Having -c(=x)-, Wherein X Is Chalogen, Attached Directly Or Indirectly To The Piperidine Ring By Nonionic Bonding Patents (Class 546/221)
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Publication number: 20120268706Abstract: The invention relates to compounds of the formula I, and to a liquid-crystalline medium, preferably having a nematic phase and negative dielectric anisotropy, which comprises one or more compounds of formula I, defined herein, for use in an electro-optical display, particularly in an active-matrix display based on the VA, ECB, PALO, FFS or IPS effect, and to the use of the compounds of the formula I for the stabilization of a liquid-crystalline medium which comprises one or more compounds of the formula II and one or more compounds of the formulae III-1 to III-4, defined herein.Type: ApplicationFiled: April 20, 2012Publication date: October 25, 2012Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Mark GOEBEL, Rocco FORTTE, Detlef PAULUTH
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Publication number: 20120238574Abstract: The present invention relates to (1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl derivatives having the general formula (I) to pharmaceutical compositions comprising the same and to the use of these (1,1,1,3,3,3-hexafluoro-2-hydroxy-propan-2-yl)phenyl derivatives in the treatment of atherosclerosis.Type: ApplicationFiled: October 26, 2010Publication date: September 20, 2012Applicant: N.V. ORGANONInventors: Andrew John Cooke, Emma Louise Carswell, David Jonathan Bennett
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Publication number: 20120149908Abstract: In a first aspect, the present invention relates to a method for the preparation of alkynylpiperidine and alkynylpiperidine derivatives. In particular, a method is provided for preparing alkynylpiperidine derivatives starting from epoxide compounds. Further, the alkynylpiperidine derivatives according to the present inventions are substituted trans-3-4-alkynylpiperidine derivatives. In another aspect, triazolylpiperidine compounds and methods for said preparation are provided. In particular, the triazolylpiperidine compounds according to the present invention are obtained by reacting an alkynylpiperidine derivatives with an organic azid, preferably, in the presence of a Cu (I) or Ru catalyst. In a preferred embodiment, 1,4-disubstituted or 1,5-disubstituted 1,2,3-triazolylpiperidine compounds are provided.Type: ApplicationFiled: December 13, 2011Publication date: June 14, 2012Inventors: Leiv K. Sydnes, Bengt Erik Haug, Rianne Harmsen
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Publication number: 20120122708Abstract: New compounds are continually sought after for the treatment and prevention of disorders. The invention relates to N-(2-oxo-1-phenylpiperidin-3-yl)sulfonamides which can be biologically and pharmacologically traced, in order to be used in the search for, and identification of, new lead compounds that can modulate the functional activity of a biological target.Type: ApplicationFiled: December 29, 2011Publication date: May 17, 2012Inventors: JOSEP CASTELLS BOLIART, David Enrique MIGUEL CENTENO, Marta PASCUAL GILABERT
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Publication number: 20120116072Abstract: Benzenesulfonamide compounds having a structure of the following general formula (I) are described. Also described, are methods for synthesizing the compounds, and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions.Type: ApplicationFiled: June 28, 2010Publication date: May 10, 2012Inventors: Laurence Clary, Sandrine Chambon, Laurent Chantalat, Pascale Mauvais, Olivier Roye, Marlene Schuppli
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Patent number: 8129376Abstract: The present invention relates to piperidine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.Type: GrantFiled: March 20, 2009Date of Patent: March 6, 2012Inventors: Kumar Sundaresan, P. Bala Koteswara Rao, Bharathiraja Ainan, Hariharasubramanian Ayyamperumal, Girish A R, Srinivas Tatiparthy, Ganesh Prabhu, Hosahalli Subramanya, Alexander Bischoff
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Publication number: 20120046276Abstract: A method of preventing or treating diseases caused by Mycobacterium, comprising administering to a subject in need of such treatment an effective amount of a pleuromutilin.Type: ApplicationFiled: October 25, 2011Publication date: February 23, 2012Applicant: Nabriva Therapeutics AGInventors: Gerd Ascher, Heinz Berner, Rosemarie Mang
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Publication number: 20120046247Abstract: This invention relates to compounds of Formula (I), (II), or (III) as shown in the specification, which contain a 1,5-diphenylpenta-1,4-dien-3-one backbone. These compounds can be used to treat cancer, inflammatory disease, or autoimmune disease.Type: ApplicationFiled: August 16, 2011Publication date: February 23, 2012Inventors: Charles C-Y Shih, Toshio Kitamura, Qian Shi, Toshiyuki Kawashima, Hui-Kang Wang
