Sulfur Containing Hetero Ring Patents (Class 514/430)
  • Patent number: 10292973
    Abstract: Compounds and pharmaceutical compositions for treating cancer by, for example, modulating immune system activity, are provided.
    Type: Grant
    Filed: July 28, 2016
    Date of Patent: May 21, 2019
    Assignee: PROGENRA, Inc.
    Inventors: Joseph Weinstock, Jian Wu, Suresh Kumar Kizhakkethil-George, Feng Wang, Matthew P. Kodrasov, Saket Agarwal
  • Patent number: 10227374
    Abstract: The present invention relates to a prodrug of 5-azacytidine or 2?-deoxy-5-azacytidine having remarkable stability against cytidine deaminase, a metabolic hydrolyzing enzyme in replacement of current injections (5-azacytidine or 2?-deoxy-5-azacytidine) which are clinically used as therapeutic agents for various myelomas including myelodysplastic syndrome. The present invention provides a compound represented by formula (1), or salt thereof, wherein, R is OR3 or a hydrogen atom, R1, R2, and R3 are each independently hydrogen atom or silyl group represented by formula (2): wherein, R4, R5, and R6 are each independently alkyl group which may have a substituent, aryl group which may have a substituent, or arylalkyl group which may have a substituent, with the provision that R1, R2, and R3 are not hydrogen atom simultaneously.
    Type: Grant
    Filed: February 22, 2018
    Date of Patent: March 12, 2019
    Assignee: Ohara Pharmaceutical Co., Ltd.
    Inventors: Magoichi Sako, Shinpei Sugiyama
  • Patent number: 10188591
    Abstract: Methods and compositions for stimulating the growth of hair are disclosed wherein said compositions include a cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl compound represented by the formula I wherein the dashed bonds represent a single or double bond which can be in the cis or trans configuration, A, B, Z, X, R1 and R2 are as defined in the specification. Such compositions are used in treating the skin or scalp of a human or non-human animal. Bimatoprost is preferred for this treatment.
    Type: Grant
    Filed: March 2, 2016
    Date of Patent: January 29, 2019
    Assignee: ALLERGAN, INC.
    Inventors: David F. Woodward, Amanda M. VanDenburgh
  • Patent number: 10159631
    Abstract: Methods and compositions for stimulating the growth of hair are disclosed wherein said compositions include a cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl compound represented by the formula I wherein the dashed bonds represent a single or double bond which can be in the cis or trans configuration, A, B, Z, X, R1 and R2 are as defined in the specification. Such compositions are used in treating the skin or scalp of a human or non-human animal. Bimatoprost is preferred for this treatment.
    Type: Grant
    Filed: March 2, 2016
    Date of Patent: December 25, 2018
    Assignee: ALLERGAN, INC.
    Inventors: David F. Woodward, Amanda M. VanDenburgh
  • Patent number: 10137119
    Abstract: The invention aims to prevent and/or treat malaria using an antimalarial drug comprising, as an active ingredient, a metal chelator represented by the following formula (I), (III), (IV), (V), (VI), or (VII), such as tris(2-pyridylmethyl)amine.
    Type: Grant
    Filed: December 19, 2017
    Date of Patent: November 27, 2018
    Assignee: RIKEN
    Inventors: Akira Wada, Hiroki Hayase, Nobumoto Watanabe, Hiroyuki Osada, Takeshi Shimizu, Konstanty Wierzba
  • Patent number: 9901641
    Abstract: The present invention relates to a prodrug of 5-azacytidine or 2?-deoxy-5-azacytidine having remarkable stability against cytidine deaminase, a metabolic hydrolyzing enzyme in replacement of current injections (5-azacytidine or 2?-deoxy-5-azacytidine) which are clinically used as therapeutic agents for various myelomas including myelodysplastic syndrome. The present invention provides a compound represented by formula (1), or salt thereof, wherein, R is OR3 or a hydrogen atom, R1, R2, and R3 are each independently hydrogen atom or silyl group represented by formula (2): wherein, R1, R5, and R6 are each independently alkyl group which may have a substituent, aryl group which may have a substituent, or arylalkyl group which may have a substituent, with the provision that R1, R2, and R3 are not hydrogen atom simultaneously.
    Type: Grant
    Filed: November 18, 2016
    Date of Patent: February 27, 2018
    Assignee: Ohara Pharmaceutical Co., Ltd.
