Hetero Ring In The Polycyclo Ring System Patents (Class 546/196)
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Patent number: 8063223Abstract: Disclosed is a benzylpiperizine compound represented by formula (1) or a pharmaceutically acceptable salt thereof, which is useful as a medicinal agent such as an antidepressant agent. (In the formula (1), R1 represents a hydrogen atom or a methyl group; R2 is a group bound in a p- or m-position relative to a methylene group and represents a chlorine atom bound in a p-position, a bromine atom bound in a p-position, a methyl group bound in a p-position, a chlorine atom bound in a m-position or a bromine atom bound to in a m-position; X represents a methylene or an oxygen atom; and n represents an integer of 1 to 3.Type: GrantFiled: February 4, 2009Date of Patent: November 22, 2011Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Tomohiro Toyoda, Hidefumi Yoshinaga
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Patent number: 8063069Abstract: The present invention is concerned with a novel benzamide derivative and the pharmaceutically acceptable acid addition salts thereof, pharmaceutical compositions comprising said novel compound, processes for preparing said compounds and compositions, and the use thereof as a medicine in the treatment of gastrointestinal motility disorders.Type: GrantFiled: October 30, 2007Date of Patent: November 22, 2011Assignee: Janssen Pharmaceutica N.V.Inventors: Joannes Adrianus Jacobus Schuurkes, Willy Joannes Carolus Van Laerhoven
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Publication number: 20110281847Abstract: The present invention relates to a selective estrogen receptor modulator of formula I or Ia: (I) (Ia); or a pharmaceutical acid addition salt thereof; useful for treating vasomotor symptoms, in particular hot flashes, night sweats and other symptoms that affect women around menopause.Type: ApplicationFiled: June 23, 2011Publication date: November 17, 2011Applicant: ELI LILLY AND COMPANYInventors: Robert Dean Dally, Jeffrey Alan Dodge, Scott Alan Frank, Ronald Jay Hinklin, Timothy Alan Shepherd, Owen Brendan Wallace
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Publication number: 20110275800Abstract: This invention relates to a compound of formula (I) and the pharmaceutically acceptable salts thereof wherein R1, R2, R4. Ar and Het are as defined herein. The invention also relates to methods of using the compound of formula (I) to treat a diseases and disorders that are mediated or sustained through the activity of CCR10.Type: ApplicationFiled: April 8, 2009Publication date: November 10, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Asitha Abeywardane, Derek Cogan, Younggi Choi, Donghong A. Gao, Daniel R. Goldberg, Alexander Heim-Riether, Craig Andrew Miller, Philip Dean Ramsden, Lana Louise Smith Keenan, Roger John Snow, Yang Yu
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Publication number: 20110245226Abstract: The present application describes substituted piperidinyl modulators of MIP-1? or CCR-1 or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using said modulators are disclosed.Type: ApplicationFiled: June 8, 2011Publication date: October 6, 2011Inventors: Percy H. Carter, Cullen L. Cavallaro, John V. Duncia, Daniel S. Gardner, John Hynes, Rui-Qin Liu, Joseph B. Santella, Dharmpal S. Dodd
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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
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Publication number: 20110224228Abstract: 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 method 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: ApplicationFiled: August 10, 2009Publication date: September 15, 2011Applicants: Merck Sharp & Dohme Corp., Scynexis, Inc.Inventors: Mark L Greenlee, Robert Wilkening, James Apgar, Donald Sperbeck, Kenneth J. Wildonger, Dongfang Meng, Dann L. Parker, JR., Ahmed Mamai
