Patents Examined by Matthew V. Grumbling
  • Antidepressant 1-arylalkyl-4-(alkoxy pyridinyl)-and 4-(alkoxypyrimidinyl) piperazine derivatives
    Patent number: 5763444
    Abstract: Novel compound of formula I and pharmaceutically acceptable salts thereof are useful CNS agents: ##STR1## wherein X is CH or N;X' is CH or a direct covalent link;Y is CH, CH.sub.2 or N;Y' is N, NH, O or S;R.sup.1 is H, Br, Cl, F, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkoxycarbonyl, CN, CONH.sub.2 or CH.sub.3 SO.sub.2 NH;n is 2 or 3;R.sup.2 is H or C.sub.1-4 alkyl;R.sup.3 is C.sub.1-4 alkoxy;R.sup.4 is H, Br, Cl, or F; andZ is CH or N.
    Type: Grant
    Filed: August 13, 1996
    Date of Patent: June 9, 1998
    Assignee: Bristol-Myers Squibb Company
    Inventors: David W. Smith, Joseph P. Yevich
  • N-(1-ethyl-4-pyrazolyl)triazoloazinesulfonamide herbicides
    Patent number: 5763359
    Abstract: Substituted N-(1-ethyl-4-pyrazolyl)triazoloazinesulfonamide compounds, such as N-(1-ethyl-5-methyl-3-(trifluoromethyl)-4-pyrazoyl)-5-methoxy-7-methyl-?1, 2,4!triazolo?1,5-c!pyrimidine-2-sulfonamide and N-(1-ethyl-5-methyl-3-(trifluoromethyl)-4-pyrazolyl)-5-methoxy-7-methyl?1, 2,4!triazolo?1,5-a!pyridine-2-sulfonamide, were prepared and found to possess selective herbicidal utility.
    Type: Grant
    Filed: August 28, 1996
    Date of Patent: June 9, 1998
    Assignee: Dow AgroSciences LLC
    Inventors: Mark J. Costales, William A. Kleschick, Robert J. Ehr, Monte R. Weimer
  • Herbicidal compounds
    Patent number: 5759956
    Abstract: A compound of the general formula (I) ##STR1## wherein A represents a group of general formula ##STR2## and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X, Q.sup.2, Q.sup.3, and n are as described in the specification. The compounds of formula (I) are useful as agricultural herbicides.
    Type: Grant
    Filed: May 8, 1996
    Date of Patent: June 2, 1998
    Assignee: American Cyanamid Company
    Inventors: Hans-Peter Niedermann, Rudi Eisenacht
  • Integrin receptor antagonists
    Patent number: 5760028
    Abstract: This invention relates to novel heterocycles including 3-?1-?3-(imidazolin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(benzylo xycarbonylamino)propionic acid, which are useful as antagonists of the .alpha..sub.v .beta..sub.3 integrin and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.
    Type: Grant
    Filed: December 20, 1996
    Date of Patent: June 2, 1998
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventors: Prabhakar Kondaji Jadhav, Joseph James Petraitis, Douglas Guy Batt
  • Lyophilized composition containing S(+)-4,4'-(1-methyl-1,2-ethanediyl)-bis(2,6-piperazinedione)
    Patent number: 5760039
    Abstract: A process of making a stable lyophilized, white to off-white, crack-free preparation of ICRF-187 in which the cake of ICRF-187 is protected against the deleterious effect of light, has a moisture content of not more than about 2% wherein the process comprises lyophilization using a starting solution of a therapeutically acceptable acid salt of ICRF-187 having a concentration of up to about 25 mg/ml and in which the primary drying stage lasts at least 30 hours, preferably at least 40 hours, and/or uses a primary drying temperature of from about 30.degree. C. to about 40.degree. C.
