The Additional Hetero Ring Is One Of The Cyclos In A Polycyclo Ring System Patents (Class 514/337)
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Patent number: 7189758Abstract: A compound of Formula (I) wherein R1, R2, R3, R4, R5, and R6 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.Type: GrantFiled: October 5, 2005Date of Patent: March 13, 2007Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Rajashekhar Betageri, David Thomson, Yan Zhang, Renee Michele Zindell
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Patent number: 7186719Abstract: Compounds of formula (II) are antibacterial agents wherein Q represents a radical of the formula: —N(OH)CH(?O) or the formula: —C(?O)NH(OH); R1 represents hydrogen, C1–C6 alkyl or C1–C6 alkyl substituted by one or more halogen atoms, or, except when Q is a radical of the formula: —N(OH)CH(?O), a hydroxy, C1–C6 alkoxy, C1–C6 alkenyloxy, amino, C1–C6 alkylamino, or di-(C1–C6 alkyl)amino group; R2 represents a substituted or unsubstituted C1–C6 alkyl, cycloalkyl(C1–C6 alkyl)- or aryl(C1–C6 alkyl)-group; and A represents a group of formula (IIA), or (IIB) wherein R4 represents the side chain of a natural or non-natural alpha amino acid, and R5 and R6 when taken together with the nitrogen atom to which they are attached form a saturated heterocyclic first ring of 5 to 7 atoms as specified in the description.Type: GrantFiled: September 30, 2004Date of Patent: March 6, 2007Assignee: British Biotech PharmaceuticalsInventors: Lisa Marie Pratt, Kenneth Noel Keavey, Gilles Denis Pain, Laurent Mounier
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Patent number: 7179821Abstract: N-(Pyridinyl)-1H-indol-1-amines of formula I provide a unique combination of blocking properties for both the potassium and sodium channels. These compounds are useful for the treatment of Demyelinating Diseases and Conditions such as Multiple Sclerosis, Spinal Cord Injury, Traumatic Brain Injury and Stroke. The compounds are also useful for Stroke Rehabilitation, the treatment of Bladder Irritation and Dysfunction, and the treatment of Neuropathic Pain and Chemokine-Induced Pain.Type: GrantFiled: March 14, 2005Date of Patent: February 20, 2007Assignee: Aventis Pharmaceuticals Inc.Inventors: Craig P Smith, Michel P Rathbone, Margaret Petty, David Rampe
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Patent number: 7157474Abstract: Compositions comprising a taxane having a heterosubstituted acetate substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.Type: GrantFiled: February 28, 2005Date of Patent: January 2, 2007Assignee: FSU Research Foundation, Inc.Inventor: Robert A. Holton
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Patent number: 7153871Abstract: PDE4 inhibition is achieved by novel compounds, e.g., aminoindazole and aminobenzofuran analogs. The compounds of the present invention are of Formulas I and II: wherein R1, R2, R3, R4, R7 and R8 are as defined herein.Type: GrantFiled: July 18, 2003Date of Patent: December 26, 2006Assignee: Memory Pharmaceuticals CorporationInventors: Richard A. Schumacher, Allen T. Hopper, Ashok Tehim
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Patent number: 7144885Abstract: This invention relates to a novel fused tricyclic heterocycle of the formula (Ia, Ib) and its use for the treatment of hyper-proliferative disordersType: GrantFiled: February 21, 2003Date of Patent: December 5, 2006Assignee: Bayer Pharmaceuticals CorporationInventors: Chengzhi Zhang, Michael Burke, Zhi Chen, Jacques Dumas, Dongping Fan, Benjamin D. Jones, Gaetan Ladouceur, Wendy Lee, Barton Phillips, Scott M. Wilhelm, Qian Zhao
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Patent number: 7129234Abstract: The invention relates to compounds of formula IType: GrantFiled: November 25, 2003Date of Patent: October 31, 2006Assignee: Pfizer Inc.Inventors: Mavis D. Adam, Mark D. Andrews, Geoffrey E. Gymer, David Hepworth, Harry R. Howard, Jr., Donald S. Middleton, Alan Stobie
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Patent number: 7122680Abstract: The present invention relates to a ?3 adrenergic receptor agonist of formula I: or a pharmaceutical salt thereof; which is useful for treating Type II diabetes and/or obesity.Type: GrantFiled: October 21, 2004Date of Patent: October 17, 2006Assignee: Eli Lilly and CompanyInventors: Cynthia Darshini Jesudason, Daniel Jon Sall, Freddie Craig Stevens, John Arnold Werner
