The Other Cyclo In The Bicyclo Ring System Is Five-membered Patents (Class 544/280)
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Publication number: 20140350034Abstract: The invention relates to compound of the formula (I) in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.Type: ApplicationFiled: January 25, 2013Publication date: November 27, 2014Applicant: NOVARTIS AGInventors: Trixi Brandl, Stefanie Flohr, Christian Markert, Kenji Namoto, Bernard Pirard, Martin Renatus
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Publication number: 20140350020Abstract: The present application relates to novel fused pyrimidines and triazines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: July 5, 2011Publication date: November 27, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Andreas Knorr, Frank Wunder, Volkhart Min-Jian Li, Walter Kroh, Lars Bärfacker
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Publication number: 20140349998Abstract: The instant invention provides compounds of formula I which are JAK3 inhibitors. Specifically, the compounds of formula I are pyrrolo[2,3-d]pyrimidine derivative compounds. The instant invention also provides methods of treating JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer, by administering the pyrrolo[2,3-d]pyrimidine-derivative compounds of formula I.Type: ApplicationFiled: November 30, 2012Publication date: November 27, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Sean P Ahearn, Matthew Christopher, Christopher Dinsmore, Joon Jung, Qinglin Pu, Alexey Rivkin, Mark E. Scott, David J. Witter, Hyun Chong Woo, Brandon Cash
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Patent number: 8895571Abstract: The present invention provides isoindolinone and pyrrolopyridinone derivatives, as well as their compositions and methods of use, that inhibit the activity of the serine/threonine kinase, Akt, and are useful in the treatment of diseases related to the activity of Akt including, for example, cancer and other diseases.Type: GrantFiled: October 12, 2012Date of Patent: November 25, 2014Assignee: Incyte CorporationInventors: Taisheng Huang, Hao Feng, Lingquan Kong, Anlai Wang, Hai Fen Ye, Chu-Biao Xue
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Publication number: 20140343035Abstract: The present invention provides a compound represented by Formula (I) (wherein R1, X1, X2, Y, and Z are as defined in the specification), or a salt thereof.Type: ApplicationFiled: January 17, 2013Publication date: November 20, 2014Inventors: Takeshi Sagara, Satoru Ito, Sachie Otsuki, Hiroshi Sootome
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3?-OH unblocked, fast photocleavable terminating nucleotides and methods for nucleic acid sequencing
Patent number: 8889860Abstract: The present invention relates generally to 3?-OH unblocked, labeled and unlabeled nucleotides and nucleosides with 5-methoxy-substituted nitrobenzyl-based photocleavable terminating groups for use in methods and systems related to DNA and RNA sequencing and analysis. These compounds, which may be represented by the following formulas: wherein the variables are defined herein, may be used as reversible terminators as they exhibit fast nucleotide incorporation kinetics, single-base termination, high nucleotide selectivity, and rapid terminating group cleavage that results in a naturally occurring nucleotide.Type: GrantFiled: September 13, 2012Date of Patent: November 18, 2014Assignee: Lasergen, Inc.Inventors: Brian Stupi, Hong Li, Weidong Wu, Megan N. Hersh, David Hertzog, Sidney E. Morris, Michael L. Metzker -
Patent number: 8889684Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R2 to R6, A, X, Y and m are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, pharmaceutical preparations which contain compounds of this kind and their use as medicaments.Type: GrantFiled: January 27, 2012Date of Patent: November 18, 2014Assignee: Boehringer Ingelheim International GmbHInventor: Heinz Stadtmueller
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Patent number: 8889697Abstract: The present invention provides active metabolites of 3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl) -1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.Type: GrantFiled: October 7, 2010Date of Patent: November 18, 2014Assignee: Incyte CorporationInventors: James D. Rodgers, Argyrios G. Arvanitis, Jack Guoen Shi, Stacey Shepard
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Publication number: 20140336503Abstract: The present invention provides biomarkers that find use as imaging agents within nuclear medicine applications (e.g., PET imaging and SPECT imaging). In particular, the present invention provides methods for identifying and characterizing osteoclast activation within subjects with radiolabeled cathepsin K inhibitors.Type: ApplicationFiled: April 30, 2014Publication date: November 13, 2014Applicant: The Regents of the University of MichiganInventors: Michael R. Kilbourn, Kenneth Kozloff, Melissa E. Rodnick
