Chalcogen Bonded Directly At 2-position Of The Oxazole Ring Patents (Class 548/229)
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Patent number: 8148363Abstract: The present invention relates to novel heterocyclic compounds of Formulae I-III; as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are pharmaceutical compositions comprising said compounds, and methods for using said compounds for treating or preventing a thromboembolic disorder.Type: GrantFiled: May 18, 2009Date of Patent: April 3, 2012Assignee: Schering CorporationInventors: Martin C. Clasby, William J. Greenlee, Yan Xia, Tin-Yau Chan, Mariappan V. Chelliah, Samuel Chackalamannil, Haiyan Pu, Keith A. Eagen, Henry Vaccaro, Brian A. McKittrick, Liyuan Wang, Xiaobang Gao
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Patent number: 8143417Abstract: In the preparation of zolmitriptan of formula III the reduction of the diazonium salt to (5)-4-(4-hydrazinobenzyl)-1,3-oxazolidin-2-one of formula IV is performed in a more concentrated mixture and by the effect on an alkali metal disulphite, preferably sodium disulphite. A zolmitriptan toluene solvate, characterized by a toluene content of 9 to 14% by weight according to the gas chromatography determination and by a maximum of the corresponding mass loss at temperatures of about 111° C. in the gravimetric analysis record. A zolmitriptan toluene solvate, showing strong Raman bands at the wave numbers of 1443 and 1354 cm?1, characteristic for the crystal lattice of zolmitriptan with built-in toluene, and further marked bands at 1004 and 786 cm?1, characteristic for toluene.Type: GrantFiled: February 25, 2008Date of Patent: March 27, 2012Assignee: Zentiva k.s.Inventors: Michal Voslar, Monika Zatopkova, Ludek Ridvan, Tomas Pekarek
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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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Publication number: 20120053342Abstract: The present invention provides methods of forming carbamates, ureas, and isocyanates. In certain embodiments these methods include the step of reacting an amine with an ester-substituted diaryl carbonate to form an activated carbamate which can be further derivatized to form non-activated carbamate or a urea. The urea or carbamate can be subjected to a pyrolysis reaction to form isocyanate.Type: ApplicationFiled: November 4, 2011Publication date: March 1, 2012Applicant: SABIC INNOVATIVE PLASTICS IP B.V.Inventors: Hatem Abdallah Belfadhel, Hans-Peter Brack, Ricardo Godoy-Lopez, Dennis James Patrick Maria Willemse
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Publication number: 20120022096Abstract: This technology relates generally to compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death. Various compounds are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like.Type: ApplicationFiled: July 7, 2011Publication date: January 26, 2012Applicant: Board of Regents of The University of Texas SystemInventors: Steven L. McKnight, Andrew A. Pieper, Joseph M. Ready, Jef K. De Brabander
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Publication number: 20110313171Abstract: The present invention relates to the preparation of aryl hydrazines and their salts by treating aryl diazonium salts with triphenyl phosphine followed by hydrolysis of the resulting triphenyl-aryl hydrazyl phosphonium salt to get aryl hydrazine or its salt.Type: ApplicationFiled: January 12, 2007Publication date: December 22, 2011Inventors: Chandra Purna Ray, Sreekanth Medikonduri, Gorantla Seeta Ramanjaneyulu
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Publication number: 20110269970Abstract: (1R)-2-[(6-{2-[(2,6-dichlorobenzyl)oxy]ethoxy}hexyl)amino]-1-(2,2-dimethyl-4H-1,3-benzodioxin-6-yl)ethanol and (5R)-3-(6-{2-[(2,6-dichlorobenzyl)oxy]ethoxy}hexyl)-5-(2,2-dimethyl-4H-1,3-benzodioxin-6-yl)-1,3-oxazolidin-2-one are claimedType: ApplicationFiled: June 21, 2011Publication date: November 3, 2011Applicant: Glaxo Group LimitedInventors: Philip Charles Box, Diane Mary Coe, Brian Edgar Looker, Inderjit Singh Mann, Panaylotis Alexandrou Procopiou
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Publication number: 20110263865Abstract: The present invention provides a novel isopropyl acetate solvate form of zolmitriptan, and a process for its preparation thereof. The present invention also provides a process for preparation of zolmitriptan polymorph A. Thus, for example, zolmitriptan isopropanol solvate was dissolved in isopropyl acetate at 25 deg C, the contents were heated to reflux for 30 minutes and the separated solid was filtered, washed with isopropyl acetate to give zolmitriptan isopropyl acetate solvate.Type: ApplicationFiled: December 24, 2008Publication date: October 27, 2011Applicant: HETERO RESEARCH FOUNDATIONInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Thungathurthy Srinivasa Rao
