Chalcogen Bonded Directly To Ring Carbon Of The Piperidine Ring Patents (Class 514/327)
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Patent number: 6570018Abstract: The present invention is directed to a novel process for the preparation of the mesylate trihydrate of the compound of formula (I), (1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidin-1-yl)-1-propanol: The present invention is further directed to a process for the preparation of a (2S)-(+)-compound of formula (II): wherein R1 is a protecting group. In addition, the present invention relates to intermediates useful in said processes.Type: GrantFiled: April 23, 2001Date of Patent: May 27, 2003Assignee: Pfizer IncInventors: Stanley Walter Walinsky, Terry Gene Sinay, Jr., Joseph Philip Rainville
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Patent number: 6566389Abstract: A method for treating or preventing symptoms of tardive dyskensia comprises administering melatonin to patient exhibiting or liable to develop such symptoms. The melatonin is administered in an amount effective to ameliorate or prevent symptoms of tardive dyskensia developing in the patient.Type: GrantFiled: November 26, 2001Date of Patent: May 20, 2003Assignee: Neurim Pharmaceuticals (1991) Ltd.Inventors: Nava Zisapel, Moshe Laudon
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Publication number: 20030092694Abstract: The invention relates to compounds of the general formula (I): 1Type: ApplicationFiled: October 11, 2002Publication date: May 15, 2003Applicant: Biovitrum, AB, a Stockholm, Sweden corporationInventors: Bjorn Nilsson, Jan Tejbrant, Benjamin Pelcman, Erik Ringberg, Markus Thor, Jonas Nilsson, Mattias Jonsson
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Publication number: 20030092734Abstract: Potent inhibitors of fatty acid amide hydrolase (FAAH) are constructed having K1's below 200 pM and activities 102-103 times more potent than the corresponding trifluoromethyl ketones. The potent inhibitors combine several features, viz.: 1.) an &agr;a-keto heterocylic head group; 2.) a hydrocarbon linkage unit employing an optimal C12-C8 chain length; and 3.) a phenyl or other &pgr;-unsaturation corresponding to the arachidonyl &Dgr;8,9/&Dgr;11,12 and/or oleyl &Dgr;9,10 positions. A preferred &agr;-keto heterocylic head group is &agr;-keto N4 oxazolopyridine, with incorporation of a second weakly basic nitrogen. Fatty acid amide hydrolase is an enzyme responsible for the degradation of oleamide (an endogenous sleep-inducing lipid) and anandamide (an endogenous ligand for cannabinoid receptors).Type: ApplicationFiled: October 8, 2002Publication date: May 15, 2003Applicant: The Scripps Research InstituteInventor: Dale L. Boger
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Publication number: 20030086916Abstract: Premature vascular senescence is reversed or prevented in tissue or cells by contacting the tissue or cells with a peroxynitrite scavenger or peroxynitrite formation inhibitor that does not diminish nitric oxide synthesis. This finds application in treatment of patients with a disorder associated with elevated levels of advanced glycation end products in blood or tissue, e.g., patients with end stage renal disease or poorly controlled diabetes, and in contacting vascular tissue or cells ex vivo to prevent occurrence of premature senescence.Type: ApplicationFiled: October 11, 2002Publication date: May 8, 2003Inventors: Michael S. Goligorsky, Jun Chen
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Patent number: 6559166Abstract: A class of phenylsulphonyl derivatives wherein the sulphonyl moiety is also attached to an N-arylalkyl-substituted azetidine, pyrrolidine or piperidine ring are selective antagonists of the human 5-HT2A receptor and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of adverse conditions of the central nervous system, including schizophrenia and depression.Type: GrantFiled: September 27, 2001Date of Patent: May 6, 2003Assignee: Merck Sharp & Dohme Ltd.Inventors: Peter Blurton, Frank Burkamp, Susan Koon-Fung Cheng, Stephen Robert Fletcher, Angus Murray MacLeod, Daniel Spinks, Monique Bodil Van Niel
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Patent number: 6559165Abstract: Methods for the prevention, treatment, or management of apnea, apnea disorders, bulimia nervosa, irritable bowel syndrome, urinary incontinence, bradycardia, bradyarrhythmia, syncope, other disorders, or symptoms thereof using (−) norcisapride, or a pharmaceutically acceptable salt thereof, substantially free of its (+) stereoisomer.Type: GrantFiled: November 28, 2000Date of Patent: May 6, 2003Assignee: Sepracor, Inc.Inventors: Paul D. Rubin, Timothy J. Barberich