    Inventors: Magoichi Sako, Shinpei Sugiyama
  • Patent number: 9717717
    Abstract: Methods and compounds for treating cancer by, for example, modulating immune system activity, are provided.
    Type: Grant
    Filed: July 28, 2016
    Date of Patent: August 1, 2017
    Assignees: Progenra, Inc., The Children's Hospital of Philadelphia
    Inventors: Joseph Weinstock, Jian Wu, Suresh Kumar Kizhakkethil-George, Feng Wang, Matthew P. Kodrasov, Saket Agarwal, Wayne W. Hancock
  • Patent number: 9675539
    Abstract: A method for treating hair loss in mammals uses compositions containing 2-decarboxy-2-phosphinico prostaglandin derivatives. The compositions can be applied topically to the skin. The compositions can arrest hair loss, reverse hair loss, and promote hair growth. Compositions containing 2-decarboxy-2-phosphinico prostaglandin derivatives can also be used to lower intraocular pressure and treat bone disorders.
    Type: Grant
    Filed: April 14, 2016
    Date of Patent: June 13, 2017
    Assignee: Duke University
    Inventors: Mitchell A. deLong, John M. McIver, Robert S. Youngquist
  • Patent number: 9227949
    Abstract: Compounds represented by the following formula (I); wherein each symbol is as defined in the specification, are useful as hyperglycemic inhibitors having a serine protease inhibitory action and as prophylactic or therapeutic drugs for diabetes.
    Type: Grant
    Filed: December 11, 2014
    Date of Patent: January 5, 2016
    Assignee: AJINOMOTO CO., INC.
    Inventors: Takahiro Koshiba, Munetaka Tokumasu, Taisuke Ichimaru, Koji Ohsumi, Tadakiyo Nakagawa, Tatsuhiro Yamada, Kayo Matsumoto, Tamotsu Suzuki
  • Publication number: 20150093372
    Abstract: The invention provides compounds, compositions, and methods for the treatment of diseases, disorders, or conditions that are modulated by matrix metalloproteinases (MMPs). The disease, disorder, or condition can include, for example, stroke, neurological disorders, or ophthalmological disorders. The treatment can include administering a compound or composition described herein, thereby providing a prodrug compound that metabolizes to an active MMP inhibitor in vivo. The MMP inhibition can be selective inhibition, for example, selective inhibition of MMP-2, MMP-9, and/or MMP-14. Thus, the invention provides non-mutagenic prodrug compounds of the formulas described herein that result in the inhibition of MMPs upon in vivo administration.
    Type: Application
    Filed: December 11, 2014
    Publication date: April 2, 2015
    Applicant: UNIVERSITY OF NOTRE DAME DU LAC
    Inventors: Mayland Chang, Shahriar Mobashery, Mijoon Lee
  • Patent number: 8980938
    Abstract: The invention relates to compounds of the formula I in which R1, R2, A, B, X and Y have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.
    Type: Grant
    Filed: December 18, 2008
    Date of Patent: March 17, 2015
    Assignee: Sanofi
    Inventors: Stephanie Hachtel, Juergen Dedio, Josef Pernerstorfer, Stephen Shimshock, Carolina Lanter
  • Publication number: 20150065554
    Abstract: Disclosed herein are methods of treating a patient at risk of developing or having a neurofibromatosis or a sporadic schwannoma. In exemplary embodiments, the method involves administering to a subject in need an effective amount of a modulator of a target related to neurofibromatosis. Also disclosed are screening assays involving the implementation of Merlin-null Schwann cells, and to compounds identified using same.
    Type: Application
    Filed: March 13, 2013
    Publication date: March 5, 2015
    Applicant: University of Central Florida Research Foundation, Inc.
    Inventor: Cristina Fernandez-Valle
  • Patent number: 8946219
    Abstract: The present invention is directed to pharmaceutical compositions and methods of using combination therapies containing [4-(6-fluoro-7-methylamino-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl)-phenyl]-5-chloro-thiophen-2-yl-sulfonylurea, or a pharmaceutically acceptable salt thereof, for the treatment of thrombosis diseases.
    Type: Grant
    Filed: October 20, 2010
    Date of Patent: February 3, 2015
    Assignee: Portola Pharmaceuticals, Inc.
