Bicyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 514/469)
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Patent number: 7115605Abstract: PDF inhibitors and novel methods for their use are provided.Type: GrantFiled: April 5, 2004Date of Patent: October 3, 2006Assignee: SmithKline Beecham CorporationInventors: Kelly M. Aubart, Siegfried B. Christensen, IV, Jacques Briand, Maxwell David Cummings
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Patent number: 7105564Abstract: The present invention provides novel compounds having a dual antagonistic activity against thromboxane A2 receptor and prostaglandin D2 receptor and pharmaceutical compositions comprising them. A compound of the formula (I): wherein R1 is —CH2—CH?CH—CH2—CH2—CH2—COOR2 or —CH?CH—CH2—CH2—CH2—COOR2; R2 is hydrogen or alkyl; m is 0 or 1; p is 0 or 1; X1 and X3 each is independently optionally substituted aryl or optionally substituted heteroaryl; X2 is a bond, —CH2—, —S—, —SO2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, or the like; X4 is —CH2—, —CH2—CH2—, —C(?O)—, or the like, have a dual antagonistic activity against both a thromboxane A2 receptor and a prostaglandin D2 receptor.Type: GrantFiled: March 2, 2000Date of Patent: September 12, 2006Assignee: Shionogi & Co., Ltd.Inventors: Tsunetoshi Honma, Yoshiharu Hiramatsu, Akinori Arimura
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Patent number: 7105568Abstract: The subject invention provides novel compounds for treatment of cardiac arrhythmia and methods of use.Type: GrantFiled: April 8, 2005Date of Patent: September 12, 2006Assignee: ARYx Therapeutics, Inc.Inventor: Pascal Druzgala
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Patent number: 7101867Abstract: Compounds represented by the formula: wherein R1 and R2 are hydrogen atom, a hydrocarbon group or a heterocyclic group, or R1 and R2 may form, together with the adjacent carbon atom, a 3- to 8-membered homocyclic or heterocyclic ring, W indicates (i) a group represented by the formula: wherein ring B indicates a 5- to 7-membered ring, or (ii) a group represented by the formula: wherein R4 indicates (1) an aliphatic hydrocarbon group, which may be substituted with an aromatic group, or (2) an acyl group containing an aromatic group, R5 is hydrogen atom, a C1-6 alkyl, or an acyl group, provided that, when W is Wa, R3 is hydrogen atom, a hydrocarbon group or a heterocyclic group, when W is Wb, R3 indicates a C6-14 aryl group, or salts thereof or prodrugs thereof have an excellent action to inhibit neurodegeneration and the like as well as an excellent brain penetrability and are low in the toxicity, thereby being useful as prophylactic or therapeutic drugs for nerve degenerative diseases and theType: GrantFiled: April 11, 2002Date of Patent: September 5, 2006Assignee: Takeda Pharmaceutical Company LimitedInventors: Shigenori Ohkawa, Yasuyoshi Arikawa, Kouki Kato, Masahiro Okura, Masaki Setoh
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Patent number: 7101912Abstract: Prodrugs of carbidopa, derivatives of carbidopa prodrugs, methods of making prodrugs of carbidopa and derivatives thereof, methods of using prodrugs of carbidopa and derivatives thereof, and compositions of prodrugs of carbidopa and derivatives thereof are disclosed.Type: GrantFiled: December 8, 2003Date of Patent: September 5, 2006Assignee: XenoPort, Inc.Inventors: Jia-Ning Xiang, Mark A. Gallop, Kenneth C. Cundy, Jianhua Li, Feng Xu, Cindy X. Zhou, Laxminarayan Bhat
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Patent number: 7098232Abstract: The present invention provides a method for preventing and treating gastrointestinal diseases such as dyspepsia, irritable bowel disease and chemotherapy-associated nausea by administering an antagonist or partial agonist of 5HT1a receptors.Type: GrantFiled: October 13, 2000Date of Patent: August 29, 2006Assignee: Athpharma LimitedInventors: Timothy G. Dinan, Patrick W. N. Keeling
