Chalcogen Attached Directly To Piperazine Ring Nitrogen By Nonionic Bonding Patents (Class 544/383)
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Patent number: 7671058Abstract: A compound represented by the following formula (I) or a salt thereof: wherein R1, R2, R3 and R4 represent hydrogen atom, a halogen atom, cyano group, nitro group, a C1-4 alkyl group, a halogenated C1-4 alkyl group or a C1-4 alkoxy group, R5 represents a halogen atom, cyano group, a C1-4 alkyl group, a halogenated C1-4 alkyl group or a C1-4 alkoxy group, R6 represents a C5-7 cycloalkyl group, a substituted C5-7 cycloalkyl group, a 5 to 7-membered completely saturated heterocyclic group or a substituted 5 to 7-membered completely saturated heterocyclic group, X represents a single bond, oxygen atom, sulfur atom, NR7, —O—CH2— or —N(R8)—CH2—, R7 represents hydrogen atom or a C1-4 alkyl group, or R7 may combine with a substituent of R6 to represent a single bond, methylene group or ethylene group, R8 represents hydrogen atom, a C1-4 alkyl group or a C7-12 aralkyl group, which is useful as an active ingredient of a medicament for prophylactic and/or therapeutic treatment of diseases caused by an activation ofType: GrantFiled: June 19, 2007Date of Patent: March 2, 2010Assignee: Institute of Medicinal Molecular Design, Inc.Inventors: Ryukou Tokuyama, Toshifumi Wakamatsu, Tatsurou Ichige, Susumu Muto, Akiko Itai
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Publication number: 20100048590Abstract: Disclosed are compounds of the formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.Type: ApplicationFiled: September 2, 2009Publication date: February 25, 2010Inventors: Andrea Gailunas, John A. Tucker, Ruth TenBrink, John Mickelson
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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: 7632838Abstract: This invention relates to inhibiting 11?HSD1.Type: GrantFiled: February 7, 2007Date of Patent: December 15, 2009Assignee: WyethInventors: Jason Shaoyun Xiang, Eddine Saiah, Steve Y. Tam, John C. Mckew, Lihren Chen, Manus Ipek, Huan-Qiu Li, Jianchang Li, Wei Li, Tarek Suhayl Mansour, Vipin Suri, Yuchuan Wu, Zhao-Kui Wan, Jinbo Lee, Eva Binnun, Douglas P. Wilson
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Publication number: 20090306382Abstract: The instant invention relates to cationic alkoxyamines, which are useful as polymerization initiators/regulators in a controlled stable free radical polymerization process to produce intercalated and/or exfoliated nanoparticles from natural or synthetic clays, The invention also relates to improved nanocomposites produced by this process and to the use of these nanocomposite compositions as, for example, coatings, sealants, caulks, adhesives and as plastic additives.Type: ApplicationFiled: August 5, 2009Publication date: December 10, 2009Inventors: ANDREAS Mühlebach, Peter Nesvadba, Andreas Kramer
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Patent number: 7629343Abstract: This invention pertains to certain carbamic acid compounds which inhibit HDAC (histone deacetylase) activity of the following formula: wherein: Cy is independently a cyclyl group; Q1 is independently a covalent bond or cyclyl leader group; the piperazin-1,4-diyl group is optionally substituted; J1 is independently a covalent bond or —C(?; O)—; J2 is independently —C(?O)— or —S(?O)2—; Q2 is independently an acid leader group; wherein: Cy is independently: C3-20carbocyclyl, C3-20heterocyclyl, or C5-20aryl; and is optionally substituted; Q1 is independently: a covalent bond; C1-7alkylene; or C1-7alkylene-X—C1-7alkylene, —X—C1-7alkylene, or C1-7alkylene-X—, wherein X is —O— or —S—; and is optionally substituted; Q2 is independently: C4-8alkylene; and is optionally substituted; and has a backbone length of at least 4 atoms; or: Q2 is independently: C5-20arylene; C5-20arylene-C1-7alkylene; C1-7alkylene-C5-20arylene; or, C1-7alkylene-C5-20arylene-C1-7alkylene; and is optionally substituted; and has a backbone leType: GrantFiled: April 3, 2003Date of Patent: December 8, 2009Assignee: Topotarget UK LimitedInventors: Clare J. Watkins, Maria-Rosario Romero-Martin, James Ritchie, Paul W Finn, Ivars Kalvinsh, Einars Loza, Klara Dikovska, Igor Starchenkov, Daina Lolya, Vija Gailite
