Three Or More Ring Hetero Atoms In The Tricyclo Ring System Patents (Class 544/250)
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Patent number: 8674113Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, L, M, W, R1, R2, R3, R4, R6, R7, R9, Ra, Rb have meanings given in the description.Type: GrantFiled: December 8, 2011Date of Patent: March 18, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Henning Priepke, Henri Doods, Alexander Heim-Riether, Raimund Kuelzer, Roland Pfau, Klaus Rudolf, Dirk Stenkamp
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Publication number: 20140073642Abstract: This invention relates to quinazoline derivatives, processes for their preparation, pharmaceutical compositions, and their use in therapy of disorders in which the modulation of toll-like-receptors is involved.Type: ApplicationFiled: May 18, 2012Publication date: March 13, 2014Applicant: Janssen R&D IrelandInventors: David McGowan, Pierre Jean-Marie Bernard Raboisson, Tim Hugo Maria Jonckers, Stefaan Julien Last, Werner Embrechts, Serge Maria Aloysius Pieters
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Patent number: 8664387Abstract: The present invention is directed to quinolinone-pyrazolone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. 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 mediated by the M1 receptor.Type: GrantFiled: December 9, 2010Date of Patent: March 4, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Scott D. Kuduk, Ronald K. Chang, Thomas J. Greshock
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Publication number: 20140057900Abstract: Compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like.Type: ApplicationFiled: August 23, 2013Publication date: February 27, 2014Applicant: Board of Regents of The University of Texas SystemInventors: Steven L. McKnight, Andrew A. Pieper, Joseph M. Ready, Enrique Fernandez
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Publication number: 20140057899Abstract: The present invention provides a new compound that has an inhibitory action against EGFR and that has cell growth inhibitory effects. The present invention further provides a pharmaceutical preparation useful for preventing and/or treating cancer, based on the EGFR inhibitory effect of the compound. A compound represented by the following Formula (I) or a salt thereof.Type: ApplicationFiled: February 22, 2013Publication date: February 27, 2014Applicant: Taiho Pharmaceutical Co., Ltd.Inventors: Takeshi Sagara, Satoru Ito, Sachie Otsuki, Katsumasa Nonoshita
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Publication number: 20140045833Abstract: The present invention relates to a novel family of inhibitors of protein kinases of Formula (1) wherein X is selected from CH2, O, S(0)n, or NR6; and process for their production and pharmaceutical compositions thereof. In particular, the present invention relates to inhibitors of the members of the Tec, Src, Btk and Lck protein kinase families.Type: ApplicationFiled: April 3, 2012Publication date: February 13, 2014Applicant: PHARMASCIENCE INC.Inventors: Alain Laurent, Yannick Rose, Stephen Morris, James Jaquith
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Publication number: 20140024654Abstract: Compounds of the following formula are provided for use with PARP: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits, and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds.Type: ApplicationFiled: September 18, 2013Publication date: January 23, 2014Applicant: Takeda Pharmaceutical Company LimitedInventors: Jason W. Brown, Anthony R. Gangloff, Andre K. Kiryanov
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Publication number: 20140024662Abstract: The present invention features compounds of Formula (I), pharmaceutical compositions, methods of synthesis, and methods for treating diseases and conditions associate with cellular necrosis. Screening assays for identifying compounds useful for treating these conditions are also described.Type: ApplicationFiled: September 25, 2013Publication date: January 23, 2014Applicants: Shanghai Institute of Organic Chemistry, President and Fellows of Harvard CollegeInventors: Junying YUAN, Chengye Yuan, Alexei Degterev
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Publication number: 20140024657Abstract: 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 (1)-(7), (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: September 20, 2013Publication date: January 23, 2014Applicant: President and Fellows of Harvard CollegeInventors: Junying YUAN, Emily S. Hsu
