxis of disorders associated with impaired cGMP balance. The invention furthermore relates to methods for producing compounds of the formula I, their use in the treatment and prophylaxis of the above diseases and in the preparation of medicaments for such diseases, and pharmaceutical preparations containing the compounds of formula I.Type: GrantFiled: August 4, 1999Date of Patent: January 18, 2005Assignee: Aventis Pharma Deutschland GmbHInventors: Ursula Schnidler, Karl Schoenafinger, Hartmut Strobel
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Patent number: 6838464Abstract: 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: GrantFiled: February 26, 2001Date of Patent: January 4, 2005Assignee: AstraZeneca ABInventors: Elizabeth Janet Pease, Emma Jane Williams, Robert Hugh Bradbury, Stuart Eric Pearson
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Patent number: 6833364Abstract: The present invention relates to novel substituted pyrazole derivatives of the general formula (I) in which the substituents R1, R2, R3, A, X and Y are each as defined, and to processes for their preparation and to their use as medicaments, in particular as medicaments for the treatment of cardiovascular disorders.Type: GrantFiled: March 26, 2001Date of Patent: December 21, 2004Assignee: Bayer HealthCare AGInventors: Alexander Straub, Achim Feurer, Cristina Alonso-Alija, Elke Stahl, Johannes-Peter Stasch, Elisabeth Perzborn, Joachim Hütter, Klaus Dembowsky
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Patent number: 6821980Abstract: The invention relates to substituted 5-benzyl-2,4-diaminopyrimidines of general formula (A) wherein R1 is C2-C3 alkyl an R2 is heterocyclyl, phenyl or naphthyl, bonded by one of its C-atoms and R3 is C2-C6 alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, heterocyclylalkyl, alkylsulfonyl, cycloalkylsulfonyl, cycloalkylalkylsulfamoyl, heterocyclysylfonyl, heterocyclylalkylsulfonyl or dialkylsulfamoyl; wherein alkyl, cycloalkyl and alyenyl can carry up to 6 carbon atoms alone or in compositions and can carry up to 6 ring members heterocyclically, alone, or in compositions and the groups R2 and R3 can be substituted; and to acid addition salts of compounds. The invention also relates to a method for producing the above 5-benzyl-2,4-diaminopyrimidines, to the intermediate. products that are produced, to corresponding medicaments and to the use of 5-benzyl-2,4-diaminopyrimidines as medicinal preparations.Type: GrantFiled: July 18, 2002Date of Patent: November 23, 2004Assignee: Basilea Pharmaceutica AGInventors: Philippe Guerry, Peter Mohr, Marc Muller, Werner Mueller, Philippe Pflieger
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Patent number: 6800630Abstract: A compound represented by the formula (I) wherein, for example, R1, R2, R3, and R4 are each independently hydrogen atom, alkyl, and the like, R5 and R6 are each independently hydrogen atom, alkyl, and the like, RB and RC are each independently hydrogen atom, alkyl, and the like, X is —O—, —S—, and the like, Y is 5-membered heteroaryl-diyl and the like, Z is optionally substituted aryl and the like, their pharmaceutically acceptable salts, or their solvates.Type: GrantFiled: July 12, 2002Date of Patent: October 5, 2004Assignee: Shionogi & Co., Ltd.Inventors: Hidekazu Tanaka, Kazuo Ueda, Shinji Suzuki, Hideyuki Takenaka
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Publication number: 20040176596Abstract: Vitamin B6-phosphate phosphatase (VB6PP), a process for producing VB6PP and a process for producing vitamin B6 from vitamin B6-phosphate (VB6P) utilizing VB6PP and cell-free extract of a specific microorganism capable of producing VB6PP.Type: ApplicationFiled: December 17, 2003Publication date: September 9, 2004Inventors: Tatsuo Hoshino, Keiko Ichikawa, Masaaki Tazoe