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Publication number: 20110218201Abstract: The compounds of Formula (I), are novel effective inhibitors of the type 4 phosphodiesterase.Type: ApplicationFiled: November 12, 2009Publication date: September 8, 2011Applicant: NYCOMED GMBHInventors: Imre Schlemminger, Beate Schmidt, Dieter Flockerzi, Hermann Tenor, Christof Zitt, Armin Hatzelmann, Degenhard Marx, Clemens Braun, Raimund Külzer, Anke Heuser, Hans-Peter Kley, Geert Jan Sterk
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Publication number: 20110217335Abstract: Disclosed are macrocyclic compounds of formulae I, I?, II, II?, III, III?, IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90.Type: ApplicationFiled: January 15, 2009Publication date: September 8, 2011Applicant: UNIVERSITE DE STRASBOURGInventors: Nicolas Winssinger, Sofia Barluenga, Martin Karplus
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Publication number: 20110212940Abstract: The present invention relates to compounds of the general formula (I) that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behçet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions.Type: ApplicationFiled: February 25, 2011Publication date: September 1, 2011Applicant: EPIX PHARMACEUTICALS, INC.Inventors: Roland Burli, Victor J. Cee, Jennifer Golden, Brian Alan Lanman, Susana Neira, Ashis Saha, Nili Schutz, Xiang Yu, Dilara McCauley, Mercedes Lobera, Yael Marantz, Jian Lin, Srinivasa R. Cheruku, Pini Orbach, Anurag Sharadendu, Robert C. Penland, Kimberley Gannon, Sharon Shacham, Silvia Noiman, Oren Becker, Zhaoda Zhang
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Publication number: 20110212955Abstract: The present invention relates to a new class of rosamine derivatives, in one embodiment, the compounds have the structure (I) or any pharmaceutically acceptable salt or solvate thereof, wherein: R1 represents aryl, Het1 or C1-6 alkyl, which latter group is optionally substituted by aryl or Het2; R2a and R2b together form C3.8 n-alkylene, which alkylene group is optionally substituted by one or more substituents selected from halo, C1-4 alkyl, C(O)OH and C(O)O—C1-4, alkyl and which alkylene group is optionally interrupted by X1; R3a and R3b together form C3-6 /7-alkylene, which alkylene group is optionally substituted by one or more substituents selected from halo.Type: ApplicationFiled: July 2, 2009Publication date: September 1, 2011Applicant: CANCER RESEARCH INITIATIVES FOUNDATIONInventors: Hong Boon Lee, Kevin Burgess, Siang Hui Lim, Liangxing Wu
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Publication number: 20110201583Abstract: The invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein R1-3, R5-7, a, X, Y, Y?, Y?, and Z are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.Type: ApplicationFiled: April 28, 2011Publication date: August 18, 2011Applicant: THERAVANCE, INC.Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
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Publication number: 20110172244Abstract: The invention provides compounds, of Formula I: pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.Type: ApplicationFiled: February 20, 2009Publication date: July 14, 2011Applicant: IRM LLCInventors: Phillip B. Alper, Robert Epple, Pierre-Yves Michellys, Daniel Mutnick, Victor Nikulin
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Publication number: 20110172226Abstract: The present invention relates to compounds of formula I or salts thereof, wherein, R1 is selected from the group consisting of hydrogen and R4; R2 is selected from the group consisting of hydrogen, acetyl and R4; R3 is selected from the group consisting of alkyl, —O-alkyl, —NH-alkyl, aryl and heterocyclyl; R4 represents a moiety (A) wherein, X is selected from the group consisting of a single bond, alkylene, alkenylene, alkynylene, arylene or a heterocyclylene moiety; R5 and R6 are same or different and are independently selected from hydrogen, alkyl, aryl or heterocyclyl; or R5 and R6 may form together with the nitrogen atom to which they are attached a heterocyclyl ring system.Type: ApplicationFiled: February 12, 2009Publication date: July 14, 2011Applicant: Sun Pharma Advanced Research Company Ltd.Inventors: Jiten Ranchhodbhai Patel, Gopalkumar Chimanlal Patel, Gaurav Sanjivkumar Sheth, Trinadha Rao Chitturi, Rajamannar Thennati