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Publication number: 20110319378Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.Type: ApplicationFiled: June 3, 2011Publication date: December 29, 2011Applicant: AMGEN INC.Inventors: Michael David BARTBERGER, Ana GONZALEZ BUENROSTRO, Hilary Plake BECK, Xiaoqi CHEN, Richard Victor CONNORS, Jeffrey DEIGNAN, Jason DUQUETTE, John EKSTEROWICZ, Benjamin FISHER, Brian Matthew FOX, Jiasheng FU, Zice FU, Felix GONZALEZ LOPEZ DE TURISO, Michael GRIBBLE, JR., Darin James GUSTIN, Julie Anne HEATH, Xin HUANG, Xianyun JIAO, Michael G. JOHNSON, Frank KAYSER, David John KOPECKY, Sujen LAI, Yihong LI, Zhihong LI, Jiwen LIU, Jonathan Dante LOW, Brian Stuart LUCAS, Zhihua MA, Lawrence McGEE, Joel McINTOSH, Dustin McMINN, Julio Cesar MEDINA, Jeffrey Thomas MIHALIC, Steven Howard Olson, Yosup REW, Philip Marley ROVETO, Daqing SUN, Xiaodong WANG, Yingcai WANG, Xuelei YAN, Ming YU, Jiang ZHU
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Patent number: 8080541Abstract: The present invention relates to the use of a compound of formula I wherein R1, R2, R3, R4, X and n are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomers and/or optical isomers for the treatment of psychoses, pain, dysfunction in memory and learning, attention deficit, schizophrenia, dementia disorders or Alzheimer's disease.Type: GrantFiled: August 19, 2010Date of Patent: December 20, 2011Assignee: Hoffman-La Roche Inc.Inventors: Sabine Kolczewski, Emmanuel Pinard
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Publication number: 20110295014Abstract: The present invention discloses processes for preparing piperidine derivative compounds of the formulae: wherein n is 0 or 1; R1 is hydrogen or hydroxy; R2 is hydrogen; or, when n is 0, R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2, provided that when n is 1, R1 and R2 are each hydrogen; R3 is —COOH or —COOR4; R4 is an alkyl or aryl moiety; A, B, and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents.Type: ApplicationFiled: August 11, 2011Publication date: December 1, 2011Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Thomas E. D'AMBRA, Garry M. PILLING
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Patent number: 8067604Abstract: Processes are disclosed for preparing piperidine derivative compounds of the formulae I, II or III:Type: GrantFiled: November 22, 2010Date of Patent: November 29, 2011Assignee: Albany Molecular Research, Inc.Inventors: Harold Meckler, Ben Littler, Prasad Raje, Michael van Brunt, Paul F Vogt
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Publication number: 20110275797Abstract: An N-acyl anthranilic acid derivative represented by general formula (1) or a salt thereof is useful for prevention or treatment of diseases associated with excessive production of collagen. (In the formula, R1 represents a carboxyl group or the like; R2 represents a hydrogen atom or the like; R3 represents an optionally substituted aryl group or the like; X1 represents a carbonyl group; X2 represents a bonding hand; X3 represents a bonding hand; X4 represents a bonding hand or the like; and A represents an optionally substituted phenyl group or the like.Type: ApplicationFiled: January 29, 2010Publication date: November 10, 2011Applicant: Toyama Chemical Co., Ltd.Inventors: Junichi Yokotani, Arihiro Takatori, Yukie Tada, Minori Yanai, Hiroshi Kato, Yoichi Taniguchi, Chiharu Tanabe
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Publication number: 20110275673Abstract: The invention relates to compounds of Formula (I). Compounds of the present invention are inhibitors of sphingosine kinase 3, and are useful in the treatment of various disorders and conditions, such as inflammatory disorders.Type: ApplicationFiled: September 17, 2009Publication date: November 10, 2011Inventors: Yibin Xiang, Bradford Hirth, John L. Kane, Junkai Liao, Kevin Noson, Christopher Yee
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Publication number: 20110263628Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.Type: ApplicationFiled: June 8, 2011Publication date: October 27, 2011Applicant: APPLIED RESEARCH SYSTEMS ARS HOLDING N.V.Inventors: Dominique Swinnen, Agnes Bombrun, Jerome Gonzalez, Stefano Crosignani, Patrick Gerber, Catherine Jorand-Lebrun
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Publication number: 20110237511Abstract: This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions, which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts.Type: ApplicationFiled: June 3, 2011Publication date: September 29, 2011Applicant: Merck Frosst CanadaInventors: Xavier Billot, John Colucci, Yongxin Han, Marie-Claire Wilson, Robert N. Young
