Three Or More Ring Hetero Atoms In The Additional Hetero Ring Patents (Class 514/236.2)
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Publication number: 20120177717Abstract: Disclosed is a drug delivery system for delivering a drug at a sustained constant rate for a long period, which can be transplanted into an affected part safely and in a simple manner and can deliver a drug to the affected part for a long period. Specifically disclosed is a sustained drug delivery system in which an implant is implanted into a body, wherein the implant is a PEG capsule comprising a box-shaped PEG and a porous PEG sheet.Type: ApplicationFiled: February 16, 2012Publication date: July 12, 2012Applicant: TOHOKU UNIVERSITYInventors: Toshiaki ABE, Nobuhiro NAGAI, Hirokazu KAJI, Takeaki KAWASHIMA, Matsuhiko NISHIZAWA, Koji NISHIDA
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Publication number: 20120172361Abstract: Compounds of the formula (I) and formula (II) and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: June 7, 2010Publication date: July 5, 2012Applicant: CALIFORNIA CAPITAL EQUITY, LLCInventors: Chunlin Tao, Qinwei Wang, Tulay Polat, Laxman Nallan, David Ho, Neil Desai
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Publication number: 20120172217Abstract: The present invention concerns novel heteroaryl-N-aryl thiosemicarbazones and their use in pest control, as insecticides and aca?cides This invention also includes preparation of the pesticide compositions containing the compounds, and methods of controlling insects using the compoundsType: ApplicationFiled: August 5, 2010Publication date: July 5, 2012Applicant: DOW AGROSCIENCES LLCInventors: Annette V. Brown, Gary D. Crouse, Thomas C. Sparks, CaSandra L. McLeod, Emily M. Rigsbee, William T. Lambert, Noormohamed M. Niyaz
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Publication number: 20120165333Abstract: The present invention relates to compounds of formula I useful in the inhibition of c-Met protein kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative disorders.Type: ApplicationFiled: April 20, 2011Publication date: June 28, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: David J. Lauffer, Pan Li, Kira McGinty, Steven M. Ronkin, Qing Tang, Anne-Laure Grillot, Nathan D. Waal
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Publication number: 20120165303Abstract: Compounds are provided that act as potent antagonists of the CCR2 or CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2 and CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, CCR9-mediated diseases, as controls in assays for the identification of CCR2 antagonists and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: March 2, 2012Publication date: June 28, 2012Applicant: ChemoCentryx, Inc.Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Sreenivas Punna, Edward J. Sullivan, Xuefei Tan, William D. Thomas, Solomon Ungashe, Yibin Zeng
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Publication number: 20120157429Abstract: The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: October 25, 2011Publication date: June 21, 2012Inventors: Marion W. Wannamaker, Francesco Salituro, Albert Pierce, Alex Aronov, Gabriel Martinez-Botella, Jian Wang, Luc Farmer, Mark Ledeboer, Tiansheng Wang, Randy Bethiel, Brian Ledford, Emilie Porter Huck
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Patent number: 8202865Abstract: The invention relates to compounds of formula I: wherein R1, R2, Ra, Rb, W, Q and S have the meanings given in claim 16. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.Type: GrantFiled: October 1, 2008Date of Patent: June 19, 2012Assignee: Merck Serono SAInventors: Anna Quattropani, Cyril Montagne, Wolfgang Sauer, Stefano Crosignani, Agnes Bombrun, Mathilde Muzerelle, Jermone Dorbais, Delphine Marin, Jerome Gonzalez, Patrick Gerber
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Patent number: 8202856Abstract: The invention relates to compounds of formula I: wherein R1, R2,Ra, Rb, X have the meanings given in claim 16. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.Type: GrantFiled: December 17, 2008Date of Patent: June 19, 2012Assignee: Merck Serono SAInventors: Anna Quattropani, Christophe Cleva, Eric Sebille, Matthias Schwarz, Delphine Marin, Agnes Bombrun, Wesley Blackaby, Charles Baker-Glenn, Chris Knight, Craig Rouse
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Publication number: 20120149661Abstract: The invention relates to tetra-substituted heteroarylic compounds of the formula (I) wherein X1, X3 and X4 are independently C or N, Y is C—H, N—H or N, wherein the total number of nitrogen atoms represented by X1, X3, X4 and Y is 1 or 2; rings A and B are independently selected from phenyl or pyridyl; R1, R4, R?, R?, n and m are as defined herein. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.Type: ApplicationFiled: August 24, 2010Publication date: June 14, 2012Applicant: NOVARTIS AGInventors: Guido Bold, Pascal Furet, Francois Gessier, Joerg Kallen, Joanna Hergovich Lisztwan, Keiichi Masuya, Andrea Vaupel