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Patent number: 7105513Abstract: The present invention relates to acylated, heteroaryl-condensed cycloalkenylamines, to pharmaceutical compositions comprising such compounds, to methods for the stimulation of the expression of endothelial NO synthase, and methods of treatment comprising administering such compounds.Type: GrantFiled: July 31, 2003Date of Patent: September 12, 2006Assignee: Sanofi-Avertis Deutschland GmbHInventors: Hartmut Strobel, Paulus Wohlfart
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Patent number: 7087625Abstract: PDE4 inhibition is achieved by novel nitroxide compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formulas I–III: wherein A, B, D, R1, R2, R3, R7, R8, R9, R10 and R6are as defined herein.Type: GrantFiled: November 19, 2003Date of Patent: August 8, 2006Assignee: Memory Pharmaceuticals CorporationInventors: Richard A. Schumacher, Elizabeth Doorly Graham, Allen T. Hopper, Ashok Tehim
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Patent number: 7081468Abstract: Ortho-substituted anthranilic acid amides and use thereof as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis are described.Type: GrantFiled: May 8, 2001Date of Patent: July 25, 2006Assignee: Schering AGInventors: Martin Krueger, Andreas Huth, Orlin Petrov, Dieter Seidelmann, Karl-Heinz Thierauch, Martin Haberey, Andreas Menrad, Alexander Ernst
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Patent number: 7056946Abstract: Taxanes having a carbonate substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.Type: GrantFiled: November 24, 2003Date of Patent: June 6, 2006Assignee: FSU Research Foundation, Inc.Inventor: Robert A. Holton
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Patent number: 7045545Abstract: The present invention provides serotonergic aminoalkylbenzofurans of Formula (I): where R, R1, R2, R3, R4, R4?, R5, R5?, and R12 are as described in the specification.Type: GrantFiled: January 19, 2000Date of Patent: May 16, 2006Assignee: Eli Lilly and CompanyInventors: Karin Briner, Joseph Paul Burkhart, Timothy Paul Burkholder, Matthew Joseph Fisher, William Harlan Gritton, Daniel Timothy Kohlman, Sidney Xi Liang, Shawn Christopher Miller, Jeffrey Thomas Mullaney, Yao-Chang Xu, Yanping Xu
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Patent number: 7034035Abstract: The present invention relates to compounds of Formula I: wherein: a) ?represents a 6-membered heterocyclic aromatic ring in which X1 is N and X2, X3 and X4 are each independently CR?; R? is independently H, halogen, cyano, hydroxy, C1-C3 alkyl, C1-C3 haloalkyl, cyclopropyl, C1-C3 alkoxy, C1-C3 haloalkoxy, C1-C3 alkylthio, aryl, C1-C3 NHC(O)alkyl, NHC(O)H, C1-C3 haloalkylthio, C2-C4 alkenyl, C2-C4 haloalkenyl, C2-C4 alkynyl, C2-C4 haloalkynyl or nitro wherein adjacent R? substituents may form a ring; b) Z is O, S or NORZ in which RZ is H or C1-C3 alkyl; and c) A represents (i) C3-C14 cycloalkyl, containing 1 or 3 heteroatoms and 0-2 unsaturations, which may be unsubstituted or substituted with halogen, hydroxy, C1-C6 alkyl, C1-C6 haloalkyl, cyano, nitro, aroyl, aryloxy, heteroaryloxy, C1-C6 alkylthio, arylthio, heteroarylthio, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C8 acyloxy, aryl, heteroaryl, C1-C6 acyl, C1-C6 carboalkoxy or amido unsubstituted or substituted with one or two C1 -C6 alkyl groups, oType: GrantFiled: December 2, 2002Date of Patent: April 25, 2006Assignee: Dow AgroSciences LLCInventors: Michael J. Ricks, William H. Dent, III, Richard B. Rogers, Chenglin Yao, Bassam S. Nader, John L. Miesel, Gina M. Fitzpatrick, Kevin G. Meyer, Noormohamed M. Niyaz, Irene M. Morrison, Robert P. Gajewski
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Patent number: 7034044Abstract: The present invention relates to compounds of formulae The compounds of the present invention are NMDA (N-methyl-D-aspartate)-receptor subtype blockers and are used in the treatment of diseases related to this receptor.Type: GrantFiled: September 26, 2003Date of Patent: April 25, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Alanine, Bernd Buettelmann, Marie-Paule Heitz Neidhart, Emmanuel Pinard, Rene Wyler
