The Benzene Ring Is Attached To Nitrogen Through An Acyclic Carbon Or Carbon Chain Patents (Class 514/487)
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Patent number: 7829564Abstract: ?-and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: December 7, 2007Date of Patent: November 9, 2010Assignee: G.D. Searle LLCInventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw
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Publication number: 20100255093Abstract: Sustained release oral dosage forms of an R-baclofen prodrug are disclosed.Type: ApplicationFiled: March 3, 2010Publication date: October 7, 2010Applicant: XenoPort, Inc.Inventors: David E. Edgren, David J. Kidney, Nikhil Pargaonkar, Derrick K. Kim, Gorm Yoder, Sami Karaborni
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Publication number: 20100256229Abstract: The present invention is directed to compositions, methods of use, and processes for the synthesis related to 3-((S)-1-(dimethylamino)ethyl)phenyl methyl-((R)-1-phenylpropan-2 yl)carbamate, and its pharmaceutically acceptable salt forms, including the hydrogen fumarate salt. The present invention also relates to a novel form polymorph of 3-((S)-1-(dimethylamino)ethyl)phenylmethyl-((R)-1-phenylpropan-2 yl)carbamate, characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well a unique crystalline structure.Type: ApplicationFiled: April 2, 2010Publication date: October 7, 2010Applicant: Colucid Pharmaceuticals, Inc.Inventors: Shoucheng Du, Marc W. Andersen, Daniel Coughlin, Alexander Kolchinski
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Publication number: 20100184812Abstract: Mutual prodrugs comprising retinoids and histone deacetylase inhibitors, methods for production of the mutual prodrugs, and methods of treatment comprising administration of the mutual prodrugs. The retinoids include all-trans retinoic acid, 13-cis retinoic acid, and retinoic acid analogs that have a substitution at C-4. Further, the mutual prodrugs of the present invention can be used as therapeutic agents for the treatment of cancer and dermatological diseases and conditions. Pharmaceutical compositions comprising the mutual prodrugs.Type: ApplicationFiled: June 6, 2008Publication date: July 22, 2010Applicant: UNIVERSITY OF MARYLAND, BALTIMOREInventors: Vincent C. O. Njar, Lalji K. Gediya, Aakanksha Khandelwal
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Publication number: 20100184768Abstract: Among other things, the present invention provides novel isoprenyl compounds capable of effectively modulating inflammatory responses and pharmaceutical, cosmetic, cosmeceutical and topical compositions comprising these isoprenyl compounds. Anti-inflammatory compounds of the present invention are useful in treating or preventing diseases or conditions associated with inflammation. Proinflammatory compounds of the present invention are useful in treating or preventing diseases or conditions associated with suppression of inflammatory responses. Thus, the present invention also provides methods useful in the treatment or prevention of diseases or conditions associated with inflammation as well as methods useful in the treatment or prevention of diseases or conditions associated with suppression of inflammatory responses.Type: ApplicationFiled: November 12, 2009Publication date: July 22, 2010Applicant: SIGNUM BIOSCIENCES, INC.Inventors: Jeffry B. Stock, Maxwell Stock, Keshava Rapole, Seung-Yub Lee, Michael Voronkov, Eduardo Perez, Joel Gordon, Shuyi Chen, Jinglong Chen
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Publication number: 20100168079Abstract: The present invention relates to biaryl-benzylamine compounds, to processes for their production, to their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: ApplicationFiled: December 21, 2009Publication date: July 1, 2010Inventors: Daniela Angst, Birgit Bollbuck, Philipp Janser, Jean Quancard
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Publication number: 20100152188Abstract: The present invention relates to novel compounds of the general formula (I), their derivatives, their analogs, their stereoisomers, their pharmaceutically acceptable salts and compositions. The present invention more particularly provides novel heterocyclic compounds of the general formula (I).Type: ApplicationFiled: August 4, 2006Publication date: June 17, 2010Inventors: Akella Satya Surya Visweswara Srinivas, Kasinathan Mathiyazhagan, Duddu Savaraiah Sharada, Thanasekaran Ponpandian, Kulasekharan Revathy, Gaddam Om Reddy, Mani Kamarai, Sriram Raiagopal
