Plural Acyclic Nitrogens Bonded Directly To The Same Carbon Or Bonded Directly To Each Other Patents (Class 514/353)
  • Patent number: 11045445
    Abstract: Method of treating endometriosis and related indications, comprising the administration of Pro-EGCG, a synthetic and derivative product of epigallocatechin-3-gallate [(?)-EGCG]. Use of PRO-EGCG in the manufacture of a medicament for treating endometriosis and related indications. Pro-EGCG for use in the treatment of endometriosis and related indications.
    Type: Grant
    Filed: May 4, 2020
    Date of Patent: June 29, 2021
    Assignees: The Hong Kong Polytechnic University, The Chinese University of Hong Kong
    Inventors: Tak-Hang Chan, Chi-Chiu Wang
  • Patent number: 10220018
    Abstract: Mitigation of long and short-term detrimental effects of exposure to low dose ionizing radiation by administration of genistein in the form of a nanosuspension to a mammal in an amount effective for achieving genistein serum levels of between 1-5 ?M in the mammal throughout a time period from exposure to the ionizing radiation to twelve hours after exposure to the ionizing radiation.
    Type: Grant
    Filed: May 11, 2018
    Date of Patent: March 5, 2019
    Assignee: Humanetics Corporation
    Inventors: Michael D. Kaytor, John L. Zenk
  • Patent number: 10064846
    Abstract: The present invention provides uses of a glucokinase activator in combination with metformin. Uses include treating type 2 diabetes, lowering blood glucose, improving insulin sensitivity, enhancing phosphorylation of glucose, and improving the therapeutic effectiveness of metformin. The invention also provides pharmaceutical compositions that comprise a GK activator and metformin. The invention also provides a salt formed between metformin and a GK activator.
    Type: Grant
    Filed: August 28, 2017
    Date of Patent: September 4, 2018
    Assignee: vTv Therapeutics LLC
    Inventors: Adnan M. M. Mjalli, Maria Carmen Valcarce Lopez
  • Patent number: 10065927
    Abstract: The instant invention relates to compounds of formula I wherein: R is selected from H, Me or Cl, and R? is selected from: H, NH2, NHCOCH3 NHCOCF3 or NHCOCH2Cl. The invention further provides a process for obtaining the compounds of formula I and their use.
    Type: Grant
    Filed: January 14, 2016
    Date of Patent: September 4, 2018
    Assignee: FUNDACÃO OSWALDO CRUZ (FIOCRUZ)
    Inventors: Núbia Boechat, Frederico Silva Castelo Branco
  • Patent number: 9993455
    Abstract: Mitigation of long term detrimental effects of exposure to medical imaging ionizing radiation by administration of an amount of genistein in the form of a nanosuspension to someone effective for achieving genistein serum levels of between 1-5 ?M in the mammal throughout a time period from exposure to medical imaging ionizing radiation to twelve hours after exposure to medical imaging ionizing radiation.
    Type: Grant
    Filed: March 6, 2017
    Date of Patent: June 12, 2018
    Assignee: Humanetics Corporation
    Inventors: Michael D. Kaytor, John L. Zenk
  • Publication number: 20150110853
    Abstract: The present invention provides methods and compositions preventing and treating radical prostatectomy-induced erectile dysfuntion. One embodiment of the present invention is directed to a method of preventing and treating radical prostatectomy-induced erectile dysfuntion by administering to a patient in need at least one thiosemicarbazone compound.
    Type: Application
    Filed: October 18, 2013
    Publication date: April 23, 2015
    Applicant: PANACEA PHARMACEUTICALS
    Inventors: Hossein A. Ghanbari, Zhi-Gang Jiang
  • Patent number: 9000014
    Abstract: The invention provides pyridonyl guanidine compounds that inhibit F1F0-ATPase, and methods of using pyridonyl guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.
