Patents by Inventor Jules A. Shafer

Jules A. Shafer has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 10201174
    Abstract: The present invention relates to processes for removal of Michael acceptors from certain compositions wherein the composition is treated with a thiol-containing compound under conditions sufficient to remove Michael acceptors and the resulting thiol-Michael adducts. Certain embodiments of the present invention enable quantification and/or removal of Michael acceptors and/or Michael acceptor precursors.
    Type: Grant
    Filed: August 1, 2016
    Date of Patent: February 12, 2019
    Assignee: Controlled Chemicals, Inc.
    Inventors: Jules A. Shafer, Vladislav V. Telyatnikov, Hao Wang
  • Patent number: 9617212
    Abstract: Compounds having an isoindolin-1-one backbone of Formula (I) are disclosed which have utility in treating and/or preventing microbial infections, tumor growth, metastasis and other macrophage migration inhibitory factor (MIF)-modulated pathological conditions. Pharmaceutical compositions and methods and use of compounds of Formula (I) are also disclosed.
    Type: Grant
    Filed: December 15, 2014
    Date of Patent: April 11, 2017
    Assignee: Controlled Chemicals, Inc.
    Inventors: Jingliang Jiao, Jules A. Shafer
  • Publication number: 20170027199
    Abstract: The present invention relates to processes for removal of Michael acceptors from certain compositions wherein the composition is treated with a thiol-containing compound under conditions sufficient to remove Michael acceptors and the resulting thiol-Michael adducts. Certain embodiments of the present invention enable quantification and/or removal of Michael acceptors and/or Michael acceptor precursors.
    Type: Application
    Filed: August 1, 2016
    Publication date: February 2, 2017
    Applicant: Controlled Chemicals, Inc.
    Inventors: Jules A. Shafer, Vladislav V. Telyatnikov, Hao Wang
  • Patent number: 9403838
    Abstract: The present invention relates to processes for removal of Michael acceptors from certain compositions wherein the composition is treated with a thiol-containing compound under conditions sufficient to remove Michael acceptors and the resulting thiol-Michael adducts. Certain embodiments of the present invention enable quantification and/or removal of Michael acceptors and/or Michael acceptor precursors.
    Type: Grant
    Filed: December 30, 2014
    Date of Patent: August 2, 2016
    Assignee: Controlled Chemicals, Inc.
    Inventors: Jules A. Shafer, Vladislav V. Telyatnikov, Hao Wang
  • Publication number: 20150175540
    Abstract: Compounds having an isoindolin-1-one backbone of Formula (I) are disclosed which have utility in treating and/or preventing microbial infections, tumor growth, metastasis and other macrophage migration inhibitory factor (MIF)-modulated pathological conditions. Pharmaceutical compositions and methods and use of compounds of Formula (I) are also disclosed.
    Type: Application
    Filed: December 15, 2014
    Publication date: June 25, 2015
    Applicant: Controlled Chemicals, Inc.
    Inventors: Jingliang Jiao, Jules A. Shafer
  • Publication number: 20150148537
    Abstract: The present invention relates to processes for removal of Michael acceptors from certain compositions wherein the composition is treated with a thiol-containing compound under conditions sufficient to remove Michael acceptors and the resulting thiol-Michael adducts. Certain embodiments of the present invention enable quantification and/or removal of Michael acceptors and/or Michael acceptor precursors.
    Type: Application
    Filed: December 30, 2014
    Publication date: May 28, 2015
    Applicant: Controlled Chemicals, Inc.
    Inventors: Jules A. Shafer, Vladislav V. Telyatnikov, Hao Wang
  • Patent number: 9034893
    Abstract: The present invention relates to processes for removal of Michael acceptors from certain compositions wherein the composition is treated with a thiol-containing compound under conditions sufficient to remove Michael acceptors and the resulting thiol-Michael adducts. Certain embodiments of the present invention enable quantification and/or removal of Michael acceptors and/or Michael acceptor precursors.
    Type: Grant
    Filed: December 6, 2010
    Date of Patent: May 19, 2015
    Assignee: Controlled Chemicals, Inc.
    Inventors: Jules A. Shafer, Vladislav V. Telyatnikov, Hao Wang
  • Publication number: 20110136849
    Abstract: The present invention relates to processes for removal of Michael acceptors from certain compositions wherein the composition is treated with a thiol-containing compound under conditions sufficient to remove Michael acceptors and the resulting thiol-Michael adducts. Certain embodiments of the present invention enable quantification and/or removal of Michael acceptors and/or Michael acceptor precursors.
