Ring Nitrogen Is Shared By Two Cyclos Patents (Class 544/282)
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Publication number: 20120046437Abstract: A salt catalyst comprises an ionic complex of i) a nitrogen base comprising one or more guanidine and/or amidine functional groups, and ii) an oxoacid comprising one or more active acid groups, the active acid groups independently comprising a carbonyl group (C?O), sulfoxide group (S?O), and/or a phosphonyl group (P?O) bonded to one or more active hydroxy groups; wherein a ratio of moles of the active hydroxy groups to moles of the guanidine and/or amidine functional groups is greater than 0 and less than 2.0. The salt catalysts are capable of catalyzing ring opening polymerization of cyclic carbonyl compounds.Type: ApplicationFiled: August 19, 2010Publication date: February 23, 2012Applicant: INTERNATIONAL BUSINESS MACHINES CORPORATIONInventors: Daniel Joseph Coady, Kazuki Fukushima, James Lupton Hedrick, Hans Werner Horn, Julia Elizabeth Rice
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Patent number: 8114871Abstract: 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: GrantFiled: April 10, 2008Date of Patent: February 14, 2012Assignees: Pfizer Inc., Pfizer Products 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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Patent number: 8106194Abstract: An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastral diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alpecia, irritable bowel syndrome, sleep disorders, dermatitides, schizophrenia, pain, etc. A pyrrolopyrimidine or pyrrolotriazine derivative substituted with a carbamoyl group represented by the following formula [I]: has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved.Type: GrantFiled: January 6, 2005Date of Patent: January 31, 2012Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Atsuro Nakazato, Taketoshi Okubo, Dai Nozawa, Tomoko Tamita, Ludo E. J. Kennis
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Publication number: 20120020881Abstract: This invention relates to novel compounds suitable for labeling by positron emitting isotopes, such as 18F, 11C, 13N and 15O, through appropriate labeling reagents, such as 18F reagents and methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by positron emission tomography (PET).Type: ApplicationFiled: December 4, 2009Publication date: January 26, 2012Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Lutz Lehmann, Timo Stellfeld, Keith Graham, Jessica Becaud, Linjing Mu
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Publication number: 20120015866Abstract: The present invention relates to prodrugs of parent drug compounds containing heteroaromatic NH groups.Type: ApplicationFiled: December 23, 2010Publication date: January 19, 2012Applicant: Alkermes, Inc.Inventors: Laura Cook Blumberg, Örn Almarsson
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Publication number: 20110297919Abstract: A heterocyclic compound represented by Formula 1 or Formula 2 below and an organic light-emitting device including the heterocyclic compound: wherein X1, X2, and R1 through R16 are defined as in the specification.Type: ApplicationFiled: May 9, 2011Publication date: December 8, 2011Applicant: Samsung Mobile Display Co., Ltd.Inventors: Yoon-Hyun KWAK, Seok-Hwan Hwang, Young-Kook Kim, Hye-Jin Jung, Jong-Hyuk Lee, Hyung-Jun Song
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Patent number: 8071767Abstract: Described herein is an improved, commercially viable and industrially advantageous process for the preparation of paliperidone intermediate 9-hydroxy-3-(2-chloroethyl)-2-methyl-4h-pyrido[1,2-a]pyrimidin-4-one and its hydrochloride salt. The process provides the paliperidone intermediate in higher yield and reduced reaction time compared to the previously disclosed processes, thereby providing for production of paliperidone and its pharmaceutically acceptable acid addition salts in high purity and in high yield.Type: GrantFiled: January 8, 2008Date of Patent: December 6, 2011Assignee: Actavis Group PTC EHFInventors: Uday Rajaram Bapat, Munusamy Jayamani, Sivaji Ravisaravanan, Vigneshwara Ravisankar
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Publication number: 20110294756Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds of Group A or Group, as defined herein, as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.Type: ApplicationFiled: November 12, 2009Publication date: December 1, 2011Inventors: Zhaoning Zhu, William J., Xianhai Huang, Jun Qin, XIaoxiang Liu, Hongmei Li, Wei Zhou, Anandan Palani, Xiaohong Zhu, Monica L. Vicarel, Mihirbaran Mandal, Zhong-Yue Sun, Chad E. Bennett, Troy Michael McCracken, Gioconda V. Gallo
