Additional Hetero Ring, Attached Directly Or Indirectly To The Bicyclo Ring System By Nonionic Bonding Patents (Class 548/465)
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Publication number: 20120077982Abstract: The present invention discloses methods for synthesizing 3-(substituted dihydroisoindolinone-2-yl)-2,6-dioxopiperidine and intermediates thereof, namely, the synthesis of compounds of the Formula (I), with each substitutional group defined in the patent specification. Owing to the advantages of high productivity, little influence to the environment and material accessibility, the methods of the present invention is suitable for industrial production.Type: ApplicationFiled: June 1, 2010Publication date: March 29, 2012Applicants: NANJING CAVENDISH BIO-ENGINEERING TECHNOLOGY CO., LTD.Inventors: Rong Yan, Hao Yang, Yongxiang Xu
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Patent number: 8143288Abstract: Compounds having the structure of formula I are described. The compounds can inhibit hepatitis C virus (HCV) replication, and in particular can inhibit the function of the HCV NS5A protein.Type: GrantFiled: June 5, 2006Date of Patent: March 27, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Michael Serrano-Wu, Makonen Belema, Lawrence B. Snyder, Nicholas A. Meanwell, Denis R. St. Laurent, Ramesh Kakarla, Van N. Nguyen, Yuping Qiu, Xuejie Yang, John E. Leet, Min Gao, Donald R. O'Boyle, II, Julie A. Lemm, Fukang Yang
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Publication number: 20120058986Abstract: 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 Q and Z are defined herein.Type: ApplicationFiled: September 2, 2011Publication date: March 8, 2012Inventors: Peter J. Connolly, Mark J. Macielag, Bin Zhu
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Patent number: 8129424Abstract: This invention relates to compounds having pharmacological activity, to compositions containing these compounds, and to a method of treatment employing the compounds and compositions. More particularly, this invention concerns certain indole derivatives and their salts and solvates. These compounds have H3 histamine receptor antagonist activity. This invention also relates to pharmaceutical compositions containing these compounds and to a method of treating disorders in which histamine H3 receptor blockade is beneficial.Type: GrantFiled: November 10, 2010Date of Patent: March 6, 2012Assignee: Athersys, Inc.Inventors: Youssef L. Bennani, Michael G. Campbell, David Dastrup, Emilie Porter Huck
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Patent number: 8124639Abstract: The present invention relates to a series of substituted bicyclic[3.1.0]heteroaryl amides of the Formula I, wherein A, Q, X, Y, Z and R1-R5 groups are defined as in the specification, that exhibit activity as glycine transport inhibitors, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their use for the enhancement of cognition and the treatment of the positive and negative symptoms of schizophrenia and other psychoses in mammals, including humans.Type: GrantFiled: August 30, 2010Date of Patent: February 28, 2012Assignee: Pfizer Inc.Inventors: Stanton F. McHardy, John A. Lowe, III
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Patent number: 8106059Abstract: The present invention is directed to compounds of formula I, below, that have the dual property of acting as cathepsin S inhibitors and of inhibiting HCV replication. Such compounds are therefore useful in treating disease states that include hepatitis C, Alzheimer's disease, and autoimmune disorders. The present invention is also directed to pharmaceutical compositions containing these compounds, and processes for preparing the compounds.Type: GrantFiled: October 22, 2008Date of Patent: January 31, 2012Assignee: ViroBay, Inc.Inventors: Leslie Jean Holsinger, Kyle Elrod, John O. Link, Michael Graupe, In Jong Kim
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Patent number: 8106187Abstract: The present invention relates to a new process for the preparation of macrocyclic HCV protease inhibitor compounds of the formula wherein R1 is an amino protecting group and X is halogen by way of a ring closing metathesis approach.Type: GrantFiled: August 7, 2009Date of Patent: January 31, 2012Assignee: Roche Palo Alto LLCInventors: Michelangelo Scalone, Helmut Stahr