    Type: Grant
    Filed: December 8, 2011
    Date of Patent: April 7, 2015
    Assignee: Lycera Corporation
    Inventors: Gary D. Glick, Alexander R. Hurd, Matthew N. Mattson, Clarke B. Taylor, Chad A. Van Huis
  • Patent number: 8962847
    Abstract: The invention relates to novel multicomponent crystals, to the production thereof, and to the use thereof for treating pain conditions, in particular of unclear genesis, by means of a simultaneous effect on pains which are caused by muscle tension or degenerative joint diseases as well as on pains that are caused by inflammatory processes. The multicomponent crystals according to the invention contain ([2-amino-6-(4-fluoro-benzylamino)-pyridin-3-yl]-carbamic acid ethyl ester (flupirtine) and an arylpropionic acid as the sole active ingredient combination and can be produced by dissolving flupirtine and the arylpropionic acid in an inert organic solvent and subsequently crystallizing the multicomponent crystal.
    Type: Grant
    Filed: December 20, 2011
    Date of Patent: February 24, 2015
    Assignee: TEVA GmbH
    Inventors: Christoph Martin Hoock, Asal Qadan, Bernd Terhaag
  • Publication number: 20150031726
    Abstract: Substituted phenylcarbamoyl alkylamino arenes; substituted phenylthiocarbamyl alkylamino arenes; substituted phenylcarbamoyl alkylamino heteroarenes; substituted phenylthiocarbamyl alkylamino heteroarenes; N-substituted aryl, N?-substituted aryl urea compounds; N-substituted aryl, N?-substituted heteroaryl urea compounds; N-substituted aryl, N?-substituted aryl thiourea compounds and N-substituted aryl, N?-substituted heteroaryl thiourea compounds are provided and may find use as androgen receptor modulators. The compounds may find particular use in treating prostate cancer, including castration-resistant prostate cancer and/or hormone-sensitive prostate cancer.
    Type: Application
    Filed: October 15, 2014
    Publication date: January 29, 2015
    Inventors: Sarvajit Chakravarty, Rajendra Parasmal Jain
  • Publication number: 20150005296
    Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
    Type: Application
    Filed: September 18, 2014
    Publication date: January 1, 2015
    Inventors: Bradley Paul Morgan, Alex Muci, Pu-Ping Lu, Erica Anne Kraynack, Todd Tochimoto, David J. Morgans, JR.
  • Publication number: 20140377247
    Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.
    Type: Application
    Filed: February 7, 2014
    Publication date: December 25, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Bing-Yan ZHU, Penglie ZHANG, Lingyan WANG, Wenrong HUANG, Erick A. GOLDMAN, Wenhao LI, Jingmei ZUCKETT, Yonghong SONG, Robert M. SCARBOROUGH
  • Publication number: 20140363489
    Abstract: The present invention provides methods and compositions for treating retinal degeneration. One embodiment of the present invention is directed to a method of treating retinal degeneration by administering to a patient in need at least one thiosemicarbazone compound.
    Type: Application
    Filed: June 7, 2013
    Publication date: December 11, 2014
    Inventors: Hossein A. Ghanbari, Zhi-Gang Jiang
  • Publication number: 20140357599
    Abstract: The present application discloses compounds of formula (I) wherein X is ?O, ?S, ?NH, ?NOH and ?NO-Me; A is —C(?O)—, —S(?O)2—, —C(?S)— and P(?O)(R5)—; B is, —O—, —(CH2)3-6—, and O—(CH2)2-5—; D is, —O—, —CR7R8— and —NR9; m is 0-12, n is 0-12, m+n is 1-20; p is 0-4; R1 is opt.sub. heteroaryl; and pharmaceutically acceptable salts thereof, and prodrugs thereof. The application also discloses the compound for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT), e.g. inflammatory and tissue repair disorders; dermatosis; autoimmune diseases, Alzheimers disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, ataxia telengiectasia.