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Publication number: 20110293889Abstract: The present invention relates to a novel process for the preparation of paliperidone and its intermediates and also relates to an improved process for the preparation of paliperidone compound of formula (I).Type: ApplicationFiled: June 15, 2009Publication date: December 1, 2011Applicant: MSN LABORATORIES LIMITEDInventors: Manne Satyanarayana Reddy, Sajja Eswaraiah, Revu Satyanarayana
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Publication number: 20110294786Abstract: A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: Wherein Y, Z, R1, R2, R3, R4, R5, R6, R7, n, m, and o are as described herein. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3?, such as Alzheimer disease.Type: ApplicationFiled: August 3, 2011Publication date: December 1, 2011Applicants: MITSUBISHI TANABE PHARMA CORPORATION, SANOFI-AVENTISInventors: Nathalie CHEREZE, Alistair LOCHEAD, Mourad SAADY, Franck SLOWINSKI, Philippe YAICHE
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Patent number: 8067425Abstract: Embodiments of this invention provide novel cyclic compounds structurally related to diketopiperazines and methods for their therapeutic use. Such compounds are neuroprotective and have utility as therapeutic agents for treatment of diseases, injuries and other conditions characterized by neuronal degeneration and/or death. Compounds are also useful for manufacture of medicaments useful for treatment of such conditions.Type: GrantFiled: August 31, 2004Date of Patent: November 29, 2011Assignee: Neuren Pharmaceuticals LimitedInventors: Margaret Anne Brimble, Jian Guan, Frank Sieg
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Patent number: 8067457Abstract: The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR2 and accordingly are useful for the treatment of a variety of inflammatory, allergic, and autoimmune diseases, disorders, or conditions.Type: GrantFiled: October 26, 2006Date of Patent: November 29, 2011Assignee: Millennium Pharmaceuticals, Inc.Inventors: Shomir Ghosh, Prakash Raman, Kevin Sprott, Amy M. Elder, Sian Griffiths, Francois Soucy, Qing Ye
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Patent number: 8067427Abstract: A pharmaceutical composition comprising ZD6474 or a pharmaceutically acceptable salt thereof, a brittle diluent and a second diluent which is practically insoluble and has ductile compression properties.Type: GrantFiled: May 18, 2005Date of Patent: November 29, 2011Assignee: AstraZeneca ABInventor: Paul William Stott
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Publication number: 20110281878Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: ApplicationFiled: May 13, 2011Publication date: November 17, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Guy W. Bemis, Francesco Gerald Salituro, John Patrick Duffy, John E. Cochran, Edmund Martin Harrington, Mark A. Murko, Keith P. Wilson, Michael Su, Vincent P. Galullo
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Publication number: 20110237576Abstract: The present invention provides a compound which has an effect of inhibiting amyloid-? production and is useful as a therapeutic agent for diseases induced by production, secretion and/or deposition of amyloid-? proteins. The present invention relates to a compound represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof: wherein A is optionally substituted carbocyclic diyl or optionally substituted heterocyclic diyl; B is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; R1 is a group such as optionally substituted lower alkyl; R2 is a group such as hydrogen; and R3a and R3b are each independently a group such as hydrogen, provided that the following compound is excluded.Type: ApplicationFiled: October 22, 2009Publication date: September 29, 2011Applicant: SHIONOGI & CO., LTD.Inventors: Shuji Yonezawa, Yuusuke Tamura, Yuuji Kooriyama, Gaku Sakaguchi
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Publication number: 20110229979Abstract: Novel conjugates and immunogens derived from risperidone and antibodies generated by these immunogens are useful in immunoassays for the quantification and monitoring of risperidone and paliperidone in biological fluids.Type: ApplicationFiled: March 16, 2010Publication date: September 22, 2011Inventors: Salvatore J. Salamone, Jodi Blake Courtney, Daniel J. Cline, Howard Sard, Vishnumurthy Hegde
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Publication number: 20110230459Abstract: The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein Ar1, n, R1, X and Y are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: ApplicationFiled: March 10, 2011Publication date: September 22, 2011Applicant: ABBOTT LABORATORIESInventors: Irene Drizin, George Doherty, Pramila A. Bhatia, Andrew O. Stewart
