Plural Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 546/113)
  • Patent number: 11198681
    Abstract: The present invention provides compounds useful as inhibitors of PAD4, compositions thereof, and methods of treating PAD4-related disorders.
    Type: Grant
    Filed: February 22, 2017
    Date of Patent: December 14, 2021
    Assignee: Padlock Therapeutics, Inc.
    Inventors: Rajesh Devraj, Gnanasambandam Kumaravel, Holly Atton, Edward Beaumont, Elise Gadouleau, Laura Gleave, Philip Stephen Kerry, Cristina Lecci, Mirco Meniconi, Nat Monck, Jordan Palfrey, Kostas Papadopoulos, Heather Tye, Philip A. Woods
  • Patent number: 11198692
    Abstract: The present invention provides, in part, compounds of Formula I, or an N-oxide thereof, or a pharmaceutically acceptable salt of the compound or the N-oxide, wherein: (R1)a, (R2)b, (R3)c, L, A, and E are as described herein; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, N-oxides, or salts, and their uses for treating M4-mediated (or M4-associated) disorders including, e.g., Alzheimer's Disease, schizophrenia (e.g., its cognitive and negative symptoms), pain, addiction, and a sleep disorder.
    Type: Grant
    Filed: June 14, 2018
    Date of Patent: December 14, 2021
    Assignee: PFIZER INC.
    Inventors: Elizabeth Mary Beck, Michael Aaron Brodney, Matthew Frank Brown, Christopher Ryan Butler, Adam Matthew Gilbert, Erik Alphie Lachapelle, Laura Ann McAllister, Daniel Paul Uccello, Lei Zhang
  • Patent number: 11059789
    Abstract: Provided herein are compounds and pharmaceutical compositions useful in modulating kinase activity, and related diseases. Also provided herein are methods of treating an eye disease or disorder in a subject. Also provided herein are methods of reducing intraocular pressure in a subject. Also provided herein are methods of modulating kinase activity in a cell. Also provided herein are methods of making the compounds provided herein, and compounds useful for the preparation of the compounds provided herein.
    Type: Grant
    Filed: August 30, 2019
    Date of Patent: July 13, 2021
    Assignee: Aerie Pharmaceuticals, Inc.
    Inventors: Mitchell A. deLong, Eric Carlson, Casey Kopczynski, Jill M. Sturdivant, Cynthia Lichorowic
  • Patent number: 11053241
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.
    Type: Grant
    Filed: November 27, 2019
    Date of Patent: July 6, 2021
    Assignee: Nimbus Lakshmi, Inc.
    Inventors: Jeremy Robert Greenwood, Craig E. Masse
  • Patent number: 11053244
    Abstract: Disclosed are compounds of Formula (I) N-oxides, or salts thereof, wherein G, A, R1, R5, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.
    Type: Grant
    Filed: June 24, 2020
    Date of Patent: July 6, 2021
    Assignee: Bristol-Myers Squibb Company
    Inventors: Alaric J. Dyckman, Dharmpal S. Dodd, Christopher P. Mussari, Trevor C. Sherwood, Brian K. Whiteley, John L. Gilmore, Sreekantha Ratna Kumar, Laxman Pasunoori, Pitani Veera Venkata Srinivas, Srinivasan Kunchithapatham Duraisamy, Subramanya Hegde, Rushith Kumar Anumula
  • Patent number: 11021481
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of HPK1, and the treatment of HPK1-mediated disorders.
    Type: Grant
    Filed: September 14, 2020
    Date of Patent: June 1, 2021
    Assignee: Nimbus Saturn, Inc.
    Inventors: Neelu Kaila, Ian Linney, Stuart Ward, Grant Wishart, Ben Whittaker, Alexandre Cote, Jeremy Robert Greenwood, Abba Leffler, Steven K. Albanese, Daniel L. Severance
  • Patent number: 10913739
    Abstract: The present disclosure relates to processes for the production of salts and crystalline forms of a compound having the formula.