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Publication number: 20120149704Abstract: The invention relates to disubstituted benzamide derivatives of the general Formula (I), their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers, prodrugs, metabolites and polymorphs. The invention also relates to processes for the preparation of the compounds of the invention, pharmaceutical compositions containing the compounds and to methods for treating type II diabetes using the compounds of the invention.Type: ApplicationFiled: June 21, 2010Publication date: June 14, 2012Applicant: CADILA HEALTHCARE LIMITEDInventor: Rajendra Kharul
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Publication number: 20120149675Abstract: The present invention is concerned with novel 1,2,3-triazole-imidazole compounds of formula (I) wherein X, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of present invention have affinity and selectivity for the GABA A ?5 receptor. Further the present invention provides a method for the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as therapeutic agents.Type: ApplicationFiled: December 2, 2011Publication date: June 14, 2012Inventor: Andrew Thomas
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Publication number: 20120135981Abstract: The present invention is concerned with novel substituted triazole and imidazole derivatives of Formula (I) wherein R1, R2, A1, A2, A3, A4, X, and Het1 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.Type: ApplicationFiled: July 13, 2010Publication date: May 31, 2012Inventors: Tongfei Wu, Henricus Jacobus Maria Gijsen, Frederik Jan Rita Rombouts, François Paul Bischoff, Didier Jean-Claude Berthelot, Daniel Oehlrich, Michel Anna Jozef De Cleyn, Serge Maria Aloysius Pieters, Garrett Berlond Minne, Adriana Ingrid Velter', Sven Franciscus Anna Van Brandt, Michel Surkyn
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Patent number: 8188075Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of treating or inhibiting angiogenesis in a subject in need thereof and methods for blocking, occluding, or otherwise disrupting blood flow in neo vasculature, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.Type: GrantFiled: August 14, 2007Date of Patent: May 29, 2012Assignee: Synta Pharmaceuticals Corp.Inventors: Weiwen Ying, Kevin Foley
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Publication number: 20120129832Abstract: Provided are a compound having an excellent hypoglycemic action, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition having an excellent therapeutic effect and/or prophylactic effect on type 1 diabetes, type 2 diabetes, and the like, which cause an increase in the blood sugar level due to abnormal sugar metabolism. A compound represented by general formula (I), or a pharmaceutically acceptable salt thereof, is disclosed.Type: ApplicationFiled: August 4, 2010Publication date: May 24, 2012Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Shigeo Yamanoi, Hidenori Namiki, Takahiro Katagiri, Mayuko Akiu, Katsuji Kagechika, Takeshi Honda, Koji Matsumoto, Ryutaro Nakashima
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Publication number: 20120129857Abstract: The present application relates to sodium 1-[6-(morpholin-4-yl)pyrimidin-4-yl]-4-(1H-1,2,3-triazol-1-yl)-1 H-pyrazol-5-olate, to processes for its preparation, to its use for the treatment and/or prophylaxis of diseases and to its use for the preparation of medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular and haematological diseases and kidney diseases, and for promoting wound healing.Type: ApplicationFiled: November 8, 2011Publication date: May 24, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Hans-Christian MILITZER, Jörg GRIES, Stefan KOEP
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Publication number: 20120122869Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.Type: ApplicationFiled: January 13, 2012Publication date: May 17, 2012Inventors: Weiwen Ying, David James, Shijie Zhang, Junghyun Chae, Teresa Przewloka, Howard P. Ng, Hao Li, Zachary Demko, Dinesh U. Chimmanamada, Chi-wan Lee, Zhenjian Du, Kevin Foley, Minghu Song, Lijun Sun, Keizo Koya, Dan Zhou, Shuzhen Qin
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Publication number: 20120121727Abstract: The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing.Type: ApplicationFiled: January 23, 2012Publication date: May 17, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Kai THEDE, Ingo FLAMME, Felix OEHME, Jens-Kerim ERGÜDEN, Friederike STOLL, Joachim SCHUHMACHER, Hanno WILD, Peter KOLKHOF, Hartmut BECK, Jörg KELDENICH, Metin AKBABA, Mario JESKE
