The Nitrogen Is Bonded Directly At The 3-position Patents (Class 552/521)
  • Patent number: 5192756
    Abstract: An aminosterol antibiotic, (3.beta.(N-[3-aminopropyl]-1,4-butanediamine)-7.alpha.,24.zeta.-dihydroxy- 5.alpha.-cholestane 24-sulfate), which can be isolated from the stomach of the common dogfish shark, Squalus acanthias, is disclosed.
    Type: Grant
    Filed: March 18, 1992
    Date of Patent: March 9, 1993
    Assignee: The Children's Hospital of Pennsylvania
    Inventors: Michael Zasloff, Karen Moore, Suzanne Wehrli
  • Patent number: 5093502
    Abstract: A process for the preparation of novel 14.alpha., 17.alpha.-dihydroxy-17.beta.-substituted steroids by reacting 14.alpha.-hydroxy-17-oxo-steroids with metal organic compounds and the use of the said novel steroids in the production of 14.alpha., 17.alpha.-methylenedioxy-pregnane derivatives.
    Type: Grant
    Filed: February 16, 1990
    Date of Patent: March 3, 1992
    Assignee: Akzo N.V.
    Inventors: Peter M. Smid, Willem J. Van Zoest, Pieter G. Weber, Arthur F. Marx
  • Patent number: 5086190
    Abstract: The present invention provides a novel compound represented as ##STR1## The present novel compound is prepared by reacting fluorine with pyridine-boron trifluoride and is useful as a fluorinating agent in the fluorination of organic compounds.
    Type: Grant
    Filed: January 29, 1991
    Date of Patent: February 4, 1992
    Assignee: Allied-Signal Inc.
    Inventors: Michael Van Der Puy, David Nalewajek, George A. Shia, William J. Wagner
  • Patent number: 5003063
    Abstract: The invention involves a two step chemical transformation of a steroidal 17-cyanohydrin (II) ##STR1## to a 17.alpha.-hydroxy-21-halo-20-keto steroid (IV) ##STR2## intermediate which can readily be converted to pharmaceutically useful corticoids.
    Type: Grant
    Filed: January 30, 1990
    Date of Patent: March 26, 1991
    Assignee: The Upjohn Company
    Inventor: John G. Reid
  • Patent number: 5001234
    Abstract: This invention provides novel cyclic hydrocarbons of the formula: ##STR1## wherein R is selected from the group consisting of CH.sub.2 .dbd.CH--CH.sub.2 --, HO--CH.sub.2 CH.sub.2 CH.sub.2 --, and CH.sub.3 ;wherein R.sub.1 is selected from the group consisting of m-trifluoromethylphenylmethyl, 2-thienylmethyl, and p-aminosulfonylphenylethyl;wherein R.sub.2 and R.sub.3 are methyl or hydrogen;wherein R.sub.4 is hydrogen or --OH;a compound of the formula ##STR2## wherein R is (CH.sub.3).sub.2 NCH.sub.2 CH.sub.2 CH.sub.2 -- or NH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 --;or a compound of the formula ##STR3## wherein the dashed line indicates that the 2-3 bond is saturated or unsaturated and, wherein R is hydrogen or methyl.These compounds are useful for inhibiting adverse physiological symptoms associated with phospholipase A.sub.2 and for treating hyperglycemia associated diseases such as diabetes and obesity.
    Type: Grant
    Filed: October 16, 1989
    Date of Patent: March 19, 1991
    Assignee: The Upjohn Company
    Inventors: Gordon L. Bundy, Gilbert A. Youngdale
  • Patent number: 4977255
    Abstract: 17.beta.-Cyano-17.alpha.-hydroxy steroids (I) are transformed to 17.alpha.-halo silyl ethers (II) which are intermediates useful in the production of progesterones (V), 17-hydroxyprogesterones (VI), corticoids (VII) and 21-halo corticoids (III) which can readily be transformed to corticoids (VII).
    Type: Grant
    Filed: April 7, 1989
    Date of Patent: December 11, 1990
    Assignee: The Upjohn Company
    Inventors: Douglas A. Livingston, Bruce A. Pearlman, Scott Denmark
  • Patent number: 4970204
    Abstract: Invented are 3-nitro- substituted steroidal synthetic compounds, pharmaceutical compositions containing the compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase including using these compounds to reduce prostate size. Also invented are intermediates used in preparing these compounds.
    Type: Grant
    Filed: August 23, 1989
    Date of Patent: November 13, 1990
    Assignee: SmithKline Beecham Corporation
    Inventors: Dennis A. Holt, Mark A. Levy, Brian W. Metcalf
  • Patent number: 4917826
    Abstract: Provided are cyclic hydrocarbons of Formula I ##STR1## with an aminoalkyl sidechain that are useful for treating phospholipase A2 mediated conditions, diabetes, and obesity.
    Type: Grant
    Filed: June 16, 1987
    Date of Patent: April 17, 1990
    Assignee: The Upjohn Company
    Inventors: Roy A. Johnson, Gordon L. Bundy, Gilbert A. Youngdale, Douglas R. Morton, Donald P. Wallach, deceased