1,3-thiazoles (including Hydrogenated) Patents (Class 546/269.7)
Polycyclo ring system having the 1,3-thiazole ring as one of the cyclos (Class 546/270.1)
1,3-thiazole ring bonded directly to the six-membered hetero ring (Class 546/270.4)
Nitrogen attached directly to the 1,3-thiazole ring by nonionic bonding (Class 546/270.7)
  • INDOLE COMPOUNDS BEARING ARYL OR HETEROARYL GROUPS HAVING SPHINGOSINE-1-PHOSPHATE (S1P) RECEPTOR BIOLOGICAL ACTIVITY
    Publication number: 20110275677
    Abstract: The invention provides well-defined aryl and/or heteroaryl substituted indoles that are useful as sphingosine-1-phosphate agonists or antagonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: January 3, 2011
    Publication date: November 10, 2011
    Applicant: ALLERGAN, INC.
    Inventors: Richard L. Beard, Haiqing Yuan, John E. Donello
  • Benzophenone derivatives useful for inhibiting formation of microtubule
    Patent number: 8053439
    Abstract: Disclosed herein are novel benzophenone derivatives represented by formula I, a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof, a pharmacological composition containing the same, and a use of the composition as therapeutic drugs. The benzophenone derivatives have an inhibition activity of microtubule formation and can be used to treat a normal proliferative state of a malignant tumor by killing the actively proliferating cells.
    Type: Grant
    Filed: September 21, 2007
    Date of Patent: November 8, 2011
    Assignee: Chong Kun Dang Pharmaceutical Corp.
    Inventors: Nam-Song Choi, Young-Mi Kim, Young-Hoon Kim, Jae-Kwang Lee, In-Taek Lim, Ho-Jin Choi, Hyun-Mo Yang, Seung-Kee Moon, Soo-Jin Kim, Hyun-Jung Yu, Jae-Su Shin, Young-Min Kwon, Sung-Sook Lee, Soon-Kil Ahn, Sun-Ju Kong
  • HETEROCYCLIC COMPOUNDS AS PHOSPHODIESTERASE INHIBITORS
    Publication number: 20110269753
    Abstract: Compounds of the formula (I), their derivatives, analogs, tautomeric forms, regioisomers, stereoisomers, polymorphs, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, N-oxides, metabolites and prodrugs thereof. These compounds are phosphodiesterase type 4 (PDE4) inhibitors. They are useful in the treatment of a variety of allergic or inflammatory diseases including asthma, COPD, chronic bronchitis, atopic dermatitis, allergic rhinitis, allergic conjunctivitis, vernal conjunctivitis, psoriasis, rheumatoid arthritis, ulcerative colitis, Crohn's disease, uveitis, NASH and lupus.
    Type: Application
    Filed: January 21, 2010
    Publication date: November 3, 2011
    Applicant: ORCHID RESEARCH LABORATORIES LTD.
    Inventors: Gopalan Balasubramanian, Sukunath Narayanan, Ganapavarapu Veera Raghava Sharma, Lavanya Andiappan, Shridhar Narayanan, Sanjeev Saxena, Sridharan Rajagopal, Santosh Lolaknath Vishwakarma, Saravanan Thirunavukkarasu
  • NOVEL THIAZOLIDINEDIONE DERIVATIVE AND USE THEREOF
    Publication number: 20110269954
    Abstract: The present invention relates to novel thiazolidinedione derivatives expressed by the following formula (I) and the uses thereof. More specifically, the present invention relates to novel thiazolidinedione derivatives expressed by the following formula (I) and a pharmaceutical composition comprising the same. The novel thiazolidinedione derivatives of formula (I) according to the present invention can be effectively used for the prevention or treatment of cardiovascular disease, gastrointestinal disease and renal disease by inhibiting the activity of 15-hydroxyprostaglandin dehydrogenase (15-PGDH) that decomposes prostaglandins as well as useful for the prevention of hair loss and the stimulation of hair growth, and osteogenic stimulation and wound healing.
    Type: Application
    Filed: December 30, 2009
    Publication date: November 3, 2011
    Inventors: Hoon Cho, Ying Wu, Cheol-Hee Choi
  • PYRIDINE, BICYCLIC PYRIDINE AND RELATED ANALOGS AS SIRTUIN MODULATORS
    Publication number: 20110263564
    Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
    Type: Application
    Filed: October 29, 2009
    Publication date: October 27, 2011
    Applicant: Sirtris Pharmaceuticals, Inc.
