The Nitrogen Is Double Or Triple Bonded Directly To Carbon Patents (Class 514/238.5)
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Patent number: 10786479Abstract: The invention provides a method of inhibiting the conversion of carnitine to trimethylamine (TMA) and lowering TMAO in an individual comprising administering to the individual one or more compositions comprising a compound set forth in Formula (I): Wherein the compound is administered in an amount effective to inhibit conversion of carnitine to TMA in the individual.Type: GrantFiled: December 1, 2016Date of Patent: September 29, 2020Assignees: The Procter & Gamble Company, The Cleveland Clinic FoundationInventors: Stanley Leon Hazen, Jose Carlos Garcia-Garcia, George Franklin Gerberick, John August Wos, David Thomas Stanton, Thomas Alfred Inglin, Michael Reilly, Angela Jane Deutsch, Jodie Michele Reed, David Blair Cody
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Publication number: 20140315898Abstract: The present invention relates to novel N-arylamide-substituted trifluoroethyl sulfide derivatives of the formula (I) in which X1, X2, X3, X4, R1, R2, R3, n have the meanings given in the description—to their use as acaricides and insecticides for controlling animal pests and to processes and intermediates for their preparationType: ApplicationFiled: December 12, 2012Publication date: October 23, 2014Applicant: BAYER CROPSCIENCE AGInventors: Adeline Koehler, Bernd Alig, Angela Becker, Arnd Voerste, Ulrich Goergens, Reiner Fischer, Wahed Ahmed Moradi, Silvia Cerezo-Galvez, Julia Johanna Hahn, Kerstin Ilg, Hans-Georg Schwarz, Takuya Gomibuchi, Masahito Ito, Daiei Yamazaki, Katsuhiko Shibuya, Eiichi Shimojo
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Patent number: 8772290Abstract: The present invention relates to an alpha-arylmethoxyacrylate derivative, a preparation method thereof and a pharmaceutical composition comprising the same, and the alpha-arylmethoxyacrylate derivative is inhibitory of HIF, which plays an important role in the regulation of genes associated with energy metabolism, vasomotion, angiogenesis and apoptosis and in the response of cells under hypoxic conditions, so that it can be used for preventing or treating of diseases such as cancer, arthritis, psoriasis, diabetic retinopathy and macular degeneration.Type: GrantFiled: April 21, 2011Date of Patent: July 8, 2014Assignee: Oscotech Inc.Inventors: Se-Won Kim, Jung Ho Kim, Se-Nyum Kim, Dae-Pil Kang, Youn Ho Han, Guo Fan Jin, Dong-Sik Jung, Sung-Ho Park, Ji Min Kim, Jhi Zheng
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Publication number: 20140179660Abstract: An N1-cyclic amine-N5-substituted phenyl biguanide derivative of Formula 1 or a pharmaceutically acceptable salt thereof, a method of manufacturing the same, and a pharmaceutical composition including the biguanide derivative or the pharmaceutically acceptable salt thereof as an active ingredient are provided. The biguanide derivatives have an effect of inhibiting cancer cell proliferation and also exhibit anticancer activity including inhibition of cancer metastasis and cancer recurrence, because they are effective in activating AMPK, which is associated with the control of energy metabolism, even when administered in a small dose compared with conventional drugs. Also, the biguanide derivatives are highly effective at lowering blood glucose and lipid concentration by AMPK activation, thus they may be effectively used to treat diabetes mellitus, obesity, hyperlipemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndrome and metabolic syndrome.Type: ApplicationFiled: August 8, 2012Publication date: June 26, 2014Applicant: HANALL BIOPHARMA CO., LTD.Inventors: Sung Wuk Kim, Chang Hee Min, Se Hwan Park, Duck Kim, Ji Sun Lee, Yong Eun Kim, Ju Hoon Oh
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Patent number: 8648071Abstract: The present invention relates to substituted hydrazonamide compounds. The invention further relates to methods of inhibiting the activity of Hs?90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted hydrazonamide compound of the invention, or a pharmaceutical composition comprising such a compound.Type: GrantFiled: June 26, 2009Date of Patent: February 11, 2014Assignee: Synta Pharmaceuticals Corp.Inventors: Joseph Burlison, Dinesh U. Chimmanamada, Weiwen Ying, Shijie Zhang, David James
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Publication number: 20140038951Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.Type: ApplicationFiled: January 15, 2013Publication date: February 6, 2014Applicant: OMEROS CORPORATIONInventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas Neil Wheeler
