1,3-oxazole Ring Or 1,3-thiazole Ring (including Hydrogenated) Patents (Class 544/369)
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Publication number: 20120136001Abstract: The invention relates to novel oxindole derivatives of general formula (I), in which the substituents A, B, R1, R2 and R3 are defined as cited in claim 1, to medicaments containing said derivatives and to the use of the latter for the prophylaxis and/or treatment of vasopressin-dependent and/or oxytocin-dependent diseases.Type: ApplicationFiled: January 30, 2012Publication date: May 31, 2012Inventors: Wilfried Lubisch, Thorsten Oost, Wolfgang Wernet, Wilfried Hornberger, Liliane Unger, Hervé Geneste
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Publication number: 20120129842Abstract: This invention relates to bisthiazole I and its therapeutic and prophylactic uses, wherein the variables A, R5, R6, and R7 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.Type: ApplicationFiled: November 16, 2011Publication date: May 24, 2012Inventors: Paul Francis JACKSON, Brett Andrew Tounge, Kristi Anne Leonard, Yan Zhang, Aihua Wang, Michael Hawkins, Umar S.M. Maharoof, Joseph Kent Barbay
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Publication number: 20120129870Abstract: The present invention is directed to piperidinyl and piperazinyl derivatives of formula (II) useful as inhibitors of the NPY Y2 receptor, pharmaceutical compositions comprising said compounds, processes for the preparation of said compounds and the use of said compounds for the treatment and/or prevention of disorders, diseases and conditions mediated by the NPY Y2 receptor.Type: ApplicationFiled: December 17, 2008Publication date: May 24, 2012Inventors: Wenying Chai, Jill A. Jablonowski, Dale A. Rudolph, Chandravadan R. Shah, Devin M. Swanson, Victoria D. Wong
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Publication number: 20120129872Abstract: This invention relates to thiazole I and its therapeutic and prophylactic uses, wherein the variables A, Q, J, R1, R3, and R5 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.Type: ApplicationFiled: November 16, 2011Publication date: May 24, 2012Inventors: Kristi Anne Leonard, Yan Zhang, Brett Andrew Tounge, Aihua Wang, Michael Hawkins, Paul Francis Jackson, Joseph Kent Barbay, Umar S.M. Maharoof
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Publication number: 20120114600Abstract: The invention provides compounds of formula (I): wherein the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are inhibitors of replication of the hepatitis C virus. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat hepatitis C viral infections, and processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: November 3, 2011Publication date: May 10, 2012Applicant: THERAVANCE, INC.Inventors: Robert Murray McKINNELL, Daniel D. LONG, Lori Jean VAN ORDEN, Lan JIANG, Mandy LOO, Daisuke Roland SAITO, Shella ZIPFEL, Eric L. Stangeland, Kassandra Lepack, Gavin Ogawa
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Patent number: 8173645Abstract: Compounds are provided for use with glucokinase that comprise the formula: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: GrantFiled: March 20, 2008Date of Patent: May 8, 2012Assignee: Takeda San Diego, Inc.Inventors: Zacharia Cheruvallath, Jun Feng, Prasuna Guntupalli, Stephen L. Gwaltney, Joanne Miura, Mark Sabat, Mingnam Tang
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Publication number: 20120108565Abstract: The present invention provides DNA Gyrase and/or Topo IV inhibitors of Formula (I), which can be used as antibacterial agents. Compounds disclosed herein can be used for treating or preventing conditions caused by or contributed by gram positive, gram negative and anaerobic bacteria, more particularly against, for example, Staphylococci, Streptococci, Enterococci, Haemophilus, Pseudomonus spp., Acenetobacter spp., Mvraxalla spp., Chlamydia spp., Mycoplasma spp., Legionella spp., Mycobacterium spp., Helicobacter, Clostridium spp., Bacteroides spp., Cotynebacterium, Bacillus spp., Enterobactericeae (E. coli, Klebsiella spp., Proteus spp., etc.) or any combination thereof. Also provided, are processes for preparing compounds disclosed herein, pharmaceutical compositions containing compounds disclosed herein, and methods of treating bacterial infections.Type: ApplicationFiled: July 30, 2009Publication date: May 3, 2012Inventors: Lalima Sharma, Jitendra A. Sattigeri, Narest Kumar, Ajay Yadav, Rijwan Momim, Shahadat Ahmed, Ian A. Cliffe, Pradip Kumar Bhatnagar, Sanjay Ghosh, V. Samuel Raj, Dilip J. Upadhyay