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Publication number: 20090286807Abstract: The present invention provides an excellent antihypertensive medicament. The medicament of the present invention comprises a compound having the general formula (I) and the like: [wherein R1: H, substitutable alkyl, substitutable alkenyl, substitutable cyclic hydrocarbon, substitutable heterocyclyl or the like; R2: H, substitutable alkyl, substitutable alkenyl, substitutable cycloalkyl or the like; R3, R4; H, substitutable alkyl, substitutable alkenyl, substitutable cycloalkyl or the like; R5, R6: H, substitutable alkyl, substitutable cycloalkyl, substitutable alkoxy or the like; R7, R8: H, substitutable alkyl, substitutable cycloalkyl or the like; X: the formula (II) or the like; A: substitutable cyclic hydrocarbon, substitutable heterocyclyl or the like; Y: a single bond, substitutable alkylene, substitutable alkenylene, —(CH2)a—X1—(CH2)b—(X1: the formula —NH—, —O— or the like; a, b: 0-5) or the like; B: substitutable cyclic hydrocarbon, substitutable heterocyclyl or the like].Type: ApplicationFiled: June 22, 2007Publication date: November 19, 2009Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Shojiro Miyazaki, Yuji Nakamura, Takahiro Nagayama, Taro Tokui, Yasuyuki Ogawa
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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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Publication number: 20090281318Abstract: The present invention relates to a novel and commercially viable process for substantially optically pure levorotatory and dextrorotatory enantiomers of cetirizine intermediate, 1-[(4-chlorophenyl)phenylmethyl]piperazine, thereby producing substantially optically pure levorotatory and dextrorotatory enantiomers of cetirizine and their pharmaceutical acceptable acid addition salts thereof in high purity and in high yield using novel intermediates.Type: ApplicationFiled: June 15, 2007Publication date: November 12, 2009Applicant: SYMED LABS LIMITEDInventors: Dodda Mohan Rao, Bitra Satyanarayana Rao
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Publication number: 20090275556Abstract: The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein R1, X, Z, R2, X1, Ar, n, R3 and R4 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR8 and accordingly are useful for the treatment of a variety of inflammatory and allergic disorders.Type: ApplicationFiled: August 27, 2008Publication date: November 5, 2009Inventors: Mingshi Dai, Bing Guan, Roert A. Bennett, Douglas F. Burdi, Shomir Ghosh, Gang Li, Charles Minor, Tracy J. Jenkins
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Publication number: 20090264417Abstract: Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.Type: ApplicationFiled: September 4, 2008Publication date: October 22, 2009Applicant: KALYPSYS, INC.Inventors: Stewart A. Noble, Guy Oshiro, James W. Malecha, Cunxiang Zhao, Carmen Robinson, Sergio G. Duron, Michael Sertic, Andrew K. Lindstrom, Andrew K. Shiau, Christopher D. Bayne, Mehmet Kahraman, Boliang Lou, Steven P. Govek
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Publication number: 20090264315Abstract: Monovalent compounds having moieties comprising at least one amino acid side chain are bound to a core molecule, which also comprises a nucleophilic moiety bound to said core molecule. Monovalent compounds also comprise a macrocyclic ring, a nucleophilic moiety, and a spacer group. Monovalent compounds may be combined into bivalent and trivalent compounds, some of which may have a labeling tag. Methods of production of bivalent compounds and contemplated uses thereof are disclosed.Type: ApplicationFiled: July 28, 2008Publication date: October 22, 2009Applicant: TEXAS A&M UNIVERSITY SYSTEMInventor: Kevin Burgess
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Publication number: 20090247499Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequalae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia.Type: ApplicationFiled: August 17, 2007Publication date: October 1, 2009Inventors: Joan M. Fletcher, Tung M. Fong, William K. Hagmann, Petr Vachal
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Publication number: 20090233909Abstract: The present invention is directed to compounds of formula (I) that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them. Wherein R3 is -alkylene-SO2NR5R6.Type: ApplicationFiled: December 1, 2005Publication date: September 17, 2009Applicant: Virobay, Inc.Inventors: Soon H. Woo, Randall W. Vivian, John O. Link
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Publication number: 20090203704Abstract: An object is to provide a novel quinoxaline derivative. Another object is to provide a light-emitting element with low driving voltage. Still another object is to provide a light-emitting element with low power consumption. Yet another object is to provide a light-emitting device and an electronic device each having low power consumption by using such a light-emitting element. A quinoxaline derivative is provided which has a structure in which at least one of carbon at a 2-position and carbon at a 3-position of quinoxaline, and carbon of a pyridine ring are bound via an arylene group.Type: ApplicationFiled: November 25, 2008Publication date: August 13, 2009Inventors: Hiroshi Kadoma, Sachiko Kawakami, Satoko Shitagaki, Satoshi Seo