    Inventors: Radha Narayan, Jeremy S. Disch, Robert B. Perni, Chi B. Vu
  • CHROMENONE ANALOGS AS SIRTUIN MODULATORS
    Publication number: 20110257174
    Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
    Type: Application
    Filed: September 29, 2009
    Publication date: October 20, 2011
    Applicant: Sirtris Pharmaceuticals, Inc.
    Inventors: Christopher Oalmann, Robert B. Perni, Chi B. Vu
  • Calcium channel antagonists
    Patent number: 8034954
    Abstract: The present invention provides novel calcium channel antagonists, and methods of treating disease sates using the novel antagonists.
    Type: Grant
    Filed: December 20, 2006
    Date of Patent: October 11, 2011
    Assignee: Icagen, Inc.
    Inventors: Gregory J. Pacofsky, Mark J. Suto, Paul Christopher Fritch
  • 2-HETEROARYL-PYRROLO[3,4-C]PYRROLE DERIVATIVES AND THEIR USE AS SCD
    Publication number: 20110245263
    Abstract: The invention relates to heterocyclic derivatives of formula I wherein R, R1, A, B, D, M, L and n are as defined herein, or their physiologically compatible salts, their pharmaceutical compositions and their uses as SCD1 inhibitors.
    Type: Application
    Filed: June 15, 2011
    Publication date: October 6, 2011
    Applicant: SANOFI-AVENTIS
    Inventors: Gerhard Zoller, Marc Dietrich Voss, Stefanie Keil, Andreas Herling, Hans Matter
  • Imidazole derivatives for the treatment of anxiety and related diseases
    Patent number: 8030339
    Abstract: This invention relates to novel imidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex, and in particular for combating anxiety and related diseases.
    Type: Grant
    Filed: October 12, 2006
    Date of Patent: October 4, 2011
    Assignee: Neurosearch A/S
    Inventors: William Dalby Brown, Janus S. Larsen, Lene Teuber, David Tristram Brown, Philip K. Ahring, Naheed Mirza, Elsebet Østergaard Nielsen
  • GUANIDINE COMPOUNDS, AND USE THEREOF AS BINDING PARTNERS FOR 5-HT5 RECEPTORS
    Publication number: 20110237589
    Abstract: The present invention relates to guanidine compounds of the general formula I corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof. The present compound further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors for the treatment of diseases which are modulated by a 5-HT5 receptor activity, in particular for the treatment of neurodegenerative and neuropsychiatric disorders as well as the associated signs, symptoms and dysfunctions.
    Type: Application
    Filed: February 4, 2011
    Publication date: September 29, 2011
    Inventors: Astrid Netz, Wilhelm Amberg, Udo Lange, Michael Ochse, Charles W. Hutchins, Francisco-Xavier Garcia-Ladona, Wolfgang Wernet, Andreas Kling, Andrea Hager-Wernet
  • CARBOXYLIC ACID DERIVATIVE CONTAINING THIAZOLE RING AND PHARMACEUTICAL USE THEREOF
    Publication number: 20110237630
    Abstract: A compound represented by the formula (I) wherein R1 and R2 are each a hydrogen atom, an alkyl group and the like, R3 is a hydrogen atom, an alkyl group and the like, R4 is a hydrogen atom, an alkyl group and the like, m is an integer of 0 to 3, X is a bond, an oxygen atom or a sulfur atom, Y is a carbonyl group, a hydroxymethylene group and the like, and Z is a halogen atom, an alkyl group, an aryl group, a heteroaryl group and the like, or a pharmaceutically acceptable salt thereof has a superior PPAR? agonist action and a lipid-lowering action, and is useful as a prophylactic or therapeutic drug for hyperlipidemia and the like.
    Type: Application
    Filed: December 1, 2009
    Publication date: September 29, 2011
    Inventor: Naoko Ando
  • Carboxylic acid derivative containing thiazole ring and pharmaceutical use thereof
    Patent number: 8026370
    Abstract: According to the present invention, a compound represented by the following formula (I) having a superior PPAR? agonist action and concurrently showing a hypolipidemic action can be provided, and further, a compound useful as a synthetic intermediate for the compound can be provided.
