The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 548/180)
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Publication number: 20110098292Abstract: The present invention provides new compounds of formula (I) as well as a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.Type: ApplicationFiled: June 29, 2005Publication date: April 28, 2011Applicant: AstraZeneca ABInventors: Jonas Malmstrom, Jenny Viklund
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Publication number: 20110065760Abstract: The present invention is related to a compound of the formula (I), (II), (III), (IV), (V): wherein Z1, Z2, Z3 and Z4 are each and independently selected from the group comprising C(O)—, —C(S)—, —C(O)—NR10—, —C(S)—NR11—, —C(N—CN)—NR12—, —S(O)—, —S(O2)—, —S(O)—NR13—, and S(O2)—NR14—, —O—, —S— or are each and individually absent; X is a spacer and is independently selected from the group comprising -M1-L1-K-L2-M2-, wherein Y.Type: ApplicationFiled: November 23, 2009Publication date: March 17, 2011Applicant: Jerini AGInventors: Jochen KNOLLE, Mike Schutkowski, Gerd Hummel, Thomas Tradler, Laurence Jobron, Claudia Christner, Dirk Scharn, Roland Stragies, Christoph Gibson, Frank Osterkamp
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Publication number: 20110065724Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: September 15, 2010Publication date: March 17, 2011Applicant: CALCIMEDICA, INC.Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers
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Publication number: 20110046185Abstract: The invention relates to compounds of formula (I) wherein the groups R and R? A, D, E, G, L, p and R1 to R10 have the stated meanings and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs.Type: ApplicationFiled: August 6, 2010Publication date: February 24, 2011Applicant: SANOFI-AVENTISInventors: Gerhard JAEHNE, Peter BELOW, Siegfried STENGELIN, Matthias GOSSEL, Thomas KLABUNDE, Irvin WINKLER
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Publication number: 20110021540Abstract: The invention provides compounds of formula wherein R1, R3, L1, L2, G1, G2, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1.Type: ApplicationFiled: November 14, 2008Publication date: January 27, 2011Applicant: ASTRAZENECA ABInventors: Johan Bylund, Maria Ek, Jorg Holenz, Martin H. Johansson, Annika Kers, Katja Narhi, Gunnar Nordvall, Liselotte Ohberg, Daniel Sohn, Jenny Viklund, Stefan Von Berg
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Publication number: 20100324071Abstract: Compounds are provided which are activators of the enzyme glucokinase and thus are useful in treating diabetes and related diseases, which compounds have the structure where Q is and R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related diseases employing the above compounds is also provided.Type: ApplicationFiled: August 30, 2010Publication date: December 23, 2010Inventors: Yan Shi, Peter T. W. Cheng, Ying Wang, Denis E. Ryono
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Publication number: 20100317543Abstract: Cyanine dye compounds having a substituted methine moiety that are nucleic acid stains, particularly for fluorescent staining of RNA, including compounds having the formula where R1 is a C1-C6 alkyl, sulfoalkyl, carboxyalkyl or C1-C6 alkoxy; each R2 is independently selected from the group consisting of H, C1-C6 alkyl, C1-C6 alkoxy, fused benzo, trifluoromethyl, amino, sulfo, carboxy and halogen, that is optionally further substituted; at least one of R3, R4, and R5 is an alkyl, aryl, heteroaryl, cyclic, or heterocyclic moiety that is optionally substituted by alkyl, amino, aminoalkyl, carboxy, nitro, or halogen; and the remaining R3, R4 or R5 are hydrogen; X is S, O, or Se; and D is a substituted or unsubstituted pyridinium, quinolinium or benzazolium moiety.Type: ApplicationFiled: August 5, 2010Publication date: December 16, 2010Applicant: LIFE TECHNOLOGIES CORPORATIONInventors: Jason Alfred DALLWIG, David Carl HAGEN, Ching-Ying CHEUNG, Gerald Alan THOMAS, Stephen YUE
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Publication number: 20100305073Abstract: The present invention relates to compounds that have CYP450 inhibiting properties and are therefore useful as boosters of certain drugs, i.e. they are able to increase at least one of the pharmacokinetic variables of certain drugs when co-administered. The invention further provides the use of said compounds as improvers of the bioavailability of certain drugs. Methods for the preparation of the compounds of the invention and pharmaceutical compositions are also provided.Type: ApplicationFiled: December 5, 2008Publication date: December 2, 2010Inventors: Tim Hugo Maria Jonckers, Wim Bert Griet Schepens, Geerwin Yvonne Paul Haché, Beate Sabine Hallenberger, Jennifer Chiyomi Sasaki, Judith Eva Baumeister, Gerben Albert Van 'T Klooster
