Ring Nitrogen In The Polycyclo Ring System Patents (Class 514/339)
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Patent number: 7915260Abstract: The invention is directed to Urotensin II antagonists. More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating Urotensin-II mediated disorders. Pharmaceutical and veterinary compositions and methods of treating cardiovascular disorders and various other disease states or conditions using compounds of the invention are also described.Type: GrantFiled: January 10, 2007Date of Patent: March 29, 2011Inventors: Bruce E. Maryanoff, William A. Kinney, Edward C. Lawson, Diane K. Luci, Nikolay Marchenko, Sergey Sviridov, Shyamali Ghosh
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Publication number: 20110071175Abstract: Compound of formula (I) are ligands of the CRTH2 receptor, useful inter alia for treatment of inflammatory conditions.Type: ApplicationFiled: December 12, 2008Publication date: March 24, 2011Inventors: George Hynd, John Gary Montana, Harry Finch, Rosa Arienzo, Barbara A. Vitabile-Woo, Mathias Domostoj
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Publication number: 20110071150Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and R4 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with calcium release-activated calcium channels (CRAC).Type: ApplicationFiled: September 23, 2010Publication date: March 24, 2011Inventors: Muzaffar Alam, Daisy Joe Du Bois, Ronald Charles Hawley, Joshua Kennedy-Smith, Ana Elena Minatti, Wylie Solang Palmer, Tania Silva, Robert Stephen Wilhelm
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Publication number: 20110071195Abstract: The present invention provides compounds of formula (I), as well as pharmaceutical acceptable salt thereof, wherein R1 to R7 have the significance given herein. The compounds are useful in the treatment of prophylaxis of diseases that are related to AMPK regulation.Type: ApplicationFiled: September 14, 2010Publication date: March 24, 2011Inventors: Li Chen, Lichun Feng, Mengwei Huang, Jia Li, Fajung Nan, Tao Pang, Lifang Yu, Mei Zhang
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Publication number: 20110071146Abstract: To provide a novel and excellent method for treating and/or preventing prostatic cancer, benign prostatic hyperplasia, acne, seborrhea, hirsutism, baldness, alopecia, precocious puberty, adrenal hypertrophy, polycystic ovary syndrome, breast cancer, lung cancer, endometriosis, leiomyoma and the like based on selective inhibitory activity against 17?HSD type 5. It was found that an N-sulfonylindole derivative, where the indole ring is substituted by a carboxy group, a carboxy-substituted lower alkyl group or a carboxy-substituted lower alkenyl group at its carbon atom, has potent selective inhibitory activity against 17?HSD type 5 and may become a therapeutic agent and/or preventive agent for benign prostatic hyperplasia, prostatic cancer and the like without accompanying adverse drug reactions due to a decrease in testosterone, and the present invention has thus been completed.Type: ApplicationFiled: November 10, 2010Publication date: March 24, 2011Inventors: Tatsuya Niimi, Akio Kamikawa, Yasushi Amano, Tomohiko Yamaguchi, Kenichi Suzumura, Kentaro Enjo, Takashi Furutani, Akio Kakefuda, Yutaka Kondoh, Masaaki Hirano
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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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Publication number: 20110071141Abstract: Condensed-ring aryl compounds of formula (I) and use of the same as a agrochemical for controlling noxious organisms wherein (X)mQ, A, R1, (Y)n and the grouping —W1—W2—W3—W4— are as defined herein.Type: ApplicationFiled: March 13, 2009Publication date: March 24, 2011Inventors: Tetsuya Murata, Yasushi Yoneta, Jun Mihara, Kei Domon, Mamoru Hatazawa, Koichi Araki, Eiichi Shimojo, Katsuhiko Shibuya, Teruyuki Ichihara, Ulrich Görgens, Arnd Voerste, Angela Becker, Eva-Maria Franken, Klaus-Helmut Müller
