Ring Nitrogen In The Polycyclo Ring System Patents (Class 544/80)
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Publication number: 20120088763Abstract: Compounds of formula (I) are inhibitors of p38 MAP kinase, useful as anti-inflammatory agents in the treatment of inter alia, diseases of the respiratory tract wherein; R1 is C1-C6 alkyl, C3-C6 cycloalkyl, phenyl which is optionally substituted, 5- or 6 membered monocyclic heteroaryl which is optionally substituted, or a radical of formula (II) wherein n is 1 or 2, and R3 and R4 are independently H or C1-C6 alkyl, or R3 and R4 taken together with the nitrogen to which they are attached form a 6-membered heterocyclic ring optionally containing a further heteroatom selected from N and O; Y is —O— or —S(O)p— wherein p is 0, 1 or 2; A is an optionally substituted divalent arylene radical, or a mono- or bicyclic heteroarylene radical, or a C3-C6 divalent cycloalkylene radical having 5 or 6 ring atoms, or a piperidinylene radical wherein the ring nitrogen is linked to R2NHC(?O)W—; W is a bond, —NH— or —C(RA)(RB), wherein RA and RB are independently H, methyl, ethyl, amino, hydroxyl or halo; and R2 is a radical as dType: ApplicationFiled: February 16, 2010Publication date: April 12, 2012Applicant: CHIESI FARMACEUTICI S.p.A.Inventors: Harry Finch, John Montana, Monique Bodil Van Niel, Chi-Kit Woo, Jamie Knight, Bohdan Waszkowycz
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Publication number: 20120076756Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: October 4, 2011Publication date: March 29, 2012Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
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Publication number: 20120065169Abstract: Oligonucleotide analogues comprising modified intersubunit linkages and/or modified 3? and/or 5?-end groups are provided. The disclosed compounds are useful for the treatment of diseases where inhibition of protein expression or correction of aberrant mRNA splice products produces beneficial therapeutic effects.Type: ApplicationFiled: May 27, 2011Publication date: March 15, 2012Inventors: Gunnar J. Hanson, Alexander Charles Rudolph, Bao Zhong Cai, Ming Zhou, Dwight D. Weller
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Publication number: 20120058984Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular Itk activity.Type: ApplicationFiled: March 15, 2010Publication date: March 8, 2012Inventors: Catherine Mary Alder, Ian Robert Baldwin, Nicholas Paul Barton, Amanda Jennifer Campbell, Aurelie Cecile Champigny, John David Harling, Aoife Caitriona Maxwell, Juliet Kay Simpson, Ian Edward David Smith, Christopher John Tame, Caroline Wilson, James Michael Woolven
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Publication number: 20120046270Abstract: The present invention encompasses compounds of general formula (1), wherein the groups R1 to R4, X1, X2, X3, X4, X5, Q, L1 and L2 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, as well as pharmaceutical preparations and formulations of these compounds.Type: ApplicationFiled: February 17, 2010Publication date: February 23, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Peter Ettmayer, Andreas Mantoulidis, Steffen Steurer
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Publication number: 20120020920Abstract: The present invention relates to a fused ring compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable a salt thereof, and a hepatitis C virus (HCV) polymerase inhibitor and a therapeutic agent for hepatitis C containing this compound. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.Type: ApplicationFiled: February 24, 2011Publication date: January 26, 2012Applicant: Japan Tobacco Inc.Inventors: Ryo Mizojiri, Shintaro Hirashima, Takahiro Oka, Kenta Aoki, Satoru Noji, Izuru Ando, Toshihiro Sato, Yasushi Niwa
