The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 548/194)
-
Patent number: 8012971Abstract: 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: GrantFiled: April 28, 2006Date of Patent: September 6, 2011Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Toshinari Sugasawa, Takashi Nakajima, Hitoshi Fujita, Toshio Kanai
-
Patent number: 8013166Abstract: This invention relates to certain aryl alkyl acid compounds, compositions, and methods for treating or preventing obesity and related diseases.Type: GrantFiled: September 5, 2008Date of Patent: September 6, 2011Assignee: Bayer Healthcare LLCInventors: Roger A. Smith, Ann-Marie Campbell, Philip Coish, Miao Dai, Susan Jenkins, Derek Lowe, Stephen J. O'Connor, Ning Su, Gan Wang, Mingbao Zhang, Lei Zhu
-
Publication number: 20110207785Abstract: The present invention relates to (R,S) 2-aryl-propionic acids and derivatives, their single enantiomer (S) and to pharmaceutical compositions containing them, which are used in the prevention and treatment of tissue damage due to the exacerbated recruitment of polymorphonucleated neutrophils (PIvTN leukocytes) at inflammation sites. The present invention provides compounds for use in the treatment of transient cerebral ischemia, bullous pemphigo, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and damages caused by ischemia and reperfusion.Type: ApplicationFiled: September 18, 2009Publication date: August 25, 2011Applicant: Dompe S.p.A.Inventors: Marcello Allegretti, Andrea Aramini, Gianluca Bianchini, Maria Candida Cesta
-
Patent number: 7998989Abstract: 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: GrantFiled: May 21, 2008Date of Patent: August 16, 2011Assignee: Korea Institute of Science and TechnologyInventors: Hoh-Gyu Hahn, Dong-Yun Shin, Kee-Dal Nam, Hye-Whon Rhim
-
Publication number: 20110178102Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.Type: ApplicationFiled: June 30, 2004Publication date: July 21, 2011Applicant: ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITYInventors: Vern L Schramm, Anthony A. Suave
-
Patent number: 7982049Abstract: 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-phenylethyl)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: January 14, 2008Date of Patent: July 19, 2011Assignee: Astellas Pharma Inc.Inventors: Souichirou Kawazoe, Kenichirou Sakamoto, Yuji Awamura, Tatsuya Maruyama, Takayuki Suzuki, Kenichi Onda, Toshiyuki Takasu
-
Publication number: 20110172278Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with or mediated by G protein-coupled receptors, in particular G protein-coupled receptor 120.Type: ApplicationFiled: June 23, 2009Publication date: July 14, 2011Applicant: IRM LLCInventors: Xiaohui He, Xuefeng Zhu, Kunyong Yang, Robert Epple, Hong Liu
-
Patent number: 7968576Abstract: This invention relates to certain aryl alkyl acid compounds, compositions, and methods for treating or preventing obesity and related diseases.Type: GrantFiled: September 8, 2008Date of Patent: June 28, 2011Inventors: Roger A. Smith, Ann-Marie Campbell, Philip Coish, Miao Dai, Susan Jenkins, Derek Lowe, Stephen J. O'Connor, Ning Su, Gan Wang, Mingbao Zhang, Lei Zhu
-
Publication number: 20110152261Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing (CRF1) receptor antagonists.Type: ApplicationFiled: August 5, 2009Publication date: June 23, 2011Inventors: David Beattie, Anny-Odile Colson, Andrew James Culshaw, Lisa Rooney, Emily Stanley, Lilya Sviridenko
-