    Type: Grant
    Filed: November 4, 2005
    Date of Patent: September 27, 2011
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Takashi Tozawa, Osamu Tsuruta, Hiroshi Kitajima, Yoshiyuki Aoki, Naoko Ando, Hiroki Tamakawa
  • FLAVIVIRUS INHIBITORS AND METHODS FOR THEIR USE
    Publication number: 20110224207
    Abstract: Methods of treating, preventing, and/or ameliorating a Flavivirus infection in a subject are disclosed. The methods comprise administering to the subject a therapeutically effective amount of a Flavivirus inhibitor, e.g., a Flavivirus serine protease inhibitor. These methods are useful in treating, preventing, and/or ameliorating Flavivurs infections such as, for example, West Nile Virus, Dengue Virus, and Japanese Encephalitis Virus.
    Type: Application
    Filed: September 23, 2009
    Publication date: September 15, 2011
    Applicant: GEORGETOWN UNIVERSITY
    Inventors: Radhakrishnan Padmanabhan, Nagarajan Pattabiraman, Niklaus Mueller, Kuppuswamy Nagarajan
  • Compounds and uses thereof in modulating amyloid ?
    Patent number: 8017629
    Abstract: Novel compounds, compositions, and kits are provided. Methods of modulating A? levels, and methods of treating a disease associated with aberrant A? levels are also provided.
    Type: Grant
    Filed: August 23, 2010
    Date of Patent: September 13, 2011
    Assignee: Neurogenetic Pharmaceuticals, Inc.
    Inventors: Soan Cheng, Daniel D. Comer, Long Mao, Guity P. Balow, David Pleynet
  • 5-Phenylthiazole derivatives and their use as p13 kinase inhibitors
    Patent number: 8017608
    Abstract: Compounds of formula I in free or salt form, wherein R1, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating diseases mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
    Type: Grant
    Filed: March 5, 2004
    Date of Patent: September 13, 2011
    Assignee: Novartis AG
    Inventors: Graham Charles Bloomfield, Ian Bruce, Catherine Leblanc, Mrinalini Sachin Oza, Lewis Whithead, Bernard Cuenoud, Thomas Hugo Keller, Louise Kirman, Clive McCarthy, Gaynor Elizabeth Woodward
  • N-(L-ALKYL-2-PHENYLETHYL)-CARBOXAMIDE DERIVATIVES AND USE THEREOF AS FUNGICIDES
    Publication number: 20110207771
    Abstract: Compounds of the formula (I) in which the substituents are as defined in claim 1 are suitable for use as microbiocides.
    Type: Application
    Filed: June 6, 2007
    Publication date: August 25, 2011
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Daniel Stierli, John J. Taylor, Harald Walter, Paul Anthony Worthington, Ramya Rajan
  • SULFONAMIDE COMPOUNDS OR SALTS THEREOF
    Publication number: 20110201616
    Abstract: [Object] A compound which is useful as an EP1 receptor antagonist is provided. [Means for Solution] The present inventors investigated EP1 receptor antagonists, and confirmed that a compound having a sulfonamide structure, in which the nitrogen atom of the sulfonamide structure is substituted with 2-fluoropropyl group, 3-fluoro-2-methylpropyl group or the like, has a potent EP1 receptor antagonistic action, thereby completing the present invention. The sulfonamide compound of the present invention has a potent EP1 receptor antagonistic action and can be used as an agent for preventing and/or treating a lower urinary tract symptom or the like.
    Type: Application
    Filed: June 22, 2009
    Publication date: August 18, 2011
    Applicant: Astellas Pharma Inc.
    Inventors: Hideki Kubota, Issei Tsukamoto, Kazunori Kamijo, Koji Kato, Yuta Fukuda, Hidenori Azami
  • NOVEL ANTIFUNGAL AGENT CONTAINING HETEROCYCLIC COMPOUND
    Publication number: 20110195999
    Abstract: The present invention provides an antifungal agent represented by the formula: wherein A1 represents a 3-pyridyl group which may have a substituent, a quinolyl group which may have a substituent, or the like; X1 represents a group represented by the formula —NH—C(?O)—, a group represented by the formula —C(?O)—NH—, or the like; E represents a furyl group, a thienyl group, a pyrrolyl group, a phenyl group, a pyridyl group, a tetrazolyl group, a thiazolyl group or a pyrazolyl group; with the proviso that A1 may have 1 to 3 substituents, and E has one or two substituents.