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Publication number: 20100292206Abstract: The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4.Type: ApplicationFiled: October 17, 2008Publication date: November 18, 2010Inventors: Shizuo Kasai, Tomohiro Kaku, Masahiro Kamaura
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Publication number: 20100273835Abstract: The invention provides compounds of general formula (I) or a pharmaceutically acceptable salt, polymorph or solvate thereof, including all tautomers and stereoisomers thereof, wherein K, W, X; Y and Z are described throughout the description and claims. The compounds of the present invention are useful as inhibitors of prolyl endopeptidase (PEP, EC 3.4.21.26) and/or IL-6.Type: ApplicationFiled: July 10, 2008Publication date: October 28, 2010Applicant: PROBIODRUG AGInventors: Ulrich Heiser, Andre J. Niestroj, Ingo Schulz
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Publication number: 20100261725Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: August 26, 2009Publication date: October 14, 2010Applicant: CALCIMEDICA, INC.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Publication number: 20100248313Abstract: The present invention relates to new optically active heteroaromatic ?-hydroxy esters useful in the synthesis of epothilone derivatives, to certain compounds used to produce these intermediates, as well as to processes for their production.Type: ApplicationFiled: December 18, 2008Publication date: September 30, 2010Inventors: Johannes Platzek, Ludwig Zorn, Bernd Buchmann, Werner Skuballa, Orlin Petrov
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Publication number: 20100240678Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification.Type: ApplicationFiled: March 10, 2010Publication date: September 23, 2010Inventors: Romyr Dominique, Robert Alan Goodnow, JR., Agnieszka Kowalczyk, Qi Qiao, Achyutharao Sidduri, Jefferson Wright Tilley
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Patent number: 7799813Abstract: The present invention relates to 5-membered azacycle compounds of formula (I), pharmaceutically acceptable salts thereof and hydrates thereof, wherein the groups are as defined in the specification. The present invention further relates to pharmaceutical compositions containing said compounds or pharmaceutically acceptable salts thereof or hydrates thereof, and to use of the pharmaceutical compositions in (i) improving skin elasticity or reducing skin wrinkles, (ii) treating diabetes, (iii) treating or relieving adverse sequelae of diabetes, (iv) treating or relieving kidney damage, (v) treating or relieving damage to blood vasculature, (vi) treating or relieving hypertension, (vii) treating or relieving retinopathy, (viii) treating or relieving damage to lens proteins, (ix) treating or relieving cataract, (x) treating or relieving peripheral neuropathy, or (xi) treating or relieving osteoarthritis.Type: GrantFiled: January 29, 2007Date of Patent: September 21, 2010Assignee: Beijing Molecule Science and Technology Co., Ltd.Inventors: Song Li, Hao Cui, Junhai Xiao, Wu Zhong, Lili Wang, Gang Cheng
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Publication number: 20100233116Abstract: The present invention provides heterocyclic derivatives hat modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: August 13, 2007Publication date: September 16, 2010Inventors: Natalie Dales, Julia Fonarev, Jianmin Fu, Rajender Kamboj, Vishnumurthy Kodumuru, Shifeng Liu, Natalia Pokrovskaia, Vandna Raina, Shaoyi Sun, Zaihui Zhang
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Patent number: 7786110Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is a group of formula A or formula B, and X, R2, R3, R4, R5, R6, Ra and Rb are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the subject compounds.Type: GrantFiled: November 8, 2007Date of Patent: August 31, 2010Assignee: Roche Palo Alto LLCInventors: Michael Patrick Dillon, Ronald Charles Hawley, Li Chen, Lichun Feng, Minmin Yang
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Patent number: 7772232Abstract: A compound of formula I wherein m, n, A, B, D, E, G, H, Y, R1, R2, R3, R4, R5, and R8, are described herein. Said compounds being useful as inhibitors of potassium channel function and in the treatment of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.Type: GrantFiled: April 13, 2005Date of Patent: August 10, 2010Assignee: Bristol-Myers Squibb CompanyInventors: James A. Johnson, John Lloyd