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Publication number: 20110065661Abstract: This application relates to methods of identifying pharmacoperone agents that can restore function to a misfolded protein, such as a misfolded protein that causes disease. Also disclosed are methods of using such pharmacoperone agents to treat a disease or disorder that results from the misfolded protein.Type: ApplicationFiled: November 24, 2010Publication date: March 17, 2011Inventor: P. MICHAEL CONN
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Publication number: 20110064698Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.Type: ApplicationFiled: September 10, 2010Publication date: March 17, 2011Inventors: Yat Sun Or, Xiaowen Peng, Ce Wang, Lu Ying, Yao-Ling Qiu
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Publication number: 20110064735Abstract: Methods for predicting a response of a patient having a lymphoma to a therapy regimen of 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione using prognostic factors of a patient's disease burden, absolute lymphocyte count or time since last rituximab therapy are disclosed. Specific methods of treating a lymphoma encompass the administration of 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione to a patient who has one or more of the favorable profiles, alone or in combination with immunosuppressive agents such as rituximab.Type: ApplicationFiled: November 9, 2010Publication date: March 17, 2011Applicant: CELGENE CORPORATIONInventors: Dennis Pietronigro, Annette Ervin-Haynes, Jerome B. Zeldis
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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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Patent number: 7906509Abstract: This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-III: wherein, variables R, X, Y1, Y2, Y3, Y4, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formulae I-III and at least one carrier, diluent or excipient.Type: GrantFiled: December 11, 2009Date of Patent: March 15, 2011Assignee: Roche Palo Alto LLCInventors: Joshua Kennedy-Smith, Rama K. Kondru, Bradley E. Loe, Yan Lou, Joel McIntosh, Timothy D. Owens, Michael Soth, Zachary Kevin Sweeney, Joshua Paul Gergely Taygerly
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Publication number: 20110059992Abstract: This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.Type: ApplicationFiled: November 11, 2010Publication date: March 10, 2011Applicants: ASTRAZENECA AB, ASTEX THERAPEUTICS LTD.Inventors: James Arnold, Phil Edwards, Mark Sylvester, Stefan Berg, Jörg Holenz, Annika Kers, Karin Kolmodin, Laszlo Rakos, Liselotte Öhberg, Rotticci Didier, Gianni Chessari, Miles Congreve, Christopher Murray, Sahil Patel
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Publication number: 20110059965Abstract: Bicyclic derivatives having formula (I) and a composition thereof are useful as ion channel antagonists:Type: ApplicationFiled: July 6, 2010Publication date: March 10, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Aarti Sameer Kawatkar, Tara Whitney, Timothy D. Neubert, Nicole Hilgraf, Andreas P. Termin, Esther Martinborough
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Publication number: 20110060009Abstract: The present teachings relate to compounds of Formula I: and pharmaceutically acceptable salts, hydrates, esters, and prodrugs thereof, wherein R1, R2, R3, R4, R5, ring A, and Z are as defined herein. The present teachings also provide methods of preparing compounds of Formula I and methods of use compounds of Formula I in treating pathologic conditions or disorders mediated wholly or in part by deacetylases.Type: ApplicationFiled: August 27, 2010Publication date: March 10, 2011Inventors: Clinton A. BROOKS, Christine Hiu-Tung CHEN, Young Shin CHO, Lei JIANG, Gang LIU, Michael SHULTZ