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Publication number: 20120115868Abstract: The present invention is concerned with novel triazole compounds of formula (I) wherein A, X, Y, u, v, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts thereof. The compounds of present invention have affinity and selectivity for the GABA A ?5 receptor. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.Type: ApplicationFiled: November 2, 2011Publication date: May 10, 2012Inventors: Stephen Deems Gabriel, Andrew Thomas
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Publication number: 20120115869Abstract: The present invention relates to compounds of formula (I) for use as pharmaceutical active compounds, as well as pharmaceutical formulations containing the same, for the treatment of allergic diseases.Type: ApplicationFiled: July 14, 2010Publication date: May 10, 2012Applicant: MERCK SERONO S.A.Inventors: Stefano Crosignani, Christophe Cleva, Anna Quattropani, Gwenaelle Desforges, Agnès Bombrun
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Publication number: 20120115844Abstract: The present invention is concerned with novel triazole compounds of formula (I) wherein A, X, Y, Z, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of present invention have affinity and selectivity for the GABA A ?5 receptor. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments.Type: ApplicationFiled: November 2, 2011Publication date: May 10, 2012Inventors: Maria-Clemencia Hernandez, Matthew C. Lucas, Andrew Thomas
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Publication number: 20120101072Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound.Type: ApplicationFiled: December 21, 2011Publication date: April 26, 2012Inventors: Joseph A. Burlison, Shijie Zhang, Weiwen Ying, Dinesh U. Chimmanamada, Minghu Song, Junghyun Chae, Stefan M. Schweizer
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Publication number: 20120101099Abstract: The disclosure provides compounds of formula I and methods for preparation thereof. The compounds act as inhibitor of histone deacetylase.Type: ApplicationFiled: July 7, 2010Publication date: April 26, 2012Applicant: ANTHEM BIOSCIENCES PRIVATE LIMITEDInventors: Natesan Selvakumar, Gavara Govinda Rajulu, Annamalai Pazhanimuthu, Sambasivam Ganesh
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Patent number: 8153631Abstract: The present invention provides a triazole compound of the following formula: a prodrug thereof or a pharmaceutically acceptable salt thereof. The above-mentioned triazole compound has superior HSD1 inhibitory activity, and is useful as an HSD1 inhibitor, a therapeutic drug of diabetes or a therapeutic drug of obesity or a therapeutic drug of metabolic syndrome.Type: GrantFiled: November 19, 2009Date of Patent: April 10, 2012Assignee: Amgen Inc.Inventors: Jay P. Powers, Mario G. Cardozo, Hiroyuki Goto, Kazuhito Harada, Katsuaki Imamura, Makoto Kakutani, Isamu Matsuda, Yasuhiro Ohe, Shinji Yata
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Publication number: 20120070467Abstract: The present invention includes and provides a method of delivering a medicament to an eye of a subject in need thereof a solution, the method comprising: (a) providing droplets containing the medicament with a specified average size and average initial ejecting velocity; and (b) delivering the medicament to the eye, where the droplets deliver a percentage of the ejected mass of the droplets to the eye.Type: ApplicationFiled: July 15, 2011Publication date: March 22, 2012Applicant: Corinthian Ophthalmic, Inc.Inventors: Bernard L. Ballou, JR., Mark Packer, Russell John Mumper, Tsontcho Inachulev
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Patent number: 8133890Abstract: Disclosed are pharmaceutical compositions comprising brimondine and timolol for topical ophthalmic delivery and a method of treatment comprising administering said composition when indicated for glaucoma and associated conditions such as elevated intraocular pressure in the eyes of humans.Type: GrantFiled: November 28, 2007Date of Patent: March 13, 2012Assignee: Allergan, Inc.Inventors: Chin-Ming Chang, Gary J. Beck, Cynthia C. Pratt, Amy L. Batoosingh
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Publication number: 20120058056Abstract: This invention concerns a method of treating hemangiomas with a beta blocker by applying the beta blocker onto the hemangiomas directly. The invention also concerns a combination therapy by using a beta blocker along with a corticosteroid or an alpha adrenergic receptor agonist for the treatment of hemangiomas.Type: ApplicationFiled: April 9, 2010Publication date: March 8, 2012Applicant: UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEYInventor: Suqin Guo