    Type: Application
    Filed: December 6, 2010
    Publication date: June 9, 2011
    Inventors: Jules A. Shafer, Vladislav V. Telyatnikov, Hao Wang
  • Patent number: 7875623
    Abstract: The present invention relates to processes for removal of Michael acceptors from certain compositions wherein the composition is treated with a thiol-containing compound under conditions sufficient to remove Michael acceptors and the resulting thiol-Michael adducts. Certain embodiments of the present invention enable quantification and/or removal of Michael acceptors and/or Michael acceptor precursors.
    Type: Grant
    Filed: November 22, 2006
    Date of Patent: January 25, 2011
    Assignee: Controlled Chemicals, Inc.
    Inventors: Jules A. Shafer, Vladislav V. Telyatnikov, Hao Wang
  • Patent number: 7479372
    Abstract: The present invention provides synthetic ?-secretase peptide substrates useful in various assays for measuring ?-secretase activity. Antibodies that recognize the synthetic substrates and uses of the antibodies in various assays are disclosed. The herein disclosed peptide substrates are hydrolyzed at rates substantially faster than the attendant Swedish mutant APP from which the substrate sequences are derived.
    Type: Grant
    Filed: September 19, 2006
    Date of Patent: January 20, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Stephen F. Brady, James E. Bruce, Elizabeth Chen-Dodson, Victor Garsky, Yueming Li, Mohinder Sardana, Jules A. Shafer, Xiaoting Tang
  • Patent number: 7230005
    Abstract: The abuse potential of a bioavailable drug such as an opiate analgesic agent is reduced and its duration of action is extended by converting it to a poorly absorbed ester prodrug or other prodrug derivative prior to formulation. Unlike many existing sustained release formulations of active pharmaceutical agents wherein an active pharmaceutical agent can be released by chewing, crushing, or otherwise breaking tablets or capsule beads containing the active pharmaceutical agent, such mechanical processing of tablets or capsule beads containing a prodrug of this invention neither releases the active drug nor compromises the controlled conversion of prodrug to drug. Moreover, tablets and capsule beads containing prodrugs of this invention or other drugs can be formulated with a sufficient amount of a thickening agent such as hydroxypropylmethylcellulose or carboxymethylcellulose to impede inappropriate intravenous and nasal administration of formulations that are not indicated for these modes of administration.
    Type: Grant
    Filed: March 15, 2004
    Date of Patent: June 12, 2007
    Assignee: Controlled Chemicals, Inc.
    Inventors: Jules A. Shafer, Vladislav V. Telyatnikov, Zhiwei Guo
  • Patent number: 7132401
    Abstract: The present invention provides synthetic ?-secretase peptide substrates useful in various assays for measuring ?-secretase activity. Antibodies that recognize the synthetic substrates and uses of the antibodies in various assays are disclosed. The herein disclosed peptide substrates are hydrolyzed at rates substantially faster than the attendant Swedish mutant APP from which the substrate sequences are derived.
    Type: Grant
    Filed: May 17, 2002
    Date of Patent: November 7, 2006
    Assignee: Merck & Co., Inc.
    Inventors: Stephen F. Brady, James E. Bruce, Elizabeth Chen-Dodson, Victor Garsky, Yueming Li, Mohinder Sardana, Jules A. Shafer, Xiaoting Tang
  • Publication number: 20040204434
    Abstract: The abuse potential of a bioavailable drug such as an opiate analgesic agent is reduced and its duration of action is extended by converting it to a poorly absorbed ester prodrug or other prodrug derivative prior to formulation. Unlike many existing sustained release formulations of active pharmaceutical agents wherein an active pharmaceutical agent can be released by chewing, crushing, or otherwise breaking tablets or capsule beads containing the active pharmaceutical agent, such mechanical processing of tablets or capsule beads containing a prodrug of this invention neither releases the active drug nor compromises the controlled conversion of prodrug to drug. Moreover, tablets and capsule beads containing prodrugs of this invention or other drugs can be formulated with a sufficient amount of a thickening agent such as hydroxypropylmethylcellulose or carboxymethylcellulose to impede inappropriate intravenous and nasal administration of formulations that are not indicated for these modes of administration.
    Type: Application
    Filed: March 15, 2004
    Publication date: October 14, 2004
    Applicant: Controlled Chemicals Inc.
    Inventors: Jules A. Shafer, Vladislav V. Telyatnikov, Zhiwei Guo
  • Patent number: 6753410
    Abstract: The present invention is directed to compounds and pharmaceutical compositions comprising the compounds which are inhibitors of the enzyme gamma secretase and which are useful in the treatment or prevention of diseases in which the beta-amyloid peptide is involved, such as Alzheimer's disease.
    Type: Grant
    Filed: March 2, 2001
    Date of Patent: June 22, 2004
    Assignee: Merck & Co., Inc.