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Publication number: 20140336207Abstract: The present invention relates to a pyrrole six-membered heteroaryl ring derivative, the preparation method therefor, and the medicinal uses thereof. Specifically, the present invention relates to a new pyrrole six-membered herteroaryl ring derivative as represented by formula (I), the preparation method therefor, a medicinal composition comprising the derivative, and a therapeutic method using same, and, in particular, the uses as a JAK inhibitor and an immunosuppressor. Substituents in formula (I) have the same definitions as in the description.Type: ApplicationFiled: December 19, 2012Publication date: November 13, 2014Inventors: Xuejun Zhang, Qing Dong, Bonian Liu, Yaoping Zhu, Xiaotao Li, Jiong Lan
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Patent number: 8883806Abstract: The present invention is related to processes for preparing chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines of Formula III, and related synthetic intermediate compounds. The chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines are useful as inhibitors of the Janus Kinase family of protein tyrosine kinases (JAKs) for treatment of inflammatory diseases, myeloproliferative disorders, and other diseases.Type: GrantFiled: February 7, 2013Date of Patent: November 11, 2014Assignee: Incyte CorporationInventor: Jiacheng Zhou
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Patent number: 8883807Abstract: The present invention is directed to piperidinone carboxamide indane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: November 10, 2011Date of Patent: November 11, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Ian M. Bell, Mark E. Fraley, Steven N. Gallicchio, Anthony Ginnetti, Helen J. Mitchell, Daniel V. Paone, Donnette D. Staas, Cheng Wang, Blair C. Zartman, Heather E. Stevenson
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Publication number: 20140323438Abstract: The disclosure provides compounds for reducing the prevalence of the perinucleolar compartment in cells, for example, of formula (I), wherein R1, R2, R3, and R4 are as defined herein, that are useful in treating a disease or disorder associated with increased prevalence of the perinucleolar compartment, such as cancer. Also disclosed is a composition containing a pharmaceutically acceptable carrier and at least one compound embodying the principles of the invention, and a method of treating or preventing cancer in a mammal.Type: ApplicationFiled: December 17, 2012Publication date: October 30, 2014Inventors: Kevin Frankowski, Samarjit Patnaik, Sui Huang, Juan Jose Marugan, John Norton, Frank J. Schoenen, Noel Terrence Southall, Steven Titus, Wei Zheng
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Publication number: 20140323504Abstract: The present invention relates to compounds of formula (I) wherein X1 to X5, Y, ZA, ZB, R and A have the meaning as cited in the description and the claims. Said compounds are useful as kinase inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds as well as the use as medicaments.Type: ApplicationFiled: September 20, 2012Publication date: October 30, 2014Inventors: Claudio Dagostin, Nigel Ramsden
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Publication number: 20140323475Abstract: The present invention belongs to the field of EP1 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP1 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP1 receptor as well as to pharmaceutical compositions comprising them.Type: ApplicationFiled: September 14, 2012Publication date: October 30, 2014Inventors: Antoni Torrens Jover, Ramon Mercé Vidal, Francesc Xavier Caldentey Frontera, Antonio David Rodríguez Garrido, Elena Carceller González, Jordi Salas Solana
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Publication number: 20140315889Abstract: The present invention relates to a novel hydroxamate derivatives, more specifically, to novel hydroxamate derivatives having inhibitory activity against Histone Deacetylase (HDAC), isomers thereof, pharmaceutically acceptable salts thereof, hydrates or solvates thereof, use for preparing pharmaceutical compositions, pharmaceutical compositions comprising the same, treatment method using said composition, and a preparing method of novel hydroxamate derivatives. The novel selective hydroxamate derivatives having inhibitory activity against Histone Deacetylase (HDAC) compositions can be used for treatment of inflammatory disease, rheumatoid arthritis, or degenerative disease.Type: ApplicationFiled: October 26, 2012Publication date: October 23, 2014Applicant: CHONG KUN DANG PHARMACEUTICAL CORP.Inventors: Yuntae Kim, Changsik Lee, Hyun-mo Yang, Hojin Choi, Jaeki Min, Soyoung Kim, Dal-Hyun Kim, Nina Ha, Jung-Min Kim, Hyojin Lim, Eunhee Ko
