Polycyclo Ring System Having A 1,2- Or 1,4-diazine As One Of The Cyclos Patents (Class 514/248)
  • Patent number: 12168657
    Abstract: The present disclosure relates to inhibitors of NLRP3 useful in the treatment of diseases and disorders inhibited by said protein.
    Type: Grant
    Filed: November 9, 2022
    Date of Patent: December 17, 2024
    Assignee: Ventus Therapeutics U.S., Inc.
    Inventors: Stéphane Dorich, Amandine Chefson
  • Patent number: 12109211
    Abstract: A sterile, ready-to-use pharmaceutical composition having hydralazine and/or a salt thereof at a concentration of less than about 20 mg/mL and a solvent comprising an organic co-solvent, wherein the hydralazine and/or salt thereof and the organic co-solvent are provided at a first weight ratio sufficient for the hydralazine and/or salt thereof to have a change in concentration of no more than about 10% after 2 months of storage at 60° C. Also described are methods of making and using the composition.
    Type: Grant
    Filed: December 27, 2022
    Date of Patent: October 8, 2024
    Assignee: ENDO OPERATIONS LIMITED
    Inventors: Kumaresh Soppimath, Tushar Hingorani, Hari A. Attluri, Harshil H. Jain
  • Patent number: 12049452
    Abstract: The invention relates to new 1:1 olaparib:hydroxybenzoic acid cocrystals. The invention also relates to new 2:1 olaparib:hydroxybenzoic acid cocrystals which may contain no water (anhydrous) or may optionally be hydrated. The invention also relates to pharmaceutical compositions containing an olaparib hydroxybenzoic acid cocrystal of the invention and a pharmaceutically acceptable carrier. The olaparib hydroxybenzoic acid cocrystals of the invention may be useful for the treatment of diseases that benefit from inhibition of poly (ADP-ribose) polymerase (PARP).
    Type: Grant
    Filed: November 10, 2022
    Date of Patent: July 30, 2024
    Assignee: NUFORMIX TECHNOLOGIES LIMITED
    Inventors: Joanne Holland, Alex Eberlin
  • Patent number: 12024524
    Abstract: The present application discloses compounds having the following formula: or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined in the specification, as well as methods of making and using the compounds disclosed herein for treating or ameliorating an IL-17 mediated syndrome, disorder and/or disease.
    Type: Grant
    Filed: April 7, 2023
    Date of Patent: July 2, 2024
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Steven Goldberg, David Kummer, John Keith, Craig Woods, Timothy Rhorer, Virginia M. Tanis, Connor Martin, Steven Meduna, Stefan McCarver, Alexander Valdes, Steven Loskot, Douglas Behenna, Alexander Rovira, Charlotte Deckhut, Xiaohua Xue
  • Patent number: 12016859
    Abstract: The present disclosure provides for methods of treating a patient with a CYP3A4 substrate drug, wherein the patient is treated with posaconazole. In some embodiments, the patient stops posaconazole treatment, waits for at least 3 days, and then is treated with the CYP3A4 substrate drug as soon as it is safe to do so. In some embodiments, treatment with the CYP3A4 substrate drug is delayed for about 3-42 days after stopping posaconazole. In some embodiments, the patient is treated with a reduced dose of the CYP3A4 substrate drug for about 3-42 days.
    Type: Grant
    Filed: March 31, 2023
    Date of Patent: June 25, 2024
    Assignee: BOW RIVER LLC
    Inventors: Sundar Srinivasan, Christina Chow Wallen
  • Patent number: 11999742
    Abstract: This invention provides for compounds of the formula: wherein the variables are defined herein, or salt thereof, compositions comprising these compounds, and methods for the treatment, control and/or prevention of a parasitic infestation and/or infection in an animal in need thereof by administering an effective amount of these compounds to said animal.
    Type: Grant
    Filed: October 28, 2022
    Date of Patent: June 4, 2024
    Inventors: Hannes Fiepko Koolman, Bart Herlé
  • Patent number: 11976071
    Abstract: The present disclosure provides bifunctional compounds of Formula (I), and pharmaceutically acceptable salts, isotopic forms, isolated stereoisomers, or mixtures of stereoisomers thereof, as IRAK4 degraders via ubiquitin proteasome pathway, and method for treating diseases modulated by IRAK4.
    Type: Grant
    Filed: August 18, 2022
    Date of Patent: May 7, 2024
    Assignee: Gilead Sciences, Inc.
    Inventors: Wylie Palmer, Jeffrey Wu, John Lee, Kerem Ozboya, Tim Kane
  • Patent number: 11883381
    Abstract: Provided herein are small molecule inhibitors of ASH1L activity and small molecules that facilitate ASH1L degradation and methods of use thereof for the treatment of disease, including acute leukemia, solid cancers and other diseases dependent on activity of ASH1L.
    Type: Grant
    Filed: May 12, 2017
    Date of Patent: January 30, 2024
    Assignee: The Regents of the University of Michigan
    Inventors: Jolanta Grembecka, Tomasz Cierpicki, David Rogawski, Dmitry Borkin, Szymon Klossowski, Zhuang Jin, Deanna Montgomery, Jing Deng, Marta Krotoska, Hao Li
  • Patent number: 11801245
    Abstract: The present disclosure provides for methods of treating a patient with a CYP3A4 substrate drug, wherein the patient is treated with posaconazole. In some embodiments, the patient stops posaconazole treatment, waits for at least 2 days, and then is treated with the CYP3A4 substrate drug as soon as it is safe to do so. In some embodiments, treatment with the CYP3A4 substrate drug is delayed for about 2-42 days after stopping posaconazole. In some embodiments, the patient is treated with a reduced dose of the CYP3A4 substrate drug for about 2-42 days.
