Nitrogen Attached Indirectly To The Diazole Ring By Acyclic Nonionic Bonding Patents (Class 548/309.7)
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Patent number: 11633415Abstract: The present invention includes CSNK1A1 inhibitors that are useful in treating or preventing a cancer in a subject. In certain embodiments, the cancer comprises a hematological cancer, such as but not limited to acute myeloid leukemia (AML) and/or MDS (myelodysplastic syndrome, including 5q-MDS). In other embodiments, the cancer comprises colon cancer.Type: GrantFiled: March 30, 2018Date of Patent: April 25, 2023Assignees: THE BROAD INSTITUTE, INC., DANA-FARBER CANCER INSTITUTE, INC.Inventors: Steven M. Corsello, Todd R. Golub, Eric Stefan, Robert Hilgraf
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Patent number: 11318117Abstract: T-PLL Therapy There is provided tinostamustine or a pharmaceutically acceptable salt thereof for use in the treatment of T-cell prolymphocytic leukemia (T-PLL) in a patient in need thereof.Type: GrantFiled: June 13, 2018Date of Patent: May 3, 2022Assignee: Purdue Pharma L.P.Inventors: Thomas Jorg Mehrling, Marco Herling
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Patent number: 10512634Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the compound. The compound is useful in therapy, for the treatment of disorders mediated by HDAC6, such as autoimmune disorders, neurodegenerative disorders and hyperproliferative disorders, such as cancer.Type: GrantFiled: May 11, 2015Date of Patent: December 24, 2019Assignee: KANCERA ABInventors: Johan Schultz, Jan Vågberg, Elisabeth Olsson, Katarina Färnegårdh, Mattias Jönsson, Kristin Hammer, Lars Krüger
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Patent number: 10369120Abstract: The present invention provides novel T type calcium channel inhibitors of formula (I), the use thereof in the treatment of a disease or condition in a mammal associated with influx of extracellular calcium via T type calcium channels, wherein R1 is C1-C4 alkyl, hydroxy, or C1-C4 alkoxy; Z is NH, NCH3, O, S, or CH2; Y is NH, O, or CH2 with the proviso that Y and Z are not the same; R2 is H, halo, NH2, C1-C4 alkyl, hydroxy, or C1-C4 alkoxy; m and n are independently selected from integers ranging from 1-5 with the proviso that m+n=an integer ranging from 2-9; and R3 is H, halo, NH2, C1-C4 alkyl, hydroxy, or C1-C4 alkoxy.Type: GrantFiled: November 5, 2015Date of Patent: August 6, 2019Assignee: University of Virginia Patent FoundationInventors: Lloyd S. Gray, Timothy L. Macdonald, Doris M. Haverstick, Jaclyn R. Patterson, William F. McCalmont
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Patent number: 10179771Abstract: The present invention discloses compounds according to Formula I: wherein Cy, R1, L1, R3, R4, R5, La, and Ra are as defined herein. Novel benzimidazoles according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic diseases, inflammatory diseases, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or hypersecretion of interferons.Type: GrantFiled: September 12, 2016Date of Patent: January 15, 2019Assignee: GALAPAGOS NVInventors: Christel Jeanne Marie Menet, Oscar Mammoliti, Javier Blanc, Mislav Orsulic, Maja Roscic
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Patent number: 9630926Abstract: The present invention is directed to bendamustine esters and bendamustine amides and their use for the treatment of cancer.Type: GrantFiled: June 16, 2016Date of Patent: April 25, 2017Assignee: IGNYTA, INC.Inventors: Roger P. Bakale, Peter D. Brown, Jian Chen, Anthony S. Drager, Rachel Y. LaBell, Robert E. McKean, Piyush R. Patel, Renee C. Roemmele
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Patent number: 9315469Abstract: Wet bendamustine hydrochloride monohydrate may be dried by a two stage process wherein rapid drying is first carried out to provide a partially dried product, which is then further dried using an inert gas of controlled relative humidity to yield dry bendamustine hydrochloride monohydrate.Type: GrantFiled: March 12, 2014Date of Patent: April 19, 2016Assignee: Johnson Matthey Public Limited CompanyInventors: Xing Fu, Jeremy Clinton Wilt