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Publication number: 20140315931Abstract: The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: April 11, 2014Publication date: October 23, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Mark Ledeboer, David Messersmith, Francois Maltais, Huai Gao, Tiansheng Wang, Jingrong Cao, John Duffy, Gabriel Martinez-Botella, Cornelia Forster, Marion Wannamaker, Francesco Salituro, Albert Pierce, Luc Farmer, Valerie Marone
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Publication number: 20140309420Abstract: This invention relates to one pot process for preparing antifolate agent pemetrexed disodium in pure form.Type: ApplicationFiled: December 14, 2012Publication date: October 16, 2014Inventors: Tuncer Aslan, Ender Kocak
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Publication number: 20140309212Abstract: The present invention provides compounds useful as inhibitors of Btk, compositions thereof, and methods of using the same.Type: ApplicationFiled: June 26, 2014Publication date: October 16, 2014Inventors: Minna Bui, Patrick Conlon, Julio H. Cuervo, Daniel A. Erlanson, Junfa Fan, Bing Guan, Brian T. Hopkins, Tracy J. Jenkins, Gnanasambandam Kumaravel, Alexey A. Lugovskoy, Doug Marcotte, Noel Powell, Daniel Scott, Laura Silvian, Art Taveras, Deping Wang, Min Zhong
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Patent number: 8859569Abstract: The present application relates to novel substituted annellated pyrimidines, methods for production thereof, use thereof alone or in combinations for treating and/or preventing diseases and use thereof for the production of medicinal products for treating and/or preventing diseases, in particular for treating and/or preventing cardiovascular diseases.Type: GrantFiled: August 30, 2012Date of Patent: October 14, 2014Assignees: Bayer Pharma Aktiengesellschaft, Bayer Intellectual Property GmbHInventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Nils Griebenow, Dieter Lang, Frank Wunder, Walter Hübsch, Niels Lindner, Alexandros Vakalopoulos, Adrian Tersteegen
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Patent number: 8859568Abstract: There are disclosed novel compounds of formula (I) wherein R1, R12, L, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of the enzyme MPO and are thereby particularly useful in the treatment or prophylaxis of neuroinflammatory disorders, cardiovascular disorders and respiratory disorders.Type: GrantFiled: November 3, 2010Date of Patent: October 14, 2014Assignee: Astrazeneca ABInventors: Anders Bögevig, Yvonne Lo-Alfredsson, Donald Pivonka, Anna-Karin Tidén
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Publication number: 20140303161Abstract: The present disclosure provides compounds and pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, TEC, BTK, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: April 9, 2013Publication date: October 9, 2014Inventor: Principia Biopharma, Inc.
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Patent number: 8853212Abstract: The present invention is directed to novel substituted aminotetrahydrothiopyrans and derivatives thereof of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: February 17, 2011Date of Patent: October 7, 2014Assignee: Merck Sharp & Dohme CorpInventors: Robert R. Wilkening, James M. Apgar, Tesfaye Biftu, Danqing Feng, Xiaoxia Qian, Lan Wei
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Patent number: 8853224Abstract: The invention relates to compounds of the general formula (I) which are inhibitors of purine nucleoside phosphorylases (PNPs) and/or nucleoside hydrolases (NHs). The invention also relates to the use of these compounds in the treatment of diseases and infections including cancer, bacterial infections, protozoal infections, and T-cell mediated disease and to pharmaceutical compositions containing the compounds.Type: GrantFiled: September 7, 2007Date of Patent: October 7, 2014Assignees: Industrial Research Limited, Albert Einstein College of Medicine of Yeshiva UniversityInventors: Keith Clinch, Gary Brian Evans, Richard Hubert Furneaux, Shivali Ashwin Gulab, Peter Michael Kelly, Vern L. Schramm, Peter Charles Tyler, Anthony David Woolhouse
