Tricyclo Ring System Having The Five-membered Hetero Ring As One Of The Cyclos Patents (Class 514/411)
  • Patent number: 10406137
    Abstract: Polymorph forms of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide are disclosed as well as their methods of synthesis and pharmaceutical compositions.
    Type: Grant
    Filed: July 2, 2018
    Date of Patent: September 10, 2019
    Assignee: Siga Technologies Inc.
    Inventors: Shanthakumar R. Tyavanagimatt, Melialani A.C.L.S. Anderson, William C. Weimers, Dylan Nelson, Tove′ C. Bolken, Dennis E. Hruby, Michael H. O'Neill, Gary Sweetapple, Kelley A. McCloughan
  • Patent number: 10383851
    Abstract: The invention includes an amount of (3aR)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-5-yl phenylcarbamate for administering to a subject and also a method of preventing or treating neurotoxicity or neurodegenerative processes in a subject in need thereof using the amount thereof.
    Type: Grant
    Filed: March 6, 2017
    Date of Patent: August 20, 2019
    Assignee: QR PHARMA, INC.
    Inventor: Maria Maccecchini
  • Patent number: 10370329
    Abstract: A process for the resolution of racemic 2-(3-ethoxy-4-methoxyphenyl)-1-(methylsulphonyl)-eth-2-ylamine using novel chiral salts is disclosed. An L-phenylalanine p-toluene-sulfonamide salt of (S)-2-(3-ethoxy-4-methoxyphenyl)-1-(methylsulphonyl)-eth-2-ylamine and a di-p-toluoyl-L-tartaric acid salt of (S)-2-(3-ethoxy-4-methoxyphenyl)-1-(methylsulphonyl)-eth-2-ylamine are also provided.
    Type: Grant
    Filed: April 22, 2016
    Date of Patent: August 6, 2019
    Inventors: Ramesh Dandala, Sureshbabu Jayachandra, Vipin Kumar Kaushik, Nageshwara Rao Achanta, Sivaprasad Dorasala
  • Patent number: 10370385
    Abstract: Compounds that inhibit digestion in blood-ingesting pests are described herein. In one embodiment, the compounds described herein block entry of blood into the midgut and thereby inhibit digestion and nutrient processing. In another embodiment, the compounds described herein prevent pathogens contained in the blood meal from entering the midgut where they could cross the epithelial cell layer and infect the mosquito. The compounds can be administered to a population of blood-ingesting pests, such as mosquitos, directly or indirectly in an effective amount to prevent mosquitoes from transmitting diseases such as malaria, dengue fever, West Nile virus and lymphatic filariasis. Preferably, the compounds are lethal to blood-ingesting pests. The compounds can be combined with one or more excipients to prepare compositions.
    Type: Grant
    Filed: July 10, 2015
    Date of Patent: August 6, 2019
    Assignee: Arizona Board of Regents on Behalf of the University of Arizona
    Inventors: Jon Njardarson, Jun Isoe, Roger Miesfeld
  • Patent number: 10328052
    Abstract: The present invention relates to the compound ((2R,2?R)-bis(((tetrahydro-2H-pyran-4-carbonyl)oxy)methyl) 1,1?-adipoylbis(pyrrolidine-2-carboxylate), pharmaceutical compositions comprising the same and the use of the same for treatment of diseases or disorders wherein depletion of serum amyloid P component (SAP) would be beneficial, including amyloidosis, Alzheimer's disease, type 2 diabetes mellitus and osteoarthritis.
    Type: Grant
    Filed: October 25, 2016
    Date of Patent: June 25, 2019
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Alexis Denis, Olivier Mirguet, Jérôme Toum
  • Patent number: 10301262
    Abstract: The present invention relates to, inter alia, a novel crystalline free-plate habit or morphology, processes for preparing the crystalline free-plate habit, and uses of the crystalline free-plate habit of the L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid (Compound 1) in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in the vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development, and atherosclerosis).
    Type: Grant
    Filed: June 21, 2016
    Date of Patent: May 28, 2019
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Anthony C. Blackburn, Ryan O. Castro, Mark Allen Hadd, You-An Ma, Antonio Garrido Montalban, Jaimie Karyn Rueter, Lee Alani Selvey, Sagar Raj Shakya, Marlon Carlos
  • Patent number: 10272095
    Abstract: The present invention relates to aryl analogs, pharmaceutical compositions containing them and their use as NRF2 regulators.
