Three Or More Hetero Atoms In The Tetracyclo Ring System Patents (Class 514/287)
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Publication number: 20130303563Abstract: The invention provides, in certain embodiments, a method of preventing and/or treating peritoneal injury and/or diminished function by administering an effective amount of one or more inhibitors of JAK. The invention also provides a pharmaceutical composition including a JAK inhibitor for the treatment of peritoneal injury and/or diminished function. In another aspect, the invention provides a method of detecting an indicator of peritoneal injury. The method entails assaying a biological sample for periostin, wherein the presence of periostin at an elevated level indicates the presence and/or degree of peritoneal injury. Also provided, are methods of identifying subject for treatment of peritoneal injury and/or diminished function, methods of determining progression of these conditions, as well as methods of determining subjects' response to treatment.Type: ApplicationFiled: March 14, 2013Publication date: November 14, 2013Inventors: Sharon ADLER, Bancha SATIRAPOJ, Ying WANG, Cynthia C. NAST, Tiane DAI
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Publication number: 20130296307Abstract: Provided herein are compounds according to Formula I and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancers such as colon, ovarian, pancreatic, breast, liver, prostate and hematologic cancers:Type: ApplicationFiled: July 10, 2013Publication date: November 7, 2013Inventors: John Hood, Sunil Kumar KC, David Mark Wallace
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Patent number: 8569331Abstract: The present invention relates to substituted benzo[f]imidazo[1,2-d]pyrido[2,3-b][1,4]diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzo[f]imidazo[1,2-d]pyrido[2,3-b][1,4]diazepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: November 1, 2011Date of Patent: October 29, 2013Assignee: ArQule, Inc.Inventors: Mark A. Ashwell, Sudharshan Eathiraj, Anton Filikov, Steffi Koerner, Jean-Marc Lapierre, Yanbin Liu, Rocio Palma, David Vensel, Shin Iimura, Akiko Shiina, Kenichi Yoshida, Takanori Yamazaki, Akihisa Matsuda
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Publication number: 20130281482Abstract: The invention provides novel nicotinic acetylcholine receptor agonists, for example, phantasmidine and derivatives thereof, for example a compound of formula (I). Also disclosed are methods of treating disorders responsive to nicotinic acetylcholine receptor agonists such as Alzheimer's disease, schizophrenia, Myasthenia Gravis, Tourette's syndrome, Parkinson's disease, epilepsy, pain, and cognitive dysfunction by treatment with the nicotinic acetylcholine for agonists.Type: ApplicationFiled: March 18, 2011Publication date: October 24, 2013Applicant: The United States of America, as represented by Secretary, Department of Health and Human ServicesInventor: Kathryn Daly
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Publication number: 20130261147Abstract: There is provided use of Lycoris aurea extracts, and/or fractions thereof, and/or lycoricidine and lycoricidinol separated from the extracts or fractions for prevention and/or treatment of dementia.Type: ApplicationFiled: August 27, 2010Publication date: October 3, 2013Applicants: HUAZHONG UNIVERSITY OF SCIENCE & TECHNOLOGY, KOREA INSTITUTE OF SCIENCE AND TECHNOLOGYInventors: Hyun Ok Yang, Hak Cheol Kwon, Jin-Soo Park, Sung-Kwon Chung, ZhiZou Wu, Hanli Ruan, Huifang Pi, Peng Zhang
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Publication number: 20130231360Abstract: The present disclosure is directed to compounds of Formula (I) which are inhibitors of Haspin kinase and DYRK kinases. The compounds of the present disclosure, and compositions thereof, are useful in the treatment of disease related to Haspin kinase and DYRK kinase expression and/or activity.Type: ApplicationFiled: April 21, 2011Publication date: September 5, 2013Applicant: THE BRIGHAM AND WOMEN S HOSPITAL, INC.Inventors: Jonathan Higgins, Debasis Patnaik, Natalia Ulyanova, Ross L. Stein, Jun Xian, Marcie Glicksman, Gregory D. Cuny
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Publication number: 20130225558Abstract: This disclosure is directed to fused tetracyclic pyrido[4,3-b>]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: February 18, 2011Publication date: August 29, 2013Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
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Publication number: 20130217675Abstract: This disclosure is directed to pyrido[4,3-b]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: February 18, 2011Publication date: August 22, 2013Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
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Patent number: 8501763Abstract: The invention provides inhibitors of focal adhesion kinase, an enzyme involved in the attachment of the cytoskeleton of a cell to an extracellular matrix, which has been implicated in processes such as cell migration, cell proliferation, and cell survival. The inhibitors are derivatives of a 5-substituted 2,4-diaminopyridine wherein the substituents are as defined herein. The invention also provides a method of using the inhibitors in treatment of cancer, and methods of preparation of the inhibitors by use of coupling reactions.Type: GrantFiled: March 10, 2008Date of Patent: August 6, 2013Assignee: The Scripps Research InstituteInventors: Congxin Liang, Marcel Koenig, Yuanjun He, Par Holmberg
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Publication number: 20130190294Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor ?2A. The compounds may also bind to and are an antagonist of the adrenergic receptor ?2B; or the compounds are not antagonists of the adrenergic receptor ?2B and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.Type: ApplicationFiled: March 7, 2013Publication date: July 25, 2013Applicant: MEDIVATION TECHNOLOGIES, INC.Inventor: Medivation Technologies, Inc
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Publication number: 20130190344Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: March 8, 2013Publication date: July 25, 2013Applicant: MEDIVATION TECHNOLOGIES, INC.Inventor: MEDIVATION TECHNOLOGIES, INC.
