The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 548/204)
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Patent number: 7208506Abstract: The present invention relates to compounds of formula I wherein R1, R2 and R3 are defined herein, their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, medicaments containing them and their manufacture, as well as the use of the above compounds in the control or prevention of illnesses such as cancer.Type: GrantFiled: June 29, 2006Date of Patent: April 24, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Edward Boyd, Frederick Brookfield, Jonathan Gridley, Manfred Kubbies, Raymond Lau, Ulrike Reiff, Georg Tiefenthaler, Wolfgang von der Saal, Thomas von Hirschheydt, Timothy Woodcock
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Patent number: 7205413Abstract: Novel solvates and crystal polymorphs of Ritonavir are disclosed, as well as methods of making them. Specific solvates of the compound include a formamide solvate and a partially desolvated solvate. Also disclosed are methods of making previously known forms of Ritonavir. Methods of using the novel forms of Ritonavir for the treatment of diseases, such as HIV-infection, are disclosed, as are pharmaceutical compositions and unit dosage forms comprising the novel forms of Ritonavir.Type: GrantFiled: May 1, 2003Date of Patent: April 17, 2007Assignee: TransForm Pharmaceuticals, Inc.Inventors: Sherry L. Morissette, Orn Almarsson, Stephen Soukasene
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Patent number: 7196107Abstract: A compound of formula (I) or pharmaceutically acceptable salts and solvates thereof. R1 and R2 are independently H or C1-3alkyl, m is 0–3; X1 is NH, NCH3, O, S; R3, R4 and R5 are independently H, CH3, CF3, OCH3, allyl or halogen; X2 is (CR10R11)n wherein n is 1 or 2; R10 and R11 independently represent H, fluorine or C1-16alkyl; R26 and R27 are independently H, C1-3 alkyl or R26 and R27 together with the carbon atom to which they are bonded form a 3–5 membered cycloalklyl ring. R6 and R7 independently represent H, fluorine or C1-16alkyl; R9 is C1-6alkyl or CF3; One of Y and Z is N, the other is S or O; Each R8 independently represents CF3, OCH3, CH3 or halogen; y is O, 1, 2, 3, 4, 5.Type: GrantFiled: December 18, 2001Date of Patent: March 27, 2007Assignee: SmithKline Beecham CorporationInventors: Paul John Beswick, Vipulkumar Patel, Michael Lawrence Sierra
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Patent number: 7192979Abstract: This invention is directed to EP4 receptor selective prostaglandin agonists of the Formula I, wherein R2, X, Z and Q are as defined in the specification. This invention is also directed to pharmaceutical compositions containing those compounds. This invention is also directed to methods of treating conditions which present with low bone mass, particularly osteoporosis, frailty, an osteoporotic fracture, a bone defect, childhood idiopathic bone loss, alveolar bone loss, mandibular bone loss, bone fracture, osteotomy, bone loss associated with periodontitis, or prosthetic ingrowth in a mammal comprising administering those compounds.Type: GrantFiled: September 23, 2003Date of Patent: March 20, 2007Assignee: Pfizer Inc.Inventors: Kimberly O. Cameron, Bruce A. Lefker
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Patent number: 7189858Abstract: N-substituted carbamoyloxyalkyl-azolium derivatives Which have antifungal activity and are useful for the treatment of fungal diseases.Type: GrantFiled: September 3, 2004Date of Patent: March 13, 2007Assignee: Basilea Pharmaceutica AGInventors: Hiroshi Fukuda, Tadakatsu Hayase, Eisaku Mizuguchi, Nobuo Shimma, Jun Ohwada, Nobuhiro Oikawa, Masahiro Sakaitani, Masao Tsukazaki, Isao Umeda
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Patent number: 7189857Abstract: A method for producing a compound represented by the general formula (I-A) or the general formula (I-B), comprising the following step: wherein R1 is an optionally substituted lower alkyl, and the like; R2 is a lower alkyl or an optionally substituted aralkyl, and the like; R3 is a lower alkyl, characterized in that a compound represented by the general formula (II-A) or the general formula (II-B) is treated with thionyl chloride.Type: GrantFiled: November 25, 2003Date of Patent: March 13, 2007Assignee: Shionogi & Co., Ltd.Inventors: Makoto Kobayashi, Haruo Koike, Masahiko Nagai