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Publication number: 20130157851Abstract: New phenylamidines are described, having general formula (I): and their use for the control of phytopathogenic fungi.Type: ApplicationFiled: August 18, 2011Publication date: June 20, 2013Applicant: ISAGRO S.P.A.Inventors: Marilena Gusmeroli, Lucio Filippini, Franco Pellacini, Paolo Bravini, Alexia Elmini, Matteo Santino Vazzola, Christian Badaracco
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Patent number: 8343963Abstract: The present invention relates to novel sulfamoyl-phenyl-ureido compounds having the formula (I) or a physiologically acceptable salt or derivative thereof which are suitable for the therapy of infections caused by protozoa and in particular uncomplicated or severe malaria caused by plasmodia.Type: GrantFiled: January 29, 2010Date of Patent: January 1, 2013Assignee: 4SC AGInventor: Stefano Pegoraro
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Patent number: 8268996Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cathepsin S.Type: GrantFiled: June 16, 2011Date of Patent: September 18, 2012Assignee: IRM LLCInventors: Hong Liu, David C. Tully, Arnab Chatterjee, Phillip B. Alper, David H. Woodmansee, Daniel Mutnick
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Patent number: 8258129Abstract: The present invention encompasses compounds of general formula (1) wherein X and R1 to R3 are as defined in the disclosure, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.Type: GrantFiled: July 5, 2007Date of Patent: September 4, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Harald Engelhardt, Gerd Bader, Guido Boehmelt, Ralph Brueckner, Thomas Gerstberger, Maria Impagnatiello, Daniel Kuhn, Otmar Schaaf, Heinz Stadtmueller, Irene Waizenegger, Andreas Zoephel
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Publication number: 20120149707Abstract: The present invention relates to an alpha-arylmethoxyacrylate derivative, a preparation method thereof and a pharmaceutical composition comprising the same, and the alpha-arylmethoxyacrylate derivative is inhibitory of HIF, which plays an important role in the regulation of genes associated with energy metabolism, vasomotion, angiogenesis and apoptosis and in the response of cells under hypoxic conditions, so that it can be used for preventing or treating of diseases such as cancer, arthritis, psoriasis, diabetic retinopathy and macular degeneration.Type: ApplicationFiled: April 21, 2011Publication date: June 14, 2012Applicant: OSCOTEC INC.Inventors: Se-Won Kim, Jung Ho Kim, Se-Nyum Kim, Dae-Pil Kang, Youn Ho Han, Guo Fan Jin, Dong-Sik Jung, Sung-Ho Park, Ji Min Kim, Jhi Zheng
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Publication number: 20120046288Abstract: The present invention relates to substituted hydrazonamide compounds. The invention further relates to methods of inhibiting the activity of Hs?90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted hydrazonamide compound of the invention, or a pharmaceutical composition comprising such a compound.Type: ApplicationFiled: June 26, 2009Publication date: February 23, 2012Inventors: Joseph A. Burlison, Dinesh U. Chimmanamada, Weiwen Ying, Shijie Zhang, David James
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Publication number: 20110305632Abstract: The present invention relates to a method of making asymmetrical bis(thiosemicarbazones), compounds useful as synthetic intermediates in the method, new bis(thiosemicarbazones) that can be readily accessed by use of the method and methods of treatment and imaging utilising some of the new bis(thiosemicarbazones).Type: ApplicationFiled: December 11, 2009Publication date: December 15, 2011Applicant: THE UNIVERSITY OF MELBOURNEInventors: Paul Stephen Donnelly, Brett Michael Paterson
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Publication number: 20110082109Abstract: The present invention provides a pharmaceutical which possesses an excellent inhibitory effect on NHE3 (Na+/H+ exchanger type 3) and effectively improves diseases or conditions of organs in which NHE3 is expressed.Type: ApplicationFiled: October 1, 2010Publication date: April 7, 2011Applicant: AJINOMOTO CO., INC.Inventors: Wataru MIYANAGA, Yoichiro Shima, Misato Noguchi, Akiko Oonuki, Yayoi Kawato, Hiroshi Iwata, Eri Harada, Ryuta Takashita, Hirokazu Ueno, Tadakiyo Nakagawa
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Publication number: 20100240654Abstract: A compound represented by the following general formula (1) or a salt thereof or a hydrate of the foregoing is safe while exhibiting suitable physicochemical stability, and is useful as therapeutic or prophylactic agents for diseases associated with thrombus formation. wherein R1a, R1b, R1c and R1d each independently represent hydrogen, etc., R2 represents optionally substituted phenyl, etc., R3 represents optionally substituted C6-10 aryl, etc., Z1, Z2 and Z3 each independently represent hydrogen, etc., Z4 represents hydrogen, etc. and X represents a single bond or —CO—, etc.Type: ApplicationFiled: June 1, 2010Publication date: September 23, 2010Inventors: Richard CLARK, Shinsuke HIROTA, Hiroshi AZUMA, Kazunobu KIRA, Nobuhisa WATANABE, Tadashi NAGAKURA, Tatsuo HORIZOE