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Patent number: 7998992Abstract: 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: GrantFiled: March 27, 2008Date of Patent: August 16, 2011Assignees: Institute of Medicinal Molecular Design, Inc., Shionogi & Co., Ltd.Inventors: Akiko Itai, Susumu Muto, Ryuko Tokuyama, Hiroshi Fukasawa, Takeshi Yanase
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Publication number: 20110190125Abstract: The invention relates to 2-(benzylsulfonyl)-oxazole derivatives, chiral 2-(benzylsulfinyl)-oxazole derivatives and 2-(benzylsulfanyl)-oxazole derivatives of general formula (I) and the salts thereof, wherein the individual radicals and indexes have the meaning indicated in the description. Also described are methods for the production thereof as well as the use of said compounds as herbicides and plant growth regulators, in particular as herbicides for selectively controlling weeds in plant crops.Type: ApplicationFiled: April 15, 2009Publication date: August 4, 2011Applicant: BAYER CROPSCIENCE AGInventors: Christopher Hugh Rosinger, Dieter Feucht, Dirk Schmutzler, Isolde Haeuser-Hahn, Jan Dittgen, Arianna Martelletti, Hansjorg Dietrich
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Publication number: 20110178059Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. The compounds have 3 cyclic groups connected by single bonds, as for example triphenyl, which are attached directly to the ring of formula I or attached at the position B.Type: ApplicationFiled: March 28, 2011Publication date: July 21, 2011Applicant: Merck Sharp & Dohme Corp.Inventors: Amjad ALI, Zhijian Lu, Peter J. Sinclair, Yi-Heng Chen, Cameron J. Smith, Hong Li
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Patent number: 7968707Abstract: A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.Type: GrantFiled: February 27, 2007Date of Patent: June 28, 2011Assignee: Abbott LaboratoriesInventors: Hing Leung Sham, Daniel W. Norbeck, Xiaoqi Chen, David A. Betebenner, Dale J. Kempf, Thomas R. Herrin, Gondi N. Kumar, Stephen L. Condon, Arthur J. Cooper, Daniel A. Dickman, Steven M. Hannick, Lawrence Kolaczkowski, Patricia A. Oliver, Daniel J. Plata, Peter J. Stengel, Eric J. Stoner, Jieh-Heh J. Tien, Jih-Hua Liu, Ketan M. Patel
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Publication number: 20110152332Abstract: The present invention relates to novel pesticidal azolidine derivatives as well as to oxazolidinone derivatives and their use as pesticides for combating animal parasites which occur in the agrochemical field and in the field of veterinary medicine, respectively. wherein X, m, R?, Q, G, U, l, A1 to A4 and R are as defined herein.Type: ApplicationFiled: November 1, 2010Publication date: June 23, 2011Applicant: Bayer CropScience AGInventors: Tetsuya Murata, Mamoru Hatazawa, Peter Brüchner, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya, Ulrich Görgens
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Publication number: 20110112157Abstract: The present invention relates to an improved process for the preparation of the active pharmaceutical ingredient zolmitriptan. In particular, it relates to an efficient process for the preparation of zolmitriptan and its pharmaceutically acceptable salts and solvates.Type: ApplicationFiled: October 3, 2008Publication date: May 12, 2011Applicant: GENERICS [UK] LIMITEDInventors: Debashish Datta, Vinayak G. Gore, Maheshkumar S. Gadakar, Kiran Pokharkar, Kiran Phatangare
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Publication number: 20110105504Abstract: This invention relates to novel compounds of the Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals.Type: ApplicationFiled: March 18, 2009Publication date: May 5, 2011Inventors: David A. Claremon, Linghang Zhuang, Yuanjle Ye, Suresh B. Singh, Colin M. Tice, Gerard McGeehan
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Patent number: 7935906Abstract: Among other things, to cause directional motion of chiral objects in a mixture in a chamber, a field is rotated relative to a chamber to cause rotation of the chiral objects. The rotation of the objects caused them to move directionally based on their chirality.Type: GrantFiled: April 15, 2008Date of Patent: May 3, 2011Assignee: Dynamic Connections, LLCInventors: Osman Kibar, Mirianas Chachisvilis, Eugene Tu, Thomas H. Marsilje
