The Additional Hetero Ring Is A Cyclo In A Polycyclo Ring System Patents (Class 548/364.4)
-
Publication number: 20130237500Abstract: The present invention relates to novel (thio)carboxamides, their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: ApplicationFiled: November 14, 2011Publication date: September 12, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Juergen Benting, Philippe Desbordes, Stephanie Gary, Joerg Greul, Tomoki Tsuchiya, Ulrike Wachendorff-Neumann
-
Publication number: 20130217727Abstract: The present invention relates to fungicidal 1-(heterocyclic carbonyl)-2-substituted pyrrolidines and their thiocarbonyl derivatives, their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions.Type: ApplicationFiled: October 20, 2011Publication date: August 22, 2013Inventors: Jurgen Benting, Peter Dahmen, Philippe Desbordes, Stephanie Gary, Hiroyuki Hadano, Jean-Pierre Vors, Ulrike Wachendorff-Neumann
-
Publication number: 20130203818Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: April 27, 2011Publication date: August 8, 2013Applicant: CALCIMEDICA, INC.Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
-
Publication number: 20130190338Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: ApplicationFiled: March 11, 2013Publication date: July 25, 2013Applicant: ALLERGAN, INC.Inventor: ALLERGAN, INC.
-
Publication number: 20130177529Abstract: Aryl substituted pyrazole derivatives are provided, as well as processes for their preparation. The invention also provides compositions and methods for the treatment of HCV by administering a compound of the present invention, alone or in combination with additional antiviral agents, in a therapeutically effective amount.Type: ApplicationFiled: November 15, 2012Publication date: July 11, 2013Inventors: Youhong Hu, Bin Xu, Yun Liao, Kenneth Nawoschik, Yixin Liu, Anthony Sandrasagra, Reza Fathi, Zhen Yang
-
Publication number: 20130172351Abstract: Novel dihydropyrazole derivatives of formula (I) wherein L, R, R3, R4, R5, R6, R7, X1, X2, X3, X4, Y, m and n have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.Type: ApplicationFiled: June 26, 2012Publication date: July 4, 2013Applicant: MERCK PATENT GMBHInventors: Henry Yu, Thomas E. Richardson, Robert James Foglesong, Lizbeth Celeste DeSelm, Andreas Goutopoulos
-
Publication number: 20130165460Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: ApplicationFiled: February 20, 2013Publication date: June 27, 2013Applicant: ALLERGAN, INC.Inventor: ALLERGAN, INC.
-
Patent number: 8455497Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.Type: GrantFiled: February 12, 2009Date of Patent: June 4, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael R. Hale, Roger Tung, Stephen Price, Robin David Wilkes, Wayne Carl Schairer, Ashley Nicholas Jarvis, Andrew Spaltenstein, Eric Steven Furfine, Vicente Samano, Istvan Kaldor, John Franklin Miller, Michael Stephen Brieger, Ronald George Sherrill
-
Publication number: 20130131119Abstract: The present invention relates to fungicidal N-[(het)arylethyl)] pyrazolecarboxamide or thiocarboxamide and their heterosubstituted analogues, their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions.Type: ApplicationFiled: June 1, 2011Publication date: May 23, 2013Inventors: Jurgen Benting, Christoph Braun, Pierre-Yves Coqueron, Pierre Cristau, Peter Dahmen, Philippe Desbordes, Stephanie Gary, Jorg Greul, Hiroyuki Hadano, Thomas Knobloch, Ruth Meissner, Ulrike Wachendorf-Neumann, Lothar Willms
-
Publication number: 20130123507Abstract: The bicyclo-substituted pyrazolon-azo derivatives of formula (I) or pharmaceutical acceptable salts, hydrates or solvates thereof, methods for their preparation, pharmaceutical compositions containing the same and their use as a therapeutic agent, especially as thrombopoietin (TPO) mimetics and their use as agonists of thrombopoietin receptor are disclosed. The definition of substituents in formula (I) are the same as defined in the description.Type: ApplicationFiled: January 16, 2013Publication date: May 16, 2013Applicants: SHANGHAI HENGRUI PHARMACEUTICAL CO. LTD., JIANGSU HENGRUI MEDICINE CO. LTD.Inventors: JIANGSU HENGRUI MEDICINE CO. LTD., SHANGHAI HENGRUI PHARMACEUTICAL CO. LTD.
