Patents Represented by Attorney John J. McDonnell
  • Patent number: 5644057
    Abstract: Disclosed are compounds of the formula ##STR1## wherein Ar represents an aryl or heteroaryl group; andR.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 represent organic or inorganic substituents,which compounds are highly selective partial agonists or antagonists at human CRF1 receptors and, thus, are useful in the diagnosis and treatment of treating stress related disorders such as post trumatic stress disorder (PTSD) as well as depression, headache and anxiety.
    Type: Grant
    Filed: May 12, 1995
    Date of Patent: July 1, 1997
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Alan Hutchison
  • Patent number: 5637758
    Abstract: Disclosed are detergent compositions comprising critical amounts of divalent cations and a minimum amount of a mixture of a salt of alpha-sulfonated methyl ester of a fatty acid, anionic surfactants and foam stabilizing auxiliary surfactants.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: June 10, 1997
    Assignee: Stepan Company
    Inventors: Branko Sajic, Irma Ryklin, Brian L. Frank, Y. Kameshwer Rao
  • 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
  • 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
  • Patent number: 5633240
    Abstract: Disclosed herein are parenteral solutions containing 7-halo-1,2,3,4-tetrahydro-3-aryl-6-quinazoline sulfonamide in Tris or Bis-Tris or Tris buffer useful in the treatment of hypertension, heart disease and heart failure and renal disease. Also disclosed are methods for preparing such solutions.
    Type: Grant
    Filed: February 13, 1995
    Date of Patent: May 27, 1997
    Assignee: Academic Pharmaceuticals
    Inventor: Vasant Ranade
  • Patent number: 4687864
    Abstract: The present invention describes 5-fluoro-3-oxaprostacyclin (PGI.sub.2) derivatives of Formula I. These compounds are useful for the treatment of platelet dysfunction, atherosclerosis, hypertension and tumor cell metastasis. Also disclosed is the process for preparing them and the appropriate intermediates. ##STR1## wherein R.sup.1 is: (a) Na, K, or 1/2 Ca, or other pharmaceutically acceptable cation(b) NR.sup.3 .sub.2 with the adjacent connecting oxygen omitted, where R.sup.3 =H, methyl, ethyl, isopropyl or a combination of these groups;(c) Alkyl of 1 to 6 carbon atoms, either branched or straight chain(d) Hydrogenwherein OH on carbon 15 is optionally on carbon 16;wherein X=OCH.sub.3 or OC.sub.2 H.sub.5 when neither C.sub.5 -C.sub.6 or C.sub.6 -C.sub.7 is a double bond and nothing if C.sub.5 -C.sub.6 or C.sub.6 -C.sub.7 is a double bond;wherein R.sup.
    Type: Grant
    Filed: September 18, 1985
    Date of Patent: August 18, 1987
    Assignee: G. D. Searle & Co.
    Inventors: Stevan W. Djuric, Leland J. Chinn, Kurt J. Rorig
  • Patent number: 4665203
    Abstract: The invention relates to compounds of the formula: ##STR1## which are useful as leukotriene D.sub.4 (LTD.sub.4) inhibitors and therefore useful in the treatment of allergies and inflammatory conditions.
    Type: Grant
    Filed: August 12, 1985
    Date of Patent: May 12, 1987
    Assignee: G. D. Searle & Co.
    Inventors: Masateru Miyano, Robert L. Shone, Daniel D. Sohn
  • Patent number: 4649147
    Abstract: This invention relates to 1-(alkenoyl)azacycloalkyl carboxylic acids and derivatives that prevent or reduce the degradation of elastin and other proteins and that thereby prevent or retard the disease states caused by said degradation.
    Type: Grant
    Filed: July 8, 1985
    Date of Patent: March 10, 1987
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis
  • Patent number: 4644071
    Abstract: This invention relates to substituted aralkoxy and aryloxyalkoxy kojic acid derivatives, which are useful as leukotriene D.sub.4 (LTD.sub.4) inhibitors and therefore useful in the treatment of allergies, inflammatory conditions, and coronary vasoconstriction.
