Patents Examined by Philip I. Datlow
  • Patent number: 5420126
    Abstract: Novel benzoxazine derivatives of the formula (I): ##STR1## are provided as well as their pharmaceutically acceptable salts and a method for their use as potassium channel activating agents 2-(3,4-Dihydro-2, 2-dimethyl-6-phenylsulfonyl-2H-1,4-benzoxazin-4-yl)pyridine N-oxide is illustrative of a benzoxazine derivative of formula (I).
    Type: Grant
    Filed: November 24, 1992
    Date of Patent: May 30, 1995
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Yuzo Matsumoto, Ryuji Tsuzuki, Akira Matsuhisa, Kazuhisa Takayama, Wataru Uchida, Masaharu Asano, Isao Yanagisawa, Toru Yoden
  • Patent number: 5418229
    Abstract: A compound of the formula ##STR1## wherein X, R.sup.1, R.sup.2, R.sup.3, R.sup..sup.4, Y, m and n are defined herein are useful as muscarinic receptor antagonists.
    Type: Grant
    Filed: May 31, 1994
    Date of Patent: May 23, 1995
    Inventors: David Alker, Peter E. Cross
  • Patent number: 5416096
    Abstract: 7-(1-Pyrrolidinyl)-3-quinolone- and -naphthyridonecarboxylic acid derivatives as antibacterial agents and feed additives, of the formula ##STR1## in which X.sup.1 is halogen,X.sup.2 is hydrogen, halogen, amino or other radical,R.sup.1 is alkyl, cycloalkyl, optionally substituted phenyl or other radical,R.sup.2 is hydrogen, alkyl or a dioxolylmethyl radical,R.sup.3 is ##STR2## and A is N, CH, C-halogen, or the like, or forms a bridge with R.sup.1,and addition products thereof.
    Type: Grant
    Filed: July 30, 1991
    Date of Patent: May 16, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Uwe Petersen, Thomas Schenke, Andreas Krebs, Klaus Grohe, Michael Schriewer, Ingo Haller, Karl G. Metzger, Rainer Endermann, Hans-Joachim Zeiler
  • Patent number: 5409909
    Abstract: A triazolo-1,4-di-azepine compound of the below given formula and a pharmacologically acceptable salt thereof are disclosed and useful in the pharmaceutical field, especially to treat allergic diseases: ##STR1## in which R1 and R2 are hydrogen or an alkyl, R3 is hydrogen or a halogen, R4 is hydrogen or an alkyl, X is --OCO--, --NHCO--, --CO-- or others and Y is a cycloalkyl, a cycloalkylalkyl, an alkynyl or others.
    Type: Grant
    Filed: March 18, 1994
    Date of Patent: April 25, 1995
    Assignee: Eisai Co., Ltd.
    Inventors: Kazuo Okano, Shuhei Miyazawa, Richard S. J. Clark, Shinya Abe, Tetsuya Kawahara, Naoyuki Kimomura, Osamu Asano, Hiroyuki Yoshimura, Mitsuaki Miyamoto, Yoshimori Sakuma, Kenzo Muramoto, Hiroshi Obaishi, Koukichi Harada, Hajime Tsunoda, Satoshi Katayama, Kouji Yamada, Shigeru Souda, Yoshimasa Machida, Kouichi Katayama, Isao Yamatsu
  • Patent number: 5407933
    Abstract: Compounds of formula (I): ##STR1## [wherein: A-- B is .dbd.C.dbd.CH--or a nitrogen atom; R.sup.1 is hydrogen, alkyl, aryl or aralkyl; and Z is alkylene] and pharmaceutically acceptable salts thereof are useful in the treatment and prevention of allergies and asthma.
    Type: Grant
    Filed: August 16, 1994
    Date of Patent: April 18, 1995
    Assignee: Sankyo Company, Limited
    Inventors: Hiroshi Fukumi, Toshiaki Sakamoto, Mitsuo Sugiyama, Yoshio Iizuka, Takeshi Yamaguchi
  • Patent number: 5403856
    Abstract: The invention relates to a method of treating cardiac insufficiency by using compounds of the formula I ##STR1## in which n is 1 or 2, R, R.sup.1, R.sup.2 and R.sup.3 are identical or different and each denote hydrogen or an organic radical and R.sup.4 R.sup.5, together with the atoms carrying them, form a mono-, bi- or tri-cyclic heterocyclic ring system. The invention furthermore relates to compounds of the formula I and agents containing these for use in the treatment of the abovementioned disease.