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Publication number: 20110178066Abstract: Chemical agents, such as derivatives of hydroxypiperidine moieties, and similar heterocyclic ring structures, including salts thereof, that act as anti-cancer and anti-tumor agents, especially where such agents modulate the activity of enzymes and structural polypeptides present in cells, such as cancer cells, or where the agents modulate levels of gene expression in cellular systems, including cancer cells, are disclosed, along with methods for preparing such agents, as well as pharmaceutical compositions containing such agents as active ingredients and methods of using these as therapeutic agents.Type: ApplicationFiled: July 21, 2010Publication date: July 21, 2011Inventors: Norman E. Ohler, Jeffrey W. Watthey, Qin Zong, Paul E. Young, Kathryn J. Strand, Stanislaw Pikul
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Publication number: 20110178077Abstract: The present invention relates to small molecule compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.Type: ApplicationFiled: June 17, 2009Publication date: July 21, 2011Inventors: Priscille Brodin, Thierry Christophe, Zaesung No, Jaeseung Kim, Auguste Genovesio, Denis Philippe Cedric Fenistein, Heekyoung Jeon, Fanny Anne Ewann, Sunhee Kang, Saeyeon Lee, Min Jung Seo, Eunjung Park, Monica Contreras Dominguez, Ji Youn Nam, Eun Hye Kim
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Publication number: 20110172431Abstract: A process is provided for producing a 1-substituted trans-4-(substituted amino)piperidin-3-ol represented by formula (III-1): The process includes a step of reacting a 1-substituted-3,4-epoxypiperidine represented by formula (I): with an amine compound represented by formula (II) in the presence of an inorganic lithium salt. By utilizing the process, trans-4-aminopiperidin-3-ol compounds useful as various chemical products, such as medicine intermediates, can be produced.Type: ApplicationFiled: September 25, 2009Publication date: July 14, 2011Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Toshiaki Aikawa, Osamu Tokuda, Tetsuya Ikemoto
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Patent number: 7973057Abstract: Thalidomide analogs that modulate tumor necrosis factor alpha (TNF-?) activity and angiogenesis are disclosed. In particularly disclosed embodiments, the thalidomide analogs are isosteric sulfur-containing analogs. Also disclosed are methods of treating a subject with the analogs.Type: GrantFiled: September 17, 2004Date of Patent: July 5, 2011Assignees: The United States of America as represented by the Department of Health and Human Services, P2D Inc.Inventors: Nigel H. Greig, Harold Holloway, Arnold Brossi, Xiaoxiang Zhu, Tony Giordano, Qian-sheng Yu, William D. Figg
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Patent number: 7968577Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I) an enantiomer, diastereomer, tautomer, solvate (e.g.Type: GrantFiled: October 31, 2007Date of Patent: June 28, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Bingwei Vera Yang, Lidia M. Doweyko, Wayne Vaccaro, Tram N. Huynh, David R. Tortolani, T. G. Murali Dhar
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Publication number: 20110105532Abstract: The present invention relates to halogen-substituted amide derivatives of the general formula (I) in which R1 to R6, Q1 to Q8, A, V, W, X, Y, n and m are each defined as described in the description—and to a process for preparation thereof and to the use thereof as insecticides and acaricides.Type: ApplicationFiled: October 27, 2010Publication date: May 5, 2011Applicant: Bayer CropScience AGInventors: Markus HEIL, Eike Kevin Heilmann, Alexander Sudau, Tobias Kapferer, Friedrich August Mühlthau, Peter Jeschke, Arnd Voerste, Ulrich Görgens, Klaus Raming, Ulrich Ebbinghaus-Kintscher, Mark Drewes, Martin Adamczewski, Angela Becker
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Publication number: 20110098320Abstract: This invention relates to novel compounds of the Formula (I), (I*), (Ia), (Ib), (Ic), (Id), (Ie), (If), (If*), (Ig), (Ih), (Ij), (Ik), (ll1-3), (Im1-3), (In1-3), (lo1-2), (Ip1-9), (Iq1-9), (Ir1-9) and (Is1-3) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.Type: ApplicationFiled: January 7, 2009Publication date: April 28, 2011Inventors: David A. Claremon, Linghang Zhuang, Yuanjie Ye, Suresh B. Singh, Colin M. Tice, Zhenrong Xu, Robert D. Simpson
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Publication number: 20110065923Abstract: Processes are disclosed for preparing piperidine derivative compounds of the formulae I, II or III:Type: ApplicationFiled: November 22, 2010Publication date: March 17, 2011Applicant: Albany Molecular Research, Inc.Inventors: Harold MECKLER, Benjamin J. Littler, Prasad Raje, Michael van Brunt, Paul F. Vogt
