Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Piperidine Ring Patents (Class 546/225)
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Patent number: 7893261Abstract: A serotonin reuptake inhibitor which can be used in the treatment of depression and which has a decreased occurrence of unwanted side effects. The serotonin reuptake inhibitors are bi-functional organic molecules which combine serotonin transporter reuptake inhibition with serotonin (5-HT, such as 5-HT2A) receptor antagonism in one molecular entity. The serotonin-selective reuptake inhibitor (SSRI) homologue portion of the molecule shows an affinity to the serotonin reuptake transporter (SERT) and has antidepressant properties. The piperazine or piperidine portion of the molecule demonstrates an affinity to 5-HT receptors and restores the undesired side effects of SSRIs.Type: GrantFiled: March 28, 2005Date of Patent: February 22, 2011Assignee: Baylor UniversityInventors: Kevin G. Pinney, Maria Graciela Miranda, James Michael Dorsey
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Patent number: 7879221Abstract: The present invention relates to a process for preparing a porous metal organic framework comprising at least two organic compounds coordinated to at least one metal ion, which comprises the steps (a) oxidation of at least one anode comprising the metal corresponding to at least one metal ion in a reaction medium in the presence of at least one first organic compound which is an optionally substituted monocyclic, bicyclic or polycyclic saturated or unsaturated hydrocarbon in which at least two ring carbons have been replaced by heteroatoms selected from the group consisting of N, O and S to form a reaction intermediate comprising the at least one metal ion and the first organic compound; and (b) reaction of the reaction intermediate at a prescribed temperature with at least one second organic compound which coordinates to the at least one metal ion, with the second organic compound being derived from a dicarboxylic, tricarboxylic or tetracarboxylic acid.Type: GrantFiled: May 11, 2007Date of Patent: February 1, 2011Assignee: BASF SEInventors: Hermann Pütter, Markus Schubert, Ingo Richter, Ulrich Müller, Natalia Trukhan
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Publication number: 20110014226Abstract: A method to identify small molecules useful as therapeutics and/or vaccines to prevent, alleviate or ameliorate a pathogenic infection or an autoimmune disorder. The method can be used to screen small molecule test compounds for the ability to disrupt particular antigen-antibody interactions of interest. In one embodiment, the antigen is a pathogen-derived antigen and the antibody decreases or inhibits virulence of the pathogen when bound to the antigen (e.g., a neutralizing antibody, antibody with serum bactericidal activity, etc.). In another embodiment, the antigen is a self-antigen (autoantigen) and the antibody is an autoantibody that is known to be associated with a pathological condition (e.g., autoimmune disorder). Compounds that bind to the antigen or antibody disrupt binding can be used as therapeutics to decrease or inhibit the autoimmune disorder.Type: ApplicationFiled: March 17, 2009Publication date: January 20, 2011Inventors: Michael J. Caulfield, Michael D. Miller, Joseph G. Joyce, Paul D. Zuck, Krista L. Getty, Vadim Dudkin, Elizabeth A. Ottinger
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Publication number: 20100324052Abstract: The invention relates to novel piperidine carboxylic acid amide derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of these novel compounds, pharmaceutical compositions comprising such compounds and especially the use of such compounds as inhibitors of renin.Type: ApplicationFiled: August 12, 2010Publication date: December 23, 2010Inventors: Olivier Bezencon, Christoph Boss, Daniel Bur, Austin Chih-Yu Chen, Olivier Corminboeuf, Daniel Dube, Walter Fischli, Corinna Grisostomi, Lubos Remen, Sylvia Richard-Bildstein, Thierry Sifferlen, Michel Therien, Thomas Weller
