Plural Piperidine Rings Patents (Class 514/316)
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Publication number: 20140275010Abstract: The present invention provides quaternary salts, such as those of Formula I: as well as the use thereof in methods of treatment for cancer.Type: ApplicationFiled: March 11, 2014Publication date: September 18, 2014Inventors: Guo Zhu Zheng, Yuan Wang, Gregg F. Keany, Kenzo Arai, Kazunobu Kira, Xiang Liu, Nick Gearhart, Baudouin Gerard
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Publication number: 20140275110Abstract: The present invention relates to novel amidomethyl-substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-dependent disorders.Type: ApplicationFiled: April 11, 2014Publication date: September 18, 2014Inventors: Thorsten Oost, Astrid Netz, Hervé Geneste, Wilfried Braje, Wolfgang Wernet, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch
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Patent number: 8835419Abstract: Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.Type: GrantFiled: November 30, 2012Date of Patent: September 16, 2014Assignee: ChemoCentryx, Inc.Inventors: Trevor T. Charvat, Junfa Fan, Christopher W. Lange, Manmohan Reddy Leleti, Yandong Li, Venkat Reddy Mali, Jeffrey P. MacMahon, Jay Powers, Sreenivas Punna, Ju Yang
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Patent number: 8835648Abstract: Heterocyclic compounds that modulate the hedgehog signaling pathway, pharmaceutical composition thereof and their therapeutic applications.Type: GrantFiled: June 9, 2010Date of Patent: September 16, 2014Assignee: Siena Biotech S.p.A.Inventors: J. Russell Thomas, Gal.la Pericot Mohr, Chiara Caramelli, Giacomo Minetto, Marta Bellini
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Publication number: 20140256699Abstract: Substituted cyclopropyl compounds of the formula I and the pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the g-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included. Another aspect of the invention that is of interest relates to compounds of formula Ia.Type: ApplicationFiled: September 24, 2012Publication date: September 11, 2014Inventors: Michael W. Miller, Andrew W. Stamford, Kallol Basu, Scott Edmondson, Zhiqiang Guo, William B. Geiss
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Publication number: 20140256756Abstract: Compounds of Formula (I) and pharmaceutically acceptable salts thereof in which X1, X2, X3, L, R3, R4, R5, R7 and n have the meanings given in the specification, are modulators of GPR119 and are useful in the treatment or prevention of diseases such as, but not limited to, type 2 diabetes, diabetic complications, symptoms of diabetes, metabolic syndrome, obesity, dyslipidemia, and related conditions.Type: ApplicationFiled: October 30, 2012Publication date: September 11, 2014Inventors: Thomas Daniel Aicher, Josef Roland Benscik, Steven Armen Boyd, Kevin Ronald Condroski, Jay Bradford Fell, John Peter Fischer, Ronald Jay Hinklin, Scott Pratt, Ajay Singh, Timothy M. Turner
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Patent number: 8829199Abstract: A compound represented by formula (I) or a pharmacologically acceptable salt thereof, which can inhibit a fibroblast growth factor receptor (FGFR) family kinase in cancer tissues. (In the formula, A represents a 5- to 10-membered heteroaryl group, or a C6-10 aryl group; R1 and R2 independently represent H, OH, X, CN, NO2, a C1-4 haloalkyl group, a C1-6 alkyl group, or the like <R1 and R2 together form a (substituted) 3- to 10-membered heterocyclyl group or a (substituted) 5- to 10-membered heteroaryl group>; R3 represents H, a C1-5 alkyl group, a C6-10 aryl group, a C1-5 alkyl group, or a C1-4 haloalkyl group; and R4 represents H, X, a C1-3 alkyl group, a C1-4 haloalkyl group, OH, CN, NO2, or the like.Type: GrantFiled: August 5, 2010Date of Patent: September 9, 2014Assignees: Chugai Seiyaku Kabushiki Kaisha, F. Hoffmann-La Roche AGInventors: Naoki Taka, Masayuki Ohmori, Kyoko Takami, Masayuki Matsushita, Tadakatsu Hayase, Ikumi Hyodo, Masami Kochi, Hiroki Nishii, Hirosato Ebiike, Yoshito Nakanishi, Toshiyuki Mio, Lisha Wang, Weili Zhao
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Publication number: 20140249130Abstract: The present invention provides novel pyrimidine amines of formula I which are potent inhibitors of spleen tyrosine kinase, or are prodrugs thereof, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis and cancer.Type: ApplicationFiled: May 4, 2012Publication date: September 4, 2014Inventors: Denis Deschenes, Michael D. Altman, John Michael Ellis, Christian Fischer, Andrew M. Haidle, Solomon D. Kattar, Alan B. Northrup, Adam J. Schell, Graham F. Smith, Brandon M. Taoka, Corey Bienstock, Maria Emilia Di Francesco, Anthony Donofrio, Scott Peterson, Kerrie B. Spencer, James Patrick Jewell, Amjad Ali, David Jonathan Bennett, Qun Dang, John Wai
