Patents by Inventor John S. Driscoll
John S. Driscoll has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Patent number: 5817799Abstract: A method of preparing a 2'-fluoro compound of the formula ##STR1## where B is selected from the group consisting of purines and pyrimidines, both of which may be substituted, comprises reacting a compound of the formula II(a) or II(b) ##STR2## where R and R' are as defined in the specification with an acid halide under conditions effective to obtain a halide of the formula ##STR3## where X is a halogen. A silane of the formula B-Si (R").sub.3 where R" is as defined in the specification, is added to this product (III) under conditions effective to obtain a compound of the formula (IV) ##STR4## The compound of formula (IV) is reacted with a reagent selected from the group consisting of ammonia, BCl.sub.3 and ((C.sub.1 -C.sub.10)alkyl).sub.4 NF, under conditions effective to obtain the compound of formula (I). The compounds of formula (I) resulting from these methods exhibit anti-HIV activities and are useful for therapy against the HIV virus.Type: GrantFiled: July 23, 1990Date of Patent: October 6, 1998Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Victor E. Marquez, John S. Driscoll, Ronald J. Wysocki, Jr., Magbool A. Siddiqui
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Patent number: 5565437Abstract: Methods of treating a human infected with human immunodeficiency virus (HIV), such as a human with AIDS, with the purina nucleotides 2',3'-dideoxy-2'-beta-fluoroadenosine (FddA) and 2',3'-dideoxy-2'-beta-fluoroinosine (FddI) are disclosed. These nucleotides are stable in an acid environment and thus can be used for oral administration. Methods of inhibiting human immunodeficiency virus replication in a human T cell using these purina nucleotides are also disclosed.Type: GrantFiled: November 10, 1992Date of Patent: October 15, 1996Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Victor E. Marquez, John S. Driscoll, Christopher K-H. Tseng, James A. Kelley, David G. Johns, Hiroaki Mitsuya
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Patent number: 5498719Abstract: The present invention provides a novel synthetic route to a key precursor, i.e., an (S,S)-.alpha.-fluoro-2,2-dimethyl-1,3-dioxolane-4-propanoic acid ester useful in the preparation of FddA and FddC. The instant diastereoselective process utilizes a novel intermediate which contains a chiral auxiliary. The chiral auxiliary can be any chiral auxiliary moiety such as for example an auxiliary containing a substituted oxazolidinone group. The intermediate containing the chiral auxiliary is fluorinated utilizing a fluorination method applied for the first time in the synthesis of fluorinated sugars to give a fluorinated intermediate which after removal of the chiral group provides the desired key intermediate. In summary, in the instant process, a fluorine is introduced diastereoselectively into an intermediate via the reaction of a chiral enolate with an electrophilic fluorinating agent and the intermediate which is fluorinated is derived from mannitol.Type: GrantFiled: January 31, 1994Date of Patent: March 12, 1996Assignee: The United States of America as represented by the Secretary of the Department of Health & Human ServicesInventors: Victor E. Marquez, John S. Driscoll, Magbool A. Siddiqui
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Patent number: 5495010Abstract: Purine nucleosides active against human immunodeficiency virus which are substituted at the 2'-position by a strong electronegative group such as fluorine are stable in an acid environment and thus can be used for oral administration.Type: GrantFiled: September 19, 1991Date of Patent: February 27, 1996Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Victor E. Marquez, John S. Driscoll, Christopher K-H. Tseng, James A. Kelley, David G. Johns, Hiroaki Mitsuya
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Patent number: 5459256Abstract: The present invention relates, in general, to prodrugs. In particular, the present invention relates to lipophilic, aminohydrolase-activated, anti-viral nucleoside prodrug compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds.Type: GrantFiled: April 10, 1991Date of Patent: October 17, 1995Assignee: The Government of the United States of America as represented by the Department of Health and Human ServicesInventors: Victor E. Marquez, John S. Driscoll, Harry Ford, Jr., James A. Kelley, Joseph J. Barchi, Jr., Hiroaki Mitsuya, Christopher K-H. Tseng, David G. Johns, Joseph E. Tomaszewski
