The Additional Hetero Ring Consists Of One Sulfur And Four Carbons Patents (Class 546/212)
  • Patent number: 10442796
    Abstract: The present invention relates to a novel 2,3,5-substituted thiophene compound having inhibitory activity against kinases, an anticancer agent including the compound as an active ingredient, and a method for preparing the compound.
    Type: Grant
    Filed: August 16, 2018
    Date of Patent: October 15, 2019
    Assignees: Korea Institute of Science and Technology, Daegu-Gyeongbuk Medical Innovation Foundation
    Inventors: Tae Bo Sim, Woo Young Hur, Chi Man Song, Ho Jong Yoon, Seung Hye Choi, Han Na Cho, Hwan Geun Choi, Nam Doo Kim, Jung Beom Son, Eun Hwa Ko, Hyun Kyoung Kim, Joong Heui Cho, Seock Yong Kang, So Young Kim, Yi Kyung Ko, Seung Yeon Lee, Suk Kyoon Yoon, Jae Hyun Bae
  • Publication number: 20150005275
    Abstract: The present invention discloses compounds according to Formula I: wherein R1, R2, R3, L, and the subscript m are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions, and methods of treatment using the same, for the treatment of cystic fibrosis by administering a compound of the invention.
    Type: Application
    Filed: May 6, 2014
    Publication date: January 1, 2015
    Inventors: Steven Emiel Van der Plas, Oscar Mammoliti, Christel Jeanne Marie Menet, Giovanni Alessandro Tricarico, Ann De De Blieck, Caroline Martine Andrée Marie Joannesse, Hans Kelgtermans, Tom Roger Lisette De Munck
  • Patent number: 8829030
    Abstract: Compounds represented by formula: Wherein X, Y and Z are as defined herein, pharmaceutically acceptable salts thereof, and related compounds, are suitable for use in treating or preventing a Flaviviridae viral infection in a host.
    Type: Grant
    Filed: November 30, 2012
    Date of Patent: September 9, 2014
    Assignee: Vertex Pharmaceuticals (Canada) Incorporated
    Inventors: Laval Chan Chun Kong, Sanjoy Kumar Das, Nghe Nguyen-Ba, Liliane Halab, Bettina Hamelin, Oswy Z. Pereira, Carl Poisson, Melanie Proulx, Thunkunta Jagadeeswar Reddy, Ming Qiang Zhang
  • Patent number: 8772489
    Abstract: Optically active 2-hydroxytetrahydrothienopyridine derivatives represented by Formula I and pharmaceutically acceptable salts, preparation method and use in the manufacture of a medicament thereof are disclosed. The pharmacodynamic experiment results show that the present compounds of Formula I are useful for inhibiting platelet aggregation. The pharmacokinetic experiment results show that the present compound of Formula I can be converted in vivo into pharmacologically active metabolites and are therefore useful for inhibiting platelet aggregation. Therefore, the present compounds are useful for the manufacture of a medicament for preventing or treating thrombosis and embolism related diseases.
    Type: Grant
    Filed: January 28, 2011
    Date of Patent: July 8, 2014
    Assignee: Jiangsu Vcare PharmaTech Co. Ltd.
    Inventors: Hongbin Sun, Jiaqi Shan, Boyu Zhang, Fang Yuan
  • Patent number: 8765764
    Abstract: A 2-acylaminothiazole derivative or a pharmaceutically acceptable salt thereof having an excellent effect of proliferating human c-mpl-Ba/F3 cells and an activity of increasing platelets based on the effect of promoting the formation of megakaryocytic colonies. A compound or a pharmaceutically acceptable salt thereof useful in treating thrombocytopenia.
    Type: Grant
    Filed: November 15, 2012
    Date of Patent: July 1, 2014
    Assignee: Astellas Pharma, Inc.
