Pyridine Ring Or Partially Hydrogenated Pyridine Ring Patents (Class 546/193)
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Patent number: 6864249Abstract: The present invention relates to a compound having formula I: and pharmaceutically acceptable salts thereof. The compounds of formula I and pharmaceutical compositions containing them are of the class of thrombin inhibitors which are useful as anticoagulants.Type: GrantFiled: November 1, 2002Date of Patent: March 8, 2005Assignee: 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: 6861530Abstract: This invention relates to substituted piperidine derivatives having at least one six-membered ring substituent. The piperidine derivatives exhibit antitumor activity and are useful as pharmaceuticals such as an antitumor agent.Type: GrantFiled: July 6, 2001Date of Patent: March 1, 2005Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Shinji Nara, Rieko Nakatsu, Yutaka Kanda, Shiro Akinaga, Mitsunobu Hara, Jun Eishima, Timothy A. Grese, Douglas L. Gernert
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Patent number: 6858629Abstract: Compounds of formula (I): where X is N or CH; A represents a group of formula (a) or (b) R1 represents hydrogen or an —NH2, —NR3R4, —NR3CO(C1-C4)Alk or —NR3SO2(C1-C4)Alk group; R2 represents hydrogen, a halogen or a (C1-C4)Alk, (C1-C4)alkoxy, —COOH, —COO(C1-C4)Alk, —CN, —CONR3R4, —NO2, —SO2NR3R4 or —NHSO2(C1-C4)Alk; m and n each represent 0, 1 or 2; R3 and R4 each represent hydrogen or a (C1-C4)Alk group; Y1 and Y2 each represent NH or O; and their salts or solvates, a process for their preparation and the pharmaceutical compositions comprising them.Type: GrantFiled: September 8, 2000Date of Patent: February 22, 2005Assignee: Sanofi-SynthelaboInventors: Roberto Cecchi, Ambrogio Oliva
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Patent number: 6852736Abstract: The invention concerns phenoxypropanolamines of formula (I) in which R1 represents a hydrogen, a group —S(O)z—(C1-C4)alk-R?, (R? being H, phenyl or (C1-C4)alkoxy), —NHSO2—(C1-C4)alk or NHCO(C1-C4)alk; m and n are each independently 0, 1 or 2; R2 and R3 independently represent a hydrogen, a (C5-C6)alkyl, (C3-C6)cycloalkyl, (C1-C4)alkoxy, hydrogen(C1-C4)alkoxy-(C1-C4)alkyl, mono- or di(C1-C4)alkamino(C1-C4)alkyl, pyrrolidino(C1-C4)alkyl, phenylamino or (C2-C4)alkenyl group, an aromatic or heteroaromatic group optionally substituted with a group R4, an aralkyl or heteroaralkyl group optionally substituted with a group R4, R2 and R3 can also together constitute a saturated or unsaturated ring of 3 to 8 atoms possibly bearing a (C1-C4)alkyl, amino (C1-C4)alkyl, carbamoyl or benzyl substituent; R4 represents a hydrogen or a halogen, or a group —CO(C1-C4)alk or a group —NHSO2—(C1-C4)alk; a group (C1-C4)alk, a group (C1-C4)alkoxy, a halogen, —COOH, —COO(C1-C4)alk, —CN, —CONR3R4, —NO2, —SO2NH2 or —NHSO2(C1-C4)alk;Type: GrantFiled: December 15, 2000Date of Patent: February 8, 2005Assignee: Sanofi-SynthelaboInventors: Philippe R. Bovy, Roberto Cecchi, Olivier Venier
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Patent number: 6846825Abstract: Compounds of formula (II) are antibacterial agents wherein Q represents a radical of the formula: —N(OH)CH(?O) or the formula: —C(?O)NH(OH); R1 represents hydrogen, C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms, or, except when Q is a radical of the formula: —N(OH)CH(?O), a hydroxy, C1-C6 alkoxy, C1-C4 alkenyloxy, amino, C1-C4 alkylamino, or di-(C1-C6 alkyl)amino group; R2 represents a substituted or unsubstituted C1-C6 alkyl, cycloalkyl(C1-C6 alkyl)- or aryl(C1-C6 alkyl)-group; and A represents a group of formula (IIA), or (IIB) wherein R4 represents the side chain of a natural or non-natural alpha amino acid, and R5 and R6 when taken together with the nitrogen atom to which they are attached form a saturated heterocyclic first ring of 5 to 7 atoms as specified in the description.Type: GrantFiled: August 10, 2000Date of Patent: January 25, 2005Assignee: British Biotech Pharmaceuticals LimitedInventors: Lisa Marie Pratt, Kenneth Noel Keavey, Gilles Denis Pain, Laurent Mounier