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Patent number: 9309233Abstract: The invention relates to the compounds of formula I and formula II or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I or formula II; and methods for treating or preventing blood clotting disorders may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of strokes in those with atrial fibrillation due to causes other than heart valve disease, and at least one additional risk factor for stroke (congestive heart failure, hypertension, age, diabetes, and prior stroke), and to prevent the formation of blood clots in the veins in adults operated to replace a hip or knee.Type: GrantFiled: March 24, 2013Date of Patent: April 12, 2016Assignee: CELLIX BIO PRIVATE LIMITEDInventor: Mahesh Kandula
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Patent number: 9273009Abstract: This invention relates to novel tetrahydronaphthalene derivatives, and pharmaceutically acceptable salts thereof according to the following formulae, in one embodiment: as described herein. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a selective T-type calcium channel blocker.Type: GrantFiled: October 21, 2013Date of Patent: March 1, 2016Assignee: Concert Pharmaceuticals, Inc.Inventors: Roger Tung, Craig E. Masse, Julie F. Liu
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Patent number: 9096627Abstract: The present invention is directed to a method of alleviating, relieving, altering, remedying, ameliorating, improving or affecting a neoplastic disease or an immune disease, the method comprising administering to a subject in need thereof an effective amount of a compound of Formula I, or a pharmaceutically acceptable salt thereof: wherein P, Z, and m are defined herein above.Type: GrantFiled: November 8, 2013Date of Patent: August 4, 2015Assignee: Purdue Pharmaceutical Products L.P.Inventors: Yu Chen, Yi Chen
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Patent number: 9079860Abstract: The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, R4, R6, R11, X1, X2, and X3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.Type: GrantFiled: March 19, 2014Date of Patent: July 14, 2015Assignee: Bristol-Myers Squibb CompanyInventors: Jon J. Hangeland, Mimi L. Quan, Joanne M. Smallheer, Gregory S. Bisacchi, James R. Corte, Todd J. Friends, Zhong Sun, Karen A. Rossi, Cullen L. Cavallaro
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Publication number: 20150133500Abstract: The invention provides compounds that are useful as sodium channel blockers. In one aspect, the invention provides compounds of Formula I: and pharmaceutically acceptable salts, solvates, hydrates, or diastereomers thereof, wherein W1, W2, W3, W4, U, G, m, R1, and R2 are defined in the disclosure. In certain embodiments, the invention provides compounds of Formulae II to V as set forth supra. The invention also provides the use of compounds of any of the above discussed formulae to treat a disorder responsive to blockade of sodium channels. In one embodiment, Compounds of the Invention are useful for treating pain.Type: ApplicationFiled: November 6, 2014Publication date: May 14, 2015Inventors: Laykea Tafesse, Jiangchao Yao, Xiaoming Zhou
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Patent number: 9024029Abstract: The present invention relates to hydroxamate compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to benzimidazole containing compounds and methods for their preparation. These compounds may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with dysregulation of histone deacetylase (HDAC).Type: GrantFiled: September 3, 2013Date of Patent: May 5, 2015Assignee: MEI Pharma, Inc.Inventors: DiZhong Chen, Hong Yan Song, Eric T. Sun, Niefang Yu, Yong Zou
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Publication number: 20150086551Abstract: The present invention relates to a class of hydroxamic acid compounds of Formula (I), which act as alkylating agents and/or inhibitors of the HDAC pathway, having potential utility in the treatment of a neoplastic disease and immune diseases.Type: ApplicationFiled: January 31, 2013Publication date: March 26, 2015Inventors: Yu Chen, Yi Chen