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Publication number: 20100210633Abstract: Chemokine receptor antagonists, in particular, compounds of Formula (I) that act as antagonists of the chemokine CCR2 receptor, including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leukocyte accumulation are described herein.Type: ApplicationFiled: October 12, 2007Publication date: August 19, 2010Applicant: EPIX Delaware, Inc.Inventors: Jian Lin, Dongli Chen, Steffi Koerner, Rosa E. Melendez, Pradyumma Mohanty, Efrat Ben-Zeev, Merav Fichman, Yael Marantz, Oren Becker, Dilara McCauley, Pini Orbach, Ashis K. Saha, Sharon Shacham, Michael Xie
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Patent number: 7777042Abstract: A composition for binding FKBP proteins is disclosed, along with a method of treating conditions associated with neuronal degeneration, wherein said composition comprises a compound of formula I, wherein, R, R1, R2, R3 and X are as defined herein.Type: GrantFiled: December 6, 2006Date of Patent: August 17, 2010Assignee: Aventis Pharmaceuticals Inc.Inventors: Raymond W. Kosley, Jr., Bruce Baron, Patrick Jimonet, John G. Jurcak, Stephen J. Shimshock, Xu-Yang Zhao, Rosy Sher, Paul J. Mueller, Jennifer Beall, Matthieu Barrague, Joseph W. Guiles
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Patent number: 7772253Abstract: This invention is concerned with compounds of the formula wherein R1 to R5, R5? and A are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.Type: GrantFiled: May 26, 2006Date of Patent: August 10, 2010Assignee: Hoffman-La Roche Inc.Inventors: Alfred Binggeli, Andreas Christ, Luke Gideon Granville Green, Wolfgang Guba, Hans-Peter Maerki, Rainer Eugen Martin, Peter Mohr
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Publication number: 20100179119Abstract: Novel compounds inhibiting the integrin ?2?1/GPIa-IIa receptor are disclosed. Also disclosed are pharmaceutical compositions containing the compounds, as well as methods of their therapeutic use. The compounds disclosed are useful, inter alia, as inhibitors of integrin ?2?1/GPIa-IIa-mediated activity.Type: ApplicationFiled: September 24, 2009Publication date: July 15, 2010Inventors: William F. DeGrado, Meredith W. Miller, Sandeep Basra, Joel S. Bennett, Sungwook Choi
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Publication number: 20100160305Abstract: 3,4,5-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4,5-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4,5-substituted piperidine compound, a method for the manufacture of a 3,4,5-substituted piperidine compound, and novel intermediates and partial steps for its synthesis. The compounds are of the formula I, wherein the substitutents are as defined in the specification.Type: ApplicationFiled: March 7, 2006Publication date: June 24, 2010Applicant: NOVARTIS AGInventors: Keiichi Masuya, Fumiaki Yokokawa, Osamu Irie, Atsuko Nihonyanagi, Takeru Ehara, Kazuhide Konishi, Takanori Kanazawa, Masaki Suzuki
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Publication number: 20100120859Abstract: The present invention relates to piperidine-based renin inhibitor compounds having carboxylate or carboxylic acid terminal groups, and their use in treating cardiovascular events and renal insufficiency.Type: ApplicationFiled: May 23, 2008Publication date: May 13, 2010Applicant: MERCK FROSST CANADA LTD.Inventors: Tom Yao-Hsiang Wu, Helene Juteau, Michel Gallant, Daniel Dube, Patrick Roy, Renee Aspiotis, Erich L. Grimm, Sebastien Laliberte, Austin Chen
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Publication number: 20100063091Abstract: The present invention relates to disubstituted piperidinyl renin inhibitor compounds having the structure (Formula I) and their use in treating cardiovascular events and renal insufficiency.Type: ApplicationFiled: November 14, 2007Publication date: March 11, 2010Inventors: Daniel Dube, Michel Gallant, Erich L. Grimm, Helene Juteau, Sebastien Laliberte, Tom Yao-Hsiang Wu
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Publication number: 20100041704Abstract: Dermal compositions comprising topical formulations of bupivacaine or ropivacaine, characterized by effective dermal absorption and long duration of dermal anesthetic activity, and intended for use in patients suffering from pruritus and dermal pain, including neuropathic pain, are provided. Compositions containing both bupivacaine and capsaicin are provided. Methods of alleviating pain by the topically administration of these compounds are also provided.Type: ApplicationFiled: January 11, 2008Publication date: February 18, 2010Inventors: A.K. Gunnar Aberg, Keith A. Johnson
