The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 548/194)
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Publication number: 20090253705Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.Type: ApplicationFiled: April 2, 2009Publication date: October 8, 2009Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Dong-Ming Shen, Liping Wang, Cheng Zhu
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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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Publication number: 20090247534Abstract: The present invention provides organic compounds of the following structure; A-L1-B-C-D-L2-E that are useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.Type: ApplicationFiled: March 28, 2007Publication date: October 1, 2009Inventors: Michael H. Serrano-Wu, Young-Shin Kwak, Wenming Liu
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Patent number: 7579366Abstract: The invention relates to epothilone analog represented by the formula I wherein (i) R2 is absent or oxygen; “a” can be either a single or double bond; “b” can be either absent or a single bond; and “c” can be either absent or a single bond, with the proviso that if R2 is oxygen then “b” and “c” are both a single bond and “a” is a single bond; if R2 is absent then “b” and “c” are absent and “a” is a double bond; and if “a” is a double bond, then R2, “b” and “c” are absent; R3 is a radical selected from the group consisting of hydrogen; lower alkyl; —CH?CH2; —C?CH; —CH2F; —CH2Cl; —CH2—OH; —CH2—O—(C1-C6-alkyl); and —CH2—S—(C1-C6-alkyl); R4 and R5 are independently selected from hydrogen, methyl or a protecting group; and R1 is as defined in the specification, or a salt of a compound of the formula I where a salt-forming group is present. A further aspect of the invention is related to the synthesis of epothilone E.Type: GrantFiled: March 11, 2003Date of Patent: August 25, 2009Assignee: The Scripps Research InstituteInventors: Kyriacos C. Nicolaou, Nigel Paul King, Maurice Raymond Verschoyle Finlay, Yun He, Frank Roschangar, Dionisios Vourloumis, Hans Vallberg, Antony Bigot
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Patent number: 7579355Abstract: The present invention is directed to compounds which contain a substituted pyridine moeity 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 20, 2004Date of Patent: August 25, 2009Assignee: Merck & Co., Inc.Inventors: Mark T. Bilodeau, Mark E. Duggan, John C. Hartnett, Craig W. Lindsley, Zhicai Wu, Zhijian Zhao
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Publication number: 20090203918Abstract: The invention relates to a method for producing enantiomers form of 2,3-diaminopropionic acid derivatives of formula (I) by asymmetric hydrogenation from compounds of formula (II).Type: ApplicationFiled: April 6, 2009Publication date: August 13, 2009Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Joerg RIEKE-ZAPP, Guenter BILLEN
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Publication number: 20090197795Abstract: This invention relates to certain aryl alkyl acid compounds, compositions, and methods for treating or preventing obesity and related diseases.Type: ApplicationFiled: August 4, 2008Publication date: August 6, 2009Applicant: Bayer HealthCare LLCInventors: Roger Smith, Ann-Marie Campbell, Philip Coish, Miao Dai, Susan Jenkins, Derek Lowe, Stephen O'Connor, Ning Su, Gan Wang, Mingbao Zhang, Lei Zhu
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Publication number: 20090170828Abstract: Azetidine derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; liver steatosis; and non-alcoholic steatohepatitis.Type: ApplicationFiled: June 8, 2007Publication date: July 2, 2009Inventors: Elise Isabel, Renata Oballa, David Powell, Joel Robichaud
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Patent number: 7553962Abstract: This invention provides cross-linked glycopeptide-cephalosporin compounds and pharmaceutically acceptable salts thereof which are useful as antibiotics. This invention also provides pharmaceutical compositions containing such compounds; methods for treating bacterial infections in a mammal using such compounds; and processes and intermediates useful for preparing such compounds.Type: GrantFiled: August 24, 2007Date of Patent: June 30, 2009Assignee: Theravance, Inc.Inventors: Paul R. Fatheree, Martin S. Linsell, Daniel Marquess, S. Derek Turner
