Polycyclo Ring System Having The Four-membered Hetero Ring As One Of The Cyclos Patents (Class 514/210.16)
  • Patent number: 11407753
    Abstract: The present description relates to compounds, forms, and pharmaceutical compositions thereof and methods of using such compounds, forms, or compositions thereof for treating or ameliorating Huntington's disease. In particular, the present description relates to substituted bicyclic heteroaryl compounds of Formula (I), forms and pharmaceutical compositions thereof and methods of using such compounds, forms, or compositions thereof for treating or ameliorating Huntington's disease.
    Type: Grant
    Filed: June 5, 2018
    Date of Patent: August 9, 2022
    Assignee: PTC THERAPEUTICS, INC.
    Inventors: Matthew G. Woll, Lukiana Amedzo, Suresh Babu, Scott J. Barraza, Anuradha Bhattacharyya, Gary Mitchell Karp, Anthony R. Mazzotti, Jana Narasimhan, Jigar Patel, Anthony Turpoff, Zhenrong Xu
  • Patent number: 11326165
    Abstract: Described herein are small molecule splicing modulator compounds that modulate splicing of mRNA, such as pre-mRNA, encoded by genes, and methods of use of the small molecule splicing modulator compounds for modulating splicing and treating diseases and conditions.
    Type: Grant
    Filed: October 15, 2021
    Date of Patent: May 10, 2022
    Assignee: SKYHAWK THERAPEUTICS, INC.
    Inventors: Michael Luzzio, Kathleen McCarthy, William Haney
  • Patent number: 11319324
    Abstract: The present invention covers substituted. Pyrazolo-pyrrolo-pyrimidine-dione (PPPD) compounds of general formula (I): in which R1, R2 and R3 are as defined herein, methods of preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of neurogenic diseases, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: October 18, 2018
    Date of Patent: May 3, 2022
    Assignees: Bayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft
    Inventors: Marcus Koppitz, Holger Siebeneicher, Nico Bräuer, Elisabeth Pook, Andrea Rotgeri, Roland Neuhaus, Oliver Martin Fischer, Jens Nagel, Adam James Davenport, James Lindsay Carr, Robert James Townsend, Nina Connelly Ursinyova, Shelley Anne Parrott
  • Patent number: 11286252
    Abstract: The present invention provides compounds of Formula (I), or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds modulate the activity of farnesoid X receptor (FXR), for example, as agonists. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
    Type: Grant
    Filed: October 31, 2018
    Date of Patent: March 29, 2022
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jianxin Feng, Chunjian Liu, Yanting Huang
  • Patent number: 11192899
    Abstract: The invention relates to quinoxaline derivatives of the general formula I, and the use of the compounds of the present invention for the treatment and/or prevention of hyperproliferative or infectious diseases and disorders in mammals, especially humans, and pharmaceutical compositions containing such compound.
    Type: Grant
    Filed: August 20, 2018
    Date of Patent: December 7, 2021
    Assignee: MERCK PATENT GMBH
    Inventors: Eva-Maria Tanzer, Kai Schiemann, Markus Klein
  • Patent number: 11186592
    Abstract: The invention relates to thiazolopyridine derivatives of the general formula I, and the use of the compounds of the present invention for the treatment and/or prevention of hyperproliferative or infectious diseases and disorders in mammals, especially humans, and pharmaceutical compositions containing such compound.
    Type: Grant
    Filed: July 2, 2018
    Date of Patent: November 30, 2021
    Assignee: Merck Patent GmbH
    Inventors: Eva-Maria Tanzer, Kai Schiemann, Markus Klein
  • Patent number: 11161856
    Abstract: Provided herein are compounds of the formula: and compositions comprising the same, which are useful as modulators of MAGL. Furthermore, the subject compounds and compositions are useful for the treatment of pain.
    Type: Grant
    Filed: August 28, 2018
    Date of Patent: November 2, 2021
    Assignee: H. LUNDBECK A/S
    Inventors: Cheryl A. Grice, Olivia D. Weber, Daniel J. Buzard, Michael B. Shaghafi
  • Patent number: 11162101
    Abstract: Described herein are small molecule splicing modulator compounds that modulate splicing of mRNA, such as pre-mRNA, encoded by genes, and methods of use of the small molecule splicing modulator compounds for modulating splicing and treating diseases and conditions.