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Publication number: 20120004221Abstract: Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; Alk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (—O—), thioether (—S—) or amino (—NR)— link, wherein R is hydrogen, —CN or C1-C3 alkyl; X is —C(?O)NR6—, —S(O)NR6—, —C(?O)O— or —S(?O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, -Cyc, or —(C1-C3 alkyl)-Cyc wherein Cyc is optionally substituted monocyclic carbocyclic or heterocyclic having 3-7 ring atoms; Z is N; R2 and R3 are as defined in the description.Type: ApplicationFiled: June 7, 2011Publication date: January 5, 2012Applicant: Biota Europe LimitedInventors: David John Haydon, Lloyd George Czaplewski, Nicholas John Palmer, Dale Robert Mitchell, John Frederick Atherall, Christopher Richard Steele, Tamara Ladduwahetty
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Publication number: 20110294779Abstract: The invention is concerned with novel imidazopyridine derivatives of formula (I) wherein R1, R2, R3, R4, R5 and A are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used for the treatment of various diseases, including central nervous system disorders such as Alzheimer's disease, Parkinson's disease, and schizophrenia.Type: ApplicationFiled: June 2, 2011Publication date: December 1, 2011Inventors: DANIELA ALBERATI, RUBÉN ALVAREZ SÁNCHEZ, KONRAD BLEICHER, ALEXANDER FLOHR, KATRIN GROEBKE ZBINDEN, MATTHIAS KOERNER, BERND KUHN, JENS-UWE PETERS, MARKUS RUDOLPH
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Publication number: 20110294781Abstract: The present invention has searched for a variety of compounds which show IL-12/IL-23 production-inhibitory activities and herein provides a pharmaceutical composition and an agent for preventing or treating IL-12/IL-23 excess production-related diseases, which comprise the compound.Type: ApplicationFiled: June 27, 2011Publication date: December 1, 2011Applicant: AJINOMOTO CO., INC.Inventors: Takashi YAMAMOTO, Ayatoshi Andou, Nobuhiko Hayakawa, Masatsugu Noguchi, Kanna Kuribayashi, Agung Eviryanti, Ryohei Yokoyama, Shunsuke Fukuda, Toshihiko Sugiura, Shunsuke Kageyama, Yoichiro Shima, Misato Noguchi
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Publication number: 20110269741Abstract: Described herein are novel enzyme inhibitors. In some embodiments the enzyme inhibitors are integrase inhibitors, particularly HIV integrase inhibitors. Also described herein are compositions containing them and methods of using them. Thus, the compounds and compositions described herein are useful for the in vitro and in vivo inhibition of HIV integrase as a method of treating or preventing HIV, AIDS or related disorders.Type: ApplicationFiled: March 28, 2011Publication date: November 3, 2011Applicant: Ardea Biosciences, Inc.Inventors: Huanming CHEN, Jianlin SONG, Jean-Michel VERNIER, Anthony B. PINKERTON, Johnny Y. NAGASAWA
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Publication number: 20110269752Abstract: The present invention relates to novel imidazo[1,2-b]pyridazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which are useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.Type: ApplicationFiled: April 28, 2011Publication date: November 3, 2011Inventors: Joaquin Pastor-Fernández, José Manuel Bartolomé-Nebreda, Gregor James Macdonald, Susana Conde-Ceide, Óscar Delgado-González, Greta Constantia Peter Vanhoof, Michiel Luc Maria Van Gool, María Luz Martin-Martín, Sergio-Alvar Alonso-de Diego, Kelly Ann Swinney, Carina Leys, Johan Erwin Edmond Weerts, Stijn Wuyts
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Publication number: 20110257170Abstract: This invention relates to compounds of Formula (I) as Pi3k inhibitors for treating autoimmune diseases, inflammatory disorders, multiple sclerosis and other diseases like cancers.Type: ApplicationFiled: September 30, 2009Publication date: October 20, 2011Applicant: MERCK SERONO SAInventors: Vincent Pomel, Pascale Gaillard, Gwenaelle Desforges, Anna Quattropani, Cyril Montagne