    Type: Grant
    Filed: June 15, 2016
    Date of Patent: April 30, 2019
    Assignees: GlaxoSmithKline Intellectual Propert Development Limited, Astex Therapeutics, Limited
    Inventors: Jeffrey K. Kerns, James Francis Callahan, Hongxing Yan, Thomas Daniel Heightman, Jeffrey Charles Boehm, Alison Jo-Anne Woolford
  • Patent number: 10183970
    Abstract: The present invention provides one or more compounds of formula (I) for conjugation to small molecules, polymers, peptides, proteins, antibodies, antibody fragments etc.
    Type: Grant
    Filed: January 28, 2015
    Date of Patent: January 22, 2019
    Assignee: Tube Pharmaceuticals GmbH
    Inventor: Wolfgang Richter
  • Patent number: 10173978
    Abstract: Small molecule carbazole compounds for use as androgen receptor inhibitors are provided herein. Also provided herein are methods for using the carbazole compounds in treating prostate cancer, including castration-resistant prostate cancer and enzalutamide-resistant prostate cancer. The methods include administering to a subject an effective amount of a compound or composition as described herein.
    Type: Grant
    Filed: August 2, 2016
    Date of Patent: January 8, 2019
    Assignee: Georgetown University
    Inventors: Milton L. Brown, Shujie Hou, Partha Banerjee, Karishma Amin
  • Patent number: 10111850
    Abstract: Pharmaceutical compositions comprising an ester anesthetic and a cholinesterase inhibitor have been found to exhibit surprising and beneficial results in achieving a long-acting nerve block for example when administered to an interfascial plane or a peri-neural location in a subject. Such pharmaceutical compositions may also contain an amide anesthetic. Pharmaceutical compositions and methods of using such compositions as described herein provide a surprising and unexpected duration of pain control and a reduced need for the use of narcotics.
    Type: Grant
    Filed: December 1, 2015
    Date of Patent: October 30, 2018
    Inventor: Samuel Wilson
  • Patent number: 10100331
    Abstract: The present invention relates to a composition for transfecting a cell with a genetic material comprising a first agent capable of directing the genetic material away from the acidic compartments in the cell and a second agent capable of stabilizing the microtubule or a network thereof. The invention also relates to the use of the composition in the manufacture of a medicament for treating a disease, a method for delivering a genetic material into a cell and a kit.
    Type: Grant
    Filed: October 29, 2013
    Date of Patent: October 16, 2018
    Assignee: Agency for Science, Technology and Research
    Inventors: Heng-Phon Too, Yoon Khei Ho, Lihan Zhou
  • Patent number: 10092510
    Abstract: The invention relates to a method of inducing emesis in animals, particularly companion animals such as dogs and cats, in situations where vomiting is desired. The method comprises administering an eye drop composition comprising a selective D2 family dopamine agonist as an active ingredient to the eye of the animal to induce emesis. The method and the composition are useful in situations involving ingestion of a potentially toxic substance or foreign body by the animal.
    Type: Grant
    Filed: September 29, 2014
    Date of Patent: October 9, 2018
    Assignee: ORION CORPORATION
    Inventors: Jouko Levijoki, Lasse Saloranta, Johanna Kokkonen
  • Patent number: 10045964
    Abstract: Polymorph forms of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide are disclosed as well as their methods of synthesis and pharmaceutical compositions.
    Type: Grant
    Filed: July 27, 2017
    Date of Patent: August 14, 2018
    Assignee: Siga Technologies Inc.
    Inventors: Shanthakumar R. Tyavanagimatt, Melialani A. C. L. S. Anderson, William C. Weimers, Dylan Nelson, Tove' C. Bolken, Dennis E. Hruby, Michael H. O'Neill, Gary Sweetapple, Kelley A. McCloughan
  • Patent number: 10005759
    Abstract: The subject matter herein is directed to carbazole-containing amide, carbamate, and urea derivatives and pharmaceutically acceptable salts or hydrates thereof of structural formula I wherein the variable R1, R2, R3, R4, R5, R6, R7, A, D, E, G, J, L, M, Q, a, and b are accordingly described. Also provided are pharmaceutical compositions containing the compounds of formula I to treat a Cry-mediated disease or disorder, such as diabetes, complications associated with diabetes, Cushing's syndrome, NASH, NAFLD, asthma, and COPD.