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Patent number: 7183416Abstract: A new crystalline polymorph of ritonavir and methods for its use and preparation are disclosed.Type: GrantFiled: July 29, 2004Date of Patent: February 27, 2007Assignee: Abbott LaboratoriesInventors: Sanjay R. Chemburkar, Ketan Patel, Harry O. Spiwek
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Patent number: 7183294Abstract: The invention relates to indole derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The indole derivatives according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.Type: GrantFiled: March 12, 2004Date of Patent: February 27, 2007Assignee: Pfizer Inc.Inventors: Alan Daniel Brown, Justin Stephen Bryans, Mark Edward Bunnage, Paul Alan Glossop, Charlotte Alice Louise Lane, Russell Andrew Lewthwaite, Simon John Mantell
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Patent number: 7173137Abstract: Epothilone A, epothilone B, analogs of epothilone and libraries of epothilone analogs are synthesized. Epothilone A and B are known anticancers agents that derive their anticancer activity by the prevention of mitosis through the induction and stabilization of microtubulin assembly. The analogs of epothilone are novel. Several of the analogs are demonstrated to have a superior cytotoxic activity as compared to epothilone A or epothilone B as demonstrated by their enhanced ability to induce the polymerization and stabilization of microtubules.Type: GrantFiled: December 9, 2003Date of Patent: February 6, 2007Assignee: The Scripps Research InstituteInventors: Kyriacos C. Nicolaou, Yun He, Sacha Ninkovic, Joaquin Pastor, Frank Roschangar, Francisco Sarabia, Hans Vallberg, Dionisios Vourloumis, Nicolas Winssinger, Zhen Yang, Nigel Paul King, Maurice Raymond Verschoyle Finlay
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Patent number: 7169930Abstract: Designed epoxide and cyclopropane epothilone analogs with substituted side-chains are disclosed and characterized with respect to their biological activities against a series of human cancer cell lines. Among the several bioactive analogs, the epothilone B analog with a thiomethyl thiazole ring stands out as the most potent.Type: GrantFiled: August 4, 2003Date of Patent: January 30, 2007Assignee: The Scripps Research InstituteInventors: Kyriacos C. Nicolaou, Andreas Ritzen, Kenji Namoto
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Patent number: 7153878Abstract: The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts thereof, Formula I. (Formula I); wherein: (a) R5 is selected from the group consisting of (C1–C6)alkyl, (C1–C6)alkenyl, aryl (C0–C4)alkyl, aryloxy(C0–C4)alkyl, arylthio(C0–C4)alkyl, and further wherein when R5 is alkyl, R5 can optionally combine with W to form a 6 membered cycloheteroalkyl ring that is fused with the oxazole or thiazole ring to which the R5 group is attached; (b) R9 is selected from the group consisting of C1–C5alkyl, C1–C5alkenyl, and arylC0–C3alkyl.Type: GrantFiled: February 13, 2003Date of Patent: December 26, 2006Assignee: Eli Lilly and CompanyInventors: Scott Eugene Conner, James Allen Knobelsdorf, Nathan Bryan Mantlo, Jeffrey Michael Schkeryantz, Quanrong Shen, Alan M Warshawsky, Guoxin Zhu
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Patent number: 7153946Abstract: A molecular conjugate is provided having the formula: wherein R1 is a de-hydroxyl or de-amino moiety respectively of a hydroxyl-bearing or amino-bearing biologically active molecule or an analog or derivative thereof, and Z is —O— or —NH—, respectively, Y is a straight or branched alkyl having 1 to 20 carbons that may be optionally substituted with one or more phenyl, a cycloalkyl optionally substituted with one or more alkyl or phenyl, or an aromatic group optionally substituted with one or more alkyl groups, electron-withdrawing groups, or electron-donating groups; and R2 is —CH?CH(W), —CH(OH)CH(OH)W, or —C(O)H, where W can be H, a straight or branched alkyl having 1 to 20 carbons that may be optionally substituted with one or more phenyl, a cycloalkyl optionally substituted with one or more alkyl or phenyl, or an aromatic group optionally substituted with one or more alkyl groups, electron-withdrawing groups, or electron-donating groups.Type: GrantFiled: November 24, 2004Date of Patent: December 26, 2006Assignee: Tapestry Pharmaceuticals, Inc.Inventors: James D. McChesney, Madhavi C. Chander, Teruna J. Siahaan, Christine R. Xu, Sterling K. Ainsworth