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Publication number: 20140018343Abstract: The present invention provides arylo-fused thienopyrimidine compounds, compositions thereof, and methods of using the same.Type: ApplicationFiled: July 11, 2013Publication date: January 16, 2014Inventors: Donna L. Romero, Shaughnessy Robinson, Matthew David Wessel, Jeremy Robert Greenwood
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Publication number: 20140018361Abstract: The present invention provides furano- and pyrrolo-pyrimidine and pyridine compounds, compositions thereof, and methods of using the same.Type: ApplicationFiled: July 11, 2013Publication date: January 16, 2014Inventors: Geraldine C. Harriman, Donna L. Romero, Craig E. Masse, Shaughnessy Robinson, Matthew David Wessel, Jeremy Robert Greenwood
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Patent number: 8629155Abstract: Disclosed are compounds of formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, U, W, X, R1, R2, R6, R7, R30 and R31 are as described above in the specification. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.Type: GrantFiled: March 15, 2012Date of Patent: January 14, 2014Assignee: Merck Sharp & Dohme, Corp.Inventors: Yusheng Wu, Ulrich Iserloh, Jared N. Cumming, Xiaoxiang Liu, Robert D. Mazzola, Zhong-Yue Sun, Ying Huang, Andrew Stamford, Brian McKittrick, Zhaoning Zhu
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Patent number: 8629154Abstract: The invention relates to substituted 2-alkylsulfanyl-3-(arylsulfonyl)-cycloalkyl[e and d]pyrazolo[1,5-a]pyrimidines, to serotonin 5-HT6 receptor antagonists, to novel drug substances and pharmaceutical compositions, comprising the said conpounds as active ingredients, to novel medicaments and methods for treatment and prophylaxis of CNS diseases of humans and warm blooded animals pathogenesis of which is associated with 5-HT6 receptors. In general formulas 1 and 2 R1 represents hydrogen or C1-C3 alkyl; R2 represents C1-C3 alkyl; R3 represents hydrogen, one or more optionally identical halogens, C1-C3 alkyl or hydroxyl optionally substituted with C1-C3 alkyl; n represents the whole numbers 1, 2 or 3.Type: GrantFiled: January 23, 2009Date of Patent: January 14, 2014Inventors: Andrey Alexandrovich Ivashchenko, Alexander Vasilievich Ivashchenko, Nikolay Filippovich Savchuk
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Publication number: 20130338134Abstract: The present invention relates to tricyclic compounds, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.Type: ApplicationFiled: June 12, 2013Publication date: December 19, 2013Inventors: Liangxing Wu, Colin Zhang, Chunhong He, Yaping Sun, Liang Lu, Ding-Quan Qian, Meizhong Xu, Jincong Zhuo, Wenqing Yao
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Patent number: 8609675Abstract: The present invention provides Fused Tricyclic Compounds of the Formula (I) wherein Q, R1, R2, R3, and R4 are as defined herein, and pharmaceutically acceptable salts of such Fused Tricyclic Compounds. The Fused Tricyclic Compounds are useful in the treatment of cancer and other proliferative disorders.Type: GrantFiled: June 30, 2010Date of Patent: December 17, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Cliff C. Cheng, Hongbo Zeng, Gerald W. Shipps, Jr., Yongqi Deng, Zhaoyang Meng, Lianyun Zhao, Yang Nan, Binyuan Sun, Duan Liu, Panduranga A. Reddy, M. Arshad Siddiqui
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Publication number: 20130330327Abstract: The present invention relates to alkoxy-substituted 2,3-dihydroimidazo[1,2-c]quinazoline compounds of general formula (I) in which R1, R2 and R3 are as defined in the claims, to methods of preparing said compounds, to intermediates for the preparation of said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: November 8, 2011Publication date: December 12, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: William Johnston Scott, Manfred Möwes, Ningshu Liu, Ursula Mönning, Ulf Bomer
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Publication number: 20130324525Abstract: The present invention relates to novel heterocyclic compounds and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): wherein Q1, Q2, R2, R3, R4, R5, and R6 are as described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: August 6, 2013Publication date: December 5, 2013Applicant: Gilead Sciences, Inc.Inventors: Matthew Abelman, Robert H. Jiang, Jeff Zablocki