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Publication number: 20110212053Abstract: Provided are compounds according to Formula (I): or stereoisomer, prodrug, polymorph, or pharmaceutically acceptable salt forms thereof, wherein X, Y, R1, R6, R7, and R8 are as defined, and which compounds are effective inhibitors of PI3-kinase and/or other medically and clinically relevant kinases. Also provided are pharmaceutical compositions and methods of using the compounds and compositions as PI3-kinase and kinase inhibitors. More particularly, the compounds of the invention provide treatments and therapeutics for human diseases regulated by, or associated with, the activity of, PI3-kinases and/or protein kinases, or mutant or variant forms thereof.Type: ApplicationFiled: June 19, 2009Publication date: September 1, 2011Inventors: Dapeng QIAN, Amy Qi Han, Mark Hamilton, Eric Wang
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Publication number: 20110124638Abstract: There is provided a compound of formula I: , or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.Type: ApplicationFiled: January 26, 2011Publication date: May 26, 2011Applicant: KUDOS PHARMACEUTICALS LIMITEDInventors: Heather Mary Ellen Duggan, Karine Malagu, Frederic Georges Marie Leroux, Niall Morrisson Barr Martin, Keith Allan Menear, Graeme Cameron Murray Smith
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Publication number: 20110105457Abstract: The purpose of the present invention is to provide a compound or a pharmaceutically acceptable salt thereof which inhibits the activity of PI3K to regulate many biological processes including the growth, differentiation, survival, proliferation, migration, metabolism, and the like of cells and is therefore useful for the prevention/treatment of diseases including inflammatory diseases, arteriosclerosis, vascular/circulatory diseases, cancer/tumors, immune system diseases, cell proliferative diseases, infectious diseases, and the like. This was achieved by providing a substituted 2-amino-5,6-nitrogenated fused ring compound shown in the present specification, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: April 16, 2009Publication date: May 5, 2011Inventors: Daisuke Taniyama, Kazuya Kano, Kazuya Okamoto, Masahiko Fujioka, Yasunori Mitsuoka
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Publication number: 20110105490Abstract: The present invention is directed to novel 2,3-dihydro-1H-isoindol-1-imine derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the thrombin PAR-1 receptor antagonists.Type: ApplicationFiled: October 28, 2010Publication date: May 5, 2011Inventors: Han-Cheng Zhang, Bruce Maryanoff, Kimberly White, Stephen C. Yabut, Hong Ye, Cailin Chen
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Publication number: 20110083984Abstract: This invention relates to novel 2,3-dihydroimidazo[1,2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: December 5, 2007Publication date: April 14, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Martin Hentemann, Jill Wood, William Scott, Martin Michels, Ann-Marie Campbell, Ann-Marie Bullion, Bruce R. Rowley, Aniko Redman
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Publication number: 20110065687Abstract: This application relates to certain novel polycyclic compounds that interact with quadruplex-forming regions of polynucleotides and thereby inhibit translation of genetic information into polypeptides. These compounds can thus provide anticancer and antibacterial and antiviral effects. The invention includes novel compounds and pharmaceutical compositions, and methods of using them to treat cancer and other conditions.Type: ApplicationFiled: April 17, 2008Publication date: March 17, 2011Inventors: Michael Schwaebe, Johnny Yasuo Nagasawa, Mustapha Haddach
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Publication number: 20110003790Abstract: The invention provides a class of compounds of Formula (I), pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly Syk, ZAP70, KDR, FMS, FLT3, c-Kit, RET, TrkA, TrkB, TrkC, IGR-IR, AIk, c-FMS, or combinations thereof.Type: ApplicationFiled: January 27, 2009Publication date: January 6, 2011Applicant: IRM LLCInventors: Qiang Ding, Yahua Liu, Xu Wu, Qihui Jin, Jianwei Che, S. Frank Yan
