Chalcogen Attached Indirectly To The Diazine Ring By Nonionic Bonding Patents (Class 544/335)
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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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Patent number: 7754888Abstract: N-Substituted (heteroaryl)alkyl sulfilimines are effective at controlling insects.Type: GrantFiled: February 9, 2007Date of Patent: July 13, 2010Assignee: Dow AgroSciences LLCInventors: Michael R. Loso, Benjamin M. Nugent, Yuanming Zhu, Richard B. Rogers, Jim X. Huang, James M. Renga, Zoltan L. Benko, Gregory T. Whiteker, John F. Daeuble
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Patent number: 7745445Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the Peroxisome Proliferator-Activated Receptor (PPAR) families, particularly the activity of PPAR?.Type: GrantFiled: May 13, 2005Date of Patent: June 29, 2010Assignee: IRM LLCInventors: Robert Epple, Mihai Azimioara
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Patent number: 7732441Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity. Such compounds are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.Type: GrantFiled: February 7, 2008Date of Patent: June 8, 2010Assignee: Theravance, Inc.Inventors: Mathai Mammen, Adam Hughes
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Publication number: 20100137323Abstract: The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: where the definitions of the variables Q, L1, , L2,M, X, L3, and A are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.Type: ApplicationFiled: January 29, 2010Publication date: June 3, 2010Applicant: Amgen Inc.Inventors: Sean P. Brown, Paul Dransfield, Jonathan B. Houze, Jinqian Liu, Jiwen Liu, Zhihua Ma, Julio C. Medina, Vatee Pattaropong, Michael J. Schmitt, Rajiv Sharma, Yingcai Wang
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Publication number: 20100137336Abstract: The present invention relates to novel compounds of Formula (I), wherein X1, X2, X3, X4, Am and Bn are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: ApplicationFiled: July 10, 2008Publication date: June 3, 2010Inventor: Christelle Boléa
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Patent number: 7728135Abstract: The present invention is directed to the synthesis of 4-[4-[(R)-[1-[cyclopropylsulfonyl)-4-piperidinyl](3-fluorophenyl)methyl]-3(S)-methyl-1-piperazinyl]-1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]-4-methylpiperidine], and intermediates therefor from readily available starting materials by a novel route.Type: GrantFiled: January 5, 2006Date of Patent: June 1, 2010Assignee: Schering CorporationInventors: Xiongwei Shi, Man Zhu, William Leong, Vilas Dahanukar, Ilia A. Zavialov, Cecelia Proietti, Shannon Zhao, Hong-Chang Lee, Yi Liu, Hoa N. Nguyen, Wenxue Wu, Bosco D'Sa, Feng Liang, Loc Thanh Tran
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Publication number: 20100127213Abstract: The present invention relates to dielectrically positive liquid-crystalline media comprising a dielectrically positive component, component A, comprising a dielectrically positive compound of the formula I in which the parameters have the meaning indicated in the specification, and optionally a second dielectrically positive component, component B, comprising one or more dielectrically positive compounds having a dielectric anisotropy of great than 3, and optionally a dielectrically neutral component, component C, and to liquid-crystal displays containing these media, especially active-matrix displays and in particular TN, IPS and FFS displays.Type: ApplicationFiled: April 1, 2008Publication date: May 27, 2010Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Markus Czanta, Andreas Taugerbeck, Renate Bender, Lars Lietzau
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Publication number: 20100130743Abstract: Novel benzenedicarboxamides of the formula (I) wherein X represents hydrogen, halogen atom, nitro, C1-6alkylsulfonyloxy, C1-6alkylsulfinyl, C1-6alkylsulfenyl or C1-6alkylsulfonyl, R1 represents C1-6alkyl, C1-6alkylthio-C1-6alkyl, C1-6alkylsulfinyl-C1-6alkyl or C1-6 alkylsulfonyl-C1-6alkyl, Y represents halogen or C1-6alkyl, m represents 0 or 1, A represents O, S, SO, SO2, CH2 or CH(CH3), and Q represents a 5- or 6-membered heterocyclic group that contains at least one hetero atom selected from the group consisting of N, O and S and can be optionally substituted; processes for their preparation, their intermediates and their use as insecticides.Type: ApplicationFiled: January 27, 2010Publication date: May 27, 2010Applicant: BAYER CROPSCIENCE AGInventors: Katsuaki Wada, Takuya Gombuchi, Yasushi Yoneta, Yuichi Otsu, Katsuhiko Shibuya, Norihiko Nakakura, Rüdiger Fischer, Tetsuya Murata, Eiichi Shimojo