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Patent number: 7550493Abstract: A halogenated benzamide derivative characterized by greater specificity for viral pathogens and less disruptive to beneficial gut microflora, according to formula (III): in which R1 is a halogen atom, and R2-R6 are independently hydrogen, hydroxyl, C1-C4 alkyl, —C1-C4 alkoxy, acyloxy, nitro, halogen, —C(O)R7 where R7 is —C1-C4 alkyl, or, aromatic including salts and hydrates of these compounds and where at least two of R2-R6 are not hydrogen and where at least one of R2-R6 are hydroxy or acyloxy.Type: GrantFiled: October 1, 2007Date of Patent: June 23, 2009Assignee: Romark Laboratories, LCInventor: Jean Francois Rossignol
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Publication number: 20090149471Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: May 8, 2007Publication date: June 11, 2009Inventors: William C. Shakespeare, Wei-Sheng Huang, David C. Dalgarno, Xiaotian Zhu, R. Matthew Thomas, Yihan Wang, Jiwei Qi, Rajeswari Sundaramoorthi, Dong Zou, Chester A. Metcalf, III, Tomi k. Sawyer, Jan Antoinette C. Romero
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Publication number: 20090143358Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides substituted aryl sulfonamides, compositions comprising these compounds, as well as methods of using these compounds or compositions in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrence of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a voltage-gated sodium channel.Type: ApplicationFiled: March 20, 2008Publication date: June 4, 2009Applicants: ICAgen, Inc., Pfizer LimitedInventors: Brian Edward Marron, Paul Christopher Fritch, Christopher John Markworth, Andrew Thomas Maynard, Nigel Alan Swain
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Publication number: 20090131439Abstract: Disclosed is a method for the prevention and/or treatment of a chronic obstructive pulmonary disease by administrating a 5-membered cyclic compound represented by the formula below: or a pharmaceutically acceptable salt of the compound or a prodrug of the compound or salt: wherein X represents an oxygen or sulfur atom; R1 represents a hydrogen atom, a substituted or unsubstituted alkyl or the like; R2 represents a hydrogen atom, a substituted or unsubstituted alkyl or the like; Y1 represents single bond, a substituted or unsubstituted alkylene or the like; the wavy line means an (E) or (Z) coordination; R3 represents a hydrogen atom, a substituted or unsubstituted aryl or the like; Y2 represents a substituted or unsubstituted alkylene or an alkenylene; R4 represents a hydrogen atom, a substituted or unsubstituted alkanoyl or the like; and R5 represents a hydrogen atom or a substituted or unsubstituted alkyl.Type: ApplicationFiled: April 28, 2006Publication date: May 21, 2009Inventors: Toshinari Sugasawa, Takashi Nakajima, Hitoshi Fujita, Toshio Kanai
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Publication number: 20090124664Abstract: The present invention relates to selected (R)-arylalkylamino derivatives of formula (I), in which R, R1 and Ar are as defined in the claims. These compounds show a surprising potent inhibitory effect on C5a induced human PMN chemotaxis. The compounds of the invention absolutely lack of CXCL8 inhibitory activity. Said compounds are useful in the treatment of pathologies depending on the chemotactic activation of neutrophils and monocytes induced by the fraction C5a of the complement. In particular, the compounds of the invention are useful in the treatment of sepsis, psoriasis, rheumatoid arthritis, ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of injury caused by ischemia and reperfusion.Type: ApplicationFiled: November 24, 2006Publication date: May 14, 2009Inventors: Marcello Allegretti, Alessio Moriconi, Andrea Aramini, Maria Candida Cesta, Andrea Beccari, Riccardo Bertini
