Carbocyclic Ring Containing Patents (Class 546/213)
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Patent number: 6984637Abstract: This invention relates to certain cyclic amine derivatives of Formula (I) that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: GrantFiled: November 21, 2003Date of Patent: January 10, 2006Assignee: Syntex (U.S.A.) LLCInventors: Leyi Gong, Denis John Kertesz, David Bernard Smith, Francisco Xavier Talamas, Robert Stephen Wilhelm
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Patent number: 6982272Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (I), (II), (Ia) and (Ib) further defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel compounds.Type: GrantFiled: April 24, 2003Date of Patent: January 3, 2006Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Michel Jose Emmanuel, Eugene R. Hickey, Weimin Liu, Denice Mary Spero, Sanxing Sun, David S. Thomson, Yancey David Ward, Erick Richard Roush Young
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Patent number: 6977260Abstract: 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: January 22, 2004Date of Patent: December 20, 2005Assignee: Allergan, Inc.Inventors: David W. Old, Danny T. Dinh
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Patent number: 6960602Abstract: The invention provides a compound of formula (I): wherein R1, R2, R3, R3a, R4, R4a, R5, and R6 are as 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: GrantFiled: March 19, 2002Date of Patent: November 1, 2005Assignee: AstraZeneca ABInventors: Jeremy Burrows, John Cumming
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Patent number: 6946476Abstract: The present invention relates to compounds represented by the structural Formula I: or a pharmaceutically acceptable salt thereof, which are useful for the treatment of metabolic and eating disorders such as obesity and hyperphagia, and for the treatment of diabetes and associated disorders.Type: GrantFiled: June 20, 2002Date of Patent: September 20, 2005Assignee: Schering CorporationInventors: Andrew Stamford, Youhao Dong, Stuart W. McCombie, Yusheng Wu
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Patent number: 6903119Abstract: The present invention relates to the compounds of the formula (I) and salts thereof (all the symbols are the same meanings as described in the specification). The compounds of the formula (I) possess inhibitory activity of N-type calcium channel, so they are useful as drug for prevention and/or treatment of cerebral infarct, transient ischemic attack, encephalomyelopathy after cardiac operation, spinal angiopathy, hypertension with stress, neurosis, epilepsy, asthma and pollakiuria etc. or agent for the treatment of pain.Type: GrantFiled: July 13, 1999Date of Patent: June 7, 2005Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Takuya Seko, Masashi Kato
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Patent number: 6890928Abstract: This invention is directed to aromatic sulfone hydroxamic acids (including hydroxamates) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.Type: GrantFiled: September 5, 2003Date of Patent: May 10, 2005Assignee: Pharmacia CorporationInventors: John N. Freskos, Yvette M. Fobian, Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, Jeffrey N. Carroll, Gary A. DeCrescenzo, Susan L. Hockerman, Darren J. Kassab, Steve A. Kolodziej, Joseph McDonald, Deborah A. Mischke, Monica B. Norton, Joseph G. Rico, John J. Talley, Clara I. Villamil, Lijuan Jane Wang
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Patent number: 6887871Abstract: There is disclosed the use of a compound of formula (I) wherein R1, R2, X, Y, V, W and Z are as defined in the specification, and pharmaceutically acceptable salts, enantiomers or racemates thereof, in the manufacture of a medicament, for the treatment or prophylaxis of diseases or conditions in which inhibition of nitric oxide synthase activity is beneficial. Certain novel compounds of formula (Ia) and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof are disclosed; together with processes for their preparation, compositions containing them and their use in therapy. The compounds of formulae (I) and (Ia) are inhibitors of the enzyme nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease.Type: GrantFiled: February 20, 2001Date of Patent: May 3, 2005Assignee: AstraZeneca ABInventors: David Cheshire, Stephen Connolly, David Cox, Peter Hamley, Antonio Mete, Austen Pimm