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Patent number: 8815869Abstract: The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein Ar1, n, R1, X and Y are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: GrantFiled: March 10, 2011Date of Patent: August 26, 2014Assignee: AbbVie Inc.Inventors: Irene Drizin, George Doherty, Pramila A. Bhatia, Andrew O. Stewart
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Patent number: 8815905Abstract: The invention relates to propionic acids, propionic acid esters, and related compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds for the treatment of various diseases or conditions, including but not limited to diseases and/or conditions of Central Nervous System (CNS).Type: GrantFiled: March 8, 2011Date of Patent: August 26, 2014Assignee: Promentis Pharmaceuticals, Inc.Inventors: Mark A. Wolf, Keith D. Barnes
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Patent number: 8815857Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1-R5 and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: GrantFiled: August 9, 2012Date of Patent: August 26, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Todd Bosanac, Angela Berry, John David Ginn, Tamara Denise Hopkins, Sabine Schlyer, Fariba Soleymanzadeh, John Westbrook, Maolin Yu, Zhonghua Zhang
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Publication number: 20140235641Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.Type: ApplicationFiled: September 21, 2012Publication date: August 21, 2014Inventors: Jason Brubaker, Joshua Close, Tony Siu, Graham Frank Smith, Luis E. Torres, Hyun Chong Woo, Jonathan R. Young, Zhongyong Wei, Feng Shi
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Publication number: 20140235611Abstract: The compound represented by the formula (I-1): wherein all the symbols have the same meanings as described in the specification, has two cyclic groups, particularly phenoxy groups at specific substitution positions and thus has high human S1P2 antagonistic activity. The compound may therefore be used as a therapeutic agent for S1P2-mediated diseases such as diseases resulting from vascular constriction, fibrosis and respiratory diseases.Type: ApplicationFiled: September 27, 2012Publication date: August 21, 2014Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Atsushi Naganawa, Kensuke Kusumi, Kazuhiro Otsuki, Tetsuya Sekiguchi, Akito Kakuuchi, Koji Shinozaki, Hiroshi Yamamoto, Shigeyuki Nonaka
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Patent number: 8809362Abstract: To provide a marker for determining sensitivity of a patient to an anti-cancer agent, and novel cancer therapeutic means employing the marker. The marker for determining sensitivity to an anti-cancer agent is formed of one or more substances selected from the group consisting of a substance or a fragment thereof detected as an anion at m/z of 149.05 to 149.06, a substance or a fragment thereof detected as an anion at m/z of 152.99 to 153.00, a substance or a fragment thereof detected as a cation at m/z of 724.34 to 724.35, the peaks being determined by means of a mass spectrometer, glycerol 3-phosphate, dihydrobiopterin, GABA, lactic acid, asparagine, aspartic acid, 2-methylbutyroylcarnitine, 1-methyladenosine, and glutathione, and a substance involved in a metabolic pathway of any of these substances.Type: GrantFiled: October 29, 2010Date of Patent: August 19, 2014Assignees: Keio University, Kabushiki Kaisha Yakult HonshaInventors: Yusuke Tanigawara, Tetsuya Suzuki, Akito Nishimuta, Shinji Sugimoto, Yoshiaki Igarashi
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Publication number: 20140221334Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. 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. The invention also provides processes for preparing compounds of the inventions.Type: ApplicationFiled: April 10, 2014Publication date: August 7, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Juan-Miguel Jimenez, Guy William Bemis, Francois Maltais, Tiansheng Wang, Ronald Marcellus Alphonsus Knegtel, Christopher John Davis, Damien Fraysse, Dean Boyall, Luca Settimo, Stephen Young, Michael Paul Mortimore
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Publication number: 20140221384Abstract: The present invention relates to nordihydroguaiaretic acid derivative compounds, namely, butane bridge modified nordihydroguaiaretic acid (NDGA) compounds and butane bridge modified tetra-O-substituted NDGA compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, metabolic diseases, such as diabetes and hypertension, or a proliferative disease, such as diverse types of cancers.Type: ApplicationFiled: April 7, 2014Publication date: August 7, 2014Applicant: ERIMOS PHARMACEUTICALS LLCInventors: Jonathan Daniel Heller, Qingqi Chen, Rocio Alejandra Lopez, Amanda Jean Morris
