At 4- Or 6-position Patents (Class 544/326)
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Patent number: 6528513Abstract: Compounds and compositions are provided which are useful for the treatment of viral infections, particularly human Cytomegalovirus infection. The compounds include novel pyrimidine-based derivatives.Type: GrantFiled: December 15, 2000Date of Patent: March 4, 2003Assignee: Tularik INCInventors: Timothy D. Cushing, Heather L. Mellon, Juan C. Jaen, John A. Flygare, Shi-Chang Miao, Xiaoqi Chen, Jay P. Powers
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Patent number: 6521627Abstract: The present invention is to provide a novel 5-iodo-4-phenethylaminopyrimidine derivative represented by the following formula (1): wherein R1 represents a halogen atom, a C2-4 acyloxy group or a hydroxyl group; R2 represents a hydrogen atom, a halogen atom, a C1-4 alkyl group, a C1-4 haloalkyl group, a C1-4 alkoxy group or a C1-4 haloalkoxy group; n is an integer of 1 to 3; and * represents an asymmetric carbon atom, useful as pesticides, a synthetic intermediate thereof and processes for producing these compounds, and pesticides containing the 5-iodo-4-phenethylaminopyrimidine derivative(s).Type: GrantFiled: October 16, 2000Date of Patent: February 18, 2003Assignee: UBE Industries, Ltd.Inventors: Katsutoshi Fujii, Yoshinori Yamanaka, Kiyoshi Tsutsumiuchi, Youichi Yoshida
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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: 6518424Abstract: Substituted pyrimidines that have the general structure: in which the symbol R1 represents a C1-C6 alkyl, C1-C6 alkoxy or halogen atom; R2 represents a phenyl group, substituted phenyl group, benzyl moiety, substituted benzyl moiety, C3-C7 cycloalkyl, or substituted C3-C7 cycloalkyl; R3 represents a hydrogen or C1-C6 alkyl group, R4 represents —H, —OH, —N3 or —NHCOCH3; and R5 represents H are provided. These compounds have activity as inhibitors of phospholipase A2, and are useful in treating disorders mediated by phospholipase A2.Type: GrantFiled: November 10, 1999Date of Patent: February 11, 2003Assignee: Elan Pharmaceuticals, Inc.Inventors: Varghese John, Russell E. Rydel, Michael S. Dappen, Eugene D. Thorsett
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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: 20020156087Abstract: New pyrimidine or pyridine based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.Type: ApplicationFiled: September 6, 2001Publication date: October 24, 2002Inventors: John M. Nuss, Stephen D. Harrison, David B. Ring, Rustum S. Boyce, Kirk Johnson, Keith B. Pfister, Savithri Ramurthy, Lynn Seely, Allan S. Wagman, Manjo Desai, Barry H. Levine
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Publication number: 20020151713Abstract: This invention relates to compounds of the formula 1Type: ApplicationFiled: May 30, 2002Publication date: October 17, 2002Applicant: Pfizer Inc.Inventor: Yuhpyng L. Chen
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Patent number: 6458803Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.Type: GrantFiled: November 23, 2001Date of Patent: October 1, 2002Assignee: G.D. Searle & Co.Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6451792Abstract: A medical composition containing, as an active constituent, a nitroetheneamine derivative represented by the formula (I): wherein the substituents are as defined in the disclosure, its stereoisomers, its tautomers or a salt thereof.Type: GrantFiled: March 20, 2001Date of Patent: September 17, 2002Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Fuminori Kato, Keizo Miyata, Hirohiko Kimura, Kazuhiro Yamamoto, Hiroyuki Ikegami, Hiromi Takeo
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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: 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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Patent number: 6423842Abstract: The present invention provides novel compounds and pharmaceutical compositions thereof useful in the treatment of pain. The compounds of the present invention are azaadamantanes, azanoradamantanes and azahomoadamantanes.Type: GrantFiled: October 5, 2001Date of Patent: July 23, 2002Assignee: UCB, S.A.Inventors: Gurmit Grewal, Anna Toy-Palmer, Xiong Cai, George Mark Latham
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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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Publication number: 20020086858Abstract: Pyrimidine derivatives have been found to be useful as neuropeptide Y receptor ligands and particularly as antagonists. These pyrimidine derivatives may be used in the form of pharmaceutical preparations for the treatment or prevention of arthritis, diabetes, eating disorders, and obesity.Type: ApplicationFiled: November 8, 2001Publication date: July 4, 2002Inventors: Volker Breu, Frank Dautzenberg, Patrizio Mattei, Werner Neidhart, Philippe Pflieger