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Patent number: 6838564Abstract: Compounds of the formula (I) in which the substituents are as defined in claim 1 are suitable for use as herbicidesType: GrantFiled: June 7, 2001Date of Patent: January 4, 2005Assignee: Syngenta Crop Protection, Inc.Inventors: Andrew Edmunds, Alain De Mesmaeker, Christoph Lüthy, Jürgen Schaetzer
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Publication number: 20040266821Abstract: Certain novel 4-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: ApplicationFiled: July 20, 2004Publication date: December 30, 2004Inventors: Feroze Ujjainwalla, Lin Chu, Mark T. Goulet, Bonnie Louridas, Matthew J. Wyvratt, Daniel Warner
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Patent number: 6835840Abstract: The present invention discloses a now and improved process for the preparation 1-substituted di-aryl-4-amino-piperidinyl compounds by a one-pot double arylation followed by optional deprotection step(s).Type: GrantFiled: June 4, 2003Date of Patent: December 28, 2004Assignee: AstraZeneca ABInventor: Andrew Griffin
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Patent number: 6835739Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: October 15, 2003Date of Patent: December 28, 2004Assignee: Millennium Pharmaceuticals, Inc.Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
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Patent number: 6833369Abstract: This invention concerns compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein X is CH or N; R1 is hydrogen, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, mono- or di(C1-6alkyl)amino, Ar1, Ar1NH—, C3-6cycloalkyl, hydroxymethyl or benzyloxymethyl; R2 is hydrogen, C1-6alkyl, amino, aminocarbonyl, mono- or di(C1-6alkyl)amino, C1-6alkyloxycarbonyl, C1-6alkylcarbonylamino, hydroxy or C1-6alkyloxy; R3, R4 and R5 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, nitro, amino, cyano, azido, C1-6alkyloxyC1-6alkyl, C1-6alkylthio, C1-6alkyloxycarbonyl or Het1; is Ar2, Ar2CH2— or Het2; Ar1 and Ar2 optionally substituted phenyl; Het1 and Het2 are optionally substituted monocyclic heterocycles; having angiogenesis inhibiting activity; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: October 19, 2001Date of Patent: December 21, 2004Assignee: Janssen Pharmaceutica, NVInventors: Raymond Antoine Stokbroekx, Marc André Ceusters, Marcel Jozef Maria Van der Aa, Marcel Gerebernus Maria Luyckx, Marc Willems, Robert W. Tuman
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Publication number: 20040254370Abstract: A compound of formula (I) 1Type: ApplicationFiled: May 11, 2004Publication date: December 16, 2004Inventors: Hisao Tajima, Yoshisuke Nakayama
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Patent number: 6831175Abstract: Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are compositions which inhibit protein kinases and methods of inhibiting protein kinases in a patient.Type: GrantFiled: December 12, 2002Date of Patent: December 14, 2004Assignee: Abbott LaboratoriesInventors: Qun Li, Keith W. Woods, Gui-Dong Zhu, John P. Fischer, Jianchun Gong, Tongmei Li, Virajkumar Gandhi, Sheela A. Thomas, Garrick K. Packard, Xiaohong Song, Jason N. Abrams, Robert B. Diebold, Jürgen Dinges, Charles W. Hutchins, Vincent S. Stoll, Saul H. Rosenberg, Vincent L. Giranda
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Publication number: 20040248888Abstract: The present invention relates to imidazole derivatives of formula I 1Type: ApplicationFiled: June 2, 2004Publication date: December 9, 2004Inventors: Bernd Buettelmann, Simona Maria Ceccarelli, Georg Jaeschke, Sabine Kolczewski, Richard Hugh Philip Porter, Eric Vieira
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Patent number: 6828337Abstract: This invention relates to new RAR selective retinoid agonists of formula I wherein the symbols are as defined in the specification to their pharmaceutically acceptable salts, individual isomers or to a racemic or non-racemic mixture; to pharmaceutical compositions containing them, and to methods for their use as therapeutic agents.Type: GrantFiled: December 19, 2002Date of Patent: December 7, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Paula Nanette Belloni, Michael Klaus, Jean-Marc Lapierre
