Abstract: The invention generally relates to solid forms of berberine ursodeoxycholate, and to pharmaceutical compositions, and methods of preparation and therapeutic use thereof. In particular, the invention relates to solid forms of berberine ursodeoxycholate and pharmaceutical compositions thereof useful in treating and/or preventing various diseases or disorders, including metabolic disorders, heart diseases, neurodegenerative diseases and liver diseases.
Abstract: Compounds and methods are provided for the treatment of disease conditions in which modification of serotonergic receptor activity has a beneficial effect. In the method, an effective amount of a compound is administered to a patient in need of such treatment.
Type:
Grant
Filed:
March 21, 2011
Date of Patent:
September 19, 2017
Assignee:
ACADIA Pharmaceuticals Inc.
Inventors:
Carl-Magnus A. Andersson, Glenn Croston, Eva Louise Hansen, Allan Kjaersgaard Uldam
Abstract: The invention described herein pertains to processes for preparing tubulysin derivatives, conjugates of tubulysins, and intermediates therefore. In one illustrative embodiment of the invention, processes for derivatives or analogs of natural tubulysins including compounds of formula (T). In another embodiment, vitamin receptor binding conjugates of tubulysins are described. The processes include one or more steps described herein. In another embodiment, a process is described for preparing a compound of formula B, wherein R5 and R6 are as described in the various embodiments herein, such as each being independently selected from optionally substituted alkyl or optionally substituted cycloalkyl; and R8 is C1-C6 n-alkyl; wherein the process comprises the step of treating a compound of formula A with a silylating agent, such as triethylsilyl chloride, and a base, such as imidazole in an aprotic solvent.
Type:
Grant
Filed:
March 29, 2013
Date of Patent:
November 29, 2016
Assignee:
Endocyte, Inc.
Inventors:
Iontcho Radoslavov Vlahov, Hari Krishna R. Santhapuram, Paul Joseph Kleindl, Christopher Paul Leamon, Fei You
Abstract: 3-(3-Chloro-1H-pyrazol-1-yl)pyridine is prepared by cyclizing 3-hydrazinopyridine•dihydrochloride with acrylonitrile to provide 1-(pyridin-3-yl)-4,5-dihydro-1H-pyrazol-3-amine, by oxidizing to provide 3-(3-amino-1H-pyrazol-1-yl)pyridine, and by converting the amino group to a chloro group by a Sandmeyer reaction.
Type:
Grant
Filed:
October 17, 2014
Date of Patent:
February 2, 2016
Inventors:
Qiang Yang, Beth Lorsbach, Xiaoyong Li, Gary Roth, David E. Podhorez
Abstract: The present invention relates to compositions and methods for the treatment of infection by enveloped viruses, such as Ebola and Lassa fever viruses.
Type:
Grant
Filed:
September 1, 2011
Date of Patent:
November 24, 2015
Assignees:
President and Fellows of Harvard College, The Brigham and Women's Hospital, Inc.
Inventors:
James Cunningham, Kyungae Lee, Tao Ren, Kartik Chandran
Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.
Type:
Grant
Filed:
May 10, 2013
Date of Patent:
November 24, 2015
Assignee:
AbbVie Inc.
Inventors:
Richard F. Clark, Bryan Sorensen, Augustine T. Osuma, Robin Frey, Kenton Longenecker, George Doherty, Michael L. Curtin, Michael R. Michaelides, Ramzi F. Sweis, Marina A. Pliushchev, Andy Judd, Todd M. Hansen, Howard R. Heyman
Abstract: The present invention relates to compounds of the general formula (S-A)n-T, in which at least one fluorescent group S is linked to a phosphorescent group T via a divalent group A, to the use thereof in an electronic device, and to a formula to a formulation and an electronic device which comprise the novel compounds.
Abstract: Disclosed is a compound of formula I, a stereoisomer thereof, a cis-trans-isomer thereof, a tautomer thereof, or a mixture thereof, or a pharmaceutically acceptable salt thereof, a solvate thereof or a prodrug thereof, wherein R1, R2, R3 and R4 are each as defined in the present application.
Type:
Grant
Filed:
June 8, 2011
Date of Patent:
November 17, 2015
Assignee:
Tianjin Hemay Bio-Tech Co., LTD.
Inventors:
Hesheng Zhang, Yingwei Chen, Qingchao He
Abstract: Substituted 5-(cyclohex-2-en-1-yl)-penta-2,4-dienes and 5-(cyclohex-2-en-1-yl)-pent-2-en-4-ynes as active agents against abiotic stress in plants The invention relates to substituted 5-(cyclohex-2-en-1-yl)penta-2,4-dienes and 5-(cyclohex-2-en-1-yl)pent-2-en-4-ynes of the formula (I) and their salts where the radicals R1, R2, R3, R4, [X—Y] and Q are each as defined in the description, to processes for preparation thereof and to the use thereof for enhancing stress tolerance in plants with respect to abiotic stress, and/or for increasing plant yield.
Type:
Grant
Filed:
March 28, 2012
Date of Patent:
November 17, 2015
Assignee:
BAYER INTELLECTUAL PROPERTY GMBH
Inventors:
Jens Frackenpohl, Thomas Müller, Ines Heinemann, Pascal Von Koskull-Döring, Christopher Hugh Rosinger, Isolde Häuser-Hahn, Martin Jeffrey Hills
Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.