    Type: Application
    Filed: August 18, 2014
    Publication date: December 4, 2014
    Inventors: Mette Knak CHRISTENSEN, Fredrik BJORKLING
  • Patent number: 8895585
    Abstract: An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. The present invention provides a nicotinamide derivative represented by the following formula (I) (wherein R1 represents a halogen atom; R2 represents a C1-12 alkyl group, a C2-12 alkenyl group, a C2-12 alkynyl group, a C3-8 cycloalkyl group, an aryl group, an ar-C1-6 alkyl group or a heterocyclic group, each optionally having at least one substituent; R3 represents an aryl group or a heterocyclic group each optionally having at least one substituent; and R4 and R5 each independently represent a hydrogen atom; and R2 and R4 may form a cyclic amino group optionally having at least one substituent together with the nitrogen atom to which they bind) or a salt thereof, and a pharmaceutical composition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.
    Type: Grant
    Filed: December 28, 2012
    Date of Patent: November 25, 2014
    Assignee: FUJIFILM Corporation
    Inventors: Hideyasu Fujiwara, Kimihiko Sato, Shinsuke Mizumoto, Yuichiro Sato, Hideki Kurihara, Yohei Kubo, Hiyoku Nakata, Yasutaka Baba, Takashi Tamura, Hidenobu Kuniyoshi, Shinji Hagiwara, Mari Yamamoto
  • Publication number: 20140323497
    Abstract: This invention is directed to methods of inhibiting coagulation or treating thrombosis using a factor Xa inhibitor and a P-glycoprotein (Pgp) inhibitor. The invention is also directed to formulations used in the methods.
    Type: Application
    Filed: November 12, 2013
    Publication date: October 30, 2014
    Applicant: Portola Pharmaceuticals, Inc.
    Inventors: Uma Sinha, George A. Mansoor, Anne Hermanowski Vosatka, Vincent R. Capodanno, Robert M. Wenslow, Richard G. Ball, Eric L. Margeiefsky, Timothy K. Maher, Itzia Zoraida Arroyo, Brett Lauring, Liam Corcoran, William Denney, Michael McNevin, Anjali Pandey
  • Publication number: 20140323486
    Abstract: The present invention provides a compound of the following formula, racemates, enantiomers and salts thereof. Also provided is the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.
    Type: Application
    Filed: December 21, 2012
    Publication date: October 30, 2014
    Inventors: Edward Malcolm Tyndall, Lloyd George Czaplewski, Colin William Gordon Fishwick, Andrew Ian Yule, Jeffrey Peter Mitchell, Kelly Helen Anderson, Gary Robert William Pitt
  • Patent number: 8865771
    Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Grant
    Filed: January 23, 2013
    Date of Patent: October 21, 2014
    Assignee: Vertex Pharamaceuticals Incorporated
    Inventors: Weichuan Caroline Chen, Paul Krenitsky, Andreas Termin, Dean Wilson
  • Patent number: 8859594
    Abstract: Disclosed are a polymorphs I-VI of N-(6-(4-chlorophenoxy)hexyl)-N?-cyano-N?-(4-pyridyl)guanidine or of a solvate thereof, a preparation method thereof, and a use thereof as a biological active ingredient. The polymorphs are useful in treatment of cancers, and diseases or disorders caused by abnormal cell proliferation.
    Type: Grant
    Filed: October 25, 2011
    Date of Patent: October 14, 2014
    Assignees: Tianjin Hemay Bio-Tech Co., Ltd., Tianjin Michele Sci-Tech Development Co., Ltd.
    Inventors: Hesheng Zhang, Xin Chen
  • Publication number: 20140287021
    Abstract: The present invention provides methods and compositions for treating chemotherapy induced peripheral neuropathy. One embodiment of the present invention is directed to a method of treating chemotherapy induced peripheral neuropathy by administering to a patient in need at least one thiosemicarbazone compound.
    Type: Application
    Filed: March 21, 2013
    Publication date: September 25, 2014
    Applicant: Panacea Pharmaceuticals
    Inventors: Hossein A. Ghanbari, Zhi-Gang Jiang
  • Publication number: 20140271812
    Abstract: The present invention provides methods and compositions for treating chemotherapy-induced cognitive impairment. One embodiment of the present invention is directed to a method of treating chemotherapy-induced cognitive impairment by administering to a patient in need at least one thiosemicarbazone compound.