    Type: Grant
    Filed: February 4, 2020
    Date of Patent: November 2, 2021
    Assignee: SKYHAWK THERAPEUTICS, INC.
    Inventors: Michael Luzzio, Kathleen McCarthy, William Haney
  • Patent number: 11130751
    Abstract: The present invention relates to substituted quinoxaline and pyridopyrazine derivatives of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as pI3K? inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Grant
    Filed: March 29, 2018
    Date of Patent: September 28, 2021
    Assignee: Janssen Pharmaceutica NV
    Inventors: Patrick René Angibaud, Olivier Alexis Georges Querolle, Didier Jean-Claude Berthelot, Christophe Meyer, Matthieu Philippe Victor Willot, Lieven Meerpoel, Thierry François Alain Jean Jousseaume
  • Patent number: 11111237
    Abstract: The present disclosure relates to a compound derivative containing a 6-7 bicyclic ring and use thereof. The compound according to the present invention can be effectively used in the prevention or treatment of diseases caused by PRMT5 by acting as a PRMT5 inhibitor.
    Type: Grant
    Filed: November 24, 2020
    Date of Patent: September 7, 2021
    Assignee: SK BIOPHARMACEUTICALS CO., LTD.
    Inventors: Yong Je Shin, Jin Hee Kim, Jun Lee, Sook Kyung Park, Ho Yeon Lee, Hyun Suk Choi, Se Hyuk Kim, Eun Ji Kang, Ho Youl Lee, Soo Yeon Jung
  • Patent number: 11078197
    Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically-acceptable salts thereof wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
    Type: Grant
    Filed: July 11, 2018
    Date of Patent: August 3, 2021
    Assignee: Bristol-Myers Squibb Company
    Inventors: Peter W. Glunz, Vladimir Ladziata, Indawati De Lucca, George O. Tora, Tarun Kumar Maishal, Raghuram Tangirala, Kamalraj Thiyagarajan
  • Patent number: 11078189
    Abstract: Benzimidazole derivatives of formula (I): wherein: R1 is —(CH2)m-R4 or R2 is halo, —(CH2)m—NH2 or —(CH2)n—C(?NH)—NH2; R3 is H or F; R4 is —NH—(CH2)2—(NH)r—R5, —NH—(CHR5R6) or a group of the following formula (A): (A) W is —(CH2)m—, —CH2—O—CH2—, —CH2—S—CH2—, —(CH2)r—S(O)2—CH2— or —(CH2)r—NR5—CH2—; m is an integer of 1 to 3; n is 1 or 2; p is 1 and V is CH; or p is O and V is N; q is 0 or 1; r is 0 or 1; R5 is H, —SO2Me, —SO2Et, —SO2CF3, —COMe, —CONMe2, —CONH2 or —CH2CH2SO2Me; R6 is H or C1-C6 alkyl; and R7 is —SO2Me, —SO2Et, —SO2CF3, —COMe, —CONMe2, —CONH2 or —CH2CH2SO2Me; and the pharmaceutically acceptable salts thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.
    Type: Grant
    Filed: July 20, 2018
    Date of Patent: August 3, 2021
    Assignee: REVIRAL LIMITED
    Inventors: Stuart George Cockerill, James Good
  • Patent number: 11059780
    Abstract: The present invention provides a substituted pyrrolidine compound having an orexin type 2 receptor agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the specification, or a salt thereof, has an orexin type 2 receptor agonist activity, and is useful as an agent for the prophylaxis or treatment of narcolepsy.
    Type: Grant
    Filed: March 7, 2018
    Date of Patent: July 13, 2021
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Masaki Daini, Yuhei Miyanohana, Satoshi Mikami, Yuichi Kajita, Masaki Ogino, Tatsuki Koike, Kohei Takeuchi
  • Patent number: 11045479
    Abstract: The present disclosure relates generally to novel molecules, compositions, and formulations for treatment of bacterial infections in general and more specifically to bacterial infections with antibiotic resistant pathogens.
