1,2,5-thiadiazoles (including Hydrogenated) Patents (Class 548/134)
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Publication number: 20040077856Abstract: PDF inhibitors and novel methods for their use are provided.Type: ApplicationFiled: August 29, 2003Publication date: April 22, 2004Inventors: Jia-Ning Xiang, Siegfried B. Christensen IV, Xiangmin Liao, Maxwell D. Cummings
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Publication number: 20040072880Abstract: Novel cycloalkyl compounds useful as inhibitors of potassium channel function (especially inhibitors of the Kv1 subfamily of voltage gated K+ channels, especially inhibitors Kv1.5 which has been linked to the ultra-rapidly activating delayed rectifier K+ current IKur), methods of using such compounds in the prevention and treatment of arrhythmia and IKur-associated conditions, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: January 31, 2003Publication date: April 15, 2004Inventors: John Lloyd, Yoon T. Jeon, Heather Finlay, Lin Yan, Michael F. Gross, Serge Beaudoin
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Patent number: 6706743Abstract: The instant invention provides &bgr;3 adrenergic receptor agonists of structural Formula (I), the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers and prodrugs, wherein Ar, R, R1, R2, R3, R4, R5, R6, R7, R8, X, and Y, are as defined herein.Type: GrantFiled: March 5, 2003Date of Patent: March 16, 2004Assignee: Pfizer IncInventors: Robert F. Day, Jennifer A. Lafontaine
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Publication number: 20040048864Abstract: Heterocyclic aromatic amides having a hydroxy group adjacent to the amide functionality are useful as antifungal agents, particularly for plants.Type: ApplicationFiled: December 2, 2002Publication date: March 11, 2004Inventors: Michael J. Ricks, Richard B. Rogers, William H. Dent, Chenglin Yao, Bassam S. Nader, Gina M. Fitzpatrick, Noormohamed M. Niyaz, Robert P. Gajewski, John L. Miesel, Kevin G. Meyer, Irene M. Morrison
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Publication number: 20040029883Abstract: The present invention relates to compounds of general formula (I), wherein the residues R represent organic radicals, X represents a bond, oxygen or —NR12 and Y represents oxygen or sulfur, processes for their preparation, pharmaceutical compositions containing them as well as their use for the production of pharmaceutical compositions for the treatment of inflammatory, autoimmune and immune diseases.Type: ApplicationFiled: November 19, 2002Publication date: February 12, 2004Inventors: Markus Albers, Thomas Lehmann, Thomas Rlle, Gerhard Mller, Gerhard Hessler, Masaomi Tajimi, Karl Ziegelbauer, Hiromi Okigami, Haruki Hasegawa
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Publication number: 20040014758Abstract: The present application describes modulators of CCR3 of formula (I): 1Type: ApplicationFiled: July 3, 2003Publication date: January 22, 2004Inventors: Dean A. Wacker, John V. Duncia, Joseph B. Santella, Daniel S. Gardner
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Patent number: 6677360Abstract: The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of pharmaceutical compositions for the treatment and prophylaxis of cancer, arteriosclerosis, restenosis, osteolytic disorders such as osteoporosis and ophthalmic diseases. The compounds according to the invention have the formula (1) wherein R1, R2, U, V, A, B, W, R3, C and R4 have the meaning as defined in the claims.Type: GrantFiled: April 6, 2001Date of Patent: January 13, 2004Assignee: Bayer AktiengesellschaftInventors: Markus Albers, Klaus Urbahns, Andrea Vaupel, Michael Härter, Delf Schmidt, Beatrix Stelte-Ludwig, Christoph Gerdes, Elke Stahl, Jörg Keldenich, Ulf Brueggemeier, Klemens Lustig
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Publication number: 20030220315Abstract: Alkenyldiarylmethane (ADAM) compounds have been found effective as anti-HIV agents. Novel ADAM compounds, their pharmaceutical formulations and a method of using same to treat viral infections are described.Type: ApplicationFiled: May 27, 2003Publication date: November 27, 2003Inventors: Mark S. Cushman, Agustin Casimiro-Garcia, William G. Rice
