Nitrogen Attached Indirectly To The Five-membered Hetero Ring By Acyclic Nonionic Bonding Patents (Class 548/566)
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Patent number: 7745642Abstract: The present invention relates to compounds of formula (I), or to salts or solvates thereof, their use in the manufacture of medicaments for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof.Type: GrantFiled: December 21, 2005Date of Patent: June 29, 2010Assignee: Glaxo Group LimitedInventors: Daniel Marcus Bradley, Roderick Alan Porter
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Publication number: 20100099871Abstract: Compounds having anti-psychotic activity are disclosed herein. In some embodiments, the compounds are atypical anti-psychotics. In some embodiments, the compounds are selective for the 5-HT2A receptor over the D2 receptor. Pharmaceutical derivatives and pharmaceutical compositions including the compounds are disclosed herein. Methods for treating a psychotic condition that include administering the compounds, a pharmaceutical derivative thereof, or a pharmaceutical composition thereof are also disclosed herein.Type: ApplicationFiled: August 17, 2009Publication date: April 22, 2010Inventors: Dwight W. Miller, Neil C. Mitchell, Bill W. Massey
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Patent number: 7692019Abstract: One aspect of the present invention relates to methods of synthesizing substituted piperidines. A second aspect of the present invention relates to stereoselective methods of synthesizing substituted piperidines. The methods of the present invention will find use in the synthesis of compounds useful for treatment of numerous ailments, conditions and diseases that afflict mammals, including but not limited to addiction and pain. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the substituted piperidines using the methods of the present invention. An additional aspect of the present invention relates to enantiomerically substituted pyrrolidines, piperidines, and azepines.Type: GrantFiled: February 28, 2006Date of Patent: April 6, 2010Assignee: Sepracor Inc.Inventors: Brian M. Aquila, Thomas D. Bannister, Gregory D. Cuny, James R. Hauske, Michele L. R. Heffernan, Michael Z. Hoemann, Donald W. Kessler, Liming Shao, Xinhe Wu, Roger L. Xie
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Publication number: 20100076024Abstract: The invention relates to compounds of formula (I) wherein the substituents are as defined in claim 1; to compositions comprising said compounds and to their use as pharmaceutical agents, in particular as inhibitors of serine proteases.Type: ApplicationFiled: February 20, 2008Publication date: March 25, 2010Inventors: Kaspar Zimmermann, Daniel Kaspar Baeschlin, Saliha Moussaoui
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Publication number: 20100069435Abstract: Provided are a technique for position-selectively introducing an amino group into a difluorobenzoic acid, a novel process for producing a quinolonecarboxylic acid derivative serving as an antibacterial agent, and intermediates in the production. The process comprises treating a compound represented by formula (6): with a base in a water-containing solvent.Type: ApplicationFiled: October 13, 2009Publication date: March 18, 2010Applicant: DAIICHI PHARMACEUTICAL CO., LTD.Inventors: MAKOTO MUTO, YUTAKA KITAGAWA
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Patent number: 7667049Abstract: An industrially advantageous process for the production of (3R,4S)-3-cyclopropylaminomethyl-4-fluoropyrrolidine or an enantiomer thereof that is useful as an intermediate for the production of novel antimicrobial agents 10-(3-cyclopropylaminomethyl-4-fluoropyrrolidinyl)pyridobenzoxazine carboxylic acid derivatives. Highly stereoselective asymmetric hydrogenation of 1-protected-4-alkoxycarbonyl-3-oxopyrrolidine, followed by ester hydrolysis, followed by amidation with cyclopropylamine gives crude crystals. The crude crystals are purified by recrystallization to give a novel compound (3R,4S)-1-protected-3-cyclopropylcarbamoyl-4-hydroxypyrrolidine or an enantiomer thereof at high optical purity. The use of these intermediates enables industrial production of high-quality products of (3R,4S)-3-cyclopropylaminomethyl-4-fluoropyrrolidine or an enantiomer thereof. The process is highly simple and can produce the desired products at high purity and stable yields.Type: GrantFiled: March 8, 2007Date of Patent: February 23, 2010Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Takayuki Gotoh, Ichirou Araya