    Type: Application
    Filed: March 14, 2013
    Publication date: September 18, 2014
    Applicant: Panacea Pharmaceuticals
    Inventors: Hossein A. Ghanbari, Zhi-Gang Jiang
  • Publication number: 20140242120
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein Y, L, A, W1, W2, and R?1 are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Application
    Filed: May 8, 2014
    Publication date: August 28, 2014
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Shoujun Chen, Lijun Sun, Yu Xie
  • Patent number: 8809371
    Abstract: An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. The present invention provides a nicotinamide derivative represented by the following formula (I) (wherein R1 represents a halogen atom; R2 represents a C1-12 alkyl group, a C2-12 alkenyl group, a C2-12 alkynyl group, a C3-8 cycloalkyl group, an aryl group, an ar-C1-6 alkyl group or a heterocyclic group, each optionally having at least one substituent; R3 represents an aryl group or a heterocyclic group each optionally having at least one substituent; and R4 and R5 each independently represent a hydrogen atom; and R2 and R4 may form a cyclic amino group optionally having at least one substituent together with the nitrogen atom to which they bind) or a salt thereof, and a pharmaceutical composition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.
    Type: Grant
    Filed: December 28, 2012
    Date of Patent: August 19, 2014
    Assignee: FUJIFILM Corporation
    Inventors: Hideyasu Fujiwara, Kimihiko Sato, Shinsuke Mizumoto, Yuichiro Sato, Hideki Kurihara, Yohei Kubo, Hiyoku Nakata, Yasutaka Baba, Takashi Tamura, Hidenobu Kuniyoshi, Shinji Hagiwara, Mari Yamamoto
  • Patent number: 8795701
    Abstract: The invention relates to a method for improving the utilization of the production potential of transgenic plants which comprises treating the plant with active compound combinations comprising an active compound from the group of the anthranilamides and at least one further insecticide.
    Type: Grant
    Filed: April 8, 2008
    Date of Patent: August 5, 2014
    Assignee: Bayer CropScience AG
    Inventors: Wolfram Andersch, Christian Funke, Heike Hungenberg, Wolfgang Thielert
  • Patent number: 8785466
    Abstract: Methods and therapeutic strategies utilizing proteinacious channels in lipid membranes of mammalian cells. The methods entail administering a pharmaceutical to a lipid membrane of a mammalian cell, and then determining the effect of the pharmaceutical on the electrophysiology of at least one vascular proteinacious channel of the lipid membrane, wherein the vascular proteinacious channel is a vascular Kv7 potassium channel and/or a vascular L-type calcium channel. The method can be used to identify pharmaceuticals that may be used to treat hypertension and/or vasospastic conditions, or to perform drug screening to assess potential cardiovascular risk of pharmaceuticals.
    Type: Grant
    Filed: October 30, 2009
    Date of Patent: July 22, 2014
    Assignee: Loyola University Chicago
    Inventors: Kenneth L. Byron, Lioubov I. Brueggemann
  • Patent number: 8778392
    Abstract: An oral disintegrating tablet containing (1) D-mannitol, (2) an active ingredient, (3) one or more disintegrating agents selected from the group consisting of crospovidone and carmellose, and (4) one or more lubricants selected from the group consisting of sodium stearyl fumarate and sucrose esters of fatty acids. The oral disintegrating tablet of the present invention has some excellent properties of (1) allowing easy production in a common facility without necessitating a specialized pharmaceutical technique, (2) having an appropriate strength that does not breakdown in the process of distribution, (3) having a fast disintegrating ability in the oral cavity, and (4) also having excellent ingestion feel such as greatly reduced bitterness or gritty feel; therefore, the tablet can be suitably used as a dosage form that is suitable for aged individuals, children, and seriously ill patients.
