Additional Ring Containing Patents (Class 546/337)
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Patent number: 7968574Abstract: The invention relates to compounds and methods for modulating one or more components of a kinase cascade. The invention relates to compounds of the formula I: or a pharmaceutically acceptable salt thereof. The compounds of the invention are useful for methods of protecting against or treating hearing loss, osteoporosis, cell proliferative disorders, obesity, diabetes, eye disease, stroke, atherosclerosis, neuropathic pain or hepatitis B.Type: GrantFiled: June 29, 2006Date of Patent: June 28, 2011Assignee: Kinex Pharmaceuticals, LLCInventor: David G. Hangauer, Jr.
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Publication number: 20110152323Abstract: The present invention discloses a group of histone deacetylase inhibitors and use thereof. The histone deacetylase inhibitors are useful in the treatment of malignant tumors and the diseases associated with differentiation and proliferation.Type: ApplicationFiled: June 9, 2009Publication date: June 23, 2011Applicants: JIANGSU GOWORTH INVESTMENT CO. LTD, SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRYInventors: Jianqi Li, Juan Feng, Wangping Cai
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ACYLAMINO-SUBSTITUTED FUSED CYCLOPENTANECARBOXYLIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS
Publication number: 20110152290Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: November 4, 2010Publication date: June 23, 2011Applicant: SANOFI-AVENTISInventors: Matthias SCHAEFER, Josef PERNERSTORFER, Dieter KADEREIT, Hartmut STROBEL, Werngard CZECHTIZKY, L. Charlie CHEN, Alena SAFAROVA, Aleksandra WEICHSEL, Marcel PATEK -
Publication number: 20110124648Abstract: The present invention discloses novel compounds of Formula I, or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.Type: ApplicationFiled: January 25, 2011Publication date: May 26, 2011Applicant: ELI LILLY AND COMPANYInventors: Scott Eugene CONNER, Guoxin ZHU, Jianke LI
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Patent number: 7943776Abstract: The invention concerns a compound of the Formula (I), wherein Qa is heteroaryl and is substituted with halogeno; R1 and R2 are each hydrogen; and Qb is phenyl or heteroaryl, and Qb may optionally bear 1 or 2 substituents selected from hydroxy, halogeno and (1-6C)alkyl, or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.Type: GrantFiled: December 15, 2004Date of Patent: May 17, 2011Assignee: Asrazeneca ABInventors: Dearg Sutherland Brown, John Graham Cumming, Ian Alun Nash
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Publication number: 20110112076Abstract: The present invention provides a compound of formula (I) said compound is inhibitor of MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-12 and/or MMP-13. Finally, the present invention also provides pharmaceutical composition that include the compound of formula (I).Type: ApplicationFiled: July 13, 2009Publication date: May 12, 2011Inventors: Leslie Wighton McQuire, Olivier Rogel, Michael Shultz, Ruben Alberto Tommasi, Sven Weiler
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Patent number: 7939552Abstract: Disclosed is a novel benzyloxypropylamine derivative having an excellent tachykinin receptor antagonistic effect. This compound shows a good transfer into the blood and a long blood half-life in the blood kinetic test using a guinea pig orally administered with the compound and is stable in an animal plasma. The compound also shows a high transfer to the central nervous system when it is orally administered to a guinea pig at a certain dose. Accordingly, the benzyloxypropylamine derivative is quite useful as a novel anti-tachykinin agent.Type: GrantFiled: March 29, 2006Date of Patent: May 10, 2011Assignee: Nippon Zoki Pharmaceutical Co., Ltd.Inventors: Kunihiko Higashiura, Takashi Ogino, Kazuhito Furukawa
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Publication number: 20110104162Abstract: The present invention relates to a compound of general formula (I): and also to the pharmaceutically acceptable salts thereof, to the isomers or isomer mixtures thereof in all proportions, in particular to an enantiomer mixture, and especially to a racemic mixture. The present invention also relates to the use of these compounds as a medicament, and in particular for the treatment of cancer, and also to the compositions containing them.Type: ApplicationFiled: June 15, 2009Publication date: May 5, 2011Applicant: Cytomics SystemsInventors: Denis Carniato, Karine Jaillardon, Olivier Busnel, Mathieu Gutmann, Jean-Francois Briand, Benoit Deprez, Dominique Thomas, Cécile Bougeret
