Chalcogen Bonded Directly To Diazine Ring Carbon Patents (Class 544/408)
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Publication number: 20030207857Abstract: The invention relates to compounds of formula I 1Type: ApplicationFiled: April 11, 2002Publication date: November 6, 2003Inventors: Mavis D. Adam, Mark D. Andrews, Geoffrey E. Gymer, David Hepworth, Harry R. Howard, Donald S. Middleton, Alan Stobie
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Publication number: 20030204085Abstract: Disclosed are compounds of the formula: 1Type: ApplicationFiled: July 30, 2002Publication date: October 30, 2003Inventors: Arthur G. Taveras, Cynthia J. Aki, Richard W. Bond, Jianping Chao, Michael Dwyer, Johan A. Ferreira, Jonathan A. Pachter, John J. Baldwin, Bernd Kaiser, Ge Li, J. Robert Merritt, Kingsley H. Nelson, Laura L. Rokosz
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Patent number: 6635641Abstract: Amide compounds represented by the formula: wherein: R1 is a moiety represented by the formula where X is selected from the group consisting of CH2, O, S, and NH; and Y is selected from the group consisting of CH2, O, and S, provided that at least one of X and Y is CH2, or X and Y together with the bond there-between form a cyclopropyl; are described. These compounds and pharmaceutical compositions containing them modulate and/or inhibit the activity of certain protein kinases and are capable of mediating tyrosine kinase signal transduction in order to modulate and/or inhibit unwanted cell proliferation.Type: GrantFiled: January 19, 2001Date of Patent: October 21, 2003Assignee: Agouron Pharmaceuticals, Inc.Inventors: Steven Lee Bender, Dilip Bhumralkar, Michael Raymond Collins, Stephen James Cripps, Judith Gail Deal, Lei Jia, Mitchell David Nambu, Cynthia Louise Palmer, Zhengwei Peng, Michael David Varney
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Publication number: 20030162958Abstract: A process for preparing a heteroaromatic compound having a heteroaromatic nucleus substituted with one or more ether groups comprising the step of: condensing at least one hydroxy-group of a compound having said heteroaromatic nucleus, said at least one hydroxy group (—OH) being substituted at &agr;- or &bgr;-positions with respect to a heteroatom of said heteroaromatic nucleus, with an alcohol containing one or more primary or secondary alcohol groups, optionally substituted with nitro, amide, ester, halogen, cyano or (hetero)aromatic groups, using the redox couple of a triaryl- or trialkylphosphine and an azodioxo-compound at a temperature between −40° C. and 160° C.Type: ApplicationFiled: December 20, 2002Publication date: August 28, 2003Applicant: AGFA-GEVAERTInventors: John R. Reynolds, Bert Groenendaal, Kyukwan Zong, Luis Madrigal
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Patent number: 6608061Abstract: A medicament for treatment of cancer comprising a compound represented by the following general formula (I) or a physiologically acceptable salt thereof: Ar1—S—R1—S—Ar2 wherein R1 represents a nonmetal bridging group; Ar1 and Ar2 independently represent a group selected from the group consisting of an aryl group which has, on its ring, one to three hydroxyl groups optionally substituted with a monovalent group and said aryl group may have one to three substituents other than hydroxyl group on its ring; and a heteroaryl group which has, on its ring, one to three hydroxyl groups optionally substituted with a monovalent group, and said heteroaryl group may have one to three substituents other than hydroxyl group on its ring.Type: GrantFiled: February 14, 2000Date of Patent: August 19, 2003Assignees: Kyoma Hakko Kogyo Co., Ltd., Fuji Photo Film Co., Ltd.Inventors: Yoshiyuki Yonetani, Takeshi Takahashi, Yuko Kanda, Tamio Mizukami, Tatsuya Tamaoki, Shun-ichi Ikeda, Masanobu Takashima, Naoki Asanuma, Tadashi Inaba, Hiroshi Takeuchi, Hiroshi Kawamoto, Yoshihisa Tsukada, Masato Satomura, Hiroshi Kitaguchi
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Publication number: 20030125338Abstract: Methods and compositions useful in the treatment of amyloidosis and conditions and diseases associated therewith, such as Alzheimer's disease, are provided. The methods involve administering to a subject in need thereof a pharmaceutical composition including one or more agents that modulate PPAR&agr; and/or PPAR&dgr; activity, resulting in an inhibition of &bgr;-amyloid production and/or release from cells of the subject, particularly brain cells.Type: ApplicationFiled: June 12, 2002Publication date: July 3, 2003Applicant: Active Pass Pharmaceuticals, Inc.Inventors: Bruce P. Connop, Amelia Grant, Parimal S. Nathwani