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Patent number: 6555556Abstract: Benzamidine derivatives of formula (I) or pharmaceutically acceptable salts thereof exhibit excellent inhibitory activity against factor Xa and are useful for treating or preventing blood coagulation disorders: wherein R1 represents a hydrogen atom, a halogen atom, an alkyl group or a hydroxyl group; R2 represents a hydrogen atom, a halogen atom or an alkyl group, R3 represents a hydrogen atom, an optionally substituted alkyl group, an aralkyl group, an optionally substituted alkanoyl group or an optionally substituted alkylsulfonyl group, R4 and R5 are the same as or different from each other and each represent a hydrogen atom, a halogen atom, an optionally substituted alkyl group, an alkoxy group, a carboxyl group, an alkoxycarbonyl group or an optionally substituted carbamoyl group, and R6 represents a substituted pyrrolidine group or substituted piperidine group.Type: GrantFiled: April 25, 2002Date of Patent: April 29, 2003Assignee: Sankyo Company, LimitedInventors: Koichi Fujimoto, Fumitoshi Asai, Hayao Matsuhashi
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Patent number: 6555541Abstract: The invention provides substituted phenyl compounds of general formula wherein R1, T, U and Ar are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.Type: GrantFiled: July 10, 2000Date of Patent: April 29, 2003Assignee: Astrazeneca UK LimitedInventors: Mark Furber, Timothy J Luker, Michael P Mortimore, Philip Thorne, Premji Meghani
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Publication number: 20030078253Abstract: The present invention provides a compound represented by Formula: 1Type: ApplicationFiled: June 3, 2002Publication date: April 24, 2003Inventors: Toshiro Yamashita, Hiroshi Nara, Masayuki Takizawa, Koji Yoshimura
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Publication number: 20030078283Abstract: This invention relates to lactam and thiolactam derivatives having useful anesthetic and conscious sedation activity. Particularly useful compounds include the diethyl lactams such as 3,3-diethyl-2-pyrrolidinone. Methods for using these compounds and pharmaceutical compositions containing these compounds are provided.Type: ApplicationFiled: July 16, 2001Publication date: April 24, 2003Inventors: James A. Ferrendelli, Douglas F. Covey
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Publication number: 20030078259Abstract: There is provided di-substituted iminoheterocyclic compounds of the following formula (I): 1Type: ApplicationFiled: November 20, 2001Publication date: April 24, 2003Inventors: Masahiro Imoto, Tatsuya Iwanami, Minako Akabane, Yoshihiro Tani
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Patent number: 6552225Abstract: A compound of formula (I) wherein: R1, R2, R3, R4, R5, R6 and R7 are as defined within; or a pharmaceutically acceptable salt or an in vivo hydrolysable ester thereof is described. The use of compounds of formula (I) in the production of an elevation of PDH activity in a warm-blooded animal such as a human being are also described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are detailed.Type: GrantFiled: June 17, 2002Date of Patent: April 22, 2003Assignee: AstraZeneca ABInventors: Roger John Butlin, Janet Elizabeth Pease, Michael Howard Block, Thorsten Nowak, Jeremy Nicholas Burrows
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Patent number: 6552045Abstract: The invention relates to methods and compositions for the prevention, treatment, or management of gastrointestinal disorders or symptoms thereof, employing two or more agents or compounds to provide a triple site action on 5-HT3 receptors, 5-HT4 receptors, and at least one of H2 receptors and proton pumps.Type: GrantFiled: January 10, 2002Date of Patent: April 22, 2003Assignee: Sepracor Inc.Inventors: Paul D. Rubin, Timothy J. Barberich
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Patent number: 6552041Abstract: The present invention relates to cyclized amide derivatives of formula (I) These cyclized amide derivatives are useful for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.Type: GrantFiled: January 3, 2002Date of Patent: April 22, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Lauffer, Michael Mullican, Brian Ledford
