Chalcogen Bonded Directly To A Piperazine Ring Carbon Patents (Class 514/255.02)
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Publication number: 20070270434Abstract: The present invention relates to compounds and methods useful as inhibitors of PPAR, particularly PPAR?, and for the treatment or prevention of PPAR-mediated diseases, including metabolic diseases.Type: ApplicationFiled: May 16, 2007Publication date: November 22, 2007Applicant: KALYPSYS, INC.Inventors: James W. Malecha, Stewart A. Noble, Sergio G. Duron, Andrew Lindstrom, Andrew Shiau, Steven Govek
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Patent number: 7288545Abstract: This invention relates to a method for treating an angiogenesis-related disease. The method includes administering to a subject in need thereof an effective amount of a piperazinedione compound having the formula: In the above formula, each of and , independently, is a single bond or a double bond; A is H or CH(RaRb) when is a single bond, or C(RaRb) when is a double bond; Z is CH(RcRd) when is a single bond, or C(RcRd) when is a double bond; each of R1 and R2, independently, is H, C(O)Re, C(O)ORe, C(O)NReRf, or SO2Re; and each of Ra, Rb, Rc, Rd, Re, and Rf, independently, is H, C1-C6 alkyl, aryl, heteroaryl, C3-C8 cycloalkyl, or C3-C8 heterocycloalkyl; or Ra and Rb taken together are C3-C8 cycloalkyl, C3-C8 heterocycloalkyl, aryl, or heteroaryl; or R1 and Ra or R1 and Rb taken together are C3-C8 cycloalkyl, C3-C8 heterocycloalkyl, aryl, or heteroaryl; provided that one of Rc and Rd is aryl or heteroaryl.Type: GrantFiled: October 20, 2003Date of Patent: October 30, 2007Assignee: AngioRx CorporationInventors: Che-Ming Teng, Hui-Po Wang, Eric I. C. Li, On Lee, Jih-Hwa Guh, Huei-Ting Chen, Ya-Bing Fan, Ya-Lan Chen
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Patent number: 7265108Abstract: Compounds represented by the following general formula: [wherein X1, X2, X3 and X4 each independently represent a single bond, C1-6 alkylene, etc.; A2 represents optionally substituted phenyl, etc.; A1 represents an optionally substituted 5- to 7-membered heterocyclic group containing —C(=Q1)- (wherein Q1 represents oxygen, sulfur or ?N—R11 (wherein R11 represents hydrogen or C1-6 alkyl)) and nitrogen, etc.; and Z1 represents piperidin-diyl, etc.], salts thereof and hydrates of the foregoing.Type: GrantFiled: July 1, 2005Date of Patent: September 4, 2007Assignee: Eisai Co., Ltd.Inventors: Fumihiro Ozaki, Mutsuko Ono, Koki Kawano, Yoshihiko Norimine, Tatsuhiro Onogi, Takashi Yoshinaga, Kiyoaki Kobayashi, Hiroyuki Suzuki, Hiroe Minami, Kohei Sawada
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Patent number: 7223751Abstract: The present invention relates to a novel sulfonamide derivatives and novel intermediates thereof, preparation thereof, and a pharmaceutical composition comprising the same, and more particularly, to novel sulfonamide derivatives and intermediates thereof that are used as angiogenesis controlling material and that can inhibit overexpression of matrix metalloproteinase that decomposes protein constituents in extracellular and basement membranes of connective tissues, and preparation methods thereof, and a pharmaceutical composition comprising the same.Type: GrantFiled: April 24, 2002Date of Patent: May 29, 2007Assignee: Kolon Ind. Inc.Inventors: Yong-Jun Chung, Kyeong-Ho Lee, Youn-Chul Kim, Ho-Jin Park
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Patent number: 7119203Abstract: This invention is directed generally to proteinase (also known as “protease”) inhibitors, and, more particularly, to piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. Such hydroxamic acids generally correspond in structure to the following formula: (wherein A1, A2, Y, E1, E2, E3, and Rx are as defined in this specification), and further include salts of such compounds. This invention also is directed to compositions of such hydroxamic acids, intermediates for the syntheses of such hydroxamic acids, methods for making such hydroxamic acids, and methods for