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Patent number: 6995162Abstract: Selected heterocyclic compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: January 10, 2002Date of Patent: February 7, 2006Assignee: Amgen Inc.Inventors: Guoqing Chen, Jeffrey Adams, Jean Bemis, Shon Booker, Guolin Cai, Lucian Di Pietro, Celia Dominguez, Daniel Elbaum, Julie Germain, Stephanie Geuns-Meyer, Michael Handley, Qi Huang, Joseph L. Kim, Tae-Seong Kim, Alexander Kiselyov, Xiaohu Ouyang, Vinod F. Patel, Leon M. Smith, Markian Stec, Andrew Tasker, Ning Xi, Shimin Xu, Chester Chenguang Yuan, Michael Croghan
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Patent number: 6992104Abstract: Taxanes having a carbonate substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.Type: GrantFiled: December 22, 2003Date of Patent: January 31, 2006Assignee: FSU Research Foundation, Inc.Inventor: Robert A. Holton
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Patent number: 6989398Abstract: Benzanilides are provided which are voltage-dependent potassium channel openers. Methods of using the benzanilides of the invention are also provided.Type: GrantFiled: February 2, 2004Date of Patent: January 24, 2006Assignee: ICAgen, Inc.Inventors: Grant A. McNaughton-Smith, Michael F. Gross, Alan D. Wickenden
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Patent number: 6967210Abstract: N-(Pyridinyl)-1H-indol-1-amines of formula I provide a unique combination of blocking properties for both the potassium and sodium channels. These compounds are useful for the treatment of Demyelinating Diseases and Conditions such as Multiple Sclerosis, Spinal Cord Injury, Traumatic Brain Injury and Stroke. The compounds are also useful for Stroke Rehabilitation, the treatment of Bladder Irritation and Dysfunction, and the treatment of Neuropathic Pain and Chemokine-Induced Pain.Type: GrantFiled: February 14, 2002Date of Patent: November 22, 2005Assignee: Aventis Pharmaceuticals Inc.Inventors: Craig P. Smith, Michel P. Rathbone, Margaret Petty, David Rampe
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Patent number: 6962942Abstract: The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds having Formula I: or pharmaceutically acceptable salts thereof; wherein Q is phenyl, benzyl, pyridyl, thienyl, indolyl, quinolinyl, benzothienyl, biphenylyl, or imidazolyl; any of which can include one or more optional substituents independently selected from halo, trifluoromethyl, hydroxy, amino, nitro, cyano, C1 alkoxy, C1-3 alkyl, methylenedioxy, carboxamido, acetamido, or amidino; X is methylene, carbonyl, or sulfonyl; Z is methylene, ethylene, or propylene; M is methylene or ethylene; and R1 R2 and R3 are independently hydrogen or C1-3 alkyl.Type: GrantFiled: September 16, 2002Date of Patent: November 8, 2005Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Scott C. Miller, Juan José Marugán Sánchez, Kristin D. Haslow, Jonathan Hall
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Patent number: 6949539Abstract: The invention provides compounds of general formula (I) in which m, A, R1 and Ar have the meanings defined in the specification; a process for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.Type: GrantFiled: June 1, 2001Date of Patent: September 27, 2005Assignee: AstraZeneca ABInventors: Lilian Alcaraz, Mark Furber
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Patent number: 6943182Abstract: The invention relates to cyclopentabenzofuran derivatives, process for their preparation, the use of cyclopentabenzofuran derivatives for the production of a medicament for the therapy of NF-?B-dependent diseases and medicaments which contain the cyclopentabenzofuran derivatives.Type: GrantFiled: May 30, 2002Date of Patent: September 13, 2005Assignee: Bayer AktiengesellschaftInventors: Walter Guarnieri, Thomas Jaetsch, Andreas Schoop, Jörg Baumgarten, Axel Kretschmer, Horst-Peter Antonicek
