Plural Ring Hetero Atoms In The Additional Hetero Ring Patents (Class 514/217.05)
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Patent number: 8058045Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain biarylamine compounds (referred to herein as BAA compounds), and especially certain pyrazin-2-yl-pyridin-2-yl-amine and pyrazine-2-yl-pyrimidin-4-yl-amine compounds of formula (I), which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc.Type: GrantFiled: October 6, 2008Date of Patent: November 15, 2011Assignee: Cancer Research Technology LimitedInventors: Ian Collins, John Charles Reader, Thomas Peter Matthews, Kwai Ming Cheung, Nicolas Proisy, David Hugh Williams, Sukhbinder Singh Klair, Jane Elizabeth Scanlon, Nelly Piton, Glynn Jonathan Addison, Michael Cherry
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Publication number: 20110251179Abstract: Compounds which are 4,7-disubstituted derivatives of 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one compounds, or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.Type: ApplicationFiled: September 17, 2009Publication date: October 13, 2011Applicant: NERVIANO MEDICAL SCIENCES S.r.lInventors: Danilo Mirizzi, Giovanni Cervi, Matteo D'Anello, Gianluca Mariano Enrico Papeo, Ron Ferguson, Francesco Casuscelli
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Publication number: 20110237570Abstract: The present invention provides substituted imidazo[1,2-b]pyridazine derivatives, pharmaceutically acceptable salts thereof, and tautomers of any of the foregoing, where such compounds inhibit ?-site amyloid precursor protein-cleaving enzyme (BACE), which may be useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease. The invention also provides pharmaceutical compositions comprising any of these compounds and the use of any of these compounds and compositions in the treatment of diseases, disorders, or conditions in which BACE is involved.Type: ApplicationFiled: March 21, 2011Publication date: September 29, 2011Applicant: HIGH POINT PHARMACEUTICALS, LLCInventors: Adnan M.M. Mjalli, Anitha Hari, Bapu Gaddam, Devi Reddy Gohimukkula, Dharma Rao Polisetti, Mohan Rao, Raju Bore Gowda, Robert Carl Andrews, Rongyuan Xie, Soumya P. Sahoo, Tan Ren, William Kenneth Banner
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Publication number: 20110224189Abstract: The present invention provides compounds of the formula: its enantiomers, diastereomers, racemic mixtures thereof, prodrugs, crystalline forms, non-crystalline forms, amorphous forms thereof, solvates thereof, metabolites thereof, and pharmaceutically acceptable salts, wherein the ring A substituent groups are fully defined in the following disclosure. The compounds of formula are inhibitors of metalloproteases such as matrix metalloproteases and sheddases, and are useful in treating diseases such as rheumatoid arthritis, psoriasis, neoplastic diseases, allergies and all those diseases wherein inhibition of MMPs is desirable.Type: ApplicationFiled: May 19, 2011Publication date: September 15, 2011Inventors: Yun-Long Li, Jincong Zhuo, David Burns, Wenqing Yao, Ravi Kumar Jalluri
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Publication number: 20110218188Abstract: The present invention relates to phenyl-pyrimidinyl-amino derivatives of formula (I) wherein Q1 and p, Ra to Rc, L1, Y, L2 and Q2 represent various substituents, 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: November 12, 2009Publication date: September 8, 2011Inventors: Christian Beier, Jurgen Benting, Isabelle Christian, Pierre-Yves Coqueron, Peter Dahmen, Ralf Dunkel, Jorg Greul, Marie-Claire Grosjean-Cournoyer, Hiroyuki Hadano, Philippe Rinolfi, Arnd Voerste, Jean-Pierre Vors, Ulrike Wachendorff-Neumann
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Patent number: 8003127Abstract: Compositions comprising a nanoparticulate corticosteroid and an antihistamine are described. The compositions are useful in the prophylaxis and chronic treatment of asthma in adults and pediatric patients and for the relief of allergic conjunctivitis, symptoms of seasonal allergic rhinitis in adults and pediatric patients. Combining an antihistamine with a nanoparticulate corticosteroid in a single formulation results in improved efficacy.Type: GrantFiled: March 23, 2006Date of Patent: August 23, 2011Assignee: Elan Pharma International LimitedInventors: Gary Liversidge, Scott Jenkins, H. William Bosch, Christian F. Wertz
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Patent number: 7998951Abstract: The invention encompasses compounds of Formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.Type: GrantFiled: March 3, 2008Date of Patent: August 16, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Kap-Sun Yeung, John F. Kadow
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Publication number: 20110178062Abstract: Certain substituted indole and benzothiophene compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.Type: ApplicationFiled: February 28, 2008Publication date: July 21, 2011Inventors: Brett D. Allison, Cheryl A. Grice, Kelly J. McClure, Alejandro Santillan, JR.