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Patent number: 7524957Abstract: The invention relates to the use of a compound of Formula (I) or a salt, solvate or prodrug thereof, wherein R1, R2, R3, n and m are as described in the specification, in the preparation of a medicament for the treatment or prevention of a disease condition mediated through glucokinase (GLK), such as type 2 diabetes. The invention also relates to a novel group of compounds of Formula (I) and to methods for preparing compounds of Formula (I).Type: GrantFiled: February 1, 2008Date of Patent: April 28, 2009Assignee: AstraZeneca ABInventors: Scott Boyd, Peter William Rodney Caulkett, Rodney Brian Hargreaves, Suzanne Saxon Bowker, Roger James, Clifford David Jones, Darren McKerrecher, Michael Howard Block, Craig Johnstone
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Publication number: 20090105474Abstract: The anthranilic acid derivative or the salt thereof represented by the general formula wherein R1 and R2 are hydrogen atom, or the like; R3 is a phenyl, cycloalkyl or bicyclic heterocyclic group which may be substituted, or the like; R4 is a phenyl, cycloalkyl or pyridyl group which may be substituted, or the like; X1 is an alkylene or alkenylene group which may be substituted or a bond; X2 is the general formula -X3-X4- or -X4-X3-, wherein X3 is a sulfur atom, an imino group or a bond, or the like; X4 means an alkylene or alkenylene group which may be substituted or a bond; is useful for a remedy such as rheumatoid arthritis, osteoarthritis and carcinoma, because it shows MMP-13 production inhibitory effect.Type: ApplicationFiled: March 14, 2006Publication date: April 23, 2009Applicant: Toyama Chemical Co., Ltd.Inventors: Junichi Yokotani, Yoichi Taniguchi, Eiji Hara, Hitoshi Akitsu, Hidehiko Tanaka, Shuzo Anzai
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Publication number: 20090093452Abstract: Disclosed are compounds and pharmaceutically acceptable salts of Formula I wherein RQ, R7, n, Q2, Q3, Y, and X1-X3 are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.Type: ApplicationFiled: August 24, 2007Publication date: April 9, 2009Inventors: Kenneth He Huang, Steven E. Hall, James Veal
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Publication number: 20090093527Abstract: Azacyclopentane derivatives of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; liver steatosis; and non-alcoholic steatohepatitis.Type: ApplicationFiled: June 8, 2007Publication date: April 9, 2009Inventors: Chun Sing Li, Yeeman K. Ramtobul
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Publication number: 20090088432Abstract: The present invention encompasses; the novel substituted heterocyclic compounds represented by formula (I) or their pharmaceutically acceptable salts, wherein the substituents in formula (I) have the meanings as defined in the specification. The invention also encompasses process for preparing such compound, pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases.Type: ApplicationFiled: September 15, 2006Publication date: April 2, 2009Inventors: Rakesh Kumar Banerjee, Ramesh Chandra Gupta, Davinder Tuli, Milind Rode, Bharat Suthar, Dhananjay Umrani, Padmaja Pathak, Tejal Choksi, Anita Chaudhary
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Publication number: 20090048248Abstract: The present invention is directed to certain hydropyranopyrrolidine compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.Type: ApplicationFiled: December 18, 2006Publication date: February 19, 2009Inventors: Robert J. DeVita, Jianming Bao, Sander G. Mills
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Publication number: 20090047687Abstract: This invention relates to novel indane acetic acid derivatives which are useful in the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic diseases. The invention also relates to intermediates useful in preparation of indane acetic derivatives and to methods of preparation.Type: ApplicationFiled: March 31, 2008Publication date: February 19, 2009Inventors: Derek B. Lowe, Philip L. Wickens, Xin Ma, Mingbao Zhang, William H. Bullock, Philip D. G. Coish, Ingo A. Mugge, Andreas Stolle, Ming Wang, Yamin Wang, Chengzhi Zhang, Hai-Jun Zhang, Lei Zhu, Manami Tsutsumi, James N. Livingston
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Publication number: 20090005568Abstract: The invention relates to substituted 2-aminothiazole derivatives useful in treating disorders that are mediated by A2a receptor function, including neurodegenerative diseases including Parkinson's disease and inflammation.Type: ApplicationFiled: August 18, 2006Publication date: January 1, 2009Applicant: Pharmacopeia Drug Discovery, Inc.Inventors: Andrew G. Cole, Axel Metzger, Ian Henderson