    Type: Grant
    Filed: July 18, 2018
    Date of Patent: June 29, 2021
    Assignee: VYOME THERAPEUTICS LIMITED
    Inventors: Shiladitya Sengupta, Suresh Rameshlal Chawrai, Shamik Ghosh, Sumana Ghosh, Nilu Jain, Suresh Sadhasivam, Richard Buchta, Anamika Bhattacharyya
  • Patent number: 11021482
    Abstract: Disclosed herein are arylpyridinone compounds and compositions useful in the treatment of ITK mediated diseases, such as inflammation, having the structures of Formulas (I)-(IV): wherein the R groups, m, n, 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: August 12, 2019
    Date of Patent: June 1, 2021
    Assignee: Adaris Therapeutics, Inc.
    Inventors: Eric Jon Jacobsen, David Randolph Anderson, James Robert Blinn, Susan Landis Hockerman, Richard Heier, Paramita Mukherjee
  • Patent number: 10919910
    Abstract: The present invention relates to seco (opened ring) macrolide compounds, to the process for preparation thereof, to the use of said seco macrolide compounds as intermediates for preparation of macrolide based macrocycles, to macrolide based macrocycles obtained from said seco macrolide compounds, to the process for preparation of macrolide based macrocycles, to the pharmaceutical compositions comprising macrolide based macrocycles, and to the use of macrolide based macrocycles as therapeutic agents.
    Type: Grant
    Filed: May 8, 2017
    Date of Patent: February 16, 2021
    Assignee: FIDELTA D.O.O.
    Inventors: Andrea Fajdetic, Maja Matanovic Skugor, Ivaylo Jivkov Elenkov, Goran Kragol, Mirjana Bukvic, Zorica Marusic Istuk, Sanja Kostrun, Dinko Ziher, Renata Rupcic, Kristina Butkovic, Marko Duksi, Ivana Ozimec Landek, Dijana Pesic, Antun Hutinec, Milan Mesic, Gordon Saxty, Visnja Poljak
  • Patent number: 10858360
    Abstract: Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors. Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.
    Type: Grant
    Filed: July 7, 2017
    Date of Patent: December 8, 2020
    Assignees: MERCK SHARP & DOHME CORP., LAWRENCE LIVERMORE NATIONAL SECURITY, LLC
    Inventors: Daniel Bensen, Zhiyong Chen, John Finn, Thanh T. Lam, Suk J. Lee, Xiaoming Li, Douglas W. Phillipson, Leslie W. Tari, Michael Trzoss, Junhu Zhang, Felice C. Lightstone, Toan B. Nguyen, Sergio E. Wong, Paul Aristoff, Michael Jung
  • Patent number: 10695334
    Abstract: Heteroaromatic carboxamides of formula (I), wherein Y, R, and X are as defined herein, and pharmaceutically acceptable salts thereof. The compounds of formula (I) can be used in methods for the treatment of diseases which can be influenced by inhibition of plasma kallikrein.
    Type: Grant
    Filed: August 14, 2019
    Date of Patent: June 30, 2020
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Eckhardt, Andreas Gollner, Elke Langkopf, Holger Wagner, Dieter Wiedenmayer
  • Patent number: 10626122
    Abstract: Disclosed herein, in part, are heteroaromatic compounds and methods of use in treating neuropsychiatric disorders, e.g., schizophrenia and major depressive disorder. Pharmaceutical compositions and methods of making heteroaromatic compounds are provided. The compounds are contemplated modulate the NMDA receptor.
    Type: Grant
    Filed: December 9, 2016
    Date of Patent: April 21, 2020
    Assignee: Cadent Therapeutics, Inc.
    Inventors: David R. Anderson, Robert A. Volkmann, Frank S. Menniti, Christopher Fanger
  • Patent number: 10618911
    Abstract: A compound of chemical formula I: or formula II: or a pharmaceutical acceptable salt thereof is disclosed. R1 is OH or OAc; X is C or N; and R2 is H, alkyl, alkoxy, benzyloxy, haloalkyl, OH, CN, NO2, or halogen, provided that when X is N, R2 is nil.