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Publication number: 20110160187Abstract: The present invention provides compounds of Formula (I) or (II) salt form or prodrug thereof, wherein variables are defined herein, that are modulators of metalloproteases such as matrix metalloproteases (MMPs) and ADAMs. The compounds or compositions described herein can be used to treat diseases associated with metalloprotease activity including, for example, arthritis, cancer, cardiovascular disorders, skin disorders, inflammation or allergic conditions.Type: ApplicationFiled: May 6, 2005Publication date: June 30, 2011Applicant: Neurogen CorporationInventors: Taeyoung Yoon, Jun Yuan, Kyungae Lee, George D. Maynard, Nian Liu
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Publication number: 20110152238Abstract: Diazapolycyclic compounds having affinity for the opioidergic receptors, preferably for the delta opioidergic receptors, with central and/or peripheral activity, having formula: A1-D1-T1??(I) wherein: A1 is a group of formula (II): wherein: R1 is phenyl wherein one of the ring hydrogen atoms is substituted with a group selected from C(O)R?, C(O)OR?, C(O)NHR? or C(O)NR3R4, R?, R3 and R4, being as defined in the application; R2 is phenyl, optionally substituted D1 is a diazapolycyclic group T1 is a group selected from H, alkyl, alkenyl, alkynyl and from the following optionally substituted groups: cycloalkyl, heterocycloalkyl, aryl, heteroaryl, cycloalkylalkyl, heterocycloalkylalkyl, arylalkyl or heteroarylalkyl, and their hydrates and solvates and pharmaceutically acceptable salts.Type: ApplicationFiled: December 13, 2010Publication date: June 23, 2011Applicant: NEUROSCIENZE PHARMANESS S.C. A.R.L.Inventors: Paolo LAZZARI, Giovanni Loriga, Stefania Ruiu, Gabrieie Murineddu, Luca Pani, Gerard Aime Pinna
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Publication number: 20110144084Abstract: The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, their synthesis, and their use as CHK-1 inhibitors.Type: ApplicationFiled: August 4, 2009Publication date: June 16, 2011Applicant: PFIZER INCInventors: John Frederick Braganza, Michael Raymond Collins, John Charles Kath, Sacha Ninkovic, Hui Li, Daniel Tyler Richter
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Publication number: 20110130386Abstract: A compound of formula (I) wherein: R1 and R2 are independently selected from hydrogen, an optionally substituted C1-7 alkyl group, C3-20 heterocyclyl group, or C5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; and RN1 and RN2 are selected from hydrogen, an optionally substituted C1-7 alkyl group, C3-20 heterocyclyl group, or C5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms.Type: ApplicationFiled: April 24, 2009Publication date: June 2, 2011Inventors: Mark Frigerio, Heather Mary Ellen Duggan, Marc Geoffrey Hummersone, Keith Allan Menear, Niall Morrison Barr Martin, Celine Cano, Roger John Griffin, Bernard Thomas Golding, Ian Robert Hardcastle
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Publication number: 20110112061Abstract: The present invention relates to a class of pyridazinones of formula I, which comprises 6-[3-(trifluoromethyl)phenyl]pyridazin-3(2H)-one as a mother nucleus, the preparation method thereof and the use thereof in manufacturing medicaments against tumors, especially liver cancer.Type: ApplicationFiled: March 18, 2009Publication date: May 12, 2011Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCESInventors: Youhong Hu, Liguang Lou, Shijun Lin, Hongbing Zhao, Zhende Liu, Yongping Xu, Bo Chao
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Publication number: 20110112075Abstract: The present invention relates to compounds of the formula I, wherein R1; R2; R3; R4; R5, R13, R16, X and M have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and thrombin and can in general be applied in conditions in which an undesired activity of factor Xa and/or thrombin are present or for the cure or prevention of which an inhibition of factor Xa and thrombin are intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: ApplicationFiled: August 18, 2010Publication date: May 12, 2011Applicant: SANOFI-AVENTISInventors: Markus FOLLMANN, Volkmar WEHNER, Jerome MENEYROL, Jean-Michel ALTENBURGER, Frédéric PETIT, Gilbert LASSALLE, Jean-Pascal HERAULT