Publication number: 20110136878Abstract: A pest control agent containing a compound represented by the following Formula (1), wherein A represents a carbon atom, a nitrogen atom, or the like, K represents a non-metal atom group necessary for forming a cyclic linking group derived from a 5- or 6-membered aromatic ring, in combination with A and two carbon atoms to which A bonds, X represents a hydrogen atom, a halogen atom, or the like, n represents an integer of from 0 to 4, T represents —C(=G1)-Q1 (wherein G1 and G2 represent an oxygen atom or the like, Q1 represents a phenyl group which may have a substituent, a heterocyclic group which may have a substituent, or the like), or the like, Q2 represents a phenyl group or the like, G3 represents an oxygen atom or the like, and R1 and R2 each independently represent a hydrogen atom, a C1-C6 alkyl group, or a group represented by -L-D, or the like (provided that at least either R1 or R2 represents a group represented by -L-D); as an active ingredient exhibits an excellent effect.Type: ApplicationFiled: June 29, 2009Publication date: June 9, 2011Applicant: Mitsui Chemicals Agro., Inc.Inventors: Yumi Kobayashi, Hiroyuki Katsuta, Michikazu Nomura, Hidetaka Tsukada, Atsushi Hirabayashi, Hidenori Daido, Yusuke Takahashi, Shinichi Banba
-
Publication number: 20110118272Abstract: Novel 3?-deoxy-3?-acylaminospectinomycin compounds are described. Also described are methods of using the 3?-deoxy-3-acylaminospectinomycin compounds and other spectinomycin analogs in treating tuberculosis and in treating microbial infections.Type: ApplicationFiled: July 26, 2010Publication date: May 19, 2011Inventors: Richard E. Lee, Jianjun Qi, Juilian G. Hurdle, Bernd Meibohm, Vnr Pavan Kumar Vaddady, Rakesh, Jiuyu Liu
-
Publication number: 20110081426Abstract: The present invention relates to new aminothiazole modulators of beta-3-adrenoreceptor activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: June 9, 2010Publication date: April 7, 2011Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Tadimeti Rao, Chengzhi Zhang
-
Publication number: 20110071298Abstract: The invention relates to processes and compounds useful for producing modified aspartic acid derivatives, such as aspartic acid aldehyde moieties. Aspartic acid derivatives are useful for preparing caspase inhibitors and/or prodrugs thereof.Type: ApplicationFiled: October 12, 2010Publication date: March 24, 2011Applicant: Vertex Pharmaceuticals IncorporatedInventors: Gerald J. Tanoury, Minzhang Chen, Andrew D. Jones, Philip L. Nyce, Martin Trudeau, David J. Guerin, John R. Snoonian
-
Publication number: 20110046137Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: The pyrazole derivatives of formula (I) or salts thereof modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor (P2X7 receptor antagonists). The invention also relates to the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment or prevention of disorders/diseases mediated by the P2X7 receptor, for example pain, inflammation or a neurodegenerative disease.Type: ApplicationFiled: May 8, 2008Publication date: February 24, 2011Inventors: Paul John Beswick, Laura Jane Chambers, Iain Patrick Chessell, David John Davies, Emmanuel Hubert Demont, Robert James Gleave, David George Hubert Livermore, Pamela Joan Theobald, Mythily Vimal, Daryl Simon Walter
-
Patent number: 7888379Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.Type: GrantFiled: May 24, 2006Date of Patent: February 15, 2011Assignee: Merck Serono SAInventors: Anna Quattropani, David Covini, Vincent Pomel, Jerome Dorbais, Thomas Rueckle
-
Publication number: 20110028481Abstract: 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: February 3, 2011Inventors: 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
-
Publication number: 20110028493Abstract: The present invention aims to provide a compound having superior pharmacological action, physicochemical properties and the like and useful as an sGC activation drug, or an agent for the prophylaxis and/or treatment of diseases such as hypertension, ischemic cardiac disease, cardiac failure, kidney disease, arteriosclerotic disease, atrial fibrillation, pulmonary hypertension, diabetes, diabetic complications, metabolic syndrome, peripheral arterial obstruction, erectile dysfunction and the like. An sGC activation drug containing a compound represented by the formula (II): wherein each symbol is as defined in the specification, or a salt thereof, as an active ingredient.Type: ApplicationFiled: April 3, 2009Publication date: February 3, 2011Inventors: Nobuyuki Matsunaga, Yoshihisa Nakada, Yusuke Ohba, Hideyuki Nakagawa