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Patent number: 6787551Abstract: The present invention relates to a thiazolidinedione derivative, represented in formula (1) below, pharmaceutically acceptable salts thereof, and/or pharmaceutically acceptable solvates thereof. Further, the present invention provides a pharmaceutical composition comprising the compound represented in formula (1) below, wherein: X represents a carbon or nitrogen atom, Y represents a hydrogen atom, an alkyl group, an alkoxy group, a halogen, or an aryl group, Z represents an oxygen, nitrogen, or sulfur atom, and R1 and R2 each represent a hydrogen atom; or R1 and R2 together form a bond.Type: GrantFiled: July 3, 2003Date of Patent: September 7, 2004Assignee: Chong Kun Dang Pharmaceutical CorporationInventors: Chung-Il Hong, Soon-Kil Ahn, Bok-Young Kim, Joong-Bok Ahn, Do-Young Lee, Hong-Woo Lee, Jae-Soo Shin
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Patent number: 6787542Abstract: The present invention relates to novel heterocyclyl-containing diaryl sulfide compounds that are useful for treating inflammatory and immune diseases, to pharmaceutical compositions comprising these compounds, and to methods of inhibiting inflammation or suppressing immune response in a mammal.Type: GrantFiled: June 25, 2001Date of Patent: September 7, 2004Assignee: ICOS CorporationInventors: Gary T. Wang, Sheldon Wang, Robert Gentles
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Publication number: 20040067937Abstract: The invention relates to novel pyrazolopyridine derivatives of formula (I) wherein R1 represents H, Cl or NH2, and R2 and R3 form; together with the heteroatoms to which they are bonded, a five to six-membered heterocycle which can be saturated or partially unsaturated, can optionally contain at least one other heteroatom from the group N, O, S and can be optionally substituted. The invention also relates to salts, isomers and hydrates of said derivatives, in the form of stimulators of soluble guanylate cyclase and as agents for treating cardiovascular diseases, hypertonia, thrombo-embolic diseases and ischaemia, sexual dysfunction, inflammations, and diseases of the central nervous system.Type: ApplicationFiled: October 23, 2003Publication date: April 8, 2004Inventors: Johannes-Peter Stasch, Achim Feurer, Stefan Weigand, Elke Stahl, Dietmar Flubacher, Cristina Alonso-Alija, Frank Wunder, Dieter Lang, Klaus Dembowsky, Alexander Straub, Elisabeth Perzborn
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Publication number: 20040063945Abstract: The present invention relates to a 6-(1-fluoroethyl)-5-iodo-4-aminopyrimidine compound represented by the following formula (1): 1Type: ApplicationFiled: July 10, 2003Publication date: April 1, 2004Inventors: Katsutoshi Fujii, Shoji Shikita
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Publication number: 20040038976Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.Type: ApplicationFiled: May 21, 2003Publication date: February 26, 2004Applicant: Millennium Pharmaceuticals, Inc.Inventors: Paul Fleming, Geraldine C.B. Harriman, Zhan Shi, Shaowu Chen
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Patent number: 6696452Abstract: This invention describes novel pyrazole compounds of formula II: wherein Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, and R2, R2′, Rx, and Ry are as described in the specification. Ring C has an ortho substituent and is optionally substituted in the non-ortho positions. R2 and R2′ are optionally taken together with their intervening atoms to form a fused ring system, such as an indazole ring; and Rx and Ry are optionally taken together with their intervening atoms to form a fused ring system, such as a quinazoline ring. The compounds are useful as protein kinase inhibitors, especially as inhibitors of GSK-3, for treating diseases such as diabetes and Alzheimer's disease.Type: GrantFiled: September 14, 2001Date of Patent: February 24, 2004Assignee: Vertex Pharmaceuticals IncorporatedInventors: Robert Davies, David Bebbington, Ronald Knegtel, Marion Wannamaker, Pan Li, Cornelia Forster, Albert Pierce
