Patents Examined by Richard Raymond
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Patent number: 7208602Abstract: This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, —X(CO)Y, or alkylene-X(CO)Y wherein X and Y are as defined herein; each R3 and each R3A are independently H, or alkyl; R11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.Type: GrantFiled: February 5, 2003Date of Patent: April 24, 2007Assignees: Schering Corporation, Pharacopeia Drug Discovery, Inc.Inventors: Dmitri A. Pissarnitski, Hubert B. Josien, Elizabeth M. Smith, John W. Clader, Theodros Asberom, Tao Guo, Douglas W. Hobbs
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Patent number: 7122677Abstract: A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceuticals compositions. Methods of treatment and combinations with other agents are also disclosed.Type: GrantFiled: November 12, 2002Date of Patent: October 17, 2006Assignee: Scherig CorporationInventors: Gregory A. Reichard, Sunil Paliwal, Neng-Yang Shih, Dong Xiao, Hon-Chung Tsui, Sapna Majmundar Shah, Cheng Wang, Michelle Laci Wrobleski
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Patent number: 7122675Abstract: Novel aryl and heteroaryl sulfonamides are disclosed. The sulfonamides, which are gamma secretase inhibitors, are represented by the formula: wherein Ar1 and Ar2 independently represent aryl or heteroaryl and Y represents a bond or a —(C(R3)2)1-3 group. Also disclosed is a method of inhibiting gamma secretase, and a method of treating Alzheimer's disease using the compounds of formula I.Type: GrantFiled: August 1, 2002Date of Patent: October 17, 2006Assignee: Schering CorporationInventors: Hubert B. Josien, John W. Clader, Theodros Asberom, Dmitri A. Pissarnitski
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Patent number: 7101878Abstract: Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.Type: GrantFiled: August 20, 1999Date of Patent: September 5, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Mark Brian Anderson, Haresh N. Vazir, David Robert Luthin, Genevieve DeGuzman Paderes, Ved P. Pathak, Lance Christopher Christie, Yufeng Hong, Eileen Valenzuela Tompkins, Haitao Li, James Faust
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Patent number: 7081538Abstract: Compounds of formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, wherein, for example, X is O, S or NH; HET is an optionally substituted C-linked 5-membered heteroaryl ring containing 2 to 4 heteroatoms independently selected from N, O and S; Q is selected from, for example, Q1 and Q2: R2 and R3 are independently hydrogen or fluoro; T is selected from a range of groups, for example, an N-linked (fully unsaturated) 5-membered heteroaryl ring system or a group of formula (TC5): wherein Rc is, for example, R13CO—, R13SO2— or R13CS—; wherein R13 is, for example, optionally substituted (1–10C)alkyl or R14C(O)O(1–6C)alkyl wherein R14 is optionally substituted (1–10C)alkyl; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are describedType: GrantFiled: November 28, 2000Date of Patent: July 25, 2006Assignee: AstraZeneca ABInventors: Michael Barry Gravestock, Michael John Betts
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Patent number: 7064218Abstract: The present invention provides novel compounds possessing one or more of the following activities: antibacterial, antifungal and antitumor activity. The compounds are of Formula (I): Pharmaceutical compositions containing these compounds, methods of making and methods for using these compounds are also provided.Type: GrantFiled: December 24, 2002Date of Patent: June 20, 2006Assignee: Genelabs Technologies, Inc.Inventors: Natalia B. Dyatkina, Dong-Fang Shi, Christopher Don Roberts, Mark Douglas Velligan, Sebastian Johannes Reinhard Liehr, Janos Botyanszki, Wentao Zhang, Alexander Khorlin, Peter Harold Nelson, Joseph Martin Muchowski
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Patent number: 7060836Abstract: Compounds of the formula (I): or a pharmaceutically acceptable salt, prodrug, solvate or polymorph thereof, wherein R, R1, and Z are as defined herein, are useful in treating or preventing a condition for which an NK2 antagonist is efficacious.Type: GrantFiled: December 17, 2002Date of Patent: June 13, 2006Assignee: Pfizer, IncInventors: Donald Stuart Middleton, Alan Stobie