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Publication number: 20120022057Abstract: The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below (I).Type: ApplicationFiled: March 16, 2010Publication date: January 26, 2012Applicant: Schering CorporationInventors: Gang Zhou, Grant Wishart, Pauline C. Ting, Robert G. Aslanian, Nicolas Zorn, Jianhua Cao
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Patent number: 8097623Abstract: There is provided compounds of formula (I), wherein X1, Q, T, Y, R1, R2, R3, R4 and R5 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation.Type: GrantFiled: December 22, 2005Date of Patent: January 17, 2012Assignee: Biolipox ABInventors: Benjamin Pelcman, Kristofer Olofsson, Martins Katkevics, Vita Ozola, Edgars Suna, Ivars Kalvins, Peteris Trapencieris, Dace Katkevica, Wesley Schaal
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Patent number: 8093411Abstract: The quenching compounds of the invention are weakly luminescent cyanines that are substituted by one or more heteroaromatic quenching moieties. The quenching compounds of the invention exhibit little or no observable luminescence and efficiently quench a broad spectrum of luminescent compounds. The chemically reactive quenching compounds possess utility for labeling a wide variety of substances, including biomolecules. These labeled substances are highly useful for a variety of energy-transfer assays and applications.Type: GrantFiled: August 30, 2010Date of Patent: January 10, 2012Assignee: AnaSpec IncorporatedInventors: Zhenjun Diwu, Jianheng Zhang, Yi Tang
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Patent number: 8080576Abstract: One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.Type: GrantFiled: February 19, 2010Date of Patent: December 20, 2011Assignee: Onyx Therapeutics, Inc.Inventors: Kevin D. Shenk, Francesco Parlati, Han-Jie Zhou, Catherine Sylvain, Mark S. Smyth, Mark K. Bennett, Guy J. Laidig
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Patent number: 8067414Abstract: The invention provides compositions and kits comprising at least one nitric oxide enhancing prostaglandin compound or a pharmaceutically acceptable salt thereof, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating ophthalmic disorders; (b) treating cerebrovascular disorders; (c) treating cardiovascular disorders; (d) treating benign prostatic hyperplasia (BPH); (e) treating peptic ulcers; (e) treating sexual dysfunctions and (f) inducing abortions. The nitric oxide enhancing prostaglandin compounds comprise at least one heterocyclic nitric oxide donor group and/or at least one nitroxide group.Type: GrantFiled: March 19, 2007Date of Patent: November 29, 2011Assignee: NiCox S.A.Inventor: David S. Garvey
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Patent number: 8063099Abstract: The invention relates to novel trans-3-aza-bicyclo[3.1.0]hexane derivatives of formula (I), wherein A, B, n and R1 are as described in the description, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists.Type: GrantFiled: July 25, 2008Date of Patent: November 22, 2011Assignee: Actelion Pharmaceuticals Ltd.Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, David Lehman, Thierry Sifferlen, Daniel Trachsel
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Publication number: 20110280804Abstract: Compounds having the general formula III?, or IV? wherein R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle or a radical of an optionally substituted cyclic or acyclic tertiary amine or isoindoline-1,3-dione: R2,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate, optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y is S; Z can be either H, O, S, S—R or NR where R groups can be either H, aryls, alkyls, or cycloalkyls; “n” can be 1 to 5 carbons in length and stereoisomers, functional analogs, and pharmaceutically acceptable salts thereof and wherein the moiety bridging R1 and N can be a substituted alkylene, optionally substituted alkenylene or optionally substituted alkynylene and where the alkylene group can include an inserted C3-C5 cycloalkyl group, aromatic, and heterocycliType: ApplicationFiled: June 1, 2011Publication date: November 17, 2011Applicants: The Board of Trustees of the Leland Stanford Junior University, University of MississippiInventors: Christopher R. McCurdy, Christophe Mesangeau, Frederick T. Chin, Michelle L. James, Bin Shen, Sanjiv Gambhir