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Patent number: 6825217Abstract: Compositions and methods are provided for treating neuropathic pain or neuropathic dysfunction that include the administration of an effective amount of a defined carbinol or a pharmaceutically acceptable salt or prodrug thereof.Type: GrantFiled: October 16, 2002Date of Patent: November 30, 2004Assignee: Endo Pharmaceuticals, Inc.Inventors: Richard Carliss, David A. H. Lee
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Patent number: 6825204Abstract: N-substituted 3-hydroxy-4-pyridinones and metal chelates, methods of preparing N-substituted 3-hydroxy-4-pyridinones and metal chelates, and pharmaceutical compositions containing new N-substituted 3-hydroxy-4-pyridinones and/or their metal chelates. Use of N-substituted 3-hydroxy-4-pyridinones and their metal chelates as pharmaceutical agents for the treatment of diseases, such as parasitic and viral infections, conditions associated with inflammation and infection, and conditions mediated by cell-proliferation or collagen formation.Type: GrantFiled: February 5, 2003Date of Patent: November 30, 2004Assignee: Bristol-Myers Squibb CompanyInventor: Shuang Liu
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Patent number: 6822093Abstract: Disclosed are novel 2-(5-halopyridyl) and 2-(5-halopyrimidinyl) magnesium halides, processes of making and their use in the efficient synthesis in their respective 5-halo-2-substituted pyridines and pyrimidines.Type: GrantFiled: December 6, 2002Date of Patent: November 23, 2004Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Jinhua J. Song, Nathan K. Yee
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Patent number: 6818658Abstract: Certain novel 4-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: GrantFiled: February 3, 2003Date of Patent: November 16, 2004Assignee: Merck & Co., Inc.Inventors: Feroze Ujjainwalla, Lin Chu, Mark T. Goulet, Bonnie Louridas, Matthew J. Wyvratt, Daniel Warner
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Publication number: 20040224959Abstract: Disclosed are compounds represented by formula (I) which have triglyceride biosynthesis inhibitory activity in the liver and inhibitory activity against the secretion of apolipoprotein B-containing lipoprotein from the liver and particularly have excellent inhibitory activity against the secretion of apolipoprotein B-containing lipoprotein, are free from side effect of accumulation of lipids in the liver, and are useful for the treatment and prevention of hyperlipidemia and arteriosclerotic diseases.Type: ApplicationFiled: June 16, 2004Publication date: November 11, 2004Inventors: Naoto Ohkura, Yukiko Hiraiwa, Tetsuya Matsushima, Kazue Sasaki, Takehiro Yamamoto, Masaharu Shiotani, Shigeki Suzuki, Yuuko Nakatani, Chizuko Kuroda, Mieko Nagasawa, Kiyoaki Katano
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Patent number: 6812235Abstract: A beta-alanine derivative of the formula (I) wherein R1 is hydrogen atom or an amino protective group; A is a lower alkylene group or a lower alkenylene group; R2 is hydrogen atom or an amino group which may be substituted with an acyl group; R3 is hydrogen atom or an aryl or aralkyl group which may be substituted with one or more of hydroxy and/or lower alkoxy, a moiety represented by the formula (II), which is a bivalent N-containing 6- to 8-membered heterocyclic group, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: August 2, 2002Date of Patent: November 2, 2004Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Mitsuru Ohkubo, Satoru Kuroda, Hideko Nakamura, Masatoshi Minagawa, Toshiaki Aoki, Kayoko Harada, Jiro Seki
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Patent number: 6809093Abstract: Compounds, compositions, and methods for treating multidrug resistance are disclosed. Suitable compounds are 2-substituted heterocyclic compounds.Type: GrantFiled: December 19, 2000Date of Patent: October 26, 2004Assignee: H. Lee Moffitt Cancer & Research Institute, Inc.Inventors: Charles Raymond Degenhardt, David Joseph Eickhoff