    Type: Grant
    Filed: April 6, 2015
    Date of Patent: June 26, 2018
    Assignee: Reset Therapeutics, Inc.
    Inventors: Ross Bersot, Paul Humphries
  • Patent number: 9994524
    Abstract: The T cells specific to human collagen type II, one of the possible autoantigens, have a crucial role in the development of rheumatoid arthritis in the context of HLA-DR4. The protein-protein interactions between the T cell receptor (TCR) and the type II collagen linked to the allele MHC of class II HLA-DR4 may thus represent the target for the development of new drugs against rheumatoid arthritis. Using computational virtual screening techniques, families of pharmacologically active molecules have been identified that interfere with the TCR/collagen II-MHCII interaction. The compounds identified here open up new possibilities in the treatment of rheumatoid arthritis.
    Type: Grant
    Filed: March 24, 2017
    Date of Patent: June 12, 2018
    Assignees: CONSIGLIO NAZIONALE DELLE RICERCHE, UNIVERSITÀ CATTOLICA DEL SACRO CUORE
    Inventors: Maria Cristina De Rosa, Francesco Ria, Bruno Giardina, Gianfranco Ferraccioli, Davide Pirolli, Chiara Nicolo′
  • Patent number: 9834563
    Abstract: The present invention relates to a compound represented by formula (I): and pharmaceutically acceptable salts thereof. The compounds of formula I are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
    Type: Grant
    Filed: December 17, 2014
    Date of Patent: December 5, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: William K. Hagmann, Bing Li, Jason W. Szewczyk, Bowei Wang, Dann Parker, Timothy Blizzard, Hubert Josien, Purakkattle Biju, Harry Chobanian, Candido Gude, Ravi P. Nargund, Barbara Pio, Qun Dang, Linus S. Lin, Bin Hu, Mingxiang Cui, Zhengxia Chen, Meibi Dai, Zaihong Zhang, Ying Lv, Lili Tian
  • Patent number: 9822060
    Abstract: A compound having a group represented by the formula (Ia): wherein R1 represents a C1 to C8 fluorinated alkyl group, R2 represents a group having an optionally substituted C5 to C18 alicyclic hydrocarbon group, and * represents a binding site.
    Type: Grant
    Filed: August 25, 2015
    Date of Patent: November 21, 2017
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Tatsuro Masuyama, Satoshi Yamamoto, Koji Ichikawa
  • Patent number: 9775845
    Abstract: The subject matter herein is directed to carbazole-containing sulfonamide derivatives and pharmaceutically acceptable salts or hydrates thereof of structural formula I wherein the variable R1, R2, R3, R4, R5, R6, R7, A, B, C?, D, E, F, G, H?, a, and b are accordingly described. Also provided are pharmaceutical compositions comprising the compounds of formula I to treat a Cry-mediated disease or disorder, such as diabetes, obesity, metabolic syndrome, Cushing's syndrome, and glaucoma.
    Type: Grant
    Filed: January 12, 2016
    Date of Patent: October 3, 2017
    Assignee: Reset Therapeutics, Inc.
    Inventors: Ross Bersot, Paul Humphries
  • Patent number: 9775830
    Abstract: Novel dihydropyrazole derivatives of formula (I) wherein L, R, R3, R4, R5, R6, R7, X1, X2, X3, X4, Y, m and n have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.
    Type: Grant
    Filed: November 3, 2016
    Date of Patent: October 3, 2017
    Assignee: Merck Patent GmbH
    Inventors: Henry Yu, Thomas E. Richardson, Robert James Foglesong, Lizbeth Celeste Deselm, Andreas Goutopoulos
  • Patent number: 9744154
    Abstract: Polymorph forms of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide are disclosed as well as their methods of synthesis and pharmaceutical compositions.
    Type: Grant
    Filed: December 4, 2015
    Date of Patent: August 29, 2017
    Assignee: SIGA TECHNOLOGIES, INC.