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Patent number: 7034148Abstract: Mixtures of metallocenyl phthalocyanines obtainable by reacting a mixture A comprising two phthalocyanines (I) and (II) with a metallocene derivative in the presence of a catalyst, and also oligomeric metallocenyl phthalocyanines, processes for preparing them, their use for, inter alia, optical recording and optical recording mediaType: GrantFiled: April 9, 2002Date of Patent: April 25, 2006Assignee: Ciba Specialty Chemicals CorporationInventors: Jürgen Beyrich, Rudolf Blattner, Jean-Luc Budry, Wolfgang Freitag, Colin Morton, Gerald Anthony Murphy, Beat Schmidhalter, Michael Schulz, Heinz Spahni, Christian Stern, Annemarie Wolleb, Heinz Wolleb, Roland Zoelper
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Patent number: 7019147Abstract: The invention relates to compounds of formula (1) and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R7, R8, R9, R10, and R11 are as defined herein. The invention also relates to methods of treating abnormal cell growth, such as cancer, in mammals by administering the compounds of formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of formula (1). The invention also relates to methods of preparing the compounds of formula (1).Type: GrantFiled: November 10, 2000Date of Patent: March 28, 2006Assignee: Pfizer Inc.Inventors: Wayne E. Barth, Michael J. Luzzio, Joseph P. Lyssikatos
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Patent number: 7005518Abstract: Fluorescent dyes are disclosed which are useful as reporter groups for labeling biomolecules. The silicon phthalocyanine dyes disclosed are preferably water soluble, isomericly pure, possess high quantum yield, and are useful in bioassays.Type: GrantFiled: October 23, 2003Date of Patent: February 28, 2006Assignee: Li-Cor, Inc.Inventors: Xinzhan Peng, Daniel R. Draney, Jiyan Chen
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Patent number: 7005517Abstract: The present invention provides a novel paramagnetic metal-phthalocyanine complexes and pharmaceutically acceptable salts thereof, which are useful as contrast agents for MRI(Magnetic Resonance Imaging), diagnostic X-ray imaging and computed tomography(CT). The present invention also provides contrast agents for imaging, comprising the new paramagnetic metal-phthalocyanine complexes. The new contrast agents of the present invention show high imaging enhancement effects at lower concentration and are safer than the previously reported contrast agents.Type: GrantFiled: January 4, 2002Date of Patent: February 28, 2006Inventors: Sung-Young Lee, Kyo-Im Koo
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Patent number: 6995269Abstract: Compounds of formula IIA and IIB are novel guanidine compounds where the variables R1 through R10 have the values set forth herein. Such compounds have use in treating diseases such as obesity and type II diabetes, and may be provided as pharmaceutical formulations in conjunction with a pharmaceutically acceptable carrier.Type: GrantFiled: March 4, 2003Date of Patent: February 7, 2006Assignee: Chiron CorporationInventors: Paul A. Renhowe, Daniel Chu, Rustum S. Boyce, David Duhl
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Patent number: 6989443Abstract: The present invention is directed to low toxicity boronated compounds and methods for their use in the treatment, visualization, and diagnosis of tumors. More specifically, the present invention is directed to low toxicity carborane-containing 5, 10, 15, 20-tetraphenylporphyrin compounds and methods for their use particularly in boron neutron capture therapy (BNCT) and photodynamic therapy (PDT) for the treatment of tumors of the brain, head, neck, and surrounding tissue. The invention is also directed to using these carborane-containing tetraphenyl porphyrin compounds to methods of tumor imaging and/or diagnosis such as MRI, SPECT, or PET.Type: GrantFiled: June 28, 2004Date of Patent: January 24, 2006Assignee: Brookhaven Science Associates, LLCInventors: Haitao Wu, Michiko Miura
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Patent number: 6974869Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: September 18, 2002Date of Patent: December 13, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventor: George V. DeLucca
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Patent number: 6890915Abstract: The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, R1, R2, R3, R4, R5, R6, R7, R11, and n are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), aggrecanase, or a combination thereof.Type: GrantFiled: May 23, 2002Date of Patent: May 10, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventors: James E. Sheppeck, Jingwu Duan, Chu-Biao Xue, Zelda Wasserman
