Three Or More Ring Hetero Atoms In The Tetracyclo Ring System Patents (Class 546/64)
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Publication number: 20090093455Abstract: The present invention provides novel quinolone compounds and pharmaceutical composition thereof which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing such compounds and compositions, and methods of making and using the same.Type: ApplicationFiled: October 3, 2008Publication date: April 9, 2009Inventors: Johnny Yasuo NAGASAWA, Fabrice PIERRE, Mustapha HADDACH, Michael SCHWAEBE, Levan DARJANIA, Jeffrey P. WHITTEN
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Publication number: 20090082565Abstract: The present invention relates to the preparation of compounds which are capable of inducing cell death such as apoptotic cell death (apoptosis), and/or for reducing a cell proliferative disorder.Type: ApplicationFiled: November 19, 2008Publication date: March 26, 2009Applicant: Cylene Pharmaceuticals, Inc.Inventors: Peter C. CHUA, Johnny Y. Nagasawa, Michael Schwaebe, Fabrice Pierre
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Patent number: 7501435Abstract: The instant invention provides for compounds which comprise substituted triazoloquinazolinones that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer.Type: GrantFiled: April 24, 2007Date of Patent: March 10, 2009Assignee: Merck & Co., Inc.Inventors: Kenneth L. Arrington, Edward J. Brnardic, Vadim Y. Dudkin, Mark E. Fraley, Shaei Y. Huang, Cheng Wang
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Patent number: 7485649Abstract: The instant invention provides for compounds which comprise fused pyrazoles that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer.Type: GrantFiled: January 5, 2006Date of Patent: February 3, 2009Assignee: Merck & Co., Inc.Inventors: Edward J. Brnardic, Mark E. Fraley, Robert M. Garbaccio
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Publication number: 20090023767Abstract: The instant invention provides for compounds which comprise fused pyrazoles that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer.Type: ApplicationFiled: December 29, 2006Publication date: January 22, 2009Inventors: Edward J. Brnardic, Mark E. Fraley
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Publication number: 20090005356Abstract: Provided herein are substituted pyrrolopyridine heterocycles and substituted pyrazolopyridine heterocycles, pharmaceutical compositions comprising said heterocycles and methods of using said heterocycles in the treatment of disease. The heterocycles disclosed herein function as kinase modulators and have utility in the treatment of diseases such as cancer, allergy, asthma, inflammation, obstructive airway disease, autoimmune diseases, metabolic disease, infection, CNS disease, brain tumor, obesity, asthma, hematological disorder, degenerative neural disease, cardiovascular disease, or disease associated with angiogenesis, neovascularization, or vasculogenesis.Type: ApplicationFiled: May 29, 2008Publication date: January 1, 2009Applicant: SGX Pharmaceuticals, Inc.Inventors: Jeffrey M. Blaney, Andreas Gosberg, Stefan N. Gradl, Gavin Hirst, Stephanie A. Hopkins, Paul A. Sprengeler, Ruo W. Steensma, Johnny Uy
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Publication number: 20080300246Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, Bcr-Abl, BMX, BTK, CHK2, b-RAF, c-RAF, CSK, c-SRC, Fes, FGFR3, Flt3, IKK?, IKK?, JNK2? 2, Lck, Met, MKK4, MKK6, MST2, NEK2, p70S6K, PDGFR?, PKA, PKB?, PKD2, Rsk1, SAPK2?, SAPK2?, SAPK3, SGK, Tie2 and TrkB kinases.Type: ApplicationFiled: August 9, 2006Publication date: December 4, 2008Applicant: IRM LLCInventors: Yongping Xie, Guobao Zhang, Xing Wang, Nathanael S. Gray, Yi Liu
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Publication number: 20080214594Abstract: The instant invention provides for compounds which comprise fused pyrazoles that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer.Type: ApplicationFiled: January 5, 2006Publication date: September 4, 2008Inventors: Edward J. Brnardic, Mark E. Fraley, Robert M. Garbaccio
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Publication number: 20080125452Abstract: Compounds of a certain formula (I), in which R1, R2, R3, R4, R5 and X have the meanings indicated in the description, are novel effective compounds with anti-proliferative and/or apoptosis inducing activity.Type: ApplicationFiled: January 26, 2006Publication date: May 29, 2008Applicant: ALTANA PHARMA AGInventors: Matthias Vennemann, Thomas Bar, Jurgen Braunger, Petra Gimmnich, Thomas Beckers, Mathias Schmidt, Thomas Ciossek, Sandra Nappe