    Type: Application
    Filed: March 14, 2011
    Publication date: August 11, 2011
    Inventors: Kazutaka NAKAMOTO, Itaru Tsukada, Keigo Tanaka, Masayuki Matsukura, Toru Haneda, Satoshi Inoue, Norihiro Ueda, Shinya Abe, Katsura Hata, Naoaki Watanabe
  • Coumarin derivatives useful as TNF? inhibitors
    Patent number: 7994318
    Abstract: Novel compounds composition capable of inhibiting TNF? and having antiimmunionflammatory and autoimmune properties useful in a pharmaceutical composition, such as for a drug containing this as an active ingredient; and a therapeutic method with the use of these novel compounds.
    Type: Grant
    Filed: March 18, 2010
    Date of Patent: August 9, 2011
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Jie Fei Cheng, Thomas Arrhenius, David Wallace, Mi Chen, Sovouthy Tith, Hirotaka Kashiwagi, Yoshiyuki Ono, Yoshiaki Watanabe
  • Bicyclic nitrogen-containing heterocyclic compounds
    Patent number: 7994202
    Abstract: 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: Grant
    Filed: July 14, 2009
    Date of Patent: August 9, 2011
    Assignee: Asahi Kasei Pharma Corporation
    Inventors: Masakazu Atobe, Kenji Naganuma, Akifumi Morimoto
  • O-BENZYL NICOTINAMIDE ANALOGS AS MGLUR5 POSITIVE ALLOSTERIC MODULATORS
    Publication number: 20110183980
    Abstract: In one aspect, the invention relates to O-benzyl nicotinamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: September 21, 2010
    Publication date: July 28, 2011
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Charles David Weaver, Shaun Stauffer, Richard Williams, Gregor MacDonald, Ya Zhou, José Manuel Bartolomé-Nebreda
  • DUAL-ACTING THIOPHENE, PYRROLE, THIAZOLE AND FURAN ANTIHYPERTENSIVE AGENTS
    Publication number: 20110178101
    Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: January 18, 2011
    Publication date: July 21, 2011
    Inventors: Paul R. Fatheree, Robert Murray McKinnell
  • BENZPYRAZOL DERIVATIVES AS INHIBITORS OF PI3 KINASES
    Publication number: 20110178063
    Abstract: The invention is directed to certain novel compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.
    Type: Application
    Filed: June 3, 2009
    Publication date: July 21, 2011
    Applicant: GLAXO GROUP LIMITED
    Inventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, John Edward Robinson, Juliet Kay Simpson, Christian Alan Paul Smethurst
  • OXAZOLE DERIVATIVES USEFUL AS INHIBITORS OF FAAH
    Publication number: 20110144119
    Abstract: The present invention is directed to certain oxazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). 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 osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzeimer Disease, and Parkinson's Disease.
    Type: Application
    Filed: July 30, 2009
    Publication date: June 16, 2011
    Inventors: Harry Chobanian, Linus S. Lin, Ping Liu, Marc D. Chioda, Robert J. DeVita, Ravi P. Nargund, Yan Guo
  • DERIVATIVES OF 1-PHENYL-2-PYRIDINYL ALKYL ALCOHOLS AS PHOSPHODIESTERASE INHIBITORS
    Publication number: 20110144070
    Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.
    Type: Application
    Filed: February 22, 2011
    Publication date: June 16, 2011
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventors: Maurizio Delcanale, Elisabetta Armani, Gabriele Amari
  • PRODRUG COMPOUNDS USEFUL AS CANNABINOID LIGANDS
    Publication number: 20110144165
    Abstract: The present invention provides for compounds of formula (I) wherein A2, L2, R1g, R2A, R3A, R4A, R1a, R1b, q1, and z are as defined in the specification, are prodrugs of CB2 receptors ligands and as such are useful in the prevention and treatment of various diseases and conditions including, but not limited to, pain.