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Patent number: 6933305Abstract: The present invention relates to an amide compound of the formula wherein R1 is a hydrogen and the like, R2 is a hydrogen and the like, X is SO2 and the like, Y is the formula (III) and the like and a is 2, an isomer thereof or pharmaceutically acceptable salts thereof. The compound of the present invention shows a remarkable and selective Rho kinase inhibitory action, is free of problematic toxicity, shows fine oral absorption and drug kinetics (absorption, distribution, metabolism, excretion and the like of the drug), and shows superior properties (e.g., stability etc.) as a compound. Accordingly, it can be used as a therapeutic drug for various diseases in which Rho kinase is involved.Type: GrantFiled: March 16, 2001Date of Patent: August 23, 2005Assignee: Mitsubishi Pharma CorporationInventors: Shinichi Takanashi, Yoichiro Naito, Hiroshi Tanaka, Masayoshi Uehata, Koshiro Katayama
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Patent number: 6919371Abstract: This invention relates to novel 2,6-substituted chroman derivatives which are useful in the treatment of beta-3 adrenoreceptor-mediated conditions.Type: GrantFiled: September 17, 2003Date of Patent: July 19, 2005Assignee: Bayer Pharmaceuticals CorporationInventors: Stephen J. O'Connor, Gaetan H. Ladouceur, William H. Bullock, Ann-Marie Campbell, Miao Dai, Robert Dally, Jacques Dumas, Holia N. Hatoum-Mokdad, Uday Khire, Wendy Lee, Qingjie Liu, Derek B. Lowe, Steven R. Magnuson, Ning Qi, Tatiana E. Shelekhin, Quanrong Shen, Roger A. Smith, Ming Wang
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Patent number: 6906088Abstract: Taxanes having a carbamoyloxy substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.Type: GrantFiled: July 11, 2003Date of Patent: June 14, 2005Assignee: FSU Research Foundation, Inc.Inventors: Robert A. Holton, Weishuo Fang
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Patent number: 6903121Abstract: Compounds of Formula 1 Formula 1 where the symbols have the meaning described in the specification, and particularly the compound of Formula 3 Formula 3 (tazarotene) exhibit synergistic anti-proliferative effect with human recombinant interferon in the treatment of solid tumors and leukemia, particularly breast cancer and acute myeloid leukemia.Type: GrantFiled: August 17, 2000Date of Patent: June 7, 2005Assignee: Allergan, Inc.Inventors: Alissar Nehme, Richard L. Beard, Roshantha A. Chandraratna
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Patent number: 6894065Abstract: Heterocyclic-substituted compounds of the formula or a pharmaceutically acceptable salt thereof, are disclosed, wherein: Z is —(CH2)n—; ?wherein R10 is absent; or ?wherein R3 is absent; the single dotted line represents an optional double bond; the double dotted line represents an optional single bond; n is 0-2; Het is an optionally substituted mono-, bi- or tricyclic heteroaromatic group; B is —(CH2)n3—, wherein n3 is 0-5, —CH2—O—, —CH2S—, —CH2—NR6—, —C(O)NR6—, —NR6C(O)—, ?optionally substituted alkenyl or optionally substituted alkynyl; X is —O— or —NR6— when the double dotted line represents a single bond, or X is H, —OH or —NHR20 when the bond is absent; Y is ?O, ?S, (H, H), (H, OH) or (H, C1-C6 alkoxy) when the double dotted line represents a single bond, or when the bond is absent, Y is ?O, ?NOR17, (H, H), (H, OH), (H, SH), (H, C1-C6 alkoxy) or (H, substituted-amino); R22 and R23 are independently —OH, —OC(O)R30, OC(O)NR30R31, or optionally substituted alkyl, alkenyl, alkynyl, heterocType: GrantFiled: June 9, 2003Date of Patent: May 17, 2005Assignee: Schering CorporationInventors: Samuel Chackalamannil, Mariappan V. Chelliah, Yan Xia
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Patent number: 6881733Abstract: The present invention provides serotonergic benzofurans of Formula (I): where A, R, R1, R2, R3, and R4 are as described in the specification.Type: GrantFiled: July 21, 2000Date of Patent: April 19, 2005Assignee: Eli Lilly and CompanyInventors: Karin Briner, Joseph Paul Burkhart, Timothy Paul Burkholder, Brian Eugene Cunningham, Matthew Joseph Fisher, William Harlan Gritton, Cynthia Darshini Jesudason, Shawn Christopher Miller, Jeffrey Thomas Mullaney, Matthew Robert Reinhard, Roger Ryan Rothhaar, Freddie Craig Stevens, Leonard Larry Winneroski, Yanping Xu, Yao-Chang Xu