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Patent number: 7560459Abstract: The present invention is directed to novel compounds of the formula (I) wherein X, R1, R2, R3, R4, R5 and R6 are as described in the specification, processes for the preparation of and pharmaceutical compositions comprising said derivatives. The compounds of the present invention are useful for the treatment of epilepsy. The invention is further directed to a process for the preparation of compounds of formula (XX), wherein X, R3, R4, R5 and R6 are as described in the specification.Type: GrantFiled: November 2, 2005Date of Patent: July 14, 2009Assignee: Janssen Pharmaceutica, N.V.Inventors: Ahmed Abdel-Magid, Cynthia Maryanoff, Steven Mehrman, Allen B. Reitz, Bruce Maryanoff
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Publication number: 20090175793Abstract: A composition comprising a selective oxytocin antagonist for use in the treatment and/or prevention of a male ejaculatory disorder; which selective oxytocin antagonist is optionally admixed with a pharmaceutically acceptable carrier, diluent or excipient.Type: ApplicationFiled: December 19, 2008Publication date: July 9, 2009Inventors: Alasdair Mark Naylor, Rachel Jane Russell, Stephen Derek Albert Street, Kim-Wah Tang, Pieter Hadewijn Van Der Graaf, Christopher Peter Wayman
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Publication number: 20090176773Abstract: The invention relates to non-peptidic molecules which modulate, especially inhibit, the interaction of protein kinase A (PKA) and A kinase anchor proteins (AKAP) and to a host or target organism that comprises said non-peptidic compounds or recognition molecules directed to said compounds, such as e.g. antibodies or chelating agents. The invention also relates to a pharmaceutical agent, especially for use in the treatment of diseases that are associated with a disturbance of the cAMP signal path, especially insipid diabetes, hypertonia, pancreatic diabetes, duodenal ulcer, asthma, heart failure, obesity, AIDS, edema, hepatic cirrhosis, schizophrenia and others. The invention also relates to the use of the inventive molecules.Type: ApplicationFiled: May 18, 2006Publication date: July 9, 2009Applicant: FORSCHUNGSVERBUND BERLIN E.V.Inventors: Enno Klussmann, Walter Rosenthal, Jorg Rademann, Frank Christian, Sina Meyer
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Publication number: 20090170871Abstract: 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: June 22, 2007Publication date: July 2, 2009Applicant: SMITHKLINE BEECHAM CORPORATIONInventors: Jakob Busch-Petersen, Christopher S. Brook, Richard M. Goodman, Edward C. Webb
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Publication number: 20090156614Abstract: This invention provides new compounds and uses thereof in treating a variety of diseases or conditions in a subject, including, inter alia, prostate cancer, muscle wasting diseases and/or disorders or a bone-related diseases and/or disorders.Type: ApplicationFiled: July 19, 2007Publication date: June 18, 2009Inventors: James T. Dalton, Duane D. Miller, Igor Rakov, Casey Bohl, Michael L. Mohler
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Publication number: 20090149448Abstract: The invention relates to substituted phenoxyacetic acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.Type: ApplicationFiled: November 22, 2005Publication date: June 11, 2009Applicant: ASTRAZENECA ABInventors: Lilian Alcaraz, Roger Victor Bonnert, Anthony Ronald Cook, Timothy Jon Luker, Rukhsana Tasneem Mohammed, Stephen Thom
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Publication number: 20090143396Abstract: Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.Type: ApplicationFiled: October 11, 2006Publication date: June 4, 2009Inventors: James W. Malecha, Andrew K. Lindstrom, Sergio G. Duron, David J. Thomas
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Publication number: 20090137396Abstract: The present invention relates to the use of piperazine compounds of the formula I or of the agriculturally useful salts of piperazine compounds of the formula I as herbicides, where in formula I the variables are as defined in the claims and the description. Moreover, the invention relates to compositions comprising, in addition to auxiliaries customary for formulating crop protection agents, piperazine compounds of the formula I or agriculturally useful salts of I, and to a process for preparing these compositions. Furthermore, the invention relates to certain piperazine compounds of the formula I, a process for preparing piperazine compounds of the formula I and a method for controlling unwanted vegetation which comprises treating plants, their seeds and/or their habitat with at least one piperazine compound of the formula I.Type: ApplicationFiled: January 4, 2007Publication date: May 28, 2009Applicant: BASF SEInventors: Eike Hupe, Cyrill Zagar, Matthias Witschel, Toralf Kuehn, William Karl Moberg, Liliana Parra Rapado, Frank Stelzer, Andrea Vescovi, Robert Reinhard, Bernd Sievernich, Klaus Grossmann, Thomas Ehrhardt