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Publication number: 20130184303Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: March 8, 2013Publication date: July 18, 2013Applicant: MEDIVATION TECHNOLOGIES, INC.Inventor: Medivation Technologies, Inc.
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Publication number: 20130184304Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: March 8, 2013Publication date: July 18, 2013Applicant: Medivation Technologies, Inc.Inventor: Medivation Technologies, Inc.
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Publication number: 20130177632Abstract: The present invention provides therapeutically effective 2,4,5-trisubstituted imidazole compounds, methods of preparing the same, and compositions comprising the compounds alone or in combination with other agents. The present invention further provides for the use of the compounds as anti-microbial agents. The anti-microbial properties of the compounds include anti-bacterial and/or anti-fungal activity.Type: ApplicationFiled: February 27, 2013Publication date: July 11, 2013Inventors: Raed H. Al-Qawasmeh, Aiping H. Young, Mario Huesca, Yoon S. Lee
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Publication number: 20130121986Abstract: The present invention concerns nitrogenated derivatives of narciclasine and pancratistatin of the following general formula (I) as well as their pharmaceutically acceptable salts. The present invention also concerns the use of these compounds in cancer therapy as well as a method for their preparation.Type: ApplicationFiled: December 26, 2012Publication date: May 16, 2013Inventors: Frederic MARION, Jean-Philippe ANNEREAU, Jacques FAHY
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Patent number: 8431564Abstract: The invention relates to ring-annulated dihydropyrrolo[2,1-a]isoquinoline compounds according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.Type: GrantFiled: July 27, 2010Date of Patent: April 30, 2013Assignee: Merck Sharp & Dohme B.V.Inventors: Cornelis Marius Timmers, Hubert Jan Jozef Loozen, Herman Thijs Stock
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Publication number: 20130090331Abstract: The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: March 26, 2012Publication date: April 11, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Youssef Bennani, Tiansheng Wang, Francesco Salituro, John Duffy
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Patent number: 8415348Abstract: The present invention concerns nitrogenated derivatives of narciclasine and pancratistatin of the following general formula (I) as well their pharmaceutically acceptable salts. The present invention also concerns the use of these compounds in cancer therapy as well as a method for their preparation.Type: GrantFiled: July 28, 2009Date of Patent: April 9, 2013Assignee: Pierre Fabre MedicamentInventors: Frédéric Marion, Jean-Philippe Annereau, Jacques Fahy
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Publication number: 20130065875Abstract: The invention provides derivatives and analogues of triazatetracyclo[7.7.0.01,13,02,7]-hexadeca-2,4,6,10,12-pentaenes, 5,7,11-triazatetracyclo[8.7.0.01,6,012,17]-heptadeca-6,8,12,14,16-pentaenes, pharmaceutical compositions comprising these compounds and methods for treatment of hepatitis C viral infections using these compounds.Type: ApplicationFiled: October 27, 2010Publication date: March 14, 2013Applicants: THE SCRIPPS RESEARCH INSTITUTE, TRUSTEES OF BOSTON UNIVERSITYInventors: John K. Snyder, Wanguo Wei, Feng Ni, Arthur Donny Strosberg, Smitha Kota, Virginia Takahashi
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Patent number: 8394815Abstract: The present invention provides therapeutically effective 2,4,5-trisubstituted imidazole compounds, methods of preparing the same, and compositions comprising the compounds alone or in combination with other agents. The present invention further provides for the use of the compounds as anti-microbial agents. The anti-microbial properties of the compounds include anti-bacterial and/or anti-fungal activity.Type: GrantFiled: December 22, 2010Date of Patent: March 12, 2013Assignee: Lorus Therapeutics Inc.Inventors: Raed H. Al-Qawasmeh, Aiping H. Young, Mario Huesca, Yoon S. Lee