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Patent number: 8598197Abstract: Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.Type: GrantFiled: April 24, 2013Date of Patent: December 3, 2013Assignee: G1 Therapeutics, Inc.Inventors: Francis X. Tavares, Jay C. Strum
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Publication number: 20130317004Abstract: 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: November 8, 2011Publication date: November 28, 2013Applicant: Bayer Intellectual Property GmbHInventors: William Johnston Scott, Ningshu Liu, Manfred Möwes, Andrea Hägebarth, Ursula Mönning, Ulf Bömer
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Publication number: 20130310394Abstract: The present invention relates to compounds of Formula I or a pharmaceutically acceptable salt thereof, wherein variables R, Ar, X, and Ar1 and n are as defined herein. The compounds are capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: ApplicationFiled: May 20, 2013Publication date: November 21, 2013Applicant: Allergan, Inc.Inventors: Thomas C. Malone, Julie A. Wurster, Clarence Eugene Hull, III
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Publication number: 20130310405Abstract: Compounds of Formula (I), which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals. The compounds of formula (I) a: useful for the treatment of cancer.Type: ApplicationFiled: December 13, 2011Publication date: November 21, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Hartmut Rehwinkel, Andrea Hägebarth, Oliver Politz, Roland Neuhaus, Ulf Bömer
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Publication number: 20130302416Abstract: New substituted tricyclic compounds of formula (I) are described, wherein R1, R2, X, Y, Z are herein defined, having protein kinase inhibiting activity. The invention includes methods to prepare the compounds of formula (I), pharmaceutical compositions containing them, and their use in therapy, in particular for the treatment of diseases caused by and/or associated with dysregulated activity of protein kinase.Type: ApplicationFiled: January 19, 2012Publication date: November 14, 2013Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Marina Caldarelli, Francesco Casuscelli, Daniele Donati, Danilo Mirizzi, Francesca Quartieri, Marco Silvagni
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Publication number: 20130302303Abstract: Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure: including steroisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein A is a ring moiety selected from: and wherein R1, R2, R3, X, Z, L1, Cycl1, L2 and Cycl2 are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.Type: ApplicationFiled: July 22, 2013Publication date: November 14, 2013Inventors: Laurence H. Hurley, Daruka Mahadevan, David J. Bearss, Hariprasad Vankayalapati, Steven L. Warner, James Welsh
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Patent number: 8580956Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.Type: GrantFiled: May 28, 2008Date of Patent: November 12, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Zhaoning Zhu, William J. Greenlee, Zhong-Yue Sun, Gioconda Gallo, Ruo Xu, Xianhai Huang, Xiaohong Zhu
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Patent number: 8580405Abstract: The present invention provides a novel naphthothiophene compound having a high lowest excited triplet level (T1).Type: GrantFiled: April 11, 2011Date of Patent: November 12, 2013Assignee: Canon Kabushiki KaishaInventors: Naoki Yamada, Jun Kamatani, Akihito Saitoh
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Publication number: 20130296305Abstract: The present invention relates to tricyclic pyrrolo derivatives of Formula (I), which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.Type: ApplicationFiled: January 19, 2012Publication date: November 7, 2013Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Marina Caldarelli, Mauro Angiolini, Italo Beria, Maria Gabriella Brasca, Francesco Casuscelli, Roberto D'Alessio, Andrea Lombardi Borgia
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Publication number: 20130287767Abstract: The invention discloses 4-(arylamino)selenophenopyrimidine derivatives of formula (I), hydrates, solvates, isomers, or pharmaceutically acceptable salts thereof; process for their preparation and methods of treating or inhibiting or controlling a cell proliferative disorders, particularly cancer using said compounds. Pharmaceutical compositions comprising 4-(arylamino)selenophenopyrimidine derivatives of formula (I) are useful for the treatment, inhibition, or control of cancer.Type: ApplicationFiled: June 7, 2013Publication date: October 31, 2013Inventors: Ganga Raju GOKARAJU, Sudhakar KASINA, Venkateswarlu SOMEPALLI, Rama Raju GOKARAJU, Venkata Kanaka Ranga Raju GOKARAJU, Kiran BHUPHATIRAJU, Trimurtulu GOLAKOTI, Krishanu SENGUPTA, Venkata Krishna Raju ALLURI