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Patent number: 6586430Abstract: Compounds of Formula 1 [Region &agr;]-[Region &bgr;]-[Region &ggr;]-[Region &dgr;] (I) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and methods of treatment using these compounds.Type: GrantFiled: December 1, 1999Date of Patent: July 1, 2003Assignee: Pfizer Inc.Inventors: Duncan Robert Armour, David Anthony Price, Blanda Luzia Christa Stammen, Anthony Wood, Manoussos Perros, Martin Paul Edwards
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Publication number: 20030092679Abstract: The present invention provides compounds which have a pyrazinone or pyridinone ring at P3 and an optionally substituted heteroaryl group at P1. These compounds have biological activity as active and potent inhibitors of thrombin. Their pharmaceutically acceptable salts, pharmaceutical compositions thereof and methods of using these compounds and pharmaceutical compositions comprising these compounds as therapeutic agents for treatment of disease states in mammals which are characterized by abnormal thrombosis are also described.Type: ApplicationFiled: July 13, 2001Publication date: May 15, 2003Inventors: Daniel Vanna Siev, Joseph Edward Semple, Mallareddy Komandla, John Eugene Reiner, Scott Jeffrey Kemp
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Publication number: 20030078235Abstract: Carbamate compounds of 2-heteroaryl-1,2-ethanediol are described. The compounds are effective in the treatment of disorders of the central nervous system, especially as anti-convulsive or anti-epileptic agents.Type: ApplicationFiled: June 21, 2002Publication date: April 24, 2003Inventors: Yong-Moon Choi, Ki-Ho Lee
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Publication number: 20030073702Abstract: Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: 1Type: ApplicationFiled: October 4, 2002Publication date: April 17, 2003Applicant: 3-Dimensional Pharmaceuticals, Inc.Inventors: Aihua Wang, Bruce Edward Tomczuk, Tianbao Lu, Richard M. Soll, John Curtis Spurlino, Roger Francis Bone
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Publication number: 20030069242Abstract: 3-Arylphenyl sulfide derivatives represented by general formula (I): 1Type: ApplicationFiled: April 15, 2002Publication date: April 10, 2003Applicant: KUMIAI CHEMICAL INDUSTRY CO., LTD.Inventors: Keiji Toriyabe, Nobuo Takefuji, Minoru Itou, Tetsuya Hirade, Kiyotoshi Nishiyama, Mitsuharu Asahida, Yasunobu Maeda, Nobuhide Wada, Toyokazu Fujisawa, Hiroyuki Yano, Masaaki Komatsu, Osamu Tada
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Patent number: 6545154Abstract: The invention relates to a process for preparing N-(5-amino-2-cyano-4-fluoro-phenyl)-sulphonamides in which, in a first step, 2-amino-4,5-difluoro-benzonitrile is reacted with sulphonyl halides in the presence of an acid acceptor and in the presence of a diluent at temperatures between 0° C. and 150° C. and, in a second step, the N-(2-cyano-4,5-difluoro-phenyl)-sulphonamides and/or N-(2-cyano-4,5-difluoro-phenyl)-sulphonimides obtained in the first step are as pure substances or as mixtures with ammonia in the presence of a diluent reacted at a temperature between 100° C. and 200° C. The invention furthermore relates to novel intermediates of the process.Type: GrantFiled: September 5, 2001Date of Patent: April 8, 2003Assignee: Bayer AktiengesellschaftInventors: Achim Hupperts, Mark Wilhelm Drewes, David Erdman, Reinhard Lantzsch
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Publication number: 20030060629Abstract: The present invention provides pyrazine derivatives that inhibit tyrosine kinase activity. Certain pyrazine derivatives are selective inhibitors of vascular endothelial growth factor (VEGF) receptor tyrosine kinase. The present invention also provides pharmaceutical formulations containing the pyrazine derivatives and methods of use of these formulations as anti-tumor agents and to treat solid-tumor cancers, angiogenesis, diabetic retinopathy, rheumatoid arthritis, endometriosis and psoriasis.Type: ApplicationFiled: September 19, 2001Publication date: March 27, 2003Inventors: Gee-Hong Kuo, Peter J. Connolly, Catherine Prouty, Alan DeAngelis, Aihua Wang, Linda Jolliffe, Steve Middleton, Stuart Emanuel
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Publication number: 20030060466Abstract: The present invention is a pyrimidine, triazine or pyrazine derivative of the formula 1Type: ApplicationFiled: May 29, 2002Publication date: March 27, 2003Inventors: Alfred Binggeli, Hans-Peter Maerki, Thierry Masquelin, Vincent Mutel, Maurice Wilhelm, Wolfgang Wostl