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Publication number: 20100197688Abstract: The present invention is directed to compounds of generic formula (I) which are inhibitors of ephrin A4. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases regulated by the EphA4 RTK signaling, such as neurological and neurodegenerative disorders and cancer.Type: ApplicationFiled: May 28, 2009Publication date: August 5, 2010Inventors: Philippe G. Nantermet, Hamaka A. Rajapakse, Takeshi Sagara, John M. Sanders, Hong Zhu
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Publication number: 20100183743Abstract: Inhibitors of poly(ADP-ribose)polymerase having a structure of Formula (I), ways to make them and methods of treating patients using them are disclosed.Type: ApplicationFiled: January 19, 2010Publication date: July 22, 2010Applicant: ABBOTT LABORATORIESInventors: Magdalena K. Przytulinska, Thomas D. Penning, Yunsong Tong
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Publication number: 20100160632Abstract: The present invention relates to zinc amide bases of the general formula (I) (R1R2N)2—Zn.aMgX12.bLiX2??(I) wherein R1 and R2 are each independently selected from substituted or unsubstituted, linear or branched alkyl, alkenyl, alkynyl or silyl derivatives thereof, and substituted or unsubstituted aryl or heteroaryl, and wherein R1 and R2 can form together a ring structure, or R1 and/or R2 can be part of a polymer structure; X12 is a divalent anion or two monovalent anions that are independent from each other; X2 is a monovalent anion; a is >0; and b is >0. The zinc amide bases can be used, amongst other things, for deprotonation and metallization of aromatics.Type: ApplicationFiled: May 14, 2008Publication date: June 24, 2010Inventors: Paul Knochel, Stefan Wunderlich
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Publication number: 20100152185Abstract: The instant invention provides compounds of formula I which are 5-lipoxygenase activating protein inhibitors. Compounds of formula I are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.Type: ApplicationFiled: December 7, 2009Publication date: June 17, 2010Inventors: Lin Chu, Mark T. Goulet, Feroze Ujjainwalla, Linda Chang, Richard Frenette, Yves Girard, Michel Therien, Dwight MacDonald, John H. Hutchinson
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Publication number: 20100130538Abstract: The present invention provides a compound represented by the formula wherein R1 is a hydrocarbon group optionally having substituent(s), amino optionally having substituent(s), hydroxy optionally having a substituent or a heterocyclic group optionally having substituent(s); R2 is a hydrogen atom or a hydrocarbon group optionally having substituent(s); Xa and Xb are each C, N, O or S; Xc and Xd are each C or N; m is 0-2; n is 1-3; ring A is a 5-membered ring optionally having substituent(s); ring B is a 6-membered ring optionally having substituent(s); and ring C is a 3- to 5-membered ring optionally having substituent(s), provided that when Xa, Xc and Xd are each C, then Xb is N or S, or a salt thereof, which is useful as an agent for the prophylaxis or treatment of a disease relating to an action of melatonin, and the like.Type: ApplicationFiled: April 25, 2008Publication date: May 27, 2010Inventors: Tatsuki Koike, Takafumi Takai, Yasutaka Hoashi
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Publication number: 20100130570Abstract: The present invention relates N-5-membered, fused, heteroaryl-methylene-N-cycloalkyl-carboxamide derivatives, their thiocarboxamide or N-substituted carboximidamide analogues, all of formula (I) wherein A represents a carbo-linked 5-membered heterocyclyl group; T represents O, S, N—Rc, N—ORd, N—NRcRd or N—CN; Z1 to Z3; W1 to W5; Y1 to Y3 and p represent various substituents; their process of preparation; their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: ApplicationFiled: July 31, 2008Publication date: May 27, 2010Applicant: Bayer SASInventors: Philippe Desbordes, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Benoit Hartmann, Philippe Rinolfi, Arounarith Tuch, Jean-Pierre Vors
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Publication number: 20100105814Abstract: An ultraviolet absorbent, containing a compound represented by formula (1): wherein X1 and X2 each are an oxygen atom, a sulfur atom, or —NR16—; R11, R12, R13, R14, R15 and R16 each are a hydrogen atom or a monovalent substituent.Type: ApplicationFiled: October 27, 2009Publication date: April 29, 2010Applicant: FUJIFILM CorporationInventors: Akihiro KANEKO, Toshihiko Yawata, Yoshihiko Fujie