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Publication number: 20110172225Abstract: 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: ApplicationFiled: September 25, 2008Publication date: July 14, 2011Applicants: Merck Sharp & Dohme Corp., Scynexis, Inc.Inventors: James M. Balkovec, Phieng Siliphaivanh, Frances A. Bouffard, Roland A. Bouffard, Michael R. Peel, Weiming Fan, Ahmed Mamai, Sarah Dimick Gray
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Patent number: 7976739Abstract: A chromene compound represented by the following formula (1), wherein, “A” is an annulated ring, R1 and R2 are hydrogen atoms, hydroxyl groups or the like groups, R3, R4, R5 and R6 are substituents such as hydroxyl groups or the like groups, “a” and “b” are, respectively, integers of 0 to 4, and “c” and “d” are, respectively, integers of 0 to 5. The chromene compound is a photochromic compound developing a color of a neutral tint, and has a high color density per a unit amount.Type: GrantFiled: August 22, 2007Date of Patent: July 12, 2011Assignee: Tokuyama CorporationInventors: Shinobu Izumi, Junji Takenaka
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Publication number: 20110165225Abstract: Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.Type: ApplicationFiled: May 26, 2009Publication date: July 7, 2011Inventors: Peter Cullis, Marcel Bally
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Publication number: 20110143141Abstract: The present invention relates to compounds represented by the following Formula I, Ring-A of the Formula I can be, for example an aryl group, and L1 is a chiral or achiral lengthening group. The compound represented by Formula I can be a photochromic compound. The present invention also relates to photochromic compositions and photochromic articles that include one or more photochromic compounds, such as represented by Formula I.Type: ApplicationFiled: December 16, 2010Publication date: June 16, 2011Applicant: TRANSITIONS OPTICAL, INC.Inventors: Meng He, Sujit Mondal, Darrin R. Dabideen, Anil Kumar, Xiao-Man Dai
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Publication number: 20110140056Abstract: The present invention relates to compounds represented by the following Formulas (I) and (II), Ring-A of Formulas I and II can be, for example, an aryl group, and Q? and Q?? can each be independently selected from groups, such as, halogen, —OH, —CN, amine groups, amide groups, carboxylic acid ester groups, carboxylic acid groups, alkenyl groups, alkynyl groups, carbonate groups, sulfide groups, and sulfonic acid ester groups. The present invention also relates to photochromic compositions and photochromic articles that include one or more photochromic compounds, such as represented by Formula II.Type: ApplicationFiled: December 16, 2010Publication date: June 16, 2011Applicant: TRANSITIONS OPTICAL, INC.Inventors: Meng He, Anil Kumar, Darrin R. Dabideen
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Publication number: 20110144159Abstract: The present invention relates to compounds of Formula (I) wherein Ar is optionally substituted phenyl or 6-membered heteroaryl moiety, or a benzisoxazole, pyrrolopyridine, or benzotriazole group; or a pharmaceutically acceptable salt thereof; processes for the preparation of the compounds; intermediates used in the preparation of the compounds; compositions containing the compounds; and uses of the compounds in treating diseases or conditions associated with fatty acid amide hydrolase (FAAH) activity, including pain, urinary incontinence, overactive bladder, emesis, cognitive disorders, anxiety, depression, sleeping disorders, eating disorders, movement disorders, glaucoma, psoriasis, multiple sclerosis, cerebrovascular disorders, brain injury, gastrointestinal disorders, hypertension, or cardiovascular disease.Type: ApplicationFiled: April 9, 2009Publication date: June 16, 2011Inventors: Lorraine Kathleen Fay, Douglas Scott Johnson, Marvin Jay Meyers, Atli Thorarensen, Lijuan Jane Wang