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Patent number: 6538016Abstract: The invention relates to &agr;-sulfin- and &agr;-sulfonamino acid amides of the general formula I including the optical isomers thereof and mixtures of such isomers, wherein n is a number zero or one; R1 is C1-C12alkyl, C1-C12alkyl substituted with C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8cycloalkyl, cyano, C1-C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl or C3-C6alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl; C2-C12alkynyl; C1-C12haloalkyl; or a group NR12R13 wherein R12 and R13 are each independently of the other hydrogen or C1-C6-alkyl, or together are tetra- or penta-methylene; R2 and R3 are each independently hydrogen; C1-C8alkyl; C1-C8alkyl substituted with hydroxy, mercapto, C1-C4alkoxy or C1-C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8cycloalkyl-C1-C4alkyl; or the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered hydrocarbon ring; R4, R5, R6 and R7 are each independently hydrogen or C1-C4alType: GrantFiled: June 1, 2001Date of Patent: March 25, 2003Assignee: Syngenta Participations AGInventors: Martin Zeller, André Jeanguenat, Clemens Lamberth
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Patent number: 6534510Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions and are selected from the group consisting of: or a pharmaceutically acceptable salt thereof, wherein A isType: GrantFiled: March 22, 2001Date of Patent: March 18, 2003Assignee: Merck & Co., Inc.Inventors: James C. Barrow, Bruce D. Dorsey, Harold G. Selnick, Phung L. Ngo
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Publication number: 20020183324Abstract: The present application describes monocyclic or bicyclic carbocycles and heterocycles and derivatives thereof of Formula I: 1Type: ApplicationFiled: October 29, 2001Publication date: December 5, 2002Inventors: Irina C. Jacobson, Ruth R. Wexler, Suanne Nakajima, Mimi L. Quan, Shuaige Wang, Joanne M. Smallheer, Jennifer Qiao
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Patent number: 6476016Abstract: Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: wherein R3, R4, R5, W, and A are as set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. 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. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described.Type: GrantFiled: July 17, 2001Date of Patent: November 5, 2002Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Aihua Wang, Bruce Edward Tomczuk, Tianbao Lu, Richard M. Soll, John Curtis Spurlino, Roger Francis Bone
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Patent number: 6472399Abstract: 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: December 12, 2001Date of Patent: October 29, 2002Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Tianbao Lu, Bruce E. Tomczuk, Thomas P. Markotan, Colleen Siedem
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Publication number: 20020128478Abstract: This invention relates to a process for the Heck coupling reaction where heterogeneous palladium catalysts are used to activate aryl halides for a carbon-carbon coupling with olefins in the presence a base and an aprotic solvent to produce aryl-olefin compounds. The process, in particular, provides for the use of aryl chlorides substituted with electron-withdrawing or electron-donating group for the cross coupling with olefins.Type: ApplicationFiled: March 4, 2002Publication date: September 12, 2002Inventors: Shane W. Krska, Thorsten S. Rosner, Yongkui Sun
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Patent number: 6444811Abstract: Compounds represented by formula I: as well as pharmaceutically acceptable salts, esters, N-oxides and hydrates thereof are disclosed. Pharmaceutical compositions and methods of use are also included. The compounds are active against the caspase-3 enzyme, and thus are useful to treat fin caspase-3 mediated diseases and conditions.Type: GrantFiled: July 19, 2000Date of Patent: September 3, 2002Assignee: Merck Frosst Canada & Co.Inventors: Yongxin Han, Andre Giroux, Robert Zamboni, Daniel J. McKay, Christopher I. Bayly, Erich L. Grimm, John Colucci
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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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Publication number: 20020061887Abstract: The present invention relates to compounds of the formula I 1Type: ApplicationFiled: November 28, 2001Publication date: May 23, 2002Applicant: Aventis Pharma Deutschland GmbHInventors: Ursula Schindler, Karl Schonafinger, Hartmut Strobel