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Publication number: 20080114017Abstract: Compounds of a certain formula (I), in which R1, R2, R3, R4, R5, R6 and X have the meanings indicated in the description, are novel effective compounds with anti-proliferative and/or apoptosis inducing activity.Type: ApplicationFiled: January 26, 2006Publication date: May 15, 2008Inventors: Matthias Vennemann, Thomas Bar, Jurgen Braunger, Petra Gimmnich
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Publication number: 20080114016Abstract: The instant invention provides for compounds which comprise fused pyrazoles that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by ad-ministering the compound to a patient in need of treatment of cancer.Type: ApplicationFiled: January 5, 2006Publication date: May 15, 2008Inventors: Edward J. Brnardic, Mark E. Fraley, Robert M. Garbaccio, Justin T. Steen
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Patent number: 7291627Abstract: The invention concerns dihydroimidazo[5,1-a]-?-carboline compounds of general formula (I) wherein in particular, R1, R2, R3, R4, R6 and R7, identical or different, independently of one another, present a hydrogen, halogen atom, an alkyl, hydroxyl, alkoxy, trihalogenoalkyl, alkylamino, dialkylamino, aryl, arylalkyl, carboxy, alkylcarbonyloxy, acyl, aryloxy or arylalkoxy group; R5 represents a hydrogen atom, an alkyl or arylalkyl group; and their isomers as well as their addition salts to a pharmaceutically acceptable acid. The inventive compounds are for use in medicine, in particular as hypnotics.Type: GrantFiled: May 16, 2002Date of Patent: November 6, 2007Assignee: MACEFInventors: Jean-Bernard Fourtillan, Marianne Fourtillan, Omar Karam, Fabien Zunino, Jean-Claude Jacquesy, Jean-Pierre Tafani
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Patent number: 7144843Abstract: An objective of the present invention is to provide a harmful organism control agent that possesses excellent control effect against harmful organisms and can be safely used. The present invention provides a compound of formula (1) or a salt thereof. The present invention also provides a harmful organism control agent comprising the compound of formula (1). wherein R1, n, R2, and R3 are as defined in the specification.Type: GrantFiled: January 31, 2002Date of Patent: December 5, 2006Assignee: Meiji Seika Kaisha, Ltd.Inventors: Kazuhiko Oyama, Takeshi Teraoka, Kazumi Yamamoto
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Patent number: 7138408Abstract: Beta-carboline hydroxamic acid compounds represented by formula (I) are described. The beta-carboline hydroxamic acid compounds and compositions containing those compounds may be used to inhibit or modulate the activity of HIV integrase enzyme and to treat HIV integrase-mediated diseases and conditions.Type: GrantFiled: October 14, 2005Date of Patent: November 21, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Atsuo Kuki, Xinqiang Li, Michael Bruno Plewe, Hai Wang, Junhu Zhang
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Patent number: 7026482Abstract: A process for preparing 1H-imidazo[4,5-c]quinolin-4-amines is disclosed. The process involves reacting a 6H-imidazo[4,5-c]tetrazolo[1,5-a]quinoline with triphenylphosphine and hydrolyzing the product thereof.Type: GrantFiled: October 27, 2004Date of Patent: April 11, 2006Inventors: John F. Gerster, Kyle J. Lindstrom
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Patent number: 7001912Abstract: Beta-carboline hydroxamic acid compounds represented by formula (I) are described. The beta-carboline hydroxamic acid compounds and compositions containing those compounds may be used to inhibit or modulate the activity of HIV integrase enzyme and to treat HIV integrase-mediated diseases and conditions.Type: GrantFiled: January 26, 2004Date of Patent: February 21, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Atsuo Kuki, Xinqiang Li, Michael Bruno Plewe, Hai Wang, Junhu Zhang
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Patent number: 6967215Abstract: Tetrahydrocarbazoles of formula where Q is —SO2—; —O—; or —(CO)—; X is —(CH)—; or —N—; m is from 1 to 3; t is 0 or 1 and the remaining substituents are as defined herein, are useful as antimicrobial active ingredients.Type: GrantFiled: September 11, 2001Date of Patent: November 22, 2005Assignee: Ciba Specialty Chemicals CorporationInventors: Wolfgang Haap, Andreas Mehlin, Karin Petzold, Dietmar Ochs, Werner Hölzl