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Publication number: 20090306042Abstract: The present invention provides compounds of formula (I) in which n, y, X1, X2, A, B, R1, R2, R3, R4 and R5 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: December 10, 2008Publication date: December 10, 2009Inventors: Mark Furber, Christopher Andrew Luckhurst, Hitesh Jayantilal Sanganee, Linda Anne Stein, Peter Alan Cage
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Patent number: 7619092Abstract: The present invention provides a novel piperidine compound of the formula [I]: wherein Ring A represents an optionally substituted benzene ring, Ring B represents an optionally substituted benzene ring, R1 represents an optionally substituted alkyl group, an optionally substituted hydroxyl group, etc., or a group of the formula: (a) wherein R11 and R12 are the same or different, and each represents hydrogen atom, a substituted carbonyl group, a substituted sulfonyl group, an optionally substituted alkyl group, etc., R2 represents hydrogen atom, etc., Z represents oxygen atom or a group represented by —N(R3)—, R3 represents hydrogen atom or an alkyl group, etc., R4 represents hydrogen atom or an alkyl group, etc., or a pharmaceutically acceptable salt thereof.Type: GrantFiled: May 29, 2003Date of Patent: November 17, 2009Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Masami Takahashi, Tsutomu Miyake, Yasunori Moritani, Hidetoshi Asai, Taketoshi Ishii, Rikako Kono
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Publication number: 20090264469Abstract: The present patent application concerns new compounds of formula (I): displaying agonistic activity at sphingosine-1-phosphate (S1P) receptors, their process of preparation and their use as immunosuppressive agents.Type: ApplicationFiled: October 18, 2005Publication date: October 22, 2009Applicants: BIO-PROJET, SUN PHARMACEUTICAL INDUSTRIES LTD.Inventors: Marc Capet, Nicolas Levoin, Isabelle Berrebi-Bertrand, Olivia Poupardin, Philippe Robert, Jean-Charles Schwartz, Jeanne-Marie Lecomte, Thennati Rajamannar, Ranjan Kumar Pal, Biswajit Samanta, Jignesh K. Jivani, Bhavesh M. Panchal, Isha H. Bhatt, Jayraj D. Aradhye
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Patent number: 7605289Abstract: Benzamide derivatives of formula I and II, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof, and pharmaceutical compositions comprising the same, are described and have therapeutic utility, particularly in the treatment of diabetes, obesity, and related conditions and disorders: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12 are defined as provided herein.Type: GrantFiled: June 8, 2006Date of Patent: October 20, 2009Assignee: Amgen, Inc.Inventors: Jay P. Powers, Michael Degraffenreid, Xiao He, Lisa Julian, Dustin L. McMinn, Daqing Sun, Yosup Rew, Xuelei Yan
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Patent number: 7572814Abstract: Certain 3,5-dibenzoyl-4-phenyl-piperidine compounds and salts thereof are provided herein. The compounds and salts may be useful in causing mitotic arrest and cell death. Also provided herein are certain pharmaceutical compositions comprising 3,5-dibenzoyl-4-phenyl-piperidine compounds or salts thereof and certain methods of use thereof.Type: GrantFiled: November 15, 2006Date of Patent: August 11, 2009Assignee: Cytokinetics, IncorporatedInventors: Scott Collibee, Zhe Yang, Luke Ashcraft, Gustave Bergnes, Bradley P. Morgan, David J. Morgans, Jr., Jianchao Wang
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Patent number: 7572815Abstract: Amide derivatives represented by the formula (I): wherein: A is a cycloalkyl group, an aryl group or a heteroaryl group; X is a nitrogen atom or CR17; Y is —NRa—, —(CRbRb?)m-, and the like; m is 0 to 4; and R1 to R17 may be the same or different and each is a hydrogen atom, a halogen atom, a cyano group, a nitro group, a carboxyl group, a formyl group, a hydroxyl group, an ammonium group, an alkyl group optionally having one or more substituents, ZR18 and the like, Z is —O—, —S(O)p-, —S(O)pO—, —NH—, —NR19-, and the like; or R1 and R2 may in combination form a ring, a pharmaceutically acceptable salt thereof, a hydrate thereof, or a solvate thereof may be applied to pharmaceutical use such as anti-inflammatory and analgesic action and the like.Type: GrantFiled: November 18, 2005Date of Patent: August 11, 2009Assignee: Ajinomoto Co., Inc.Inventors: Tadakiyo Nakagawa, Tamotsu Suzuki, Kaoru Takenaka, Shinichi Fujita, Youji Yamada, Yoichiro Shima, Tatsuya Okuzumi, Toshihiko Yoshimura, Masanao Yoshida, Masahiro Murata
