Patents by Inventor Ben E. Evans

Ben E. Evans 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).

  • Publication number: 20040138242
    Abstract: This invention is directed to dihydropyrimidines which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for relaxing lower urinary tract tissue, treating benign prostatic hyperplasia and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: November 6, 2003
    Publication date: July 15, 2004
    Applicants: Merck and Co., Inc., Synaptic Pharmaceutical Corporation
    Inventors: Donghui Cui, Margaret R. Davis, Michael Dunn, Ben E. Evans, Hanumath P. Kari, Bharat Lagu, Dhanapalan Nagarathnam, Kamlesh P. Vyas, Kanyin Zhang
  • Patent number: 6680323
    Abstract: This invention is directed to dihydropyrimidines which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for relaxing lower urinary tract tissue, treating benign prostatic hyperplasia and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: June 4, 2001
    Date of Patent: January 20, 2004
    Assignee: Synaptic Pharmaceutical Corporation
    Inventors: Donghui Cui, Margaret R. Davis, Michael Dunn, Ben E. Evans, Hanumath P. Kari, Bharat Lagu, Dhanapalan Nagarathnam, Kamlesh P. Vyas, Kanyin Zhang
  • Patent number: 6387893
    Abstract: Spirotricyclic azacycloalkyl compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds is also described. One application of these compounds, which are alpha 1a adrenergic receptor antagonists, is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
    Type: Grant
    Filed: September 27, 2000
    Date of Patent: May 14, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Ben E. Evans, Jacob M. Hoffman, Kevin F. Gilbert, Kenneth E. Rittle
  • Patent number: 6326372
    Abstract: Lactam and cyclic urea derivatives and their pharmaceutically acceptable salts are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are typically selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
    Type: Grant
    Filed: September 27, 2000
    Date of Patent: December 4, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Ben E. Evans, Kevin F. Gilbert
  • Publication number: 20010041707
    Abstract: This invention is directed to dihydropyrimidines which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for relaxing lower urinary tract tissue, treating benign prostatic hyperplasia and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: June 4, 2001
    Publication date: November 15, 2001
    Applicant: Merck and Co., Inc
    Inventors: Donghui Cui, Margaret R. Davis, Michael Dunn, Ben E. Evans, Hanumath P. Kari, Bharat Lagu, Dhanapalan Nagarathnam, Kamlesh P. Vyas, Kanyin Zhang
  • Patent number: 6274585
    Abstract: This invention is directed to dihydropyrimidines which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for relaxing lower urinary tract tissue, treating benign prostatic hyperplasia and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: December 23, 1999
    Date of Patent: August 14, 2001
    Assignee: Synaptic Pharmaceutical Corporation
    Inventors: Donghui Cui, Margaret R. Davis, Michael Dunn, Ben E. Evans, Hanumath P. Kari, Bharat Lagu, Dhanapalan Nagarathnam, Kamlesh P. Vyas, Kanyin Zhang
  • Patent number: 5952351
    Abstract: This invention relates to novel compounds, their synthesis and use as selective .alpha..sub.1a adrenergic receptor antagonists. One application of the compounds is in the treatment of benign prostatic hyperplasia. The compounds are selective in their ability to relax smooth muscle tissue enriched in the .alpha..sub.1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.
    Type: Grant
    Filed: August 13, 1997
    Date of Patent: September 14, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Ben E. Evans, Gerald S. Ponticello, Jacob M. Hoffman
  • Patent number: 5756504
    Abstract: Compounds of the formula X--Y--R, or the pharmaceutically acceptable salts and esters thereof, wherein X is ##STR1## Y is --SO.sub.2 --, --(CH.sub.2).sub.p -- or --CO--(CH.sub.2).sub.p --; R is unsubstituted or substituted phenyl where said substitutents are one or more of R.sup.5, R.sup.6 or R.sup.7 ; R.sup.1 is hydrogen, cyano, phenyl, --CONHR.sup.2, --CONR.sup.2 R.sup.2, --(CH.sub.2).sub.m --OR.sup.2, --(CH.sub.2).sub.p --S(O).sub.r --R.sup.2, --(CH.sub.2).sub.m --CO.sub.2 R.sup.2, --(CH.sub.2).sub.m --N.sub.3, --(CH.sub.2).sub.m --NH.sub.2 or --(CH.sub.2).sub.m --NR.sup.2 R.sup.2 ; R.sup.2 is hydrogen, C.sub.3-8 cycloalkyl or C.sub.1-5 alkyl; R.sup.5 and R.sup.6 are each independently selected from hydrogen, C.sub.1-5 alkoxy, halogen or --(CH.sub.2).sub.n --N(R.sup.2)--C(O)--R.sup.18 ; R.sup.7 is hydrogen or ##STR2## R.sup.11 is selected from hydrogen, C.sub.1-5 alkyl-carbonyl, --Z--R.sup.13, ##STR3## or substituted C.sub.