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Patent number: 8569295Abstract: The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.Type: GrantFiled: July 28, 2010Date of Patent: October 29, 2013Assignee: Merck Patent GmbHInventors: Xiaoling Chen, Srinivasa R. Karra, Bayard R. Huck, Ruoxi Lan, Amanda E. Sutton, Andreas Goutopoulos, Brian L. Hodous, Reinaldo Jones
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Publication number: 20130281474Abstract: This invention relates to novel fused tricyclic compounds that are inhibitors of mammalian Target of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP, and are useful in the treatment of cellular proliferative diseases, for example cancer and other proliferative disorders.Type: ApplicationFiled: September 26, 2011Publication date: October 24, 2013Applicant: MERCK SHARP & DOHME CORP.Inventors: Zhaoyang Meng, Panduranga Abdulla Reddy, M. Arshad Siddiqui
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Publication number: 20130274257Abstract: The present invention provides substituted tricyclic heteroaryl compounds, including, for example, pyridoindoles, pyrimidinoindoles and triazinoindoles that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases such as immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.Type: ApplicationFiled: March 15, 2013Publication date: October 17, 2013Inventors: Argyrios G. Arvanitis, James D. Rodgers, Louis Storace, Beverly Folmer
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Patent number: 8552018Abstract: Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure: including steroisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein A is a ring moiety selected from: and wherein R1, R2, R3, X, Z, L1, Cycl1, L2 and Cycl2 are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.Type: GrantFiled: March 18, 2011Date of Patent: October 8, 2013Assignees: Arizona Board of Regents on behalf of the University of Arizona, Astex Pharmaceutials, Inc.Inventors: Laurence H. Hurley, Daruka Mahadevan, David J. Bearss, Hariprasad Vankayalapati, Sridevi Bashyam, Steven L. Warner, James Welsh
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Publication number: 20130261113Abstract: 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: June 3, 2013Publication date: October 3, 2013Inventors: Martin HENTEMANN, Jill WOOD, William SCOTT, Martin MICHELS, Ann-Marie CAMPBELL, Ann BULLION, Ronald ROWLEY, Aniko REDMAN
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Patent number: 8546410Abstract: Heteroaryl-fused macrocyclic 2,4-diaminopyrimidine compounds of formula (I) wherein W, G1, G2, A1 and R1 are defined in the description, compositions comprising such compounds, methods for making the compounds, and methods of treating and preventing the progression of diseases, conditions, and disorders using such compounds and compositions are described herein.Type: GrantFiled: May 5, 2009Date of Patent: October 1, 2013Assignee: AbbVie Inc.Inventors: Huaqing Liu, Irene Drizin, Marlon D. Cowart, Robert J. Altenbach
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Patent number: 8541417Abstract: Compounds of the following formula are provided for use with PARP: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits, and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds.Type: GrantFiled: July 29, 2010Date of Patent: September 24, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Jason W. Brown, Anthony R. Gangloff, Andre A. Kiryanov
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Patent number: 8541430Abstract: The present invention relates to novel compounds, their pharmaceutically acceptable salts, and their isomers, stereoisomers, conformers, tautomers, polymorphs, hydrates and solvates. The present invention also encompasses pharmaceutically acceptable compositions of said compounds and process for preparing novel compounds. The invention further relates to the use of the above-mentioned compounds for the preparation of medicament for use as pharmaceuticals.Type: GrantFiled: September 8, 2010Date of Patent: September 24, 2013Assignee: Torrent Pharmaceuticals LimitedInventors: Sanjay Srivastava, Laxmikant Chhipa, Ramesh Chandra Gupta, Shailesh Deshpande, Anita Chaudhari, Anookh Mohanan, Chaitanya Dutt, Vijay Chauthaiwale, Murali Badanthadka, Prashant G. Jamadarkhana