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Patent number: 7091240Abstract: A diverse set of tubulin binding agents have been discovered which are structurally characterized, in a general sense, by a semi-rigid molecular framework capable of maintaining aryl-aryl, pseudo pi stacking distances appropriate for molecular recognition of tubulin. In phenolic or amino form, these ligands may be further functionalized to prepare phosphate esters, phosphate salts, phosphoramidates, and other prodrugs capable of demonstrating selective targeting and destruction of tumor cell vasculature.Type: GrantFiled: April 29, 2003Date of Patent: August 15, 2006Assignees: Oxigene, Inc., Baylor UniversityInventors: Kevin G. Pinney, Vani P. Mocharla, Zhi Chen, Charles M. Garner, Mallinath Hadimani, Raymond Kessler, James M. Dorsey, Klaus Edvardsen, David J. Chaplin, Joseph Prezioso, Usha Ghatak, legal representative, Anjan Ghatak, deceased
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Patent number: 7087635Abstract: The present invention relates to a ?3 adrenergic receptor agonist of formula I: or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful for treating Type 2 diabetes and/or obesity.Type: GrantFiled: March 16, 2005Date of Patent: August 8, 2006Assignee: Eli Lilly and CompanyInventors: Daniel Jon Sall, Jolie Anne Bastian, Cynthia Darshini Jesudason, Don Richard Finley, Freddie Craig Stevens, Vincent Patrick Rocco, Patrick Gianpietro Spinazze, John Xiaoqiang He, John Arnold Werner, William George Trankle, Andrew Michael Ratz, Theo Schotten, Gerd Reuhter
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Patent number: 7078565Abstract: Disclosed are phenyl-alkylene benzamides useful as orexin antagonistsType: GrantFiled: October 30, 2002Date of Patent: July 18, 2006Assignee: SmithKline Beecham plcInventors: Wai Ngor Chan, Amanda Johns, Roderick Alan Porter, Rachel Elizabeth Anne Stead, Mythily Vimal
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Patent number: 7071227Abstract: Purified antiviral compounds, pharmaceutical formulations containing the compounds, and methods of use of the compounds are provided. The compositions of the invention are isolated antiviral components from plant extracts derived from, for example, Salvia miltiorrhiza, that find use in the treatment of viral infections, such as by inhibiting the activity of viral integrase. Methods for isolation and purification of the antiviral compounds are additionally provided.Type: GrantFiled: September 25, 2001Date of Patent: July 4, 2006Assignee: The Johns Hopkins UniversityInventors: Ru Chih C. Huang, Ibrahim Shawky Abd Elazem, Hong Shan Chen
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Patent number: 7049334Abstract: A method for enhancing learning and memory or treating amnesia. The method includes administrating to a subject in need thereof a compound of the formula (I): A is H, R, or ?each of Ar1, Ar2, and Ar3, independently, is phenyl, thienyl, furyl, or pyrrolyl; each of R1, R2, R3, R4, R5, and R6, independently, is H, nitro, halogen, R, OH, OR, C(O)OH, C(O)OR, C(O)SH, C(O)SR, C(O)NH2, C(O)NHR, C(O)NRR?, ROH, ROR?, RSH, RSR?, ROC(O)R?OH, NHR, NRR?, RNHR?, or RNR?R?; or R1 and R2 together, R3 and R4 together, or R5 and R6 together are ORO; wherein each of R, R?, and R?, independently is C1˜C6 alkyl; and n is 1, 2, or 3. The compound is in an effective amount for enhancing learning and memory or treating amnesia.Type: GrantFiled: September 13, 2002Date of Patent: May 23, 2006Assignee: Carlsbad Technology, Inc.Inventors: Wen-Mei Fu, Keng-Chen Liang, Wei-Lin Chien, Sheng-Chu Kuo, Fang-Yuan Lee, Che-Ming Teng
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Patent number: 7045518Abstract: Selected sulfonylalkanoylamino hydroxyethylamine sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: October 3, 2003Date of Patent: May 16, 2006Assignee: G.D. Searle & Co.Inventors: Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Raj Nagarajan, Joseph J. McDonald
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Patent number: 7037933Abstract: The subject invention pertains to novel compounds (and salts thereof), and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns methods of making the novel compounds. The novel compounds are rapidly metabolized analogs of amiodarone, having the distinct and advantageous characteristic of being metabolized to a less lipophilic compound. This results in an improved safety profile. The new compounds have particular utility for treating life-threatening ventricular tachyarrhythmias, especially in patients with congestive heart failure (CHF). The compounds also provide effective management for ventricular arrhythmias and supraventricular arrhythmias, including atrial fibrillation and re-entrant tachyarrhythmias involving accessory pathways.Type: GrantFiled: March 7, 2005Date of Patent: May 2, 2006Assignee: ARYx Therapeutics, Inc.Inventor: Pascal Druzgala