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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: 6841682Abstract: This invention relates a to a series of heterocyclic substituted piperazines of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the ?-1a adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this disease.Type: GrantFiled: November 26, 2001Date of Patent: January 11, 2005Assignee: Janseen Pharmaceutica N.V.Inventors: Richard H. Hutchings, Haripada Khatuya, Gee-Hong Kuo, Xiaobing Li, William V. Murray, Catherine Prouty, Frank Villani, Nelson C. F. Yim, Cynthia Maryanoff
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Patent number: 6828318Abstract: Compounds of formula (1): wherein R1, R2, R3, R4, R5 and R6 are independently selected from hydrogen, alkyl, aryl and non-aromatic heterocyclic groups, or each of one or more pair(s) of the substituent groups R1 to R6 may together form a 3,4,5,6,7 or 8-membered ring containing 0,1 or 2 heteroatom(s); R7 is selected from alkyl, aryl and non-aromatic heterocyclic groups; and R8 is selected from hydrogen, halogen, alkyl, aryl and non-aromatic heterocyclic groups; and pharmaceutically acceptable salts and prodrugs thereof, are useful for treating conditions generally associated with abnormalities in glutamatergic transmission.Type: GrantFiled: March 31, 2003Date of Patent: December 7, 2004Assignee: Vernalis Research LimitedInventors: Michael Frederick Snape, Roger John Gillespie, Claire Elizabeth Dawson, Steven Michael McAteer, Suneel Gaur
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Patent number: 6787650Abstract: A compound of the formula: [wherein R1 is a hydrocarbon group which may be substituted; R2 is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; R3 is halogen atoms, a carbamoyl group which may be substituted, a sulfamoyl group which may be substituted, an acyl group derived from sulfonic acid, a C1-4 alkyl group which may be substituted, a C1-4 alkoxy group which may be substituted, an amino group which may be substituted, a nitro group or a cyano group; R4 is hydrogen atoms or a hydroxy group; n is 0 or 1; and p is 0 or 1 to 4]; or a salt thereof, has potent CCR5 antagonistic activity and can be advantageously used as a medicament for inhibition of HIV infection to human peripheral blood mononuclear cells, especially for the treatment or prevention of AIDS.Type: GrantFiled: April 5, 2002Date of Patent: September 7, 2004Assignee: Takeda Chemical Industries, Ltd.Inventors: Osamu Kurasawa, Shinichi Imamura, Shohei Hashiguchi, Osamu Nishimura, Naoyuki Kanzaki, Masanori Baba
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Publication number: 20040152731Abstract: Compounds of general formula (1): R1 is selected from any one of phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl and pyridine N-oxide; where each R1 phenyl ring and R1 heteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C1-C6 alkyl, NO2, CF3, C1-C6 alkoxy, chloro, fluoro, bromo, and iodo. The substitutions on the phenyl ring and on the heteroaromatic ring may take place in any position on said ring systems; are disclosed and claimed in the present application, as well as salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain, anxiety and functional gastrointestinal disorders.Type: ApplicationFiled: November 13, 2003Publication date: August 5, 2004Inventors: William Brown, Andrew Griffin, Christopher Walpole
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Patent number: 6756387Abstract: Compounds of general formula I R1 is selected from any one of phenyl, pyridinyl, thienyl, furanyl, imidazolyl, triazolyl and thiazolyl; where each R1 phenyl ring and R1 heteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C1-C6 alkyl, NO2, CF3, C1-C6 alkoxy, chloro, fluoro, bromo, and iodo. The substitutions on the phenyl ring and on the heteroaromatic ring may take place in any position on said ring systems; are disclosed and claimed in the present application, as well as salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.Type: GrantFiled: January 16, 2003Date of Patent: June 29, 2004Assignee: AstraZeneca ABInventors: William Brown, Christopher Walpole, Zhongyong Wei