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Publication number: 20140296260Abstract: The invention relates to novel quinazolinone compounds and their use as inhibitors of PI3 kinases, for example, PI3K?, for treating and/or preventing diseases, disorder, and conditions associated with modulating PI3 kinase activity. Novel 3-aryl-2-((arylamino)methyl)quinazolin-4(3H)-one derivatives and pharmaceutically acceptable salts or solvates thereof and their use for the treatment or prevention of diseases, disorders, and conditions associated with the activity of one or more PI3 kinase, such as PI3K?, are disclosed.Type: ApplicationFiled: March 28, 2014Publication date: October 2, 2014Inventors: Ben C. Askew, Takeru Furuya
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Publication number: 20140296206Abstract: Compounds and compositions useful for treating disorders related to Kit are described herein.Type: ApplicationFiled: March 14, 2014Publication date: October 2, 2014Applicant: BLUEPRINT MEDICINES CORPORATIONInventors: Lucian V. DiPietro, Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu, Steven Mark Wenglowsky, Douglas Wilson, Yulian Zhang
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Publication number: 20140296261Abstract: The invention provides a compound represented by formula (I) which may modulate a kinase, and a pharmaceutical composition thereof, as well as the method for preventing or treating a protein kinase mediated disease or condition.Type: ApplicationFiled: November 14, 2012Publication date: October 2, 2014Applicants: CENTAURUS BIOPHARMA CO., LTD., CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD,Inventors: Dengming Xiao, Jijun Li, Yan Zhu, Yuandong Hu, Huting Wang, Zhe Wang, Zanping Wang, Yongheng Wei, Yinghui Sun, Qiong Wu, Hui Zhang, Yong Peng, Fansheng Kong, Ying Sun, Hong Luo, Yongxin Han
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Publication number: 20140296204Abstract: The invention is directed to substituted heteroaryl derivatives. Specifically, the invention is directed to compounds according to Formula Q: wherein D, L, M, W, X, Y, and Z are defined herein. The compounds of the invention are inhibitors of DNA methyltransferase (DNMT) activity—including DNMT1, DNMT3a, or DNMT3b—and are useful in the treatment of cancer and hyperproliferative diseases. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting DNMT activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: ApplicationFiled: October 23, 2012Publication date: October 2, 2014Inventors: Thomas Francis Hendrickson, Koc-Kan Ho, Michael David Saunders, Brian John Stevens, Krzysztof Swierczek, Kevin Bret Wright
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Patent number: 8846698Abstract: The present invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as Trk antagonists.Type: GrantFiled: April 4, 2012Date of Patent: September 30, 2014Assignee: Pfizer LimitedInventors: Mark David Andrews, Sharanjeet Kaur Bagal, Karl Richard Gibson, Kiyoyuki Omoto, Thomas Ryckmans, Sarah Elizabeth Skerratt, Paul Anthony Stupple
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Publication number: 20140288070Abstract: Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on at least one Raf protein kinase. In certain aspects and embodiments, the described compounds are active in inhibiting proliferation of a Ras mutant cell line. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of B-Raf V600E mutant protein kinase, including melanoma, glioma, glioblastoma multiforme, pilocytic astrocytoma, colorectal cancer, thyroid cancer, lung cancer, ovarian cancer, prostate cancer, liver cancer, gallbladder cancer, gastrointestinal stromal tumors, biliary tract cancer, and cholangiocarcinoma.Type: ApplicationFiled: March 17, 2014Publication date: September 25, 2014Inventors: Prabha N. Ibrahim, Wayne Spevak, Hanna Cho, Songyuan Shi, Chao Zhang, Ying Zhang
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Publication number: 20140288084Abstract: In one aspect, the invention relates to substituted 2-(4-heterocyclylbenzyl)isoindolin-1-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: October 28, 2012Publication date: September 25, 2014Applicant: VANDERBILT UNIVERSITYInventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Woods, Corey R. Hopkins, Bruce J. Melancon, Michael S. Poslusney, Darren W. Engers
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Publication number: 20140288096Abstract: The present invention provides novel PI3-Kinase antagonists and methods of use thereof.Type: ApplicationFiled: October 18, 2013Publication date: September 25, 2014Applicant: The Regents of the University of CaliforniaInventors: Zachary A. Knight, Olusegun Williams, Kevan M. Shokat