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Patent number: 8129358Abstract: Disclosed are new substituted pyrazole and triazole compounds of Formula (I) and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the derivatives together with pharmaceutically acceptable carriers, and uses thereof:Type: GrantFiled: November 8, 2007Date of Patent: March 6, 2012Assignee: Novartis AGInventors: Yi Xia, Kris G. Mendenhall, Paul A. Barsanti, Annette O. Walter, David Duhl, Paul A. Renhowe
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Patent number: 8119634Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: January 4, 2011Date of Patent: February 21, 2012Assignee: Theravance, Inc.Inventors: Brooke Blair, Paul R. Fatheree, Melissa Fleury, Roland Gendron, Ryan Hudson, Robert Murray McKinnell, Michael Wilson
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TRIAZOLE AND IMIDAZOLE DERIVATIVES FOR USE AS TGR5 AGONISTS IN THE TREATMENT OF DIABETES AND OBESITY
Publication number: 20120040985Abstract: The present invention comprises TGR5 agonists of structural formula I, wherein X, R1, R2, and R5 are defined herein, as well as N-oxides of them and pharmaceutically acceptable salts thereof. The invention further comprises composition comprising the compounds, N-oxides, and/or pharmaceutically acceptable salts thereof. The invention also comprises use of the compounds and compositions for treating diseases in which TGR5 is a mediator or is implicated. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases in which TGR5 is a mediator or is implicated.Type: ApplicationFiled: February 12, 2010Publication date: February 16, 2012Applicant: EXELIXIS PATENT COMPANY LLCInventors: Venkataiah Bollu, Brant Clayton Boren, Jackaline Dalgard Julien, Brenton T. Flatt, Nadia Haq, Sarah Hudson, Raju Mohan, Michael Morrissey, Benjamin Pratt, Tie-Lin Wang, Richard Martin, Xiao-Hui Gu -
Publication number: 20120040837Abstract: (1,3,5)-Triazinyl phenyl hydrazones are effective at controlling insects.Type: ApplicationFiled: October 19, 2011Publication date: February 16, 2012Applicant: DOW AGROSCIENCES LLCInventors: Noormohamed M. Niyaz, Katherine A. Guenthenspberger, Ricky Hunter, Annette V. Brown, Jaime S. Nugent
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Publication number: 20120040984Abstract: The invention relates to compounds of the formula (I) either (i) in the state of a base or an acid addition salt, or (ii) in the state of an acid or a base addition salt, as well as to a method for preparing same and to the therapeutic applications thereof.Type: ApplicationFiled: January 27, 2010Publication date: February 16, 2012Applicant: SANOFIInventors: Eykmar Fett, Patrick Mougenot, Claudie Namane, Eric Nicolai, Christophe Philippo
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Publication number: 20120034321Abstract: The invention provides methods for treating ophthalmic disorders comprising at least one nitric oxide enhancing prostaglandin compound or a pharmaceutically acceptable salt thereof, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The nitric oxide enhancing prostaglandin compounds comprise at least one heterocyclic nitric oxide donor group and/or at least one nitroxide group.Type: ApplicationFiled: October 18, 2011Publication date: February 9, 2012Inventor: David S. Garvey
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Publication number: 20120028980Abstract: Methods for managing visceral pain in mammalian subjects are described, in which a NK-1 receptor antagonist is administered to the subject before, during or after administration of general anesthesia. The methods and uses of NK-1 receptor antagonists described herein provide improved visceral pain management and MAC reduction when used with volatile anesthetics for general anesthesia.Type: ApplicationFiled: July 27, 2011Publication date: February 2, 2012Applicant: COLORADO STATE UNIVERSITYInventors: Pedro Boscan, David Twedt
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Publication number: 20120027723Abstract: The present invention relates to taurine or taurine-like substances for the prevention and treatment of a disease associated with retinal ganglion cell degeneration. More particularly the invention relates to a substance selected from the group consisting of taurine, a taurine precursor, a taurine metabolite, a taurine derivative, a taurine analog and a substance required for the taurine biosynthesis for the prevention and treatment of a disease associated with retinal ganglion cell degeneration.Type: ApplicationFiled: July 26, 2011Publication date: February 2, 2012Inventor: Serge Picaud