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Patent number: 8987468Abstract: The invention encompasses a compound derived from hydroxamic acid that may be used to slow the expansion of cancer cells and thus is effective in the treatment of cancer. Generally, the disclosed compound includes a benzimidazole group coupled to a hydroxyamide of five or more unsubstituted carbon atoms and any pharmaceutically acceptable salts, solvates and chemically protected forms thereof. Also disclosed are pharmacological compositions including the compound and methods of using the compound to slow the expansion of cancer cells as well as methods of using the compound to treat cancer.Type: GrantFiled: February 3, 2009Date of Patent: March 24, 2015Assignee: The Translational Genomics Research InstituteInventors: Tong Wang, Stephen Gately
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Publication number: 20150045551Abstract: The present invention provides agents for treating or preventing diseases such as mood disorder, anxiety disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal disease, drug addiction, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immune-related disease, alopecia.Type: ApplicationFiled: March 29, 2013Publication date: February 12, 2015Applicant: TAISHO PHARMACEUTICAL CO., LTDInventors: Mitsukane Yoshinaga, Tomoko Ishizaka, Daisuke Wakasugi, Shin-ichi Shirokawa, Nobutaka Hattori, Shuhei Kashiwa, Takeshi Kuwada, Youichi Shimazaki
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Publication number: 20150011591Abstract: The present invention is directed to a compound of Formula I or a pharmaceutically acceptable salt thereof; wherein R, R1, R2, R3, R4, m, and n are as defined herein, to pharmaceutical compositions comprising said compound, and to methods of treating diseases or conditions mediated by elevated persistent sodium current, such as an ocular disorder, multiple sclerosis, seizure disorder, and chronic pain.Type: ApplicationFiled: September 24, 2014Publication date: January 8, 2015Inventors: George R. Ehring, Ellen Chao, Herman Ng, Hau Ton, Jia Chian Li, Joseph S. Adorante, Michael E. Garst, Howard B. Rind, Mark R. Hansen, Alfred Arthur Avey, JR., Lloyd Jay Dolby, Shervin Esfandiari, Vivian R. MacKenzie, Jeremiah Andrew Marsden, David Charles Muchmore
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Patent number: 8927587Abstract: The invention relates to benzimidazole and imidazopyridine derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new Nav1.8 modulators of formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7. X and Y are as defined in the description. Nav1.8 modulators are potentially useful in the treatment of a wide range of disorders, particularly pain.Type: GrantFiled: January 29, 2013Date of Patent: January 6, 2015Assignee: Pfizer LImitedInventors: Sharanjeet Kaur Bagal, Alan Daniel Brown, Mark Ian Kemp, Wolfgang Klute, Laia Malet Sanz, Brian Edward Marron, Duncan Charles Miller, Sarah Elizabeth Skerratt, Mark J. Suto, Christopher William West
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Publication number: 20140378453Abstract: The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.Type: ApplicationFiled: June 27, 2014Publication date: December 25, 2014Inventors: Aleksandr KOLESNIKOV, Roopa RAI, William Dvorak SHRADER, Steven M. TORKELSON, Kieron E. WESSON, Wendy B. YOUNG
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Publication number: 20140371316Abstract: The present invention provides a process for the synthesis of substituted phenoxymethylpropiomc acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).Type: ApplicationFiled: November 23, 2012Publication date: December 18, 2014Inventors: Jill S. FABRICANT, Iraj LALEZARI
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Publication number: 20140315945Abstract: The present invention relates to azole compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.Type: ApplicationFiled: March 14, 2014Publication date: October 23, 2014Applicant: EPIZYME, INC.Inventors: John Emmerson Campbell, Kevin Wayne Kuntz