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Publication number: 20080312291Abstract: The present invention relates to novel thiazole and oxazole derivatives having a positive allosteric GABAB receptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS). The compounds are represented by the general formula (I) wherein X1 and X2 are selected from 0 and N or S and N and R1, R2 and Y are as defined in the description. For example, R1 may be alkyl, alkoxy, thioalkoxy or aryl, R2 may be alkoxy and Y may be a carbonylamino-linked substituent containing an aryl or heteroaryl group.Type: ApplicationFiled: December 21, 2006Publication date: December 18, 2008Inventors: Udo Bauer, Linda Gustafsson, Maria Saxin, Tor Svensson
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Publication number: 20080312223Abstract: The invention provides a compound of the formula (I): or a salt, N-oxide, tautomer or solvate thereof, wherein X is CR5 or N; each of Q1 and Q2 is a carbon atom; Q3 is selected from S and CH; Q4 is selected from CR2 and S; provided that one of Q3 and Q4 is S and the other of Q3 and Q4 is not S; wherein when Q3 is S, there is a double bond between Q1 and Q4 and a double bond between Q2 and the adjacent ring nitrogen atom N; and when Q4 is S, there is a double bond between Q1 and Q2, and a double bond between Q3 and the adjacent ring nitrogen atom N; A is a bond or —(CH2)m—(B)n—; B is C?O, NR8(C?O) or O(C?O) wherein R1 is hydrogen or C1_4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; m is 0, 1 or 2; n is 0 or 1; Ro is hydrogen or, together with NRg when present, forms a group —(CH2)p— wherein p is 2 to 4; R1 is hydrogen, a carbocyclic or heterocyclic group having from 3 to 12 ring members, or an optionally substituted C1-8 hydrocarbyl group; R2 is hydrogen, halogen, methoxy, or a C1-4 hydrocarbyType: ApplicationFiled: December 30, 2005Publication date: December 18, 2008Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Valerio Berdini, Michael Alistair O'Brien, Theresa Rachel Phillips, Paul Graham Wyatt
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Publication number: 20080293786Abstract: Novel 2-imino-1,3-thiazoline based compounds represented by Chemical Formula I, and T-type calcium channel inhibitors containing the compound are provided. The T-type calcium channel inhibitors according to the present invention are useful as a treating agent of diseases associated with over-expression of the T-type calcium channel.Type: ApplicationFiled: May 21, 2008Publication date: November 27, 2008Applicant: Korea Institute of Science and TechnologyInventors: Hoh-Gyu Hahn, Dong-Yun Shin, Kee-Dal Nam, Hye-Whon Rhim
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Publication number: 20080269220Abstract: A compound represented by the formula (1): wherein each symbol is as defined in the specification, and a salt thereof and a prodrug thereof unexpectedly have superior GPR40 receptor agonist activity, superior in the properties as a pharmaceutical product such as stability and the like, and can be a safe and useful pharmaceutical agent as a drug for the prophylaxis or treatment of GPR40 receptor related pathology or diseases such as diabetes and the like.Type: ApplicationFiled: March 14, 2005Publication date: October 30, 2008Inventors: Tsuneo Yasuma, Nobuyuki Negoro, Shinobu Sasaki
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Publication number: 20080255141Abstract: Novel compounds selected from 2-(3-aminoaryl)amino-4-aryl-thiazoles of formula (I) that selectively modulate, regulate, and/or inhibit signal transductions mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferation metabolic, allergic and degenerative disorders. More particularly, these compounds are potent and selective c-kit inhibitors.Type: ApplicationFiled: July 18, 2007Publication date: October 16, 2008Inventors: Marco Ciufolini, Camille Wermuth, Bruno Gielthen, Alain Moussy
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Patent number: 7427635Abstract: The present invention relates to compounds of the formula which are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as, cancer, cognative and CNS disorders and inflammatory/autoimmune diseases.Type: GrantFiled: August 11, 2005Date of Patent: September 23, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Xin-Jie Chu, Nader Fotouhi, Nicholas J. S. Huby, Norman Kong, Lee Apostle McDermott, John Moliterni, Zhuming Zhang