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Patent number: 7960385Abstract: The invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein R1-3, R5-7, a, X, Y, Y?, Y?, and Z are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.Type: GrantFiled: September 5, 2008Date of Patent: June 14, 2011Assignee: Theravance, Inc.Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
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Publication number: 20110129678Abstract: Described herein are compounds generally comprising an indeno[2?,3?:3,4]naptho[1,2-b]pyran structure. Such compounds may be useful for their photochromic properties, and be used in certain photochromic compositions. Such compositions may further comprise other photochromic compositions and/or materials. Additionally, such compounds and/or compositions may be suitable for preparing certain photochromic articles. Also described herein are methods for preparing certain photochromic compounds, compositions, and articles.Type: ApplicationFiled: December 16, 2010Publication date: June 2, 2011Applicant: Transitions Optical, Inc.Inventors: Meng He, Darrin R. Dabideen, Anil Kumar, Ruisong Xu
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Patent number: 7951822Abstract: The object is to provide a novel LXR? agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. The solving means is a 1,3-dihydroisobenzofuran derivative represented by the following general formula (1) or salt thereof, or their solvate.Type: GrantFiled: March 30, 2009Date of Patent: May 31, 2011Assignee: Kowa Company, Ltd.Inventors: Ayumu Okuda, Takayuki Matsuda, Toru Miura, Koichi Yamazaki, Yuki Yamaguchi, Minoru Koura, Sayaka Kurobuchi, Yuichiro Watanabe, Kimiyuki Shibuya
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Patent number: 7951823Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating channel activating proteases, and methods for, using such compounds to treat, ameliorate or prevent a condition associated with a channel activating protease, including but not limited to prostasin, PRSS22, TMPRSS11 (e.g., TMPRSS11B, TMPRSS11E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), matriptase (MTSP-1), CAP2, CAP3, trypsin, cathepsin A, or neutrophil elastase.Type: GrantFiled: May 16, 2007Date of Patent: May 31, 2011Assignee: IRM LLCInventors: David C. Tully, Arnab K. Chatterjee, Agnes Vidal, Hank Michael James Petrassi, Zhiwei Wang, Badry Bursulaya, Glen Spraggon
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Publication number: 20110124674Abstract: Disclosed are a compound of a formula (I) and its pharmaceutically-acceptable salt: wherein Q is CH or N; R1a, R1b, R1c and R1d are independently a C1-6 alkyl, a halo-C1-6 alkyl, etc.; R2 is a hydrogen atom, etc.; R3 is independently a hydrogen atom, a C1-6 alkyl, etc., or two R3's, taken together, form a bridge such as methylene, etc.; R4a and R4b are independently a hydrogen atom, a C1-6 alkyl, etc.; Z is a bicyclic aromatic hetero ring, etc.; Ar is a benzene ring, etc.; m1 and m2 are independently 0, 1 or 2; n is an integer of from 1 to 4. The compound and its salt act as a melanin concentrating hormone receptor antagonist, and are useful as a preventive or remedy for central system disorders, cardiovascular disorders, metabolic disorders, etc.Type: ApplicationFiled: July 14, 2009Publication date: May 26, 2011Inventors: Hiroyuki Kishino, Nagaaki Sato, Takao Suzuki
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Publication number: 20110118312Abstract: Disclosed is a benzylpiperizine compound represented by formula (1) or a pharmaceutically acceptable salt thereof, which is useful as a medicinal agent such as an antidepressant agent. (In the formula (1), R1 represents a hydrogen atom or a methyl group; R2 is a group bound in a p- or m-position relative to a methylene group and represents a chlorine atom bound in a p-position, a bromine atom bound in a p-position, a methyl group bound in a p-position, a chlorine atom bound in a m-position or a bromine atom bound to in a m-position; X represents a methylene or an oxygen atom; and n represents an integer of 1 to 3.Type: ApplicationFiled: January 20, 2011Publication date: May 19, 2011Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.Inventors: Tomohiro TOYODA, Hidefumi YOSHINAGA