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Publication number: 20090187024Abstract: The invention pertains to a process for preparing stable anhydrous Ropivacaine hydrochloride, the process involving preparing Ropivacaine hydrochloride from Ropivacaine base, wherein Ropivacaine base is provided having a chiral purity of more than 95%, and wherein the isolation involves the use of isopropanol and hydrochloride, and is performed under water-free conditions. Ropivacaine base may be provided at high chiral purity by N-propylating L-pipecolic acid 2,6-xylidide hydrochloride in the presence of a phase transfer catalyst, wherein the reaction involves a biphasic reaction mixture containing an alkaline aqueous phase and an organic phase. The invention further pertains to stable anhydrous Ropivacaine hydrochloride obtainable by the above process.Type: ApplicationFiled: April 25, 2007Publication date: July 23, 2009Applicant: DISHMAN PHARMACEUTICALS AND CHEMICALS LTD.Inventors: Janmejay Rajnikant Vyas, Venkata Satya Varma Nidadavolu, Denish Hasmukhlal Shah
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Publication number: 20090187020Abstract: The invention relates to new compounds of formula (III): wherein R is a C1-C4 linear or branched alkyl group. The invention also relates to new compounds of formula (IV) wherein M is a metal. The invention also relates to methods of making compounds of formulas (III) and (IV) and to methods of making donepezil and pharmaceutically acceptable salts thereof, such as donepezil hydrochloride, using the compounds.Type: ApplicationFiled: January 3, 2007Publication date: July 23, 2009Applicant: CIPLA LIMITEDInventors: Srinivas Laxminarayan Pathi, Vinod Acharya, Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan
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Publication number: 20090156623Abstract: N-aryl piperidine substituted biphenylcarboxamides compounds of formula (I) methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes.Type: ApplicationFiled: January 9, 2009Publication date: June 18, 2009Inventors: Lieven Meerpoel, Leo Jacobus Jozef Backx, Peter Walter Maria Roevens
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Publication number: 20090137566Abstract: The invention relates to substituted 3,4- or higher substituted piperididine compounds, the use thereof for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; pharmaceutical formulations or products comprising said compounds, and/or a method of treatment comprising administering said compounds, a method for the manufacture of said compounds, as well as novel intermediates, starting materials and/or partial steps for their synthesis. The compounds preferably have the formula I, wherein the moieties R1, R2, R11 and W are as defined in the specification.Type: ApplicationFiled: May 24, 2006Publication date: May 28, 2009Inventors: Takeru Ehara, Yuko Hitomi, Kazuhide Konishi, Kelichi Masuya
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Patent number: 7517892Abstract: One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.Type: GrantFiled: September 12, 2001Date of Patent: April 14, 2009Assignee: Sepracor Inc.Inventors: Brian M. Aquila, Thomas D. Bannister, Gregory D. Cuny, James R. Hauske, Joanne M. Holland, Paul E. Persons, Heike Radeke, Fengjiang Wang, Liming Shao
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Publication number: 20090062342Abstract: The invention relates to novel amine derivatives and the use thereof as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors of renin.Type: ApplicationFiled: March 7, 2007Publication date: March 5, 2009Applicant: Actelion Pharmaceuticals Ltd.Inventors: Olivier Bezencon, Daniel Bur, Olivier Corminboeuf, Corinna Grisostomi, Lubos Remen, Sylvia Richard-Bildstein, Thomas Weller