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Patent number: 6548518Abstract: The invention relates to methods and compositions for the prevention, treatment, or management of gastrointestinal disorders or symptoms thereof, employing two or more agents or compounds to provide a triple site action on 5-HT3 receptors, 5-HT4 receptors, and at least one of H2 receptors and protons pumps.Type: GrantFiled: January 10, 2002Date of Patent: April 15, 2003Assignee: Sepracor, Inc.Inventors: Paul D. Rubin, Timothy J. Barberich
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Patent number: 6541488Abstract: The invention relates to the use of direct or indirect selective inhibitors of factor Xa acting via antithrombin III, alone or in combination with one or more compounds with anti-platelet aggregation activity, for the preparation of medicines intended to prevent and to treat thromboembolic arterial diseases. The subject of the invention is also pharmaceutical compositions containing one or more direct or indirect selective inhibitors of factor Xa which act via antithrombin III in combination with one or more compounds with anti-platelet aggregation activity, and optionally one or more pharmaceutically acceptable vehicles.Type: GrantFiled: February 11, 2000Date of Patent: April 1, 2003Assignees: Sanofi-Synthelabo, Akzo NobelInventors: André Bernat, Jean Marc Herbert, Maurice Petitou, Ronald Van Amsterdam
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Patent number: 6528531Abstract: Trisubstituted pyrroles are antiprotozoal agents useful in the treatment and prevention of protozoal diseases in human and animals, including the control of coccidiosis in poultry.Type: GrantFiled: November 10, 2000Date of Patent: March 4, 2003Assignee: Merck & Co., Inc.Inventors: Tesfaye Bitfu, Danqing D. Feng, Gui-Bai Liang, Mitree M. Ponpipom, Xiaoxia Qian, Michael H. Fisher, Matthew J. Wyvratt, Robert L. Bugianesi
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Patent number: 6525069Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: June 21, 2000Date of Patent: February 25, 2003Assignee: Bristol-Myers Squibb Pharma Co.Inventors: Soo S. Ko, George V. Delucca, John V. Duncia, Ui Tae Kim, Dean A. Wacker, Changsheng Zheng
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Patent number: 6521640Abstract: The present invention provides a new of sulfasalazine as a potent agent for the treatment of neuronal death.Type: GrantFiled: April 21, 2000Date of Patent: February 18, 2003Assignee: Neurotech Co., Ltd.Inventors: Byoung Joo Gwag, Young Ae Lee, Bo Rum Ryu
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Patent number: 6518286Abstract: The invention provides compounds of general formula (I) wherein: R1 represents optionally substituted, C1-C12 alkyl or optionally substituted 3- to 10-membered saturated or unsaturated ring system comprising up to two ring carbon atoms that form carbonyl groups and comprising up to 4 ring heteroatoms independently selected from nitrogen, oxygen and sulfur; m is 0-1; Q represents OCH2, C1-C4 alkylene or C2-C4 alkenylene; T represents C(O)NH, or when m is 0, T may additionally represent a bond or NH, or when m is 1 and Q represents C1-C4 alkylene, T may additionally represent NH; n is 1-4; each R2 and R3 independently represents H or C1-C4 alkyl; V represents N, and W represents N or CH; X represents O, C(O), CH(OH), SO2, NH or N(C1-C6 alkyl), provided that when W represents N, then X represents either C(O) or SO2 and when W represents CH, then X is other than SO2; R4 represents optionally substituted phenyl; R5 and R6 each independently represent H, C1-C6 alkyl or hydroxyC1-C6 alkyl, or R5 and R6 together withType: GrantFiled: June 1, 2000Date of Patent: February 11, 2003Assignee: AstraZeneca ABInventors: Andrew Baxter, Stephen Brough, Nicholas Kindon, Thomas McInally, Bryan Roberts, Stephen Thom
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Patent number: 6518310Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present 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, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: March 16, 2001Date of Patent: February 11, 2003Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L Fedde, Carl R Illig, Thomas P. Markotan, Thomas P Stagnaro