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Publication number: 20110059937Abstract: This invention relates to novel compounds and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: ApplicationFiled: November 12, 2010Publication date: March 10, 2011Inventor: Jakob Busch-Petersen
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Publication number: 20110053904Abstract: The present invention relates to the use of a compound of formula I wherein R1, R2, R3, R4, X and n are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomers and/or optical isomers for the treatment of psychoses, pain, dysfunction in memory and learning, attention deficit, schizophrenia, dementia disorders or Alzheimer's disease.Type: ApplicationFiled: August 19, 2010Publication date: March 3, 2011Inventors: Sabine Kolczewski, Emmanuel Pinard
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Publication number: 20110034450Abstract: The present application relates to novel carboxylic acid derivatives having an oxo-substituted azaheterocyclic partial structure, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.Type: ApplicationFiled: April 6, 2009Publication date: February 10, 2011Applicant: BAYER SCHERING PHARMA AKTIEGESELLSCHAFTInventors: Michael Hahn, Eva-Maria Becker, Andreas Knorr, Dirk Schneider, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder, Friederike Stoll, Stefan Heitmeier, Klaus Münter, Nils Griebenow, Thomas Lampe, Sherif El Sheikh, Volkhart Min-Jian Li
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Publication number: 20110028515Abstract: Compounds of formula (I) as well as pharmaceutically acceptable salts thereof can be used in the form of pharmaceutical compositions, wherein A1, A2, R1, R2, R3 and R4 have the significance given in claim 1.Type: ApplicationFiled: July 23, 2010Publication date: February 3, 2011Inventors: Jean Ackermann, Aurelia Conte, Daniel Hunziker, Werner Neidhart, Matthias Nettekoven, Stanley Wertheimer
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Patent number: 7863452Abstract: Processes are disclosed for preparing piperidine derivative compounds of the formulae I, II or III: The processes involve reacting a compound of formula Ia, IIa or IIIa with isobutyrate or an isobutyrate equivalent.Type: GrantFiled: January 20, 2009Date of Patent: January 4, 2011Assignee: Albany Molecular Research, Inc.Inventors: Harold Meckler, Ben Littler, Prasad Raje, Michael van Brunt, Paul F Vogt
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Patent number: 7858798Abstract: Processes are disclosed for preparing piperidine derivative compounds of the formulae I, II or III:Type: GrantFiled: January 20, 2009Date of Patent: December 28, 2010Assignee: Albany Molecular Research, Inc.Inventors: Harold Meckler, Ben Littler, Prasad Raje, Michael van Brunt, Paul F Vogt
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Publication number: 20100292206Abstract: The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4.Type: ApplicationFiled: October 17, 2008Publication date: November 18, 2010Inventors: Shizuo Kasai, Tomohiro Kaku, Masahiro Kamaura
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Patent number: 7829583Abstract: This invention provides biphenyl derivatives of formula I: wherein R1, R2, R3, R4, R5, R6, R7, W, a, b and c are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The biphenyl derivatives of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such biphenyl derivatives are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.Type: GrantFiled: July 13, 2007Date of Patent: November 9, 2010Assignee: Theravance, Inc.Inventors: Mathai Mammen, Adam Hughes, Yan Chen
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Publication number: 20100280250Abstract: A compound comprising a prodrug of a prostaglandin EP4 agonist, wherein said prodrug is an ester, ether, or amide of an amino acid is disclosed herein. Maintenance of the colonic mucosal barrier by method comprising administering a therapeutically effective amount of a prostaglandin EP4 agonist to a colon of a mammal is also disclosed herein. Dosage forms, medicaments, and compositions, related thereto are also disclosed.Type: ApplicationFiled: July 12, 2010Publication date: November 4, 2010Inventors: Wha-Bin Im, Robert M. Burk, Mark Holoboski
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Patent number: 7812035Abstract: 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: December 11, 2002Date of Patent: October 12, 2010Assignee: Sepracor Inc.Inventors: Heike Radeke, Liming Shao