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Patent number: 8795699Abstract: A method of repelling wasps, which method comprises using a preparation comprising (a) one or more of ethyl 3-(N-n-butyl-N-acetylamino)propionate, dihydronepetalactone, and extract of catmint, and (b) at least one compound selected from certain perfume ingredients. This abstract is neither intended to define the invention disclosed in this specification nor intended to limit the scope of the invention in any way.Type: GrantFiled: May 14, 2008Date of Patent: August 5, 2014Assignee: Beiersdorf AGInventors: Rainer Kroepke, Jens Schulz, Jens Nielsen, Stephanie Von Der Fecht
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Patent number: 8796254Abstract: Disclosed are uses of carboxamide, sulfonamide and amine compounds for the treatment and amelioration of disorders and conditions related to oxidative stress, mitochondrial dysfunction, free radical damage and metabolic inefficiency, among others. Also described are methods for increasing exercise endurance, exercise efficiency and aerobic workload using the compounds described herein.Type: GrantFiled: March 31, 2011Date of Patent: August 5, 2014Assignee: Rigel Pharmaceuticals, Inc.Inventors: Donald Payan, Yasumichi Hitoshi, Todd Kinsella
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Patent number: 8791136Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: GrantFiled: July 29, 2011Date of Patent: July 29, 2014Assignee: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Donald Payan, Rajinder Singh, Simon Shaw, David Carroll, Yasumichi Hitoshi
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Patent number: 8785449Abstract: Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R3, R4, D, J, Z, T, p, q, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: GrantFiled: September 18, 2012Date of Patent: July 22, 2014Assignee: Rigel Pharmaceuticals, Inc.Inventors: Jiaxin Yu, Hui Hong, Ihab S. Darwish, Xiang Xu, Rajinder Singh
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Patent number: 8778929Abstract: The present invention relates to new compounds of general formula (I), wherein the groups R1 to R3, X1, X2, X3 and L1 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof in such a treatment.Type: GrantFiled: September 28, 2009Date of Patent: July 15, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Steffen Steurer, Peter Ettmayer, Andreas Mantoulidis
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Publication number: 20140194440Abstract: The present invention relates to novel 5,6-disubstituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the manufacture of a medicament.Type: ApplicationFiled: September 27, 2013Publication date: July 10, 2014Inventors: Wilfried Braje, Thorsten Oost, Astrid Netz, Wolfgang Wernet, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch
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Publication number: 20140187546Abstract: Cystine analogs that improve the solubility of L-cystine in urine for treatment of cystinuria and which have the structure: and pharmaceutically acceptable salts, solvates and prodrugs thereof, wherein each R and R? pair are independently selected from (i) or (ii); (i) R and R? are independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alcohol, substituted or unsubstituted aryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocyclic, and substituted or unsubstituted heteroaryl, or (ii) R and R? together form a substituted or unsubstituted heterocyclic ring structure, or a substituted or unsubstituted heteroaryl ring structure; X is hydrogen, or an alkyl; and Y is O or S.Type: ApplicationFiled: January 2, 2014Publication date: July 3, 2014Applicant: Rutgers, The State University of New JerseyInventors: Longqin Hu, Amrik Sahota
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Publication number: 20140187581Abstract: The present invention relates to novel compounds of formula (I), and their pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their pharmaceutically acceptable salts. The compounds of formula (I) are useful in the treatment of various disorders that are related to 5-HT4 receptors.Type: ApplicationFiled: January 5, 2012Publication date: July 3, 2014Applicant: SUVEN LIFE SCIENCES LIMITEDInventors: Ramakrishna Nirogi, Abdul Rasheed Mohammed, Suresh Yarlagadda, Srinivasa Rao Ravella, Anil Karbhari Shinde, Ramasastri Kamphampati, Praveen Kumar Roayapalley, Pradeep Jayarajan, Gopinadh Bhyrapuneni, Sriramachandra Murthy Patnala, Jyothsna Ravula, Venkateswarlu Jasti