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Publication number: 20110118262Abstract: Disclosed are compounds of formula (I) and compositions of the present invention which are inhibitors of the sodium proton exchanger isoform-1 (NHE-I). Also disclosed are methods of using and making the same.Type: ApplicationFiled: June 24, 2009Publication date: May 19, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Joerg Martin Bentzien, Stephen James Boyer, Jennifer Burke, Anne Bettina Eldrup, Xin Guo, John David Huber, Thomas Martin Kirrane, Fariba Soleymanzadeh, Alan David Swinamer
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Publication number: 20110105463Abstract: Compounds of Formula (I): in which A1, A2, W, L, G, R7a, R7b, R8, R9 and R10 have the meanings given in the specification, are DP2 receptor modulators useful in the treatment of immunologic diseases.Type: ApplicationFiled: June 24, 2009Publication date: May 5, 2011Applicant: ARRAY BIOPHARMA INC.Inventors: Laurence E. Burgess, Christopher T. Clark, Adam Cook, Christopher P. Corrette, Robert Kirk DeLisle, George A. Doherty, Kevin W. Hunt, Todd T. Romoff
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Publication number: 20110105475Abstract: The present invention relates to compounds of formula (I) wherein the substituents are as defined in the claims, including pharmaceutical compositions thereof and for their use in the treatment and/or prevention and/or amelioration of one or more symptoms of disease or disorders related to the activity of FXR. The invention is also directed to intermediates and to a method of preparation of compounds of formula (I).Type: ApplicationFiled: March 30, 2009Publication date: May 5, 2011Applicant: MERXCK PATENT GESELLSCHAFTInventors: Didier Roche, Giséle Mautino, Ingo Kober, Francis Contard, Serge Christmann-Franck, Saumitra Sengupta, Ramesh Sistla, Gummadi Venkateshwar Rao
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Patent number: 7935822Abstract: The present invention relates to carboxamide-substituted dyes, the production and use of such dyes as labeling groups in analytics.Type: GrantFiled: December 18, 2003Date of Patent: May 3, 2011Assignee: ATTO-TEC GmbHInventors: Jutta Arden-Jacob, Karl-Heinz Drexhage, Monika Hamers-Schneider, Norbert Kemnitzer, Alexander Zilles
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Patent number: 7928125Abstract: Disclosed are N-aroyl cyclic amine derivatives having the formula: where the variables are as define herein, and their use as pharmaceuticals, specifically as orexin receptor antagonists.Type: GrantFiled: October 29, 2007Date of Patent: April 19, 2011Assignee: SmithKline Beecham LimitedInventors: Clive Leslie Branch, Wai Ngor Chan, Amanda Johns, Christopher Norbert Johnson, David John Nash, Riccardo Novelli, Jean-Pierre Pilleux, Roderick Alan Porter, Rachel Elizabeth Anne Stead, Geoffrey Stemp
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Patent number: 7919509Abstract: To provide a novel LXR? agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. [Solving Means] A 2-oxochromene derivative represented by the following general formula (1) or salt thereof, or their solvate.Type: GrantFiled: February 27, 2009Date of Patent: April 5, 2011Assignee: Kowa Company, Ltd.Inventors: Ayumu Okuda, Takayuki Matsuda, Toru Miura, Hidefumi Ozawa, Ayako Tosaka, Koichi Yamazaki, Yuki Yamaguchi, Sayaka Kurobuchi, Yuichiro Watanabe, Kimiyuki Shibuya
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Patent number: 7919508Abstract: The present invention provides compounds of formula I: a stereoisomer or a pharmaceutically acceptable salt thereof, wherein the variables R1, R2, R3, R4, X and n are defined as defined herein. Additionally, a method for treating dopamine-related neurological disorders selected form the group consisting of neurological, psychological, cardiovascular, cognitive or attention disorders, substance abuse and addictive behavior, or a combination thereof, comprising administering to a patient in need of such treatment a therapeutically effective amount of compounds of formula I.Type: GrantFiled: October 24, 2006Date of Patent: April 5, 2011Assignee: Aventis Pharmaceuticals Inc.Inventors: Gregory Shutske, Keith J. Harris, Kenneth J. Bordeau, Michael R. Angelastro, Stanly John, Joseph T. Klein, Jinqi Lu, Catherine Bomont