    Type: Grant
    Filed: July 24, 2018
    Date of Patent: February 9, 2021
    Assignee: Vitae Pharmaceuticals, LLC (121374)
    Inventors: Robert J. Duguid, John A. Grosso, Sergiy Krasutsky
  • Patent number: 10844056
    Abstract: The present invention relates to HSP90 inhibitors containing fused amino pyridine core that are useful as inhibitors of HSP90 and their use in the treatment of HSP90 related diseases and disorders such as cancer, an autoimmune disease, or a neurodegenerative disease.
    Type: Grant
    Filed: August 28, 2019
    Date of Patent: November 24, 2020
    Assignee: Curis, Inc.
    Inventors: Xiong Cai, Changgeng Qian, Haixiao Zhai
  • Patent number: 10781204
    Abstract: The present invention provides compounds of formula I, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.
    Type: Grant
    Filed: June 13, 2018
    Date of Patent: September 22, 2020
    Assignee: Nimbus Lakshmi, Inc.
    Inventors: Craig E. Masse, Jeremy Robert Greenwood, Donna L. Romero, Geraldine C. Harriman, Ronald T. Wester, Mee Shelley, Joshua Jahmil Kennedy-Smith, Markus Dahlgren, Sayan Mondal, Shaughnessy Robinson
  • Patent number: 10723735
    Abstract: This invention relates to novel processes for synthesizing [1-(4-Methanesulfonyl-2-trifluoromethyl-benzyl)-2-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl]-acetic acid and to intermediates that are used in such processes.
    Type: Grant
    Filed: March 29, 2018
    Date of Patent: July 28, 2020
    Inventors: Fabrice Gallou, Philipp Lustenberger, Christian Mathes, Qiangbiao Pan, Benli Zou
  • Patent number: 10682344
    Abstract: A method of treating liver fibrosis with CCR2 antagonists is provided. The liver fibrosis may be associated with non-alcoholic steatohepatitis (NASH), non-alcoholic fatty liver disease (NAFLD), emerging cirrhosis, non-cirrhotic hepatic fibrosis, type 2 diabetes mellitus (T2DM) or metabolic syndrome (MS).
    Type: Grant
    Filed: June 2, 2017
    Date of Patent: June 16, 2020
    Assignee: ChemoCentryx, Inc.
    Inventors: Zhenhua Miao, Israel Charo
  • Patent number: 10647716
    Abstract: Provided herein are heterocyclic compounds of Formula (I), pharmaceutical compositions containing such a compound and their therapeutic uses, methods for their preparation, intermediate compounds, pharmaceutical compositions containing such a compound, and their therapeutic uses.
    Type: Grant
    Filed: June 14, 2019
    Date of Patent: May 12, 2020
    Assignee: Plexxikon Inc.
    Inventors: Prabha N. Ibrahim, Wayne Spevak, Jiazhong Zhang, Songyuan Shi, Ben Powell, Yan Ma
  • Patent number: 10647675
    Abstract: Provided is a compound showing excellent Antifungal activity against Trichophyton fungus, which is a major causative microorganism of superficial mycosis, and high effectiveness on diseases caused by Trichophyton fungi. A biaryl derivative represented by the formula (I) or a salt thereof: wherein ring A is an optionally substituted phenyl, or an optionally substituted 5- or 6-membered ring heteroaryl (ring A may be further condensed to form an optionally substituted fused ring); Q is CH2, C?O, NH, O, S or the like; X1, X2 and X3 are CR1 or N; Y is CH or N; Z is CR2b or N; R2a and R2b are each a hydrogen atom, a halogen atom, an optionally substituted C1-C6 alkyl group, a C1-C6 haloalkyl group or the like; R2a and R2b may form, together with carbon atoms bonded thereto, an optionally substituted carbocycle, or an optionally substituted heterocycle.
    Type: Grant
    Filed: September 14, 2016
    Date of Patent: May 12, 2020
    Assignee: KAKEN PHARMACEUTICAL CO., LTD.