    Type: Grant
    Filed: March 12, 2008
    Date of Patent: July 15, 2014
    Assignee: Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Makoto Matsuoka, Hiroyuki Nishii, Maki Kawamura
  • Patent number: 8772320
    Abstract: An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. The present invention provides a nicotinamide derivative represented by the following formula (I) (wherein R1 represents a halogen atom; R2 represents a C1-12 alkyl group, a C2-12 alkenyl group, a C2-12 alkynyl group, a C3-8 cycloalkyl group, an aryl group, an ar-C1-6 alkyl group or a heterocyclic group, each optionally having at least one substituent; R3 represents an aryl group or a heterocyclic group each optionally having at least one substituent; and R4 and R5 each independently represent a hydrogen atom; and R2 and R4 may form a cyclic amino group optionally having at least one substituent together with the nitrogen atom to which they bind) or a salt thereof, and a pharmaceutical composition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.
    Type: Grant
    Filed: December 28, 2012
    Date of Patent: July 8, 2014
    Assignee: FUJIFILM Corporation
    Inventors: Hideyasu Fujiwara, Kimihiko Sato, Shinsuke Mizumoto, Yuichiro Sato, Hideki Kurihara, Yohei Kubo, Hiyoku Nakata, Yasutaka Baba, Takashi Tamura, Hidenobu Kuniyoshi, Shinji Hagiwara, Mari Yamamoto
  • Publication number: 20140179620
    Abstract: The present invention relates to methods of gene expression profiling for inflammatory bowel disease pathogenesis, in which the differential expression in a test sample from a mammalian subject of one or more IBD markers relative to a control is determined, wherein the differential expression in the test sample is indicative of an IBD in the mammalian subject from which the test sample was obtained.
    Type: Application
    Filed: August 12, 2013
    Publication date: June 26, 2014
    Applicant: GENENTECH, INC.
    Inventors: Alexander R. Abbas, Hilary Clark, Lauri Diehl, Charles Lees, Colin L. Noble, Jack Satsangi
  • Publication number: 20140162996
    Abstract: One aspect of the disclosure relates to derivatives of aryl and heterocyclic ureido aryl and heterocyclic carboxamido isobutyric acids, dichlorophenyl urea, curcumin, and 1,3-diazetidine-2,4-dione, and pharmaceutical compositions thereof. The derivatives disclosed herein can modulate development of adipocytes and various cancer cells, including resistant cancer cells and cancer stem cells. Another aspect of the disclosure relates to the use of the derivatives and pharmaceutical compositions disclosed herein in treatment of obesity and various cancers.
    Type: Application
    Filed: July 29, 2013
    Publication date: June 12, 2014
    Applicant: CITY OF HOPE
    Inventors: Samuel RAHBAR, James L. FIGAROLA, Christopher LINCOLN, David HORNE, Rachael MOONEY, Monika POLEWSKI, George SOMLO, Lixin YANG
  • Patent number: 8716283
    Abstract: The invention, in some aspects, relates to compounds and compositions useful for inhibiting Type III secretion systems in pathogenic bacteria, such as Yersinia Pestis. In some aspects, the invention relates to methods for discovering inhibitors of the Type III secretion system and uses of such inhibitors in the treatment and prevention of disease.
    Type: Grant
    Filed: April 1, 2009
    Date of Patent: May 6, 2014
    Assignees: University of Massachusetts, President and Fellows of Harvard College
    Inventors: Jon Goguen, Ning Pan, Kyungae Lee
  • Publication number: 20140051727
    Abstract: The invention provides pyridonyl guanidine compounds that inhibit F1F0-ATPase, and methods of using pyridonyl guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.
    Type: Application
    Filed: December 8, 2011
    Publication date: February 20, 2014
    Applicant: Lycera Corporation
    Inventors: Gary D. Glick, Alexander R. Hurd, Matthew N. Mattson, Clarke B. Taylor, Chad A. Van Huis
  • Publication number: 20140038910
    Abstract: Disclosed herein are novel pharmaceutical agents which are useful as integrin receptor antagonists that mediate the pathologic processes of angiogenesis and fibrosis and as such are useful in pharmaceutical compositions and in methods for treating conditions mediated by these integrins by inhibiting or antagonizing these integrins. The novel pharmaceutical agents include those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such pharmaceutical agents. Methods and intermediates useful for making the pharmaceutical agents and methods of using the pharmaceutical agents are also provided.