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Publication number: 20110065743Abstract: Kappa opioid receptor antagonists are provided that yield significant improvements in functional binding assays to kappa opioid receptors, and the use of these antagonists in treatment of disease states that are ameliorated by binding of the kappa opioid receptor such as heroin or cocaine addictions.Type: ApplicationFiled: October 25, 2010Publication date: March 17, 2011Applicant: Research Triangle InstituteInventors: Frank Ivy CARROLL, Hernan A. Navarro, Lawrence E. Brieaddy, Scott P. Runyon, James B. Thomas
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Publication number: 20110065707Abstract: The present invention relates to compounds of formula (I) as well as pharmaceutically acceptable salts thereof, wherein A1, A2, R1, R2, R3, R4, R5 and R6 have the significance given herein.Type: ApplicationFiled: September 3, 2010Publication date: March 17, 2011Inventors: Jean Ackermann, Aurelia Conte, Werner Neidhart, Matthias Nettekoven, Stanley Wertheimer
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Patent number: 7902253Abstract: An isoflavone derivative of tectorigenin compound as shown in formula (II), its preparation method and the antiviral medicine containing it as an effective constituent. The compound structure is shown as follows: Where:: R1 is H, NH2 or SO3M; R2 is OR?; R3 is H or —CH2NR?; where R? is H, —CH2COONa or —CH2CH2NMe2; NR? is or —NMe2; M is H, Na, K or N+H (CH2CH2OH)3.Type: GrantFiled: May 14, 2004Date of Patent: March 8, 2011Assignees: Chengdu Dikang Pharmaceutical Institute, Sichuan Dikang Sci-Tech Pharmaceutical Co., Ltd.Inventors: Xuemin Xu, Chongjun Yuan, Jia Wang, Shangbin Qi, Hai Yin, Yanming Zeng
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Publication number: 20110049445Abstract: The present invention provides ophthalmic devices comprising at least one photochromic material which is an indeno-fused naphthopyran having a pi-conjugation extending group bonded to the 11-position of the indeno-fused naphthopyran, the pi-conjugation extending group having at least one pendent halo-substituted group bonded thereto. The pi-conjugation extending group extends the pi-conjugation system of said indeno-fused naphthopyran. The 13-position of the indeno-fused naphthopyran is substantially free of spiro-substituents. The invention further provides photochromic materials of specified structure, photochromic compositions, photochromic articles and optical elements that include the photochromic materials. Other non-limiting embodiments relate to methods of making the ophthalmic devices comprising photochromic materials.Type: ApplicationFiled: September 1, 2010Publication date: March 3, 2011Inventors: Anu Chopra, Jun Deng, Beon-Kyu Kim, David B. Knowles, Frank F. Molock, JR., Victor A. Montes, Stephen D. Straight, Wenjing Xiao, Huayun Yu
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Patent number: 7893090Abstract: Disclosed are N-aroyl cyclic amine derivatives having the formula: where the variables are as define herein, and their use as pharmaceuticals, specifically as orexin receptor antagonists.Type: GrantFiled: October 30, 2007Date of Patent: February 22, 2011Assignee: SmithKline Beecham LimitedInventors: Clive Leslie Branch, Wai Ngor Chan, Amanda Johns, Christopher Norbert Johnson, David John Nash, Riccardo Novelli, Jean-Pierre Pilleux, Roderick Alan Porter, Rachel Elizabeth Anne Stead, Geoffrey Stemp