    Inventors: Pamela B. Conley, Patrick Andre, Uma Sinha
  • Patent number: 8895587
    Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4, G1, n, A1, A2, A3, A4, Y1, Y2, and Y3 are as defined in the claims. The invention also relates to processes and intermediates for preparing these compounds, to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising these compounds and to methods of using these compounds to control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: May 15, 2012
    Date of Patent: November 25, 2014
    Assignee: Syngenta Participations AG
    Inventors: Jerome Yves Cassayre, Myriem El Qacemi, Torsten Luksch, Peter Renold
  • Publication number: 20140343049
    Abstract: The present invention relates to compounds of formula (IA) wherein QA is QA1 or QA2 P is P1, heterocycyl or heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, Z, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (IA), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (IA) and to methods of using the compounds of formula (IA) to control insect, acarine, nematode and mollusc pests.
    Type: Application
    Filed: August 10, 2012
    Publication date: November 20, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Julie Clementine Toueg, Tomas Smejkal, Sebastian Volker Wendeborn, Jerome Yves Cassayre, Myriem El Qacemi, Bernhard Breit, Lisa Diab, Regis Jean Georges Mondiere, Nicolas Poirier
  • Patent number: 8871903
    Abstract: Methods to synthesize self-assembling peptides embedded with complex organic electronic subunits are provided.
    Type: Grant
    Filed: October 22, 2012
    Date of Patent: October 28, 2014
    Assignee: The Johns Hopkins University
    Inventors: John D. Tovar, Allix M. Sanders
  • Patent number: 8815937
    Abstract: The present invention relates, in various embodiments, to a compound represented by Structural Formula (I), pharmaceutically acceptable salts or prodrugs thereof, and compositions comprising said compounds, or pharmaceutically acceptable salts or prodrugs thereof. Methods of using compounds of Structural Formulas (I) and (la) or compositions comprising compounds of Structural Formulas (I) and (la), or pharmaceutically acceptable salts or prodrugs thereof, to treat ischemia or ischemia-reperfusion injury are also disclosed.
    Type: Grant
    Filed: November 10, 2011
    Date of Patent: August 26, 2014
    Assignee: Ischemix LLC
    Inventors: Alexander B. Baguisi, Reinier Beeuwkes, Ralph Casale, Steven A. Kates, Alan S. Lader
  • Patent number: 8785480
    Abstract: In one embodiment, processes for the preparation of certain functionalized pyridine N-oxides are provided. In one form, the functionalized pyridine N-oxides include 2-substituted-5-(1-alkylthio)alkyl-pyridine N-oxides. Further embodiments, forms, objects, features, advantages, aspects, and benefits shall become apparent from the description.
    Type: Grant
    Filed: June 13, 2013
    Date of Patent: July 22, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Douglas C. Bland, Ronald Ross, Jr., Peter L. Johnson, Timothy C. Johnson
  • Publication number: 20140194376
    Abstract: The present invention provides compounds of formula (I) wherein G1 is oxygen; R1 is hydrogen; R2 is group (P) L is a bond, methylene or ethylene; one of A1 and A2 is S, SO or SO2 and the other is —C(R4)R4—; R3 is hydrogen or methyl; each R4 is independently hydrogen or methyl; Y2 and Y3 are independently CH or nitrogen, wherein Y2 and Y3 are not both nitrogen; X2 is C—X6 or nitrogen; X1, X3 and X6 are independently hydrogen, halogen or trihalomethyl, wherein at least two of X1, X3 and X6 are not hydrogen; X4 is trifluoromethyl, difluoromethyl or chlorodifluoromethyl. The invention also provides intermediates useful for the preparation of compounds of formula (I), as well as methods of controlling insects, acarines, nematodes or molluscs using the compounds of formula (I).