    Inventors: Atsushi Watanabe, Yuuki Sato, Keiji Ogura, Yoshiyuki Tatsumi
  • Patent number: 10597396
    Abstract: This invention pertains generally to compounds of Formula (A), as further described herein, which act as beta-lactamase inhibitors, and salts, crystalline forms and formulations thereof. In certain aspects, the invention pertains to methods of using such compounds in combination with a beta-lactam antibiotic to treat infections caused by Gram-negative bacteria, including drug-resistant strains.
    Type: Grant
    Filed: September 28, 2017
    Date of Patent: March 24, 2020
    Assignee: Novartis AG
    Inventors: Anthony Casarez, Markus Furegati, Guido Koch, Xiaodong Lin, Flavio Ossola, Folkert Reck, Robert Lowell Simmons, Qingming Zhu
  • Patent number: 10526328
    Abstract: Compounds represented by formula 1 can be potent and/or partially selective for the Kv7.2/7.3 heteromultimer. They may be useful in treating disorders related to seizures, pain, neurotransmitter release, etc.
    Type: Grant
    Filed: September 7, 2018
    Date of Patent: January 7, 2020
    Assignee: Knopp Biosciences LLC
    Inventors: Lynn Resnick, George T. Topalov, Charles A. Flentge, James S. Hale, David A. Mareska, Justin K. Belardi, Kai Zhang, Scott S. Harried
  • Patent number: 10519143
    Abstract: Disclosed is a new indole compound, in particular, the compound as shown in formula (I), and a preparation method, pharmaceutical composition and use thereof as an estrogen receptor down-regulator in preparing drugs for treating estrogen receptor-positive breast cancer.
    Type: Grant
    Filed: March 24, 2017
    Date of Patent: December 31, 2019
    Assignee: LUOXIN PHARMACEUTICAL (SHANGHAI) CO., LTD.
    Inventors: Jianyu Lu, Charles Z. Ding, Lihong Hu, Huijun He, Shuhui Chen, Jiaqiang Dong, Tie-Lin Wang
  • Patent number: 10414754
    Abstract: Compounds of formula (I) wherein Ra, Rb, Rc, Rd, T, R3, R4, R5, X, Y and Het are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.
    Type: Grant
    Filed: February 27, 2018
    Date of Patent: September 17, 2019
    Assignees: LES LABORATOIRES SERVIER, VERNALIS (R&D) LTD
    Inventors: Arnaud Le Tiran, Thierry Le Diguarher, Jérôme-Benoît Starck, Jean-Michel Henlin, Guillaume De Nanteuil, Olivier Geneste, James Edward Paul Davidson, James Brooke Murray, I-Jen Chen
  • Patent number: 10407427
    Abstract: Novel processes are disclosed for manufacture of N-(3-(5-(4-chlorophenyl)-l H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonamide (I), wherein no protection-deprotection sequences or halogenation steps are required and use of palladium catalysts is minimized.
    Type: Grant
    Filed: June 30, 2017
    Date of Patent: September 10, 2019
    Assignee: FERMION OY
    Inventor: Antti Kataja
  • Patent number: 10377743
    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, stereoisomer or prodrug thereof, wherein A, B, R?, Q, W, X, Y, Z, n1, n2 and 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: October 6, 2017
    Date of Patent: August 13, 2019
    Assignee: Araxes Pharma LLC
    Inventors: Liansheng Li, Jun Feng, Yuan Liu, Pingda Ren, Yi Liu, Tao Wu, Yi Wang
  • Patent number: 10221180
    Abstract: The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a mammal, and in particular to inhibitors of NF-?B-inducing kinase (NIK—also known as MAP3K14) useful for treating diseases such as cancer, inflammatory disorders, metabolic disorders and autoimmune disorders. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds or pharmaceutical compositions for the prevention or treatment of diseases such as cancer, inflammatory disorders, metabolic disorders including obesity and diabetes, and autoimmune disorders.