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Patent number: 6642180Abstract: The present invention relates to novel biphenyl-substituted cyclic ketoenols of the formula (I) in which W represents hydrogen, halogen, alkyl, alkoxy, alkenyloxy, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro or cyano, X represents halogen, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro, cyano or in each case optionally substituted phenyl, phenoxy, phenylthio, phenylalkoxy or phenylalkylthio, Y represents in each case optionally substituted cycloalkyl, aryl or hetaryl, Z represents hydrogen, halogen, alkyl, alkoxy, halogenoalkyl or halogenoalkoxy, CKE represents one of the groups in which A, B, D, L, M, Q1, Q2, Q3, Q4, Q5 and Q6 are as defined in the description, to preparation and to their use as pesticides and herbicides.Type: GrantFiled: January 25, 2002Date of Patent: November 4, 2003Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Alan Graff, Thomas Bretschneider, Christoph Erdelen, Mark Wilhelm Drewes, Dieter Feucht
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Publication number: 20030203900Abstract: Cathepsin S is a highly active cysteine protease belonging to the papain superfamily. It is found mainly in lymph nodes, spleen, and macrophages and this limited occurrence suggests the potential involvement of this enzyme in the pathogenesis of degenerative disease. The invention relates to novel protease inhibitors, particularly inhibitors of the cysteine proteases of the papain superfamily and more particularly to Cathepsin S. The inhibitors are Furanone derivatives of Formula (II) which have a characteristic non-hydrogen substituent R5. They are selective over other members of the family and in particular show selectivity over other members of the Cathepsin family such as L and K.Type: ApplicationFiled: November 16, 2001Publication date: October 30, 2003Inventors: Martin Quibell, Steven Taylor, Urszula Grabowska, Magnus Nilsson, Veronique Morisson
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Patent number: 6635630Abstract: Compound represented by the structural formula or a pharmaceutically acceptable salt thereof, wherein Ar1 and Ar2 are optionally substituted heteroaryl or optionally substituted phenyl; X1 is —O—, —S—, —SO—, —SO2—, —NR12—, —NCOR12— or —NR12SO2R15; is selected from the group consisting of X2 is —O—, —S— or —NR5—; Y is ═O, ═S or ═NR11; Y1 is H, C1-C6 alkyl, —NR17R13, —SCH3, R19-aryl(CH2)n6—, R19-heteroaryl-(CH2)n6—, —(CH2)n6—heterocycloalkyl, —(C1-C3)alkyl-NH—C(O)O(C1-C6)alkyl or —NHC(O)R15; R5 is H or —(CH2)n1—G, wherein n1 is 0-5, G is H, —CF3, —CHF2, —CH2F, —OH, —O—(C1-C6 alkyl), —SO2R13, —O—(C3-C8 cycloalkyl), —NR13R14, —SO2NR13R14, —NR13SO2R15, —NR13COR12, —NR12(CONR13Type: GrantFiled: June 6, 2002Date of Patent: October 21, 2003Assignee: Schering CorporationInventors: Neng-Yang Shih, Ho-Jane Shue, Gregory A. Reichard, Sunil Paliwal, David J. Blythin, John J. Piwinski, Dong Xiao, Xiao Chen
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Patent number: 6620940Abstract: The present invention relates to 3-chloro-4-halo-1,2,5-thiadiazole compounds, a method of producing novel mono- and di-substituted-1,2,5-thiadiazoles therefrom, as well as mono- and di-substituted -1,2,5-thiadiazoles.Type: GrantFiled: September 27, 2000Date of Patent: September 16, 2003Assignee: Eli Lilly and CompanyInventor: Roger Lewis Robey
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Publication number: 20030158155Abstract: A compound of the formula (1): 1Type: ApplicationFiled: October 15, 2002Publication date: August 21, 2003Inventors: Yozo Hori, Fumihiko Watanabe, Hiroshige Tsuzuki, Shingo Furue, Yoshinori Tamura
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Patent number: 6605630Abstract: The invention concerns a compound of the formula (I): wherein, for example: T is of the formula (IA), (IB), or (IC); R1 is of the formula —NHC(═O)Rb wherein Rb is (1-4C)alkyl; R2 and R3 are hydrogen or fluoro; >A—B— is >C═CH— (but not when T is (IA)) or >CH—CH2—; wherein when T is of the formula (IA) or (IB); R6 is, for example, (1-4C)alkyl; R5 is hydrogen, R10CO—, R10SO2— or R10CS— wherein R10 is, for example, optionally substituted phenyl, or (1-10C)alkyl, or when T is of the formula (IA), (IB); or (IC): R5 and R6 are linked to give a 5- or 6-membered ring which is fused to the ring shown in (IA), (IB), or (IC) so as to give an optionally substituted bicyclic ring; and pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them, and their use as antibacterial agents.Type: GrantFiled: February 18, 2000Date of Patent: August 12, 2003Assignee: Syngenta LimitedInventor: Michael Barry Gravestock
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Patent number: 6603013Abstract: The present invention relates to a process wherein heterogeneous finely-dispersed palladium catalysts are used in a cross-coupling reaction of alkenyl halides and aryl or heteroaryl boronic acids in the presence of base in an aprotic solvent to produce aryl- or heteroaryl-olefin compounds of Formula I:Type: GrantFiled: July 16, 2001Date of Patent: August 5, 2003Assignee: Merck & Co., Inc.Inventors: Yongkui Sun, Carl LeBlond, John R. Sowa, Jr.
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Publication number: 20030144281Abstract: Disclosed are substituted benzimidazole compounds of formula(I): 1Type: ApplicationFiled: November 5, 2002Publication date: July 31, 2003Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Charles Cywin, Jinbo Lee, Steven S. Pullen, Gregory Paul Roth, Christopher Ronald Sarko, Roger John Snow, Noel Stewart Wilson
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Publication number: 20030134801Abstract: The present invention relates to a compound having formula I: 1Type: ApplicationFiled: November 1, 2002Publication date: July 17, 2003Applicant: LG Life Sciences, Ltd.Inventors: Koo Lee, Won Hyuk Jung, Cheol Won Park, Sang Koo Lee, Sun Hwa Lee, Hee Dong Park
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Patent number: 6589914Abstract: The dihalopropene compounds of the general formula (I) have excellent insecticidal/acaricidal activity, so that they are satisfactorily effective for the control of noxious insects, mites and ticks.Type: GrantFiled: March 4, 2002Date of Patent: July 8, 2003Assignee: Sumitomo Chemical Company, LimitedInventors: Noriyasu Sakamoto, Sanshiro Matsuo, Masaya Suzuki, Taro Hirose, Kazunori Tsushima, Kimitoshi Umeda
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Publication number: 20030105327Abstract: There is provided a process for preparing a pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid which comprises condensing an amino acid and N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanine.Type: ApplicationFiled: November 18, 2002Publication date: June 5, 2003Applicant: KANEKA CORPORATIONInventors: Yasuyoshi Ueda, Koichi Kinoshita, Tadashi Moroshima, Yoshifumi Yanagida, Yoshihide Fuse
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Publication number: 20030083315Abstract: The present invention provides a benzimidazole derivative or its. pharmaceutically permissible salt expressed by the following formula (1). Further, the present invention provides a human chymase activity inhibitor containing the substance as an active ingredient.Type: ApplicationFiled: September 14, 2001Publication date: May 1, 2003Inventors: Naoki Tsuchiya, Yoshiyuki Matsumoto, Hiroshi Saitou, Tsuyoshi Mizuno
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Patent number: 6555559Abstract: The present invention provides novel PGI2 derivatives and an anti Helicobacter agent, a platelet function potentiating agent or a cervical ripening agent containing any of the derivatives.Type: GrantFiled: August 1, 2000Date of Patent: April 29, 2003Assignee: Toray Industries, Inc.Inventors: Hisanori Wakita, Naohiro Yamada, Hitoshi Hatakeyama, Takeshi Ishigaki, Noriyuki Hirano, Takeshi Mori
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Publication number: 20030069237Abstract: The present application describes nitrogen containing heterobicyclics and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.Type: ApplicationFiled: April 26, 2002Publication date: April 10, 2003Inventors: John M. Fevig, Joseph Cacciola, Charles G. Clark, Qi Han, Patrick Yuk Sun Lam, Donald J.P. Pinto, James R. Pruitt, Mimi L. Quan, Karen A. Rossi