treating conditions (particularly pathological conditions) associated with MMP activity and/or aggrecanase activity.Type: GrantFiled: April 25, 2003Date of Patent: October 10, 2006Assignee: Pharmacia CorporationInventors: Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, David L. Brown, Jeffery N. Carroll, Yiyuan Chen, Yvette M. Fobian, John N. Freskos, Alan F. Gasiecki, Margaret L. Grapperhaus, Robert M. Heintz, Susan L. Hockerman, Darren J. Kassab, Ish K. Khanna, Stephen A. Kolodziej, Mark A. Massa, Joseph J. McDonald, Brent V. Mischke, Deborah A. Mischke, Patrick B. Mullins, Mark A. Nagy, Monica B. Norton, Joseph G. Rico, Michelle A. Schmidt, Nathan W. Stehle, John J. Talley, William F. Vernier, Clara I. Villamil, Lijuan J. Wang, Thomas A. Wynn
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Patent number: 7115611Abstract: This invention relates to compounds of the formula wherein one of R5, R6 and R7 is and X1, X2, Y1 to Y4, R1 to R13 and m and n are defined in the description, and to all enantiomers and pharmaceutically acceptable salts and/or esters thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are modulated by PPAR? and/or PPAR? agonists.Type: GrantFiled: October 29, 2004Date of Patent: October 3, 2006Assignee: Hoffmann-la Roche Inc.Inventors: Jean Ackermann, Johannes Aebi, Alfred Binggeli, Uwe Grether, Georges Hirth, Bernd Kuhn, Hans-Peter Maerki, Markus Meyer, Peter Mohr, Matthew Blake Wright
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Patent number: 7105507Abstract: The present invention relates compounds of formula (I), wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of formulae: (a), (b), (c), (d), and (e); and R1, R2, R3, R4, R5, R6, R7, R13, R14, R15, R16, R17, R21a and R21b are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.Type: GrantFiled: May 16, 2001Date of Patent: September 12, 2006Assignee: Merck Sharp & Dohme LimitedInventors: Jose Luis Castro Pineiro, Kevin Dinnell, Jason Matthew Elliott, Gregory John Hollingworth, Duncan Edward Shaw, Christopher John Swain
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Patent number: 7094778Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: wherein X, Y, and Z are O, S or NR5, and the other substituents are as defined in the specification; and prodrugs, individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.Type: GrantFiled: October 14, 2003Date of Patent: August 22, 2006Assignee: Syntex (U.S.A.) LLCInventors: Charles Alois Dvorak, Lawrence Emerson Fisher, Keena Lynn Green, Ralph New Harris, III, Hans Maag, Anthony Prince, David Bruce Repke, Russell Stephen Stabler
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Patent number: 6989383Abstract: The present invention relates to methods of treating cancer using a combination of a compound which is an antineoplastic agent and a compound which is a inhibitor of prenyl-protein transferase, which methods comprise administering to said mammal, either sequentially in any order or simultaneously, amounts of at lest two therapeutic agents selected from a group consisting of a compound which is an antineoplastic agent and a compound which is an inhibitor or prenyl-protein transferase. The invention also relates to methods of preparing such compositions.Type: GrantFiled: June 4, 1998Date of Patent: January 24, 2006Assignee: Sloan-Kettering Institute For Cancer ResearchInventors: Neal Rosen, Laura Sepp-Lorenzino, Mark M. Moasser, Allen I. Oliff, Jackson B. Gibbs, Nancy Kohl, Samuel L. Graham, George C. Prendergast
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Patent number: 6972287Abstract: The present invention provides a method of treating Alzheimer's disease using a compound of Formula (I). Also provided is a method of inhibiting the aggregation of amyloid proteins using a compound of the Formula (I) and a method of imaging amyloid deposits, as well as new compounds of Formula (I).Type: GrantFiled: May 31, 2000Date of Patent: December 6, 2005Assignee: Pfizer Inc.Inventors: Corinne Elizabeth Augelli-Szafran, Mark Robert Barvian, Christopher Franklin Bigge, Shelly Ann Glase, Shunichiro Hachiya, John Steven Kiely, Takenori Kimura, Yingjie Lai, Annette Theresa Sakkab, Mark James Suto, Larry Craswell Walker, Tomoyuki Yasunaga, Nian Zhuang