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Publication number: 20100197640Abstract: The present invention relates to novel sulfamoyl-phenyl-ureido compounds having the formula (I) or a physiologically acceptable salt or derivative thereof which are suitable for the therapy of infections caused by protozoa and in particular uncomplicated or severe malaria caused by plasmodia.Type: ApplicationFiled: January 29, 2010Publication date: August 5, 2010Applicant: 4SC AGInventor: Stefano PEGORARO
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Patent number: 7750032Abstract: The invention provides trisubstituted pyrazoles and imidazoles of Formula I: wherein L2, q, R13, R14, R15, R16, Z1 and Z2 are as described in the Summary of the Invention; and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the peroxisome proliferator-activated receptor (PPAR) families, particularly the activity of PPAR?.Type: GrantFiled: February 3, 2006Date of Patent: July 6, 2010Assignee: IRM LLCInventors: Christopher Cow, Robert Epple, Xing Wang, Yongping Xie, Hans Martin Seidel
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Patent number: 7662849Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.Type: GrantFiled: June 4, 2004Date of Patent: February 16, 2010Assignee: ViroBay, Inc.Inventors: John W. Patterson, Soon H. Woo
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Publication number: 20080293722Abstract: The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of ion channel function, and treatment of disease and disease symptoms, particularly those mediated by certain calcium channel subtype targets.Type: ApplicationFiled: March 15, 2005Publication date: November 27, 2008Applicant: WyethInventors: Robert Zelle, Christopher Todd Baker, Paul Will, Vincent P. Galullo
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Patent number: 7452891Abstract: The present invention discloses compounds which, are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.Type: GrantFiled: January 28, 2005Date of Patent: November 18, 2008Assignee: Schering CorporationInventors: John W. Clader, Hubert B. Josien, Anandan Palani, Tin Yau Chan
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Patent number: 7365070Abstract: This invention provides compounds and methods for treating melanocortin receptor associated disorders, such as weight loss disorders including cachexia resulting from cancer and other chronic illnesses. The compounds are represented by formula I: wherein X is oxygen or sulfur; G is G1 or G2: L1, L2, L3 and Q are linker groups, and Rings A, B and C, and R1-R14 are described in the specification. The compounds are antagonists of melanocortin receptors.Type: GrantFiled: December 4, 2003Date of Patent: April 29, 2008Assignee: Ore Pharmaceuticals Inc.Inventors: Tricia J. Vos, Michael Patane, Michael E. Solomon, Christopher Blackburn, Mihaela D. Danca
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Patent number: 7129238Abstract: The invention is concerned with novel mandelic acid derivatives of formula (I) wherein R1 to R10, X and Y are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds inhibit the formation of coagulation factors Xa, IXa and thrombin induced by factor VIIa and tissue factor.Type: GrantFiled: November 21, 2003Date of Patent: October 31, 2006Assignee: Hoffmann-La Roche Inc.Inventors: David William Banner, Luca Claudio Gobbi, Katrin Groebke Zbinden, Ulrike Obst, Christoph Martin Stahl
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Patent number: 6927218Abstract: Compounds, compositions and methods treating arthritic disorders such as osteoarthritis or rheumatoid arthritis, and for treating other diseases associated with altered mitochondrial function, such as cancer, psoriasis, stroke, Alzheimer's Disease and diabetes. The compounds of this invention have the following structure (I): including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein R1-5 are as defined herein. The methods of this invention are directed to administering to a warm-blooded animal in need thereof an effective amount of a compound of structure (I), typically in the form of a pharmaceutical composition.Type: GrantFiled: March 11, 2003Date of Patent: August 9, 2005Assignee: Migenix Corp.Inventors: Soumitra S. Ghosh, Tomas R. Szabo
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Patent number: 6849626Abstract: The invention relates to semicarbazides of the general formula I where R1, R2, R3, R4 and I have the meaning indicated in claim 1. The compounds of the formula I can be employed as pharmaceutical active compounds in human and veterinary medicine, in particular for the control and prevention of thromboembolic disorders such as thrombosis, mycocardial infarct, arteriosclerosis, inflammation, apoplexy, angina pectoris, restenosis after angioplasty and intermittent claudication.Type: GrantFiled: August 21, 2001Date of Patent: February 1, 2005Assignee: Merck Patent GmbHInventors: Werner Mederski, Horst Juraszyk, Dieter Dorsch, Christos Tsaklakidis, Johannes Gleiltz, Christopher Barnes
