Patents Represented by Attorney, Agent or Law Firm Gabor L. Szekeres
  • Patent number: 5723666
    Abstract: Compounds of the formula ##STR1## have retinoid-like or retinoid antagonist-like biological activity.
    Type: Grant
    Filed: June 21, 1996
    Date of Patent: March 3, 1998
    Assignee: Allergan
    Inventors: Vidyasagar Vuligonda, Richard L. Beard, Alan T. Johnson, Min Teng, Tae K. Song, Roshantha A. Chandraratna
  • Patent number: 5723620
    Abstract: A compound of the formula ##STR1## wherein all variables are as defined in the specification having retinoid-like activity.
    Type: Grant
    Filed: November 3, 1995
    Date of Patent: March 3, 1998
    Assignee: Allergan
    Inventors: Vidyasagar Vuligonda, Min Teng, Richard L. Beard, Alan T. Johnson, Yuan Lin, Roshantha A. Chandraratna
  • Patent number: 5716952
    Abstract: Pharmaceutical compositions and a method are disclosed for treating glaucoma and/or ocular hypertension in the mammalian eye by administering to the mammalian eye the pharmaceutical composition of the invention which contains as the active ingredient one or more muscarinic antagonist compounds. Examples of muscarinic antagonists utilized in the pharmaceutical composition and method of treatment are: 10H-thieno(3,4-b)(1,5)benzodiazepin-10-one 4,9-dihydro-3-methyl-4-((4-methyl-1-piperazinyl)acetyl) (telenzepine); 5,11-dihydro-11?4'-methyl-1'-piperazinyl)-acetyl!-6H-pyrido?2,3-b!?1,4!ben zodiazepin-6-one (pirenzepine); racemic 11-??2-(Diethylamino)methyl!-1-piperidinyl!-acetyl!-5,11-dihydro-6H-pyrido ?2,3-b!?1,4!benzodiazepin-6-one (AF-DX 116); dextrorotatory 11-??2-(Diethylamino)methyl!-1-piperidinyl!-acetyl!-5,11-dihydro-6H-pyrido ?2,3-b!?1,4! benzodiazepin-6-one (AF-DX 250); an ophthalmically acceptable salt of 4-diphenylacetoxy-1,1-dimethyl piperidine (4-DAMP); .alpha.-cyclohexyl, -.alpha.
    Type: Grant
    Filed: March 18, 1992
    Date of Patent: February 10, 1998
    Assignee: Allergan
    Inventors: Elizabeth WoldeMussie, Guadalupe Ruiz
  • Patent number: 5714621
    Abstract: Compounds of the formula ##STR1## where W is (CH.sub.2).sub.n where n is 1 or 2, or n is 0 and W represents lower alkyl groups attached to each oxygen;m is an integer between 1 and 8;R.sub.1 is COOH or a pharmaceutically acceptable salt thereof, COOR.sub.4, CONR.sub.5 R.sub.6, CONR.sub.5 SO.sub.2 R.sub.7, CH.sub.2 OH, CH.sub.2 OR.sub.7, CH.sub.2 O--COR.sub.7, CH.sub.2 O--CONR.sub.5,R.sub.7, CH.sub.2 OCOOR.sub.7, CH.sub.2 NH.sub.2, CH.sub.2 NR.sub.5 R.sub.6, CH.sub.2 NR.sub.5 COR.sub.7, CHO, CH(OR.sub.8).sub.2, CHOR.sub.9 O, --COR.sub.10, CR.sub.10 (OR.sub.8).sub.2, or CR.sub.10 OR.sub.9 O, where R.sub.4 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R.sub.4 is phenyl or lower alkylphenyl, R.sub.5 and R.sub.6 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or phenyl or lower alkylphenyl, R.sub.7 is alkyl of 1 to 10 carbons, phenyl or lower alkylphenyl, R.sub.8 is lower alkyl, and R.sub.
    Type: Grant
    Filed: February 27, 1996
    Date of Patent: February 3, 1998
    Assignee: Allergan
    Inventors: Robert M. Burk, David F. Woodward
  • Patent number: 5710288
    Abstract: Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification, are capable of lowering intraocular pressure in the eye of a mammal.
