Abstract: The subject invention relates to pyrimidine-thioalkyl and alkylether compounds of Formula (I) and pyrimidine-thioalkyl and alkylethers of Formula (IA), namely the compounds of Formula (I) where R.sup.4 is selected from the group consisting of --H or --NR.sub.15 R.sub.16 where R.sub.15 is --H and R.sub.16 is --H, C.sub.1 -C.sub.6 alkyl, --NH.sub.2 or R.sub.15 and R.sub.16 taken together with the --N form 1-pyrrolidino, 1-morpholino or 1-piperidino; and R.sub.6 is selected from the group consisting of --H, or halo (preferably --Cl); with the overall proviso that R.sub.4 and R.sub.6 are not both --H. The compounds of Formula (IA) are useful in the treatment of individuals who are HIV positive.
Type:
Grant
Filed:
May 9, 1996
Date of Patent:
November 9, 1999
Assignee:
Pharmacia & Upjohn Company
Inventors:
Richard A. Nugent, Stephen T. Schlachter, Michael J. Murphy, Joel Morris, Richard C. Thomas, Donn G. Wishka, Fritz Reusser, Gary J. Cleek, Irene W. Althaus
Abstract: This invention provides oxazolidine protected taxol analogs of the Formula: ##STR1## which are useful intermediates to make various taxol analogues.
Abstract: The invention provides a controlled release composition comprising a compressed core containing a drug having two parallel planar surfaces (i.e. the top and bottom), and a seal coating surrounding the core except on said planar surfaces (i.e. on all lateral surfaces). The seal coating comprises a film coating of an impermeable material.
Abstract: This invention provides 7-deoxy-.DELTA..sup.12,13 -iso-taxol of formula (I) which are useful for the treatment of the same cancers for which taxol has been shown active.
Type:
Grant
Filed:
July 23, 1996
Date of Patent:
October 13, 1998
Assignee:
Pharmacia & Upjohn Company
Inventors:
Nancy A. Wicnienski, Robert C. Kelly, Peter G. M. Wuts
Abstract: There are disclosed 18-thiomarcfortine derivatives of the natural products marcfortine A, B and C, C-18 thioparaherquamide and derivatives thereof, novel N-1 marcfortines A, B, and C and derivatives thereof, novel N-1 paraherquamide and derivatives thereof usefull in the treatment and prevention of helninth and arthropod infections of animals and plants.Any inquiry concerning this communication or earlier communications from the examiner should be directed to Examiner Robert T. Bond whose telephone number is (703)308-4711. The examiner can normally be reached on Monday through Friday from 8:00 AM to 4:30 PM.
Abstract: Novel GRF PEPTIDES having Thr, Val or Ile at position 2, having an amino acid selected from the group consisting of Ala, Val, Leu, Ile or Gly at position 15, and optionally substituted with Val or Ile at position 19 are described. Compositions and the method of stimulating the release of growth hormone utilizing GRF PEPTIDES having Thr, Val or Ile at position 2 and having an amino acid selected from the group consisting of Ala, Val, Leu, Ile or Gly at position 15 are also described. The GRF PEPTIDES of the present invention have enhanced stability in plasma.
Abstract: There are disclosed 14.alpha.-hydroxymarcfortine derivatives of the natural products marcfortine A, B, C, and D useful in the treatment and prevention of helminth and arthropod infections of animals and plants. The synthetic derivatives are of Formula (I).
Abstract: This invention provides some new synthetically obtained compounds of formula I and II ##STR1## which are useful as chemical intermediates. Representative formula I or II compounds have also been shown to possess useful ranges of antitumor activity in standard laboratory animal tests.In addition, the compounds of formula I or II can be linked to monoclonal antibodies, either directly or via known linking group, as a means of selectively delivering the CC-1065 analogs (Compounds of Formula I and II) to those target cells expressing the target antigen and thus selectively eliminating those diseased cells from the animal or human. Further, the compounds of formula I and II can be linked to soluble human CD4 or a soluble human CD4 protein fragment capable of binding to the gp120 envelope protein of the human immuno-virus and thus eliminate virally infected cells.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
April 14, 1998
Assignee:
Pharmacia & Upjohn Company
Inventors:
Robert C. Kelly, Mark A. Mitchell, Paul A. Aristoff
Abstract: This invention relates to compounds of Formula I ##STR1## which are useful in association with a pharmaceutical carrier as antiatherosclerotic agents. In addition, various compounds of Formula I are useful inhibitors of cell proliferation.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
December 30, 1997
Assignee:
Pharmacia & Upjohn Company
Inventors:
Ronald B. Gammill, Thomas M. Judge, Joel Morris
Abstract: This invention relates to coated medicaments and a process for providing spray coated gelatinous coverings for such medicaments. This invention is also directed to novel gelatinous compositions for spray coating tablets, caplets, pellets, granules and the like.
Type:
Grant
Filed:
December 2, 1994
Date of Patent:
November 4, 1997
Assignees:
Pharmacia & Upjohn Company, L. Perrigo Company
Abstract: This invention relates to the method for treating the form of alopecia commonly known as "male pattern baldness" which comprises regular topical application to the affected areas of the human scalp of a composition containing as at least one of its active ingredients of Formula I. It also encompasses the aforesaid compound itself for use as a therapeutic agent to arrest and reverse male pattern alopecia.