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Publication number: 20100121061Abstract: The present invention generally relates to nicotinic compounds, in the form of aryl substituted olefinic compounds, as well as pro-drug, N-oxide, metabolite and pharmaceutically acceptable salt forms thereof. Methods of modulating neurotransmitter release via administration of the compounds, pro-drugs, N-oxides and/or pharmaceutically acceptable salts are also disclosed.Type: ApplicationFiled: December 8, 2009Publication date: May 13, 2010Applicant: Targacept, Inc.Inventors: William S. Caldwell, Gary M. Dull, Balwinder S. Bhatti, Srishailkumar B. Hadimani, Haeil Park, Jared M. Wagner, Peter A. Crooks, Patrick M. Lippiello, Merouane Bencherif
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Publication number: 20100120714Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein W is O or S; V is a direct bond or NR3; Q is or CR6aR6b, O, NR7, C?N—O—R7 or C(?O); Y is —C(R5)?N—O—(CR8aR8b)p—X—(CR9aR9b)q—SiR10aR10bR10c; or a phenyl ring substituted as defined in the disclosure; or Z; and R1, R2, R3, R4, R5, R6a, R7, R8a, R8b, R9b, R10a, R10b, R10c, Z, p and q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.Type: ApplicationFiled: April 4, 2008Publication date: May 13, 2010Applicant: E.I. DU PONT DE NEMOURS AND COMPANYInventors: Bruce Lawrence Finkelstein, Andrew Edmund Taggi, Jefrey Keith Long, Paula Louise Sharpe, Chi-ping Tseng, Stephen Frederick Mccann, Amy X. Ding, Steven Lewis Swann, JR.
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Publication number: 20100113477Abstract: The present invention provides aryl- or heteroaryl-diketo acid compounds effective to inhibit an activity of a Mycobacterial malate synthase enzyme or to inhibit a malate synthase activity in other bacteria having the enzyme. The compounds may be phenyl-naphthyl-, or thienyl-substituted diketo acids and carboxylate derivatives thereof. Also provided are methods of treating tuberculosis or other pathophysiological conditions associated with a malate synthase enzyme with the inhibitory compounds and methods of in silico design of the inhibitory compounds. In addition, the present invention provides the inhibitory compounds designed by this method. Furthermore, three-dimensional X-ray crystal structures of the Mycobacterial malate synthase complexed with the inhibitory compounds are provided. Further still a method for stabilizing an aromatic or heteroaromatic diketo acid or its prodrug or close analog in solution by derivatizing at least the ortho position on the aromatic ring is provided.Type: ApplicationFiled: October 20, 2009Publication date: May 6, 2010Inventors: Joel S. Freundlich, James C. Sacchettini, Inna V. Kriger, Thomas R. Ioerger, Vijay Gawandi
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Patent number: 7709490Abstract: This invention relates to a compound of formula I, wherein R1, R2, m, n and X are as defined herein, or a physiologically tolerated salt thereof, its pharmaceutical composition and use for lowering blood glucose, treating diabetes, or increasing insulin release.Type: GrantFiled: November 10, 2008Date of Patent: May 4, 2010Assignee: Sanofi-AventisInventors: Elisabeth Defossa, Jochen Goerlitzer, Thomas Klabunde, Viktoria Dietrich, Siegfried Stengelin, Guido Haschke, Andreas Herling, Stefan Bartoschek
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Publication number: 20100099673Abstract: The present invention relates to compounds represented by Formula (I): and pharmaceutically acceptable salts thereof. The present invention also provides pharmaceutical compositions comprising the instant compounds. This invention further provides methods to treat and prevent pain, respiratory and non-respiratory diseases.Type: ApplicationFiled: January 11, 2008Publication date: April 22, 2010Inventors: Mark T. Bilodeau, Nathan R. Kett, Craig Lindsley, Peter J. Manley, Jeffrey Y. Melamed, Daniel Vincent Paone, B. Wesley Trotter, Zhicai Wu