    Type: Grant
    Filed: May 3, 1996
    Date of Patent: January 20, 1998
    Assignee: Allergan
    Inventors: Robert M. Burk, David F. Woodward
  • Patent number: 5708015
    Abstract: A pharmaceutical composition, useful for treating animals of the mammalian species, including humans, to treat diseases and conditions which normally respond to treatment with alpha.sub.2 adrenergic agents, contains as its active alpha.sub.2 adrenergic agent ingredient one or more compounds of the formula ##STR1## where X is O, S or NH; n is an integer with the values of 0, 1 or 2; when n is 0 then R.sub.1 is lower alkyl having 1 to 6 carbon atoms and R.sub.2 is H or lower alkyl having 1 to 6 carbon atoms; when n is 1 or 2, then R.sub.1 and R.sub.2 both are methylene (CH.sub.2), or methylene substituted with an R.sub.5 group where R.sub.5 is lower alkyl of 1 to 6 carbons; R.sub.3 and R.sub.4 independently are H or lower alkyl having 1 to 6 carbons; R.sub.6 is H or lower alkyl of 1 to 6 carbons.
    Type: Grant
    Filed: October 29, 1996
    Date of Patent: January 13, 1998
    Assignee: Allergan
    Inventors: Michael E. Garst, James E. Burke, Larry A. Wheeler
  • Patent number: 5698700
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 -R.sub.5 X, Y, A, B are as defined in the specification have retinoid-like biological activity.
    Type: Grant
    Filed: May 31, 1996
    Date of Patent: December 16, 1997
    Assignee: Allergan
    Inventors: Tae K. Song, Roshantha A. Chandraratna
  • Patent number: 5696162
    Abstract: Compounds of Formula 1 ##STR1## wherein m is 1-4; R.sub.1 -R.sub.4 independently are hydrogen, lower alkyl of 1 to 6 carbons, Cl, Br, or I; R.sub.5 is hydrogen, lower alkyl of 1 to 6 carbons, Cl, Br, I, lower alkoxy or lower thioalkoxy of 1-6 carbons; R.sub.6 is hydrogen, lower alkyl, Cl, Br, I, OR.sub.11, SR.sub.11, OCOR.sub.11, SCOR.sub.11, NH.sub.2, NHR.sub.11, N(R.sub.11).sub.2, NHCOR.sub.11 OR NR.sub.11 --COR.sub.11 ; R.sub.20 is independently hydrogen or lower alkyl; Y is an aromatic group such as phenyl or naphthyl, or a heteroaryl group selected from a group consisting of pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl and oxazolyl; A is (CH.sub.2).sub.n where n is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds, alkynyl having 2-6 carbons and 1 or 2 triple bonds; 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.2 OR.sub.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: December 9, 1997
    Assignee: Allergan
    Inventor: Roshantha A. Chandraratna
  • Patent number: 5688957
    Abstract: Compounds of the formula ##STR1## where R.sub.1, R.sub.2, R.sub.3, and R.sub.4 independently are H or lower alkyl of 1 to 10 carbons; R.sub.5 is lower alkyl of 1 to 10 carbons, fluoro, chloro, bromo, iodo, nitro, or fluoroalkyl having 1 to 10 carbons; m is an integer having the value of 1-4; n is an integer having the value of 0-4; Y is phenyl or a heteroaryl group selected from a group consisting of pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl and oxazolyl, said Y group being optionally substituted with one or more R.sub.5 group; A is (CH.sub.2).sub.p where p is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds, alkynyl having 2-6 carbons and 1 or 2 triple bonds, and 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.2 OR.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.
    Type: Grant
    Filed: December 29, 1995
    Date of Patent: November 18, 1997
    Assignee: Allergan
    Inventors: Min Teng, Roshantha A. Chandraratna
  • Patent number: 5677320
    Abstract: Compounds of Formula 1 ##STR1## wherein the symbols are as defined in the specification, have retinoid like biological activity.
