Polycyclo Ring System Having A 1,2- Or 1,4-diazine As One Of The Cyclos Patents (Class 514/248)
  • Patent number: 11512089
    Abstract: The present invention discloses phthalazine isoxazole alkoxy derivatives, a preparation method thereof, a pharmaceutical composition, and a use thereof. The present invention provides a compound represented by Formula I, cis-trans isomers thereof, enantiomers thereof, diastereoisomers thereof, racemates thereof, solvates thereof, hydrates thereof, and pharmaceutically acceptable salts or prodrugs thereof. The compound has an excellent inverse agonist effect with respect to ?5-GABAA.
    Type: Grant
    Filed: March 12, 2019
    Date of Patent: November 29, 2022
    Assignees: SHANGHAI SIMR BIOTECHNOLOGY CO., LTD, SHANGHAI SIMRD BIOTECHNOLOGY CO., LTD
    Inventors: Fei Wang, Jinhua Wu, Yun Jin, Yong Sun, Shuai Li
  • Patent number: 11466008
    Abstract: Provided herein are co-crystal forms comprising 5-(2,6-dichlorophenyl)-2-(2,4-difluorophenylthio)-6H-pyrimido[1,6-b]pyridazin-6-one (VX-745): and compositions thereof, useful as inhibitors of one or more protein kinases and which exhibit desirable characteristics for the same.
    Type: Grant
    Filed: September 18, 2018
    Date of Patent: October 11, 2022
    Assignee: EIP Pharma, LLC
    Inventors: John Jahangir Alam, Jeffrey Douglas Wilson
  • Patent number: 11370769
    Abstract: Provided herein are TRPC5 inhibitors and methods of using the same, e.g., to protect podocytes and/or treat kidney disease.
    Type: Grant
    Filed: September 7, 2018
    Date of Patent: June 28, 2022
    Assignees: Board of Regents of the University of Nebraska, The Brigham and Women's Hospital, Inc.
    Inventors: Corey Hopkins, Anna Greka
  • Patent number: 11345710
    Abstract: Disclosed are imidazo[1,2-b]pyrimido[4,5-d]pyridazin-5(6H)-one compounds, specifically represented by the Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein A and R1-R5 are defined herein. Compounds having Formula I are Wee1 kinase inhibitors. Therefore, compounds of the disclosure may be used to treat diseases caused by abnormal Wee1 activity.
    Type: Grant
    Filed: July 10, 2018
    Date of Patent: May 31, 2022
    Assignee: IMPACT THERAPEUTICS (SHANGHAI), INC
    Inventors: Suixiong Cai, Ye Edward Tian, Zhiqiang Dong, Xiaozhu Wang
  • Patent number: 11319319
    Abstract: The present disclosure relates to inhibitors of NLRP3 useful in the treatment of diseases and disorders inhibited by said protein and having the Formula (I):
    Type: Grant
    Filed: November 17, 2021
    Date of Patent: May 3, 2022
    Assignee: Ventus Therapeutics U.S., Inc.
    Inventors: Stéphane Dorich, Amandine Chefson, Alexandre C{hacek over (o)}té
  • Patent number: 11311539
    Abstract: Disclosed are methods of alleviating or preventing one or more symptoms associated with fragile X syndrome in an individual in need thereof via administration of a therapeutically effective amount of a GABA(A) alpha 2 and/or 3 partial agonist. The one or more symptoms may include impaired functional communication, anxiety, inattention, hyperactivity, sensory reactivity, autonomic nervous system dysregulation, aberrant eye gaze, self-injury, aggression, seizures, EEG abnormalities, including but not limited to, abnormal spectral analysis, event related potentials which may include auditory and visual responses, abnormalities in cortical responses as evoked by transcranial magnetic stimulation including resting and active motor thresholds and abnormal responses in measures of cortical inhibition and excitation, aberrant impaired cognitive function, compromised daily living skills, or a combination thereof.