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Publication number: 20080221088Abstract: The present application provides novel thiazole derivatives that are useful as activators of Adenosine 5?-Monophosphate-Activated Protein Kinase and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: June 23, 2006Publication date: September 11, 2008Inventors: Vijay Kumar Potluri, Saibal Kumar Das, Pradip Kumar Sasmal, Javed Iqbal, Parimal Misra, Ranjan Chakrabarti, Rashmi Talwar
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Patent number: 7423156Abstract: This invention relates to certain aryl alkyl acid compounds, compositions, and methods for treating or preventing obesity and related diseases.Type: GrantFiled: January 27, 2006Date of Patent: September 9, 2008Assignee: Bayer Pharmaceuticals CorporationInventors: Roger Smith, Ann-Marie Campbell, Philip Coish, Miao Dai, Susan Jenkins, Derek Lowe, Stephen O'Connor, Ning Su, Gan Wang, Mingbao Zhang, Lei Zhu
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Patent number: 7423055Abstract: The present invention relates to novel compounds selected from 2-(3-aminoaryl)amino-4-aryl-thiazoles that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. More particularly, these compounds are potent and selective c-kit inhibitors.Type: GrantFiled: August 1, 2003Date of Patent: September 9, 2008Assignee: AB ScienceInventors: Marco Ciufolini, Camille Wermuth, Bruno Gielthen, Alain Moussy
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Publication number: 20080207703Abstract: The present invention provides novel heterocyclic urea compounds having useful antibacterial activity, pharmaceutical compositions comprising one or more of these compounds, methods of making the same, and methods of using the same.Type: ApplicationFiled: July 23, 2007Publication date: August 28, 2008Applicant: Replidyne, Inc.Inventors: Joseph Guiles, Thale Jarvis, Sarah Strong, Xicheng Sun
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Patent number: 7414067Abstract: This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.Type: GrantFiled: March 24, 2004Date of Patent: August 19, 2008Assignees: Merck & Co. Inc., Evotec OAIInventors: Edward Andrew Boyd, Michael H. Fisher, Maria L. Garcia, Gregory J. Kaczorowski, Peter T. Meinke, William H. Parsons, Stephen Price, John Stibbard
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Patent number: 7408069Abstract: A method for preparing a compound of the structure I,Type: GrantFiled: August 3, 2006Date of Patent: August 5, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Bernd Schaefer, Frank Haunert, Norbert Goetz
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Publication number: 20080146625Abstract: Disclosed herein are pyrazole glucokinase activators of the formula (I): that are useful for the treatment of metabolic diseases and disorders.Type: ApplicationFiled: December 6, 2007Publication date: June 19, 2008Inventors: Steven Joseph Berthel, Robert Francis Kester, Douglas Eric Murphy, Thomas Jay Prins, Frank Ruebsam, Chinh Viet Tran, Dionisios Vourloumis
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Patent number: 7384928Abstract: A compound of the formula: (wherein, T is S, SO or O; X is halogen, CN, carbamoyl optionally substituted with lower alkyl, lower alkyl, lower alkoxy, or lower alkylthio; A is substituted lower alkylene (wherein the substituent is optionally substituted mono lower alkyl, optionally substituted lower alkylidene, or optionally substituted lower alkylene); Z+ is an optionally substituted, a cation and an N atom-containing heterocyclic group), ester, amino-protected compound wherein the amino bonds to a thiazole ring at the 7-position, or pharmaceutically acceptable salt or solvate thereof.Type: GrantFiled: March 18, 2003Date of Patent: June 10, 2008Assignee: Shionogi & Co., Ltd.Inventors: Yasuhiro Nishitani, Yoshinori Yamano