Type:
Grant
Filed:
May 10, 2013
Date of Patent:
November 17, 2015
Assignee:
AbbVie Inc.
Inventors:
Richard F. Clark, Bryan Sorensen, Augustine T. Osuma, Robin Frey, Kenton Longenecker, George Doherty, Michael L. Curtin, Michael R. Michaelides, Ramzi F. Sweis, Marina A. Pliushchev, Andy Judd, Todd M. Hansen, Howard R. Heyman
Abstract: The present invention provides tricyclic fused thiophene derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
Abstract: The invention relates to compounds of macrocyclic picolinamides of Formula I suitable to control or prevent growth of fungi.
Type:
Grant
Filed:
September 29, 2014
Date of Patent:
November 10, 2015
Assignee:
Dow AgroSciences LLC
Inventors:
Timothy P. Martin, Kevin G. Meyer, Benjamin Nugent, Chenglin Yao, W. John Owen, Anne M. Wilson, Ian O'Callaghan, Jeremy Wilmot, Johnathan E. DeLorbe, William Dent, III
Abstract: The present invention relates to novel compounds of formula (A) and (B) as modulators of GPR-119, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of GPR-119 mediated diseases or disorders with them.
Type:
Grant
Filed:
June 8, 2012
Date of Patent:
November 10, 2015
Assignee:
RHIZEN PHARMACEUTICALS SA
Inventors:
Dhanapalan Nagarathnam, Swaroop Kumar V. S. Vakkalanka, Srikant Viswanadha, Gayatri S. Merikapudi
Abstract: Certain 2-halophenyl, 2,4-dihalophenyl (e.g. 2,4-dichlorophenyl), 3,4-dichlorophenyl (e.g. 3,4-dichlorophenyl), 2,6-dichlorophenyl (2,6-dichlorophenyl) and 2,5-diakoxyphenyl (e.g. 2,5-dimethoxyphenyl) derivatives of tetrahydro-?-carbolines are provided, along with their pharmaceutically acceptable salts; prodrugs and solvates, and compositions containing the compounds. The compounds are useful for the prevention and treatment of cancer, and other indications where PDE5 inhibitors have shown benefits including erectile dysfunction, pulmonary hypertension, enhancing cognitive function, cystic fibrosis, or enhancing the activity of conventional chemotherapeutic drugs. Methods for fabricating the compounds are also provided.
Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are diazole lactam derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.
Type:
Grant
Filed:
December 20, 2013
Date of Patent:
October 27, 2015
Assignee:
ChemoCentryx, Inc.
Inventors:
Xi Chen, Dean R. Dragoli, Pingchen Fan, Juan C. Jaen, Yandong Li, Jay P. Powers, Viengkham Malathong, Sreenivas Punna, Hiroko Tanaka, Penglie Zhang
Abstract: Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the retrovirus family of viruses such as the Human Immunodeficiency Virus (HIV).
Type:
Grant
Filed:
July 10, 2013
Date of Patent:
October 20, 2015
Assignee:
ViiV Healthcare UK Limited
Inventors:
Martha Alicia De La Rosa, Brian Alvin Johns, Wieslaw Mieczyslaw Kazmierski, Vicente Samano, Lita Suwandi, David Temelkoff, Emile Velthuisen, Jason Gordon Weatherhead
Abstract: The invention provides compounds of formula (I) and methods of treating a Mycobacterium infection or tuberculosis, or inhibiting DprE1 with the same.
Type:
Grant
Filed:
July 10, 2014
Date of Patent:
October 20, 2015
Assignees:
Global Alliance for TB Drug Development, Foundation for Neglected Disease Research
Inventors:
Pravin S. Shirude, Maruti N. Naik, Vikas Narayan Shinde, Shahul Hameed Peer Mohamed, Monalisa Chatterji, Radha K. Shindil
Abstract: The present invention concerns derivatives of heteroarylsulfonamides, notably as blockers of Kv potassium channels, and more particularly of channels Kv1.5, Kv4.3 or Kv11.1, their application in clinical therapy and their preparation methods. These compounds correspond to the following general formula (I): where R1 represents one or more substituents of the phenyl core X such as: hydrogen, halogen, trifluoromethyl, trifluoromethoxy, linear or branched C1-C4 alkyl, or linear or branched C1-C4 alkoxy, A represents oxygen or sulphur, B represents nitrogen when n=1 or 2 and D represents —C(?O)—, or B represents CH when n=0 and D represents —CH2O— or when n=1 and D represents —O—, R2 represents a hydrogen, a methyl, a fluorine or chlorine atom or a methoxy, HetAr represents a pyridyl or quinolyl group, possibly substituted by a group such as a linear or branched C1-C4 alkyl, a linear or branched C1-C4 alkoxy, a halogen, or a trifluoromethyl, and to their pharmaceutically acceptable salts.
Type:
Grant
Filed:
August 15, 2014
Date of Patent:
October 13, 2015
Assignee:
PIERRE FABRE MEDICAMENT
Inventors:
Elisabeth Dupont-Passelaigue, Isabelle Le Roy, Christophe Pignier
Abstract: The present invention relates to compounds defined by formula I wherein the variables R1-R8 are defined as in the description, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of cholesterol ester transfer protein (CETP) and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this protein.
Type:
Grant
Filed:
August 16, 2012
Date of Patent:
October 6, 2015
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Thomas Trieselmann, Dieter Hamprecht, Holger Wagner