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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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Patent number: 6352997Abstract: The present invention provides for a method of treating polycystic ovary syndrome in a subject in need of such treatment comprising the administration of a therapeutically effective amount of a compound of structural formula I: to the subject. The present invention further provides for a method for improving fertility and the response to in vitro fertilization (I.V.F.), comprising administration of therapeutically effective amount of compound of structural formula I to the subject. Further, the present invention provides for compositions useful in the methods of the present invention, as well as a method of manufacture of a medicament useful for treating polycystic ovary syndrome or for improving fertility or the response to in vitro fertilization (I.V.F.).Type: GrantFiled: May 3, 1999Date of Patent: March 5, 2002Assignee: Merck & Co., Inc.Inventors: Joanne Waldstreicher, Georgianna S. Harris
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Patent number: 6329378Abstract: Disclosed are pharmaceutical compositions comprising aryl and heteroaryl hydrazone, hydrazine and thiosemicarbazone derivatives of formulae I and II, and methods for using the compositions as antifungal agents. The invention also relates to novel aryl and heteroaryl hydrazone, hydrazine and thiosemicarbazone derivatives of formulae I and II, their preparation, to pharmaceutical compositions containing them, and to methods of using them to alleviate fungal infections.Type: GrantFiled: February 10, 2000Date of Patent: December 11, 2001Assignee: Anadys Pharmaceuticals, Inc.Inventors: Xiaodan Mei, Peng Wang, Andrei Caracoti, Pamela Mingo, Vincent Boyd, Robert Murray, Nicholas J. Sisti, Yi Bin Xiang, Shuhao Zhu, C. Richard Wobbe, Daniel Moore
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Patent number: 6325860Abstract: A method for making highly potent flavorful and aromatic substances for use in a smoking article is disclosed. The method includes providing a mixture containing hydroxyketone, a Strecker aldehyde, and ammonium hydroxide, and subjecting the mixture to heat treatment for a time and under conditions sufficient to provide a flavorful and aromatic composition.Type: GrantFiled: February 15, 2000Date of Patent: December 4, 2001Assignee: R. J. Reynolds Tobacco CompanyInventor: William Monroe Coleman, III
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Publication number: 20010039343Abstract: This invention relates to a process for the manufacture of compounds which are useful to make either pesticides that can be used as fungicides, herbicides, insecticides, rodenticides or biocides, or pharmaceutical compounds for both human and veterinary application.Type: ApplicationFiled: March 13, 2001Publication date: November 8, 2001Inventors: Mark Joseph Mulvihill, James Joseph Gallagher, Brian Scott MacDougall, Damian Gerard Weaver
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Publication number: 20010034051Abstract: New bicyclic 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 in the treatment of 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: December 14, 2000Publication date: October 25, 2001Inventors: John M. Nuss, Savithri Ramurthy
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Patent number: 6291674Abstract: A process for preparing alkoxypyrazine derivatives of the general formula: These alkoxypyrazine derivatives are obtained by reacting a glyoxal derivative of the general formula: and an aminoimidate of the general formula:Type: GrantFiled: February 20, 2001Date of Patent: September 18, 2001Assignee: Lonza AGInventor: Rudolf Fuchs
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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: 6235905Abstract: A process for preparing alkoxypyrazine derivatives of the general formula: These alkoxypyrazine derivatives are obtained by reacting a glyoxal derivative of the general formula: and an amlinoimidate of the general formula: The alkoxypyrazine derivatives are important intermediates for preparing pharmaceutically active compounds.Type: GrantFiled: January 28, 2000Date of Patent: May 22, 2001Assignee: Lonza AGInventor: Rudolf Fuchs
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Patent number: 6204263Abstract: Pyrazinone compounds are described, including compounds of the Formula I: wherein X is O, NR11 or CH═N, R3-R11, Ra, Rb, Rc, W, m, and n are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. 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. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described.Type: GrantFiled: June 11, 1999Date of Patent: March 20, 2001Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Tianbao Lu, Bruce E. Tomczuk, Thomas P. Markotan