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Publication number: 20140275004Abstract: Disclosed are compound of Formula (Ia), wherein R1, R2, and R3 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds may be used as agents in the treatment of diseases, including cancer. Also provided are pharmaceutical compositions, comprising one or more compounds of Formula (Ia).Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Inventors: Alan S. Florjancic, Yunsong Tong, Thomas D. Penning, Andrew J. Souers, Rajeev Goswami
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Patent number: 8835444Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing factor (CRF) receptor antagonists Formula (I).Type: GrantFiled: January 31, 2011Date of Patent: September 16, 2014Assignee: Novartis AGInventors: David Beattie, Ian Bruce, Anny-Odile Colson, Andrew James Culshaw, Thomas Sharp
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Publication number: 20140256668Abstract: The present disclosure relates to compounds of formula (I-A) using the compounds wherein Ring A and the variables X, Y, R3a, R3b, R3c, R3d, R4, R5, R5?, and m are defined herein, to pharmaceutical compositions comprising the compounds, and methods of using the compounds.Type: ApplicationFiled: May 23, 2013Publication date: September 11, 2014Applicant: MILLENNIUM PHARMACEUTICALS, INC.Inventors: Stephen CRITCHLEY, Thomas G. Gant, Steven P. Langston, Edward J. Olhava, Stephane Peluso
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Publication number: 20140256941Abstract: This invention relates to processes and intermediates for making {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile, useful in the treatment of diseases related to the activity of Janus kinases (JAK) including inflammatory disorders, autoimmune disorders, cancer, and other diseases.Type: ApplicationFiled: March 5, 2014Publication date: September 11, 2014Applicant: Incyte CorporationInventors: Pingli Liu, Dengjin Wang, Yongzhong Wu, Ganfeng Cao, Michael Xia
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Publication number: 20140256705Abstract: The present invention provides for compounds of formula (I) wherein R1, R2, A1, A2, A3, A4, X, and Y have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).Type: ApplicationFiled: March 11, 2014Publication date: September 11, 2014Inventors: Lisa A. Hasvold, Dachun Liu, Keith F. McDaniel, John Pratt, George S. Sheppard, Carol K. Wada, Kevin R. Woller
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Patent number: 8829013Abstract: The present invention provides salt forms of (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile that are useful in the modulation of Janus kinase activity and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.Type: GrantFiled: April 18, 2014Date of Patent: September 9, 2014Assignee: Incyte CorporationInventors: James D. Rodgers, Hui-Yin Li
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Publication number: 20140249168Abstract: The present application relates to novel trifluoromethyl-substituted fused pyrimidines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: February 28, 2014Publication date: September 4, 2014Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Markus FOLLMANN, Johannes-Peter STASCH, Gorden REDLICH, Dieter LANG, Alexandros VAKALOPOULOS, Frank WUNDER, Adrian TERSTEEGEN
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Patent number: 8822480Abstract: The present invention relates to Bicyclic Heterocycle Derivatives of Formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G-protein coupled receptor (GPCR) such as GPR119 in a patient.Type: GrantFiled: July 15, 2009Date of Patent: September 2, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Santhosh Francis Neelamkavil, Craig D. Boyle, Samuel Chackalamannil, William J. Greenlee, Bernard R. Neustadt, Andrew W. Stamford
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Patent number: 8822481Abstract: The present invention provides salt forms of (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile that are useful in the modulation of Janus kinase activity and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.Type: GrantFiled: April 18, 2014Date of Patent: September 2, 2014Assignee: Incyte CorporationInventors: James D. Rodgers, Hui-Yin Li
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Publication number: 20140243315Abstract: The ectopic expression of Mer receptor tyrosine kinase (Mer) has been identified as a tumor cell survival gene product in Acute Lymphoblastic Leukemia (ALL) cells and a potential cause of ALL chemoresistance. Hence, we investigated whether the development of small molecule Mer inhibitors was possible. A first aspect of the present invention is a compound (sometimes referred to as an “active compound” herein) of Formula I, IA, or IB.Type: ApplicationFiled: October 1, 2012Publication date: August 28, 2014Applicant: The University of North Carolina at Chapel HillInventors: Xiaodong Wang, Jing Liu, Weihe Zhang, Stephen Frye, Dmitri Kireev