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Patent number: 7700602Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment, prevention or amelioration of a disease or disorder characterized by elevated ?-amyloid deposits or ?-amyloid levels in a patient.Type: GrantFiled: December 10, 2008Date of Patent: April 20, 2010Assignee: Wyeth LLCInventors: Michael S. Malamas, James J. Erdei, Iwan S. Gunawan, Ping Zhou, Yinfa Yan, Dominic A. Quagliato
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Patent number: 7700584Abstract: The present invention provides curcumol derivatives of the following formula (I) or pharmaceutical acceptable salts thereof: wherein, Y is selected from the group consisting of ?CHR2, —CH2R2, ?O, ?—OH or —OR1;R1 is selected from H, R, RCO or HO3S; and R is selected from the group consisting of H; saturated or unsaturated linear C1-10 hydrocarbon group and the like; R2 is selected from the group consisting of F; Cl; Br; I; H; —OH; —OR; —HSO3 and the like; with the proviso that both R1 and R2 are not H. The present invention also provides anti-tumor or antiviral pharmaceutical compositions comprising said derivatives or pharmaceutical acceptable salts thereof. The present invention further provides the use of said derivatives or pharmaceutical acceptable salts thereof in the preparation of a medicament for prophylaxis and/or treatment tumor or an antiviral medicament.Type: GrantFiled: May 26, 2005Date of Patent: April 20, 2010Assignee: Hangzhou Minsheng Pharmaceuticals Co., Ltd.Inventors: Shulong Wang, Dianwu Guo, Zhaoke Meng
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Publication number: 20100086955Abstract: Ghrelin O-acyltransferase (GOAT) is inhibited with designed small molecules. Methods comprise contacting the GOAT with an inhibitor and detecting a resultant inhibition.Type: ApplicationFiled: October 1, 2009Publication date: April 8, 2010Inventors: Patrcik G. Harran, Michael S. Brown, Joseph L. Goldstein, Jing Yang, Tong-Jin Zhao
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Publication number: 20100087448Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt or hydrate thereof, to a process for preparing the compound of formula (I), and to use of the compound of formula (I) or a pharmaceutically acceptable salt or hydrate thereof as a medicament, in particular as a medicament for the treatment and prevention of type B hepatitis.Type: ApplicationFiled: July 9, 2007Publication date: April 8, 2010Inventors: Song Li, Guoming Zhao, Guangqiang Xia, Lili Wang, Zhibing Zheng, Yunde Xie, Wu Zhong, Junhai Xiao, Xingzhou Li, Hao Cui
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Publication number: 20100081665Abstract: The present invention provides tricyclic compounds, arylamide compounds, and other compounds, and compositions comprising the same, for treating malaria, and methods of treating malaria comprising administering such compounds to an animal.Type: ApplicationFiled: July 28, 2009Publication date: April 1, 2010Inventors: Richard W. Scott, Doron Greenbaum, Dahui Liu, Xiaodong Fan, Yongjiang Xu, Haizhong Tang, Ehab Khalil
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Patent number: 7687508Abstract: This invention relates generally to modulators of chemokine receptor activity having unexpected combination of desirable pharmacological properties. Pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and prevention of inflammatory, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases, particularly diabetes, Crohn's disease, atherosclerosis, and multiple sclerosis, along with methods of preparing compounds and intermediates therefor. Metabolites of active compounds are also provided herein, pharmaceutical compositions and use thereof are also provided.Type: GrantFiled: July 25, 2007Date of Patent: March 30, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Percy H. Carter, Robert J. Cherney, John Hynes, Soo S. Ko, Anurag S. Srivastava, Zili Xiao, Michael G. Yang
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Publication number: 20100075990Abstract: Multiheteroaryl compounds, their preparation, pharmaceutical compositions comprising these compounds, and their pharmaceutical use in the prevention and treatment of prostaglandin D2 mediated diseases and conditions that may be modulated by the inhibition of hematopoietic prostaglandin D synthase (H-PGDS).Type: ApplicationFiled: September 22, 2009Publication date: March 25, 2010Applicant: CAYMAN CHEMICAL COMPANYInventors: Gregory W. Endres, Pil Heui Lee, Kirk Lang Olson, James Bernard Kramer, Fred Lawrence Ciske, Stephen Douglas Barrett
