The Additional Hetero Ring Contains Nitrogen As The Only Ring Hetero Atom [e.g., N-(cyclopentylcarbonyl-l-histidyl)-pyrrolidine, Etc.] Patents (Class 548/314.7)
-
Publication number: 20120142689Abstract: In one aspect, the invention relates to compounds of formula I: where Y, R1, R2, n, and Q are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: ApplicationFiled: December 1, 2011Publication date: June 7, 2012Applicant: THERAVANCE, INC.Inventors: Eric L. STANGELAND, Lori Jean VAN ORDEN, Daisuke Roland SAITO
-
Publication number: 20120135997Abstract: The present invention provides, for example, the following compounds as a pharmaceutical composition for treating diseases induced by production, secretion or deposition of amyloid ? proteins. The present invention provides a pharmaceutical composition for suppressing amyloid ? production comprising a compound of the formula: wherein A is a benzene ring, a pyridine ring or a pyrimidine ring, X is sultam, lactam, sulfonamide or the like, C is substituted or unsubstituted imidazolyl, substituted or unsubstituted oxazolyl or the like, R2, R3 and R4 are each independently hydrogen, halogen, hydroxy, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy or the like, its pharmaceutically acceptable salt or a solvate thereof.Type: ApplicationFiled: July 15, 2010Publication date: May 31, 2012Applicant: Shionogi & Co., Ltd.Inventors: Issei Kato, Kazuya Kano
-
Publication number: 20120122889Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-?) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (I)-(I), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF-? induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.Type: ApplicationFiled: December 23, 2009Publication date: May 17, 2012Applicant: President and Fellows of Harvard CollegeInventors: Junying Yuan, Emily S. Hsu
-
Publication number: 20120123115Abstract: Disclosed is an ionic liquid which is stable over a wide potential range and exhibits a high ionic conductivity. The ionic liquid comprises a cyclic guanidine salt represented by the following formula (1): wherein R1 and R2 each is independently an alkyl group or an alkoxyalkyl group, X is a methylene group, an oxygen atom, a sulfur atom, or R3N; R3 is an alkyl group, an alkoxyalkyl group, or an acyl group; l, m, and n each is an integer in the range of 1-6; Y? is a monovalent anion such as (R4SO2)2N?, R4SO3?, R4COO?, BF4?, PF6?, NO3?, (CN)2N?, (CHO)2N?, NCS?, R4OSO3?, R4SO2S?, and a halogen ion. The ionic liquid is useful for a variety of electrolytes, particularly for electrolytes of electrochemical cells.Type: ApplicationFiled: January 25, 2012Publication date: May 17, 2012Inventors: Atsushi Kawada, Aya Tashiro, Toshihiro Kumagai
-
Publication number: 20120111796Abstract: Boron selective ionic liquids and polymeric ionic liquids, methods of making and methods of using the same are disclosed.Type: ApplicationFiled: August 10, 2009Publication date: May 10, 2012Applicant: UNIVERSITY OF TOLEDOInventor: Jared L. Anderson
-
Publication number: 20120115855Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.Type: ApplicationFiled: December 2, 2009Publication date: May 10, 2012Applicant: PRESIDIO PHARMACEUTICALS, INC.Inventors: Leping Li, Min Zhong
-
Publication number: 20120115918Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.Type: ApplicationFiled: December 16, 2011Publication date: May 10, 2012Applicant: ABBOTT LABORATORIESInventors: David A. DeGoey, Allan C. Krueger, Charles W. Hutchins, Warren M. Kati, William A. Carroll
-
Publication number: 20120108635Abstract: The invention relates to novel arylpyrroline compounds of formula (I) which have excellent insecticidal activity and which can thus be used as an insecticide.Type: ApplicationFiled: May 18, 2010Publication date: May 3, 2012Applicant: Bayer CropScience AGInventors: Tetsuya Murata, Yasushi Yoneta, Hidetoshi Kishikawa, Jun Mihara, Daiei Yamazaki, Mamoru Hatazawa, Norio Sasaki, Kei Domon, Eiichi Shimojo, Teruyuki Ichihara, Katsuhiko Shibuya, Masashi Ataka, Ulrich Görgens
