Polycyclo Ring System Having The Four-membered Hetero Ring As One Of The Cyclos Patents (Class 514/210.16)
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Patent number: 11407753Abstract: 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: GrantFiled: June 5, 2018Date of Patent: August 9, 2022Assignee: 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
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Patent number: 11326165Abstract: 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: GrantFiled: October 15, 2021Date of Patent: May 10, 2022Assignee: SKYHAWK THERAPEUTICS, INC.Inventors: Michael Luzzio, Kathleen McCarthy, William Haney
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Patent number: 11319324Abstract: 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: GrantFiled: October 18, 2018Date of Patent: May 3, 2022Assignees: Bayer Aktiengesellschaft, Bayer Pharma AktiengesellschaftInventors: 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
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Patent number: 11286252Abstract: 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: GrantFiled: October 31, 2018Date of Patent: March 29, 2022Assignee: Bristol-Myers Squibb CompanyInventors: Jianxin Feng, Chunjian Liu, Yanting Huang
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Patent number: 11192899Abstract: 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: GrantFiled: August 20, 2018Date of Patent: December 7, 2021Assignee: MERCK PATENT GMBHInventors: Eva-Maria Tanzer, Kai Schiemann, Markus Klein
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Patent number: 11186592Abstract: 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: GrantFiled: July 2, 2018Date of Patent: November 30, 2021Assignee: Merck Patent GmbHInventors: Eva-Maria Tanzer, Kai Schiemann, Markus Klein
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Patent number: 11161856Abstract: 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: GrantFiled: August 28, 2018Date of Patent: November 2, 2021Assignee: H. LUNDBECK A/SInventors: Cheryl A. Grice, Olivia D. Weber, Daniel J. Buzard, Michael B. Shaghafi
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Patent number: 11162101Abstract: 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: GrantFiled: February 4, 2020Date of Patent: November 2, 2021Assignee: SKYHAWK THERAPEUTICS, INC.Inventors: Michael Luzzio, Kathleen McCarthy, William Haney
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Patent number: 11130751Abstract: 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: GrantFiled: March 29, 2018Date of Patent: September 28, 2021Assignee: Janssen Pharmaceutica NVInventors: Patrick René Angibaud, Olivier Alexis Georges Querolle, Didier Jean-Claude Berthelot, Christophe Meyer, Matthieu Philippe Victor Willot, Lieven Meerpoel, Thierry François Alain Jean Jousseaume
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Patent number: 11111237Abstract: 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: GrantFiled: November 24, 2020Date of Patent: September 7, 2021Assignee: 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
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Patent number: 11078197Abstract: 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: GrantFiled: July 11, 2018Date of Patent: August 3, 2021Assignee: Bristol-Myers Squibb CompanyInventors: Peter W. Glunz, Vladimir Ladziata, Indawati De Lucca, George O. Tora, Tarun Kumar Maishal, Raghuram Tangirala, Kamalraj Thiyagarajan
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Patent number: 11078189Abstract: 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: GrantFiled: July 20, 2018Date of Patent: August 3, 2021Assignee: REVIRAL LIMITEDInventors: Stuart George Cockerill, James Good
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Patent number: 11059780Abstract: 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: GrantFiled: March 7, 2018Date of Patent: July 13, 2021Assignee: Takeda Pharmaceutical Company LimitedInventors: Masaki Daini, Yuhei Miyanohana, Satoshi Mikami, Yuichi Kajita, Masaki Ogino, Tatsuki Koike, Kohei Takeuchi
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Patent number: 11045479Abstract: 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: GrantFiled: July 18, 2018Date of Patent: June 29, 2021Assignee: VYOME THERAPEUTICS LIMITEDInventors: Shiladitya Sengupta, Suresh Rameshlal Chawrai, Shamik Ghosh, Sumana Ghosh, Nilu Jain, Suresh Sadhasivam, Richard Buchta, Anamika Bhattacharyya
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Patent number: 11021482Abstract: 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: GrantFiled: August 12, 2019Date of Patent: June 1, 2021Assignee: Adaris Therapeutics, Inc.Inventors: Eric Jon Jacobsen, David Randolph Anderson, James Robert Blinn, Susan Landis Hockerman, Richard Heier, Paramita Mukherjee
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Patent number: 10919910Abstract: 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: GrantFiled: May 8, 2017Date of Patent: February 16, 2021Assignee: 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