-
Publication number: 20130116247Abstract: Compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts there-of. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies.Type: ApplicationFiled: April 5, 2011Publication date: May 9, 2013Applicant: MANNKIND CORPORATIONInventors: Qingping Zeng, Andras Toro, John Bruce Patterson, Warren Stanfield Wade, Zoltan Zubovics, Yun Yang, Zhipeng Wu
-
Publication number: 20130102790Abstract: The present invention relates to N-cycloalkyl-N-bicyclicmethylene-carboxamide, thiocarboxamide or N-substituted carboximidamide derivatives of formula (I) wherein A represents a carbo-linked, 5-membered heterocyclyl group, T represents O or S, Z1 represents a C3-C7-cycloalkyl group, X represents N or a CZ7 and Y1, Y2, Z2, Z3, L1 and L2 represent various substituents. Their process of preparation, the preparation of intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions are also disclosed.Type: ApplicationFiled: December 13, 2012Publication date: April 25, 2013Inventors: Jurgen BENTING, Peter DAHMEN, Philippe DESBORDES, Stephanie GARY, Pierre GENIX, Benoit HARTMANN
-
Patent number: 8410135Abstract: The invention is directed to 4,5-dihydro-(1H)-pyrazole (pyrazoline) derivatives as cannabinoid CB1 receptor modulators, to pharmaceutical compositions comprising these compounds, to methods for their syntheses, to methods for preparing novel intermediates useful for their syntheses, and to methods for preparing compositions. The invention also relates to the uses of compounds and compositions administered to patients to achieve a therapeutic effect in multiple sclerosis, traumatic brain injury, pain including chronic pain, neuropathic pain, acute pain and inflammatory pain, osteoporosis, appetite disorders, epilepsy, Alzheimer's disease, Tourette's syndrome, cerebral ischaemia, emesis, nausea, and gastrointestinal disorders. Compounds of the present disclosure are directed to formula (I): wherein the substituents have the definitions given in the specification.Type: GrantFiled: June 11, 2008Date of Patent: April 2, 2013Assignee: Solvay Pharmaceuticals B.V.Inventors: Josephus H. M. Lange, Hendrik C. Wals, Bernard J. Van Vliet, Mahmut Yildirim
-
Publication number: 20130035323Abstract: The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives are GlyT1 inhibitors.Type: ApplicationFiled: August 3, 2012Publication date: February 7, 2013Applicant: Abbott GmbH & Co. KGInventors: Wilhelm AMBERG, Udo LANGE, Frauke POHLKI
-
Patent number: 8367710Abstract: The bicyclo-substituted pyrazolon-azo derivatives of formula (I) or pharmaceutical acceptable salts, hydrates or solvates thereof, methods for their preparation, pharmaceutical compositions containing the same and their use as a therapeutic agent, especially as thrombopoietin (TPO) mimetics and their use as agonists of thrombopoietin receptor are disclosed. The definition of substituents in formula (I) are the same as defined in the description.Type: GrantFiled: January 4, 2009Date of Patent: February 5, 2013Assignees: Jiangsu Hengrui Medicine Co. Ltd., Shanghai Hengrui Pharmaceutical Co. Ltd.Inventors: Peng Cho Tang, Hejun Lü, Hao Zheng, Yiqian Chen, Hongbo Fei, Shenglan Wang, Li Wang
-
Publication number: 20130023576Abstract: Pyrazole compounds of formula (Ia) or (Ib) and pharmaceutically acceptable salts thereof, wherein Ra, Rb, Rc, Rd, Y1, Y2, Y3, Y4, Y5, Z, R1, R2, n and R3 have one of the meanings as indicated in the specification and claims, to their use as medicaments, to pharmaceutical formulations containing the compounds and to pharmaceutical formulations containing the compounds in combination with one or more active substances.Type: ApplicationFiled: January 19, 2012Publication date: January 24, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Ralf Anderskewitz, Domnic Martyres, Thorsten Oost, Wolfgang Rist, Peter Seither