-
Patent number: 8163793Abstract: The invention relates to a compound of formula (I) wherein A, R1-R6 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: GrantFiled: April 16, 2010Date of Patent: April 24, 2012Assignee: Hoffman-La Roche Inc.Inventors: Rubén Alvarez Sánchez, David Banner, Simona M. Ceccarelli, Uwe Grether, Wolfgang Haap, Peter Hartman, Guido Hartmann, Hans Hilpert, Holger Kuehne, Harald Mauser, Jean-Marc Plancher
-
Patent number: 8153673Abstract: Compounds of the formula (I) wherein Z is SO2(N6) or N(R7)SO2 or N(R7)SO2N(R6) useful as metalloproteinase inhibitors, especially as inhibitors of MMP12.Type: GrantFiled: January 26, 2010Date of Patent: April 10, 2012Assignee: AstraZeneca ABInventors: Anders Eriksson, Matti Lepistö, Michael Lundkvist, Magnus Munck Af Rosenschöld, Pavol Zlatoidsky
-
Patent number: 8129543Abstract: Disclosed is an ionic liquid which is stable over a wide potential range and exhibits a high ionic conductivity. The ionic liquid comprises a cyclic guanidine salt represented by the following formula (1): wherein R1 and R2 each is independently an alkyl group or an alkoxyalkyl group, X is a methylene group, an oxygen atom, a sulfur atom, or R3N; R3 is an alkyl group, an alkoxyalkyl group, or an acyl group; l, m, and n each is an integer in the range of 1-6; Y? is a monovalent anion such as (R4SO2)2N?, R4SO3?, R4COO?, BF4?, PF6?, NO3?, (CN)2N?, (CHO)2N?, NCS?, R4OSO3?, R4SO2S?, and a halogen ion. The ionic liquid is useful for a variety of electrolytes, particularly for electrolytes of electrochemical cells.Type: GrantFiled: February 26, 2008Date of Patent: March 6, 2012Assignee: Nippon Steel Chemical Co., Ltd.Inventors: Atsushi Kawada, Aya Tashiro, Toshihiro Kumagai
-
Publication number: 20120053165Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.Type: ApplicationFiled: March 2, 2010Publication date: March 1, 2012Applicant: Pfizer Inc.Inventors: Martin Patrick Allen, Christopher William Am Ende, Michael Aaron Brodney, Amy Beth Dounay, Douglas Scott Johnson, Martin Youngjin Pettersson, Jacob Bradley Schwartz, Tuan Phong Tran
-
Patent number: 8124639Abstract: The present invention relates to a series of substituted bicyclic[3.1.0]heteroaryl amides of the Formula I, wherein A, Q, X, Y, Z and R1-R5 groups are defined as in the specification, that exhibit activity as glycine transport inhibitors, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their use for the enhancement of cognition and the treatment of the positive and negative symptoms of schizophrenia and other psychoses in mammals, including humans.Type: GrantFiled: August 30, 2010Date of Patent: February 28, 2012Assignee: Pfizer Inc.Inventors: Stanton F. McHardy, John A. Lowe, III
-
Publication number: 20120039847Abstract: The present invention provides compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: August 12, 2011Publication date: February 16, 2012Inventor: Shu-Hai Zhao
-
Publication number: 20120040948Abstract: The present invention relates to aminoindane derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminoindane derivatives, and the use of such aminoindane derivatives for therapeutic purposes. The aminoindane derivatives are GlyT1 inhibitors.Type: ApplicationFiled: August 10, 2011Publication date: February 16, 2012Applicants: Abbott Laboratories, Abbott GmbH & Co. KGInventors: Frauke POHLKI, Udo Lange, Wilhelm Amberg, Michael Ochse, Berthold Behl, Charles W. Hutchins
-
Publication number: 20120040947Abstract: The present invention relates to tetraline and indane derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such tetraline and indane derivatives, and the use of such tetraline and indane derivatives for therapeutic purposes. The tetraline and indane derivatives are GlyT1 inhibitors.Type: ApplicationFiled: August 10, 2011Publication date: February 16, 2012Applicants: Abbott Laboratories, Abbott GmbH & Co. KGInventors: Frauke Pohlki, Udo Lange, Wilhelm Amberg, Michael Ochse, Berthold Behl, Charles W. Hutchins