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Patent number: 6967202Abstract: The invention provides a method of synthesizing a diketopiperazine of the formula: wherein: R1 is —CH2COR3, or —CH2CH2COR3; R2 is the side chain of an amino acid selected from the group consisting of glycine, alanine, valine, leucine, isoleucine, serine, threonine, aspartic acid, asparagine, glutamic acid, glutamine, lysine, hydroxylysine, histidine, arginine, phenylalanine, tyrosine, tryptophan, thyroxine, cysteine, methionine, norvaline and ornithine; R3 is —OH, —NH2, —OR4, —NHR4, or —NR4R4; and each R4 is independently an alkyl, aryl, alkylaryl, or arylalkyl.Type: GrantFiled: August 2, 2001Date of Patent: November 22, 2005Assignee: DMI Biosciences, Inc.Inventors: Nagaraja K. R. Rao, Stephen Turner
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Patent number: 6916816Abstract: Disclosed are compounds of formula (I) wherein: L is (a) optionally substituted by replacement of one or more of the hydrogen atoms on the phenanthrene ring system by one or more groups other than hydrogen; A is CH2, SO2 or C?O; X is CO2H, PO3H2, PO2H2, PO2HR5, PO2HOR5, SO3H, SO2H, or tetrazole; and R1, R2, R3, R4 and R5 are independently selected from H, alkyl, alkenyl, alkynyl, aryl and aralkyl; or a pharmaceutically acceptable acid salt or base addition salt or an in vivo hydrolysable ester or amide thereof.Type: GrantFiled: December 18, 2000Date of Patent: July 12, 2005Assignees: The Board of Regents of the University of Nebraska, The University of BristolInventors: Daniel T. Monaghan, David E. Jane, Heong Wai Tse
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Patent number: 6900213Abstract: The invention relates to bisaryl derivatives of the formula I, wherein (R,R) is selected from (H,H), O, (H,CH3), (H,OH) and (H,CN); Ar is substituted phenyl and A is a group of formula II, III, IV or V: An example is (3S,6S)-1-N-(7-phenylheptyl)-3-(4-(3,4,5-trimethoxyphenyl)benzyl)-4-N-methyl-6-methyl-2,5-dioxo-1,4-piperazine: The compounds of the invention have FSH receptor modulatory activity and can be used for the control of fertility, for contraception or for treatment of hormone-dependent disorders.Type: GrantFiled: July 21, 2003Date of Patent: May 31, 2005Assignee: Pharmacopeia Drug Discovery, Inc.Inventors: Tao Guo, Koc-Kan Ho, Edward McDonald, Roland Ellwood Dolle, Kurt W. Saionz, Steven G. Kultgen, Ruiyan Liu, Guizhen Dong, Peng Geng, Anton Egbert Peter Adang, Nicole Corine Renee Van Straten
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Patent number: 6878707Abstract: Compounds of formula (I) wherein R2—C, R3—C, R4—C or R5—C may be replaced by N; and wherein n is 1, 2 or 3; R1 is aryl, heteroaryl or (aryl or heteroaryl)-lower alkoxy; R2, R3, R4 and R5 are independently hydrogen, lower alkyl, lower alkoxy, halo, trifluoromethyl or cyano; R6 is (i) or (ii) m is 1, 2 or 3; R7 is hydrogen, lower alkyl (aryl or heteroaryl)-lower alkyl, lower alkoxy, (aryl or heteroaryl)-lower alkoxy, hydroxy, oxo, lower alkylenedioxy or lower alkanoyloxy; W is O, S or NR8; R8 is —CORa, (iii), —COORd, —SO2Re, hydrogen, optionally substituted lower alkyl, aryl, heteroaryl or (aryl or heteroaryl)-lower alkyl; Ra, Rd and Re are independently optionally substituted lower alkyl, cycloalkyl, adamantyl, aryl, heteroaryl or (aryl or heteroaryl)-lower alkyl; Rb and Rc are independently hydrogen, cycloalkyl, optionally substituted lower alkyl, aryl, heteroaryl or (aryl or heteroaryl) lower alkyl; or Rb and Rc together represent lower alkylene; and pharmaceutically acceptable salts thereof; and enantiType: GrantFiled: January 16, 2001Date of Patent: April 12, 2005Assignee: Novartis AGInventor: Gary Michael Ksander
