Chalcogen Bonded Directly To A Piperazine Ring Carbon Patents (Class 514/255.02)
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Publication number: 20100273785Abstract: Provided herein are 2,5-disubstituted arylsulfonamide CCR3 antagonists of Formula I or II, and pharmaceutical compositions thereof: wherein X, Y, Z, and R1-R5 are as defined herein. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.Type: ApplicationFiled: April 21, 2010Publication date: October 28, 2010Inventors: Tai Wei Ly, Garrett Thomas Potter
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Patent number: 7820676Abstract: Drug delivery systems have been developed based on the formation of diketopiperazine carboxylate salts and microparticles containing the same. The systems may further comprise a bioactive agent. Related methods for making and using the biologically active agent delivery compositions are also provided. In certain embodiments, the pharmaceutically acceptable salts described can be formed by removal of solvent by methods including distillation, evaporation, spray drying or lyophilization.Type: GrantFiled: August 23, 2005Date of Patent: October 26, 2010Assignee: MannKind CorporationInventors: Andrea Leone-Bay, Destardi Moye-Sherman, Bryan R. Wilson
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Publication number: 20100267690Abstract: Guanidine derivatives having a condensed tricyclic ring of formula 1: are disclosed, wherein U is C(O), CRaRb, O, NRa or S(O)m; V is CRaRb or NRa; W is S(O)m; wherein Ra is H, alkyl, cycloalkyl, alkenyl or aralkyl; Rb is H, alkyl, OH, ORa or OCORa, and m is the integer 0, 1 or 2; R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein with the proviso that at least one of R1, R2, R3, R4, R5, R6, R7 or R8 is guanidino or guanidino carbonyl. These derivatives are sodium-proton exchange inhibitors and are useful as medicaments for the treatment of, for example, organ disorders associated with ischemia and reperfusion, cardiac arrhythmia, cardiac hypertrophy, hypertension, cell proliferative disorders and diabetes.Type: ApplicationFiled: June 30, 2010Publication date: October 21, 2010Applicant: Piramal Life Sciences LimitedInventors: Bansi LAL, Swati Bal-Tembe, Usha Ghosh, Arun Kumar Jain, Tulsidas More, Anil Ghate, Jacqueline Trivedi, Sapna Parikh
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Patent number: 7816389Abstract: 14-O—[(((C1-6)Alkoxy-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O—[(((C1-6)Mono- or dialkylamino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Hydroxy-(C1-6)-alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Formyl-(C0-5)-alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Guanidino-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Ureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Thioureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Isothioureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins and their use as pharmaceuticals.Type: GrantFiled: January 11, 2007Date of Patent: October 19, 2010Assignee: Nabriva Therapeutics Forschungs GmbHInventors: Klaus Thirring, Gerd Ascher, Susanne Paukner, Werner Heilmayer, Rodger Novak
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Publication number: 20100249101Abstract: The present invention relates to compounds of formula I, 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 inhibitors of the blood clotting enzymes, especially factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: ApplicationFiled: January 7, 2010Publication date: September 30, 2010Applicant: SANOFI-AVENTISInventors: Henning STEINHAGEN, Hauke SZILLAT, Markus FOLLMANN, Reinhard KIRSCH, Volkmar WEHNER, Hans MATTER, Martin LORENZ, Kent W. Neuenschwander, Anthony C. SCOTESE
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Patent number: 7767666Abstract: Certain substituted butyl and butynyl benzyl amine compounds are histamine H3 receptor and/or serotonin transporter modulators useful in the treatment of histamine H3 receptor- and/or serotonin-mediated diseases.Type: GrantFiled: June 21, 2007Date of Patent: August 3, 2010Assignee: Janssen Pharmaceutica NVInventors: John M. Keith, Michael A. Letavic, Emily M. Stocking