    Type: Grant
    Filed: July 11, 1984
    Date of Patent: February 17, 1987
    Assignee: G. D. Searle & Co.
    Inventors: Miyano Masateru, Robert L. Shone
  • Patent number: 4639524
    Abstract: Compositions of matter are disclosed of compounds of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein X represents a halo, lower alkyl, hydrogen, trifluoromethyl, phenyl, or lower alkoxy substituent; Y represents --CN, --CONH.sub.2, --CON(R.sub.1).sub.2 or --CO.sub.2 R.sub.1 where R.sub.1 is a lower alkyl; m is the integer 1 or 2 and n is an integer from 1 to 3 inclusive; R.sub.2 represents lower alkyl; R.sub.3 represents lower alkyl or acetyl, aroyl, phenacetyl or trifluoracetyl; A, B, and D are carbonyl or methylene such that when one of A, B, or D is carbonyl, the others are methylene and R.sub.3 is lower alkyl, whereas when R.sub.3 is acetyl, aroyl, phenacetyl or trifluoroacetyl, A, B, and D are methylene. These compounds have utility as antiarrhythmic agents.
    Type: Grant
    Filed: July 9, 1984
    Date of Patent: January 27, 1987
    Assignee: G. D. Searle & Co.
    Inventors: Bipinchandra N. Desai, Robert J. Chorvat, Kurt J. Rorig
  • Patent number: 4617411
    Abstract: This invention relates to novel 3-oxa-15-desoxy-16-hydroxy-16-alkyl prostaglandins of the E.sub.2 series and the 5,6-acetylene derivatives thereof. These compounds are useful for their gastric antisecretory, cytoprotective, antiulcer, and antihypertensive activity. In addition the invention also discloses certain novel trialkylsilyl acetylenic intermediates.
    Type: Grant
    Filed: March 25, 1985
    Date of Patent: October 14, 1986
    Assignee: G. D. Searle & Co.
    Inventors: Paul W. Collins, Richard M. Weier
  • Patent number: 4603121
    Abstract: The invention relates to novel enkephalin analogs of the formula: ##STR1## which are useful as analgesic agents.
    Type: Grant
    Filed: September 14, 1984
    Date of Patent: July 29, 1986
    Assignee: G. D. Searle & Co.
    Inventors: Donald W. Hansen, Jr., David A. Jones, Jr., Robert H. Mazur, James M. Schlatter
  • Patent number: 4565882
    Abstract: The invention relates to substituted dihydrobenzopyrans carboxylates of the formula: ##STR1## wherein A is a methylene chain having 1-10 carbon atoms, inclusive, optionally substituted by hydroxy;wherein V is:(a) hydrogen;(b) hydroxy;(c) .dbd.O; or(d) R.sub.6 CH.sub.2 O--;wherein R.sub.1 is:(a) --COCH.sub.3 ;(b) --CHOHCH.sub.3 ;(c) --C.sub.2 H.sub.5 ;(d) -hydrogen; or(e) --COOC.sub.2 H.sub.5wherein R.sub.2 is:(a) -hydrogen;(b) -hydroxy; or(c) R.sub.12 CH.sub.2 CO.sub.2 --;wherein R.sub.3, R.sub.4, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10, R.sub.11 and R.sub.12 each of which may be the same or different, are:(a) hydrogen;(b) lower-alkyl having 1-6 carbon atoms inclusive; or(c) allyl;wherein R.sub.5 is:(a) hydrogen; or(b) R.sub.7 CH.sub.2 C(O)--;wherein R.sub.13 is hydrogen, hydroxy, alkoxy of 1 to 6 carbon atoms inclusive, or --OM wherein M is an alkali metal, alkyl of 1 to 6 carbon atoms, inclusive, or NR.sub.8.sup..sym. R.sub.9 R.sub.10 R.sub.11, or HNR.sub.8.sup..sym. R.sub.9 R.sub.