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Patent number: 6803468Abstract: The present invention relates to an improved and industrially advantageous process for the preparation of N-(5-methylnicotinoyl)-4-hydroxypiperidine of Formula I, as shown in the accompanied drawings. This compound is a key intermediate for the synthesis of rupatadine, a potent dual antagonist of histamine and platelet-activating factor (PAF).Type: GrantFiled: June 20, 2003Date of Patent: October 12, 2004Assignee: Ranbaxy Laboratories LimitedInventors: Yatendra Kumar, Mohan Prasad, Shallendra Kumar Singh
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Publication number: 20040176386Abstract: Compounds of the formula I 1Type: ApplicationFiled: February 26, 2004Publication date: September 9, 2004Applicant: AstraZeneca ABInventors: Christophe B. Barlaam, Robert I. Dowell, Maurice R.V. Finlay, Nicholas J. Newcombe, Howard Tucker, David Waterson
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Patent number: 6787522Abstract: Compounds of formula (I) are antibacterials: wherein: R1 represents hydrogen, or C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms; R2 represents a group R10—(X)n—(ALK)m— wherein R10 represents hydrogen, or a C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, cycloalkyl, aryl, or heterocyclyl group, any of which may be unsubstituted or substituted by (C1-C6)alkyl, (C1-C6)alkoxy, hydroxy, mercapto, (C1-C6)alkylthio, amino, halo (including fluoro, chloro, bromo and iodo), trifluoromethyl, cyano, nitro, —COOH, —CONH2, —COORA, —NHCORA, —CONHRA, —NHRA, —NRARB, or —CONRARB wherein RA and RB are independently a (C1-C6)alkyl group, and ALK represents a straight or branched divalent C1-C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radical, and may be interrupted by one or more non-adjacent —NH—, —O— or —S— linkages, X represents —NH—, —O— or —S—, anType: GrantFiled: April 30, 2002Date of Patent: September 7, 2004Assignee: British Biotech PharmaceuticalsInventors: Michael George Hunter, Raymond Paul Beckett, John Martin Clements, Mark Whittaker, Stephen John Davies, Lisa Marie Pratt, Zoe Marie Spavold, Steven Launchbury
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Patent number: 6787559Abstract: This invention relates to certain sulfonamide derivatives that are inhibitors of procollagen C-proteinase, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: GrantFiled: October 9, 2002Date of Patent: September 7, 2004Assignee: Syntex (U.S.A.) LLC.Inventors: Roland Joseph Billledeau, Chris Allen Broka, Jeffrey Allen Campbell, Jian Jeffrey Chen, Sharon Marie Dankwardt, Nancy Delaet, Leslie Ann Robinson, Keith Adrian Murray Walker
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Patent number: 6784191Abstract: A benzamidine derivative of the following formula, analogs thereof and pharmaceutically acceptable salts thereof have an effect of inhibiting the blood coagulation based on their excellent effect of inhibiting activated blood-coagulation factor X. Thus, a blood-coagulation inhibitor or an agent for preventing or treating thrombosis or embolism, containing one of those compounds as the active ingredient, is provided.Type: GrantFiled: June 10, 2002Date of Patent: August 31, 2004Assignee: Ajinomoto Co., Inc.Inventors: Kaoru Yoshida, Tadakiyo Nakagawa, Takashi Kayahara
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Patent number: 6784182Abstract: Compounds of formula (I) in which R2, X, Y, Cy, L and Lp(D)n have the meanings given in the specification, are inhibitors of the serine protease, factor Xa and are useful in the treatment of cardiovascular disorders.Type: GrantFiled: February 4, 2002Date of Patent: August 31, 2004Assignee: Eli Lilly and CompanyInventors: John Walter Liebeschuetz, Christopher William Murray, Stephen Clinton Young, Nicholas Paul Camp, Stuart Donald Jones, William Alexander Wylie, John Joseph Masters, Michael Robert Wiley, Scott Martin Sheehan, David Birenbaum Engel, Brian Morgan Watson
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Patent number: 6784192Abstract: The present invention provides a novel compound having a superior Na+ channel inhibitory activity. Namely, it provides a compound represented by the following formula (I), a salt thereof or a hydrate of them. In the formula, the ring A represents a ring represented by the formula: (wherein R1 represents a hydrogen atom etc.; and R2 represents indicates a hydrogen atom and the like) etc.; W represents an optionally substituted C1-6 alkylene group etc.; Z represents an optionally substituted C6-14 aromatic hydrocarbon cyclic group etc.; and l represents an integer from 0 to 6.Type: GrantFiled: July 19, 2002Date of Patent: August 31, 2004Assignee: Eisai Co., Ltd.Inventors: Fumihiro Ozaki, Toshihiko Kaneko, Mutsuko Tabata, Yoshinori Takahashi, Kazuki Miyazaki, Junichi Kamata, Ichiro Yoshida, Masayuki Matsukura, Hiroyuki Suzuki, Takashi Yoshinaga, Hiroki Ishihara, Hiroshi Katoh, Kohei Sawada, Tatsuhiro Onogi, Kiyoaki Kobayashi, Miyuki Ohkubo
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Patent number: 6770661Abstract: This invention relates to aryl substituted pyridines of Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Ar and R1-R4 are set in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, including diabetic neuropathy, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, and as antiarrhythmics.Type: GrantFiled: September 6, 2002Date of Patent: August 3, 2004Assignee: Euro-Celtique S.A.Inventors: Bin Shao, R. Richard Goehring
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Publication number: 20040127706Abstract: Compounds of Formula I have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4 and are useful for treating disease whose symptoms and or damage are related to the binding of VCAM-1 to cells expressing VLA-4.Type: ApplicationFiled: September 24, 2003Publication date: July 1, 2004Inventors: Gerald Lewis Kaplan, Achyutharao Sidduri, Jefferson Wright Tilley
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Publication number: 20040127517Abstract: The present invention relates to compounds of formula (I): 1Type: ApplicationFiled: October 20, 2003Publication date: July 1, 2004Inventors: Marco Baroni, Bernard Bourrie, Pierre Casellas
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Patent number: 6756386Abstract: The present invention relates to novel pyridylether derivatives which are cholinergic ligands at nicotinic Ach receptors. The compounds of the invention are useful for the treatment of conditions, disorders, or diseases involving the cholinergic system of the central nervous system, pain, inflammatory diseases, diseases caused by smooth muscle contractions and as assistance in the cessation of chemical substance abuse.Type: GrantFiled: April 14, 2000Date of Patent: June 29, 2004Assignee: NeuroSearch A/SInventors: Dan Peters, Gunnar M. Olsen, Simon F. Nielsen, Elsebet Østergaard Nielsen
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Publication number: 20040121997Abstract: A hydroxyformamidine compound represented by the following formula or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 24, 2003Publication date: June 24, 2004Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Matsunaga, Hideaki Amada
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Publication number: 20040121994Abstract: Compounds of formula (I) 1Type: ApplicationFiled: December 20, 2002Publication date: June 24, 2004Inventors: Steven N. Anderson, Pramila Bhatia, Teodozyj Kolasa, Masaki Nakane, Meena V. Patel, Jeffrey J. Rohde, Zhiren Xia, Henry Q. Zhang
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Patent number: 6753337Abstract: Compounds of the formula: useful in the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.Type: GrantFiled: December 21, 2001Date of Patent: June 22, 2004Assignee: Wyeth Holdings CorporationInventors: Jeremy I. Levin, Aranapakam M. Venkatesan, James M. Chen, Arie Zask, Vincent P. Sandanayaka, Mila T. Du, Jannie L. Baker
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Patent number: 6750228Abstract: A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9 and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor.Type: GrantFiled: May 12, 2000Date of Patent: June 15, 2004Assignee: Pharmacia CorporationInventors: Thomas E Barta, Daniel P Becker, Louis J Bedell, Terri L Boehm, Jeffrey N Carroll, Gary A DeCrescenzo, Yvette M Fobian, John N Freskos, Daniel P Getman, Joseph J McDonald, Madeleine H Li, Susan L Hockerman, Susan C Howard, Steve A Kolodziej, Deborah A Mischke, Joseph G Rico, Nathan W Stehle, Michael B Tollefson, William F Vernier, Clara I Villamil