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Patent number: 7932396Abstract: A compound of general formula (I): A process for preparing this compound. A compound of general formula (II): A fungicide composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.Type: GrantFiled: May 17, 2006Date of Patent: April 26, 2011Assignee: Bayer Cropscience AGInventors: Darren Mansfield, Pierre-Yves Coqueron, Heiko Rieck, Philippe Desbordes, Alain Villier, Marie-Claire Grosjean-Cournoyer, Pierre Genix
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Publication number: 20110092461Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.Type: ApplicationFiled: December 6, 2010Publication date: April 21, 2011Inventors: Janet L. GUNZNER, Daniel Sutherlin, Mark S. Stanley, Liang Bao, Georgette M. Castanedo, Rebecca L. Lalonde, Shumei Wang, Mark E. Reynolds, Scott J. Savage, Kimberly Malesky, Michael S. Dina
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Publication number: 20110070329Abstract: Described is a new cooling agent represented by Formula I and compositions with known coolers having cooling properties and the application of Formula I in foodstuffs and chewing gum: wherein X, Y is independently selected from a C1-C4 straight or branched alkyl or H atom; and m is 0, 1 or 2, Z when present is nitrogen, W and W? are selected independently from the group consisting of H, OH, C1-C4 straight or branched alkyl, and a C1-C4 straight or branched alkoxy or W is group (CH2)n-R, where n is 0 or 1 and R is a group with non-bonding electrons. Useful groups with non-bonding electrons are halogens, OH, OMe, OEt, NO2, CN, Ac, SO2NH2, CHO, CO2H, CONH2, CONHR2, where R2 is selected from C1-C4, and C1-C4 alkyl carboxylates such as CO2Me or CO2Et.Type: ApplicationFiled: September 18, 2009Publication date: March 24, 2011Inventors: Arkadiusz Kazimierski, Kenneth J. Kraut
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Patent number: 7906629Abstract: Activated haptens useful for generating immunogens to HIV protease inhibitors, immunogens useful for producing antibodies to HIV protease inhibitors, and antibodies and labeled conjugates useful in immunoassays for the HIV protease inhibitor saquinavir. The novel haptens feature an activated functionality at the central, non-terminal hydroxyl group. Also described are monoclonal antibodies specific for saquinavir having less than 10% cross-reactivity with lopinavir, nelfinavir, amprenavir, ritonavir, and indinavir, and a murine hybridoma producing said antibodies.Type: GrantFiled: January 31, 2007Date of Patent: March 15, 2011Assignee: Roche Diagnostics Operations, Inc.Inventors: Gerald F. Sigler, Raymond A. Hui, Ina Deras, Erasmus Huber, Herbert W. Von Der Eltz
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Publication number: 20110059940Abstract: The disclosure provides compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their uses in inhibiting ?-amyloid peptide (?-AP) production.Type: ApplicationFiled: May 7, 2009Publication date: March 10, 2011Inventors: Paul J. Gilligan, Michael G. Yang, Jianliang Shi
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Publication number: 20110039852Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein that are antagonists of PGD2 receptors. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: ApplicationFiled: January 29, 2009Publication date: February 17, 2011Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: John Howard Hutchinson, Brian Andrew Stearns, Jill Melissa Scott, Yen Pham Truong, Jeffrey Roger Roppe, Nicholas Simon Stock, Jeannie M. Arruda, Thomas Jon Seiders, Bowei Wang, Deborah Volkots
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Patent number: 7884116Abstract: It is an object of the invention to provide a novel octahydronaphthalene derivative with an activity of inhibiting ICAM-4 expression and a pharmaceutically acceptable salt thereof. The invention encompasses, for example, agents for suppressing ICAM-1, therapeutic agents for inflammatory diseases, therapeutic agents for rheumatoid arthritis, immunosuppressive agents, and agents for suppressing cell growth, comprising N-(pyridin-3-ylmethyl)-(2E,4E)-5-[(1S,2S,4aR,6R,7S,8S,8aS)-7-hydroxy-2,6,8-trimethyl-1,2,4a,5,6,7,8,8a-octahydronaphthalen-1-yl]-2-methylpenta-2,4-dienamide as an active ingredient.Type: GrantFiled: December 24, 2004Date of Patent: February 8, 2011Assignee: Nippon Shinyaku Co., Ltd.Inventor: Naoyoshi Yamada
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Publication number: 20110028509Abstract: The invention relates to compounds of formula I wherein R1, R2, R4, Ra, Rb, Rc, Re, A*, W1, W2 and W3 are as defined in claim 16, for the treatment of CXCR3 related diseases.Type: ApplicationFiled: April 8, 2009Publication date: February 3, 2011Applicant: MERCK SERONO SAInventors: Stefano Crosignani, Christophe Cleva, Christos Tsaklakidis, Lars Burgdorf