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Publication number: 20110112074Abstract: The present invention relates to compounds of the formula I, wherein R1; R2; R3; R4; R5, R16, X and M have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa and thrombin and can in general be applied in conditions in which an undesired activity of factor Xa and/or thrombin are present or for the cure or prevention of which an inhibition of factor Xa and thrombin are intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: ApplicationFiled: August 18, 2010Publication date: May 12, 2011Applicant: SANOFI-AVENTISInventors: Markus FOLLMANN, Volkmar WEHNER, Jean-Michel ALTENBURGER, Gilbert LASSALLE, Jean-Pascal HERAULT
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Publication number: 20110098271Abstract: The invention concerns chromenone derivatives of Formula I or a pharmaceutically-acceptable salts thereof, wherein each of R1, R2, R3, R4, R5, R6, R7, R8, n and R9 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.Type: ApplicationFiled: October 22, 2010Publication date: April 28, 2011Applicant: ASTRAZENECA ABInventors: Bernard Christophe BARLAAM, Sebastien Louis DEGORCE, Christine Marie Paul LAMBERT-VAN DER BREMPT, Remy Robert MORGENTIN, Patrick PLE
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Publication number: 20110092481Abstract: The present invention is related to novel compounds of formula (I) having P2X7 antagonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment or prophylaxis of diseases associated with P2X7 receptor activity in animals, in particular humans.Type: ApplicationFiled: April 21, 2009Publication date: April 21, 2011Inventors: Christopher John Love, Joseph Elisabeth Leenaerts, Ludwig Paul Cooymans, Donald Alec Labsack, Bryan James Branstetter, Jason Christopher Rech, Elizabeth Ann Gleason, Jennifer Diane Venable, Danielle Wiener, Deborah Margaret Smith, James Guy Breitenbucher
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Publication number: 20110065684Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, L1, L2, X, Y, Q and Z have defined meanings.Type: ApplicationFiled: August 13, 2010Publication date: March 17, 2011Inventors: Laurence Anne Mevellec, Ludo E.J. Kennis, Josephus Carolus Mertens, Jacobus A.J. Van Dun, Maria V.F. Somers, Walter B.L. Wouters
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Patent number: 7906505Abstract: Compounds which inhibit the activity of anti-apoptotic family protein members, compositions containing the compounds and methods of treating diseases during which occur expression one or more than one of an anti-apoptotic family protein member are disclosed.Type: GrantFiled: May 3, 2010Date of Patent: March 15, 2011Assignee: Abbott LaboratoriesInventors: Milan Bruncko, Hong Ding, Steven W. Elmore, Aaron R. Kunzer, Christopher L. Lynch, William J. McClellan, Cheol Min Park, Xiahong Song, Xilu Wang
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Publication number: 20110059118Abstract: The present invention relates to the use of novel compounds of Formula I, wherein the variables m, n, p, q, Q, r, R, R?, X, X?, Y, Z1, Z2, and Z3 are defined as described herein, which inhibit JAK and are useful for the treatment of auto-immune and inflammatory diseases.Type: ApplicationFiled: September 9, 2010Publication date: March 10, 2011Inventors: Javier de Vicente Fidalgo, Johannes Cornelius Hermann, Remy Lemoine, Hongju Li, Allen John Lovey, Eric Brian Sjogren, Michael Soth
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Publication number: 20110027397Abstract: Disclosed are compositions that inhibit brain blood vessel leakage, compositions for treating autism spectrum disorders, methods of treating autism spectrum disorders, and methods of screening for an autism spectrum disorder.Type: ApplicationFiled: August 3, 2009Publication date: February 3, 2011Inventor: Theoharis C. THEOHARIDES
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Patent number: 7879832Abstract: The present invention relates to a combination of ciclesonide with antihistamines.Type: GrantFiled: August 29, 2003Date of Patent: February 1, 2011Assignee: Nycomed GmbHInventors: Degenhard Marx, Helgert Müller
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Publication number: 20110014127Abstract: Described herein are methods for effectively and accurately measuring a patient response upon administration of one or more drugs to the patient. The methods are more sensitive than current methodologies. Also described herein are compositions comprising an analgesic and a sufficient amount of an antihistamine to enhance the analgesic properties of the analgesic. With respect to these compositions, the methods described herein are useful for evaluating qualities of pain, definite improvement, and one or more bodily functions of a subject afflicted with pain. The compositions described herein are useful in improving the quality of pain in a subject or a bodily function of a subject afflicted with pain or definite improvement of a subject afflicted with pain.Type: ApplicationFiled: January 5, 2009Publication date: January 20, 2011Inventor: Bernard P. Schachtel