    Type: Grant
    Filed: January 6, 1984
    Date of Patent: January 21, 1986
    Assignee: G. D. Searle & Co.
    Inventors: Masateru Miyano, Robert L. Shone
  • Patent number: 4560754
    Abstract: This invention relates to 5-(substituted phenyl)-5-[(substituted amino)alkyl]-1,3-diazabicyclo[4.4.0]decan-4-ones and 5-(substituted phenyl)-5-[(substituted amino)-alkyl]-1,3-diazabicyclo[4.4.0]dec-2-en-4-ones that are useful as antiarrhythmic agents.
    Type: Grant
    Filed: July 30, 1984
    Date of Patent: December 24, 1985
    Assignee: G. D. Searle & Co.
    Inventors: Gilbert W. Adelstein, Robert J. Chorvat
  • Patent number: 4559336
    Abstract: This invention relates to 8-chlorodibenz[b,f][1,4]oxazepine-10(11H)-carboxylic acid, 2-(sulfinyl- and sulfonyl-containing acyl)hydrazides that are useful as prostaglandin antagonists and analgesic agents.
    Type: Grant
    Filed: February 25, 1985
    Date of Patent: December 17, 1985
    Assignee: G.D. Searle & Co.
    Inventor: Richard A. Mueller
  • Patent number: 4559337
    Abstract: This invention relates to 8-chlorodibenz[b,f][1,4]-oxazepine-10(11H)-carboxylic acid, 2-(alkoxy-containing acyl)hydrazides that are useful as prostaglandin antagonists and analgesic agents.
    Type: Grant
    Filed: February 25, 1985
    Date of Patent: December 17, 1985
    Assignee: G.D. Searle & Co.
    Inventor: Richard A. Mueller
  • Patent number: 4555362
    Abstract: This invention encompasses a method and intermediates for preparing a commercial sweetening agent, .alpha.-L-aspartyl-L-phenylalanine methyl ester. The process involves reacting L-aspartic acid with diketene to form N-acetoacetyl-L-aspartic acid which is converted to N-acetoacetyl-L-aspartic anhydride by reaction with acetic anhydride. N-acetoacetyl-L-aspartic anhydride is reacted with L-phenylalanine methyl ester to provide N-acetoacetyl-.alpha.-L-aspartyl-L-phenylalanine methyl ester which is converted to .alpha.-L-aspartyl-L-phenylalanine methyl ester by reaction with hydroxylamine hydrochloride.
    Type: Grant
    Filed: May 15, 1984
    Date of Patent: November 26, 1985
    Assignee: G. D. Searle & Co.
    Inventors: Hugh L. Dryden, Jr, John B. Hill
  • Patent number: 4554359
    Abstract: This invention relates to methods of preventing or reducing the degradation of elastin and other proteins and thereby preventing or retarding the disease states caused by said degradation by administering compounds of the formula: ##STR1## or their pharmacologically acceptable salts.
    Type: Grant
    Filed: January 9, 1984
    Date of Patent: November 19, 1985
    Assignee: G. D. Searle & Co.
    Inventors: Harman S. Lowrie, John S. Baran
  • Patent number: 4554353
    Abstract: This invention encompasses compounds of the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof wherein n is 2 or 3 and R.sub.1 and R.sub.2 are n-propyl, isopropyl, or R.sub.1 and R.sub.2 together with N form a 2,6-dimethyl-1-piperidinyl group. The compounds of this invention are useful as antiarrhythmic agents.
    Type: Grant
    Filed: August 3, 1984
    Date of Patent: November 19, 1985
    Assignee: G. D. Searle & Co.
    Inventors: Robert J. Chorvat, Bipinchandra N. Desai
  • Patent number: 4551279
    Abstract: This invention relates to methods of preventing or reducing the degradation of elastin and other proteins and thereby preventing or retarding the disease states caused by said degradation by administering compounds, some of which are novel, of the formula: ##STR1## or their pharmacologically acceptable salts.
    Type: Grant
    Filed: January 9, 1984
    Date of Patent: November 5, 1985
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis