Patents Examined by Donald G. Daus
  • Water-soluble esters of camptothecin compounds
    Patent number: 5646159
    Abstract: Non-toxic camptothecin prodrugs are prepared by esterifying the 20-position hydroxyl group of camptothecin derivatives.
    Type: Grant
    Filed: July 20, 1994
    Date of Patent: July 8, 1997
    Assignee: Research Triangle Institute
    Inventors: Monroe E. Wall, Mansukh C. Wani
  • 6-heterocyclic-4-amino-1,2,2a,3,4,5-hexahydrobenz [CD]indoles
    Patent number: 5643934
    Abstract: 6-Heterocyclic-4-amino-1,2,2a,3,4,5-hexahydrobenz[cd]indoles are provided which are useful in modifying the function of serotonin in mammals.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: July 1, 1997
    Assignee: Eli Lilly and Company
    Inventors: Richard N. Booher, David E. Lawhorn, Michael J. Martinelli, Charles J. Paget, Jr., John M. Schaus
  • 6-heterocyclic-4-amino-1,2,2A,3,4,5-hexahydrobenz[CD]indoles
    Patent number: 5643910
    Abstract: 6-Heterocyclic-4-amino-1,2,2a,3,4,5-hexahydrobenz-[cd]indoles are provided which are useful in modifying the function of serotonin in mammals.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: July 1, 1997
    Assignee: Eli Lilly and Company
    Inventors: Richard N. Booher, David E. Lawhorn, Michael J. Martinelli, Charles J. Paget, Jr., John M. Schaus
  • 6-heterocyclic-4-amino-1,3,4,5,-tetrahydrobenz [cd]indoles
    Patent number: 5643930
    Abstract: 6-heterocyclic-4-amino-1,3,4,5-tetrahydrobenz-[cd]indoles are provided which are useful in modifying the function of serotonin in mammals.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: July 1, 1997
    Assignee: Eli Lilly and Company
    Inventors: Richard N. Booher, David E. Lawhorn, Charles J. Paget, Jr., John M. Schaus
  • 6-heterocyclic-4-amino-1,3,4,5-tetrahydrobenz[cd] indoles
    Patent number: 5641797
    Abstract: 6-heterocyclic-4-amino-1,3,4,5-tetrahydrobenz-[cd]indoles are provided which are useful in modifying the function of serotonin in mammals.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: June 24, 1997
    Assignee: Eli Lilly and Company
    Inventors: Richard N. Booher, David E. Lawhorn, Charles J. Paget, Jr., John M. Schaus
  • Oral hypoglycemic agents
    Patent number: 5641796
    Abstract: Antihyperglycemic compounds selected from the group consisting of C-substituted pentacycloazoles and N-alkyl-substituted pentacycloazoles.
    Type: Grant
    Filed: November 1, 1994
    Date of Patent: June 24, 1997
    Assignee: Eli Lilly and Company
    Inventors: Samuel J. Dominianni, Lora L. Fitch, Klaus K. Schmiegel
  • 6-heterocyclic-4-amino-1,2,2a,3,4,5-hexahydrobenz[cd]indoles
    Patent number: 5641794
    Abstract: 6-Heterocyclic-4-amino-1,2,2a,3,4,5-hexahydrobenz-[cd]indoles are provided which are useful in modifying the function of serotonin in mammals.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: June 24, 1997
    Assignee: Eli Lilly Company
    Inventors: Richard N. Booher, David E. Lawhorn, Michael J. Martinelli, Charles J. Paget, Jr., John M. Schaus
  • Oxazoline derivative, process for preparing the same and agricultural and horticultural chemical for controlling noxious organisms containing the same
    Patent number: 5639771
    Abstract: Disclosed are an oxazoline compound represented by the formula (I): ##STR1## wherein R.sup.1 represents halogen, hydrogen, alkyl, alkoxy, haloalkyl, haloalkoxy, phenyl, phenoxy, benzyl, benzyloxy, pyridyloxy, pyridylmethyloxy, alkoxy-substituted alkyl, nitro, cyanomethyloxy, haloalkylsulfonyloxy, alkylsulfonyloxy, or alkylthio; R.sup.2 represents hydrogen, halogen, alkyl, haloalkyl, alkoxy, alkylthio, or haloalkoxy; R.sup.1 and R.sup.2 may be combined to form a saturated or unsaturated 6-membered ring with oxygen; R.sup.3 represents hydrogen, halogen or alkoxy; R.sup.4 represents hydrogen, alkyl, or halogen; R.sup.5 represents hydrogen, halogen, or alkyl; X.sup.1 represents halogen, alkyl, haloalkyl, or alkoxy; X.sup.2 represents halogen, hydrogen, or alkoxy; X.sup.
    Type: Grant
    Filed: November 25, 1994
    Date of Patent: June 17, 1997
    Assignee: Ube Industries, Ltd.
    Inventors: Tokio Obata, Katsutoshi Fujii, Shoji Shikita, Kouichi Goka
  • 17-amino substituted 4-azasteroid 5.alpha.-reductase inhibitors
    Patent number: 5639741
    Abstract: Novel amino substituted 4-azasteroid 5.alpha.-reductase inhibitors of formula (I). ##STR1## wherein A is (a), (b) or (c), are claimed as well as pharmaceutically acceptable salts and formulations thereof. These compounds are effective in inhibiting testosterone 5.alpha.-reductase(s) and are thus useful in the treatment of a number of hyperandrogenic conditions including benign prostatic hypertrophy, acne, seborrhea, female hirsutism, and male and female pattern baldness (alopecia).
    Type: Grant
    Filed: March 20, 1995
    Date of Patent: June 17, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Bruce E. Witzel, Jeffrey P. Bergman, Richard L. Tolman
  • Substituted aryl and cycloalkyl imidazolones; a new class of GABA brain receptor ligands
    Patent number: 5637725
    Abstract: Disclosed are compounds of the formula: ##STR1## wherein: T is NH, O, or S;X is hydrogen, hydroxyl, lower alkyl, or an optionally substituted amide;the W ring is an optionally substituted aryl or heteroaryl group; and ##STR2## represents an optionally substituted benzo group or an optionally substituted 5, 6, 7, or 8 membered ring.These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: June 10, 1997
    Assignee: Neurogen Corporation
    Inventors: Robert W. DeSimone, Charles A. Blum
  • Substituted aryl and cycloalkyl imidazolones; a new class of GABA brain receptor ligands
    Patent number: 5637724
    Abstract: Disclosed are compounds of the formula: ##STR1## wherein: T is NH, O, or S;X is hydrogen, hydroxyl, lower alkyl, or an optionally substituted amide;the W ring is an optionally substituted aryl or heteroaryl group; and ##STR2## represents an optionally substituted benzo group or an optionally substituted 5, 6, 7, or 8 membered ring.These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: June 10, 1997
    Assignee: Neurogen Corporation
    Inventors: Robert W. DeSimone, Charles A. Blum
  • 11,7 Substituted camptothecin derivatives and formulations of 11,7 substituted camptothecin derivatives and methods for uses thereof
    Patent number: 5633260
    Abstract: The novel compounds 11-hydroxy-7-ethyl camptothecin and 11-hydroxy-7-methoxy camptothecin (11,7-HECPT and 11,7-HMCPT) are active anticancer compounds which are poorly soluble in water. Because of their novelty, 11,7-HECPT and 11,7-HMCPT derivatives have not been directly administered by parenteral or oral routes to human subjects as an antitumor composition for the purpose of inhibiting the growth of cancer cells. The claimed compositions are useful as compared to the water soluble camptothecin derivatives, such as CPT-11, in clinical trials. The unpredictable interpatient variability in the metabolic production of an active metabolite from CPT-11 limits the utility of CPT-11. This invention overcomes these limitations by claiming novel pharmaceutically acceptable lactone stable formulations of 11,7-HECPT or 11,7-HMCPT, to directly administer to patients.
    Type: Grant
    Filed: August 24, 1995
    Date of Patent: May 27, 1997
    Assignee: BioNumerik Pharmaceuticals, Inc.
    Inventors: Frederick H. Hausheer, Kochat Haridas
  • 6-heterocyclic-4-amino-1,2,2a,3,4,5-hexahydrobenz[cd] indoles
    Patent number: 5633273
    Abstract: 6-Heterocyclic-4-amino-l,2,2a,3,4,5-hexahydrobenz-[cd]indoles are provided which are useful in modifying the function of serotonin in mammals.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: May 27, 1997
    Assignee: Eli Lilly and Company
    Inventors: Richard N. Booher, David E. Lawhorn, Michael J. Martinelli, Charles J. Paget, Jr., John M. Schaus
  • Pyridazine derivatives
    Patent number: 5631255
    Abstract: The present invention relates to pyridazine derivatives of formula: ##STR1## which are useful as ligands of cholinergic receptors, in particular, receptors of the M.sub.1 type.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: May 20, 1997
    Assignee: Sanofi
    Inventors: Robert Boigegrain, Roger Brodin, Jean P. Kan, Dominique Olliero, Camille G. Wermuth
  • Oxazole amines as intermediates in the manufacture of insecticidal pyrroles
    Patent number: 5631379
    Abstract: The present invention provides 5-amino-4-aryl-2-perfluoroalkyl-1,3-oxazole derivatives, a method for the preparation of said derivatives and their use as a key intermediate in the manufacture of insecticidal, acaricidal and nematocidal arylpyrrole compounds.
    Type: Grant
    Filed: November 22, 1994
    Date of Patent: May 20, 1997
    Assignee: American Cyanamid Company
    Inventor: Venkataraman Kameswaran
  • 6-heterocyclic-4-amino-1,2,2A,3,4,5-hexahydrobenz [CD] indoles
    Patent number: 5627199
    Abstract: 6-Heterocyclic-4-amino-1,2,2a,3,4,5-hexahydrobenz[cd]indoles are provided which are useful in modifying the function of serotonin in mammals.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: May 6, 1997
    Assignee: ELi Lilly and Company
    Inventors: Richard N. Booher, David E. Lawhorn, Michael J. Martinelli, Charles J. Paget, Jr., John M. Schaus
  • 6-heterocyclic-4-amino-1,3,4,5-tetrahydrobenz[cd]indoles
    Patent number: 5624944
    Abstract: 6-heterocyclic-4-amino-1,3,4,5-tetrahydrobenz[cd]indoles are provided which are useful in modifying the function of serotonin in mammals.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: April 29, 1997
    Assignee: Eli Lilly and Company
    Inventors: Richard N. Booher, David E. Lawhorn, Charles J. Paget, Jr., John M. Schaus
  • Enediyne quinone imines and methods of preparation and use thereof
    Patent number: 5622958
    Abstract: A quinone imine enediyne possessing cytotoxic activity towards cancer cells having the general structure: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are independently the same or different and are H, Br, Cl, F, NH.sub.2, CO.sub.2 H, or OH or a linear or branched alkyl, etc.; wherein R.sub.4 is H, OH or a linear or branched alkoxy, linear or branched alkoxycarbonyl, etc.; wherein R.sub.5 is H, Br, Cl, F, O.dbd., OH or S--SR, or a linear or branched alkyl, etc.; wherein R.sub.6 is H, Br, Cl, F, CO.sub.2 H, OH or S--SR', or a linear or branched alkyl, etc; wherein R.sub.7 is H, OH or S--SR", or a linear or branched alkyl, linear or branched alkoxycarbonyl, linear or branched alkoxy or linear or branched hydroxyalkyl group; and wherein R, R' and R" are independently the same or different and are a linear or branched alkyl, linear or branched acyl or linear or branched alkoxyalkyl group.
    Type: Grant
    Filed: December 1, 1994
    Date of Patent: April 22, 1997
    Assignee: Sloan-Kettering Institute for Cancer Research
    Inventors: Samuel J. Danishefsky, Matthew D. Shair, Taeyoung Yoon, T.-C. Chou
  • Benzopyrrolizinoquinolizinones
    Patent number: 5622957
    Abstract: A compound selected from those of general formula (I): ##STR1## wherein A represents a bivalent radical ##STR2## and R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.6, R.sub.7, R.sub.8, R.sub.9 and Z are as defined in the description,the isomers and pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same which are useful in the treatment of depression and anxiety.
    Type: Grant
    Filed: May 3, 1995
    Date of Patent: April 22, 1997
    Assignee: Adir et Compagnie
    Inventors: Jean-Daniel Brion, Claude Thal, Luc Demuynck, Jean-Gilles Parmentier, Jean Lepagnol, Pierre Lestage, Jean-Fran.cedilla.ois Pujol, Pascal Schmitt, Pierre Potier
  • Pyrrole pyridazine and pyridazinone anti-inflammatory agents
    Patent number: 5622948
    Abstract: Pyrrole pyridazine and pyridazinone compounds are described. These compounds are useful as anti-inflammatory agents in the treatment of inflammation and pain. The preparation of these compounds, their pharmaceutically acceptable salts, and pharmaceutical compositions containing these compounds, is also described.
    Type: Grant
    Filed: December 1, 1994
    Date of Patent: April 22, 1997
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: James P. Dunn, Chakk S. Ramesha, Jim W. Barnett, Denis J. Kertesz, Aaron B. Miller, David Morgans, Jr., C. Elliott Sigal, Eric B. Sjogren, David B. Smith, Francisco X. Talamas