The Additional Five-membered Hetero Ring Consists Of Three Ring Carbons, And Of Nitrogen And Chalcogen In Adjacent Ring Positions (e.g., Isoxazolyl, Isothiazolyl, Etc.) Patents (Class 514/254.04)
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Publication number: 20120277211Abstract: Methods and compositions that relate to genetic markers of psychotic disorders, e.g., schizophrenia (SZ), are provided. For example, in certain aspects methods for determinations of a SULT4A1-1 haplotype are described. Furthermore, the invention provides methods and compositions involving treatment of psychotic disorders using the haplotype status.Type: ApplicationFiled: November 4, 2010Publication date: November 1, 2012Applicant: SUREGENE LLCInventors: Timothy L. Ramsey, Mark D. Brennan
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Publication number: 20120252797Abstract: Isoxazoles of formula (A) or (B) wherein R1 is a group of formula (IB) The isoxazoles are inhibitors of HSP90 activity, and useful for the treatment of, for example, cancers.Type: ApplicationFiled: June 18, 2012Publication date: October 4, 2012Applicants: Vernalis (Cambridge) Limited, The Institute of Cancer Research, Cancer Research Technology Ltd.Inventors: Martin James Drysdale, Brian William Dymock, Harry Finch, Paul Webb, Edward McDonald, Karen Elizabeth James, Kwai Ming Cheung, Thomas Peter Matthews
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Publication number: 20120245176Abstract: A compound of Formula I is set forth, including pharmaceutically acceptable salts thereof: wherein Het is a 5 or 6-membered heterocycle with —N, —O, or —S adjacent to the —Ar substituent or adjacent to the point of attachment for the —Ar substituent; Ar is aryl or heteroaryl; R is —CH3, —CH2F, —CHF2 or —CH?CH2; V is —H, —CH3 or ?O; W is —NO2, —Cl, —Br, —CH2OH, or —CN; X is —Cl, —Br, —F, —CH3, —OCH3, or —CN; Y is —CH or —N; and Z is —CH or —N. This compound is useful in compositions for the prevention and treatment of influenza virus.Type: ApplicationFiled: September 23, 2011Publication date: September 27, 2012Inventors: Christopher W. Cianci, Samuel Gerritz, Sean Kim, David R. Langley, Guo Li, Bradley C. Pearce, Annapurna Pendri, Shuhao Shi, Weixu Zhai, Shirong Zhu
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Patent number: 8273736Abstract: Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: GrantFiled: November 20, 2009Date of Patent: September 25, 2012Assignee: Abbott LaboratoriesInventors: Patrick Betschmann, Andrew F. Burchat, David J. Calderwood, Michael L. Curtin, Steven K. Davidsen, Heather M. Davis, Robin R. Frey, Howard R. Heyman, Gavin C. Hirst, Peter Hrnciar, Michael R. Michaelides, Melanie A. Muckey, Kelly D. Mullen, Paul Rafferty, Carol K. Wada
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Publication number: 20120238539Abstract: A compound of Formula I is set forth, including pharmaceutically acceptable salts thereof: wherein Het is a 5 or 6-membered heterocycle with —N, —O, or —S adjacent to the —Ar substituent or adjacent to the point of attachment for the —Ar substituent; Ar is aryl or heteroaryl; R is —CH3, —CH2F, or —CH?CH2; W is —NO2, —Cl, —Br, —CHO, —CH?CH2, or —CN; X is —Cl, —CH3, or —CN; Y is —CH or —N; and Z is C1-C6 alkyl, C3-C6 cycloalkyl, substituted aryl, substituted heteroaryl, OR1, or NHR1, wherein R1 is selected from the group of H, aryl, heteroaryl, C1-C6 alkyl and C3-C6 cycloalkyl. This compound is useful in compositions for the prevention and treatment of influenza virus.Type: ApplicationFiled: September 6, 2011Publication date: September 20, 2012Inventors: Christopher W. Cianci, Samuel Gerritz, Guo Li, Bradley C. Pearce, Annapurna Pendri, Shuhao Shi, Weixu Zhai, Shirong Zhu
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Publication number: 20120231092Abstract: Treatment regimens for mood disorders that include administration of buprenorphine, alone or in combination with additional pharmacological agents are described. Specifically, treatment regimens that alleviate racing thoughts associated with bipolar disorder, and pharmaceutical compositions and kits for use therein are described. Dosing regimens, compositions, and kits including buprenorphine for treating mania associated with opioid withdrawal are also described.Type: ApplicationFiled: March 14, 2012Publication date: September 13, 2012Applicant: ComGenRx, Inc.Inventors: Bryan T. Oronsky, Neil C. Oronsky
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Patent number: 8258139Abstract: The invention relates to a medicament or a method for treating mental disorders, in detail, ADHD comprising lurasidone, or a combination of lurasidone and a D4 receptor agonist.Type: GrantFiled: May 23, 2011Date of Patent: September 4, 2012Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Kazuhito Ikeda, Takeo Ishiyama
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Publication number: 20120219641Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.Type: ApplicationFiled: February 14, 2012Publication date: August 30, 2012Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: David D. Manning, Christopher Lawrence Cioffi