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Patent number: 8048862Abstract: The embodiments provide compounds of the general Formulae I, II, III, IV, V, VI, VII, and X, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.Type: GrantFiled: April 14, 2009Date of Patent: November 1, 2011Assignee: InterMune, Inc.Inventors: Scott D. Seiwert, Leonid Beigelman, Brad Buckman, Antitsa Dimitrova Stoycheva, Steven B. Porter, Williamson Ziegler Bradford, Vladimir Serebryany
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Publication number: 20110263844Abstract: The present invention is directed to a method for the preparation of macrocyclic compounds of formula (I), comprising the step of cyclizing a diene of formula (II), in the presence of a catalyst, wherein R1-R6, A, W and V are as defined herein. The present invention is also directed to intermediate compounds of formula II.Type: ApplicationFiled: May 5, 2009Publication date: October 27, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Chutian Shu, Chris Hugh Senanayake, Zhulin Tan, Nathan Yee, Xingzhong Zeng
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Publication number: 20110257237Abstract: The present invention, relates to novel processes for the preparation of sunitinib malate formula (I), pharmaceutical compositions comprising said polymorph and the use of the said pharmaceutical compositions in the treatment of various forms of cancer.Type: ApplicationFiled: July 9, 2009Publication date: October 20, 2011Applicant: GENERICS [UK] LIMITEDInventors: Abhay Gaitonde, Vinayak Gore, Bharati Choudhari, Mahesh Hublikar, Prakash Bansode, Sunanda Phadtare
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Publication number: 20110257130Abstract: Compounds are provided which can be useful in reducing the activity of an angiotensin-converting enzyme and thus be used to treat or prevent a renin-angiotensin aldosterone system-related disorder. These compounds include lipoic acid derivatives such as prolyl lipoic acid and pipecolinyl lipoic acid, and other compounds, and these compounds are useful in treating hypertension, stroke, or other renin-angiotensin aldosterone system-related disorders in human or animal patients. Pharmaceutical compositions prepared using these compounds and methods of treatment using these compounds are also provided.Type: ApplicationFiled: October 16, 2009Publication date: October 20, 2011Inventor: Desikan Rajagopal
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Patent number: 8039470Abstract: The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of kinase-mediated processes, and treatment of disease and disease symptoms, particularly those mediated by certain kinase enzymes.Type: GrantFiled: January 28, 2010Date of Patent: October 18, 2011Assignee: Tyrogenex, Inc.Inventors: Congxin Liang, Ming Qi, Shu Gao, Zhigang Li
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Patent number: 8039467Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF-? or combinations thereof.Type: GrantFiled: October 20, 2009Date of Patent: October 18, 2011Assignee: Schering CorporationInventor: Chaoyang Dai
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Patent number: 8030341Abstract: The present invention relates to symmetric and asymmetric dimeric Dmt (2?,6?-ditnethyl) compounds and Dmt derivative compounds with dual ? and ? opioid receptor antagonist activity. Also, the present invention provides compositions comprising these compounds and it provides methods of using these compounds.Type: GrantFiled: August 30, 2006Date of Patent: October 4, 2011Assignees: The United States of America as represented by the Secretary of the Department of Health and Human Services, Kobe Gakuin UniversityInventors: Lawrence H. Lazarus, Yoshio Okada, Tingyou Li
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Publication number: 20110237559Abstract: In its many embodiments, the present invention relates to a novel class of 6-substituted sulfonyl-1,3,3-trialkyl-6-azabicyclo[3.2.1]octane compounds useful to inhibit 11?-hydroxysteroid dehydrogenase type-I, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the expression of 11?-hydroxysteroid dehydrogenase type-I using such compounds or pharmaceutical compositions.Type: ApplicationFiled: August 12, 2008Publication date: September 29, 2011Applicant: Schering CorporationInventors: Craig D. Boyle, Samuel Chackalamannil, Unmesh Shah, Claire M. Lankin
