Five-membered Nitrogen Hetero Ring Attached Directly Or Indirectly To The Piperazine Ring By Nonionic Bonding Patents (Class 514/253.09)
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Publication number: 20100249127Abstract: The present invention relates to substituted indolo-pyridinone compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted indolo-pyridinone compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: March 31, 2010Publication date: September 30, 2010Applicant: ArQule, Inc.Inventors: Nivedita Namdev, Manish Tandon, Jianqiang Wang, Audra Dalton, David Vensel, Rocio Palma, Mark A. Ashwell, Neil Westlund
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Publication number: 20100249128Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I): wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications (including in particular diabetic retinopathy, nephropathy or neuropathy), cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, viral diseases, inflammatory disorders, or diseases in which the liver is a target organ.Type: ApplicationFiled: April 10, 2008Publication date: September 30, 2010Inventors: Iriny Botrous, Yufeng Hong, Hui Li, Kevin Kun-Chin Liu, Seiji Nukui, Min Teng, Eileen Valenzuela Tompkins, Chunfeng Yin
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Publication number: 20100240618Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: ApplicationFiled: September 8, 2009Publication date: September 23, 2010Applicant: ChemoCentryx, Inc.Inventors: Andrew M.K. Pennell, James B. Aggen, J.J. Kim Wright, Subhabrata Sen, Brian E. McMaster, Daniel Joseph Dairaghi, Wei Chen, Penglie Zhang
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Publication number: 20100239657Abstract: The inventive composite having a nanoscale particle size can specifically deliver therapeutic nucleic acids or drugs to the liver and selectively release them into hepatic cells to manifest potent therapeutic effects without inducing any enzymatic abnormalities or pathological damage to the normal liver function, when administered together with the therapeutic agents.Type: ApplicationFiled: June 1, 2010Publication date: September 23, 2010Applicant: MOGAM BIOTECHNOLOGY RESEARCH INSTITUTEInventors: Meehyein KIM, Soo In Kim, Duckhyang Shin, Mahnhoon Park
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Publication number: 20100234389Abstract: An object of the present invention is to provide a novel fused-ring compound which has a FAAH inhibitory effect and is useful as an analgesic. The present invention relates to a compound represented by formula (I): wherein symbols are as defined in the specification, or salt thereof.Type: ApplicationFiled: October 9, 2008Publication date: September 16, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masakuni Kori, Mitsunori Kouno
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Publication number: 20100234394Abstract: New substituted benzimidazole compounds, compositions, and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.Type: ApplicationFiled: April 13, 2010Publication date: September 16, 2010Inventors: Mina E. Aikawa, Payman Amiri, Jeffrey H. Dove, Barry Haskell Levine, Christopher McBride, Teresa E. Pick, Daniel J. Poon, Savithri Ramurthy, Paul A. Renhowe, Cynthia Shafer, Darrin Stuart, Sharadha Subramanian
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Publication number: 20100234431Abstract: A compound of the following formula: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, X, Y, and Z are as defined herein. Also disclosed is a method for inhibiting actively of fibroblast activation protein or for treating cancer or inflammation conditions with such a compound.Type: ApplicationFiled: February 19, 2010Publication date: September 16, 2010Applicant: National Health Research InstitutesInventors: Weir-Tong Jiaang, Xin Chen
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Publication number: 20100234390Abstract: The present invention provides novel compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and compositions, metabolites and prodrugs thereof. The novel compounds are useful as antibacterial agents in the treatment of conditions such as nosocomial pneumonia, community acquired pneumonia, infections caused by vancomycin resistant enterococci (VRE), methicillin resistant Staphylococcus aureus (MRSA), Heamophilus influenzae (HI) and penicillin resistant Streptococcus pneumoniae (PRSP). The compounds of the present invention are effective against a number of human or animal pathogens including VRE, PRSP, HI and MRSA.Type: ApplicationFiled: June 20, 2008Publication date: September 16, 2010Inventors: Simi Pushpan, Uma Ramachandran, Mrinalkanti Kundu