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Patent number: 7037932Abstract: There is provided a heretoaryloxy 3-substituted propanamine compound of formula (I): wherein A is selected from —O— and —S—; X is selected from phenyl optionally substituted with up to 5 substituents selected from halo, C1–C4 alkyl and C1–C4 alkoxy, and thienyl optionally substituted with up to 3 substituents selected from halo and C1–C4 alkyl; Y is selected from benzothienyl, indolyl and benzofuranyl, optionally substituted with up to 5 substituents selected from halo, C1–C4 alkyl, C1–C4 alkoxy, nitro, acetyl and cyano; and when Y is indolyl it may be substituted or further substituted by an N-substituent selected from C1–C4 alkyl; R1 and R2 are each independently H or C1–C4 alkyl; and pharmaceutically acceptable salts thereof.Type: GrantFiled: May 6, 2002Date of Patent: May 2, 2006Assignee: Eli Lilly and CompanyInventors: Peter Gallagher, Richard Edmund Rathmell, Maria Ann Fagan
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Patent number: 7022733Abstract: This invention provides estrogen receptor modulators of formula I, having the structure wherein R, R?, A, A?, X, Y, and Y are as defined in the specification, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: April 21, 2004Date of Patent: April 4, 2006Assignee: WyethInventors: Christopher P. Miller, Michael D. Collini, David H. Kaufman, Robert L. Morris, Robert R. Singhaus, Jr., John W. Ullrich, Heather A. Harris, James C. Keith, Jr., Leo M. Albert, Rayomand J. Unwalla
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Patent number: 7019024Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 9, 2001Date of Patent: March 28, 2006Assignee: Allelix Neuroscience Inc.Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
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Patent number: 7015246Abstract: The invention relates to novel benzofuran derivatives, to processes for preparing them and to their uses in medicaments.Type: GrantFiled: October 10, 2002Date of Patent: March 21, 2006Assignee: Bayer AktiengesellschaftInventors: Carsten Schmeck, Ulrich Müller, Gunter Schmidt, Josef Pernerstorfer, Hilmar Bischoff, Axel Kretschmer, Verena Vöhringer, Christiane Faeste, Helmut Haning, Markus Hauswald, Delf Schmidt, Martin Zoche, Heiner Apeler, Willi Jonghaus, Peter Reinemer
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Patent number: 7008636Abstract: This invention provides compounds of Formula I having the structure or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.Type: GrantFiled: May 11, 2004Date of Patent: March 7, 2006Assignee: WyethInventors: John A. Butera, Craig E. Caufield, Russell F. Graceffa, Alexander Greenfield, Eric G. Gundersen, Lisa Marie Havran, Alan H. Katz, Joseph R. Lennox, Scott C. Mayer, Robert E. McDevitt
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Patent number: 7008950Abstract: A compound of the formula: wherein R1 and R2 each is H or a hydrocarbon group which may be substituted, or R1 and R2 form a 3- to 8-membered carbo or heterocyclic ring which may be substituted; R3 is H, a lower alkyl which may be substituted or an aromatic group which may be substituted; R4 is (1) an aromatic group which may be substituted, (2) an aliphatic hydrocarbon group substituted by an aromatic group which may be substituted, which hydrocarbon group may be further substituted or (3) an acyl; X and Y each is oxygen or sulfur which may be oxidized; and ring A is a benzene ring which may be further substituted, or a salt thereof, is useful for an agent for suppressing neurodegeneration.Type: GrantFiled: June 4, 1998Date of Patent: March 7, 2006Assignee: Takeda Chemical Industries, Ltd.Inventors: Shigenori Ohkawa, Masaki Setoh, Mitsuru Kakihana, Masahiro Okura
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Patent number: 7005448Abstract: The present invention provides novel compounds, compositions containing the compounds of the invention in a pharmaceutically acceptable excipient and methods for using the compositions for lowering intraocular pressure.Type: GrantFiled: December 5, 2002Date of Patent: February 28, 2006Assignee: Alcon, Inc.Inventor: Jesse A. May
