Patents Represented by Attorney Prabodh I. Almaula
  • Patent number: 6156534
    Abstract: Disclosed is a process for the synthesis of .beta.-lactam antibacterials using soluble side chain esters in the presence of enzyme acylase. Also disclosed are novel esters useful as reactants in said process.
    Type: Grant
    Filed: October 22, 1998
    Date of Patent: December 5, 2000
    Assignee: Bristol-Myers Squibb Company
    Inventors: John J. Usher, Guna Romancik
  • Patent number: 5922907
    Abstract: Disclosed is a process for the synthesis of .beta.-lactam antibacterials using soluble side chain esters in the presence of enzyme acylase. Also disclosed are novel esters useful as reactants in said process.
    Type: Grant
    Filed: July 17, 1997
    Date of Patent: July 13, 1999
    Assignee: Bristol-Myers Squibb Co.
    Inventors: John J. Usher, Guna Romancik
  • Patent number: 5869734
    Abstract: A process for preparing optically active (S)-(-) and (R)-(+)-deoxyspergualin and salts thereof of the formula I ##STR1## by reacting a compound of formula II ##STR2## with a compound of formula III ##STR3## in the presence of a condensing/dehydrating agent and an organic or inorganic base in an organic solvent to form a compound of formula IV ##STR4## which can then be converted to the desired final product of formula I via deprotection and hydrogenolysis.
    Type: Grant
    Filed: September 23, 1996
    Date of Patent: February 9, 1999
    Assignee: Bristol-Myers Squibb Co.
    Inventors: Xuebao Wang, John K. Thottathil
  • Patent number: 5837702
    Abstract: Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein X is alkyl, Y is a single bond, --CH.sub.2 --, --C(O)--, --O--, --S-- or --N(R.sup.8)-- where R.sup.8 is hydrogen, alkyl, haloalkyl, aryl, arylalkyl, cycloalkyl or (cycloalkyl)alkyl, and R.sup.1 to R.sup.7 are as defined herein. These compounds have potassium channel activating activity and are useful, therefore for example, as cardiovascular agents.
    Type: Grant
    Filed: August 30, 1994
    Date of Patent: November 17, 1998
    Assignee: Bristol-Myers Squibb Co.
    Inventors: George C. Rovnyak, Karnail S. Atwal, Dinos P. Santafianos, Charles Z. Ding
  • Patent number: 5837828
    Abstract: The present invention concerns neutral sugar derivatives of pradimicins, their use as antifungal agents, methods for their preparation, and intermediates for their synthesis.
    Type: Grant
    Filed: May 2, 1995
    Date of Patent: November 17, 1998
    Assignee: Bristol-Myers Squibb Co.
    Inventors: Shimpei Aburaki, Tetsuro Yamasaki, Toshikazu Oki, Seiji Iimura, Hajime Kamachi, Hideo Kamei, Takayuki Naito
  • Patent number: 5705645
    Abstract: Antibacterial activity is exhibited by novel compounds having the formula ##STR1## where R.sub.1, R.sub.2, and M are as defined herein and X is --(CH.sub.2).sub.n -- wherein n is 0, 1, 2, 3 or 4 or CR.sub.3 R.sub.4 wherein R.sub.3 and R.sub.4 are the same or different and each is hydrogen, --CH.sub.3 or --C.sub.2 H.sub.5 or R.sub.3 and R.sub.4 taken together with the carbon atom to which they are attached form a 3, 4, 5, 6 or 7-membered cycloalkyl ring.
    Type: Grant
    Filed: March 7, 1995
    Date of Patent: January 6, 1998
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: William H. Koster, Joseph E. Sundeen, Henner Straub, Peter Ermann, Uwe D. Treuner, Kent Amsberry, Michael Fakes, Sailesh A. Varia
  • Patent number: 5627192
    Abstract: The present invention relates to novel dihydroquinolines which are useful for cholesterol lowering and as antioxidant agents. Also provided is a process for preparing the dihydroquinolines of the present invention, pharmaceutical compositions, and a method of treating or inhibiting hypercholesterolemia, hyperlipidemia, atherosclerosis, and LDL oxidation which comprises administering to birds and mammals in need of such treatment an effective amount of a compound of the present invention.