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Patent number: 7790898Abstract: Substituted 3-phenylpiperidine compounds corresponding to Formula I in which R1 and R2 have the meanings defined in the specification, methods for preparing such compounds, pharmaceutical compositions containing such compounds, and the use of such compounds for treating or inhibiting various conditions, especially pain.Type: GrantFiled: January 26, 2007Date of Patent: September 7, 2010Assignee: Gruenenthal GmbHInventors: Joerg Holenz, Helmut Buschmann, Michael Finkam
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Publication number: 20100210592Abstract: The invention relates to the use of compounds of formula I wherein the substituents are described in the description and claims for the treatment of psychoses, dysfunction in memory and learning, schizophrenia, dementia, attention deficit disorders or Alzheimer's disease. The invention also relates to some compounds of formula I and pharmaceutical compositions containing them.Type: ApplicationFiled: February 11, 2010Publication date: August 19, 2010Inventors: Sabine Kolczewski, Hans-Peter Marty, Robert Narquizian, Emmanuel Pinard, Henri Stalder
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Publication number: 20100204199Abstract: Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-Beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: enantiomers, diastereomers, solvates, or salts thereof, wherein A, W, X and Z are defined herein.Type: ApplicationFiled: April 14, 2010Publication date: August 12, 2010Inventors: Xiang-Yang Ye, Jeffrey A. Robl, Ronald L. Hanson, Zhiwei Guo, Ramesh N. Patel
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Publication number: 20100197640Abstract: The present invention relates to novel sulfamoyl-phenyl-ureido compounds having the formula (I) or a physiologically acceptable salt or derivative thereof which are suitable for the therapy of infections caused by protozoa and in particular uncomplicated or severe malaria caused by plasmodia.Type: ApplicationFiled: January 29, 2010Publication date: August 5, 2010Applicant: 4SC AGInventor: Stefano PEGORARO
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Publication number: 20100197715Abstract: The present invention relates to a compound of formula I wherein R1, R2, and Ar are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer thereof. These compounds and their pharmaceutical compositions are useful in the treatment of neurological and neuropsychiatric disorders.Type: ApplicationFiled: January 20, 2010Publication date: August 5, 2010Inventors: Sabine Kolczewski, Emmanuel Pinard, Henri Stalder
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Publication number: 20100191475Abstract: Materials, methods and a computer system are provided which facilitate the identification and characterization of modulators of potassium ion channels, particularly the HERG channel.Type: ApplicationFiled: March 4, 2010Publication date: July 29, 2010Inventors: Scott Perschke, Ming Liu
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Patent number: 7759487Abstract: The present invention discloses a novel process to prepare ketone amides, which are useful intermediates for the preparation of antagonists of CCR5 receptor and therefore useful for the treatment of HIV virus infected mammals. It specifically discloses a novel process to synthesize 1-(2,4-dimethylpyrimidine-5-carbonyl)-4-piperidone, 1-[(2,4-dimethyl-3-pyridinyl)carbonyl]-4-piperidone and related compounds. A salient feature of the invention is the use of a three-phase reaction medium with an organic phase and a buffer salt slurry.Type: GrantFiled: January 5, 2006Date of Patent: July 20, 2010Assignee: Schering CorporationInventors: Shen-Chun Kuo, David Jieh-Shyh Tsai, Hongbiao Liao
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Publication number: 20100168170Abstract: There is provided compounds of formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, m, n, q and r have meanings given in the description, and pharmaceutically acceptable derivatives thereof, which compounds are useful in the treatment of diseases and conditions associated with inflammation.Type: ApplicationFiled: March 12, 2008Publication date: July 1, 2010Inventors: Benjamin Pelcman, Christian Krog-Jensen, Yaping Shen, James Gee Kan Yee, Lloyd F. Mackenzie, Yuanlin Zhou, Kang Han, Jeffery R. Raymond
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Publication number: 20100168171Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: The compounds or salts modulate P2X7 receptor function and are capable of interfering with the effects of ATP at the P2X7 receptor. The invention also provides the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment or prevention of disorders mediated by the P2X7 receptor, for example pain, inflammation or a neurodegenerative disease, in particular pain such as inflammatory pain, neuropathic pain or visceral pain.Type: ApplicationFiled: March 20, 2008Publication date: July 1, 2010Inventors: Paul John Beswick, Robert James Gleave, Jon Graham Anthony Steadman, Daryl Simon Walter