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Patent number: 10858360Abstract: 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: GrantFiled: July 7, 2017Date of Patent: December 8, 2020Assignees: MERCK SHARP & DOHME CORP., LAWRENCE LIVERMORE NATIONAL SECURITY, LLCInventors: 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
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Patent number: 10695334Abstract: 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: GrantFiled: August 14, 2019Date of Patent: June 30, 2020Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Eckhardt, Andreas Gollner, Elke Langkopf, Holger Wagner, Dieter Wiedenmayer
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Patent number: 10626122Abstract: 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: GrantFiled: December 9, 2016Date of Patent: April 21, 2020Assignee: Cadent Therapeutics, Inc.Inventors: David R. Anderson, Robert A. Volkmann, Frank S. Menniti, Christopher Fanger
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Patent number: 10618911Abstract: 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: GrantFiled: October 23, 2018Date of Patent: April 14, 2020Assignee: SHAANXI UNIVERSITY OF SCIENCE AND TECHNOLOGYInventors: Han Li, Yuzhi Liu, Nan Qin, Juan Xia, Shaomeng Pei, Chengyuan Liang, Lei Tian
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Patent number: 10537539Abstract: 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: GrantFiled: September 22, 2010Date of Patent: January 21, 2020Assignee: NOVARTIS AGInventors: Thérèse Di Paolo, Dominik Feuerbach, Baltazar Gomez-Mancilla, Donald Johns
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Patent number: 10385055Abstract: 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: GrantFiled: September 10, 2014Date of Patent: August 20, 2019Assignees: MERCK SHARP & DOHME CORP., LAWRENCE LIVERMORE NATIONAL SECURITY, LLCInventors: 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
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Patent number: 10246439Abstract: 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: GrantFiled: May 24, 2018Date of Patent: April 2, 2019Assignee: 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
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Patent number: 10208052Abstract: 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: GrantFiled: March 20, 2018Date of Patent: February 19, 2019Assignee: FORMA Therapeutics, Inc.Inventors: Xiaozhang Zheng, Neal Green, Gary Gustafson, David R. Lancia, Jr., Lorna Mitchell, Tatiana Shelekhin
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Patent number: 10131644Abstract: 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: GrantFiled: June 30, 2016Date of Patent: November 20, 2018Assignee: 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
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Patent number: 9981963Abstract: 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: GrantFiled: September 25, 2014Date of Patent: May 29, 2018Assignee: Janssen Pharmaceutica NVInventors: 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
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Patent number: 9802944Abstract: 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: GrantFiled: September 21, 2016Date of Patent: October 31, 2017Assignee: Hoffmann-La Roche Inc.Inventors: Patrick Di Giorgio, Jerome Hert, Daniel Hunziker, Holger Kuehne, Patrizio Mattei, Markus Rudolph
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Patent number: 9540396Abstract: 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: GrantFiled: November 1, 2011Date of Patent: January 10, 2017Assignees: 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
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Patent number: 9474762Abstract: 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: GrantFiled: May 19, 2015Date of Patent: October 25, 2016Assignee: NOVARTIS AGInventors: Chao Chen, Haibing Deng, Haibing Guo, Feng He, Lei Jiang, Fang Liang, Yuan Mi, Huixin Wan, Yao-Chang Xu, Hongping Yu, Ji Yue Zhang
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Patent number: 9334278Abstract: 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: GrantFiled: August 19, 2013Date of Patent: May 10, 2016Assignee: Hoffmann-La Roche Inc.Inventors: Johannes Cornelius Hermann, Joshua Kennedy-Smith, Matthew C. Lucas, Fernando Padilla, Ryan Craig Schoenfeld, Peter Michael Wovkulich
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Patent number: 9168253Abstract: 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: GrantFiled: May 25, 2011Date of Patent: October 27, 2015Assignee: HUTCHISON MEDIPHARMA LIMITEDInventors: Weihan Zhang, Wei-Guo Su, Haibin Yang, Yumin Cui, Yongxin Ren, Xiaoqiang Yan
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Publication number: 20150065465Abstract: 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: ApplicationFiled: November 4, 2014Publication date: March 5, 2015Inventors: 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
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Patent number: 8957060Abstract: 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: GrantFiled: May 30, 2012Date of Patent: February 17, 2015Inventor: Jeffrey Alan Klein