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Publication number: 20130053367Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor ?2A. The compounds may also bind to and are an antagonist of the adrenergic receptor ?2B; or the compounds are not antagonists of the adrenergic receptor ?2B and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.Type: ApplicationFiled: February 17, 2012Publication date: February 28, 2013Inventors: Andrew Asher Protter, Sarvajit Chakravarty, Rajendra Parasmal Jain, Michael John Green
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Publication number: 20130053366Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are adrenergic receptor ?2B antagonists. The compounds may also bind to and antagonize adrenergic receptor ?1B. The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption. The compounds may also be used to treat diseases or conditions that are, or are expected to be, responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular and renal disorders is particularly described.Type: ApplicationFiled: February 17, 2012Publication date: February 28, 2013Inventors: Andrew Asher Protter, Sarvajit Chakravarty, Rajendra Parasmal Jain, Michael John Green
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Publication number: 20130053363Abstract: [Problem] To provide a compound useful as medicine having PDE4B inhibitory activity, in particular, as an active ingredient of a composition for treating or preventing schizophrenia, Alzheimer's disease, dementia, depression and the like. [Measures for Solution] The present inventors examined compounds having PDE4B inhibitory activity and found that a tricyclic or tetracyclic imidazo[1,2-a]pyridine derivative or salts thereof had a superior PDE4B inhibitory activity, thereby completing the present invention. The imidazo[1,2-a]pyridine derivative can be used as an agent for treating or preventing schizophrenia, Alzheimer's disease, dementia, depression and the like.Type: ApplicationFiled: October 26, 2012Publication date: February 28, 2013Applicant: Astellas Pharma Inc.Inventor: Astellas Pharma Inc.
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Publication number: 20130046283Abstract: Methods and intravascular treatment devices for treating atherosclerosis are provided.Type: ApplicationFiled: May 4, 2012Publication date: February 21, 2013Applicant: Medtronic Vascular, Inc.Inventors: Ayala Hezi-Yamit, Susan Edwards, Carol Sullivan, Oluwashola Shakirat Sulaimon, Lori Garcia, Stefan Tunev
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Patent number: 8318764Abstract: The present invention relates to the use of novel macrocyclic compounds of Formula I, wherein the variables Q, Q1, Q2, Q3, and Q4 are defined as described herein, which inhibit JAK and are useful for the treatment of auto-immune and inflammatory diseases.Type: GrantFiled: September 17, 2010Date of Patent: November 27, 2012Assignee: Roche Palo Alto LLCInventors: Alam Jahangir, Stephen M Lynch, Michael Soth, Hanbiao Yang
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Patent number: 8293762Abstract: Heteroarylpyridinone derivatives represented by formula (I) wherein R1, R2, R3, R4, R5, and X are as defined in the specification, compositions thereof, and methods of use thereof. Particularly, there are described isoquinolinoyrrolopyridinones, pharmaceutical compositions including them and their use as therapeutic agents in the treatment of cancer and cell proliferation disorders.Type: GrantFiled: February 18, 2008Date of Patent: October 23, 2012Assignee: Nerviano Medical Sciences S.R.L.Inventors: Ermes Vanotti, Maria Menichincheri, Alessandra Scolaro
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Publication number: 20120258980Abstract: A method for treating an individual infected with drug-resistant bacteria resistant to at least one drug, the method including: administering to the individual an antibacterial agent for drug-resistant bacteria which comprises at least one of a nybomycin and a derivative thereof, wherein the antibacterial agent for drug-resistant bacteria is effective to the drug-resistant bacteria resistant to at least one drug.Type: ApplicationFiled: May 9, 2012Publication date: October 11, 2012Inventors: Masayuki Igarashi, Keiichi Hiramatsu
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Publication number: 20120225903Abstract: The invention relates to 2-substituted quinoline derivatives, to a method for preparing same, and to the use thereof for drug production, particularly for treating infections caused by protozoa, such as leishmaniases, trypanosomiases, toxoplasmoses, and/or infections caused by retroviruses such as, for example, HIV or HTLV.Type: ApplicationFiled: May 15, 2009Publication date: September 6, 2012Inventors: Alain Fournet, Bernardin Akagah, Bruno Figadere, Anh Tuan Lormier