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Publication number: 20120021989Abstract: The invention relates to procedures and methods of determining a susceptibility to cardiac arrhythmia, including Atrial Fibrillation, Atrial Flutter and Stroke, by assessing the presence or absence of alleles at polymorphic markers found to be associated with risk of these conditions. The invention further relates to kits encompassing reagents for assessing such markers, and diagnostic 5 methods, uses and procedures for utilizing such susceptibility markers.Type: ApplicationFiled: March 30, 2010Publication date: January 26, 2012Applicant: deCODE Genetics ehf.Inventors: Hilma Holm, Daniel Gudbjartsson
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Publication number: 20120022066Abstract: The present invention describes novel triazines, their related pyrimidines and their use in controlling insects. This invention also includes new synthetic procedures, intermediates for preparing the compounds, pesticide compositions containing the compounds, and methods of controlling insects using the compounds.Type: ApplicationFiled: July 20, 2011Publication date: January 26, 2012Applicant: Vestaron CorporationInventors: Robert M. Kennedy, Bruce A. Steinbaugh
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Publication number: 20120015941Abstract: The present invention provides novel amide and sulfonamide substituted heterocyclic urea compounds having useful antibacterial activity. Use of these compounds as pharmaceutical compositions and method of their production are also provided.Type: ApplicationFiled: July 23, 2008Publication date: January 19, 2012Applicant: CRESTONE, INC.Inventors: Joseph Guiles, Thale Jarvis, Sarah Strong, Xicheng Sun, Jian Qiu, John C. Rohloff
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Publication number: 20120015944Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5, R6 R7 and R8 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.Type: ApplicationFiled: September 22, 2011Publication date: January 19, 2012Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
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Publication number: 20120010172Abstract: The present application discloses compounds of formula (I) wherein X is ?O, ?S, ?NH, ?NOH and ?NO-Me; A is —C(?O)—, —S(?O)2—, —C(?S)— and P(?O)(R5)—; B is, —O—, —(CH2)3-6—, and O—(CH2)2-5—; D is, —O—, —CR7R8— and —NR9; m is 0-12, n is 0-12, m+n is 1-20; p is 0-4; R1 is opt.sub. heteroaryl; and pharmaceutically acceptable salts thereof, and prodrugs thereof. The application also discloses the compound for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT), e.g. inflammatory and tissue repair disorders; dermatosis; autoimmune diseases, Alzheimers disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, ataxia telengiectasia.Type: ApplicationFiled: August 31, 2009Publication date: January 12, 2012Applicant: McDERMOTT WILL & EMERY LLPInventors: Mette Knak Christensen, Fredrik Bjorkling
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Publication number: 20120009151Abstract: Disclosed herein are novel triazines and related compounds, the synthesis thereof, and compositions, including pharmaceutical compositions, comprising the novel triazines and related compounds. Such novel triazines and related compounds function to inhibit or block entry of viruses of the Flaviviridae family, including Hepatitis C virus (HCV), into cells that are susceptible to virus infection. These compounds are useful for the treatment, therapy and/or prophylaxis of viral diseases and infection, including HCV infection.Type: ApplicationFiled: December 19, 2008Publication date: January 12, 2012Applicant: Progenics Pharmaceuticals, Inc.Inventors: Amy Qi Han, Glen A. Coburn, Kathleen P. Provoncha, Yakov Rotshteyn
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Publication number: 20120004211Abstract: The invention relates to the use of compounds having pharmacological activity towards the sigma receptor, and more particularly to 1,2,4-triazole derivatives of formula I to processes of preparation of such compounds and to pharmaceutical compositions comprising them.Type: ApplicationFiled: September 12, 2011Publication date: January 5, 2012Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Nadine Jagerovic, Jose Maria Cumella-Montanchez, Maria Pilar Goya-Laza, Alberto Dordal Zueras, Maria Rosa Cuberes-Altisent
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Publication number: 20120004198Abstract: Provided herein are non-peptide GLP-1 receptor modulator compounds, for example, of Formula I, pharmaceutical compositions comprising such compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of a metabolic disorder.Type: ApplicationFiled: February 2, 2011Publication date: January 5, 2012Applicant: ARGUSINA INC.Inventors: Jiayu LIAO, Yufeng Hong, Yong Wang, Thomas W. Von Geldern, Kanyin E. Zhang