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Patent number: 6414149Abstract: This invention is directed to sorbitol dehydrogenase inhibitory compounds of the formula I, wherein R1, R2 and R3 are as defined in the specification. This invention is also directed to pharmaceutical compositions containing those compounds and methods of treating or preventing diabetic complications, particularly diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, diabetic macroangiopathy and diabetic cardiomyopathy by administering such compounds to a mammal suffering from diabetes and therefore at risk for developing such complications. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula I of this invention with an aldose reductase inhibitor and to methods of treating or preventing diabetic complications therewith.Type: GrantFiled: March 29, 2000Date of Patent: July 2, 2002Assignee: Pfizer Inc.Inventors: Margaret Y. Chu-Moyer, Banavara L. Mylari, William J. Zembrowski
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Publication number: 20020055632Abstract: 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: ApplicationFiled: July 17, 2001Publication date: May 9, 2002Inventors: Johannes Aebi, Daniel Bur, Alexander Chucholowski, Henrietta Dehmlow
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Publication number: 20020049322Abstract: The invention provides compounds of formula (I), 1Type: ApplicationFiled: March 19, 2001Publication date: April 25, 2002Inventors: Alan John Collis, David Nathan Abraham Fox, Julie Newman
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Publication number: 20020040141Abstract: 2-Methyl-4-amino-5-aminomethylpyrimidine of the formula 1 1Type: ApplicationFiled: March 20, 2001Publication date: April 4, 2002Inventors: Hansgeorg Ernst, Matthias Frauenkron, Johann-Peter Melder, Frank Funke, Andreas Keller
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Patent number: 6365740Abstract: 2-Methyl-4-amino-5-aminomethylpyrimidine of the formula 1 is prepared by reacting 2-methyl-4-amino-5-alkoxymethylpyrimidine of the formula 2 where R=C1-C6-alkyl, with ammonia in the presence of a catalyst.Type: GrantFiled: March 20, 2001Date of Patent: April 2, 2002Assignee: BASF AktiengesellschaftInventors: Hansgeorg Ernst, Matthias Frauenkron, Johann-Peter Melder, Frank Funke, Andreas Keller
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Publication number: 20020016328Abstract: Corticotropin-releasing factor (CRF) antagonists having the formulae 1Type: ApplicationFiled: January 17, 2001Publication date: February 7, 2002Inventor: Yuhpyng L. Chen
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Publication number: 20020007063Abstract: Calculated performance improvements are expected from a particularly new class of compounds, geminal-bis(difluoramino)-substituted heterocyclic nitramines, when formulated into explosives and propellants. This invention involves novel and nonintuitive methods for the preparation of certain derivatives of 2,2-bis(difluoramino)-N-nitro-1,3-propanediamine which are suitable precursors leading to 5,5-bis(difluoramino)hexahydro-1,3-dinitropyrimidine (RNFX). The invention also involves novel and nonintuitive methods for the preparation of RNFX, a specific member of a general class of compounds with the substructure 2,2-bis(difluoramino)-N-nitro-1,3-propanediamine. RNFX is produced by the use of key intermediates, including tetrahydropyrimidin-5(4H)-ones, which allow formation of the target structural subcomponent, 2,2-bis(difluoramino)-N-nitro-1,3-propanediamine, and a more specific substructure of 2,2-bis(difluoramino)-N,N′-dinitro-1,3-propanediamine.Type: ApplicationFiled: July 23, 2001Publication date: January 17, 2002Inventors: Robert Dale Chapman, Ba Van Nguyen
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Patent number: 6329373Abstract: A compound of formula (I) wherein X is a —CONHOH group and the R groups are defined in the claims. The compounds are inhibitors of matrix metalloproteinases involved in tissue degradation and inhibitors of the release of tumour necrosis factor from cells.Type: GrantFiled: January 7, 2000Date of Patent: December 11, 2001Assignee: British Biotech Pharmaceuticals, Ltd.Inventors: Fionna Mitchell Martin, Christopher Norman Lewis, Mark Whittaker