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Publication number: 20150031652Abstract: 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: ApplicationFiled: August 1, 2014Publication date: January 29, 2015Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
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Publication number: 20140349987Abstract: 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: ApplicationFiled: December 3, 2012Publication date: November 27, 2014Inventors: Christoph Steeneck, Olaf Kinzel, Christian Gege, Gerald Kleymann, Thomas Hoffmann
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Publication number: 20140343033Abstract: 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: ApplicationFiled: August 4, 2014Publication date: November 20, 2014Applicant: Takeda Califomia, Inc.Inventors: Edcon Chang, Michael B. Wallace
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Publication number: 20140343032Abstract: 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: ApplicationFiled: May 16, 2014Publication date: November 20, 2014Applicant: 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
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Publication number: 20140336166Abstract: 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: ApplicationFiled: October 26, 2012Publication date: November 13, 2014Applicant: NOVARTIS AGInventors: Emmanuelle Briard, Pascal Furet, Andreas Lerchner, Peter Meier, Branko Radetich, David Andrew Sandham, Yanyi Zhu
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Publication number: 20140323462Abstract: 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: ApplicationFiled: July 10, 2014Publication date: October 30, 2014Inventors: Simona M. Ceccarelli, Carine Guerot, Henner Knust
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Publication number: 20140315880Abstract: 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: ApplicationFiled: July 1, 2014Publication date: October 23, 2014Inventors: Srinivasa Rao Akireddy, Balwinder Singh Bhatti, Ronald Joseph Heemstra, Srinivasa V. Murthy, Jon-Paul Strachan, Yunde Xiao
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Patent number: 8853197Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infection is disclosed.Type: GrantFiled: June 3, 2014Date of Patent: October 7, 2014Assignee: 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
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Publication number: 20140287028Abstract: 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: ApplicationFiled: June 3, 2014Publication date: September 25, 2014Applicant: BAYER INNOVATION GMBHInventors: Hans-Herrmann SCHULZ, Gunther SCHLIMBACH
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Publication number: 20140288042Abstract: 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: ApplicationFiled: October 25, 2012Publication date: September 25, 2014Inventors: Shawn P. Walsh, Alexander Pasternak, Zhi-Cai Shi, Brian Cato, Esther Y. Kim
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Publication number: 20140249129Abstract: 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: ApplicationFiled: February 20, 2014Publication date: September 4, 2014Applicant: Boehringer Ingelheim International GmbHInventors: Christian GNAMM, Thorsten OOST, Stefan PETERS, Klaus RUDOLF
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Patent number: 8822450Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infection is disclosed.Type: GrantFiled: August 24, 2012Date of Patent: September 2, 2014Assignee: 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
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Patent number: 8822495Abstract: 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: GrantFiled: August 14, 2008Date of Patent: September 2, 2014Assignee: SanofiInventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Gerhard Hessler, Torsten Haack, Petra Lennig
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Patent number: 8809552Abstract: 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: GrantFiled: October 26, 2012Date of Patent: August 19, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Simona M. Ceccarelli, Carine Guerot, Henner Knust
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Publication number: 20140206661Abstract: 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: ApplicationFiled: January 21, 2014Publication date: July 24, 2014Applicant: NOVARTIS AGInventors: Jake AXFORD, Natalie DALES, Moo Je SUNG
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Patent number: 8772276Abstract: 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: GrantFiled: April 30, 2012Date of Patent: July 8, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Scott D. Kuduk, Jason W. Skudlarek
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Patent number: 8742110Abstract: 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: GrantFiled: August 12, 2011Date of Patent: June 3, 2014Assignee: 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