    Inventors: Keizo Sugasawa, Susumu Watanuki, Yuji Koga, Hiroshi Nagata, Ryutaro Wakayama, Fukushi Hirayama, Ken-Ichi Suzuki
  • Publication number: 20140179925
    Abstract: Disclosed herein are methods of treating a patient suffering from a cognitive disorder using compounds of Formulas 1 and 2 wherein the variables have the meaning disclosed in the specification
    Type: Application
    Filed: December 18, 2013
    Publication date: June 26, 2014
    Applicant: Allergan, Inc.
    Inventors: John E. Donello, Fabien J. Schweighoffer, Lauren M. Luhrs
  • Patent number: 8686152
    Abstract: The present invention is directed to 4,4-di-substituted piperidine derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1.
    Type: Grant
    Filed: March 9, 2011
    Date of Patent: April 1, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Bart L. DeCorte, Renee L. DesJarlais, Yifang Huang, Michael H. Parker, Dennis J. Hlasta
  • Patent number: 8580965
    Abstract: Substituted sulfonamide compounds with bradykinin receptor (B1R) modulating activity; processes for the preparation thereof, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat or inhibit pain and/or other disorders and/or disease states.
    Type: Grant
    Filed: October 16, 2007
    Date of Patent: November 12, 2013
    Assignee: Gruenenthal GmbH
    Inventors: Stefan Oberboersch, Melanie Reich, Stefan Schunk, Sabine Hees, Ruth Jostock, Michael Engels, Achim Kless, Thomas Christoph, Klaus Schiene, Tieno Germann, Edward Bijsterveld
  • Patent number: 8546588
    Abstract: This invention provides compounds of formula (I): wherein X1, X2, X3, R2, R4b, R1, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Grant
    Filed: February 25, 2011
    Date of Patent: October 1, 2013
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
  • Patent number: 8492407
    Abstract: The invention provides compounds of the formula: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a, Z and Q 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: Grant
    Filed: May 17, 2012
    Date of Patent: July 23, 2013
    Assignee: Theravance, Inc.
    Inventors: Craig Husfeld, YuHua Ji, Rick Lee, Li Li, YongQi Mu, Cameron Smith, Johnny Uy
  • Patent number: 8486971
    Abstract: The invention relates to compounds of the formula (I), where: R1 is: a —NR5R6 group; an unsubstituted or substituted phenyl; R2 is: a (C1-C4)alkyl; an —X—R7 group; R3 and R4 each are independently a substituted phenyl; R5 is a hydrogen atom or a (C1-C4)alkyl; R6 is an unsubstituted or substituted (C1-C4)alkyl; or R5 and R6 together with the nitrogen atom to which they are bonded constitute an unsubstituted or substituted heterocyclic compound; X is a (C1-C5)alkylene; R7 is an —OR8 group, a —NR9R10 group, an —SO2—(C1-C4)alkyl group; R8 is a hydrogen atom or a (C1-C4)alkyl; R9 is a hydrogen atom or a (C1-C4)alkyl; R10 is a hydrogen atom, a —COR11 group, an —SO2R11 group or a —CO(CH2)mOH group; R11 is an unsubstituted or substituted (C1-C4)alkyl; m is 1, 2 or 3. The invention also relates to methods for preparing same and to the therapeutic use thereof.
    Type: Grant
    Filed: March 25, 2010
    Date of Patent: July 16, 2013
    Assignee: Sanofi
    Inventors: Jean-Philippe Ducoux, Murielle Rinaldi-Carmona, Arnaud Rouquette
  • Patent number: 8455521
    Abstract: Diaminoalkanes of below Formula I have now been found which are orally active and bind to aspartic proteases to inhibit their activity: They are useful in the treatment or amelioration of diseases associated with elevated levels of aspartic protease activity. The invention also relates to a method for the use of the compounds of Formula I in ameliorating or treating aspartic protease related disorders in a subject in need thereof comprising administering to said subject an effective amount of a compound of Formula I.