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Patent number: 8026237Abstract: Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.Type: GrantFiled: July 30, 2005Date of Patent: September 27, 2011Assignee: Exelixis, Inc.Inventors: Lynne Canne Bannen, Jeff Chen, Lisa Esther Dalrymple, Brenton T Flatt, Timothy Patrick Forsyth, Xiao-Hui Gu, Morrison B Mac, Larry W Mann, Grace Mann, Richard Martin, Raju Mohan, Brett Murphy, Michael Charles Nyman, William C Stevens, Tie-Lin Wang, Yong Wang, Jason H Wu
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Patent number: 8022250Abstract: 1-Phenylalkanecarboxylic acid derivatives, the processes for the preparation thereof and the use thereof in the treatment and/or prevention of neurodegenerative diseases such as Alzheimer's disease.Type: GrantFiled: December 24, 2009Date of Patent: September 20, 2011Assignee: Chiesi Farmaceutici S.p.A.Inventors: Luca Raveglia, Ilaria Peretto, Stefano Radaelli, Bruno Pietro Imbimbo, Andrea Rizzi, Gino Villetti
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Patent number: 8008491Abstract: The present invention relates to a series of substituted aza-indole derivatives of the formula I: wherein R, R1, R2, R3, R4, X and Y are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5?-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.Type: GrantFiled: June 17, 2008Date of Patent: August 30, 2011Assignee: Aventis Pharmaceuticals, Inc.Inventors: John Ziqi Jiang, Jack Roger Koehl, Shujaath Mehdi, Neil Moorcroft, Kwon Yon Musick, Philip Marvin Weintraub, Paul Robert Eastwood
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Patent number: 8008320Abstract: The present invention relates to a compound of formula (I) wherein R1 is H, C1-C6-alkyl, phenyl-C1-C4-alkyl or phenyl, R2 is a phenyl group which is substituted with 2 or 3 C1-C6-alkoxy groups and R3 is indolyl or azaindolyl which may carry one or two substituents independently selected from C1-C6-alkyl, C1-C6-alkoxy, phenyl, OH, halogen, NH2, C1-C6-alkylamino, di-C1-C6-alkylamino, heteroaryl with 5 or 6 ring atoms containing 1 or 2 heteroatoms which are independently selected from O, N, and S and heterocyclyl with 5 or 6 ring atoms containing 1 or 2 heteroatoms which are independently selected from O, N, and S and the physiologically acceptable salts thereof as well as the physiologically acceptable solvates of the compounds of formula 1 and of the salts thereof. The compounds of formula (I) are suitable for controlling angiogenesis.Type: GrantFiled: December 7, 2005Date of Patent: August 30, 2011Assignee: Johannes Gutenberg-UniversitatisInventors: Gerd Dannhardt, Christian Peifer, Stanislav Plutizki, Jan-Peter Kramb
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Publication number: 20110190349Abstract: The present invention relates to a compound of formula I wherein R1/R2 are independently from each other hydrogen, (CR2)o-cycloalkyl, optionally substituted by lower alkyl or hydroxy, or are lower alkyl or heterocycloalkyl, and o is 0 or 1; and R may be the same or different and is hydrogen or lower alkyl; or R1 and R2 may form together with the N atom to which they are attached a heterocycloalkyl group, selected from the group consisting of pyrrolidinyl, piperidinyl, 3-aza-bicyclo[3.1.0]hex-3-yl or 2-aza-bicyclo[3.1.Type: ApplicationFiled: January 21, 2011Publication date: August 4, 2011Inventors: Sabine Kolczewski, Emmanuel Pinard
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Patent number: 7985763Abstract: A compound of the following formula: in which R1, R2, R3, U, V, T, W, X, Y, Z, m, n, p, x, y, and z are as defined herein. Also disclosed are (1) a pharmaceutical composition containing such a compound, and (2) a method for treating Hepatitis C virus infection using such a compound.Type: GrantFiled: March 26, 2008Date of Patent: July 26, 2011Assignee: National Health Research InstitutesInventors: Li-Wen Wang, Tsu-An Hsu, Yen-Chun Lee, Iou-Jiun Kang, Chung-Chi Lee, Yu-Sheng Chao, Jyh-Haur Chern
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Publication number: 20110177006Abstract: The invention provides optical agents, including compositions, preparations and formulations, and methods of using and making optical agents. Optical agents of the present invention include dyes, and derivatives thereof, having a fused ring backbone structure having dithienofuran core. In some embodiments, dyes of the present invention are dithienofuran dyes having a dithienofuran core optionally functionalized to provide useful optical, biological, pharmacokinetic and/or physical properties.Type: ApplicationFiled: September 29, 2009Publication date: July 21, 2011Inventors: Raghavan Rajagopalan, William L. Neumann, Amruta Poreddy, John N. Freskos, Richard B. Dorshow