    Type: Grant
    Filed: October 22, 2015
    Date of Patent: March 5, 2019
    Assignee: Janssen Pharmaceutica NV
    Inventors: George Hynd, Patrizia Tisselli, Calum Macleod, Samuel Edward Mann, Terry Aaron Panchal, John Gary Montana, Stephen Colin Price
  • Patent number: 10202373
    Abstract: The present invention provides a compound of formula I: wherein R1, X1, X2, R2, R3, R4, R5, n, and m are as described in the specification. Such compounds are inhibitors of VPS34 and thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Grant
    Filed: January 13, 2015
    Date of Patent: February 12, 2019
    Assignee: MILLENNIUM PHARMACEUTICALS, INC.
    Inventors: Indu T. Bharathan, Chris Blackburn, Jeffrey P. Ciavarri, Jouhara Chouitar, Courtney A. Cullis, Natalie D'Amore, Paul E. Fleming, Kenneth M. Gigstad, Krista E. Gipson, Mario Girard, Yongbo Hu, Janice Lee, Gang Li, Mansoureh Rezaei, Michael D. Sintchak, Francois Soucy, Stephen G. Stroud, Tricia J. Vos, He Xu, Yingchun Ye
  • Patent number: 10195188
    Abstract: The present disclosure describes methods of treating pancreatic cancer and limiting over-expression of oncogenes, activating tumor suppressor genes or regulating signaling proteins in patients comprising administering compounds and pharmaceutical combinations as described herein.
    Type: Grant
    Filed: September 1, 2017
    Date of Patent: February 5, 2019
    Assignee: ChemoCentryx, Inc.
    Inventors: Petrus Bekker, Shichang Miao, Israel Charo, Tom Schall
  • Patent number: 10160755
    Abstract: Compounds of Formula I: or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein R1, R2, Q1, Q2, and Q3, are described in this disclosure, compositions thereof, and methods and uses thereof.
    Type: Grant
    Filed: April 7, 2016
    Date of Patent: December 25, 2018
    Assignee: Plexxikon Inc.
    Inventors: Jack Lin, Phuongly Pham, John Buell, Ken Dong, Prabha Ibrahim, Wayne Spevak, Garson Tsang, Guoxian Wu, Ying Zhang
  • Patent number: 10072005
    Abstract: 4-Azaindole derivatives which are modulators of muscarinic acetylcholine receptor (mAChR) M1 and which may be effective for the prevention or disease modifying or symptomatic treatment of cognitive deficits associated with neurological disorders such as Alzheimer-type dementia (AD) or dementia with Lewy bodies (DLB), and a pharmaceutical composition comprising a 4-azaindole derivative as an active ingredient.
    Type: Grant
    Filed: January 19, 2018
    Date of Patent: September 11, 2018
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Andrew Payne, Jose Luis Castro Pineiro, Louise Michelle Birch, Afzal Khan, Alan James Braunton, James Edward Kitulagoda, Motohiro Soejima
  • Patent number: 10059693
    Abstract: The present invention provides novel compounds of any one of Formulae (I)-(III), and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I)-(III) and pharmaceutical compositions thereof that are mucus penetrating. The invention also provides methods and kits for using the inventive compounds, and pharmaceutical compositions thereof, for treating and/or preventing diseases associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor (e.g., vascular endothelial growth factor (VEGF)), such as proliferative diseases (e.g., cancers, benign neoplasms, inflammatory diseases, autoimmune diseases) and ocular diseases (e.g., macular degeneration, glaucoma, diabetic retinopathy, retinoblastoma, edema, uveitis, dry eye, blepharitis, and post-surgical inflammation) in a subject in need thereof.
    Type: Grant
    Filed: October 12, 2017
    Date of Patent: August 28, 2018
    Assignee: Kala Pharmaceuticals, Inc.