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Patent number: 7005428Abstract: Novel methods for the medical treatment and/or inhibition of the development of hypercholesterolemia in susceptible warm-blooded animals including humans involving administration of selective estrogen receptor modulator particularly compounds having the general structure: and an amount of a sex steroid precursor selected from the group consisting of dehydroepiandrosterone, dehydroepiandrosterone sulfate, androst-5-ene-3?,17?-diol and compounds converted in vivo to one of the foregoing precursor. Further administration of bisphosphonates in combination with selective estrogen receptor modulators and/or sex steroid precursor is disclosed for the medical treatment and/or inhibition of the development of osteoporosis. Pharmaceutical compositions for delivery of active ingredient(s) and kit(s) useful to the invention are also disclosed.Type: GrantFiled: September 24, 1999Date of Patent: February 28, 2006Assignee: Endorecherche, Inc.Inventor: Fernand Labrie
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Patent number: 7001924Abstract: The present invention features compounds useful for inhibiting RNase P activity. These compounds can be used as therapeutics for treating or preventing a variety of bacterial infections. The compounds belong to several classes including mono- and bis-guanylhydrazones, guanylhydrazone mimetics, and benzothiazolium compounds. Exemplary compounds are compounds of formula I: Y—(NR?)k—U1—(NR?)I—A—(NR1)m—U2—(NR2)n—Z??I with substituents as described herein.Type: GrantFiled: September 23, 2002Date of Patent: February 21, 2006Assignee: Message PharmaceuticalsInventors: Tony Giordano, Michael A. Sturgess, Samala J. Rao
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Patent number: 6998407Abstract: Chemical compounds which are antagonists of Monocyte Chemoattractant Protein-1 (MCP-1) function, pharmaceutical compositions comprising these compounds, methods of treatment employing these compounds and compositions, and processes for preparing these compounds. The compounds are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection.Type: GrantFiled: November 18, 2003Date of Patent: February 14, 2006Assignees: Telik, Inc., Sanwa Kagaku Kenkyusho Co. Ltd.Inventors: Edgardo Laborde, Louise Robinson, Fanying Meng, Brian T. Peterson, Hugo O. Villar, Steven E. Anuskiewicz, Yoshiro Ishiwata, Shoji Yokochi, Yukiharu Matsumoto, Takuji Kakigami, Hideaki Inagaki, Takahito Jomori, Kouji Matsushima
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Patent number: 6987194Abstract: Insecticidal (dihalopropenyl) phenylalkyl substituted dihydrobenzofuran and dihydrobenzopyran derivatives of Formula I are disclosed. These compounds provide unexpected insecticidal activity across a spectrum of insect pests combined with desirable physical properties including improved photostability. wherein x and y are integers independently selected from 0 or 1; and B is a bridging group *—(CR16R17)q—(CR18R19)r—(CR20R21)s—Lt—(CR22R23)u—(CR24R25)v—(CR26R27)w—, where the asterisk denotes attachment at A; and q, r, s, u, v and w are integers independently selected from 0, 1 and 2; and t is an integer selected from 0 and 1. A, D, E, G, M, R through R11, and R16 through R27, inclusively, are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I and methods of controlling insects by applying said compositions to a locus where insects are present or are expected to be present are also disclosed.Type: GrantFiled: April 27, 2004Date of Patent: January 17, 2006Assignee: FMC CorporationInventors: George Theodoridis, Edward J. Barron, Dominic P. Suarez, Y. Larry Zhang, Ping Ding, David M. Roush, Stephen F. Donovan, Frank J. Zawacki, Walter H. Yeager, John W. Lyga, Daniel H. Cohen