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Patent number: 8859780Abstract: The present invention is directed to a compound of Formula I or a pharmaceutically acceptable salt thereof; wherein R, R1, R2, R3, R4, m, and n are as defined herein, to pharmaceutical compositions comprising said compound, and to methods of treating diseases or conditions mediated by elevated persistent sodium current, such as an ocular disorder, multiple sclerosis, seizure disorder, and chronic pain.Type: GrantFiled: December 27, 2012Date of Patent: October 14, 2014Assignee: Allergan, Inc.Inventors: George R. Ehring, Ellen Chao, Herman Ng, Hau Ton, Jia Chian Li, Joseph S. Adorante, Michael S. Garst, Howard B. Rind, Mark R. Hansen, Alfred Arthur Avey, Jr., Lloyd Jay Dolby, Shervin Esfandiari, Vivian R. MacKenzie, Jeremiah Andrew Marsden, David Charles Muchmore
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Publication number: 20140288302Abstract: A pharmaceutical composition including a compound of formula (I): its pharmaceutically acceptable salt, or a solvate thereof. Ring A is nitrogen-containing hetero ring, Ring A may be substituted with a substituent other than a group represented by formula: —C(R1R2)—C(?O)—NR3R4 and a group represented by formula: —R5, a broken line represents presence or absence of a bond, Z is —NR6—, ?N—, —O—, or —S—, R6 is halogen or substituted or unsubstituted alkyl, R1 and R2 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy or substituted or unsubstituted alkyl, R3 is hydrogen or substituted or unsubstituted alkyl, R4 is hydrogen or substituted or unsubstituted alkyl, R3 and R4 taken together with the adjacent nitrogen atom to which they are attached may form a substituted or unsubstituted ring, R5 is hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl.Type: ApplicationFiled: March 18, 2014Publication date: September 25, 2014Applicant: Shionogi & Co., Ltd.Inventors: Koji MASUDA, Shiro KIDA, Kyohei HAYASHI, Manabu KATOU, Naoki YOSHIKAWA, Akira KUGIMIYA, Mado NAKAJIMA, Nobuyuki TANAKA
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Publication number: 20140249148Abstract: Provided herein are inhibitors of HDAC3, as well as methods of treatment comprising administering those compounds to a subject in need thereof.Type: ApplicationFiled: January 31, 2014Publication date: September 4, 2014Inventors: John H. van Duzer, Ralph Mazitschek
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Patent number: 8809549Abstract: The present invention relates to particular esters of bendamustine and related compounds, and medical uses thereof.Type: GrantFiled: April 25, 2013Date of Patent: August 19, 2014Inventors: Helmut Schickaneder, Armin Buschauer, Guenther Bernhardt, Christian Schickaneder, Michael Limmert, Stefan Huber
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Publication number: 20140228380Abstract: The present invention provides a method of inhibiting, suppressing or preventing levodopa-induced dyskinesia in a patient suffering from Parkinson's Disease, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention. The present invention further provides a method of inhibiting, suppressing or preventing Parkinson's Disease in a patient, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention.Type: ApplicationFiled: August 2, 2013Publication date: August 14, 2014Applicants: University of Medicine and Dentistry New Jersey Medical School, Philadelphia Health & Education Corporation d/b/a Drexel University College of MedicineInventors: Sandhya Kortagere, Eldo V. Kuzhikandahil
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Publication number: 20140221667Abstract: The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.Type: ApplicationFiled: April 11, 2014Publication date: August 7, 2014Applicant: Pharmacyclics, Inc.Inventors: Daniel A. DICKMAN, Dange Vijay KUMAR, Colin O'BRYAN, Roopa RAI, William Dvorak SHRADER
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Publication number: 20140187533Abstract: The invention relates to compounds useful in treating conditions associated with voltage-gated ion channel function, particularly conditions associated with sodium channel activity. More specifically, the invention concerns compounds (e.g., compounds according to any of Formulas (I)-(XIII) or Compounds (1)-(236) of Table 1) that are useful in treatment of a variety of diseases and conditions.Type: ApplicationFiled: March 2, 2012Publication date: July 3, 2014Applicant: Zalicus Pharmaceuticals Ltd.Inventors: Hassan Pajouhesh, Richard Holland, Lingyun Zhang, Hossein Pajouhesh, Jason Lamontagne, Brendan Whelan