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Publication number: 20120108591Abstract: A new class of alkylsulfinyl thiazolides is described. These compounds show strong activity against hepatitis viruses.Type: ApplicationFiled: October 28, 2011Publication date: May 3, 2012Inventors: J. Edward Semple, Jean-Francois Rossignol
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Patent number: 8163746Abstract: Provided is an agent for treating or preventing urinary frequency, urinary urgency and urinary, incontinence which are associated with overactive bladder, a lower urinary tract disease such as interstitial cystitis and chronic prostatitis accompanied by lower urinary tract pain, and various diseases accompanied by pain. A novel azolecarboxamide derivative in which an azole ring such as thioazole or oxazole is bonded to a benzene ring, pyridine ring or pyrimidine ring through carboxamide was confirmed to have a potent trkA receptor-inhibitory activity and found to be an agent for treating or preventing lower urinary tract disease and various diseases accompanied by pain, which is excellent in efficacy and safety, and thus the present invention was accomplished.Type: GrantFiled: April 19, 2007Date of Patent: April 24, 2012Assignee: Astellas Pharma Inc.Inventors: Keizo Sugasawa, Kenichi Kawaguchi, Takaho Matsuzawa, Ryushi Seo, Hironori Harada, Akira Suga, Tomoaki Abe, Hidenori Azami, Shunichiro Matsumoto, Takashi Shin, Masayuki Tanahashi, Toru Watanabe
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Publication number: 20120083490Abstract: The present invention features compounds of formula I or pharmaceutically acceptable salts, solvates or prodrugs thereof, and methods of using the same to inhibit the metabolizing activities of CYP enzymes. The present invention also features methods of using these compounds, salts, solvates or prodrugs to improve the pharmacokinetics of drugs that are metabolized by CYP enzymes.Type: ApplicationFiled: December 8, 2011Publication date: April 5, 2012Applicant: ABBOTT LABORATORIESInventors: Larry L. Klein, Hui-Ju Chen, Ming C. Yeung, Charles A. Flentge, John T. Randolph, Peggy P. Huang, Douglas K. Hutchinson, Dale J. Kempf
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Patent number: 8148367Abstract: Disclosed are compounds, pharmaceutical compositions, kits, articles of manufacture, methods of using, and methods of preparing compounds having the formula: wherein the variables are as defined herein. The disclosed compounds are inhibitors of Renin.Type: GrantFiled: January 9, 2008Date of Patent: April 3, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Lily Kwok, Betty Lam, Zhe Li, Zhiyuan Zhang
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Patent number: 8148541Abstract: Disclosed herein are rhodanine derivatives, a method for the preparation thereof, and a pharmaceutical composition containing the same. The rhodanine derivatives have inhibitory activity against protein phosphatases (PPase) such as PTP1B, Prl-3, LAR, CD45, Cdc25A, Cdc25B, Cdc25C, Yop, PP1 and VHR, and can be applied for the prevention and treatment of PPase-caused diseases, including autoimmune diseases, diabetes, impaired glucose intolerance, insulin resistance, obesity, cancers, etc. when the inhibitory activity thereof is modulated.Type: GrantFiled: December 8, 2006Date of Patent: April 3, 2012Assignee: Korea Research Institute of Bioscience and BiotechnologyInventors: Seong Eon Ryu, Seung Jun Kim, Dae Gwin Jeong, Sang Hyeup Lee, Suk Kyeong Jung, Hwan Mook Kim, Song Kyu Park, Ki Ho Lee, Chang Woo Lee, Joong-Kwon Choi, Jin Hee Ahn
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Publication number: 20120077975Abstract: The present disclosure relates to compounds effective as human protein tyrosine phosphatase beta (HPTP-?) inhibitors thereby regulating angiogenesis. The present disclosure further relates to compositions comprising said human protein tyrosine phosphatase beta (HPTP-?) inhibitors, and to methods for regulating angiogenesis.Type: ApplicationFiled: December 1, 2011Publication date: March 29, 2012Inventors: Jeffrey Lyle Gray, Kande K. D. Amarasinghe, Cynthia Monesa Clark, Ryan Matthew Nichols, Matthew B. Maier