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Publication number: 20120220603Abstract: Compounds of formula (I) which are useful in ameliorating conditions characterized by unwanted sodium and/or calcium channel activity, particularly unwanted NaV 1.7, NaV 1.8, or CaV 3.2 channel activity are disclosed. Specifically, a series of compounds containing piperidine or piperazine linked through an amide, isoxazole or similar linker to an aryl ring are described and are shown to be useful for the treatment of pain or epilepsy. A is selected from Formulae (i) or (ii).Type: ApplicationFiled: September 3, 2010Publication date: August 30, 2012Applicant: ZALICUS PHARMACEUTICALS LTD.Inventors: Hassan Pajouhesh, Mike Grimwood, Yongbao Zhu, Yanbing Ding, Richard Holland
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Patent number: 8252799Abstract: The present invention is directed to therapeutic agents of the formula (I) which are atypical antipsychotics and which are useful in the treatment of neurological and psychiatric disorders associated with dopamine D2 and serotonin 5-HT2A neurotransmission dysfunction. wherein; R1 is C1-6alkyl, which is unsubstituted or substituted with 1-6 fluoro, wherein R1 and the hydroxyl group on the ring are attached to the same carbon atom; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: April 3, 2008Date of Patent: August 28, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Mark T. Bilodeau, Kausik K. Nanda, B. Wesley Trotter
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Publication number: 20120214790Abstract: The present invention provides compounds which show high effectiveness against positive symptoms, negative symptoms and cognitive dysfunction in schizophrenia and reduce conventional side-effect risks as well as have remarkable effects for central neurological diseases associated with cognitive dysfunction other than schizophrenia. N-Acyl cyclic amine derivatives of formula (1): wherein Ar1 and Ar2 are aryl or heteroaryl; V is nitrogen, or CR3; W1 is a single bond, —C(O)—, etc.; W2 is C1-alkylene; W3 is a single bond, methylene, —NH—, —CR4?CR5—, etc.; Ring Q is a group of formula (a) in which n is 0 or 1; m is 0 to 2; k is 1 to 3; Z is a single bond, methylene, oxygen, etc.; R1a, R1b and R1c are each, same or different, hydrogen, hydroxyl, halogen, cyano, C1-6 alkyl, etc.; or pharmaceutically acceptable salts thereof are provided.Type: ApplicationFiled: March 11, 2011Publication date: August 23, 2012Inventors: Megumi Maruyama, Naoya Kinomura, Satoshi Nojima, Masahiro Takamura, Keisuke Kakiguchi, Hiroto Tatamidani
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Publication number: 20120208773Abstract: The present invention provides for a pharmaceutical composition that includes tetrabenazine and a release-retarding agent; and a method of treating a hyperkinetic movement disorder (e.g., Huntington's disease, chorea associated with Huntington's disease, hemiballismus, senile chorea, tic disorders, tardive dyskinesia, myoclonus, dystonia and/or Tourette's syndrome). The method includes administering an effective amount of the pharmaceutical composition, for a period of time effective to treat the hyperkinetic movement disorder.Type: ApplicationFiled: August 12, 2010Publication date: August 16, 2012Applicant: Valeant International (Barbados) SRLInventors: Andrew John Duffield, Graham Jackson, Steven E. Frisbee, Okponanabofa Eradiri, John CK Lai
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Publication number: 20120202775Abstract: Compounds having drug and bio-affecting properties are described herein, including their properties, pharmaceutical compositions and methods of use. In particular, tricyclic aryl or heteroaryl piperazine diamide derivatives that possess unique antiviral activity are set forth. These compounds are useful for the treatment of HIV and AIDS.Type: ApplicationFiled: August 4, 2011Publication date: August 9, 2012Inventors: Tao Wang, Zhongxing Zhang, Zhiwei Yin, John F. Kadow, Nicholas A. Meanwell
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Publication number: 20120195985Abstract: The present invention provides compounds that are glycine transporter 1 (hereinafter referred to as GlyT-1) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of GlyT-1 such as cognitive disorders associated with Schizophrenia, ADHD (attention deficit hyperactivity disorder), MCI (mild cognitive impairment), and the like. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.Type: ApplicationFiled: March 21, 2012Publication date: August 2, 2012Applicant: Amgen Inc.Inventors: Stephen Hitchcock, Albert Amegadzie, Wenyuan Qian, Xiaoyang Xia, Scott S. Harried
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Publication number: 20120196861Abstract: The present invention relates to compounds of the general formula (I), and the pharmaceutically acceptable salt or solvate thereof, as anti-inflammatory and immunomodulatory agents.Type: ApplicationFiled: January 27, 2012Publication date: August 2, 2012Applicant: 4SC Discovery GmbHInventors: Johann LEBAN, Stefan TASLER, Roland BAUMGARTNER, Wael SAEB, Carine CHEVRIER
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Publication number: 20120178733Abstract: The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.Type: ApplicationFiled: August 19, 2011Publication date: July 12, 2012Inventors: Bing-Yan Zhu, Shawn M. Bauer, Zhaozhong J. Jia, Gary D. Probst, Yanchen Zhang, Robert M. Scarborough
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Publication number: 20120172372Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: ApplicationFiled: December 30, 2011Publication date: July 5, 2012Inventors: Bradley Paul Morgan, Alex Muci, Pu-Ping Lu, Erica Anne Kraynack, Todd Tochimoto, David J. Morgans, JR.