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Patent number: 6753335Abstract: Compounds of general formula I R1 is selected from any one of phenyl, pyridinyl, thienyl, furanyl, imidazolyl, and triazolyl; where each R1 phenyl ring and R1 heteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C1-C6 alkyl, NO2, CF3, C1-C6 alkoxy, chloro, fluoro, bromo, and iodo. The substitutions on the phenyl ring and on the heteroaromatic ring may take place in any position on said ring systems; are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.Type: GrantFiled: January 21, 2003Date of Patent: June 22, 2004Assignee: AstraZeneca ABInventors: William Brown, Christopher Walpole, Zhongyong Wei
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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: 6710060Abstract: 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: (wherein A represents, for example, phenyl group substituted with R1 and R2 or unsubstituted thienyl group; R1 and R2 each independently represent, for example, hydrogen atom, halogen atom or lower alkoxycarbonyl group; R3 represents, for example, hydrogen atom; R4 represents, for example, lower alkyl group; R5 represents, for example, lower alkoxy group; R6 represents, for example, hydrogen atom; R7 and R8 each represent, for example, hydrogen atom, respectively; X represents, for example, a single bond; Y represents, for example, methylene group or benzylidene group substituted with R1; and Z represents, for example, methylene group.Type: GrantFiled: October 4, 2001Date of Patent: March 23, 2004Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Ichiro Yamamoto, Manabu Itoh, Fumiaki Yamasaki, Yutaka Miyazaki, Shinichi Ogawa
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Patent number: 6696234Abstract: A silver halide photosensitive material contains a compound of the following general formula (I): wherein A1a represents a group selected from among CR1aR2a, NR1a, an oxygen atom and sulfur atom, A1b represents a group selected from among CR1bR2b, NR1b, an oxygen atom and sulfur atom, and each of R1a, R2a, R1b, R2b and R3 represents a hydrogen atom or a substituent, provided that, in the groups of CR1aR2a and CR1bR2b, R1aR2a and R1bR2b may represent a single divalent substituent, n represents an integer of 1 to 4, provided that, when n is 2 or more, a plurality of A1bs may be the same or different.Type: GrantFiled: September 24, 2002Date of Patent: February 24, 2004Assignee: Fuji Photo Film Co., Ltd.Inventors: Tadashi Inaba, Masaru Takasaki, Atsushi Matsunaga, Mamoru Sakurazawa, Shinichi Ichikawa
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Patent number: 6693117Abstract: Compounds of general formula (I) are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.Type: GrantFiled: August 19, 2002Date of Patent: February 17, 2004Assignee: AstraZeneca Canada Inc.Inventors: Daniel Delorme, Edward Roberts, Zhongyong Wei
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Patent number: 6689794Abstract: This invention is directed to aromatic sulfone hydroxamates (also known as “aromatic sulfone hydroxamic acids”) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.Type: GrantFiled: May 10, 2002Date of Patent: February 10, 2004Assignee: Pharmacia CorporationInventors: John N. Freskos, Yvette M. Fobian, Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, Jeffery N. Carroll, Gary A. DeCrescenzo, Susan L. Hockerman, Darren J. Kassab, Steve A. Kolodziej, Joseph McDonald, Deborah A. Mischke, Monica B. Norton, Joseph G. Rico, John J. Talley, Clara I. Villamil, Lijuan Jane Wang
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Patent number: 6683074Abstract: This invention relates to certain cyclic amine derivatives of Formula (I) that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: GrantFiled: September 26, 2001Date of Patent: January 27, 2004Assignee: Syntex (U.S.A.) LLCInventors: Leyi Gong, Denis John Kertesz, David Bernard Smith, Francisco Xavier Talamas, Robert Stephen Wilhelm
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Patent number: 6677369Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: April 25, 2002Date of Patent: January 13, 2004Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, Jr., Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