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Publication number: 20110177007Abstract: The invention provides optical agents, including compositions, preparations and formulations, and methods of using and making optical agents. Optical agents of the present invention include dyes, and derivatives thereof, having a fused ring backbone structure having dithienopyrrole core. In some embodiments, dyes of the present invention are dithienopyrrole dyes having a dithienopyrrole core optionally functionalized to provide useful optical, biological, pharmacokinetic and/or physical properties.Type: ApplicationFiled: September 29, 2009Publication date: July 21, 2011Inventors: Raghavan Rajagopalan, William L. Neumann, Amruta Poreddy, John N. Freskos, Richard B. Dorshow
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Patent number: 7977371Abstract: Objects of the present invention are to study on the synthesis of a novel pyrrole derivative having a ureido group and an aminocarbonyl group as substituents or a salt thereof, to find a pharmacological effect of the derivative or a salt thereof, and to find a medicinal agent which has a prophylactic and/or therapeutic effect on a retinal disease or the like through oral administration. A compound represented by the general formula (1) or a salt thereof has an inhibitory activity against the production of interleukin-6 and/or an inhibitory effect on choroidal neovascularization, and is therefore useful as a prophylactic and/or therapeutic agent for a disease associated with interleukin-6, an ocular inflammatory disease and/or a retinal disease.Type: GrantFiled: February 26, 2008Date of Patent: July 12, 2011Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Kenji Kawashima, Hiroshi Enomoto, Noriko Ishizaka, Minoru Yamamoto, Kazuhiro Kudou, Masaaki Murai, Takaaki Inaba, Kazuyoshi Okamoto
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Publication number: 20110160178Abstract: The invention relates to heterosubstituted N-thiolated beta-lactams, compositions comprising these compounds, methods for their production, and methods of use as antibiotics to inhibit the growth of bacteria. In one embodiment, the compounds have the structure shown in formula (A) or formula (B) or formula (C): wherein the R groups are as defined in the specification. The antibacterial agents of the invention can be administered to a human or animal to treat or inhibit bacterial infection, such as that of Staphylococcus species, including methicillin-resistant Staphylococcus aureus (MRSA).Type: ApplicationFiled: November 22, 2010Publication date: June 30, 2011Applicant: University of South FloridaInventors: EDWARD TUROS, Praveen Ramaraju
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Publication number: 20110144179Abstract: The present invention generally relates to substituted heterocyclic mercaptosulfonamide compounds, precursors, and derivatives as well as methods for the preparation of and pharmaceutical compositions comprising these compounds. These compounds are designed to be potent selective inhibitors of matrix metalloproteinases (MMPs), including, for example, gelatinases, collagenases, matrilysins, metalloelastase, stromelysin, and membrane-type 1 matrix metalloproteinase. These inhibitors may be used for the control of physiological and pathological processes and disease conditions in which MMPs are believed to play significant functions.Type: ApplicationFiled: September 2, 2009Publication date: June 16, 2011Inventors: Martin A. Schwartz, Yonghao Jin, Qing-Xiang (Amy) Sang
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Publication number: 20110124622Abstract: The invention relates to isoindolones of formula, (I) with anti-cancer and/or anti-inflammatory activity and more specifically with MEK kinase inhibitory activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth, treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.Type: ApplicationFiled: July 1, 2009Publication date: May 26, 2011Applicant: Genentech, Inc.Inventors: Emanuela Gancia, Robert Andrew Heald, Philip Jackson, Stephen Price
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Publication number: 20110118477Abstract: Process for the preparation of sunitinib malate form I via sunitinib acetate and polymorphs of said intermediate.Type: ApplicationFiled: July 23, 2009Publication date: May 19, 2011Applicant: TEVA PHARMACEUTICAL INDUSTRIES LTD.Inventors: Alexandr Jegorov, Ales Gavenda, Pavel Vraspir, Augusto Canavesi, Francesca Scarpitta