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Publication number: 20120165341Abstract: A therapeutic/preventive agent for cognitive dysfunctions, which comprises as an active ingredient an imide derivative of the following formula [1]: wherein Z is a group of the formula [2]: D is a group of —(CH2)p-A-(CH2)q—; G is ?N—, —CH—, etc.; and Ar is an aromatic heterocyclic group, etc.Type: ApplicationFiled: February 29, 2012Publication date: June 28, 2012Inventors: Yukihiro OHNO, Takeo ISHIYAMA
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Publication number: 20120149715Abstract: High throughput and virtual screening methods are disclosed that can identify potential anti-viral agents. The virtual screening methods identify agents that interact with a viral nucleoprotein binding site. The high throughput methods identify compounds that inhibit viral infection by binding to viral nucleoprotein. Also disclosed are pharmaceutical formulations useful for treating or preventing viral infections, especially influenza A.Type: ApplicationFiled: May 31, 2011Publication date: June 14, 2012Inventors: Yi Tsun Richard Kao, Kwok-Yung Yuen, Dan Yang, Lihong Hu, Guanhua Chen, Bo-Jian Zheng
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Publication number: 20120142701Abstract: Cell-based and cell-free assays are disclosed that detect compounds that promote aggregation of proteins, glycoproteins, and protein-nucleic acid complexes. Also disclosed are pharmaceutical formulations useful for treating or preventing viral infections, bacterial infections, cancer, and diseases involving hyper-proliferative cells.Type: ApplicationFiled: May 31, 2011Publication date: June 7, 2012Inventors: Yi Tsun Richard Kao, Kwok-Yung Yuen
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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: 20120129850Abstract: Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.Type: ApplicationFiled: January 24, 2012Publication date: May 24, 2012Inventors: Shripad Bhagwat, Qi Chao, Robert M. Grotzfeld, Hitesh K. Patel, Kelly G. Sprankle
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Publication number: 20120122792Abstract: S-t-butyl protected cysteine di-peptide analogs and related compounds and methods of using these compounds for the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of Central Nervous System (CNS).Type: ApplicationFiled: November 11, 2011Publication date: May 17, 2012Applicant: PROMENTIS PHARMACEUTICALS, INC.Inventors: Edward M. Johnson, II, Daniel G. Lawton
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Publication number: 20120115778Abstract: Methods for treating eating disorders associated with excessive weight gain, suppressing appetite, reducing body weight, or treating obesity in an animal by administering one or more antagonists of the serotonin Htr1a or Htr2b receptor, or a Tph2 inhibitor are provided, or combinations thereof.Type: ApplicationFiled: July 15, 2010Publication date: May 10, 2012Applicant: The Trustees of Columbia University in the City of New YorkInventors: Gerard Karsenty, Vijay Yadav, Franck Oury
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Publication number: 20120115879Abstract: The invention relates to a medicament or a method for treating mental disorders, in detail, ADHD comprising lurasidone, or a combination of lurasidone and a D4 receptor agonist.Type: ApplicationFiled: May 23, 2011Publication date: May 10, 2012Inventors: Kazuhito IKEDA, Takeo Ishiyama
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Patent number: 8173637Abstract: A pharmaceutical composition that contains an atypical antipsychotic drug and succinic acid, fumaric acid or a mixture of succinic acid and fumaric acid.Type: GrantFiled: September 5, 2008Date of Patent: May 8, 2012Assignee: Handa Pharmaceuticals, LLCInventors: Fang-yu Liu, Zhi-qun Shen
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Publication number: 20120108545Abstract: Monomeric and dimeric trioxane fluoroaryl amides, 5-carbon-linked, C-10 non-acetal trioxane dimer esters; trioxane silylamides; and trioxane dimer orthoesters and methods of their use for treating subjects infected with malaria or other parasitic infectious diseases including, but not limited to, toxoplasmic infection; subjects afflicted with psychiatric conditions associated with toxoplasmic infection; and subjects afflicted with cancer.Type: ApplicationFiled: May 19, 2010Publication date: May 3, 2012Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Gary H. Posner, Lauren E. Woodard, David R. Levine, Deuk Kyu Moon, Bryan T. Mott