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Publication number: 20110003798Abstract: The invention provides a novel class of 2,7-naphthyridin derivatives; pharmaceutical compositions comprising such compounds and methods of using such compounds to treat o prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly Syk, ZAP70, KDR, FMS, FLT*, c-Kit, RET, TrkA, TrkB, TrkC-GR-1R, Alk, c-FMS or combinations thereof.Type: ApplicationFiled: January 27, 2009Publication date: January 6, 2011Applicant: IRM LLCInventors: Barun Okram, Tetsuo Uno, Qiang Ding, Yahua Liu, Yunho Jin, Qihui Jin, Xu Wu, Jianwei Che, S. Frank Yan, Xueshi Hao
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Publication number: 20100331293Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjogren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute LymphobType: ApplicationFiled: June 25, 2010Publication date: December 30, 2010Applicant: AMGEN INC.Inventors: Timothy D. Cushing, Paul John Dransfield, Felix Gonzalez Lopez De Turiso, Michael G. Johnson, Todd Kohn, Vatee Pattaropong, Jillian L. Simard
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Publication number: 20100305084Abstract: Formula I (Ia and Ib) compounds wherein (i) X1 is N and X2 is S, (ii) X1 is CR7 and X2 is S, (iii) X1 is N and X2 is NR2, (iv) X1 is CR7 and X2 is O, or (v) X1 is CR7 and X2 is NR2, including stereoisomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: May 26, 2010Publication date: December 2, 2010Inventors: Georgette Castanedo, David Goldstein, Rama Kondru, Matthew Lucas, Wylie Palmer, Stephen Price, Brian Safina, Pascal Pierre Alexandre Savy, Eileen Mary Seward, Daniel P. Sutherlin, Zachary K. Sweeney
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Publication number: 20100305096Abstract: Formula I (Ia and Ib) compounds wherein (i) X1 is N and X2 is S, (ii) X1 is CR7 and X2 is S, (iii) X1 is N and X2 is NR2, or (iv) X1 is CR7 and X2 is O, including stereoisomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: May 26, 2010Publication date: December 2, 2010Inventors: Georgette Castanedo, Bryan Chan, David Goldstein, Rama Kondru, Matthew Lucas, Wylie Palmer, Stephen Price, Brian Safina, Pascal Pierre Alexandre Savy, Eileen Mary Seward, Daniel P. Sutherlin, Zachary K. Sweeney
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Publication number: 20100266543Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: February 9, 2010Publication date: October 21, 2010Inventors: Yao-Ling Qiu, Ce Wang, Lu Ying, Xiaowen Peng, Yat Sun Or
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Publication number: 20100267700Abstract: A novel method for immunosuppressive in a mammal suffering from an immune disease, including administering to the mammal a therapeutically effective amount of a heterocyclic compound represented by the general formula (I) (wherein X or other variables are as defined in the specification) or a pharmaceutically acceptable salt thereof is disclosed. A novel heterocyclic compound represented by the general formula (II) (wherein X or other variables are as defined in the specification) or a pharmaceutically acceptable salt thereof is also disclosed.Type: ApplicationFiled: May 24, 2010Publication date: October 21, 2010Applicant: ZENYAKU KOGYO KABUSHIKI KAISHAInventors: Kazuhiko Haruta, Shinichi Yaguchi, Toshiyuki Matsuno, Yoshio Tsuchida, Tetsuo Watanabe, Kimitomo Yoshioka, Ryogo Yui
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Publication number: 20100249063Abstract: [Problems] The object is to improve the absorbability of a heterocyclic compound including s-triazine and a pyrimidine derivative in vitro. [Means for Solving Problems] Disclosed is, for example, an amorphous body of a heterocyclic compound as represented by the general formula (I) [wherein each of R's and others is as defined in the description] including s-triazine and a pyrimidine derivative, or a hydrate, a solvate or a pharmaceutically acceptable salt of the heterocyclic compound. Also disclosed is a process for producing the amorphous body. Further disclosed are: a solid dispersion comprising the amorphous body; and a medicinal preparation comprising the solid dispersion.Type: ApplicationFiled: November 21, 2008Publication date: September 30, 2010Applicant: Zenyaku Kogyo Kabushiki KaishaInventors: Tadaaki Sugama, Nobuhiro Ishihara, Yoshiharu Tanaka, Masayuki Takahashi, Shinichi Yaguchi, Tetsuo Watanabe