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Patent number: 6545022Abstract: Novel amines of formulas 1D and 1E are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases, and gastrointestinal disorders, especially IBS. Processes for the preparation and intermediates useful in the preparation are also disclosed.Type: GrantFiled: April 7, 2000Date of Patent: April 8, 2003Assignee: Pfizer Inc.Inventors: Justin Stephen Bryans, David Christopher Horwell, Clare Octavia Kneen, David Juergen Wustrow
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Publication number: 20030064985Abstract: A compound of formula (I) or its enantiomers or diastereoisomers thereof: 1Type: ApplicationFiled: December 17, 2001Publication date: April 3, 2003Inventors: Christiane Yoakim, Bruno Hache, William W. Ogilvie, Jeffrey O'Meara, Peter White, Nathalie Goudreau
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Publication number: 20030065190Abstract: The present invention relates to novel spiro compounds of the formula (I) 1Type: ApplicationFiled: September 13, 2002Publication date: April 3, 2003Inventors: Hubert Spreitzer, Josef Salbeck, Frank Weissortel
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Patent number: 6537948Abstract: The present invention relates to an uracil compound of the formula [I]: [wherein, Q—R3 represents a R3-substituted group of a 5-membered or 6-membered heterocyclic ring having one or two nitrogen selected from the group consisting of moieties represented in the specification (wherein, this heterocyclic ring may be substituted with at least one kind of substituent, Y represents oxygen, sulfur, imino or C1 to C3 alkylimino, R1 represents C1 to C3 alkyl or C1 to C3 haloalkyl, R2 represents C1 to C3 alkyl, R3 represents carboxy C1 to C6 alkyl, C1 to C6 alkoxycarbonyl C1 to C6 alkyl, OR7, SR8, N(R9)R10 or the like, X1 represents halogen, cyano, thiocarbamoyl or nitro, X2 represents hydrogen or halogen. {wherein, each of R7, R8 and R10 independently represents carboxy C1 to C6 alkyl, C1 to C6 alkoxycarbonyl C1 to C6 alkyl, C1 to C6 haloalkoxycarbonyl C1 to C6 alkyl, or the like, and R9 represents hydrogen or C1 to C6 alkyl.}.].Type: GrantFiled: January 31, 2001Date of Patent: March 25, 2003Assignee: Sumitomo Chemical Company, LimitedInventors: Yoshitomo Tohyama, Yuzuru Sanemitsu
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Patent number: 6525086Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, A, X, T, Q, Z, U, Y, Ar, p and n are as defined in the specification. These compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).Type: GrantFiled: March 14, 2001Date of Patent: February 25, 2003Assignee: Novo Nordisk A/SInventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
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Publication number: 20030008874Abstract: The invention provides compounds of formula (I) wherein R0, R1, R2 and A are as defined in the description, and the preparation thereof. The compounds of formula (I) have high affinity as &agr;2 adrenoceptors and hence are useful as pharmaceuticals.Type: ApplicationFiled: July 24, 2002Publication date: January 9, 2003Inventors: Max Peter Seiler, Joachim Nozulak
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Patent number: 6503912Abstract: The present application relates to novel guanidine derivatives of the formula (I) in which R1 represents a five- or six-membered heterocyclic group; R2 represents hydrogen or alkyl, R3 represents the groupings —OR4, —OCOR5, —OCOOR6, —OCONR7R8 and —OSO2R9, where R4, R5 and R6 independently of one another represent alkyl, alkoxyalkyl, halogenoalkyl, alkenyl, alkinyl, alkylaminoalkyl, dialkylaminoalkyl, optionally substituted cycloalkyl and in each case optionally substituted phenyl or benzyl, R7 and R8 independently of one another represent hydrogen, alkyl, alkenyl and in each case optionally substituted phenyl or benzyl and R9 represents alkyl or optionally substituted phenyl, A represents the groupings —CH2CH2—, (CH2)3 and —CH═CH— and z represents cyano or nitro, with the proviso that, if Z represents NO2 and A represents —CH2CH2—, the radical R2 represents hydrogen; and the compound of the formula (I) in whichType: GrantFiled: June 28, 2000Date of Patent: January 7, 2003Assignee: Bayer AktiengesellschaftInventors: Klaus Wagner, Christoph Erdelen, Wolfram Andersch, Ulrike Wachendorff-Neumann, Andreas Turberg, Norbert Mencke