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Patent number: 6960585Abstract: Compounds of formula (I), or pharmaceutically-acceptable salts thereof, are useful in treating inflammatory and immune diseases and disorders, wherein X, Y1, Y2, and R2-4 are as defined in the specification.Type: GrantFiled: September 27, 2001Date of Patent: November 1, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Francis Beaulieu, Carl Quellet, Makonen Belema, Yuping Qiu, Xuejie Yang, Fred C. Zusi
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Patent number: 6949646Abstract: Imidazonaphthyridine and tetrahydroimidazonaphthyridine compounds induce the biosynthesis of cytokines such as interferon and tumor necrosis factor. The compounds exhibit antiviral and antitumor properties. Methods of preparing the compounds and intermediates useful in the preparation of the compounds are also disclosed.Type: GrantFiled: December 3, 2004Date of Patent: September 27, 2005Assignee: 3M Innovative Properties Co.Inventors: John F. Gerster, Kyle J. Lindstrom, Stephen L. Crooks, Philip D. Heppner, Gregory J. Marszalek, Peter V. Maye, Bryon A. Merrill, John W. Mickelson, Michael J. Rice
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Patent number: 6927292Abstract: The invention relates to compounds of Formula (1), in which the substituents and symbols have the meanings indicated in the description. The compounds are valuable intermediates for the preparation of pharmaceutical active compounds.Type: GrantFiled: July 31, 2002Date of Patent: August 9, 2005Assignee: Altana Pharma AGInventors: Jörg Senn-Bilfinger, Peter Jan Zimmermann
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Patent number: 6858620Abstract: Compounds of general structural formula (I), and use of the compounds or salts or solvates thereof as therapeutic agents, are disclosedType: GrantFiled: September 17, 2001Date of Patent: February 22, 2005Assignee: Lilly ICOS, LLCInventors: Mark W. Orme, Jason Scott Sawyer, Alain Claude-Marie Daugan, Romain Luc Marie Gosmini, Lisa M. Schultze
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Patent number: 6852727Abstract: Benzimidazo[4,5-f]isoquinolinone derivatives are inhibitors of Janus protein tyrosine kinases (Jak), and as such are useful as immunosuppressants, and in the treatment of diseases including asthma, allergies, autoimmune diseases.Type: GrantFiled: July 26, 2002Date of Patent: February 8, 2005Assignee: Merck & Co., Inc.Inventors: Joung L. Goulet, Rose M. Cubbon, Richard T. Cummings, Xingfang Hong, Peter J. Sinclair, James E. Thompson
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Patent number: 6838456Abstract: Compounds of the general structural formula and use of the compounds and salts and solvates thereof, as therapeutic agents.Type: GrantFiled: September 17, 2001Date of Patent: January 4, 2005Assignee: Lilly ICOS LLCInventors: Mark W. Orme, Jason Scott Sawyer, Alain Claude-Marie Daugan, Françoise Gellibert, Romain Luc Marie Gosmini
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Publication number: 20040265628Abstract: The invention provides organic compounds of the general structure (1) 1Type: ApplicationFiled: April 16, 2004Publication date: December 30, 2004Inventors: Suning Wang, Ruiyao Wang
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Patent number: 6809096Abstract: A pharmaceutical composition including an efficient amount of a compound selected among the compounds of formulae (I) and (Ia). The compounds have interesting cytotoxic properties leading to a therapeutic use as antitumoral medicines.Type: GrantFiled: February 13, 2002Date of Patent: October 26, 2004Assignee: Laboratoire L. LafonInventors: Evelyne Delfourne, Francis Darro, Jean Bastide, Robert Kiss, Armand Frydman
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Publication number: 20040204436Abstract: Imidazonaphthyridine and tetrahydroimidazonaphthyridine compounds induce the biosynthesis of cytokines such as interferon and tumor necrosis factor. The compounds exhibit antiviral and antitumor properties. Methods of preparing the compounds and intermediates useful in the preparation of the compounds are also disclosed.Type: ApplicationFiled: April 14, 2004Publication date: October 14, 2004Inventors: John F. Gerster, Kyle J. Lindstrom, Stephen L. Crooks, Philip D. Heppner, Gregory J. Marszalek, Peter V. Maye, Bryon A. Merrill, John W. Mickelson, Michael J. Rice