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Patent number: 7153815Abstract: A insecticide characterized by containing as active ingredient a hydrazone derivative of formula (I) wherein A and Q are an aryl or a heterocyclic group, W is oxygen atom, an aminylene, an alkylene group, an oxyalkylene group or an alkyleneoxy, X1 and X2 are hydrogen atom, an alkyl, an alkenyl, an alkynyl, an aryl, a heterocyclic group, formyl, an acyl, an alkoxycarbonyl, an aryloxycarbonyl, a heterocyclic oxycarbonyl, an alkylsulfinyl, an arylsulfinyl, a heterocyclic sulfinyl, an alkylsulfonyl, an arylsulfonyl or a heterocyclic sulfonyl, Y is oxygen atom or sulfur atom, Z is hydrogen atom, a halogen atom, cyano, an alkyl, an alkenyl, an alkynyl, an amino, an alkoxy or an alkylthio, the substituents may be substituted; and novel hydrazon derivatives.Type: GrantFiled: January 10, 2003Date of Patent: December 26, 2006Assignee: Nihon Nohyaku Co., Ltd.Inventors: Shinji Kawata, Shuko Okui, Shigeru Suzuki, Toshiki Fukuchi, Akiyuki Suwa
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Patent number: 7148359Abstract: A new crystalline polymorph of ritonavir and methods for its use and preparation are disclosed.Type: GrantFiled: May 4, 2005Date of Patent: December 12, 2006Assignee: Abbott LaboratoriesInventors: Sanjay R. Chemburkar, Ketan Patel
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Patent number: 7144904Abstract: Composition, article of manufacture for and method of treating malaria in a human having an infestation of Plasmodium protozoans are described. The method comprises administering a therapeutically-effective amount of a compound of formula (I) or (IV), i.e. sufficient quantity to reduce the population of Plasmodium. The composition of the invention is a compound of formula (I) or (IV) with a pharmaceutical excipient. The article of manufacture is the composition in combination with labeling for treating malaria. The substituents are detailed in the specification.Type: GrantFiled: November 19, 2004Date of Patent: December 5, 2006Assignee: University of Florida Research Foundation, Inc.Inventor: Raymond J. Bergeron, Jr.
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Patent number: 7141672Abstract: 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: January 8, 2004Date of Patent: November 28, 2006Assignee: WyethInventor: Michael S. Malamas
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Patent number: 7141533Abstract: The present invention relates to novel compounds of the formula (I) in which A, B, W, G and Het are each as defined in the description, to a plurality of processes for their preparation and to their use as pesticides and herbicides.Type: GrantFiled: May 21, 2004Date of Patent: November 28, 2006Assignee: Bayer CropScience AGInventors: Reiner Fischer, Thomas Bretschneider, Axel Trautwein, Astrid Ullmann, Mark Wilhelm Drewes, Christoph Erdelen, Peter Dahmen, Dieter Feucht, Rolf Pontzen
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Patent number: 7125863Abstract: Compounds according to formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is CO, CH2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1–5 are new. The compounds of the invention are inhibitors of dipeptidyl peptidase IV.Type: GrantFiled: April 26, 2001Date of Patent: October 24, 2006Assignee: Ferring BVInventors: David Michael Evans, Gary Robert William Pitt
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Patent number: 7105556Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2, X3 and X4 are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.Type: GrantFiled: May 22, 2002Date of Patent: September 12, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Peter T. Cheng, Yoon Jeon, Wei Wang
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Patent number: 7105551Abstract: The present invention provides compounds of formula (I).Type: GrantFiled: December 19, 2001Date of Patent: September 12, 2006Assignee: SmithKline Beecham CorporationInventors: Rodolfo Cadilla, Romain Luc Marie Gosmini, Millard Hurst Lambert, III, Michael Lawrence Sierra