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Publication number: 20100099128Abstract: The present invention relates to an enzyme substrate for detecting peptidase activity in microorganisms, of formula (I) below: in which X is S; NX1; O; or NX1-CO; R1 is nothing or one of the following substituents: Cl, Br, F, I, OH, or an alkyl, aryl or carboxyl group; R2 is nothing or one of the following substituents: Cl; O—CH2—O; O—CH3; F, diethylenediamine-CH3, NR3R4, Br, I, OH, an alkyl, aryl or carboxyl group, NO2, or X1 is selected from: H, C2H4Ph, OH, an alkyl group and an aryl group; R3 and R4 are independently H or an alkyl group containing from 1 to 4 carbon atoms and P is a peptide.Type: ApplicationFiled: May 29, 2008Publication date: April 22, 2010Inventors: Olivier Fabrega, Arthur James, Vindhya Lakshika Salwatura, Sylvain Orenga, Stephen Stanforth
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Publication number: 20100041891Abstract: A compound having GPR52 agonist activity or a salt thereof is provided. The compound can be provided as a preventive/therapeutic agent for schizophrenia or the like. The compound is represented by the following formula: wherein A represents —CONRa— or —NRaCO—, Ra represents a hydrogen atom or the like, B represents a hydrogen atom or the like, a ring Cy1 represents a six-membered aromatic ring which may have one or more substituents in addition to a group represented by -A-B, a ring Cy2 represents a six-membered ring which may be substituted with a halogen atom or the like, a ring Cy3 represents a five- or six-membered ring which may have one or more substituents; X represents C1-2 alkylene or the like, m represents an integer of 0 to 2, and a ring Cy4 represents a six-membered aromatic ring which may have one or more substituents.Type: ApplicationFiled: August 11, 2009Publication date: February 18, 2010Applicant: Takeda Pharmaceutical Company LimitedInventors: Masaki Setoh, Mitsunori Kouno, Yuhei Miyanohana, Masakuni Kori
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Patent number: 7645782Abstract: The present invention relates to new Macrocycles of formula (I) and their use for the treatment of cancer.Type: GrantFiled: November 28, 2003Date of Patent: January 12, 2010Assignees: Morphochem Aktiengesellschaft fur Kombinatorische ChemieInventors: Wolfgang Richter, Lutz Weber
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Patent number: 7626035Abstract: The present invention relates to new optically active heteroaromatic ?-hydroxy esters useful in the synthesis of epothilone derivatives, to certain compounds used to produce these intermediates, as well as to processes for their production.Type: GrantFiled: January 3, 2005Date of Patent: December 1, 2009Assignee: Bayer Schering Pharma AGInventors: Johannes Platzek, Ludwig Zorn, Bernd Buchmann, Werner Skuballa, Orlin Petrov
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Patent number: 7622467Abstract: The invention provides novel ?2 adrenergic receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with ?2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.Type: GrantFiled: January 11, 2005Date of Patent: November 24, 2009Assignee: Theravance, Inc.Inventors: Robert M. McKinnell, John R. Jacobsen, Sean G. Trapp, Daisuke R. Saito
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Publication number: 20090275588Abstract: The invention relates to novel sulfonamide compounds and their use as orexin receptor antagonists.Type: ApplicationFiled: April 10, 2007Publication date: November 5, 2009Applicant: Actelion Pharmaceuticals Ltd.Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen, Cornella Zumbrunn Acklin
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Publication number: 20090264405Abstract: Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.Type: ApplicationFiled: October 30, 2006Publication date: October 22, 2009Inventors: Amjad Ali, Julianne A. Hunt, Florida Kallashi, Jennifer Kowalchick, Dooseop Kim, Cameron J. Smith, Peter J. Sinclair, Ramzi F. Sweis, Gayle E. Taylor, Christopher F. Thompson, Liya Chen, Nazia Quraishi
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Publication number: 20090258906Abstract: The invention relates to compounds of the formula I in which R1, R2, A, B, X and Y have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.Type: ApplicationFiled: December 18, 2008Publication date: October 15, 2009Applicant: SANOFI-AVENTISInventors: Stephanie HACHTEL, Juergen DEDIO, Josef PERNERSTORFER, Stephen SHIMSHOCK, Carolina LANTER, Raymond KOSLEY
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Publication number: 20090215827Abstract: The invention relates to compounds of the formula I in which R1, R2, X, A, B and Y1 to Y4 have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.Type: ApplicationFiled: December 17, 2008Publication date: August 27, 2009Applicant: SANOFI-AVENTISInventors: Stephanie HACHTEL, Juergen DEDIO, Stephen SHIMSHOCK, Carolina LANTER