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Patent number: 6664253Abstract: The invention relates to new compounds of formula I or the pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, X and Ar1 have the meanings given in the specification, as well as the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin) antagonists.Type: GrantFiled: October 16, 2001Date of Patent: December 16, 2003Assignee: Boehringer Ingelheim Pharma KGInventors: Horst Dollinger, Franz Esser, Birgit Jung, Gerd Schnorrenberg, Kurt Schromm, Georg Speck
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Patent number: 6664273Abstract: The present invention discloses compounds, which are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.Type: GrantFiled: November 25, 2002Date of Patent: December 16, 2003Assignee: Schering CorporationInventors: Duane A. Burnett, Wen-Lian Wu
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Patent number: 6645980Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.Type: GrantFiled: November 20, 2000Date of Patent: November 11, 2003Assignee: Sepracor Inc.Inventors: Gregory D. Cuny, Liming Shao, James R. Hauske, Michele L. R. Heffernan, Brian M. Aquila, Xinhe Wu, Fengjiang Wang, Thomas D. Bannister
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Patent number: 6627629Abstract: 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 29, 2001Date of Patent: September 30, 2003Assignee: Bristol-Myers Squibb PharmaInventors: Soo S. Ko, James R. Pruitt, Dean A. Wacker, Douglas G. Batt
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Patent number: 6617325Abstract: The present invention relates to biphenyl derivatives of general formula wherein Ra to Rg and n are defined as in claim 1, the isomers and salts thereof, particularly the physiologically acceptable salts thereof, which are valuable inhibitors of the microsomal triglyceride-transfer protein (MTP), medicaments containing these compounds and their use, as well as the preparation thereof.Type: GrantFiled: May 15, 2002Date of Patent: September 9, 2003Assignee: Boehringer Ingelheim Pharma KGInventors: Thorsten Lehmann-Lintz, Armin Heckel, Leo Thomas, Michael Mark
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Patent number: 6605626Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: September 21, 2001Date of Patent: August 12, 2003Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson Jr., Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
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Patent number: 6605623Abstract: 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: August 12, 2003Assignee: Bristol-Myers Squibb Pharma Co.Inventors: Soo S. Ko, George V. DeLucca, John V. Duncia, Joseph B. Santella, III, Dean A. Wacker
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Patent number: 6605608Abstract: The present invention relates to the compounds of the formula (I) and salts thereof (all the symbols are the same meanings as described in the specification). The compounds of the formula (I) possess inhibitory activity of N-type calcium channel, so they are useful as drug for prevention and/or treatment of cerebral infarct, transient ischemic attack, encephalomyelopathy after cardiac operation, spinal angiopathy, hypertension with stress, neurosis, epilepsy, asthma and pollakiuria etc. or agent for the treatment of pain.Type: GrantFiled: December 22, 2000Date of Patent: August 12, 2003Assignee: Ono Pharmaceutical Co., LtdInventors: Takuya Seko, Masashi Kato
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Publication number: 20030139417Abstract: A compound of general formula (I) 1Type: ApplicationFiled: April 12, 2002Publication date: July 24, 2003Inventors: Wolfgang Eberlein, Wolfhard Engel, Klaus Rudolf, Henri Doods, Gerhard Hallermayer, Eckhart Bauer
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Patent number: 6538002Abstract: The present in to s directed to compounds of the formula I: (wherein R1, R2, R3, R7, R8, X, Y, Z, 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: March 25, 2003Assignee: Merck & Co., Inc.Inventors: Paul E. Finke, Malcolm Maccoss, Sander G. Mills, Bryan Oates
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Patent number: 6528532Abstract: The present invention provides HIV aspartyl protease inhibitors of the formula: and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein n is 3 or 4, Y is O, S, NH or N—CN, wherein Cx may be, for example COOH, or CH2OH, wherein R1 is selected from the group consisting of a benzenesulfonyl group of formula II as defined herein, wherein R2 may be, for example, iso-butyl, or 3-methylbutyl, and wherein R3 and R4 are as defined herein.Type: GrantFiled: May 13, 2002Date of Patent: March 4, 2003Assignee: Pharmacor Inc.Inventors: Brent Richard Stranix, Abderrahim Bouzide, Gilles Sauvé