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Patent number: 6686469Abstract: The invention relates to compounds of the general formula wherein R1 is unsubstituted or mono- to penta-substituted aryl, whereby the substituents are selected from the group consisting for instance of OH, Halogen, CN, C1-C6-alkyl, optionally substituted C3-C8-cycloalkyl and optionally substituted C3-C8-cycloalkenyl; A is for instance a single bond, C1-C12-alkylene or O; X1 and X2, independently of one another, are R10; X3 is H or R10; R10 is for instance halogen, CN, NO2, C1-C6-alkyl, C3-C8-cycloalkyl or C1-C6-haloalkyl; R21 and R22, independently of one another are for instance H, halogen, CN, NO2, OH, SH, C1-C6-alkyl, C3-C8-cycloalkyl, C1-C6-alkyl-C3-C8-cycloalkyl or C3-C8-cycloalkyl-C1-C6-alkyl; R23 and R24, independently of one another, are for instance H, C1-C6-alkyl, C3-C8-cycloalkyl, C3-C8-cycloalkyl-C1-C6-alkyl, C1-C6-haloalkyl or C3-C8-halocycloalkyl; m is 1, 2, 3 or 4; and n is 0, 1 or 2; as well as the physiologically acceptable addition compounds, a method of producingType: GrantFiled: November 5, 2001Date of Patent: February 3, 2004Assignee: Novartis Animal Health US, Inc.Inventors: Martin Eberle, André Jeanguenat, Werner Zambach, Arthur Steiger, Saleem Farooq
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Publication number: 20040006094Abstract: This invention provides novel neuroprotective 4-pyrimidineamine derivatives and neuroprotective pharmaceutical compositions comprising 4-pyrimidinamines. This invention also provides methods of using these compositions to prevent ischemic cell death, particularly neuronal cell death, and reduce the likelihood of neuronal cell death in a subject due to a traumatic event. Finally, this invention provides an apparatus for administering to a subject the instant pharmaceutical compositions.Type: ApplicationFiled: March 25, 2003Publication date: January 8, 2004Inventors: Elfrida R. Grant, Frank K. Brown, Robert Allan Zivin, Michael McMillian, Zhong Zhong, Malcolm Scott, Allen B. Reitz, Tina Morgan Ross
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Patent number: 6660738Abstract: The present invention relates to pyrrolidine derivatives useful as inhibitors of metalloproteases, e.g. zinc proteases, and which are effective in treating disease states associated with vasoconstriction.Type: GrantFiled: July 17, 2001Date of Patent: December 9, 2003Assignee: Hoffmann-La Roche Inc.Inventors: Johannes Aebi, Daniel Bur, Alexander Chucholowski, Henrietta Dehmlow
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Publication number: 20030216382Abstract: The present invention provides compounds of formula (I) 1Type: ApplicationFiled: February 10, 2003Publication date: November 20, 2003Inventors: Markus Boehringer, Bernd Michael Loeffler, Jens-Uwe Peters, Matthias Steger, Peter Weiss
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Patent number: 6645968Abstract: Compounds of formula I: are useful in treating diseases prevented by or ameliorated with potassium channel openers. Also disclosed are potassium channel opening compositions and a method of opening potassium channels in a mammal.Type: GrantFiled: February 5, 2001Date of Patent: November 11, 2003Assignee: Abbott LaboratoriesInventors: Robert J. Altenbach, Hao Bai, Jorge D. Brioni, William A. Carroll, Murali Gopalakrishnan, Robert J. Gregg, Mark W. Holladay, Peggy P. Huang, John F. Kincaid, Michael E. Kort, Philip R. Kym, John K. Lynch, Arturo Perez-Medrano, Henry Q. Zhang
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Patent number: 6632820Abstract: A pyrimidine derivative of formula (I) wherein, for example, R1 is-(1-6C)alkyl or (3-5C)alkenyl [optionally substituted by a phenyl substituent]; Q1 and Q2 are independently selected from phenyl, naphthyl, indanyl and 1,2,3,4-tetrahydronaphthyl; and one or both of Q1 and Q2 bears one substituent of formula (Ia) [provided that when present in Q1 the substituent of formula (Ia) is not adjacent to the —NH-link]; wherein, for example, X is CH2, O, S or NH; Y is H or as defined for Z; Z is OH, SH, NH2, (1-4C)alkoxy, (1-4C)alkylthio, —NH(1-4C)alkyl, —N[(1-4C)alkyl]2 or —NH-(3-8C)cycloalkyl; n is 1, 2 or 3; m is 1, 2 or 3; and Q1 and Q2 may each optionally bear other substituents selected from halogeno, (1-6C)alkyl, cyano and (2-4C)alkenyl, 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 describeType: GrantFiled: February 26, 2001Date of Patent: October 14, 2003Assignee: AstraZeneca ABInventors: Gloria Anne Breault, Philip John Jewsbury, Janet Elizabeth Pease