    Type: Grant
    Filed: October 23, 2018
    Date of Patent: April 14, 2020
    Assignee: SHAANXI UNIVERSITY OF SCIENCE AND TECHNOLOGY
    Inventors: Han Li, Yuzhi Liu, Nan Qin, Juan Xia, Shaomeng Pei, Chengyuan Liang, Lei Tian
  • Patent number: 10537539
    Abstract: The invention concerns the use of a nicotinic acetylcholine receptor alpha 7 activators for the treatment, prevention or delay of progression of dyskinesia associated with dopamine agonist therapy in Parkinson's Disease.
    Type: Grant
    Filed: September 22, 2010
    Date of Patent: January 21, 2020
    Assignee: NOVARTIS AG
    Inventors: Thérèse Di Paolo, Dominik Feuerbach, Baltazar Gomez-Mancilla, Donald Johns
  • Patent number: 10385055
    Abstract: Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors. Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.
    Type: Grant
    Filed: September 10, 2014
    Date of Patent: August 20, 2019
    Assignees: MERCK SHARP & DOHME CORP., LAWRENCE LIVERMORE NATIONAL SECURITY, LLC
    Inventors: John Finn, Leslie William Tari, Zhiyong Chen, Junhu Zhang, Douglas Phillipson, Suk Joong Lee, Michael Trzoss, Daniel Bensen, Xiaoming Li, Min Teng, Voon Ong, Allen John Borchardt, Thanh To Lam, Felice C. Lightstone, Sergio E. Wong, Toan B. Nguyen
  • Patent number: 10246439
    Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts and esters thereof: which inhibit the Apoptosis signal-regulating kinase 1 (ASK-1), which associated with autoimmune disorders, neurodegenerative disorders, inflammatory diseases, chronic kidney disease, cardiovascular disease. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from ASK-1 related disease. The invention also relates to methods of treating an ASK-1 related disease in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention specifically relates to methods of treating ASK-1 associated with hepatic steatosis, including non-alcoholic fatty liver disease (NAFLD) and non-alcohol steatohepatitis disease (NASH).
    Type: Grant
    Filed: May 24, 2018
    Date of Patent: April 2, 2019
    Assignee: ENANTA PHARMACEUTICALS, INC.
    Inventors: Brett Granger, Guoqiang Wang, Ruichao Shen, Jun Ma, Xuechao Xing, Jing He, Yong He, Jiang Long, Bin Wang, Yat Sun Or
  • Patent number: 10208052
    Abstract: Compositions for the activation of PKR are provided, as well as therapeutic administration of the compositions for the treatment of pyruvate kinase-related medical conditions, such as pyruvate kinase deficiency (PKD).
    Type: Grant
    Filed: March 20, 2018
    Date of Patent: February 19, 2019
    Assignee: FORMA Therapeutics, Inc.
    Inventors: Xiaozhang Zheng, Neal Green, Gary Gustafson, David R. Lancia, Jr., Lorna Mitchell, Tatiana Shelekhin
  • Patent number: 10131644
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, X1, X2, X3, X4, Y, Z, A, R1, R2, R3, R4, R5 R6, R7, R8, R9, R10, R11, R12 and R13 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis, muscular sclerosis and psoriasis.
    Type: Grant
    Filed: June 30, 2016
    Date of Patent: November 20, 2018
    Assignee: Genentech, Inc.
    Inventors: Monique Bodil van Niel, Benjamin Fauber, Emanuela Gancia, Simon Gaines, Alberto Gobbi, Christopher Hurley, Tammy Ladduwahetty, Olivier Rene, David Vesey, Stuart Ward, Paul Winship
  • Patent number: 9981963
    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: September 25, 2014
    Date of Patent: May 29, 2018
    Assignee: Janssen Pharmaceutica NV
    Inventors: George Hynd, Patrizia Tisselli, David Edward Clark, Janusz Jozef Kulagowski, Calum MacLeod, Samuel Edward Mann, Fabien Jean Ghislain Roussel, Stephen Colin Price, John Gary Montana
  • Patent number: 9802944
    Abstract: Compounds of formula (I) wherein R1, R2, A, W, m, n, p and q are as described herein, compositions including the compounds and methods of using the compounds as autotaxin inhibitors.