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Publication number: 20100069243Abstract: The present invention relates to novel pyrimidylmethyl-sulfonamide compounds and to their N-oxides, their agriculturally acceptable salts and their veterinarily acceptable salts and also to agricultural compositions comprising at least one such compound as active component, and also to their use for controlling harmful fungi. The present invention also relates to a method for controlling arthropod pests.Type: ApplicationFiled: November 21, 2007Publication date: March 18, 2010Applicant: BASF SEInventors: Jan Klaas Lohmann, Wassilios Grammenos, Michael Puhl, Jochen Dietz, Bernd Müller, Joachim Rheinheimer, Jens Renner, Marianna Vrettou, Sarah Ulmschneider, Thomas Grote
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Publication number: 20100069405Abstract: The present invention is directed to compounds and compositions for the treatment of neurological diseases that cause neurogenic and neuropathic pain, inflammatory diseases, renal ischaemia, cardiovascular disease and other pathologies caused by the presence of endogenous cannabinoids and or other substrates resulting from the metabolic activities of fatty acid amido hydrolase (FAAH). These compounds are represented by the formula (I): wherein A, n, R1, R7 and R8 are as defined herein.Type: ApplicationFiled: November 24, 2009Publication date: March 18, 2010Applicant: SANOFI-AVENTISInventors: Ahmed Abouabdellah, Regine Bartsch-Li, Christian Hoornaert, Antoine Ravet
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Publication number: 20100063044Abstract: The present invention relates to aniline derivatives of formula I: wherein R1, R2, R3, R4, Z and q are as defined herein; or salts thereof and their use.Type: ApplicationFiled: August 17, 2009Publication date: March 11, 2010Applicant: H. Lundbeck A/SInventors: Christian Wenzel Tornoe, Mario Rottlãnder, Daniel Rodriguez Greve, Nikolay Khanzhin, Andreas Ritzén, William Patrick Watson
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Publication number: 20100048900Abstract: The invention relates to an agent which contains ectoines for the prophylactic or therapeutic treatment of endothelial function disturbances, in particular the VLS.Type: ApplicationFiled: December 3, 2007Publication date: February 25, 2010Inventors: Thomas Schwarz, Georg Lentzen
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Publication number: 20100041635Abstract: The invention provides compounds that inhibit PIM kinases and Flt3 kinase, and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation.Type: ApplicationFiled: June 30, 2009Publication date: February 18, 2010Inventors: Mustapha HADDACH, Johnny Yasuo NAGASAWA
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Publication number: 20100029689Abstract: PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formula I: wherein R1, R2, R3, and R4 are as defined herein.Type: ApplicationFiled: July 2, 2009Publication date: February 4, 2010Applicants: MEMORY PHARMACEUTICALS CORPORATION, ROCHE PALO ALTO LLCInventors: Allen T. HOPPER, Joan Marie CAROON, Elbert CHIN, Robert F. DUNN, Sharada Shenvi LABADIE, Jim LI, Richard Allen SCHUMACHER, Francisco Xavier TALAMAS
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Patent number: 7655649Abstract: The present invention is directed to compounds which contain substituted pyridazines and pyrimidines moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.Type: GrantFiled: April 5, 2005Date of Patent: February 2, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Mark T. Bilodeau, Peter C. Chua, Nicholas D. P. Cosford, Jacob M. Hoffman, Johnny Yasuo Nagasawa
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Patent number: 7652142Abstract: In its many embodiments, the present invention provides a novel class of bipiperidinyl compounds as inhibitors of the CCR5 receptors, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with CCR5 using such compounds or pharmaceutical compositions. The invention also relates to the use of a combination of a compound of this invention and one or more antiviral or other agents useful in the treatment of Human Immunodeficiency Virus (HIV). The invention further relates to the use of a compound of this invention, alone or in combination with another agent, in the treatment of solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis.Type: GrantFiled: November 1, 2004Date of Patent: January 26, 2010Assignee: Schering CorporationInventors: Michael W. Miller, Jack D. Scott