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Publication number: 20040110952Abstract: The invention provides a compound of formula (1): wherein R1, R2, R3, R3a, R4, R4a, R5, and R6 are defined; or a pharmaceutically acceptable salt thereof or a solvate thereof; compositions containing these compounds, processes for preparing them and their use as modulators of chemokine activity (especially CCR5 activity).Type: ApplicationFiled: August 26, 2003Publication date: June 10, 2004Inventors: Jeremy Burrows, John Cumming, Howard Tucker
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Patent number: 6747037Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; wherein X, Y, Z, D and R3 are as defined in the specification.Type: GrantFiled: June 6, 2003Date of Patent: June 8, 2004Assignee: Allergan, Inc.Inventors: David W. Old, Thang D. Dinh
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Patent number: 6747028Abstract: This invention concerns compounds of formula (I) prodrugs, addition salts, or stereochemically isomeric forms thereof for use as, inter alia, respiratory syncytial virus replication inhibitors; their preparation, compositions containing them and methods of their use in treating respiratory syncytial viral infections.Type: GrantFiled: December 27, 2001Date of Patent: June 8, 2004Assignee: Hanssen Pharmaceutica, N.V.Inventors: Frans Eduard Janssens, Kathleen Petrus Marie-José Meersman, François Maria Sommen, Koenraad Jozef Lodewijk Marcel Andries
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Patent number: 6743808Abstract: 4-Aryl-1-(indanmethyl, dihydrobenzofuranmethyl or dihydrobenzothiophenemethyl)piperidine, -tetrahydropyridine or -piperazine compounds of general formula (I), wherein one of X and Y is CH2 and the other one is CH2, O or S; Z is N, C, CH or COH; Ar is an optionally substituted aryl group; R1 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, acyl, thioacyl, alkylsulfonyl, trifluoromethylsulfonyl, arylsulfonyl, a group R9VCO— where V is O or S and R9 is alkyl or aryl, or a group R10R11NCO— or R10R11NCS— wherein R10 and R11 are hydrogen, alkyl or aryl, or R10 and R11 are linked to form a ring; R2 is hydrogen, alkyl, cycloalkyl or cycloalkylalkyl or R1 and R2 are linked to form a ring; R3-R5 are hydrogen, halogen, alkyl, alkylcarbonyl, phenylcarbonyl, alkoxy, alkylthio, hydroxy, alkylsulfonyl, cyano, trifluoromethyl, cycloalkyl, cycloalkylalkyl or nitro; R6 and R7 are hydrogen or alkyl or they are linked to constitute 3-7-membered ring; R8 is hydrogen or alkyl; hType: GrantFiled: April 14, 2000Date of Patent: June 1, 2004Assignee: H. Lundbeck A/SInventors: Jens Kristian Perregaard, John Willie Stenberg, Bitten Hansen
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Publication number: 20040102432Abstract: The invention provides compounds of formula (I): as modulators of chemokine and H1 receptor activity. The compounds are especially useful in the treatment of asthma and rhinitis.Type: ApplicationFiled: February 13, 2003Publication date: May 27, 2004Inventors: Hitesh Sanganee, Brian Springthorpe
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Publication number: 20040102450Abstract: This invention is directed to oxoazaheterocycyl compounds which inhibit Factor Xa, to oxoazaheterocycyl compounds which inhibit both Factor Xa and Factor IIa, to pharmaceutical compositions comprising these compounds, to intermediates useful for preparing these compounds, to a method of directly inhibiting Factor Xa and to a method of simultaneously directly inhibiting Factor Xa and Factor IIa..Type: ApplicationFiled: July 25, 2003Publication date: May 27, 2004Applicant: AVENTIS PHARMACEUTICALS INC.Inventors: William R. Ewing, Michael R. Becker, Yong Mi Choi-Sledeski, Heinz W. Pauls, Wei He, Stephen M. Condon, Roderick S. Davis, Barbara A. Hanney, Alfred P. Spada, Christopher J. Burns, John Z. Jiang, Aiwen Li, Michael R. Myers, Wan F. Lau, Gregory B. Poli, Mark A. Bobko, Robert L. Morris, Joseph M. Karpinski, Timothy F. Gallagher, Kent W. Neuenschwander, Robert D. Groneberg, Jean-Francois Sabuco