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Publication number: 20100323994Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I imidazopyridazines inhibit protein kinase activity thereby making them useful as anticancer agents.Type: ApplicationFiled: February 6, 2009Publication date: December 23, 2010Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Brian E. Fink, Soong-Hoon Kim, Yufen Zhao, Ping Chen, Wayne Vaccaro, Litai Zhang, Ashvinikumar V. Gaval, Dharmpal S. Dodd, Libing Chen
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Publication number: 20100311730Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain biarylamine compounds (referred to herein as BAA compounds), and especially certain pyrazin-2-yl-pyridin-2-yl-amine and pyrazine-2-yl-pyrimidin-4-yl-amine compounds of formula (I), which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionisi?q radiation.Type: ApplicationFiled: October 6, 2008Publication date: December 9, 2010Applicant: CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Ian Collins, John Charles Reader, Thomas Peter Matthews, Kwai Ming Cheung, Nicolas Proisy, David Hugh Williams, Sukhbinder Singh Klair, Jane Elizabeth Scanlon, Nelly Piton, Glynn Jonathan Addison, Michael Cherry
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Publication number: 20100311729Abstract: The present invention relates to compounds are of the formula I, processes for the preparation thereof, more generally these compounds for use in the treatment of the human or animal body, in the treatment of an inflammatory or obstructive airway disease, disorders commonly occurring in connection with transplantation, or a proliferative disease, which disease responds to an inhibition of kinases of the PI3-kinase-related protein kinase family.Type: ApplicationFiled: May 9, 2008Publication date: December 9, 2010Inventors: Hans-Georg Capraro, Patricia Imbach, Giorgio Caravatti, Pascal Furet, Jiong Lan, Sabrina Pecchi, Joseph Schoepfer
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Publication number: 20100286114Abstract: Heterocyclic compounds that modulate the hedgehog signaling pathway, pharmaceutical composition thereof and their therapeutic applications.Type: ApplicationFiled: December 10, 2008Publication date: November 11, 2010Applicant: SIENA BIOTECH S.P.A.Inventors: Russell John Thomas, Gal.la Pericot Mohr, Giacomo Minetto, Annette Cornelia Bakker, Pietro Ferruzzi
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Patent number: 7829560Abstract: 1,4 disubstituted napthylenes, of formula (I), are disclosed. These compounds may be useful in treating cell-proliferative diseases.Type: GrantFiled: July 8, 2005Date of Patent: November 9, 2010Assignee: Arqule, Inc.Inventors: Mark A. Ashwell, Yanbin Liu, Syed Ali, Jason Hill, Woj Wrona
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Publication number: 20100280007Abstract: The present invention is directed to novel pyridizinone derivatives that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of the histamine H3 receptor, including, for example, neurodegenerative disorders, sleep/wake disorders, attention deficit hyperactivity disorder and cognition.Type: ApplicationFiled: June 15, 2010Publication date: November 4, 2010Applicant: CEPHALON, INC.Inventors: Edward R. Bacon, Thomas R. Bailey, Nadine C. Becknell, Sankar Chatterjee, Derek Dunn, Greg A. Hostetler, Robert L. Hudkins, Kurt A. Josef, Lars J.S. Knutsen, Ming Tao, Allison L. Zulli
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Publication number: 20100280008Abstract: The present invention relates to chemical compounds having a general formula I wherein A1-8, D?, L1, L2, R1, R6-8 and n are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of such kinases. For example, the compounds are capable of modulating Aurora kinase thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of Aurora kinase.Type: ApplicationFiled: June 30, 2010Publication date: November 4, 2010Applicant: Amgen Inc.Inventors: Holly Deak, Stephanie Geuns-Meyer, Brian L. Hodous, Zihao Hua, Matthew Martin, Hanh Nho Nguyen, Philip Olivieri, Kathleen Panter, Karina Romero, Laurie Schenkel, Ryan White