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Patent number: 6800659Abstract: Novel styrylacrylonitrile compounds which are useful in treating a variety of cell proliferative disorders such as cancer are disclosed.Type: GrantFiled: April 12, 2001Date of Patent: October 5, 2004Assignee: HSC Research and Development Limited PartnershipInventors: Chaim M. Roifman, Thomas Grunberger, Olga Rounova, Demin Peter, Nigel Sharfe
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Publication number: 20040110756Abstract: The invention relates to new anthracene derivatives of the general Formula 1 and to their synthesis and use as pharmaceutical preparations, especially for the treatment of a tumor.Type: ApplicationFiled: July 17, 2003Publication date: June 10, 2004Inventors: Peter Emig, Eckhard Gunther, Beate Aue, Emmanuel Polymeropoulos, Silke Baasner, Peter Schmidt
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Publication number: 20040110755Abstract: The present invention relates to pharmaceutical combinations therapies based on p38 kinase inhibitors and another active ingredient, pharmaceutical compositions comprising such combinations, processes for preparing them and their use in the treatment of cytokine mediated diseases.Type: ApplicationFiled: August 11, 2003Publication date: June 10, 2004Applicants: Boehringer Ingelheim Pharmaceuticals, Inc., Boehringer Ingelheim FranceInventors: Stefan Simianer, Pascal Bilbault, Michael L. Cappola, Susan Lynn Way
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Publication number: 20040082563Abstract: Novel compounds of the formula (I) formula (I) in which W, E, X, Y, T, R1, R2, R2′, and R2″ are as defined in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders and for the treatment of tumours.Type: ApplicationFiled: September 16, 2003Publication date: April 29, 2004Inventors: Dieter Dorsch, Bertram Cezanne, Werner Mederski, Christos Tsaklakidis, Johannes Gleitz, Christopher Barnes
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Publication number: 20040077641Abstract: Novel pyridylpyrimidines of the formula 1Type: ApplicationFiled: August 19, 2003Publication date: April 22, 2004Inventors: Thomas Bretschneider, Mazen Es-Sayed, Rudiger Fischer, Fritz Maurer, Christoph Erdelen, Peter Losel
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Publication number: 20040077647Abstract: Disclosed are compounds of formula (I): 1Type: ApplicationFiled: August 1, 2003Publication date: April 22, 2004Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier Francesco Cirillo, Abdelhakim Hammach, Victor Kamhi, Neil Moss, Paul S. Riska, Christopher Pargellis
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Patent number: 6720319Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formula (Ia) and (Ib) where R2, R3, R4, R5, R6, R7, R8, Het and X are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds.Type: GrantFiled: October 1, 2002Date of Patent: April 13, 2004Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Weimin Liu, Denice M. Spero, David S. Thomson, Yancey D. Ward, Erick R. R. Young
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Publication number: 20040048858Abstract: The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula 1Type: ApplicationFiled: December 19, 2002Publication date: March 11, 2004Inventors: James A. Sikorski, Charles Q. Meng, M. David Weingarten, Kimberly J. Worsencroft, Liming Ni
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Patent number: 6703389Abstract: Methods and compositions for treating humans suffering from, or preventing a human from suffering, a physiological or psychiatric disease, disorder, or a condition where inhibiting reuptake of norepinephrine is a benefit are disclosed. The compositions comprise a compound having a pharmacological selectivity of serotonin (Ki)/norepinephrine (Ki) of at least about 5000. Examples of such compounds include reboxetine, and more preferably optically pure (S,S) enantiomer of reboxetine. The methods generally include administration of a therapeutic amount of such compositions. Also disclosed are preparations of a medicament from the composition, and uses of the composition in a manufacture of the medicament to treat a human suffering from, or preventing a human from suffering, a physiological or psychiatric disease, disorder, or condition.Type: GrantFiled: December 14, 2001Date of Patent: March 9, 2004Assignee: Pharmacia & Upjohn CompanyInventors: Erik H. F. Wong, Saeeduddin Ahmed, Robert C. Marshall, Robert McArthur, Duncan P. Taylor, Lars Birgerson, Pasquale Cetera