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Publication number: 20100234356Abstract: The present invention relates to compounds useful as Chemokine Receptor antagonists. Compounds of general formula I are provided: or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and compositions for the inhibition of Chemokine Receptors and also for the treatment of various diseases, conditions, or disorders, including acute or chronic inflammatory disease, cancer, and osteolytic bone disorders.Type: ApplicationFiled: October 13, 2009Publication date: September 16, 2010Applicant: Millennium Pharmaceuticals, Inc.Inventors: Gerard Rosse, Linli Wei, Kenneth G. Carson
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Publication number: 20100234352Abstract: The present invention is directed to compounds represented by Formula (I) or a pharmaceutically acceptable salt, ester, or prodrug thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.Type: ApplicationFiled: January 29, 2010Publication date: September 16, 2010Inventors: Bing-Yan Zhu, Shawn M. Bauer, Zhaozhong J. Jia, Yonghong Song, Gary D. Probst, Yanchen Zhang, Robert M. Scarborough
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Patent number: 7795261Abstract: This invention concerns substituted I-piperidin-4-yl-4-pyrrolidin-3-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK3 antagonistic activity and a combined NK1/NK2/NK3 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of schizophrenia, anxiety, depression, emesis and IBS. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in claim 1.Type: GrantFiled: December 17, 2003Date of Patent: September 14, 2010Assignee: Janssen Pharmaceutica NVInventors: Frans Eduard Janssens, François Maria Sommen, Benoît Christian Albert Ghislain De Boeck, Joseph Elisabeth Leenaerts
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Publication number: 20100226918Abstract: The present invention relates to compounds of the formula I, in which R1; R2; R3; R4; R5; R6; R7; R8; R9; R10; R11; R12; R13; A; B, D and E have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable e.g. for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 is 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: December 16, 2009Publication date: September 9, 2010Applicant: SANOFI-AVENTISInventors: Otmar KLINGLER, Joerg CZECH, Werngard CZECHTIZKY, Tilo WEISS, Melitta JUST
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Publication number: 20100222357Abstract: The present invention relates to indol-3-yl-carbonyl-piperidin and piperazin derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the residues R1 to R3 are as defined herein. The invention also relates to pharmaceutical compositions containing such compounds, and methods for preparation of the compounds and compositions. The invention further relates to methods for treating dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxiety and depressive disorders.Type: ApplicationFiled: May 13, 2010Publication date: September 2, 2010Inventors: Caterina Bissantz, Christophe Grundschober, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Patent number: 7786129Abstract: The present invention is concerned with new 3,3-disubstituted indol-2-one derivatives of the general Formula (I), wherein R1 stands for hydrogen, halogen, alkyl having 1-7 carbon atom(s) or sulfonamido; R2 represents hydrogen or halogen; R3 denotes hydrogen, alkyl having 1-7 carbon atom(s) optionally carrying an aryl substituent or aryl optionally carrying one or two halogen substituent(s); R4 stands for alkyl having 1-7 carbon atom(s); R5 represents a group of the general Formula (II a) or (II b), wherein Q and W each represents nitrogen or CH; R6, R7 and R8 each stands for hydrogen, halogen, trifluoromethyl, alkyl or alkoxy having 1-7 carbon atom(s), or R6 and R7 together represent ethylenedioxy; m is 0, 1, or 2; a is a single, double or triple bond; n is 0, 1 or 2; and pharmaceutically acceptable acid addition salts thereof which are useful in the treatment or prophylaxis of diseases of the central nervous system, the gastrointestinal system and the cardiovascular system.Type: GrantFiled: May 11, 2005Date of Patent: August 31, 2010Assignee: Egis Gyogyszergyar NyrtInventors: Balázs Volk, József Barkóczy, Gyula Simig, Tibor Mezei, Rita Kapillerné Dezsöfi, Endréné Flórian, István Gacsályi, Katalin Pallagi, Gábor Gigler, György Lévay, Krisztina Móricz, Csilla Leveleki, Nóra Sziray, Gábor Szénási, András Egyed, László Gábor Hársing
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Patent number: 7786124Abstract: The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: or a pharmaceutically acceptable salt, solvate or ester thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, zenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.Type: GrantFiled: March 19, 2007Date of Patent: August 31, 2010Assignee: Schering CorporationInventors: Stuart B. Rosenblum, Joseph A. Kozlowski, Neng-Yang Shih, Brian F. McGuinness, Douglas W. Hobbs
