Abstract: The present invention provides pharmaceutical formulations suitable for intravenous injection comprising a lyophilized anti-ulcerative agent reconstituted in isotonic solutions suitable for intravenous administration, such as 5% dextrose or 0.9% sodium chloride. The solutions are brought to a pH of between about 9 and about 12, preferably between about pH 10 and 11, by a glycine-sodium hydroxide buffer. Such formulations are chemically and physically stable, and do not significantly change color, for at least between about 6 and about 12 hours at room temperature, and are stable to color change for from between about 24 and 48 hours if kept at 5° C.
Type:
Grant
Filed:
April 14, 2000
Date of Patent:
June 12, 2007
Assignee:
Eisai Co., Ltd.
Inventors:
James McShane, Ray Wood, Sumio Watanabe, Kiyoshi Iwamoto, Katsumi Onai
Abstract: Methods for treating cardiovascular and related diseases such as arrhythmia are described. The methods are directed to concurrently administering a compound such as pyridoxal-5?-phosphate, pyridoxamine, pyridoxal, or a 3-acylated pyridoxal analogue with a therapeutic cardiovascular compound.
Abstract: The invention relates to piperazine derivatives, to processes for their preparation, to pharmaceutical compositions containing them, and to their medical use. The novel compounds are antagonists of tachykinins, including substance P and other neurokinins.
Type:
Grant
Filed:
October 5, 2004
Date of Patent:
November 13, 2007
Assignee:
SmithKline Beecham Corporation
Inventors:
Giuseppe Alvaro, Romano DiFabio, Riccardo Giovannini, Giuseppe Guercio, Yves St-Denis, Antonella Ursini
Abstract: The present invention provides dyes of the general formula (I) where D, R1 to R7 and n are each as defined in claim 1, processes for their preparation and their use.
Abstract: Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of The compoundic mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.
Type:
Grant
Filed:
January 10, 2014
Date of Patent:
August 30, 2016
Assignee:
Board of Regents, The University of Texas System
Inventors:
Patrick G Harran, Xiaodong Wang, Jef K. DeBrabander, Lin Li, Ranny Mathew Thomas, Hidetaka Suzuki
Abstract: A tissue adhesives and sealant formed by reacting a polyglycerol aldehyde with a water-dispersible, multi-arm amine is described. The tissue adhesive and sealant may be useful for medical and veterinary applications, including, but not limited to, wound closure, supplementing or replacing sutures or staples in internal surgical procedures such as intestinal anastomosis and vascular anastomosis, tissue repair, preventing leakage of fluids such as blood, bile, gastrointestinal fluid and cerebrospinal fluid, ophthalmic procedures, drug delivery, and to prevent post-surgical adhesions.
Abstract: The present invention describes a method for the synthesis of enantiomerically pure 3-amidinophenylalanine derivatives, which are used as pharmaceutically effective urokinase inhibitors, by starting from 3-cyanophenylalanine derivatives. The methods of manufacture comprising only one synthesis step lead to new intermediates, namely 3-hydroxyamidino- and 3-amidrazonophenylalanine derivatives. These intermediates or their acetyl derivatives can be reduced into the desired 3-amidino-phenylalanine derivatives under gentle conditions (H2 or ammonium formiate formate, Pd/C (approx. 10%), ethanol/water, room temperature, normal pressure or also H2, Pd/C, AcOH or HCl/ethanol, 1-3 bar) in excellent yields and in an enantiomeric excess of up to 99.9%.
Abstract: The present invention concerns deuterated catecholamine derivatives as well as pharmaceuticals containing these compounds. In addition, the invention concerns the use of deuterated catecholamine derivatives as well as physiologically acceptable salts thereof, and also pharmaceutical compositions, which contain these compounds, also in combination with enzyme inhibitors, for the treatment of dopamine deficiency diseases or diseases which are based on disrupted tyrosine transport or disrupted tyrosine decarboxylase, as well as other disorders.
Abstract: The present invention relates to the field of synthesizing anti-infective compounds. More particularly, the invention relates to synthesizing a family of quinolone compounds useful as anti-infective agents. The invention includes a process for preparing a quinolone compound wherein less than about 0.40% of dimeric impurity of the quinolone is produced.
Type:
Grant
Filed:
June 18, 2015
Date of Patent:
November 28, 2017
Assignee:
MELINTA THERAPEUTICS, INC.
Inventors:
Roger Hanselmann, Maxwell M. Reeve, Graham Johnson
Abstract: The invention relates to substituted dihydroquinazolines and to processes for their preparation and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for use as antiviral agents, in particular against cytomegalo viruses.
Type:
Grant
Filed:
April 9, 2015
Date of Patent:
April 17, 2018
Assignee:
AICURIS ANTI-INFECTIVE CURES GMBH
Inventors:
Tobias Wunberg, Judith Baumeister, Ulrich Betz, Mario Jeske, Thomas Lampe, Susanne Nikolic, Jurgen Reefschlager, Rudolf Schohe-Loop, Frank Sussmeier, Holger Zimmermann, Rolf Grosser, Kerstin Henninger, Guy Hewlett, Jorg Keldenich, Dieter Lang, Peter Nell
Abstract: The invention provides compounds of Formula (I) and Formula (II) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
Type:
Grant
Filed:
March 1, 2017
Date of Patent:
February 5, 2019
Assignee:
AbbVie Inc.