-
Publication number: 20120323016Abstract: The present invention relates to the preparation of a class of novel, optically active compounds derived from oligomeric proanthocyanidins (OPCs), more particularly to oligomers of epicatechin. These compounds include multidentate ligands and their metal complexes for use in catalysis. Methods of depolymerising proanthocyanidins to form catechins, and particularly depolymerising proanthocyanidins derived from plant sources to form novel epicatechins having application in catalysis are disclosed.Type: ApplicationFiled: December 17, 2010Publication date: December 20, 2012Applicant: NATIONAL UNIVERSITY OF SINGAPOREInventors: Dejian Huang, Wei Chen, Runyun Ni, Caili Fu, Yi Ling Quek
-
Patent number: 8329899Abstract: Compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) and methods of inhibiting Hsp90 in a cell, treating or preventing a proliferation disorder in a mammal and treating cancer in a mammal comprising administering a compound of formula (I) to a patient or a cell. Variable R5 is an optionally substituted heteroaryl; an optionally substituted 6 to 14-membered aryl; a bicyclic 9-member heterocycle optionally substituted at any substitutable nitrogen or carbon atoms; or a substituent R18, defined herein. Ring A is an aryl or a heteroaryl optionally further substituted with one or more substituents in addition to R3. Substituent R3 is defined herein.Type: GrantFiled: February 14, 2011Date of Patent: December 11, 2012Assignee: Synta Pharmaceuticals, Corp.Inventors: Weiwen Ying, Shijie Zhang, Zhenjian Du, Kevin Foley
-
Publication number: 20120302609Abstract: The invention relates to pyrazoline substituted compounds and methods for activating PKM2. The compounds and methods are useful in treating or preventing a disease or disorder selected from cancer, cell proliferative disorder, inflammatory disorder, metabolic disorder, and immune system disorder.Type: ApplicationFiled: May 23, 2012Publication date: November 29, 2012Applicant: Dynamix Pharmaceuticals LTD.Inventors: Oren M. Becker, Alina Shitrit, Nili Schutz, Efrat Ben-Zeev, Avihai Yacovan, Rachel Ozeri, Daniel Sherman, Vered Behar, Osnat Kashtan, Alexander Konson
-
Publication number: 20120302566Abstract: The present invention relates to compounds defined by formula (I) wherein the variables R1, R2, R3, m, and n are defined as in claim 1, possessing valuable pharmacological activity. Particularly, the compounds are activators of the receptor GPR40 and thus are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.Type: ApplicationFiled: November 30, 2011Publication date: November 29, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Frank Himmelsbach, Remko Bakker, Matthias Eckhardt, Dieter Hamprecht, Elke Langkopf, Holger Wagner
-
Publication number: 20120289506Abstract: 5-membered heterocyclic derivatives represented by general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof. In the formula (I), T represents nitro, cyano and the like; ring J represents aryl or heteroaryl; Q represents carboxy, 5-tetazolyl and the like; Y represents H, OH, NH2, halogen, haloalkyl and the like; X1 and X2 independently represent CR2 or N; R2 represents H, alkyl and the like; R1 represents halogen, cyano, haloalkyl, A-D-E-G-L-M, —N(-D-L-M)2 and the like, A represents a single bond, O, S and the like; D, G and M independently represent optionally substituted alkylene, cycloalkylene, heterocycloalkylene, arylene, heteroarylene and the like; E and L independently represent a single bond, O, S, COO, SO2 and the like.Type: ApplicationFiled: June 12, 2012Publication date: November 15, 2012Applicant: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Kazuo Shimizu, Yasushi Takigawa, Hideki Fujikura, Masato Iizuka, Masahiro Hiratochi, Norihiko Kikuchi
-