    Inventors: Shanthakumar R. Tyavanagimatt, Melialani A.C.L.S. Anderson, William C. Weimers, Dylan Nelson, Tove′ C. Bolken, Dennis E. Hruby, Michael H. O'Neill, Gary Sweetapple, Kelley A. McCloughan
  • Patent number: 9701676
    Abstract: 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: Grant
    Filed: August 23, 2013
    Date of Patent: July 11, 2017
    Assignee: Board of Regents of the University of Texas System
    Inventors: Steven L. McKnight, Andrew A. Pieper, Joseph M. Ready, Enrique Fernandez
  • Patent number: 9642841
    Abstract: The present invention features compositions and methods for treatment of snoring. We describe compositions comprising an antihistamine or a pharmaceutically acceptable salt thereof and one or more dietary supplements or pharmaceutically acceptable salts thereof. The compositions can be administered to a subject suffering from snoring.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: May 9, 2017
    Inventors: James M. Hand, Linda M. Hand
  • Patent number: 9629825
    Abstract: The invention relates to a pharmaceutical composition comprising a first pharmacologically active ingredient selected from (1r,4r)-6?-fluoro-N,N-dimethyl-4-phenyl-4?,9?-dihydro-3?H-spiro[cyclohexane-1,1?-pyrano[3,4,b]indol]-4-amine and the physiologically acceptable salts thereof, and a second pharmacologically active ingredient selected from gabapentinoids and the physiologically acceptable salts thereof.
    Type: Grant
    Filed: March 15, 2016
    Date of Patent: April 25, 2017
    Assignee: Gruenenthal GmbH
    Inventors: Stefanie Frosch, Klaus Linz, Thomas Christoph
  • Patent number: 9462455
    Abstract: Disclosed is a method, performed in a Body Area Network (BAN) enabled media experience device for enabling transmission of a media experience according to a stored, predefined user configuration associated with an identification data, userID, of a BAN enabled communication device, the method comprising: establishing a connection between the BAN enabled media experience device and the BAN enabled communication device by using BAN; retrieving the identification data, userID, of the BAN enabled communication device; retrieving the stored, predefined user configuration associated with the userID of the BAN enabled communication device; and initiating transmission of the media experience by the BAN enabled media experience device according to the stored, predefined user configuration.
    Type: Grant
    Filed: November 11, 2014
    Date of Patent: October 4, 2016
    Assignees: SONY CORPORATION, SONY MOBILE COMMUNICATIONS INC.
    Inventors: Aleksandar Rodzevski, Thomas Bolin, Henrik Bengtsson, Erik Bengtsson, Kristian Tärnhed, Malin Larsson, Ola Thörn
  • Patent number: 9447041
    Abstract: The present invention relates to processes and intermediates useful in the preparation of (R)-2-(7-(4-cyclopentyl-3-(trifluromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid of Formula (I) and salts thereof, an S1P1 receptor modulator that is useful in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development and atherosclerosis).
    Type: Grant
    Filed: September 30, 2015
    Date of Patent: September 20, 2016
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Antonio Garrido Montalban, Daniel J. Buzard, John A. DeMattei, Tawfik Gharbaoui, Stephen R. Johannsen, Ashwin M. Krishnan, Young Mi Kuhlman, You-An Ma, Michael John Martinelli, Suzanne Michiko Sato, Dipanjan Sengupta
  • Patent number: 9393232
    Abstract: Disclosed are substituted 5-(3,5-dimethylisoxazol-4-yl)indoline-2-one compounds, pharmaceutical compositions comprising at least one such 4 substituted 5-(3,5-dimethylisoxazol-4-yl)indoline-2-one compound processes for the preparation thereof, and the use thereof for inhibiting BET family of bromodomains and for treating disorders mediated thereby, such as certain cancers.
    Type: Grant
    Filed: April 14, 2014
    Date of Patent: July 19, 2016
    Assignee: BeiGene, Ltd.
    Inventors: Bo Ren, Changyou Zhou, Hexiang Wang
  • Patent number: 9365586
    Abstract: The present invention relates to a process for preparing dithiinetetracarboximides by reaction of succinic monoamides with thionyl chloride, with continuous performance of at least one of the process steps.