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Publication number: 20140179750Abstract: The disclosure relates to Prostaglandin receptor EP2 antagonists, derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to methods of treating or preventing conditions and diseases in which EP2 receptor activation has a physiological role, such as but not limited to, brain injury, inflammatory diseases, neuroinflammation after a seizure, pain, endometriosis, cancer, rheumatoid arthritis, skin inflammation, vascular inflammation, colitis, and neurological disorders by administering a pharmaceutical composition comprising a compound disclosed herein to a subject in need thereof.Type: ApplicationFiled: June 19, 2012Publication date: June 26, 2014Applicant: EMORY UNIVERSITYInventors: Jianxiong Jiang, Thota Ganesh, Yuhong Du, Pahk Thepchatri, Yi Quan, Ray J. Dingledine
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Patent number: 8748411Abstract: Chemical compounds derived by in silico molecular modelling, having a well defined structure suitable for the blocking of the phosphorylation event, through the specific interaction of the chemical with the Casein Kinase 2 enzyme substrate phosphorylation domain or it's neighbourhood. This invention comprises also the pharmaceutical compositions containing such compounds, and their use in the preparation of medicines or agents for the treatment of diseases or conditions related with neoplasic processes.Type: GrantFiled: May 5, 2006Date of Patent: June 10, 2014Assignee: Centro de Ingenieria Genetica y BiotechnologiaInventors: Rolando Eduardo Rodriguez Fernandez, Roberto Vera Alvarez, Ania De La Nuez Veulens, Yuliet Mazola Reyes, Silvio Ernesto Perea Rodriguez, Boris Ernesto Acevedo Castro, Alexis Musacchio Lasa, Raimundo Ubieta Gómez
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Publication number: 20140155444Abstract: This invention relates to novel tetrahydronaphthalene derivatives, and pharmaceutically acceptable salts thereof according to the following formulae, in one embodiment: as described herein. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a selective T-type calcium channel blocker.Type: ApplicationFiled: October 21, 2013Publication date: June 5, 2014Applicant: Concert Pharmaceuticals Inc.Inventors: Roger Tung, Craig E. Masse, Bhaumik A. Pandya
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Publication number: 20140142321Abstract: This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3? OH kinase family (hereinafter PI3 kinases), suitably, PI3K?, PI3K?, PI3K?, and/or PI3K?. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3K? selective benzimidazoles compounds for treating cancer.Type: ApplicationFiled: January 27, 2014Publication date: May 22, 2014Applicant: GlaxoSmithKline LLCInventors: Junya Qu, Ralph A. Rivero, Robert Sanchez, Rosanna Tedesco
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Patent number: 8729117Abstract: The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.Type: GrantFiled: September 20, 2012Date of Patent: May 20, 2014Assignee: Pharmacyclics, Inc.Inventors: Daniel A. Dickman, Dange Vijay Kumar, Colin O'Bryan, Roopa Rai, William Dvorak Shrader
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Patent number: 8716491Abstract: The present invention is directed toward benzimidazolium dye compounds of formula (I) as follows: wherein, n is an integer from 2-10, m is an integer from 2-10, X1 and X2 are independently a halogen, Q is H or a resin, and R is (aromatic)o-(linker)p-with the linker being saturated or unsaturated C1-C5 hydrocarbons, each aromatic independently being a substituted or unsubstituted aromatic or heteroaromatic, o being 1 or 2, and p being 0 or 1. Methods of making and using these compounds are also disclosed.Type: GrantFiled: July 18, 2007Date of Patent: May 6, 2014Assignee: New York UniversityInventors: Young-Tae Chang, Shenliang Wang
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Publication number: 20140114067Abstract: Provided are a benzimidazole derivative modulating mitochondrial functions and having pharmaceutical activity as a neuro-protective agent, and a pharmaceutical composition including the compound as an active ingredient.Type: ApplicationFiled: October 8, 2013Publication date: April 24, 2014Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGYInventors: Ae Nim PAE, Sun Joon MIN, Eun Joo ROH, Ha Yun YANG, Tae Hoon KIM, Beoung Gun PARK, Yong Seo CHO