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Patent number: 7645757Abstract: The present invention is directed to compounds and compositions for the treatment of neurological diseases that cause neurogenic and neuropathic pain, inflammatory diseases, renal ishaemia, cardiovascular disease and other pathologies caused by the presence of endogenous cannabinoids and or other substrates resulting from the metabolic activities of fatty acid amido hydrolase (FAAH). These compounds are represented by the formula alkylene group; a salt thereof, or a hydrate or a solvate of said compound or said salt; where the variables are as defined in the attached specification.Type: GrantFiled: August 14, 2006Date of Patent: January 12, 2010Assignee: sanofi-aventisInventors: Ahmed Abouabdellah, Regine Bartsch-Li, Christian Hoornaert, Antoine Ravet
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Publication number: 20100004268Abstract: The present invention relates to an optically pure compound of formula (I) or a pharmaceutically acceptable salt or hydrate thereof, a process for preparing the optically pure compound of formula (I), and use of the optically pure compound of formula (I) or a pharmaceutically acceptable salt or hydrate thereof as a medicament, in particular as a medicament for the treatment and prevention of type B hepatitis.Type: ApplicationFiled: July 9, 2007Publication date: January 7, 2010Inventors: Song Li, Guangqiang Xia, Guoming Zhao, Lili Wang, Zhibing Zheng, Yunde Xie, Wu Zhong, Junhai Xiao, Xingzhou Li, Hao Cui
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Publication number: 20090312328Abstract: [Object] A compound that can be used as an agent for treating a disease associated with an EP1 receptor, in particular, a lower urinary tract symptom. [Means for Solution] It was confirmed that a sulfonamide compound having an amide structure and characterized by a chemical structure in which a carbon atom in the amide bonds to the N atom in sulfonamide through lower alkylene, or a salt thereof, has a potent EP1 receptor antagonistic activity, accomplishing the present invention. Since the sulfonamide compound of the present invention or a pharmaceutically acceptable salt thereof has a potent EP1 receptor antagonistic activity, it is useful as an agent for treating a disease associated with an EP1 receptor, in particular, a lower urinary tract symptom.Type: ApplicationFiled: August 9, 2007Publication date: December 17, 2009Applicant: Astellas Pharma Inc.Inventors: Hideki Kubota, Susumu Toda, Issei Tsukamoto, Yuta Fukuda, Ryutaro Wakayama, Kazuki Ono, Toru Watanabe, Hidenori Azami
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Publication number: 20090306047Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.Type: ApplicationFiled: June 8, 2009Publication date: December 10, 2009Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert Mazzola, John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X.H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter
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Patent number: 7629348Abstract: What is described are compounds of the formulae (I) and (II) where the symbols and indices have the meanings given in the description. These compounds are suitable for controlling animal pests.Type: GrantFiled: May 31, 2007Date of Patent: December 8, 2009Assignee: Merial LimitedInventors: Marion Beckmann, Oswald Ort, Uwe Döller, Gerhard Krautstrunk, Wolfgang Schaper, Peter Lümmen, Daniela Jans, Waltraud Hempel, Jutta Maria Waibel, Barbara Lörkens
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Publication number: 20090286261Abstract: An exemplary embodiment may be directed to a fluorescence polarization assay that screens compounds or agents for their affinity to hematopoietic prostaglandin D synthase (H-PGDS) based on their ability to displace a fluorophore-containing detection analyte bound to an enzyme comprising the primary amino acid sequence of H-PGDS. Another exemplary embodiment utilizes an enzyme having a maltose binding protein amino-acid sequence fused with an N-terminus of the enzyme.Type: ApplicationFiled: May 13, 2009Publication date: November 19, 2009Applicant: CAYMAN CHEMICAL COMPANYInventors: Kirk W. Maxey, Jeffrey K. Johnson, Karie L. McGowan, Nisha Palackal, Gregory W. Endres