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Publication number: 20110098468Abstract: A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.Type: ApplicationFiled: December 14, 2010Publication date: April 28, 2011Applicant: OPKO Health, Inc.Inventors: Sunil Paliwal, Gregory A. Reichard, Cheng Wang, Dong Xiao, Hon-Chung Tsui, Neng-Yang Shih, Juan D. Arredondo, Michelle Laci Wrobleski, Anandan Palani
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Patent number: 7932278Abstract: The present application relates to novel 2-aminoethoxyacetic acid derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular thromboembolic disorders.Type: GrantFiled: September 14, 2006Date of Patent: April 26, 2011Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Christian R. Thomas, Susanne Röhrig, Elisabeth Perzborn
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Publication number: 20110077272Abstract: A pharmaceutical composition includes triptans, such as sumatriptan, and may be used in therapy. The composition may be administered via the inhaled route.Type: ApplicationFiled: February 2, 2009Publication date: March 31, 2011Applicant: Vectura LimitedInventor: Mark Jonathan Main
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Patent number: 7915271Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. The compounds have 3 cyclic groups connected by single bonds, as for example triphenyl, which are attached directly to the ring of formula I or attached at the position B.Type: GrantFiled: December 29, 2006Date of Patent: March 29, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Zhijian Lu, Peter J. Sinclair, Yi-Heng Chen, Cameron J. Smith, Hong Li
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Publication number: 20110065682Abstract: The present invention relates to novel heterocyclic compounds of Formulae I-III; as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are pharmaceutical compositions comprising said compounds, and methods for using said compounds for treating or preventing a thromboembolic disorder.Type: ApplicationFiled: May 18, 2009Publication date: March 17, 2011Inventors: Martin C. Clasby, William J. Greenlee, Yan Xia, Tin-Yau Chan, Mariappan V. Chelliah, Samuel Chackalamannil, Haiyan Pu,, Keith A. Eagen, Henry Vaccaro, Brian A. McKittrick,, Liyuan Wang, Xiaobang Gao
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Patent number: 7897783Abstract: A method whereby a compound having HCV replication inhibitory activity and desired optical activity can be synthesized selectively and at high yield in a small number of steps by using a compound having a specific chiral auxiliary as a starting compound is provided. A compound represented by the formula (1-8): [wherein Y represents a group represented by the following formula: Q represents a protected carbonyl group; D represents —(CH2)m—R?, etc.; and n represents an integer of 0 to 10].Type: GrantFiled: February 16, 2006Date of Patent: March 1, 2011Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Tatsuya Kato, Nobuaki Kimura, Akemi Mizutani, Toshihiko Makino, Kenichi Kawasaki, Hiroshi Fukuda, Susumu Komiyama, Takuo Tsukuda
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Publication number: 20110039696Abstract: The invention relates to 2-[(1H-pyrazol-4-ylmethyl)-sulfonyl]-oxazole derivatives, chiral 2-[(1H-pyrazol-4-ylmethyl)-sulfinyl]-oxazole derivatives, and 2-[(1H-pyrazol-4-ylmethyl)-sulfanyl]-oxazole derivatives of general formula (I) and the salts thereof, methods for the production thereof, and the use thereof as herbicides and plant growth regulators, in particular as herbicides for selectively controlling weeds in plant crops.Type: ApplicationFiled: April 15, 2009Publication date: February 17, 2011Applicant: BAYER CROPSCIENCE AGInventors: Heinz Kehne, Hansjorg Dietrich, Dieter Feucht, Dirk Schmutzler, Isolde Hauser-Hahn, Christian Paulitz, Jan Dittgen, Arianna Marteletti, Christopher Hugh Rosinger
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Publication number: 20110033544Abstract: Methods are provided for the engineering of inhalable dry powder pharmaceutical formulations with desired pharmacokinetic profiles and parameters. Compositions with improved pharmacokinetics are disclosed.Type: ApplicationFiled: May 14, 2010Publication date: February 10, 2011Applicant: SHIN NIPPON BIOMEDICAL LABORATORIES, LTD.Inventors: Ryoichi Nagata, Shunji Haruta
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Publication number: 20110034450Abstract: The present application relates to novel carboxylic acid derivatives having an oxo-substituted azaheterocyclic partial structure, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.Type: ApplicationFiled: April 6, 2009Publication date: February 10, 2011Applicant: BAYER SCHERING PHARMA AKTIEGESELLSCHAFTInventors: Michael Hahn, Eva-Maria Becker, Andreas Knorr, Dirk Schneider, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder, Friederike Stoll, Stefan Heitmeier, Klaus Münter, Nils Griebenow, Thomas Lampe, Sherif El Sheikh, Volkhart Min-Jian Li