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Publication number: 20110060010Abstract: The present invention provides a pharmaceutically acceptable strong acid salt of 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)piperidine-2,6-dione, a solvate thereof, a process for preparing the same and use in the preparation of a medicament for treating diseases or physiological abnormities by inhibiting inflammatory factors or angiogenesis. The water-solubility of the pharmaceutically acceptable strong acid salts of 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)piperidine-2,6-dione is quite higher than that of 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)piperidine-2,6-dione. The present invention also provides polymorphs of a pharmaceutically acceptable strong acid salt of 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)piperidine-2,6-dione and a solvate thereof.Type: ApplicationFiled: September 13, 2010Publication date: March 10, 2011Applicants: TIANJIN HEMAY BIO-TECH CO., LTD, TIANJIN MICHELE SCI-TECH DEVELOPMENT CO., LTDInventor: Hesheng Zhang
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Publication number: 20110053955Abstract: Heterocyclic compounds which are inhibitors of Mitrogen-Activated Protein Kinase-Activated Protein Kinase-2 (MAPKAP-K2) as described, in addition to their use in the treatment of cytokine mediated diseases.Type: ApplicationFiled: February 7, 2008Publication date: March 3, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Asitha Abeywardane, Denise Andersen, Tina Marie Morwick, Roger John Snow, Yancey David Ward
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Publication number: 20110052589Abstract: Ligands of CCX-CKR2 and the biological role of CCX-CKR2 in cancer is described.Type: ApplicationFiled: June 11, 2010Publication date: March 3, 2011Applicant: ChemoCentryx, Inc.Inventors: Jennifer M. Burns, Bretton Summers, Maureen C. Howard, Thomas J. Schall
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Publication number: 20110053937Abstract: The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, m, p, s, t, R1, R2, R3, R4, R5, R6, R7, X, Y, Q and Z have defined meanings.Type: ApplicationFiled: November 3, 2010Publication date: March 3, 2011Inventors: Jean Fernand Armand Lacrampe, Christophe Meyer, Yannick Aimé Eddy Ligny, Imre Christian Francis Csoka, Luc Van Hijfte, Janine Arts, Bruno Schoentjes, Camille Georges Wermuth, Bruno Giethlen, Jean-Marie Contreras, Muriel Joubert
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Publication number: 20110039880Abstract: Aryl substituted sulfonamide compounds of formula (I): wherein bond, X, Y, R1, R2, R3, m, and n are defined herein. Also disclosed is a method for treating cancer with these compounds.Type: ApplicationFiled: August 9, 2010Publication date: February 17, 2011Applicants: Taipei Medical University, DCB-USA LLCInventors: Jing-Ping Liou, Jang-Yang Chang
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Publication number: 20110039821Abstract: The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein: Ring A is (4-12)-membered heterocyclyl; Ring B is a fused benzene ring selected from the group consisting of: Ring A, ring B, ring C, R1, R1a, R2, R3, R4, L2, n, t, w, and z are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of glucokinase, the method comprising administering to a mammal an effective amount of a compound of formula (I).Type: ApplicationFiled: October 27, 2010Publication date: February 17, 2011Inventors: Hao Bai, Simon Bailey, Dilip Ramakant Bhumralkar, Feng C. Bi, Fengli Guo, Mingying He, Paul Stuart Humphries, Anthony Lai Ling, Jihong Lou, Seiji Nukui, Ru Zhou
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Publication number: 20110039855Abstract: The present invention provides a compound of the Formula (I), or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a compound of Formula (I) in combination with a suitable carrier, diluent, or excipient; and methods for treating or preventing physiological disorders, particularly reduced bone mass, osteoporosis, osteopenia, reduced muscle mass or strength, or erectile dysfunction comprising administering a compound of Formula (I), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 14, 2009Publication date: February 17, 2011Applicant: ELI LILLY AND COMPANYInventors: Prabhakar Kondaji Jadhav, Venkatesh Krishnan, Euibong Jemes Kim
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Patent number: 7888351Abstract: The present invention relates to compounds of the formula; and their use in therapy.Type: GrantFiled: April 10, 2007Date of Patent: February 15, 2011Assignee: Novartis AGInventors: Daniel Kaspar Baeschlin, Garry Fenton, Kenji Namoto, Nils Ostermann, Richard Sedrani, Finton Sirockin