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Publication number: 20130245048Abstract: The present invention provides 4-Aza-2,3-didehydropodophyllotoxin compound of general formula A (4a-4z and 4aa-4ae) as useful potential antitumour agents against human cancer cell lines. The present invention further provides a process for the synthesis of 4-Aza-2,3-didehydropodophyllotoxin compounds (4a-4z and 4aa-4ae).Type: ApplicationFiled: March 25, 2011Publication date: September 19, 2013Applicant: Council of Scientific & Industrial ResearchInventors: Kamal Ahmed, Suresh Paidakula, Ashwini Kumar Banala, Mallareddy Adla, Venkat Reddy Papagari, Rasheed Tamboli Jaki
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Publication number: 20130245049Abstract: The present invention relates to compounds of formula (A), as further defined herein, having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. The invention further relates to the use of such compounds, optionally combined with one or more other drugs having antiviral activity, for the treatment of animals suffering from viral infections, in particular HIV infection.Type: ApplicationFiled: November 15, 2011Publication date: September 19, 2013Applicant: Katholieke Universiteit LeuvenInventors: Patrick Chaltin, Frauke Christ, Zeger Debyser, Marc De Maeyer, Arnaud Marchand, Damien Marchand, Arnout Voet
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Patent number: 8530651Abstract: The present invention relates to a novel process for producing quinazoline compounds which are useful in therapy. More specifically, the compounds produced by the process of the invention are useful in the treatment of a number of cardiovascular diseases. The process of the invention provides 6,7-dichloro-1,5-dihydroimidazo[2,1-b]quinazolin 2(3H)-one, more commonly known as anagrelide and its analogues in a clean and efficient manner.Type: GrantFiled: November 30, 2009Date of Patent: September 10, 2013Assignee: Shire LLCInventor: Bernard Golding
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Patent number: 8530487Abstract: Compounds and compositions for treating disorders related to TRPA1 are described herein.Type: GrantFiled: January 29, 2010Date of Patent: September 10, 2013Assignee: Hydra Biosciences, Inc.Inventors: Xinyuan Wu, Spencer David Kimball, Ping Chen, Ding Zhou, Shaoping Peng
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Publication number: 20130231328Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.Type: ApplicationFiled: January 10, 2013Publication date: September 5, 2013Applicant: NIMBUS IRIS, INC.Inventors: Geraldine C. Harriman, Ronald T. Wester, Donna L. Romero, Shaughnessy Robinson, Mee Shelley, Matthew David Wessel, Jeremy Robert Greenwood, Craig E. Masse, Rosana Kapeller-Libermann
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Patent number: 8524722Abstract: This invention relates to novel compounds and processes for their preparation, methods of treating diseases, particularly cancer, comprising administering said compounds, and methods of making pharmaceutical compositions for the treatment or prevention of disorders, particularly cancer.Type: GrantFiled: September 2, 2008Date of Patent: September 3, 2013Assignee: Bayer Intellectual Property GmbHInventors: Hartmut Schirok, Ying Li-Sommer, Michael Brands, Mario Lobell, Adrian Tersteegen, Herbert Himmel, Karl-Heinz Schlemmer, Dieter Lang, Kirstin Petersen, Matthias Renz, Dominik Mumberg, Jens Hoffmann, Gerhard Siemeister, Ulf Bömer
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Patent number: 8513270Abstract: The present invention provides substituted tricyclic heteroaryl compounds, including, for example, pyridoindoles, pyrimidinoindoles and triazinoindoles that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases such as immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.Type: GrantFiled: December 20, 2007Date of Patent: August 20, 2013Assignee: Incyte CorporationInventors: Argyrios G. Arvanitis, James D. Rodgers, Louis Storace, Beverly Folmer
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Publication number: 20130211083Abstract: The present invention relates to a novel process for producing anagrelide, 6,7-dichloro-1,5-dihydroimidazo[2,1-b]quinazolin 2(3H)-one, or certain analogues thereof. The process of the invention also provides improved processes for producing key intermediates required for the synthesis of anagrelide or certain analogues thereof.Type: ApplicationFiled: October 21, 2011Publication date: August 15, 2013Applicant: SHIRE LLCInventor: Paul McGee