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Publication number: 20100124543Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.Type: ApplicationFiled: July 16, 2009Publication date: May 20, 2010Applicant: Vertex Pharmaceuticals IncorporatedInventors: Roger Dennis Tung, Michael Robin Hale, Christopher Todd Baker, Eric Steven Furfine, Istvan Kaldor, Wieslaw Mieczylaw Kazmierski, Andrew Spaltenstein
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Publication number: 20100119603Abstract: A pharmaceutical composition comprises nanoparticles comprising a poorly water-soluble drug, ethylcellulose, and a bile salt.Type: ApplicationFiled: April 21, 2008Publication date: May 13, 2010Inventors: warren Kenyon Miller, Michael Mark Morgen, Daniel Tod Smithey
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Publication number: 20100113591Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.Type: ApplicationFiled: November 5, 2009Publication date: May 6, 2010Applicant: BELLUS Health (International) LimitedInventors: Xianqi Kong, David Migneault, Isabelle Valade, Xinfu Wu, Francine Gervais
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Publication number: 20100093811Abstract: Compounds of Formula I are disclosed: (I), wherein XA, k, R1, R2, R3, R4, R5, R5A, R6, R6A, R7 and R8 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: September 22, 2008Publication date: April 15, 2010Inventors: Craig A. Coburn, Joseph P. Vacca, Hemaka A. Rajapakse, Kristen L.G. Jones, Philippe Nantermet, James C. Barrow, Keith P. Moore, Steven S. Sharik, Cory Theberge, Abbas M. Walji
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Publication number: 20100069405Abstract: The present invention is directed to compounds and compositions for the treatment of neurological diseases that cause neurogenic and neuropathic pain, inflammatory diseases, renal ischaemia, cardiovascular disease and other pathologies caused by the presence of endogenous cannabinoids and or other substrates resulting from the metabolic activities of fatty acid amido hydrolase (FAAH). These compounds are represented by the formula (I): wherein A, n, R1, R7 and R8 are as defined herein.Type: ApplicationFiled: November 24, 2009Publication date: March 18, 2010Applicant: SANOFI-AVENTISInventors: Ahmed Abouabdellah, Regine Bartsch-Li, Christian Hoornaert, Antoine Ravet
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Publication number: 20100016381Abstract: The present invention provides an emulsion composition comprising (A) a compound stable in an acidic range, and (B) a buffer, wherein the pH is adjusted from about 3.7 to about 5.5.Type: ApplicationFiled: April 27, 2006Publication date: January 21, 2010Applicant: Takeda Pharmaceutical Company LimitedInventors: Naoki Asakawa, Takayuki Doen
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Publication number: 20090318393Abstract: A controlled pesticide delivery system includes a film-forming alkanol solution of at least one amphiphilic polymer and at least one pesticide composition for the treatment of at least one pest in gardens, landscapes, forests, and wooden structures, targeting at least one pest selected from fire ants, tent caterpillars, gypsy moths, wood-boring beetles, and bark beetles during at least one phase of their life cycles.Type: ApplicationFiled: June 19, 2009Publication date: December 24, 2009Inventor: Shalaby W. Shalaby
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Publication number: 20090281178Abstract: Compounds useful for promoting lysosomal processes and thereby ameliorating the disruption of cellular and functional integrity induced by A? and other protein and glycoconjugate species are provided. Methods for the treatment of neurodegenerative diseases that involve protein accumulation and aggregation in the brain, such as Alzheimer's, Parkinson's and Huntington's Disease, are also provided.Type: ApplicationFiled: April 20, 2009Publication date: November 12, 2009Inventors: Ben A. Bahr, Dennis Wrigth
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Publication number: 20090192096Abstract: Compounds of the formula I, in which R(1), R(2), R(3), R(4), R(5), R(6), R(7), R(8), R(30) and R(31) have the meanings indicated in the claims, are very particularly suitable as novel and antiarrythmic active compounds, in particular for the treatment and prophylaxis of atrial arrythmias, e.g. atrial fibrillation (AF), or atrial flutter.Type: ApplicationFiled: April 6, 2009Publication date: July 30, 2009Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Joachim BRENDEL, Wolfgang SCHMIDT, Peter BELOW