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Patent number: 6680317Abstract: This invention relates to novel compounds of Formula (I), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: GrantFiled: September 17, 2002Date of Patent: January 20, 2004Assignee: SmithKline Beecham CorporationInventors: Michael R. Palovich, Katherine L. Widdowson, Hong Nie
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Patent number: 6638930Abstract: Substituted heterocycles of the general structural formula: are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.Type: GrantFiled: April 17, 2001Date of Patent: October 28, 2003Assignee: Merck & Co. Inc.Inventors: Conrad P. Dorn, Paul E. Finke, Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Mark Stuart Chambers, Timothy Harrison, Tamara Ladduwahetty, Brian John Williams
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Publication number: 20030199509Abstract: Disclosed are pharmaceutical compositions comprising brimondine and timolol for topical ophthalmic delivery and a method of treatment comprising administering said composition when indicated for glaucoma and associated conditions such as elevated intraocular pressure in the eyes of humans.Type: ApplicationFiled: April 19, 2002Publication date: October 23, 2003Inventors: Chin-Ming Chang, Gary J. Beck, Cynthia C. Pratt, Amy L. Batoosingh
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Patent number: 6562821Abstract: Compounds, compositions and methods treating arthritic disorders such as osteoarthritis or rheumatoid arthritis, and for treating other diseases associated with altered mitochondrial function, such as cancer, psoriasis, stroke, Alzheimer's Disease and diabetes. The compounds of this invention have the following structure (I): including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein R1-5 are as defined herein. The methods of this invention are directed to administering to a warm-blooded animal in need thereof an effective amount of a compound of structure (I), typically in the form of a pharmaceutical composition.Type: GrantFiled: February 27, 2002Date of Patent: May 13, 2003Assignee: MitoKorInventors: Soumitra S. Ghosh, Tomas R. Szabo
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Patent number: 6552025Abstract: Compositions, methods of use, isolation and biosynthesis of diimino-piperazine derivatives useful for the modification of sphingolipid metabolism and other biological functions are described. The preferred derivative is 2,6-bis-(&ohgr;-aminobutyl)-3,5-diimino-piperazine. This is a naturally occurring biochemical compound isolated from cells. The diimino-piperazine derivatives are useful as therapeutic agents when administered to patients to treat diseases and disorders involving cell regulation.Type: GrantFiled: November 17, 2000Date of Patent: April 22, 2003Assignee: Emory UniversityInventors: Alfred H. Merrill, Jr., Lisa Warden, Dennis C. Liotta
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Publication number: 20030049287Abstract: The invention relates to cosmetic and/or dermatological preparations which contain, in part, novel catechol oximes of formula (I). Said preparations can promote, in physiological systems, the natural defense mechanisms against free radicals and reactive oxygen compounds, or can be used as protective agents in cosmetic or pharmaceutical products whose oxidation-sensitive constituents should be protected from autooxidation.Type: ApplicationFiled: June 12, 2002Publication date: March 13, 2003Inventors: Jakob Peter Ley, William Johncock, Johannes Kaulen
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Patent number: 6525036Abstract: The present invention relates to novel cysteine protease inhibitors of Formula I: the pharmaceutically acceptable salts and N-oxide derivatives thereof, their use as therapeutic agents and methods of making them.Type: GrantFiled: January 5, 2001Date of Patent: February 25, 2003Assignee: Merck & Co., Inc.Inventors: Renata Marcella Oballa, Petpiboon Prasit, Joel Stephane Robichaud, Elise Isabel, Eduardo Setti, Dan-Xiong Wang, Rohan V. Mendonca, Shankar Venkatraman
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Publication number: 20030032643Abstract: Disclosed is the compound (+)-(2S,3S)-2-(3-chlorophenyl)-3,5,5-trimethyl-2-morpholinol and pharmaceutically acceptable salts and solvates thereof, pharmaceutical compositions comprising them, and processes for their preparation; also disclosed is a method of treating depression, attention deficit hyperactivity disorder (ADHD), obesity, migraine, pain, sexual dysfunction, Parkinson's disease, Alzheimer's disease, addiction to cocaine or tobacco products, seasonal affective disorder, chronic fatigue, narcolepsy or cognitive impairment using such compound, salts, solvates or compositions.Type: ApplicationFiled: May 17, 2002Publication date: February 13, 2003Inventors: John A. Ascher, Johnston Andrews Joseph, Learned-Coughlin Marie Susan, Alan Bye