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Publication number: 20140243312Abstract: Described herein are pyrrolo{2,3-d}pyrimidine derivatives, their use as Janus Kinase (JAK) inhibitors, and pharmaceutical compositions containing them.Type: ApplicationFiled: February 19, 2014Publication date: August 28, 2014Applicant: Pfizer Inc.Inventors: Matthew Frank Brown, Ashley Edward Fenwick, Mark Edward Flanagan, Andrea Gonzales, Timothy Allan Johnson, Neelu Kaila, Mark J. Mitton-Fry, Joseph Walter Strohbach, Ruth E. TenBrink, John David Trzupek, Rayomand Jal Unwalla, Michael L. Vazquez
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Publication number: 20140243306Abstract: The present invention describes new pyrrolo pyrimidine derivatives and pharmaceutically acceptable salts thereof which appear to interact with Bruton's tyrosine kinase (Btk). Accordingly, the novel pyrrolo pyrimidines may be effective in the treatment of autoimmune disorders, inflammatory diseases, allergic diseases, airway diseases, such as asthma and chronic obstructive pulmonary disease (COPD), transplant rejection, cancers e.g. of hematopoietic origin or solid tumors.Type: ApplicationFiled: July 7, 2012Publication date: August 28, 2014Applicant: NOVARTIS AGInventors: Richard Heng, Elizabeth Kate Hoegenauer, Guido Koch, Robert Alexander Pulz, Anna Vulpetti, Rudolf Waelchli
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Patent number: 8815876Abstract: The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G protein-coupled receptor (GPCR) in a patient. The compounds are of structure (I).Type: GrantFiled: July 15, 2009Date of Patent: August 26, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Santhosh Francis Neelamkavil, Craig D. Boyle, Bernard R. Neustadt, Samuel Chackalamannil, William J. Greenlee
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Patent number: 8815858Abstract: The invention is related to anti-viral compounds of formula (A) as defined in the claims, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well to processes and intermediates useful for preparing such compounds.Type: GrantFiled: May 20, 2011Date of Patent: August 26, 2014Assignee: Gilead Sciences, Inc.Inventors: Kyla Bjornson, Steven S. Bondy, You-chul Choi, Chien-Hung Chou, Ruchika Mishra, James D. Trenkle, Winston C. Tse, Randall W. Vivian, James G. Taylor
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Patent number: 8809352Abstract: The present invention includes novel compound and methods of treating a disease or disorder by antagonizing Bcl-2 family proteins, particularly compounds of formula (I): or pharmaceutically acceptable salt thereof, as well as methods of treating a disease, disorder, or syndrome associated with Bcl-2 inhibition, particularly hyperproliferative diseases. The present invention also includes pharmaceutical compositions including compounds of formula I and pharmaceutically acceptable salts thereof.Type: GrantFiled: September 8, 2010Date of Patent: August 19, 2014Assignee: Novartis AGInventors: Karen Miller-Moslin, Bakary-Barry Toure, Michael Scott Visser, Naeem Yusuff
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Publication number: 20140228366Abstract: The present application relates to novel heteroaryl-substituted pyrazolopyridines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: July 5, 2012Publication date: August 14, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Nils Griebenow, Dieter Lang, Frank Wunder
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Patent number: 8796294Abstract: The present invention is directed to a compound of Formula I or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula I to treat cancer.Type: GrantFiled: June 4, 2012Date of Patent: August 5, 2014Assignee: Exelixis Patent Company LLCInventors: Suleyman Bahceci, William Bajjalieh, Jeff Chen, Sergey Epshteyn, Timothy Patrick Forsyth, Tai Phat Huynh, Byung Gyu Kim, James W. Leahy, Matthew Sangyup Lee, Gary L. Lewis, Morrison B. Mac, Grace Mann, Charles K. Marlowe, Brian Hugh Ridgway, Joan C. Sangalang, Xian Shi, Craig Stacy Takeuchi, Yong Wang
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Publication number: 20140213574Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: ApplicationFiled: April 16, 2014Publication date: July 31, 2014Applicant: Celgene Avilomics Research, Inc.Inventors: Juswinder Singh, Russell Petter, Richland Wayne Tester, Arthur F. Kluge, Hormoz Mazdiyasni, William Frederick Westlin, III, Deqiang Niu, Lixin Qiao