    Type: Application
    Filed: July 17, 2013
    Publication date: February 6, 2014
    Applicant: Saint Louis University
    Inventors: Peter RUMINSKI, David GRIGGS
  • Patent number: 8642630
    Abstract: It relates to an endogenous repair factor production accelerator which comprises one or at least two selected from prostaglandin (PG) I2 agonist, EP2 agonist and EP4 agonist. Since prostaglandin (PG) I2 agonist, EP2 agonist or EP4 agonist has various endogenous repair factor production accelerating action, angiogenesis acceleration action and stem cell differentiation induction action, it is useful as preventive and/or therapeutic agents for ischemic organ diseases (e.g., arteriosclerosis obliterans, Buerger disease, Raynaud disease, myocardial infarction, angina pectoris, diabetic neuropathy, spinal canal stenosis, cerebrovascular accidents, cerebral infarction, pulmonary hypertension, bone fracture, Alzheimer disease, etc.) and various cell and organ diseases.
    Type: Grant
    Filed: April 4, 2013
    Date of Patent: February 4, 2014
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Yoshiki Sakai, Akio Nishiura, Teppei Ogata
  • Publication number: 20140024621
    Abstract: The invention generally relates to aminopyridines and methods of use thereof. In certain embodiments, the invention provides an aminopyridine or a pharmaceutically-acceptable salt thereof, in which the aminopyridine or the salt thereof includes a cleavable functional group that substantially prevents extra-hepatic hydrolysis.
    Type: Application
    Filed: July 23, 2012
    Publication date: January 23, 2014
    Applicant: MS THERAPEUTICS LIMITED
    Inventors: Michael J. Hudson, Alan Palmer, Richard Todd, Patrick Camilleri
  • Patent number: 8604212
    Abstract: Septic shock is known to lead to, at the end stage, systematic inflammatory reaction syndrome and multiple organ failure (MOF) and cause the patients' death. In both diseases, the patient dies finally of MOF, and the infiltration by inflammatory cells plays a key role for MOF. Thus, development of therapeutic agents for septic shock by suppressing the infiltration by inflammatory cells has been desired. To provide a therapeutic or preventive agent for shock, comprising as an active ingredient a diaminotrifluoromethylpyridine derivative represented by the formula (I) or its salt: wherein X is a cycloalkylcarbonyl group, an alkenylcarbonyl group, a thiophenecarbonyl group or a benzoyl group which may be substituted by a halogen atom; and Y is an alkylsulfonyl group.
    Type: Grant
    Filed: May 17, 2010
    Date of Patent: December 10, 2013
    Assignee: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Shuichi Yotsuya, Hiroshi Shikama
  • Patent number: 8604065
    Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof, and use for treating cancer thereof are disclosed, wherein, the definitions of X, Y, R1, R2 and n are described in description.
    Type: Grant
    Filed: November 18, 2010
    Date of Patent: December 10, 2013
    Inventors: Hesheng Zhang, Xin Chen, Yingwei Chen, Junjie Cong, Xingwen Li
  • Publication number: 20130310346
    Abstract: The present invention provides methods and compositions for treating or preventing bacterial infections, where a pharmaceutically acceptable iron chelator that reduces biological availability of iron for one or more strains of bacteria, such as VK28 or an analog or derivative thereof is administered to a patient in need of treatment. The method also provides methods and compositions where an iron chelator and an antibiotic are administered to a patient in need of treatment for a bacterial infection.
    Type: Application
    Filed: January 31, 2012
    Publication date: November 21, 2013
    Applicant: Government of the United States, as represented by the Secretary of the Army
    Inventor: Daniel Zurawski
  • Publication number: 20130295051
    Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below.
    Type: Application
    Filed: September 2, 2011
    Publication date: November 7, 2013
    Inventors: Kenneth W. Bair, Alexandre J. Buckmelter, Bingsong Han, Jian Lin, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Xiaozhang Zheng
  • Publication number: 20130281494
    Abstract: Disclosed are a polymorphs I-VI of N-(6-(4-chlorophenoxy)hexyl)-N?-cyano-N?-(4-pyridyl)guanidine or of a solvate thereof, a preparation method thereof, and a use thereof as a biological active ingredient. The polymorphs are useful in treatment of cancers, and diseases or disorders caused by abnormal cell proliferation.