    Type: Grant
    Filed: December 5, 2019
    Date of Patent: April 26, 2022
    Assignee: Children's Hospital Medical Center
    Inventors: Craig Erickson, Tori Lynn Schaefer
  • Patent number: 11299494
    Abstract: Compounds of formula (I) or a stereoisomer or pharmaceutically-acceptable salt thereof, are useful in the modulation of IL-12, IL-23 and/or IFN?, by acting on Tyk-2 to cause signal transduction inhibition.
    Type: Grant
    Filed: November 16, 2017
    Date of Patent: April 12, 2022
    Assignee: Bristol-Myers Squibb Company
    Inventors: David S. Weinstein, John V. Duncia, Steven H. Spergel
  • Patent number: 11267819
    Abstract: This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.
    Type: Grant
    Filed: January 9, 2020
    Date of Patent: March 8, 2022
    Assignee: Celltaxsis, LLC
    Inventors: Damian O. Arnaiz, Greg Brown, Emmanuel Claret, Arwed Cleve, David Davey, William Guilford, Seock-Kyu Khim, Thomas Kirkland, Monica J. Kochanny, Amy Liang, David Light, John Parkinson, Guo Ping Wei, Bin Ye
  • Patent number: 11203575
    Abstract: A new method for producing a crystalline form of 5-amino-2,3-dihydro-1,4-phthalazinedione (luminol) is provided. Advantageous uses for this crystalline form as a detecting agent or as an agent for forensic purposes are disclosed, as well a pharmaceutical composition containing said crystalline form.
    Type: Grant
    Filed: February 15, 2017
    Date of Patent: December 21, 2021
    Assignee: MetrioPharm AG
    Inventors: Thomas Martin, Josef Breu, Juliane Fleissner, Wolfgang Brysch, Jörg Von Wegerer
  • Patent number: 11180493
    Abstract: The present disclosure relates to stimulators of soluble guanylate cyclase (sGC), pharmaceutical formulations comprising them and their uses thereof, alone or in combination with one or more additional agents, for treating various diseases, wherein an increase in the concentration of nitric oxide (NO) and/or an increase in the concentration of cyclic Guanosine Monophosphate (cGMP) might be desirable. Various compounds are disclosed, including those of Formula (I).
    Type: Grant
    Filed: November 7, 2017
    Date of Patent: November 23, 2021
    Assignee: Cyclerion Therapeutics, Inc.
    Inventors: Glen Robert Rennie, Timothy Claude Barden, Thomas Wai-Ho Lee, Rajesh R. Iyengar, Takashi Nakai, Ara Mermerian, Lei Jia, Karthik Iyer, G-Yoon Jamie Im, Paul Allan Renhowe, Joon Jung, Peter Germano, Kim Tang
  • Patent number: 11135227
    Abstract: The present invention relates to pyrimidine compounds that are useful as anti-proliferative agents. More particularly, the present invention relates to oxygen linked and substituted pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative disorders including tumours and cancers as well as other disorders or conditions related to or associated with kinases.
    Type: Grant
    Filed: November 7, 2019
    Date of Patent: October 5, 2021
    Assignee: CTI BIOPHARMA CORP.
    Inventors: Stephanie Blanchard, Cheng Hsia Angelina Lee, Harish Kumar Mysore Nagaraj, Anders Poulsen, Eric T. Sun, Yee Ling Evelyn Tan, Anthony Deodaunia William
  • Patent number: 11129827
    Abstract: Provided herein are compounds and pharmaceutical compositions comprising said compounds useful as modulators of MAGL and/or FAAH. The subject compounds and compositions are useful for the treatment of pain and neurological disorders.
    Type: Grant
    Filed: June 4, 2019
    Date of Patent: September 28, 2021
    Assignee: Abide Therapeutics, Inc.
    Inventors: Cheryl A. Grice, Justin S. Cisar, Katharine K. Duncan, Yu Feng, John J. M. Wiener, Olivia D. Weber
  • Patent number: 11111218
    Abstract: A new crystalline form of 5-amino-2,3-dihydro-1,4-phthalazinedione (luminol) is provided. Advantageous uses for this crystalline form as a detecting agent or as an agent for forensic purposes are disclosed, as well a pharmaceutical composition containing said crystalline form.