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Publication number: 20140076036Abstract: The present invention relates to dabigatran etexilate and related substances and use of the substances as reference standards and markers. There are also provided processes of detecting the substances in samples of dabigatran etexilate, or pharmaceutically acceptable salts or solvates thereof, and also for analyzing the purity of samples of dabigatran etexilate, or pharmaceutically acceptable salts or solvates thereof. There are still further provided processes of preparing dabigatran etexilate and related substances, and pharmaceutical compositions containing the same.Type: ApplicationFiled: May 10, 2012Publication date: March 20, 2014Applicant: Medichem S.A.Inventors: Judit Serra Miralles, Ernesto Durán López, Lingxiang Rao
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Patent number: 8633235Abstract: Compounds of Formula (I) or pharmaceutically acceptable salts thereof; wherein R1, R2, R3, and R4 are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.Type: GrantFiled: September 24, 2004Date of Patent: January 21, 2014Assignee: Neomed InstituteInventors: Ziping Liu, Daniel Pagé, Christopher Walpole, Hua Yang
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Publication number: 20140004243Abstract: The present invention provides a compound having a salty taste enhance activity, and a salty taste enhancer containing the compound, and the like. The present invention relates to a salty taste enhancer for a food or drink, which contains a compound represented by the following formula: wherein each symbol is as defined in the specification, or an edible salt thereof.Type: ApplicationFiled: September 6, 2013Publication date: January 2, 2014Applicant: AJINOMOTO CO., INC.Inventors: Yuki TAHARA, Yusuke Amino, Takami Maekawa, Yuzuru Eto, Takashi Miyaki, Wakana Saikawa, Yuko Kai, Yutaka Ishiwatari
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Patent number: 8609864Abstract: The disclosure includes hydroxamic compounds of Formula I: (I) wherein P, Z, and m are defined herein. Also disclosed is a method for treating a neoplastic disease or an immune disease with these compounds.Type: GrantFiled: January 7, 2010Date of Patent: December 17, 2013Assignee: Purdue Pharmaceutical Products, L.P.Inventors: Yu Chen, Yi Chen
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Publication number: 20130296346Abstract: The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, prodrug or solvate thereof, a method of synthesis of said compounds, pharmaceutical compositions comprising them and their use as a medicament for treating inflammatory diseases.Type: ApplicationFiled: November 22, 2011Publication date: November 7, 2013Applicant: Faes Farma, S.A.Inventors: Rosa Rodes Solanes, Neftali Garcia Dominguez, Beatriz Lopez Ortega, Melchor Alvarez De Mon Soto, Antonio De La Hera Martinez, Ana Munoz Munoz, Francisco Ledo Gomez
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Patent number: 8575361Abstract: This invention relates to novel tetrahydronaphthalene derivatives, and pharmaceutically acceptable salts thereof according to the following formulae, in one embodiment: as described herein. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a selective T-type calcium channel blocker.Type: GrantFiled: September 7, 2011Date of Patent: November 5, 2013Assignee: Concert Pharmaceuticals Inc.Inventors: Roger Tung, Craig E. Masse
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Patent number: 8563589Abstract: Embodiments of the invention relate to the treatment of neuropathic pain in mammals. Embodiments of the invention include methods for treating neuropathic pain with benzimidazole derivatives with PPARgamma agonist activity, as well as methods for preparing medicaments used in such treatments of mammalian pain.Type: GrantFiled: July 29, 2010Date of Patent: October 22, 2013Inventors: Lillian W. Chiang, Tage Honore