    Type: Grant
    Filed: April 10, 1997
    Date of Patent: June 2, 1998
    Assignee: Chiron Corporation
    Inventors: Josephus J. M. Holthuis, Alwinus A. Voetman
  • 1.3 oxa (thia) zines and pest control agents
    Patent number: 5760033
    Abstract: A compound represented by the chemical formula ?1!: ##STR1## wherein Z is oxygen or sulfur, Y is halogen, optionally substituted alkyl, optionally substituted alkoxycarbonyl, optionally substituted alkoxy, S(O).sub.p r.sup.1 wherein p denotes an integer from 0 to 2, r.sup.1 is optionally substituted alkyl, nitro, cyano or optionally substituted amino, m denotes an integer from 1 to 3, R.sub.1, R.sub.2 and R.sub.4 are same or different one another and each independently hydrogen, optionally substituted alkyl or optionally substituted phenyl, R.sub.3 is alkyl, alkenyl, aralkyl, cycloalkyl, phenyl, naphthyl, pyridyl, furyl or thienyl, those which substituents can be further optionally substituted by halogen, hydroxy, optionally substituted alkyl or the like, and a chemical agent for controlling pests.
    Type: Grant
    Filed: August 25, 1995
    Date of Patent: June 2, 1998
    Inventors: Yasuo Yamada, Takashi Kishimoto, Michihiko Matsuda, Renpei Hatano, Takao Iwasa, Makio Yano
  • 4-aminoquinazoline EGFR Inhibitors
    Patent number: 5760041
    Abstract: This invention provides a compound having the formula ##STR1## wherein: X is phenyl which is optionally substituted;R and R.sub.1 are each, independently, hydrogen, halogen, alkyl, alkoxy, hydroxy, or trifluoromethyl;R.sub.2 is hydrogen, alkyl, alkoxy, hydroxy, trifluoromethyl;Y is a radical selected from the group consisting of ##STR2## R.sub.3 is independently hydrogen, alkyl, carboxy, carboalkoxy, phenyl, or carboalkyl;n=2-4;or a pharmaceutically acceptable salt thereof, with the proviso that each R.sub.3 of Y may be the same or different which are useful as antineoplastic agents.
    Type: Grant
    Filed: January 21, 1997
    Date of Patent: June 2, 1998
    Assignee: American Cyanamid Company
    Inventors: Allan Wissner, Bernard D. Johnson, Middleton B. Floyd, Jr., Douglas B. Kitchen
  • Spirocycle integrin inhibitors
    Patent number: 5760029
    Abstract: This invention relates to novel heterocycles, including (S)-2-phenylsulfonylamino-3-???8-(2-pyridinylaminomethyl)-!-1-oxa-2-azaspi ro-?4,5!-dec-2-en-3-yl!carbonylamino! propionic acid, which are useful as antagonists of the .alpha..sub.v .beta..sub.3 integrin and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.
    Type: Grant
    Filed: March 13, 1997
    Date of Patent: June 2, 1998
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventors: Prabhakar Kondaji Jadhav, Joanne Marie Smallheer
  • Process for preparing amino acid esters useful as intermediates for compounds containing a fused bicyclic ring
    Patent number: 5756832
    Abstract: Amino acid esters of the formula ##STR1## wherein m is zero or one and R.sub.3 is an acid protecting group are prepared. These amino acid esters are useful as intermediates in the preparation of fused bicyclic ring compounds.
    Type: Grant
    Filed: May 9, 1997
    Date of Patent: May 26, 1998
    Assignee: Bristol-Myers Squibb Co.
    Inventor: Jeffrey A. Robl
  • Quinazolinone derivatives as cholyecystokinin (CCK) ligands
    Patent number: 5756502
    Abstract: Novel quinazolinone derivatives with good binding affinity for the CCK-A and CCK-B receptors, pharmaceutical compositions containing them, methods of using them and a novel process for their preparation are taught. The compounds are useful agents to suppress appetite, reduce gastric acid secretion, and the like.
    Type: Grant
    Filed: July 10, 1995
    Date of Patent: May 26, 1998
    Assignee: Warner-Lambert Company
    Inventor: Janak Khimchand Padia
  • Substituted 3-(aminoalkylamino)-1,2-benzisoxazoles and related compounds
    Patent number: 5756754
    Abstract: This application relates to compounds of the formula ##STR1## wherein R.sup.1, X, Y and n are as defined in the specification; and pharmaceutically acceptable addition salts thereof and optical and geometric isomers or racemic mixtures thereof; which compounds are useful for the treatment of various memory dysfunctions characterized by a decreased cholinergic function such as Alzheimer's disease. Compounds of this invention also inhibit monoamine oxidase and hence are useful as antidepressants.