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Publication number: 20030153557Abstract: The present invention relates to thienyl substituted acylguanidine derivatives, such as compounds of formula (I) in which R1, R2, R4, R6, A, B and D have the meanings indicated in the claims, their physiologically tolerable salts and their prodrugs. The compounds of the present invention are valuable pharmaceutical active compounds. They are vitronectin receptor antagonists and inhibitors of bone resorption by osteoclasts. They are suitable, for example, for the therapy and prophylaxis of diseases which are caused at least partially by an undesired extent of bone resorption, for example of osteoporosis. The invention furthermore relates to processes for the preparation of thienyl substituted acylguanidines, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: ApplicationFiled: November 14, 2002Publication date: August 14, 2003Applicant: Aventis Pharma Deutschland GmbH and Genentech, Inc.Inventors: Karl-Heinz Scheunemann, Jochen Knolle, Amuschirwan Peyman, David William Will, Denis Carniato, Jean-Francois Gourvest, Thomas Gadek, Robert McDowell, Sarah Catherine Bodary, Robert Andrew Cuthbertson
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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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Substituted pyrimidines, processes for their preparation, and their use as pesticides and fungicides
Patent number: 6596727Abstract: Substituted 4-amino- and 4-alkoxy-cycloalkylpyrimidines, processes for their preparation, and their use as pesticides and fungicides The invention relates to compounds of the formula in which R1, R2, R3 and Q are as defined in the description, X is NH or oxygen and E is a bond or a 1- to 4-membered carbon chain, to a process for their preparation, to agents containing them, and to their use in the control of pests and as fungicides.Type: GrantFiled: March 15, 1996Date of Patent: July 22, 2003Assignee: Hoechst AktiengesellschaftInventors: Wolfgang Schaper, Rainer Preuss, Gerhard Salbeck, Peter Braun, Werner Knauf, Burkhard Sachse, Anna Waltersdorfer, Manfred Kern, Peter Lümmen, Werner Bonin -
Patent number: 6548512Abstract: The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D may be C(═NH)NH2, which are useful as inhibitors of factor Xa.Type: GrantFiled: January 27, 2000Date of Patent: April 15, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Donald Joseph Phillip Pinto, James Russell Pruitt, Joseph Cacciola, John Matthew Fevig, Qi Han, Michael James Orwat, Mimi Lifen Quan, Karen Anita Rossi
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Publication number: 20030045718Abstract: The invention relates to crystalline salts of the compound (E)-7-[4-(4-fluorophenyl)-6-iso-propyl-2-[methyl(methyl-sulfonyl)amino]pyrimidin-5-yl]-(3R,5S)-3,5-dihydroxyhept-6-enoic acid of formula (I),as well as processes for their manufacture, pharmaceutical compositions containing them, and their uses.Type: ApplicationFiled: August 15, 2002Publication date: March 6, 2003Inventors: Nigel Philip Taylor, Tetsuo Okada
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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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Publication number: 20030022794Abstract: Novel agrichemical quaternary salts, compositions and a method to prepare them are disclosed.Type: ApplicationFiled: September 5, 2002Publication date: January 30, 2003Inventors: Robert D. Wysong, Chia-Chung Chen, Chuen-Ing Tseng, Arturo Aclaro Tirol
