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.
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.
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.
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
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.
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
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
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.
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.
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
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.
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.
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
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.
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.
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.
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.
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
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.