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Patent number: 5336764Abstract: A compound has the formula ##STR1## wherein R is selected from the group consisting of (C.sub.7 -C.sub.20)aroyl, (C.sub.6 -C.sub.20)aryl, aralkyl and alkylaryl, and (C.sub.1 -C.sub.10)alkyl-di(C.sub.6 -C.sub.20)aryl Si, R' is selected from the group consisting of (C.sub.1 -C.sub.10)alkyl, (C.sub.7 -C.sub.20)aroyl and (C.sub.2 -C.sub.12)acyl, all of which may be further substituted with O, S, N or alkyl, and R'" is selected from the group consisting of halogen, (C.sub.1 -C.sub.10)alkoxy, (C.sub.1 -C.sub.10)acyloxy, O-methane-sulfonyl and O-p-toluenesulfonyl. A composition of matter comprises 0.001 to 99.999 wt % of the above compound.Type: GrantFiled: October 29, 1992Date of Patent: August 9, 1994Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Victor E. Marquez, John S. Driscoll, Ronald J. Wysocki, Jr., Maqbool A. Siddiqui
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Patent number: 4992472Abstract: Several analogues of hexamethylene bis[acetamide] were found to be effective differentiating agents. The most effective of these compounds was 3,3'-(1,6-hexandiyl)bis[5,5-dimethyl-2,4-imidazolinedione].Type: GrantFiled: May 1, 1989Date of Patent: February 12, 1991Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: John S. Driscoll, Alberto Haces, Theodore Breitman
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Patent number: 4975434Abstract: Cyclopentenyl pyrimidine compounds have potent anti-viral, anti-tumor and differentiating activity. Of these compounds, cyclopentenyl cytosine has proved to be particularly effective in a variety of tumors, as well as having good antiviral activity and potent differentiating properties.Type: GrantFiled: January 31, 1989Date of Patent: December 4, 1990Assignee: The United States of America as represented by the Secretary of the Department of Health and Human ServicesInventors: Victor E. Marquez, John S. Driscoll, Mu-Ill Lim, Christopher K. Tseng, Alberto Haces, Robert I. Glazer
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Patent number: 4968690Abstract: The new compound 3-deazaneplanocin A has been discovered to have potent anti-viral, anti-tumor activity and differentiating activity. A simple method for preparing 3-deazaneplanocin A has been developed involving nucleophilic substitution, which method can also be used to prepare a great variety of carbocyclic nucleosides.Type: GrantFiled: January 19, 1989Date of Patent: November 6, 1990Assignee: United States Government as represented by the Secretary of the Dept. of Health and Human ServicesInventors: Victor E. Marquez, John S. Driscoll, Mu-Ill Lim, Christopher K. Tseng, Alberto Haces, Robert I. Glazer
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Patent number: 4882346Abstract: Several analogues of hexamethylene bis[acetamide] were found to be effective differentiating agents. The most effective of these compounds was 3,3'-(1,6-hexandiyl)bis[5,5-dimethyl-2,4-imidazolinedione].Type: GrantFiled: June 16, 1987Date of Patent: November 21, 1989Assignee: The United States of America as reprsented by the Department of Health and Human ServicesInventors: John S. Driscoll, Alberto Haces, Theodore Breitman
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Patent number: 4788181Abstract: 5-substituted 2',3'-dideoxycytidine compounds and their monophosphates are disclosed which have been found to have potent activity against retroviruses. The 5-fluoro-and 5-aza-substituted 2',3'-dideoycytidine compounds have been found to be effective against HTLV-III/LAV virus.Type: GrantFiled: September 29, 1986Date of Patent: November 29, 1988Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: John S. Driscoll, Victor E. Marquez, Chong-Ho Kim, James A. Kelley
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Patent number: 4704384Abstract: The use of aziridinyl quinones as antitumor agents is disclosed. A compound which has been found to be particularly effective is the compound 2,5-diaziridinyl-3,6-bis (carboethoxyamino)-1,4-benzoquinone. Treatment is described in connection with various forms of leukemia, for example, as well as B16 melanoma, Lewis lung carcinoma, and the ependymoblastoma brain tumor system.Type: GrantFiled: December 18, 1981Date of Patent: November 3, 1987Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: John S. Driscoll, A. Hameed Khan, Feng-Te Chou
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Patent number: 4572452Abstract: A slitting and winding machine for tape includes a base (12) having a working surface (22) with a tape supply support (20) and a take-up mandrel assembly (80) at opposite ends of the working surface, along with a cutter mechanism (54) between the mandrel assembly and the working surface. A pair of spaced rolls (40) of leader material and a roll (42) of connecting material are supported on the base on one side of the working surface and have adjacent edges overlapping to be drawn over the tape and replace a segment that is previously removed. The mechanism cuts the wide tape into narrow strips and alternate strips are directed across specially designed guide rollers (100) toward respective mandrels of the mandrel assembly. The cutter mechanism includes a grooved roller (60) and a cutter blade support bar (68) that is designed for quick change of cutter blades.Type: GrantFiled: November 21, 1984Date of Patent: February 25, 1986Assignee: Illinois Carbon ProductsInventors: John S. Driscoll, Robert E. Palka