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Publication number: 20110034460Abstract: 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: ApplicationFiled: August 4, 2010Publication date: February 10, 2011Applicant: Les Laboratoires ServierInventors: Jean-Claude Ortuno, Alexis Cordi, Jean-Michel Lacoste, Vincent Lacoste, Pauline Lacoste, Imre Fejes, Michael Burbridge, John Hickman, Alain Pierre
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Publication number: 20110028447Abstract: This invention relates to compounds, pharmaceutical compositions and methods for the treatment of a condition mediated by CB1 receptor activity in a mammalian subject including a human, which comprises administering to a mammal in need of such treatment a therapeutically effective amount of the compound of formula (I) wherein R1, R2 and R3 are as defined in this specification.Type: ApplicationFiled: February 26, 2009Publication date: February 3, 2011Inventors: Ingrid Price Buchler, Michael Joseph Hayes, Shridhar Gajanan Hegde, Susan Landis Hockerman, Darin Eugene Jones, Steven Wade Kortum, Joseph Gerace Rico, Ruth Elizabeth TenBrink, Kun Ken Wu
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Publication number: 20110021573Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the antagonists of PGD2 receptors described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: ApplicationFiled: February 25, 2009Publication date: January 27, 2011Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: John Howard Hutchinson, Brian Andrew Stearns, Thomas Jonathan Seiders, Jill Melissa Scott, Jeannie M. Arruda, Bowei Wang
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Publication number: 20110003825Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4 and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of ?-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.Type: ApplicationFiled: August 23, 2010Publication date: January 6, 2011Applicant: Schering CorporationInventors: Ying Huang, Guoqing Li, Andrew W. Stamford
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Patent number: 7863307Abstract: An efficient process is disclosed for producing a compound that is an inhibitor of CETP. The last step of the process is the coupling of an oxazolidinone derivative with a biphenyl moiety to provide a compound of formula (I). In a specific embodiment of this synthesis, a crystalline product is produced which is characterized as a non-solvated crystalline polymorph.Type: GrantFiled: June 29, 2006Date of Patent: January 4, 2011Inventors: Ross A. Miller, Aaron S. Cote
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Publication number: 20100324046Abstract: The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: June 24, 2008Publication date: December 23, 2010Inventors: Paul Harrington, Richard W. Heidebrecht, JR., Solomon Kattar, Thomas A. Miller, Karin M. Otte, Phieng Siliphaivanh, Paul Tempest, Kevin J. Wilson, David J. Witter
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Publication number: 20100305174Abstract: The present invention relates to novel heterocyclic derivatives of formula (I) and their pharmaceutically acceptable salts, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts, their pharmaceutical compositions, and their prodrugs thereof. The present invention more particularly provides novel compounds of the general formula (1).Type: ApplicationFiled: April 12, 2006Publication date: December 2, 2010Applicant: ORCHID RESEARCH LABORATORIES LIMITEDInventors: Surendrakumar Satyanarayan Pandey, Gadam Om Reddy, Shiv Kumar Agarwal, Gajendra Singh, Santhanagopalan Chithra, Debendranath Dey, Abhijeet Nag, Kadnur Venkatachalapathi Sanjay
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Publication number: 20100292241Abstract: The present invention is directed to 3,5-disubstituted-1,3-oxazolidin-2-one derivatives which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neuro-ological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: January 14, 2009Publication date: November 18, 2010Applicant: Merck Sharp & Dohme Corp.Inventors: Edward Brnardic, Mark Fraley, Mark Layton, Robert Garbaccio