Publication number: 20120238541Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.Type: ApplicationFiled: September 17, 2010Publication date: September 20, 2012Applicant: Almac Discovery LimitedInventors: Mark Peter Bell, Timothy Harrison, Sumita Bhattacharyya, James Samuel Shane Rountree, Frank Burkamp, Stephen Price, Calum MacLeod, Richard Leonard Elliott, Phillip Smith, Toby Jonathan Blench, Colin Roderick O'Dowd, Lixin Zhang, Graham Peter Trevitt, Hazel Joan Dyke
-
Patent number: 8268877Abstract: Compounds of formula (I) in which the substituents are as defined in claim 1, are suitable for use as microbiocides.Type: GrantFiled: June 7, 2010Date of Patent: September 18, 2012Assignee: Syngenta Crop Protection, LLCInventors: Harald Walter, Daniel Stierli
-
Patent number: 8242159Abstract: Disclosed herein are novel 1,3-dihydro-5-isobenzofurancarbonitrile derivatives represented by Formula 1, or pharmaceutically acceptable salts thereof. Also disclosed is a pharmaceutical composition for treating or preventing premature ejaculation including the compound. The 1,3-dihydro-5-isobenzofurancarbonitrile derivatives have a short half-life and inhibit the ejaculation process by selectively inhibiting serotonin reuptake via a serotonin reuptake transporter present in a presynaptic neuron. Thus, the compounds are useful in the treatment and prevention of premature ejaculation.Type: GrantFiled: October 31, 2008Date of Patent: August 14, 2012Assignee: Dong-A Pharmaceutical. Co., LtdInventors: Yeong Geon Lee, Soo-Jung Choi, Tae-Kyung Kang, Mi-Jeong Seo, Chang-Yong Shin, Kyung-Seok Lee, Gook-Jun Ahn, Seul-Min Choi, Yong-Duck Kim, Dong-Hwan Kim, Kyung-Koo Kang, Hyun-Joo Shim, Dong-Sung Kim, Byoung-Ok Ahn, Moo-Hi Yoo
-
Publication number: 20120202815Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein Y is a 5-membered, fully or partially unsaturated heterocyclic ring containing 2-4 carbon atoms and 2-3 nitrogen atoms as ring members, the ring substituted with Z on a ring member atom connected through an adjacent single ring member atom to the ring member atom attaching the heterocyclic ring to the phenyl ring of Formula 1, and optionally further substituted with up to 2 substituents independently selected from R5 on carbon atom ring members and from R6 on nitrogen atom ring members; Z is an 8-, 9-, 10- or 11-membered fused heterobicyclic ring system containing ring members selected from carbon atoms and 1 to 4 heteroatoms independently selected from up to 2O, up to 2S and up to 4 N atoms, wherein up to 3 carbon atom ring members are independently selected from C(?O) and C(?S), and the sulfur atom ring members are independently selected from S(?O)u(?NR7)z, the ring system optionally substituted wiType: ApplicationFiled: October 12, 2010Publication date: August 9, 2012Applicant: E.I.DU PONT DE NEMOURS AND COMPANYInventors: John Lawrence Andreassi II, Andrew Edmund Taggi
-
Patent number: 8231754Abstract: An dye compound of the following formula (1): wherein D represents a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group; L represents ?CR2—, ?N—, or ?N—NH—; R1 represents a monovalent substituent; R2 represents a hydrogen atom or a cyano group; n indicates an integer of from 0 to 4; when n is 2 or more, then plural R1's may be the same or different.Type: GrantFiled: February 27, 2009Date of Patent: July 31, 2012Assignee: FUJIFILM CorporationInventors: Yoshihiko Fujie, Tetsuya Watanabe, Hisashi Mikoshiba
-
Patent number: 8217044Abstract: There are provided compounds of the formula wherein X, Y and R1 to R8 are as described herein and the enantiomers and pharmaceutically acceptable salts and esters thereof which compounds have anticancer activity.Type: GrantFiled: March 28, 2011Date of Patent: July 10, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Xin-Jie Chu, Qingjie Ding, Nan Jiang, Jing Zhang, Zhuming Zhang
-