-
Publication number: 20120040977Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.Type: ApplicationFiled: February 22, 2010Publication date: February 16, 2012Applicant: PRESIDIO PHARMACEUTICALS, INC.Inventors: Leping Li, Min Zhong
-
Publication number: 20120035351Abstract: Sterically hindered imidazole ligands are described, along with their synthesis, which are capable of coordinating to Group 2 metals, such as: calcium, magnesium, strontium, in an eta-5 coordination mode which permits the formation of monomeric or dimeric volatile complexes. A compound comprising one or more polysubstituted imidazolate anions coordinated to a metal selected from the group consisting of barium, strontium, magnesium, radium or calcium or mixtures thereof. Alternatively, one anion can be substituted with and a second non-imidazolate anion.Type: ApplicationFiled: January 28, 2011Publication date: February 9, 2012Applicant: AIR PRODUCTS AND CHEMICALS, INC.Inventors: John Anthony Thomas Norman, Melanie K. Perez, Moo-Sung Kim
-
Publication number: 20120014914Abstract: The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt, or mixtures thereof, that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are useful as antiviral agents. The invention further relates to pharmaceutically acceptable compositions comprising said compounds either for ex vivo use or for administration to a patient suffering from HCV infection and processes for preparing the compounds. The invention also relates to methods of treating an HCV infection in a patient by administering a pharmaceutical composition comprising a compound of this invention.Type: ApplicationFiled: September 21, 2011Publication date: January 19, 2012Applicant: Vertex Pharmaceuticals IncorporatedInventors: Luc J. Farmer, Robert B. Perni, Govinda Rao Bhisetti, Keith P. Wilson
-
Publication number: 20120010235Abstract: Compounds of formula and enantiomers and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control, amelioration or prevention of cancer.Type: ApplicationFiled: June 30, 2011Publication date: January 12, 2012Inventors: Xin-Jie Chu, Qingjie Ding, Nan Jiang, Jin-Jun Liu, Tina Morgan Ross, Zhuming Zhang
-
Publication number: 20110312996Abstract: The embodiments provide compounds of the general Formulae VI, VII, VIII, IX, X, XI, XII, XIII, XIV, and XV as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.Type: ApplicationFiled: May 16, 2011Publication date: December 22, 2011Applicant: InterMune, Inc.Inventors: Brad Buckman, John B. Nicholas, Vladimir Serebryany, Scott D. Seiwert
-
Publication number: 20110306615Abstract: According to the present invention, a compound represented by formula (I): wherein Q is: A is a hydrogen atom, a halogen atom, —ORa or a C1-4 alkyl group which may be substituted by one or more halogen atoms; E is independently selected from a C1-6 alkyl group; m is selected from integers from 0 to 3; R2 and R3 are independently selected from a C1-6 alkyl group; X1 and X2 are independently selected from O and S; Y is selected from an arylene group and a divalent 5- or 6-membered monocyclic or 8- to 10-membered condensed heterocyclic group, wherein the arylene group and the heterocyclic group may be substituted by 1 to 3 substituents independently selected from E1; E1 is independently selected from a hydroxyl group, a halogen atom, a C1-4 alkyl group, a cyano group, a C1-4 alkoky group, a carbamoyl group, a C1-4 alkylcarbamoyl group, a di(C1-4 alkyl)carbamoyl group, an amino group, a C1-4 alkylamino group, a di(C1-4 alkylamino group, a sulfamoyl group, a C1-4 alkylsulfamoyl group and a di(C1-4 alkyl)suType: ApplicationFiled: September 9, 2005Publication date: December 15, 2011Applicant: CHUGAI SEIYAKU KABUSHIKI KAISHAInventors: Kazutaka Tachibana, Haruhiko Sato, Masateru Ohta, Mitsuaki Nakamura, Takuya Shiraishi, Hitoshi Yoshino, Takashi Emura, Akie Honma, Etsuro Onuma, Hiromitsu Kawata, Kenji Taniguchi
-