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Patent number: 7531535Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: GrantFiled: December 13, 2007Date of Patent: May 12, 2009Assignee: Bristol-Meyers Squibb CompanyInventors: Donald J. P. Pinto, Jennifer X. Qiao
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Patent number: 7524848Abstract: Diaza heterocyclic amide derivatives according to Formula (I) have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: where R5, R6, R7, R8, R9, R10, m, Q, X, and Y are set forth in the description.Type: GrantFiled: March 22, 2007Date of Patent: April 28, 2009Assignee: Amgen Inc.Inventors: Jay P. Powers, Daqing Sun, Xuelei Yan
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Patent number: 7517884Abstract: Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.Type: GrantFiled: May 16, 2006Date of Patent: April 14, 2009Assignee: Kalypsys Inc.Inventors: James W. Malecha, Sergio G. Duron, Andrew K. Lindstrom
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Publication number: 20090093492Abstract: This invention relates to novel compounds of Formula (I) to (VII), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: ApplicationFiled: October 9, 2007Publication date: April 9, 2009Inventors: Jakob Busch-Petersen, Michael R. Palovich, Katherine L. Widdowson
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Patent number: 7514430Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: July 28, 2005Date of Patent: April 7, 2009Assignee: Bristol-Myers Squibb Pharma CompanyInventor: George V. DeLucca
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Publication number: 20090069344Abstract: The present invention is directed to compounds of formula (I): where X, Y, R1, R2 and R3 are defined therein, which can act as modulators of viral replication and/or virus production, especially of the hepatitis C virus (HCV).Type: ApplicationFiled: September 29, 2005Publication date: March 12, 2009Inventors: Immacolata Conte, Caterina Ercolani, Claudio Giuliano, Giovanni Migliaccio, Ian Stansfield, Gessica Filocamo, Veronica Suriano
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Publication number: 20090069302Abstract: The present invention relates generally to novel therapeutic compounds and AXOR 109 agonists, and processes for the manufacture and use of the same.Type: ApplicationFiled: January 19, 2007Publication date: March 12, 2009Applicant: SMITHKLINE BEECHAM CORPORATIONInventors: Jerzy Ryszard Szewczyk, Christopher P. Laudeman, Thomas Dock, Zibin Chen, Anderson Evans, Yue H. Li
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Publication number: 20090069304Abstract: Since it is thought that if the activity of MMP-13 can be inhibited, this will largely contribute to improvement or prevention of progession of pathological states, particularly, osteoarthritis (OA), resulting from or associated with the MMP-13 activity, the development of MMP-13 inhibitors is anticipated. There are provided a compound represented by the general formula (I): wherein R1 is optionally substituted aryl etc.; Z is C1-C5 alkylene which may be substituted and may be interrupted with a substituent selected from Substituent group a etc.; A is the formula: (R6 and R7 are each independently halogen, lower alkyl etc.; m and n are each independently 0, 1, or 2); R2 is a hydrogen atom, optionally substituted lower alkyl etc.; R3 is a hydrogen atom, optionally substituted lower alkyl etc.; R4 is a hydrogen atom; or R3 and R4 may be taken together with an adjacent carbon atom to from a ring; R5 is hydroxy, lower alkyloxy etc.Type: ApplicationFiled: March 1, 2007Publication date: March 12, 2009Applicant: SHIONOGI & CO., LTD.Inventors: Mikayo Hayashi, Fumihiko Watanabe
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Publication number: 20090054460Abstract: Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: ApplicationFiled: January 11, 2008Publication date: February 26, 2009Inventors: Jian J. Chen, Ben C. Askew, Kaustav Biswas, Jennifer N. Chau, Derin C. D'Amico, Scott Harried, Thomas Nguyen, Wenyuan Qian, Jiawang Zhu, Christopher H. Fotsch, Aiwen Li, Qingyian Liu, Nobuku Nishimura, Tanya Peterkin, Babak Riahi, Chester Chenguang Yuan, Nianhe Han, Rana Nomak, Kevin Yang