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Patent number: 7880011Abstract: A method of making a compound of formula II comprising the reaction of a compound of formula RCONH2 with a compound of formula III R being a moiety having between 1 and 15 carbon atoms and optionally from 1 to 5 heteroatoms independently selected from oxygen, nitrogen and sulfur, and X and Y being independently selected front the group consisting of H, methyl, ethyl, OMe, OEt, and mixtures thereof; the reaction being performed in a solvent in the presence of a base. The method is useful for the inexpensive manufacture of certain commercially-valuable compounds, including some that have desirable cooling properties.Type: GrantFiled: July 15, 2008Date of Patent: February 1, 2011Assignee: Givandan, S.A.Inventors: Stefan Michael Furrer, David C. Bom, David Max Dastrup, Ioana Maria Ungureanu
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Patent number: 7879863Abstract: The present invention provides a novel compound having a kininogenase-inhibitory action and its pharmaceutical use. The compounds are represented by the formulas (A), (B), (C), (E) and (H): wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: September 29, 2006Date of Patent: February 1, 2011Assignee: Ajinomoto Co., Inc.Inventors: Munetaka Tokumasu, Masayuki Sugiki, Haruko Hirashima, Hideki Matsumoto, Toshihiko Yoshimura, Yasuko Nogi, Mitsuo Takahashi, Manabu Kitazawa, Akiko Oonuki, Naoyuki Fukuchi, Yoichiro Shima
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Publication number: 20110021528Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.Type: ApplicationFiled: October 1, 2010Publication date: January 27, 2011Applicant: PHARMACYCLICS, INC.Inventors: Erik J. Verner, Martin Sendzik, Chitra Baskaran, Joseph J. Buggy, James Robinson
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Patent number: 7875636Abstract: The present invention is directed to pyridyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. 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 T-type calcium channels are involved.Type: GrantFiled: April 11, 2007Date of Patent: January 25, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: James C. Barrow, Thomas S. Reger, Zhi-Qiang Yang
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Publication number: 20110015396Abstract: Disclosed herein is a class of tunable phenylacetylene compounds as well as compositions and methods for their use as host compounds for ligand binding. In certain examples the hosts report binding events by exhibiting altered spectroscopic properties, such as different fluorescent emission spectra.Type: ApplicationFiled: September 28, 2010Publication date: January 20, 2011Applicant: The State of Oregon on behalf of the University of OregonInventors: Michael M. HALEY, Darren W. JOHNSON, Orion B. BERRYMAN, Charles A. JOHNSON, Calden N. STIMPSON
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Publication number: 20110014186Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.Type: ApplicationFiled: March 23, 2009Publication date: January 20, 2011Inventors: Claus Ehrhardt, Leslie Wighton McQuire, Pascal Rigollier, Olivier Rogel, Michael Shultz, Ruben Alberto Tommasi
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Publication number: 20110009638Abstract: Disclosed is a method for preparing a compound of Formula 1 wherein Q and Z are as defined in the disclosure comprising distilling water from a mixture comprising a compound of Formula 2, a compound of Formula 3, a base comprising at least one compound selected from the group consisting of alkaline earth metal hydroxides of Formula 4 wherein M is Ca, Sr or Ba, alkali metal carbonates of Formula 4a wherein M1 is Li, Na or K, 1,5-diazabicyclo[4.3.0]non-5-ene and 1,8-diazabicyclo[5.4.0]undec-7-ene, and an aprotic solvent capable of forming a low-boiling azeotrope with water.Type: ApplicationFiled: April 8, 2009Publication date: January 13, 2011Applicant: E.I. DU PONT DE NEMOURS AND COMPANYInventor: Gary David Annis
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Publication number: 20110009447Abstract: Substituted benzoic acid amides of formula (I) and their use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis as well as their intermediate products for the production of benzoic acid amides are described.Type: ApplicationFiled: April 24, 2001Publication date: January 13, 2011Inventors: Andreas Huth, Dieter Seidelmann, Karl-Heinz Thierauch
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Publication number: 20100331329Abstract: The invention concerns a compound of the formula (I) wherein Ring A is heterocyclyl; m is 0-4 and each R1 is a group such as hydroxy, halo, trifluoromethyl and cyano; R2 is halo and n is 0-2; and each R4 is a group such as hydroxy, halo, trifluoromethyl and cyano; p is 0-4; and R3 is amino or hydroxy; or pharmaceutically-acceptable salts or in-vivo-hydrolysable ester or amide thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical condions mediated by histone deacetylase.Type: ApplicationFiled: September 10, 2010Publication date: December 30, 2010Applicant: ASTRAZENECA ABInventors: Elaine Sophie Elizabeth Stokes, Craig Anthony Roberts, Michael James Waring