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Patent number: 6200984Abstract: A compound of the general formula I: is disclosed as useful in treating disorders of the central nervous system. Pharmaceutical compositions, processes for preparing the compounds and methods of treatment are also disclosed.Type: GrantFiled: October 5, 1998Date of Patent: March 13, 2001Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Allen B. Reitz, James J. McNally, Pauline Sanfilippo
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Patent number: 6194416Abstract: The present invention relates to therapeutically active compounds of the formula: wherein G is an azacyclic or azabicyclic ring system, W is oxygen or sulfur, r is 0, 1, or 2, and R is defined in the specification; and to methods of treatment using, and pharmaceutical compositions comprising, these compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.Type: GrantFiled: April 10, 1997Date of Patent: February 27, 2001Assignee: Eli Lilly and CompanyInventors: Leander Merritt, Jon K. Reel, John S. Ward, Celia A. Whitesitt
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Patent number: 6187776Abstract: The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.Type: GrantFiled: July 23, 1999Date of Patent: February 13, 2001Assignee: Eli Lilly and CompanyInventors: Leander Merritt, John S. Ward
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Patent number: 6159980Abstract: Corticotropin releasing factor (CRF) antagonists of Formula (I) ##STR1## and their use in treating psychiatric disorders and neurological diseases including major depression, anxiety-related disorders, post-traumatic stress disorders, supranuclear palsy and eating disorders.Type: GrantFiled: September 15, 1997Date of Patent: December 12, 2000Assignee: Dupont Pharmaceuticals CompanyInventors: Argyrios Georgios Arvanitis, Richard E. Olson, Charles R. Arnold, III, William E. Frietze
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Patent number: 6147078Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: ##STR1## wherein ##STR2##Type: GrantFiled: May 19, 1999Date of Patent: November 14, 2000Assignee: Merck & Co., Inc.Inventors: Philip E. Sanderson, Matthew G. Stanton, Suresh K. Balani
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Patent number: 6143887Abstract: The novel process of the present invention involves the stereoselective synthesis of certain 16.beta.-substituted 4-aza-5.alpha.-androstan-3-ones and the useful intermediates obtained therein.Type: GrantFiled: May 11, 1999Date of Patent: November 7, 2000Assignee: Merck & Co., Inc.Inventors: Dominick F. Gratale, Richard L. Tolman, Soumya P. Sahoo
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Patent number: 6136827Abstract: The present invention is directed to cyclic amines of the formula I: ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, m and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.Type: GrantFiled: July 21, 1998Date of Patent: October 24, 2000Assignee: Merck & Co., Inc.Inventors: Charles G. Caldwell, Paul E. Finke, Malcolm Maccoss, Laura C. Meurer, Sander G. Mills, Bryan Oates
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Patent number: 6114524Abstract: The present invention relates to a process for producing a compound represented by the formula (II): ##STR1## wherein X is a halogen atom, each of A.sup.1, A.sup.2 and A.sup.3 are the same or different and are selected from a carbon atom or a nitrogen atom, provided that at least A.sup.1, A.sup.2, or A.sup.3 is a nitrogen atom. Each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and are selected from a hydrogen atom, a lower alkyl group, a cyano group, a carboxyl group, a lower alkoxycarbonyl group, a halogen atom, and a nitro group. It is also provided that where R.sup.1 and R.sup.2 are adjacent to each other, R.sup.1 and R.sup.2 may be combined with each other to form a 5- or 6-membered ring which may carry on the ring thereof one substituent selected from the group consisting of a lower alkyl group, a nitrile group, a carboxyl group, a lower alkoxycarbonyl group, a carbamoyl group, a halogen atom, a nitro group, and an amino-(lower alkyl) group.Type: GrantFiled: June 8, 1999Date of Patent: September 5, 2000Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Shigemitsu Okada, Ryosuke Ushijima, Kiyofumi Ishikawa
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Patent number: 6071900Abstract: The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.Type: GrantFiled: March 22, 1999Date of Patent: June 6, 2000Assignee: Eli Lilly and CompanyInventors: Leander Merritt, John S. Ward
