Purine Containing (including Hydrogenated) Patents (Class 544/228)
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Patent number: 7977343Abstract: Novel adenine derivatives of the formula (I), in which R1, R2, R3, X and Y have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.Type: GrantFiled: July 20, 2006Date of Patent: July 12, 2011Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Hans-Peter Buchstaller, Hans-Michael Eggenweiler, Bertram Cezanne, Michael Wolf
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Patent number: 7741318Abstract: Compounds having the structural formula I are disclosed, wherein A is alkylene, or optionally substituted arylene, cycloalkylene or heteroaryldiyl; X is —C(O)— or —S(O)2—; R1 is alkyl or cycloalkyl; R2 is hydrogen, halo or —CN; R3 is hydrogen or alkyl; R4 is hydrogen, alkyl, alkoxy, hydroxyalkyl, aminoalkyl-, cycloalkyl, heterocycloalkyl, heterocycloalkyl substituted by alkyl, optionally substituted arylalkyl or optionally substituted heteroarylalkyl; or R3 and R4, form an optionally substituted 5-7 membered ring, said ring optionally comprising an additional heteroatom ring member; R7 is alkyl, optionally substituted phenyl, optionally substituted heteroaryl, cycloalkyl, halo, morpholinyl, optionally substituted piperazinyl, or optionally substituted azacycloalkyl.Type: GrantFiled: December 19, 2005Date of Patent: June 22, 2010Assignee: Schering CorporationInventors: Martin C. Clasby, Samuel Chackalamannil, Bernard R. Neustadt, Xiaobang Gao
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Patent number: 6919449Abstract: The present invention relates to a method for the preparation of cephalosporin antibiotic of the formula (II), which comprises hydrolyzing and halogenating the ester of formula (III) by photochemical irradiation in one pot using a halogenating agent in the absence or presence of a solvent, to produce compound of formula (I), activating the 4-halogeno-2-substitutedimino-3-oxo-butyric acid of formula (I) using conventional activation agents gives compound of formula (IV), condensing the activated compound of the formula (IV) with 7-amino cephem derivative of the formula (V) to produce a compound of formula (VI), and cyclizing the compound of formula (VI) with thiourea to give cephalosporin compounds of the formula (II).Type: GrantFiled: September 18, 2002Date of Patent: July 19, 2005Assignee: Orchid Chemicals and Pharmaceuticals LimitedInventors: Pandurang Balwant Deshpande, Parven Kumar Luthra, Pratik Ramesh Sathe, Sivakumaran Sundaravadivelan, Praveen Nagesh Ganesh
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Patent number: 6734143Abstract: The present invention provides 2-methoxyimino-2-(pyridinyloxymethyl) phenyl acetamides according to formula (I) as well as their use as fungicidal compounds.Type: GrantFiled: February 27, 2003Date of Patent: May 11, 2004Assignee: Dow AgroSciences LLCInventors: Neil Vincent Kirby, Jenifer Lynn Adamski Butz, Brent Jeffrey Rieder, James M. Renga, Jeannie Rachel Phillips Cetusic, Irene Mae Morrison, John Todd Mathieson, Gary David Gustafson
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Patent number: 6531484Abstract: Pyrrolidine compounds of Formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8a, R8b, j, k, 1, m, and n are defined herein) are described. The compounds are modulators of CCR5 chemokine receptor activity. The compounds are useful, for example, in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.Type: GrantFiled: October 10, 2001Date of Patent: March 11, 2003Assignee: Merck & co., Inc.Inventors: Christopher A. Willoughby, Keith Rosauer, Kevin T. Chapman, Sander G. Mills, Dong-Ming Shen, Min Shu
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Patent number: 6136827Abstract: The present invention is directed to cyclic amines of the formula I: ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, m and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.Type: GrantFiled: July 21, 1998Date of Patent: October 24, 2000Assignee: Merck & Co., Inc.Inventors: Charles G. Caldwell, Paul E. Finke, Malcolm Maccoss, Laura C. Meurer, Sander G. Mills, Bryan Oates
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Patent number: 5955501Abstract: Compounds having anti-inflammatory and other activities are disclosed. The compounds are derived from phorboids of the diterpene- and benzolactam-classes.Type: GrantFiled: June 7, 1995Date of Patent: September 21, 1999Assignee: Procyon Pharmaceuticals, Inc.Inventors: Paul E. Driedger, James Quick
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Patent number: 5770591Abstract: A bis(platinum) complex having the structure: ##STR1## wherein X, Y, Z, X', Y', and Z' are the same or different ligands and are halide, sulphate, phosphate, nitrate, carboxylate, substituted carboxylate, dicarboxylate, substituted dicarboxylate primary or secondary amine, sulfoxide, phosphine, pyridine-type nitrogen and the like; preferably, there is at least one Pt-anion bond on each Pt molecule; and A is a diamine or polyamine.Complexes of trans geometry ?PtX.sub.2 (L)(L')! where at least L is a planar ligand such as pyridine but preferably quinoline and L' may be amine, sulfoxide or substituted sulfoxide and X is a chloride, nitrate or carboxylate.A process for obtaining bis(platinum) complexes where the two platinum coordination spheres may contain different ligands in each sphere and where the geometry of each platinum coordination sphere may be the same or different.Type: GrantFiled: November 10, 1994Date of Patent: June 23, 1998Assignee: The University of Vermont and State Agricultural CollegeInventor: Nicholas Farrell
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Patent number: 5728691Abstract: Derivatives of 7-aminoceph-3-em-4-carboxylic acid with 6-fluoroquinolone derivatives in which the cephem and 6-fluoroquinolone moieties are bound to each other through a carboxamido bond as well as the pharmaceutical compositions containing them are described. These compounds possess antibacterial, growth promoting and probiotic activity.Type: GrantFiled: August 22, 1996Date of Patent: March 17, 1998Assignees: Laboratorios Aranda S.A. De C.V., Judith Marcia Arrieta MunguiaInventor: Miguel Angel Corpi Constantino
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Patent number: 5506243Abstract: Since sulfonamide derivatives of the present invention show strong inhibitory activity against cysteine protease such as calpain papain, cathepsin B, cathepsin H, cathepsin L, they can be used as remedies for muscular dystrophy, cataract, myocardial infarction, stroke, Alzheimer's disease, amyotrophia, osteoporosis, hypercalcemia or the like.Type: GrantFiled: April 28, 1994Date of Patent: April 9, 1996Assignee: Mitsubishi Kasei CorporationInventors: Ryoichi Ando, Toshiro Sakaki, Chizuko Takahashi, Yoshiyuki Fujimura
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Patent number: 5484763Abstract: There are provided substituted benzisoxazole and benzisothiazole compounds having the structural formula I ##STR1## Further provided are compositions and methods comprising those compounds for the control of undesirable plant species.Type: GrantFiled: February 10, 1995Date of Patent: January 16, 1996Assignee: American Cyanamid CompanyInventor: Peter J. Wepplo
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Patent number: 4716232Abstract: 1-(Vinyl phosphonate adduct) pyrazolidinones are intermediates to bicyclic pyrazolidinone antimicrobial compounds.Type: GrantFiled: May 14, 1986Date of Patent: December 29, 1987Assignee: Eli Lilly and CompanyInventor: Robert J. Ternansky
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Patent number: 4388326Abstract: Organic sulfoxides having a latent allyl group bound to the sulfur are enzyme inhibitors of the suicide or K.sub.cat type.Type: GrantFiled: May 7, 1980Date of Patent: June 14, 1983Assignee: Merck & Co., Inc.Inventor: Raymond A. Firestone