    Type: Application
    Filed: October 25, 2011
    Publication date: October 24, 2013
    Applicants: Tianjin Michele Sci-Tech Development Co., Ltd., Tianjin Hemay Bio-Tech Co., Ltd.
    Inventors: Hesheng Zhang, Xin Chen
  • Publication number: 20130273034
    Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes.
    Type: Application
    Filed: September 2, 2011
    Publication date: October 17, 2013
    Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Bingsong Han, Jian Lin, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Xiaozhang Zheng, Po-Wai Yuen
  • Publication number: 20130267567
    Abstract: The invention relates to novel multicomponent crystals, to the production thereof, and to the use thereof for treating pain conditions, in particular of unclear genesis, by means of a simultaneous effect on pains which are caused by muscle tension or degenerative joint diseases as well as on pains that are caused by inflammatory processes. The multicomponent crystals according to the invention contain ([2-amino-6-(4-fluoro-benzylamino)-pyridin-3-yl]-carbamic acid ethyl ester (flupirtine) and an arylpropionic acid as the sole active ingredient combination and can be produced by dissolving flupirtine and the arylpropionic acid in an inert organic solvent and subsequently crystallizing the multicomponent crystal.
    Type: Application
    Filed: December 20, 2011
    Publication date: October 10, 2013
    Applicant: AWD.PHARMA GMBH & CO. KG
    Inventors: Christoph Martin Hoock, Asal Qadan, Bernd Terhaag
  • Publication number: 20130261157
    Abstract: The invention relates to novel multicomponent crystals, to the production thereof, and to the use thereof for treating pain conditions, in particular of unclear genesis, by means of a simultaneous effect on pains which are caused by muscle tension or degenerative joint diseases as well as on pains that are based on inflammatory processes. The novel multicomponent crystals contain ([2-amino-6-(4-fluoro-benzylamino)-pyridin-3-yl]-carbamic acid ethyl ester (flupirtine) and 2-[2-[(2,6-dichlorphenyl)-amino]-phenyl]-acetic acid (diclofenac) as the sole active ingredient combination and can be produced by dissolving the two components in a molar ratio of 1.0:0.9 to 1.0:1.1 in an inert organic solvent and subsequently crystallizing the complex compound.
    Type: Application
    Filed: December 20, 2011
    Publication date: October 3, 2013
    Applicant: AWD.PHARMA GMBH & CO. KG
    Inventors: Christoph Martin Hoock, Asal Qadan, Bernd Terhaag
  • Patent number: 8513286
    Abstract: Compounds of the formula (I) in which the substituents are as defined in claim 1 are suitable for use as microbiocides.
    Type: Grant
    Filed: February 20, 2008
    Date of Patent: August 20, 2013
    Assignee: Syngenta Crop Protection LLC
    Inventors: Paul Anthony Worthington, Daniel Stierli, Fredrik Cederbaum, Kurt Nebel, Antoine Daina
  • Patent number: 8486950
    Abstract: The invention provides compounds of Formula I, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, B, D, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and methods of use thereof.
    Type: Grant
    Filed: June 10, 2010
    Date of Patent: July 16, 2013
    Assignee: F. Hoffmann-La Roche AG
    Inventors: Simon Charles Goodacre, Yingjie Lai, Jun Liang, Steven R. Magnuson, Kirk D. Robarge, Mark S. Stanley, Vickie Hsiao-Wei Tsui, Karen Williams, Birong Zhang, Aihe Zhou
  • Publication number: 20130172310
    Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.
    Type: Application
    Filed: September 12, 2012
    Publication date: July 4, 2013
    Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
  • Patent number: 8466200
    Abstract: The present invention relates to 2-adamantylurea derivatives of formula I as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11?-HSD1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.