    Type: Grant
    Filed: September 21, 2016
    Date of Patent: October 31, 2017
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Patrick Di Giorgio, Jerome Hert, Daniel Hunziker, Holger Kuehne, Patrizio Mattei, Markus Rudolph
  • Patent number: 9540396
    Abstract: The invention provides novel substituted 6-arylamino pyridone carboxamides represented by Formula I, or a pharmaceutically acceptable salt, solvate, poly-morph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as inhibitors of MEK and are useful in the treatment of inflammatory diseases, cancer and other hyperproliferative diseases. The invention further provides a method of treatment for inflammatory diseases, cancer and other hyperproliferative diseases in mammals, especially humans.
    Type: Grant
    Filed: November 1, 2011
    Date of Patent: January 10, 2017
    Assignees: Centaurus Biopharma Co., Ltd., Chia Tai Tianqing Pharmaceutical Group Co., Ltd.
    Inventors: Dengming Xiao, Li Zhu, Yuandong Hu, Shixin Wang, Rong Yu, Wei Hu, Zhi Liang, Xijie Liu, Quan Hu
  • Patent number: 9474762
    Abstract: The invention relates to compounds of formula (I) and salts thereof: wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).
    Type: Grant
    Filed: May 19, 2015
    Date of Patent: October 25, 2016
    Assignee: NOVARTIS AG
    Inventors: Chao Chen, Haibing Deng, Haibing Guo, Feng He, Lei Jiang, Fang Liang, Yuan Mi, Huixin Wan, Yao-Chang Xu, Hongping Yu, Ji Yue Zhang
  • Patent number: 9334278
    Abstract: The present invention relates to the use of novel pyrrolo[2,3-b]]pyrazines wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Grant
    Filed: August 19, 2013
    Date of Patent: May 10, 2016
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Johannes Cornelius Hermann, Joshua Kennedy-Smith, Matthew C. Lucas, Fernando Padilla, Ryan Craig Schoenfeld, Peter Michael Wovkulich
  • Patent number: 9168253
    Abstract: Provided are certain quinazoline compounds, compositions thereof and methods of use thereof. These quinazoline compounds can effectively inhibit the overexpression and/or overactivity of epidermal growth factor receptor (EGFR).
    Type: Grant
    Filed: May 25, 2011
    Date of Patent: October 27, 2015
    Assignee: HUTCHISON MEDIPHARMA LIMITED
    Inventors: Weihan Zhang, Wei-Guo Su, Haibin Yang, Yumin Cui, Yongxin Ren, Xiaoqiang Yan
  • Publication number: 20150065465
    Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazotriazines inhibit protein kinase activity thereby making them useful as anticancer agents.
    Type: Application
    Filed: November 4, 2014
    Publication date: March 5, 2015
    Inventors: Ashok Vinayak Purandare, Brian E. Fink, Ashvinikumar V. Gavai, Walter Lewis Johnson, Amy C. Hart, Liqi He, Tram N. Huynh, Jennifer Inghrim, Harold Mastalerz, Xiaopeng Sang, Christine M. Tarby, Honghe Wan, Wayne Vaccaro, Guifen Zhang, Yufen Zhao, Kurt Zimmermann
  • Patent number: 8957060
    Abstract: Disclosed herein are solutions and kits for tumescent antibiotic delivery. Embodiments of the solution comprise an antibiotic component, an anesthetic component and a vasoconstrictor component. In addition, a method of use is disclosed comprising subcutaneous delivery of the solution. The disclosed solution, kit and method of subcutaneous delivery can be used for a variety of surgical procedures including liposuction, mastectomy and others. The tumescent antibiotic solution can be administered to a patient in situations where establishing IV access is difficult, impossible, or undesirable. A variety of delivery methods appropriate for surgical settings, as well as for use by first responders are likewise disclosed.