-
Patent number: 7879888Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.Type: GrantFiled: May 24, 2006Date of Patent: February 1, 2011Assignee: Merck Serono SAInventors: Anna Quattropani, David Covini, Vincent Pomel, Jerome Dorbais, Thomas Rueckle
-
Patent number: 7871999Abstract: The present invention relates to substituted thiazoles, to methods for the production thereof, to medicaments containing these compounds and to the use thereof for producing medicaments.Type: GrantFiled: June 26, 2008Date of Patent: January 18, 2011Assignee: Gruenenthal GmbHInventors: Michael Haurand, Klaus Schiene, Sven Kühnert, Melanie Reich
-
Publication number: 20100298340Abstract: This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.Type: ApplicationFiled: April 12, 2007Publication date: November 25, 2010Applicants: AstraZeneca AB, Astex Therapeutics Ltd.Inventors: Stefan Berg, Karin Kolmodin
-
Publication number: 20100298391Abstract: The present invention provides an amide compound represented by the formula (1): wherein R1 and R2 independently represent a hydrogen atom or a methyl group; and Cy1 represents a C3-C6 cycloalkyl group, said compound having excellent plant disease controlling effect.Type: ApplicationFiled: November 19, 2008Publication date: November 25, 2010Inventors: Takashi Komori, Makoto Kurahashi
-
Patent number: 7838681Abstract: The invention relates to a method of synthesizing heterocyclic compounds. The invention is characterised in that it consists in opening a compound having formula (I), wherein: —X represents NH, O, S or a N-p group, p being a protective group, such as Boc or Troc; —Y represents N, O, S; —Z represents NH2 or NH-p; and —R1 represents a C1-C6 alkoxy radical, aryloxy, such as phenyloxy, or a pyrrolyl radical, said radicals being optionally substituted, or the salts thereof, and the isomers of the aforementioned compounds. Moreover, the above-mentioned opening step is performed in conditions such as to produce a heterocycle having formula (II), wherein: —X, Y and Z are as defined above; —R2 represents a —CH?CH—CH2—NH—COR1 or —CH?CH—CH2—NH—CO group; and R3 occupies one, two or three positions and represents a halogen. The invention can be used to synthesise natural products.Type: GrantFiled: April 30, 2004Date of Patent: November 23, 2010Assignees: Centre National de la Recherche Scientifique (C.N.R.S.), Universite de Paris SudInventors: Ali Al Mourabit, Nathalie Travert, Robert Abou-Jneid, Saïd Ghoulami
-
Patent number: 7820704Abstract: The present invention provides substituted heteroaryl derivatives of Formula (I), methods of their preparation, pharmaceutical compositions comprising the compounds of Formula (I), and methods of use in treating human or animal disorders. The compounds of the invention can be useful as inhibitors of action of AgRP on a melanocortin receptor and thus can be useful for the management, treatment, control, or the adjunct treatment of diseases which may be responsive to the modulation of melanocortin receptors including obesity-related disorders.Type: GrantFiled: April 20, 2005Date of Patent: October 26, 2010Assignee: TransTech Pharma, Inc.Inventors: Adnan M. M. Mjalli, Bapu R. Gaddam, Ghassan Qabaja, Govindan Subramanian, Jeff Zhu, John Dankwardt, Murty N. Arimilli, Robert C. Andrews, Samuel Victory, Ye E. Tian
-