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Patent number: 8765764Abstract: A 2-acylaminothiazole derivative or a pharmaceutically acceptable salt thereof having an excellent effect of proliferating human c-mpl-Ba/F3 cells and an activity of increasing platelets based on the effect of promoting the formation of megakaryocytic colonies. A compound or a pharmaceutically acceptable salt thereof useful in treating thrombocytopenia.Type: GrantFiled: November 15, 2012Date of Patent: July 1, 2014Assignee: Astellas Pharma, Inc.Inventors: Keizo Sugasawa, Susumu Watanuki, Yuji Koga, Hiroshi Nagata, Ryutaro Wakayama, Fukushi Hirayama, Ken-Ichi Suzuki
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Publication number: 20140179737Abstract: This invention is directed to derivatives of piperidine-2,6-dione, or their organic or inorganic salts thereof, a methods of synthesis of these derivatives, and their application as active pharmaceutical ingredient as inhibitors of TNF? releasing in cells, the derivative of piperidine-2,6-dione being of the general formula (I): wherein n represents 1, 2, 3, 4, 5 or 6; R1 represents from one to four of the same or different substituents selected from F, Cl, Br, C1-4 alkyl, OH, OC1-4 alkyl, NO2, NHC(O)C1-4 alkyl, NH2, NH(C1-4 alkyl), N(C1-4 alkyl)2; R2 represents OR3, NR3R4, N(R3)COR4, O2CR5; R3 and R4 represent independently and at each occurrence H or C1-4 alkyl; R5 represents CHR6NR7R8, CHR6NR9C(O)CHR10NR7R8, a heterocycle W or CHR6NR9C(O)W; R6, R9, R10 represent independently and at each occurrence H, or C1-4 alkyl; R7 and R8 represent independently and at each occurrence H, C1-4 alkyl, or R7 and R8 taken together represent 1,3-propylene, 1,4-butylene, 1,5-pentylene, or 1,6-hexylene; W represents four-mType: ApplicationFiled: December 18, 2013Publication date: June 26, 2014Applicant: Tianjin Hemay Bio-Tech Co., Ltd.Inventor: Hesheng Zhang
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Publication number: 20140179738Abstract: The present invention provides N-substituted-heterocycloalkyloxybenzamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment of the invention is a compound having the structure in which R1, R2, R3, R4, T, n, w and x are as described herein. In certain embodiments of the invention, a compound of the present invention activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: ApplicationFiled: February 25, 2014Publication date: June 26, 2014Applicant: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Jiaxin Yu, Hui Hong, Sambaiah Thota, Xiang Xu, Ihab S. Darwish
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Publication number: 20140179686Abstract: The present invention relates to novel vanilloid receptor ligands, to a process for the production thereof, to pharmaceutical preparations containing these compounds and to the use of these compounds for the production of pharmaceutical preparations.Type: ApplicationFiled: February 25, 2014Publication date: June 26, 2014Applicant: Gruenenthal GmbHInventors: Jeewoo LEE, Hyung Chul Ryu, Robert FRANK, Gregor BAHRENBERG, Jean DE VRY, Thomas CHRISTOPH, Derek John SAUNDERS, Klaus SCHIENE, Bernd SUNDERMANN
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Publication number: 20140171397Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, s, t, W, Ar1, R1, R2, R3, R4, R6, R7, and R8 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: ApplicationFiled: September 11, 2013Publication date: June 19, 2014Applicant: THERAVANCE, INC.Inventors: Mathai Mammen, YuHua Ji, YongQi Mu, Craig Husfeld, Li Li
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Patent number: 8754225Abstract: The invention provides a process of preparing an intermediate useful in the synthesis of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and a process of preparing a crystalline freebase of the ester.Type: GrantFiled: June 30, 2011Date of Patent: June 17, 2014Assignee: Theravance, Inc.Inventor: Pierre-Jean Colson
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Publication number: 20140161731Abstract: Described are a compound of formula (II) or (III): The compounds are effective in the treatment of disease, including a tauopathy condition or a disease of tau protein aggregation.Type: ApplicationFiled: February 14, 2014Publication date: June 12, 2014Applicant: WisTa Laboratories Ltd.Inventors: Scott Clunas, John Mervyn David Storey, Janet Elizabeth Rickard, David Horsley, Charles Robert Harrington, Claude Michel Wischik
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Patent number: 8741894Abstract: Provided herein are arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.Type: GrantFiled: March 17, 2011Date of Patent: June 3, 2014Assignee: Axikin Pharmaceuticals, Inc.Inventors: Tai Wei Ly, Garrett Thomas Potter, Jared Andrew Forrester
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Publication number: 20140148467Abstract: Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R3, R4, D, J, Z, T, p, q, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: ApplicationFiled: February 3, 2014Publication date: May 29, 2014Applicant: Rigel Pharmaceuticals, Inc.Inventors: Jiaxin Yu, Hui Hong, Ihab S. Darwish, Xiang Xu, Rajinder Singh