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Publication number: 20120196889Abstract: The present invention relates to novel catecholamine derivatives of Formula I, to processes for their preparation, pharmaceutical compositions containing them and to their use in therapy.Type: ApplicationFiled: February 24, 2010Publication date: August 2, 2012Applicant: H. Lundbeck A/SInventors: Benny Bang-Andersen, Mogens Larsen, Klaus Gundertofte, Morten Jorgensen, Jennifer Larsen, Niels Mork, HåKan Wikström
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Publication number: 20120108624Abstract: Disclosed herein are methods of treating Parkinsons disease while maintaining a low dyskinesia induction profile and methods of reversing dyskinesias comprising administering a therapeutically effective amount of a compound of the invention. The present invention further relates to uses and pharmaceutical compositions of said compounds in the manufacture of medicaments in treating the same.Type: ApplicationFiled: February 26, 2010Publication date: May 3, 2012Inventors: Håkan Wikström, Morten Jørgensen, Niels Mork, Jennifer Larsen, Lars Torup, Benny Bang-Andersen
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Publication number: 20120095006Abstract: This invention relates to the use of certain cyclic guanosine 3?,5?-monophosphate phosphodiesterase type five (cGMP PDE5) inhibitors, including in particular the compound sildenafil, for the treatment of pulmonary hypertension.Type: ApplicationFiled: December 16, 2011Publication date: April 19, 2012Inventors: Ghazwan Saleem Butrous, Timothy Michael Lukas, Ian Machin
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Patent number: 8148392Abstract: 2-indolyl imidazo[4,5-d]phenanthroline compounds of Formula (I) and methods of using same in the treatment of cancer, in particular, solid cancers and leukemia are provided. Pharmaceutical compositions comprising the compounds are also provided.Type: GrantFiled: May 25, 2006Date of Patent: April 3, 2012Assignee: Lorus Therapeutics Inc.Inventors: Mario Huesca, Aiping H. Young, Yoon Lee, Aye Aye Khine, Jim A. Wright, Lisa Lock, Raed Al-Qawasmeh
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Publication number: 20120058940Abstract: Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.Type: ApplicationFiled: July 1, 2010Publication date: March 8, 2012Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Peter R. GUZZO, Matthew David SURMAN, Alan John HENDERSON, May Xiaowu JIANG
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Patent number: 8106090Abstract: The present invention is directed to compounds of formula (I): or a pharmaceutically acceptable salt thereof; wherein A is (II); X is selected from CH, CF and N, R8 is selected from H, C1-C6 alkyl, aryl, heteroaryl, C1-C6 alkylaryl, C1-C6 alkylheteroaryl, C2-C6 alkyl-O—C1-C6 alkyl, C1-C6 haloalkyl, hydroxy C2-C6 alkyl, —C(O)R9 and —SO2R9, or R7 and R8 combine to form (III), (IV); W is selected from CR1O and CR15, R1O is selected from H, halo, —C(O)NR13R14, C1-C6 alkyl, aryl, heteroaryl, C1-C6 alkylaryl, C1-C6 alkylheteroaryl, C1-C6 alkyl-O—C1-C6 alkyl and hydroxy C1-C6 alkyl; Het is a N-linked 5-membered heteroaryl ring optionally substituted with 1-3 substituents selected from methoxy, Cl, F, CH3, CF3, aryl, heteroaryl, C1-C4 alkylaryl or C1-C4 alkylheteroaryl, for use as inhibitors of the DPP-IV enzyme in the treatment or prevention of conditions including Type II diabetes.Type: GrantFiled: July 14, 2006Date of Patent: January 31, 2012Assignee: Eli Lilly and CompanyInventors: Larry Chris Blaszczak, Shon Roland Pulley, Michael Alan Robertson, Scott Martin Sheehan, Qing Shi, Michael Robert Wiley
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Patent number: 8097635Abstract: An object of the present invention is to provide a safe and highly effective insulin resistance improving agent or therapeutic agent for type II diabetes. According to the present invention, an insulin resistance improving agent or a therapeutic agent for type II diabetes comprising a compound represented by general formula (I) (wherein R1, R2, and R3 are the same as or different from each other, and each represents lower alkyl, lower alkenyl, lower alkynyl, aralkyl, araryl, phenyl, or a hydrogen atom) or a salt thereof as an active ingredient can be provided.Type: GrantFiled: September 19, 2007Date of Patent: January 17, 2012Assignees: Kyowa Hakko Bio Co., Ltd., Mitsubishi Gas Chemical Company, Inc.Inventors: Mika Sumi, Fumiko Ogino, Toshikazu Kamiya, Masahiko Nakano, Kazutoshi Kikkawa