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Patent number: 6066736Abstract: A process for preparing alkoxypyrazine derivatives of the general formula: ##STR1## These alkoxypyrazine derivatives are obtained by reacting a glyoxal derivative of the general formula: ##STR2## and an aminomidiate of the general formula: ##STR3## The alkoxypyrazine derivatives are important intermediates for preparing pharmaceutically active compounds.Type: GrantFiled: June 29, 1998Date of Patent: May 23, 2000Assignee: Lonza AGInventor: Rudolf Fuchs
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Patent number: 6048869Abstract: The novel compounds of the present invention are those of structural formula I: ##STR1## or a pharmaceutically acceptable salt, ester, or stereoisomer thereof, which are inhibitors of 5.alpha.-reductase. The compounds of formula I are useful in the oral, systemic, parenteral or topical treatment of hyperandrogenic conditions. Methods of using the compounds of formula I for the treatment of hyperandrogenic conditions such as acne vulgaris, seborrhea, androgenic alopecia, male pattern baldness, female hirsutism, benign prostatic hyperplasia, and the prevention and treatment of prostatic carcinoma, as well as the treatment of prostatitis the treatment of sweat-related conditions such as apocrine gland sweating, hyperhidrosis, and hydradenitis suppurativa, the treatment of polycystic ovary syndrome, the prevention and treatment of bone loss and related diseases, and the prevention and treatment of premature labor are provided, as well as pharmaceutical compositions for the compounds of formula I.Type: GrantFiled: July 26, 1999Date of Patent: April 11, 2000Assignee: Merck & Co., Inc.Inventors: Derek Von Langen, Susan D. Aster, Donald W. Graham
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Patent number: 6030462Abstract: A smoking article is provided having improved flavor and aroma when smoked and contains one or more smokable materials having free amino acids contained therein. The smoking article comprises a selectively enriched content of at least one amino acid selected from the group consisting of serine, threonine and analogs thereof, and is substantially free of exogenous non-sugar Maillard-functional carbonyl compounds.Type: GrantFiled: October 22, 1998Date of Patent: February 29, 2000Assignee: R.J. Reynolds Tobacco CompanyInventors: Chi-Kuen Shu, Brian Michael Lawrence, Cynthia Stewart Stokes, Milly Mee Lee Wong, Robert Henry Powell
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Patent number: 6015774Abstract: Novel pyrazin-2-one derivatives of formula [1] are provided, ##STR1## which are useful as active ingredients of herbicides, wherein R.sup.1 is hydrogen or alkyl; R.sup.2 is haloalkyl; R.sup.3 is optionally substituted alkyl; alkenyl, or alkynyl; and Q is optionally substituted phenyl. Also provided are their use and intermediates for their production.Type: GrantFiled: March 20, 1998Date of Patent: January 18, 2000Assignee: Sumitomo Chemical Company, LimitedInventors: Akira Shuto, Hisayuki Hoshi, Yuzuru Sanemitsu
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Patent number: 6011038Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: ##STR1## for example: ##STR2##Type: GrantFiled: September 3, 1998Date of Patent: January 4, 2000Assignee: Merck & Co., Inc.Inventors: Bruce D. Dorsey, Philip E. Sanderson, Terry A. Lyle
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Patent number: 6008237Abstract: Substituted 5-aryl-2,4-thiazolidinediones are potent agonists of PPAR, and are therefore useful in the treatment, control or prevention of diabetes, hyperglycemia, hyperlipidemia (including hypercholesterolemia and hypertriglyceridemia), atherosclerosis, obesity, vascular restenosis, and other PPAR .alpha., .delta. and/or .gamma. mediated diseases, disorders and conditions.Type: GrantFiled: December 17, 1998Date of Patent: December 28, 1999Assignee: Merck & Co., Inc.Inventors: Soumya P. Sahoo, Richard L. Tolman, Wei Han, Jeffrey Bergman, Conrad Santini, Victoria K. Lombardo, Ranjit Desai, Julia K. Boueres, Dominick F. Gratale
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Patent number: 5998618Abstract: A process for preparing 3-alkoxy-5-alkylpyrazin-2-amines of the general formula: ##STR1## wherein R.sup.1 is a C.sub.1-4 -alkyl group or an aryl group and R.sup.2 is a C.sub.1-4 -alkoxy group or an aryloxy group, starting either from aminomalononitrile or from aminoacetonitrile.Type: GrantFiled: October 22, 1998Date of Patent: December 7, 1999Assignee: Lonza AGInventors: Walter Brieden, Rudolf Fuchs
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Patent number: 5998444Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, Q.sup.4, and Q.sup.5 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of SP and NKA are useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.Type: GrantFiled: November 26, 1997Date of Patent: December 7, 1999Assignee: Zeneca Ltd.Inventor: Keith Russell