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Publication number: 20010044537Abstract: This invention is directed to poly-hydroxylated monocyclic N-heterocyclic derivatives selected from the following formula: 1Type: ApplicationFiled: May 4, 2001Publication date: November 22, 2001Applicant: Berlex Laboratories, Inc.Inventor: Gary B. Phillips
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Publication number: 20010044536Abstract: This invention is directed to poly-hydroxylated monocyclic N-heterocyclic derivatives selected from the following formula: 1Type: ApplicationFiled: May 4, 2001Publication date: November 22, 2001Inventor: Gary B. Phillips
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Publication number: 20010034445Abstract: Compounds of formula (I) are disclosed which are vitronectin receptor antagonists useful in the treatment of osteoporosis.Type: ApplicationFiled: January 24, 2001Publication date: October 25, 2001Applicant: SmithKline Beecham CorporationInventors: Fadia E. Ali, William E. Bondinell, Richard M. Keenan, Thomas Wen-Fu Ku, William H. Miller, James Samanen
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Publication number: 20010027202Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.Type: ApplicationFiled: February 2, 2001Publication date: October 4, 2001Inventors: Bernd Riedl, Jaques Dumas, Uday Khire, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood, Mary-Katherine Monahan, Reina Natero, Joel Renick, Robert N. Sibley
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Publication number: 20010023291Abstract: This invention is directed to polyhydroxylated 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: 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: 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: 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: 6251916Abstract: The present invention provides novel compounds and pharmaceutical compositions thereof useful in the treatment of pain. The compounds of the present invention are azaadamantanes, azanoradamantanes and azahomoadamantanes.Type: GrantFiled: May 9, 2000Date of Patent: June 26, 2001Assignee: UCB, S. A.Inventors: Gurmit Grewal, Anna Toy-Palmer, Xiong Cai, George Mark Latham
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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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Patent number: 6197729Abstract: Compounds of formula I where R1 is hydrogen, chlorine, fluorine or methyl, R2 and R3, which may be the same or different from each other, are hydrogen, halogen, cyano, (C1-C4)-alkyl, vinyl, ethynyl, (C1-C4)-alkoxy, (C1-C4)-alkoxy-(C1-C4)-alkyl, fluorovinyl or fluoroethyl, or R2 and R3 together with the linking carbon atoms form a benzo ring, and R4 is (C2-C4)-alkyl, (C2-C4)-alkenyl or (C3-C4)-alkinyl, each of which is substituted by at least two fluorine atoms and optionally substituted by C1-4-alkoxy, cyanomethoxy, (C3-C4)-alkenyloxy or (C3-C4)-alkinyloxy, are useful as pesticides, especially against insects, acarids and fungi. The invention includes a novel process for fluorinating certain pyrimidines.Type: GrantFiled: July 29, 1999Date of Patent: March 6, 2001Assignee: Hoechst Schering AgrevoInventors: Martin Märkl, Wolfgang Schaper, Oswald Ort, Harald Jakobi, Ralf Braun, Gerhard Krautstrunk, Ulrich Sanft, Werner Bonin, Herbert Stark, Sergej Pasenok, Ivan Cabrera
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Patent number: 6191149Abstract: A pharmaceutical composition comprising a compound of the following general formula [I] or its salt. wherein R1 represents aryl or a heteroaromatic group. R2 represents hydrogen, alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, hydroxyalkyl, haloalkyl, alkoxy, alkylthio, amino, monoalkylamino, dialkylamino, or phenyl. R3 and R4 independently represent hydrogen or alkyl or R3 and R4 taken together with the adjacent N atom represent a 5- through 7-membered cyclic amino group. A represents a single bond C2-10 alkylene. W represents O, S, or (CH2)n (where CH may be substituted by alkyl; n is an integer of 1 or 2). X, Y, and Z may be the same or different and each represents CH (which may be substituted by alkyl), or N. Provided, however, that the case in which X, Y, and Z concurrently represent CH is excluded. The compound of the invention has excellent neuronal death inhibitory activity and is useful as a therapeutic drug for cerebrovascular diseases.Type: GrantFiled: June 16, 1999Date of Patent: February 20, 2001Assignee: Nippon Shinyaku, Co., Ltd.Inventors: Shoichi Chokai, Yojiro Ukai, Tomiyoshi Aoki, Kyoichi Ideguchi
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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