    Type: Grant
    Filed: September 23, 1996
    Date of Patent: May 26, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Mark G. Bock, Ben E. Evans, J. Christopher Culberson, Kevin F. Gilbert, Kenneth E. Rittle, Peter D. Williams
  • Patent number: 5693643
    Abstract: Compounds of formula (I) wherein X is (a) or (b), R is Het as defined in the description. These compounds are oxytocin and vasopressin antagonists useful in the treatment of preterm labor, dysmenorrhea, and for the stoppage of labor preparatory to Cesarean delivery.
    Type: Grant
    Filed: August 15, 1995
    Date of Patent: December 2, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Kevin Gilbert, Peter D. Williams, Ben E. Evans, Doug W. Hobbs, Daniel F. Veber
  • Patent number: 5670509
    Abstract: Compounds of the formula X-Y-Z-R.sup.1 wherein:X is ##STR1## Y is --CO-- or --SO.sub.2 --; Z is an optional substituent selected from --NH--, --O--, --CHR--, --CH.dbd.CH--, --CH.dbd., --(CH.sub.2).sub.m -- or--CHCHOH--; andR.sup.1 is --CH.sub.3 --, --CH(CH.sub.3).sub.2, or substituted phenyl are tocolytic oxytocin antagonists useful in the treatment of pre-term labor, stripping labor preparatory to Caesarean delivery and dysmenorrhea.
    Type: Grant
    Filed: April 5, 1995
    Date of Patent: September 23, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Ben E. Evans, Douglas W. Hobbs, Joseph M. Pawluczyk, Douglas J. Pettibone, Kenneth E. Rittle, Peter D. Williams
  • Patent number: 5665719
    Abstract: Compounds of the formula ##STR1## X is --O--, --NH-- and --NR.sup.8 --; Y is --CH.sub.2 --, --CHR.sup.8 -- and --C(R.sup.8).sub.2 --; R.sup.1 is camphor-10-yl, C.sub.1-5 alkoxyl, styryl, hydroxystyryl, furyl, unsubstituted or substituted thienyl, naphthyl, indolyl, tetrahydronaphthyl, unsubstituted, mono- or di-substituted pyridyl, pyrazinyl, unsubstituted or substituted cyclohexyl where the substituent is R.sup.4, and unsubstituted or substituted phenyl where the substituents on phenyl are R.sup.5, R.sup.6 and R.sup.7 ; R.sup.2 is hydrogen, C.sub.1-5 alkoxy, C.sub.1-5 alkyl, amino, C.sub.1-5 alkylcarbonylamino, nitro or halogen; R.sup.3 is hydrogen, C.sub.1-5 alkoxycarbonyl, cyano or carbamoyl; R.sup.4 is one to two of hydrogen, oxo, hydroxy, C.sub.1-5 alkoxy, C.sub.1-5 alkoxycarbonylamino-C.sub.1-5 alkyl and amino-C.sub.1-5 alkyl; R.sup.5, R.sup.6 are each independently selected from hydrogen, halogen, C.sub.1-5 alkyl, hydroxyl and C.sub.1-5 alkoxy; R.sup.7 is ##STR2## W is CO or SO.sub.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: September 9, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Mark G. Bock, Ben E. Evans, Peter D. Williams, Roger M. Freidinger, Douglas J. Pettibone, Doug W. Hobbs, Paul S. Anderson
  • Patent number: 5464788
    Abstract: Compounds of the formula X--Y--R, or the pharmaceutically acceptable salts and esters thereof, wherein X is ##STR1## Y is --SO.sub.2 --, --(CH.sub.2).sub.p -- or --CO--(CH.sub.2).sub.p --; R is unsubstituted or substituted phenyl where said substitutents are one or more of R.sup.5, R.sup.6 or R.sup.7 ; R.sup.1 is hydrogen, cyano, phenyl,--CONHR.sup.2, --CONR.sup.2 R.sup.2, --(CH.sub.2).sub.m --OR.sup.2, --(CH.sub.2).sub.p --S(O).sub.r --R.sup.2, --(CH.sub.2).sub.m --CO.sub.2 R.sup.2, --(CH.sub.2).sub.m --N.sub.3, --(CH.sub.2).sub.m --NH.sub.2 or --(CH.sub.2).sub.m --NR.sup.2 R.sup.2 ; R.sup.2 is hydrogen, C.sub.3-8 cycloalkyl or C.sub.1-5 alkyl; R.sup.5 and R.sup.6 are each independently selected from hydrogen, C.sub.1-5 alkoxy, halogen or --(CH.sub.2).sub.n --N(R.sup.2)--C(O)--R.sup.18 ; R.sup.7 is hydrogen or ##STR2## R.sup.11 is selected from hydrogen, C.sub.1-5 alkylcarbonyl, ##STR3## or substituted C.sub.