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Patent number: 6977306Abstract: According to the present invention, citalopram hydrobromide dissolved in a solvent containing at least one member selected from the group consisting of alcohol having 1-3 carbon atoms, water and acetone is crystallized or recrystallized while controlling the cooling rate, thereby to 1) provide an industrial method for crystallizing citalopram hydrobromide, which enables easy control of the crystal characteristics, such as particle size, particle size distribution and aspect ratio and the like of the crystal, and 2) provide citalopram hydrobromide crystal having crystal characteristics useful as a pharmaceutical bulk.Type: GrantFiled: April 2, 2001Date of Patent: December 20, 2005Assignee: Sumitomo Chemical Company, LimitedInventors: Tetsuya Ikemoto, Nobuhiro Arai, Masami Igi
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Patent number: 6969730Abstract: Compounds of formula (I) or a pharmaceutically acceptable salts or prodrug thereof which are useful for the modulation of the histamine-3 receptors in mammals and which are useful for the treatment of disorders ameliorated by histamine-3 receptor ligands.Type: GrantFiled: February 25, 2002Date of Patent: November 29, 2005Assignee: Abbott LaboratoriesInventors: Marlon D. Cowart, Youssef L. Bennani, Ramin Faghih, Gregory A. Gfesser, Lawrence A. Black
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Patent number: 6962929Abstract: The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, vascular restenosis, microbial infections, and psoriasis, or as lead compounds for the development of such agents.Type: GrantFiled: October 11, 2002Date of Patent: November 8, 2005Assignee: Tularik Inc.Inventors: John A. Flygare, Julio Cesar Medina, Bei Shan, David Louis Clark, Terry J. Rosen
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Patent number: 6960613Abstract: Use of escitalopram (the S-(+)-enantiomer of citalopram) or a pharmaceutically acceptable salt thereof for the preparation of a medicament useful in the treatment of neurotic disorders is provided, including anxiety states, in particular generalised anxiety disorder and social anxiety disorder, post traumatic stress disorder, obsessive compulsive disorder and panic attacks.Type: GrantFiled: August 20, 2003Date of Patent: November 1, 2005Assignee: H. Lundbeck A/SInventors: Connie Sanchez, Sandra Hogg
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Patent number: 6949583Abstract: The invention relates to benzofuran or benzothiophene derivatives, to processes for preparing them, to pharmaceutical compositions comprising them, and to the method of use thereof in the treatment of pathological syndromes of the cardiovascular system.Type: GrantFiled: August 21, 2001Date of Patent: September 27, 2005Assignee: Sanofi-SynthelaboInventors: Jean-Louis Assens, Claude Bernhart, Frédérique Cabanel-Haudricourt, Patrick Gautier, Dino Nisato
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Patent number: 6946483Abstract: The invention relates to novel (aminoalkenyl-benzoyl) benzofuran or benzothiophene derivatives of general formula: These compounds are of use as medicaments, in particular in the treatment of pathological syndromes of the cardiovascular system.Type: GrantFiled: August 23, 2001Date of Patent: September 20, 2005Assignee: Sanofi-AventisInventors: Jean-Louis Assens, Claude Bernhart, Frédérique Cabanel-Haudricourt, Victor Dos Santos, Patrick Gautier, Dino Nisato
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Patent number: 6939865Abstract: A subject-matter of the invention is a pharmaceutical composition for parenteral administration, characterized in that it comprises: dronedarone or one of its pharmaceutically acceptable salts as active principle; a physiologically acceptable buffer solution capable of maintaining the pH of the composition between 3 and 5; a physiologically acceptable water-soluble ?-cyclodextrin derivative.Type: GrantFiled: December 10, 2001Date of Patent: September 6, 2005Assignee: Sanofi-AventisInventors: Frédérique Bourriague-Seve, Thierry Breul
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Patent number: 6933317Abstract: Compounds of the general formula (I) which are metabolically stable and have an antagonistic activity against PGD2 receptor: ? wherein Y is bicyclic ring; R1 is optionally substituted heteroaryl; R2 is hydrogen, etc.; R3 is —CH2—CH2—CH2—CH2—CH?CH—COOR4, —CH2—CH2—CH2—CH2—X1—CH2—COOR4, —CH2—CH?CH—CH2—X1—CH2—COOR4 or —CH2—CH2—CH2—COOR4; R4 is hydrogen, etc.; X1 is —O—, etc.Type: GrantFiled: October 26, 2001Date of Patent: August 23, 2005Assignee: Shionogi & Co. Ltd.Inventors: Norihiko Tanimoto, Yoshiharu Hiramatsu, Tsunetoshi Honma, Masanao Inagaki