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Patent number: 8133889Abstract: Compounds of formula (I): wherein: m and n represent 1 or 2, A represents a pyrrolyl group, X represents a C(O), S(O) or SO2 group, R1 and R2 represent an alkyl group or, together with the nitrogen atom carrying them, form a heterocyclic group, R3 and R4, together with the atoms carrying them, form a heterocyclic group, R5 represents a hydrogen atom or an alkyl group, R6 represents a hydrogen atom or a halogen atom. Medicinal products containing the same which are useful in treating cancer.Type: GrantFiled: August 4, 2010Date of Patent: March 13, 2012Assignee: Les Laboratoires ServierInventors: Jean-Claude Ortuno, Alexis Cordi, Jean-Michel Lacoste, Vincent Lacoste, legal representative, Pauline Lacoste, legal representative, Imre Fejes, Michael Burbridge, John Hickman, Alain Pierre
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Patent number: 8129389Abstract: The invention relates to novel oxindole derivatives of general formula (I), in which the substituents A, B, R1, R2 and R3 are defined as cited in claim 1, to medicaments containing said derivatives and to the use of the latter for the prophylaxis and/or treatment of vasopressin-dependent and/or oxytocin-dependent diseases.Type: GrantFiled: March 23, 2006Date of Patent: March 6, 2012Assignee: Abbott GmbH & Co. KGInventors: Wilfried Lubisch, Thorsten Oost, Wolfgang Wernet, Wilfried Hornberger, Liliane Unger, Hervé Geneste
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Publication number: 20120053149Abstract: The present invention relates to thiazole derivatives of formula I and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.Type: ApplicationFiled: April 21, 2010Publication date: March 1, 2012Inventors: Eva Caroff, Kurt Hilpert, Francis Hubler, David Lehmann, Emmanuel Meyer, Dorte Renneberg
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Publication number: 20120046286Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): And salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.Type: ApplicationFiled: April 28, 2010Publication date: February 23, 2012Inventors: Julie Nicole Hamblin, Paul Spencer Jones, Suzanne Elaine Keeling, Joelle Le, Charlotte Jane Mitchell, Nigel James Parr
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Patent number: 8119812Abstract: An object of the present invention is to provide thiazolidinone derivatives. More specifically, an object of the present invention is to provide novel compounds having a CDC7 inhibitory action. The present invention provides thiazolidinone derivatives represented by the formula (I) The compounds of the present invention inhibit the CDC7 protein kinase activity, and suppress cell proliferation.Type: GrantFiled: April 19, 2010Date of Patent: February 21, 2012Assignees: SBI Biotech Co., Ltd., Crystalgenomics, Inc.Inventors: Takayuki Irie, Masaaki Sawa, Sayuri Ito, Chika Tanaka, Seong Gu Ro, Choul Hong Park
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Patent number: 8119626Abstract: 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: GrantFiled: November 20, 2008Date of Patent: February 21, 2012Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Kazutoshi Sugawara, Tetsuji Matsudaira, Hiroshi Sugama, Masao Nawano, Rikiya Ohashi
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Publication number: 20120028990Abstract: A 3-aryl or heteroaryl-substituted indole derivative which is effective as a preventive or remedy for various diseases is provided. [Means for Resolution] A compound represented by a formula (I) or a pharmaceutically acceptable salt thereof is provided. In the formula, R1 represents a hydrogen atom, C1-6 alkyl et al; R2 represents a hydrogen atom, C1-6 alkyl et al; Z represents aryl or heteroaryl (with the proviso that imidazolyl is excluded); and W represents a group represented by the formula (w-1) or (w-2). In the formula, R3 represents C1-6 alkyl et al; Yl and Y2 both represent a hydrogen atom or Y1 and Y2 together form —CH2-CH2-; Q represents CH or N; Ar represents phenyl, furyl et al; R4 and R5 each independently represent a hydrogen atom or C1-6 alkyl or R4 and R5 together with the nitrogen atom form pyrrolidine et al.Type: ApplicationFiled: April 14, 2010Publication date: February 2, 2012Inventors: Takashi Fujimura, Hiroyuki Kishino, Takashi Mizutani, Shunji Sakuraba, Takahide Sasaki, Nagaaki Sato
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Publication number: 20120028920Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.Type: ApplicationFiled: October 11, 2011Publication date: February 2, 2012Inventors: Hiroshi YAMASHITA, Hideaki Kuroda, Nobuaki Ito, Shin Miyamura, Kunio Oshima, Jun Matsubara, Haruka Takahashi, Tae Fukushima, Satoshi Shimizu, Kazumi Kondo, Yohji Sakurai, Takeshi Kuroda, Shinichi Taira, Motohiro Itotani, Tatsuyoshi Tanaka