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Patent number: 6503926Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: and physiologically acceptable salts thereof.Type: GrantFiled: July 28, 1999Date of Patent: January 7, 2003Assignees: Millennium Pharmaceuticals, Inc., Kyowa Hakko Kogyo Co., Ltd.Inventors: Jay R. Luly, Yoshisuke Nakasato, Etsuo Ohshima, Hiroki Sone, Osamu Kotera, Geraldine C. B. Harriman
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Publication number: 20020161005Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation.Type: ApplicationFiled: July 28, 1999Publication date: October 31, 2002Inventors: JAY R. LULY, YOSHISUKE NAKASATO, ETSUO OHSHIMA, HIROKI SONE, OSAMU KOTERA, GERALDINE C. B. HARRIMAN
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Publication number: 20020137736Abstract: There are provided novel compounds of formula (I) 1Type: ApplicationFiled: February 27, 2001Publication date: September 26, 2002Inventors: Kenneth Mattes, Robert Murray, Eifion D Phillips, Hans Schmitthenner
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Patent number: 6455545Abstract: Compounds of general formula (I) are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.Type: GrantFiled: January 18, 2001Date of Patent: September 24, 2002Assignee: AstraZeneca Canada Inc.Inventors: Daniel Delorme, Edward Roberts, Zhongyong Wei
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Patent number: 6451797Abstract: Heterocyclic derivatives of di-N-substituted piperazine or 1,4 di-substituted piperidine compounds in accordance with formula I (including all isomers, salts and solvates) wherein wherein one of Y and Z is —N— and the other is —N— or —CH—; X is —O—, —S—, —SO—, —SO2— or —CH2—; Q is R is alkyl, cycloalkyl, optionally substituted aryl or heteroaryl; R1, R2 and R3 are H or alkyl; R4 is alkyl, cyclolalkyl or R5 is H, alkyl, —C(O)alkyl, arylcarbonyl, —SO2alkyl, aryl-sulfonyl —C(O)Oalkyl, aryloxycarbonyl, —C(O)NH-alkyl or aryl-aminocarbonyl, wherein the aryl portion is optionally substituted; R6 is H or alkyl; and R7 is H, alkyl, hydroxyalkyl or alkoxyalkyl; are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of treatment are also disclosed.Type: GrantFiled: February 28, 2000Date of Patent: September 17, 2002Assignee: Schering CorporationInventors: Joseph A. Kozlowski, Stuart W. McCombie, Jayaram R. Tagat, Susan F. Vice
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Patent number: 6348597Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer 0 or 1; R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1 represented hydroxy, m is an integer 0.Type: GrantFiled: April 4, 2001Date of Patent: February 19, 2002Assignee: Merrell Pharmaceuticals, Inc.Inventors: Richard C. Krauss, Robert M. Strom, Carey L. Scortichini, William J. Kruper, Richard A. Wolf, Weishi W. Wu, Albert A. Carr, David A. Hay, Duane E. Rudisill, Gianbattista Panzone
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Patent number: 6313122Abstract: This application relates to a compound of formula (I), a pharmaceutically acceptable salt of the compound, or a prodrug thereof, as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: March 20, 2000Date of Patent: November 6, 2001Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, Jr., Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
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Patent number: 6303637Abstract: The present invention relates to a class of heterocyclic compounds of Formula I that are useful as potassium channel inhibitors to treat autoimmune disorders, cardiac arrhythmias, and the like.Type: GrantFiled: October 21, 1999Date of Patent: October 16, 2001Assignee: Merck & Co., Inc.Inventors: Jianming Bao, Andrew Kotliar, Frank Kayser, William H. Parsons, Kathleen M. Rupprecht, Christopher F. Claiborne, David A. Claremon, Nigel Liverton, Wayne J. Thompson
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Patent number: 6288084Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by the following structural formula: and physiologically acceptable salts thereof.Type: GrantFiled: January 21, 1999Date of Patent: September 11, 2001Assignees: Millennium Pharmaceuticals, Inc., Kyowa Hakko Kogyo Co., Ltd.Inventors: Jay R. Luly, Yoshisuke Nakasato, Etsuo Ohshima