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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: 7101702Abstract: The invention relates to a new process for concentrating epothilones in culture media, a new process for the production of epothilones, a new process for separating epothilones A and B and a new strain obtained by mutagenesis for the production of epothilones, as well as aspects related thereto. New crystal forms of epothilone B are also described.Type: GrantFiled: June 12, 2003Date of Patent: September 5, 2006Assignee: Novartis AGInventors: Hans Hofmann, Marion Mahnke, Klaus Memmert, Frank Petersen, Thomas Schupp, Ernst Kusters, Michael Mutz
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Patent number: 7098228Abstract: The present invention provides compounds of formula I as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R4, A and n have the significance given in the specification. The compounds or their salts may be administered to a patient for treating non-insulin dependent diabetes mellitus.Type: GrantFiled: November 21, 2003Date of Patent: August 29, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Alfred Binggeli, Uwe Grether, Hans Hilpert, Georges Hirth, Bernd Kuhn, Hans-Peter Maerki, Markus Meyer, Peter Mohr
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Patent number: 7094792Abstract: The present invention relates to compounds with the formula (I) and also to pharmaceutical compositions comprising the compounds, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.Type: GrantFiled: November 22, 2002Date of Patent: August 22, 2006Assignee: Biovitrum ABInventors: Tjeerd Barf, Rikard Emond, Guido Kurz, Marianne Nilsson, Jerk Vallgårda, Lian Zhang
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Patent number: 7091225Abstract: Compounds of formula (I) and pharmaceutically acceptable salts, solvates and hydrolysable esters thereof wherein X is O or S X1 is O or S; X is S or O; R1 and R2 are independently H, methyl, or halogen; R4 and R5 are independently H or C1-3 alkyl or R4 and R5 may, together with the carbon atom to which they are bonded, form a 3–5 membered cycloalkyl ring; R6 and R7 are independently H, C1-3 alkyl, or allyl; each R3 is independently halogen, C1-6 straight or branched alkyl, or CF3; and y is 0, 1, 2, 3, 4 or 5 act as hPPAR alpha agonists.Type: GrantFiled: December 18, 2001Date of Patent: August 15, 2006Assignee: SmithKline Beecham CorporationInventor: Michael Lawrence Sierra
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Patent number: 7078422Abstract: A phenylacetic acid derivative represented by the general formula (II) (wherein R11 and R12 each represents hydrogen, C1-8 alkyl, C1-8 alkoxy, C1-8 alkyl substituted by one to three halogen atoms, an optionally substituted phenyl, naphthyl, pyridyl, thienyl, or furyl group, etc.; X1 and Z1 each represents —C(?O)—, —C(?O)NH, —NHC(?O)—, —CH?CH—, a bond, etc.Type: GrantFiled: February 19, 2002Date of Patent: July 18, 2006Assignee: Nippon Chemiphar Co., Ltd.Inventors: Shogo Sakuma, Tsuyoshi Endo, Takashi Kanda, Seiichiro Masui
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Patent number: 7053069Abstract: Pharmaceutical compositions containing C-21 modified epothilone derivatives, methods for their preparation and dosing regimen for administration of these epothilone compounds are provided. The compositions are stable and readily prepared for administration by dissolution in aqueous vehicles suitable for intravenous administration. A process for formulating C-21 modified epothilone derivatives for oral and parenteral administration is disclosed.Type: GrantFiled: May 13, 2003Date of Patent: May 30, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Francis Y. F. Lee, Thomas A. Haby, Vijay H. Naringrekar, Krishnaswamy S. Raghavan, Miriam K. Franchini
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Patent number: 7045532Abstract: ACE-2 inhibitors for the treatment of body weight and related disorders are disclosed. ACE-2 inhibitors include peptides and small molecules. Examples of small molecule ACE-2 inhibitors include compounds of formula (I): Z-???(I) Wherein Z is a zinc coordinating moiety and ? is an amino-acid mimicking moiety, and pharmaceutically acceptabale salts thereof. Methods of using the inhibitors and pharmaceutical compositions containing the inhibitors to treat a body weight disorder, to decrease appetite, to increase muscle mass, to decrease body fat, to treat diabetes and to treat a state associated with altered lipid metabolism, are also described.Type: GrantFiled: October 31, 2001Date of Patent: May 16, 2006Assignee: Millennium Pharmaceuticals, Inc.Inventors: Susan L. Acton, Timothy D. Ocain, Alexandra E. Gould, Natalie A. Dales, Bing Guan, James A. Brown, Michael Patane, Vivek J. Kadambi, Michael Solomon, Alain Stricker-Krongrad
