Acyclic Nitrogen Bonded Directly To A -c(=x)- Group, Wherein X Is Chalcogen Patents (Class 546/247)
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Publication number: 20100204275Abstract: This invention relates to novel N-piperidin-4-ylmethyl amide derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy, and to pharmaceutical compositions comprising the compounds of the invention.Type: ApplicationFiled: July 31, 2008Publication date: August 12, 2010Applicant: NeuroSearch A/SInventors: Dan Peters, Birgitte L. Eriksen, John Paul Redrobe, Gordon Munro, Elsebet Østergaard Nielsen
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Publication number: 20100144720Abstract: Pharmaceutical compositions containing organic compounds or salts thereof that serve as modulators for the SDF-1 or I-TAC chemokines are disclosed. The compounds and compositions are useful in the treatment of cancer, especially in the inhibition of cancer proliferation, growth, and metastasis. Methods of interfering with SDF-1 and/or I-TAC binding to the CCXCKR2 receptor and treating cancer using the compounds and pharmaceutical compositions of the present invention are also disclosed.Type: ApplicationFiled: December 11, 2009Publication date: June 10, 2010Applicant: ChemoCentryx, Inc.Inventors: Anita Melikian, Jennifer Burns, Brian E. McMaster, Thomas Schall, John J. Wright
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Patent number: 7723349Abstract: The present invention provides a compound of Formula I or Formula II: enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula I and II are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.Type: GrantFiled: April 23, 2004Date of Patent: May 25, 2010Assignee: Incyte CorporationInventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Fenglei Zhang, Brian Metcalf
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Publication number: 20100034813Abstract: Disclosed are new substituted pyrazole and triazole compounds of Formula (I) and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the derivatives together with pharmaceutically acceptable carriers, and uses thereof:Type: ApplicationFiled: November 8, 2007Publication date: February 11, 2010Inventors: Yi Xia, Kris G. Mendenhall, Paul A. Barsanti, Annette O. Walter, David Duhl, Paul A. Renhowe
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Publication number: 20100029687Abstract: [Problem] To provide a compound which can be used for treating diseases in which a calcium sensing receptor (CaSR) participates, particularly hyperparathyroidism. [Means for Resolution] It was found that a novel piperidine derivative which is characterized in that one of a 3-position and a 4-position is substituted with an aminomethyl group substituted with an arylalkyl group or the like and the other position is substituted with aryl, heteroaryl or the like, or a salt thereof, has an excellent CaSR agonistic regulatory action, and also has excellent selectivity with a CYP2D6 inhibitory action having a possibility of causing drug interaction. Based on the above, this novel piperidine derivative is useful as a therapeutic agent for diseases in which CaSR participates (hyperparathyroidism, renal osteodystrophy, hypercalcemia, and the like).Type: ApplicationFiled: November 14, 2007Publication date: February 4, 2010Applicant: ASTELLAS PHARMA INC.Inventors: Shunichiro Hachiya, Kazuhiro Ikegai, Ryotaro Ibuka, Taisuke Takahashi, Makoto Oku, Ryushi Seo, Yoh Terada, Masanao Sanagi
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Publication number: 20100016602Abstract: Disclosed is an arylamidine derivative represented by the following general formula: (wherein R1 and R2 independently represent an optionally substituted C3-4 alkyl group) or a salt thereof, which is useful as an antifungal agent.Type: ApplicationFiled: December 27, 2006Publication date: January 21, 2010Applicant: Toyama Chemical Co., Ltd.Inventor: Kazuya Hayashi
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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: 20090306077Abstract: The present invention relates to a study on the synthesis of a novel N-(2-aminophenyl)benzamide derivative having an urea structure and represented by the general formula (1); and the utilization of a pharmacological effect of the derivative. A compound represented by the general formula (1) or a salt thereof has an effect of cellular morphological change on trabecular meshwork cells and is effective in the prevention and/or treatment of a disease considered to be related to intraocular pressure. In the formula, R1 and R2 represent a hydrogen atom, a lower alkyl group, or the like; R3 represents a hydroxy group, a lower alkoxy group, a lower cycloalkyloxy group, an aryloxy group, or the like; R4 and R5 represent a halogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group, or the like; X represents a lower alkylene group or the like; Y represents a single bond, a lower alkylene group, or the like; l and m represent 0, 1, 2, or the like.Type: ApplicationFiled: December 26, 2007Publication date: December 10, 2009Inventors: Hiroyuki Mogi, Hisashi Tajima, Noriko Mishina, Yusuke Yamazaki, Shinji Yoneda, Katsuhiko Watanabe, Junko Fujikawa, Minoru Yamamoto