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Publication number: 20120022078Abstract: A novel aryl indole derivative is provided that is effective as a preventive or remedy for various diseases. A compound represented by a formula (I) or a pharmaceutically acceptable salt thereof: (I) wherein R1 is a hydrogen atom, halogen, C1-6alkyl, haloC1-6alkyl, C1-6alkyloxy, or haloC1-6alkyloxy; R2 represents C1-6alkyl or haloC1-6alkyl; R3 represents a hydrogen atom, C1-6alkyl, or haloC1-6alkyl; and Ar represents an aryl or heteroaryl, wherein the aryl or the heteroaryl may be substituted with 1 to 3 substituents such as halogen, C1-6alkyl, haloC1-6alkyl, and C1-6alkyloxy.Type: ApplicationFiled: April 7, 2010Publication date: January 26, 2012Applicant: MSD K.K.Inventors: Hiroyuki Kishino, Sayaka Mizutani, Shunji Sakuraba, Nagaaki Sato
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Patent number: 8101618Abstract: A compound represented by the formula (I): or a pharmaceutically acceptable salt thereof, wherein: R1 represents a branched lower alkyl group having from 3 to 9 carbon atoms or the like; R2 represents a 6-membered heteroaryl group having 1 or 2 nitrogen atoms or the like; R3 represents a hydrogen atom, an alkanoylamino group or the like; R4 represents a hydrogen atom, a lower alkyl group or the like; X1 represents an oxygen atom or a sulfur atom; X2 represents an oxygen atom or a single bond; and m indicates an integer of from 0 to 4. This compound has a metabotropic glutamate receptor 1 inhibitory effect, and therefore is useful for the treatment of a brain disorder such as convulsion, acute pain, inflammatory pain, chronic pain, cerebral infraction or transient cerebral ischemic attack, a mental dysfunction such as schizophrenia, and a disease such as anxiety and drug addition.Type: GrantFiled: April 5, 2006Date of Patent: January 24, 2012Assignee: MSD K.K.Inventors: Hiroshi Kawamoto, Toshifumi Kimura, Hisashi Ohta, Akio Sato, Atsushi Satoh, Gentaroh Suzuki
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Publication number: 20120015958Abstract: The present invention relates to 1-(4-ureidobenzoyl)piperazine derivatives having the general Formula I (We bring to your attention that formula I is not provided on this electronic version as it is provided in the abstract of the paper copy) Wherein R1 is (C1-8)alkyl, (C3-8)cycloalkyl or (C3-8)cycloalkyl(C1-3)alkyl, each of which may be substituted by hydroxy, cyano or halogen; R2 represents 1 or 2 optional halogens; R3 is (C1-6)alkyl, (C3-6)cycloalkyl or (C3-6)cycloalkyl(C1-3)alkyl, each of which may be substituted by one or more halogens; A represents a heteroaryl ring system comprising 1-3 heteroatoms selected from N, O and S, which ring system is 5- or 6-membered when X is C, and 5-membered when X is N; n is 1 or 2; or a pharmaceutically acceptable salt thereof; to pharmaceutical compositions comprising the same, and to the use of a these 1-(4-ureidobenzoyl)piperazine derivatives for the manufacture of a medicament for treating or preventing atherosclerosis and related disorders associated with cholesterType: ApplicationFiled: August 26, 2009Publication date: January 19, 2012Inventors: Andrew John Cooke, David Jonathan Bennett, Andrew Stanley Edwards, Andrew Laird Roughton, Irina Neagu, Jui-Hsiang Chan, Koc Kan Ho, Nasrin Ansari, Michelle Lee Morris, Yajing Rong, Michael Ohlmeyer
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Publication number: 20120015957Abstract: The present invention is directed to piperidinyl and piperazinyl derivatives of formula (I) useful as inhibitors of the NPY Y2 receptor, pharmaceutical compositions comprising said compounds, processes for the preparation of said compounds and the use of said compounds for the treatment and/or prevention of disorders, diseases and conditions mediated by the NPY Y2 receptor.Type: ApplicationFiled: December 17, 2008Publication date: January 19, 2012Inventors: Wenying Chai, Curt A. Dvorak, Jill A. Jablonowski, Dale A. Rudolph, Chandravadan R. Shah, Victoria D. Wong