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Patent number: 8022075Abstract: To provide a diagnostic drug which binds specifically to an amyloid aggregate and/or an amyloid deposit, to thereby realize imaging and quantification of a disease caused by amyloid aggregation and/or deposition. The invention provides a compound represented by formula (1): (wherein X1 represents an optionally substituted bicyclic heterocyclic group; X2 represents a hydrogen atom, a halogen atom, or a chelate-forming group; ring A represents a benzene ring or a pyridine ring; and ring B represents an optionally substituted 5-membered aromatic heterocyclic group which is bonded to the benzene ring or the pyridine ring via a carbon atom of ring B), a salt thereof, a solvate of any of these, or a transition metal coordination compound of any of these, and a diagnostic, preventive, or therapeutic drug containing the same.Type: GrantFiled: November 30, 2006Date of Patent: September 20, 2011Assignees: Fujifilm Ri Pharma Co., Ltd., Daiichi Sankyo Company, LimitedInventors: Kazunori Bando, Kazumi Taguchi
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Publication number: 20110213147Abstract: The invention relates to new heterocyclic compounds of general formula (I), and their salts with a base or an acid: The invention also relates to a process for the preparation of these compounds as well as their use as medicaments, in particular as anti-bacterial agents.Type: ApplicationFiled: May 10, 2011Publication date: September 1, 2011Inventors: Maxime Lampilas, Jozsef Aszodi, David Alan Rowlands, Claude Fromentin
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Publication number: 20110212976Abstract: The present application describes deuterium-enriched risperidone, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: July 5, 2010Publication date: September 1, 2011Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20110207754Abstract: The present invention relates to cyclobutane and methylcyclobutane derivatives, as well as their salts, compositions, and methods of use, which are Janus kinase (JAK) inhibitors useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer and myeloproliferative disorders.Type: ApplicationFiled: February 18, 2011Publication date: August 25, 2011Applicant: INCYTE CORPORATIONInventors: Yun-Long Li, James D. Rodgers
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Publication number: 20110178068Abstract: The invention provides a method of sustained delivery of a tertiary amine-containing parent drug comprising administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile quaternary ammonium salts of tertiary amine-containing parent drugs (or tertiary imine-containing parent drugs) that are derivatized through aldehyde-linked prodrug moieties that reduce the solubility of the prodrug compound at a reference pH as compared to the parent drug. The physical, chemical and solubility properties of these derivatives can be further modulated by the choice of counterion X?. In one embodiment, the present invention provides a prodrug compound of Formula I: where R1-R5 are defined in the written description of the invention.Type: ApplicationFiled: December 23, 2010Publication date: July 21, 2011Applicant: Alkermes, Inc.Inventors: Orn Almarsson, Laura Cook Blumberg, Julius F. Remenar
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Publication number: 20110178077Abstract: The present invention relates to small molecule compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.Type: ApplicationFiled: June 17, 2009Publication date: July 21, 2011Inventors: Priscille Brodin, Thierry Christophe, Zaesung No, Jaeseung Kim, Auguste Genovesio, Denis Philippe Cedric Fenistein, Heekyoung Jeon, Fanny Anne Ewann, Sunhee Kang, Saeyeon Lee, Min Jung Seo, Eunjung Park, Monica Contreras Dominguez, Ji Youn Nam, Eun Hye Kim
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Publication number: 20110166156Abstract: Compounds of Formula I and Formula II and their use for the treatment of neurological and psychiatric disorders including schizophrenia and manic or mixed episodes associated with bipolar I disorder with or without psychotic features is disclosed.Type: ApplicationFiled: December 23, 2010Publication date: July 7, 2011Applicant: Alkermes, Inc.Inventors: Laura Cook Blumberg, Örn Almarsson
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Publication number: 20110160227Abstract: The invention described herein relates to certain bicyclic heteroaromatic N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.Type: ApplicationFiled: August 21, 2009Publication date: June 30, 2011Inventors: Antony Shaw, Rosanna Tedesco
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Patent number: 7968553Abstract: Tetrahydro-4H-pyrido[1,2-a]pyrimidines and related compounds of Formula A: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein n is an integer equal to zero, 1, 2 or 3, and R1, R3, R4, R12, R14, R16, R30, R32, R34 and R36 are defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: GrantFiled: March 12, 2008Date of Patent: June 28, 2011Assignee: Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.p.A.Inventors: Benedetta Crescenzi, Olaf Kinzel, Ester Muraglia, Federica Orvieto, Giovanna Pescatore, Michael Rowley, Vincenzo Summa