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Publication number: 20100210659Abstract: The present invention relates to a compounds of formula I wherein A, Ar, R, R2, R3, R4, p, and o are as defined in the specification and claims or to a pharmaceutically active salt thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, bipolar disorders, anxiety and attention deficit hyperactivity disorder (ADHD).Type: ApplicationFiled: February 11, 2010Publication date: August 19, 2010Inventors: Henner Knust, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer
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Patent number: 7776862Abstract: The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: and the pharmaceutically acceptable salts, solvates and esters thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.Type: GrantFiled: February 14, 2006Date of Patent: August 17, 2010Assignee: Schering CorporationInventors: Brian F. McGuinness, Stuart B. Rosenblum, Joseph A. Kozlowski, Gopinadhan N. Anilkumar, Seong Heon Kim, Neng-Yang Shih, Chung-Her Jenh, Paul J. Zavodny, Douglas W. Hobbs, Guizhen Dong, Yuefei Shao, Lisa Guise Zawacki, Cangmeng Yang, Carolyn Dilanni Carroll
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Publication number: 20100203039Abstract: The present invention is directed to compounds of Formula I: which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment of diseases related to chemokine receptor expression and/or activity.Type: ApplicationFiled: April 16, 2010Publication date: August 12, 2010Inventor: Chu-Biao Xue
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Publication number: 20100204227Abstract: Provided herein are isoindoline compounds, pharmaceutical compositions comprising one or more of such compounds, and methods of their use for treating, preventing, or managing various diseases.Type: ApplicationFiled: October 29, 2009Publication date: August 12, 2010Inventors: George W. MULLER, Alexander L. Ruchelman
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Publication number: 20100204210Abstract: This invention relates to methods of treating pulmonary diseases in patients that beta adrenergic receptor agonist therapy is not effective. The method comprises the steps of: identifying a patient who suffers from a pulmonary disease and has reduced responsiveness to treatment with one or more beta adrenergic receptor agonists, and administering to the patient an effective amount of a Rho kinase inhibitor compound, wherein said pulmonary disease is selected from the group consisting of: asthma, chronic obstructive pulmonary disease, respiratory tract illness caused by respiratory syncytial virus infection such as RSV-induced wheezing, airway hyperreactivity, or bronchiolitis, bronchiectasis, alpha-1-antitrypsin deficiency, lymphangioleiomyomatosis, cystic fibrosis, bronchiolitis or wheezing caused by agents other than respiratory syncytial virus, chronic bronchitis, and occupational lung diseases.Type: ApplicationFiled: December 3, 2009Publication date: August 12, 2010Inventor: Scott Sorensen
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Publication number: 20100197700Abstract: The present invention provides selective 5-HT7 receptor antagonist compounds of Formula I and their use in the treatment of migraine: where A is —C(H)? or —N? and R1-7 are as defined herein.Type: ApplicationFiled: September 30, 2008Publication date: August 5, 2010Inventors: Valentina O Badescu, Sandra Ann Filla, Peter Thaddeus Gallagher, Maria Ann Whatton
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Publication number: 20100197664Abstract: Disclosed are compounds of the formula I wherein A, Y, R1, R2, R3, R4 and R5 are defined, suitable for treating diseases and symptoms of diseases caused at least to some extent by stimulation of bradykinin-B1 receptors, the preparation thereof and the use thereof.Type: ApplicationFiled: July 23, 2008Publication date: August 5, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Iris Kauffmann-Hefner, Angelo Ceci, Henri Doods, Norbert Hauel, Ingo Konetzki, Annette Schuler-Metz, Rainer Walter
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Publication number: 20100196368Abstract: New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.Type: ApplicationFiled: March 12, 2010Publication date: August 5, 2010Applicant: NOVARTIS VACCINES AND DIAGNOSTICS, INC.Inventors: Payman Amiri, Wendy Fantl, Teresa Hansen, Barry Haskell Levine, Christopher McBride, Daniel J. Poon, Savithri Ramurthy, Paul A. Renhowe, Cynthia M. Shafer, Sharadha Subramanian, Leonard Sung