    Type: Grant
    Filed: May 30, 2012
    Date of Patent: February 17, 2015
    Inventor: Jeffrey Alan Klein
  • Publication number: 20150031652
    Abstract: Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.
    Type: Application
    Filed: August 1, 2014
    Publication date: January 29, 2015
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
  • Publication number: 20140349987
    Abstract: The invention provides modulators for the orphan nuclear receptor ROR? and methods for treating ROR? mediated diseases by administrating these novel ROR? modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo carboxamide compounds of Formula (1) and the enantiomers, diastereomers, N-oxides, tautomers, solvates and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: December 3, 2012
    Publication date: November 27, 2014
    Inventors: Christoph Steeneck, Olaf Kinzel, Christian Gege, Gerald Kleymann, Thomas Hoffmann
  • Publication number: 20140343033
    Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 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 immunological disorders, cardiovascular disease, cancer, and other diseases, disorders or conditions associated with PI3K?.
    Type: Application
    Filed: August 4, 2014
    Publication date: November 20, 2014
    Applicant: Takeda Califomia, Inc.
    Inventors: Edcon Chang, Michael B. Wallace
  • Publication number: 20140343032
    Abstract: The invention provides novel compounds having the general formula: wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as or pharmaceutically acceptable salts, or tautomerism isomers, or enantiomers, or diastereomers thereof. The invention also contains compositions including the compounds and methods of using the compounds.
    Type: Application
    Filed: May 16, 2014
    Publication date: November 20, 2014
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Lei Guo, Taishan Hu, Yimin Hu, Buelent Kocer, Buyu Kou, Gangqin Li, Xianfeng Lin, Haixia Liu, Hong Shen, Houguang Shi, Guolong Wu, Zhisen Zhang, Mingwei Zhou, Wei Zhu
  • Publication number: 20140336166
    Abstract: The invention relates to PI3K inhibitors of the formula (I) • in which all of the variables are as defined in the specification, to their preparation, to their medical use, in particular to their use in the treatment of cancer and neurodegenerative disorders, and to medicaments comprising them.
    Type: Application
    Filed: October 26, 2012
    Publication date: November 13, 2014
    Applicant: NOVARTIS AG
    Inventors: Emmanuelle Briard, Pascal Furet, Andreas Lerchner, Peter Meier, Branko Radetich, David Andrew Sandham, Yanyi Zhu
  • Publication number: 20140323462
    Abstract: Provided are compounds of Formula I, R1-L1-A-L2-R2??(I), and stereoisomers, tautomers and pharmaceutically acceptable salts thereof, wherein A, L1, L2, R1 and R2 are defined herein. The present invention also provides a pharmaceutical composition and methods of using such compounds. The compounds are useful for therapy and/or prophylaxis in a patient, and in particular to inhibitors of Soluble Epoxide Hydrolase (sEH).
    Type: Application
    Filed: July 10, 2014
    Publication date: October 30, 2014
    Inventors: Simona M. Ceccarelli, Carine Guerot, Henner Knust
  • Publication number: 20140315880
    Abstract: The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).
    Type: Application
    Filed: July 1, 2014
    Publication date: October 23, 2014
    Inventors: Srinivasa Rao Akireddy, Balwinder Singh Bhatti, Ronald Joseph Heemstra, Srinivasa V. Murthy, Jon-Paul Strachan, Yunde Xiao
  • Patent number: 8853197
    Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infection is disclosed.
    Type: Grant
    Filed: June 3, 2014
    Date of Patent: October 7, 2014
    Assignee: Wockhardt Ltd.
    Inventors: Mahesh Vithalbhai Patel, Prasad Keshav Deshpande, Satish Bhawasar, Sachin Bhagwat, Mohammad Alam Jafri, Amit Mishra, Laxmikant Pavase, Sunil Gupta, Rajesh Kale, Sanjeev Joshi
  • Publication number: 20140287028
    Abstract: The use of chemotherapeutic agents for the preparation of a medicament for the topical and/or local treatment of diseases caused by bacteria and/or for prophylaxis in humans or animals.