Publication number: 20110301174Abstract: The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R1 is a nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle, the nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle optionally has substituent(s), R2 is an optionally substituted C6-14 aryl group, an optionally substituted thienyl group or an optionally substituted pyridyl group, R3 and R4 are each a hydrogen atom, or one of R3 and R4 is a hydrogen atom and the other is an optionally substituted lower alkyl pup, an acyl group, a halogen atom, a cyano group or a nitro group, and R5 is an alkyl group or a salt thereof.Type: ApplicationFiled: June 8, 2011Publication date: December 8, 2011Applicant: Takeda Pharmaceutical Company LimitedInventors: Masahiro Kajino, Atsushi Hasuoka, Haruyuki Nishida
-
Publication number: 20110301173Abstract: The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R1 is a nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle, the nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle optionally has substituent(s), R2 is an optionally substituted C6-14 aryl group, an optionally substituted thienyl group or an optionally substituted pyridyl group, R3 and R4 are each a hydrogen atom, or one of R3 and R4 is a hydrogen atom and the other is an optionally substituted lower alkyl group, an acyl group, a halogen atom, a cyano group or a nitro group, and R5 is an alkyl group or a salt thereof.Type: ApplicationFiled: June 8, 2011Publication date: December 8, 2011Applicant: Takeda Pharmaceutical Company LimitedInventors: Masahiro Kajino, Atsushi Hasuoka, Haruyuki Nishida
-
Publication number: 20110294819Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS5A protein.Type: ApplicationFiled: December 21, 2010Publication date: December 1, 2011Inventors: Omar D. Lopez, Denis R. St. Laurent, Jason Goodrich, Jeffrey Lee Romine, Michael Serrano-Wu, Fukang Yang, Ramesh Kakarla, Xuejie Yang, Yuping Qiu, Lawrence B. Snyder
-
Publication number: 20110281875Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula (I).Type: ApplicationFiled: July 8, 2011Publication date: November 17, 2011Inventors: Mark G. PALERMO, Sushil Kumar SHARMA, Christopher STRAUB, Run-Ming WANG, Leigh ZAWEL, Yanlin ZHANG, Zhuoliang CHEN, Yaping WANG, Fan YANG, Wojciech WRONA, Gang LIU, Mark G. CHAREST, Feng HE
-
Publication number: 20110275657Abstract: Melanocortin receptor modulators, processes for preparing them and use thereof in human medicine and cosmetics are described. Melanocortin receptor modulators corresponding to formula (I): compositions containing them, processes for their preparation and their use in pharmaceutical or cosmetic compositions are also described.Type: ApplicationFiled: November 4, 2009Publication date: November 10, 2011Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Claire Bouix-Peter, Itaru Suzuki, Isabelle Pelisson, Pascal Collette, Samuel Tabet, Guillaume Lafitte
-
Publication number: 20110274638Abstract: Compounds derived from oxoazetidine corresponding to general formula (I) compositions containing same, processes for their preparation and their use in pharmaceutical or cosmetic compositions are described.Type: ApplicationFiled: November 4, 2009Publication date: November 10, 2011Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Claire Bouix-Peter, Itaru Suzuki, Nicolas Rodeville, Pascale Mauvais, Jean-Claude Pascal
-
Publication number: 20110269742Abstract: Disclosed are Serotonin 5-HT2B receptor inhibitors of the formula I. Also disclosed are methods of making and methods of using these compounds.Type: ApplicationFiled: December 14, 2009Publication date: November 3, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Derek Cogan, Neil Moss, Christopher Ronald Sarko, Samantha Jayne Bamford, Pui Leng Loke, Spencer Charles R. Napier, Heather Tye, Mark Whittaker
-