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Patent number: 7825155Abstract: Disclosed is a compound represented by the formula (1) below, a prodrug thereof or a pharmaceutically acceptable salt of either, which is useful as a therapeutic, preventive or ameliorating agent for diabetes and the like. (In the formula, R3 represents an optionally substituted carbamoyl group or the like; X represents a hydroxyl group or the like; W1 and W2 independently represent a single bond or methylene; R7 and R8 independently represent a hydrogen atom, an optionally substituted alkyl group or the like; and Ar represents an optionally substituted aryl group or the like.Type: GrantFiled: September 13, 2006Date of Patent: November 2, 2010Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Teruhisa Tokunaga, Tsuyoshi Takasaki, Kozo Yoshida, Ryu Nagata
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Publication number: 20100267714Abstract: The invention provides novel heterocyclic compounds, pharmaceutical compositions and methods of treatment that modulate levels of MIF expression and treat disorders associated with high or low levels of MIF expression.Type: ApplicationFiled: May 4, 2010Publication date: October 21, 2010Inventors: William L. Jorgensen, Richard J. Bucala
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Patent number: 7816394Abstract: Methods of transdermally delivering a therapeutic amount of an indole serotonin receptor agonist to an individual in need thereof, e.g., to provide a therapeutic level of an indole serotonin receptor agonist to an individual in need thereof, are provided. Also provided are transdermal formulations of indole serotonin receptor agonists that find use in practicing the subject methods.Type: GrantFiled: November 17, 2006Date of Patent: October 19, 2010Assignee: Teikoku Pharma USA Inc.Inventors: Kunio Yoneto, Katsuyuki Inoo
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Patent number: 7816354Abstract: The present invention is directed to compounds of Formula I: Wherein R1, R2, Y, m and n are further defined in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.Type: GrantFiled: December 6, 2006Date of Patent: October 19, 2010Assignee: AstraZeneca ABInventors: Abdelmalik Slassi, Methvin Isaac, Ian Egle, Fupeng Ma, Babu Joseph, Joshua Clayton, Krzysztof Swierczek
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Publication number: 20100240659Abstract: 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 Ring A is a group represented by the formula: Ring B is optionally substituted heteroaryl, provided that optionally substituted isoxazole is excluded, or optionally substituted heterocycle, R1 is hydrogen or optionally substituted alkyl, R2 is —OR5, —SR5, halogen, halogenated alkyl or the like, R3 is optionally substituted alkyl or the like, R4 is optionally substituted alkyl or the like, R5 is optionally substituted alkyl or the like, R6 is hydrogen or the like, R7 and R8 are each independently hydrogen or the like, R10 and R11 are each independently hydrogen or the like, R12 is optionally substituted alkyl or the like, m and p are each independently integer of 1 to 3.Type: ApplicationFiled: May 7, 2008Publication date: September 23, 2010Applicant: SHIONOGI & CO., LTD.Inventors: Koji Masuda, Tomoyuki Ogawa, Takuji Nakatani
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Publication number: 20100234365Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cannabinoid Receptor 1 (CB1).Type: ApplicationFiled: December 12, 2007Publication date: September 16, 2010Applicant: IRM LLCInventors: Hong Liu, Xiaohui He, Dean Phillips, Xuefeng Zhu, Kunyong Yang, Thomas Lau, Baogen Wu, Yongping Xie, Truc Ngoc Nguyen, Xing Wang
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Publication number: 20100222326Abstract: The present invention relates to new compounds, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: April 24, 2008Publication date: September 2, 2010Applicant: UCB PHARMA, S.A.Inventors: Benoit Kenda, Laurent Turet, Yannick Quesnel, Philippe Michel, Ali Ates
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Patent number: 7786154Abstract: A compound having the formula or a pharmaceutically acceptable salt or a prodrug thereof is disclosed herein. Y, A, and B are as described herein. Methods, compositions, and medicaments related to these compounds are also disclosed.Type: GrantFiled: May 22, 2009Date of Patent: August 31, 2010Assignee: Allergan, Inc.Inventor: David W. Old
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Patent number: 7776855Abstract: This invention includes oxazolidinone prodrug compounds of Formula (I) and Formula (II) as defined herein. The prodrugs are convertible by natural biological processes into an active ingredient possessed of antimicrobial properties useful in treating bacterial infections in mammals.Type: GrantFiled: July 9, 2007Date of Patent: August 17, 2010Assignee: Janssen Pharmaceutica N.V.Inventors: Mark J. Macielag, Manomi A. Tennakoon