    Type: Grant
    Filed: February 15, 2017
    Date of Patent: September 7, 2021
    Assignee: METRIOPHARM AG
    Inventors: Thomas Martin, Josef Breu, Juliane Fleissner, Wolfgang Brysch, Jörg Von Wegerer
  • Patent number: 11089783
    Abstract: The invention relates to novel compounds of the formula (I) in which R1, R2, R3, R4, A1, A2 and n have the definitions given above, to agrochemical formulations comprising the compounds of formula (I) and to their use as acaricides and/or insecticides for controlling animal pests, particularly arthropods and especially insects and arachnids.
    Type: Grant
    Filed: April 25, 2018
    Date of Patent: August 17, 2021
    Assignee: Bayer Aktiengesellschaft
    Inventors: Marc Mosrin, Ruediger Fischer, Dominik Hager, Laura Hoffmeister, Nina Kausch-Busies, David Wilcke, Matthieu Willot, Kerstin Ilg, Ulrich Goergens, Daniela Portz, Sascha Eilmus, Andreas Turberg
  • Patent number: 11040979
    Abstract: Compounds and compositions useful for treating disorders related to KIT and PDGFR are described herein.
    Type: Grant
    Filed: March 29, 2018
    Date of Patent: June 22, 2021
    Assignee: Blueprint Medicines Corporation
    Inventors: Brian L. Hodous, Joseph L. Kim, Kevin J. Wilson
  • Patent number: 11040952
    Abstract: Provided are a phthalazinone compound, method for preparation thereof, pharmaceutical composition thereof, and a use thereof; the structure of said phthalazinone compound is as represented by formula I; the compound of said formula I is targeted to a viral nucleocapsid; it can inhibit the replication of a virus by means of interference of the viral nucleocapsid, has a potent activity for inhibiting HBV DNA replication and a good liver targeting, can stably exist and enrich in the liver, and is a new and effective anti-HBV inhibitor.
    Type: Grant
    Filed: February 10, 2020
    Date of Patent: June 22, 2021
    Assignee: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Youhong Hu, Jianping Zuo, Dong Lu, Li Yang, Limin Zeng, Feifei Liu, Yunzhe Zhang, Wuhong Chen, Xiankun Tong
  • Patent number: 11007192
    Abstract: The invention relates to 5-amino-2,3-dihydro-1,4-phthalazinedione or related compounds, compositions or combinations thereof, for use in the treatment of chronic progressive multiple sclerosis, in particular primary and secondary progressive multiple sclerosis. The invention in particular relates to the use of 5-amino-2,3-dihydro-1,4-phthalazinedione sodium salt for said purposes.
    Type: Grant
    Filed: November 6, 2017
    Date of Patent: May 18, 2021
    Assignee: Metriopharm AG
    Inventors: Wolfgang Brysch, Astrid Kaiser, Claudia Van Laak, Beate Ludescher, Maliha Shah, Jörg Von Wegerer
  • Patent number: 10981907
    Abstract: Polycyclic derivatives of formula I wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.
    Type: Grant
    Filed: November 27, 2018
    Date of Patent: April 20, 2021
    Assignee: Syngenta Participations AG
    Inventors: Andrew Edmunds, Michel Muehlebach, Pierre Marcel Jung, Andre Jeanguenat
  • Patent number: 10927125
    Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, tautomer, prodrug or stereoisomer thereof, wherein R1, R2a, R3a, R3b, R4a, R4b, G1, G2, L1, L2, m1, m2, A, B, W, X, Y, Z and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
    Type: Grant
    Filed: June 24, 2019
    Date of Patent: February 23, 2021
    Assignee: ARAXES PHARMA LLC
    Inventors: Liansheng Li, Jun Feng, Tao Wu, Pingda Ren, Yi Liu, Yuan Liu, Yun Oliver Long
  • Patent number: 10927117
    Abstract: The present invention relates to a crystalline form of (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide for inhibiting Btk, methods of preparation thereof and pharmaceutical compositions, and use of the crystalline form above in the treatment of a disease, or in the manufacturing of a medicament for the treatment of a disease.