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Patent number: 7888364Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.Type: GrantFiled: September 2, 2005Date of Patent: February 15, 2011Assignee: Curis, Inc.Inventors: Janet L. Gunzner, Daniel Sutherlin, Mark S. Stanley, Liang Bao, Georgette M. Castanedo, Rebecca L. Lalonde, Shumei Wang, Mark E. Reynolds, Scott J. Savage, Kimberly Malesky, Michael S. Dina
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Patent number: 7888336Abstract: The invention provides well-defined aryl and/or heteroaryl substituted indoles that are useful as spingosine-1-phosphate agonists or antagonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.Type: GrantFiled: September 18, 2008Date of Patent: February 15, 2011Assignee: Allergan, Inc.Inventors: Richard L. Beard, Haiqing Yuan, John E. Donello
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Publication number: 20110033393Abstract: The present invention relates to hydrazone compounds of Formula I: and pharmaceutically acceptable salts and stereoisomers thereof, wherein R1, R2, R3, R4, L1, and L2 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I as inhibitors of TRPM5 protein.Type: ApplicationFiled: May 12, 2010Publication date: February 10, 2011Inventors: Philip STEIN, Robert DAINES, Dennis SPROUS, Harold O'GRADY
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Publication number: 20110034514Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of 5-lipoxygenase-activating protein (FLAP). Also described herein are methods of using such FLAP modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions or diseases.Type: ApplicationFiled: October 18, 2010Publication date: February 10, 2011Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: John Howard Hutchinson, Nicholas Simon Stock, Jeffrey Roger Roppe
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Publication number: 20110034507Abstract: The present invention relates to farnesoid X receptors (FXR, NR1H4). FXR is a member of the nuclear receptor class of ligand-activate transcription factors. More particularly, the present invention relates to compounds useful as agonists for FXR, pharmaceutical formulations comprising such compounds, and therapeutic use of the same. Novel isoxazole compounds are disclosed as part of pharmaceutical compositions for the treatment of a condition mediated by decreased FXR activity, such as obesity, diabetes, cholestatic liver disease, liver fibrosis, and metabolic syndrome.Type: ApplicationFiled: June 13, 2008Publication date: February 10, 2011Applicant: SMITHKLINE BEECHAM CORPORATIONInventors: Adwoa Akwabi-Ameyaw, David Norman Deaton, Robert Blount McFadyen, Frank Navas, III
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Publication number: 20110034515Abstract: This invention relates to modulation of the ?7 nicotinic acetylcholine receptor (nAChR) by a compound of formula (I) or a salt thereofType: ApplicationFiled: April 16, 2009Publication date: February 10, 2011Inventors: Kevin Dinnell, Andrew P. Lightfoot, Howard Robert Marshall
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Publication number: 20110033417Abstract: The present invention relates to 2,3-Substituted Indole Derivatives, compositions comprising at least one 2,3-Substituted Indole Derivative, and methods of using the 2,3-Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: August 27, 2008Publication date: February 10, 2011Inventors: Gopinadhan N. Anilkumar, 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, Stephen J. Gavalas, Yueheng Jiang, Patrick A. Pinto, Haiyan Pu, Oleg B. Selyutin, Bancha Vibulbhan, Li Wang, Wanli Wu, Weiying Yang, Yuhua Huang, Hsueh-Cheng Huang, Robert Palermo, Boris Feld