    Inventors: Alan John Nadin, Joseph George Neduvelil, Mohinder K. Sardana, Jules A. Shafer, Stephen J. Gardell, Ming-Tain Lai, Yueming Li, Bruce D. Dorsey, Dennis C. Dean
  • Publication number: 20020013276
    Abstract: The present invention provides a compound of formula I or a salt thereof: 1
    Type: Application
    Filed: March 2, 2001
    Publication date: January 31, 2002
    Inventors: Alan John Nadin, Joseph George Neduvelil, Mohinder K. Sardana, Jules A. Shafer, Stephen J. Gardell, Ming-Tain Lai, Yueming Li, Bruce D. Dorsey, Dennis C. Dean
  • Patent number: 5798377
    Abstract: A compound which inhibits human thrombin and where has the structure ##STR1## such as ##STR2##
    Type: Grant
    Filed: October 21, 1996
    Date of Patent: August 25, 1998
    Assignee: Merck & Co., Inc.
    Inventors: William C. Lumma, Thomas J. Tucker, Keith M. Witherup, Stephen F. Brady, Willie L. Whitter, Joseph P. Vacca, Craig Coburn, Jules A. Shafer
  • Patent number: 5728557
    Abstract: A method for introducing a mutation into a desired site in Herpes Simplex Virus Type 1 uses a set of starting vectors, where each starting vector has a fragment of the substantially complete HSV-1 genome and also DNA which overlaps with a sequential genomic fragment contained in other starting vectors, so that upon co-transfection of a host cell, replication of viral DNA, and recombination, a mutated replicable virus is formed. The starting vector containing a gene which is to be mutated is replaced by a replacement vectors. The replacement vectors contain a copy of the mutated gene and overlapping DNA, and genomic DNA which was present in the starting vector. A host cell is transformed with the replacement vectors and the remaining starting vectors under conditions allowing replication of viral DNA and recombination to form a replicating mutated virus. In preferred embodiments, the protease gene is mutated.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: March 17, 1998
    Assignee: Merck & Co., Inc.
    Inventors: R. Bruce Register, Jules A. Shafer
  • Patent number: 5672582
    Abstract: 4-substituted cyclohexylamine derivatives which are thrombin catalytic site inhibitors and which are useful as anticoagulants. These compounds show selectivity for thrombin over other trypsin-like enzymes and have oral bioavailability.
    Type: Grant
    Filed: October 12, 1994
    Date of Patent: September 30, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Daniel F. Veber, S. Dale Lewis, Jules A. Shafer, Dong-Mei Feng, Ruth F. Nutt, Stephen F. Brady
  • Patent number: 5646000
    Abstract: The invention is directed to a series of novel compounds, and their pharmaceutically acceptable salts, of the formula ##STR1## wherein R is C.sub.0-6 alkyl substituted with R.sup.5 or a mono or polycyclic aromatic or heteroaromatic system comprised of 5 or 6-membered aromatic or heteroaromatic rings that are either unsubstituted or substituted with one or more of R.sup.1 and R.sup.2 ; R.sup.1 and R.sup.2 are independently C.sub.1-6 alkyl, carboxyl, hydroxyl, azido, nitro, amino, C.sub.1-6 alkylamino, C.sub.1-6 dialkylamino, arylamino, aryl C.sub.1-6 alkylamino, hydroxysulfonyl or arylazo; aryl is a phenyl or naphthyl ring which is unsubstituted or substituted with one or more of R.sup.3 and R.sup.4 ; R.sup.3 and R.sup.4 are independently C.sub.1-6 alkyl, azido, nitro, amino, C.sub.1-6 dialkylamino or hydroxysulfonyl; R.sup.5 is ##STR2## provided that when R is an unsubstituted monocyclic ring, the monocyclic ring is not phenyl or pyridyl.
    Type: Grant
    Filed: September 29, 1994
    Date of Patent: July 8, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Bohumil Bednar, Melissa Egbertson, Robert J. Gould, George D. Hartman, Jules A. Shafer
  • Patent number: 4795714
    Abstract: An adjustable accumulated thermal exposure indicator device, and method of use, for affixing to and indicating deterioration of perishable goods and the like, comprising (1) a reactant yielding material that reacts via one or more steps at a rate depending on time, temperature, and pH to provide an amine and (2) an indicator that reacts at a time, temperature, concentration and pH dependent rate with the amine to produce a visible reaction that is indicative of the expiration of a predetermined time-temperature history related to the useful life of the goods to which the device is affixed. Also provided is a device or article that is responsive to accumulated thermal exposure for the controlled release of immobilized alcohols and amines.
    Type: Grant
    Filed: July 22, 1985
    Date of Patent: January 3, 1989
    Inventor: Jules A. Shafer