    Inventors: Winston Zapanta Ong, Pawel Wojciech Nowak, John Thomas Feutrill, Jinsoo Kim
  • Patent number: 10059692
    Abstract: The present invention provides novel compounds of any one of Formulae (I)-(III), and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I)-(III) and pharmaceutical compositions thereof that are mucus penetrating. The invention also provides methods and kits for using the inventive compounds, and pharmaceutical compositions thereof, for treating and/or preventing diseases associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor (e.g., vascular endothelial growth factor (VEGF)), such as proliferative diseases (e.g., cancers, benign neoplasms, inflammatory diseases, autoimmune diseases) and ocular diseases (e.g., macular degeneration, glaucoma, diabetic retinopathy, retinoblastoma, edema, uveitis, dry eye, blepharitis, and post-surgical inflammation) in a subject in need thereof.
    Type: Grant
    Filed: October 12, 2017
    Date of Patent: August 28, 2018
    Assignee: Kala Pharmaceuticals, Inc.
    Inventors: Winston Zapanta Ong, Pawel Wojciech Nowak, John Thomas Feutrill, Jinsoo Kim
  • Patent number: 9975894
    Abstract: Provided herein are heterocyclic compounds of Formula (I), pharmaceutical compositions containing such a compound and their therapeutic uses, methods for their preparation, intermediate compounds, pharmaceutical compositions containing such a compound, and their therapeutic uses.
    Type: Grant
    Filed: August 29, 2017
    Date of Patent: May 22, 2018
    Assignee: Plexxikon Inc.
    Inventors: Prabha N. Ibrahim, Wayne Spevak, Jiazhong Zhang, Songyuan Shi, Ben Powell, Yan Ma
  • Patent number: 9974795
    Abstract: Provided is a pharmaceutical composition comprising a Cdc7 inhibitor and an M phase promoter. In particular, the Cdc7 inhibitor contained in the pharmaceutical composition is a furanone derivative represented by formula (I), or a pharmaceutically acceptable salt thereof. (In the formula, A is —COOR1 or a hydrogen atom; R1 is a hydrogen atom, an optionally substituted hydrocarbon group, or an optionally substituted heterocycle; R2 and R3 are the same or different and are each a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted phenyl group, an optionally substituted heterocycle, an optionally substituted heterocyclic condensed ring, or an optionally substituted amino group. Alternatively, R2 and R3 may, together with the nitrogen atoms bonding the same, form an optionally substituted heterocycle or optionally substituted heterocyclic condensed ring. R4 is a hydrogen atom or halogen atom.
    Type: Grant
    Filed: January 26, 2015
    Date of Patent: May 22, 2018
    Assignee: CARNA BIOSCIENCES, INC.
    Inventors: Yoko Funakoshi, Chika Tanaka, Tokiko Asami, Masaaki Sawa
  • Patent number: 9926312
    Abstract: 4-Azaindole derivatives which are modulators of muscarinic acetylcholine receptor (mAChR) M1 and which may be effective for the prevention or disease modifying or symptomatic treatment of cognitive deficits associated with neurological disorders such as Alzheimer-type dementia (AD) or dementia with Lewy bodies (DLB), and a pharmaceutical composition comprising a 4-azaindole derivative as an active ingredient.
    Type: Grant
    Filed: September 30, 2014
    Date of Patent: March 27, 2018
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Andrew Payne, Jose Luis Castro Pineiro, Louise Michelle Birch, Afzal Khan, Alan James Braunton, James Edward Kitulagoda, Motohiro Soejima
  • Patent number: 9918990
    Abstract: The present invention relates to compounds represented by the general Formula I which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.
    Type: Grant
    Filed: June 20, 2016
    Date of Patent: March 20, 2018
    Assignee: Incyte Corporation
    Inventors: Eddy W. Yue, Andrew P. Combs, Brent Douty
  • Patent number: 9908882
    Abstract: A process for preparing halogenated azaindole compounds makes use of stable reagents including a brominating reagent, a boroxine and a sulfonic anhydride to enhance the selectivity and yield of the final product. In addition, the process is associated with various other advantages, including the ability to recycle reagents, cost reduction, and improved manufacturability.