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Publication number: 20100273779Abstract: The present invention is directed to novel pyridizinone derivatives that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of the histamine H3 receptor, including, for example, neurodegenerative disorders, sleep/wake disorders, attention deficit hyperactivity disorder and cognition.Type: ApplicationFiled: June 15, 2010Publication date: October 28, 2010Applicant: CEPHALON, INC.Inventors: Edward R. Bacon, Thomas R. Bailey, Nadine C. Becknell, Sankar Chatterjee, Derek Dunn, Greg A. Hostetler, Robert L. Hudkins, Kurt A. Josef, Lars J.S. Knutsen, Ming Tao, Allison L. Zulli
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Publication number: 20100256117Abstract: Methods are provided for treating fibrotic connective tissue diseases such as scleroderma and conditions such as surgically-induced adhesions using compounds that activate the signaling pathways of hepatocyte growth factor.Type: ApplicationFiled: November 13, 2008Publication date: October 7, 2010Inventor: Latha Paka
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Publication number: 20100249030Abstract: The present invention relates to a method of treating cancer by pretreatment with anti-mitotic agents followed by at least one aurora kinase inhibitor. Extensive illustrations are provided for the antimitotic agents and aurora kinase inhibitors that are useful in the inventive treatment.Type: ApplicationFiled: July 28, 2008Publication date: September 30, 2010Inventor: Andrea Dawn Basso-Porcaro
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Patent number: 7803795Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2 L1, L2, X, Y, Q and Z have defined meanings.Type: GrantFiled: June 28, 2005Date of Patent: September 28, 2010Assignee: Janssen Pharmaceutica N.V.Inventors: Laurence Anne Mevellec, Ludo Edmond Josephine Kennis, Josephus Carolus Mertens, Jacobus Alphonsus Josephus Van Dun, Maria Victorina Francisca Somers, Walter Boudewijn Leopold Wouters
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Publication number: 20100216777Abstract: Methods for using aminopyrazine analogs to treat rho kinase-mediated diseases or rho kinase-mediated conditions, including controlling intraocular pressure and treating glaucoma, are disclosed. Ophthalmic pharmaceutical compositions useful in the treatment of eye diseases such as glaucoma, and additionally useful for controlling intraocular pressure, the compositions comprising an effective amount of aminopyrazine analogs, are also disclosed.Type: ApplicationFiled: May 5, 2010Publication date: August 26, 2010Applicant: ALCON, INC.Inventors: Mark R. Hellberg, Andrew Rusinko, Alan J. Henderson, Cheng Guo, Mark Hadden, Hélène Y. Decornez
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Publication number: 20100210627Abstract: The invention provides compounds according to formula (I) their use and methods for preparation wherein A, X, Y, R1, R2 and R3 are defined herein. The compounds of the invention inhibit specific serine/threonine kinases involved in inflammatory processes and aberrant cell proliferation, and are thus useful for treating associated diseases and pathological conditions such as Pim kinase-mediated diseases and pathological conditions involving inflammation, including Chron's disease, inflammatory bowel disease, rheumatoid arthritis, and chronic inflammatory disease, or aberrant cell proliferation including various cancers.Type: ApplicationFiled: August 15, 2007Publication date: August 19, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Wang Mao, Tina Marie Morwick, Anthony S. Prokopowicz, III
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Publication number: 20100210628Abstract: The invention is directed to novel sEH inhibitors and their use in the treatment of diseases mediated by the sEH enzyme. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, R3, R5a, R6a A, B, Y, x, and m are defined below, and to pharmaceutically-acceptable salts thereof. The compounds of the invention are sEH inhibitors and can be used in the treatment of diseases mediated by the sEH enzyme, such as hypertension. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting sEH and treatment of conditions associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: ApplicationFiled: October 10, 2008Publication date: August 19, 2010Inventors: Yun Ding, Reema K. Thalji, Joseph P. Marino, JR.