Publication number: 20110263558Abstract: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.Type: ApplicationFiled: March 15, 2011Publication date: October 27, 2011Applicant: EXELIXIS, INC.Inventors: Naing Aay, Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Simona Costanzo, Jeffry Kimo Curtis, Steven Charles DeFina, Larisa Dubenko, Anagha Abhijit Joshi, Abigail R. Kennedy, Angie Inyoung Kim, Elena S. Koltun, Jean-Claire Limun Manalo, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang
-
Publication number: 20110251168Abstract: The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.Type: ApplicationFiled: June 16, 2011Publication date: October 13, 2011Inventors: Chu-Biao Xue, Brian W. Metcalf, Hao Feng, Ganfeng Cao, Taisheng Huang, Changsheng Zheng, Darius J. Robinson, Amy Qi Han
-
Publication number: 20110237579Abstract: The invention relates to non-macrocyclic, non-peptidic, substituted heterocyclic compounds useful for inhibiting hepatitis C virus (“HCV”) replication, particularly functions of the non-structural 5A (“NS5A”) protein of HCVType: ApplicationFiled: December 2, 2009Publication date: September 29, 2011Applicant: PRESIDIO PHARMACEUTICALS, INC.Inventors: Leping Li, Min Zhong
-
Publication number: 20110230533Abstract: Embodiments disclosed herein relate to new imidazolidinedione derivatives, methods of making these compounds, and methods of using the same to prevent, treat, or inhibit malaria in a subject.Type: ApplicationFiled: October 2, 2009Publication date: September 22, 2011Inventors: Ai Jeng Lin, Michael P. Kozar, Michael T. O'Neil, Alan J. Magill, David L. Saunders
-
Patent number: 8022072Abstract: An azolylmethylidenehydrazine derivative represented by the formula (I) wherein Ar is an aryl group optionally having substituent(s) or a heteroaryl group optionally having substituent(s), R1 and R2 are the same or different and each is an alkyl group, a cycloalkyl group, an aralkyl group optionally having substituent(s), an aryl group optionally having substituent(s), a heteroarylalkyl group optionally having substituent(s), or R1 and R2 are bonded to each other to form a nitrogen-containing heterocyclic group optionally having substituent(s), and X is CH or a nitrogen atom, or a pharmacologically acceptable salt thereof is useful as a medicament, particularly as an antifungal agent, or an anti-inflammatory agent or an antiallergic agent.Type: GrantFiled: June 17, 2008Date of Patent: September 20, 2011Assignee: Kaken Pharmaceutical Co., Ltd.Inventors: Hironobu Ogura, Yoshiyuki Tatsumi, Yuji Fukamizu
-
Patent number: 7998959Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1 and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 such as obesity and diabetes.Type: GrantFiled: January 11, 2007Date of Patent: August 16, 2011Assignee: Incyte CorporationInventors: Wenqing Yao, David M. Burns, Lihua Chen, Jincong Zhuo, Chunhong He
-
Publication number: 20110183961Abstract: The invention relates to compounds of the formula (I) where: R is a (C1-C6)alkyl group, a halo(C1-C6)alkyl group; R1 is a hydrogen atom; R2 is a heterocyclic group bound by a carbon atom, a heterocyclic-(C1-C4)alkyl group, said groups being optionally substituted; R3 and R4 represent independently from each other an optionally substituted phenyl group; X is a hydrogen atom, a halogen, a cyano, a (C1-C6)alkyl group, a halo(C1-C6)alkyl group, a (C1-C6)alkoxy group, a halo(C1-C6)alkoxy group or a (C1-C6)alkylS(0)p group; and p is 0 to 2. The invention also relates to a method for preparing same and to the therapeutic application thereof.Type: ApplicationFiled: August 13, 2009Publication date: July 28, 2011Applicant: SANOFI-AVENTISInventors: Florian Auger, Patrick Bernardelli, Jean-François Sabuco, Corinne Terrier
-