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Patent number: 6509003Abstract: The present invention relates to N-alkylpiperidine derivatives represented by general formula (1) or (2); wherein R1 represents optionally fluorinated lower alkyl; R2 represents lower alkyl; and R3 represents alkenyl substituted at the 1-position with hydroxy, lower alkoxy, lower alkoxyalkyloxy, lower alkoxyalkyloxyalkyloxy, or lower alkanoyloxy and substituted at the end with radioactive iodine, or alkenyloxymethyl substituted at the end with a radioactive iodine reagent containing the same for assaying central local AchE activity; a method for assaying the central local AchE activity; and labeled precursors of the above compounds. After easily passing through the blood-brain barrier, these compounds are hydrolyzed specifically by AchE in the brain into alcohols, which are then captured by the brain. In contrast, alcohols formed outside the brain do not migrate into the brain. The compounds of the invention emit &ggr;-rays at an appropriate energy level.Type: GrantFiled: January 19, 2001Date of Patent: January 21, 2003Assignees: Daiichi Pure Chemicals Co., Ltd., Daiichi Radioisotope Laboratories, Ltd.Inventors: Toshiaki Irie, Kiyoshi Fukushi, Hiroki Namba, Masaomi Iyo, Nobuo Ikota, Shinichiro Nagatsuka, Takao Ueda, Masaru Nishiura, Keizo Takatoku, Isamu Yomoda
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Patent number: 6509359Abstract: A compound having the formula: wherein all variables are as defined in the specification, for use as a neuramninidase inhibitor.Type: GrantFiled: March 17, 2000Date of Patent: January 21, 2003Inventors: Wayne J. Brouillette, Venkatram Reddy Atigadda, Ming Luo, Yarlagadda S. Babu
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Patent number: 6506901Abstract: This invention provides compounds of Formula I having the structure wherein A, B, Z, R and R1 are as defined hereinbefore, or a pharmaceutically acceptable salt thereof, which are useful in treating or inhibiting metabolic disorders related to insulin resistance or hyperglycemia (typically associated with obesity or glucose intolerance), atherosclerosis, gastrointestinal disorders, neurogenetic inflammation, glaucoma, ocular hypertension and frequent urination; and are particularly useful in the treatment or inhibition of type II diabetes.Type: GrantFiled: July 12, 2001Date of Patent: January 14, 2003Assignee: WyethInventors: Robert John Steffan, Mark Anthony Ashwell, Jeffrey Claude Pelletier, William Ronald Solvibile, Edward Martin Matelan
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Patent number: 6506777Abstract: The present invention is directed to compounds of the formula I: (wherein R1, R2, R3, R4, R5, R7, R8, X, n, x and y 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-5 and/or CCR-3.Type: GrantFiled: June 8, 2000Date of Patent: January 14, 2003Assignee: Merck & Co., Inc.Inventors: Paul E. Finke, Jennifer L. Loebach, Malcolm Maccoss, Sander G. Mills
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Patent number: 6503897Abstract: Compounds of formula (I) are antibacterial agents wherein: R3 and R4, taken together with the carbon atoms to which they are respectively attached, form an optionally substituted saturated carbocyclic or heterocyclic ring of 5 to 16 atoms, which may be benz-fused or fused to a second optionally substituted saturated carbocyclic or heterocyclic ring of 5 to 16 atoms; and R1 and R2 are as defined in the specification.Type: GrantFiled: August 22, 2001Date of Patent: January 7, 2003Assignee: British Biotech Pharmaceuticals Ltd.Inventors: Raymond Paul Beckett, Mark Whittaker, Zoe Marie Spavold
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Publication number: 20020188006Abstract: The present invention relates to a compound represented by the following formula (I) or a salt thereof, or a pharmaceutical composition containing the compound as an effective ingredient: 1Type: ApplicationFiled: October 4, 2001Publication date: December 12, 2002Applicant: Mochida Pharmaceutical Co., Ltd.Inventors: Ichiro Yamamoto, Manabu Itoh, Fumiaki Yamasaki, Yutaka Miyazaki, Shinichi Ogawa
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Patent number: 6492395Abstract: A pharmaceutically acceptable topical formulation for the treatment and/or prevention of skin ailments, more particularly of fibriotic nature such as fibriotic lesional tissues, contiguous warts, contact dermatitis, and keloids, and to assist the healing of burns after surgery, comprising as active ingredient a substituted pyridone of the formula: n-(R1)-R2-2-(1H)pyridone or a pharmaceutically acceptable salt or ester thereof, where R1 is selected from methyl, ethyl, propyl, carboxyl and a carboxymethyl or carboxyethyl ester group, R2 is selected from phenyl, methylphenyl, ethylphenyl, propylphenyl, and a carboxyphenyl or carboxyethylphenyl ester group, and n is 3, 4 or 5, together with an excipient, characterized in that the excipient comprises, one or more plasticisers, one or more antioxidants, one or more gel-forming agents and sufficient pH adjusting agent to bring the pH of the formulation to a value from 4 to 8. The preferred active ingredient is 5-methyl-1-phenyl-2-(1H)pyridone (Pirfenidone).Type: GrantFiled: May 23, 2001Date of Patent: December 10, 2002Assignee: Mepha AGInventors: Max Werner Scheiwe, Shitotomo Yamauchi