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Patent number: 7041690Abstract: The present invention provides compounds of Formula I, compositions and methods that are useful for treating viral infections and associated diseases, particularly HCV infections and associated diseasesType: GrantFiled: June 30, 2003Date of Patent: May 9, 2006Assignee: Pharmacia & Upjohn Company, LLCInventors: Barry Craig Finzel, Hua Gao, Meredith L. Greene, Rebecca J. Gross, Richard Allen Nugent, Jeffrey A. Pfefferkorn
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Patent number: 7030139Abstract: Compounds of general formula (I), 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 painType: GrantFiled: April 18, 2002Date of Patent: April 18, 2006Assignee: AstraZeneca ABInventors: Yun-Xing Cheng, Miroslaw Tomaszewski, Christopher Walpole, Hua Yang
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Patent number: 7030239Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formula (XII) useful in treating Alzheimer's disease and other similar diseases.Type: GrantFiled: May 18, 2004Date of Patent: April 18, 2006Assignee: Elan Pharmaceuticals, Inc.Inventors: Roy Hom, Shumeye S. Mamo, Jay Tung, Andrea Gailunas, Varghese John, Lawrence Y. Fang
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Patent number: 7022719Abstract: The present invention relates to compositions and methods for inhibiting and reversing nonenzymatic cross-linking (protein aging). Accordingly, compositions are disclosed which comprise an agent capable of inhibiting the formation of advanced glycosylation endproducts of target proteins, and which additionally reverse pre-formed crosslinks in the advanced glycosylation endproducts by cleaving alpha-dicarbonyl-based protein crosslinks present in the advanced glycosylation endproducts. Certain useful agents are thiazolium salts. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated. A novel immunoassay for detection of the reversal of the nonenzymatic crosslinking is also disclosed.Type: GrantFiled: April 18, 2003Date of Patent: April 4, 2006Assignee: Alteon, Inc.Inventors: Anthony Cerami, Peter C. Ulrich, Dilip R. Wagle, San-Bao Hwang, Sara Vasan, John J. Egan
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Patent number: 7001916Abstract: Disclosed are epothilone compounds of formula I, which are useful as pharmaceutical compounds for treating, for example, malignant tumors and chronic inflammatory diseases and are useful in anti-angiogenesis therapy.Type: GrantFiled: February 11, 2000Date of Patent: February 21, 2006Assignee: Schering, AGInventors: Ulrich Klar, Werner Skuballa, Bernd Buchmann, Wolfgang Schwede, Michael Schirner
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Patent number: 6998256Abstract: Methods are provided for purification of epothilone D and epothilone D analogs from epothilone producing cells such as, for example, Sorangium cellulosum and Myxococcus xanthus (recombinant). Epothilone can be purified from fermentation broth, for example by using resins, chromatography, and crystallization. Epothilone D can be crystallized from a binary solvent system in which water is the forcing solvent.Type: GrantFiled: September 19, 2001Date of Patent: February 14, 2006Assignee: Kosan Biosciences, Inc.Inventor: Robert L. Arslanian
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Patent number: 6989450Abstract: The present invention relates to methods for use in producing epothilones and analogs and derivatives thereof. A general method according to the present invention broadly comprises performing an aldol condensation of a first compound with a second compound thereby to form a third compound selected from the formulas: and stereoisomers thereof, and performing a macrolactonization of the third compound. The present invention also provides chemical compounds, and methods for producing such chemical compounds, that are useful in producing epothilones and analogs and derivatives thereof.Type: GrantFiled: October 15, 2001Date of Patent: January 24, 2006Assignee: The University of MississippiInventor: Mitchell A. Avery