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Publication number: 20100197667Abstract: The invention provides compounds of formula I: wherein a, b, c, m, s, t, W, Z, Ar, R1, R2, R3, R6, and R7 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: ApplicationFiled: April 14, 2010Publication date: August 5, 2010Applicant: THERAVANCE, INC.Inventors: Yu-Hua JI, Mathai MAMMEN, Craig HUSFELD, Li LI, YongQi MU, Aaron KUSHNER, Eric STANGELAND, Trevor MISCHKI, Adam HUGHES, Sarah DUNHAM
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Patent number: 7767674Abstract: The present invention provides kinase inhibitors of Formula I:Type: GrantFiled: June 15, 2005Date of Patent: August 3, 2010Assignee: Eli Lilly and CompanyInventors: Tiechao Li, Mark Andrew Pobanz, Chuan Shih, Yong Wang, Boyu Zhong, Jesus Andres Blas, Alfonso De Dios, Beatriz Lopez De Uralde-Garmendia, Luisa Maria Martin Cabrejas
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Publication number: 20100190802Abstract: Disclosed are carboxamide compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R3, R4, T, p, q, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: ApplicationFiled: January 28, 2010Publication date: July 29, 2010Applicant: Rigel Pharmaceuticals Inc.Inventors: Ihab S. Darwish, Hui Hong, Rajinder Singh, Xiang Xu
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Patent number: 7763616Abstract: The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: or a pharmaceutically acceptable salt, solvate or ester thereof, wherein the various moieties are defined herein. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.Type: GrantFiled: February 14, 2006Date of Patent: July 27, 2010Assignee: Schering CorporationInventors: Wensheng Yu, Seong Heon Kim, Gopinadhan N. Anilkumar, Stuart B. Rosenblum, Bandarpalle B. Shankar, Brian F. McGuinness, Douglas W. Hobbs, Yuefei Shao
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Publication number: 20100179122Abstract: Compounds of Formula (I): are HIV reverse transcriptase inhibitors, wherein R1, R2, R3, R4 and R5 are defined herein. The compounds of Formula (I) and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: June 23, 2006Publication date: July 15, 2010Inventors: Craig W. Lindsley, William H. Leister, Scott E. Wolkenberg
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Publication number: 20100179141Abstract: Disclosed are compounds of the formula (I) wherein X is N or CH, and Y is N or CR5. Also disclosed are methods of treating JNK and ERK mediated diseases using the compounds of formula 1.0.Type: ApplicationFiled: December 17, 2007Publication date: July 15, 2010Inventors: David B. Belanger, M. Arshad Siddiqui, Patrick J. Curran, Blake Hamann, Lianyun Zhao, Panduranga Adulla P. Reddy, Praveen K. Tadikonda, Gerald W. Shipps, JR., Umar Faruk Mansoor
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Patent number: 7754750Abstract: Compounds of the formula (I) wherein z is SO2 or SO, useful as metalloproteinase inhibitors, especially as inhibitors of MMP12.Type: GrantFiled: May 6, 2008Date of Patent: July 13, 2010Assignee: AstraZeneca ABInventors: Anders Eriksson, Matti Lepistö, Michael Lundkvist, Magnus Munck Af Rosenschöld, Pavol Zlatoidsky
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Patent number: 7754723Abstract: Compounds of formulae: where Ar1, Ar2, R3, R4, and m are disclosed herein, or a pharmaceutically acceptable salt thereof (a “Nitro(cyano)vinylpiperazine Compound”); compositions comprising an effective amount of a Nitro(cyano)vinylpiperazine Compound; and methods for treating or preventing pain and other conditions in an animal comprising administering to an animal in need thereof an effective amount of a Nitro(cyano)vinylpiperazine Compound are disclosed.Type: GrantFiled: June 28, 2006Date of Patent: July 13, 2010Inventors: Qun Sun, Laykea Tafesse
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Patent number: 7754721Abstract: Compounds of the formula: or pharmaceutically acceptable salts thereof, wherein m, n, X, Y, Z, Ar, R1, R2, R3, R4, R5, R6 and R7 are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.Type: GrantFiled: August 17, 2007Date of Patent: July 13, 2010Assignee: Roche Palo Alto LLCInventors: David Scott Carter, Ryan Craig Schoenfeld, Robert James Weikert
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Publication number: 20100168124Abstract: The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: or a pharmaceutically acceptable salt, solvate or ester thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.Type: ApplicationFiled: December 21, 2009Publication date: July 1, 2010Inventors: Stuart B. Rosenblum, Joseph A. Kozlowski, Neng-Yang Shih, Brian F. McGuinness, Douglas W. Hobbs