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Patent number: 6492393Abstract: Disclosed are novel aromatic compounds of the formula (I) wherein G, X, Ar, L and Q are defined herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.Type: GrantFiled: November 16, 2000Date of Patent: December 10, 2002Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Steffen Breitfelder, Pier F. Cirillo, Ming-Hong Hao, Eugene R. Hickey, Rajiv Sharma, Sanxing Sun, Hidenori Takahashi
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Patent number: 6492332Abstract: This invention relates to a method of inhibiting tumor cell adhesion, pain, and inflammation at a wound during a surgical procedure by delivering an irrigation solution containing a tumor cell anti-adhesion agent and a plurality of additional agents to an operative site during the surgical procedure. In addition, methods of inhibiting tumor cell attachment and implantation during a surgical procedure as well as inhibiting tumor metastasis during a surgical procedure are also provided.Type: GrantFiled: September 11, 2000Date of Patent: December 10, 2002Assignee: Omeros CorporationInventors: Gregory A. Demopulos, Pamela Pierce-Palmer, Jeffrey M. Herz, Darrell L. Tanelian
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Patent number: 6492392Abstract: The present invention provides 2-piperidone compounds or pharmaceutically acceptable salts thereof, which have a potent activity of inhibiting the proliferation of tumor cells and thus are useful as medicaments, as well as antitumor agents containing these compounds. The 2-piperidone compound is represented by the following formula (I): wherein R1 represents —(CH2)nR1a {wherein n is an integer of from 0 to 5, and R1a represents amino, lower alkylamino, di(lower alkyl)amino, substituted or unsubstituted aryl, or a substituted or unsubstituted heterocyclic group}, and R2 and R3 independently represent lower alkyl which may be substituted by lower alkoxycarboyl; lower alkenyl, aralkyl or lower alkynyl which may be substituted by substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group; substituted or unsubstituted aryl; or a substituted or unsubstituted heterocyclic group.Type: GrantFiled: January 12, 2000Date of Patent: December 10, 2002Assignees: Kyowa Hakko Kogyo Co., Ltd., Eli Lilly & Co.Inventors: Yutaka Kanda, Rieko Tanaka, Mitsunobu Hara, Jun Eishima, Shiro Akinaga, Tadashi Ashizawa
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Publication number: 20020177588Abstract: 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: ApplicationFiled: September 17, 2001Publication date: November 28, 2002Inventors: Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, Jeffery N. Carroll, Gary A. DeCrescenzo, Yvette M. Fobian, John N. Freskos, Daniel P. Getman, Joseph J. McDonald, Gunnar J. Hanson, Susan L. Hockerman, Susan C. Howard, Steve A. Kolodziej, Hui Li, Deborah A. Mischke, Joseph G. Rico, Nathan W. Stehle, Michael B. Tollefson, William F. Vernier, Clara I. Villamil
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Publication number: 20020173504Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: ApplicationFiled: July 27, 2001Publication date: November 21, 2002Inventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James E. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
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Patent number: 6476054Abstract: The present invention is directed to cyclic amines of the formula I: (wherein R1, R2, R3, 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: October 17, 2000Date of Patent: November 5, 2002Assignee: Merck & Co., Inc.Inventors: Charles G. Caldwell, Paul E. Finke, Malcolm Maccoss, Sander G. Mills, Bryan Oates, Dooseop Kim, Shankaran Kothandaraman, Liping Wang