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Publication number: 20110028468Abstract: This invention provides a compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein R1 is substituted or unsubstituted alkyl or the like, R2 is hydrogen or substituted or unsubstituted alkyl, Ring A is monocyclic or bicyclic aromatic heterocycle, R3 is substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or substituted or unsubstituted heterocycle, R4 is halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl or the like, m is an integer between 0 and 2, n is an integer between 0 and 5, R is halogen, oxo, cyano, nitro, substituted or unsubstituted alkyl or the like, and p is an integer between 0 and 2 as novel compounds having NPY Y5 antagonistic activity.Type: ApplicationFiled: April 20, 2009Publication date: February 3, 2011Applicant: Shinonogi & Co., LtdInventors: Masahiro Sakagami, Hiroshi Hashizume, Satoru Tanaka, Takayuki Okuno, Hiroshi Yari, Keisuke Tonogaki, Naoki Kouyama
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Publication number: 20110028486Abstract: The present invention relates to modulation of the ?7 nicotinic acetylcholine receptor (nAChR) by a compound of List A or a salt thereof, which may be represented, but is not limited to the compound N-[(2-Trifluoromethyl-1H-indol-5-yl)methyl]-5-(trifluoromethyl)-2-pyrimidinecarboxamide.Type: ApplicationFiled: April 16, 2009Publication date: February 3, 2011Inventors: Kevin Dinnell, Andrew P. Lightfoot, Howard Robert Marshall
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Publication number: 20110028455Abstract: Disclosed are compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein X is —O—, —N(R3)—, —S—, —S(O)— or —S(O)2—; R2 is a C1-4 alkyl group or —CF3; and R1, R3, R4 and p are as defined herein; wherein the compounds are useful as kinase inhibitors. Also disclosed are pharmaceutical compositions containing, and intermediate compounds and methods for making the compounds of formula (I) and their pharmaceutically acceptable salts; and methods of using the foregoing to treat inflammatory and autoimmune diseases such as asthma, colitis, multiple sclerosis, psoriasis, arthritis, rheumatoid arthritis, inflammatory bowel disease, and joint inflammation.Type: ApplicationFiled: December 12, 2008Publication date: February 3, 2011Applicant: Wyeth LLCInventors: Diane Harris Boschelli, Yanong Daniel Wang, Amarnauth Shastrie Prashad, Zhong Li, Chuansheng Niu
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Publication number: 20110028463Abstract: [Problems] To provide a compound that is useful as an agent for treating chronic renal insufficiency or an agent for treating diabetic nephropathy. [Means for Solving Problems] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic action, and as a result, they have found that various amide derivatives having a carboxylic group or an equivalent thereof exhibit an excellent EP4 receptor antagonistic action, thereby completing the present invention. Since the compound of the present invention has an excellent EP4 receptor antagonistic action, it is useful as an agent for preventing and/or treating chronic renal insufficiency or diabetic nephropathy.Type: ApplicationFiled: July 2, 2008Publication date: February 3, 2011Applicant: Astellas Pharma Inc.Inventors: Eisuke Nozawa, Ryotaro Ibuka, Kazuhiro Ikegai, Keisuke Matsuura, Tatsuya Zenkoh, Ryushi Seo
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Publication number: 20110028519Abstract: Compounds of Formula I are described along with pharmaceutical formulations thereof, and methods of treating disorders such as diabetes and neurodegenerative diseases with such compounds.Type: ApplicationFiled: October 11, 2010Publication date: February 3, 2011Inventor: Michael C. Pirrung
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Patent number: 7879839Abstract: The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.Type: GrantFiled: July 27, 2005Date of Patent: February 1, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Christopher J. Dinsmore, Jeffrey M. Bergman, Douglas C. Beshore, B. Wesley Trotter, Kausik K. Nanda, Richard Isaacs, Linda S. Payne, Lou Anne Neilson, Zhicai Wu, Mark T. Bilodeau, Peter J. Manley, Adrienne E. Balitza