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Publication number: 20120015159Abstract: Cyclic carbamate functional compounds, which are the reaction product of a cyclic carbamate having an acrylate functional group, such as N-(2-acryloyloxyethyl)oxazolidinone, with aliphatic amine compounds, said cyclic carbamate functional compounds being useful as oxygen scavengers in energy-curable compositions, such as inks, coatings and adhesives, that comprise (a) the cyclic carbamate functional compound, (b) reactive monomers and/or oligomers and, optionally, (c) a photoinitiator.Type: ApplicationFiled: March 11, 2010Publication date: January 19, 2012Applicant: Sun Chemical B.V.Inventors: Shaun Herlihy, Brian Rowatt
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Publication number: 20120010200Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.Type: ApplicationFiled: September 22, 2011Publication date: January 12, 2012Inventors: Jiacheng Zhou, Ashoke Bhattacharjee, Shili Chen, Yi Chen, Jay J. Farmer, Joel A. Goldberg, Roger Hanselmann, Rongliang Lou, Alia Orbin, Adegboyega K. Oyelere, Joseph M. Salvino, Dane M. Springer, Jennifer Tran, Deping Wang, Yusheng Wu
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Publication number: 20120004213Abstract: The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.Type: ApplicationFiled: September 15, 2011Publication date: January 5, 2012Applicant: FOREST LABORATORIES HOLDINGS LIMITEDInventors: Kumar SUNDARESAN, Sandeep N. RAIKAR, Srinivasa Raju SAMMETA, Ganesh PRABHU, Hosahalli SUBRAMANYA, Alexander BISCHOFF
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Publication number: 20110319448Abstract: The invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein R1-3, R5-7, a, X, Y, Y?, Y?, and Z are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.Type: ApplicationFiled: September 9, 2011Publication date: December 29, 2011Applicant: THERAVANCE, INC.Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
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Publication number: 20110312969Abstract: Compounds of general formula (I): wherein R1, R2, R3, R4, R5, R6, X and Y are as defined herein are inhibitors of Bcl-2 and are useful for treating diseases characterised by abnormal cell growth and/or dysregulated apoptosis.Type: ApplicationFiled: December 8, 2009Publication date: December 22, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Stephen Peter East, Mark Whittaker, Osamu Ichihara, Adrian Kotei Kotei, Smantha Jayne Bamford
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Publication number: 20110306620Abstract: Heteroarylpiperidine and -piperazine derivatives of the formula (I), in which the symbols have the meanings given in the description and agrochemically active salts thereof and their use for controlling phytopathogenic harmful fungi and also processes for preparing compounds of the formula (I).Type: ApplicationFiled: October 27, 2010Publication date: December 15, 2011Applicant: Bayer CropScience AGInventors: Pierre Cristau, Nicola Rahn, Tomoki Tsuchiya, Joachim Kluth, Pierre Wasnaire, Sebastian Hoffmann, JĂĽrgen Benting, Ulrike Wachendorff-Neumann, Thomas Seitz
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Publication number: 20110301149Abstract: The present invention provides compounds which antagonize epsilon protein kinase C (PKC?). These compounds have a structural formula (Ia), (Ic) or (II). The present invention also provides pharmaceutical compositions containing these compounds and methods of treating various diseases, conditions, and/or symptoms by using these compounds.Type: ApplicationFiled: October 12, 2009Publication date: December 8, 2011Applicant: VM DISCOVERY INC.Inventor: Jay Jie-Qiang Wu
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Publication number: 20110301143Abstract: Heterocyclic compounds of structural formula (I), or a pharmaceutically acceptable salt thereof, wherein W is a R1— substituted heteroaryl, R1 is an heteroaryl ring substituted with an ester or carboxylic acid containing radical, X-T is N—CR5R6, C?CR5 or CR13—CR5R6, Y is a bond or —C(O)—, a and b represent an integer selected from 1 to 4, and Ar is an optionally substituted phenyl or naphtyl, are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD) The heterocyclic compounds 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, cancer, liver steatosis, and non-alcoholic steatohepatitis.Type: ApplicationFiled: February 18, 2010Publication date: December 8, 2011Inventors: Elise Isabel, Nicolas Lachance, Jean-Philippe Leclerc, Serge Leger, Renata M. Oballa, David Powell, Yeeman K. Ramtohul, Patrick Roy, Geoffrey K. Tranmer, Renee Aspiotis, Lianhai Li, Evelyn Martins