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Publication number: 20130210845Abstract: Proteinopathies result from the proteasome not acting efficiently enough to eliminate harmful proteins and prevent the formation of the pathogenic aggregates. As described herein, inhibition of proteasome-associated deubiquitinase Usp14 results in increased proteasome efficiency. The present invention therefore provides novel compositions and methods for inhibition of Usp14, enhancement of proteasome activity and treatment of proteinopathies.Type: ApplicationFiled: July 22, 2011Publication date: August 15, 2013Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGEInventors: Daniel J. Finley, Randall W. King, Byung-Hoon Lee, Min J. Lee, Timothy C. Gahman
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Patent number: 8507502Abstract: Fused bicyclic or tricyclic compounds of formula (I): wherein A, B, C, X, Y, m, and n are defined herein. Also disclosed are a method for inhibiting EGFR kinase activity and a method for treating cancer with these compounds.Type: GrantFiled: November 9, 2009Date of Patent: August 13, 2013Assignee: National Health Research InstitutesInventors: Hsing-Pang Hsieh, Selvaraj Mohane Coumar, Tsu-An Hsu, Wen-Hsing Lin, Yi-Rong Chen, Yu-Sheng Chao
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Patent number: 8501755Abstract: This invention relates to compounds of Formula (I), wherein the variables are as disclosed in the specification, to pharmaceutical compositions containing them, to methods of making the compounds and pharmaceutical compositions, and to methods of using the compounds and pharmaceutical compositions for treating or preventing disorders, in particular cancer.Type: GrantFiled: March 20, 2007Date of Patent: August 6, 2013Assignee: Bayer Intellectual Property GmbHInventors: Chengzhi Zhang, Kanwar Sidhu, Mario Lobell, Gaetan Ladouceur, Qian Zhao, Zheng Liu, Kristen M. Allegue, Chetan P. Darne, Jason Newcom
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Publication number: 20130172328Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia or so on represented by the formula (I):Type: ApplicationFiled: June 22, 2011Publication date: July 4, 2013Applicant: CROSSWING INC.Inventors: Takahiko Taniguchi, Masato Yoshikawa, Kasei Miura, Tomoaki Hasui, Eiji Honda, Keisuke Imamura, Makoto Kamata, Haruhi Kamisaki, John F. Quinn, Joseph Raker, Fatoumata Camara, Yi Wang
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Patent number: 8475686Abstract: The present invention relates to bridged pyridoquinazoline and phenanthroline compounds, and organic semiconducting materials containing these compounds. The invention also relates to devices containing these compounds, including electronic, optoelectronic, or electroluminescent elements, such as organic light-emitting diodes, field effect transistors, photo detectors, and organic solar cells.Type: GrantFiled: December 2, 2009Date of Patent: July 2, 2013Assignee: Novaled AGInventor: Omrane Fadhel
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Patent number: 8471009Abstract: The invention relates to substituted 2-alkylamino-3-(arylsulfonyl)cycloalkyl[e or d]pyrazolo[1,5-a]pyrimidines, to serotonin 5-HT6 receptor antagonists, to novel drug substances and pharmaceutical compositions comprising the said compounds as active ingredients, and to novel medicaments and method for treatment and prophylaxis of various CNS diseases. 2-Alkylamino-3-arylsulfonylcycloalkyl[e]pyrazolo[1,5-a]pyrimidines of general formula 1 and 2-alkylamino-3-arylsulfonylcycloalkyl[d]pyrazolo[1,5-a]pyrimidines of general formula 2, wherein: R1 is hydrogen or C1-C3 alkyl; R2 is C1-C3 alkyl; R3 is hydrogen, one or more optionally identical halogen atoms, C1-C3 alkyl or hydroxyl group optionally substituted with C1-C3 alkyl; n is the whole numbers 1, 2 or 3.Type: GrantFiled: January 23, 2009Date of Patent: June 25, 2013Inventors: Andrey Alexandrovich Ivashchenko, Nikolay Filippovich Savchuk, Alexander Vasilievich Ivashchenko
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Patent number: 8466283Abstract: 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: GrantFiled: December 5, 2007Date of Patent: June 18, 2013Assignee: Bayer Intellectual Property GmbHInventors: Martin Hentemann, Jill Wood, William Scott, Martin Michels, Ann-Marie Campbell, Ann-Marie Bullion, Bruce R. Rowley, Aniko Redman