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Publication number: 20100036119Abstract: The present invention relates to ?,?-difluoroamines, fluorinating reagents comprising ?,?-difluoroamines and also processes for preparing ?,?-difluoroamines and fluorinating reagents comprising ?,?-difluoroamines.Type: ApplicationFiled: October 16, 2009Publication date: February 11, 2010Applicant: LANXESS DEUTSCHLAND GMBHInventors: WOLFGANG EBENBECK, PETRA HILGERS, ALBRECHT MARHOLD, JAN ALEXANDER BARTEN, ALEXANDER KOLOMEITSEV, GERD-VOLKER ROSCHENTHALER
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Publication number: 20090325916Abstract: Compounds of formula I or II and pharmaceutical compositions and kits containing these compounds are provided. Also provided are methods of inducing contraception, providing hormone replacement therapy, treating cycle-related symptoms, or treating or preventing benign or malignant neoplastic disease using the compounds of formula I, formula II, or formula III.Type: ApplicationFiled: September 2, 2009Publication date: December 31, 2009Applicant: WyethInventors: Puwen Zhang, Jeffrey Curtis Kern, Eugene Anthony Terefenko, Eugene John Trybulski
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Patent number: 7638639Abstract: This invention is directed to compounds of formula I: wherein R1-R5 and a-e are as defined in the specification; or pharmaceutically-acceptable salt or solvate or stereoisomer thereof. The invention also directed to pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors using such compounds.Type: GrantFiled: January 30, 2008Date of Patent: December 29, 2009Assignee: Theravance, Inc.Inventors: Mathai Mammen, Adam Hughes, Yu-hua Ji, Li Li, Weijiang Zhang
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Publication number: 20090292129Abstract: A process for resolving a compound in racemic form comprising the following steps is described: a) reacting a compound in racemic form with a resolving agent, b) forming a diastereoisomeric complex of the resolving agent and an enantiomer of interest, c) separating the enantiomer of interest from the obtained diastereoisomer, wherein such a process is characterized in that said resolving agent is a compound of Formula (I). A diastereoisomeric complex between the resolving agent of Formula (I) and the enantiomer of interest is also described. The process according to the invention allows acid and basic racemic mixtures to be separated.Type: ApplicationFiled: February 1, 2007Publication date: November 26, 2009Applicant: ABIOGEN PHARMA S.P.A.Inventors: Elio Napolitano, Rita Fiaschi, Chiara Bechini, Gabriella Brunetto
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Patent number: 7615648Abstract: The present invention provides compounds of formula (I) wherein A is (1), (2), (3), (4), (5), (6) or (7) and wherein R1, R7, y and Ar1 are defined herein. The compounds are inhibitors of the uptake of one or more monoamines selected from serotonin, norepinephrine and dopamine and, as such, may be useful in the treatment of disorders of the central and/or peripheral nervous system.Type: GrantFiled: May 19, 2005Date of Patent: November 10, 2009Assignee: Eli Lilly and CompanyInventors: John Richard Harris, Barry Peter Clark, Peter Thaddeus Gallagher, Maria Ann Whatton
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Patent number: 7615566Abstract: This invention is directed to compounds of formula I: wherein R1-R5 and a-e are as defined in the specification; or pharmaceutically-acceptable salt or solvate or stereoisomer thereof. The invention also directed to pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors using such compounds.Type: GrantFiled: January 30, 2008Date of Patent: November 10, 2009Assignee: Theravance, Inc.Inventors: Mathai Mammen, Adam Hughes, Yu-hua Ji, Li Li, Weijiang Zhang
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Publication number: 20090227593Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).Type: ApplicationFiled: May 21, 2009Publication date: September 10, 2009Applicant: Abbott LaboratoriesInventors: Huaqing Liu, Arthur A. Hancock, Kathryn J. Hancock, Marlon D. Cowart
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Patent number: 7582656Abstract: Compounds of the formula (I): in which the radicals R and R1 to R10 are as defined in the description, processes for the preparation of them, use thereof for the treatment of cardiovascular diseases, and pharmaceutical compositions comprising them.Type: GrantFiled: June 28, 2005Date of Patent: September 1, 2009Assignee: Merck Patent GesellschaftInventors: Didier Roche, Bruno Roux, Isabelle Berard