    Type: Grant
    Filed: May 28, 2010
    Date of Patent: June 4, 2013
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh, Patrick T. Flaherty, Jean-Pierre Wery
  • Patent number: 8410137
    Abstract: The subject matter of the invention is compounds corresponding to formula (I), in which: R1 and R2, together with the nitrogen atom to which they are attached, constitute a saturated heterocyclic radical containing from 4 to 7 atoms, which is preferably substituted; one of the two substituents R3 and R6 is a group Y-A-R9; Y is an oxygen atom or an —S(O)n?—, or —OSO2 group; A is an unsubstituted (C1-C4) alkylene group; R9 is an —OR19, —CH3, —NR19R20, —CONR19R20, —NR15COR19, —S(O)nR21, or —NR13SO2R21 group; —R10 is a hydrogen atom or a (C1-C4) alkyl group. The present invention also relates to the methods of preparation and the therapeutic uses of the compounds of formula (I).
    Type: Grant
    Filed: July 30, 2009
    Date of Patent: April 2, 2013
    Assignee: Sanofi
    Inventors: Francis Barth, Jean-Philippe Ducoux, Patrick Gueule, Murielle Rinaldi-Carmona, Arnaud Rouquette
  • Patent number: 8399488
    Abstract: The invention provides compounds of formula I: wherein a, b, c, m, s, t, W, Z, Ar, R1, R2, R3, R6, and R7 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
    Type: Grant
    Filed: January 11, 2012
    Date of Patent: March 19, 2013
    Assignee: Theravance, Inc.
    Inventors: YuHua Ji, Mathai Mammen, Craig Husfeld, Li Li, YongQi Mu, Aaron Kushner, Eric Stangeland, Trevor Mischki, Adam Hughes, Sarah Dunham
  • Patent number: 8377966
    Abstract: The invention provides compounds of formula I: wherein a, b, c, m, n, q, r, W, Z1, Ar1, Z2, Y, R1, R2, and R3 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
    Type: Grant
    Filed: January 25, 2012
    Date of Patent: February 19, 2013
    Assignee: Theravance, Inc.
    Inventors: YongQi Mu, YuHua Ji, Mathai Mammen, Viengkham Malathong
  • Patent number: 8372991
    Abstract: Described herein are compounds of Formula (I): wherein A, J, Z, X, R1 and R4 are defined herein, 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: Grant
    Filed: March 17, 2011
    Date of Patent: February 12, 2013
    Assignee: Calcimedica, Inc.
    Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Patent number: 8362008
    Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11?-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11?-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.
    Type: Grant
    Filed: December 11, 2008
    Date of Patent: January 29, 2013
    Assignee: The University Of Edinburgh
    Inventors: Scott Peter Webster, Jonathan Robert Seckl, Brian Robert Walker, Peter Ward, Thomas David Pallin, Hazel Joan Dyke, Trevor Robert Perrior
  • Publication number: 20130012489
    Abstract: The invention relates to compounds of the formulae (I), (II) and (III) in which R1, R2, R3, R4, Y, W1, W2, L, A, Alk, Cyc, Ar, Het1, Het2, Hal and n have the meaning indicated in claim 1, and/or physiologically acceptable salts, tautomers and stereo-isomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumours, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I) by reaction of compounds of the formulae (II) and (III) and optionally conversion of a base or acid of the compounds of the formula (I) into one of their salts.
    Type: Application
    Filed: February 17, 2011
    Publication date: January 10, 2013
    Applicant: MERCK PATENT GMBH
    Inventors: Werner Mederski, Thomas Fuchss, Frank Zenke
  • Patent number: 8338429
    Abstract: A 2-acylaminothiazole derivative or a pharmaceutically acceptable salt thereof having an excellent effect of proliferating human c-mpl-Ba/F3 cells and an activity of increasing platelets based on the effect of promoting the formation of megakaryocytic colonies. A compound or a pharmaceutically acceptable salt thereof useful in treating thrombocytopenia.
    Type: Grant
    Filed: November 10, 2009
    Date of Patent: December 25, 2012
    Assignee: Astellas Pharma, Inc.