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Publication number: 20090211038Abstract: The present disclosure relates to a novel dye composition for the dyeing and/or lightening of keratin materials, such dye comprising a hemicyanin styryl chromophore thiol or disulfide dye of formula (I) or (II): the organic or mineral acid salts thereof, optical isomers and geometric isomers thereof, and the solvates thereof such as hydrates. The present disclosure further relates to a dyeing process with a lightening effect on keratin materials, in particular keratin fibers, including human keratin fibers such as the hair, using said composition. This composition makes it possible to obtain a coloring with a lightening effect which is particularly resistant and visible on dark keratin fibers.Type: ApplicationFiled: September 19, 2008Publication date: August 27, 2009Inventors: Andrew GREAVES, Nicolas DAUBRESSE
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Publication number: 20090202921Abstract: The present invention provides an optical recording composition comprising at least one compound denoted by general formula (I) and a holographic recording medium comprising a recording layer, wherein the recording layer comprises at least one compound denoted by general formula (I). In general formula (I), each of A1 and A2 independently denotes —CR4R5—, —O—, —NR6—, —S—, or —C(?O)—, each of R4, R5, and R6 independently denotes a hydrogen atom or a substituent, R1 denotes a substituent, n denotes an integer ranging from 0 to 4, each of R2 and R3 independently denotes a substituent having a Hammett substituent constant, ?p value, of greater than 0, R2 and R3 do not form a ring structure by bonding together, and at least one from among R1, R2, R3, A1, and A2 comprises at least one polymerizable group.Type: ApplicationFiled: February 10, 2009Publication date: August 13, 2009Applicant: FUJIFILM CorporationInventors: Hiroyuki SUZUKI, Satoru Yamada
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Patent number: 7569688Abstract: Provided is a pharmaceutical composition containing a propane-1,3-dione derivative as the active ingredient, particularly a GnRH receptor antagonist. Also, provided is a propane-1,3-dione derivative having a GnRH antagonistic effect.Type: GrantFiled: June 20, 2005Date of Patent: August 4, 2009Assignee: Astellas Pharma Inc.Inventors: Masaaki Hirano, Eiji Kawaminami, Akira Toyoshima, Hiroyuki Moritomo, Norio Seki, Ryutaro Wakayama, Minoru Okada, Toshiyuki Kusayama
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Patent number: 7553859Abstract: The present invention relates to new Macro-cycles of Formula (I), and their use for the treatment of cancer.Type: GrantFiled: July 15, 2003Date of Patent: June 30, 2009Assignees: Gesellschaft fuer Biotechnologische Forschung mbH (GBF)Inventors: Gerhard Hoefle, Wolfgang Richter
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Publication number: 20090143376Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, chemotherapeutic induced neuropathy, neuropathy associated with an ischemic event, polyglutamine diseases, ocular diseases and/or disorders, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: March 3, 2006Publication date: June 4, 2009Applicant: Sitris Pharmaceuticals, Inc.Inventors: Michael Milburn, Jill Milne, Jean Bemis, Joseph J. Nunes, Roger Xie, Karl D. Nomington, Chi B. Vu
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Publication number: 20090054479Abstract: The present invention is directed to compounds represented by the following structural formula, Formula I: wherein: (a) X is selected from the group consisting of a single bond, O, S, S(O)2 and N; (b) U is an aliphatic linker; (c) Y is selected from the group consisting of C, O, S, NH and a single bond; (d) E is C(R3)(R4)A or A and wherein (i) A is selected from the group consisting of carboxyl, tetrazole, C1-C6 alkylnitrile, carboxamide, sulfonamide and acylsulfonamide; (e) B is selected from the group consisting of S, O, C, and N; (f) Z is selected from the group consisting of N and C; with the proviso that when B is C then Z is N.Type: ApplicationFiled: April 9, 2008Publication date: February 26, 2009Inventors: Scott Eugene Conner, Nathan Bryan Mantlo, Guoxin Zhu
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Publication number: 20090048225Abstract: The present invention provides a novel compound of Formula (I) or a pharmaceutically acceptable salt thereof, having histamine-H3 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 obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.Type: ApplicationFiled: August 15, 2005Publication date: February 19, 2009Inventors: Don Richard Finley, Terry Patrick Finn, Philip Arthur Hipskind, William Joseph Hornback, Cynthia Darshini Jesudason, Takako Takakuwa