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Publication number: 20100190794Abstract: The present invention relates to herbicidally active compositions comprising at least one piperazinedione compound of the formula I in which: Rx, Ry are each hydrogen or together are a chemical bond; R1 is cyano or nitro; R2 is hydrogen, fluorine, chlorine, C1-C2-alkyl, ethenyl or C1-C2-alkoxy; R3 is fluorine or hydrogen; R4 is methyl; R5 is hydrogen, methyl or ethyl; R6 is hydrogen, methyl or ethyl; and R7 is hydrogen or halogen; and at least one further active compound selected from the group consisting of b1) lipid biosynthesis inhibitors; b2) acetolactate synthase inhibitors (ALS inhibitors); b3) photosynthesis inhibitors; b4) protoporphyrinogen-IX oxidase inhibitors, b5) bleacher herbicides; b6) enolpyruvyl shikimate 3-phosphate synthase inhibitors (EPSP inhibitors); b7) glutamine synthetase inhibitors; b8) 7,8-dihydropteroate synthase inhibitors (DHP inhibitors); b9) mitose inhibitors; b10) inhibitors of the synthesis of very long chain fatty acids (VLCFA inhibitors); b11) cellulose biosynthesis iType: ApplicationFiled: June 11, 2008Publication date: July 29, 2010Applicant: BASF SEInventors: Eike Hupe, William Karl Moberg, Robert Reinhard, Bernd Sievernich, Elmar Kibler
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Patent number: 7763620Abstract: The present invention relates to piperazinone compounds, pharmaceutical compositions containing those compounds and methods of treating tumors and cancer, among other disease states and conditions in mammalian patients, especially including humans.Type: GrantFiled: August 23, 2002Date of Patent: July 27, 2010Assignees: Yale University, University of South FloridaInventors: Andrew D. Hamilton, Said Sebti, Hairuo Peng
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Publication number: 20100168112Abstract: The present invention provides aryl nitrones, compositions comprising the same and methods of their use for the treatment or prevention of oxidative, ischemic, ischemia/reperfusion-related and chemokine mediated conditions.Type: ApplicationFiled: July 15, 2009Publication date: July 1, 2010Inventors: Michael G. KELLY, John Kincaid, Satyanarayana Janagani
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Publication number: 20100144708Abstract: The present invention relates to new heterocyclic compounds containing nitrogen atoms or pharmaceutically acceptable salts thereof, a process for the preparation thereof, and a pharmaceutical composition comprising the same for treatment of cancer. The compounds according to the present invention induce DNA damage due to reactive oxygen species to activate c-abl and p53, induce RhoB to generate apoptosis, and induce cell death by down-regulating Bcl2 involved in cell survival, which is generated by dysregulated signals via the mitochondria pathway, thereby inhibiting tumor cell growth and inducing apoptosis. Accordingly, the composition according to the present invention can be used to treat cancer.Type: ApplicationFiled: August 10, 2007Publication date: June 10, 2010Applicants: Korea Research Instititute of Bioscience and Biotechnology, Seoul Pharma, Co., Ltd.Inventors: Gyoon Hee Han, Eun Hyun Choi, Jee Sun Yang, Sung Hee Hong, Myung Sook Kim, Mi Sun Won, Kyung Sook Chung, Dong Myung Kim, Hyang Sook Yoo, Hwan Mook Kim, Song Kyu Park, Ki Ho Lee, Chang Woo Lee, Youn Woong Choi, Yong Mi Jeong, Byung Gu Min
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Publication number: 20100105686Abstract: The present invention relates to new sulfonamide derivatives of formula (I) wherein R1-R8 and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these same compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.Type: ApplicationFiled: October 27, 2007Publication date: April 29, 2010Inventors: Gyula Beke, Eva Bozo, Sandor Farkas, Katalin Hornok, Gyorgy Keseru, Eva Schmidt, Eva Szentirmay, Istvan Vago, Monika Vastag
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Publication number: 20100105698Abstract: The invention provides diketopiperazines of formula I. The invention also provides pharmaceutical compositions comprising the diketopiperazines, or pharmaceutically-acceptable salts or prodrugs thereof, as the active ingredient. The invention further provides therapeutic treatments that utilize the diketopiperazines of formula I, including inhibition of a proliferative disease or condition, inhibition of angiogenesis, treatment of an angiogenic disease or condition, treatment of cancer and precancerous conditions, treatment of a fibrotic disorder, treatment of a viral infection, treatment of an Akt-mediated disease or condition, inhibition of the production, release or both of matrix metalloproteinase-9, and inhibition of Akt activation.Type: ApplicationFiled: May 27, 2009Publication date: April 29, 2010Applicant: DMI LIFE SCIENCES, INC.Inventor: David Bar-Or