    Type: Application
    Filed: June 3, 2014
    Publication date: September 25, 2014
    Applicant: BAYER INNOVATION GMBH
    Inventors: Hans-Herrmann SCHULZ, Gunther SCHLIMBACH
  • Publication number: 20140288042
    Abstract: This invention relates to compounds of Formula I having the following general structure: Z1—Y1—(CH2)n1—R—(CH2)n2—Y2—Z2 wherein R represents a fused bicyclic or spirocyclic aliphatic diamine and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
    Type: Application
    Filed: October 25, 2012
    Publication date: September 25, 2014
    Inventors: Shawn P. Walsh, Alexander Pasternak, Zhi-Cai Shi, Brian Cato, Esther Y. Kim
  • Publication number: 20140249129
    Abstract: This invention relates to substituted bicyclic dihydropyrimidinones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other autoimmune and allergic disorders, allograft rejection, and oncological diseases.
    Type: Application
    Filed: February 20, 2014
    Publication date: September 4, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Christian GNAMM, Thorsten OOST, Stefan PETERS, Klaus RUDOLF
  • Patent number: 8822450
    Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infection is disclosed.
    Type: Grant
    Filed: August 24, 2012
    Date of Patent: September 2, 2014
    Assignee: Wockhardt Ltd.
    Inventors: Mahesh Vithalbhai Patel, Prasad Keshav Deshpande, Satish Bhawsar, Sachin Bhagwat, Mohammed Alam Jafri, Amit Mishra, Laxmikant Pavase, Sunil Gupta, Rajesh Kale, Sanjeev Joshi
  • Patent number: 8822495
    Abstract: The invention relates to azacyclyl-substituted aryldihydroisoquinolinones and their derivatives, and their physiologically tolerated salts and physiologically functional derivatives, their preparation, medicaments comprising at least one azacyclyl-substituted aryldihydroisoquinolinone of the invention or its derivative, and the use of the azacyclyl-substituted aryldihydroisoquinolinones of the invention and their derivatives as MCH antagonists.
    Type: Grant
    Filed: August 14, 2008
    Date of Patent: September 2, 2014
    Assignee: Sanofi
    Inventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Gerhard Hessler, Torsten Haack, Petra Lennig
  • Patent number: 8809552
    Abstract: Provided are compounds of Formula I, R1-L1-A-L2-R2??(I), and stereoisomers, tautomers and pharmaceutically acceptable salts thereof, wherein A, L1, L2, R1 and R2 are defined herein. The present invention also provides a pharmaceutical composition and methods of using such compounds. The compounds are useful for therapy and/or prophylaxis in a patient, and in particular to inhibitors of Soluble Epoxide Hydrolase (sEH).
    Type: Grant
    Filed: October 26, 2012
    Date of Patent: August 19, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Simona M. Ceccarelli, Carine Guerot, Henner Knust
  • Publication number: 20140206661
    Abstract: The present invention provides a compound of Formula (X) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: January 21, 2014
    Publication date: July 24, 2014
    Applicant: NOVARTIS AG
    Inventors: Jake AXFORD, Natalie DALES, Moo Je SUNG
  • Patent number: 8772276
    Abstract: The present invention is directed to alkyne benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
    Type: Grant
    Filed: April 30, 2012
    Date of Patent: July 8, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Jason W. Skudlarek
  • Patent number: 8742110
    Abstract: Substituted spirocyclic amines of structural formula (I) are selective antagonists of the somatostatin subtype receptor 5 (SSTR5) and are useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as Type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, Metabolic Syndrome, depression, and anxiety.
    Type: Grant
    Filed: August 12, 2011
    Date of Patent: June 3, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joseph L. Duffy, Jianming Bao, Debra L. Ondeyka, Sriram Tyagarajan, Patrick Shao, Feng Ye, Revathi Katipally, Aaron Zwicker, Edward C. Sherer, Michael A. Plotkin, Remond Moningka, Zahid Hussain, Harold B. Wood, Feroze Ujjainwalla, F. Anthony Romero, Paul E. Finke, Yi Zang, Weiguo Liu