    Type: Grant
    Filed: January 31, 1994
    Date of Patent: April 4, 1995
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Rainer Henning, Hansjorg Urbach, Volker Teetz, Rolf Geiger, Bernward Scholkens
  • Patent number: 5403836
    Abstract: A benzazepine derivative that acts as a nonpeptidyl platelet aggregation inhibitor is provided. This inhibitor potently inhibits fibrinogen binding to the GPII.sub.b III.sub.a receptor and is provided in therapeutic compositions for the treatment of diseases for which blocking platelet aggregation is indicated. These nonpeptidyl inhibitors are provided in combination with thrombolytics and anticoagulants.
    Type: Grant
    Filed: May 6, 1993
    Date of Patent: April 4, 1995
    Assignee: Genentech, Inc.
    Inventors: Brent Blackburn, Robert McDowell, Thomas Gadek, Rob Webb
  • Patent number: 5395932
    Abstract: The present invention provides substituted dibenzoxazepine compounds of Formula I: ##STR1## wherein X is oxygen, sulfur ##STR2## A is --CH.sub.2 -- or ##STR3## E and F may be --CH, oxygen, nitrogen or sulfur, and may not be the same; G is oxygen, nitrogen or sulfur; with the proviso that when G is oxygen or sulfur, one of E or F is nitrogen, which are useful as analgesic agents for the treatment of pain, and as prostaglandin-E.sub.2 antagonists for the treatment of prostaglandin-E.sub.2 mediated diseases, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, a method for eliminating or ameliorating pain in an animal, and a method for treating prostaglandin-E.sub.2 mediated diseases in an animal, comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
    Type: Grant
    Filed: April 30, 1993
    Date of Patent: March 7, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Nizal S. Chandrakumar, Timothy J. Hagen, Barnett S. Pitzele, Sofya Tsymbalov, E. Ann Hallinan
  • Patent number: 5393760
    Abstract: Compounds of the formula ##STR1## wherein L, M, R, T and X are set forth in the description, as well as hydrates or solvates thereof, which inhibit thrombin-induced platelet aggregation and clotting of fibrinogen in plasma, are described. The compounds of formula I are prepared by amidination or, depending on whether L is NH or O, by amide formation or esterification.
    Type: Grant
    Filed: June 15, 1993
    Date of Patent: February 28, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean Ackermann, David Banner, Klaus Gubernator, Paul Hadvary, Kurt Hilpert, Klaus Muller, Ludvik Labler, Gerard Schmid, Thomas B. Tschopp, Hans P. Wessel, Beat Wirz
  • Patent number: 5393747
    Abstract: The present invention provides methods for treating convulsions, ischemia and other diseases responsive to prostaglandin-E.sub.2 antagonists in an animal comprising administering a therapeutically-effective amount of a substituted dibenzoxazepine compound of Formula I, or a pharmaceutically-acceptable salt thereof, to the animal: ##STR1## wherein Y is oxygen, sulfur, --SO-- or --SO.sub.2 --, R.sup.1 is hydrogen, halogen or --CF.sub.3, R.sup.2 is hydrogen, halogen, --OH or --OCH.sub.3, R.sup.3 is hydrogen, alkyl, aryl, alkyl-substituted aryl or aryl-substituted alkyl, m is an integer of from 1 to 5, X is ##STR2## R.sup.4 is hydrogen, alkyl, aryl, alkyl-substituted aryl, trifluoromethyl-substituted aryl or aryl-substituted alkyl, and R.sup.5 and R.sup.6 are each independently hydrogen, alkyl, aryl, alkyl-substituted aryl or aryl-substituted alkyl.
    Type: Grant
    Filed: November 17, 1993
    Date of Patent: February 28, 1995
    Assignee: G. D. Searle & Co.