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Patent number: 7704957Abstract: The present invention relates to a composition for inhibiting HIV activity comprising the extract of Paecilomyces sp. (Tochu-kaso) J300. More particularly, the present invention relates to a composition for inhibiting HIV activity comprising 3-[5-(methoxy-ethyl)-3,6-dioxo-piperazine-2-yl]propionic acid represented by Formula 1 and 4-methyl-2-[(pyrrolidine-2-carbonyl)-2-amino]pentanoic acid represented by Formula 2 that are extracted from Paecilomyces sp. (Tochu-kaso) J300; and to a medical composition and food composition containing the same.Type: GrantFiled: April 9, 2002Date of Patent: April 27, 2010Assignee: Rural Development AdministrationInventors: Sae-Yun Cho, Sang-Duk Ji, Seong-Kyu Song, Kwan-Hee Lee
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Publication number: 20100086609Abstract: Methods are provided for purifying peptides and proteins by incorporating the peptide or protein into a diketopiperazine or competitive complexing agent to facilitate removal one or more impurities, from the peptide or protein. Formulations and methods also are provided for the improved transport of active agents across biological membranes, resulting for example in a rapid increase in blood agent concentration. The formulations include microparticles formed of (i) the active agent, which may be charged or neutral, and (ii) a transport enhancer that masks the charge of the agent and/or that forms hydrogen bonds with the target biological membrane in order to facilitate transport. In one embodiment, insulin is administered via the pulmonary delivery of microparticles comprising fumaryl diketopiperazine and insulin in its biologically active form. This method of delivering insulin results in a rapid increase in blood insulin concentration that is comparable to the increase resulting from intravenous delivery.Type: ApplicationFiled: December 10, 2009Publication date: April 8, 2010Applicant: MANNKIND CORPORATIONInventors: Solomon S. Steiner, Rodney J. Woods, Joseph W. Sulner
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Publication number: 20100069370Abstract: Certain substituted sulfonamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: ApplicationFiled: September 3, 2009Publication date: March 18, 2010Inventors: Bradley Paul Morgan, Fady Malik, Erica Anne Kraynack, Alexander Ramon Muci, Xiangping Qian, David J. Morgans, JR.
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Publication number: 20100048590Abstract: Disclosed are compounds of the formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.Type: ApplicationFiled: September 2, 2009Publication date: February 25, 2010Inventors: Andrea Gailunas, John A. Tucker, Ruth TenBrink, John Mickelson
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Publication number: 20100048573Abstract: The present invention relates to compounds and methods for the treatment of bacterial infections. Because their mechanism of action does not involve killing of bacteria or inhibiting their growth, the potential for these compounds to induce drug resistance in bacteria is minimized. Through inhibiting bacterial virulence, the present invention provides a novel means of treating bacterial infections.Type: ApplicationFiled: October 20, 2008Publication date: February 25, 2010Inventors: Vanessa Sperandio, John R. Falck, Donald R. Stewart
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Publication number: 20100048550Abstract: The present invention relates to novel compounds of general formula (I) which are thyroid receptor ligands and are preferably selective for the thyroid hormone receptor beta(TR-Beta). Further, the present invention relates to processes of preparing such compounds, their tautomeric forms, novel intermediates involved in their synthesis, their pharmaceutically acceptable salts, methods for using such compounds and pharmaceutical compositions containing them.Type: ApplicationFiled: October 15, 2007Publication date: February 25, 2010Inventors: Saurin Raval, Preeti Raval, Braj Lohray, Vidya Bhushan Lohray, Pankaj R. Patel
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Patent number: 7662816Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a ?-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.Type: GrantFiled: August 4, 2004Date of Patent: February 16, 2010Assignee: Schering CorporationInventors: Jared N. Cumming, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voigt, Yusheng Wu, Ying Huang, Yan Xia, Samuel Chackalamannil, Tao Guo, Douglas W. Hobbs, Thuy X. H. Le, Jeffrey F. Lowrie, Kurt W. Saionz, Suresh D. Babu