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Patent number: 6921774Abstract: The invention provides novel compounds of the formula I below: wherein the meaning of each substituent is defined in the application. The compounds are useful as inhibitors of the glycine transporter and useful in the treatment of diseases responsive to the inhibition of the glycine transporter. The invention provides a pharmaceutical composition comprising a compound of Formula I as defined above and the use of compounds as above for the manufacture of medicaments for treatment of diseases responsive to ligands of the glycine transporter.Type: GrantFiled: January 17, 2003Date of Patent: July 26, 2005Assignee: H. Lundbeck A/SInventors: Ejner Knud Moltzen, Paul Garrick Smith, Christian Krog-Jensen, Klaus Peter Bøgesø
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Patent number: 6916941Abstract: Crystalline particles of escitalopram oxalate with a particle size of at least 40 ?m is disclosed. Method for the manufacture of said crystalline particles and pharmaceutical compositions comprising said crystalline particles are also disclosed.Type: GrantFiled: March 31, 2003Date of Patent: July 12, 2005Assignee: H. Lundbeck A/SInventors: Troels Volsgaard Christensen, Ken Liljegren, Michiel Onne Elema, Lene Andresen, Shashank Mahashabde, Sebastian P. Assenza
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Patent number: 6911469Abstract: A sulfonamide compound of the formula (I): R1—SO2NHCO—A—X—R2??(I) wherein R1 is alky, alkenyl, alkynyl and the like; A is an optionally substitutedheteropolycyclic group except benzimidazolyl, indolyl, 4,7-dihydrobenzimidazolyland 2,3-dihydrobenzoxazinyl; X is alkylene, oxa, oxa(lower)alkylene and the like; and R2 is optionally substituted aryl, substituted biphenylyl and the like, a salt thereof and a pharmaceutical composition comprising the same. The sulfonamide compound is effective for the diseases treatable based on their blood sugar level-depressing activity, cGMP-PDE (especially PDE-V)-inhibiting activity, smooth muscle relaxing activity, bronchodilating activity, vasodilating activity, smooth muscle cell suppressing activity, and antiallergic activity.Type: GrantFiled: January 17, 2002Date of Patent: June 28, 2005Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Hiroshi Kayakiri, Yoshito Abe, Hitoshi Hamashima, Hitoshi Sawada, Tsuyoshi Mizutani, Teruo Oku, Noritsugu Yamasaki, Osamu Onomura, Masahiro Nishikawa, Takahiro Hiramura, Takafumi Imoto
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Patent number: 6908944Abstract: A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of formula I: It has been surprisingly discovered that the pharmaceutical composition of the present invention is effective for the treatment of increased urge to urinate or urinary incontinence. Also disclosed are methods of treatment using the pharmaceutical compositions.Type: GrantFiled: May 30, 2003Date of Patent: June 21, 2005Assignee: Gruenenthal GmbHInventors: Thomas Christoph, Elmar Friderichs
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Patent number: 6903086Abstract: This invention relates to compounds which are generally IP receptor antagonists and which are represented by Formula I: wherein G1 is selected from the group consisting of a, b1 and b2, and A and G2 are as defined in the specification; or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.Type: GrantFiled: March 1, 2002Date of Patent: June 7, 2005Assignee: SYNTEX (U.S.A.) LLCInventors: Francisco Javier Lopez-Tapia, Dov Nitzan, Counde O'Yang
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Patent number: 6894074Abstract: The invention relates to insecticidal mixtures comprising compounds of the formula (I) in which X?, Y?, Z?, n, G?, A? and B? are as defined above and agonists and/or antagonists of nicotinic acetylcholine receptors, for protecting plants against attack by pests.Type: GrantFiled: September 29, 2003Date of Patent: May 17, 2005Assignee: Bayer AktiengesellschaftInventors: Thomas Bretschneider, Reiner Fischer, Christoph Erdelen, Ernst Brück