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Publication number: 20110118476Abstract: The present invention is directed to a 2-deoxyribose-5-phosphate aldolase (DERA) chemoenzymatic process for making chiral compounds.Type: ApplicationFiled: July 23, 2008Publication date: May 19, 2011Inventors: David W. Bauer, Padraig M. O'Nell, Timothy J. Watson, Shanghui Hu
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Publication number: 20110105580Abstract: The present invention relates to novel polymorphic forms of N-[2-(diethylamino)ethyl]-5-[(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl-2,4-dimethyl-1H-pyrrole-3-carboxamide-Sunitinib base (I). The present invention also relates to methods of preparing such polymorphic crystals.Type: ApplicationFiled: April 16, 2008Publication date: May 5, 2011Inventors: Srinivasa Krishna Murthy Konduri, Bhujanga rao Adibhatla Kali Satya, Nannapaneni Venkaiah Chowdary
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Publication number: 20110098469Abstract: The present invention provides a 1-thio-D-glucitol compound of the following formula, which shows the action of inhibiting the activity of SGLT2, a pharmaceutically acceptable salt of the compound, or a hydrate of the compound or the salt; and a pharmaceutical comprising such a compound as an active ingredient, especially, a pharmaceutical for preventing or treating diabetes, diabetes-related disease, or diabetic complication. The invention also provides a method for producing the 1-thio-D-glucitol compound and its intermediate.Type: ApplicationFiled: December 30, 2010Publication date: April 28, 2011Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Hiroyuki KAKINUMA, Yuko Hashimoto, Takahiro Ol, Hitomi Takahashi
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Patent number: 7932277Abstract: The embodiments provide compounds of the general Formula I, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments provide compounds of the general Formula II, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.Type: GrantFiled: May 9, 2008Date of Patent: April 26, 2011Assignees: InterMune, Inc., Array Biopharma Inc.Inventors: Scott Seiwert, Steven W. Andrews, Leonid Beigelman, Lawrence M. Blatt, Brad Buckman, Kevin R. Condroski, Yutong Jiang, Robert J. Kaus, April L. Kennedy, Timothy S. Kercher, Michael A. Lyon, Bin Wang
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Patent number: 7928136Abstract: The present invention relates to substituted 2-indolinone containing zinc-binding moiety based derivatives that have enhanced or unique properties as inhibitors of protein tyrosine kinase (PTK) receptors and their use in the treatment of PTK related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.Type: GrantFiled: September 10, 2007Date of Patent: April 19, 2011Assignee: Curis, Inc.Inventors: Xiong Cai, Changgeng Qian, Stephen Gould
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Patent number: 7927830Abstract: Chemically reactive carbocyanine dyes incorporating an indolium ring moiety that is substituted at the 3-position by a reactive group or by a conjugated substance, and their uses, are described. Conjugation through this position results in spectral properties that are uniformly superior to those of conjugates of spectrally similar dyes wherein attachment is at a different position. The invention includes derivative compounds having one or more benzo nitrogens.Type: GrantFiled: May 29, 2008Date of Patent: April 19, 2011Assignee: Life Technologies CorporationInventors: Ching-Ying Cheung, Stephen Yue, Wai-Yee Leung
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Publication number: 20110086073Abstract: The present invention describes nanoprodrugs of non-steroidal anti-inflammatory drug (NSAIDs) and nanoprodrugs of ?-lipoic acid-containing and NSAIDs. These nanoprodrugs have antioxidant properties and stimuli-responsiveness, which can be used to treat various disease conditions.Type: ApplicationFiled: April 8, 2009Publication date: April 14, 2011Applicant: Cedars-Sinai Medical CenterInventors: John S. Yu, Bong Seop Lee