    Inventors: Keizo Sugasawa, Susumu Watanuki, Yuji Koga, Hiroshi Nagata, Ryutaro Wakayama, Fukushi Hirayama, Ken-ichi Suzuki
  • Publication number: 20120258965
    Abstract: The invention relates to N-hydroxylsulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxylsulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxylsulfonamide derivatives.
    Type: Application
    Filed: June 22, 2012
    Publication date: October 11, 2012
    Applicants: The Johns Hopkins University, Cardioxyl Pharmaceuticals
    Inventors: John P. TOSCANO, Frederick Arthur Brookfield, Andrew D. Cohen, Stephen Martin Courtney, Lisa Marie Frost, Vincent Jacob Kalish
  • Publication number: 20120208848
    Abstract: Improved formulations of gacyclidine for direct administration to the inner or middle ear.
    Type: Application
    Filed: April 25, 2012
    Publication date: August 16, 2012
    Applicant: NEUROSYSTEC CORPORATION
    Inventors: Thomas Jay Lobl, John Vinton Schloss, Jacob E. Pananen
  • Patent number: 8211916
    Abstract: N- and O-substituted 4[2-diaromaticmethoxy and methylamino)alkyl] piperidines exhibit high CNS activity with respect to the dopamine transporter (DAT) and serotonin transporter (SERT). Preferred compounds exhibit highly differential behavior as between the DAT and SERT and between the DAT and the norepinephrine transporter (NET). The compounds have utility in treating CNS disorders, including but not limited to cocaine addiction, depression, and Parkinson's disease.
    Type: Grant
    Filed: January 22, 2008
    Date of Patent: July 3, 2012
    Assignee: Wayne State University
    Inventor: Aloke K. Dutta
  • Patent number: 8153669
    Abstract: Compounds of formula (I), in salt or zwitterionic form, wherein J, L, M, R1, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
    Type: Grant
    Filed: December 22, 2005
    Date of Patent: April 10, 2012
    Assignee: Novartis AG
    Inventors: Neil John Press, Stephen Paul Collingwood
  • Patent number: 8138206
    Abstract: Disclosed is a substance having an antagonistic effect on the binding of histamine to a histamine H3 receptor or an inhibitory effect on the activity which a histamine H3 receptor constantly exhibits. A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof; (I) wherein R1 represents a phenyl group which may be substituted or the like and R2 represents a cyano group which may be substituted or the like, or R1 and R2 together form an aliphatic heterocylic ring which may be substituted; R3 represents a group represented by the formula (II-1) below; and all of X1 to X4 represent a carbon atom or the like: (II-1) where R4 and R5 represent a lower alkyl group or the like; and m1 represents an integer of 2 to 4.
    Type: Grant
    Filed: May 29, 2006
    Date of Patent: March 20, 2012
    Assignee: MSD. K.K.
    Inventors: Shiho Ishikawa, Tsuyoshi Nagase, Nagaaki Sato, Hidekazu Takahashi, Shigeru Tokita, Toshihiro Wada
  • Publication number: 20120065231
    Abstract: The present invention provides a compound represented by the formula (I) or its salt, solvate, or physiologically functional derivative; and a pharmaceutical composition which is useful for treatment or prevention of conditions or disorders having sensitivity to selective androgen receptor modulation, the composition comprising the above-described compound; among others:
    Type: Application
    Filed: April 28, 2010
    Publication date: March 15, 2012
    Applicant: SUMITOMO CHEMICAL COMPANY LTD.
    Inventors: Koichiro Harada, Kozo Motonaga, Koichi Saito, Akio Tanaka
  • Publication number: 20120046317
    Abstract: The present invention relates to a new class of heterocyclic compounds and pharmaceutically acceptable salts thereof, process for preparing the same, pharmaceutical composition containing these compounds and to their use in treatment of diseases caused due to formation and accumulation of AGEs (Advanced Glycation end products). The compounds of the present invention are useful for the treatment of diabetic and aging-related complications caused by formation and accumulation of AGEs, such as neuropathy, nephropathy, microangiopathy, retinopathy, hypertension, heart failure, atherosclerosis, Alzheimer's disease & dermatological disorders.