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Patent number: 7563930Abstract: Provided are crystalline forms of Cinacalet HCl and processes for their preparation.Type: GrantFiled: November 22, 2006Date of Patent: July 21, 2009Assignee: Teva Pharmaceutical Industries LtdInventors: Shlomit Wizel, Revital Lifshitz-Liron, Sharon Avhar-Maydan
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Publication number: 20090182011Abstract: Chimeric nitrate esters and their use in the treatment of depression are disclosed. The chimeric nitrate esters also are useful in the treatment of depression and comorbidity associated with aging.Type: ApplicationFiled: January 15, 2009Publication date: July 16, 2009Applicant: UNIVERSITY OF ILLINOIS CHICAGOInventor: Gregory R.J. Thatcher
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Patent number: 7560483Abstract: The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.Type: GrantFiled: June 21, 2005Date of Patent: July 14, 2009Assignee: XenoPort, Inc.Inventors: Mark A. Gallop, Jia-Ning Xiang, Fenmei Yao, Laxminarayan Bhat, Cindy X. Zhou
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Publication number: 20090149510Abstract: The invention relates to compounds and methods for modulating one or more components of a kinase cascade.Type: ApplicationFiled: July 7, 2008Publication date: June 11, 2009Inventor: David G. Hangauer, JR.
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Publication number: 20090143307Abstract: The invention describes compounds, compositions, and methods of using the same comprising a chemical moiety covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.Type: ApplicationFiled: September 2, 2008Publication date: June 4, 2009Applicant: SHIRE LLCInventors: Travis Mickle, Suma Krishnan, Barney Bishop, Christopher Lauderback, James Scott Moncrief, Robert Oberlender, Thomas Piccariello, Bernhard J. Paul, Christopher A. Verbicky
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Publication number: 20090118365Abstract: Methods of treating neuropathic pain, musculoskeletal pain, and back spasm associated with musculoskeletal pain in a patient comprising orally administering a therapeutically effective dose of a prodrug of a GABAB agonist having a high oral bioavailability of the corresponding GABAB agonist are disclosed.Type: ApplicationFiled: November 6, 2008Publication date: May 7, 2009Applicant: XenoPort, IncInventors: Joseph C. Benson, III, Peter A. Virsik, Daniel M. Canafax
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Publication number: 20090023664Abstract: ?- and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: ApplicationFiled: December 7, 2007Publication date: January 22, 2009Applicant: G.D. SEARLE LLCInventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw
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Publication number: 20090005438Abstract: A method for preventing and treating prostatic diseases and skin cancer using naturally or artificially synthesized isothiocyanates compounds or the derivatives or metabolites thereof.Type: ApplicationFiled: November 14, 2006Publication date: January 1, 2009Inventors: Jingcai Cheng, Jenwei Chiao, Haiya Jin, Chengjuan Zhong
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Publication number: 20080234265Abstract: Disclosed is the use of a combination of histone deacetylase inhibitors and epidermal growth factor receptor (EGFR) inhibitors to treat cancer.Type: ApplicationFiled: March 13, 2006Publication date: September 25, 2008Applicant: THE REGENTS OF THE UNIVERSITY OF COLORADOInventors: Samir E. Witta, Paul A. Bunn, Harry A. Drabkin, Robert M. Gemmill, Daniel Chuen-Fong Chan