    Type: Application
    Filed: August 24, 2012
    Publication date: July 10, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Jerome Yves Cassayre, Peter Renold, Thomas Pitterna, Myriem El Qacemi
  • Publication number: 20140171312
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 19, 2014
    Applicant: Dow AgroSciences LLC
    Inventors: William C. Lo, James E. Hunter, Gerald B. Watson, Akshay Patny, Pravin S. Iyer, Joshodeep Boruwa
  • Publication number: 20140171309
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 19, 2014
    Applicant: DOW AGROSCIENCES LLC
    Inventors: William C. Lo, James E. Hunter, Gerald B. Watson, Akshay Patny, Pravin S. Iyer, Joshodeep Boruwa
  • Publication number: 20140171311
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 19, 2014
    Applicant: DOW AGROSCIENCES LLC
    Inventors: William C. Lo, James E. Hunter, Gerald B. Watson, Akshay Patny, Pravin S. Iyer, Joshodeep Boruwa
  • Publication number: 20140171314
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 19, 2014
    Applicant: Dow AgroSciences LLC
    Inventors: William C. Lo, James E. Hunter, Gerald B. Watson, Akshay Patny, Pravin S. Iyer, Joshodeep Boruwa
  • Publication number: 20140171308
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 19, 2014
    Applicant: Dow AgroSciences LLC
    Inventors: William C. Lo, James E. Hunter, Gerald B. Watson, Akshay Patny, Pravin S. Iyer, Joshodeep Boruwa
  • Publication number: 20140107161
    Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R2, R3, R4, G1, n, A1, A2, A3, A4, Y1, Y2, and Y3 are as defined in the claims. The invention also relates to processes and intermediates for preparing these compounds, to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising these compounds and to methods of using these compounds to control insect, acarine, nematode and mollusc pests.
    Type: Application
    Filed: May 12, 2012
    Publication date: April 17, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Jerome Yves Cassayre, Myriem El Qacemi, Torsten Luksch, Peter Renold
  • Publication number: 20140094446
    Abstract: Compositions comprising cyclic amino acids or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier. Said compositions are for use in the treatment of pain. Pain includes both acute and chronic forms of pain. The preferred cyclic amino acid is 1-aminocyclobutane-1-carboxylic acid (ACBC).
    Type: Application
    Filed: July 29, 2013
    Publication date: April 3, 2014
    Applicant: Therexcell Pharma Inc.
    Inventors: Ernest Puil, Bernard A. MacLeod, Richard Wall
  • Patent number: 8680139
    Abstract: Disclosed are novel compounds which are useful as therapeutics, especially in anti-neoplastic therapy and in other therapeutic regimes where cysteine protease inhibition is implicated.
    Type: Grant
    Filed: March 31, 2010
    Date of Patent: March 25, 2014
    Assignee: Progenra
    Inventors: Ping Cao, Joseph Weinstock, William D. Kingsbury, Craig A. Leach, Suresh Kumar Kizhakkethil-George, Benjamin Nicholson
  • Patent number: 8642643
    Abstract: The invention relates to compounds of the formula I in which R1, R2, A, B, X and Y have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.
    Type: Grant
    Filed: December 18, 2008
    Date of Patent: February 4, 2014
    Assignee: Sanofi
    Inventors: Stephanie Hachtel, Juergen Dedio, Josef Pernerstorfer, Stephen Shimshock, Carolina Lanter, Raymond Kosley
  • Patent number: 8623896
    Abstract: A compound of formula (I), wherein A1, A2, A3, A4, G1, L, R1, R2, R3, R4, Y1, Y2 and Y3 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc and nematode pests.
    Type: Grant
    Filed: December 16, 2008
    Date of Patent: January 7, 2014
    Assignee: Syngenta Crop Protection, LLC
    Inventors: Peter Renold, Werner Zambach, Peter Maienfisch, Michel Muehlebach
  • Publication number: 20140005235
    Abstract: The present invention relates to novel triazole derivatives of formula (I) having insecticidal activity, to processes and intermediates for preparing them, to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests wherein A1, A2, A3, A4, A5, A6, G1, G2, R1, R2, R3, L, Q1, Q2, R4, R5, R6, R7, Q2, Y1, Y2, Y3, Y4, Y5, Y6, Y7, Y8, and Y9 are as defined in claim 1; or salts or N-oxides thereof.
    Type: Application
    Filed: March 19, 2012
    Publication date: January 2, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Pierre Joseph, Marcel Jung, Ottmar Franz Hueter, Peter Renold, Thomas Pitterna
  • Publication number: 20130338116
    Abstract: The present invention relates generally to pharmaceutical agents, and in particular, to metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of dual acting MMP-2 and MMP-9 inhibiting compounds that exhibit increased potency, metabolic stability and/or reduced toxicity in relation to currently known MMP-2 and MMP-9 inhibitors for the treatment of pain and other diseases. Additionally, the present invention relates to methods for treating pain, addiction and/or withdrawal symptoms in a patient comprising administering to the patient a pain-reducing effective amount of a present compound.