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Patent number: 6846815Abstract: This invention is directed to quinoline/quinoxaline compounds which inhibit platelet-derived growth factor tyrosine kinase and/or Lck tyrosine kinase, to pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders/conditions involving cellular differentiation, proliferation, extracellular matrix production or mediator release and/or T cell activation and proliferation.Type: GrantFiled: February 3, 2003Date of Patent: January 25, 2005Assignee: Aventis Pharmaceuticals Inc.Inventors: Michael R. Myers, Alfred P. Spada, Paul E. Persons, Martin P. Maguire
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Patent number: 6835726Abstract: Compounds and compositions are provided which are useful for the treatment of viral infections, particularly human Cytomegalovirus infection. The compounds include novel pyrimidine-based derivatives.Type: GrantFiled: January 24, 2003Date of Patent: December 28, 2004Assignee: Amgen Inc.Inventors: Timothy D. Cushing, Heather L. Mellon, Juan C. Jaen, John A. Flygare, Shi-Chang Miao, Xiaoqi Chen, Jay P. Powers
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Patent number: 6780864Abstract: The invention relates to a group of novel piperazine and piperidine derivatives of formula (I), wherein: S1 is hydrogen, halogen, alkyl (1-3C), CN, CF3, OCF3, SCF3, alkoxy (1-3C), amino or mono- or dialkyl (1-3C) substituted amino, or hydroxy; X represents NR3, S, CH2, O, SO or SO2, wherein R3 is H or alkyl (1-3C); . . . Z represents ═C or —N; —R1 independently represent H or alkyl (1-3C), or R1 and R2 together can form a bridge 2 or 3 C-atoms; R4 is hydrogen or alkyl (1-3C); Q is methyl, ethyl, ethyl substituted with one or more fluorine atoms, cyclopropyl—methyl, optionally substituted with one or more fluorine atoms, and salts and prodrugs thereof. It has been found that these compounds have both partial dopamine D2-receptor agonism and partial serotonin 5-HT1A-receptor agonism mediated activities.Type: GrantFiled: August 14, 2001Date of Patent: August 24, 2004Assignee: DUPHAR International Research BVInventors: Roelof Feenstra, Johannes A. M. Van Der Heijden, Cornelis G. Kruse, Stephen K. Long, Johannes Mos, Gerben M. Visser, Gustaaf J. M. Van Scharrenburg, Gerrit P. Toorop
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Patent number: 6770636Abstract: Compounds of formula 1, wherein: R1 is hydrogen, hydroxy, CF3, NO2, CN, halogen, C1-C8-alkyl, or C1-C8-alkoxy; R2, R3, and R4 independently of one another are hydrogen, C1-C8-alkyl, hydroxy, NO2, CN, C1-C8-alkoxyl, CF3, or halogen; R5 and R6 independently of one another are hydrogen or a group consisting of C1-C8-alkyl, C2-C8-alkenyl, C3-C8-alkynyl, C3-C8-cycloalkyl, C3-C8-cycloalkyl-C1-C6-alkylene, C5-C8-cycloalkenyl, C5-C8-cycloalkenyl-C1-C6-alkylene, C6-C10-aryl, and C6-C10-aryl-C1-C6-alkylene, each optionally substituted by a group consisting of C1-C6-alkyl, C2-C6-alkenyl, halogen, C1-C6-alkyloxy, —NH2, —NH(C1-C4-alkyl), —N(C1-C4-alkyl)2, hydroxy, ═O, —COOH, —CO—OC1-C4-alkyl, —CONH2, —CONH(C1-C4-alkyl), —CON(C1-C4-alkyl)2, and CF3, or R5 and R6 together with the nitrogen atom are a saturated or unsaturated 5-, 6-, 7-, or 8-membered heterocyclic group optionally containing one or two further heteroatoms consisting of sulfur, oType: GrantFiled: July 24, 2001Date of Patent: August 3, 2004Assignee: Boehringer Ingelheim Pharma KGInventors: Klaus Fuchs, Werner Stransky, Matthias Grauert, Adrian Carter, Wolfram Gaida, Thomas Weiser, Helmut Ensinger
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Patent number: 6573265Abstract: The invention relates to the use of 1-(aminoalkyl)-3-quinoxaline-2-one derivatives, especially 1-diethylaminoethyl-3-quinoxaline-2-one derivatives of the formula (I), where R 3 is hydroxy, methoxy, ethoxy or hydrogen, or pharmaceutically compatible salts thereof, for the preparation of compounds having an antioxidant action and used for preventing or treating diseases caused by free radicals of the cellular oxygen metabolism, stimulating nerve cell growth, antagonizing glutamate receptors and/or stimulating the growth notably of glutamergic nerve cells.Type: GrantFiled: December 18, 2000Date of Patent: June 3, 2003Assignee: Phafag AktiengesellschaftInventors: Klaus Ehrenberger, Dominik Felix, Peter König, Burkhard Poeggeler