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Publication number: 20090048226Abstract: The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1? converting enzyme (“ICE”) inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”), apoptosis-, interferon-? inducing factor-(IGIF), or interferon-?-(“IFN-?”) mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to methods for inhibiting caspase activity and decreasing IGIF production and IFN-? production and methods for treating interleukin-1, apoptosis-, and interferon-?-mediated diseases using the compounds and compositions of this invention.Type: ApplicationFiled: January 22, 2008Publication date: February 19, 2009Inventors: Marion W. Wannamaker, Guy W. Bemis, Paul S. Charifson, David J. Lauffer, Michael D. Mullican, Mark A. Murcko, Keith P. Wilson, James W. Janetka, Robert J. Davies, Anne-Laure Grillot, Zhan Shi, Cornelia J. Forster
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Publication number: 20090030046Abstract: Compounds are provided which are activators of the enzyme glucokinase and thus are useful in treating diabetes and related diseases, which compounds have the structure where Q is and R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related diseases employing the above compounds is also provided.Type: ApplicationFiled: July 25, 2008Publication date: January 29, 2009Inventors: Yan Shi, Peter T.W. Cheng, Ying Wang, Denis E. Ryono
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Patent number: 7482466Abstract: 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: GrantFiled: November 14, 2007Date of Patent: January 27, 2009Assignee: Pharmacyclics, Inc.Inventors: Erik J. Verner, Hon C. Hui
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Publication number: 20080305051Abstract: A compound of the formula I in which X and Y are selected as follows: (i) X is H and Y is selected from the group consisting of (ii) X and Y together form a bivalent radical selected from the group consisting of —O—CH2—O—, —N?CH—O— and —N?CH—S— thus forming together with the carbon atoms to which the radical is attached a 5-membered ring. The compounds have cooling properties and are useful in, for example, foodstuffs, dentifrices and cosmetics.Type: ApplicationFiled: February 23, 2006Publication date: December 11, 2008Inventors: Lucienne Cole, Stefan Michael Furrer, Christophe C. Galopin, Pablo Victor Krawec, Adam Mazur, Jay Patrick Slack
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Patent number: 7456204Abstract: The present invention is directed to novel cyclohexylglycine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: June 10, 2004Date of Patent: November 25, 2008Assignee: Merck & Co., Inc.Inventors: Scott D. Edmondson, Anthony Mastracchio, Emma R. Parmee
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Publication number: 20080255214Abstract: 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: November 14, 2007Publication date: October 16, 2008Applicant: PHARMACYCLICS, INC.Inventors: Erik J. Verner, Hon C. Hui
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Publication number: 20080242868Abstract: The present invention describes a novel process for preparing an epothilone derivative using substituted pyridines and methyltrioxorhenium as catalyst.Type: ApplicationFiled: March 27, 2008Publication date: October 2, 2008Inventors: Johannes PLATZEK, Orlin Petrov, Stephan Pruhs
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Patent number: 7423156Abstract: This invention relates to certain aryl alkyl acid compounds, compositions, and methods for treating or preventing obesity and related diseases.Type: GrantFiled: January 27, 2006Date of Patent: September 9, 2008Assignee: Bayer Pharmaceuticals CorporationInventors: Roger Smith, Ann-Marie Campbell, Philip Coish, Miao Dai, Susan Jenkins, Derek Lowe, Stephen O'Connor, Ning Su, Gan Wang, Mingbao Zhang, Lei Zhu
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Publication number: 20080193700Abstract: The invention relates to novel optical recording media, which comprise particular novel metal chelates and have an excellent recording and playback quality, especially at a wavelength of from 300 to 500 nm.Type: ApplicationFiled: April 25, 2005Publication date: August 14, 2008Applicant: CIBA SPECIALTY CHEMICALS HOLDING INC.Inventors: Heinz Wolleb, Annemarie Wolleb, Frank Bienewald, Beat Schmidhalter, Jean-Luc Budry
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Publication number: 20080167307Abstract: According to the present invention, a compound represented by the following formula (I) having a superior PPAR? agonist action and concurrently showing a hypolipidemic action can be provided, and further, a compound useful as a synthetic intermediate for the compound can be provided.Type: ApplicationFiled: November 4, 2005Publication date: July 10, 2008Applicant: Mitsubishi Phama CorporationInventors: Takashi Tozawa, Osamu Tsuruta, Hiroshi Kitajima, Yoshiyuki Aoki, Naoko Ando, Hiroki Tamakawa