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Patent number: 6887877Abstract: The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating Flaviviridae viral infection.Type: GrantFiled: June 11, 2002Date of Patent: May 3, 2005Assignee: ViroChem Pharma Inc.Inventors: Laval Chan Chun Kong, Jean Bedard, Sanjoy Kumar Das, Nghe Nguyen Ba, Oswy Z. Pereira, Stephen Joseph Shuttleworth, Mohammad Arshad Siddiqui, Wuyi Wang
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Patent number: 6884821Abstract: Novel carboxylic acid derivatives of general formula (I), salts of the same, esters thereof, or hydrates of them, which are useful as insulin resistance improvers; and drugs containing the derivatives as the active ingredient. In said formula, R1 is hydrogen, hydroxyl, alkyl, or the like; L is a single bond, a double bond, alkylene, or the like; M is a single bond, alkylene, or the like; T is a single bond, alkylene, or the like; W is carboxyl, —CON(RW1)RW2, or the like; represents a single or double bond; X is oxygen, alkenylene, or the like; Y is an aromatic hydrocarbon group which may contain a heteroatom, or the like; and Z is an aromatic hydrocarbon group which may contain a heteroatom.Type: GrantFiled: September 29, 2000Date of Patent: April 26, 2005Assignee: Eisai Co., Ltd.Inventors: Masanobu Shinoda, Eita Emori, Fumiyoshi Matsuura, Toshihiko Kaneko, Norihito Ohi, Shunji Kasai, Hideki Yoshitomi, Kazuto Yamazaki, Sadakazu Miyashita, Taro Hibara, Takashi Seiki, Richard Clark, Hitoshi Harada
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Patent number: 6878706Abstract: Compounds according to the following formula (I): wherein the variables Q and R1 to R6 are as described herein, which reversibly inhibit the cysteine proteases, such as cathepsins K, S, F, L and B; pharmaceutical compositions containing such compounds, and method of treating diseases and pathological conditions exacerbated by these cysteine proteases such as, but not limited to rheumatoid arthritis, multiple sclerosis and other autoimmune diseases, osteoporosis, asthma, Alzheimer's disease, atherosclerosis and endometriosis.Type: GrantFiled: March 27, 2003Date of Patent: April 12, 2005Assignee: Boehringer Ingelheim Pharmaceuticals Inc.Inventors: Thomas A. Gilmore, Eugene Richard Hickey, Weimin Liu, Peter Allen Nemoto, Denice M. Spero
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Patent number: 6869939Abstract: The present invention provides aqueous parenteral formulations containing an antiarrhythmic agent, such as amiodarone, and a sulfoalkyl ether cyclodextrin. The liquid formulations are clear, sterilizable, and chemically and physically stable. The liquid formulations do not require a surfactant and do not precipitate upon dilution with distilled water or other pharmaceutically acceptable liquid carrier. The sulfoalkyl ether cyclodextrin-containing formulation provides significant advantages over other cyclodextrin-containing formulations of amiodarone. The formulation can be prepared in acidic, neutral and slightly basic medium while providing acceptable concentrations of amiodarone suitable for parenteral administration. An SAE-CD-containing formulation of amiodarone can be provided in liquid form or as a reconstitutable powder. Moreover, highly concentrated solutions exceeding 200 mg of amiodarone per mL can be prepared.Type: GrantFiled: May 4, 2002Date of Patent: March 22, 2005Assignee: CyDex, Inc.Inventors: Gerold L. Mosher, Karen T. Johnson, Atef A. Gayed
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Patent number: 6869972Abstract: The subject invention pertains to novel compounds (and salts thereof), and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns methods of making the novel compounds. The novel compounds are rapidly metabolized analogs of amiodarone, having the distinct and advantageous characteristic of being metabolized to a less lipophilic compound. This results in an improved safety profile. The new compounds have particular utility for treating life-threatening ventricular tachyarrhythmias, especially in patients with congestive heart failure (CHF). The compounds also provide effective management for ventricular arrhythmias and supraventricular arrhythmias, including atrial fibrillation and re-entrant tachyarrhythmias involving accessory pathways.Type: GrantFiled: March 11, 2004Date of Patent: March 22, 2005Assignee: ARYx TherapeuticsInventor: Pascal Druzgala