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Patent number: 8735426Abstract: Compounds corresponding to formula I: which act as vanilloid receptor ligands, pharmaceutical compositions containing such compounds, a process for the producing such compounds, and the use thereof to treat or inhibit pain and/or various other disorders or conditions.Type: GrantFiled: April 11, 2008Date of Patent: May 27, 2014Assignee: Gruenenthal GmbHInventors: Robert Frank, Gregor Bahrenberg, Thomas Christoph, Klaus Schiene, Jean De Vry, Derek Saunders, Bernd Sundermann, Jeewoo Lee
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Publication number: 20140142081Abstract: Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.Type: ApplicationFiled: November 21, 2013Publication date: May 22, 2014Applicant: AGIOS PHARMACEUTICALS, INCInventors: Rene M. Lemieux, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Jeremy Travins, Yongsheng Chen
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Publication number: 20140142067Abstract: The present invention is directed to use of a series of compounds and compositions comprising the same for activating telomerase and treating diseases, disorders and/or conditions related thereto.Type: ApplicationFiled: November 12, 2013Publication date: May 22, 2014Applicant: BEN-GURION UNIVERSITY OF THE NEGEV RESEARCH AND DEVELOPMENT AUTHORITYInventors: Aviv GAZIT, Shimon SLAVIN, Esther PRIEL, Sara YITZCHAK
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Patent number: 8729081Abstract: The present invention provides compounds which antagonize epsilon protein kinase C (PKC?). These compounds have a structural formula (Ia), (Ic) or (II). The present invention also provides pharmaceutical compositions containing these compounds and methods of treating various diseases, conditions, and/or symptoms by using these compounds.Type: GrantFiled: October 12, 2009Date of Patent: May 20, 2014Assignee: VM Discovery Inc.Inventor: Jay Jie-Qiang Wu
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Publication number: 20140135304Abstract: The present invention relates to novel compounds of formula (I), and their pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their pharmaceutically acceptable salts. The compounds of formula (I) are useful in the treatment of various disorders that are related to Histamine H3 receptors.Type: ApplicationFiled: June 7, 2011Publication date: May 15, 2014Applicant: SUVEN LIFE SCIENCES LIMITEDInventors: Ramakrishna Nirogi, Anil Karbhari Shinde, Ramasastri Kambhampati, Amol Dinakar Deshpande, Adi Reddy Dwarampudi, Narasimhareddy Gangadasari, Sangram Keshari Saraf, Vishwottam Nagaraj Kandikere, Pradeep Jayarajan, Ishtiyaque Ahmad, Mohmadsadik Abdulhamid Mulla, Venkateswarlu Jasti
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Publication number: 20140135314Abstract: Piperidine compounds and pharmaceutically useful salts thereof, a pharmaceutical composition including an effective amount of the racemic or enantiomerically enriched piperidine compounds to treat gastrointestinal diseases, and a method of treating gastrointestinal diseases in a mammal are provided.Type: ApplicationFiled: January 17, 2014Publication date: May 15, 2014Applicant: SK BIOPHARMACEUTICALS CO., LTD.Inventors: Coo-Min CHUNG, Hyung-Jin JUN, Jin-Sung KIM, Hui-Ho KIM, Hye-Kyung MIN, Yong-Gil KIM, Jong-Gil CHOI, Hongwook KIM
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Patent number: 8722742Abstract: Use of chemical compounds obtained in silico for the preparation of pharmaceutical compositions to attenuate or inhibit Dengue virus infection. Particularly, through the interference or the modulation of several stages of viral replication cycle related with the entry of virus into host cells and the assembly of mature progeny virions. The invention also comprises the use of such pharmaceutical compositions for prophylactic and/or therapeutic treatment of infection caused by all four serotypes of Dengue virus and other flaviviruses.Type: GrantFiled: February 27, 2009Date of Patent: May 13, 2014Assignee: Centro de Ingenieria Genetica y BiotecnologiaInventors: Yuliet Mazola Reyes, Glay Chinea Santiago, Osmany Guirola Cruz, Roberto Vera Alvarez, Vivian Huerta Galindo, Noralvis Fleitas Salazar, Alexis Musacchio Lasa
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Publication number: 20140128395Abstract: There is provided inter alia a compound which is an NK-1 receptor antagonist for use in the treatment or prevention of CNV. There is also provided a compound which is an NK-1 antagonist for use in the treatment of chemical burns of the eye particularly alkali burns of the eye. There is also provided a pharmaceutical composition for topical administration to the eye comprising an NK-1 antagonist and an antibiotic agent.Type: ApplicationFiled: July 4, 2012Publication date: May 8, 2014Inventor: Giulio Ferrari