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Patent number: 8088788Abstract: [1,2]Imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and imidazo[4,5-c]pyridines) substituted with a fused ring containing an oxygen and/or nitrogen atom attached at the 1- and/or 2-position, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: GrantFiled: March 14, 2007Date of Patent: January 3, 2012Assignee: 3M Innovative Properties CompanyInventors: Tushar A. Kshirsagar, Karl J. Manske, Larry R. Krepski, Joan T. Moseman, George W. Griesgraber, Sarah Johannessen Slania, Scott E. Langer, Philip D. Heppner
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Patent number: 8088785Abstract: Compositions and uses associated with the MT477 family of compounds are disclosed. Particular structural features and properties of the compounds are described in detail. Uses include administering an MT477 family member to a patient for therapeutic purposes. Compositions include chemicals belonging to the MT477 family and pharmaceuticals that contain such chemicals.Type: GrantFiled: December 10, 2009Date of Patent: January 3, 2012Assignee: Medisyn Technologies, Inc.Inventors: Javier Llompart, Jorge Galvez, Kollol Pal
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Publication number: 20110306629Abstract: The present application relates to novel C-1 substituted analogues of pancratistatin and 7-dexoypancratistatin of Formula (I), pharmaceutical compositions thereof and the use of said compounds of Formula (I) in the treatment of cancer The application also relates to processes for the preparation of said compound of Formula (I) and intermediates thereof.Type: ApplicationFiled: December 17, 2009Publication date: December 15, 2011Applicant: BROCK UNIVERSITYInventors: Tomas Hudlicky, Jonathan Collins
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Patent number: 8044065Abstract: Compounds of a certain formula I, in which R1, R2, R3, R4 and X have the meanings indicated in the description, are novel effective compounds with Eg5 inhibitory, anti-proliferative and/or apoptosis inducing activity.Type: GrantFiled: March 30, 2010Date of Patent: October 25, 2011Assignee: Altana Pharma AGInventors: Matthias Vennemann, Thomas Baer, Gudrun Groegor
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Patent number: 8034938Abstract: Substituted fused [1,2]imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and 6,7,8,9-tetrahydroimidazo[4,5-c]naphthyridines) with a —CH(—R1)— group in the fused ring at the 1-position of the imidazo ring, wherein R1 includes a functional group, for example, an amide, sulfonamide, urea, carbamate, ester, ketone, ether, a thio analog of the forgoing, sulfone, oxime, or hydroxylamine, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: GrantFiled: December 29, 2005Date of Patent: October 11, 2011Assignee: 3M Innovative Properties CompanyInventors: George W. Griesgraber, Tushar A. Kshirsagar, Sarah J. Slania, Michael E. Danielson
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Publication number: 20110245272Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: September 23, 2010Publication date: October 6, 2011Inventors: Rajendra Parasmal Jain, Sarvajit Chakravarty
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Publication number: 20110218184Abstract: The present invention provides novel quinolone compounds and pharmaceutical composition thereof which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing such compounds and compositions, and methods of making and using the same.Type: ApplicationFiled: March 9, 2011Publication date: September 8, 2011Applicant: CYLENE PHARMACEUTICALS, INC.Inventors: Johnny Yasuo NAGASAWA, Fabrice Pierre, Mustapha Haddach, Michael Schwaebe, Levan Darjania, Jeffrey P. Whitten