    Type: Grant
    Filed: March 18, 2013
    Date of Patent: June 14, 2016
    Assignees: Bayer Cropscience AG, Bayer Intellectual Property GmbH
    Inventors: Thomas Himmler, Thomas Geller, Lars Rodefeld, Mark James Ford, Guenter Hoemberger, Dieter Heinz
  • Patent number: 9364472
    Abstract: Amino, amido, and heterocyclic compounds are disclosed. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, diabetes complications, inflammation, and neurodegeneration, obesity, cancer, ischemia/reperfusion injury, cardiovascular disease and other diseases related to RAGE activity.
    Type: Grant
    Filed: August 6, 2015
    Date of Patent: June 14, 2016
    Assignees: New York University, The Research Foundation for The State University of New York
    Inventors: Ann Marie Schmidt, Ravichandran Ramasamy, Alexander Shekhtman, Vivek Rai, Michaele B. Manigrasso
  • Patent number: 9346818
    Abstract: Provided in the present invention are novel benzodioxole derivatives and preparation methods thereof. These compounds represented by formula (I) or pharmaceutically acceptable salts thereof have acetylcholinesterase inhibitory activity, so can be used in the treatment or prevention of Alzheimer's disease. The definitions of R1, R2 and A of formula (I) can be seen in the description.
    Type: Grant
    Filed: July 3, 2013
    Date of Patent: May 24, 2016
    Assignee: Zhejiang Hisun Pharmaceutical Co., Ltd.
    Inventors: Hua Bai, Xuyang Zhao, Jinqing Zhong, Yongxiang Gong, Qifeng Zhu, Xiaoyu Liu, Xiaohe Zheng, Lifei Liu
  • Patent number: 9345737
    Abstract: Topical compositions are provided useful for treating keratosis. The compositions comprise an extract of the plant Hamelia patens and are applied topically to skin having radiation dermatitis to relieve symptoms thereof.
    Type: Grant
    Filed: February 12, 2014
    Date of Patent: May 24, 2016
    Assignee: BERRY PHARMACEUTICALS, L.L.C.
    Inventor: Don Wayne Berry
  • Patent number: 9345736
    Abstract: Topical compositions are provided useful for treating radiation dermatitis. The compositions comprise an extract of the plant Hamelia patens and are applied topically to skin having radiation dermatitis to relieve symptoms thereof.
    Type: Grant
    Filed: March 16, 2013
    Date of Patent: May 24, 2016
    Assignee: BERRY PHARMACEUTICALS, L.L.C.
    Inventor: Don Wayne Berry
  • Patent number: 9339466
    Abstract: Polymorph forms of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide are disclosed as well as their methods of synthesis and pharmaceutical compositions.
    Type: Grant
    Filed: March 23, 2011
    Date of Patent: May 17, 2016
    Assignee: SIGA TECHNOLOGIES, INC.
    Inventors: Shanthakumar R. Tyavanagimatt, Melialani A. C. L. Stone, William C. Weimers, Dylan Nelson, Tove′ C. Bolken, Dennis E. Hruby, Michael H. O'Neill, Gary Sweetapple, Kelley A. McCloughan
  • Patent number: 9295665
    Abstract: There are provided inter alia methods and compounds useful for decreasing neovascularization (e.g., choroidal neovascularization) in a subject in need thereof.
    Type: Grant
    Filed: March 5, 2014
    Date of Patent: March 29, 2016
    Assignee: ALLERGAN, INC.
    Inventors: Jenny W. Wang, David F. Woodward
  • Patent number: 9253980
    Abstract: The present invention relates to the use of dithiine-tetracarboximide compounds of formula I as defined in the description, and the N-oxides, and salts thereof for combating harmful fungi and seed coated with at least one such compound. The invention also relates to novel dithiine-tetracarboximides, processes and intermediates for preparing these compounds and also to compositions comprising at least one such compound.
    Type: Grant
    Filed: April 10, 2012
    Date of Patent: February 9, 2016
    Assignee: BASF SE
    Inventors: Bernd Mueller, Nadege Boudet, Jochen Dietz, Wassilios Grammenos, Jan Klaas Lohmann, Richard Riggs, Ian Robert Craig, Jurith Montag, Egon Haden
  • Patent number: 9221837
    Abstract: The present invention relates to a new process for preparing dithiine-tetracarboximides.