    Type: Application
    Filed: August 16, 2013
    Publication date: December 19, 2013
    Inventor: Irving Sucholeiki
  • Patent number: 8603947
    Abstract: A description is given of (4-haloalkyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, Y, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.
    Type: Grant
    Filed: July 20, 2011
    Date of Patent: December 10, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Hartmut Ahrens, Dieter Feucht, Elmar Gatzweiler, Isolde Haeuser-Hahn, Christopher Hugh Rosinger
  • Patent number: 8569349
    Abstract: Compounds comprising formula (I) or a pharmaceutically acceptable salt thereof, a dashed line represent the presence or absence of a double bond, are disclosed, wherein J1, J2, U1, B, Y, and A are as described in claims 1-12. Methods, compositions, and medicaments related thereto are also disclosed, for treating glaucoma, inflammatory bowel disease and baldness.
    Type: Grant
    Filed: May 4, 2009
    Date of Patent: October 29, 2013
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Vinh X. Ngo
  • Patent number: 8569335
    Abstract: The present invention relates to compounds derived from taurine with non-steroidal anti inflammatory activity. In a first embodiment, the present invention relates to compounds derived from taurine, in which taurine is bound directly by means of an amide bond or through an spacing group, to a compound selected from the group of non-steroidal anti inflammatory compounds, cited as derived from taurine presenting the Formula (I): in which R means the component with non-steroidal anti inflammatory activity. In a second embodiment, the invention provides a process for obtaining the compounds of Formula (I) by reaction of taurine with a compound belonging to the group of non-steroidal anti inflammatory (NSAIs), in order to obtain a compound derived from taurine by direct bond or through a spacing group of the taurine to the NSAI. The invention also relates to the pharmaceutical compositions comprising at least one compound derived from taurine presenting non-steroidal anti inflammatory activity.
    Type: Grant
    Filed: April 9, 2009
    Date of Patent: October 29, 2013
    Assignees: EMS S.A., Universidade Estadual Paulista Julio de Mesquinta Filho—UNESP
    Inventors: Ednir D. Vizioli, Chung M. Chin, Renato F. Menegon, Lorena Blau, Jean L. Santos, Maria D. Longo
  • Publication number: 20130261099
    Abstract: Fatty acid inhibitors, pharmaceutical compositions including fatty acid inhibitors, methods for using fatty acid inhibitors to treat a variety of diseases, and methods for preparing fatty acid inhibitors are provided herein.
    Type: Application
    Filed: May 24, 2013
    Publication date: October 3, 2013
    Applicant: LIFE TECHNOLOGIES CORPORATION
    Inventor: Bruce BRANCHAUD
  • Patent number: 8507546
    Abstract: The present invention relates to the use of inhibitors of scavenger receptor class proteins, in particular ScarB1 for the production of a medicament for treatment of and/or prophylaxis against infections, involving liver cells and/or hematopoietic cells, in particular malaria.
    Type: Grant
    Filed: July 13, 2012
    Date of Patent: August 13, 2013
    Assignees: Instituto de Medicina Molecular, Faculdade de Medicina da Universidade de Lisboa, Cenix Bioscience GmbH
    Inventors: Michael Hannus, Cecilie Martin, Maria M. Mota, Miguel Prudencio, Christina Dias Rodrigues
  • Publication number: 20130165485
    Abstract: A compound of formula (I): where A, B, C, G, m, n, o, p, R1, R2, R3, R4, R5, R6, X, R7, R8, R9, R10 and R11 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.
    Type: Application
    Filed: February 20, 2013
    Publication date: June 27, 2013
    Applicant: Syngenta Crop Protection LLC
    Inventors: Jerome Yves Cassayre, Peter Renold, Vladimir Bobosik, Myriem El Qacemi, Anne Jacqueline Dalencon, Werner Zambach, Christopher Richard Godfrey, Thomas Pitterna, Pierre Joseph Jung, Jagadish Pabba
  • Publication number: 20130064878
    Abstract: The invention provides a method of accelerating the healing process of a skin or subdermal wound. The method can include administering to a mammal afflicted with a skin or subdermal wound an effective amount of a gelatinase inhibitor, or a pharmaceutically acceptable salt thereof, wherein the gelatinase inhibitor is effective to accelerate the healing process of the skin wound. The method is particularly effective when the mammal is suffering from diabetes. The gelatinase inhibitor can be topically administered, for example, in the form of a cream, gel, lotion, ointment, salve, or solution.