    Type: Application
    Filed: December 15, 2010
    Publication date: June 16, 2011
    Applicant: ABBOTT LABORATORIES
    Inventors: Derek W. Nelson, Michael J. Dart, Xueqing Wang, Bo Liu, Teodozyj Kolasa, Meena Patel
  • 2-ALKOXY-SUBSTITUTED DICYANOPYRIDINES AND THEIR USE
    Publication number: 20110136871
    Abstract: The present application relates to novel 2-alkoxy-substituted dicyanopyridines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders.
    Type: Application
    Filed: May 22, 2009
    Publication date: June 9, 2011
    Applicant: BAYER SCHERING AKTIENGESELLSCHAFT
    Inventors: Walter Hübsch, Daniel Meibom, Alexandros Vakalopoulos, Barbara albrecht-Küpper, Peter Nell, Katja Zimmermann, Frank Süssmeier, Joerg Keldenich
  • FUNGICIDAL N-(2-PYRIDYLPROPYL) CARBOXAMIDE DERIVATIVES AND THEIR OXA, AZA AND THIA ANALOGUES
    Publication number: 20110136874
    Abstract: The present invention relates to fungicide N-(2-pyridylpropyl)carboxamide derivative and its oxa, aza and thia analogues of formula (I), their process of preparation and intermediate compound for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions. wherein A, T, W, X, n and Z3 to Z7 represent various substituents.
    Type: Application
    Filed: August 6, 2009
    Publication date: June 9, 2011
    Inventors: Samir Bennabi, Pierre-Yves Coqueron, Philippe Desbordes, Stéphanie Gary, Rachel Rama, Philippe Rinolfi, Jürgen Benting, Peter Dahmen
  • Soluble Guanylate Cyclase Activators
    Publication number: 20110118282
    Abstract: A compound having the structure useful for treatment or prevention of cardiovascular diseases, endothelial dysfunction, diastolic dysfunction, atherosclerosis, hypertension, angina pectoris, thromboses, restenoses, myocardial infarction, strokes, cardiac insufficiency, pulmonary hypertonia, erectile dysfunction, asthma bronchiale, chronic kidney insufficiency, diabetes, or cirrhosis of the liver in a human or animal patient.
    Type: Application
    Filed: September 2, 2008
    Publication date: May 19, 2011
    Inventors: Amy R. Bittner, Christopher Joseph Sinz, Jiang Chang, Ronald M. Kim, J.W. Mirc, Emma R. Parmee, Qiang Tan
  • 4-CARBOXAMIDE INDAZOLE DERIVATIVES USEFUL AS INHIBITORS OF P13-KINASES
    Publication number: 20110112070
    Abstract: 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 P13-kinase activity.
    Type: Application
    Filed: June 3, 2009
    Publication date: May 12, 2011
    Inventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Katherine Louise Jones, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, Christian Alan Paul Smethurst, Yoshiaki Washio
  • NOVEL MODULATORS OF CALCIUM RELEASE-ACTIVATED CALCIUM CHANNEL
    Publication number: 20110105447
    Abstract: Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.
    Type: Application
    Filed: October 6, 2010
    Publication date: May 5, 2011
    Applicants: Incozen Therapeutics Pvt. Ltd., Rhizen Pharmaceuticals SA
    Inventors: Meyyappan Muthuppalaniappan, Srikant Viswanadha, Gayatri S. Merikapudi, Swaroop Kumar V.S. Vakkalanka
  • WATER SOLUBLE SMALL MOLECULE INHIBITORS OF THE CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR
    Publication number: 20110105565
    Abstract: Provided herein are highly water soluble, thiazolidinone derivative compounds and glycine hydrazide derivative compounds that inhibit the ion transport activity of the cystic fibrosis transmembrane conductance regulator (CFTR). The compounds, and compositions comprising the compounds, described herein are useful for treating diseases, disorders, and sequelae of diseases, disorders, and conditions that are associated with aberrantly increased CFTR activity, for example, secretory diarrhea. The compounds may also be used for inhibiting expansion or preventing formation of cysts in persons who have polycystic kidney disease.