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Publication number: 20100204209Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.Type: ApplicationFiled: May 29, 2008Publication date: August 12, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Heiner Ebel, Stefan Peters, Silke Hobbie
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Patent number: 7772432Abstract: The invention concerns amide derivatives of the Formula (I) wherein R3 is (1-6C)alkyl or halogeno; Q is aryl or heteroaryl which optionally bears 1, 2, 3 or 4 substituents such as hydroxy, halogeno, trifluoromethyl, cyano, (1-6C)alkyl, (1-6C)alkoxy, halogeno-(1-6C)alkyl, hydroxyl-(1-6C)alkyl, di-[(1-6C)akly]amino-(1-6C)alkyl, hydroxy-(2-6C)alkoxy, (1-6C)alkoxy-(2-6C)alkoxy, di-[(1-6C)alkyl]amino-(2-6C)alkoxy, amino(2-6C)alkylamino, N-(1-6C)alkyl-(1-6C)alkylamino-(2-6C)alkylamino, aryl, aryl-(1-6C)alkoxy, heteroaryl, heteroaryl-(1-6C)alkoxy, heterocyclyl, heterocyclyl-(1-6C)alkyl, heterocyclyloxy and heterocyclyl-(1-6C)alkoxy; p is 0-2 and R2 is a substituent such as hydroxy and halogeno; q is 0-4; and R4 includes optionally substituted aryl, cycloalkyl, heteroaryl and heterocyclyl; or pharmaceutically-acceptable salts or in-vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytType: GrantFiled: September 23, 2004Date of Patent: August 10, 2010Assignee: AstraZeneca ABInventors: Dearg Sutherland Brown, George Robert Brown
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Patent number: 7758877Abstract: The present invention provides for a storage stable pharmaceutical liquid suspension for oral administration having a pharmaceutically effective amount of an antihistamine. The storage stable suspension preferably contains loratadine. The present invention further provides a process of preparing the storage stable pharmaceutical liquid suspension as well as a method of treating a mammal with a therapeutically effective amount of loratadine in the stable pharmaceutical liquid suspension.Type: GrantFiled: February 2, 2005Date of Patent: July 20, 2010Assignee: Taro Pharmaceuticals U.S.A., Inc.Inventors: Satish Asotra, Shen Gao, Xiaoli Wang
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Publication number: 20100179118Abstract: The present invention relates to a compound represented by the following formula (I), which is useful as an antiallergic agent and/or an anti-inflammatory agent, or a physiologically acceptable salt thereof and the like: wherein R1 and R2 are the same or different and each is an optionally substituted aryl group and the like, R3 is a hydrogen atom, a C1-6 alkyl group and the like, R4 and R5 are the same or different and each is a hydrogen atom, a halogen atom, a hydroxy group, a C1-6 alkyl group and the like, X is a single bond or —C(R6)(R7)—, R6 and R7 are the same or different and each is a hydrogen atom, a halogen atom, an optionally substituted C1-6 alkyl group and the like, or R6 and R7 optionally form, together with the carbon atom bonded thereto, an optionally substituted C3-8 cycloalkyl group and the like, ring group A is an azetidin-1-yl group and the like, m is 0, 1 or 2, and n is 0, 1 or 2.Type: ApplicationFiled: September 7, 2007Publication date: July 15, 2010Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.Inventors: Michinori Ozawa, Tomoya Shiro, Takaaki Sumiyoshi, Mari Itoh
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Patent number: 7745427Abstract: The present invention is directed to compounds of Formula (I) and Formula (II) (where variables R1, R2, R3, R4, A, B, G, J, Q, T, U, V, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: October 18, 2005Date of Patent: June 29, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Daniel V. Paone, Diem N. Nguyen, Christopher S. Burgey, James Z. Deng