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Patent number: 6150370Abstract: Disclosed are compounds which are inhibitors of metalloproteases having the following structure: ##STR1## where Ar, W, X, Y, Z, R.sub.1 and R.sub.2 have the meanings described in the specification and optical isomers, diastereomers, and enantiomers thereof or a pharmaceutically-acceptable salt, or biohydrolyzable amides, esters, or imides thereof. Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by unwanted metalloprotease activity using these compounds or pharmaceutical compositions.Type: GrantFiled: August 26, 1997Date of Patent: November 21, 2000Assignee: The Procter & Gamble CompanyInventors: Stanislaw Pikul, Kelly Lynn McDow-Dunham, Neil Gregory Almstead, Biswanath De, Michael George Natchus, Yetunde Olabisi Taiwo
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Patent number: 6107299Abstract: Compounds of formula I, N-oxides or salts, thereof ##STR1## in which q is 0, 1 or 2A is CH and D is N.sup.+ R.times.1/n Q.sup.n- or A is N and D is N.sup.+ R.times.1/n Q.sup.n- or A is CH or N and D is Nor A is N.sup.+ R.times.1/n Q.sup.n- and D is N, R is CR.sup.6 R.sup.7 D.sup.a R.sup.8,Q.sup.n- is an inorganic or organic anion, n being 1, 2, 3 or 4;X is NH, O or S(O).sub.q, (q is 0, 1 or 2); and the R groups have various meanings as defined in the claims are useful pesticidal, especially insecticidal activity.Type: GrantFiled: May 18, 1999Date of Patent: August 22, 2000Assignee: Hoechst Schering AgrEvo GmbHInventors: Harald Jakobi, Matthias Eckhardt, Wolfgang Schaper, Ralf Braun, Gerhard Krautstrunk, Oswald Ort, Ulrich Sanft, Maria-Theresia Thonessen, Werner Bonin
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Patent number: 6096753Abstract: Selected novel substituted pyrimidinone and pyridone compounds are effective for prophylaxis and treatment of diseases, such as TNF-.alpha., IL-1.beta., IL-6 and/or IL-8 mediated diseases, and other maladies, such as 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, 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 4, 1997Date of Patent: August 1, 2000Assignee: Amgen Inc.Inventors: Ulrike D. Spohr, Michael J. Malone, Nathan B. Mantlo
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Patent number: 6096768Abstract: This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.Type: GrantFiled: April 29, 1999Date of Patent: August 1, 2000Assignee: Rhone-Poulenc Rorer LimitedInventors: Michael John Ashton, David Charles Cook, Garry Fenton, Susan Jacqueline Hills, Ian Michael McFarlane, Andrew David Morley, Malcolm Norman Palfreyman, Andrew James Ratcliffe, Brian William Sharp, Sukanthini Thurairatnam, Bernard Yvon Jack Vacher, Nigel Vicker
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Patent number: 6093718Abstract: This invention concerns heterocyclic derivatives which are useful in inhibiting oxido-squalene cyclase, processes for their preparation and pharmaceutical compositions containing them. The present invention is also concerned with heterocyclic derivatives capable of inhibiting cholesterol biosynthesis and hence in lowering cholesterol levels in blood plasma. The present invention also relates to methods of using such heterocyclic derivatives in diseases and medical conditions such as hypercholesterolemia and atherosclerosis.Type: GrantFiled: February 12, 1999Date of Patent: July 25, 2000Assignee: Zeneca LimitedInventors: David Waterson, Elaine Sophie Elizabeth Stokes, George Robert Brown, Nicholas John Newcombe
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Patent number: 6080750Abstract: A pyrimidine compound of the formula [I] ##STR1## wherein R1 is H, C.sub.1 -C.sub.4 lower alkyl, halogen atom, --OH, C.sub.1 -C.sub.4 lower alkoxy, C.sub.1 -C.sub.6 hydroxy(lower)alkoxy or --NH.sub.2 ; R2 is H, --NH.sub.2 or --NHCOCH.sub.3 ; R3 is --NR5(CH.sub.2)i--CH.sub.2 OH; R4 is H, halogen atom, --NH.sub.2, --CN, --CHO, --CH.sub.2 OH, --COOH, --CH.sub.2 NH.sub.2, --CONH.sub.2 or --CH.dbd.N--A wherein A is --OH, C.sub.1 -C.sub.4 lower alkyl or C.sub.1 -C.sub.4 lower alkoxy; R5 is H or C.sub.1 -C.sub.4 lower alkyl; and i is an integer of 1 to 4, and an anti-rotavirus agent comprising, as an active ingredient, a compound of the formula [I] wherein R3 is a group selected from the following: ##STR2## The novel pyrimidine compound of the present invention and related derivatives thereof have superior anti-rotavirus action and are useful for the prophylaxis and treatment of rotaviral diseases.Type: GrantFiled: May 6, 1997Date of Patent: June 27, 2000Assignee: Nippon Shoji Kaisha Ltd.Inventors: Masakatsu Hisaki, Yoichiro Ohta, Kenji Kawanishi, Yasuko Ichigobara, Fuzuki Iwakura, Masanobu Azuma, Tatsuo Suzutani, Manabu Node, Kiyoharu Nishide