    Type: Application
    Filed: March 25, 2009
    Publication date: May 5, 2011
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Alan S. Verkman, Nitin D. Sonawane
  • ORGANIC COMPOUNDS
    Publication number: 20110105530
    Abstract: 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: Application
    Filed: June 25, 2009
    Publication date: May 5, 2011
    Inventors: Natalie Dales, Zaihui Zhang, Jianmin Fu, Duanjie Hou, Shaoyi Sun, Vishnumurthy Kodumuru, Natalia Pokrovskaia
  • THIAZOLE DERIVATIVES
    Publication number: 20110105486
    Abstract: Wherein n is an integer of from 0 to 3; R1A is a 5-membered aromatic heterocyclic group containing at least one oxygen atom; R2A is —COR8 (wherein R8 is aryl); R3A is hydrogen or lower alkyl; and R12 represents cycloalkyl, aryl, aralkyl, alicyclic heterocyclic group, aromatic heterocyclic group, alicyclic hetocyclic-alkyl, or aromatic heterocyclic-alkyl, and R1A, R2A, R3A and R12 are individually optionally substituted.
    Type: Application
    Filed: December 6, 2010
    Publication date: May 5, 2011
    Applicant: KYOWA HAKKO KIRIN CO., LTD.
    Inventors: Takao Nakajima, Masamori Sugawara, Shin-ichi Uchida, Tetsuji Ohno, Yuji Nomoto, Noriaki Uesaka, Yoshisuke Nakasato
  • THIAZOLIDINE COMPOUNDS AS OREXIN RECEPTOR ANTAGONISTS
    Publication number: 20110105491
    Abstract: The invention relates to thiazolidine derivatives of the formula (I) wherein A, B, and R1 are as described in the description, to salts, especially pharmaceutically acceptable salts, of such compounds and to their use as medicaments, especially as orexin receptor antagonists.
    Type: Application
    Filed: July 7, 2009
    Publication date: May 5, 2011
    Inventors: Hamed Aissaoui, Christoph Boss, Julien Hazemann, Ralf Koberstein, Romain Siegrist, Thierry Sifferlen
  • FUSED RING COMPOUNDS AND USE THEREOF
    Publication number: 20110098297
    Abstract: The present invention aims to provide a glucokinase activator useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, obesity and the like. The present invention provides a glucokinase activator containing a compound represented by the formula (I): wherein each symbol is defined in the specification, or a salt thereof or a prodrug thereof.
    Type: Application
    Filed: April 9, 2009
    Publication date: April 28, 2011
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Tsuneo Yasuma, Nobuyuki Takakura
  • Agent for Enhancing Corneal Epithelial Barrier Function
    Publication number: 20110092524
    Abstract: The invention relates to a pharmacological action of a compound which functions as a PPAR? agonist on the barrier function of the corneal epithelium. A PPAR? agonist such as rivoglitazone, DRF-2593, GW-544 or BMS-298585 exhibits an excellent effect of enhancing the corneal epithelial barrier function in a test for enhancement of corneal epithelial barrier function, and therefore is useful as a preventive agent or a therapeutic agent for ocular infection or ocular unidentified complaint caused by a decrease in the corneal epithelial barrier function. Further, the PPAR? agonist can enhance the corneal epithelial barrier function of diabetic patients, patients with decreased corneal epithelial barrier function due to aging and patients who underwent refractive surgery such as PRK (photorefractive keratectomy) or LASIK (laser in situ keratomileusis) or cataract surgery.
    Type: Application
    Filed: February 25, 2009
    Publication date: April 21, 2011
    Applicant: SANTEN PHARMACEUTICAL CO., LTD.
    Inventors: Shin-ichiro Hirai, Atsushi Yoshida
  • ALKYNYL ALCOHOLS AS KINASE INHIBITORS
    Publication number: 20110086834
    Abstract: Selected compounds are effective for prophylaxis and treatment of inflammation and inflammatory disorders, such as NIK-mediated disorders. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, inflammation and the like.
    Type: Application
    Filed: June 26, 2009
    Publication date: April 14, 2011
    Applicant: AMGEN INC.