Publication number: 20110178060Abstract: The present invention relates to a compound represented by the formula wherein ring A is a nitrogen-containing heterocycle; ring B is an aromatic ring optionally having substituent(s); ring D is an aromatic ring optionally having substituent(s); L is a group represented by the formula R2, R3, R4a and R4b are each independently a hydrogen atom, an optionally halogenated C1-6 alkyl group or an optionally halogenated C3-6 cycloalkyl group, or R2 and R3 are optionally bonded via an alkylene chain or an alkenylene chain, or R4a and R4b are optionally bonded via an alkylene chain or an alkenylene chain; R1 is a hydrogen atom or a substituent; m and n are each independently an integer of 0 to 5; m+n is an integer of 2 to 5; and is a single bond or double bond, or a salt thereof; and the like.Type: ApplicationFiled: September 18, 2009Publication date: July 21, 2011Inventors: Junya Shirai, Hideyuki Sugiyama, Taku Kamei, Hironobu Maezaki
-
Publication number: 20110160192Abstract: Compounds of formula (I): Z?-CO-A-B—NH-Z (I) wherein: Z is H or an amino protecting group; Z? is OH, a protected or activated hydroxyl group or Cl; A is an optionally substituted C5-6 arylene group; and B is an optionally substituted C5-6 arylene group.Type: ApplicationFiled: March 7, 2011Publication date: June 30, 2011Applicant: SPIROGEN LIMITEDInventors: Philip Wilson Howard, Geoffrey Wells
-
Patent number: 7968591Abstract: 1,3-disubstituted 4-methyl-1H-pyrrole-2-carboxamides corresponding to formula I methods for their production, pharmaceutical compositions containing them, and the use thereof for noradrenalin receptor regulation, particularly for inhibiting noradrenalin reuptake, and/or for 5-HT receptor regulation, particularly for inhibiting 5-hydroxy tryptophan reuptake, and/or for opioid receptor regulation and/or for batrachotoxin (BTX) receptor regulation and/or for treating or inhibiting pain and other conditions.Type: GrantFiled: December 9, 2008Date of Patent: June 28, 2011Assignee: Gruenenthal GmbHInventors: Stefan Oberboersch, Bernd Sundermann, Corinna Sundermann, Edward Bijsterveld, Hagen-Heinrich Hennies
-
Publication number: 20110152236Abstract: The invention relates to compounds of the formula (I) where: R is a (C1-C6)alkyl group, a halo(C1-C6)alkyl group; R1 is a hydrogen atom; R2 is a heteroaromatic group or a heteroaromatic(C1-C4)alkyl group, said groups being optionally substituted; R3 and R4 represent independently from each other an optionally substituted phenyl group; Y is a hydrogen atom, a halogen, a cyano, a (C1-C6)alkyl group, a halo(C1-C6)alkyl group, a (C1-C6)alkoxy group, a halo(C1-C6)alkoxy group or a (C1-C6)alkylS(O)p group; and p is 0 to 2. Said compounds can be in the form— of a base or a salt for addition to an acid. The invention also relates to a method for preparing same and to the therapeutic application thereof.Type: ApplicationFiled: August 13, 2009Publication date: June 23, 2011Applicant: SANOFI-AVENTISInventors: Patrick Bernardelli, Jean-Francois Sabuco, Corinne Terrier
-
Publication number: 20110144110Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.Type: ApplicationFiled: August 14, 2009Publication date: June 16, 2011Applicant: N30 PHARMACEUTICALS, LLCInventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
-
Publication number: 20110142856Abstract: The present invention relates to a compound represented by formula (I-0): wherein symbols in formula have the same meanings as described in the present specification, a salt thereof, an N-oxide thereof or a solvate thereof or a prodrug thereof, and medical use thereof. The compound of the present invention has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoidarthritis, arthritis, retinopathy, pulmonary fibrosis, transplanted organ rejection, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiovascular disease, metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.), or an agent for regeneration therapy.Type: ApplicationFiled: February 15, 2011Publication date: June 16, 2011Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Masaya KOKUBO, Yoshikazu Takaoka, Shiro Shibayama
-
Publication number: 20110136875Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.Type: ApplicationFiled: August 14, 2009Publication date: June 9, 2011Applicant: N30 PHARMACEUTICALS, LLCInventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