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Patent number: 6476067Abstract: Compounds of formula (I) are in the preparation of antibacterial agents, wherein: R1 represents hydrogen, C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms; R2 represents a group R10(X)n—(ALK)— wherein R10 represents hydrogen, a C1-C6 alkyl, C2-C6 alkenyl, C1-C6 alkynyl, cycloalkyl, aryl, or heterocyclyl group, any of which may be unsubstituted or substituted by (C1-C6)alkyl, (C1-C6)alkoyy, hydroxy, mercapto, (C1-C6)alkylthio, amino, halo, 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, which may be interrupted by one or more non-adjacent —NH—, —O— or —S— linkages, X represents —NH—, —O— or —S—, and n is 0 or 1, R represents hydrogen or C1-C6Type: GrantFiled: June 14, 2001Date of Patent: November 5, 2002Assignee: British BiotechInventors: Michael George Hunter, Raymond Paul Beckett, Martin John Clements, Mark Whittaker
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Patent number: 6469029Abstract: The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds having Formula I: or pharmaceutically acceptable salts thereof; wherein Q is phenyl, benzyl, pyridyl, thienyl, indolyl, quinolinyl, benzothienyl, biphenylyl, or imidazolyl; any of which can include one or more optional substituents independently selected from halo, trifluoromethyl, hydroxy, amino, nitro, cyano, C1-3 alkoxy, C1-3 alkyl, methylenedioxy, carboxamido, acetamido, or amidino; X is methylene, carbonyl, or sulfonyl; Z is methylene, ethylene, or propylene; M is methylene or ethylene; and R1 R2 and R3 are independently hydrogen or C1-3 alkyl.Type: GrantFiled: September 13, 2000Date of Patent: October 22, 2002Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Scott C. Miller, Juan JosĂ© MarugĂ¡n SĂ¡nchez, Kristin D. Haslow, Jonathan Hall
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Publication number: 20020151538Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: ApplicationFiled: July 27, 2001Publication date: October 17, 2002Inventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, James J. Droste, Steven S. Henry, Stacey L. McDaniel, Russell D. Stucky, Warren J. Porter
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Patent number: 6465487Abstract: Methods for inhibiting morphogenesis of host cell membrane-budding viruses and infections caused thereby using compounds that inhibit host cell glucosidase or glucosyltransferase enzymes. Methods for treating lipid storage diseases using compounds that inhibit glucosyl transferance enzymes.Type: GrantFiled: December 10, 1998Date of Patent: October 15, 2002Assignees: Synergy Pharmaceuticals, Inc., Thomas Jefferson University, The Chancellor, Masters and Scholars of the University of OxfordInventors: Timothy M. Block, Raymond A. Dwek, Baruch S. Blumberg, Anand Mehta, Frances Platt, Terry D. Butters, Nicole Zitzmann
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Patent number: 6458806Abstract: Aryl alkenamides derivatives of Formula I or a pharmaceutically acceptable salt thereof are novel MCP-1 antagonists and are thus useful in the treatment of inflammation, atherosclerosis, restenosis, and immune disorders such as arthritis and transplant rejection where V═O,S, NH or a bond; Ar can be unsubstituted or substituted benzimidazole, phenyl, biphenyl, pyridyl, naphthyl, quinoline or isoquinoline. The other meanings for the terms are recited in the specification below.Type: GrantFiled: August 12, 1997Date of Patent: October 1, 2002Assignee: Millennium Pharmaceuticals, Inc.Inventors: Richard John Booth, Kenneth Gordon Carson, David Thomas Connor, Roberta Ellen Glynn, Bruce David Roth, Charles F. Schwender, Bharat Kalidas Trivedi, Paul Charles Unangst
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Patent number: 6458843Abstract: This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is oxygen or sulfur; R1, R21, R22 and R23 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; or R22 and R23, together with the N, form a heterocycle; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR24, CR25R26, C(O), NR24C(O), C(O)NR24, SO, SO2 or a covalent bond; where R24, R25 and R26 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl.Type: GrantFiled: October 21, 1999Date of Patent: October 1, 2002Assignee: Euro-Celtique S.A.Inventors: Yan Wang, Sui Xiong Cai, Nancy C. Lan, John F. W. Keana, Victor I. Ilyin, Eckard Weber
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Publication number: 20020137738Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: ApplicationFiled: July 27, 2001Publication date: September 26, 2002Inventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James E. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
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Publication number: 20020137737Abstract: This invention relates to novel lactams having the Formula (I): 1Type: ApplicationFiled: June 1, 2001Publication date: September 26, 2002Inventor: Richard E. Olson