    Type: Grant
    Filed: December 17, 2015
    Date of Patent: March 6, 2018
    Assignee: ViiV HEALTHCARE UK (NO.4) LIMITED
    Inventors: Michael S. Bultman, Benjamin Cohen, Francisco Gonzalez-Bobes, Matthew R. Hickey
  • Patent number: 9872894
    Abstract: Disclosed are immunogenic compositions that include one or more polypeptides that, when administered to a subject with adjuvant, elicit an immune response against medullary thyroid cancer. Disclosed are methods of eliciting an immune response and/or treating cancer, such as medullary thyroid carcinoma or other thyroid carcinomas.
    Type: Grant
    Filed: February 17, 2017
    Date of Patent: January 23, 2018
    Inventor: Timothy Andrew Erickson
  • Patent number: 9845321
    Abstract: The present invention is concerned with novel 1,3-dihydro-2H-benzimidazol-2-one derivatives substituted with heterocycles having formula (I) stereoisomeric forms thereof, and the pharmaceutically acceptable addition salts, and the solvates thereof, wherein R4, R5, Z and Het have the meaning defined in the claims. The compounds according to the present invention are useful as inhibitors on the replication of the respiratory syncytial virus (RSV). The invention further concerns the preparation of such novel compounds, compositions comprising these compounds, and the compounds for use in the treatment of respiratory syncytial virus infection.
    Type: Grant
    Filed: January 8, 2016
    Date of Patent: December 19, 2017
    Assignee: Janssen Sciences Ireland UC
    Inventors: Abdellah Tahri, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Sandrine Marie Helene Vendeville, Lili Hu, Samuel Dominique Demin, Ludwig Paul Cooymans
  • Patent number: 9695200
    Abstract: Disclosed herein are heterocyclic compounds and compositions useful in the treatment of ITK mediated diseases, such as inflammation, having the structure of Formula (I): wherein R1, R2, and X are as defined in the detailed description. Methods of inhibition of ITK activity in a human or animal subject are also provided.
    Type: Grant
    Filed: January 25, 2016
    Date of Patent: July 4, 2017
    Assignee: Confluence Life Sciences, Inc.
    Inventors: Eric Jon Jacobsen, James Robert Blinn, John Robert Springer, Susan L. Hockerman
  • Patent number: 9663514
    Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein G, p, R1, R2, R3a, R4, and R5 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating disorders, diseases, and conditions involving the immune system and inflammation, including rheumatoid arthritis, cancer, and other disorders, diseases, and conditions for which inhibition of SYK is indicated.
    Type: Grant
    Filed: May 7, 2015
    Date of Patent: May 30, 2017
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Mitsunori Kono, Zhe Nie
  • Patent number: 9650379
    Abstract: The present invention relates to novel azaindole derivatives, and more particularly, to novel azaindole derivatives having histone deacetylase (HDAC) inhibitory activity, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof or solvates thereof, the use thereof for the preparation of pharmaceutical compositions, pharmaceutical compositions containing the same, a method of treating disease using the pharmaceutical compositions, and methods for preparing the novel azaindole derivatives. The novel azaindole derivatives according to the present invention are selective histone deacetylase (HDAC) inhibitors, and may be used as agents for treating malignant tumor diseases, inflammatory diseases, rheumatoid arthritis, and neurodegenerative diseases.
    Type: Grant
    Filed: December 12, 2014
    Date of Patent: May 16, 2017
    Assignee: CHONG KUN DANG PHARMACEUTICAL CORP.
    Inventors: Changsik Lee, Hyun-Mo Yang, Changkon Lee, Miseon Bae, Soyoung Kim, Youngil Choi, Nina Ha, Jaekwang Lee, Jungtaek Oh, Hyeseung Song, Ilhyang Kim, Daekyu Choi, Jaeki Min, Hyojin Lim, Daekwon Bae
  • Patent number: 9624217
    Abstract: Provided are novel compounds of Formula (I): pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by ROR?. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I) and methods for their use in treating one or more inflammatory, metabolic, autoimmune and other diseases or disorders.