    Type: Application
    Filed: August 13, 2012
    Publication date: March 14, 2013
    Applicant: UNIVERSITY OF NOTRE DAME DU LAC
    Inventors: Mayland Chang, Mark A. Suckow, Shahriar Mobashery
  • Publication number: 20130052184
    Abstract: The invention provides compounds, compositions, and methods for the treatment of diseases, disorders, or conditions that are modulated by matrix metalloproteinases (MMPs). The disease, disorder, or condition can include, for example, stroke, neurological disorders, or ophthalmological disorders. The treatment can include administering a compound or composition described herein, thereby providing a prodrug compound that metabolizes to an active MMP inhibitor in vivo. The MMP inhibition can be selective inhibition, for example, selective inhibition of MMP-2, MMP-9, and/or MMP-14. Thus, the invention provides non-mutagenic prodrug compounds of the formulas described herein that result in the inhibition of MMPs upon in vivo administration.
    Type: Application
    Filed: March 4, 2011
    Publication date: February 28, 2013
    Applicant: UNIVERSITY OF NOTRE DAME DU LAC
    Inventors: Mayland Chang, Shahriar Mobashery, Mijoon Lee
  • Publication number: 20130005752
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Application
    Filed: June 19, 2012
    Publication date: January 3, 2013
    Applicant: Viamet Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Zachary A. Buchan, Michael T. Sullenberger
  • Publication number: 20120329769
    Abstract: The present invention relates to compounds of formula (I) wherein Q is Q1 or Q2 P is P1, heterocyclylor heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, Y1, Z, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.
    Type: Application
    Filed: January 31, 2011
    Publication date: December 27, 2012
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Myriem El Qacemi, Jerome Yves Cassayre, Julie Clementine Toueg, Peter Renold, Thomas Pitterna
  • Publication number: 20120329649
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
    Type: Application
    Filed: June 21, 2012
    Publication date: December 27, 2012
    Inventors: James E. Hunter, William C. Lo, Gerald B. Watson, Akshay Patny, Gary D. Gustafson, Dan Pernich, William K. Brewster, Debra L. Camper, Beth Lorsbach, Michael R. Loso, Thomas C. Sparks, Hemant Joshi, Adiraj Mandaleswaran, Ramadevi Sanam, Rambabu Gundla, Pravin S. Iyer
  • Patent number: 8338443
    Abstract: The use of a compound of formula I wherein Y is a single bond, C?O, C?S or S(O)m, where m is 0, 1 or 2; the ring is a 6-membered aromatic or is a 5 or 6 membered heteroaromatic ring; Z and Z? are joined by a single or a double bond and are ?C— or —N— provided that both are not N; Ra, R1, R2, R3, R3a, R4 and R8 are specified organic groups; n is 2, 3 or 4 and p is 0-4; or salts or N-oxides thereof or compositions containing them in controlling insects, acarines, nematodes or molluscs. Novel compounds are also provided.
    Type: Grant
    Filed: December 6, 2006
    Date of Patent: December 25, 2012
    Assignee: Syngenta Crop Protection LLC
    Inventors: Jérôme Cassayre, Peter Maienfisch, Fredrik Cederbaum, Louis-Pierre Molleyres
  • Patent number: 8288423
    Abstract: The present invention relates to novel oxazolidinone derivatives with cyclic amidines, and prodrugs, hydrates, solvates, isomers and pharmaceutically acceptable salts thereof, and processes for preparing the same, and pharmaceutical compositions comprising the same. The oxazolidinone derivatives with cyclic amidines, and prodrugs, hydrates, solvates, isomers and pharmaceutically acceptable salts thereof can be usefully employed as an anticoagulant for treating thromboembolism and tumors via inhibition of coagulation factor Xa.
    Type: Grant
    Filed: May 9, 2008
    Date of Patent: October 16, 2012
    Assignee: Legochem Bioscience Ltd.