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Publication number: 20040097425Abstract: The present invention relates to a compound of the formula (I)wherein R1 is benzofuranyl substituted by halogen, or styryl substituted by halogen; R2 is substituted hydroxy, substituted mercapto or substituted sulfonyl; and X is or pharmaceutically acceptable salts thereof. The compound (1) of the present invention and pharmaceutically acceptable salts thereof possess a strong inhibitory activity on the production of nitric oxide (NO), and are useful for prevention and/or treatment of NO-mediated diseases in human being and animals.Type: ApplicationFiled: December 23, 2003Publication date: May 20, 2004Inventors: Ichiro Shima, Takehiko Ohkawa, Kentaro Sato, Naoki Ishibashi, Kenichiro Imamura
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Publication number: 20040097499Abstract: The present invention provides certain amide, carbamate and urea derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.Type: ApplicationFiled: July 3, 2003Publication date: May 20, 2004Inventors: MacKlin Brian Arnold, David Michael Bender, Thomas John Bleisch, Winton Dennis Jones, Paul Leslie Ornstein, Hamid H. Zarrinmayeh, Dennis Michael Zimmerman
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Publication number: 20040097546Abstract: Certain novel 4-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: ApplicationFiled: August 19, 2003Publication date: May 20, 2004Inventors: Mark T. Goulet, Ravi P. Nargund, Iyassu K. Sebhat, Feroze Ujjainwalla, Thomas F. Walsh, Daniel Warner, Zhixiong Ye, Jonathan R. Young, Raman K. Bakshi
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Publication number: 20040097551Abstract: Compounds of formula (I): 1Type: ApplicationFiled: July 11, 2003Publication date: May 20, 2004Inventors: Terence D. Butters, Raymond A. Dwek, George WJ Fleet, Michael Glen Orchard, Frances Mary Platt
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Publication number: 20040092501Abstract: Certain novel 4-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: ApplicationFiled: August 19, 2003Publication date: May 13, 2004Inventors: Mark T. Goulet, Ravi P. Nargund, Feroze Ujjainwalla, Thomas F. Walsh, Daniel Warner
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Patent number: 6734179Abstract: The present invention relates to compounds of the formula wherein R1 and R2 are as described within. The compounds of formula I have been found to be adenosine receptor ligands. Specifically, the compounds of the present invention have a good affinity to the A2A-receptor and they may be used in the treatment of diseases, related to this receptor.Type: GrantFiled: December 2, 2002Date of Patent: May 11, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Flohr, Roland Jakob-Roetne, Roger David Norcross, Claus Riemer
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Patent number: 6730677Abstract: Compounds of general structural formula (1) are shown to have AMPA receptor enhancing properties. The compounds are useful for such therapeutic purposes as facilitating the learning of behaviors dependent upon AMPA receptors, and in treating conditions, such as memory impairment, in which AMPA receptors, or synapses utilizing these receptors, are reduced in numbers or efficiency. They may also be used to enhance excitatory synaptic activity in order to restore an imbalance between brain subregions, as in treatment of schizophrenia or schizophreniform behavior.Type: GrantFiled: April 27, 2001Date of Patent: May 4, 2004Assignee: The Regents of the University of CaliforniaInventors: Gary A. Rogers, Christopher M. Marrs
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Publication number: 20040082569Abstract: An amide of the formula I 1Type: ApplicationFiled: October 20, 2003Publication date: April 29, 2004Applicant: Abbott GmbH & Co., KGInventors: Wilfried Lubisch, Achim Moller, Hans-Jorg Treiber, Monika Knopp