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Patent number: 7619050Abstract: The instant invention relates to novel alkoxyamine initiators/regulators containing an ethylenically unsaturated, radically polymerizable group. The compounds are useful for the preparation of complex polymeric architectures. Further aspects of the invention are a polymerizable composition and a polymerization process comprising the alkoxyamine initiators/regulators, a macroinitiator obtainable by said polymerization process and a process for polymerizing with the macroinitiator.Type: GrantFiled: May 17, 2005Date of Patent: November 17, 2009Assignee: Ciba Specialty Chemicals CorporationInventors: Peter Nesvadba, Andreas Kramer, Lucienne Bugnon
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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: 20090227790Abstract: The present application is directed to therapeutic compounds, compositions, and methods for culturing neuronal cells and for preventing and the treatment of neurodegenerative diseases, such as Parkinson's disease and amyotrophic lateral sclerosis (ALS).Type: ApplicationFiled: April 7, 2009Publication date: September 10, 2009Inventor: Leu-Fen H. Lin
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Publication number: 20090198033Abstract: The invention relates to new alkoxyamines suitable for hydrosilylation reactions, to siloxane modified alkoxamines and to siloxane modified polymers and to their use as slip and leveling agent or as dispersant. The alkoxamines are compounds of formula (I) or (II) wherein A is a group capable of forming a stable free nitroxyl radical A.Type: ApplicationFiled: October 16, 2006Publication date: August 6, 2009Inventors: Lothar Alexander Engelbrecht, Peter Nesvadba
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Publication number: 20090143386Abstract: The present invention provides compounds useful for inhibiting the ADAM-10 protein. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role. The invention also provides methods for making bis-aryl ether sulfonyl chlorides and ADAM-10 modulators therefrom.Type: ApplicationFiled: February 2, 2009Publication date: June 4, 2009Inventors: S. David Brown, Lynne Canne-Bannen, Erick Wang Co, Vasu Jammalamadaka, Rickard George Khoury, Moon Hwan Kim, Donna T. Le, Amy Lew Tsuhako, Morrison B. Mac, Shumeye Mamo, John M. Nuss, Michael P. Prisbylla, Wei Xu
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Publication number: 20090118330Abstract: The present invention relates to novel diurea derivatives that block intracellular signal transduction and thereby inhibit the production of pro-inflammatory cytokines, especially interleukin-2 (IL-2) and/or induce apoptosis in activated T-cells. It further discloses such a compound for use as a medicament, the use of said compound for the manufacturing of a medicament for the treatment of immune disorders which benefit from inhibition of production of IL-2 and other pro-inflammatory cytokines and/or induction of apoptosis in activated T-cells, a pharmaceutical composition comprising said compound and a method of treatment comprising administration of a pharmaceutically effective amount of said compound.Type: ApplicationFiled: January 19, 2005Publication date: May 7, 2009Inventors: Aina Lisbeth Abramo, Lars Olof Goran Pettersson, Kerstin Ingalill Andersson, Asa Anette Sundstedt
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Patent number: 7456203Abstract: Disclosed are multibinding compounds which are muscarinic receptor antagonists. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is, independently of each other, a muscarinic receptor antagonist or an allosteric modulator provided that at least one of said ligand is a muscarinic receptor antagonist. The multibinding compounds of this invention are useful in the treatment and prevention of diseases such as chronic obstructive pulmonary disease, chronic bronchitis, irritable bowel syndrome, urinary incontinence, and the like.Type: GrantFiled: April 29, 2003Date of Patent: November 25, 2008Assignee: Theravance, Inc.Inventors: James Aggen, John H. Griffin, Mathai Mammen, Daniel Marquess, Edmund J. Moran, David Oare