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Patent number: 7494999Abstract: Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.Type: GrantFiled: October 25, 2005Date of Patent: February 24, 2009Assignee: Kalypsys, IncInventors: Stewart A. Noble, Guy Oshiro, James W. Malecha, Cunxiang Zhao, Carmen Robinson, Sergio G. Duron, Michael Sertic, Andrew K. Lindstrom, Andrew K. Shiau, Christopher D. Bayne, Mehmet Kahraman, Boliang Lou, Steven P. Govek
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Publication number: 20090042899Abstract: Piperazinyl- or piperidinylamine-sulfamic acid amides and their use for the manufacture of a medicament in diseases mediated by the action of steroid sulfatase.Type: ApplicationFiled: September 16, 2008Publication date: February 12, 2009Inventor: Philipp Lehr
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Patent number: 7485646Abstract: A serotonin 5-HT3 receptor agonist containing a compound represented by the general formula (1) [R1, R3 and R5 represent hydrogen atom, a lower alkyl group, a lower alkenyl group, a halogen atom, hydroxyl group, amino group, a lower alkoxy group, carboxyl group, carbamoyl group, or nitro group, R2 and R4 represent a halogen atom, hydroxyl group, or amino group, R6 represents hydrogen atom, a lower alkyl group, or a lower alkenyl group, R7 represents hydrogen atom, a lower alkyl group, a lower alkenyl group, or an aralkyl group, and m and n are integers of 1 to 3] or a physiologically acceptable salt thereof as an active ingredient and having both a serotonin 5-HT3 receptor antagonistic action and a serotonin 5-HT3 receptor activating action.Type: GrantFiled: September 8, 2005Date of Patent: February 3, 2009Assignee: Research Foundation Itsuu LaboratoryInventors: Tamaki Jikyo, Koichi Shudo
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Patent number: 7485644Abstract: The invention provides compounds of formula (I): or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein ring B represents a monocyclic aryl ring having six ring atoms or a monocyclic heteroaryl ring having up to six ring atoms and containing one or more ring heteroatoms wherein each said heteroatom is nitrogen; R2 represents a group selected from C1-6 alkyl or aryl, which said group is substituted by one or more fluorine groups; n is 1, 2 or 3; and R1 represents an optionally substituted group selected from C1-6 alkyl, C5-7 cycloalkyl, heterocycloalkyl, aryl, heteroaryl, C1-6 alkyl-aryl, C1-6 alkyl-heteroaryl, C1-6 alkyl-cycloalkyl or C1-6 alkyl-heterocycloalkyl. Processes for their preparation; pharmaceutical compositions containing them; and their use in the treatment of a disease condition mediated by one or more metalloproteinase enzymes.Type: GrantFiled: June 23, 2004Date of Patent: February 3, 2009Assignee: AstraZeneca ABInventors: Maurice Raymond Verschoyle Finlay, David Waterson
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Publication number: 20090029971Abstract: Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.Type: ApplicationFiled: September 4, 2008Publication date: January 29, 2009Applicant: KALYPSYS, INC.Inventors: Stewart A. Noble, Guy Oshiro, James W. Malecha, Cunxiang Zhao, Carmen Robinson, Sergio G. Duron, Michael Sertic, Andrew K. Lindstrom, Andrew K. Shiau, Christopher D. Bayne, Mehmet Kahraman, Boliang Lou, Steve P. Govek
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Publication number: 20080312231Abstract: Substituted sulfonamide compounds corresponding to formula I pharmaceutical compositions comprising them, a process for preparing them, and the use of such compounds to treat or inhibit pain and other disorders or disease states.Type: ApplicationFiled: April 30, 2008Publication date: December 18, 2008Applicant: Gruenenthal GmbHInventors: Beatrix MERLA, Stefan Oberboersch, Melanie Reich, Bernd Sundermann, Werner Englberger, Timo Struenker, Ruth Jostock, Sabine Hees, Edward Bijsterveld, Fritz Theil, Heinz Graubaum
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Publication number: 20080312216Abstract: The present invention relates to a compound of formula I wherein R1, R2, R3, R4, R9, R10, m and n are as defined herein, or to a pharmaceutically acceptable acid addition salt thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, bipolar disorders, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: ApplicationFiled: June 3, 2008Publication date: December 18, 2008Inventors: Henner Knust, Matthias Nettekoven, Hasane Ratni, Xihan Wu