    Inventors: Guoqing Chen, Timothy D. Cushing, Paul Faulder, Benjamin Fisher, Xiao He, Kexue Li, Zhihong Li, Wen Liu, Lawrence R. Mcgee, Vatee Pattaropong, Jennifer L. Seganish, Youngshook Shin, Zhulun Wang
  • INDOLE DERIVATIVES AS CRAC MODULATORS
    Publication number: 20110071150
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and R4 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with calcium release-activated calcium channels (CRAC).
    Type: Application
    Filed: September 23, 2010
    Publication date: March 24, 2011
    Inventors: Muzaffar Alam, Daisy Joe Du Bois, Ronald Charles Hawley, Joshua Kennedy-Smith, Ana Elena Minatti, Wylie Solang Palmer, Tania Silva, Robert Stephen Wilhelm
  • Indoles and Their Therapeutic Use
    Publication number: 20110071175
    Abstract: Compound of formula (I) are ligands of the CRTH2 receptor, useful inter alia for treatment of inflammatory conditions.
    Type: Application
    Filed: December 12, 2008
    Publication date: March 24, 2011
    Inventors: George Hynd, John Gary Montana, Harry Finch, Rosa Arienzo, Barbara A. Vitabile-Woo, Mathias Domostoj
  • NEW CHEMICAL COMPOUNDS
    Publication number: 20110059938
    Abstract: The present invention encompasses compounds of general formula (1) wherein the groups R2 to R4, L, Q and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
    Type: Application
    Filed: November 15, 2010
    Publication date: March 10, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Steffen STEURER, Peter ETTMAYER, Andreas MANTOULIDIS, Ioannis SAPOUNTZIS, Martin STEEGMAIER
  • RESPIRATORY DISEASE TREATMENT
    Publication number: 20110053986
    Abstract: There is provided a pharmaceutical composition that is adapted for pulmonary administration by inhalation, which composition comprises a glitazone, such as pioglitazone or rosiglitazone, and one or more pharmaceutically acceptable carriers and/or excipients, and wherein the glitazone content of the composition consists of at least 95% by weight of the 5R enantiomer and less than 5% by weight of the 5S enantiomer. There is also provided a use and kit.
    Type: Application
    Filed: August 4, 2010
    Publication date: March 3, 2011
    Inventors: Harry Finch, Craig Fox, Mohammed Sajad, Monique Bodil Van Niel, Andrew Forrest
  • PYRIDYLAMINOACETIC ACID COMPOUND
    Publication number: 20110054172
    Abstract: The present invention provides a novel pyridylaminoacetic acid compound represented by the following formula (1): (wherein R1, R2, R3, Y and Z are as defined in the description and claims), or a pharmacologically acceptable salt thereof. The pyridylaminoacetic acid compound has EP2 agonistic action and is therefore useful as a therapeutic and/or prophylactic agent for respiratory diseases such as asthma or chronic obstructive pulmonary disease.
    Type: Application
    Filed: March 12, 2009
    Publication date: March 3, 2011
    Inventors: Ryo Iwamura, Masayuki Tanaka, Tetsushi Katsube, Manabu Shigetomi, Eiji Okanari, Yasunori Tokunaga, Hiroshi Fujiwara
  • PROCESS FOR THE PREPARATION OF 4-[2-(5-ETHYL-2-PYRIDYL)ETHOXY]NITROBENZENE AND PIOGLITAZONE
    Publication number: 20110046382
    Abstract: A process for the preparation of 4-[2-(5-ethyl-2-pyridyl)ethoxy]nitrobenzene is described, which comprises the step of reacting 2-(5-ethyl-2-pyridyl)ethanol with 1-fluoro-4-nitrobenzene in acetone in the presence of an alkali metal hydroxide. The intermediate 4-[2-(5-ethyl-2-pyridyl)ethoxy]nitrobenzene is used for the preparation of pioglitazone.
    Type: Application
    Filed: April 28, 2008
    Publication date: February 24, 2011
    Applicant: Erregierre S.P.A.
    Inventors: Massimo Ferrari, Marcello Ghezzi, Emanuele Ghezzi
  • FUSED CYANOPYRIDINES AND THE USE THEREOF
    Publication number: 20110046162
    Abstract: The present application relates to novel substituted fused cyanopyridine derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, preferably for the treatment and/or prevention of cardiovascular disorders.