    Type: Grant
    Filed: March 15, 1995
    Date of Patent: May 6, 1997
    Assignee: Bristrol-Myers Squibb Company
    Inventors: Bradley C. Pearce, John J. Wright
  • Patent number: 5411969
    Abstract: The present invention relates to novel dihydroquinolines which are useful for cholesterol lowering and as antioxidant agents. Also provided is a process for preparing the dihydroquinolines of the present invention, pharmaceutical compositions, and a method of treating or inhibiting hypercholesterolemia, hyperlipidemia, atherosclerosis, and LDL oxidation which comprises administering to birds and mammals in need of such treatment an effective amount of a compound of the present invention.
    Type: Grant
    Filed: April 16, 1993
    Date of Patent: May 2, 1995
    Assignee: Bristol-Myers Squibb Company
    Inventors: Bradley C. Pearce, John J. Wright
  • Patent number: 5410029
    Abstract: The present invention concerns neutral sugar derivatives of pradimicins, their use as antifungal agents, methods for their preparation, and intermediates for their synthesis.
    Type: Grant
    Filed: March 10, 1994
    Date of Patent: April 25, 1995
    Assignee: Bristol-Myers Squibb Company
    Inventors: Shimpei Aburaki, Tetsuro Yamasaki, Toshikazu Oki, Seiji Iimura, Hajime Kamachi, Hideo Kamei, Takayuki Naito
  • Patent number: 5391765
    Abstract: The present invention relates to novel nitroxides which are useful for cholesterol lowering and as antioxidant agents. Also provided is a process for preparing the nitroxides of the present invention, pharmaceutical compositions, and a method of treating or inhibiting hypercholesterolemia, hyperlipidemia, atherosclerosis, and LDL oxidation which comprises administering to birds and mammals, in need of such treatment an effective amount of a compound of the present invention.
    Type: Grant
    Filed: April 16, 1993
    Date of Patent: February 21, 1995
    Assignee: Bristol-Myers Squibb Company
    Inventors: Bradley C. Pearce, John J. Wright
  • Patent number: 5380713
    Abstract: This invention relates to novel arginine aldehydes, their salts and hydrates, which compounds selectively exhibit serine proteases inhibitory activity, are highly stable in aqueous solutions, and are useful for anti-trypsin and anti-thrombin activity.
    Type: Grant
    Filed: April 11, 1994
    Date of Patent: January 10, 1995
    Assignee: Bristol-Myers Squibb Company
    Inventors: Neelakantan Balasubramanian, Denis R. St. Laurent
  • Patent number: 5380854
    Abstract: A novel series of oxazole derivatives having enhanced water solubility bioavailability and metabolic stability is disclosed in the Formula I ##STR1## or pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: July 14, 1993
    Date of Patent: January 10, 1995
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jeffrey L. Romine, Nicholas A. Meanwell, Scott W. Martin
  • Patent number: 5362879
    Abstract: A novel series of oxazole derivatives having the Formulae I and II ##STR1## wherein R is H or C.sub.1 -C.sub.5 lower alkyl,X is N or CH,Y is H or CO.sub.2 R.sup.1, or CO.R.sup.2, provided that when X isCH, Y is not H,R.sup.1 is C.sub.1 -C.sub.5 lower alkyl, or phenylmethyl, andR.sup.2 is C.sub.1 -C.sub.5 alkyl; ##STR2## wherein R is H or C.sub.1 -C.sub.5 lower alkyl,X is (CH.sub.2).sub.n or para or meta substituted phenylwherein the substituent is OR.sup.2,R.sup.2 is C.sub.1 -C.sub.5 alkyl, andn is an integer of 4 to 8,or a pharmaceutically acceptable salt thereof.The compounds are useful as inhibitors of ADP-induced blood platelet aggregation in human platelet-rich plasma.
    Type: Grant
    Filed: April 15, 1993
    Date of Patent: November 8, 1994
    Assignee: Bristol-Myers Squibb Company
    Inventor: Nicholas A. Meanwell
  • Patent number: 5348960
    Abstract: A series of 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-ones having enhanced water solubility bioavailability and metabolic stability is disclosed in the Formula I ##STR1## wherein R.sup.1 is H, or C.sub.1 -C.sub.4 lower alkyl;R.sup.2 is H, or (CH.sub.2).sub.m R.sup.3 ;R.sup.3 is tetrahydro-2H-pyranyl, C.sub.1 -C.sub.8 alkyl, C.sub.4 -C.sub.8 cycloalkyl, or substituted or unsubstituted phenyl, wherein the substituents are halogen, alkoxy, or trifluoromethyl;m is an integer of 1-3; andn is an integer of 1-5;or pharmaceutically acceptable salt thereof.The compounds are useful as inhibitors of ADP-induced blood platelet aggregation in human platelet-rich plasma.