    Type: Grant
    Filed: June 19, 1997
    Date of Patent: May 26, 1998
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Gerard J. O'Malley, Mark G. Palermo
  • Process for preparing analgesic compounds
    Patent number: 5756730
    Abstract: A process for preparing a compound of the formula (I) ##STR1## in which, R.sup.1 and R.sup.2 are the same or different and each is hydrogen or C.sub.1 -C.sub.6 alkyl, or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a heterocyclic ring which is unsubstituted or substituted and is a 5-membered or 6-membered N-heterocycle which optionally has a further heteroatom which is oxygen, nitrogen or sulfur; E is methylene; ring A is a unsubstituted or unsubstituted aryl ring, or a substituted or an unsubstituted heteroaryl ring; R.sup.3 is a C.sub.1 -C.sub.6 alkyl and R.sup.4 is hydrogen, or R.sup.3 and R.sup.4 together are a group of the formula --(CR.sup.a R.sup.b).sub.m --C(.dbd.Y)-- (IV), wherein each of R.sup.a and R.sup.b is hydrogen or C.sub.1 -C.sub.
    Type: Grant
    Filed: January 28, 1997
    Date of Patent: May 26, 1998
    Assignee: Sankyo Company, Limited
    Inventors: Atsusuke Terada, Yoshio Iizuka, Kazuyuki Wachi, Kenji Fujibayashi
  • Fused benzo compounds containing a nitrogen heterocycle for the treatment of central nervous system disorders
    Patent number: 5753661
    Abstract: Fused benzo compounds of formula I are provided, wherein A is a 2 to 6 membered hydrocarbon spacer group, B is a polar divalent group selected from a group (a); U is C, N or CH; X is a divalent 3-4 membered chain optionally comprising one or more heteroatoms; R.sup.1 is an aliphatic hydrocarbon group, arylalkyl or diphenylalkyl; R.sup.2 and R.sup.3 are hydrogen or alkyl or together form an ethylene or propylene bridge; R.sup.4, R.sup.5 and R.sup.6 are hydrogen or substituents; R.sup.7 and R.sup.8 are hydrogen or substituents including --COOR.sup.9 and --CONR.sup.10 R.sup.11 ; are 5-HT.sub.1A receptor ligands useful in the treatment of CNS disorders. Pharmaceutical compositions comprising the compounds and their use for the manufacture of a pharmaceutical preparation are also provided.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: May 19, 1998
    Assignee: H. Lundbeck A/S
    Inventors: Ejner K. Moltzen, Jens Perregaard, Henrik Pedersen
  • Metalloproteinase inhibitors, pharmaceutical compositions containing them and their pharmaceutical uses
    Patent number: 5753653
    Abstract: The invention relates to compounds of the formula I ##STR1## in which Q is a divalent radical having four ring atoms which together with C* and N form a six-membered ring, each of these four ring atoms being unsubstituted or substituted by a suitable substituent and at least one being a heteroatom selected from O, N and S, with the remainder being carbon atoms; and Ar is an aryl or heteroaryl group. The invention further relates to pharmaceutically acceptable prodrugs and pharmaceutically acceptable salts of these compounds. The invention also relates to methods of inhibiting the activity of metalloproteinases, especially MMPs or TNF-.alpha., by administering a compound of the formula I or a salt or prodrug thereof. The invention further relates to pharmaceutical compositions comprising an effective amount of these compounds, salts, and prodrugs.