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Patent number: 7384968Abstract: The present invention relates to compounds of the Formula I wherein R1, R3, R4, R5, R6 and R7 are as defined. Compounds of the Formula I have activity inhibiting production of A?-peptide. The invention also relates to pharmaceutical compositions and methods of treating disorders and diseases, for example, neurodegenerative and/or neurological disorders, e.g., Alzheimer's disease, in a mammal comprising compounds of the Formula I.Type: GrantFiled: March 11, 2005Date of Patent: June 10, 2008Assignee: Pfizer Inc.Inventor: Yuhpyng L. Chen
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Publication number: 20080132479Abstract: The problem of the present invention is to provide a useful compound as a glucokinase activating agent, which is the oxime derivative of the formula [I]: wherein Ring A is aryl or heteroaryl; Q is cycloalkyl, heterocycle, alkyl or alkenyl; Ring T is heteroaryl or heterocycle; R1 and R2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl or the like; R3 and R4 are independently hydrogen atom, hydroxy, oxo, halogen atom or the like; R5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl or the like; or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: July 10, 2006Publication date: June 5, 2008Inventors: Kazutoshi Sugawara, Tetsuji Matsudaira, Hiroshi Sugama, Masao Nawano, Rikiya Chashi
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Publication number: 20080125432Abstract: The present invention relates to compounds that interact with ion channels. In particular, the invention relates to compounds having the structural Formula having the structural Formula I, II, III or IV, stereoisomers, tautomers, racemics, prodrugs, metabolites thereof, or a pharmaceutically acceptable salt and/or solvate thereof, wherein X, Y1, Y2, R1, n, R3, R8, R9, R10, L1, L2, Ar1 and Ar2 are defined in claim 1. The invention also relates to methods for preparing said compounds, to pharmaceutical compositions comprising said compounds, and to the use of said compounds in methods for treatment of the human and animal body.Type: ApplicationFiled: December 1, 2005Publication date: May 29, 2008Applicant: Devgen NVInventors: Petra Blom, Jan Octaaf De Kerpel, Eric Pierre Paul Rene Fourmaintraux, Titus Jan Kaletta, Dirk Leysen
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Patent number: 7358267Abstract: Compounds, compositions and methods are provided that are useful in the treatment or prevention of a condition or disorder mediated by an uncoupling protein. In particular, the compounds of the invention modulate the expression and/or activity of UCP3.Type: GrantFiled: June 27, 2002Date of Patent: April 15, 2008Assignee: Amgen Inc.Inventors: M. Catherine Amaral, Jin-Long Chen, Juan C. Jaen, David N. Johnston, Paul Rafferty
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Patent number: 7342117Abstract: To provide novel crystals useful as an ingredient for the production of a diabetes remedy. The invention is concerned with ?-form crystal and ?-form crystal of (R)-2-(2-aminothiazol-4-yl)-4?-[2-[(2-hydroxy-2-phenyleth-yl)amino]ethyl]acetanilide. The ?-form crystal does not exhibit hygroscopicity and has stability such that it can be used as a medicine, and is useful for mass synthesis in the industrial production. The ?-form crystal does not relatively exhibit hygroscopicity and is also useful as a production intermediate of the ?-form crystal.Type: GrantFiled: October 20, 2002Date of Patent: March 11, 2008Assignee: Astellas Pharma Inc.Inventors: Souichirou Kawazoe, Kenichirou Sakamoto, Yuji Awamura, Tatsuya Maruyama, Takayuki Suzuki, Kenichi Onda, Toshiyuki Takasu
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Patent number: 7309791Abstract: The invention relates to new compounds, being 3-phenylpropionic acid derivatives of formula I wherein W represents COOH group or its bioisosters, or —COO—C1–C4-alkyl group; Y represents NH, N—C1–C10-alkyl, O, or S; Z represents NH, N—C1–C10-alkyl, N-aryl, N-heteroaryl, S, or O; X represents O, S, NH, N—C1–C10-alkyl, N-aryl, NSO2—C1–C10-alkyl, N—SO2-aryl, or N—SO2-heteroaryl; R1, to R6 each independently represent hydrogen atom or a substituent defined in the description; A is as defined in the description; n represents an integer from 0 to 4, inclusive; and pharmaceutically acceptable salts thereof. The compounds are the ligands of PPAR-gamma receptor and are useful as medicaments.Type: GrantFiled: January 12, 2006Date of Patent: December 18, 2007Assignee: Adamed Sp. z.o.oInventors: Zbigniew Majka, Katarzyna Ewa Rusin, Dominik Daniel Kludkiewicz, Krzysztof Kurowski, Katarzyna Joanna Matusiewicz, Tomasz Stawinski, Daniel Sulikowski, Piotr Kowalczyk