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Publication number: 20090124664Abstract: The present invention relates to selected (R)-arylalkylamino derivatives of formula (I), in which R, R1 and Ar are as defined in the claims. These compounds show a surprising potent inhibitory effect on C5a induced human PMN chemotaxis. The compounds of the invention absolutely lack of CXCL8 inhibitory activity. Said compounds are useful in the treatment of pathologies depending on the chemotactic activation of neutrophils and monocytes induced by the fraction C5a of the complement. In particular, the compounds of the invention are useful in the treatment of sepsis, psoriasis, rheumatoid arthritis, ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of injury caused by ischemia and reperfusion.Type: ApplicationFiled: November 24, 2006Publication date: May 14, 2009Inventors: Marcello Allegretti, Alessio Moriconi, Andrea Aramini, Maria Candida Cesta, Andrea Beccari, Riccardo Bertini
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Publication number: 20090062366Abstract: [Problem] To provide a compound which may be used in treating diseases in which a calcium sensing receptor (CaSR) is concerned, particularly hyperparathyroidism. [Means for Resolution] It was found that novel pyrrolidine derivatives which are characterized by the possession of aminomethyl group substituted with arylalkyl group or the like, or salts thereof, have excellent CaSR agonistic regulatory activity and also have excellent selectivity with CYP2D6 inhibitory activity having a possibility of causing drug interaction. Based on the above, these novel pyrrolidine derivatives are useful as therapeutic agents for treating diseases in which CaSR is concerned (hyperparathyroidism, renal osteodystrophy, hypercalcemia and the like).Type: ApplicationFiled: May 18, 2006Publication date: March 5, 2009Applicant: ASTELLAS PHARAMA INC.Inventors: Shunichiro Hachiya, Makoto Oku, Hana Mukai, Takashi Shin, Keisuke Matsuura, Ryushi Seo, Takashi Kamikubo, Yoh Terada, Masanao Sanagi, Kousei Yoshihara, Taisuke Takahashi
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Publication number: 20090054420Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).Type: ApplicationFiled: August 21, 2008Publication date: February 26, 2009Applicant: ABBOTT LABORATORIESInventors: Robert J. Altenbach, Lawrence A. Black, Sou-Jen Chang, Marlon D. Cowart, Ramin Faghih, Gregory A. Gfesser, Yi-Yin Ku, Huaqing Liu, Kirill A. Lukin, Diana L. Nersesian, Yu-ming Pu, Padam N. Sharma, Youssef L. Bennani, Michael P. Curtis
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Publication number: 20090029962Abstract: The present invention relates to compounds of formula I wherein R1, R2, R3, Ar, n and o are as defined herein and to their pharmaceutically acceptable active salts. Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and are useful for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.Type: ApplicationFiled: July 21, 2008Publication date: January 29, 2009Inventors: Guido Galley, Annick Goergler, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Patent number: 7482364Abstract: Substituted phenylalkynes of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.Type: GrantFiled: October 18, 2007Date of Patent: January 27, 2009Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Richard Apodaca, Xiaohu Deng, Jill A. Jablonowski, Neelakandha Mani, Chennagiri R. Pandit, Wei Xiao
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Publication number: 20090023935Abstract: An industrially advantageous process for the production of (3R,4S)-3-cyclopropylaminomethyl-4-fluoropyrrolidine or an enantiomer thereof that is useful as an intermediate for the production of novel antimicrobial agents 10-(3-cyclopropylaminomethyl-4-fluoropyrrolidinyl)pyridobenzoxazine carboxylic acid derivatives. Highly stereoselective asymmetric hydrogenation of 1-protected-4-alkoxycarbonyl-3-oxopyrrolidine, followed by ester hydrolysis, followed by amidation with cyclopropylamine gives crude crystals. The crude crystals are purified by recrystallization to give a novel compound (3R,4S)-1-protected-3-cyclopropylcarbamoyl-4-hydroxypyrrolidine or an enantiomer thereof at high optical purity. The use of these intermediates enables industrial production of high-quality products of (3R,4S)-3-cyclopropylaminomethyl-4-fluoropyrrolidine or an enantiomer thereof. The process is highly simple and can produce the desired products at high purity and stable yields.Type: ApplicationFiled: March 8, 2007Publication date: January 22, 2009Inventors: Takayuki Gotoh, Ichirou Araya