    Type: Grant
    Filed: August 15, 2017
    Date of Patent: February 23, 2021
    Assignee: BEIGENE SWITZERLAND GMBH
    Inventors: Zhiwei Wang, Yunhang Guo, Gongyin Shi
  • Patent number: 10898471
    Abstract: The present invention is directed to methods of inhibiting LTA4-h in a human patient and method of treating a condition ameliorated by the inhibition of leukotriene A4 hydrolase activity in a human patient comprising administering to said human patient the compound, 4-{5-[4-(4-Oxazol-2-yl-phenoxy)-benzyl]-2,5-diaza-bicyclo[2.2.1]hept-2-ylmethyl}-benzoic acid.
    Type: Grant
    Filed: June 17, 2019
    Date of Patent: January 26, 2021
    Assignee: CELLTAXIS, LLC
    Inventors: Eric B. Springman, Margaret McCrann Pugh, Lopa Bhatt, Ralph Grosswald
  • Patent number: 10875866
    Abstract: A compound of Formula (I): pharmaceutically acceptable salts thereof, deuterated analogs thereof, compositions thereof, and methods of treating disease using a compound thereof, wherein the variable substituents are disclosed herein.
    Type: Grant
    Filed: July 11, 2019
    Date of Patent: December 29, 2020
    Assignee: Gilead Sciences, Inc.
    Inventors: Stephen Ammann, Elizabeth M. Bacon, Gediminas Brizgys, Elbert Chin, Chienhung Chou, Jeromy J. Cottell, Marilyn Ndukwe, James G. Taylor, Nathan E. Wright, Zheng-Yu Yang, Sheila M. Zipfel
  • Patent number: 10875858
    Abstract: The present invention relates to a process for preparing halogenated pyridine derivatives of the formula (II) proceeding from compounds of the structure Q-H via intermediates of the formula (IIIa) or (IIIb) in which Q is a structural element where the symbol # indicates the bond to the rest of the molecule and A, Q1, Q2, Q3, Q4, Q5 and Q6 have the definitions given in the description, W is halogen, Y is halogen, CO2R1 or NO2, where R1 is (C1-C6)-alkyl or (C1-C6)-haloalkyl, and R2 is halogen or —O-pivaloyl.
    Type: Grant
    Filed: August 9, 2017
    Date of Patent: December 29, 2020
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Marc Mosrin, Ruediger Fischer, Dominik Hager, Laura Hoffmeister, Nina Kausch-Busies, David Wilcke, Matthieu Willot
  • Patent number: 10875864
    Abstract: The present invention provides a compound having the following structure: Compositions and methods for using the same in the treatment of skin disorders and other Pim kinase-associated conditions are also disclosed.
    Type: Grant
    Filed: July 2, 2019
    Date of Patent: December 29, 2020
    Assignee: SUMITOMO DAINIPPON PHARMA ONCOLOGY, INC.
    Inventors: Yong Xu, Benjamin Gary Brenning, Steven G. Kultgen, Xiaohui Liu, Michael David Saunders, Koc-Kan Ho
  • Patent number: 10874667
    Abstract: The present invention relates to the field of pharmaceutical synthesis, and in particular to an antitumor heterocyclic imidazole compound (I), namely: a pharmaceutical salt of 4-(3-(4-(1H-imidazo[4,5-b]pyridine-5-yl)piperazine-1-carbonyl)-4-fluorobenzyl)phthalazine-1(dihydro)-ketone, a preparation method therefor, a pharmaceutical composition thereof and a use thereof in the preparation of antitumor drugs. The pharmaceutical salt of the compound (I) in the present invention may be used in the preparation of a medicament for the treatment or prevention of conditions which can be improved by inhibiting PARP activity.
    Type: Grant
    Filed: October 11, 2017
    Date of Patent: December 29, 2020
    Assignee: Shanghai Huilin Life Scinece & Technology Co., Ltd.
