Polycyclo Ring System Patents (Class 564/270)
  • Patent number: 6114392
    Abstract: The invention relates to the use of agmatine, in the treatment of acute neurotrauma (such as stroke) and degenerative disorders of the central and peripheral nervous system (such as dementia).The invention further provides novel compounds of general formula I (which are quinuclidine derivatives), formula II (which are norbornane derivatives), formula III (which are adamantane derivatives), and formula IV (which are phenothiazine derivatives): ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are each independently hydrogen, hydroxy, substituted or unsubstituted C.sub.1-4 alkyl, substituted or unsubstituted C.sub.1-4 alkoxy, halogeno, amino, phenyl, or R.sub.4 NR.sub.5 ; R.sub.4 and R.sub.5 are each independently hydrogen, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NH--NHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--(NR.sub.7 .dbd.)CNHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NH(NR.sub.7 .dbd.)CNHR.sub.6 wherein n is from 0-5, y is from 0-5 and each x is independently from 1-5; R.
    Type: Grant
    Filed: April 16, 1996
    Date of Patent: September 5, 2000
    Inventors: Gad M. Gilad, Varda H. Gilad
  • Patent number: 6054614
    Abstract: 4-(3,4-Dichlorophenyl)-3,4-dihydro-2H-naphthalen-1-ylidene-methylamine and related analogs are prepared from .alpha.-tetralone by a facile three-step process. This compound is the required intermediate to prepare sertraline, (1S-cis)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthylamin e. Sertraline has selective serotonin uptake inhibitor activity making it a valuable antidepressant pharmaceutical product.
    Type: Grant
    Filed: April 23, 1998
    Date of Patent: April 25, 2000
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Sai P. Shum, Paul A. Odorisio, Stephen D. Pastor
  • Patent number: 6002034
    Abstract: Certain olefins such as ethylene, .alpha.-olefins and cyclopentene can be polymerized by using catalyst system containing a nickel or palladium .alpha.-diimine complex, a metal containing hydrocarbylation compound, and a selected Lewis acid, or a catalyst system containing certain nickel[II] or palladium[II] compounds, an .alpha.-diimine, a metal containing hydrocarbylation compound, and optionally a selected Lewis acid. The process advantageously produces polyolefins useful for molding resins, films, elastomers and other uses.
    Type: Grant
    Filed: October 14, 1998
    Date of Patent: December 14, 1999
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Stephan James McLain, Jerald Feldman
  • Patent number: 5886224
    Abstract: Disclosed herein are processes for polymerizing ethylene, acyclic olefins, and/or selected cyclic olefins, and optionally selected olefinic esters or carboxylic acids, and other monomers. The polymerizations are catalyzed by selected transition metal compounds, and sometimes other co-catalysts. Since some of the polymerizations exhibit some characteristics of living polymerizations, block copolymers can be readily made. Many of the polymers produced are often novel, particularly in regard to their microstructure, which gives some of them unusual properties. Numerous novel catalysts are disclosed, as well as some novel processes for making them. The polymers made are useful as elastomers, molding resins, in adhesives, etc. Also described herein is the synthesis of linear .alpha.-olefins by the oligomerization of ethylene using as a catalyst system a combination a nickel compound having a selected .alpha.-diimine ligand and a selected Lewis or Bronsted acid, or by contacting selected .alpha.
    Type: Grant
    Filed: July 10, 1997
    Date of Patent: March 23, 1999
    Assignees: E. I. du Pont de Nemours and Company, University of North Carolina
    Inventors: Maurice S. Brookhart, Lynda Kaye Johnson, Samuel David Arthur, Jerald Feldman, Kristina Ann Kreutzer, Alison Margaret Anne Bennett, Edward Bryan Coughlin, Steven Dale Ittel, Anju Parthasarathy, Daniel Joseph Tempel
  • Patent number: 5846907
    Abstract: Pyrazol-4-ylbenzoyl compounds of the formula I ##STR1## where Z is a 5- or 6-membered heterocyclic saturated or unsaturated radical, Q is a pyrazole ring and L and M are as defined in the specification, their use as herbicidal compounds and to processes for preparing the compounds.
    Type: Grant
    Filed: July 30, 1997
    Date of Patent: December 8, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Wolfgang von Deyn, Regina Luise Hill, Uwe Kardorff, Stefan Engel, Martina Otten, Marcus Vossen, Peter Plath, Harald Rang, Albrecht Harreus, Hartmann Konig, Helmut Walter, Karl-Otto Westphalen, Ulf Misslizt
  • Patent number: 5705694
    Abstract: The present invention provides a novel trinitrofluorenonimine derivative represented by the general formula (1): ##STR1## wherein R.sup.0 is an alkyl group; and R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different and indicate a hydrogen atom, an alkyl, an alkoxy, an aryl, an aralkyl, a halogen atom or an alkyl halide. This derivative is superior in electron transferring capability and compatibility with binding resin. Accordingly, an electrophotosensitive material comprising this derivative as an electron transferring material is superior in sensitivity.