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Patent number: 7495105Abstract: The present invention describes a method of separation of the enantiomers of N-(2,6-dimethylphenyl)-1-propyl-2-piperidinocarboxamide. Another object of the present invention refers to the enantiomeric manipulation of the enantiomers of N-(2,6-dimethylphenyl)-1-propyl-2-piperidinocarboxamide, in order to achiever compounds and pharmaceutical compositions presenting diverse enantiomeric excesses of (S)-N-(2,6-dimethylphenyl)-1-propyl-2-piperidinocarboxamide, in order to quantify and determine the participation of (R)-N-(2,6-dimethylphenyl)-1-propyl-2-piperidinocarboxamide in the anesthetic and cardiotoxic effects. These compounds and compositions enantiomerically manipulated demonstrate to present a significant improvement in itsanesthetic properties, presenting a cardiotoxic profile equivalent to pure enantiomer, a (S)-N-(2,6-dimethylphenyl)-1-propyl-2-piperidinocarboxamide.Type: GrantFiled: October 8, 2002Date of Patent: February 24, 2009Assignee: Cristalia Produtos Quimicos Farmaceuticos Ltda.Inventors: Valter Freiro Torres Russo, Elisa Mannochio de Souza Russo, Ogari de Castro Pacheco
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Publication number: 20090042943Abstract: The present invention relates to compounds of formula (I) wherein R1 and A are as defined in the specification as dual modulators of the serotonin 5-HT2a and dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use as medicaments. Compounds of general formula (I) have high affinity for the dopamine D3 and serotonin (5-Hydroxytryptamine; 5-HT) 5-HT2A receptors and are effective in the treatment of psychotic disorders, as well as other diseases such as depression and anxiety, drug dependence, dementias and memory impairment.Type: ApplicationFiled: August 1, 2008Publication date: February 12, 2009Inventors: Luca Gobbi, Georg Jaeschke, Rosa Maria Rodriguez Sarmiento, Lucinda Steward
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Publication number: 20090042730Abstract: The invention relates to novel aryl ketones of the formula (I) in which A1, A2, Q, R1, R2, X, Y and Z are as defined in the description, their use as herbicides and processes and intermediates for their preparation.Type: ApplicationFiled: September 4, 2008Publication date: February 12, 2009Inventors: Stefan Herrmann, Dorothee Hoischen, Kristian Kather, Klaus-Helmut Muller, Otto Schallner, Hans-Georg Schwarz, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen
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Publication number: 20090023730Abstract: The invention provides compounds and pharmaceutically acceptable salts of Formula I wherein the variables A1, A2, R1, R2, V, W, X, Y, and Z are defined herein. Certain compounds of Formula I described herein which possess potent antiviral activity. The invention particularly provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These infectious diseases include viral infections, particularly HCV infections.Type: ApplicationFiled: February 25, 2008Publication date: January 22, 2009Applicant: ACHILLION PHARMACEUTICALSInventors: Avinash Phadke, Dawei Chen, Milind Deshpande, Andrew Thurkauf, Xiangzhu Wang, Yiping Shen, Cuixian Liu, Jesse Quinn, Junko Ohkanda, Shouming Li
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Publication number: 20090018103Abstract: Diaminoalkanes of Formula I have now been found which are orally active and bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with elevated levels of aspartic protease activity. The invention also relates to a method for the use of the compounds of Formula I in ameliorating or treating aspartic protease related disorders in a subject in need thereof comprising administering to said subject an effective amount of a compound of Formula I.Type: ApplicationFiled: October 7, 2005Publication date: January 15, 2009Applicant: VITAE PHARMACEUTICAL, INCInventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillar, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh, Patrick T. Flaherty, Jean-Pierre Wery