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Patent number: 6060468Abstract: The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.1a, R.sup.2, R.sup.2a, p, r and s are as defined in the detailed part of the present description or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for treatment of indications caused by or related to secretion and circulation of insulin antagonising peptides.Type: GrantFiled: October 3, 1997Date of Patent: May 9, 2000Assignee: Novo Nordisk A/SInventors: Tine Krogh J.o slashed.rgensen, Erik Fischer, Rolf Hohlweg, Knud Erik Andersen, Uffe Bang Olsen, Zdenek Polivka, Vladimir Valenta, Karel Sindelar
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Patent number: 6043248Abstract: The subject invention relates to pyrimidine-thioalkyl and alkylether compounds of Formula (I) and pyrimidine-thioalkyl and alkylethers of Formula (IA), namely the compounds of Formula (I) where R.sub.4 is selected from the group consisitng of --H or --NR.sub.15 R.sub.16 where R.sub.15 is --H and R.sub.16 is --H, C.sub.1 -C.sub.6 alkyl, NH.sub.2 or R.sub.15 and R.sub.16 taken together with the --N form 1-pyrrolidino, 1-morpholino or 1-piperidino; and R.sub.6 is selected from the group consisting of --H, or halo (preferably --Cl); with the overall proviso that R.sub.4 and R.sub.6 are not both --H. The compounds of Formula (IA) are useful in the treatment of individuals who are HIV positive being inhibitors of viral reverse transcriptase.Type: GrantFiled: October 17, 1997Date of Patent: March 28, 2000Assignee: Pharmacia & Upjohn CompanyInventors: Richard A. Nugent, Stephen T. Schlachter, Michael J. Murphy, Joel Morris, Richard C. Thomas, Donn G. Wishka, Gary J. Cleek, David R. Graber
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Patent number: 6030972Abstract: Compounds of the formula ##STR1## where A, B, D, R.sup.1 and R.sup.2 have the meanings stated in the description, are described. The compounds are suitable for controlling diseases.The novel compounds are prepared via compounds of the formulaH.sub.2 N--CH.sub.Type: GrantFiled: July 30, 1997Date of Patent: February 29, 2000Assignee: BASF AktiengesellschaftInventors: Hans-Joachim Bohm, Hans Wolfgang Hoffken, Wilfried Hornberger, Stefan Koser, Helmut Mack, Thomas Pfeiffer, Werner Seitz, Thomas Zierke
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Patent number: 6011155Abstract: N-(N'-substituted glycyl)-2-cyanopyrrolidines of formula I ##STR1## Compounds of formula I inhibit DPP-IV (dipeptidyl-peptidase-IV) activity. They are therefore indicated for use as pharmaceuticals in inhibiting DPP-IV and in the treatment of conditions mediated by DPP-IV, such as non-insulin-dependent diabetes mellitus, arthritis, obesity, osteoporosis and further conditions of impaired glucose tolerance.Type: GrantFiled: October 31, 1997Date of Patent: January 4, 2000Assignee: Novartis AGInventor: Edwin Bernard Villhauer
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Patent number: 5962479Abstract: Corticotropin-releasing factor (CRF) antagonists having formulae (I), (II) or (III) wherein the dashed lines, A, B, Y, Z, G, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.16 and R.sub.17 are as defined in the description, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment of CNS and stress-related disorders.Type: GrantFiled: December 6, 1996Date of Patent: October 5, 1999Assignee: Pfizer Inc.Inventor: Yuhpyng Liang Chen
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Patent number: 5935978Abstract: This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.Type: GrantFiled: July 28, 1993Date of Patent: August 10, 1999Assignee: Rhone-Poulenc Rorer LimitedInventors: Garry Fenton, Andrew David Morley, Malcolm Norman Palfreyman, Andrew James Ratcliffe, Brian William Sharp, Sukanthini Thurairatnam, Bernard Yvon Jack Vacher, Michael John Ashton, David Charles Cook, Susan Jacqueline Hills, Ian Michael McFarlane, Nigel Vicker
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Patent number: 5932730Abstract: Carboxylic acid derivatives ##STR1## where R-R.sup.6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.Type: GrantFiled: March 27, 1997Date of Patent: August 3, 1999Assignee: BASF AktiengesellschaftInventors: 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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Patent number: 5919792Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are .alpha.v.beta.3 antagonists, .alpha.v.beta.5 antagonists or dual .alpha.v.beta.3/.alpha.v.beta.5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation and tumor growth.Type: GrantFiled: October 28, 1997Date of Patent: July 6, 1999Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, George D. Hartman, William F. Hoffman, Nathan C. Ihle