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Patent number: 8716312Abstract: The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.Type: GrantFiled: November 17, 2009Date of Patent: May 6, 2014Assignee: Merck Sharp & Dohme CorporationInventors: Pauline C. Ting, Robert Aslanian, Mary Ann Caplen, Jianhua Cao, Tin-Yau Chan, David Kim, Hyunjin Kim, Jae-Hun Kim, Rongze Kuang, Joe F. Lee, John Schwerdt, Heping Wu, Nicolas Zorn
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Patent number: 8716313Abstract: The invention provides crystalline forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and pharmaceutically acceptable solvates thereof. The crystalline form can be a freebase, or a salt such as a diphosphate, monosulfate or dioxalate salt. The invention also provides pharmaceutical compositions comprising these crystalline compounds or prepared using these compounds; processes and intermediates for preparing the crystalline compounds; and methods of using these compounds to treat a pulmonary disorder.Type: GrantFiled: January 14, 2013Date of Patent: May 6, 2014Assignee: Theravance, Inc.Inventors: Sabine Axt, Timothy J Church
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Publication number: 20140121195Abstract: Benzimidazole, benzopyrazole and benzotriazole compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.Type: ApplicationFiled: October 17, 2013Publication date: May 1, 2014Applicant: ChemoCentryx, Inc.Inventors: Manmohan Reddy Leleti, Yandong Li, Venkat Reddy Mali, Jay Powers, Ju Yang
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Patent number: 8703803Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylocholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and or gastrointestinal tract disorders.Type: GrantFiled: September 21, 2012Date of Patent: April 22, 2014Inventors: Peter A. Crooks, Linda P. Dwoskin, Roger Papke, Guangrong Zheng, Sangeetha Sumithran
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Patent number: 8703934Abstract: The present application relates to novel substituted 4-amino-3,5-dicyano-2-thiopyridine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of hypertension and other cardiovascular disorders.Type: GrantFiled: November 17, 2007Date of Patent: April 22, 2014Assignee: Bayer Intellectual Property GmbHInventors: Peter Nell, Nicole Diedrichs, Barbara Albrecht-Küpper, Alexandros Vakalopoulos, Frank Süβmeier, Joerg Keldenich
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Patent number: 8703774Abstract: The present invention relates to novel carbamate-substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-dependent disorders.Type: GrantFiled: December 5, 2008Date of Patent: April 22, 2014Assignee: AbbVie Deutschland GmbH & Co. KGInventors: Astrid Netz, Thorsten Oost, Herve Geneste, Wilfried Braje, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch, Andrea Hager-Wernet
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Patent number: 8703775Abstract: The present invention relates to novel amidomethyl-substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-dependent disorders.Type: GrantFiled: December 5, 2008Date of Patent: April 22, 2014Assignee: AbbVie Deutschland GmbH & Co. KGInventors: Thorsten Oost, Astrid Netz, Herve Geneste, Wilfried Braje, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch, Andrea Hager-Wernet
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Patent number: 8697727Abstract: The present invention provides N-substituted-heterocycloalkyloxybenzamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment of the invention is a compound having the structure in which R1, R2, R3, R4, T, n, w and x are as described herein. In certain embodiments of the invention, a compound of the present invention activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: GrantFiled: July 18, 2011Date of Patent: April 15, 2014Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Jiaxin Yu, Hui Hong, Sambaiah Thota, Xiang Xu, Ihab S. Darwish
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Patent number: 8691845Abstract: The present invention relates to nordihydroguaiaretic acid derivative compounds, namely, butane bridge modified nordihydroguaiaretic acid (NDGA) compounds and butane bridge modified tetra-O-substituted NDGA compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, metabolic diseases, such as diabetes and hypertension, or a proliferative disease, such as diverse types of cancers.Type: GrantFiled: July 30, 2012Date of Patent: April 8, 2014Assignee: Erimos Pharmaceuticals LLCInventors: Jonathan Daniel Heller, Qingqi Chen, Rocio Alejandra Lopez, Amanda Jean Morris