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Patent number: 6878714Abstract: Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: July 17, 2002Date of Patent: April 12, 2005Assignee: Amgen Inc.Inventors: Benny Askew, Jeffrey Adams, Shon Booker, Guoqing Chen, Lucian V. DiPietro, Daniel Elbaum, Julie Germain, Stephanie D. Geuns-Meyer, Gregory J. Habgood, Michael Handley, Qi Huang, Tae-Seong Kim, Aiwen Li, Nobuko Nishimura, Rana Nomak, Vinod F. Patel, Babak Riahi, Joseph L. Kim, Ning Xi, Kevin Yang, Chester Chenguang Yuan
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Patent number: 6875768Abstract: Heterocyclic amine derivatives represented by general formula (I): wherein R1, R2 and R3 represent each H, optionally halogenated C3-6 cycloalkyl, etc.; Q represents an optionally substituted heterocycle containing O, S or N; X represents halogeno, cyano, halo(C1-6)alkyl, etc.; n is from 1 to 4; and Z1 and Z2 represent each O or S; and intermediates thereof represented by the following general formula (IV?): Q?—NH2 wherein Q? represents a definite heterocycle selected from among those represented by Q. Agricultural/horticultural insecticides having a remarkable effect of controlling pest insects of crops such as rice, fruit trees and vegetables, as well as various agricultural, forestry, horticultural and stored grain pest insects.Type: GrantFiled: July 4, 2000Date of Patent: April 5, 2005Assignee: Nihon Nohyako Co., Ltd.Inventors: Kouzou Machiya, Kazuyoshi Endoh, Takashi Furuya, Hayami Nakao, Makoto Gotoh, Eiji Kohno, Masanori Tohnishi, Kazuyuki Sakata, Masayuki Morimoto, Akira Seo
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Patent number: 6872716Abstract: One aspect of the present invention relates to heterocyclic compounds comprising a sulfonamide moiety. A second aspect of the present invention relates to the use of the heterocyclic compounds comprising a sulfonamide moiety to treat diseases, afflictions or maladies caused at least in part by abnormal activity of one or more GPCRs or ligand-gated ion channels. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds comprising a sulfonamide moiety, and the screening of those libraries for biological activity, e.g., in animal models of psychosis.Type: GrantFiled: January 28, 2004Date of Patent: March 29, 2005Assignee: Sepracor, Inc.Inventors: Xinhe Wu, Brian M. Aquila, Liming Shao, Heike Radeke, Gregory D. Cuny, James R. Hauske, Roger L. Xie
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Patent number: 6872730Abstract: The present invention relates to novel substituted benzofurans and benzothiophenes compounds that are antagonists of alpha V (?v) integrins, for example ?v?3 and ?v?5 integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment of pathological conditions mediated by ?v?3 and ?v?5 integrins, including such conditions as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis. The compounds have the general formula I: where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, m, n, i, j and k are defined herein.Type: GrantFiled: April 26, 2002Date of Patent: March 29, 2005Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Beth M. Anaclerio, Juan J. Marugan Sanchez, Victor J. Marder, David C. U'Prichard, Bruce E. Tomczuk
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Patent number: 6872747Abstract: A novel class of decalactones with the general formula (I) and their stereoisomers is disclosed. A method for the synthesis of the decalactones of general formula (I) and the use of the decalactones in pharmaceutical compositions is also described.Type: GrantFiled: May 9, 2002Date of Patent: March 29, 2005Assignee: Biotecmarin GmbHInventors: Gerhard Bringmann, Peter Prokosch, Ru Angelie Edrada, Markus Heubes, Sudarsono, Eckhard Gunter
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Patent number: 6864276Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) agonists or antagonists of nicotinic acetylcholine receptors.Type: GrantFiled: May 7, 2001Date of Patent: March 8, 2005Assignee: Bayer Cropscience AGInventors: Reiner Fischer, Christoph Erdelen
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Patent number: 6861446Abstract: Taxanes having a heterosubstituted acetate substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.Type: GrantFiled: November 24, 2003Date of Patent: March 1, 2005Assignee: FSU Research Foundation, Inc.Inventor: Robert A. Holton