    Type: Grant
    Filed: January 7, 2016
    Date of Patent: April 18, 2017
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: David A. Claremon, Lawrence Wayne Dillard, Chengguo Dong, Yi Fan, Lanqi Jia, Zhijie Liu, Stephen D. Lotesta, Andrew Marcus, Suresh B. Singh, Colin M. Tice, Jing Yuan, Wei Zhao, Yajun Zheng, Linghang Zhuang
  • Patent number: 9580419
    Abstract: The present invention provides pyrrolo[2,3-b]pyridine-4-yl amines pyrrolo[2,3-b]pyrimidin-4-yl amines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases and cancer.
    Type: Grant
    Filed: July 15, 2015
    Date of Patent: February 28, 2017
    Assignees: Incyte Corporation, Incyte Holdings Corporation
    Inventors: James D. Rodgers, Haisheng Wang, Andrew P. Combs, Richard B. Sparks
  • Patent number: 9505765
    Abstract: 4-alkoxy/aralkoxy-5-substituted-pyrrolopyrimidine compounds, pharmaceutically acceptable salts, solvates and pharmaceutical compositions of compounds embraced by Formula (I), provide a therapeutic benefit to subjects with disease conditions, especially cancer, wherein R1 and R2 are as defined in the detailed description.
    Type: Grant
    Filed: July 26, 2013
    Date of Patent: November 29, 2016
    Assignee: CONFLUENCE LIFE SCIENCES INC.
    Inventors: Eric Jonathan Jacobsen, John Robert Springer, James Robert Blinn, Balekudru Devadas
  • Patent number: 9408924
    Abstract: Compounds are disclosed that are useful for noninvasive imaging in the near-infrared spectral range.
    Type: Grant
    Filed: November 24, 2014
    Date of Patent: August 9, 2016
    Assignee: LI-COR, INC.
    Inventors: Xinshe Xu, Daniel R. Draney, Lael Cheung
  • Patent number: 9408835
    Abstract: A pharmaceutical composition containing, as the active ingredient, 4-{[(1R,2s,3S,5s,7s)-5-hydroxy-2-adamantyl]amino}-1H-pyrrolo[2,3-b]pyridine-5-carboxamide, of which the solubility in an acidic pH region is different from that in a neutral pH region, with rapid disintegration property and rapid drug dissolution property as well as the expectation of a good drug dosing compliance, is provided. The pharmaceutical composition for oral administration of the present invention contains 4-{[(1R,2s,3S,5s,7s)-5-hydroxy-2-adamantyl]amino}-1H-pyrrolo[2,3-b]pyridine-5-carboxamide or a pharmaceutically acceptable salt thereof, and a hydrophilic lubricant, and is useful as a pharmaceutical composition for oral administration with rapid disintegration property and rapid drug dissolution property as well as the expectation of a good drug dosing compliance.
    Type: Grant
    Filed: March 28, 2014
    Date of Patent: August 9, 2016
    Assignee: ASTELLAS PHARMA INC.
    Inventors: Seiji Takae, Hiroyuki Kojima, Atsushi Sakurai, Tetsuya Tamura, Hiroaki Tasaki, Atsushi Muro
  • Patent number: 9409909
    Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
    Type: Grant
    Filed: July 29, 2014
    Date of Patent: August 9, 2016
    Assignee: ChemoCentryx, Inc.
    Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M. K. Pennell, Edward J. Sullivan, William D. Thomas, Solomon Ungashe, Penglie Zhang, Jay Powers, Sreenivas Punna
  • Patent number: 9403822
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
    Type: Grant
    Filed: March 11, 2015
    Date of Patent: August 2, 2016
    Assignee: ABBVIE INC.