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Publication number: 20080200511Abstract: The present invention relates to novel compounds of Formula (I) wherein ‘X’ represents an amino acid group, ‘n’ is an integer between 1 and 4, ‘R1’ represents benzyl, t-butyl or 9-fluorenylmethyl and ‘R2’ represents a tetramethylmercaptoimidazole derivative or —S+R3R4, wherein R3 and R4 each independently represent lower alkyl, or a pharmaceutically and/or veterinarily acceptable derivative thereof. The present invention further relates to pharmaceutical formulations of said compound and the use thereof in the preparation of a medicament for inhibiting diseases in which transglutaminase has been implicated. Advantageously, the medicament is for treating fibrosis, scarring and/or cancer. Additionally, the invention relates to a method of inhibiting autoimmune diseases such as coeliac disease, neurodegeneration and chronic inflammatory diseases (e.g. of the joints including rheumatoid arthritis and osteoarthritis in a subject).Type: ApplicationFiled: June 16, 2004Publication date: August 21, 2008Applicant: ASTON UNIVERSITYInventors: Martin Griffin, Ian George Coutts, Robert Edward Saint
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Patent number: 7393967Abstract: Provided is a process for preparing cinacalcet, (R)-?-methyl-N-[3-[3-(trifluoromethyl)phenyl]propyl]-1-naphthalenemethane amine.Type: GrantFiled: April 27, 2007Date of Patent: July 1, 2008Assignee: Teva Pharmaceutical Industries Ltd.Inventor: Revital Lifshitz-Liron
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Patent number: 7339078Abstract: Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, compositions, and methods for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: August 10, 2006Date of Patent: March 4, 2008Assignee: G.D. Searle LLCInventors: Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Raj Nagarajan, David L Brown, Joseph J McDonald
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Patent number: 7294735Abstract: Isolated cinacalcet carbamate, processes for the preparation thereof, and processes for the use of cinacalcet carbamate as a reference marker and standard are provided. Also provided are cinacalcet salts substantially free of cinacalcet carbamate, and processes for the preparation thereof.Type: GrantFiled: May 23, 2006Date of Patent: November 13, 2007Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Revital Lifshitz-Liron, Yuriy Raizi, Revital Ramaty, Esti Marom
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Patent number: 7262209Abstract: The invention relates to compounds of the general formula wherein Ar1, Ar2, R4, R5, R6, R7, R8, W, X, a and b have the significances given in the specification, and optionally the enantiomers thereof. The active ingredients have advantageous pesticidal properties. They are especially suitable for controlling parasites on warm-blooded animals.Type: GrantFiled: October 2, 2002Date of Patent: August 28, 2007Assignee: Novartis Animal Health US, Inc.Inventors: Thomas Goebel, Pierre Ducray
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Patent number: 7141609Abstract: ?- and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: April 21, 2005Date of Patent: November 28, 2006Assignee: G.D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Deborah E. Bertenshaw, Robert M. Heintz
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Patent number: 7109221Abstract: Fungicidal mixtures comprise as active components a) an amide compound of the formula I A-CO—NR1R2I ?in which A, R1 and R2 are as defined in the description, and b) dimethomorph or flumetover, and/or c) a valinamide of the formula III ?in which R13 is C3–C4-alkyl and R14 is naphthyl or phenyl, where the phenyl radical is substituted in the 4-position by a halogen atom, a C1–C4-alkyl or C1–C4-alkoxy group, and/or d) benalaxyl, ofurace, metalaxyl, furalaxyl or oxydixyl, and/or e) 1-(2-cyano-2-methoxyiminoacetyl)-3-ethylurea in a synergistically effective amount.Type: GrantFiled: June 28, 2002Date of Patent: September 19, 2006Assignee: BASF AktiengesellschaftInventors: Klaus Schelberger, Maria Scherer, Karl Eicken, Manfred Hampel, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann
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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: 6861539Abstract: Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: August 12, 2003Date of Patent: March 1, 2005Assignee: G. D. Searle & Co.Inventors: Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Raj Nagarajan, David L Brown, Joseph J McDonald
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Patent number: 6852738Abstract: A class of acyl sulfamides comprises compounds that are potent ligands for PPAR gamma and generally have antagonist or partial agonist activity. The compounds may be useful in the treatment, control or prevention of obesity, non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, inflammation, and other PPAR gamma mediated diseases, disorders and conditions.Type: GrantFiled: January 25, 2002Date of Patent: February 8, 2005Assignee: Merck & Co., Inc.Inventors: A. Brian Jones, John J. Acton, III