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Patent number: 6288085Abstract: The present invention relates to certain novel piperidine derivatives, to processes for their preparation, to pharmaceutical formulations containing them and to their use in medical therapy, particularly in the treatment of psychotic disorders.Type: GrantFiled: June 17, 1999Date of Patent: September 11, 2001Assignee: Akzo Nobel N.V.Inventors: Duncan Robertson Rae, Samuel George Gibson
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Publication number: 20010011092Abstract: Novel compounds of the formula 1Type: ApplicationFiled: January 25, 2001Publication date: August 2, 2001Inventors: Deen Tulshian, Ginny D. Ho, Lisa S. Silverman, Julius J. Matasi, Robbie L. McLeod, John A. Hey, Richard W. Chapman, Ana Bercovici, Francis M. Cuss
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Patent number: 6265433Abstract: The present invention provides compounds having the structure: and pharmaceutically acceptable salts and stereoisomers thereof that are useful in the treatment of inflammatory diseases which are mediated by LTB4 production, such as psoriasis, ulcerative colitis, IBD, and asthma.Type: GrantFiled: May 14, 1999Date of Patent: July 24, 2001Assignee: G. D. Searle & CompanyInventors: Barbara Baosheng Chen, Helen Chen, Mark Andrew Russell, Julie Marion Miyashiro, James Malecha, Thomas Dale Penning
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Patent number: 6262044Abstract: The present invention provides novel compounds, novel compositions, 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. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, immune dysfunctions including autoimmunity diseases with dysfunctions of the coagulation system, allergic diseases including asthma, osteoporosis, proliferative disorders including cancer and psoriasis, diseases with decreased or increased synthesis or effects of growth hormone, diseases with decreased or increased synthesis of hormones or cytokines that regulate the release of/or response to growth hormone, diseases of the brain including Alzheimer's disease and schizophrenia, and infectious diseases.Type: GrantFiled: March 11, 1999Date of Patent: July 17, 2001Assignees: Novo Nordisk A/S, Ontogen CorporationInventors: Niels Peter Hundahl Møller, Henrik Sune Andersen, Lars Fogh Iversen, Ole Hvilsted Olsen, Sven Branner, Daniel Dale Holsworth, Farid Bakir, Luke Milburn Judge, Frank Urban Axe, Todd Kevin Jones, William Charles Ripka, Yu Ge, Roy Teruyuki Uyeda
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Patent number: 6197791Abstract: Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflammatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states.Type: GrantFiled: August 26, 1998Date of Patent: March 6, 2001Assignee: American Cyanamid CompanyInventors: Aranapakam Mudumbai Venkatesan, George Theodore Grosu, Jamie Marie Davis, Jannie Lea Baker, Jeremy Ian Levin
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Patent number: 6187792Abstract: Compounds of general formula (I) are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.Type: GrantFiled: March 5, 1998Date of Patent: February 13, 2001Assignee: Astra Pharma Inc.Inventors: Daniel Delorme, Edward Roberts, Zhongyong Wei
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Patent number: RE38257Abstract: A piperidine compound of the formula (I): wherein A is a fused aromatic ring; R is hydrogen, chloro or methoxy; X is (CH2)n, which may be substituted, in which n is 0 or an integer of 1 to 10, —CH≡CH—, —C≡C—, —O—, —S—, —NH—, —N(COCH3)—, —N(COOC2H5)—, —N(CHO)—, —N(CH3)—, —CO—, —SO—, or —SO2—; Y is —CH≡CH—, —CH2CH2—, —CH2CO—, —O—, —S—, —NH—, —OCH2—, —SCH2—, —NHCH2—, —CH(OH)CH2— or —CH(OH)CH(OH)—; and Q is substituted or unsubstituted n-hexyl, carboxypropyl, ethoxycarbonylpropyl, cyanopropyl, cyclohexyl, phenyl, indanyl, naphthyl, tetrahydronaphthyl, benzocycloheptyl, piperidinyl, tetrahydroisoquinolinyl, indolyl, pyrolyl, furyl, thienyl, thiazolyl, oxazolyl or N-methylpyrolyl, wherein any one or more of tType: GrantFiled: February 10, 1999Date of Patent: September 23, 2003Assignee: Ajinomoto Co., Inc.Inventors: Masataka Shoji, Kozo Toyota, Chikahiko Eguchi, Ryota Yoshimoto, Yoshikatsu Koyama, Hideki Domoto, Akira Kamimura