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Publication number: 20100029648Abstract: This invention relates to inhibiting 11?HSD1.Type: ApplicationFiled: August 11, 2009Publication date: February 4, 2010Inventors: Jason Shaoyun Xiang, Eddine Saiah, Steve Y. Tam, John C. McKew, Lihren Chen, Manus Ipek, Katherine Lee, Huan-Qiu Li, Jianchang Li, Wei Li, Tarek Suhayl Mansour, Vipin Suri, Richard Vargas, Yuchuan Wu, Zhao-Kui Wan, Jinbo Lee, Eva Binnun, Douglas P. Wilson
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Publication number: 20100010011Abstract: Compounds of formula (I), where R1 and R3 are H or (C1-C4)-alkyl; R2 is H or a C-radical derived from one of the known ring systems with 1-4 rings; X1 is a (C1-C6)-alkyl biradical derived from a linear or branched carbon chain; and X2 is —NH—, —NH—(CH2)1-3—COO—, —NH—(CH2)1-3—S—, or —NH—CO—(CH2)1-3—S—, are useful as blood-brain barrier shuttles (BBB). BBB shuttle-cargo constructs, the cargo being a substance susceptible to form an amide or an ester or a disulfide bound with X2 and being unable to cross the blood-brain barrier by itself, are useful as medicaments.Type: ApplicationFiled: August 28, 2007Publication date: January 14, 2010Inventors: Ernest Giralt Lledó, Meritxell Teixidó Turà
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Publication number: 20090291919Abstract: Methods are disclosed for treating ophthalmic conditions related to the production of toxic visual cycle products that accumulate in the eye, and are associated with reactions of the visual cycle during medical procedures that expose the eye to light, most commonly the various forms of ophthalmic surgery. Compounds and compositions useful in the these methods, either alone or in combination with other therapeutic agents, are also described, along with methods of screening for new agents useful in said treatments.Type: ApplicationFiled: January 21, 2009Publication date: November 26, 2009Applicant: University of Florida Research Foundation, Inc.Inventors: Shalesh Kaushal, Syed M. Noorwez
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Publication number: 20090286808Abstract: The present invention provides compositions and methods useful in the treatment and/or prevention of ophthalmic conditions and diseases, such as retinitis pigmentosa, that are dependent upon or related to misfolded opsin proteins in vivo. In addition, screening assays for agents useful in such treatment methods are described.Type: ApplicationFiled: January 21, 2009Publication date: November 19, 2009Applicant: University of Florida Research Foundation, Inc.Inventors: Shalesh Kaushal, Syed M. Noorwez, David A. Ostrov
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Publication number: 20090286807Abstract: The present invention provides an excellent antihypertensive medicament. The medicament of the present invention comprises a compound having the general formula (I) and the like: [wherein R1: H, substitutable alkyl, substitutable alkenyl, substitutable cyclic hydrocarbon, substitutable heterocyclyl or the like; R2: H, substitutable alkyl, substitutable alkenyl, substitutable cycloalkyl or the like; R3, R4; H, substitutable alkyl, substitutable alkenyl, substitutable cycloalkyl or the like; R5, R6: H, substitutable alkyl, substitutable cycloalkyl, substitutable alkoxy or the like; R7, R8: H, substitutable alkyl, substitutable cycloalkyl or the like; X: the formula (II) or the like; A: substitutable cyclic hydrocarbon, substitutable heterocyclyl or the like; Y: a single bond, substitutable alkylene, substitutable alkenylene, —(CH2)a—X1—(CH2)b—(X1: the formula —NH—, —O— or the like; a, b: 0-5) or the like; B: substitutable cyclic hydrocarbon, substitutable heterocyclyl or the like].Type: ApplicationFiled: June 22, 2007Publication date: November 19, 2009Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Shojiro Miyazaki, Yuji Nakamura, Takahiro Nagayama, Taro Tokui, Yasuyuki Ogawa
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Publication number: 20090264417Abstract: Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.Type: ApplicationFiled: September 4, 2008Publication date: October 22, 2009Applicant: KALYPSYS, INC.Inventors: Stewart A. Noble, Guy Oshiro, James W. Malecha, Cunxiang Zhao, Carmen Robinson, Sergio G. Duron, Michael Sertic, Andrew K. Lindstrom, Andrew K. Shiau, Christopher D. Bayne, Mehmet Kahraman, Boliang Lou, Steven P. Govek