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Patent number: 6726919Abstract: A sterile, injectable homogenized dispersion of micromatrices or microdroplets having a mean diameter from about 50 nm to about 1000 nm comprising about 1% to about 7.5% of propofol, about 1% to about 8% of a propofol-soluble diluent, and about 0.67% to about 5% of a surface stabilizing amphiphilic agent suspended in an aqueous medium containing a synergetic quantity of antimicrobial agent and a tonicity modifying amount of a pharmaceutically acceptable water-soluble hydroxyl-group-containing excipient, wherein the ratio of propofol to diluent is in the range of about 0.25 to about 7.5 while the ratio of propofol to amphiphilic agent is in the range from about 0.4 to about 1.5, and wherein the viscosity of the dispersion is in the range of 1.1 to 8 cps, processes for the formation of the dispersion, and methods of use are disclosed.Type: GrantFiled: June 14, 2001Date of Patent: April 27, 2004Assignee: RTP Pharma, Inc.Inventors: Gary W. Pace, Michael G. Vachon, Awadesh K. Mishra, Robert A. Snow
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Publication number: 20040039016Abstract: Compounds useful for inhibiting HIV protease are disclosed. Methods of making the compounds, and their use as therapeutic agents, for example, in treating wild-type HIV and of multidrug-resistant strains of HIV, also are disclosed.Type: ApplicationFiled: March 6, 2003Publication date: February 26, 2004Inventors: Arun K. Ghosh, Geoffrey M. Bilcer, Thippeswamy Devasamudram
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Patent number: 6696488Abstract: Novel (hydroxyethyl)ureas are described. These compounds are effective inhibitors of certain aspartyl proteases, notably secretases involved in the enzymatic cleavage of amyloid precursor protein (APP) to yield amyloid-&bgr; peptide. Methods are provided for administering the novel compounds to treat &bgr;-amyloid-associated diseases, notably Alzheimer's disease.Type: GrantFiled: August 10, 2001Date of Patent: February 24, 2004Assignee: The Brigham and Women's Hospital, Inc.Inventors: Michael S. Wolfe, Dennis J. Selkoe
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Patent number: 6696497Abstract: A fungicidal composition comprises an acceptable carrier and/or surface active agent and a synergistically effective amount of (a) at least one benzophenone of formula I wherein R1, R2, R3, R4, R5, R6, R7, m and n have the meaning given; and at least one compound of formula II in which Ar and R8 have the meaning given. The composition is useful in a method of controlling the growth of phytopathogenic fungi at a locus. The method comprises applying synergistically effective amounts of (a) and (b) to the locus.Type: GrantFiled: February 13, 2001Date of Patent: February 24, 2004Assignee: BASF AktiengesellschaftInventors: Ewald Sieverding, Gunter Reichert
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Patent number: 6683210Abstract: Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: March 15, 2002Date of Patent: January 27, 2004Assignee: G. D. Searle & Co.Inventors: Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Raj Nagarajan, David L Brown, Joseph J McDonald
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Publication number: 20030229087Abstract: Novel active compound combinations of compounds of the formula (I) 1Type: ApplicationFiled: November 6, 2002Publication date: December 11, 2003Inventors: Astrid Mauler-Machnik, Ulrike Wachendorff-Neumann, Herbert Gayer
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Publication number: 20030139470Abstract: The invention relates to 3,4-dihydroxybenzyl-substituted carbonic acid derivatives, to their production, and to their use as antioxidants or free-radical scavengers, especially in cosmetic and pharmaceutical preparations and in foodstuffs and stimulants, to protect cells and tissues from the harmful effects of radicals and reactive oxygen compounds that accelerate aging. The invention further relates to cosmetic and pharmaceutical preparations and to foodstuffs and stimulants that comprises the inventive 3,4-dihydroxybenzyl-substituted carbonic acid derivatives.Type: ApplicationFiled: December 19, 2002Publication date: July 24, 2003Inventors: Jakob Peter Ley, William Johncock, Roland Langner