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Patent number: 6958401Abstract: A method for making epothilones and epothilone analogs is described, as are novel compounds made by the method. One embodiment of the method was used to synthesize epothilone B by a convergent approach that entailed Wittig coupling of an ylide derived from phosphonium bromide with an aldehyde. The former was prepared from propargyl alcohol by a nine-step pathway which installed both trisubstituted double bonds with clean Z configuration. Macrolactonization of a resulting seco acid provided the following intermediate diene epothilone analog. Selective saturation of the 9,10-olefin and subsequent epoxidation provided epothilone B.Type: GrantFiled: January 27, 2003Date of Patent: October 25, 2005Assignee: The State of Oregon acting by and through the State Board of Higher Education on behalf of Oregon State UniversityInventors: James David White, Rich Garrett Carter, Kurt Frederick Sundermann
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Patent number: 6949566Abstract: A compound of the formula (I): wherein R1 is hydroxy and the like; R2 is optionally substituted lower alkyl and the like; R3 is hydrogen atom and the like; R4 is optionally substituted arylene and the like; R5 is a group represented by the formula: and the like; R6 is optionally substituted aryl and the like, its optically active substance, its prodrug, their pharmaceutically acceptable salt, or solvate thereof and metalloproteinase inhibitors containing them.Type: GrantFiled: September 28, 2001Date of Patent: September 27, 2005Assignee: Shionogi & Co. Ltd.Inventors: Fumihiko Watanabe, Yoshinori Tamura
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Patent number: 6946561Abstract: The invention relates to a desorption process for epothilones, especially epothilone A and/or epothilone B, from resins and new production, work-up or purification processes or manufacturing methods for epothilones comprising said desorption process, as well as the use of certain solvents for the desorption of epothilones from resins.Type: GrantFiled: December 5, 2001Date of Patent: September 20, 2005Assignee: Novartis AGInventors: Ernst Küsters, Heinz Unternährer
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Patent number: 6936628Abstract: The invention relates to methods of increasing the bioavailability of orally administered epothilones. Epothilones administered by the methods of the invention are sufficiently bioavailable to have a pharmacological effect. The invention further relates to pharmaceutical compositions, pharmaceutical dosage forms, and kits for use in the methods of the invention.Type: GrantFiled: April 1, 2003Date of Patent: August 30, 2005Assignee: Bristol-Myers Squibb CompanyInventor: Francis Y. F. Lee
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Patent number: 6936627Abstract: The invention describes novel nitrosated and/or nitrosylated H2 receptor antagonist compounds, and novel compositions comprising at least one H2 receptor antagonist compound that is optionally substituted with at least one NO and/or NO2 group, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase and/or at least one nonsteroidal antiinflammatory drug, antacid, bismuth-containing reagent or anti-viral agent.Type: GrantFiled: October 29, 2002Date of Patent: August 30, 2005Assignee: NitroMed, Inc.Inventors: David S. Garvey, L. Gordon Letts, Chia-En Lin, Tiansheng Wang
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Patent number: 6936602Abstract: Compounds of the general formula (I): or salts thereof, which exhibit CCR5 antagonism and exert preventive and therapeutic effects against HIV infections: wherein R1 is a 5- to 6-membered aromatic ring which bears a substituent represented by the general formula: R-Z1-X-Z2- (wherein R1 is hydrogen or optionally substituted hydrocarbyl; X is optionally substituted alkylene; and Z1 and Z2 are each a heteroatom) and may be further substituted, with R being optionally bonded to the aromatic ring to form another ring; Y is optionally substituted imino; and R2 and R3 are each optionally substituted aliphatic hydrocarbyl or an optionally Substituted hetero-alicyclic group.Type: GrantFiled: June 15, 2000Date of Patent: August 30, 2005Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuru Shiraishi, Masanori Baba, Yoshio Aramaki, Naoyuki Kanzaki, Osamu Nishimura