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Patent number: 7879851Abstract: An enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein, or a salt or ester thereof, as an inhibitor of HCV NS5B polymerase.Type: GrantFiled: February 17, 2009Date of Patent: February 1, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Youla S. Tsantrizos, Catherine Chabot, Pierre Beaulieu, Christian Brochu, Martin Poirier, Timothy A. Stammers, Bounkham Thavonekham, Jean Rancourt
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Publication number: 20110021572Abstract: The present invention relates to hydroximoyl-tetrazole derivatives, their process of preparation, preparation intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: ApplicationFiled: March 18, 2009Publication date: January 27, 2011Inventors: Christian Beier, Jurgen Benting, Isabelle Christian, Pierre-Yves Coqueron, Christophe Dubost, Pierre Genix, Benoit Hartmann, Daniela Portz, Arnd Voerste, Ulrike Wachendorff-Neumann
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Publication number: 20110021498Abstract: Compounds of formula (I) have checkpoint kinase 1 (CHK1) inhibitory activity: wherein R1, R2, R5 and R6 are independently selected from hydrogen, hydroxy, methyl, trifluoromethyl, hydroxymethyl, methoxy, trifluoromethoxy, methylamino and dimethylamino; R3, and R4 are independently selected from hydrogen, hydroxy, C1-C3 alkyl, fluoro-(C1-C3)-alkyl, hydroxy-(C1C3)-alkyl, C1-C3 alkoxy, fluoro-(C1-C3)-alkoxy, hydroxy-(C1-C3)-alkoxy, -AIk-N(R11)—R12, -0-AIk-N(R11)—R12, —C(?O)OH, carboxy-(C1-C3)-alkyl, or —C(?O)—NH—R13; AIk is a straight or branched chain divalent C1-C6 alkylene radical; R7 and R8 are independently selected from hydrogen, hydroxy, or C1-C3 alkoxy; X is a straight chain divalent C1-C3 alkylene radical, optionally substituted on one or more carbons by R9 and/or R10; W is selected from —C(?O)—N(—R16)— or —N(—R17)—C(?O)—; Y is hydrogen, C1-C3 alkyl, C1-C3 alkoxy, or halo; and Q is selected from optionally substituted phenyl, optionally substituted cyclohexyl, or an optionally substituted 6-membered monType: ApplicationFiled: January 20, 2009Publication date: January 27, 2011Applicant: VERNALIS (R & D) LTDInventors: Stephen Stokes, Nicolas Foloppe, Andrea Fiumana, Martin Drysdale, Simon Bedford, Paul Webb
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Publication number: 20110021556Abstract: The invention relates to 3,3 disubstituted pyrrole derivatives useful for treatment of diseases associated with monoamine reuptake inhibitors. Also provided pharmaceutical compositions, methods of using, and methods of preparing the compounds.Type: ApplicationFiled: March 10, 2009Publication date: January 27, 2011Applicant: Hoffman-La Roche, Inc.Inventors: Matthew C. Lucas, Ryan Craig Schoenfeld, Robert James Weikert
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Publication number: 20110015217Abstract: This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protecting from neuron cell death.Type: ApplicationFiled: January 11, 2010Publication date: January 20, 2011Inventors: STEVEN L. MCKNIGHT, ANDREW A. PIEPER, JOSEPH M. READY, JEF K. DE BRABANDER
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Publication number: 20110015235Abstract: This invention relates to novel phenylethynyl derivatives of 8-aza-bicyclo[3.2.1]octane useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: ApplicationFiled: February 4, 2009Publication date: January 20, 2011Inventors: Dan Peters, John Paul Redrobe, Elsebet Østergaard Nielsen
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Publication number: 20110015232Abstract: The present invention relates to novel IAP inhibitor compounds of: Formula (I).Type: ApplicationFiled: October 10, 2007Publication date: January 20, 2011Inventors: Mark G. Charest, Christine Hiu-Tung CHEN, Ming Chen, Zhuoliang Chen, Miao Dai, Feng He, Huangshu Lei, Christopher Straub, Run-Ming David Wang, Leigh Zawel