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Publication number: 20110144092Abstract: A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein X, R1, R2, R3, R4, and m are defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I), intermediates thereof and their use in therapeutics.Type: ApplicationFiled: December 15, 2010Publication date: June 16, 2011Applicants: SANOFI-AVENTIS, MITSUBISHI TANABE PHARMA CORPORATIONInventors: Aude FAYOL, Alistair LOCHEAD, Mourad SAADY, Julien VACHE, Philippe YAICHE
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Publication number: 20110144132Abstract: A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein Y, R1, R2, R3, and R4 are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I), intermediates thereof and their use in therapeutics.Type: ApplicationFiled: December 15, 2010Publication date: June 16, 2011Applicants: SANOFI-AVENTIS, MITSUBISHI TANABE PHARMA CORPORATIONInventors: Aude FAYOL, Alistair LOCHEAD, Mourad SAADY, Julien VACHE, Philippe YAICHE
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Publication number: 20110137031Abstract: An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastral diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alpecia, irritable bowel syndrome, sleep disorders, dermatitides, schizophrenia, pain, etc. A pyrrolopyrimidine or pyrrolotriazine derivative substituted with a carbamoyl group represented by the following formula [I]: has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved.Type: ApplicationFiled: January 6, 2005Publication date: June 9, 2011Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Atsuro Nakazato, Taketoshi Okubo, Dai Nozawa, Tomoko Tamita, Ludo E.J. Kennis
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Patent number: 7951809Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: April 3, 2008Date of Patent: May 31, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Guy W. Bemis, Francesco G. Salituro, John P. Duffy, John E. Cochran, Edmund M. Harrington, Mark A. Murcko, Keith P. Wilson, Michael Su, Vincent P. Galullo
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Publication number: 20110124863Abstract: The present invention relates to an improved process for obtaining Paliperidone, I, comprising alkylating compound VI, or a salt thereof, with compound V, or a salt thereof, using a base selected from triethylamine or diisopropylethylamine and, optionally, a solvent. Moreover, the invention relies on the preparation of intermediates used in such process.Type: ApplicationFiled: May 28, 2009Publication date: May 26, 2011Inventors: Juan Huguet Clotet, Noelia Calcerrada Muñoz
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Patent number: 7939537Abstract: Pyridopyrimidine carboxamide compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein R1, R2, R3, R4, R5 and R6 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: GrantFiled: September 26, 2006Date of Patent: May 10, 2011Assignee: Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.p.A.Inventors: Vincenzo Summa, Olaf Kinzel, Monica Donghi
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Publication number: 20110104110Abstract: The present invention relates to Substituted Indole Derivatives, compositions comprising at least one Substituted Indole Derivative, and methods of using these Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: August 27, 2008Publication date: May 5, 2011Inventors: Gopinadhan N. Anikumar, 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
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Patent number: 7932385Abstract: A compound of formula (7.2) or an acid addition salt thereof. The compound can be used as a reference standard for monitoring the presence thereof in a paliperidone sample, including monitoring the completion of a paliperidone reaction. Reduction in the amount of the compound in paliperidone can be achieved by crystallization in the presence of a hydride reductant.Type: GrantFiled: July 10, 2009Date of Patent: April 26, 2011Assignee: Synthon BVInventors: Jozef Krajcovic, Jiri Bartl, Petr Benovsky
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Publication number: 20110087024Abstract: The present invention relates to a process for the preparation of 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[1,2-a]-pyrimidin-4-one; and its use in the synthesis of paliperidone.Type: ApplicationFiled: April 20, 2009Publication date: April 14, 2011Applicant: GLENMARK HOUSEInventors: Koilpillai Joseph Prabahar, Pravin Bhalchandra Kulkarni, Laxmikant Madhukar Kelkar, Sanjay Anantha Kale, Shashank Gopal Potdar, Krishna Baban Narwade, Mubeen Ahmed Khan, Jitendra Ramakant Thorat