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Publication number: 20130274243Abstract: The invention relates to benzimidazole and imidazopyridine derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new Nav1.8 modulators of formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, X and Y are as defined in the description. Nav1.8 modulators are potentially useful in the treatment of a wide range of disorders, particularly pain.Type: ApplicationFiled: January 29, 2013Publication date: October 17, 2013Inventors: Sharanjeet Kaur Bagal, Alan Daniel Brown, Mark Ian Kemp, Wolfgang Klute, Laia Malet Sanz, Brian Edward Marron, Duncan Charles Miller, Sarah Elizabeth Skerratt, Mark J. Suto, Christopher William West
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Patent number: 8552032Abstract: The present invention is directed to novel bicyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1.Type: GrantFiled: December 16, 2010Date of Patent: October 8, 2013Assignee: Janssen Pharmaceutica NVInventors: Edward C. Lawson, Dennis J. Hlasta, Shyamali Ghosh, Renee L. DesJarlais, Carsten Schubert
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Patent number: 8513434Abstract: This invention relates to novel tetrahydronaphthalene derivatives, and pharmaceutically acceptable salts thereof according to the following formulae, in one embodiment: as described herein. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a selective T-type calcium channel blocker.Type: GrantFiled: March 2, 2011Date of Patent: August 20, 2013Assignee: Concert Pharmaceuticals Inc.Inventors: Roger Tung, Craig E. Masse
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Patent number: 8492555Abstract: The invention relates to crystalline salts of isobutyric acid (1R*,2R*,4R*)-2-(2-{[3-(4,7 -dimethoxy-1H-benzoimidazol-2-yl)-propyl]-methyl-amino}-ethyl)-5-phenyl-bicyclo[2.2.2]oct-5-en-2-yl ester, processes for the preparation thereof, pharmaceutical compositions containing said crystalline salts, and their use as medicaments, especially as calcium channel blockers.Type: GrantFiled: October 21, 2009Date of Patent: July 23, 2013Assignee: Actelion Pharmaceuticals Ltd.Inventors: Stefan Abele, Stéphanie Combes, Jacques-Alexis Funel, Kurt Hilpert, Francis Hubler, Katharina Reichenbaecher, Dorte Renneberg, Markus Von Raumer
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Patent number: 8486984Abstract: The present invention relates to an aminomethyl substituted bicyclic aromatic compound of the formula I The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.Type: GrantFiled: October 14, 2005Date of Patent: July 16, 2013Assignee: Abbott GmbH & Co., KGInventors: Karla Drescher, Andreas Haupt, Liliane Unger, Sean C. Turner, Wilfried Braje, Roland Grandel
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Publication number: 20130172389Abstract: The present invention is directed to a compound of Formula I or a pharmaceutically acceptable salt thereof; wherein R, R1, R2, R3, R4, m, and n are as defined herein, to pharmaceutical compositions comprising said compound, and to methods of treating diseases or conditions mediated by elevated persistent sodium current, such as an ocular disorder, multiple sclerosis, seizure disorder, and chronic pain.Type: ApplicationFiled: December 27, 2012Publication date: July 4, 2013Applicant: Allegan, Inc.Inventor: Allergan, Inc.
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Patent number: 8471038Abstract: The invention provides a compound for the treatment or prophylaxis of pathology involving SNS, specifically diseases such as neuropathic pain, nociceptive pain, dysuria, multiple sclerosis and the like.Type: GrantFiled: December 25, 2009Date of Patent: June 25, 2013Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Katsunori Tsuboi, Yusuke Yamai, Hitoshi Watanabe, Hironori Kinoshita
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Patent number: 8461351Abstract: A sterically bulky stabilizer that includes an alkylated-benzimidazolone compound, where the sterically bulky stabilizer is associated non-covalently with a benzimidazolone pigment, and the presence of the sterically bulky stabilizer limits the extent of particle growth and aggregation, to afford nanoscale pigment particles.Type: GrantFiled: July 28, 2011Date of Patent: June 11, 2013Assignees: Xerox Corporation, National Research Council of CanadaInventors: Rina Carlini, Darren Andrew Makeiff