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Patent number: 7476686Abstract: The invention provides compounds and pharmaceutically acceptable salts of Formula I wherein the variables A1, A2, R1, R2, V, W, X, Y, and Z are defined herein. Certain compounds of Formula I described herein which possess potent antiviral activity. The invention particularly provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These infectious diseases include viral infections, particularly HCV infections.Type: GrantFiled: December 17, 2004Date of Patent: January 13, 2009Assignee: Achillion Pharmaceuticals, Inc.Inventors: Dawei Chen, Milind Deshpande, Andrew Thurkauf, Avinash Phadke, Xiangzhu Wang, Yiping Shen, Cuixian Liu, Jesse Quinn, Junko Ohkanda, Shouming Li
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Publication number: 20080275028Abstract: The present invention relates to compounds with ?7 nAChR agonistic activity, processes for their preparation, pharmaceutical compositions containing the same and the use thereof for the treatment of neurological, psychiatric, cognitive, immunological and inflammatory disorders.Type: ApplicationFiled: July 19, 2005Publication date: November 6, 2008Inventors: Giovanni Gaviraghi, Chiara Ghiron, Hendrik Bothmann, Renza Roncarati, Georg Christian Terstappenn
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Publication number: 20080262230Abstract: Disclosed is a novel benzyloxypropylamine derivative having an excellent tachykinin receptor antagonistic effect. This compound shows a good transfer into the blood and a long blood half-life in the blood kinetic test using a guinea pig orally administered with the compound and is stable in an animal plasma. The compound also shows a high transfer to the central nervous system when it is orally administered to a guinea pig at a certain dose. Accordingly, the benzyloxypropylamine derivative is quite useful as a novel anti-tachykinin agent.Type: ApplicationFiled: March 29, 2006Publication date: October 23, 2008Applicant: Nippon Zoki Pharmaceutical Co., LTD.Inventors: Kunihiko Higashiura, Takashi Ogino, Kazuhito Furukawa
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Publication number: 20080207689Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.Type: ApplicationFiled: July 3, 2007Publication date: August 28, 2008Inventors: Alan Daniel Brown, Mark Edward Bunnage, Charlotte Alice Louise Lane, Russell Andrew Lewthwaite, Paul Alan Glossop, Kim James, David Anthony Price
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Patent number: 7410971Abstract: A compound represented by the following general formula (1) or (100), a salt thereof or a hydrate of the foregoing has excellent cell adhesion inhibitory action or cell infiltration inhibitory action, and is useful as a therapeutic or prophylactic agent for various inflammatory diseases and autoimmune diseases associated with adhesion and infiltration of leukocytes, such as inflammatory bowel disease (particularly ulcerative colitis or Crohn's disease), irritable bowel syndrome, rheumatoid arthritis, psoriasis, multiple sclerosis, asthma and atopic dermatitis. wherein R10 represents optionally substituted cycloalkyl, etc., R20-23 represent hydrogen, alkyl, alkoxy, etc., R30-32 represent hydrogen, alkyl, oxo, etc., and R40 represents optionally substituted alkyl, etc.Type: GrantFiled: December 24, 2004Date of Patent: August 12, 2008Assignee: Eisai R&D Management Co., Ltd.Inventors: Tetsuya Kawahara, Makoto Kotake, Naoki Yoneda, Shinsuke Hirota, Masayoshi Ohkuro
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Patent number: 7390905Abstract: The present invention relates to a piperidine compound represented by the formula [I]: wherein Ring A represents an optionally substituted benzene ring, Ring B represents an optionally substituted benzene ring, R1 represents an optionally substituted hydoxyl group, a substituted thiol group, a substituted sulfonyl group, etc., or a group represented by the formula: R11 represents a substituted carbonyl group or a substituted sulfonyl group, R12 represents hydrogen atom or an optionally substituted alkyl group, R2 represents hydrogen atom, etc., Z represent oxygen atom or a group represented by —N(R3)—, R3 represents an optionally substituted alkyl group, etc., R4a represents an optionally substituted alkyl group, R4b represents an optionally substituted alkyl group, or a pharmaceutically acceptable salt thereof, having an excellent tachykinin receptor antagonistic action.Type: GrantFiled: November 26, 2004Date of Patent: June 24, 2008Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Masami Takahashi, Tsutomu Miyake, Takeshi Yamanaka, Hidetoshi Asai, Rikako Kono