Publication number: 20120157487Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: ApplicationFiled: December 9, 2011Publication date: June 21, 2012Applicant: ALLERGAN, INC.Inventors: Haiqing Yuan, Richard I. Beard, Xiaoxia Liu, John E. Donello, Veena Viswanath, Michael E. Garst
-
Patent number: 8188085Abstract: Novel derivatives of enfumafungin are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (1,3)-?-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.Type: GrantFiled: August 7, 2009Date of Patent: May 29, 2012Assignees: Merck Sharp & Dohme Corp., Seynexis, Inc.Inventors: Mark L. Greenlee, Robert Wilkening, James Apgar, Donald Sperbeck, Kenneth J. Wildonger, Dongfang Meng, Dann L. Parker, Jr., Gregory J. Pacofsky, Brian H. Heasley, Ahmed Mamai, Kingsley Nelson
-
Publication number: 20120129818Abstract: Ortho methoxy phenolic compounds are provided that include methylenedioxyphenyl ferulate and ferulylproline and derivatives thereof. Pharmaceutical compositions comprising the compounds and methods of using the compounds for treating cardiovascular diseases, including hypertension, atherosclerosis, coronary heart disease, angina, stroke, and myocardial infarction, are further provided. The compounds are also useful in reducing low-density lipoprotein oxidation, improving or increasing vasodilation, and reducing plaque destabilization in a subject.Type: ApplicationFiled: April 23, 2010Publication date: May 24, 2012Inventor: Desikan Rajagopal
-
Publication number: 20120129828Abstract: The present invention relates to compounds of Formula (I) that are have activity as S1P1 receptor modulating agents, more specifically to specifically compounds that are S1P1 receptor agonists. The invention also related to the use of such compounds to treat diseases associated with inappropriate S1P1 receptor activity such as autoimmune diseases.Type: ApplicationFiled: June 18, 2009Publication date: May 24, 2012Inventors: Victor J. Cee, Jian Lin, Xiang Y. Yu, Zhaoda Zhang
-
Publication number: 20120123129Abstract: The present invention relates to the use of compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R3, R9, R10, R11, R12 and G have the meanings given above as insecticides and/or acaricides and/or fungicides.Type: ApplicationFiled: April 28, 2010Publication date: May 17, 2012Applicant: Bayer CropScience AGInventor: Alfred ANGERMANN
-
Patent number: 8178689Abstract: The present invention provides novel compounds of formula I, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.Type: GrantFiled: June 9, 2011Date of Patent: May 15, 2012Assignee: Hoffman-La Roche Inc.Inventor: Ramakanth Sarabu
-
Publication number: 20120108645Abstract: Compounds of formula (I) in which the substituents are as defined in claim 1, are suitable for use as microbiocides.Type: ApplicationFiled: June 7, 2010Publication date: May 3, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Harald Walter, Daniel Stierli
-
Patent number: 8168796Abstract: There are provided novel fluorescent agents, such as pyrazoline compounds represented by formula (I): (wherein R1, R2 and R3 are as defined in the specification), having an ethynyl group in the molecule, which have high absorptivity in the ultraviolet-visible short wavelength range (for example, 350 nm-420 nm).Type: GrantFiled: January 19, 2009Date of Patent: May 1, 2012Assignee: Nippon Chemical Works Co., Ltd.Inventors: Kazuhiko Mizuno, Hideyuki Takagaki, Hirokazu Iwahashi, Kaname Inoue
-
Publication number: 20120101103Abstract: Compounds of Formula I: (I) in which A, A1, R1, R7a, R7b, R8 and R10 have the meanings given in the specification, are DP2 receptor inhibitors useful in the treatment of useful in the treatment and prevention of immunologic diseases, allergic diseases such as asthma, allergic rhinitis and atopic dermatitis, and other inflammatory diseases mediated by prostaglandin D2 (PGD2). The compounds of Formula I may also be useful in treating diseases or medical conditions involving the Th2 T cell via production of IL-4, IL-5 and/or IL-13.Type: ApplicationFiled: December 18, 2009Publication date: April 26, 2012Applicant: ARRAY BIOPHARMA INC.Inventors: Adam Cook, Kevin W. Hunt, Robert Kirk Delisle, Todd Romoff, Christopher T. Clark, Ganghyeok Kim, Christopher P. Corrette, George A. Doherty, Laurence E. Burgess