    Type: Grant
    Filed: February 7, 2012
    Date of Patent: June 18, 2013
    Assignee: Merck Patent GmbH
    Inventors: Denis Carniato, Christine Charon, Johannes Gleitz, Didier Roche, Bjoern Hock
  • Publication number: 20130131111
    Abstract: The invention relates to a nicotinamide mononucleotide (NMN) modulator useful as a neuroprotective medicament in the treatment of neurodegenerative disorders, in particular but not exclusively disorders involving axon degeneration of neuronal tissue such as Wallerian degeneration, to the use of NMN as a biomarker for axon degeneration, to a method of demonstrating axon degeneration using an NMN-based biomarker, to a diagnostic kit for detecting axon degeneration, to a method of screening for an NMN modulator, and to an NMN modulator identified using the aforementioned screening method.
    Type: Application
    Filed: April 19, 2011
    Publication date: May 23, 2013
    Applicant: Babraham Institute
    Inventors: Michael Coleman, Laura Conforti
  • Patent number: 8436026
    Abstract: It relates to an endogenous repair factor production accelerator which comprises one or at least two selected from prostaglandin (PG) 12 agonist, EP2 agonist and EP4 agonist. Since prostaglandin (PG) 12 agonist, EP2 agonist or EP4 agonist has various endogenous repair factor production accelerating action, angiogenesis acceleration action and stem cell differentiation induction action, it is useful as preventive and/or therapeutic agents for ischemic organ diseases (e.g., arteriosclerosis obliterans, Buerger disease, Raynaud disease, myocardial infarction, angina pectoris, diabetic neuropathy, spinal canal stenosis, cerebrovascular accidents, cerebral infarction, pulmonary hypertension, bone fracture, Alzheimer disease, etc.) and various cell and organ diseases.
    Type: Grant
    Filed: February 20, 2008
    Date of Patent: May 7, 2013
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Yoshiki Sakai, Akio Nishiura, Teppei Ogata
  • Publication number: 20130096163
    Abstract: The present invention relates to a flupirtine-containing lyophilisate, the use of this lyophilisate to produce a pharmaceutical composition to be parenterally applied, a procedure to produce a flupirtine-containing pharmaceutical composition to be parenterally applied, and a procedure to produce the flupirtine-containing lyophilisate as well as the flupirtine-containing pharmaceutical composition produced using the lyophilisate. For this purpose a lyophilisate is provided which contains the active ingredient flupirtine in the form of a physiologically tolerated salt, which has a solubility in water of at least 2.5 mg/ml, preferably at least 5 mg/ml, especially preferably at least 10 mg/ml, and contains one or more cyclodextrins or cyclodextrin derivatives, and which may be used to produce a pharmaceutical composition to be parenterally applied.
    Type: Application
    Filed: June 14, 2011
    Publication date: April 18, 2013
    Applicant: AWD.PHARMA GMBH & CO. KG
    Inventors: Christoph Martin Hoock, Asal Qadan, Bernd Terhaag, Rudy Thoma
  • Publication number: 20130096138
    Abstract: Disclosed are novel thiourea or urea derivatives inhibitory of HIV activity. Also provided are a method for preparing the thiourea or urea derivatives, and a pharmaceutical composition for the prophylaxis or therapy of AIDS comprising the derivatives. Having high inhibitory activity against HIV, the thiourea or urea derivatives can be effectively used in the prophylaxis or therapy of AIDS.
    Type: Application
    Filed: June 17, 2011
    Publication date: April 18, 2013
    Applicant: AVIXGEN INC.
    Inventors: Ji Chang You, Gyoon Hee Han, Chul Ho Lee, Doo Na Song, Koo Hwan Chung
  • Patent number: 8415344
    Abstract: Methods for treatment of depression-related mood disorders in mammals, particularly humans are disclosed. The methods of the invention include administration of compounds capable of enhancing glutamate transporter activity in the brain of mammals suffering from depression. ATP-sensitive K+ channel openers and ?-lactam antibiotics are used to enhance glutamate transport and to treat depression-related mood disorders and depressive symptoms.
    Type: Grant
    Filed: November 30, 2011
    Date of Patent: April 9, 2013
    Assignee: Brookhaven Science Associates, LLC
    Inventor: Fritz Henn