-
Patent number: 7951819Abstract: The present invention pertains to certain imidazo[4,5-b]pyridin-2-one and oxazolo[4,5 b]pyridin-2-one compounds and analogs thereof, which, inter alia, inhibit RAF (e.g., B RAF) activity, inhibit cell proliferation, treat cancer, etc. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., B-RAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and conditions that are ameliorated by the inhibition of RAF, RTK, etc., proliferative conditions such as cancer (e.g., colorectal cancer, melanoma), etc.Type: GrantFiled: April 26, 2007Date of Patent: May 31, 2011Assignees: Cancer Research Technology Limited, The Institute of Cancer Research: Royal Cancer Hospital, Astex Therapeutics LimitedInventors: Dan Niculescu-Duvaz, Caroline Joy Springer, Richard Malcolm Marais, Harmen Dijkstra, Delphine Menard, Ion Niculescu-Duvaz, Lawrence Davies, Arnaud Nourry
-
Patent number: 7951808Abstract: Imidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor expression, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.Type: GrantFiled: February 8, 2007Date of Patent: May 31, 2011Assignee: Janssen Pharmaceutica NVInventors: Daniel J. Buzard, James P. Edwards, David E. Kindrachuk, Jennifer D. Venable
-
Publication number: 20110112154Abstract: 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: January 18, 2011Publication date: May 12, 2011Inventors: Bradley Paul MORGAN, Fady Malik, Erica Anne Kraynack, Alexander Ramon Muci, Xiangping Qian, David J. Morgans, JR.
-
Publication number: 20110092553Abstract: The present invention provides azole derivatives of Formula (I), methods of their preparation, pharmaceutical compositions comprising the compounds of Formula (I), and their use in treating human or animal disorders. The compounds of the invention can be useful as inhibitors of protein tyrosine phosphatases and thus can be useful for the management, treatment, control, or the adjunct treatment of diseases mediated by PTPase activity. Such diseases include Type I diabetes and Type II diabetes.Type: ApplicationFiled: November 19, 2010Publication date: April 21, 2011Applicant: TransTech Pharma, Inc.Inventors: Adnan M.M. Mjalli, Dharma R. Polisetti, Govindan Subramanian, James C. Quada, JR., Murty N. Arimilli, Ravindra R. Yarragunta, Robert C. Andrews, Rongyuan Xie
-
Publication number: 20110086860Abstract: A compound represented by Formula (I) is provided: wherein Ar1 represents an imidazolyl group which may be substituted with 1 to 3 substituents; Ar2 represents a phenyl group which may be substituted with 1 to 3 substituents; X1 represents (1) —C?C— or (2) a double bond etc., which may be substituted; R1 and R2 represent, for example, a C1-6 alkyl group which may be substituted, or a pharmacologically acceptable salt thereof and to the use thereof as pharmaceutical agents.Type: ApplicationFiled: December 21, 2010Publication date: April 14, 2011Inventors: Teiji KIMURA, Koki Kawano, Eriko Doi, Noritaka Kitazawa, Kogyoku Shin, Takehiko Miyagawa, Toshihiko Kaneko, Koichi Ito, Mamoru Takaishi, Takeo Sasaki, Hiroaki Hagiwara
-
Publication number: 20110082172Abstract: Pyrrolidinone carboxamide compounds are provided that are useful for inhibiting the binding of ligands to the ChemR23 receptor.Type: ApplicationFiled: September 21, 2010Publication date: April 7, 2011Applicant: ChemoCentryx, Inc.Inventors: Trevor T. Charvat, Hiufung Chu, Antoni Krasinski, Christopher W. Lange, Manmohan Reddy Leleti, Jay P. Powers, Sreenivas Punna, Timothy J. Sullivan, Solomon Ungashe
-
Publication number: 20110071125Abstract: This invention relates to novel substituted phenylamino-benzene compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: May 9, 2008Publication date: March 24, 2011Inventors: Joachim Rudolph, Jaques Dumas, Li Yingfu, Daniel Auclair, Mario Lobell, Marion Hitchcock, Ingo Hartung, Marcus Koppitz, Dominic Brittain, Florian Puehler, Kirstin Petersen, Judith Guenther, Benjamin Bader