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Publication number: 20090286792Abstract: The present invention relates to 3-cycloalkylaminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, X, Y and Z are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as modulators of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.Type: ApplicationFiled: November 19, 2008Publication date: November 19, 2009Inventors: Chu-Biao Xue, Brian W. Metcalf, Amy Qi Han, Darius J. Robinson, Changsheng Zheng, Anlai Wang, Yingxin Zhang
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Publication number: 20090281125Abstract: The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein the substituents are as defined herein, compositions containing such compounds and the uses of such compounds for the treatment of various diseases and conditions such as asthma.Type: ApplicationFiled: July 9, 2009Publication date: November 12, 2009Inventors: Tanisha D. Blake, Bruce C. Hamper, Wei Huang, James R. Kiefer, JR., Joseph B. Moon, Bradley E. Neal, Kirk L. Olson, Matthew J. Pelc, Barbara A. Schweitzer, Atli Thorarensen, John I. Trujillo, Steven R. Turner
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Publication number: 20090275598Abstract: The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: where the definitions of the variables Q, L1, L2, M, X, L3, and A are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.Type: ApplicationFiled: July 10, 2009Publication date: November 5, 2009Applicant: Amgen Inc.Inventors: Michelle Akerman, Sean Brown, Jonathan B. Houze, Jinqian Liu, Jiwen Liu, Zhihua Ma, Julio C. Medina, Wei Qiu, Michael J. Schmitt, Rajiv Sharma, Yingcai Wang, Liusheng Zhu
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Patent number: 7612068Abstract: The present invention relates to compounds of formula I wherein the substituents are as defined below. The compounds of formula I are useful for the treatment of diseases such as schizophrenia, including both the positive and the negative symptoms of schizophrenia and other psychoses.Type: GrantFiled: April 27, 2004Date of Patent: November 3, 2009Assignee: H. Lundbeck A/SInventors: Garrick P. Smith, Gitte K. Mikkelsen, Kim Andersen, Daniel R. Greve, Jorgen Eskildsen
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Publication number: 20090270421Abstract: Potent inhibitors of fatty acid amide hydrolase (FAAH) are constructed having Ki's below 200 pM and activities 102-103 times more potent than the corresponding trifluoromethyl ketones. The potent inhibitors combine several features, viz.: 1.) an ?-keto heterocylic head group; 2.) a hydrocarbon linkage unit employing an optimal C12-C8 chain length; and 3.) a phenyl or other ?-unsaturation corresponding to the arachidonyl ?8,9/?11,12 and/or oleyl ?9,10 positions. A preferred ?-keto heterocylic head group is ?-keto N4 oxazolopyridine, with incorporation of a second weakly basic nitrogen. Fatty acid amide hydrolase is an enzyme responsible for the degradation of oleamide (an endogenous sleep-inducing lipid) and anandamide (an endogenous ligand for cannabinoid receptors).Type: ApplicationFiled: April 24, 2009Publication date: October 29, 2009Applicant: The Scripps Research InstituteInventor: Dale L. Boger
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Publication number: 20090264401Abstract: A compound of formula (I): and pharmaceutically-acceptable salts thereof wherein the variable groups are defined within; their use in the inhibition of 11?HSD1, processes for making them and pharmaceutical compositions comprising them are also described.Type: ApplicationFiled: April 21, 2009Publication date: October 22, 2009Applicant: AstraZeneca ABInventors: Adrian Liam GILL, Andrew Leach, Martin Packer, James Stewart Scott, Pernilla Sorme, John Gibbin Swales, Paul Robert Owen Whittamore
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Patent number: 7598423Abstract: This application relates to a substituted hydroxyphenyl ketone compound of formula I, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof and its use in treating migraine. This application also relates to processes for preparing a compound of formula I, and intermediate compounds useful therein.Type: GrantFiled: November 15, 2005Date of Patent: October 6, 2009Assignee: Eli Lilly and CompanyInventors: Thomas Daniel Aicher, Guillermo S. Cortez, Todd Michael Groendyke, Albert Khilevich, James Allen Knobelsdorf, Fredrik Pehr Marmsater, Jeffrey Michael Schkeryantz, Tony Pisal Tang, Nicholas Andrew Magnus