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Publication number: 20110009379Abstract: [Problems] A compound, which is useful as an active ingredient for a pharmaceutical composition, for example a pharmaceutical composition for treating constipation-type irritable bowel syndrome, atonic constipation and/or functional gastrointestinal disorder, is provided. [Means for Solution] The present inventors have extensively studied compounds having TRPA1 channel activation activity, and confirmed that an indolinone compound has a TRPA1 channel activation activity, and thus completed the present invention. The indolinone compound of the present invention has a TRPA1 channel activation activity and can be used as an active ingredient of a pharmaceutical composition for preventing and/or treating constipation-type irritable bowel syndrome, atonic constipation and/or functional gastrointestinal disorder or the like.Type: ApplicationFiled: March 30, 2009Publication date: January 13, 2011Applicant: ASTELLAS PHARMA INC.Inventors: Hidetaka Kaku, Tomofumi Takuwa, Michihito Kageyama, Katsura Nozawa, Hitoshi Doihara
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Publication number: 20110009447Abstract: Substituted benzoic acid amides of formula (I) and their use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis as well as their intermediate products for the production of benzoic acid amides are described.Type: ApplicationFiled: April 24, 2001Publication date: January 13, 2011Inventors: Andreas Huth, Dieter Seidelmann, Karl-Heinz Thierauch
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Publication number: 20110009428Abstract: The compounds of the subject invention have a structure according to formula I: wherein X is S or SO2; R1 is (1C-6C)alkyl, (3C-6C)alkenyl, or (3C-6C)alkynyl, each optionally substituted with (3C-6C)cycloalkyl, OH, OC(O)(1C-4C)alkyl, (1C-4C)alkoxy, halogen, cyano, formyl, C(O)(1C-4C)alkyl, CO2H, CO2(1C-4C)alkyl, C(O)NR5R6, S(O)(1C-4C)alkyl or S(O)2(1C-4C)alkyl; R2 is hydrogen, (1C-4C)alkyl or C(O)(1C-4C)alkyl; R3 is a phenyl group optionally substituted with (1C-4C)alkyl, (1C-4C)fluoroalkyl, (1C-4C)alkoxy, (1C-4C)fluoroalkoxy, halogen, cyano or nitro; or R3 is a 5- or 6-membered aromatic heterocyclic ring structure optionally substituted with (1C-4C)alkyl, (1C-4C)fluoroalkyl, (1C-4C)alkoxy, halogen or cyano; R4 is a phenyl group or an aromatic 6-membered heterocycle, substituted at the ortho position with 1-hydroxy(1C-4C)alkyl, (1C-4C)alkoxy, C(O)(1C-4C)alkyl, CO2(1C-4C)alkyl, C(O)NH2, cyano, nitro, or CH?NOR7, and optionally further substituted with (1C-2C)alkyl, (1C-2C)fluoroalkyl or halogen; or R4Type: ApplicationFiled: September 22, 2010Publication date: January 13, 2011Applicant: N.V. OrganonInventors: Jaap Van Der Louw, Neeltje Miranda Teerhuis, Johannes Petrus Maria Lommerse, Herman Thijs Stock, Pedro Harold Han Hermkens
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Publication number: 20110009456Abstract: Methods of using di, tri, and tetracyclic acylhydrazide derivatives and analogs, as well as pharmaceutical compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus.Type: ApplicationFiled: December 21, 2009Publication date: January 13, 2011Applicant: Siga Technologies Inc.Inventors: Robert Jordan, Thomas R. Bailey, Susan R. Rippin
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Publication number: 20110009453Abstract: Disclosed herein are compositions and methods for treating inflammation using S1 P3 receptor inhibitors.Type: ApplicationFiled: March 16, 2009Publication date: January 13, 2011Inventors: John E. Donello, Mohammed I. Dibas
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Patent number: 7868024Abstract: The invention relates to compounds of formula (I): Wherein X1, X2, X3, X4, Y and W are as described herein. The invention also relates to a preparation method and to a therapeutic application.Type: GrantFiled: July 17, 2009Date of Patent: January 11, 2011Assignee: Sanofi-AventisInventors: Laurent Dubois, Yannick Evanno, André Malanda, Christian Maloizel
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Patent number: 7868008Abstract: The present invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined for formula I in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.Type: GrantFiled: February 15, 2006Date of Patent: January 11, 2011Assignee: AstraZeneca ABInventors: Bradford Van Wagenen, Radhakrishnan Ukkiramapandian, Joshua Clayton, Ian Egle, James Empfield, Methvin Isaac, Fupeng Ma, Abdelmalik Slassi, Gary Steelman, Rebecca Urbanek, Sally Walsh