    Inventors: Young Lag Cho, Ho Young Song, Dae Yon Lee, Sung Yoon Baek, Sang Eun Chae, Sang Hui Jo, Yeon Ok Kim, Hyang Sook Lee, Ju Hyun Park, Tae Kyo Park, Sung Ho Woo, Yong Zu Kim
  • Patent number: 8283375
    Abstract: The disclosure herein provides a compound of formula 1. The disclosure also provides a method of synthesizing the compound of formula 1. The compound of formula 1 or its pharmaceutical acceptable salts, as well as polymorphs, solvates, and hydrates thereof may be formulated as pharmaceutical composition. The pharmaceutical composition of compound of formula 1 or the final compound may be formulated for non-invasive peroral, topical (example transdermal), enteral, transmucosal, targeted delivery, sustained release delivery, delayed release, pulsed release and parenteral methods. Such compositions may be used to treat chronic pain manifested with chronic diseases or its associated complications. The compound may also be offered as a kit.
    Type: Grant
    Filed: March 13, 2012
    Date of Patent: October 9, 2012
    Assignee: Krisani Biosciences (P) Ltd.
    Inventor: Mahesh Kandula
  • Patent number: 8278355
    Abstract: The invention provides for the use of isovaline or a pharmaceutically acceptable salt thereof for the treatment of Pain in a mammalian subject in some preferred embodiments, the invention provides for the treatment of acute and chronic Pain syndromes where other drug therapies have limited efficacy or unacceptable toxicity in said subject.
    Type: Grant
    Filed: September 12, 2007
    Date of Patent: October 2, 2012
    Assignee: Therexcell Pharma Inc.
    Inventors: Ernest Puil, Bernard Ansel MacLeod, Thomas Michael Stokes, Wei Liu
  • Publication number: 20120237615
    Abstract: The present invention provides O-nitro compounds, pharmaceutical compositions of O-nitro compounds and methods of using O-nitro compounds and/or pharmaceutical compositions thereof to treat or prevent diseases or disorders characterized by abnormal cell proliferation, such as cancer, inflammation, cardiovascular disease and autoimmune disease.
    Type: Application
    Filed: May 30, 2012
    Publication date: September 20, 2012
    Applicants: RADIORX, INC., C/O INTERWEST VENTURE PARTNERS, ALLIANT TECHSYSTEMS INC.
    Inventors: Mark D. Bednarski, Lynn M. Oehler, Susan Knox, Louis Cannizzo, Kirstin Warner, Robert Wardle, Stephen Velarde, Shoucheng Ning
  • Publication number: 20120190724
    Abstract: The present invention provides a novel xanthone derivative compound or a pharmaceutically acceptable salt thereof. The compound is useful as a chemosensitizer that reduces anticancer drug resistance.
    Type: Application
    Filed: August 19, 2010
    Publication date: July 26, 2012
    Applicant: EWHA UNIVERSITY INDUSTRY COLLABORATION FOUNDATION
    Inventors: Young Hwa Na, Young Joo Kwon, Hwa Jeong Lee, Song Wha Chae, Sang Wook Woo, Hee Ju Cho
  • Patent number: 8147809
    Abstract: Soft anticholinergic esters of the formulas: wherein R1 and R2 are both phenyl or one of R1 and R2 is phenyl and the other is cyclopentyl; R is C1-C8 alkyl, straight or branched chain; and X? is an anion with a single negative charge; and wherein each asterisk marks a chiral center; said compound having the R, S or RS stereoisomeric configuration at each chiral center unless specified otherwise, or being a mixture thereof.
    Type: Grant
    Filed: June 30, 2009
    Date of Patent: April 3, 2012
    Inventor: Nicholas S. Bodor
  • Patent number: 8093287
    Abstract: The present invention provides novel compounds of formulas I-IX, as described herein. Also provided are compositions of compounds of formulas I-IX, methods of making compounds of formulas I-IX, and methods of using compounds of formulas I-IX. The compounds of the invention can be used to inhibit matrix metalloproteinases, and are useful to treat conditions and diseases associated therewith.
    Type: Grant
    Filed: March 14, 2011
    Date of Patent: January 10, 2012
    Assignees: University of Notre Dame du Lac, Wayne State University
    Inventors: Mijoon Lee, Masahiro Ikejiri, Mayland Chang, Rafael Fridman, Shahriar Mobashery