    Inventors: Xing Fan, Wenhua Li, Jihong Qin
  • Patent number: 10869864
    Abstract: Described herein are combinations comprising a therapeutically effective amount of a first agent and a therapeutically effective amount of a second agent, wherein the first agent is an inhibitor of ALK, ROS1, TrkA, TrkB, or TrkC activity, or a combination thereof, and methods of using such combinations in the treatment of patients having cancer.
    Type: Grant
    Filed: December 15, 2016
    Date of Patent: December 22, 2020
    Assignee: IGNYTA, INC.
    Inventors: Gang Li, Ge Wei, Zachary D. Hornby, Jonathan Ee-ren Lim
  • Patent number: 10813909
    Abstract: A combination of three well-known and FDA approved compounds has been discovered to significantly suppress the proliferation of pancreatic cancer cells in clinically relevant models of pancreatic cancer. Embodiments of the invention include compositions of matter comprising a combination of agents such as metformin, simvastatin, and digoxin as well as methods of treating cancers using such agents. Illustrative methods include combining a population of pancreatic cancer cells with amounts of metformin, simvastatin, and digoxin sufficient to inhibit expression of BIRC5 protein in the population of pancreatic cancer cells, thereby inhibiting the growth of the population of pancreatic cancer cells.
    Type: Grant
    Filed: May 19, 2017
    Date of Patent: October 27, 2020
    Assignee: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Francis C. Brunicardi, Robbi L. Sanchez
  • Patent number: 10774086
    Abstract: The disclosure generally relates to compounds of formula (I), including their salts, as well as compositions and methods of using the compounds to treat disorders associated with GSK-3.
    Type: Grant
    Filed: November 27, 2017
    Date of Patent: September 15, 2020
    Assignee: Bristol-Myers Squibb Company
    Inventors: Richard A. Hartz, Vijay T. Ahuja, Prasanna Sivaprakasam, Gene M. Dubowchik, John E. Macor
  • Patent number: 10745381
    Abstract: The present invention relates to indoline-based compounds that inhibit Rho-associated protein kinase (ROCK) activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of inhibiting ROCK activity and methods for treating, for example cerebral cavernous malformation syndrome (CCM) and cardiovascular diseases using the compounds and pharmaceutical compositions of the present invention.
    Type: Grant
    Filed: November 6, 2019
    Date of Patent: August 18, 2020
    Assignee: Cervello Therapeutics, LLC.
    Inventors: Matthew Randolph Lee, Anthony Joseph Varano, Jr.
  • Patent number: 10668074
    Abstract: The specification describes the use of selected DPP IV inhibitors for the treatment of physiological functional disorders and for reducing the risk of the occurrence of such functional disorders in at-risk patient groups. In addition, the use of the above-mentioned DPP IV inhibitors in conjunction with other active substances is described, by means of which improved treatment outcomes can be achieved. These applications may be used to prepare corresponding medicaments.
    Type: Grant
    Filed: August 14, 2018
    Date of Patent: June 2, 2020
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Klaus Dugi, Frank Himmelsbach, Michael Mark
  • Patent number: 10653805
    Abstract: This document relates to compounds useful for targeting PARP1. Also provided herein are methods for using such compounds to detect and image cancer cells.
    Type: Grant
    Filed: September 28, 2018
    Date of Patent: May 19, 2020
    Assignee: The General Hospital Corporation
    Inventors: Thomas Reiner, Edmund J. Keliher, Ralph Weissleder
  • Patent number: 10647720
    Abstract: The present application provides novel pyrimido-pyridazinone compounds and methods for preparing and using these compounds. These compounds are useful in treating inflammation in patients by administering one or more of the compounds to a patient. In one embodiment, the novel pyrimido-pyridazinone compound is of Formula (I) and R1 and R2 are defined herein.
    Type: Grant
    Filed: November 30, 2018
    Date of Patent: May 12, 2020
    Assignee: Asan BioSciences, LLC
    Inventors: Aranapakam Venkatesan, Roger Smith, Subramanya Hosahalli, Vijay Potluri, Sunil Kumar Panigrahi, Vishnu Basetti, Karunasree Kunta
  • Patent number: 10538523
    Abstract: The present invention relates to pyrazolopyridazine derivatives. More particularly, it relates to 4-(biphenyl-3-yl)-1H-pyrazolo[3,4-c]pyridazine derivatives of formula (I), and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4 and R5 are as defined in the description. The pyrazolopyridazine derivatives of the present invention modulate the activity of the GABAA receptor. They may useful in the treatment of a number of conditions, including pain and epilepsy.