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Publication number: 20020173492Abstract: Compounds of formula (I) or pesticidally acceptable salts thereof, compositions containing them and methods of use.Type: ApplicationFiled: February 1, 2002Publication date: November 21, 2002Inventor: Tai-Teh Wu
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Publication number: 20020128232Abstract: The present invention relates to novel angiogenic-inhibitory compounds of formula (I) 1Type: ApplicationFiled: October 12, 2001Publication date: September 12, 2002Inventors: Scott A. Henderson, Barry R. Matthews
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Publication number: 20020119998Abstract: The present invention relates to certain substituted oxadiazole, thiadiazoles and triazole peptoids which are useful as inhibitors of serine proteases. Compounds of the invention are useful for treating, for example, adult respiratory distress syndrome, septic shock, and myocardial ischemia-reperfusion injury.Type: ApplicationFiled: November 16, 2001Publication date: August 29, 2002Inventors: Albert Gyorkos, Lyle W. Spruce
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Publication number: 20020052510Abstract: This invention relates to novel N-linked sulfonamides of N-heterocyclic carboxylic acid and carboxylic acid isosteres, their preparation, and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, and for treating alopecia and promoting hair growth.Type: ApplicationFiled: December 3, 1998Publication date: May 2, 2002Inventors: GREGORY S. HAMILTON, MARK H. NORMAN, YONG-QIAN WU
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Publication number: 20020045641Abstract: The present invention is directed to novel carboxylic acids and isosteres of heterocyclic ring compounds which have multiple heteroatoms within the heterocyclic ring, novel derivatives containing N-linked diketos, sulfonamides, ureas and carbamates attached thereto, their preparation and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, as well as for treating alopecia and promoting hair growth.Type: ApplicationFiled: February 6, 2001Publication date: April 18, 2002Inventors: Gregory S. Hamilton, Mark H. Norman, Yong-Qian Wu
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Publication number: 20020035137Abstract: Compounds of formula (I) 1Type: ApplicationFiled: July 31, 2001Publication date: March 21, 2002Inventors: Gang Liu, Bruce G. Szczepankiewicz, Zhonghua Pei, Zhili Xin, Thorsten K. Oost, David A. Janowick
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Patent number: 6340697Abstract: Various oxime derivatives are provided, which do not cause any chemical damage to plants and which exhibit sufficient effectiveness against various plant diseases. The oxime derivatives are expressed by two general chemical formulas (1) and (2), as follows. Agricultural chemicals and plant disease control chemicals are also provided which contain the above mentioned oxime derivatives as active ingredients. Test results of these agricultural chemicals and the plant disease control chemicals are proved to be very effective for downey mildews and late blights or Phytophthora rot etc.Type: GrantFiled: June 12, 2000Date of Patent: January 22, 2002Assignee: Dainippon Ink and Chemicals, Inc.Inventors: Takeo Kobori, Tomoko Goto, Hitoshi Kondo, Hiroyuki Tsuboi, Mika Iiyama, Toru Asada, Takashi Goto
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Patent number: 6331537Abstract: This invention relates to novel N-heteorocyclic carboxylic acids and carboxylic acid isosteres, their preparation and use for treating neurological disorders including physically damaged nerves and neurodengenerative diseases, for treating alopecia and promoting hair growth, for treating vision disorders and/or improving vision, and for treating memory impairment and/or enhancing memory performance by administering such compounds.Type: GrantFiled: December 2, 1999Date of Patent: December 18, 2001Assignee: GPI Nil Holdings, Inc.Inventors: Gregory S. Hamilton, Mark H. Norman, Yong-Qian Wu