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Publication number: 20110319404Abstract: The present invention relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating non-Hodgkin's lymphoma, in a subject in need thereof.Type: ApplicationFiled: September 7, 2011Publication date: December 29, 2011Inventor: Kevin Foley
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Publication number: 20110319414Abstract: The present invention provides a novel P2X3 and/or P2X2/3 receptor antagonist. A compound represented by the formula (I); wherein Ra, Rb and Rc are, (a) Ra and Rb are taken together ?Z; and Rc is a group represented by R1c; or (b) Rb and Rc are taken together to form a bond; and Ra is a group represented by —Y—R1a; R1a and R1c are each independently hydrogen, substituted or unsubstituted alkyl, etc.; R2 and R3 are each independently substituted or unsubstituted aryl, etc.; R4a and R4b are each independently hydrogen, substituted or unsubstituted alkyl, etc.; X is —N(R5)—, etc.; R5 is hydrogen, substituted or unsubstituted lower alkyl, etc.; —Y— is —O—, etc.; ?Z is ?O, etc.; and n is an integer of 0 to 4.Type: ApplicationFiled: February 10, 2010Publication date: December 29, 2011Inventors: Hiroyuki Kai, Takayuki Kameyama, Tsuyoshi Hasegawa, MIho Oohara, Yukio Tada, Takeshi Endoh
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Publication number: 20110319400Abstract: Disclosed are compounds, compositions and methods for treating pain, including inflammatory, visceral, and acute pain. Such compounds are represented by Formula (I) as follows: wherein A1, L1, D, and Q are defined herein.Type: ApplicationFiled: June 27, 2011Publication date: December 29, 2011Inventors: Christopher M. Flores, Paul R. Wade
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Publication number: 20110312930Abstract: The present application relates to novel aryl compounds with aminoalkyl substituents, to processes for their preparation, to their use for treatment and/or prevention of diseases and to their use for the preparation of medicaments for treatment and/or prevention of diseases, in particular for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be carried out as monotherapy or also in combination with other medicaments or further therapeutic measures.Type: ApplicationFiled: October 31, 2009Publication date: December 22, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Michael Härter, Hartmut Beck, Peter Ellinghaus, Kerstin Berhörster, Susanne Greschat, Karl-Heinz Thierauch
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Publication number: 20110312939Abstract: The present invention relates to new compounds of general formula (I), wherein the groups R1 to R3, X1, X2, X3 and L1 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof in such a treatment.Type: ApplicationFiled: September 28, 2009Publication date: December 22, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Steffen Steurer, Peter Ettmayer, Andreas Mantoulidis
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Publication number: 20110311479Abstract: The present invention is directed to modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.Type: ApplicationFiled: August 29, 2011Publication date: December 22, 2011Inventors: Andrew P. Combs, Eddy W. Yue
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Publication number: 20110306597Abstract: The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein the substituents are defined herein, to compositions containing such compounds and to the uses of such compounds for the treatment of allergic and respiratory conditions.Type: ApplicationFiled: June 12, 2009Publication date: December 15, 2011Inventors: James Michael Crawforth, Paul Alan Glossop, Bruce Cameron Hamper, Wei Huang, Bradley Elwood Neal, Simon John Mantell, Kirk Olson, Atli Thorarensen, Steve Ronald Turner
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Patent number: 8076330Abstract: The present invention relates generally to pyrrolidine and thiazolidine DPP-IV inhibitor compounds. The present invention also provides synthetic methods for preparation of such compounds, methods of inhibiting DPP-IV using such compounds and pharmaceutical formulations containing them for treatment of DPP-IV mediated diseases, in particular, Type-2 diabetes.Type: GrantFiled: January 13, 2011Date of Patent: December 13, 2011Assignee: Amgen Inc.Inventors: Heiko Kroth, Tim Feuerstein, Frank Richter, Jürgen Boer, Michael Essers, Bert Nolte, Matthias Schneider, Matthias Hochgürtel, Fritz-Frieder Frickel, Arthur G. Taveras, Christoph Steeneck