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Patent number: 6455549Abstract: A pharmaceutical composition, especially a pharmaceutical composition for the alleviation or treatment of symptoms due to ischemic diseases and symptoms derived from seizures, epilepsy, and migraine, and a Ca2+ overload suppressant, containing an arylpiperidinol or arylpiperidine derivative having the formula (I): wherein, R is H, an optionally substituted phenyl, an optionally substituted phenoxy, or an optionally substituted benzoyl, A is a connecting bond, a cycloalkylene, or an alkenylene optionally substituted with a lower alkyl, B is an alkylene optionally substituted with OH or an alkoxy or —NHCO(CH2)n— where n is an integer of 1 to 5, E is a connecting bond, O, or a methylene, X is OH or H provided that when E is O or a methylene, X is not H, and Y and Z are independently H, a halogen, an alkoxy, or an alkyl optionally substituted with a halogen.Type: GrantFiled: March 20, 1998Date of Patent: September 24, 2002Assignee: Suntory LimitedInventors: Hirokazu Annoura, Kyoko Nakanishi, Shigeki Tamura
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Patent number: 6455531Abstract: Compounds having therapeutic utility are of the formula wherein NB2 is heterocycloalkyl and R1 and R2 are each various substituents or a cyclic group.Type: GrantFiled: March 28, 2001Date of Patent: September 24, 2002Assignee: Darwin Discovery, Ltd.Inventors: David Alan Owen, Andrew Douglas Baxter, Robert John Watson, Duncan Robert Hannah, John Gary Montana
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Publication number: 20020123492Abstract: The present invention relates beta-amino acid derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.Type: ApplicationFiled: January 3, 2002Publication date: September 5, 2002Inventors: David Lauffer, Michael Mullican
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Patent number: 6444686Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: December 17, 1999Date of Patent: September 3, 2002Assignee: Brsitol-Myers Squibb Pharma CompanyInventors: Soo S. Ko, George V. DeLucca, John V. Duncia, Ui Tae Kim, Joseph B. Santella, III, Dean A. Wacker
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Patent number: 6440999Abstract: An intimal thickening inhibitory agent comprising, as an active ingredient, a compound represented by formula (1): wherein x represents an oxygen atom or a group of formula (2) —S—(O)n (2) wherein n represents an integer of from 0 to 2, R1 represents a hydrogen atom or an acyl group; R2 represents a hydrogen atom, a lower alkyl group or a lower alkenyl group; R3 represents a lower alkyl group; and R4, R5, and R6, which may be the same or different, each represent a hydrogen atom or a substituted or unsubstituted alkyl group; or R3 and R4 may be taken together to form a 5-membered ring; or R5 and R6 may be taken together to form a cycloalkyl group; provided that R6 is nil when R3 and R4 are taken together to form benzofuran or benzo[b]thiophene.Type: GrantFiled: August 14, 2000Date of Patent: August 27, 2002Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Osamu Cynshi, Reiko Sekimori, Yoshiaki Kato
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Publication number: 20020115667Abstract: Methods for treatment of disorders associated with glycolipid accumulation, such as Niemann-Pick Type C (NPC) disease, comprising administering a therapeutically effective amount of an inhibitor of glucosylceramide synthesis. Inhibitors of glucosylceramide synthesis include N-butyldeoxynojirimycin, N-butyldeoxygalactonojirimycin, and N-nonyldeoxynojirimycin; 1-phenyl-2-decanoylamino-3-morpholino-1-propanol (PDMP), D-threo-1-phenyl-2-decanoylamino-3-morpholino-1-propanol and structurally related analogues thereof; and agents capable of increasing the rate of neuronal glycolipid degradation.Type: ApplicationFiled: October 19, 2001Publication date: August 22, 2002Inventors: Steven Walkley, Gordon D. Holt
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Patent number: 6436938Abstract: The present invention relates to a method of treating depression, especially refractory depression, in a mammal, including a human, by administering to the mammal a sigma receptor ligand in combination with an antidepressant agent. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, a sigma receptor ligand and a serotonin reuptake inhibitor.Type: GrantFiled: October 9, 2001Date of Patent: August 20, 2002Assignee: Pfizer Inc.Inventor: Harry Ralph Howard, Jr.