    Type: Application
    Filed: May 6, 2010
    Publication date: February 23, 2012
    Inventors: Chaitanya Dutt, Vijay Chauthaiwale, Ramesh Chandra Gupta, Manish Patel, Jignesh Kotecha, Sachin Latad, Jaya Abraham, Sanjay Srivastava, Milin Rode, Shailesh Deshpande, Anita Chaudhary, Amit Kumar Kesarwani
  • Patent number: 8106191
    Abstract: New compounds are disclosed for multimerizing immunophilins and proteins containing immunophilin or immunophilin-related domains. The compounds are of the formula M-L-Q where M is a synthetic ligand for an FKBP protein.
    Type: Grant
    Filed: June 13, 2003
    Date of Patent: January 31, 2012
    Assignee: ARIAD Pharmaceuticals, Inc.
    Inventors: Dennis A. Holt, Terence P. Keenan, Tao Guo, Edgardo Laborde, Wu Yang
  • Patent number: 8012995
    Abstract: The present invention is related to sulfonamide derivatives of formula (I0 notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK 2 and 3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation.
    Type: Grant
    Filed: September 28, 2000
    Date of Patent: September 6, 2011
    Assignee: Merck Serono SA
    Inventors: Stephen Arkinstall, Serge Halazy, Dennis Church, Montserrat Camps, Thomas Rueckle, Jean Pierre Gotteland, Marco Biamonte
  • Patent number: 7964734
    Abstract: Raloxifene acid addition salts or solvates thereof, having improved dissolution properties in media comprising hydrochloric acid are described, compared with similar preparations based on raloxifene or raloxifene hydrochloride. The disclosed acid addition salts or solvates thereof show an improved bioavailability in media comprising hydrochloric acid, such as the gastric juice. The acid addition salts or solvates thereof are addition salts or solvates of raloxifene and a pharmaceutical acceptable acid selected among succinic acid, lactic acid, malonic acid or sulphuric acid. Further, crystalline forms of the raloxifene salts and solvates thereof are disclosed. The raloxifene acid addition salts and/or solvates thereof are useful for the preparation of pharmaceutical composition for oral administration capable of fast and reliable release of the active ingredients in the stomach of the patient, in particular for the treatment of cancer or osteoporosis, or for inhibiting cartilage degradation.
    Type: Grant
    Filed: September 30, 2003
    Date of Patent: June 21, 2011
    Assignee: A/S Gea Farmaceutisk Fabrik
    Inventors: Gunnar Leo Karup, Søren Bols Pedersen
  • Publication number: 20110130381
    Abstract: Inhibitors of dihydroorotate dehydrogenase (DHODH) for the Plasmodium enzyme have been identified and characterized. The inhibitors have high specificity, submicromolar efficacy against cultured parasite strains, exhibit drug-like properties, and are not overtly cytotoxic.
    Type: Application
    Filed: May 7, 2009
    Publication date: June 2, 2011
    Inventors: Cecilia Bastos, Michael L. Booker, Cassandra A. Celatka, Jon C. Clardy, Joseph Cortese, Vishal P. Patel, Renato Skerlj, Roger C. Wiegand, Dyann F. Wirth
  • Patent number: 7947730
    Abstract: Compounds of formula I in salt or zwitterionic form wherein, wherein R1, R2, R3, R4, R5, J, L and M have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
    Type: Grant
    Filed: June 23, 2004
    Date of Patent: May 24, 2011
    Assignee: Novartis AG
    Inventors: Stephen Paul Collingwood, Urs Baettig, Clive McCarthy
  • Patent number: 7902181
    Abstract: The present invention provides compounds of formula (I) in which n, y, X1, X2, A, B, R1, R2, R3, R4 and R5 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: December 10, 2008
    Date of Patent: March 8, 2011
    Assignee: AstraZeneca AB
    Inventors: Mark Furber, Christopher Andrew Luckhurst, Hitesh Jayantilal Sanganee, Linda Anne Stein, Peter Alan Cage
  • Publication number: 20100305328
    Abstract: Processes for preparing pure tiagabine, a piperidine carboxylic acid, using pharmaceutically acceptable acid addition salts of tiagabine esters are provided. L(+)-tartaric acid, oxalic acid and dibenzoyl L(+)-tartaric acid addition salts of tiagabine esters are also provided. Further, processes for preparing acid addition salts of tiagabine esters are provided.