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Patent number: 8071600Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.Type: GrantFiled: August 31, 2006Date of Patent: December 6, 2011Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hiroshi Yamashita, Hideaki Kuroda, Nobuaki Ito, Shin Miyamura, Kunio Oshima, Jun Matsubara, Haruka Takahashi, Tae Fukushima, Satoshi Shimizu, Kazumi Kondo, Yohji Sakurai, Takeshi Kuroda, Shinichi Taira, Motohiro Itotani, Tatsuyoshi Tanaka
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Publication number: 20110294780Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: ApplicationFiled: May 24, 2011Publication date: December 1, 2011Inventors: Gilles Bignan, Wing Cheung, Micheal Gaul, Hui Huang, Xun Li, Raymond Patch, Sharmila Patel, Mark Player, Guozhang Xu, Bao-Ping Zhao, Jian Liu
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Publication number: 20110294813Abstract: Disclosed is a compound which is useful as an 11?-hydroxysteroid dehydrogenase type 1 inhibitor. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein R1 is optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted heterocycle or optionally substituted heterocyclealkyl, X is —O—, —NR3—, —NR3C(?O)— or —NR3S(?O)2—, R2 is optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl, R3 is hydrogen or optionally substituted alkyl.Type: ApplicationFiled: June 30, 2011Publication date: December 1, 2011Applicants: SHIONOGI & CO., LTD., INSTITUTE OF MEDICINAL MOLECULAR DESIGN, INC.Inventors: Akiko Itai, Susumu Muto, Ryuko Tokuyama, Hiroshi Fukasawa, Takeshi Yanase
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Publication number: 20110288083Abstract: The present invention relates to a method of identifying compounds useful in inhibiting protein kinase-like endoplasmic reticulum protein kinase (PERK). The method comprises providing a first model comprising PERK active domains, where the said active domains are selected from the group consisting of the peptide spanning from amino acid residue Asp144 to amino acid residue Ser191 of SEQ ID NO: 1 and a peptide comprising the amino acid residue at position 7 of SEQ ID NO: 1, providing one or more candidate compounds, evaluating contact between the candidate compounds and the first model to determine which of the one or more candidate compounds have an ability to bind to and/or fit in the first model, and identifying the compounds which, based on said evaluating, have the ability to bind to and/or fit in the first model as compounds potentially useful for inhibiting PERK.Type: ApplicationFiled: May 19, 2011Publication date: November 24, 2011Applicant: NEW YORK UNIVERSITYInventors: Timothy CARDOZO, Hong WANG, David Ron
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Publication number: 20110282058Abstract: The present invention provides 3-{(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl}thiazolidine (compound I) useful as a dipeptidyl peptidase-IV inhibitor, which has superior properties of stability and hygroscopicity, and reproducible crystal structure, and a production method thereof.Type: ApplicationFiled: July 29, 2011Publication date: November 17, 2011Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Tomohiro YOSHIDA, Hiroshi SAKASHITA, Naoko UEDA, Shinji KIRIHARA, Satoru UEMORI, Reiko TSUTSUMIUCHI, Fumihiko AKAHOSHI
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Patent number: 8058299Abstract: 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. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.Type: GrantFiled: May 1, 2008Date of Patent: November 15, 2011Assignee: VIA Pharmaceuticals, Inc.Inventors: David Robert Bolin, Adrian Wai-Hing Cheung, Fariborz Firooznia, Matthew Michael Hamilton, Lee Apostle McDermott, Yimin Qian, Jenny Tan, Weiya Yun
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Publication number: 20110275636Abstract: Disclosed herein are new compounds of desazadesferrothiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity.Type: ApplicationFiled: May 4, 2011Publication date: November 10, 2011Applicant: FerroKin BioSciences, Inc.Inventor: James Malecha
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Patent number: 8053436Abstract: The present invention is related to piperazine derivatives of carbazole of formula (I) notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such piperazine derivatives of carbazole. Said piperazine derivatives of carbazole are efficient modulators, in particular efficient inhibitors, of the Bax function and/or activation. The present invention is furthermore related to novel piperazine derivatives of carbazole as well as methods of their preparation.Type: GrantFiled: October 18, 2000Date of Patent: November 8, 2011Assignee: Merck Serono SAInventors: Serge Halazy, Dennis Church, Bruno Antonsson, Agnes Bombrun, Patrick Gerber, Jean-Claude Martinou