    Type: Application
    Filed: December 9, 2008
    Publication date: February 24, 2011
    Applicant: BAYER SCHERING PHARMA
    Inventors: Peter Nell, Alexandros Vakalopoulos, Frank Süssmeier, Barbara Albrecht-Küpper, Katja Zimmermann, Jörg Keldenich, Daniel Meibom
  • Indole compounds bearing aryl or heteroaryl groups having sphingosine 1-phosphate (S1P) receptor biological activity
    Patent number: 7888336
    Abstract: The invention provides well-defined aryl and/or heteroaryl substituted indoles that are useful as spingosine-1-phosphate agonists or antagonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: September 18, 2008
    Date of Patent: February 15, 2011
    Assignee: Allergan, Inc.
    Inventors: Richard L. Beard, Haiqing Yuan, John E. Donello
  • Pharmaceutical Combinations Comprising Specified Age Breaker and Further Drugs, I.A. Antihypertensive Drugs, Antidiabetic Drugs Etc.
    Publication number: 20110034378
    Abstract: The present invention relates to a combination, such as a combined preparation or pharmaceutical composition comprising: (a) compound of formula (I), and/or (II) or a pharmaceutically acceptable salt thereof; (b) at least one therapeutic agent selected from the group consisting of: an antihypertensive agent; an antidiabetics agent; a hypolipidemic agent; an antiplatelet agent; an antiobesity agent; an antithrombotic agent; an agent for diabetic vascular complications; and an agent for treatment of heart failure; or a pharmaceutically acceptable salts thereof, optionally in presence of a pharmaceutically acceptable carrier for separate, simultaneous or sequential use. The present invention also relates to a use of such combination for the treatment of mammal including human being. R1, R2, R3, R1, R2, R3, R4, R5, X, Y, A and B and m are as defined in the specification.
    Type: Application
    Filed: January 21, 2009
    Publication date: February 10, 2011
    Inventors: Chaitanya Dutt, Deepa Joshi, Ram Gupta, Kumarprafull Chandra
  • 2,3-SUBSTITUTED INDOLE DERIVATIVES FOR TREATING VIRAL INFECTIONS
    Publication number: 20110033417
    Abstract: The present invention relates to 2,3-Substituted Indole Derivatives, compositions comprising at least one 2,3-Substituted Indole Derivative, and methods of using the 2,3-Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Application
    Filed: August 27, 2008
    Publication date: February 10, 2011
    Inventors: Gopinadhan N. Anilkumar, Frank Bennett, Tin-Yau Chan, Kevin X. Chen, Mousumi Sannigrahi, Francisco Velazquez, Srikanth Venkatraman, Qingbei Zeng, Jose S. Duca, Charles A. Lesburg, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Neng-Yang Shih, Stephen J. Gavalas, Yueheng Jiang, Patrick A. Pinto, Haiyan Pu, Oleg B. Selyutin, Bancha Vibulbhan, Li Wang, Wanli Wu, Weiying Yang, Yuhua Huang, Hsueh-Cheng Huang, Robert Palermo, Boris Feld
  • SELECTIVE SUBTYPE ALPHA 2 ADRENERGIC AGENTS AND METHODS FOR USE THEREOF
    Publication number: 20110034517
    Abstract: The invention provides well-defined heterocyclic compounds that are useful as subtype selective alpha 2 adrenergic agonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with selective subtype modulation of alpha 2 adrenergic receptors.
    Type: Application
    Filed: January 14, 2009
    Publication date: February 10, 2011
    Applicant: ALLERGAN, INC.
    Inventors: Todd M. Heidelbaugh, Ken Chow, Santosh C. Sinha, Phong X. Nguyen, Wenkui K. Fang, Ling Li, Janet A. Takeuchi, Smita S. Bhat
  • IMAGING THE CENTRAL NERVOUS SYSTEM
    Publication number: 20110027178
    Abstract: The present invention provides novel compounds which may be used as in vivo imaging agents. The compounds of the invention are useful in a method to image the expression of P2X7 receptors in a subject, as a means to facilitate the diagnosis of a range of disease states.
    Type: Application
    Filed: February 26, 2009
    Publication date: February 3, 2011
    Inventors: Paul Alexander Jones, Ian Wilson, Veronique Morrison-Iveson, Clare Jones, John Woodcraft, Alex Jackson, Duncan Wynn