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Patent number: 7858621Abstract: This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, heart disease and so on.Type: GrantFiled: July 27, 2007Date of Patent: December 28, 2010Assignee: Amorepacific CorporationInventors: Sun-Young Kim, Jin Kwan Kim, Ki-Wha Lee, Byoung Young Woo, Song Seok Shin, Joo-Hyun Moh, Sung-Il Kim, Yeon Su Jeong, Kyung Min Lim, Jin Kyu Choi, Jun Yong Ha, Hyun-Ju Koh, Young-Ho Park, Young-Ger Suh, Hee-Doo Kim, Hyeung-Geun Park, Uh Taek Oh
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Publication number: 20100324025Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.Type: ApplicationFiled: September 21, 2009Publication date: December 23, 2010Applicant: University of WashingtonInventors: Niels H. Andersen, Jason Bowman, Alice L. Erwin, Eric A. Harwood, Toni Kline, Khisimuzi E. Mdluli, Simon Ng, Keith B. Pfister, Ribhi Shawar, Allan S. Wagman, Asha Yabannavar
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Publication number: 20100324086Abstract: A compound of formula (1) as well as pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising the compound. The compound is useful for the treatment of disorder from pain, fever, inflammation and cancer.Type: ApplicationFiled: February 19, 2009Publication date: December 23, 2010Applicant: Novasaid ABInventors: Johan Wannberg, Mathias Alterman, Patric Stenberg, Jacob Westman
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Publication number: 20100324102Abstract: A compound of general formula (I) A process for preparing this compound. A fungicidal composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.Type: ApplicationFiled: October 17, 2007Publication date: December 23, 2010Applicant: BAYER CROPSCIENCE AGInventors: Pierre-Yves Coqueron, Philippe Desbordes, Pierre Genix, Marie-Claire Grosjean-Cournoyer, Darren Mansfield, Joseph Perez, Heiko Rieck, Alain Villier
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Publication number: 20100317865Abstract: Covalent conjugates of an ?,?-disubstituted glycine ester and a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid and the ?,?-disubstituted glycine ester is conjugated to the modulator at a position remote from the binding interface between the inhibitor and the target enzyme or receptor pass into cells and the active acid hydrolysis product accumulates within the cells.Type: ApplicationFiled: February 27, 2009Publication date: December 16, 2010Applicant: c/o Chroma Therapeutics Ltd.Inventors: Alan Hornsby Davidson, Alan Hastings Drummond, David Festus Charles Moffat, Alistair David Graham Donald, Stephen John Davies
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Publication number: 20100292485Abstract: Process for the preparation of a N-[2-(2-pyridinyl)ethyl]carboxamide derivative of general formula (I) or a salt thereof Intermediate of general formula (II) Intermediate of general formula (III)Type: ApplicationFiled: July 30, 2010Publication date: November 18, 2010Applicant: BAYER CROPSCIENCE S.A.Inventors: Frédéric LHERMITTE, Pierre-Yves COQUERON, Philippe DESBORDES, Thomas HIMMLER
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Publication number: 20100286125Abstract: Compounds having the formula wherein the symbols have the meaning described in the specification are hydroxamic acid derivatives of 4-phenyl-4-hydroxy-butyric acid and capable of inhibiting the lethal effects of infection by anthrax bacteria and are useful in the treatment of poisoning by anthrax.Type: ApplicationFiled: March 28, 2008Publication date: November 11, 2010Inventors: Alan T. Johnson, Seongjin Kim
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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: 20100273828Abstract: The present invention relates to novel 4-(4-pyridyl)-benzamides of the formula (I). The compounds I possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of Rho kinases (ROCKs).Type: ApplicationFiled: August 26, 2008Publication date: October 28, 2010Inventors: Helmut Mack, Nicole Teusch, Bernhard K. Müller, Wilfried Hornberger, Michael F. Jarvis, Daryl Sauer, Steve Swann, JR., Anil Vasudevan
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Publication number: 20100256202Abstract: The invention relates to compounds corresponding to formula (I): In which Ar1, Ar2, Q, Y, Z, Alk?, k and m are as defined herein. The invention further relates to their preparations, intermediates therefor and their therapeutic uses.Type: ApplicationFiled: April 7, 2010Publication date: October 7, 2010Applicant: SANOFI-AVENTISInventors: Lionel BARRE, Christian CONGY, Philippe POINTEAU, Murielle RINALDI-CARMONA
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Publication number: 20100256147Abstract: The invention relates to compounds and methods for modulating one or more components of a kinase cascade.Type: ApplicationFiled: April 14, 2008Publication date: October 7, 2010Inventor: David G. Hangauer, JR.