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Patent number: 4275057Abstract: Seven-membered heterocyclic nucleosides used to inhibit the deamination enzyme responsible for the inactivation of arabinosylcytosine (ara--C). Preferred nucleosides containing a seven-member aglycone are as follows: ##STR1## Preferred aglycones are as follows: ##STR2## Active components utilized against pyrimidine deaminases from mammalian tissues (mouse kidney and human liver) showed optimum advantage when compared with tetrahydrouridine (THU).Type: GrantFiled: January 28, 1980Date of Patent: June 23, 1981Assignee: The United States of America as represented by the Department of Health, Education and WelfareInventors: Victor E. Marquez, Paul S. Liu, John S. Driscoll
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Patent number: 4233215Abstract: The use of aziridinyl quinones as antitumor agents against transplanted tumors in mice is disclosed. A compound which has been found to be particularly effective is the compound 2,5-diaziridinyl-3,6-bis (carboethoxyamino)-1,4-benzoquinone. Treatment is described in connection with several transplanted mouse tumor test systems including various forms of leukemia, for example, as well as B16 melanoma, Lewis lung carcinoma, and the ependymoblastoma brain tumor system.Type: GrantFiled: October 24, 1978Date of Patent: November 11, 1980Assignee: United States of AmericaInventors: John S. Driscoll, A. Hameed Khan, Feng-Te Chou
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Patent number: 4146622Abstract: The use of aziridinyl quinones as antitumor agents against transplanted tumors in mice is disclosed. A compound which has been found to be particularly effective is the compound 2,5-diaziridinyl-3,6-bis (carboethoxyamino)-1,4-benzoquinone. Treatment is described in connection with several transplanted mouse tumor test systems including various forms of leukemia, for example, as well as B16 melanoma, Lewis lung carcinoma, and the ependymoblastoma brain tumor system.Type: GrantFiled: January 12, 1977Date of Patent: March 27, 1979Assignee: The Government of the United StatesInventors: John S. Driscoll, A. Hameed Khan, Feng-te Chou
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Patent number: 4105774Abstract: Hydantoin derivatives of varying lipophilic character were prepared as nigen mustard carriers for CNS anti-tumor evaluation in transplanted mouse tumor test systems. Activity was studied in the murine ependymoblastoma brain tumor system. Multiple cures were observed for three of the four analogs examined. The compounds were also active in the intraperitoneal leukemia L1210 and P388 systems as well as in B16 melanoma and Lewis lung carcinoma.Type: GrantFiled: July 28, 1975Date of Patent: August 8, 1978Assignee: The United States of America as represented by the Secretary of StateInventors: John S. Driscoll, Victor E. Marquez, Geoffrey Peng
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Patent number: 4058602Abstract: The compound 5,6-dihydro-5-azacytidine, 5AC[H], and non-toxic acid addition salts such as the hydrochloride, together with its preparation from 5-azacytidine (5-AC) by reduction of the 5,6-double bond of 5-AC with an alkali metal borohydride such as sodium borohydride. Additionally, 5,6-dihydro-5-azacytidine, 5AC[H], has antitumor activity for murine leukemia systems L1210 and P388 as an injectable. In comparison with the parent compound, 5-AC, the antitumor activity is comparable and 5AC[H] exhibits a more favorable therapeutic index. It also has better solution stability over a broad pH range. A structure for the HCl salt is given below.Type: GrantFiled: August 9, 1976Date of Patent: November 15, 1977Assignee: The United States of America as represented by the Department of Health, Education and WelfareInventors: John A. Beisler, Mohamed M. Abbasi, John S. Driscoll
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Patent number: D267628Type: GrantFiled: November 24, 1980Date of Patent: January 18, 1983Inventors: John S. Driscoll, John J. Cushing
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Patent number: D283103Type: GrantFiled: November 14, 1983Date of Patent: March 25, 1986Assignee: John S. DriscollInventors: John J. Cushing, John S. Driscoll