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Publication number: 20120108588Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I): wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications (including in particular diabetic retinopathy, nephropathy or neuropathy), cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, viral diseases, inflammatory disorders, or diseases in which the liver is a target organ.Type: ApplicationFiled: January 6, 2012Publication date: May 3, 2012Applicant: Pfizer, Inc.Inventors: Iriny Botrous, Yufeng Hong, Hui Li, Kevin Kun-Chin Liu, Seiji Nukui, Min Teng, Eileen Valenzuela Tompkins, Chunfeng Yin
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Publication number: 20120091022Abstract: The present invention relates to a composition comprising N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]-(2R,3R)-2,3-tetramethylene-butyl]-(1?R,2?S,3?R,4?S)-2,3-bicyclo[2,2,1]heptanedicarboximide or a pharmaceutically acceptable acid addition salt thereof. In detail, the composition relates to a sustained release formulation for injection which maintains an effective blood level of the above-mentioned compound.Type: ApplicationFiled: October 18, 2011Publication date: April 19, 2012Inventors: Takashi NAKAGAWA, Norimasa Koseki
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Patent number: 8148379Abstract: A therapeutic/preventive agent for cognitive dysfunctions, which comprises as an active ingredient an imide derivative of the following formula [1]: wherein Z is a group of the formula [2]: D is a group of —(CH2)p-A-(CH2)q—; G is ?N—, —CH—, etc.; and Ar is an aromatic heterocyclic group, etc.Type: GrantFiled: June 17, 2008Date of Patent: April 3, 2012Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Yukihiro Ohno, Takeo Ishiyama
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Publication number: 20120077800Abstract: The present invention relates to the discovery of a novel opioid modulator effective in reducing pharmacologically induced weight gain associated with atypical antipsychotic use. The present invention provides methods of reducing antipsychotic induced weight gain, methods for suppressing food intake and reducing ghrelin levels induced by atypical antipsychotic medications in a patient.Type: ApplicationFiled: August 23, 2011Publication date: March 29, 2012Applicant: Alkermes, Inc.Inventors: Daniel Deaver, Mark Todtenkopf
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Publication number: 20120077802Abstract: Provided herein are spiro-cyclic compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.Type: ApplicationFiled: June 9, 2010Publication date: March 29, 2012Applicant: SUNOVION PHARMACEUTICALS INC.Inventors: Milan Chytil, Sharon R. Engel, Qun Kevin Fang
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Patent number: 8138169Abstract: Treatment regimens for mood disorders that include administration of buprenorphine, alone or in combination with additional pharmacological agents are described. Specifically, treatment regimens that alleviate racing thoughts associated with bipolar disorder, and pharmaceutical compositions and kits for use therein are described. Dosing regimens, compositions, and kits including buprenorphine for treating mania associated with opioid withdrawal are also described.Type: GrantFiled: April 10, 2009Date of Patent: March 20, 2012Assignee: ComgenRx, Inc.Inventors: Bryan T. Oronsky, Neil C. Oronsky
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Patent number: 8138190Abstract: Diaza heterocyclic amide derivatives according to Formula (I) have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: where R5, R6, R7, R8, R9, R10, m, Q, X, and Y are set forth in the description.Type: GrantFiled: March 17, 2009Date of Patent: March 20, 2012Assignee: Amgen Inc.Inventors: Jay P. Powers, Daqing Sun, Xuelei Yan
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Publication number: 20120046266Abstract: The present invention relates to substituted resorcinol derivatives which inhibit the activity of Heat Shock Protein HSP90. The compounds of the invention are therefore useful in treating proliferative diseases such as cancer and neurodegenerative diseases. The present invention also provides processes for preparing these compounds, pharmaceutical compositions comprising them, methods of treating diseases and the pharmaceutical compositions comprising these compounds.Type: ApplicationFiled: April 16, 2010Publication date: February 23, 2012Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Maria Gabriella Brasca, Elena Casale, Ron Ferguson, Paolo Polucci, Fabio Zuccotto
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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: 8110572Abstract: Compounds that inhibit Aurora-kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.Type: GrantFiled: July 16, 2008Date of Patent: February 7, 2012Assignee: Abbott LaboratoriesInventors: Yujia Dai, Zhiqin Ji, Michael R. Michaelides