    Type: Application
    Filed: July 29, 2010
    Publication date: December 2, 2010
    Applicant: RANBAXY LABORATORIES LIMITED
    Inventors: Prosenjit BOSE, Pramod KUMAR, Shilpi MITTAL, Yatendra KUMAR
  • Publication number: 20100267696
    Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11?-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11?-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.
    Type: Application
    Filed: December 11, 2008
    Publication date: October 21, 2010
    Applicant: THE UNIVERSITY OF EDINBURGH
    Inventors: Scott Peter Webster, Jonathan Robert Seckl, Brian Robert Walker, Peter Ward, Thomas David Pallin, Hazel Joan Dyke, Trevor Robert Perrior
  • Patent number: 7790747
    Abstract: The present invention relates to chemokine receptor binding compounds, pharmaceutical compositions and their use. More specifically, the present invention relates to modulators of chemokine receptor activity, preferably modulators of CCR5. These compounds demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).
    Type: Grant
    Filed: June 14, 2006
    Date of Patent: September 7, 2010
    Assignee: Genzyme Corporation
    Inventors: Yuanxi Zhou, Elyse Bourque, Yongbao Zhu, Jonathan Langille, Markus Metz, Wen Yang, Ernest J. McEachern, Curtis Harwig, Ian R. Baird, Tong-Shuang Li, Renato T. Skerlj
  • Patent number: 7790753
    Abstract: Compounds of formula (I) as defined herein: are useful for treating behavioral disorders associated with dementia, psychoses, in particular schizophrenia (deficient form and productive form) and acute or chronic extrapyramidal symptoms induced by neuroleptics; for the treatment of various forms of anxiety, panic attacks, phobias, and compulsive obsessive disorders; for treating various forms of depression, including psychotic depression; for treating disorders caused by alcohol abuse or weaning from alcohol, sexual behavior disorders, eating disorders and for treating migraine.
    Type: Grant
    Filed: April 17, 2006
    Date of Patent: September 7, 2010
    Assignee: sanofi-aventis
    Inventors: Gihad Dargazanli, Genevieve Estenne-Bouhtou, Corinne Veronique
  • Patent number: 7754737
    Abstract: Diaminoalkanes of Formula I have now been found which are orally active and bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with elevated levels of aspartic protease activity. The invention also relates to a method for the use of the compounds of Formula I in ameliorating or treating aspartic protease related disorders in a subject in need thereof comprising administering to said subject an effective amount of a compound of Formula I.
    Type: Grant
    Filed: October 7, 2005
    Date of Patent: July 13, 2010
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh, Patrick T. Flaherty, Jean-Pierre Wery
  • Patent number: 7750025
    Abstract: Compounds of formula (I) as defined herein: are useful for treating behavioral disorders associated with dementia, psychoses, in particular schizophrenia (deficient form and productive form) and acute or chronic extrapyramidal symptoms induced by neuroleptics; for the treatment of various forms of anxiety, panic attacks, phobias, and compulsive obsessive disorders; for treating various forms of depression, including psychotic depression; for treating disorders caused by alcohol abuse or weaning from alcohol, sexual behavior disorders, eating disorders and for treating migraine.