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Publication number: 20100249424Abstract: Disclosed is a method for preparing a compound of Formula 1 wherein R1 is CHX2, CX3, CX2CHX2 or CX2CX3; each X is independently Cl or F; Z is optionally substituted phenyl; and Q is phenyl or 1-naphthalenyl, each optionally substituted as defined in the disclosure; comprising contacting a compound of Formula 2 with hydroxylamine in the presence of a base. The present invention also relates to novel compounds of Formula 2, useful as starting materials for the aforedescribed method.Type: ApplicationFiled: August 4, 2008Publication date: September 30, 2010Applicant: E.I.DuPont De Nemours and CompanyInventors: Gary David Annis, Brenton Todd Smith
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Publication number: 20100249123Abstract: The present invention provides new compounds of formula I, wherein Q, R1, R2, R4, R5, R6, Xi, R7, R8, M and G1n are defined as in formula I; invention compounds are modulators of follicle-stimulating hormone—(“FSH”) which are useful for male and female contraception as well as other disorders modulated by FSH receptor.Type: ApplicationFiled: March 19, 2008Publication date: September 30, 2010Applicant: ADDEX PHARMA SAInventors: Beatrice Bonnet, Brice Campo, Luca Raveglia, Mauro Riccaboni
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Patent number: 7803946Abstract: Disclosed herein is a class of tunable phenylacetylene compounds as well as compositions and methods for their use as host compounds for ligand binding. In certain examples the hosts report binding events by exhibiting altered spectroscopic properties, such as different fluorescent emission spectra.Type: GrantFiled: December 14, 2007Date of Patent: September 28, 2010Inventors: Michael M. Haley, Darren W. Johnson, Orion B. Berryman, Charles A. Johnson, Calden N. Stimpson
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Patent number: 7799824Abstract: Quaternary salt compounds of Formula (I) or pharmaceutically acceptable forms thereof, which are CCR2 antagonists and are useful in preventing, treating or ameliorating CCR2 mediated inflammatory syndromes, disorders or diseases in a subject in need thereof.Type: GrantFiled: June 22, 2005Date of Patent: September 21, 2010Assignee: OraPharma, Inc.Inventors: Bharat Lagu, Michael Wachter
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Patent number: 7795315Abstract: The present invention provides novel compounds of the general formula (I) and pharmaceutically acceptable salts thereof, processes for the manufacture of these novel compounds and medicaments containing such compounds. The compounds of the present invention show anti-proliferative and differentiation-inducing activity, which results in inhibition of tumor cell proliferation, induction of apoptosis and inhibition of invasion. The invention also covers the use of such compounds for the treatment of diseases such as cancer and for the manufacture of corresponding medicaments.Type: GrantFiled: January 23, 2009Date of Patent: September 14, 2010Assignee: Hoffman-La Roche Inc.Inventors: Li Chen, Yun He, Jason Christopher Wong
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Patent number: 7790901Abstract: Process for the preparation of a N-[2-(2-pyridinyl)ethyl]carboxamide derivative of general formula (I) or a salt thereof Intermediate of general formula (II) Intermediate of general formula (III).Type: GrantFiled: December 19, 2005Date of Patent: September 7, 2010Assignee: Bayer Cropscience S.A.Inventors: Frédéric Lhermitte, Pierre-Yves Coqueron, Philippe Desbordes, Thomas Himmler
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Publication number: 20100222337Abstract: Conventional fungicidal compositions have had practical problems such that either a preventive effect or a curative effect is inadequate, the residual effect tends to be inadequate, or the controlling effect against plant diseases tends to be inadequate depending upon the application site, and a fungicidal composition to overcome such problems has been desired. The present invention provides a fungicidal composition containing a carboxylic acid amide derivative of the formula (I) or a salt thereof, as an active ingredient: wherein A is phenyl which may be substituted, benzodioxolanyl which may be substituted, or benzodioxanyl which may be substituted; B is 2- or 3-pyridyl which may be substituted; each of R1 and R2 is alkyl, or R1 and R2 may together form a 3- to 6-membered saturated carbon ring, provided that when B is 3-pyridyl which may be substituted, A is phenyl substituted by at least two substituents.Type: ApplicationFiled: December 13, 2006Publication date: September 2, 2010Applicant: Ishihara Sangyo Kaisha, Ltd.Inventors: Yuji Nakamura, Shigeru Mitani, Shintaro Tsukuda