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Publication number: 20100249099Abstract: Provided herein are pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides, e.g., compounds of Formulae IA, IB, and IC, and their pharmaceutical compositions, preparation, and use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs.Type: ApplicationFiled: March 26, 2010Publication date: September 30, 2010Applicant: Pathway Therapeutics LimitedInventors: Gordon William Rewcastle, Swarnalatha Akuratiya Gamage, Jack Urquhart Flanagan, Anna Claire Giddens, Kit Yee Tsang
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Publication number: 20100240646Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R1, R2, R3, R4, R5, R6, X and Z are as described in the specification.Type: ApplicationFiled: June 3, 2010Publication date: September 23, 2010Inventors: Alaric Dyckman, John Hynes, Katerina Leftheris, Chunjian Liu, Stephen T. Wrobleski
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Publication number: 20100233122Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: March 1, 2010Publication date: September 16, 2010Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
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Publication number: 20100216767Abstract: The invention provides novel compounds that are inhibitors of PDK1. Also provided are pharmaceutical compositions including the compounds, and methods of treating proliferative diseases, such as cancers, with the compounds or compositions.Type: ApplicationFiled: December 20, 2007Publication date: August 26, 2010Inventors: Mina Aikawa, Payman Amiri, Steven Bashman, Jeffrey Dove, Rama Jain, Xiaodong Lin, Jeremy Murray, Savithri Ramurthy, Alice Rico, Wei Shu, Sharadha Subramanian, Xiaojing Michael Wang, Robert L. Warne, Yasheen Zhou
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Patent number: 7727985Abstract: This invention provides beta-carboline compounds of formula I: wherein Ring A is a substituted pyridinyl, pyrimidinyl, morpholinyl, piperidinyl, piperazinyl, pyrrolidinyl, pyranyl, tetrahydrofuranyl, cyclohexyl, cyclopentyl or thiomorpholinyl ring and R1, R2 and R3 are as described in the specification. The compounds are IKK-2 inhibitors that are useful for treating IKK-2-mediated diseases such as inflammatory diseases and cancer.Type: GrantFiled: April 9, 2004Date of Patent: June 1, 2010Assignee: Millennium Pharmaceuticals, Inc.Inventors: Michael E. Hepperle, Julie Fields Liu, Francois Soucy, Yingchun Ye, Robert S. Murray, Raman Prakash, Jeremy D. Little, Alfredo Castro, Hormoz Mazdiyasni, Paul E. Fleming, Dominic Reynolds
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Patent number: 7718653Abstract: A compound of formula (I) where one of A1, A2 or A3 is N, and the others are independently selected from CH or N; ring B is a fused 5 or 6-membered carbocyclic or heterocyclic ring which is optionally substituted as defined in the specification, and R1, R2, R3, R4, and n are as defined in the specification. The compounds are inhibitors of EphB4 or EphA2 and therefore may be useful in pharmaceutical compositions for the treatment of conditions such as cancer.Type: GrantFiled: July 16, 2008Date of Patent: May 18, 2010Assignee: AstraZeneca ABInventors: Bernard Christophe Barlaam, Richard Ducray, Jason Grant Kettle
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Patent number: 7696202Abstract: The invention relates to heterocyclic compounds, compositions including the compounds and methods of using and methods of making thereof. The compounds (and compositions) are useful, inter alia, in modulating IL-12 production and processes mediated by IL-12.Type: GrantFiled: November 10, 2005Date of Patent: April 13, 2010Assignee: Synta Pharmaceuticals Corp.Inventors: Lijun Sun, Elena Kostik, Teresa Przewloka, Howard P. Ng, Dinesh Chimmanamada, Zachary Demko