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Patent number: 7446204Abstract: This invention is directed to Amino substituted Aryloxybenzylpiperidine derivatives which are ligands at the MCH1 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by admixing a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject a therapeutically effective amount of a compound of the subject invention.Type: GrantFiled: September 20, 2005Date of Patent: November 4, 2008Assignee: H. Lundbeck A/SInventors: Mohammad R. Marzabadi, Chien-An Chen, Yu Jiang, Kai Lu, Kim Andersen
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Publication number: 20080248093Abstract: The present invention is directed to water-soluble derivatives of 2,6-diisopropylphenol (Propofol). The compounds act as prodrugs of 2,6-diisopropylphenol and metabolize rapidly to Propofol thereby providing an alternative to the water-insoluble 2,6-diisopropylphenol. Pharmaceutical compositions comprising these compounds, methods of induction and maintenance of anesthesia or sedation as well as methods of treating neurodegenerative diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.Type: ApplicationFiled: July 24, 2007Publication date: October 9, 2008Inventors: Subramanian Marappan, Cris Davenport, Sepehr Sarshar
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Publication number: 20080234247Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.Type: ApplicationFiled: March 17, 2008Publication date: September 25, 2008Applicant: Sepracor, Inc.Inventors: Brian M. Aquila, James R. Hauske, Liming Shao
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Publication number: 20080207630Abstract: The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts, solvates, hydrates or pharmaceutically acceptable formulations thereof. These compounds may be used to modulate cellular proliferation and to prevent and/or treat proliferative diseases.Type: ApplicationFiled: April 13, 2006Publication date: August 28, 2008Inventors: Robert Eckl, Roswitha Taube, Michael Almstetter, Michael Thormann, Andreas Treml, Christopher Straub, Zhuoliang Chen
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Publication number: 20080161577Abstract: 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: July 3, 2008Inventors: Mathai Mammen, Adam Hughes, Yu-hua Ji, Li Li, Weijiang Zhang
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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: 7297793Abstract: Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula: or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein the variables are as defined herein.Type: GrantFiled: February 8, 2006Date of Patent: November 20, 2007Assignee: G.D. Searle, LLCInventors: John N. Freskos, Daniel P. Getman, John J. Talley, James A. Sikorski
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Patent number: 7199158Abstract: Succinoylamino hydroxyethylamino sulfonyl urea derivatives of the formula: wherein R1–R6, R7, R7?, R8, R30–R34, X?, Y, Y?, t, x, and n are as defined herein, are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: July 18, 2005Date of Patent: April 3, 2007Assignee: G.D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
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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: 7129228Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.Type: GrantFiled: January 7, 2004Date of Patent: October 31, 2006Assignee: Sepracor Inc.Inventors: Gregory D. Cuny, Liming Shao, James R. Hauske, Michele L. R. Heffernan, Brian M. Aquila, Xinhe Wu, Fengjiang Wang, Thomas D. Bannister
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Patent number: 7125825Abstract: Viscoelastic surfactants are described for use in aqueous systems to generate thickened fluids. The surfactants are alkyl amidoamine salts of inorganic acids and/or organic acids. The fluids may also contain inorganic salts, organic salts or mixtures thereof. Additionally, the fluids may contain a co-surfactant. These fluids are particularly useful in oilfield applications such as hydraulic fracturing, gravel packing, drilling, completion, etc. Viscoelastic fluids of the invention are also useful in industrial and consumer product fluid applications as rheology control agents.Type: GrantFiled: April 25, 2003Date of Patent: October 24, 2006Assignee: Tomah Products, Inc.Inventor: David Kelly Moss