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Patent number: 7888510Abstract: It was an object of the present invention to provide novel compounds that are suitable in particular as active substances in medicaments, preferably in medicaments for the regulation of neuropeptide Y receptors, particularly preferably of neuropeptide Y5 (NPY5) receptor, for the regulation of food ingestion (food intake), preferably for the prophylaxis and/or treatment of disorders of food ingestion, such as obesity, anorexia, cachexia, bulimia or type II (non insulin dependent) diabetes, for the prophylaxis and/or treatment of disorders of the peripheral nervous system, disorders of the central nervous system, anxiety, depression, cognitive disorders, preferably memory disorders, cardiovascular diseases, pain, epilepsy, arthritis, hypertensive syndrome, inflammatory diseases, immune diseases and other NPY5 mediated disorders in animals and mammals, including man.Type: GrantFiled: July 29, 2004Date of Patent: February 15, 2011Assignee: Laboratorios del Dr. Esteve S.A.Inventors: Antoni Jover Torrens, Josep Mas Prio, Alberto Dordal Zueras, Maria Angeles Fisas Escasany, Helmut-Heinrich Buschmann
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Patent number: 7880021Abstract: 3-hydroxyflavone derivatives are useful in the detection and the quantification of cell apoptosis. Such derivatives are also useful as fluorescent probes in studying lipid asymmetry of cell plasma membrane and in detecting apopoptic cells. The derivatives can be used to monitor the evolution of diseases involving cell apoptosis.Type: GrantFiled: October 11, 2006Date of Patent: February 1, 2011Assignees: Centre National de la Recherche Scientifique (CNRS), Universite Louis Pasteur (Strasbourg I)Inventors: Yves Mely, Andrey Klymchenko, Oleksandr Demchenko, Vasyl Shynkar
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Publication number: 20110021528Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.Type: ApplicationFiled: October 1, 2010Publication date: January 27, 2011Applicant: PHARMACYCLICS, INC.Inventors: Erik J. Verner, Martin Sendzik, Chitra Baskaran, Joseph J. Buggy, James Robinson
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Publication number: 20110015185Abstract: The present invention relates to compounds of formula (I): wherein P, R3, W1, and W2 are as described herein, to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds for the preparation of a medicament against 5-HT6 receptor-related disorders.Type: ApplicationFiled: September 28, 2010Publication date: January 20, 2011Applicant: BIOVITRUM ABInventors: Gary Johansson, Peter Brandt, Björn M. Nilsson
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Publication number: 20110009396Abstract: The present invention provides compounds represented by formula 1: wherein, R1 R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13 and X are as defined in the specification, in all its stereoisomeric and tautomeric forms and mixtures thereof in all ratios, and its pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable polymorphs and prodrugs. These compounds are useful for treatment of inflammatory disorders including those caused by elevated levels of proinflammatory cytokines such as Tumor Necrosis Factor (TNF-? and/or interleukins (IL-1?, IL-6, IL-8). The invention also relates to processes for the manufacture of compounds of formula 1 and pharmaceutical compositions containing them.Type: ApplicationFiled: July 25, 2008Publication date: January 13, 2011Inventors: Dilip Narayanrao Bhedi, Ram Asrey Vishwakarma, Vaishali Deka, Dattatray Maruti More, Manivannan Ramalingam, Ashish Suthar, Rada Dalal, Sapna Parikh, Aditi Amol Tannu
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Publication number: 20100331367Abstract: This invention relates to novel N-aryl-N-piperidin-4-yl-propionamide derivatives useful as opioid receptor ligands. In other aspects the invention relates to the use of these compounds in a method for therapy, such as for the treatment of pain, and to pharmaceutical compositions comprising the compounds of the invention.Type: ApplicationFiled: December 18, 2008Publication date: December 30, 2010Applicant: NeuroSearch A/SInventors: Dan Peters, Gordon Munro, Elsebet Ostergaard Nielsen
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Publication number: 20100331298Abstract: Chemokine receptor antagonists, in particular, compounds of Formula (I) that act as antagonists of the chemokine CCR2 receptor, including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leukocyte accumulation are described herein.Type: ApplicationFiled: December 10, 2008Publication date: December 30, 2010Applicant: CytoPathfinder, Inc.Inventors: Efrat Ben-Zeev, Dongli Chen, Merav Fichman, Shomir Ghosh, Steffi Koerner, Jian Lin, Yael Marantz, Rosa E. Melendez, Pradyumna Mohanty, Sharon Shacham, Zhaoda Zhang