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Publication number: 20020187979Abstract: Compounds of formula (I) 1Type: ApplicationFiled: March 29, 2002Publication date: December 12, 2002Inventors: Paul Vincent Fish, Jackie Diane Kendall, Gavin Alistair Whitlock
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Patent number: 6436933Abstract: Methods and compositions that act as specific inhibitors of ALF activity for the prophylaxis and treatment of anthrax infections.Type: GrantFiled: March 26, 2001Date of Patent: August 20, 2002Assignee: Structural Bioinformatics Inc.Inventors: Darryl Rideout, Venkatachalapathi V. Yalamoori, Kalyanaraman Ramnarayan, Mark Shenderovich, Jian Hua Zheng, Jason Sun, Christina Niemeyer
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Publication number: 20020107249Abstract: Methods and compositions for treating humans suffering from, or preventing a human from suffering, a physiological or psychiatric disease, disorder, or a condition where inhibiting reuptake of norepinephrine is a benefit are disclosed. The compositions comprise a compound having a pharmacological selectivity of serotonin (K,)/norepinephrine (K1) of at least about 5000. Examples of such compounds include reboxetine, and more preferably optically pure (S,S) enantiomer of reboxetine. The methods generally include administration of a therapeutic amount of such compositions. Also disclosed are preparations of a medicament from the composition, and uses of the composition in a manufacture of the medicament to treat a human suffering from, or preventing a human from suffering, a physiological or psychiatric disease, disorder, or condition.Type: ApplicationFiled: January 23, 2002Publication date: August 8, 2002Applicant: Pharmacia & Upjohn CompanyInventors: Erik H.F. Wong, Saeeduddin Ahmed, Robert C. Marshall, Robert McArthur, Duncan P. Taylor, Lars Birgerson
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Publication number: 20020103194Abstract: This invention relates to a novel class of partial or full muscarinic receptor agonists intermediates for their preparation, and pharmaceutical compositions and methods of use for the treatment or prevention of diseases the treatment or prevention of which is mediated by muscarinic receptor agonismType: ApplicationFiled: February 15, 2000Publication date: August 1, 2002Inventors: Anabella Villalobos, Daniel Yohannes, Jolanta Nowakowski, Dane Liston
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Publication number: 20020086864Abstract: Methods and compositions for treating humans suffering from, or preventing a human from suffering, a physiological or psychiatric disease, disorder, or a condition where inhibiting reuptake of norepinephrine is a benefit are disclosed. The compositions comprise a compound having a pharmacological selectivity of serotonin (K1)/norepinephrine (K1) of at least about 5000. Examples of such compounds include reboxetine, and more preferably optically pure (S,S) enantiomer of reboxetine. The methods generally include administration of a therapeutic amount of such compositions. Also disclosed are preparations of a medicament from the composition, and uses of the composition in a manufacture of the medicament to treat a human suffering from, or preventing a human from suffering, a physiological or psychiatric disease, disorder, or condition.Type: ApplicationFiled: January 4, 2002Publication date: July 4, 2002Applicant: Pharmacia & Upjohn CompanyInventors: Erik H.F. Wong, Saeeduddin Ahmed, Robert C. Marshall, Robert McArthur, Duncan P. Taylor, Lars Birgerson, Pasquale Cetera
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Patent number: 6395897Abstract: Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel compounds.Type: GrantFiled: November 5, 1999Date of Patent: May 28, 2002Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Charles L. Cywin, Michel J. Emmanuel, Leah L. Frye, Denice M. Spero, David S. Thomson, Yancey D. Ward
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Patent number: 6365626Abstract: The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors.Type: GrantFiled: December 7, 2000Date of Patent: April 2, 2002Assignee: Parker Hughes InstituteInventors: Fatih M. Uckun, Yaguo Zheng, Sutapa Ghosh
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Patent number: 6303652Abstract: The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors.Type: GrantFiled: March 19, 1999Date of Patent: October 16, 2001Assignee: Hughes InstituteInventors: Fatih M. Uckun, Yaguo Zheng, Sutapa Ghosh
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Patent number: 6294575Abstract: The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors.Type: GrantFiled: October 16, 2000Date of Patent: September 25, 2001Assignee: Parker Hughes InstituteInventors: Fatih M. Uckun, Yaguo Zheng, Sutapa Ghosh