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Patent number: 7476672Abstract: This invention is directed to acetylenic compounds as inhibitors of a nicotinamide adenine dinucleotide oxidase hydride donor useful in treating or ameliorating a reactive oxygen species mediated inflammatory disorder.Type: GrantFiled: January 10, 2006Date of Patent: January 13, 2009Assignee: Janssen Pharmaceutica N.V.Inventors: Scott Beers, Elizabeth A. Malloy, Michael P. Wachter
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Patent number: 7456209Abstract: IAP binding molecules and compositions including these are disclosed. The IAP binding molecules interact with IAPs (inhibitor of apoptosis proteins) in cells and may be used to modify apoptosis in cells treated with such molecules. Embodiments of these compounds have a Kd of less that 0.1 micromolar. Methods of using these IAP binding molecules for therapeutic, diagnostic, and assay purposes are also disclosed.Type: GrantFiled: July 15, 2005Date of Patent: November 25, 2008Assignee: Tetralogic Pharmaceuticals CorporationInventors: Stephen M. Condon, Matthew G. LaPorte, Yijun Deng, Susan R. Rippin
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Publication number: 20080287506Abstract: Certain novel N,N-di(heteroarylalkyl)amine derivatives have provided unexpected insecticidal and acaricidal activity. These compounds are represented by formula (I): wherein Ar Ar1, a, b, c, R, Rd, Re, Rf, Rg, Rh, R?, R3 and Rk are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.Type: ApplicationFiled: October 27, 2005Publication date: November 20, 2008Applicant: Bayer CropScience AGInventors: David M. Roush, John F. Chiarello, George Theodoridis, Hongyan Qi
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Publication number: 20080226716Abstract: Compounds that provide for sustained systemic concentrations of GABA analogs following oral administration to animals are disclosed. Pharmaceutical compositions including, and methods using, such compounds are also disclosed.Type: ApplicationFiled: May 28, 2008Publication date: September 18, 2008Applicant: XenoPortInventors: Mark Gallop, Kenneth C. Cundy, Randall A. Scheuerman, Ronald W. Barrett, Noa Zerangue
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Patent number: 7423059Abstract: The present invention relates to certain imine-substituted heterocyclic compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for the treatment or prophylaxis of neurological injury and neurodegenerative disorders.Type: GrantFiled: June 28, 2004Date of Patent: September 9, 2008Assignee: WyethInventors: Graham J. Durant, Michael Maillard, Jun Qing Guo
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Publication number: 20080176906Abstract: The present invention provides a novel pyrrole derivative having excellent androgen receptor antagonism, which is represented by the formula: wherein R1 represents a hydrogen atom, a cyano group or a group represented by the formula COORA (wherein RA represents an optional substituted C1-6 alkyl group), R2 and R4 are the same or different, and each represents a hydrogen atom, a C1-6 alkyl group, a C3-6 cycloalkyl group, a trifluoromethyl group, an amino-C1-6 alkyl group, a mono- or di-substituted amino-C1-6 alkyl group, an optionally halogenated C1-6 alkyl group substituted with an optionally substituted hydroxyl group, a C2-6 alkenyl group substituted with an optionally substituted hydroxyl group, a C1-6 alkyl group substituted with an optionally substituted and optionally oxidized thiol group, an optionally substituted with and optionally oxidized thiol group, a cyano group, an acyl group, an optionally substituted oxazolyl group or a 1,3-dioxolan-2-yl group, R3 represents a group represented by the forType: ApplicationFiled: December 13, 2005Publication date: July 24, 2008Applicant: Takeda Pharmaceutical Company LimitedInventors: Nobuyuki Matsunaga, Takenori Hitaka
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Publication number: 20080146649Abstract: This invention is directed to compounds of formula I: wherein R1-R5 and a-e are as defined in the specification; or pharmaceutically-acceptable salt or solvate or stereoisomer thereof. The invention also directed to pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors using such compounds.Type: ApplicationFiled: January 30, 2008Publication date: June 19, 2008Inventors: Mathai Mammen, Adam Hughes, Yu-hua Ji, Li Li, Weijiang Zhang