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Publication number: 20100222317Abstract: The present invention relates to compounds of formula (I); and pharmaceutically acceptable salts thereof and individual enantiomers and diastereomers thereof, as GIyT1 inhibitors for treating neurological and psychiatric disorders.Type: ApplicationFiled: November 23, 2006Publication date: September 2, 2010Inventors: Wesley Peter Blackaby, Richard Thomas Lewis, Elizabeth Mary Naylor
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Publication number: 20100216849Abstract: This invention relates to novel biphenylcarboxamides of the formula (I) in which R, Z, X, Y, m, n and A are as defined in the disclosure, to a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and to novel intermediates and their preparation.Type: ApplicationFiled: April 30, 2010Publication date: August 26, 2010Inventors: Ralf Dunkel, Hans-Ludwig Elbe, Heiko Rieck, Ulrike Wachendorff-Neumann, Peter Dahmen, Peter Lösel, Karl-Heinz Kuck, Astrid Mauler-Machnik, Jörg Nico Greul
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Patent number: 7777045Abstract: Process for the preparation of a 2-ethylaminopyridine derivative of general formula (I) or a salt thereof Process for the preparation of a N-[2-(2-pyridinyl)ethyl]carboxamide derivative of general formula (II) or a salt thereof Intermediate of general formula (III)Type: GrantFiled: December 19, 2005Date of Patent: August 17, 2010Assignee: Bayer Cropscience S.A.Inventors: Frédéric Lhermitte, Gilles Perrin-Janet, Paul Dufour, Pierre-Yves Coqueron
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Publication number: 20100204284Abstract: Hetero-substituted acetanilide derivatives are disclosed as analgesic agents. The compounds of the invention are useful in methods for treating a disease or condition in a mammal characterized by pain and/or fever.Type: ApplicationFiled: March 31, 2010Publication date: August 12, 2010Inventors: John R. Carson, James J. McNally
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Publication number: 20100184990Abstract: The invention describes an improved process for the manufacture of a Flecainide intermediate viz N-(pyridin-2-ylmethyl)-2,5-bis(2,2,2-trifluoroethoxy)benzamide (II). It consists of reacting 2,5-bis(2,2,2-trifluoroethoxy)benzoic acid with an acid chloride in a solvent mixture in presence of a base at ?10 to ?50° C. The resulting mixed anhydride is then condensed with 2-aminomethylpyridine at ?10 to ?40° C. and the resulting product after aqueous workup is purified by crystallization. This affords the intermediate II in vastly improved yields and quality. The intermediate II on catalytic hydrogenation affords N-(2-piperidinylmethyl)-2,5-bis(2,2,2-trifluoroethoxy)benzamide (Flecainide), isolated as its acetate.Type: ApplicationFiled: September 9, 2005Publication date: July 22, 2010Inventors: Harmander Pal Singh Chawla, Anil Shankar Chowdhary, Piyush Bhikhubhai Limbad, Rajesh Jagannathbhai Jha, Vipul Narbheshankar Joshi
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Publication number: 20100168070Abstract: The invention relates to substituted 1,2-ethylenediamines of general formula (I), wherein the radicals R1-R13, A, B, L and i are as defined in the description and in the claims. The invention also relates to the use thereof for treating Alzheimer's disease (AD) and similar diseases.Type: ApplicationFiled: August 8, 2006Publication date: July 1, 2010Inventors: Niklas Heine, Klaus Fuchs, Christian Eickmeier, Stefan Peters, Cornelia Dorner-Ciossek, Sandra Handschuh, Herbert Nar, Klaus Klinder
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Publication number: 20100160327Abstract: The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: June 21, 2006Publication date: June 24, 2010Inventors: Jonathan Grimm, Paul Harrington, Richard Heidebrecht, JR., Thomas Miller, Karin Otte, Phieng Siliphaivanh, David Sloman, Matthew Stanton, Kevin Wilson, David Witter, Solomon Kattar, Paul Tempest