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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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Patent number: 6329366Abstract: A pharmaceutical compound of the formula in which R1 and R2 are each hydrogen, halo, cyano or methyl, the dotted line represents an optional double bond, where R4 and R5 are each hydrogen, C1-6 alkyl, cyclopropyl or cyclopropyl-C1-6 alkyl, n is 0 or 1, and R3 is —SR6, —SOR6, —SO2R6, —COR6, —CH2OH or —CONHR7, where R6 is C1-6 alkyl and R7 is hydrogen or C1-6 alkyl; provided that when one of R1 and R2 is hydrogen and the other is fluoro, R4 and R5 are each hydrogen or C1-6 alkyl, and n is 0, then R3 is not —COR6 or —CONHR7; and salts thereof.Type: GrantFiled: November 18, 1999Date of Patent: December 11, 2001Assignee: Eli Lilly and Company LimitedInventors: John Fairhurst, Peter Thaddeus Gallagher, Martin Victor Miles
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Patent number: 6329421Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.Type: GrantFiled: February 25, 1997Date of Patent: December 11, 2001Assignee: Merck Frosst Canada & Co.Inventors: Petpiboon Prasit, Daniel Guay, Zhaoyin Wang, Serge Leger, Michel Therien
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Publication number: 20010047017Abstract: The present invention is directed to new 1-(1H-1,2,4-triazol-1-yl)butan-2-ol derivatives of the formula (I), 1Type: ApplicationFiled: March 22, 2001Publication date: November 29, 2001Inventors: Susumu Komiyama, Nobuo Shimma, Takuo Tsukuda
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Patent number: 6320050Abstract: 2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 2-position being a substituted phenyl group and at the 3-position being a cycloalkyl ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.Type: GrantFiled: March 15, 2000Date of Patent: November 20, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Fred Thomas Bizzarro, Wendy Lea Corbett, Joseph Francis Grippo, Nancy-Ellen Haynes, George William Holland, Robert Francis Kester, Ramakanth Sarabu
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Patent number: 6297374Abstract: Insecticides of the formula in which n is 0 or 1, X is S, O, or Y is N or Z is a 5- or 6-membered nitrogen-containing heterocyclic ring, and R to R9 variously represent hydrogen or specified organic radicals.Type: GrantFiled: May 11, 1999Date of Patent: October 2, 2001Assignee: Nihon Bayer Agrochem K.K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Koichi Moriya
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Patent number: 6262089Abstract: New compounds have the formula: wherein R, R1, X and Y have the meanings described herein. Methods are set forth for synthesizing these compounds and using these compounds to treat diseases associated with amyloidosis, such as Alzheimer's disease, maturity onset diabetes mellitus, familial amyloid polyneuropathy, scrapie, and Kreuzfeld-Jacob disease.Type: GrantFiled: February 16, 2000Date of Patent: July 17, 2001Assignee: Hoffman-La Roche Inc.Inventors: Cornelia Hertel, Torsten Hoffmann, Roland Jakob-Roetne, Roger David Norcross
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Patent number: 6225329Abstract: The present invention provides novel compounds of Formula 1, compositions containing these compounds, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTP&agr;, LAR and HePTP or the like, wherein A, R1, R2, R3, R4, R16 and R17 are as defined in the specification.Type: GrantFiled: March 9, 1999Date of Patent: May 1, 2001Assignee: Novo Nordisk A/SInventors: Lutz Stefan Richter, Henrik Sune Andersen, Josef Vagner, Claus Bekker Jeppesen, Niels Peter Hundahl Møller, Sven Branner, Jing Su, Farid Bakir, Luke Milburn Judge