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Patent number: 6503913Abstract: The invention relates to new 2-heterocyclically substituted dihydropyrimidines, medicaments which contain these 2-heterocyclically substituted dihydropyrimidines, and a process for preparation of medicaments. The invention furthermore relates to the use of the 2-heterocyclically substituted dihydropyrimidines for the production of a medicament, in particular for the treatment of acute or chronic viral diseases, in particular for the production of a medicament for the treatment of acute or chronic hepatitis B infections.Type: GrantFiled: October 18, 2000Date of Patent: January 7, 2003Assignee: Bayer AktiengesellschaftInventors: Siegfried Goldmann, Jürgen Stoltefuss, Arnold Paessens, Erwin Graef, Stefan Lottmann
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Patent number: 6479498Abstract: The compounds of this invention comprise 2-10 ligands covalently connected, each of the ligands being capable of binding to a ligand binding site in a Na+ channel, thereby modulating the biological activities thereof.Type: GrantFiled: November 9, 2001Date of Patent: November 12, 2002Assignee: Theravance, Inc.Inventors: Daniel Marquess, Seok-Ki Choi, David T. Beattie, John H. Griffin, Scott Armstrong, Timothy J. Church, Thomas E. Jenkins, David C. Green
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Publication number: 20020137755Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.Type: ApplicationFiled: November 21, 2001Publication date: September 26, 2002Inventors: Mark T. Bilodeau, George D. Hartman, Jacob M. Hoffman, John T. Sisko, Peter J. Manley, Anthony M. Smith, Thomas J. Tucker, William C. Lumma, Leonard Rodman
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Patent number: 6440976Abstract: Compounds described by the chemical structural formula or a pharmaceutically acceptable salt thereof, are useful in the treatment of pain, migraine, depression, anxiety, schizophrenia, Parkinson's disease, stroke, and in the treatment of neuropathies including postherpetic neuralgia, central pain from spinal cord injury, and phantom limb pain.Type: GrantFiled: June 25, 2001Date of Patent: August 27, 2002Assignee: Merck & Co., Inc.Inventors: David A. Claremon, John A. McCauley, Nigel J. Liverton, Cory R. Theberge
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Publication number: 20020082420Abstract: A compound of formula (I) 1Type: ApplicationFiled: August 21, 2001Publication date: June 27, 2002Inventors: Frank Himmelsbach, Elke Langkopf, Stefan Blech, Birgit Jung, Thomas Metz
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Publication number: 20010023292Abstract: This invention is directed to poly-hydroxylated monocyclic N-heterocyclic derivatives selected from the following formulae: 1Type: ApplicationFiled: May 4, 2001Publication date: September 20, 2001Applicant: Berlex Laboratories, Inc.Inventor: Gary B. Phillips
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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: 6281221Abstract: The invention relates to novel substituted 1,3-dioxan-5-ylamino-heterocyclic compounds of the formula in which A is CH or N; X is NH, O or S(O)q, where q=0-2; Y is O or S(O)m, where m=0-2, and R1, R2, R3, R4, R4′ and R5 have the meanings given in the description, processes for their preparation and their use as pest control compositions and fungicides.Type: GrantFiled: September 25, 1998Date of Patent: August 28, 2001Assignee: Hoechst Scering AgrEvo GmbHInventors: Wolfgang Schaper, Werner Knauf, Ulrich Sanft, Manfred Kern, Heinz Ehrhardt, Adolf Heinz Linkies, Dieter Bernd Reuschling, Werner Bonin
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Patent number: 6245763Abstract: Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII: wherein X is O or NR9 and Het, R1, R7, R8, R12-R15, Ra, Rb, Rc, Z, and n are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing such compounds. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal, comprising a compound of the invention in a pharmaceutically acceptable carrier.Type: GrantFiled: January 14, 2000Date of Patent: June 12, 2001Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Tianbao Lu, Bruce E. Tomczuk, Thomas P. Markotan, Colleen Siedem