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Publication number: 20040176597Abstract: The invention relates to compounds of Formula (1), in which the substituents and symbols have the meanings indicated in the description. The compounds are valuable intermediates for the preparation of pharmaceutical active compounds.Type: ApplicationFiled: January 30, 2004Publication date: September 9, 2004Inventors: Jorg Senn-Bilfinger, Peter Jan Zimmermann
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Publication number: 20040147538Abstract: Compounds, compositions and methods are provided that are useful in the treatment and/or prevention of a condition or disorder mediated by a G-protein coupled receptor. In particular, the compounds of the invention are useful in the treatment and/or prevention of eating disorders, obesity, anxiety disorders and mood disorders.Type: ApplicationFiled: November 6, 2003Publication date: July 29, 2004Inventors: Xi Chen, Xiaoqi Chen, Pingchen Fan, Juan Jaen, Leping Li, Jeffrey Thomas Mihalic
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Patent number: 6747039Abstract: The present invention relates to a group of aza-anthrapyrazole compounds having antitumor activity, and processes for their preparation. Compositions containing the aza-anthrapyrazole compounds and methods of treating tumors and cancer in mammals with the compounds of the present invention are also disclosed.Type: GrantFiled: March 12, 2002Date of Patent: June 8, 2004Assignee: Albany Molecular Research, Inc.Inventor: Simon N. Haydar
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Publication number: 20040097535Abstract: There are described tetrahydrocarbazoles of formula (1) or (2). The compounds are suitable as antimicrobial active ingredients.Type: ApplicationFiled: March 13, 2003Publication date: May 20, 2004Inventors: Wolfgang Haap, Andreas Mehlin, Karin Petzold, Dietmar Ochs, Werner Holzl
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Publication number: 20040082787Abstract: Compounds of general structural formula (I), and use of the compounds or salts or solvates thereof as therapeutic agents, are disclosed.Type: ApplicationFiled: March 3, 2003Publication date: April 29, 2004Inventors: Mark W Orme, Jason Scott Sawyer, Alain Claude-Marie Daugan, Romain Luc Marie Gosmini, Lisa M Schultze
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Patent number: 6720420Abstract: The present invention provides oxazine compounds having aromatic, heteroaromatic, or aliphatic substituents at the 2 position of the oxazine moiety.Type: GrantFiled: December 21, 2001Date of Patent: April 13, 2004Assignee: Johnson & Johnson Vision Care, Inc.Inventors: Weili Zhao, Erick M. Carreira
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Patent number: 6699899Abstract: Imido and amido substituted acylhydroxamic acids which reduce the levels of TNF&agr; and inhibit phosphodiesterase in a mammal. A typical embodiment is (3-(1,3-dioxoisoindolin-2-yl)-3-(3-ethoxy-4-methoxyphenyl)propanoylamino)propanoate.Type: GrantFiled: December 21, 1999Date of Patent: March 2, 2004Assignee: Celgene CorporationInventors: Hon-Wah Man, George W Muller, Shaei Y Huang
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Patent number: 6686466Abstract: The present invention provides photochromic oxazine compounds and methods for their manufacture, which compounds are useful as photochromic compounds. The compounds of the invention have aromatic substituents on the 2 position of the oxazine moiety.Type: GrantFiled: November 13, 2001Date of Patent: February 3, 2004Assignee: Johnson & Johnson Vision Care, Inc.Inventors: Weili Zhao, Erick M. Carreira
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Publication number: 20040019213Abstract: A process for preparing 1H-imidazo[4,5-c]quinolin-4-amines is disclosed. The process involves reacting a 6H-imidazo[4,5-c]tetrazolo[1,5-a]quinoline with triphenylphosphine and hydrolyzing the product thereof.Type: ApplicationFiled: July 21, 2003Publication date: January 29, 2004Applicant: 3M Innovative Properties CompanyInventors: John F. Gerster, Kyle J. Lindstrom