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Publication number: 20100069380Abstract: Provided herein are compounds that modulate the activity of a bacterial peptidyl tRNA hydrolase, including compositions and dosage forms comprising the compounds. Further provided herein are methods for screening and identifying compounds that modulate the activity of a bacterial peptidyl tRNA hydrolase. In particular, provided herein are assays for the identification of compounds that inhibit or reduce the activity of a bacterial peptidyl tRNA hydrolase. The methods provided herein provide a simple, sensitive assay for high-throughput screening of libraries of compounds to identify pharmaceutical leads useful for preventing, treating, and managing a bacterial infection or one or more symptoms thereof. Further provided herein are methods for preventing or inhibiting bacterial proliferation as well as methods for preventing, treating, and/or managing a bacterial infection using such compounds and compositions.Type: ApplicationFiled: September 21, 2007Publication date: March 18, 2010Inventors: Soongyu Choi, Arthur Branstrom, Scott A. Gothe, Richard Lipman, Tamil Arasu, Richard G. Wilde
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Publication number: 20100069358Abstract: The present invention provides a compound of formula (I); or a pharmaceutically acceptable salt thereof in the inhibition of c-Jun N-terminal kinase (JNK) activity and particularly in the treatment of neurodegenerative disorders, inflammatory diseases and/or and autoimmune diseases. The invention also provides processes for the manufacture of said compounds of formula (I) or a pharmaceutically acceptable salt thereof and compositions containing them.Type: ApplicationFiled: August 5, 2009Publication date: March 18, 2010Applicant: Eisai R&D Management Co., Ltd.Inventors: Piotr Pawel GRACZYK, Paschalis DIMOPOULOS, Christopher Neil FARTHING, Gurpreet Singh BHATIA, Afzal KHAN
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Patent number: 7678792Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit, PDGFR?, PDGFR?, CSF1R, Abl, BCR-Abl, CSK, JNK1, JNK2, p38, p70S6K, TGF?, SRC, EGFR, trkB, FGFR3, FLT3, Fes, Lck, Syk, RAF, MKK4, MKK6, SAPK2?, BRK, KDR, c-raf or b-raf kinase, or mutant forms thereof.Type: GrantFiled: October 16, 2007Date of Patent: March 16, 2010Assignee: IRM LLCInventors: Donatella Chianelli, Christopher Cow, Yun He, Songchun Jiang, Xiaolin Li, Xiaodong Liu, Zuosheng Liu, Jon Loren, Valentina Molteni, Juliet Nabakka, Pingda Ren, Taebo Sim, Xiaodong Wang, Shuli You
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Publication number: 20100022529Abstract: The present invention provides amidophenoxyindazole compounds useful in the treatment of cancer.Type: ApplicationFiled: July 15, 2009Publication date: January 28, 2010Inventors: Tiechao LI, Mark Andrew POBANZ, Chuan SHIH, Zhipei WU, Wei Jennifer YANG, Boyu ZHONG
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Publication number: 20090318434Abstract: There is provided a process for the preparation of a compound of Formula 1, the use of said process in the preparation of a compound of Formula 5 or a phosphate, sulphate, hydrogensulphate, malate, citrate, tartrate or fumarate salt thereof, and the use of the fumarate salt in a composition for use in therapy.Type: ApplicationFiled: June 18, 2009Publication date: December 24, 2009Applicant: AstraZeneca ABInventors: Helen Blade, Gwydion Huw Churchill, Angela Charlotte Currie, Benjamin Charles Dobson, Martin Neal Kenworthy, Lyn Powell, Steven Anthony Raw, Peter Samuel Hynes
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Publication number: 20090258857Abstract: The present invention encompasses compounds of general formula (1) wherein R1, M1, L1 and Q are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or anomalous cell proliferation, and the use thereof for preparing a pharmaceutical composition with the above-mentioned properties.Type: ApplicationFiled: June 13, 2007Publication date: October 15, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Ulrich Reiser, Peter Ettmayer, Oliver Kraemer, Peter Sennhenn, Walter Spevak