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Patent number: 7994187Abstract: HIV inhibitory compounds of formula: salts, hydrates, solvates, N-oxides, or stereoisomers thereof, wherein A forms pyridine, pyrimidine, pyrazine, pyridazine, triazine, imidazole, pyrazole, triazole, tetrazole, oxazole, isoxazole, oxadiazole, thiazole, isothiazole, and thiadiazole; R1 is halo, cyano, nitro, C1-6alkyl, polyhaloC1-6alkyl, —C1-6alkyl-OR4, —C(?O)—R5, —C(?O)—OR4, —C(?O)—NR6R7, —OR4, —O—C(?O)—C1-6alkyl, —O—C1-6alkyl-OR4, —O—C1-6alkyl-NR6R7, —O—C1-6alkyl-O—C(?O)—C1-6alkyl, —O—C1-6alkyl-C(?O)—OR4, —O—C1-6alkyl-C(?O)—NR6R7, —NR6R7, —NR8—C(?O)—R5, —NR8—C(?O)—OR4, —NR8—C(?O)—NR6R7, —NR8—C(?O)—C1-6alkyl-C(?O)—OR4, —NR8—C1-6alkyl-OR4, —NR8—C1-6alkyl-NR6R7, —NR8—C1-6alkyl-imidazolyl, —NR8—SO2R9, —N?CH—NR6R7, —NH—C(?NH)—NH2, —SO2NR6R7, and —O—PO(OR8)2; D forms pyridine, pyrimidine, pyrazine, pyridazine, pyrrole, imidazole, pyrazole, furane, oxazole, isoxazole, thiophene, thiazole, and isothiazole; R2 is C1-6alkyl, polyhaloC1-6alkyl, halo, cyano, —COOR4, —OR4, and —NR6R7; R3 is phenyl, pyridyl, pyrimidType: GrantFiled: April 3, 2007Date of Patent: August 9, 2011Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Bart Rudolf Romanie Kesteleyn, Wim Bert Griet Schepens
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Publication number: 20110190312Abstract: The invention relates to a combination which comprises: (a) an epothilone; and (b) a protein tyrosine kinase inhibitor; and optionally (c) a derivative of rapamycin; for simultaneous, separate or sequential use, in particular, for the delay of progression or treatment of a proliferative disease, especially cancer.Type: ApplicationFiled: April 13, 2011Publication date: August 4, 2011Inventors: Jerry Min-Jian Huang, Anandhi Ranganathan Johri, Ronald Richard Linnartz, Paul M.J. McSheehy
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Publication number: 20110136800Abstract: The present invention relates to compounds defined by formula I wherein the variables R1, R2, R3, R4, and m are defined as in claim 1, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.Type: ApplicationFiled: November 5, 2010Publication date: June 9, 2011Inventors: Matthias Eckhardt, Stefan Peters, Herbert Nar, Frank Himmelsbach, Linghang Zhuang
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Publication number: 20110123516Abstract: The present invention concerns nitrogenated derivatives of narciclasine and pancratistatin of the following general formula (I) as well their pharmaceutically acceptable salts. The present invention also concerns the use of these compounds in cancer therapy as well as a method for their preparation.Type: ApplicationFiled: July 28, 2009Publication date: May 26, 2011Applicant: PIERRE FABRE MEDICAMENTInventors: Frédéric Marion, Jean-Philippe Annereau, Jacques Fahy
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Publication number: 20110112086Abstract: The present invention provides pyridinone analogs which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing pyridinone analogs, and methods of using the same.Type: ApplicationFiled: June 8, 2007Publication date: May 12, 2011Applicant: CYLENE PHARMACEUTICALS, INC.Inventors: Fabrice Pierre, Michael Schwaebe
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Publication number: 20110104110Abstract: The present invention relates to Substituted Indole Derivatives, compositions comprising at least one Substituted Indole Derivative, and methods of using these Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: August 27, 2008Publication date: May 5, 2011Inventors: Gopinadhan N. Anikumar, Frank Bennett, Tin-Yau Chan, Kevin X. Chen, Mousumi Sannigrahi, Francisco Velazquez, Srikanth Venkatraman, Qingbei Zeng, Jose S. Duca, Charles A. Lesburg, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Neng-Yang Shih
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Publication number: 20110104109Abstract: The present invention relates to Tetracyclic Indole Derivatives, compositions comprising at least one Tetracyclic Indole Derivative, and methods of using the Tetracyclic Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: August 27, 2008Publication date: May 5, 2011Inventors: Frank Bennett, Qingbei Zeng, Srikanth Venkatraman, Mousumi Sannigrahi, Kevin X. Chen, Gopinadhan N. Anilkumar, Stuart B. Rosenblum, Joseph A. Kozlowski, F. George Njoroge
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Publication number: 20110105490Abstract: The present invention is directed to novel 2,3-dihydro-1H-isoindol-1-imine derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the thrombin PAR-1 receptor antagonists.Type: ApplicationFiled: October 28, 2010Publication date: May 5, 2011Inventors: Han-Cheng Zhang, Bruce Maryanoff, Kimberly White, Stephen C. Yabut, Hong Ye, Cailin Chen