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Patent number: 6683142Abstract: The present invention relates to 1-alkoxy-polyalkyl-piperidine derivatives containing a structural element of formula (I) wherein G1, G2, G3, G4 are independently C1-C6alkyl with the proviso that at least one is not methyl or G1 and G2 or G3 and G4, or G1 and G2 and G3 and G4 together form a C5-C12cycloalkyl group; G5, G6 independently are H, C1-C18alkyl, phenyl, naphthyl or a group COOC1-C18alkyl and X represents a group such that the free radical X. derived from X is capable of initiating polymerization of ethylenically unsaturated monomers, with the proviso that compounds A1 and A2 are excluded Further subjects of the invention are a polymerizable composition comprising a) at least one ethylenically unsaturated monomer and b) a 1-alkoxy-polyalkyl-piperidine derivative, a process for polymerizing ethylenically unsaturated monomers, and the use of 1-alkoxy-polyalkyl-piperidine derivatives for controlled polymerization.Type: GrantFiled: December 11, 2001Date of Patent: January 27, 2004Assignee: Ciba Specialty Chemicals CorporationInventors: Andreas Kramer, Peter Nesvadba
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Patent number: 6667405Abstract: Disclosed is a compound represented by the following formula (I): wherein Z1 represents an atomic group necessary to form a 5- or 6-membered nitrogen-containing heterocyclic ring; Z2 represents an atomic group necessary to form a 5- or 6-membered heterocyclic ring, Z2 may further be substituted, or may be condensed with a hetero ring or a benzene ring; R1 represents a hydrogen atom, a halogen atom, a mercapto group, an alkyl group, an alkenyl group, an aryl group, an alkylthio group, an alkenylthio group, or an arylthio group; L1 and L2 each represents a methine group; p1 represents 0 or 1; V1 represents a substituent; and n represents 0, 1 or 2, and when n represents 2, a plurality of V1 may be the same or different.Type: GrantFiled: November 1, 2001Date of Patent: December 23, 2003Assignee: Fuji Photo Film Co., Ltd.Inventors: Katsumi Kobayashi, Takashi Katoh, Junji Nishigaki
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Patent number: 6664260Abstract: Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain ether and heterocyclyl or heteroaryl functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.Type: GrantFiled: December 6, 2001Date of Patent: December 16, 2003Assignee: 3M Innovative Properties CompanyInventors: Leslie J. Charles, Joseph F. Dellaria, George W. Griesgraber, Philip D. Heppner, Karl J. Manske, John W. Mickelson, Michael J. Rice
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Publication number: 20030207906Abstract: Compounds of the general structural formula and use of the compounds and salts and solvates thereof, as therapeutic agents.Type: ApplicationFiled: February 28, 2003Publication date: November 6, 2003Inventors: Mark W. Orme, Jason Scott Sawyer, Alain Claude-Marie Daugan, Francoise Gellibert, Romain Luc Marie Gosmini
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Patent number: 6624305Abstract: A process for preparing 1H-imidazo[4,5-c]quinolin-4-amines is disclosed. The process involves reacting a 6H-imidazo[4,5-c]tetrazolo[1,5-a]quinoline with triphenylphosphine and hydrolyzing the product thereof.Type: GrantFiled: February 6, 2003Date of Patent: September 23, 2003Assignee: 3M Innovative Properties CompanyInventors: John F. Gerster, Kyle J. Lindstrom
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Process to prepare (5R)-(methylamino)-5, 6-dihydro-4H-imidazo[4,5,1-ij]-quinolin-2(1H)-one
Patent number: 6586595Abstract: The present invention is an improved prosess to prepare (5R)-(methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one the compound of formula (VII)Type: GrantFiled: August 22, 2001Date of Patent: July 1, 2003Assignee: Pharmacia & Upjohn CompanyInventor: Peter Guillaume Marie Wuts -
Publication number: 20030091505Abstract: The present invention provides compounds of Formula (I): 1Type: ApplicationFiled: October 15, 2002Publication date: May 15, 2003Inventor: Jian-Min Fu
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Patent number: 6562964Abstract: Compounds of the formula (I): wherein A, Y, R, X, R1, R2, R3 and R4 are as defined above are inhibitors of rotamase enzymes in particular FKBP-12 and FKBP-52. The compounds therefore moderate neuronal regeneration and outgrowth and can be used for treating neurological disorders arising from neurodegenerative diseases or other disorders involving nerve damage.Type: GrantFiled: January 23, 2002Date of Patent: May 13, 2003Assignee: Pfizer IncInventors: Mark Ian Kemp, Michael John Palmer, Mark Allen Sanner, Martin James Wythes