    Inventors: E. Ann Hallinan, Robert K. Husa, Karen B. Peterson
  • Patent number: 5393753
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is H, C.sub.1 -C.sub.7 alkyl, C.sub.3 -C.sub.7 cycloalkyl, CF.sub.3, aryl, substituted aryl, heteroaryl, -O-C.sub.1 -C.sub.7 alkyl, or -O-C.sub.3 -C.sub.7 cycloalkyl; R.sup.2 and R.sup.3 are each independently H, C.sub.1 -C.sub.7 alkyl, C.sub.3 -C.sub.7 cycloalkyl, CF.sub.3, NO.sub.2, halogen, OR.sup.7, NR.sup.8 R.sup.9 or S(O).sub.m R.sup.10, wherein m is 0, 1 or 2; R.sup.4 is H, C.sub.1 -C.sub.7 alkyl, arylmethyl, or substituted arylmethyl; R.sup.5 and R.sup.6 are each independently H, C.sub.1 -C.sub.7 alkyl, C.sub.3 -C.sub.7 cycloalkyl, aryl, substituted aryl, heteroaryl, arylmethyl, substituted arylmethyl, or taken together constitute a chain of (CH.sub.2).sub.k groups, wherein k is 3, 4, or 5; R.sup.7, R.sup.8 and R.sup.9 are each independently H, C.sub.1 -C.sub.7 alkyl, -C(.dbd.O)-(C.sub.1 -C.sub.7 alkyl), -C(.dbd.O)-aryl, or -(C.dbd.O)heteroaryl; R.sup.10 is C.sub.1 -C.sub.7 alkyl, C.sub.3 -C.sub.
    Type: Grant
    Filed: April 6, 1993
    Date of Patent: February 28, 1995
    Assignee: Schering Corporation
    Inventor: Richard J. Friary
  • Patent number: 5389630
    Abstract: Diamine compounds of formula (I) or an addition salt thereof are provided: ##STR1## These compounds have an excellent cerebral protective action, are very safe, and exhibit a strong action when orally administered, and therefore, medicines containing such compounds are effective for treating disorders caused by cerebral hemorrhage, cerebral infarction, subarachnoid hemorrhage, transient ischemic attack, cerebrovascular disorders and the like, or preventing progress of such disorders.
    Type: Grant
    Filed: January 22, 1993
    Date of Patent: February 14, 1995
    Assignee: Kowa Co., Ltd.
    Inventors: Seiichi Sato, Kiyoshi Kawamura, Yoshio Takahashi, Koichiro Watanabe, Sadahiro Shimizu, Tomio Ohta
  • Patent number: 5389677
    Abstract: Composition and method for enhancing therapeutic effects of topically applied agents are disclosed. The cosmetic or therapeutic composition may include one or more of cosmetic or pharmaceutical agents present in a total amount of from 0.01 to 40 percent and one or more of hydroxycarboxylic acids or related compounds present in a total amount of from 0.01 to 99 percent by weight of the total composition. The cosmetic and pharmaceutical agents may include but not limited to age spots, wrinkles and keratoses removing agents; vitamins; aloes; sun screens; tanning, depigmenting and shampooing agents; antiyeasts; antifungal, antibacterial and antiviral agents; topical bronchial dilators and topical cardiovascular agents; hormonal agents; vasodilators; retinoids and other dermatological agents. The hydroxycarboxylic acids and related compounds include organic alpha and beta hydroxycarboxylic acids, alpha and beta ketocarboxylic acids and salts thereof.
    Type: Grant
    Filed: July 12, 1993
    Date of Patent: February 14, 1995
    Inventors: Ruey J. Yu, Eugene J. Van Scott
  • Patent number: 5387585
    Abstract: The novel imidazodiazepine derivatives of the formula: ##STR1## wherein the substituents are as described in the specification, can be used for the control or prevention of epileptic seizures, anxiety, tension and excitation states, sleep disorders, schizophrenic symptoms, hepatic encephalopathy and senile dementia, as well as, in the partial or complete antagonization of undesired side-effects of substances acting on benzodiazepine receptors after over-dosage or after their use in intensive medicine and in anesthesia.
    Type: Grant
    Filed: November 15, 1993
    Date of Patent: February 7, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rene Borer, Walter Gassner, Max Gerecke, Emilio Kyburz
  • Patent number: 5385938
    Abstract: Preventive as well as therapeutic treatment to alleviate cosmetic conditions and symptoms of dermatologic disorders with amphoteric compositions containing alpha hydroxyacids, alpha ketoacids, related compounds or polymeric forms of hydroxyacids is disclosed. The cosmetic conditions and the dermatologic disorders in which the amphoteric compositions and the polymeric compounds may be useful include dry skin, dandruff, acne, keratoses, psoriasis, eczema, pruritus, age spots, lentigines, melasmas, wrinkles, warts, blemished skin, hyperpigmented skin, kyperkeratotic skin, inflammatory dermatoses, skin changes associated with aging, and skin requiring cleansers.