    Type: Grant
    Filed: January 9, 1997
    Date of Patent: October 14, 1997
    Assignee: Allergan
    Inventor: Roshantha A. Chandraratna
  • Patent number: 5677323
    Abstract: Retinoid-like activity is exhibited by compounds of the formula ##STR1## where X is S, O; R.sub.1, R.sub.2 and R.sub.3 are hydrogen or lower alkyl; R.sub.4 and R.sub.5 are hydrogen or lower alkyl with the proviso that R.sub.4 and R.sub.5 cannot both be hydrogen, A is, oxazolyl; n is 0-5, and B is H, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH.sub.2 OH or an ether or ester derivative, or --CHO or an acetal derivative, or --COR.sub.1 or a ketal derivative where R.sub.1 is --(CH.sub.2).sub.m CH.sub.3 where m is 0-4, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: October 29, 1996
    Date of Patent: October 14, 1997
    Assignee: Allergan
    Inventor: Roshantha A. S. Chandraratna
  • Patent number: 5677451
    Abstract: Compounds of the formula ##STR1## where R.sub.1 and R.sub.2, independently are alkyl groups having 2 to 8 carbons; R.sub.3 is hydrogen or lower alkyl; X is S, O or N-R.sub.4 where R.sub.4 is hydrogen or lower alkyl; Y is phenyl or pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, and pyrazinyl; A is (CH.sub.2).sub.n where n is 0-5, or lower branched chain alkyl, alkenyl having 2 to 6 carbons and 1 or 2 double bonds, alkynyl having 2 to 6 carbons and 1 or 2 triple bonds; B is hydrogen, COOH or a salt thereof, COOR.sub.5, CONR.sub.6 R.sub.7, --CH.sub.2 OH, CH.sub. 2OR.sub.8, CH.sub.2 OCOR.sub.8, CHO, CH(OR.sub.9).sub.2, CHOR.sub.10 O, --COR.sub.11, CR.sub.11 (OR.sub.9).sub.2, or CR11OR.sub.10 O, where R.sub.5 is alkyl of 1 to 10 carbons, or cycloalkyl of 5 to 10 carbons, or R.sub.5 is phenyl or lower alkylphenyl, R.sub.6 and R.sub.7 independently are hydrogen, alkyl of 1 to 10 carbons, or cycloalkyl of 5 to 10 carbons, or phenyl or lower alkylphenyl, R.sub.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: October 14, 1997
    Assignee: Allergan
    Inventor: Roshantha A. S. Chandraratna
  • Patent number: 5675024
    Abstract: Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification have retinoid-like biological activity.
    Type: Grant
    Filed: November 22, 1995
    Date of Patent: October 7, 1997
    Assignee: Allergan
    Inventors: Min Teng, Tien T. Duong, Roshantha A. Chandraratna
  • Patent number: 5674910
    Abstract: Compounds of the formula ##STR1## where the dotted line represents a bond or the absence of a bond, the wavy lines represent bonds which are either in cis or trans configuration; R.sub.1 represents H, or CO--R.sub.2 where R.sub.2 is lower alkyl of 1 to 6 carbons, carbocyclic aryl or heterocyclic aryl; or carbocyclic aryl or heteroaryl substituted lower alkyl group; X represents CO--NR.sub.3 R.sub.4, CH.sub.2 OH, CH.sub.2 OR.sub.5, CH.sub.2 O--COR.sub.6, and CH.sub.2 --NR.sub.3 R.sub.4, where R.sub.3 and R.sub.4 independently are H or lower alkyl, R.sub.5 is lower alkyl of 1 to 6 carbons, and R.sub.6 is lower alkyl of 1 to 6 carbons, carbocyclic aryl or heterocyclic aryl; or carbocyclic aryl or heteroaryl substituted lower alkyl group, and n is an integer between 0 and 8 are capable of lowering intraocular pressure in the eye of a mammal.