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Publication number: 20040254182Abstract: This invention relates to compounds which are useful as enhanced propertied pharmaceutical compounds for both human and veterinary application. The pharmaceutical compounds which are suitable for use in this invention are those compounds which can be substituted with a moiety, said moiety comprising a substituent which enhances or changes the properties of the pharmaceutical compound. The chemical modification of drugs into labile derivatives with enhanced physicochemical properties that enable better transport through biological barriers is a useful approach for improving-drug delivery.Type: ApplicationFiled: December 17, 2002Publication date: December 16, 2004Inventors: Mark Joseph Mulvihill, Steven Howard Shaber
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Publication number: 20040235858Abstract: Compounds of the formula I 1Type: ApplicationFiled: February 5, 2004Publication date: November 25, 2004Inventor: Howard Tucker
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Patent number: 6818645Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: wherein X, Y, and Z are O, S, or NR4, and the other substituents are as defined in the specification; and prodrugs, individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.Type: GrantFiled: August 1, 2003Date of Patent: November 16, 2004Assignee: Syntex (U.S.A.) LLCInventors: Robert James Weikert, Ann Marie Madera, Russell Stephen Stabler
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Publication number: 20040214832Abstract: Disclosed are piperazine derivatives, their manufacture and use as inhibitors of renin.Type: ApplicationFiled: March 26, 2004Publication date: October 28, 2004Inventors: Cuiman Cai, Emma Hazel Clay, Dennis M. Downing, Jeremy John Edmunds, Daniel Dale Holsworth, Tingsheng Li, Noel Aaron Powell
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Publication number: 20040180901Abstract: Compounds of the formula (I) useful as metalloproteinase inhibitors, especially as inhibitors of MMP 13.Type: ApplicationFiled: January 29, 2004Publication date: September 16, 2004Inventors: Raymond Finlay, David Waterson
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Publication number: 20040176386Abstract: Compounds of the formula I 1Type: ApplicationFiled: February 26, 2004Publication date: September 9, 2004Applicant: AstraZeneca ABInventors: Christophe B. Barlaam, Robert I. Dowell, Maurice R.V. Finlay, Nicholas J. Newcombe, Howard Tucker, David Waterson
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Publication number: 20040171518Abstract: The present invention is directed to stabilized polypeptide compositions. Typical embodiments of the present invention provide improved methods and materials for maintaining the stability of insulin polypeptide formulations. In particular, the disclosure provided herein teaches that the aggregation of insulin polypeptides can be inhibited by combining them with a class of compounds having the general formula A1—L1—S—L2—A2, wherein S comprises from one to seven consecutive atoms selected from the group consisting of nitrogen, carbon, and oxygen, wherein at least one of the atoms is a carbon atom; L1 and L2 are linking groups having from two to twelve atoms selected from the group consisting of nitrogen, carbon, oxygen, sulfur, and phosphorus; and A1 and A2 are carboxylic acid groups.Type: ApplicationFiled: February 27, 2003Publication date: September 2, 2004Applicant: Medtronic MiniMed, Inc.Inventors: William Peter Van Antwerp, Joseph C. Walsh
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Publication number: 20040157817Abstract: The present invention provides certain cycloalkenylsulfonamide derivatives of the formula: 1Type: ApplicationFiled: November 6, 2003Publication date: August 12, 2004Inventors: Buddy Eugene Cantell, Dennis Michael Zimmermann
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Publication number: 20040152703Abstract: The invention relates to bisaryl derivatives of the formula I, 1Type: ApplicationFiled: July 21, 2003Publication date: August 5, 2004Inventors: Tao Guo, Koc-Kan Ho, Edward McDonald, Roland Ellwood Dolle, Kurt W. Saionz, Steven G. Kultgen, Ruiyan Liu, Guizhen Dong, Peng Geng, Anton Egbert Peter Adang, Nicole Corine Renee Van Straten