    Type: Grant
    Filed: August 30, 1993
    Date of Patent: September 20, 1994
    Assignee: Bristol-Myers Squibb Company
    Inventors: Piyasena Hewawasam, Nicholas A. Meanwell
  • Patent number: 5348969
    Abstract: A novel series of oxazole derivatives having enhanced water solubility bioavailability and metabolic stability is disclosed in the Formula I ##STR1## Y is CH.sub.3, Ph, or OH, provided that when Y is OH, the compound exists in the keto-enol tautaumerism form ##STR2## R.sup.1 is Ph or Th; R.sup.2 is H or CH.sub.2 R.sup.3 ;R.sup.3 is H, OCH.sub.3, C.sub.1 -C.sub.5 lower alkyl, or CO.sub.2 R.sup.4 ;R.sup.4 is H or C.sub.1 -C.sub.5 lower alkyl;R.sup.5 is H or CH.sub.3 ;R.sup.6 is OHCHN or H.sub.2 N; andR.sup.7 is H or OH;or pharmaceutically acceptable salt thereof.The compounds are useful as inhibitors of ADP-induced blood platelet aggregation in human platelet-rich plasma.
    Type: Grant
    Filed: April 3, 1992
    Date of Patent: September 20, 1994
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jeffrey L. Romine, Nicholas A. Meanwell
  • Patent number: 5328932
    Abstract: The present invention provides new thrombin inhibiting bisamidines derivatives, their pharmaceutically acceptable salts and hydrates, methods for their preparation, pharmaceutical composition, a process for their preparation, and use of the compounds in treatment of thrombosis, ischemia and stroke.
    Type: Grant
    Filed: June 17, 1993
    Date of Patent: July 12, 1994
    Assignee: Bristol-Myers Squibb Company
    Inventors: Neelakantan Balasubramanian, William Teh-Wei Han
  • Patent number: 5321046
    Abstract: Disclosed herein are novel unsymmetrical dithiol ketals which are useful in the treatment or prevention of hypercholesterolemia, hyperlipoproteinemia, and atherosclerosis.
    Type: Grant
    Filed: October 27, 1992
    Date of Patent: June 14, 1994
    Assignee: Bristol-Myers Squibb Company
    Inventors: Sing-Yuen Sit, John J. Wright, Jeff A. Field
  • Patent number: 5318993
    Abstract: The present invention relates to novel benzoquinones which are useful as antihyperlipidemic agents. The present invention also provides a process for their preparation, pharmaceutical compositions, and a method for treating birds and mammals in need thereof which comprises administering to said host an effective amount of a benzoquinone of the present invention.
    Type: Grant
    Filed: April 16, 1993
    Date of Patent: June 7, 1994
    Assignee: Bristol-Myers Squibb Company
    Inventor: Bradley C. Pearce
  • Patent number: 5318989
    Abstract: The present invention relates to a novel and efficient process for the preparation of 8-hydroxybicyclo[7.3.1]tridec-4-ene-2,6-diyne ring system which is part of the aglycone of esperemicin and to novel cytotoxic antitumor agents having said bicyclic ring system. The present invention also provides a method for treating mammalian malignant tumors by administering to an animal in need of such treatment an antitumor effective amount of a compound of the present invention.
    Type: Grant
    Filed: December 18, 1992
    Date of Patent: June 7, 1994
    Assignee: Bristol-Myers Squibb Company
    Inventors: John F. Kadow, Mark D. Wittman
  • Patent number: 5296508
    Abstract: The invention relates to novel farnesylated tetrahydro-naphthalenols, that inhibit HMGR activity which results in a decrease in serum total cholesterol, a decrease in LDL cholesterol levels, and inhibition of LDL oxidation. The farnesylated tetrahydro-naphthalenols of the present invention are thus useful for cholesterol/lipid lowering in cases of hypercholesterolemia, hyperlipidemia, and atherosclerosis.
    Type: Grant
    Filed: December 23, 1992
    Date of Patent: March 22, 1994
    Assignee: Bristol-Myers Squibb Company
    Inventor: Bradley C. Pearce