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Patent number: 6936719Abstract: Compounds of formula (I) are useful as inhibitors of trypsin like serine protease enzymes such as thrombin, factor VIIa, factor Xa, TF/FVIIa, and trypsin. These compounds could be useful to treat and/or prevent clotting disorders, and as anticoagulating agents.Type: GrantFiled: December 18, 2003Date of Patent: August 30, 2005Assignee: BioCryst Pharmaceuticals, Inc.Inventors: Yarlagadda S. Babu, R. Scott Rowland, Pooran Chand, Pravin L. Kotian, Yahya El-Kattan, Shri Niwas
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Patent number: 6930187Abstract: An improved method of synthesis of 21-amino epothilone derivatives which provides a one-pot conversion of 21-hydroxy epothilones to highly desirable 21-amino epothilones in high yield.Type: GrantFiled: February 13, 2003Date of Patent: August 16, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Denis Favreau, Joydeep Kant, Kathia Levesque, Shaopeng Wang, Zhengrong Guo, Brian Leslie James
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Patent number: 6924300Abstract: To provide a novel oxyiminoalkanoic acid derivative which has excellent hypoglycemic and hypolipidemic actions and which is used for the prevention or treatment of diabetes mellitus, hyperlipemia, insulin insensitivity, insulin resistance and impaired glucose tolerance.Type: GrantFiled: December 27, 2002Date of Patent: August 2, 2005Assignee: Takeda Chemical Industries, Ltd.Inventors: Yu Momose, Hiroyuki Odaka, Hiroshi Imoto, Hiroyuki Kimura, Junichi Sakamoto
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Patent number: 6916813Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts thereof, are useful for modulating mitochondrial F1F0 ATPase activity and treating ischemic conditions including myocardial infarction, congestive heart failure, and cardiac arrhythmias.Type: GrantFiled: December 10, 2002Date of Patent: July 12, 2005Assignee: Bristol-Myers Squibb Co.Inventors: Karnail S. Atwal, Gary J. Grover, Charles Z. Ding, Philip D. Stein, John Lloyd, Saleem Ahmad, Lawrnce G. Hamann, David Green, Francis N. Ferrara
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Patent number: 6903131Abstract: Disclosed are compounds of the formula (I) or a pharmaceutically acceptable salt or solvate thereof. The compounds are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.Type: GrantFiled: October 11, 2002Date of Patent: June 7, 2005Assignees: Schering Corporation, Pharmacopeia Drug Discovery, Inc.Inventors: Arthur G. Taveras, Michael Dwyer, Johan A. Ferreira, Viyyoor M. Girijavallabhan, Jianping Chao, John J. Baldwin, J. Robert Merritt, Ge Li
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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: 6900331Abstract: The present invention provides the following new compounds: (R)-C14-methyl-epothilone B, (S)-C14-methyl-epothilone B, (S)-C14-methyl-epothilone D, and (R)-C14-methyl-epothilone D and methods for synthesizing these compounds.Type: GrantFiled: February 28, 2003Date of Patent: May 31, 2005Assignee: University of Notre DameInventors: Richard E. Taylor, Yue Chen
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Patent number: RE39356Abstract: The present invention relates to a process for the preparation of epothilone analogs by initially forming novel ring-opened epothilones and carrying out a macrolactamization reaction thereon. The subject process is amenable to being carried out in a single reaction vessel without isolation of the intermediate compound and provides at least about a three-fold increase in yield over prior processes for preparing the desired epothilone analogs.Type: GrantFiled: February 11, 2005Date of Patent: October 17, 2006Assignee: Bristol-Myers Squibb Co.Inventors: Wen Sen Li, John E. Thornton, Zhenrong Guo, Shankar Swaminathan, Robert M. Borzilleri, Soong-Hoon Kim, Denis Favreau
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Patent number: RE39575Abstract: The present invention is directed to chemical compositions of substituted thioacetamides, processes for the preparation thereof and uses of the compositions in the treatment of diseases.Type: GrantFiled: November 23, 2004Date of Patent: April 17, 2007Assignee: Cephalon, Inc.Inventors: Edward R. Bacon, Sankar Chatterjee, Derek Dunn, John P. Mallamo, Jeffry L. Vaught, Matthew S. Miller