    Inventors: Zhi-Fu Tao, Xilu Wang, Andrew J Souers, Nathaniel D. Catron, Gerard M. Sullivan
  • Patent number: 9382244
    Abstract: The compound 4-(2-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-2,7-naphthyridin-1-ylamine and pharmaceutically usable salts and/or tautomers thereof. The use of this compound for the treatment of tumors, tumor growth, tumor metastases and/or AIDS.
    Type: Grant
    Filed: September 9, 2013
    Date of Patent: July 5, 2016
    Assignee: Merck Patent GmbH
    Inventors: Alfred Jonczyk, Frank T. Zenke, Christiane Amendt
  • Patent number: 9382242
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Q is a bond or —N(R5)—; T is a bond, —O—, —C(O)—; S, —N(R5)—, or —C(R6?R7?); U is a bond or —C(R6)(R7)— Y is C or N; Z is C or N; ring A, including variables Y and Z, is a three to nine membered cycloalkyl, cycloalkenyl, heterocyclyl, heterocyclenyl, aryl, and heteroaryl ring having 0 to 4, preferably 0 to 2, heteroatoms independently selected from the group consisting of O, S, N and —N(R)—, wherein ring A is unsubstituted or substituted with 1 to 5 independently selected R1 moieties and/or oxo when ring A is cycloalkyl, cycloalkenyl, heterocyclyl or heterocyclenyl; and R, R1, R2, R3, R4, R5, R6, R6, R7 and R7? are as defined in the specification; pharmaceutical compositions comprising the compounds of formula I and the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases.
    Type: Grant
    Filed: March 26, 2014
    Date of Patent: July 5, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Andrew W. Stamford, Guoqing Li
  • Patent number: 9353107
    Abstract: The present application relates to novel 3-(pyrazolyl)-1H-pyrrolo[2,3-b]pyridine derivatives of formula (I), as protein kinase inhibitors. The invention particularly relates to compounds of formula (I), preparation of compounds and pharmaceutical compositions thereof. The invention further relates to pharmaceutically acceptable salts and compositions comprising the said novel 3-(pyrazolyl)-1H-pyrrolo[2,3-b]pyridine derivatives and their use in the treatment of various disorders.
    Type: Grant
    Filed: July 1, 2013
    Date of Patent: May 31, 2016
    Assignees: Aurigene Discovery Technologies Limited, Um Pharmauji Sdn. Bhd.
    Inventors: Venkateshwar Rao Gummadi, Subramanya Hosahalli, Srinivas Nanduri, Girish Aggunda Renukappa
  • Patent number: 9340540
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.
    Type: Grant
    Filed: February 27, 2015
    Date of Patent: May 17, 2016
    Assignee: NIMBUS LAKSHMI, INC.
    Inventors: Craig E. Masse, Jeremy Robert Greenwood, Donna L. Romero, Geraldine C. Harriman, Ronald T. Wester, Mee Shelley, Joshua Jahmil Kennedy-Smith, Markus Dahlgren
  • Patent number: 9340573
    Abstract: Disclosed are compounds of Formula (I) or pharmaceutically acceptable salts thereof, wherein W, Y, Z, R1, R2, R3 and R4 are as described in this application, and methods of using the compounds in the treatment of cancer.
    Type: Grant
    Filed: October 8, 2013
    Date of Patent: May 17, 2016
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Joan Heather Hogg, Yan Lou
  • Patent number: 9321764
    Abstract: The present invention provides for compounds of formula (I) wherein R1, R2, R3, R4, and R5 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: April 26, 2016
    Assignee: AbbVie Inc.
    Inventors: Le Wang, John Pratt, Lisa A. Hasvold, Dachun Liu, Yujia Dai, Steven D. Fidanze, James H. Holms, Robert A. Mantei, Keith F. McDaniel, George S. Sheppard, William J. McClellan
  • Patent number: 9315501
    Abstract: The present invention relates to bicyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.
    Type: Grant
    Filed: November 26, 2014
    Date of Patent: April 19, 2016
    Assignee: Incyte Corporation
    Inventors: Eddy W. Yue, Andrew P. Combs, Andrew W. Buesking