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Publication number: 20090209530Abstract: The invention pertains to novel cyclin dependent kinase inhibitors (cdks) and specifically, but not exclusively, as inhibitors of cdk/cyclin complexes. As described herein, the inhibitors of this invention are capable of inhibiting the cell-cycle machinery and consequently may be useful in modulating cell-cycle progression, ultimately controlling cell growth and differentiation. Such compounds would be useful for treating subjects having disorders associated with excessive cell proliferation.Type: ApplicationFiled: December 21, 2004Publication date: August 20, 2009Applicant: GPC Biotech, Inc.Inventors: Nicholas Bockovich, Arthur F. Kluge, Chris Oalmann, Krishna K. Murthi, Siya Ram, Zhongguo Wang, Jianxing Huang
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Publication number: 20090156803Abstract: The present invention provides a condensed furan compound of the formula (I): wherein Ring X is benzene, pyridine, or the like; Y is an optionally substituted amino, an optionally substituted cycloalkyl, an optionally substituted aryl, an optionally substituted saturated heterocyclic group, an optionally substituted unsaturated heterocyclic group; A is a single bond, lower alkylene, lower alkenylidene, lower alkenylene or an oxygen atom; R3 is hydrogen or the like; and, R4 is hydrogen, or the like, or pharmaceutically acceptable salts thereof, which is useful as a medicament, particularly, as an activated blood coagulation factor X inhibitor.Type: ApplicationFiled: January 29, 2009Publication date: June 18, 2009Inventors: Takayuki Kawaguchi, Hidenori Akatsuka, Toru Iijima, Tatsuya Watanabe, Jun Murakami, Takashi Mitsui
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Publication number: 20090143368Abstract: A composition for inhibiting the extracellular matrix gene transcription comprising a cinnamoyl compound represented by the formula (I): and an inert carrier, or the like.Type: ApplicationFiled: March 2, 2006Publication date: June 4, 2009Inventors: Hiroaki Shiraki, Kiyoshi Higashi, Yoshitaka Tomigahara, Junya Takahashi
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Publication number: 20090137579Abstract: The present invention is directed to the compound of formula (II), or a solvate thereof, or crystalline forms thereof; to a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formula (II), including crystalline forms thereof, and a pharmaceutically acceptable carrier; and to the use of a compound of formula (II), or crystalline forms thereof, for treating a patient suffering from, or subject to, a pathological condition capable of being ameliorated by inhibiting IKK-2, and methods related thereto.Type: ApplicationFiled: October 22, 2008Publication date: May 28, 2009Applicant: Millennium Pharmaceuticals, Inc.Inventors: Frederick A. Hicks, Martin Ian Cooper, Marianne Langston, Adrian St. Clair Brown
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Publication number: 20090131422Abstract: The present invention is directed to the Tartrate, Mono-Hydrochloride, Malonate and p-Toluenesulfonate Salts of the compound of formula (I), or solvates thereof, or crystalline forms thereof; to a pharmaceutical composition comprising a pharmaceutically effective amount of the Salts, including crystalline forms thereof, and a pharmaceutically acceptable carrier; and to the use of the Salts, including crystalline forms thereof, for treating a patient suffering from, or subject to, a pathological condition capable of being ameliorated by inhibiting IKK-2, and methods related thereto.Type: ApplicationFiled: October 22, 2008Publication date: May 21, 2009Applicant: Millennium Pharmaceuticals, Inc.Inventors: Frederick A. Hicks, Martin Ian Cooper, Adrian St Clair Brown
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Publication number: 20090111803Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF—or combinations thereof.Type: ApplicationFiled: December 18, 2008Publication date: April 30, 2009Inventors: Wensheng Yu, Ling Tong, Lei Chen, Joseph A. Kozlowski, Brian J. Lavey, Neng-Yang Shih, Vincent S. Madison, Guowei Zhou, Peter Orth, Zhuyan Guo, Michael K.C. Wong, De-Yi Yang, Seong Heon Kim, Bandarpalle B. Shankat