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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: 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: 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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Patent number: 8088778Abstract: The invention includes benzisoxazole piperazine compositions and methods of using them for modulating sleep.Type: GrantFiled: February 11, 2009Date of Patent: January 3, 2012Assignee: Hypnion, Inc.Inventors: Daniel Coughlin, James F. White, Kazumi Shiosaki, David G. Hangauer, Michael Solomon, Dale M. Edgar
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Publication number: 20110312938Abstract: Disclosed are compounds and pharmaceutically acceptable salts of Formula (I) wherein R1, R2, R3, and RN are as defined herein. Compounds of Formula (I) are useful in the prevention and/or treatment of neurological and psychiatric disorder, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the disclosure and methods of treating the aforementioned conditions using such compounds.Type: ApplicationFiled: June 30, 2009Publication date: December 22, 2011Applicant: Ironwood Pharmaceuticals, Inc.Inventors: Regina Graul, John Jeffrey Talley, Ara Mermerian
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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, Jürgen Benting, Ulrike Wachendorff-Neumann, Thomas Seitz
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Publication number: 20110301133Abstract: The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF receptor TrkA.Type: ApplicationFiled: December 8, 2009Publication date: December 8, 2011Applicant: VM Pharma LLCInventors: Jay Jie-Qiang Wu, Ling Wang
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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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Publication number: 20110301150Abstract: Provided are a substituted azole derivative and pharmaceutically acceptable salts thereof, a pharmaceutical composition including an effective amount of the derivative, and a method for treating Parkinson's disease in a mammal including administering an effective amount of the compound to the mammal. The azole derivative of the following Formula (I) and pharmaceutically useful salts thereof have an efficacy against Parkinson's disease from inhibitory effects of the activity of MAO-B.Type: ApplicationFiled: February 25, 2010Publication date: December 8, 2011Inventors: Cheol-Hyoung Park, Hye-Kyung Min, Mi-Jung Lim, Ji-Won Lee, Jin-Yong Chung, Choon-Ho Ryu, Yeo-Jin Yoon, Mi-Kyung Ji, Joo-Young Park
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Publication number: 20110288088Abstract: Substituted pyrrolo-pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with dysregulated protein kinase activity, like cancer.Type: ApplicationFiled: May 17, 2011Publication date: November 24, 2011Applicant: NERVIANO MEDICAL SCIENCES S.r.I.Inventors: Tiziano BANDIERA, Andrea LOMBARDI BORGIA, Sten Christian ORRENIUS, Ettore PERRONE, Italo BERIA, Daniele FANCELLI, Arturo GALVANI
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Publication number: 20110269768Abstract: This invention is directed to a compound of Formula (I): and forms thereof, wherein A, B, E, G, X and L2 are as defined herein and their use as urotensin II receptor antagonists.Type: ApplicationFiled: July 14, 2011Publication date: November 3, 2011Inventors: William A. Kinney, Edward C. Lawson, Shyamali Ghosh, Diane K. Luci, David F. McComsey
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Patent number: 8044213Abstract: The invention is directed to compounds of formula (1) and pharmaceutically acceptable salts thereof, methods for the preparation thereof, and methods of use thereof.Type: GrantFiled: December 10, 2009Date of Patent: October 25, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Jianping Cai, Shaoqing Chen, Yi Chen, Xin-Jie Chu, Robert Alan Goodnow, Jr., Kang Le, Kin-Chun Luk, Steven Gregory Mischke, Peter Michael Wovkulich
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Publication number: 20110245221Abstract: The present invention relates to formula I compounds having antitumoural activities through, as one possible biological target, the molecular chaperone heat shock protein 90 (Hsp90) inhibition. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of Hsp90 is responsive, and the pharmaceutical compositions containing such compounds.Type: ApplicationFiled: June 30, 2009Publication date: October 6, 2011Applicant: SIGMA-TAU RESEARCH SWITZERLAND S.A.Inventors: Giuseppe Giannini, Walter Cabri, Daniele Simoni, Riccardo Baruchello, Paolo Carminati, Gabriella Singrossi, Silvia Carminati, Giuseppe Paolo Carminati, Claudio Pisano