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Patent number: 6166028Abstract: Compounds of the formula ##STR1## are useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpesvirus.Type: GrantFiled: November 22, 1999Date of Patent: December 26, 2000Assignee: American Home Products CorporationInventors: Jonathan Bloom, Martin DiGrandi, Russell Dushin, Stanley Lang, Bryan O'Hara
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Patent number: 6159994Abstract: Compounds of formula (I) and pharmaceutically acceptable salt thereof are useful as histamine H.sub.3 receptor ligands. R.sup.1 is an optional substituent such as C.sub.1 to C.sub.6 alkyl. The moiety (1) replaces any available hydrogen atom on a carbon or nitrogen atom in the ring which includes X. R.sup.2 is C.sub.1 to C.sub.8 hydrocarbylene (in which one or more hydrogen atoms may be replaced by halogen atoms, and up to 2 carbon atoms may be replaced by oxygen, nitrogen or sulfur atoms); R.sup.3 replaces any available hydrogen atom on a carbon or nitrogen atom in the ring which includes X, and is hydrogen or C.sub.1 to C.sub.15 hydrocarbyl (in which one or more hydrogen atoms may be replaced by halogen atoms, and up to 3 carbon atoms may be replaced by oxygen, nitrogen or sulfur atoms); the (or each) R.sup.4 group is independently selected from H, non-aromatic C.sub.1 to C.sub.6 hydrocarbyl, and aryl (C.sub.1 to C.sub.3 alkyl); X is --SO-- or --SO.sub.2 --; Y and Z are each hydrogen, or together represent .Type: GrantFiled: March 13, 2000Date of Patent: December 12, 2000Assignee: James Black FoundationInventors: Iain Mair McDonald, David John Dunstone, Matthew John Tozer
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Patent number: 6150532Abstract: The present invention relates to novel protein tyrosine phosphatase modulating compounds having the general structure shown in Formula (A1), to methods for their preparation, to compositions comprising the compounds, to their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention relates to modulation of the activity of molecules with phosphotyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganism, eukaryoic cells, whole animals and human being. R' and R" are independently selected from the group consisting of hydrogen, halo, cyano, nitro, trihalomethyl, alkyl, arylalkyl. R'" is selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, arylalkyl. X is aryl. Y is selected from hydrogen or ##STR1## wherein (*) indicates a potential point of attachment to X.Type: GrantFiled: December 11, 1998Date of Patent: November 21, 2000Inventors: Adnan Mjalli, Sepehr Sarshar, Xiaodong Cao, Farid Bakir
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Patent number: 6107311Abstract: A compound having the structure: ##STR1## wherein (a) n is from 1 to about 3;(b) X is selected from the group consisting of O, S, SO, or SO.sub.2 ;(c) Y is independently hydrogen or straight, branched or cyclic alkyl having from 1 to about 4 carbon atoms, or the Y's are bonded together to form an alkanyl ring having from about 3 to about 7 atoms;(d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen;(e) W is O or S; and(f) Het is a heteroaryl group comprising one or more rings each ring containing from about 5 to about 6 atoms other than hydrogen and wherein the group contains at least one heteroatom selected from O, N, or S.pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.Type: GrantFiled: April 9, 1998Date of Patent: August 22, 2000Assignee: The Procter & Gamble CompanyInventors: Laurence Ichih Wu, John Michael Janusz
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Patent number: 6060492Abstract: The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective .beta.3 adrenergic receptor agonists useful in the treatment of Type II diabetes and obesity. The invention provides compounds and method of treating type II diabetes, comprising administering to a mammal in need thereof compounds of the Formula II: ##STR1## The variables in Formula II are defined herein.Type: GrantFiled: June 25, 1997Date of Patent: May 9, 2000Assignee: Eli Lilly and CompanyInventors: Michael Gregory Bell, Thomas Alan Crowell, Donald Paul Matthews, John Hampton McDonald, III, David Andrew Neel, Anthony John Shuker, Mark Alan Winter