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Patent number: 6846819Abstract: Compounds of the formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment of bacterial infections.Type: GrantFiled: October 6, 2000Date of Patent: January 25, 2005Assignee: Affinium Pharmaceuticals, Inc.Inventors: William H. Miller, Kenneth A. Newlander, Mark A. Seefeld, Irene N. Uzinskas, Walter E. DeWolf, Jr., Dalia R. Jakas
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Patent number: 6846817Abstract: The invention provides nicotine receptor agonists of formula I: wherein R1, x, y, and n have any of the values given in the specification, or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions comprising such a compound or salt, methods for preparing such a compound or salt, and methods for modulating (e.g. antagonizing or activating) nicotine receptors with such a compound or salt.Type: GrantFiled: November 30, 2001Date of Patent: January 25, 2005Assignee: Regents of the University of MinnesotaInventor: S. Mbua Ngale Efange
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Patent number: 6835743Abstract: Process for the protection of a building that has already been built or is going to be built, whereby an effective amount of an insecticidally active compound is spread around or under the said building at discrete locations. The insecticide may be an arylpyrazole.Type: GrantFiled: May 13, 2002Date of Patent: December 28, 2004Assignee: Bayer CropScience S.A.Inventor: Yasuo Kimura
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Patent number: 6833378Abstract: Corticotropin-releasing factor (CRF) antagonists having the formulae wherein the dashed lines, A, B, Y, Z, G, R3, R4, R5, R6, R16 and R17 are as defined in the application, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment disorders including CNS and stress-related disorders.Type: GrantFiled: January 17, 2001Date of Patent: December 21, 2004Assignee: Pfizer IncInventor: Yuhpyng L. Chen
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Patent number: 6828332Abstract: The present invention provides compounds of formula (I) and a method of inhibiting the reuptake of serotonin and antagonizing the serotonin receptor which comprises administering to a subject in need of such treatment an effective amount of a compound of formula (I).Type: GrantFiled: February 27, 2002Date of Patent: December 7, 2004Assignee: Eli Lilly and CompanyInventors: Daniel Timothy Kohlman, Sidney Xi Liang, Yao-Chang Xu
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Publication number: 20040242593Abstract: 1′-substituted cannabinoid derivatives of delta-8-tetrahydrocannabinol, delta-9-tetrahydrocannabinol, and delta-6a-10a-tetrahydrocannabinol that have affinity for the cannabinoid receptor type-1 (CB-1) and/or cannabinoid receptor type-2 (CB-2). Compounds having activity as either agonists or antagonists of the CB-1 and/or CB-2 receptors can be used for treating CB-1 or CB-2 mediated conditions.Type: ApplicationFiled: May 20, 2004Publication date: December 2, 2004Inventors: Bob M. Moore, Antonio M. Ferreira, Mathangi Krishnamurthy
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Publication number: 20040242641Abstract: The present invention discloses (1S,5S)-3-(5,6-dichloro-3-pyridinyl)-3,6-diazabicyclo[3.2.0]heptane and its use to treat pain and other disorders associated with the nicotinic acetylcholine receptor.Type: ApplicationFiled: May 27, 2003Publication date: December 2, 2004Inventors: Michael J. Buckley, Jianguo Ji
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Publication number: 20040235852Abstract: Compounds of Formula I are useful for inhibiting serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein and have improved pharmacokinetic properties. These compounds may be used in methods of preventing and/or treating clotting disorders.Type: ApplicationFiled: May 19, 2004Publication date: November 25, 2004Inventors: Alan G. Olivero, Daniel P. Sutherlin
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Publication number: 20040235902Abstract: A compound represented by the following general formula (I) or a salt thereof: 1Type: ApplicationFiled: June 15, 2004Publication date: November 25, 2004Inventors: Tetsuo Nagano, Kazuya Kikuchi, Tomoya Hirano, Satoko Maruyama