    Type: Grant
    Filed: September 3, 2011
    Date of Patent: December 29, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Thomas Himmler, Frank Volz, Thomas Geller
  • Patent number: 9220672
    Abstract: The present invention relates to a peptide of the following formula (I) X1(X2)-X3-X4 or a salt or solvate thereof, wherein is an amino acid comprising two or more NH-functionalities, and X2, X3, and X4 are, independently from one another, an amino acid residue, and wherein the salt or solvate is preferably a physiologically acceptable salt or solvate.
    Type: Grant
    Filed: February 3, 2012
    Date of Patent: December 29, 2015
    Assignee: ORGANOBALANCE GMBH
    Inventor: Christine Lang
  • Patent number: 9210929
    Abstract: The present invention relates to novel strigolactam derivatives of formula (I), to processes and intermediates for preparing them, to plant growth regulator compositions comprising them and to methods of using them for controlling the growth of plants and/or promoting the germination of seeds.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: December 15, 2015
    Assignee: Syngenta Participations AG
    Inventors: Mathilde Denise Lachia, Alain De Mesmaeker, Emmanuelle Villedieu-Percheron, Hanno Christian Wolf, Pierre Joseph Marcel Jung, Franciscus Cornelis Lanfermeijer, Paul Willem Jan Van Den Wijngaard, Claudio Screpanti
  • Patent number: 9175320
    Abstract: The present invention relates to processes and intermediates useful in the preparation of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid of Formula (Ia) and salts thereof, an S1P1 receptor modulator that is useful in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development and atherosclerosis).
    Type: Grant
    Filed: August 20, 2014
    Date of Patent: November 3, 2015
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Antonio Garrido Montalban, Daniel J. Buzard, John A. DeMattei, Tawfik Gharbaoui, Stephen R. Johannsen, Ashwin M. Krishnan, Young Mi Kuhlman, You-An Ma, Michael John Martinelli, Suzanne Michiko Sato, Dipanjan Sengupta
  • Patent number: 9169207
    Abstract: The present invention relates to the treatment of breast cancer which is estrogen receptor positive (ER+) and/or human epidermal growth factor receptor 2 positive (HER2) and/or progesterone receptor positive (PR) and/or facilitates chromatin transcription positive (FACT+) with a curaxin, including curaxin 137. The present invention also pertains to a method of identifying a subject who has a breast cancer tumor and is likely to respond to treatment with a curaxin.
    Type: Grant
    Filed: March 27, 2013
    Date of Patent: October 27, 2015
    Assignee: Incuron, LLC
    Inventors: Andrei Gudkov, Katerina Gurova
  • Patent number: 9169220
    Abstract: The present invention relates to non-charged oxime compounds which are acetyl cholinesterase (AChE) reactivators of inhibited AChE and which protect against organophosphate poisoning both peripherally and in the central nervous system. Also disclosed are pharmaceutical compositions and methods for preparing the reactivator compounds and associated intermediates.
    Type: Grant
    Filed: July 2, 2014
    Date of Patent: October 27, 2015
    Assignee: SOUTHWEST RESEARCH INSTITUTE
    Inventors: Stanton F. McHardy, Richard M. Corbett, Donald M. Maxwell, Michael W. Tidwell, Bismarck Campos, Christopher J. Bemben
  • Patent number: 9102712
    Abstract: Novel peptide compounds and pharmaceutical compositions thereof are disclosed that have a formula represented by the following formula (I) wherein L1, L2, L3, Z, R1, R2, R4 and R5 are as described herein. The compounds demonstrate antimicrobial activity and may be prepared as pharmaceutical compositions and used for the prevention and treatment of a variety of conditions in mammals including humans where microbial invasion is involved. The present peptides are particularly valuable as their effect is rapid, broad in spectrum and mostly indifferent to resistance provided by standard antibiotics.
    Type: Grant
    Filed: August 26, 2011
    Date of Patent: August 11, 2015
    Assignee: New York University
    Inventors: Filbert Totsingan, Neville Robert Kallenbach
  • Patent number: 9095140
    Abstract: The present invention relates to the use of novel and of known dithiine-tetracarboximides for controlling phytopathogenic fungi, and to methods of controlling phytopathogenic fungi in plant protection, and to plant protection compositions comprising these dithiine-tetracarboximides.