-
Patent number: 8153682Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, G, Y, R1, R2, R3, and R4 are defined herein.Type: GrantFiled: July 18, 2008Date of Patent: April 10, 2012Assignee: Janssen Pharmaceutica, NVInventors: Shawn T. Branum, Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Michele C. Jetter, Yi Liu, Donald Ludovici, Mark J. Macielag, Jay M. Matthews, James J. McNally, Laura M. Reaney, Ronald K. Russell, Ning Qin, Christopher Teleha, Kenneth M. Wells, Scott C. Youells, Mark A. Youngman
-
Patent number: 8143302Abstract: The presently disclosed subject matter provides compositions that selectively bind cyclooxygenase-2 and comprise a therapeutic and/or diagnostic moiety. Also provided are methods for using the disclosed compositions for diagnosing (i.e., by imaging) a target cell and/or treating a disorder associated with a cyclooxygenase-2 biological activity.Type: GrantFiled: June 11, 2010Date of Patent: March 27, 2012Assignee: Vanderbilt UniversityInventors: Lawrence J. Marnett, Md. Jashim Uddin, Brenda C. Crews
-
Publication number: 20120053132Abstract: Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 enzymes.Type: ApplicationFiled: November 1, 2011Publication date: March 1, 2012Applicant: Sequoia Pharmaceuticals, Inc.Inventors: Michael Eissenstat, Dehui Duan
-
Publication number: 20120028938Abstract: The present invention relates to pyrazole compounds of formula (I) and pharmaceutically acceptable salts thereof having CRTH2-activity, wherein W, L1, L2, X, L3, Y, R1 and R2 are as defined in the specification and claims, to their use as medicaments and to pharmaceutical formulations, containing said compounds or containing a combination of said compounds with one or more active substances.Type: ApplicationFiled: January 24, 2011Publication date: February 2, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Thorsten OOST, Ralf ANDERSKEWITZ, Dieter Wolfgang HAMPRECHT, Christoph HOENKE, Domnic MARTYRES, Wolfgang RIST, Peter SEITHER
-
Publication number: 20120028800Abstract: Compounds of Formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.Type: ApplicationFiled: January 25, 2010Publication date: February 2, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Christopher John Mathews, John Finney, James Nicholas Scutt, Louisa Robinson, John Stephen Delaney
-
Patent number: 8106085Abstract: The present invention relates to indoline-substituted pyrazoline compounds of formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.Type: GrantFiled: July 17, 2006Date of Patent: January 31, 2012Assignee: Laboratorios Del Dr. Esteve, S.A.Inventors: Antonio Torrens Jover, Susana Yenes Minguez
-
Publication number: 20110313002Abstract: The present invention provides novel compounds of formula I, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.Type: ApplicationFiled: June 9, 2011Publication date: December 22, 2011Inventor: Ramakanth Sarabu
-
Publication number: 20110305776Abstract: The present invention relates to novel compounds, methods, and compositions capable of decreasing HIF hydroxylase enzyme activity, thereby increasing the stability and/or activity of hypoxia inducible factor (HIF).Type: ApplicationFiled: November 11, 2009Publication date: December 15, 2011Applicant: FibroGen, Inc.Inventors: Wen-Bin Ho, Lee A. Flippin, Craig Mossman, Eric D. Turtle, Lee R. Wright
-