Publication number: 20100267697Abstract: The present teachings provide compounds of Formula (I) and pharmaceutically acceptable salts, hydrates, and esters thereof, wherein Ar, R1, R2, R3, p, and X are defined herein. The present teachings also provide processes for producing said compounds and their pharmaceutically acceptable salts, hydrates and esters, and methods of treating a pathological condition or disorder, or alleviating a symptom thereof, using said compounds including their pharmaceutically acceptable salts, hydrates and esters. The compounds can be useful in modulating ion channel activity including treating a variety of conditions associated with the abnormal modulation of one or more voltage-gated calcium channels.Type: ApplicationFiled: December 11, 2007Publication date: October 21, 2010Applicant: WyethInventors: Vincent P. Galullo, Robert Zelle, Danielle Soenen, Christopher Todd Baker, Paul Will, Hormoz Mazdiyasni, Jinsong Guo, Andrew Fensome, Jeffrey Curtis Kern, William Jay Moore, Edward George Melenski, Justin Kaplan
-
Patent number: 7799738Abstract: 2-Acylaminothiazole-4-carboxamides of the formula (I) and application thereof as an insecticide. wherein R1 represents phenyl which may be optionally substituted, or a 5- or 6-membered heterocyclic group containing at least one hetero atom selected from a group consisting of N, O and S which may be optionally substituted, R2 represents halogen, C1-6 alkyl or C1-6 haloalkyl, R3 represents C1-6 haloalkyl, C1-6 haloalkoxy, C1-6 haloalkylthio, C1-6 haloalkylsulfinyl or C1-6 haloalkylsulfonyl, R4 represents halogen, C1-6 alkyl or C1-6 haloalkyl, and X represents hydrogen, halogen, C1-6 alkyl or C1-6 haloalkyl, and the use of the new compounds as insecticides.Type: GrantFiled: October 26, 2006Date of Patent: September 21, 2010Assignee: Bayer CropScience AGInventors: Akihiko Yanagi, Yukiyoshi Watanabe, Jun Mihara, Katsuhiko Shibuya, Eiichi Shimojo, Akira Emoto
-
Publication number: 20100233116Abstract: The present invention provides heterocyclic derivatives hat modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: August 13, 2007Publication date: September 16, 2010Inventors: Natalie Dales, Julia Fonarev, Jianmin Fu, Rajender Kamboj, Vishnumurthy Kodumuru, Shifeng Liu, Natalia Pokrovskaia, Vandna Raina, Shaoyi Sun, Zaihui Zhang
-
Publication number: 20100216792Abstract: The invention is directed to arylpyrrolidines compounds which exhibit excellent insecticidal efficacy and which may be used as in the agrochemical field or in the field of veterinary medicine. The compounds are represented by formula (I): wherein the respective substituents are defined in the specification.Type: ApplicationFiled: October 14, 2009Publication date: August 26, 2010Applicant: Bayer CropScience AGInventors: Ulrich Görgens, Jun Mihara, Tetsuya Murata, Daiei Yamazaki, Yasushi Yoneta, Koichi Araki, Norio Sasaki, Kei Domon, Mamoru Hatazawa, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya
-
Publication number: 20100197569Abstract: 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: ApplicationFiled: April 13, 2010Publication date: August 5, 2010Applicant: THERAVANCE, INC.Inventors: Paul R. Fatheree, Martin S. Linsell, Daniel D. Long, Daniel Marquess, Edmund J. Moran, Matthew B. Nodwell, S. Derek Turner, James Aggen
-
Publication number: 20100197501Abstract: The invention relates to 1-(thiazolyl)- and 1-(isothiazolyl)pyrazol-4-ylacetic acid derivatives of the general formula (I) and salts thereof in which Het, R1, R2, R3, R4, R5, R6 and n are as defined in claim 1. The compounds (I) or salts thereof are suitable for use as herbicides and plant growth regulators, in particular as herbicides for the selective control of harmful plants in crops of useful plants and can be prepared by processes as described in claim 9.Type: ApplicationFiled: December 3, 2009Publication date: August 5, 2010Applicant: Bayer CropScience AGInventors: Arianna Martelletti, Harald Jakobi, Jan Dittgen, Isolde Haeuser-Hahn, Dieter Feucht, Christopher Hugh Rosinger
-
Publication number: 20100184981Abstract: A compound represented by the following general formula (1), or a salt thereof, has serine protease inhibiting activity, and particularly excellent inhibiting activity against clotting factor VIIa. This compound or a salt thereof is useful as therapeutic and/or prophylactic agents for diseases associated with thrombus formation. wherein R1 represents hydrogen, R2 represents optionally substituted phenyl, etc., R3 represents optionally substituted C6-10 aryl, etc.Type: ApplicationFiled: January 15, 2010Publication date: July 22, 2010Inventors: Richard Clark, Atsushi Takemura, Nobuhisa Watanabe, Osamu Asano, Tadashi Nagakura, Kimiyo Tabata