    Type: Grant
    Filed: April 17, 2006
    Date of Patent: July 6, 2010
    Assignee: sanofi-aventis
    Inventors: Gihad Dargazanli, Genevieve Estenne-Bouhtou, Pascale Magat
  • Publication number: 20100125079
    Abstract: The invention provides compounds of formula I: wherein a, b, c, m, n, q, r, W, Z1, Ar1, Z2, Y, R1, R2, and R3 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
    Type: Application
    Filed: January 25, 2010
    Publication date: May 20, 2010
    Applicant: THERAVANCE, INC.
    Inventors: YongQi Mu, Yu-Hua Ji, Mathai Mammen, Viengkham Malathong
  • Patent number: 7718673
    Abstract: The invention is directed to novel isonipecotamide derivatives of Formula (I): which are useful in treating integrin-mediated disorders.
    Type: Grant
    Filed: January 16, 2003
    Date of Patent: May 18, 2010
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Michael J. Costanzo, William J. Hoekstra, Bruce E. Maryanoff
  • Patent number: 7700627
    Abstract: Disclosed herein is a compound having a structure or a pharmaceutically acceptable salt, prodrug, or bioisostere thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: July 17, 2007
    Date of Patent: April 20, 2010
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Danny T. Dinh
  • Patent number: 7683173
    Abstract: The invention provides compounds of formula I: wherein a, b, c, d, f, W, Q, Y, R1, R2, and R3 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
    Type: Grant
    Filed: November 5, 2008
    Date of Patent: March 23, 2010
    Assignee: Theravance, Inc.
    Inventors: Yu-Hua Ji, Craig Husfeld, Mathai Mammen, YongQi Mu, Eric L. Stangeland
  • Patent number: 7683077
    Abstract: The present invention provides a piperidine derivative represented by the following formula or analogs thereto, which are used for agents for treating or preventing various diseases related to 5-HT7.
    Type: Grant
    Filed: May 19, 2004
    Date of Patent: March 23, 2010
    Assignee: Ajinomoto Co., Inc.
    Inventors: Shingo Makino, Naoyuki Fukuchi, Sayaka Asari, Masaki Hashimoto, Tetsuo Yano, Youji Yamada, Munetaka Tokumasu, Masataka Shoji, Itsuya Tanabe, Shinichi Fujita, Hideki Matsumoto
  • Patent number: 7667042
    Abstract: Stable polymorphic forms III, IV and substantially amorphous form of an anticonvulsant, tiagabine hydrochloride.
    Type: Grant
    Filed: December 24, 2004
    Date of Patent: February 23, 2010
    Assignee: Sun Pharma Advanced Research Company Ltd.
    Inventors: Muthukumaran Natarajan, Nileshkumar Sureshbhai Patel, Mehul Chandrakatbhai Bhatt, Srinivasu Kilaru, Rajamannar Thennati
  • Patent number: 7645754
    Abstract: The subject invention provides compounds having the structure: wherein, R1 is a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(?O)NRaRb, —NRaRb, —NRaC(?O)NRaRb, —NRaC(?O)ORa, —OC(?O)NRaRb, or —NHC(?O) Ra; R2 is hydrogen or a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(?O)NRaRb, —NRaRb, —NRaC(?O)NRaRb, —NRaC(?O)ORa, —OC(?O)NRaRb, or —NHC(?O)Ra, or R1, R2 and N together form a substituted piperazine, substituted azetidine ring, or a pyrrolidine ring substituted with —(CH2)2OH or —CH2C(?O)OH; R3 is a substituted or unsubstituted phenyl or a 5-6 membered heteroaryl ring, wherein the substituent is halogen, hydroxyl, cyano, (C1-C15)alkyl, (C1-C15)alkoxy, or —NRaRb; R4 is hydrogen or substituted or unsubstituted (C1-C15)alkyl; R5 is —(CH2)mOR6, —CHNOR7, —C(?O)NR8R9, —(CH2)mC(?O)OR10, —(CH2)kC(?O)NR11R12; wherein R6 is a substituted or unsubstituted (C1-C30)alkyl, (C3-C10)cycloalkyl, or an aryl, heteroaryl
    Type: Grant
    Filed: June 19, 2007
    Date of Patent: January 12, 2010
    Assignee: OSI Pharmaceuticals, Inc.