Patent number: 8071782Abstract: This invention concerns the synthesis of highly substituted pyrazoles, which are structural components of pharmacological compounds, through reaction of hydrazones with nitroolefins.Type: GrantFiled: October 2, 2008Date of Patent: December 6, 2011Assignee: Janssen Pharmaceutica NVInventors: Xiaohu Deng, Neelakandha S. Mani
-
Publication number: 20110293520Abstract: The present invention relates to a compound represented by formula (E). The present invention also relates to a compound represented by the formula (E) for use in the treatment or prevention of diseases linked to protein aggregation and/or neurodegenerative diseases. Moreover, the present invention relates to pharmaceutical and diagnostic compositions comprising the compound of the invention as well as to a kit. Furthermore, the present invention relates to a method of imaging deposits of aggregated protein. A kit for preparing a detectably labelled compound of the present invention is also disclosed. Formula (E) wherein X, Y and L are independently nondirectionally selected from —C(R1)(R2)—, —C(R3)?, —N(R4)—, —N?, —N+(R5)?, —O— and —S—; M and Z are independently nondirectionally selected from formula (I) and formula (II).Type: ApplicationFiled: June 9, 2009Publication date: December 1, 2011Inventors: Armin Giese, Uwe Bertsch, Hans Kretzschmar, Mathias Habeck, Thomas Hirschberger, Paul Tavan, Christian Griesinger, Andrei Leonov, Sergey Ryazanov, Petra Weber, Markus Geissen, Martin H. Groschup, Jens Wagner
-
Publication number: 20110281795Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.Type: ApplicationFiled: January 15, 2010Publication date: November 17, 2011Inventors: Songnian Lin, Fengqi Zhang, Emma R. Parmee, Sunita V. Dewnani
-
Patent number: 8039502Abstract: A new class of phosphoinositide-dependent kinase-1 (PDK-1) inhibitors of Formula I: wherein X wherein X is —CF3, Ar is selected from and R is selected from where R? is L-Lys, D-Lys, ?-Ala, L-Lue, L-Ile, Phe, SO2CH2CH2NH2, SO2NH2, Asn, Glu or Gyl, and R? is methyl, ethyl, allyl, CH2CH2OH, CH2CN, CH2CH2CN, CH2CONH2,Type: GrantFiled: July 24, 2008Date of Patent: October 18, 2011Assignee: The Ohio State University Research FoundationInventors: Ching-Shih Chen, Hao-Chieh Chiu, Dasheng Wang, John S. Gunn, Larry S. Schlesinger
-
Patent number: 8039640Abstract: The invention relates to new morphine compounds of the formula: where R1 represents a C1-6 alkyl radical and the radicals R2 and R3 are independently selected from the group consisting of hydrogen atoms, methyl groups and acetyl groups.Type: GrantFiled: February 15, 2007Date of Patent: October 18, 2011Assignee: Universitätsklinikum FreiburgInventor: Rainer Trittler
-
Publication number: 20110230463Abstract: [Object] Provided is a compound which has an excellent S1P1 agonist action, and is useful particularly as an active ingredient for an agent for preventing and/or treating a disease induced by undesirable lymphocyte infiltration or a disease induced by abnormal proliferation or accumulation of cells. [Means for Solution] According to the present invention, a 2H-chromene compound or a derivative thereof which has an excellent S1P1 agonist action, and is useful particularly as an active ingredient of an agent for preventing and/or treating a disease induced by undesirable lymphocyte infiltration or a disease induced by abnormal proliferation or accumulation of cells can be provided. The 2H-chromene compound and a derivative thereof which are the compounds of the present invention have an S1P1 agonist action, and can be used particularly for prevention and/or treatment of a disease induced by undesirable lymphocyte infiltration or a disease induced by abnormal proliferation or accumulation of cells.Type: ApplicationFiled: December 4, 2009Publication date: September 22, 2011Applicant: ASTELLAS PHARMA INC.Inventors: Hironori Harada, Kazuyuki Hattori, Kazuya Fujita, Sunao Imada, Tatsuaki Morokata