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Publication number: 20010000028Abstract: Nonalcoholic steatohepatitis (NASH) is a disease of the liver characterized by inflammation and damage to the liver cells. Typically, steatohepatitis involves inflammation of the liver related to fat accumulation, and mimics alcoholic hepatitis but is observed in patients who seldom or never consume alcohol. Nonalcoholic steatohepatitis can lead to serious liver damage, and ultimately cirrhosis. The present invention provides methods and compositions useful for the treatment or alleviation of nonalcoholic steatohepatitis and the pharmaceutical formulations for their administration to a human. Specifically, compositions comprised of lecithin, antioxidants and vitamin B complex are administered parenterally, most preferably by oral administration. Specific therapeutic formulations include admixtures of these compounds and specific dosage formulations include daily oral administrations of these compounds in tablet or powder forms.Type: ApplicationFiled: November 29, 2000Publication date: March 15, 2001Inventors: Houn Simon Hsia, David Fan
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Patent number: 6197795Abstract: The present invention relates to the discovery of novel, low molecular weight, non-peptide inhibitors of matrix metalloproteinases (e.g.Type: GrantFiled: June 11, 1999Date of Patent: March 6, 2001Assignee: American Cyanamid CompanyInventors: Jeremy Ian Levin, Frances Christy Nelson
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Patent number: 6175008Abstract: Disclosed are processes for preparing compounds of the formula (I) and pharmaceutically acceptable salts or esters thereof: wherein R2 is a purine or pyrimidine base or an analogue or derivative thereof; and Z is S, S═O or SO2. The invention also relates to intermediates of use in the preparation of these compounds.Type: GrantFiled: June 6, 1995Date of Patent: January 16, 2001Assignee: BioChem Pharma Inc.Inventors: Bernard Belleau, Tarek Mansour, Allan Tse, Colleen A. Evans, Haolun Jin, Boulos Zacharie, Nghe Nguyen-Ba
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Patent number: 6174901Abstract: Selected novel substituted pyridine and pyridazine compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as cancer, pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, cancer, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: December 18, 1998Date of Patent: January 16, 2001Assignee: Amgen Inc.Inventors: Nathan B. Mantlo, Chan-Kou Hwang, Ulrike D. Spohr
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Patent number: 6172227Abstract: Novel 4,5-diamino pyrimidine derivatives are described by the following general formula I: in which X is a direct bond, C1-4 alkylene, C1-4 alkyleneoxy, C1-4 alkoxyphenyl or phenyl C1-4 alkylene; Y is a direct bond or C1-2 alkyl, R1 is (i) 5-15 membered cyclic or fused heterocompound which includes one or two atoms selected from a group consisting of nitrogen, oxygen and sulfur and which is substituted with one or two substituents selected from a group consisting of hydrogen, halogen, nitro, hydroxy, C1-6 alkyl, C3-6 alkenyl and halogen C1-4 alkoxy, (ii) C4-10 carbocyclic compound or (iii) hydroxy C1-4 alkoxy, R2 is 5-15 membered cyclic or fused heterocompound which includes one or two nitrogen atoms and, optionally, one oxygen or sulfur atom, and which is substituted with one or two substituents selected from a group consisting of hydrogen, hydroxy, halogen, nitro, hydroxy C1-5 alkyl, C1-6 alkyl, C3-6 alkenyl and halogen C1-4 alkoxy; R3 is hydrogen, in which R4 and R5 areType: GrantFiled: September 16, 1997Date of Patent: January 9, 2001Assignee: Cheil Jedang CorporationInventors: Myung Xik Xiang, Byoung Chool Suh, Chung Keun Rhee, Kwang Hyuk Lee, Youn Ha Lee, Young Gi Kim