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Patent number: 6541484Abstract: A class of substituted and/or ring-fused pyrazolo[3,4-b]pyridine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent on the pyrazole nitrogen atom adjacent the pyridine nucleus, and an optionally substituted cycloalkyl-alkoxy, aryl-alkoxy or heteroaryl-alkoxy substituent on the carbon atom adjacent the pyridine ring nitrogen atom, are selective ligands for GABAA receptors, in particular having high affinity for the &bgr;2 and/or &bgr;3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse neurological disorders, including anxiety and convulsions.Type: GrantFiled: June 14, 2002Date of Patent: April 1, 2003Assignee: Merck Sharp & Dohme LimitedInventors: Ian James Collins, Linda Elizabeth Keown, Leslie Joseph Street
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Patent number: 6476021Abstract: Novel fused tetracyclic heterocyclic compounds having a potent and highly selective effect of inhibiting cyclic GMP phosphodiesterase (cGMP-PDE) and a high safety; a process for producing the same; drugs characterized by containing at least one of these compounds as the active ingredient, in particular, preventives and/or remedies for pulmonary hypertension, ischemic heart diseases, erectile insufficiency, female sexual dysfunction or diseases against which cGMP-PDE inhibitory effects are efficacious and intermediates useful in producing the above compounds.Type: GrantFiled: May 26, 2000Date of Patent: November 5, 2002Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Masayuki Ohashi, Hidemitsu Nishida, Toshiyuki Shudo
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Patent number: 6469021Abstract: Non-peptide compounds that act as antagonists of the intestinal hormone glucagons-like peptide 1 (GLP-1) have a 9H-b-carboline central motif. The compounds exhibit advantageous physical, chemical and biological properties and inhibit GLP-1 peptide binding to the GLP-1 receptor and/or prevent activation of the receptor by bound GLP-1. The invention further relates to a method of inhibiting the binding of GLP-1 to the GLP-1 receptor and a method of inhibiting the activation of the GLP-1 receptor. Intermediate compounds useful for making non-peptide GLP-1 receptor antagonists are also described.Type: GrantFiled: October 26, 2001Date of Patent: October 22, 2002Assignee: Agouron Pharmaceuticals, Inc.Inventors: Larry Kenneth Truesdale, Richard A. Bychowski, Javier Gonzalez, Atsuo Kuki, Ranjan Jagath Rajapakse, Min Teng, Dan Kiel, Daljit S. Dhanoa, Yufeng Hong, Tso-sheng Chou, Anthony L. Ling, Michael David Johnson, Vlad Edward Gregor
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Patent number: 6451809Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof where R1-R4 and A are defined herein, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors and are, therefore, useful in the diagnosis and treatment of anxiety, Down Syndrome, depression, sleep, cognitive and seizure disorders, overdose with benzodiazepine drugs and for enhancement of alertness.Type: GrantFiled: January 16, 2001Date of Patent: September 17, 2002Assignee: Neurogen CorporationInventors: Bogumila Rachwal, Pamela Albaugh, Kenneth Shaw
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Publication number: 20020081626Abstract: Methods and kits for determine arginine compounds are discussed. The methods and kits of the invention can be used for the diagnosis of arginine compound associated disorders.Type: ApplicationFiled: July 5, 2001Publication date: June 27, 2002Inventors: Rima Kaddurah-Daouk, Thomas W. Bell, Alisher B. Khasanov
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Patent number: 6384045Abstract: This invention provides cancer-active tricyclic and tetracyclic oxypyrones and a method of synthesizing these compounds. Preferred compounds have aryl groups at the 3-position of the oxypyrone ring. The tricyclic oxypyrone synthetic method is a simple condensation reaction of pyrones with cyclohexenecarboxaldehydes, providing high yields and using few steps. The tetracyclic oxypyrone synthetic method is a simple condensation reaction of carvones with pyrones.Type: GrantFiled: June 24, 1999Date of Patent: May 7, 2002Assignee: Kansas State University Research FoundationInventors: Duy H. Hua, Jean-Pierre Perchellet
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Patent number: 6355802Abstract: The present invention is an improved prosess to prepare (5R)-(methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one the compound of formula (VII).Type: GrantFiled: January 31, 2000Date of Patent: March 12, 2002Assignee: Pharmacia & Upjohn COmpanyInventor: Peter Guillaume Marie Wuts