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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: 20100125075Abstract: Compounds of formula (II) are antibacterial agents wherein Q represents a radical of the formula: —N(OH)CH(?O) or the formula: —C(?O)NH(OH); R1 represents hydrogen, C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms, or, except when Q is a radical of the formula: —N(OH)CH(?O), a hydroxy, C1-C6 alkoxy, C1-C6 alkenyloxy, amino, C1-C6 alkylamino, or di-(C1-C6 alkylamino group; R2 represents a substituted or unsubstituted C1-C6 alkyl, cycloalkyl(C1-C6 alkyl)- or aryl(C1-C6 alkyl)-group; and A represents a group of formula (IIA), or (IIB) wherein R4 represents the side chain of a natural or non-natural alpha amino acid, and R5 and R6 when taken together with the nitrogen atom to which they are attached form a saturated heterocyclic first ring of 5 to 7 atoms as specified in the description.Type: ApplicationFiled: December 14, 2006Publication date: May 20, 2010Applicant: British Biotech Pharmaceuticals Ltd.Inventors: Lisa Marie Pratt, Kenneth Noel Keavey, Gilles Denis Pain, Laurent Mounier
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Patent number: 7683077Abstract: The present invention provides a piperidine derivative represented by the following formula or analogs thereto, which are used for agents for treating or preventing various diseases related to 5-HT7.Type: GrantFiled: May 19, 2004Date of Patent: March 23, 2010Assignee: Ajinomoto Co., Inc.Inventors: Shingo Makino, Naoyuki Fukuchi, Sayaka Asari, Masaki Hashimoto, Tetsuo Yano, Youji Yamada, Munetaka Tokumasu, Masataka Shoji, Itsuya Tanabe, Shinichi Fujita, Hideki Matsumoto
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Publication number: 20100069638Abstract: The present invention provides an sulfonamide derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. A compound of the general formula (II): wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a nitrogen-containing non-aromatic heterocyclic ring etc.; the ring C is an aromatic carbocyclic ring etc.; R1 is carboxy etc.; R2 is independently a halogen atom etc.; R3 is optionally substituted alkyloxy etc.; R4 is independently a halogen atom etc.; R5 is independently optionally substituted alkyl etc.; M is sulfonyl etc.; Y is a single bond etc.; L1 is a single bond etc.; L2 is a single bond etc.; k is 0, 1, 2, 3 or 4; n is 0, 1 or 2; and q is 0, 1, 2 or 3; provided that a) k is not 0 when the ring B is a 6-membered nitrogen-containing heterocyclic ring containing one or two nitrogen atom(s) and the ring C is a benzene ring, etc.Type: ApplicationFiled: November 20, 2009Publication date: March 18, 2010Inventors: Akira Kugimiya, Masahiko Fujioka, Yuki Tachibana, Takami Murashi
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Publication number: 20100063040Abstract: The present invention provides an sulfonamide derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. A compound of the general formula (II): wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a nitrogen-containing non-aromatic heterocyclic ring etc.; the ring C is an aromatic carbocyclic ring etc.; R1 is carboxy etc.; R2 is independently a halogen atom etc.; R3 is optionally substituted alkyloxy etc.; R4 is independently a halogen atom etc.; R5 is independently optionally substituted alkyl etc.; M is sulfonyl etc.; Y is a single bond etc.; L1 is a single bond etc.; L2 is a single bond etc.; k is 0, 1, 2, 3 or 4; n is 0, 1 or 2; and q is 0, 1, 2 or 3; provided that a) k is not 0 when the ring B is a 6-membered nitrogen-containing heterocyclic ring containing one or two nitrogen atom(s) and the ring C is a benzene ring, etc.Type: ApplicationFiled: September 25, 2006Publication date: March 11, 2010Inventor: Akira Kugimiya
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Patent number: 7662816Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a ?-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.Type: GrantFiled: August 4, 2004Date of Patent: February 16, 2010Assignee: Schering CorporationInventors: Jared N. Cumming, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voigt, Yusheng Wu, Ying Huang, Yan Xia, Samuel Chackalamannil, Tao Guo, Douglas W. Hobbs, Thuy X. H. Le, Jeffrey F. Lowrie, Kurt W. Saionz, Suresh D. Babu
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Patent number: RE43390Abstract: 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: May 15, 2012Assignees: GlaxoSmithKline LLC, SmithKline Beecham LimitedInventors: Valerie Joan Berry, Steven Dabbs, Colin Henry Frydrych, Eric Hunt, Francis Dominic Sanderson, Gary Woodnutt