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Patent number: 6573284Abstract: Novel pro-drugs and assay reagents are provided which are useful as therapeutic agents especially for delivery and targetting therapeutically active agents to melanoma cells. The pro-drugs and assay reagents are substrates for tyrosinase and may be represented by the formula TyrX—B—ThrAg*. The compounds of formula TyrX—B—ThrAg* are capable of releasing a therapeutically active agent or assayable substance (ThrAg) at a desired location. TyrX— being a residue of an optionally substituted tyrosine analogue.Type: GrantFiled: June 14, 1999Date of Patent: June 3, 2003Inventors: Patrick Anthony Riley, Andrew Photiou, Tariq Hussain Khan, Helen Mary Osborn
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Publication number: 20020173542Abstract: New active compound combinations of valinamide derivatives of the formula (I) 1Type: ApplicationFiled: May 6, 2002Publication date: November 21, 2002Inventors: Heinz-Wilhelm Dehne, Wilhelm Brandes, Karl-Heinz Kuck, Thomas Seitz
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Patent number: 6465457Abstract: Fungicidal compounds of formula (I): wherein W is CH3O.Type: GrantFiled: August 18, 1994Date of Patent: October 15, 2002Assignee: Zeneca LimitedInventors: Ian Richard Matthews, Christopher Richard Ayles Godfrey, John Martin Clough
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Patent number: 6455581Abstract: &agr;- and &bgr;-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: May 25, 1995Date of Patent: September 24, 2002Assignee: G.D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw
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Publication number: 20020102279Abstract: The methods and compositions of the invention and the compounds used in the invention involve a novel immunosuppression mechanism, accelerated lymphocyte homing immunosuppression (ALH-immunosuppression). For example, the compound FTY720 specifically directs lymphocytes to the peripheral lymph nodes, mesenteric lymph nodes, and Peyer's patches. By reversibly sequestering lymphocytes in these tissues, the compounds can inhibit an immune response in a mammal. Understanding these mechanisms provides a novel immunosuppression therapy that can synergistically interact with other immunosuppressive compounds. Screening methods for identifying similar ALH-immunosuppression compounds are also described. The invention allows better treatments and therapies wherever an immunosuppression regimen is desired.Type: ApplicationFiled: June 15, 1999Publication date: August 1, 2002Inventors: KENJI CHIBA, KUNITOMO ADACHI
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Patent number: 6416789Abstract: A wood treatment material having a synergistic combination of fungicides including boron-containing compounds, organo-iodine compounds and amine-oxides is provided. This combination is shown to be especially effective in providing resistance to decay, mold and mildew when wood is treated with this combination. Also provided is wood treated by this combination, and a method of treatment for composite wood.Type: GrantFiled: January 5, 2001Date of Patent: July 9, 2002Assignee: Kop-Coat, Inc.Inventors: Brian Marks, Alan S. Ross, Hans A. Ward
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Publication number: 20020086900Abstract: Methods of synthesizing pharmacologically useful oxazolidinones are disclosed, and, in particular, a method of manufacturing a 5-(tert-butylcarbamoyl)-aminomethyl-oxazolidinone by condensing a carbamate with a tert-butylcarbamoyl protected derivative of glycidylamine or 3-amino-1-halopropanol.Type: ApplicationFiled: October 17, 2001Publication date: July 4, 2002Inventors: William R. Perrault, Robert C. Gadwood
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Publication number: 20020002192Abstract: The compounds of formula I are useful in treating gastrointestinal disorders associated with antagonizing the motilin receptor. The compounds compete with erythromycin and motilin for the motilin receptor. In addition the compounds are antagonists of the contractile smooth muscle response to those ligands.Type: ApplicationFiled: March 9, 2001Publication date: January 3, 2002Inventors: Robert H. Chen, Min A Xiang