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Publication number: 20040138206Abstract: The present invention relates to a novel sulfonamide derivatives and novel intermediates thereof, preparation thereof, and a pharmaceutical composition comprising the same, and more particularly, to novel sulfonamide derivatives and intermediates thereof that are used as angiogenesis controlling material and that can inhibit overexpression of matrix metalloproteinase that decomposes protein constituents in extracellular and basement membranes of connective tissues, and preparation methods thereof, and a pharmaceutical composition comprising the same.Type: ApplicationFiled: December 11, 2003Publication date: July 15, 2004Inventors: Yong-Jun Chung, Kyeong-Ho Lee, Youn-Chul Kim, Ho-Jin Park
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Patent number: 6762178Abstract: Hydroxamic acids having the formula are useful in treating disease conditions mediated by TNF-&agr;, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.Type: GrantFiled: June 14, 2001Date of Patent: July 13, 2004Assignee: Wyeth Holdings CorporationInventors: Jeremy I. Levin, James M. Chen
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Publication number: 20040132738Abstract: This invention relates to a method for treating an angiogenesis-related disease.Type: ApplicationFiled: October 20, 2003Publication date: July 8, 2004Inventors: Che-Ming Teng, Hui-Po Wang, Eric I. C. Li, On Lee, Jih-Hwa Guh, Huei-Ting Chen, Ya-Bing Fan, Ya-Lan Chen
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Publication number: 20040127494Abstract: There is provided a series of novel &agr;-(N-sulfonamido)acetamide compounds of the Formula (I) 1Type: ApplicationFiled: December 20, 2002Publication date: July 1, 2004Inventors: Michael F. Parker, Katharine E. McElhone, Robert A. Mate, Joanne J. Bronson, Yonghua Gai, Carl P. Bergstrom, Lawrence R. Marcin, John E. Macor
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Publication number: 20040121963Abstract: The present invention relates to a composition for inhibiting HIV activity comprising the extract of Paecilomyces sp. (Tochu-kaso) J300. More particularly, the present invention relates to a composition for inhibiting HIV activity comprising 3-[5-(methoxy-ethyl)-3,6-dioxo-piperazine-2-yl]propionic acid represented by Formula I and 4-methyl-2-[(pyrolidine-2-carbonyl)-2-amino] pentanoic acid represented by Formula 2 that are extracted from Paecilomyces sp. (Tochu-kaso) J300; and to a medical composition and food composition containing the same.Type: ApplicationFiled: January 6, 2004Publication date: June 24, 2004Inventors: Sae-Yun Cho, Sang-Duk Ji, Seong-Kyu Song, Kwan-Hee Lee
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Publication number: 20040122020Abstract: The invention provides compounds of general formula (I), wherein R1, X, Y, n, R2, Z1, Z2, A1, A2, Q, R3, R4, R5, R6, R7, R8, t and R16 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: January 8, 2004Publication date: June 24, 2004Inventors: Tomas Eriksson, Karolina Lawitz
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Publication number: 20040122021Abstract: Levorotatory and dextrorotatory enantiomers of 1-[(4-chlorophenyl)phenylmethyl]-4-[(4-methylphenyl)sulfonyl]piperazine of the formula 1Type: ApplicationFiled: December 2, 2003Publication date: June 24, 2004Inventors: Eric Cossement, Guy Bodson, Jean Gobert
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Publication number: 20040116404Abstract: Disclosed are sulphones which modulate the action of gamma-secretase. The compounds are useful in the treatment or prevention of Alzheimer's disease.Type: ApplicationFiled: October 1, 2003Publication date: June 17, 2004Inventors: Jose Luis Castro Pineiro, Ian Churcher, Kevin Dinnell, Timothy Harrison, Sonia Kerrad, Alan John Nadin, Paul Joseph Oakley, Andrew Pate Owens, Duncan Edward Shaw, Martin Richard Teall, Susannah William, Brian John Williams