    Type: Grant
    Filed: September 21, 2022
    Date of Patent: October 31, 2023
    Assignee: BOW RIVER LLC
    Inventors: Sundar Srinivasan, Christina Chow Wallen
  • Patent number: 11795172
    Abstract: The present invention provides a fused heteroaryl compound having a CaMKII inhibitory action, which is expected to be useful as an agent for the prophylaxis or treatment of cardiac diseases (particularly catecholaminergic polymorphic ventricular tachycardia, postoperative atrial fibrillation, heart failure, fatal arrhythmia) and the like. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the description, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 24, 2021
    Date of Patent: October 24, 2023
    Assignee: Cardurion Pharmaceuticals, Inc.
    Inventors: Nobuyuki Matsunaga, Junya Shirai, Tomohiro Okawa, Yasufumi Miyamoto, Zenyu Shiokawa, Takashi Nakahata, Akito Shibuya, Akira Kawada, Malcolm MacCoss
  • Patent number: 11702422
    Abstract: The present application discloses compounds having the following formula: or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined in the specification, as well as methods of making and using the compounds disclosed herein for treating or ameliorating an IL-17 mediated syndrome, disorder and/or disease.
    Type: Grant
    Filed: January 14, 2022
    Date of Patent: July 18, 2023
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Steven Goldberg, Timothy B. Rhorer, Connor Martin, Steven P. Meduna, Stefan McCarver, Alexander Valdes, Douglas Behenna, Xiaohua Xue, John Keith
  • Patent number: 11701353
    Abstract: The present invention provides methods for inhibiting Fyn kinase, using 5-3-pyridin-2-amine, 6-3-imidazo[1,2-a] pyrazine, 6-3-imidazo[1,2-b] pyridazine, N-(5-imidazo [2,1-b][1,3,4] thiadiazol-2-yl)-amine, 4-3-1H-pyrazolo[3,4-b] pyridine, and N-(3-imidazo [1,2-b] pyridazin-6-yl) amine compounds and methods of treatment, prevention, inhibition or amelioration of diseases and conditions associated with Fyn kinase using such compounds.
    Type: Grant
    Filed: June 9, 2020
    Date of Patent: July 18, 2023
    Assignee: Pathways Neuro Pharma, Inc.
    Inventor: Warren C. Lau
  • Patent number: 11690915
    Abstract: The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.
    Type: Grant
    Filed: September 15, 2021
    Date of Patent: July 4, 2023
    Assignee: Revolution Medicines, Inc.
    Inventors: Naing Aay, G. Leslie Burnett, James Cregg, Adrian L. Gill, John E. Knox, Elena S. Koltun, Yang Liu, Andreas Buckl, Bianca Jennifer Lee, David E. Wildes, Meghan A. Rice, Mallika Singh
  • Patent number: 11691979
    Abstract: The present application discloses compounds having the following formula: or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined in the specification, as well as methods of making and using the compounds disclosed herein for treating or ameliorating an IL-17 mediated syndrome, disorder and/or disease.
    Type: Grant
    Filed: April 28, 2021
    Date of Patent: July 4, 2023
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Steven Goldberg, Craig Woods, Timothy B. Rhorer, Connor Martin, Steven P. Meduna, Stefan McCarver, Alexander Valdes, Steven Loskot, Douglas Behenna, Alexander Raymond Rovira, Xiaohua Xue
  • Patent number: 11584750
    Abstract: The present invention belongs to the pharmaceutical field, and provides crystalline forms, solvates and the crystalline forms thereof of the compound (S)-4-amino-6-((1-(3-chloro-6-phenylimidazo[1,2-b]pyridazin-7-yl)ethyl)amino)pyrimidine-5-carbonitrile of the formula shown below, and the pharmaceutical compositions comprising the same as well as the methods of preparing the same and the use thereof.
    Type: Grant
    Filed: April 18, 2019
    Date of Patent: February 21, 2023
    Assignee: HUTCHISON MEDIPHARMA LIMITED
    Inventors: Zhenping Wu, Wenji Li, Ling Feng
  • Patent number: 11584744
    Abstract: The present disclosure is generally directed to compositions useful in the inhibition of MetRS and methods for treating diseases that are ameliorated by the inhibition of MetRS.
    Type: Grant
    Filed: June 22, 2018
    Date of Patent: February 21, 2023
    Assignee: University of Washington
    Inventors: Erkang Fan, Zhongsheng Zhang, Wenlin Huang, Frederick S. Buckner
  • Patent number: 11535622
    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: December 3, 2020
    Date of Patent: December 27, 2022
    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: 11524000
    Abstract: This disclosure relates to inhibitors of Mcl-1 stimulated homologous recombination (HR) DNA repair and uses for treating cancer. In certain embodiments, this disclosure relates to methods of treating cancer comprising administering an inhibitor of Mcl-1 in combination with other anti-cancer agents, e.g., that induce DNA replication stress. In certain embodiments, this disclosure relates to methods of treating cancer comprising administering compounds disclosed herein in combination with hydroxyurea, olaparib, or combinations thereof.
    Type: Grant
    Filed: October 23, 2018
    Date of Patent: December 13, 2022
    Assignee: Emory University
    Inventors: Xingming Deng, Guo Chen, Abu Syed Md Anisuzzaman
  • 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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