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Publication number: 20080139556Abstract: A composition for binding FKBP proteins is disclosed, along with a method of treating conditions associated with neuronal degeneration, wherein said composition comprises a compound of formula I, wherein, R, R1, R2, R3 and X are as defined herein.Type: ApplicationFiled: December 6, 2006Publication date: June 12, 2008Applicant: AVENTIS PHARMACEUTICALS INC.Inventors: Raymond W. KOSLEY, Bruce Baron, Patrick Jimonet, John G. Jurcak, Stephen J. Shimshock, Xu-yang Zhao, Rosy Sher, Paul J. Mueller, Jennifer Beall, Matthieu Barrague, Joseph W. Guiles
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Patent number: 7368443Abstract: The present invention is directed to 2,6-disubstituted piperidine and piperazine analogs having the following general formula: which are used to treat diseases of the central nervous system, drug abuse, and withdrawal therefrom as well as treating eating disorders.Type: GrantFiled: March 31, 2004Date of Patent: May 6, 2008Assignee: University of Kentucky Research FoundationInventors: Peter A. Crooks, Linda Dwoskin, Marlon D. Jones, Dennis Keith Miller, Seth Davin Norholm, Guangrong Zheng, Sairam Krishamurthy
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Patent number: 7361666Abstract: 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: April 11, 2002Date of Patent: April 22, 2008Assignee: Sepracor, Inc.Inventors: Brian M. Aquila, James R. Hauske, Liming Shao
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Patent number: 7332607Abstract: The present invention provides various processes for the preparation of (R)-?-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol.Type: GrantFiled: May 6, 2004Date of Patent: February 19, 2008Assignees: Aventis Holdings Inc., Sanofi Aventis Deutschland GmbHInventors: Sandra K. Stolz-Dunn, Jonathan Evans, Ian A. Tomlinson
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Patent number: 7294637Abstract: One aspect of the present invention relates to a method of treating of drug addiction or drug dependence in a mammal, comprising the step of administering to a mammal in need thereof a therapuetically effective amount of a heterocyclic compound, e.g., a 3-substituted piperidine. In a preferred embodiment, the method of the present invention treats cocaine addiction or methamphetamine addiction.Type: GrantFiled: February 4, 2004Date of Patent: November 13, 2007Assignee: Sepracor, Inc.Inventors: Brian M. Aquila, Thomas D. Bannister, Gregory D. Cuny, James R. Hauske, Joanne M. Holland, Paul E. Persons, Heike S. Radeke, Fengjiang Wang, Liming Shao
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Publication number: 20070232653Abstract: The present invention relates to a process for the preparation of cis substituted cyclic ?-aryl or heteroaryl carboxylic acid derivatives in high diastereo- and enantioselectivity by enantioselective hydrogenation in accordance with the following scheme wherein X, Ar, n, and m are defined herein and corresponding salts thereof.Type: ApplicationFiled: March 30, 2007Publication date: October 4, 2007Inventors: Stephan Bachmann, Michelangelo Scalone, Patrick Schnider
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Patent number: 7276511Abstract: The invention provides a compound which exhibits satisfactory peroral absorbability and excellent antagonistic activity against NK-1 receptor or NK-2 receptor.Type: GrantFiled: August 2, 2004Date of Patent: October 2, 2007Assignee: Zeria Pharmaceutical Co., Ltd.Inventors: Masaaki Nagasawa, Nobuo Kawase, Nobuyuki Tanaka, Hideki Nakamura, Naoki Tsuzuike, Masakazu Murata
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Patent number: 7273946Abstract: Prostaglandin nitroderivatives having improved pharmacological activity and enhanced tolerability are described. They can be employed for the treatment of glaucoma and ocular hypertension.Type: GrantFiled: January 5, 2005Date of Patent: September 25, 2007Assignee: Nicox S.A.Inventors: Eninnio Ongini, Valerio Chiroli, Francesca Benedini, Piero Del Soldato