    Type: Grant
    Filed: November 22, 2016
    Date of Patent: January 21, 2020
    Assignee: PFIZER LIMITED
    Inventors: Kevin Neil Dack, Robert McKenzie Owen, David Cameron Pryde
  • Patent number: 10525047
    Abstract: The present invention provides for a method of treating cancer and/or reducing proliferation of cancer cells, the method comprising administering to a subject in need of such treatment a composition comprising a PIM kinase inhibitor that exhibits changes of mRNA splicing in combination with a compound that modulates/inhibits activity of an RNA splicing factor protein. Further, changes in splicing of mRNAs and phosphorylation of RNA splicing factors can be used as biomarkers for patient responsiveness to anti-PIM treatment and also suggest effective combinatorial therapies, including synergistic combination.
    Type: Grant
    Filed: March 22, 2017
    Date of Patent: January 7, 2020
    Assignee: UNIVERSITY OF MARYLAND, BALTIMORE COUNTY
    Inventors: Charles J. Bieberich, Xiang Li, Tejashree Joglekar
  • Patent number: 10434132
    Abstract: The present invention is related to a galactolipids-enriched plant extract, prepared by extracting a plant sample selected from a group consisting of: Gynura divaricata subsp. formosana (Asteraceae) (GD), Murdannia bracteata (C. B. Clarke) J. K. Morton ex D. Y. Hong (Commelinaceae) (MB), and Crassocephalum rabens S. Moore (Asteraceae) (CR) with a series of solvents. A pharmaceutical, nutritional, or healthcare composition for protecting or treating acute fulminant hepatitis, for protecting or treating sepsis or related indication thereof, and a composition for skin whitening are also provided herein. These compositions all comprise effective amounts of the galactolipids-enriched plant extracts or purified compounds thereof as bioactive ingredients.
    Type: Grant
    Filed: October 26, 2018
    Date of Patent: October 8, 2019
    Assignee: Academia Sinica
    Inventors: Lie-Fen Shyur, Jia-Hua Feng, Maria Karmella Apaya
  • Patent number: 10428076
    Abstract: The invention provides compounds of the Formula (I) or a pharmaceutically acceptable salts thereof, wherein X, Y, Z, R1, R2, R4, Ra, and the subscripts m, p, and q are as described herein. The compounds or their pharmaceutically acceptable salts can modulate the body's production of cyclic guanosine monophosphate (“cGMP”), and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The invention also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose.
    Type: Grant
    Filed: June 27, 2018
    Date of Patent: October 1, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Raphaelle Berger, Yi-Heng Chen, Guoqing Li, Joie Garfunkle, Hong-Dong Li, Shouwu Miao, Subharekha Raghavan, Cameron J. Smith, John Stelmach, Alan Whitehead, Rui Zhang, Yong Zhang, Jianmin Fu, Gang Ji, Falong Jiang
  • Patent number: 10350197
    Abstract: The present invention is directed to methods of inhibiting LTA4-h in a human patient and method of treating a condition ameliorated by the inhibition of leukotriene A4 hydrolase activity in a human patient comprising administering to said human patient the compound, 4-{5-[4-(4-Oxazol-2-yl-phenoxy)-benzyl]-2,5-diaza-bicyclo[2.2.1]hept-2-ylmethyl}-benzoic acid.
    Type: Grant
    Filed: November 2, 2017
    Date of Patent: July 16, 2019
    Assignee: Celtaxsys, Inc.
    Inventors: Eric B. Springman, Margaret McCrann Pugh, Lopa Bhatt, Ralph Grosswald
  • Patent number: 10351561
    Abstract: The present invention provides compounds of formula (I) that are PDE1 enzyme inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders. The present invention also provides pharmaceutical compositions comprising compounds of the invention and methods of treating disorders using the compounds of the invention.