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Publication number: 20100324296Abstract: A naphthopyran compound represented by the formula B1 and B2 may include a phenyl, naphthyl, or heterocyclic aromatic group, or may combine to form one or more aromatic rings. B1 and B2 may further include one or more substituents. Ra may include an alkyl, polycycloalkyl, alkenyl, polyalkenyl, haloalkyl, perhaloalkyl, alkynyl, polyalkynyl, hydroxyalkynyl, polyhydroxyalkynyl; or (C3-20)cycloalkyl group. Rb and Rc may include hydrogen or alkyl groups, or may combine to form a saturated heterocyclic group, or together with an adjacent phenyl group may form a julolidinyl group. R3, R4, R5, R6, and R10 may include hydrogen, halogen, —Ra, —OH, —ORa, —O—CO—Ra, —CN, —NO2, —SO2Ra, —SORa, —SH, —SRa, —NH2, —NHRa, —NRaRa, or —NRbRc; or any two or more may combine to form a cyclic group. R7 is a mesogenic group. And the naphthopyran, which may be referred to as a dichroic-photochromic compound, may be incorporated into an optical article.Type: ApplicationFiled: October 17, 2007Publication date: December 23, 2010Inventors: Ludmila Sukhomlinova, Linli Su, Tamas Kosa, Bahman Taheri
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Patent number: 7855193Abstract: The present invention relates to compounds of the general formula (I) that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behçet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions.Type: GrantFiled: July 24, 2006Date of Patent: December 21, 2010Assignee: EPIX Pharmaceuticals, Inc.Inventors: Ashis K. Saha, Nili Schutz, Xiang Yu, Dilara McCauley, Mercedes Lobera, Yael Marantz, Jian Lin, Srinivasa R. Cheruku, Pini Orbach, Anurag Sharadendu, Robert Christian Penland, Kimberley Gannon, Sharon Shacham, Silvia Noiman, Oren Becker
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Patent number: 7842808Abstract: The present invention relates to compounds of Formula (I) as antagonists of calcitonin gene-related peptide receptors (“CGRP-receptor”), pharmaceutical compositions comprising them, methods for identifying them, methods of treatment using them and their use in therapy for treatment of neurogenic vasodilation, neurogenic inflammation, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.Type: GrantFiled: January 5, 2007Date of Patent: November 30, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Prasad V. Chaturvedula, Ling Chen, Rita Civiello, Andrew P. Degnan, Gene M. Dubowchik, Xiaojun Han, Xiang Jun J. Jiang, Guanglin Luo, John E. Macor, Graham S. Poindexter, George O. Tora
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Publication number: 20100286201Abstract: New polymorphic forms of (S)-2-((4-benzofuranyl)carbonylamino methyl)-1-((4-(2-methyl-5-(4-fluorophenyl))thiazolyl)carbonyl)piperidine, methods for their preparation and use in medicine.Type: ApplicationFiled: September 11, 2008Publication date: November 11, 2010Inventor: Leanda Jane Kindon
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Publication number: 20100256142Abstract: A functionalized polycyclic compound can have a structure of Formula 1 or salt, prodrug, analog, or derivative thereof, which compound can be prepared by providing a diene; reacting the diene with a dienophile under sufficient conditions for a combined Diels-Alder/acylation reaction so as to provide a polycyclic compound having a carboxylic acid; and coupling the carboxylic acid with an amine-containing compound or a hydroxyl-containing compound so as to form an amide or an ester and producing a compound having a structure of Formula 1. The compound can be used for modulating an opioid receptor, which can be conducted by administering to an opioid receptor a functionalized polycyclic compound as described herein in an effective amount to modulate the functionality of the opioid receptor. Such opioid modulation can provide a biological benefit to a subject.Type: ApplicationFiled: September 25, 2009Publication date: October 7, 2010Inventors: Jeffrey Aube, Bryan L. Roth, Partha Ghosh, Kevin J. Frankowski