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Publication number: 20100197680Abstract: The present application relates to novel lactam-substituted dicarboxylic acid derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.Type: ApplicationFiled: March 15, 2008Publication date: August 5, 2010Inventors: Michael Hahn, Eva-Maria Becker, Andreas Knorr, Dirk Schneider, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder, Dieter Lang
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Publication number: 20100197675Abstract: This invention relates to novel compounds of the Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 ?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.Type: ApplicationFiled: February 26, 2008Publication date: August 5, 2010Inventors: David A. Claremon, Gerard McGeehan, Suresh B. Singh, Colin M. Tice, Yuanjie Ye, Wei Zhao
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Patent number: 7750165Abstract: The invention provides two crystalline forms A and B of the skeletal muscle relaxant and anxiolytic agent, Metaxalone of formula (I), and a process for preparation thereof. The two crystalline forms A and B are bioavailable. The invention further provides pharmaceutical compositions comprising the two bioavailable crystalline forms, useful for the relief of discomforts associated with acute, painful musculoskeletal conditions.Type: GrantFiled: December 29, 2006Date of Patent: July 6, 2010Assignee: Fresenius Kabi Oncology LimitedInventors: Jayanta Chattopadhyay, Subrata Sarkar, Jyan Shankar Mahanty, Susanta Hazra, Moloy Mitra, Manoj Kumar Singh
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Patent number: 7741327Abstract: 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 metabolic diseases and disorders such as, for example, type II diabetes mellitus.Type: GrantFiled: March 9, 2009Date of Patent: June 22, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Steven Joseph Berthel, John A Brinkman, Stuart Hayden, Nancy-Ellen Haynes, Robert Francis Kester, Lee Apostle McDermott, Yimin Qian, Ramakanth Sarabu, Nathan Robert Scott, Jefferson Wright Tilley
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Publication number: 20100145064Abstract: A method for the preparation of zolmitriptan or its pharmaceutically acceptable salts, comprising isolation of a crystalline salt of zolmitriptan, its optional re-purification and conversion to the substance of formula (III). Zolmitriptan hydrochloride in the crystalline state.Type: ApplicationFiled: February 25, 2008Publication date: June 10, 2010Inventors: Michal Voslar, Monika Zatopkova, Hana Petrickova, Lucie Tisovska
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Publication number: 20100137243Abstract: Compounds of Formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, and compounds as shown in Formula (I) wherein C is for example (D), (E), (F); wherein A and B are independently selected from (i) and (ii); R2a to R3b are independently selected from hydrogen and fluorine; R1a and R1b are independently selected from, for example, hydroxy, —NHC(?W)R4, (a) and (b); wherein W is O or S; R4 is, for example, hydrogen, amino, (1-4C)alkyl; HET-1 is, for example, a C-linked 5-membered heteroaryl ring; HET-2 is, for example, an N-linked 5-membered, fully or partially unsaturated heterocyclic ring; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described.Type: ApplicationFiled: May 28, 2008Publication date: June 3, 2010Applicant: AstraZeneca ABInventors: Michael Barry Gravestock, Neil James Hales, Michael Lingrad Swaim, Sheila Irene Hauck, Stuart Dennett Mills
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Publication number: 20100136024Abstract: A composition comprises a material capable of selectively controlling a level or activity of HDAC6 in an ocular environment for effecting ocular neuroprotection in subjects in risk of developing or worsening an ocular neurodegenerative condition, or for treating or controlling glaucoma. Such a composition can be administered to a patient in combination with another therapy directed at providing ocular neuroprotection or treating or controlling glaucoma.Type: ApplicationFiled: October 19, 2009Publication date: June 3, 2010Inventor: Stephen P. Bartels
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Publication number: 20100137349Abstract: The present application relates to N-chlorinated oxazolidinone, hydantoin and imidazolidinone compounds of Formula I or pharmaceutically acceptable salts thereof, and associated compositions and methods of use as antimicrobial agents.Type: ApplicationFiled: November 4, 2009Publication date: June 3, 2010Inventors: Rakesh K. Jain, Eddy Low, Charles Francavilla, Timothy P. Shiau, Bum Kim, Satheesh K. Nair