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Publication number: 20100152147Abstract: The present invention provides pharmaceutical compositions comprising azelastine, or a pharmaceutically acceptable salt or ester thereof including azelastine hydrochloride, and optionally one or more additional active agents. Preferred such compositions further comprise one or more pharmaceutically acceptable carriers or excipients that reduce the amount of post-nasal drip, and/or that minimize or mask the unpleasant bitter taste associated with post-nasal drip, of the compositions into the oral cavity, upon intranasal or ocular administration of the compositions. Especially effective excipients used in the compositions of the present invention are hypromellose as a viscosity modifier and sucralose as a taste-masking agent.Type: ApplicationFiled: September 29, 2009Publication date: June 17, 2010Inventors: Dennis Fuge, John Higson, Bryan A. Roecklein, Gul Balwani, Alexander D. D'Addio
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Publication number: 20100144610Abstract: An aspect of the present invention provides for a medicament including a solution containing pleconaril or a pharmaceutically acceptable salt thereof, wherein at least one solvent including the solution is a pleconaril-dissolving hydrofluorocarbon.Type: ApplicationFiled: February 17, 2010Publication date: June 10, 2010Inventors: Saeed M. Chaudhry, Julianne Berry, Joel A. Sequeira
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Patent number: 7732438Abstract: Compounds of Formula (I) and Formula (II) (where variables R1, R2, R4, A, B, W, X, Y and Z are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: October 12, 2005Date of Patent: June 8, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Daniel V. Paone, Anthony W. Shaw, Craig M. Potteiger
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Publication number: 20100137268Abstract: The present invention relates to new phthalazinone modulators of H1 receptor activity and/or modulators of LTC4 production, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: December 3, 2009Publication date: June 3, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventor: Thomas G. Gant
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Publication number: 20100137285Abstract: The present invention provides compounds having formula (I) or (II): and pharmaceutically acceptable derivatives thereof, wherein m, p, R1, R2, R3 and R4 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of diseases, disorders or conditions associated with HGF/SF or other cytokine activity.Type: ApplicationFiled: November 30, 2009Publication date: June 3, 2010Applicant: ANGION BIOMEDICA CORP.Inventors: David E. Zembower, Jasbir Singh, Rama K. Mishra
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Patent number: 7723330Abstract: Compounds of Formulas Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: GrantFiled: March 6, 2007Date of Patent: May 25, 2010Assignees: Array BioPharma Inc., Genentech, Inc.Inventors: James F. Blake, Steven Armen Boyd, Jason De Meese, Kin Chiu Fong, John J. Gaudino, Tomas Kaplan, Allison L. Marlow, Jeongbeob Seo, Allen A. Thomas, Hongqi Tian, Frederick Cohen, Wendy B. Young
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Publication number: 20100120741Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of H1R and/or H4R for the treatment or prevention of inflammatory, autoimmune, allergic, and ocular diseases.Type: ApplicationFiled: September 10, 2009Publication date: May 13, 2010Applicants: Kalypsys, Inc., Alcon Research, LtdInventors: Allen J. Borchardt, Clay Beauregard, Travis Cook, Robert L. Davis, Daniel A. Gamache, John M. Yanni
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Patent number: 7709468Abstract: The present invention is directed to novel imidazopyrazine and imidazopyrimidine compounds of formula (I) wherein the variables are as defined herein. The compounds of formula (I) are useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.Type: GrantFiled: September 1, 2006Date of Patent: May 4, 2010Assignee: Abbott LaboratoriesInventors: David J. Calderwood, Kristine E. Frank, Patrick Betschmann, Gavin C. Hirst, Eric C. Brieinlinger, Michael J. Morytko, Richard W. Dixon