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Publication number: 20090227599Abstract: Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.Type: ApplicationFiled: March 3, 2009Publication date: September 10, 2009Applicant: KALYPSYS, INC.Inventors: Stewart A. Noble, Guy Oshiro, James W. Malecha, Cunxiang Zhao, Sergio G. Duron, Andrew K. Lindstrom, Andrew K. Shiau, Boliang Lou, Steven P. Govek, David J. Thomas
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Patent number: 7582632Abstract: Compounds of Formula (I): or pharmaceutically acceptable salts thereof, are useful in the prophylactic and therapeutic treatment of hyperglycemia and diabetes.Type: GrantFiled: April 16, 2007Date of Patent: September 1, 2009Assignee: Prosidion LimitedInventors: Matthew Colin Thor Fyfe, Lisa Sarah Gardner, Maseo Nawano, Martin James Procter, Chrystelle Marie Rasamison, Karen Lesley Schofield, Vilasben Kanji Shah, Kosuke Yasuda
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Patent number: 7572787Abstract: The present invention relates to substituted sulfonamide compounds of the general formula (I), wherein P is sulfonamide or amide-substituted sulfonic acid, which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous system.Type: GrantFiled: August 25, 2006Date of Patent: August 11, 2009Assignee: Biovitrum ABInventors: Patrizia Caldirola, Ulf Bremberg, Gary Johansson, Andrew Mott, Annika Jenmalm Jensen, Katarina Beierlien, Markus Thor, Lars Tedenborg
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Publication number: 20090186867Abstract: A method of treating or preventing diseases or conditions mediated through the action of oxytocin which comprises administering to a human in need thereof of an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: March 27, 2009Publication date: July 23, 2009Inventors: Alan David Borthwick, Richard Jonathan Hatley, Deirdre Mary Bernadette Hickey, John Liddle, David George Hubert Livermore, Andrew McMurtrie Mason, Neil Derek Miller, Fabrizio Nerozzi, Steven Leslie Sollis, Anna Katrin Szardenings, Paul Graham Wyatt
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Patent number: 7560459Abstract: The present invention is directed to novel compounds of the formula (I) wherein X, R1, R2, R3, R4, R5 and R6 are as described in the specification, processes for the preparation of and pharmaceutical compositions comprising said derivatives. The compounds of the present invention are useful for the treatment of epilepsy. The invention is further directed to a process for the preparation of compounds of formula (XX), wherein X, R3, R4, R5 and R6 are as described in the specification.Type: GrantFiled: November 2, 2005Date of Patent: July 14, 2009Assignee: Janssen Pharmaceutica, N.V.Inventors: Ahmed Abdel-Magid, Cynthia Maryanoff, Steven Mehrman, Allen B. Reitz, Bruce Maryanoff
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Publication number: 20090176773Abstract: The invention relates to non-peptidic molecules which modulate, especially inhibit, the interaction of protein kinase A (PKA) and A kinase anchor proteins (AKAP) and to a host or target organism that comprises said non-peptidic compounds or recognition molecules directed to said compounds, such as e.g. antibodies or chelating agents. The invention also relates to a pharmaceutical agent, especially for use in the treatment of diseases that are associated with a disturbance of the cAMP signal path, especially insipid diabetes, hypertonia, pancreatic diabetes, duodenal ulcer, asthma, heart failure, obesity, AIDS, edema, hepatic cirrhosis, schizophrenia and others. The invention also relates to the use of the inventive molecules.Type: ApplicationFiled: May 18, 2006Publication date: July 9, 2009Applicant: FORSCHUNGSVERBUND BERLIN E.V.Inventors: Enno Klussmann, Walter Rosenthal, Jorg Rademann, Frank Christian, Sina Meyer
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Publication number: 20090176768Abstract: Diaza heterocyclic amide derivatives according to Formula (I) have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: where R5, R6, R7, R8, R9, R10, m, Q, X, and Y are set forth in the description.Type: ApplicationFiled: March 17, 2009Publication date: July 9, 2009Inventors: JAY P. POWERS, Daqing Sun, Xuelei Yan
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Publication number: 20090170871Abstract: This invention relates to novel compounds and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: ApplicationFiled: June 22, 2007Publication date: July 2, 2009Applicant: SMITHKLINE BEECHAM CORPORATIONInventors: Jakob Busch-Petersen, Christopher S. Brook, Richard M. Goodman, Edward C. Webb