    Type: Grant
    Filed: August 7, 1992
    Date of Patent: January 31, 1995
    Inventors: Ruey J. Yu, Eugene J. Van Scott
  • Patent number: 5384316
    Abstract: Compounds of formula (I) are provided, wherein R.sup.1 represents OH or OCH.sub.3 ; R.sup.2 represents OH or H; R.sup.3 represents methyl, ethyl, propyl or allyl; X represents O, (H,OH) or (H,H); m represents 0 or 1; n represents 1 or 2; and pharmaceutically acceptable derivatives thereof; provided that when n is 1, then R.sup.3 is allyl or propyl. The compounds are indicated inter alia as immunosuppresive agents.
    Type: Grant
    Filed: February 18, 1993
    Date of Patent: January 24, 1995
    Assignee: Fisons plc
    Inventors: David K. Donald, Mark Furber
  • Patent number: 5382578
    Abstract: The present invention provides substituted dibenzoxazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, and for the treatment of convulsions and ischemia, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain and for the treatment of convulsions and ischemia, in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
    Type: Grant
    Filed: November 19, 1993
    Date of Patent: January 17, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Robert K. Husa, Timothy J. Hagen, E. Ann Hallinan
  • Patent number: 5382579
    Abstract: A triazolo-1,4-azepine compound of the below given formulas and a pharmacologically acceptable salt thereof are disclosed and useful in the pharmaceutical field, especially to allergic diseases. ##STR1## in which R1 and R2 are hydrogen or an alkyl, R3 is hydrogen or a halogen, R4 is hydrogen or an alkyl, X is --OCO--, --NHCO--, --CO-- or others and Y is a cycloalkyl, a cycloalkylalkyl, an alkynyl or others.
    Type: Grant
    Filed: August 26, 1991
    Date of Patent: January 17, 1995
    Assignee: Eisai Co., Ltd.
    Inventors: Kazuo Okano, Shuhei Miyazawa, Richard S. J. Clark, Shinya Abe, Tetsuya Kawahara, Naoyuki Shimomura, Osamu Asano, Hiroyuki Yoshimura, Mitsuaki Miyamoto, Yoshimori Sakuma, Kenzo Muramoto, Hiroshi Obaishi, Koukichi Harada, Hajime Tsunoda, Satoshi Katayama, Kouji Yamada, Shigeru Souda, Yoshimasa Machida, Kouichi Katayama, Isao Yamatsu
  • Patent number: 5380721
    Abstract: Aryl-fused- and hetaryl-fused-2,4-diazepines of formula XXXVI, benzodiazocines of formula XXX, benzodiazepines of formula II ##STR1## .delta.-aminoamides of formula III and aryldimethanamines of formula XXXVII ##STR2## wherein A is an aryl or hetaryl ring;R.sup.1 is hydrogen, alkyl, aryl or hetaryl;R.sup.2 is hydrogen, alkyl, substituted alkyl, or aryl;R.sup.3 is alkyl, aryl, aralkyl or heteroatom substituted alkyl or aralkyl;R.sup.4 is hydrogen or alkyl;R.sup.5 is hydrogen, alkyl, aryl or hetaryl;R.sup.6 is hydrogen, alkyl, alkoxy, halogen or a fused benzene ring;R.sup.9 is hydrogen, alkyl, or substituted alkyl; andR.sup.10 is hydrogen, alkyl, or substituted alkyl.The invention further relates to processes for the preparation of, pharmaceutical compositions containing, and methods of treating cardiac arrhythmia with the compounds of formulas XXXVI, XXX, II, III, and XXXVII.
    Type: Grant
    Filed: May 31, 1994
    Date of Patent: January 10, 1995
    Assignee: Sterling Winthrop Inc.
    Inventors: Robert E. Johnson, Donald C. Schlegel, Alan M. Ezrin
  • Patent number: 5378840
    Abstract: The present invention provides dibenzoxazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
    Type: Grant
    Filed: August 24, 1993
    Date of Patent: January 3, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Albert C. Lee, E. Ann Hallinan, Timothy J. Hagen, Robert K. Husa, Sofya Tsymbalov, Jean-Pierre Van Hoeck