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Patent number: 7122551Abstract: Compounds of the formula I useful as metalloproteinase inhibitors, especially as inhibitors of MMP 13.Type: GrantFiled: February 26, 2004Date of Patent: October 17, 2006Assignee: AstraZeneca ABInventors: Bernard Christophe Barlaam, Robert Ian Dowell, Maurice Raymond Verschoyle Finlay, Nicholas John Newcombe, Howard Tucker, David Waterson
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Patent number: 6995180Abstract: A compound of the formula I: wherein R1, R2, R3 and R4 are as defined herein. Further provided are methods of using such compounds for the treatment of diabetes and related diseases, and to pharmaceutical compositions containing such compounds.Type: GrantFiled: October 21, 2003Date of Patent: February 7, 2006Assignee: Bristol Myers Squibb CompanyInventors: David R. Magnin, Lawrence G. Hamann
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Patent number: 6867217Abstract: The invention relates to substituted polycyclic aryl and heteroaryl pyridone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.Type: GrantFiled: May 18, 2000Date of Patent: March 15, 2005Assignee: Pharmacia CorporationInventors: Michael S. South, Qingping Zeng, Ashton T. Hamme, II, Melvin L. Rueppel
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Patent number: 6809207Abstract: The present invention provides certain alpha-amino acids and derivatives thereof, such as, but not limited to, esters, amides and salts. These derivatives may comprise such representative side groups as a phenyl, pyridyl, piperidinyl, tetrahydropyranyl, tetrahydrothiopyranyl, or thienyl group. The present invention further provides a method for synthesizing alpha-amino acids and derivatives thereof via a modified Ugi type reaction using an aldehyde, ammonium formate and a C1-C5 alkyl isocyanide. The compounds provided by this method are useful in the development of new pharmaceuticals for the treatment of human diseases.Type: GrantFiled: July 24, 2002Date of Patent: October 26, 2004Assignee: PharmaCore, Inc.Inventors: Sekar Alla, Seung-Yong Choi, Dale Dhanoa, Elso DiFranco, Galina Krokhina, Keqiang Li, Balasubramanian Thiagarajan, Wen-Chun Zhang
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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: 6790854Abstract: A substance having affinity for an opioid &dgr; receptor, which is represented by the following general formula (I): wherein, X represents a group of the general formula: —CO—N(R5)(R6) (II) and the like, n represents 1 to 3, R1 and R2 represent a hydrogen atom, a halogen atom, a lower alkyl group and the like, R3 represents a hydrogen atom, a halogen atom, a lower alkyl group and the like, R4 represents a saturated or unsaturated monocyclic or bicyclic carbocyclic group and the like, R5 to R12 represent a hydrogen atom, a lower alkyl group and the like, and R3 and R4, R5 and R6, R7 or R8 and R9 and R10 may bind to each other to form a cyclic structure, and a medicament useful for preventive and/or therapeutic treatment of central nervous system diseases and peripheral nervous system diseases comprising the substance as an active ingredient.Type: GrantFiled: March 13, 2003Date of Patent: September 14, 2004Assignee: Meiji Seika Kaisha, Ltd.Inventors: Masaki Tsushima, Kaori Tadauchi, Kenji Asai, Naoko Miike, Toshiaki Kudo
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Patent number: 6787522Abstract: Compounds of formula (I) are antibacterials: wherein: R1 represents hydrogen, or C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms; R2 represents a group R10—(X)n—(ALK)m— wherein R10 represents hydrogen, or a C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, cycloalkyl, aryl, or heterocyclyl group, any of which may be unsubstituted or substituted by (C1-C6)alkyl, (C1-C6)alkoxy, hydroxy, mercapto, (C1-C6)alkylthio, amino, halo (including fluoro, chloro, bromo and iodo), trifluoromethyl, cyano, nitro, —COOH, —CONH2, —COORA, —NHCORA, —CONHRA, —NHRA, —NRARB, or —CONRARB wherein RA and RB are independently a (C1-C6)alkyl group, and ALK represents a straight or branched divalent C1-C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radical, and may be interrupted by one or more non-adjacent —NH—, —O— or —S— linkages, X represents —NH—, —O— or —S—, anType: GrantFiled: April 30, 2002Date of Patent: September 7, 2004Assignee: British Biotech PharmaceuticalsInventors: Michael George Hunter, Raymond Paul Beckett, John Martin Clements, Mark Whittaker, Stephen John Davies, Lisa Marie Pratt, Zoe Marie Spavold, Steven Launchbury