    Type: Grant
    Filed: December 21, 2017
    Date of Patent: July 16, 2019
    Assignee: H. Lundbeck A/S
    Inventors: Jan Kehler, Lars Kyhn Rasmussen, Morten Langgard, Mikkel Jessing, Paulo Jorge Vieira Vital, Karsten Juhl, Mauro Marigo
  • Patent number: 10329307
    Abstract: The present invention provides compounds of Formula I: wherein Y, AA, W, R3? R2, R4, R5, R6, R7, X1, X2, X3, X4 and X5 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug or esters or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders.
    Type: Grant
    Filed: September 19, 2016
    Date of Patent: June 25, 2019
    Assignee: Universite de Montreal
    Inventors: Alain Martel, Francois Tremblay
  • Patent number: 10258620
    Abstract: The invention relates to the provision of a new crystalline form for 5-amino-2,3-dihydrophthalazine-1,4-dione sodium, the use of this form for medical purposes, methods for producing the crystalline form according to the invention, as well as pharmaceutical preparations comprising said form.
    Type: Grant
    Filed: December 18, 2015
    Date of Patent: April 16, 2019
    Assignee: Metriopharm AG
    Inventors: Thomas Martin, Josef Breu, Wolfgang Brysch, David Kosel, Beate Ludescher, Michael Niedermaier, Jörg Von Wegerer
  • Patent number: 10251885
    Abstract: The present invention relates generally to antifugal compositions. In an embodiment, the antifungal compositions are effective for application to nails and surrounding skin, and comprise at least one volatile solvent, at least one film forming substance, and at least one pyrimidone derivative of formula I, such as albaconazole. These compositions are capable of treating an infection caused by fungi, such as onychomychosis.
    Type: Grant
    Filed: May 27, 2010
    Date of Patent: April 9, 2019
    Assignee: ALLERGAN PHARMACEUTICALS INTERNATIONAL LIMITED
    Inventors: Jon Lenn, Hans Hofland, Edward Hsia
  • Patent number: 10253047
    Abstract: Trisubstituted bicyclic heterocyclic compounds (e.g., chromenones and quinolines) and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
    Type: Grant
    Filed: June 13, 2017
    Date of Patent: April 9, 2019
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Alfredo C. Castro, Catherine A. Evans, Martin R. Tremblay
  • Patent number: 10238630
    Abstract: The invention features methods for treating cancer in a patient in need thereof by administering eribulin, in combination with one or more PARP inhibitors, and, optionally, a platinum-based antineoplastic drug, and kits therefor. The invention is based in part on the observation that combinations of eribulin mesylate, a PARP inhibitor (e.g., E7449), and, optionally, a platinum-based antineo-plastic drug (e.g., carboplatin), show improved (e.g., synergistic) antitumor effects. Therefore, the present invention features methods of preventing and treating cancer (e.g., homologous recombination (HR)-deficient cancer by the use of combinations of eribulin (e.g., eribulin mesylate) and one or more PARP inhibitors (e.g., E7449 or a pharmaceutically acceptable salt thereof (e.g., the tartrate salt), optionally in combination with a platinum-based antineoplastic drug (e.g., carboplatin).
    Type: Grant
    Filed: May 28, 2015
    Date of Patent: March 26, 2019
    Assignee: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: David Cox, Alton Kremer, Sharon McGonigle, Jiayi Wu
  • Patent number: 10226293
    Abstract: The present invention provides a drug eluting surgical screw and a method for manufacturing a drug eluting surgical screw. The drug eluting surgical screw may include a shaft having a threaded portion, a head having a drive recess disposed at a proximal end of the shaft, the drive recess having a reservoir region and a driver engagement region, and at least one or more drug eluting components disposed within the reservoir region of the drive recess in a manner that does not substantially impair a connection between a driver and the surgical screw when the driver is operably disposed within the driver engagement region, each of the at least one or more drug eluting components including a carrier matrix and a therapeutic agent, the therapeutic agent being at least 20 wt % of the drug eluting component prior to any implantation of the drug eluting surgical screw.