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Publication number: 20110076214Abstract: One aspect of the present invention relates to salts that are room-temperature ionic liquids (RTILs), methods of making them, and methods of using them in connection with temporary or permanent gas sequestration. Another aspect of the present invention relates to a class of solvents which can be transformed into RTILs by exposure to a gas, and methods of using them in connection with temporary or permanent gas sequestration.Type: ApplicationFiled: January 28, 2008Publication date: March 31, 2011Applicant: Georgetown University Office of Technology commercializationInventors: Tao Yu, Richard G. Weiss, Taisuke Yamada, Mathew George
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Patent number: 7915412Abstract: The present invention relates to a process for preparing paliperidone from its intermediate 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[1,2-a]-pyrimidin-4-one.Type: GrantFiled: August 14, 2007Date of Patent: March 29, 2011Assignee: Teva Pharmaceutical Industries, Ltd.Inventors: Santiago Ini, Naama Chasid, Yaron Shmuely, Kobi Chen
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Patent number: 7915251Abstract: The invention provides ?-helix mimetic structures of formula (I) with the definitions of A, B, D, E, G, W, R1 and R2 as set out in the description and a chemical library relating thereto. The compounds, pharmaceutical compositions comprising the compounds, and methods of the invention using the compounds, relate to the treatment of diseases including fibrosis, such as pulmonary fibrosis.Type: GrantFiled: March 15, 2006Date of Patent: March 29, 2011Assignee: Institute for Chemical GenomicsInventors: Michael Kahn, Masakatsu Eguchi
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Publication number: 20110071167Abstract: The present invention relates generally to the field of treatment and prophylaxis of retinal degenerative diseases. More particularly, the present invention contemplates a method for preventing, reducing the risk of development of, or otherwise treating or ameliorating the symptoms of, age-related macular degeneration (AMD) or related retinal conditions in mammals and in particular humans. The present invention further provides therapeutic compositions enabling dose-dependent or dose-specific administration of agents useful in the treatment and prophylaxis of age-related macular degeneration or related retinal degenerative conditions.Type: ApplicationFiled: November 23, 2010Publication date: March 24, 2011Applicant: PRANA BIOTECHNOLOGY LIMITEDInventors: Ashley BUSH, Colin Louis MASTERS, Penelope Jane HUGGINS, Jack Gordon PARSONS, Gaik Beng KOK, Vijaya KENCHE, Mariana EL SOUS
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Publication number: 20110053915Abstract: The invention relates to novel heterocyclic compounds and to the use thereof, to pharmaceutical compositions containing said chemical compounds as an active ingredient and to the use thereof for producing medicinal preparations for the human being and warm-blood animals for treating diseases caused by the aberrant activity of an Hedgehog (Hh)-signal system, in particular oncological diseases. The invention also relates to the use of the above-mentioned compounds in the form of ‘molecular pharmacological tools’ for examining (in vitro and in vivo) the biochemical features of the Hh-signal system, in particular, the interaction of Hh protein and transmembrane proteins, namely, suppressor Patched (Ptc) and protooncogenic proteins.Type: ApplicationFiled: December 12, 2008Publication date: March 3, 2011Applicant: ALLA CHEM, LLCInventors: Andrey Alexandrovich Ivaschenko, Yan Vadimovich Lavrovsky, Sergey Viktorovich Malyarchuk, Ilya Matusovich Okun, Nikolay Filippovich Savchuk, Sergey Yevgenievich Tkachenko, Alexander Viktorovich Khvat, Alexander Vasilievich Ivaschenko
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Publication number: 20110053930Abstract: The present invention provides small molecule inhibitors of BMP signaling. These compounds may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation.Type: ApplicationFiled: March 13, 2009Publication date: March 3, 2011Applicants: The Brigham and Women's Hospital, Inc., The General Hospital CorporationInventors: Paul B. Yu, Gregory D. Cuny, Kenneth D. Bloch, Randall T. Peterson, Charles C. Hong
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Publication number: 20110053918Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.Type: ApplicationFiled: June 27, 2008Publication date: March 3, 2011Inventors: Zhaoning Zhu, William J. Greenlee, Robert D. Mazzola, JR., Jun Qin, Xianhai Huang, Anandan Palani