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Publication number: 20040157843Abstract: The present invention relates to the use of 2-amino-thiazoline derivatives of formula (I): 1Type: ApplicationFiled: January 26, 2004Publication date: August 12, 2004Applicant: Aventis Pharma S.A.Inventors: Antony Bigot, Jean-Christophe Carry, Serge Mignani
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Patent number: 6740741Abstract: Novel diazo derivatives useful for the deacidification of paper material and the process for their preparation comprising three steps starting from an amine and ethyl chlorocarbonate, are described.Type: GrantFiled: July 3, 2002Date of Patent: May 25, 2004Assignees: Consiglio Nazionale delle Ricerche, Universita'degli Studi di UdineInventors: Antonio Zappala', Andrea Gorassini, Angelo Guimanini, Giancarlo Verardo
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Patent number: 6737528Abstract: Vinylic hindered amine light stabilizers as novel polylmerizable light stabilizers are disclosed and have the general formula (I): wherein: R1 is C1 to C8: alkyl, alkoxy, alkyl phenyl, hydroxy alkyl (all linear and branched), allyl, acyl, cycloalkyl (cyclopentyl, cyclohexyl or curnyl: linear and branched); R2 is hydrogen and methyl, R3 is vinyl, C1-C4 vinyl alkyl [H2C═C(R4)C1-C4], R4 is H, C1-C4 alky and alkyl phenyl and R5 is H, C1-C4 alkyl, X is O, NH, C1-C8 alkyloxy and alkylamino: (linear or branched).Type: GrantFiled: February 22, 2001Date of Patent: May 18, 2004Assignee: Council of Scientific and Industrial ResearchInventors: Shrojal Mohitkumar Desai, Raj Pal Singh
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Patent number: 6677332Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.Type: GrantFiled: May 25, 2000Date of Patent: January 13, 2004Assignee: Sepracor, Inc.Inventors: Gregory D. Cuny, Liming Shao, James R. Hauske, Michele L. R. Heffernan, Brian M. Aquila, Xinhe Wu, Fengjiang Wang, Thomas D. Bannister
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Patent number: 6667342Abstract: Compounds of formula (I), pharmaceutically acceptable salts or in vivo hydrolysable esters thereof, wherein: Ring X is phenyl or a six membered heteroaryl ring containing one or two ring nitrogens where said nitrogens are optionally oxidised to form the N-oxide; R1 and R2 are substituents as defined within; R3 and R4 are defined within and are alkyl or halo alkyl or together form a halocycloalkyl ring; R5 is a substituent as defined within; Y—Z is a linking group as defined within; are useful in the production of a elevation of PDH activity in a warm-blooded animal such as a human being. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are described.Type: GrantFiled: August 22, 2000Date of Patent: December 23, 2003Assignee: Astrazeneca ABInventors: David S Clarke, Jeremy N Burrows, Paul Ro Whittamore, Roger J Butlin, Thorsten Nowak
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Patent number: 6653321Abstract: Methods for treating conditions associated with hyperglycemia, especially Type II diabetes, with novel naphthylsulfonic acids and related compounds. These compounds, as single stereoisomers or mixtures of stereoisomers, or their pharmaceutically acceptable salts, are useful in methods of stimulating the kinase activity of the insulin receptor, enhancing the activation of the insulin receptor by insulin, and stimulating the uptake of glucose into cells. A variety of antidiabetic compounds and pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.Type: GrantFiled: July 28, 2000Date of Patent: November 25, 2003Assignee: Telik, Inc.Inventors: Wayne R. Spevak, Songyuan Shi, Prasad V. V. S. V. Manchem, Michael R. Kozlowski, Steven R. Schow, Robert T. Lum, Louise Robinson, Jeong Weon Park
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Publication number: 20030083498Abstract: Compounds and methods of preparing compounds of the formula:Type: ApplicationFiled: July 9, 2002Publication date: May 1, 2003Inventors: Thomas P. Sassi, Ram B. Gupta
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Patent number: 6538138Abstract: The invention relates to processes for the preparation of compounds of the formula wherein R is a 2-piperidyl or 2-pyridyl radical, and pharmaceutically acceptable salts thereof, the process comprising the steps of: a) reacting 2,5-bis(2,2,2-trifluoroethoxy)benzoic acid or a salt thereof with a haloacetonitrile to form a cyanomethyl ester of formula b) reacting the ester with an amine of the formula RCH2NH2, where R is as defined above.Type: GrantFiled: April 3, 2000Date of Patent: March 25, 2003Assignee: FineTech Ltd.Inventors: Arie L. Gutman, Genady Nisnevich, Eleonora Shkolnik, Igor Zaltzman