-
Publication number: 20100145043Abstract: Disclosed herein are 2,4-disubstituted-5-aminocarbonyl-1,3-thiazole derivatives, a preparation method thereof, and a therapeutic agent for treating inflammatory diseases induced by SPC, which contains the derivative as an active ingredient. The anti-inflammatory effect of the 2,4-disubstituted-5-aminocarbonyl-1,3-thiazole derivatives was analyzed through a test employing human dermal cells and an animal test using mice and, as a result, it was found that the derivatives showed excellent inhibitory activity on SPC receptor compared to thiazole derivatives known in the prior art. Thus, the 2,4-disubstituted-5-aminocarbonyl-1,3-thiazole derivatives or pharmaceutically acceptable salts thereof are useful as active ingredients in therapeutic agents for treating inflammatory diseases, such as inflammation, pruritus and skin infection, which appear in atopic dermatitis and other diseases induced by SPC activity. wherein R1, R2, R3 and R4 are as defined in the specification.Type: ApplicationFiled: September 30, 2009Publication date: June 10, 2010Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGYInventors: Young-Dae Gong, Taeho Lee, Moon-Kook Jeon, Heeyeong Cho, Jae Yang Kong, Gildon Choi, Dae Young Jeong, Soon-Hee Hwang
-
Publication number: 20100144806Abstract: A compound of the formula (I): wherein each symbol is as defined in the description, a salt s thereof, and a prodrug thereof of the present invention unexpectedly have a superior GPR40 receptor agonist activity and superior properties as pharmaceutical products such as stability and the like, and can be safe and useful pharmaceutical agents for the prophylaxis or treatment of GPR40 receptor-related pathology or diseases in mammals.Type: ApplicationFiled: July 28, 2006Publication date: June 10, 2010Applicant: Takeda Pharmaceutical Company LimitedInventors: Tsuneo Yasuma, Nobuyuki Negoro
-
Publication number: 20100144805Abstract: A composition and method for inhibiting proliferation of a tumor cell compared to a non-tumor cell. Also described are methods of screening for a composition that inhibits cap-dependent translation compared to cap-independent translation of proteins.Type: ApplicationFiled: January 20, 2006Publication date: June 10, 2010Inventors: Gerhard Wagner, Michael Chorev, Nathan Moerke, Huseyin Aktas, José Halperin
-
Publication number: 20100113520Abstract: Provided herein are electrophilically enhanced kinase inhibitors. Also provided herein are methods of making and utilizing the same.Type: ApplicationFiled: November 5, 2008Publication date: May 6, 2010Applicant: PRINCIPIA BIOPHARMA, INC.Inventor: Richard Miller
-
Publication number: 20100113435Abstract: The present invention relates to compounds with the formula (II) and also to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.Type: ApplicationFiled: November 16, 2009Publication date: May 6, 2010Inventors: Tjeerd BARF, Rikard Emond, Guido Kurz, Jerk Vallgarda, Marianne Nilsson
-
Patent number: 7696354Abstract: 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: April 9, 2008Date of Patent: April 13, 2010Assignee: Shionogi & Co., Ltd.Inventors: Yasuhiro Nishitani, Yoshinori Yamano
-
Publication number: 20100087442Abstract: The present invention relates to a diketohydrazine derivative of formula (I) and a pharmaceutically acceptable salt thereof (the symbols in the formula have the same meaning as described in the specification). The compound of formula (I) has an inhibitory activity against cysteine protease, and it is useful for the treatment of inflammatory diseases, immune diseases, ischemic diseases, respiratory diseases, circulatory diseases, blood diseases, neuronal diseases, hepatic or biliary diseases, osseous or articular diseases, metabolic diseases, etc. And the compound has inhibitory activity against elastase and it is also useful for the treatment of COPD (chronic obstacle pulmonary diseases).Type: ApplicationFiled: September 24, 2009Publication date: April 8, 2010Applicant: ONO PHARMACEUTICAL CO., LTDInventors: Akira Hatayama, Hiroshi Tsuruta, Yasuo Ochi, Haruo Imawaka, Kazuyuki Ohmoto