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Publication number: 20100168088Abstract: The present invention relates to a compound of formula I wherein Ar1, Ar2, R1, R2, R3, n, o, and p are as described herein or to a pharmaceutically active salt, to all stereoisomeric forms, including individual diastereoisomers and enantiomers as well as to racemic and non-racemic mixtures thereof. Compounds of the invention are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: ApplicationFiled: October 2, 2009Publication date: July 1, 2010Inventors: Caterina Bissantz, Philippe Jablonski, Henner Knust, Matthias Nettekoven, Angélique Patiny-Adam, Hasane Ratni, Claus Riemer
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Publication number: 20100160323Abstract: The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.Type: ApplicationFiled: December 22, 2009Publication date: June 24, 2010Inventors: Alexander Bischoff, Hosahalli Subramanya, Kumar Sundaresan, Srinivasa Raju Sammeta, Anil Kumar Vaka
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Publication number: 20100160262Abstract: The present invention provides treatment methods involving modulating a sirtuin activity and/or a sirtuin mRNA and/or a sirtuin polypeptide level. In some embodiments, the present invention provides treatment methods involving modulating SIRT1 activity and/or SIRT mRNA and/or polypeptide level. The present invention provides methods of inhibiting SIRT1 Tat deacetylase activity. Methods of inhibiting SIRT1 Tat deacetylase activity are useful for treating immunodeficiency virus infections, particularly human immunodeficiency virus (HIV) infection. Thus, the present invention provides methods of treating an immunodeficiency virus infection, generally involving inhibiting SIRT1 Tat deacetylase activity. The present invention further provides methods of identifying agents that modulate sirtuin activity (e.g., SIRT1 activity), particularly ability of sirtuins to interact with (e.g., bind and/or deacetylate) a substrate, e.g., a viral substrate such as a Tat polypeptide.Type: ApplicationFiled: December 23, 2008Publication date: June 24, 2010Inventors: Melanie Ott, Eric M. Verdin, Manfred Jung
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Publication number: 20100152183Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.Type: ApplicationFiled: December 4, 2009Publication date: June 17, 2010Applicant: ABBOTT LABORATORIESInventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura Hexamer, Aaron Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt
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Publication number: 20100152158Abstract: Substituted disulfonamide compounds corresponding to formula I: In which R1, R2, R3, R4a, R4b, R5a, R5b, R8, R9a, R9b, R10, R11, a, b, s, t and A have defined meanings, pharmaceutical compositions containing one or more such compounds, processes for preparing such compounds, and a method of using such compounds for the treatment or inhibition of pain and/or other conditions mediated by the bradykinin receptor 1 (BR1).Type: ApplicationFiled: November 6, 2009Publication date: June 17, 2010Applicant: GRUENENTHAL GmbHInventors: Melanie REICH, Stefan Schunk, Ruth Jostock, Sabine Hees, Tieno Germann, Michael Franz-Martin Engels
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Publication number: 20100152200Abstract: The present invention relates to chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides compounds as inhibitors of alphaviruses.Type: ApplicationFiled: November 16, 2009Publication date: June 17, 2010Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: David J. Miller, Daniel C. Peltier, Weiping Peng
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Publication number: 20100152168Abstract: The present invention relates to novel benzimidazolone derivatives of the general formula (I) in which the substituents R1, R2, R3, A1, A2, and B are as defined in claim 1, medicaments comprising these, and the use thereof for the prophylaxis and/or treatment of vasopressin-dependent diseases.Type: ApplicationFiled: August 24, 2007Publication date: June 17, 2010Applicant: ABBOTT GMBH & CO. KGInventors: Torsten Arndt, Thorsten Oost, Wilfried Lubisch, Wolfgang Wernet, Wilfried Hornberger, Liliane Unger, Juliana Ruiz Caro
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Publication number: 20100144591Abstract: The present invention relates to compounds of formula (I); compositions comprising the compounds, and methods of using the compounds to treat or prevent pain, diabetes, a diabetic complication, impaired glucose tolerance (IGT) or impaired fasting glucose (IGT) in a patient.Type: ApplicationFiled: February 27, 2008Publication date: June 10, 2010Inventors: Robert G. Aslanian, Jean E. Lachowicz, Michael Y. Berlin, Joyce J. Hwa