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Publication number: 20080138704Abstract: An object of the present invention is to provide a material for an electrolytic solution having improved ionic conductivity and, showing excellent in low temperature property, being stable with time, and being electrochemically stable at a high potential, and an ionic material-containing composition exhibiting excellent fundamental performance such as electrochemical stability, and preferably used in a variety of utilities. Another object of the present invention is to provide utilities thereof. The material for an electrolytic solution is the material containing an ionic compound, and the material comprises a cyano group-containing anion represented by the formula (1); and 1 to 99% by mass of a solvent in 100% by mass of the material for an electrolytic solution.Type: ApplicationFiled: May 9, 2005Publication date: June 12, 2008Applicant: Nippon Shokubai Co., Ltd.Inventors: Keiichiro Mizuta, Keiko Takebe
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Patent number: 7354942Abstract: The present invention is directed to benzylether and benzylamino derivative compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: GrantFiled: November 19, 2004Date of Patent: April 8, 2008Assignee: Merck & Co., Inc.Inventors: Philippe G. Nantermet, Hemaka A. Rajapakse, Harold G. Selnick, Shaun R. Stauffer, Mary Beth Young
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Patent number: 7351718Abstract: This invention is directed to compounds of formula I: wherein R1-R5 and a-e are as defined in the specification; or pharmaceutically-acceptable salt or solvate or stereoisomer thereof. The invention also directed to pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors using such compounds.Type: GrantFiled: November 21, 2006Date of Patent: April 1, 2008Assignee: Theravance, Inc.Inventors: Mathai Mammen, Adam Hughes, Yu-hua Ji, Li Li, Weijiang Zhang
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Patent number: 7351717Abstract: This invention is directed to compounds of formula I: wherein R1-R5 and a-e are as defined in the specification; or pharmaceutically-acceptable salt or solvate or stereoisomer thereof. The invention also directed to pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors using such compounds.Type: GrantFiled: November 21, 2006Date of Patent: April 1, 2008Assignee: Theravance, Inc.Inventors: Mathai Mammen, Adam Hughes, Yu-hua Ji, Li Li, Weijiang Zhang
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Patent number: 7348356Abstract: Disclosed are compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment or prevention of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the beta-secretase enzyme is involved.Type: GrantFiled: July 28, 2006Date of Patent: March 25, 2008Assignee: Merck & Co., Inc.Inventors: Craig A. Coburn, Shawn J. Stachel, Joseph P. Vacca
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Patent number: 7338952Abstract: This invention is directed to acetylenic compounds as inhibitors of a nicotinamide adenine dinucleotide oxidase hydride donor useful in treating or ameliorating a reactive oxygen species mediated inflammatory disorder.Type: GrantFiled: January 10, 2006Date of Patent: March 4, 2008Assignee: Janssen Pharmaceutica N.V.Inventors: Scott Beers, Elizabeth A. Malloy, Michael P. Wachter
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Patent number: 7268152Abstract: Compounds of Formula (IA) and Formula (IB) wherein R1, R2, R3, R4, R5, and R6 are as defined herein for Formula (IA) or Formula (IB), 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: March 21, 2003Date of Patent: September 11, 2007Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Younes Bekkali, Mario G. Cardozo, Christian Hanke Justus Joachim Harcken, Thomas M. Kirrane, Daniel Kuzmich, John Robert Proudfoot, Hossein Razavi, Hidenori Takahashi, David S. Thomson, Ji Wang, Renee Zindell
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Patent number: 7256191Abstract: The subject invention provides compounds which are easily metabolized by the metabolic drug detoxification systems. Particularly, fluvoxamine analogs which have been designed to include esters within the structure of the compounds are taught. Also provided are methods of treating depression and affective disorders, such as obsessive compulsive disorder. Pharmaceutical compositions of the fluvoxamine analogs are also taught.Type: GrantFiled: August 31, 2004Date of Patent: August 14, 2007Assignee: Aryx TherapeuticsInventor: Pascal Druzgala