-
Publication number: 20100056586Abstract: Compounds which inhibit microbial growth or attenuate the virulence of pathogen microorganisms. Compounds of the invention inhibit UDP-galactopyranose mutase (UGM) and have activity as inhibitors of microbial growth of microorganisms which contain this enzyme and particularly those microorganisms in which this enzyme is responsible for the incorporation of galactofuranose residues, particularly for uridine 5?-diphosphate (UDP) galactopyranose mutase. Compounds of the invention inhibit UDP-galactopyranose mutase (UGM) and have activity to attenuate virulence of pathogenic microorganisms, including mycobacteria.Type: ApplicationFiled: April 27, 2009Publication date: March 4, 2010Inventors: Laura Lee Kiessling, Emily Carla Dykhuizen, John F. May
-
Publication number: 20100056587Abstract: Substituted aminothiazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted aminothiazole, and methods of use in treating human or animal disorders. The compounds may be useful as inhibitors of action of AgRP on a melanocortin receptor and thus may be useful for the management, treatment, control, or the adjunct treatment of diseases which may be responsive to the modulation of melanocortin receptors including obesity-related disorders.Type: ApplicationFiled: August 25, 2009Publication date: March 4, 2010Inventors: Adnan M. M. Mjalli, Bapu Gaddam, Robert C. Andrews, Samuel Victory, Suparna Gupta
-
Publication number: 20100029718Abstract: The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: September 19, 2007Publication date: February 4, 2010Inventors: Natalie Dales, Zaihui Zhang, Rajender Kamboj, Jianmin Fu, Shaoyi Sun, Natalia Pokrovskaia, Serguei Sviridov
-
Publication number: 20100029733Abstract: A nitrogen-containing bicyclic heterocyclic compound represented by the following formula (1) is provided. When the compound or a salt thereof is administered to a human being or an animal, the compound has a strong antagonistic action against EP1 receptors, and is useful, for example, as an active ingredient of a medicine for the prevention and/or treatment of overactive bladder. The compound is also useful as an active ingredient of a medicine for the prevention and/or treatment of symptoms such as frequency urinary, urinary urgency, or urinary incontinence.Type: ApplicationFiled: July 14, 2009Publication date: February 4, 2010Applicant: ASAHI KASEI PHARMA CORPORATIONInventors: Masakazu Atobe, Kenji Naganuma, Akifumi Morimoto
-
Patent number: 7655804Abstract: The present invention relates to a diketohydrazine derivative of formula (I) and a pharmaceutically acceptable salt thereof (the symbols in the formula have the same meaning as described in the specification). The compound of formula (I) has an inhibitory activity against cysteine protease, and it is useful for the treatment of inflammatory diseases, immune diseases, ischemic diseases, respiratory diseases, circulatory diseases, blood diseases, neuronal diseases, hepatic or biliary diseases, osseous or articular diseases, metabolic diseases, etc. And the compound has inhibitory activity against elastase and it is also useful for the treatment of COPD (chronic obstacle pulmonary diseases).Type: GrantFiled: April 24, 2003Date of Patent: February 2, 2010Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Akira Hatayama, Hiroshi Tsuruta, Yasuo Ochi, Haruo Imawaka, Kazuyuki Ohmoto
-
Patent number: 7652146Abstract: The invention is directed to processes for preparing 2-aminothiazole-5-carboxamides of formula I wherein R1, R2, R3, R4 and R5 are as defined as set forth in the specification herein.Type: GrantFiled: February 3, 2005Date of Patent: January 26, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Bang-Chi Chen, Rulin Zhao, Bei Wang