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Publication number: 20080311076Abstract: Compounds of formula (Ia) are found to be active in inhibiting replication of flaviviridae viruses, wherein R1, R2, R3 and R4 are as defined in the claims.Type: ApplicationFiled: April 28, 2005Publication date: December 18, 2008Applicant: ARROW THERAPEUTICS LIMITEDInventors: Keith Charles Spencer, Helena Dennison, Neil Mathews, Michael Christopher Barnes, Surinder Singh Chana
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Publication number: 20080267914Abstract: Compounds of formula (Ia) are found to be active in inhibiting replication of flaviviridae viruses (Ia), wherein R1 and R2 are the same or different and represent hydrogen, halogen, -L-O—R3, -L-O-L-A or -L-O-L?-A?, wherein each L is the same or different and represents a direct bond or a C1-C4 alkylene group; L? represents a direct bond or a C2-C4 alkylene group; R3 represents hydrogen, C1-C4 alkyl or C1-C4 haloalkyl; A represents a 5- to 10-membered heterocyclyl group; and A? represents a C6-C1 aryl group; wherein at least one of R1 and R2 is -L-O—R3, -L-O-L-A or -L-O-L?-A?.Type: ApplicationFiled: October 9, 2006Publication date: October 30, 2008Inventors: Michael Christopher Barnes, Surinder Singh Chana, Helena Dennison, Lyn Jennens, Neil Mathews, Christopher John Pilkington, Keith Charles Spencer, Alexander James Floyd Thomas
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Publication number: 20080221096Abstract: The present disclosure relates to a pyridofuropyrimidine derivative of formula (I): wherein G1 is a group chosen from —CR6R7— and —O— wherein R6 and R7 are independently chosen from hydrogen atoms and C1-4 alkyl groups; R1 and R2 are independently chosen from hydrogen atoms and C1-4 alkyl groups; R3 is chosen from C1-4 alkyl, C1-4 alkoxy, amino, hydroxy, mono-C1-4alkylamino, di-C1-4alkylamino, C3-8cycloalkylamino, aryl, heteroaryl and saturated N-containing heterocyclyl groups which are bound to the pyridine ring through their nitrogen atom, all of them being optionally substituted by one or more substituents chosen from halogen atoms and hydroxy, C1-4 alkyl, C1-4alkoxy-C1-4alkyl, aryl-C1-4alkyl, —O(CO)OR8, C1-4 alkoxy, —(CO)NR8R9, —CN, —CF3, —NR8R9, —SR8 and —SO2NH2 groups wherein R8 and R9 are each independently chosen from a hydrogen atom or a C1-4 alkyl group; R4 and R5 are independently chosen from hydrogen atoms, C1-4alkyl groups, hydroxyl-C1-4alkyl groups and groups of formula (II): wherein p aType: ApplicationFiled: July 21, 2006Publication date: September 11, 2008Inventors: Joan Taltavull Moll, Luis Miguel Pages Santacana
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Patent number: 7410990Abstract: This invention features a compound of formula (I): R1 is aryl or heteroaryl; each of R2 and R4, independently, is H, halogen, CN, alkyl, ORa, or NRaRb; R3 is H, halogen, CN, alkyl, alkenyl, alkynyl, aryl, heteroaryl, cyclyl, heterocyclyl, ORa, OC(O)Ra, OC(O)NRaRb, NRaRb, NRaC(O)Rb, NRaS(O)RbNRaS(O)2Rb, NRaC(O)NRbRc, NRaC(S)NRbRc, NRaC(NRb)NRcRd, NRaC(O)ORb, S(O)NRaRb, S(O)2NRaRb, S(O)Ra, S(O)2Ra, C(O)Ra, C(O)ORa, or C(O)NRaRb; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; A is O, S, S(O), S(O)2, or NRe; B is N or CRf; X is O, S, S(O), S(O)2, NRe, or C(O); Y is a covalent bond, C(O), C?NRa, O, S, S(O), S(O)2, or NRe; Z is N or CH; each of U and V, independently, is N or CR; and W is O, S, or NRe; in which each of Ra, Rb, Rc, and Rd, independently, is H, alkyl, aryl, heteroaryl, cyclyl, or heterocyclyl; Re is H, alkyl, aryl, acyl, or sufonyl; and Rf is H, alkyl, aryl, acyl, sulfonyl, alkoxyl, amino, ester, amide, CN, or halogen.Type: GrantFiled: October 3, 2006Date of Patent: August 12, 2008Assignee: Synta Pharmaceuticals Corp.Inventors: Lijun Sun, Mitsunori Ono, Yumiko Wada, Weiwen Ying, Teresa Przewloka, Elena Kostik
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Patent number: 7074929Abstract: This invention relates to novel compounds, compositions, and methods for the treatment of physiological disorders associated with an excess of neuropeptide Y.Type: GrantFiled: November 10, 2003Date of Patent: July 11, 2006Assignees: Neurogen Corp., Pfizer, Inc.Inventors: Raymond F. Horvath, Jennifer Tran, Stéphane De Lombaert, Kevin J. Hodgetts, Philip A. Carpino, David A. Griffith