    Type: Grant
    Filed: December 6, 1996
    Date of Patent: May 19, 1998
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Steven L. Bender, Michael J. Melnick
  • Carboxylic acid compound having condensed ring, salt thereof and pharmaceutical use thereof
    Patent number: 5753670
    Abstract: A novel carboxylic acid compound having a condensed ring; which is represented by the formula (I) ##STR1## wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, a pharmaceutical composition thereof and pharmaceutical use thereof. The novel carboxylic acid compound having a condensed ring and pharmacologically acceptable salt thereof of the present invention have superior GPIIb/IIIa antagonism in mammals inclusive of human; can be administered orally; have long life in blood and low toxicity; and show less side-effects. Accordingly, they are extremely useful for the prophylaxis and treatment of thrombotic diseases and other diseases.
    Type: Grant
    Filed: March 26, 1997
    Date of Patent: May 19, 1998
    Assignee: The Green Cross Corporation
    Inventors: Shinichiro Ono, Tomohiro Yoshida, Atsuyuki Ashimori, Keigo Kosaka, Takehiro Okada, Kazuhiro Maeda, Masahiro Eda, Fumio Mori, Yoshihisa Inoue, Hajime Ebisu, Teruaki Imada, Ruriko Ikegawa, Feng Wang, Norifumi Nakamura
  • Heterocyclic compounds, their production and use
    Patent number: 5753664
    Abstract: A novel compound of the formula:A--Z--Ar.sup.1 1'CO--Ar.sup.2wherein A is a condensed pyrimidinone or condensed pyridazinone ring; Ar.sup.1 and Ar.sup.2 are independently a ring; Z is a divalent group, or a salt thereof which have an excellent antitumor activity.
    Type: Grant
    Filed: March 13, 1996
    Date of Patent: May 19, 1998
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Tetsuya Aono, Shogo Marui, Fumio Itoh, Masuo Yamaoka, Masafumi Nakao
  • Dihydropyridazinones, pyridazinones and related compounds as fungicides
    Patent number: 5753642
    Abstract: This invention relates to substituted dihydropyridazinones, pyridazinones and related compounds, of the formula ##STR1## wherein A, Q, D and R1 are as defined within, compositions containing these compounds and methods of controlling agricultural and mammalian fungal diseases.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: May 19, 1998
    Assignee: Rohm and Haas Company
    Inventors: Enrique Luis Michelotti, Anne Ritchie Egan, Ronald Ross, Jr., Willie Joe Wilson
  • Antiretroviral hydrazine derivatives
    Patent number: 5753652
    Abstract: The invention relates to compounds of formula ##STR1## and salts, pharmaceutical compositions, intermediates and processes of preparation thereof.
    Type: Grant
    Filed: April 4, 1995
    Date of Patent: May 19, 1998
    Assignee: Novartis Corporation
    Inventors: Alexander Fassler, Guido Bold, Marc Lang, Shripad Bhagwat, Peter Schneider
  • Pharmaceutical diketopiperazine compounds
    Patent number: 5750530
    Abstract: A diketopiperazine of formula (I): ##STR1## wherein each of R.sub.7 and R.sub.8 which may be the same or different; is hydrogen or a nitro group;Y is ##STR2## --O-- or --S--, wherein each of R.sub.9 and R.sub.10 which may be the same or different, is hydrogen or a nitro group;n is 0, 1 or 2;m is an integer of 1 to 6;each R.sub.6, which may be the same or different, is a C.sub.1 -C.sub.6 alkyl group; andX is selected from(i) a phenyl group of the following formula ##STR3## and the salts and esters thereof; have activity as inhibitors of plasminogen activator inhibitor.
    Type: Grant
    Filed: December 17, 1996
    Date of Patent: May 12, 1998
    Assignee: Xenova Limited
    Inventors: Justin Stephen Bryans, Adrian John Folkes, Christopher John Latham
  • Quinoxalinedione derivatives, their production and use in pharmaceutical agents
    Patent number: 5750525
    Abstract: Compounds of formula I are described ##STR1## in which R.sup.1, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 have the meanings mentioned in the application as well as their production and use in pharmaceutical agents.
    Type: Grant
    Filed: March 8, 1996
    Date of Patent: May 12, 1998
    Assignee: Schering Aktiengesellschaft
    Inventors: Andreas Huth, Lechoslaw Turski