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Patent number: 7262211Abstract: Novel compounds having activity as non-covalent inhibitors of urokinase and having activity in reducing or inhibiting blood vessel formation are provided. These compounds have at a group having a guanidino moiety or derivative thereof. These compounds are useful in vitro for monitoring plasminogen activator levels and in vivo in treatment of conditions which are ameliorated by inhibition of or decreased activity of urokinase and in treating pathologic conditions wherein blood vessel formation is related to a pathologic condition.Type: GrantFiled: December 4, 2002Date of Patent: August 28, 2007Assignee: Dendreon CorporationInventors: Amir P. Tamiz, L. Josue Alfaro-Lopez, Odile Esther Levy, Joseph Edward Semple
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Patent number: 7247729Abstract: A method of manufacturing a pipecolamide derivative, characterized in that pipecolic acid or an acid salt thereof is reacted with an amine in an inert solvent in the presence of a condensing agent such as dicyclohexylcarbodiimide, 1-ethyl-2-(2-dimethylaminopropyl)carbodiimide, methanesulfonyl chloride or phosphoryl chloride. Pipecolamide derivatives, particularly in optically active forms thereof can be efficiently and economically manufactured without harmful gas by-products.Type: GrantFiled: September 10, 2002Date of Patent: July 24, 2007Assignee: Mercian CorporationInventors: Toshio Tsuchida, Katsura Kaneko, Naoki Matsumoto
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Patent number: 7238709Abstract: This invention relates to hindered carbamate derivatives that are muscarinic receptor antagonists, pharmaceutical compositions comprising such compounds, and methods of preparing these compounds.Type: GrantFiled: December 7, 2000Date of Patent: July 3, 2007Assignee: Theravance, Inc.Inventors: Mathai Mammen, David Oare
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Patent number: 7153869Abstract: This invention relates to a series of substitituted amino acids of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention are small molecules which bind to the erythropoietin receptor and compete with the natural ligand for binding to this receptor.Type: GrantFiled: March 12, 2004Date of Patent: December 26, 2006Inventors: Peter J. Connolly, Victor T. Bandurco, Steven K. Wetter, Sigmond Johnson, Jacqueline Bussolari, William V. Murray
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Patent number: 7135483Abstract: Substituted heterocyclinc compounds are disclosed. The compounds are useful for treating multidrug resistance. The compounds can be formulated in compositions with a carrier and, optionally, a therapeutic agent.Type: GrantFiled: November 29, 2001Date of Patent: November 14, 2006Assignee: H. Lee Moffitt Cancer Center & Research Institute, Inc.Inventors: Charles Raymond Degenhardt, David Joseph Eickhoff
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Patent number: 7084144Abstract: A compound having the general formula (I): wherein: X is N or C; R0 is H, a lower alkyl group, a lower O-alkyl group, lower alkyl group, a benzyl group, a phenyl group, a heterocyclic amine group, a cycloalkyl group, a cycloalkyl group substituted with O-alkyl or, a furyl group; R1 and R2 are, independently, H, an amine group, a lower alkyl group, a lower O-alkyl group, a lower S-alkyl group or a lower N-alkyl group, or R1 and R2 taken together with the carbon atoms to which they are attached form a five-membered carbocyclic or heterocyclic ring, where the heteroatoms of the heterocyclic ring are one or two oxygen atoms, and/or where any substituent on said carbocyclic or heterocyclic ring is chosen from O, S and N; n is 0,1,2,3 or 4; m is 0 or 1; and pharmaceutically acceptable salts thereof; with the proviso that said compound is not 1-[(4-methoxyphenyl)sulfonyl]piperazine or 1-(1,3-benzodioxol-5-ylsulfonyl)piperazine.Type: GrantFiled: May 19, 2004Date of Patent: August 1, 2006Assignee: The Jordanian Pharmaceutical MFG & Medical Equipment CO LTDInventor: Adnan Badwan
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Patent number: RE39128Abstract: The present invention relates to pleuromutilin derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medical therapy, particularly antibacterial therapy.Type: GrantFiled: October 27, 1998Date of Patent: June 13, 2006Assignee: SmithKline Beecham p.l.c.Inventors: Valerie Joan Berry, Steven Dabbs, Colin Henry Frydrych, Eric Hunt, Francis Dominic Sanderson, Gary Woodnutt