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Publication number: 20080275027Abstract: The invention relates to compounds of formula (I) or salts and solvates thereof, processes for their preparation, to compositions containing them and to their use in the treatment of various disorders, such as allergic rhinitis: wherein R1 and R2 are as defined in the specification.Type: ApplicationFiled: July 17, 2006Publication date: November 6, 2008Inventors: Rachael Ann Ancliff, Mark James Bamford, Simon Teanby Hodgson, Christopher Allan Parr, Panayiotic Alexandrou Procopiou, David Matthew Wilson, Michael Woodrow
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Patent number: 7446210Abstract: The present invention is directed to novel compounds of Formula I: and forms and pharmaceutical compositions thereof, and the use thereof as inhibitors of Factor Xa.Type: GrantFiled: October 24, 2005Date of Patent: November 4, 2008Assignee: Janssen Pharmaceutica N.V.Inventors: Tianbao Lu, Tho V. Thieu, Yu-Kai Lee, Daniel J. Parks, Thomas P. Markotan, Wenxi Pan, Karen L. Milkiewicz, Mark R. Player
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Patent number: 7439362Abstract: Piperazinyl- or piperidinylamine-sulfamic acid amides and their use for the manufacture of a medicament in diseases mediated by the action of steriod sulfatase.Type: GrantFiled: March 27, 2003Date of Patent: October 21, 2008Assignee: Novartis AGInventor: Philipp Lehr
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Publication number: 20080242666Abstract: The present invention relates to Compound S of Formula (I).Type: ApplicationFiled: December 22, 2005Publication date: October 2, 2008Inventors: Colin Andrew Leach, John Liddle, Simon Peace, Joanne Philp, Ian Edward David Smith, Lamont Roscoe Terrell, Jing Zhang
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Publication number: 20080207620Abstract: The present application provides for a compound of Formula IV, or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods and include the administration of such compounds with at least one additional therapeutic agent.Type: ApplicationFiled: February 22, 2008Publication date: August 28, 2008Inventors: Manoj C. Desai, Allen Y. Hong, Hon C. Hui, Hongtao Liu, Randall W. Vivian, Lianhong Xu
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Publication number: 20080194520Abstract: The present invention is related to 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: December 19, 2005Publication date: August 14, 2008Inventors: Dominique Swinnen, Agnes Bombrun, Patrick Gerber, Catherine Jorand-Lebrun
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Publication number: 20080188659Abstract: This invention relates to methods for preparing halogenated amines.Type: ApplicationFiled: February 7, 2008Publication date: August 7, 2008Applicant: WyethInventors: Eddine Saiah, Huan-Qiu Li, Adrian Huang
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Publication number: 20080139564Abstract: Certain substituted phenyl propyl amine compounds are histamine H3 receptor and/or serotonin transporter modulators useful in the treatment of histamine H3 receptor- and/or serotonin-mediated diseases.Type: ApplicationFiled: November 14, 2007Publication date: June 12, 2008Inventors: John M. Keith, Jennifer M.B. Miller, Emily M. Stocking
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Patent number: 7371747Abstract: The present invention is directed to novel cyanoalkylamino derivatives that are inhibitors of cysteine protease such as cathepsins K, S, B and L, in particular cathepsin K Pharmaceutical composition comprising these compounds, method of treating diseases mediated by unregulated cysteine protease activity, in particular cathepsin K utilizing these compounds and methods of preparing these compounds are also disclosed.Type: GrantFiled: November 13, 2002Date of Patent: May 13, 2008Assignee: Merck Frosst Canada & Co.Inventors: Cameron Black, Sheldon N. Crane, Dana Davis, Eduardo L. Setti
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Patent number: 7365075Abstract: The present invention provides Aryl Sulfonamide Compounds having the formula: and prodrugs or pharmaceutically acceptable salts or prodrugs thereof. The Aryl Sulfonamide Compounds are useful for treating diabetes, obesity, and other diseases and disorders.Type: GrantFiled: December 20, 2004Date of Patent: April 29, 2008Assignee: Amgen Inc.Inventors: Michael R. DeGraffenreid, Xiao He, Jay P. Powers, Daqing Sun, Xuelei Yan
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Publication number: 20070270434Abstract: The present invention relates to compounds and methods useful as inhibitors of PPAR, particularly PPAR?, and for the treatment or prevention of PPAR-mediated diseases, including metabolic diseases.Type: ApplicationFiled: May 16, 2007Publication date: November 22, 2007Applicant: KALYPSYS, INC.Inventors: James W. Malecha, Stewart A. Noble, Sergio G. Duron, Andrew Lindstrom, Andrew Shiau, Steven Govek