    Type: Grant
    Filed: November 17, 1995
    Date of Patent: January 6, 1998
    Assignee: Mita Industrial Co., Ltd.
    Inventors: Hirofumi Kawaguchi, Yasufumi Mizuta, Syunichi Matsumoto, Nobuko Akiba, Toshiyuki Fukami, Ichiro Yamazato, Hisakazu Uegaito, Yuji Tanaka
  • Patent number: 5639912
    Abstract: A dianilinoglutacondialdehyde compound is described, which is represented by the following formula (Ia) or (Ib): ##STR1## wherein R.sup.1 and R.sup.2 each represents an alkyl group or an aryl group and may be connected to each other; R.sup.3 represents a hydrogen atom, an alkyl group, an alkoxy group or a halogen atom; R.sup.4 and R.sup.5 each represents a hydrogen atom or a non-metallic atom which is required to be connected to each other to form a 5- or 6-membered ring; and X.sup.- represents BF.sub.4.sup.-, SbF.sub.6.sup.- or PF.sub.6.sup.-. A process for the preparation of the compound as described above is also described.
    Type: Grant
    Filed: April 3, 1996
    Date of Patent: June 17, 1997
    Assignee: Fuji Photo Film co., Ltd.
    Inventor: Toru Harada
  • Patent number: 5599967
    Abstract: Compounds of the formula ##STR1## wherein the symbols have the meaning defined in the specification have retinoid-like biological activity.
    Type: Grant
    Filed: December 29, 1994
    Date of Patent: February 4, 1997
    Assignee: Allergan
    Inventors: Vidyasagar Vuligonda, Richard L. Beard, Alan T. Johnson, Min Teng, Tae K. Song, Roshantha A. Chandraratna
  • Patent number: 5498755
    Abstract: Compounds of the formula ##STR1## wherein the R.sub.1 groups independently are hydrogen, lower alkyl, or two geminal R.sub.1 groups jointly represent an oxo (.dbd.O) or a thio (.dbd.S) group; R.sub.2 is hydrogen or lower alkyl, or halogen; M is or --N.dbd.CR.sub.4 -- or --R.sub.4 C.dbd.N-- where R.sub.4 is hydrogen or lower alkyl; X is C(R.sub.1).sub.2 ; Y is phenyl optionally substituted with an R.sub.3 group which is lower alkyl or halogen; A is (CH.sub.2).sub.n where n is 0-5, lower branched chain alkyl, cycloalkyl, alkenyl, alkynyl; B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.7, CR.sub.7 (OR.sub.12).sub.2, or CR.sub.7 OR.sub.13 O, where R.sub.7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R.sub.8 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R.sub.8 is phenyl or lower alkylphenyl, R.
    Type: Grant
    Filed: August 23, 1994
    Date of Patent: March 12, 1996
    Inventors: Roshantha A. Chandraratna, Min Teng
  • Patent number: 5461078
    Abstract: Compounds of formula (I) ##STR1## in which R.sub.1 is CH.dbd.CHR, CH.dbd.NNHR, CH.dbd.N--A--N(O)R'R" or CH.sub.2 --NH--A--N(O)R'R" and R.sub.2 is separately selected from hydrogen, CH.dbd.CHR, CH.dbd.NNHR, CH.dbd.N--A--(O)R'R" and CH.sub.2 --NH--A--N(O)R'R", wherein A is a C.sub.2-4 alkylene group with a chain length between N or NH and N(O)R'R" of at least 2 carbon atoms, R is a thiazolyl or imidazolyl group in which the tertiary nitrogen atom is in N-oxide form, and R' and R" are each separately selected from C.sub.1-4 alkyl groups and C.sub.2-4 hydroxyalkyl and C.sub.3-4 dihydroxyalkyl groups in which the carbon atom attached to the nitrogen atom does not carry a hydroxy group and no carbon atom is substituted by two hydroxy groups, or R' and R" together are a C.sub.2-6 alkylene group which with the nitrogen atom to which R' and R" are attached forms a heterocyclic group having 3 to 7 atoms in the ring, and R.sub.3, R.sub.4, R.sub. 5 and R.sub.
    Type: Grant
    Filed: October 12, 1993
    Date of Patent: October 24, 1995
    Assignee: British Technology Group Limited
    Inventor: Laurence H. Patterson
  • Patent number: 5154887
    Abstract: Certain phenalenimine fluorescent compounds represented by the structure ##STR1## wherein R' and R" are independently hydrogen, alkyl, cycloalkyl, aryl or a heterocycle, or R' comprises the carbon and heteroatoms which form a fused ring with the compound nucleus, are useful in biomedical and analytical determinations. These compounds can be used for staining cells, as well as for the determination of various analytes found in human or animal biological fluids. Such determinations can be carried out in solution or by using dry analytical elements. The fluorescent compounds can be reacted with quinone nuclei to form reducible compounds which are also useful in analytical methods. In addition, the compounds can be incorporated into what are known as "loadable" latex particles to form detectable labels and biological reagents.