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Patent number: 7550462Abstract: Compounds of formula (I) wherein R1 is 2-indanyl, R2 is 1-methylpropyl, R3 is a group selected from 2,6-dimethyl-3-pyridyl or 4,6-dimethyl-3-pyridyl, R4 represents methyl and R5 represents hydrogen or methyl or, R4 and R5 together with the nitrogen atom to which they are attached represent morpholino and pharmaceutically acceptable derivatives thereof are described, as are processes for their preparation, pharmaceutical compositions containing them and their use in medicine, particularly their use as oxytocin antagonists.Type: GrantFiled: June 21, 2005Date of Patent: June 23, 2009Assignee: Glaxo Group LimitedInventors: Alan David Borthwick, Deirdre Mary Bernadette Hickey, John Liddle, Andrew McMurtrie Mason
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Publication number: 20090156553Abstract: The invention relates to the use of piperazine compounds of formula (I) or the agriculturally useful salts of piperazine compounds of formula (I) as herbicides, the variables in formula (I) being defined as cited in the claims and the description.Type: ApplicationFiled: December 29, 2006Publication date: June 18, 2009Applicant: BASF SEInventors: Eike Hupe, Cyrill Zagar, Matthias Witschel, Toralf Kuhn, William Karl Moberg, Liliana Parra Rapado, Frank Stelzer, Andrea Vescovi, Michael Puhl, Robert Reinhard, Bernd Sievernich, Klaus Grossmann, Thomas Ehrhardt, Michael Rack
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Patent number: 7531535Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: GrantFiled: December 13, 2007Date of Patent: May 12, 2009Assignee: Bristol-Meyers Squibb CompanyInventors: Donald J. P. Pinto, Jennifer X. Qiao
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Patent number: 7517884Abstract: Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.Type: GrantFiled: May 16, 2006Date of Patent: April 14, 2009Assignee: Kalypsys Inc.Inventors: James W. Malecha, Sergio G. Duron, Andrew K. Lindstrom
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Publication number: 20090069344Abstract: The present invention is directed to compounds of formula (I): where X, Y, R1, R2 and R3 are defined therein, which can act as modulators of viral replication and/or virus production, especially of the hepatitis C virus (HCV).Type: ApplicationFiled: September 29, 2005Publication date: March 12, 2009Inventors: Immacolata Conte, Caterina Ercolani, Claudio Giuliano, Giovanni Migliaccio, Ian Stansfield, Gessica Filocamo, Veronica Suriano
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Publication number: 20090069304Abstract: Since it is thought that if the activity of MMP-13 can be inhibited, this will largely contribute to improvement or prevention of progession of pathological states, particularly, osteoarthritis (OA), resulting from or associated with the MMP-13 activity, the development of MMP-13 inhibitors is anticipated. There are provided a compound represented by the general formula (I): wherein R1 is optionally substituted aryl etc.; Z is C1-C5 alkylene which may be substituted and may be interrupted with a substituent selected from Substituent group a etc.; A is the formula: (R6 and R7 are each independently halogen, lower alkyl etc.; m and n are each independently 0, 1, or 2); R2 is a hydrogen atom, optionally substituted lower alkyl etc.; R3 is a hydrogen atom, optionally substituted lower alkyl etc.; R4 is a hydrogen atom; or R3 and R4 may be taken together with an adjacent carbon atom to from a ring; R5 is hydroxy, lower alkyloxy etc.Type: ApplicationFiled: March 1, 2007Publication date: March 12, 2009Applicant: SHIONOGI & CO., LTD.Inventors: Mikayo Hayashi, Fumihiko Watanabe
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Publication number: 20090054460Abstract: Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: ApplicationFiled: January 11, 2008Publication date: February 26, 2009Inventors: Jian J. Chen, Ben C. Askew, Kaustav Biswas, Jennifer N. Chau, Derin C. D'Amico, Scott Harried, Thomas Nguyen, Wenyuan Qian, Jiawang Zhu, Christopher H. Fotsch, Aiwen Li, Qingyian Liu, Nobuku Nishimura, Tanya Peterkin, Babak Riahi, Chester Chenguang Yuan, Nianhe Han, Rana Nomak, Kevin Yang
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Patent number: 7494999Abstract: Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.Type: GrantFiled: October 25, 2005Date of Patent: February 24, 2009Assignee: Kalypsys, IncInventors: Stewart A. Noble, Guy Oshiro, James W. Malecha, Cunxiang Zhao, Carmen Robinson, Sergio G. Duron, Michael Sertic, Andrew K. Lindstrom, Andrew K. Shiau, Christopher D. Bayne, Mehmet Kahraman, Boliang Lou, Steven P. Govek