-
Publication number: 20100010057Abstract: Compounds of formula (I) are inhibitors of P13 kinase activity, and useful in treatment of, inter alia, autoimmune, inflammatory and proliferative diseases: wherein: s is 0 or 1; U is hydrogen or halogen; X is —(C?O), an optionally substituted divalent phenylene, pyridinylene, pyrimidinylene, or pyrazinylene radical, or a bond; P is optionally substituted C1-C6 alkyl and Z is —(CH2)Z—X1-L1-NHCHR1R2; or Z is optionally substituted C1-C6 alkyl and P is —(CH2)Z—X1-L1-NHCHR1R2; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; X1 is (i) a bond; —NR4C(?O)NR5— or —NR4S(?O)2—; or except when X is —(C?O)— (ii) —C(?O)—, —S(?O)2—, or —S(?O)2NR4— wherein R4 and R5 are independently hydrogen or optionally substituted C1-C6 alkyl; and z and L1 are as defined in the specification.Type: ApplicationFiled: May 3, 2007Publication date: January 14, 2010Applicant: CHROMA THERAPEUTICS LTD.Inventors: David Charles Festus Moffat, Stephen Davies, Sonia Maria Alesso, Delphine Francoise Monique Launay
-
Patent number: 7645799Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, and ring B are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: GrantFiled: November 7, 2008Date of Patent: January 12, 2010Assignee: Bristol-Myers Squibb CompanyInventors: James R. Corte, Mimi L. Quan, Joanne M. Smallheer, Donald J. P. Pinto
-
Publication number: 20090306022Abstract: The present invention pertains, at least in part, to novel 7-substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.Type: ApplicationFiled: June 9, 2009Publication date: December 10, 2009Applicants: Trustees of Tufts College, Paratek Pharmaceuticals, Inc.Inventors: Mark L. Nelson, Roger Frechette, Peter Viski, Mohamed Ismail, Todd Bowser, Beena Bhatia, David Messersmith, Laura McIntyre, Darrell Koza, Glen Rennie, Paul Sheahan, Paul Hawkins, Atul Verma, Tadeusz Warchol, Upul Bandarage
-
Publication number: 20090298866Abstract: The present application relates to compounds of formula (I) or a pharmaceutically acceptable derivative thereof: formula (I) wherein X, R1, R2, and R3 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.Type: ApplicationFiled: July 9, 2007Publication date: December 3, 2009Inventors: Adrian Hall, David Nigel Hurst, Tiziana Scoccitti, Pamela Joan Theobald
-
Publication number: 20090291936Abstract: 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: November 20, 2008Publication date: November 26, 2009Inventors: Kazutoshi Sugawara, Tetsuji Matsudaira, Hiroshi Sugama, Masao Nawano, Rikiya Ohashi
-
Publication number: 20090281142Abstract: [Problem] To provide a compound which is useful as a GK activator. [Means for Resolution] As a result of an extensive study on thiazole derivatives, the present inventors have found that a compound having an oxamoyl group, a glycol group or the like on a thiazole ring and a compound having an acetamide group substituted by a bicyclic heteroaryl group such as a quinolyl have a good GK activation effect, and thereby have accomplished the present invention. Since the compounds of the present invention have a good GK activation effect, these are useful as therapeutic agents for diabetes, particularly type II diabetes.Type: ApplicationFiled: August 30, 2006Publication date: November 12, 2009Applicant: ASTELLAS PHARMA INC.Inventors: Masahiko Hayakawa, Takahiro Nigawara, Kazuyuki Tsuchiya, Naoki Ishibashi, Mitsuaki Okumura, Yuichiro Kawamoto, Akira Nagayoshi
-
Publication number: 20090270456Abstract: This invention relates to newly identified compounds for inhibiting hYAK3 and/or CK2 proteins and methods for treating diseases associated with the imbalance or inappropriate activity of hYAK3 and/or CK2 proteins.Type: ApplicationFiled: January 6, 2005Publication date: October 29, 2009Inventors: Masaichi Hasegawa, Kazuya Kano, Masato Nakano, Mariko Yamabe