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Patent number: 7253185Abstract: The present invention provides amino ceramide-like compounds which inhibit glucosyl ceramide (GlyCer) formation by inhibiting the enzyme GlyCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.Type: GrantFiled: April 29, 2005Date of Patent: August 7, 2007Assignees: The Regents of the University of Michigan, Genzyme CorporationInventors: James A. Shayman, David J. Harris, Craig Siegel, Carol A. Nelson, Diane P. Copeland
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Patent number: 7250521Abstract: 2,5-Bisaryl-?1-pyrrolines of the formula (I) in which Ar1 and Ar2 are as defined in the description can be prepared by reacting aroylpyrrolidinones of the formula (II) in which Ar1 and Ar2 are as defined in the description with an acid, if appropriate in the presence of a diluent.Type: GrantFiled: April 8, 2002Date of Patent: July 31, 2007Inventors: Udo Kraatz, Andrew Plant, Ernst Kysela, Albrecht Marhold
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Patent number: 7247748Abstract: Disclosed is a compound having the formula (I) pharmaceutically acceptable salts or solvates thereof and pharmaceutical compositions containing the same, wherein the structural variables are as defined herein.Type: GrantFiled: March 26, 2003Date of Patent: July 24, 2007Assignee: SmithKline CorporationInventors: Scott K. Thompson, James S. Frazee, Lara S. Kallander, Chun Ma, Joseph P. Marino, Michael J. Neeb, Ning Wang
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Patent number: 7220777Abstract: The invention provides compounds of formula (I) a salt, or solvate thereof.Type: GrantFiled: October 15, 2002Date of Patent: May 22, 2007Assignee: SmithKline Beecham P.L.C.Inventors: Sula Anne Armstrong, Dieter Wolfgang Hamprecht, Martin Jones, David Richard Witty, Kamal A Al-Barazanji, Mohammad Tadayyon
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Patent number: 7217707Abstract: N-(2-aminoaryl-propionyl)-amides of formula (1) are described. The process for their preparation and pharmaceutical preparations thereof are also described. The amides of the invention are useful in the prevention and treatment of tissue damage due to the exacerbate recruitment of polymorphonuclear neutrophils (leukocytes PMN) at the inflammatory sites. In particular, the invention relates to the R enantiomers of 2-(aminoaryl)-propionyl amides of formula (1) for use in the ihibition of the chemotaxis of neutrophils induced by IL-8. The compounds of the invention are used in the treatment of psoriasis, ulcerative cholitis, glomerular nephritis, acute respiratory insufficiency, idiopathic fibrosis, and rheumatoid arthritis.Type: GrantFiled: April 11, 2001Date of Patent: May 15, 2007Assignee: Dompe S.p.A.Inventors: Marcello Allegretti, Riccardo Bertini, Cinzia Bizzarri, Vilma Sabbatini, Ginfranco Caselli, Maria Candida Cesta, Janete Peloia Barroso Gandolfi, legal representative, Giulio Agostino Gandolfi, legal representative, Maria Carla Gandolfi, legal representative, Arrigo Aldo Gandolfi, legal representative, Francesco Colotta, Carmelo Gandolfi, deceased
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Patent number: 7217706Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.Type: GrantFiled: February 14, 2002Date of Patent: May 15, 2007Assignee: Astellas Pharma Inc.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
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Patent number: 7205316Abstract: Compounds of formula (I) wherein R1 or R2 is a tricyclic or bicyclic ring, each of which contains at least two heteroatoms, and R1, R2, R3, R3a, R3b, R4, R5, L, X, X?, Y, Y?, Z, and Z? are as defined herein, are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).Type: GrantFiled: May 6, 2005Date of Patent: April 17, 2007Assignee: Abbott LaboratoriesInventors: Robert J. Altenbach, Lawrence A. Black, Marlon D. Cowart, Huaqing Liu
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Patent number: 7186843Abstract: This invention provides a quinolone derivative having potent antibacterial activity against various bacteria including drug-resistant strains which is a compound of the following formula wherein R1 is an optionally substituted aromatic group, a salt of the same or a hydrate of both.Type: GrantFiled: April 29, 2004Date of Patent: March 6, 2007Assignee: Daiichi Pharmaceutical Co. Ltd.Inventors: Makoto Takemura, Hisashi Takahashi, Katsuhiro Kawakami, Toshiyuki Takeda, Rie Miyauchi
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Patent number: 7183292Abstract: This invention is directed to compounds of formula I: wherein R1–R5 and a-e are as defined in the specification; or pharmaceutically-acceptable salt or solvate or stereoisomer thereof. The invention also directed to pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors using such compounds.Type: GrantFiled: June 10, 2004Date of Patent: February 27, 2007Assignee: Theravance, Inc.Inventors: Mathai Mammen, Adam Hughes, Yu-hua Ji, Li Li, Weijiang Zhang