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Publication number: 20110071156Abstract: The present invention relates to novel 1,3-dihydroindol-2-one (oxindole) derivatives of the formula (I) in which A, R3, R4, R5, R6, and R7 are defined according to claim 1, and to medicaments containing them for the treatment of diseases. In particular, the novel oxindole derivatives can be used for the control and/or prophylaxis of various vasopressin-dependent or oxytocin-dependent diseases.Type: ApplicationFiled: July 20, 2010Publication date: March 24, 2011Applicant: Abbott GmbH & Co. KGInventors: Thorsten Oost, Wilfried Hornberger, Herve Geneste, Daryl Richard Sauer, Wolfgang Wernet, Andrea Hager-Wernet, Liliane Unger, Wilfried Lubisch
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Patent number: 7910753Abstract: The quenching compounds of the invention are weakly luminescent cyanines that are substituted by one or more heteroaromatic quenching moieties. The quenching compounds of the invention exhibit little or no observable luminescence and efficiently quench a broad spectrum of luminescent compounds. The chemically reactive quenching compounds possess utility for labeling a wide variety of substances, including biomolecules. These labeled substances are highly useful for a variety of energy-transfer assays and applications.Type: GrantFiled: September 7, 2005Date of Patent: March 22, 2011Assignee: AnaSpec IncorporatedInventors: Zhenjun Diwu, Jianheng Zhang, Yi Tang
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Publication number: 20110065685Abstract: The present invention provides novel compounds of Formula (I) which are CB2 selective ligands useful for the treatment of pain.Type: ApplicationFiled: June 14, 2010Publication date: March 17, 2011Applicant: Abbott LaboratoriesInventors: Jennifer M. Frost, Karin Tietje, Michael J. Dart, Michael D. Meyer
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Publication number: 20110059966Abstract: This invention relates to compounds having pharmacological activity, to compositions containing these compounds, and to a method of treatment employing the compounds and compositions. More particularly, this invention concerns certain indole derivatives and their salts and solvates. These compounds have H3 histamine receptor antagonist activity. This invention also relates to pharmaceutical compositions containing these compounds and to a method of treating disorders in which histamine H3 receptor blockade is beneficial.Type: ApplicationFiled: November 10, 2010Publication date: March 10, 2011Inventors: Youssef L. Bennani, Michael G. Campbell, David Dastrup, Emilie Porter Huck
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Publication number: 20110059955Abstract: The present invention relates to novel 3-aminoalkyl-1,3-dihydro-2H-indol-2-one derivatives, to their preparation and to their therapeutic application. The compounds of the present invention correspond to the formula (I): in which the variables are as set forth in the specification. These compounds exhibit a strong affinity and a high selectivity for human arginine-vasopressin (AVP) V1a receptors and some compounds additionally exhibit a strong affinity for AVP V1b receptors.Type: ApplicationFiled: August 18, 2010Publication date: March 10, 2011Applicant: SANOFI-AVENTISInventors: Loic FOULON, Laurent GOULLIEUX, Brigitte POUZET, Claudine SERRADEIL-LE GAL, Gerard VALETTE
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Patent number: 7893279Abstract: The present invention provides a VLA-4 inhibitor having high water-solubility and excellent long-term stability; i.e., sodium trans-4-[1-[2,5-dichloro-4-[(1-methyl-1H-3-indolylcarbonyl)amino]phenylacetyl]-(4S)-methoxy-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylate pentahydrate.Type: GrantFiled: October 7, 2009Date of Patent: February 22, 2011Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Makoto Ono, Shigeru Noguchi
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Publication number: 20110039827Abstract: This invention provides compounds of formula (I): wherein R1, R2, G, m, n, p and q 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: ApplicationFiled: June 21, 2010Publication date: February 17, 2011Applicant: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Jeffrey P. Ciavarri, Kenneth M. Gigstad, He Xu
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Patent number: 7888383Abstract: There are provided according to the invention compounds of formula (I) in free or salt form, wherein R1, R2, R4, R5, R6, D, X, W, m and n are as described in the specification, process for preparing them, and their use as pharmaceuticals.Type: GrantFiled: December 7, 2006Date of Patent: February 15, 2011Assignee: Novartis AGInventor: David Andrew Sandham