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Publication number: 20090041753Abstract: The present invention relates to compositions and methods for targeting CXC-chemokine mediated signaling for treatment of a myelin disorder.Type: ApplicationFiled: September 26, 2007Publication date: February 12, 2009Inventors: Robert H. Miller, Dolly A. Padovani-Claudio
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Publication number: 20090011994Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1, R2, R3, R8, and R9 are defined herein. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I.Type: ApplicationFiled: June 18, 2008Publication date: January 8, 2009Inventors: Philip D. Stein, Sharon N. Bisaha, Saleen Ahmad, Khehyong Ngu, William N. Washburn
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Publication number: 20080312216Abstract: The present invention relates to a compound of formula I wherein R1, R2, R3, R4, R9, R10, m and n are as defined herein, or to a pharmaceutically acceptable acid addition salt thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, bipolar disorders, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: ApplicationFiled: June 3, 2008Publication date: December 18, 2008Inventors: Henner Knust, Matthias Nettekoven, Hasane Ratni, Xihan Wu
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Patent number: 7449466Abstract: This invention provides cyclicamino-phenyl sulfamate derivatives represented by a formula wherein each of R1 and R2 stands for hydrogen or lower alkyl; each of R3 and R4 stands for hydrogen, halogen, cyano or the like; A stands for nitrogen or CH; B stands for CH2, SO2, CO, optionally substituted phenyl or the like; and R5 stands for alkyl, phenyl, amino or the like, or salts thereof which exhibit excellent steroid sulfatase inhibitory activity and are useful for prevention or treatment of diseases associated with steroids such as estrogen, androgen and the like.Type: GrantFiled: May 7, 2004Date of Patent: November 11, 2008Assignee: Aska Pharmaceutical Co., Ltd.Inventors: Shigehiro Takegawa, Shigeki Iwashita, Makoto Okada, Takayoshi Nakagawa, Naoyuki Koizumi, Tomohito Fujii
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Publication number: 20080255150Abstract: The invention relates to substituted aryl acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.Type: ApplicationFiled: November 1, 2006Publication date: October 16, 2008Applicant: ASTRAZENECA ABInventor: Timothy Luker
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Publication number: 20080242666Abstract: The present invention relates to Compound S of Formula (I).Type: ApplicationFiled: December 22, 2005Publication date: October 2, 2008Inventors: Colin Andrew Leach, John Liddle, Simon Peace, Joanne Philp, Ian Edward David Smith, Lamont Roscoe Terrell, Jing Zhang
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Publication number: 20080221123Abstract: The present invention relates to piperazinone compounds, pharmaceutical compositions containing those compounds and methods of treating tumors and cancer, among other disease states and conditions in mammalian patients, especially including humans.Type: ApplicationFiled: August 23, 2002Publication date: September 11, 2008Inventors: Andrew D. Hamilton, Said Sebti, Hairuo Peng
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Publication number: 20080146544Abstract: The present invention provides analogs of a Lysofylline (LSF), and synthetic methods for the preparation of such analogs. The have the active side chain moiety (5-R-hydroxyhexyl) of LSF and can have greater potency and oral bioavailability than LSF.Type: ApplicationFiled: February 25, 2008Publication date: June 19, 2008Inventors: Timothy L. MacDonald, Jerry L. Nadler, Peng Cui
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Patent number: 7332153Abstract: Cosmetic formulations containing a cosmetic active and a continuous phase comprising a water-immiscible liquid carrier, such as, amongst other materials, silicone oils, branched aliphatic alcohols or liquid aromatic/aliphatic esters that is structured by a cyclodipeptide derivative having the general formula in which RA represents a carbocyclic or heterocyclic group containing not more than 2 rings, other than unsubstituted cyclohexyl.Type: GrantFiled: January 17, 2003Date of Patent: February 19, 2008Assignee: Unilever Home & Personal Care USA Division of Conopco, Inc.Inventors: Shameem Bhatia, Jan van Esch, Colette Marie Fairclough, Kevin Ronald Franklin, Paul Hugh Findlay, Nicholas Webb, Michael Stephen White