Inventors:
Neil Wishart, Kristine E. Frank, Michael Friedman, Dawn M. George, Kent D. Stewart, Grier A. Wallace
Abstract: There is disclosed pyridine-and pyrimidinecarboxamide compounds useful as pharmaceutical agents, synthesis processes, and pharmaceutical compositions which include pyridine-and pyrimidinecarboxamides compounds. More specifically, there is disclosed a genus of CXCR2 inhibitor compounds that are useful for treating a variety of inflammatory and neoplastic disorders.
Abstract: Provided herein are tripeptide epoxy ketone protease inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula (X): and pharmaceutically acceptable salts and compositions including the same. The compounds and compositions provided herein may be used, for example, in the treatment of diseases including inflammation and neurodegenerative disease.
Type:
Grant
Filed:
June 23, 2017
Date of Patent:
March 19, 2019
Assignee:
ONYX THERAPEUTICS INC.
Inventors:
Dustin McMinn, Henry Johnson, Simeon Bowers, David C. Moebius
Abstract: Provided are a thieno[3,2-d]pyrimidine derivative of formula (I) or a pharmaceutically acceptable salt thereof having inhibitory activity for protein kinase, and a pharmaceutical composition comprising same for prevention and treatment of abnormal cell growth diseases.
Type:
Grant
Filed:
October 13, 2017
Date of Patent:
June 25, 2019
Assignee:
Hanmi Pharm. Co. Ltd.
Inventors:
In Hwan Bae, Jung Beom Son, Sang Mi Han, Eun Joo Kwak, Ho Seok Kim, Ji Young Song, Eun Young Byun, Seung Ah Jun, Young Gil Ahn, Kwee Hyun Suh
Abstract: In preferred embodiments, the present invention provides methods of treatment and pharmaceutical compositions for the suppression, alleviation and prevention of the often chronic, severe and debilitating pain that can accompany inflammatory diseases and neuropathic insults, pain that is often unresponsive to conventional analgesic treatment. The preferred embodiments of the present invention further relate to methods of treatment and pharmaceutical compositions using benzodiazepine derivatives that provide suppression, alleviation and prevention of neuropathic pain, migraine-related pain and inflammatory pain with reduced sedative and ataxic side effects.
Type:
Grant
Filed:
September 16, 2016
Date of Patent:
July 2, 2019
Assignee:
WISYS TECHNOLOGY FOUNDATION, INC.
Inventors:
James M. Cook, Shengming Huang, Rahul Edwankar, Ojas A. Namjoshi, Zhi-Jian Wang, Qi Huang, Xiaohui He, Xiaoyan Li, Jianming Yu, Dongmei Han
Abstract: Convenient methods of preparing aza-dibenzocyclooctynes are disclosed herein. Aza-dibenzocyclooctynes attached to a surface are also disclosed herein. Aza-dibenzocyclooctynes can be reacted with azides to form heterocyclic compounds. Such reactions can be useful in a wide variety of applications including, for example, labeling surfaces.
Type:
Grant
Filed:
December 16, 2016
Date of Patent:
July 30, 2019
Assignee:
UNIVERSITY OF GEORGIA RESEARCH FOUNDATION, INC.
Inventors:
Vladimir V. Popik, Alexander Kuzmin, Andrei Polukhtine
Abstract: Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy. In a specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN2 into mRNA that is transcribed from the SMN2 gene. In another specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 into mRNA that is transcribed from the SMN1 gene. In yet another embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 and SMN2 into mRNA that is transcribed from the SMN1 and SMN2 genes, respectively.
Type:
Grant
Filed:
September 5, 2017
Date of Patent:
November 5, 2019
Assignees:
PTC Therapeutics, Inc., F. Hoffmann-La Roche
Inventors:
Matthew G. Woll, Guangming Chen, Soongyu Choi, Amal Dakka, Song Huang, Gary Mitchell Karp, Chang-Sun Lee, Chunshi Li, Jana Narasimhan, Nikolai Naryshkin, Sergey Paushkin, Hongyan Qi, Anthony A. Turpoff, Marla L. Weetall, Ellen Welch, Tianle Yang, Nanjing Zhang, Xiaoyan Zhang, Xin Zhao, Emmanuel Pinard, Hasane Ratni
Abstract: The present invention relates to novel hydroxamic acids which are specific histone deacetylase (HDAC) inhibitors and/or TTK/Mps1 kinase inhibitors, including pharmaceutically acceptable salts thereof, which are useful for modulating HDAC and/or TTK/Mps1 kinase activity, pharmaceutical compositions comprising these compounds, and processes for their preparation.
Type:
Grant
Filed:
May 1, 2018
Date of Patent:
November 5, 2019
Assignee:
The Regents of the University of Colorado, A Body Corporate
Inventors:
Xuedong Liu, Gan Zhang, Daniel Chuen-Fong Chan, Anthony D. Piscopio
Abstract: The present invention provides for compounds of Formula I and embodiments and salts thereof for the treatment of diseases (e.g., neurodegenerative diseases). R1, R2, R3, X1, X2, A and Cy variable in Formula all have the meaning as defined herein.
Type:
Grant
Filed:
February 22, 2018
Date of Patent:
February 11, 2020
Assignee:
Genentech, Inc.
Inventors:
Anthony Estrada, Alan G. Olivero, Snahel Patel, Michael Siu, Joseph Lyssikatos, Malcolm Huestis, Terry Kellar