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Patent number: 7291744Abstract: The present application describes modulators of chemokine receptors of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: November 12, 2004Date of Patent: November 6, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Soo S. Ko, Douglas G. Batt, George V. Delucca, John V. Duncia, Daniel S. Gardner, Joseph B. Santella
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Patent number: 7265109Abstract: Compounds of formula I as well as pharmaceutically acceptable salts and esters thereof, wherein the substituents have the significance given in the specification, and the compounds are neuropeptide Y(NPY) antagonists which are useful in the treatment of obesity.Type: GrantFiled: August 10, 2004Date of Patent: September 4, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Werner Neidhart, Matthias Heinrich Nettekoven, Philippe Pflieger, Sven Taylor
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Patent number: 7253197Abstract: Compounds of formula I as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R4 have the significance given in the specification, and the compounds, salts and esters can be used for the treatment of obesity.Type: GrantFiled: August 5, 2003Date of Patent: August 7, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Wolfgang Guba, Patrizio Mattei, Werner Neidhart, Matthias Heinrich Nettekoven, Philippe Pflieger
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Patent number: 7250508Abstract: 7-[2-(2-aminothiazol-4-yl)-2-(methylcarbonyloxyimino)acetamido]-3-vinyl-cephem-4-carboxylic acid of formula I in the form of a crystalline salt and use thereof, e.g. in the preparation of pure cefdinir. In another aspect this invention relates to the compound of formula I in the form of a salt, optionally in crystalline form, wherein the salt is selected from the group consisting of phosphate, hydrogen phosphate, mesylate, tosylate, sulfate, hydrogen sulfate and sulfamate.Type: GrantFiled: August 12, 2003Date of Patent: July 31, 2007Assignee: Sandoz AGInventors: Peter Kremminger, Siegfried Wolf, Johannes Ludescher
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Patent number: 7250431Abstract: Thiazole derivatives of formula I are provided as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R5, a and b have the significance given in the specification. The compounds are neuropeptide Y Y5 receptor antagonists which can be used for the treatment of obesity.Type: GrantFiled: August 10, 2004Date of Patent: July 31, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Werner Neidhart, Matthias Heinrich Nettekoven, Philippe Pflieger
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Patent number: 7244278Abstract: The object of the present invention is a ready-to-use agent for coloring keratin fibers containing (i) at least one heterocyclic hydrazone derivative of formula (I), (ii) at least one aromatic enamine of formula (IIa) or an acid addition compound thereof (IIb) and (iii) at least one oxidant, a multicomponent kit and a method for coloring keratin fibers by use of said agentType: GrantFiled: November 11, 2004Date of Patent: July 17, 2007Assignee: Wella AGInventors: Cecile Pasquier, Veronique Buclin, Caroline Kiener, Nadja Duc-Reichlin, Hans-Juergen Braun
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Patent number: 7179827Abstract: This invention concerns novel thiazole compounds. Methods of using these compounds for the treatment, prevention and management of various diseases or disorders, as well as pharmaceutical compositions of these compounds, are also disclosed.Type: GrantFiled: March 31, 2005Date of Patent: February 20, 2007Assignee: Lexicon Genetics IncorporatedInventors: Haihong Jin, Zhi-Cai Shi, Heidi Theis, Hartmuth Kolb
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Patent number: 7173129Abstract: The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the application.Type: GrantFiled: June 7, 2004Date of Patent: February 6, 2007Assignee: Athero Genics, Inc.Inventors: Kimberly J. Worsencroft, Liming Ni, Zhihong Ye, Charles Q. Meng, M. David Weingarten, Jacob E. Simpson, James A. Sikorski