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Publication number: 20040224975Abstract: The invention relates to nicotinamide derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The nicotinamide derivatives according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic, respiratory diseases, disorders and conditions, as well as wounds.Type: ApplicationFiled: June 9, 2004Publication date: November 11, 2004Applicant: Pfizer Inc.Inventors: Simon Balley, Elisabeth C. L. Gautier, Alan J. Henderson, Thomas V. Magee, Anthony Marfat, John P. Mathias, Dale G. McLeod, Sandra M. Monaghan, Blanda L. C. Stammen
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Patent number: 6809113Abstract: Compounds which are antagonists of MCP-1 function and are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection; pharmaceutical compositions comprising these compounds; and the use of these compounds and compositions in the prevention or treatment of such diseases.Type: GrantFiled: February 27, 2002Date of Patent: October 26, 2004Assignees: Telik, Inc., Sanwa Kagaku Kenkyusho Co.Inventors: Edgardo Laborde, Louise Robinson, Fanying Meng, Brian T. Peterson, Hugo O. Villar, Steven E. Anuskiewicz, Yoshiro Ishiwata, Shoji Yokochi, Yukiharu Matsumoto, Takuji Kakigami, Hideaki Inagaki, Takahito Jomori, Kouji Matsushima
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Patent number: 6800619Abstract: Described herein are compounds that are useful as caspase inhibitors having the formula: wherein Ring A is an optionally substituted piperidine, tetrahydroquinoline or tetrahydroisoquinoline ring; R1 is hydrogen, CN, CHN2, R, or CH2Y; R is an optionally substituted group selected from an aliphatic group, an aryl group, or an aralkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; and R3 is hydrogen, an optionally substituted aryl group, an optionally substituted aralkyl group, or an optionally substituted C1-6 aliphatic group, R4 is an optionally substituted group selected from an aryl group or a heterocyclyl group, or R3 and R4 taken together with the nitrogen to which they are attached optionally form a substituted or unsubstituted monocyclic, bicyclic or tricyclic ring.Type: GrantFiled: September 12, 2001Date of Patent: October 5, 2004Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Ronald Knegtel, Michael Mortimore
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Patent number: 6794392Abstract: The novel benzamide derivative represented by formula (1) and the novel anilide derivative represented by formula (13) of this invention has differentiation-inducing effect, and are, therefore, useful a therapeutic or improving agent for malignant tumors, autoimmune diseases, dermatologic diseases and parasitism. In particular, they are highly effective as an anticancer drug, specifically to a hematologic malignancy and a solid carcinoma.Type: GrantFiled: October 13, 1999Date of Patent: September 21, 2004Assignee: Schering AktiengesellschaftInventors: Tsuneji Suzuki, Tomoyuki Ando, Katsutoshi Tsuchiya, Osamu Nakanishi, Akiko Saito, Takashi Yamashita, Yoshinori Shiraishi, Eishi Tanaka
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Publication number: 20040176418Abstract: A crystalline polymorph of a bislulfate salt of a thrombin receptor antagonist compound, which exhibits a powder x-ray diffraction profile substantially the same as that shown in FIG. 1, or which exhibits a differential scanning calorimtery profile substantially the same as that shown in FIG.Type: ApplicationFiled: January 9, 2004Publication date: September 9, 2004Applicant: Schering CorporationInventors: Tiruvettipuram K. Thiruvengadam, Wenxue Wu, Tao Wang, John S. Chiu, Susan Bogdanowich-Knipp, Anastasia Pavlovsky, William J. Greenlee, Michael P. Graziano, Teddy Kosoglou, Madhu Chintala, Samuel Chackalamannil
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Patent number: RE38968Abstract: The current invention provides a method useful for inhibiting the loss of bone using 6-hydroxy-2-(4-hydroxyphenyl)-benzo(B)-thien-3-yl-4[2-piperidin-1-ethoxyphenol]methanone hydrochloride.Type: GrantFiled: February 27, 2003Date of Patent: February 7, 2006Assignee: Eli Lilly and CompanyInventors: Larry J. Black, George J. Cullinan