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Publication number: 20030050310Abstract: Compounds of formula (I) are matrix metalloproteinase inhibitors wherein X represents a carboxylic acid group —COOH, or a hydroxamic acid group —CONHOH;R2 represents a radical of formula (II): R3—(ALK)m—(Q)p—(ALK)n—, and W represents a cyclic amino radical of formula (IIIA) or (IIIB): 1Type: ApplicationFiled: September 12, 2002Publication date: March 13, 2003Applicant: British Biotech Pharmaceuticals Ltd.Inventor: Fionna Mitchell Martin
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Patent number: 6521707Abstract: The invention relates to novel isocyanates containing tertiary amino groups, a process for preparing them, and also their use for the synthesis and modification of polymers. The invention provides isocyanates of the formula (I) where R1 and R2 are, independently of one another, alkyl having from 1 to 6 carbon atoms, where R1 and R2 may be joined to form a ring, Z is alkylene having from 2 to 6 carbon atoms, n is an integer from 0 to 20, Y is alkylene having from 2 to 6 carbon atoms. The alkyl radicals R1 and R2 may be linear or branched or joined to form an aliphatic ring. The alkylene radical Z preferably contains from 2 to 4 carbon atoms.Type: GrantFiled: November 1, 2001Date of Patent: February 18, 2003Assignee: Bayer AktiengesellschaftInventors: Wolfgang Podszun, Joachim Krüger, Kamelia Karlou-Eyrisch
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Patent number: 6515124Abstract: Aromatic dehydroamino acids are disclosed that are active as LFA-1 arnagonists This activity enables these compounds to prevent inflammation which is a consequence of T cell activation and accordingly reduce or eliminate inflammatory skin disease psoriasis.Type: GrantFiled: January 5, 2001Date of Patent: February 4, 2003Assignee: Hoffman-La Roche Inc.Inventors: Nader Fotouhi, Paul Gillespie, Robert William Guthrie, Sherrie Lynn Pietranico-Cole, Weiya Yun
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Patent number: 6515024Abstract: Succinoylamino hydroxyethylamino sulfonyl urea derivatives are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: December 11, 2001Date of Patent: February 4, 2003Assignee: G. D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
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Patent number: 6506778Abstract: The invention is directed to acylphenylurea derivatives and their physiologically tolerated salts and physiologically functional derivatives. Compounds of the formula I in which the radicals have the stated meanings, and their physiologically tolerated salts and a process for their preparation are described. The compounds are suitable, for example, for treating type II diabetes.Type: GrantFiled: June 8, 2001Date of Patent: January 14, 2003Assignee: Aventis Pharma Deutschland GmbHInventors: Elisabeth Defossa, Thomas Klabunde, Hans-Joerg Burger, Andreas Herling, Karl-Heinz Baringhaus
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Patent number: 6479502Abstract: Compounds of formula (I) are matrix metalloprotemase inhibitors wherein X represents a carboxylic acid group —COOH, or a hydroxamic acid group —CONHOH;R2 represents a radical of formula (II): R3—(ALK)m—(Q)p—(ALK)n.Type: GrantFiled: February 21, 2001Date of Patent: November 12, 2002Assignee: British Biotech PharmaceuticalsInventor: Fionna Mitchell Martin
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Patent number: 6458812Abstract: Amide derivatives of 1,4 di-substituted piperidine compounds of the formula: or a pharmaceutically acceptable salt, ester or solvate thereof, wherein R1 is optionally substituted cycloalkyl, cycloalkylalkyl, aryl, arylalkyl or heteroaryl; R2 is H, alkyl, or optionally substituted cycloalkyl, cycloalkylalkyl, heterocycloalkyl, bridged cycloalkyl, or bridged heterocycloalkyl; R3 is alkyl or —CH2OH; and R4 is H or alkyl; are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed.Type: GrantFiled: December 17, 2001Date of Patent: October 1, 2002Assignee: Schering CorporationInventors: Brian A. McKittrick, Guihua Guo, Zhaoning Zhu, Yuanzan Ye
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Patent number: 6451791Abstract: An amidoaromatic ring sulfonamide hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed, as are a treatment process that comprises administering a contemplated amidoaromatic ring sulfonamide hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: June 4, 1999Date of Patent: September 17, 2002Assignee: Monsanto CompanyInventors: Robert M. Heintz, Daniel P. Getman, Joseph J. McDonald, Gary A. DeCrescenzo, Susan C. Howard, S. Zaheer Abbas