    Type: Grant
    Filed: March 24, 1994
    Date of Patent: November 7, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Mark G. Bock, Ben E. Evans, J. Christopher Culberson, Kevin F. Gilbert, Kenneth E. Rittle, Peter D. Williams
  • Patent number: 5324726
    Abstract: Benzodiazepine analogs of the formula: ##STR1## wherein: R.sup.3 is ##STR2## --NH(CH.sub.2).sub.2 --.sub.3 NHCOR.sup.7, ##STR3## or --X.sup.11 NR.sup.18 SO.sub.2 (CH.sub.2).sub.q R.sup.7 ; R.sup.7 is O,S,HH, or NR.sup.15 with the proviso that X.sup.7 can be NR.sup.15 only when R.sup.1 is not H.are disclosed which are antagonists of gastrin and cholecystokinin (CCK) with enhanced aqueous solubility and have properties useful in the treatment of disorders of gastric secretion, appetite regulation, gastrointestinal motility, pancreatic secretion, and dopaminergic function, as well as in treatment producing potentiation of morphine and other opiate analgesics.
    Type: Grant
    Filed: October 29, 1992
    Date of Patent: June 28, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Mark G. Bock, Ben E. Evans, Roger M. Freidinger
  • Patent number: 5223509
    Abstract: This invention relates to certain .beta.-carbolines, which are antagonists of the functions of cholecystokinin (CCK) and gastrin, to pharmaceutical compositions comprising these compounds, and to the use of these compounds in the prevention and treatment of disorders of the gastrointestinal, central nervous and appetite-regulatory systems of mammals, especially of humans.
    Type: Grant
    Filed: February 21, 1992
    Date of Patent: June 29, 1993
    Assignee: Merck & Co., Inc.
    Inventor: Ben E. Evans
  • Patent number: 5210082
    Abstract: Pharmaceutical compositions containing aromatic 2-benzazepines with fused 5- or 6-membered heterocyclic rings are disclosed which are useful in the treatment of panic disorder or anxiety disorder.
    Type: Grant
    Filed: May 16, 1991
    Date of Patent: May 11, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Mark G. Bock, Ben E. Evans, Roger M. Freidinger
  • Patent number: 5206237
    Abstract: Pharmaceutical compositions containing benzodiazepines of the formula: ##STR1## are disclosed which are useful in the treatment of panic disorder or anxiety disorder.
    Type: Grant
    Filed: May 14, 1991
    Date of Patent: April 27, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Roger M. Freidinger, Mark G. Bock, Ben E. Evans
  • Patent number: 5206234
    Abstract: Benzolactam analogs of the formula: ##STR1## are disclosed which are antagonists of gastrin and cholecystokinin (CCK).
    Type: Grant
    Filed: June 20, 1991
    Date of Patent: April 27, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Mark G. Bock, Roger M. Freidinger, Ben E. Evans
  • Patent number: 5204349
    Abstract: Compounds of the formula: ##STR1## where R.sup.1 is hydrogen or hydroxy and R.sup.2 is a substituted amino group, a substituted heterocyclic ring or a substituted alkyl. These compounds are oxytocin and vasopressin antagonists useful in the treatment of preterm labor, dysmenorrhea and for the stoppage of labor preparatory to cesarean delivery, timing of parturition, uterine hyperactivity, endometriosis, hypertension, congestive heart failure, hyponatremia and cognitive disorders. Also disclosed are pharmaceutical compositions containing these compounds, methods of their use and methods of their preparation.
    Type: Grant
    Filed: September 16, 1991
    Date of Patent: April 20, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Mark G. Bock, Ben E. Evans, Roger M. Freidinger, Kevin Gilbert, Doug W. Hobbs, James B. Hoffman, George F. Lundell, Douglas J. Pettibone
  • Patent number: 5185331
    Abstract: Pharmaceutical compositions containing Triazolobenzodiazepines of the formula: ##STR1## are disclosed which are useful in the treatment of panic disorder or anxiety disorder.
    Type: Grant
    Filed: May 14, 1991
    Date of Patent: February 9, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Roger M. Freidinger, Mark G. Bock, Ben E. Evans
  • Patent number: 5177071
    Abstract: Pharmaceutical compositions containing 6-membered heterocyclic rings are disclosed which are useful in the treatment of panic disorder or anxiety disorder.
    Type: Grant
    Filed: June 17, 1991
    Date of Patent: January 5, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Roger M. Freidinger, Ben E. Evans, Mark G. Bock