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Publication number: 20040092530Abstract: The invention provides methods for treating neuropsychiatric disorders such as schizophrenia, Alzheimer's Disease, autism, depression, benign forgetfulness, childhood learning disorders, closed head injury, and attention deficit disorder. The methods entail administering to a patient diagnosed as having a neuropsychiatric disorder a pharmaceutical composition containing (i) a therapeutically effective amount of D-alanine (or a modified form thereof), provided that the composition is substantially free of D-cycloserine, and/or (ii) D-serine (or a modified form thereof), and/or (iii) 105 to 500 mg of D-cycloserine (or a modified form thereof), and/or (iv) N-methylglycine (or a modified form thereof).Type: ApplicationFiled: September 23, 2003Publication date: May 13, 2004Applicant: The General Hospital Corporation, a Massachusetts corporationInventors: Guochuan Tsai, Joseph Coyle
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Patent number: 6734184Abstract: Arylpiperazines of formula (I) useful as metalloproteinase inhibitors, especially as inhibitors of MMP 13.Type: GrantFiled: February 26, 2001Date of Patent: May 11, 2004Assignee: AstraZeneca ABInventors: Bernard C Barlaam, Nicholas J Newcombe, Howard Tucker, David Waterson
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Publication number: 20040087581Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: 1Type: ApplicationFiled: October 14, 2003Publication date: May 6, 2004Inventors: Charles Alois Dvorak, Lawrence Emerson Fisher, Keena Lynn Green, Ralph New Harris, Hans Maag, Anthony Prince, David Bruce Repke, Russell Stephen Stabler
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Publication number: 20040087596Abstract: The efficacy of levodopa therapy in patients being treated for Parkinson's disease is enhanced by administering high doses of a partial glycine agonist. The frequency and severity of levodopa-induced side effects in Parkinson's disease patients are also reduced by administration of a partial glycine agonist.Type: ApplicationFiled: September 11, 2003Publication date: May 6, 2004Inventor: Jay S. Schneider
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Patent number: 6730783Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: April 22, 2003Date of Patent: May 4, 2004Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan
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Publication number: 20040077632Abstract: The present invention is related to substantially hydrophilic sulfonamide derivatives, or sulfonamide derivatives having a substantially hydrophilic moiety, of formula I notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK 3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation.Type: ApplicationFiled: September 10, 2003Publication date: April 22, 2004Inventors: Serge Halazy, Dennis Church, Stephen J. Arkinstall, Marco Biamonte, Monserrat Camps, Jean-Pierre Gotteland, Thomas Rueckle
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Publication number: 20040053917Abstract: The present invention is related to benzsulfonamide derivatives of formula I notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such benzsulfonamide derivatives. Said benzsulfonamide derivatives are ef-ficient modulators of the JNK pathway, they are in particular efficient and selective in-hibitors of JNK 2 and 3. The present invention is furthermore related to novel benzsul-fonamide derivatives as well as to methods of their preparation (I). The compounds of formula I according to the present invention being suitable pharma-ceutical agents are those wherein Ar1 is a substituted or unsubstituted aryl or heteroaryl group. X is O or S, preferably O.R1 is hydrogen or a C1-C6-alkyl group, preferably H.R2 is hydrogen, —COOR3, —CONR3R3′, OH, a C1-C4 alkyl substituted with an OH group, a hydrazido carbonyl group, a sulfate, a sulfonate, an amine or an ammonium salt; n is either 0 or 1, preferably 1.Type: ApplicationFiled: September 8, 2003Publication date: March 18, 2004Inventors: Serge Halazy, Dennis Church, Stephen J. Arkinstall, Marco Biamonte, Montserrat Camps, Jean-Pierre Gotteland, Thomas Rueckle