    Type: Grant
    Filed: December 14, 1995
    Date of Patent: October 7, 1997
    Assignee: Allergan
    Inventors: Michael E. Garst, Robert M. Burk
  • Patent number: 5675033
    Abstract: Compounds of Formula 1 ##STR1## wherein Z is selected from the group consisting of the radicals shown in Formula 2 and in Formula 3, ##STR2## Y is cycloalkyl or cycloalkenyl of 3 to 8 carbons optionally substituted with one or two R.sub.4 groups, or Y is selected from phenyl, pyridyl, thienyl, furyl, pyrrolyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, oxazolyl, and imidazolyl, said groups being optionally substituted with one or two R.sub.4 groups, the divalent Y radical being substituted by the Z and --CR.sub.1 .dbd.CR.sub.1 --CR.sub.1 .dbd.CR.sub.1 groups on adjacent carbons; X is S, O, or NR.sub.5 ; n is 1 or 2; R.sub.1 and R.sub.2 independently are H, lower alkyl or fluoroalkyl; R.sub.3 is hydrogen, lower alkyl, Cl or Br; R.sub.4 is lower alkyl, fluoroalkyl or halogen; R.sub.5 is H or lower alkyl, and 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.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: October 7, 1997
    Assignee: Allergan
    Inventors: Vidyasagar Vuligonda, Roshantha A. Chandraratna
  • Patent number: 5672710
    Type: Grant
    Filed: November 3, 1995
    Date of Patent: September 30, 1997
    Assignee: Allergan
    Inventors: Richard L. Beard, Diana F. Colon, Roshantha A. Chandraratna
  • Patent number: 5663347
    Abstract: Compounds of the formula ##STR1## where R.sub.1 and R.sub.2, independently are alkyl groups having 2 to 8 carbons; R.sub.3 is hydrogen or lower alkyl; X is S, O or N--R.sub.4 where R.sub.4 is hydrogen or lower alkyl; Y is phenyl or pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, and pyrazinyl; A is (CH.sub.2).sub.n where n is 0-5, or lower branched chain alkyl, alkenyl having 2 to 6 carbons and 1 or 2 double bonds, alkynyl having 2 to 6 carbons and 1 or 2 triple bonds; B is hydrogen, COOH or a salt thereof, COOR.sub.5, CONR.sub.6 R.sub.7, --CH.sub.2 OH, CH.sub.2 OR.sub.8, CH.sub.2 OCOR.sub.8, CHO, CH(OR.sub.9).sub.2, CHOR.sub.10 O, --COR.sub.11, CR.sub.11 (OR.sub.9).sub.2, or CR.sub.11 OR.sub.10 O, where R.sub.5 is alkyl of 1 to 10 carbons, or cycloalkyl of 5 to 10 carbons, or R.sub.5 is phenyl or lower alkylphenyl, R.sub.6 and R.sub.7 independently are hydrogen, alkyl of 1 to 10 carbons, or cycloalkyl of 5 to 10 carbons, or phenyl or lower alkylphenyl, R.sub.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: September 2, 1997
    Assignee: Allergan
    Inventor: Roshantha A. S. Chandraratna
  • Patent number: 5663357
    Abstract: Compounds of the formula ##STR1## wherein the symbols have the meaning described in the specification, have retinoid-like biological activity.
    Type: Grant
    Filed: November 22, 1995
    Date of Patent: September 2, 1997
    Assignee: Allergan
    Inventors: Min Teng, Tien T. Duong, Roshantha A. Chandraratna
  • Patent number: 5648514
    Abstract: Compounds of the formula ##STR1## wherein the symbols have the meaning described in the specification, have retinoid-like biological activity.
    Type: Grant
    Filed: December 29, 1994
    Date of Patent: July 15, 1997
    Assignee: Allergan
    Inventors: Alan T. Johnson, Min Teng, Vidyasagar Vuligonda, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Roshantha A. Chandraratna
  • Patent number: 5648503
    Abstract: Compounds of the formula ##STR1## which have retinoid-like biological activity.
    Type: Grant
    Filed: May 31, 1996
    Date of Patent: July 15, 1997
    Assignee: Allergan
    Inventors: Vidyasagar Vuligonda, Richard L. Beard, Alan T. Johnson, Min Teng, Tae K. Song, Roshantha A. Chandraratna