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Patent number: 7598236Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: GrantFiled: December 15, 2007Date of Patent: October 6, 2009Assignee: Abbott LaboratoriesInventors: Michael R. Schrimpf, Karin R. Tietje, Richard B. Toupence, Jianguo Ji, Anwer Basha, William H. Bunnelle, Jerome F. Daanen, Jennifer M. Frost, Kevin B. Sippy
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Patent number: 7589114Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-?]imidazole-3-sulfonyl]-azetidine-carboxylic acids, esters and amides which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.Type: GrantFiled: April 4, 2006Date of Patent: September 15, 2009Assignee: Boehringer Ingelheim International GmbHInventor: Steven Richard Brunette
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Patent number: 7589115Abstract: Derivatives of [6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonylamino]-propionamide which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.Type: GrantFiled: October 15, 2007Date of Patent: September 15, 2009Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Terence Alfred Kelly, Jin Mi Kim, René Marc Lemieux
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Publication number: 20090227603Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification.Type: ApplicationFiled: February 23, 2009Publication date: September 10, 2009Inventors: Romyr Dominique, Robert Alan Goodnow, JR., Agnieszka Kowalczyk, Jianping Lou, Qi Qiao, Achyutharao Siddurl, Jefferson Wright Tilley
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Publication number: 20090221547Abstract: The present invention relates to immunosuppressants, processes for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction. This application relates to compounds selected from Formula (Ia), (Ib), (Ic) and (Id).Type: ApplicationFiled: August 22, 2006Publication date: September 3, 2009Applicant: IRM LLCInventors: Wenqi Gao, Yongqin Wan, Jiqing Jiang, Yi Fan, Nathanael S. Gray, Shifeng Pan
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Publication number: 20090203696Abstract: Disclosed are compounds according to formula (I): wherein A, Q, X, Y, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as defined herein. The disclosure also relates to pharmaceutical compositions containing a compound of formula (I), to processes for preparing the compounds of formula (I), and to methods of using the compounds of formula (I).Type: ApplicationFiled: December 15, 2008Publication date: August 13, 2009Applicant: SANOFI-AVENTISInventors: Jozsef Zsolt BOCSKEI, Gary MCCORT, Hans MATTER, Henning STEINHAGEN, Berangere THIERS
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Patent number: 7569591Abstract: The present invention relates to compounds that inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.Type: GrantFiled: July 29, 2004Date of Patent: August 4, 2009Assignee: Vertex Pharmaceuticals IncorporatedInventors: Paul S. Charifson, David D. Deininger, Anne-Laure Grillot, Yusheng Liao, Steven M. Ronkin, Dean Stamos, Emanuele Perola, Tiansheng Wang, Arnaud LeTiran, Joseph Drumm
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Publication number: 20090186868Abstract: A compound represented by the general formula (1) [X1 and X2 represent hydrogen atom, a halogen atom, hydroxyl group and the like, R1 represents a phenyl group, R2 represents an alkyl group, an alkenyl group, or an alkoxy group, R3 represents hydrogen atom, a halogen atom, hydroxyl group, or an alkoxy group, R4 represents hydrogen atom, or an alkyl group, Z1 and Z2 represent hydrogen atom, a halogen atom, hydroxyl group and the like, Z3 represents cyano group, an alkyl group, an alkenyl group and the like, Z4 represents an alkyl group, an alkenyl group, an alkynyl group and the like, and represents a single bond or a double bond], which shows high antitumor effect against cancer cells including drug resistant cells.Type: ApplicationFiled: October 24, 2006Publication date: July 23, 2009Applicant: Daiichi Sankyo Company LimitedInventors: Kouichi Uoto, Yasuyuki Takeda, Atsunobu Sakamoto, Yoshihiro Takayanagi