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Patent number: 7169928Abstract: Use of a compound of formula (A), wherein: W is a residue which imparts antagonistic and/or agonistic activity at histamine H3-receptors when attached to an imidazole ring in 4(5) position; R1 and R2 may be identical or different and represent each independently a lower alkyl or cycloalkyl, or taken together with the nitrogen atom to which they are attached, a saturated nitrogen-containing ring (i) as defined, a non-aromatic unsaturated nitrogen-containing ring (ii) as defined, a morpholino group, or a N-substituted piperazino group as defined for preparing medicaments acting as antagonists and/or agonists at the H3-receptors of histamine.Type: GrantFiled: June 1, 2004Date of Patent: January 30, 2007Assignee: Societe Civile BioprojectInventors: Jean-Charles Schwartz, Jean-Michel Arrang, Monique Garbarg, Jeanne-Marie Lecomte, Xavier Ligneau, Walter G. Schunack, Holger Stark, Charon Robin Ganellin, Fabien Leurquin, Sigurd Elz
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Patent number: 7166601Abstract: The present invention relates to novel substituted diamine derivatives for the formula wherein R1, R2, R3, R4, X1, X2, X3, X4, A, Y and n are as described in the specification, pharmaceutical compositions containing them and intermediates used in their manufacture. More particularly, the compounds of the invention are motilin receptor antagonists useful for the treatment of associated conditions and disorders such as gastrointestinal reflux disorders, eating disorders leading to obesity and irritable bowel syndrome.Type: GrantFiled: April 26, 2006Date of Patent: January 23, 2007Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Sigmond G. Johnson, Ralph A. Rivero
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Patent number: 7138416Abstract: The invention discloses a novel series of compound represented by general formula (I), its derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, pharmaceutically acceptable salts, and solvates wherein X, n, k, z, R1, R2, R3, R4, R5 and R6 are as defined in the specification that are useful in (i) normalizing elevated blood glucose levels in diabetics, (ii) treating disorders related to glucose intolerance and (iii) for scavenging free radicals in mammals.Type: GrantFiled: April 8, 2003Date of Patent: November 21, 2006Assignee: Torrent Pharmaceuticals Ltd.Inventor: Alangudi Sankaranarayanan
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Patent number: 7132422Abstract: The invention provides sodium channel modulating compounds which are useful for treating diseases or conditions associated with sodium channel activity, such as neuropathic pain. The invention also provides pharmaceutical compositions comprising a compound of the present invention, as well as therapeutic methods comprising administering such a compound or salt to a mammal (e.g. a human).Type: GrantFiled: February 4, 2005Date of Patent: November 7, 2006Assignee: Theravance, Inc.Inventors: Seok-Ki Choi, Paul R. Fatheree, David C. Green, Daniel Marquess
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Patent number: 7126028Abstract: Process for the preparation of chiral compounds of formula (I) comprising contacting a compound of formula (II) with a source of hydrogen or halide; wherein A is a chiral center; X is selected from oxygen, sulphur and nitrogen; n is selected from 0 and 1 and is equal to the valence of X less 2; B is a fragment CR 3 2; Z is hydrogen or halogen; with the proviso that when X is nitrogen, n is 1, one of R 1 and two of R 2 are hydrogen, BZ is CHPh 2, the other R 1 and R 2 do not form together a five membered heterocyclic (pyrrolidone) ring; novel intermediates, novel compounds, polymers and libraries thereof and the use thereof as fine chemicals, and compositions thereof.Type: GrantFiled: December 6, 1999Date of Patent: October 24, 2006Assignee: The University Court of the University of St. AndrewsInventor: David O'Hagan
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Patent number: RE39558Abstract: Compounds of this formula are useful for treating or preventing, obesity, breast cancer, osteoporosis, endometriosis, cardiovascular disease and prostatic disease.Type: GrantFiled: December 23, 2004Date of Patent: April 10, 2007Assignee: Pfizer Inc.Inventors: Kimberly O. Cameron, Paul A. DaSilva Jardine, Robert L. Rosati