    Type: Grant
    Filed: September 15, 2014
    Date of Patent: August 4, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Thomas Seitz, Ulrike Wachendorff-Neumann, Jürgen Benting, Peter Dahmen, Arnd Voerste, Ralf Dunkel, Stefan Hillebrand, Klaus-Günther Tietjen, Stephane Brunet
  • Patent number: 9044385
    Abstract: Methods for treating a vascular disease by delivering therapeutic compositions with enhanced endothelium targeting are disclosed.
    Type: Grant
    Filed: May 16, 2007
    Date of Patent: June 2, 2015
    Assignee: Abbott Cardiovascular Systems Inc.
    Inventors: Stephen Pacetti, Syed Faiyaz Ahmed Hossainy, Florian Niklas Ludwig
  • Publication number: 20150148359
    Abstract: Uses of a compound of any of Formulas I-VI as a cytotoxic inhibitor of undifferentiated cells are disclosed herein, as well as pharmaceutical compositions comprising a compound of any of Formulas I-VI, and methods for identifying a lead candidate for inhibiting undifferentiated cells. Further disclosed are uses of an SCD-1 inhibitor as a cytotoxic inhibitor of undifferentiated cells.
    Type: Application
    Filed: May 22, 2013
    Publication date: May 28, 2015
    Inventors: Uri Ben-David, Nissim Benvenisty, Payal Arora, Qing-Fen Gan, Ralph J. Garippa
  • Publication number: 20150141418
    Abstract: The present invention relates to methods, compounds, and compositions for inhibiting angiogenesis. More particularly, the present invention relates to methods, compounds, and compositions for inhibiting VEGF production.
    Type: Application
    Filed: January 26, 2015
    Publication date: May 21, 2015
    Applicant: PTC Therapeutics, Inc.
    Inventors: William Lennox, Hongyan Qi, Duck-Hyung Lee, Soongyu Choi, Young-Choon Moon
  • Publication number: 20150133527
    Abstract: Methods are provided herein for treating cardiac arrhythmias, such as for treating an arrhythmia syndrome, for example Brugada syndrome, in a subject. In some embodiments, the methods include selecting a subject with Brugada syndrome and administering to the subject an effective amount of an agent that increases the expression or activity of SIRT1 in the subject. In some embodiments, the agent increases Nav1.5 activation. In some embodiments, the agent increases the expression or activity of SRIT1 and increases Nav1.5 activation.
    Type: Application
    Filed: May 6, 2013
    Publication date: May 14, 2015
    Inventors: Barry London, Kaikobad J. Irani
  • Publication number: 20150126473
    Abstract: The present disclosure provides an isolated particle comprising very high density, ultra small, lipid depleted apo B containing particles, and may also contain cytokeratin 8. The isolated particle is useful in diagnostic assays, which are also provided.
    Type: Application
    Filed: June 14, 2012
    Publication date: May 7, 2015
    Applicant: Children's Hospital & Research Center at Oakland
    Inventors: Ronald M. Krauss, Mohmed Elfatih Ashmaig
  • Publication number: 20150126573
    Abstract: The present invention relates to methods and compositions for the prevention or treatment of chronic obstructive pulmonary disease.
    Type: Application
    Filed: May 7, 2013
    Publication date: May 7, 2015
    Inventors: Jorge Bernardo Boczkowski, Serge Adnot, Maylis Dagouassat, Jean-Marie Gagliolo
  • Patent number: 9023394
    Abstract: Controlled release formulations and methods for preparing controlled release formulations for delivery of active drug substances are described herein. The formulations described herein may be employed to produce pharmaceutical compositions, such as controlled release dosage forms, adjusted to a specific administration scheme.
    Type: Grant
    Filed: June 26, 2013
    Date of Patent: May 5, 2015
    Assignee: Egalet Ltd.
    Inventors: Christine Andersen, Karsten Lindhardt, Jan Martin Oevergaard, Louise Inoka Lyhne-Iversen, Martin Rex Olsen, Anne-Mette Haahr, Pernille Kristine Hoeyrup Hemmingsen
  • Patent number: 9023864
    Abstract: Compound of formula I are antagonists of the PGD2 receptor, CRTH2, and as such are useful in the treatment and/or prevention of CRTH2-mediated diseases such as asthma.
    Type: Grant
    Filed: February 7, 2013
    Date of Patent: May 5, 2015
    Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: Carl Berthelette, Michael Boyd, John Colucci, Karine Villeneuve, Joey L. Methot