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Patent number: 6706745Abstract: The present invention relates to a biphenylamidine derivative of the general formula (1): or a pharmaceutically acceptable salt thereof, which is a novel compound functioning as a clinically applicable FXa inhibitor.Type: GrantFiled: May 18, 2000Date of Patent: March 16, 2004Assignee: Teijin LimitedInventors: Takayuki Hara, Tomohisa Nakada, Yasunobu Takano, Satoshi Sugiura, Takaharu Tsutsumi, Yoshiharu Takazawa, Reiko Takarada
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Publication number: 20040043026Abstract: The present invention relates to findings that reducing the activity of Plasminogen Activator Inhibitor-1 (PAI-1) suppresses an excessive deposition of collagen which is known as a cause for the formation of abnormal scars. These abnormal scars include but are not limited to keloids, adhesions, hypertrophic scars, skin disfiguring conditions, fibrosis, fibrocystic conditions, contractures, and scleroderma, all of which are associated with or caused by an excessive deposit of collagen in a wound healing process. Accordingly, aspects of the present invention are directed to the reduction of PAI-1 activity to decrease an excessive accumulation of collagen, prevent the formation of an abnormal scar, and/or treat abnormal scars that result from an excessive accumulation of collagen.Type: ApplicationFiled: May 13, 2003Publication date: March 4, 2004Inventors: Tai-Lan Tuan, Paul D. Benya, David Warburton
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Publication number: 20040038865Abstract: Compositions and methods have been developed for transporting compounds across membranes with little or no toxicity and, when targeted through the appropriate routes of administration (i.e., lung, gastrointestinal (GI) tract), little or no immune stimulation. The compositions can mediate cellular delivery of compounds that would otherwise not enter cells and enhance the intracellular delivery of compounds that would otherwise enter cells inefficiently. The methods are carried out by contacting a proximal face of a lipid bilayer or membrane (e.g. the surface of an intact cell) with a complex containing a compound (e.g., a therapeutic agent) and a diketopiperazine (DKP). DKP and the compound are non-covalently associated with each other or covalently bound to each other.Type: ApplicationFiled: August 1, 2003Publication date: February 26, 2004Applicant: MannKind CorporationInventors: Cohava Gelber, Kathleen Rousseau
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Publication number: 20040034018Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: 1Type: ApplicationFiled: August 1, 2003Publication date: February 19, 2004Inventors: Robert James Weikert, Ann Marie Madera, Russell Stephen Stabler
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Patent number: 6693100Abstract: The use for the manufacture of a medicament for treating psoriasis of dexrazoxane, the d-isomer of 1,2-bis(3,5-dioxopiperazin-1-yl)-propane, or a physiologically acceptable salt thereof.Type: GrantFiled: June 11, 2002Date of Patent: February 17, 2004Inventors: Iervant Zarmanian, Jadranka Rogan-Grgas
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Patent number: 6686349Abstract: The invention relates to novel tetracyclic pyrroloquinolone derivatives of the formula (I) or (II): wherein all variables are as herein defined, pharmaceutical compositions containing the compounds and their use for the treatment of sexual dysfunction.Type: GrantFiled: November 12, 2002Date of Patent: February 3, 2004Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Weiqin Jiang, Zhihua Sui
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Publication number: 20040019016Abstract: There is provided a compound of Formula I 1Type: ApplicationFiled: November 20, 2002Publication date: January 29, 2004Inventors: Barry Victor Lloyd Potter, Lok Wai Lawrence Woo, Atul Purohit, Michael John Reed, Oliver Brook Sutcliffe, Christian Bubert