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Patent number: 6867218Abstract: The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).Type: GrantFiled: February 20, 2003Date of Patent: March 15, 2005Assignee: Novo Nordisk A/SInventors: John Patrick Mogensen, Per Sauerberg, Paul Stanley Bury, Lone Jeppesen, Ingrid Pettersson
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Patent number: 6861444Abstract: Compounds of the general formula (I): or a salt thereof, wherein R1 is hydrogen, hydroxyl or halogen; R2 is NHSO2CH3, SO2NHCH3 or the like; R5 and R6 each independently is hydrogen, C1-6 alkyl, optionally substituted phenyl or optionally substituted benzyl; X is NH, sulfur, oxygen or methylene; Y is oxygen, NR7, sulfur, methylene or a bond; and * represents an asymmetric carbon atom. The compounds are useful as a medicine for treating or preventing diabetes, obesity, hyperlipidemia, digestive diseases, depression or urinary disturbances.Type: GrantFiled: April 25, 2001Date of Patent: March 1, 2005Assignee: Asahi Kasei Pharma CorporationInventors: Shunichi Ikuta, Shiro Miyoshi, Kohei Ogawa
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Patent number: 6849659Abstract: A solid unit dosage form comprising citalopram, which is prepared by direct compression of a mixture of citalopram base or a pharmaceutically acceptable salt thereof and pharmaceutically acceptable excipients, or by filling of said mixture in a hard gelatine capsule. Large crystals of a pharmaceutical acceptable salt of citalopram and method for the manufacture of said large crystals.Type: GrantFiled: December 5, 2000Date of Patent: February 1, 2005Assignee: H. Lundbeck A/SInventors: Ken Liljegren, Per Holm, Ole Nielsen, Sven Wagner
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Patent number: 6849749Abstract: A method for the preparation of citalopram comprising reductive hydrolysis of a compound of Formula (IV): wherein R is a N,N-disubstituted amid group or an optionally substituted 4,5-dihydro-1,3-oxazol-2-yl group, and conversion of the resulting 5-formyl compound to citalopram.Type: GrantFiled: October 15, 2001Date of Patent: February 1, 2005Assignee: H. Lundbeck A/SInventor: Hans Petersen
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Patent number: 6849649Abstract: The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R1 is optionally substituted C1-6alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C1-6alkoxy, —NR2R3 or —NR4SO2R5; X is the linkage —(CH2)n— or —(CH2)q—O— (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C1-4alkoxy; hydroxy; hydroxy(C1-3alkyl); C3-7cycloalkyl; carbocyclyl; heterocyclyl; or by C1-4alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.Type: GrantFiled: October 28, 2003Date of Patent: February 1, 2005Assignee: Pfizer Inc.Inventors: Stephen Challenger, Andrew Simon Cook, Adam Thomas Gillmore, Donald Stuart Middleton, David Cameron Pryde, Alan Stobie
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Publication number: 20040266850Abstract: The invention relates to novel fungicidally active compound combinations ofType: ApplicationFiled: May 7, 2004Publication date: December 30, 2004Inventors: Ulrike Wachendorff-Neumann, Thomas Seitz, Herbert Gayer, Ulrich Heinemann, Bernd-Wieland Kruger, Wolfgang Kramer, Lutz Assmann
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Publication number: 20040266864Abstract: This invention relates to novel compositions of matter containing enantiomerically enriched (−)-desmethylcitalopram, (+)-didesmethylcitalopram, or (−)-didesmethylcitalopram or mixtures thereof in optimal ratios. Contrary to prior teachings, the enantiomerically enriched citalopram metabolites disclosed herein possess potent serotonin reuptake inhibitory activity, with minimal inhibitory effects on the reuptake of other known monoamines, e.g., norepinephrine (NE) or dopamine (DA). The present invention also discloses methods for treating disorders, dysfunctions and diseases for which inhibition of serotonin reuptake is therapeutically beneficial. In particular, the present invention discloses a method for treating various forms of depression with pharmaceutical compositions described herein.Type: ApplicationFiled: May 7, 2004Publication date: December 30, 2004Applicant: Sepracor Inc.Inventors: Larry R. Bush, Mark G. Currie, Q. Kevin Fang, Chris H. Senanayake