Type:
Grant
Filed:
January 11, 1994
Date of Patent:
July 1, 1997
Assignee:
The Upjohn Company
Inventors:
Jackson B. Hester, Jr., Kaushik D. Meisheri
Abstract: This invention provides 7-deoxy-.DELTA..sup.6,7 -taxol and 7-deoxy-.DELTA..sup.6,7 -taxol analogs of Formula I: ##STR1## The compounds of Formula I are useful for the same cancers for which taxol has been shown active, including human ovarian cancer, breast cancer, and malignant melanoma as well as lung cancer, gastric cancer, colon cancer, head and neck cancer, and leukemia.
Type:
Grant
Filed:
June 10, 1994
Date of Patent:
September 17, 1996
Assignee:
The Upjohn Company
Inventors:
Robert C. Kelly, Roy A. Johnson, Harvey I. Skulnick, Eldon G. Nidy
Abstract: A method for altering the immunoregulatory system of humans and animals by administering a compound of the formula: ##STR1## wherein X.sub.3 is equal to X, X.sub.4, or X.sub.5 wherein X.sub.4 is fluoro, chloro, bromo or iodo, and X.sub.5 is mono-, di- or trihalomethyl, mono-, di or trifluoroethyl, perfluoropropyl, and wherein X is alkyl of from 1 to 3 carbon atoms, inclusive, 2-propynyl and 2-propenyl, and X.sub.1 is as defined in the specification.
Abstract: This invention concerns chemical compounds of general Formula ICPI.sub.1 -R.sub.5 -T-R'.sub.5 -CPI.sub.2 IThe compounds of Formula I are useful as uv light absorbers, antibacterial agents, and are particularly useful as antitumor agents. Representative compounds of Formula I have been shown to possess useful ranges of antitumor activity in standard laboratory animal tests.
Abstract: 6-Aryl pyrimidinol compounds, also can be named 6-aryl pyrimidinone or 6-aryl-isocytosine novel compounds, also novel and old compounds useful for treating viral infections and inducing interferon production. Dosage forms and method of treatment are disclosed.
Type:
Grant
Filed:
January 21, 1993
Date of Patent:
July 18, 1995
Assignee:
The Upjohn Company
Inventors:
Wendell Wierenga, Harvey I. Skulnick, Dale A. Stringfellow
Abstract: Novel 1,2,3-thiadiazole compounds, new and old 1,2,3-thiadiazole compositions and method of anti-thrombotic treatment are systemically administered to a human or animal.
Type:
Grant
Filed:
June 4, 1987
Date of Patent:
March 24, 1992
Assignee:
The Upjohn Company
Inventors:
Edward W. Thomas, Ronald H. Rynbrandt, deceased
Abstract: This invention concerns a process for killing internal parasites, especially nematodes, trematodes and cestodes affecting warm blooded animals such as sheep, cattle, swine, goats, dogs, cats, horses and humans as well as poultry by administering an effective amount of a compound of the Formula I. ##STR1## The compounds are readily prepared by conventional chemical reactions.
Type:
Grant
Filed:
January 30, 1990
Date of Patent:
September 17, 1991
Assignee:
The Upjohn Company
Inventors:
Douglas L. Rector, George A. Conder, Sylvester D. Folz
Abstract: This invention concerns a process for killing internal parasites, especially nematodes and cestodes affecting warm blooded animals such as sheep, cattle, swine, goats, dogs, cats, horses and humans as well as poultry by administering an effective amount of a compound of the Formula I: ##STR1## Certain of the compounds of Formula I are novel and in further embodiments of the invention provide novel compounds and compositions for use in the process of the invention. The compounds are readily prepared by conventional chemical reactions. Various pyridinyl acylhydrazones of Formula I demonstrate broad-spectrum anthelmintic activity in sheep upon oral and/or parenteral administration.
Type:
Grant
Filed:
September 1, 1989
Date of Patent:
June 11, 1991
Assignee:
The Upjohn Company
Inventors:
Douglas L. Rector, George A. Conder, Sylvester D. Folz
Abstract: A method for treating bacterial or protozoal humans and animals by administering a 6-aryl pyrimidine compound or a salt thereof in association with a pharmaceutical carrier.
Abstract: 1,2,8,8a-Tetrahydrocyclopropa[3]pyrrolo(3,2-e)indol-4(5H)-ones, and related compounds of formulas I and intermediate therefor II ##STR1## wherein R.sub.2, R.sub.2 ', R.sub.3, R.sub.5, R.sub.50 and X are as defined in the specification, e.g., (7bR,8aS)-1,2,8,8a -tetrahydro-7-methyl-2-[[5-(((1H-indol-2-yl)carbonyl)amino)-1H-indol-2-yl] carbonyl]cyclopropa[pyrrolo[3,2-e]indol-4(5H)-one (U-71,184), as purified, and its racemic form (U-68,415), and related compounds, are useful as ultraviolet light absorbers and as antibacterials. The lead compounds are useful as antitumor drug compounds in standard laboratory animal tests.
Type:
Grant
Filed:
November 30, 1989
Date of Patent:
December 18, 1990
Assignee:
The Upjohn Company
Inventors:
Robert C. Kelly, Martha A. Warpehoski, Wendell Wierenga