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Publication number: 20110039825Abstract: The invention relates to novel ligands the broad spectrum of biological activity of which includes simultaneously ?-adrenoceptors, dopamine receptors, histamine receptors, imidazoline receptors and serotonin receptors, among them serotonin 5-HT7 receptors, which are compounds of general formula 1 in the form of free bases, geometrical isomers, racemic mixtures or individual optical isomers, pharmaceutically acceptable salts and/or hydrates, wherein: R1 is a substituent of amino group, selected from hydrogen, optionally substituted C1-C4 alkyl, acyl, heterocyclyl, alkoxycarbonyl, substituted sulfonyl; R2 is a substituent of cyclic system, selected from hydrogen, halogen, optionally substituted C1-C4 alkyl, CF3, CN, alkoxy, alkoxycarbonyl, carboxyl, heterocyclyl or substituted sulfonyl; Ar is optionally substituted aryl not necessarily annalated with heterocyclyl, or optionally substituted aromatic heterocyclyl; W is optionally substituted (CH2)m group, optionally substituted CH?CH group, optionally substType: ApplicationFiled: December 19, 2008Publication date: February 17, 2011Applicant: Alla Chem, LLCInventors: Andrey Alexandrovich Ivashchenko, Vasilievich Ivashchenko, Yan Vadimovich Lavrovsky, Oleg Dmitrievich Mitkin, Nikolay Filippovich Savchuk, Sergey Yevgenievich Tkachenko, Ilya Matusovich Okun
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Publication number: 20110039842Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. The present invention further provides a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. Pharmaceutical compositions comprising a compound of formula (I) are also provided.Type: ApplicationFiled: July 2, 2009Publication date: February 17, 2011Inventors: John Joseph Deadman, Eric Dale Jones, Giang Thanh Le, David Ian Rhodes, Neeranat Theinthong, Nicholas Andrew Van de Graff, Lisa Jane Winfield
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Publication number: 20110021772Abstract: The invention relates to new heterocyclic compounds of general formula (I), and their salts with a base or an acid: The invention also relates to a process for the preparation of these compounds as well as their use as medicaments, in particular as anti-bacterial agents.Type: ApplicationFiled: April 16, 2010Publication date: January 27, 2011Inventors: Maxime Lampilas, Jozsef Aszodi, David Alan Rowlands, Claude Fromentin
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Patent number: 7872011Abstract: The present invention relates to selective inhibitors of phosphoinositide (PI) 3-kinase ?, use of the selective inhibitors in anti-thrombotic therapy, and a method for screening compounds useful for the new anti-thrombotic therapy by detecting selective inhibitory activity of PI 3-kinase ? of the compound. The invention also relates to novel compounds that are inhibitors of PI 3-kinase.Type: GrantFiled: December 27, 2007Date of Patent: January 18, 2011Assignee: AstraZeneca ABInventors: Shaun P. Jackson, Alan D. Robertson, Vijaya Kenche, Philip Thompson, Hishani Prabaharan, Karen Anderson, Belinda Abbott, Isaac Goncalves, Warwick Nesbitt, Simone Shoenwaelder, Dilek Saylik
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Publication number: 20110009366Abstract: The present invention provides a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. Further provided is a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. A pharmaceutical composition or medicament comprising a compound of Formula I is also provided.Type: ApplicationFiled: April 23, 2010Publication date: January 13, 2011Applicant: AVEXA LIMITEDInventors: Eric Dale Jones, Jonathan Alan Victor Coates, David Ian Rhodes, John Joseph Deadman, Nicholas Andrew Vandegraff, Lisa Jane Winfield, Neeranat Thienthong, William Issa, Neil Choi, Katherinie Macfarlane
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Publication number: 20110008259Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using such CFTR modulators.Type: ApplicationFiled: June 11, 2010Publication date: January 13, 2011Applicant: Vertex Pharmaceuticals IncorporatedInventors: Hayley Binch, Peter D.J. Grootenhuis, Albert Pierce, Lev T.D. Fanning
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Publication number: 20100311969Abstract: The present invention relates to a process for preparation and purification of 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one, also known as paliperidone or 9-hydroxy risperidone. The invention also relates to the preparation of intermediates useful in the process.Type: ApplicationFiled: February 5, 2009Publication date: December 9, 2010Applicant: WATSON PHARMA PRIVATE LIMITEDInventors: Amit Anant Chavan, Ashutosh Vijay Joshi, Manjunath Narayan Bhanu
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Publication number: 20100298566Abstract: A process for the preparation of a psychotropic agent Paliperidone. Preferably, this invention relates to a method for the purification of Paliperidone by making its acid addition salts.Type: ApplicationFiled: November 7, 2008Publication date: November 25, 2010Applicant: ORCHID CHEMICALS & PHARMACEUTICALS LIMITEDInventors: Arulmoli Thangavel, Arunagiri Muthulingam, Thirugnanasambandan Shanmuganathan, Rengasamy Vadivelan, Gurusamy Kasiyappan Saravanakumar, Rao Siripragada Mahender