    Type: Grant
    Filed: May 28, 1991
    Date of Patent: October 13, 1992
    Assignee: Eastman Kodak Company
    Inventors: Bruce E. Babb, Fred T. Oakes
  • Patent number: 5112869
    Abstract: This invention concerns compounds having the structure: ##STR1## wherein each of R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.2', R.sup.3', R.sup.4', and R.sup.5', is independently hydrogen (--H), or a hydroxyl (--OH), methoxy (--OMe), methyl (--Me), carboxaldehyde (--CHO) or phenylformazen (Ph--N.dbd.CH--) group.This invention also provides a novel process of synthesizing the compounds of the subject invention, including intermediate compounds useful in the process.The present invention also provides pharmaceutical compositions comprising a pharmaceutically effective amount of a compound according to the subject invention and a pharmaceutically acceptable carrier. Finally, the invention provides spermicidal methods and methods of killing or of retarding the proliferation of, cancer cells.
    Type: Grant
    Filed: April 4, 1989
    Date of Patent: May 12, 1992
    Assignee: Sloan-Kettering Institute For Cancer Research
    Inventors: Kyoichi A. Watanabe, Tsann-Long Su, Jai-Tung Huang
  • Patent number: 5079245
    Abstract: The compounds 2-trifluoromethyl-7-substituted-6,7,8,9-tetrahydro-[5H]-benzocycloheptenes are disclosed and disclosed to be useful in the treatment of metabolic illnesses such as diabetes, obesity, and their complications. A perferred compound is 2-trifluoromethyl-7-amino-6,7,8,9-tetrahydro-[5H-benzocycloheptane.
    Type: Grant
    Filed: July 5, 1989
    Date of Patent: January 7, 1992
    Assignee: Adir et Compagnie
    Inventors: Michel Wierzbicki, Pierre Hugon, Jacques Duhault, Francoise Lacour
  • Patent number: 4855500
    Abstract: An improved condensation process for preparing N-[4-(3,4-dichlorophenyl)-3,4-dihydro-1(2H)-naphthalenylidene]methanamine from 4-(3,4-dichlorophenyl)-3,4-dihydro-1(2H)-naphthalenone and methylamine is disclosed. The process involves the use of a hydratable molecular sieve having a pore size that is at least about three Angstrom units in diameter as the dehydrating agent (catalyst) in a reaction-inert aprotic organic solvent. The ketimine final product so produced is known to be useful as an intermediate leading to cis-(1S)(4S)-N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthal enamine (sertraline), which is an anti-depressant agent.
    Type: Grant
    Filed: May 4, 1988
    Date of Patent: August 8, 1989
    Assignee: Pfizer Inc.
    Inventor: James C. Spavins
  • Patent number: 4788130
    Abstract: Novel 2,3-dihydro-1H-indene derivatives and salts thereof represented by the general formula (1), ##STR1## [wherein R.sup.1 and R.sup.2 are each a hydrogen atom, a lower alkyl group, a phenyl group which may have halogen atoms and/or alkyl groups as the substituents on the phenyl ring; R.sup.3 is a halogen atom or a lower alkyl group; R.sup.4 is a hydrogen atom, a halogen atom, a phenyl-lower alkyl group, a cycloalkyl-lower alkyl group or the like; R.sup.5 is a hydroxyimino group, an alkylamino group or a group of the formula --NHR.sup.8 (wherein R.sup.8 is a hydrogen atom, a halogen-substituted lower alkanoyl group or the like); R.sup.6 is a hydrogen atom or a phenyl group; and R.sup.7 is a hydrogen atom or a lower alkyl group].
    Type: Grant
    Filed: August 29, 1985
    Date of Patent: November 29, 1988
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Yasuo Oshiro, Hiraki Ueda, Kazuyuki Nakagawa
  • Patent number: 4232158
    Abstract: 10,11-Dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imines, derivatives and pharmaceutically acceptable salts thereof are useful as antianxiety agents, as muscle relaxants and in the treatment of extrapyramidal disorders such as in Parkinson's disease. They are prepared by treatment of a 5H-dibenzo[a,d]cyclohepten-5-one with ammonia to give the 5-imine, acylation of the imine, treatment of the protected imine with an organolithium to provide the 5-substituted-5-acylamino compound, treatment with acid or base to cause ring closure to a 5-substituted-5,10-acylimino compound followed by removal of the protecting group, either hydrolytically or hydrogenolytically.
    Type: Grant
    Filed: June 4, 1979
    Date of Patent: November 4, 1980
    Assignee: Merck & Co., Inc.
    Inventors: Kenneth L. Shepard, Daniel G. Brenner