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Publication number: 20110263571Abstract: Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis. An amide derivative represented by the following formula (I) wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, or a hydrate or solvate thereof.Type: ApplicationFiled: October 27, 2009Publication date: October 27, 2011Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Seigo Ishibuchi, Hidemasa Hikawa, Akiko Tarao, Jun-ichi Endoh, Kunitomo Adachi, Kazuhiro Maeda, Kaoru Tashiro
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Patent number: 8044079Abstract: The invention relates to novel oxindole derivative of general formula (I), wherein the substituents R1, R2, A, B, and Y are defined as in Claim 1. The invention further relates to medicaments containing said derivatives, and use thereof for the prevention and/or treatment of vasopressin-dependent diseases.Type: GrantFiled: December 1, 2006Date of Patent: October 25, 2011Assignee: Abbott GmbH & Co. KGInventors: Thorsten Oost, Wilfried Lubisch, Wolfgang Wernet, Wilfried Hornberger, Liliane Unger, Herve Geneste, Astrid Netz
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Patent number: 8039463Abstract: The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.Type: GrantFiled: March 20, 2009Date of Patent: October 18, 2011Assignee: Forest Laboratories Holdings LimitedInventors: Kumar Sundaresan, Sandeep N. Raikar, Srinivasa Raju Sammeta, Ganesh Prabhu, Hosahalli Subramanya, Alexander Bischoff
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Publication number: 20110251176Abstract: Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is a thiazolyl, picolinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: April 6, 2011Publication date: October 13, 2011Inventor: Xiaojing Wang
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Publication number: 20110224211Abstract: Disclosed are compounds, stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, their preparation, use, and compositions thereof for treating an infection mediated at least in part by a virus in the Flaviviridae family of viruses.Type: ApplicationFiled: November 19, 2009Publication date: September 15, 2011Inventors: Frank Ulrich Schmitz, Roopa Rai, Christopher Ron Roberts, Wieslaw Kazmierski, Richard Grimes
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Publication number: 20110218182Abstract: The invention relates to chemical compounds of formula (I), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of PIM-1 and/or PIM-2, and/or PIM-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of PIM kinase related conditions and diseases, preferably cancer.Type: ApplicationFiled: July 2, 2009Publication date: September 8, 2011Applicant: ASTRAZENECA ABInventors: Leslie Dakin, James Edward Dowling, Michelle Lamb, Jon Read, Qibin Su, Xiaolan Zheng
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Patent number: 8008302Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof, in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.Type: GrantFiled: July 25, 2005Date of Patent: August 30, 2011Assignee: Merck Serono SAInventors: Dominique Swinnen, Agnes Bombrun, Jerome Gonzalez, Stefano Crosignani, Patrick Gerber, Catherine Jorand-Lebrun
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Patent number: 8003790Abstract: The present invention provides 3-{(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl}thiazolidine (compound I) useful as a dipeptidyl peptidase-IV inhibitor, which has superior properties of stability and hygroscopicity, and reproducible crystal structure, and a production method thereof.Type: GrantFiled: February 17, 2006Date of Patent: August 23, 2011Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Tomohiro Yoshida, Hiroshi Sakashita, Naoko Ueda, Shinji Kirihara, Satoru Uemori, Reiko Tsutsumiuchi, Fumihiko Akahoshi
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Publication number: 20110200586Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: ApplicationFiled: February 16, 2011Publication date: August 18, 2011Inventors: Gilles BIGNAN, Micheal Gaul, Guozhang Xu, Bao-Ping Zhao