    Inventors: Arlindo Castelhano, Bryan McKibben, Arno Steinig
  • Patent number: 7638525
    Abstract: The present invention is directed to novel trisubstituted thiophene derivatives, pharmaceutical compositions containing them and their use in the treatment or prevention of disorders and diseases mediated by agonists and antagonists of the progesterone receptor. The clinical usage of these compounds are related to hormonal contraception, the treatment and/or prevention of secondary dysmenorrhea, amenorrhea, dysfunctional uterine bleeding, uterine leiomyomata, endometriosis; polycystic ovary syndrome, carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon or prostate. Additional uses of the invention include stimulation of food intake.
    Type: Grant
    Filed: October 21, 2005
    Date of Patent: December 29, 2009
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Weiqin Jiang, James J. Fiordeliso, Zhihua Sui
  • Patent number: 7638536
    Abstract: A 2-acylaminothiazole derivative or a pharmaceutically acceptable salt thereof having an excellent effect of proliferating human c-mpl-Ba/F3 cells and an activity of increasing platelets based on the effect of promoting the formation of megakaryocytic colonies. A compound or a pharmaceutically acceptable salt thereof useful in treating thrombocytopenia.
    Type: Grant
    Filed: January 15, 2003
    Date of Patent: December 29, 2009
    Assignee: Astellas Pharma Inc.
    Inventors: Keizo Sugasawa, Susumu Watanuki, Yuji Koga, Hiroshi Nagata, Kazuyoshi Obitsu, Ryutaro Wakayama, Fukushi Hirayama, Ken-ichi Suzuki
  • Publication number: 20090253656
    Abstract: The present invention is directed to a breast cancer resistance protein (BCRP/ABCG2) inhibitor. The BCRP inhibitor contains, as an active ingredient, an acrylonitrile derivative represented by formula (1): wherein one of R1 and R2 represents a cyano group and the other represents a hydrogen atom; Ar1 represents a group selected from among the groups represented by formulas (2) to (4): and Ar2 represents an aromatic hydrocarbon group having a condensed ring which may be substituted by a halogen atom, or a group selected from among the groups represented by the following formulas (5) to (15): or a salt thereof.
    Type: Application
    Filed: March 29, 2006
    Publication date: October 8, 2009
    Applicant: Kabushiki Kaisha Yakult Honsha
    Inventors: Ryuta Yamazaki, Yukiko Nishiyama, Tomio Furuta, Takeshi Matsuzaki, Hiroshi Hatano, Oh Yoshida, Masato Nagaoka, Ritsuo Aiyama, Shusuke Hashimoto, Yoshikazu Sugimoto
  • Patent number: 7595331
    Abstract: N- and O-substituted 4[2-diaromaticmethoxy and methylamino)alkyl]piperidines exhibit high CNS activity with respect to the dopamine transporter (DAT) and serotonin transporter (SERT). Preferred compounds exhibit highly differential behavior as between the DAT and SERT and between the DAT and the norepinephrine transporter (NET). The compounds have utility in treating CNS disorders, including but not limited to cocaine addiction, depression, and Parkinson's disease.
    Type: Grant
    Filed: December 8, 2004
    Date of Patent: September 29, 2009
    Assignee: Wayne State University
    Inventor: Aloke K. Dutta
  • Patent number: 7544700
    Abstract: The present invention is related to sulfonamide derivatives having a lipophilic moiety and which are substantially soluble. Said compounds are notably for use as pharmaceutically active compounds. The present invention also related to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK 2 and 3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation.
    Type: Grant
    Filed: September 27, 2001
    Date of Patent: June 9, 2009
    Assignee: Laboratoires Serono SA
    Inventors: Serge Halazy, Dennis Church, Stephen J. Arkinstall, Marco Biamonte, Montserrat Camps, Jean-Pierre Gotteland, Thomas Rueckle