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Publication number: 20040018152Abstract: Compositions containing biologically active molecules encapsulated in self-assembling, diketopiperazine microspheres (TECHNOSPHEREs™) and methods for making and administering such compositions are described herein. The compositions can be used to immunize individuals against agents of biological warfare. The biologically active molecules include atropine, antibodies, antigens, and antibiotics. The compositions can be placed in an inhalation device for self-administration. Pulmonary delivery of TECHNOSPHERE™ encapsulated atropine, antibodies, vaccines, and antibiotics provides an accelerated onset of immunity to the targeted disease. Furthermore, the TECHNOSPHERE™ encapsulated atropine, antibodies, vaccines, and antibiotics are stable formulations, suitable for stockpiling, rapid dissemination and mass treatment.Type: ApplicationFiled: January 17, 2003Publication date: January 29, 2004Applicant: Pharmaceutical Discovery CorporationInventors: Solomon S. Steiner, Cohava Gelber, Robert S. Feldstein, Roderike Pohl
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Publication number: 20040014745Abstract: This invention relates to new amide compounds having the potentiation of the cholinergic activity, etc., and represented by general formula [I].Type: ApplicationFiled: July 15, 2003Publication date: January 22, 2004Applicant: Fujisawa Pharmaceutical Co. Ltd.Inventors: Akira Yamada, Satoshi Aoki
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Patent number: 6680312Abstract: The present invention is to provide a compound or a salt thereof represented by the formula: wherein R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, the ring A is an optionally substituted divalent nitrogen-containing heterocyclic group, X′ is an optionally substituted alkylene chain, Y is an optionally substituted divalent cyclic group, X is a chemical bond or an optionally substituted alkylene chain, and Z is (1) an optionally substituted amino group, (2) an optionally substituted imidoyl group or (3) an optionally substituted nitrogen-containing heterocyclic group, or a pro-drug thereof, which has activated coagulation factor X inhibitory activity and which are useful as anti-coagulants.Type: GrantFiled: April 24, 2002Date of Patent: January 20, 2004Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroyuki Tawada, Fumio Itoh, Hiroshi Banno, Zen-ichi Terashita
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Patent number: 6677336Abstract: Novel compounds of the general formula: and pharmaceutically acceptable acid addition salts thereof, wherein the compounds are useful in therapy to protect skeletal muscles against damage resulting from trauma or to protect skeletal muscles subsequent to muscle or systemic diseases such as intermittent claudication, to treat shock conditions, to preserve donor tissue and organs used in transplants, in the treatment of cardiovascular diseases including atrial and ventricular arrhythmias, Prinzmetal's (variant) angina, stable angina, and exercise induced angina, congestive heart disease, and myocardial infarction.Type: GrantFiled: February 22, 2001Date of Patent: January 13, 2004Assignee: CV Therapeutics, Inc.Inventors: Jeff Zablocki, Elfatih Elzein, Grigory Nudelman, Tim Marquart, Brent K. Blackburn, Venkata P. Palle
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Patent number: 6673811Abstract: Disclosed are 1H-Pyrrolo[3,2-b]pyridine-3-carboxylic acid amides that bind to the benzodiazepine site of GABAA receptors. Such compounds can be used to modulate ligand binding to GABAA receptors in vivo and in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals, and livestock animals.Type: GrantFiled: November 19, 2002Date of Patent: January 6, 2004Assignees: Neurogen Corporation, Pfizer, Inc.Inventors: George D. Maynard, Manuka Ghosh, Christopher J. O'Donnell