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Publication number: 20100144716Abstract: The present invention relates to the CGRP-antagonists of general formula I wherein R1, R2, R3, R4 and X are defined as in claim 1, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, mixtures and salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, as well as those compounds of general formula I in which one or more hydrogen atoms are replaced by deuterium, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.Type: ApplicationFiled: February 18, 2010Publication date: June 10, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Stephan Georg MUELLER, Klaus RUDOLF, Philipp LUSTENBERGER, Dirk STENKAMP, Marco SANTAGOSTINO, Fabio PALEARI, Gerhard SCHAENZLE, Kirsten ARNDT, Henri DOODS
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Publication number: 20100144752Abstract: The invention relates to heterocyclylamide-substituted thiazoles, pyrroles and thiophenes and to processes for preparing them, to their use for the treatment and/or prophylaxis of diseases, and to their use for the production of medicaments for the treatment and/or prophylaxis of diseases, particularly for use as antiviral agents, especially against cytomegaloviruses.Type: ApplicationFiled: July 1, 2006Publication date: June 10, 2010Inventors: Holger Zimmermann, David Brückner, Kerstin Henninger, Martin Hendrix, Martin Radtke
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Publication number: 20100130477Abstract: Disclosed herein is at least one spirocyclobutyl piperidine derivative, at least one pharmaceutical composition comprising at least one spirocyclobutyl piperidine derivative disclosed herein, and at least one method of using at least one spirocyclobutyl piperidine derivative disclosed herein for treating at least one histamine H3 receptor associated condition therewith.Type: ApplicationFiled: November 23, 2009Publication date: May 27, 2010Applicant: ASTRAZENECA ABInventors: Peter Bernstein, Dean Brown, Andrew Griffin, Maxime C. Tremblay, Steven Wesolowski
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Publication number: 20100129321Abstract: The present invention relates to pharmaceutical compositions for treating virus infections and/or diseases caused thereby comprising 4{4-[3-(4-chloro-3-trifluoromethylphenyl)-ureido]-3-fluorophenoxy}-pyridine-2-carboxylic acid methylamide optionally combined with at least one additional therapeutic agent.Type: ApplicationFiled: December 6, 2006Publication date: May 27, 2010Applicant: BAYER HEALTHCARE LLCInventors: Olaf Weber, Bernd Riedl
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Publication number: 20100130446Abstract: The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof. The compound of the present invention has a glucokinase activity, and is useful as a medicament such as an agent for the prophylaxis or treatment of diabetes, obesity and the like, and the like.Type: ApplicationFiled: April 25, 2008Publication date: May 27, 2010Applicant: TAKEDA PHARMACEUTICAS COMPANY LIMITEDInventors: Tsuneo Yasuma, Kentaro Hashimoto, Masahiro Ito
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Publication number: 20100120743Abstract: A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.Type: ApplicationFiled: December 17, 2009Publication date: May 13, 2010Applicant: High Point Pharmaceuticals, LLCInventors: Anette Gundertofte, Anker Steen Jorgensen, Gita Camilla Tejlgaard Kampen, Henrik Sune Andersen, Inge Thoger Christensen, John Paul Kilburn
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Publication number: 20100113359Abstract: The present invention relates to new dimethylphenoxy inhibitors of viral protease or parasitic enzymes, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: November 5, 2009Publication date: May 6, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20100113475Abstract: The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R11, R12, R13, Q, Z, and p are as described herein. Compounds of the present invention are useful for the treatment of cancers.Type: ApplicationFiled: October 27, 2009Publication date: May 6, 2010Inventors: Jerry Leroy ADAMS, Thomas H. Faitg, Neil W. Johnson, Hong Lin
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Publication number: 20100105679Abstract: Various 5-substituted 1-substituted indazoles are described, as are pharmaceutical compositions containing these compounds and methods of treatment of diseases using these compounds. Other embodiments are also described.Type: ApplicationFiled: January 9, 2008Publication date: April 29, 2010Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Peter Robert Guzzo, Matthew David Surman, Alan John Henderson, Mark Hadden, May Xiaowu Jiang