    Type: Grant
    Filed: November 10, 2017
    Date of Patent: March 12, 2019
    Assignee: DePuy Synthes Products, Inc.
    Inventors: David A. Armbruster, Anurag Pandey
  • Patent number: 10214512
    Abstract: The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma Kallikrein.
    Type: Grant
    Filed: October 24, 2016
    Date of Patent: February 26, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jiayi Xu, Amjad Ali, Wei Zhou, Ying-Duo Gao, Scott D. Edmondson, Eric Mertz, Santhosh F. Neelamkavil, Weiguo Liu, Wanying Sun, Dong-Ming Shen, Bart Harper, Cheng Zhu, Thomas Bara, Yeon-Hee Lim, Meng Yang
  • Patent number: 10207002
    Abstract: Disclosed are formulations and tablets made therefrom comprising the compound of Formula IA or Formula IB which have sustained-release properties, and the dispersion containing the compounds of Formula IA or IB which facilitates such sustained release: Formula IA, Formula IB.
    Type: Grant
    Filed: June 21, 2016
    Date of Patent: February 19, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Pranav Gupta, David Monteith
  • Patent number: 10183944
    Abstract: The present application provides novel pyrimido-pyridazinone compounds and methods for preparing and using these compounds. These compounds are useful in treating inflammation in patients by administering one or more of the compounds to a patient. In one embodiment, the novel pyrimido-pyridazinone compound is of Formula (I) and R1 and R2 are defined herein.
    Type: Grant
    Filed: April 25, 2016
    Date of Patent: January 22, 2019
    Assignee: Asana BioSciences, LLC
    Inventors: Aranapakam Venkatesan, Roger Astbury Smith, Hosahalli Subramanya, Vijay Potluri, Sunil Kumar Panigrahi, Vishnu Basetti, Karunasree Kunta
  • Patent number: 10167259
    Abstract: The present invention relates generally to novel allosteric regulators of proteasome activity, methods for preparation and use, and pharmaceutical compositions thereof. Specifically piperidine-2-carboxylic acid derivatives containing 1-oxo-aroyl group and a lipophilic ester side chain are disclosed as allosteric inhibitors of proteasome 2S activity, and as therapeutic agents for the treatment of proteasome-associated disorders in a subject.
    Type: Grant
    Filed: June 13, 2014
    Date of Patent: January 1, 2019
    Assignee: The Board of Regents of the University of Texas System
    Inventors: Pawel A. Osmulski, Maria E. Gaczynska
  • Patent number: 10159673
    Abstract: Disclosed are methods of alleviating or preventing one or more symptoms associated with fragile X syndrome in an individual in need thereof via administration of a therapeutically effective amount of a GABA(A) alpha 2 and/or 3 partial agonist. The one or more symptoms may include impaired functional communication, anxiety, inattention, hyperactivity, sensory reactivity, autonomic nervous system dysregulation, aberrant eye gaze, self-injury, aggression, seizures, EEG abnormalities, including but not limited to, abnormal spectral analysis, event related potentials which may include auditory and visual responses, abnormalities in cortical responses as evoked by transcranial magnetic stimulation including resting and active motor thresholds and abnormal responses in measures of cortical inhibition and excitation, aberrant impaired cognitive function, compromised daily living skills, or a combination thereof.
    Type: Grant
    Filed: November 21, 2017
    Date of Patent: December 25, 2018
    Assignee: Children's Hospital Medical Center
    Inventors: Craig Erickson, Tori Lynn Schaefer
  • Patent number: 10155726
    Abstract: Substituted pyridines that modulate HIF-2a activity, pharmaceutical compositions containing the substituted pyridines, and methods of using these chemical entities for treating proliferative diseases and conditions associated with HIF-2a activity are described herein.
    Type: Grant
    Filed: March 4, 2016
    Date of Patent: December 18, 2018
    Assignee: PELOTON THERAPEUTICS, INC.
    Inventors: Paul Wehn, Rui Xu, Hanbiao Yang