Analogs of biologically active, naturally occurring polyamines, pharmaceutical compositions and methods of treatment
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-031/13
A61K-031/445
C07C-211/00
C07D-403/00
출원번호
US-0233400
(2002-09-04)
발명자
/ 주소
Bergeron, Jr.,Raymond J.
출원인 / 주소
University of Florida Research Foundation, Inc.
대리인 / 주소
Miles &
인용정보
피인용 횟수 :
0인용 특허 :
16
초록▼
Polyamines having the formula: or a salt thereof with a pharmaceutically acceptable acid wherein: R 1-R6 may be the same or different and are alkyl, aryl, aryl alkyl, cycloalkyl, optionally having an alkyl chain interrupted by at least one etheric oxygen atom, or hydrogen; N1, N2, N3 and N4 are
Polyamines having the formula: or a salt thereof with a pharmaceutically acceptable acid wherein: R 1-R6 may be the same or different and are alkyl, aryl, aryl alkyl, cycloalkyl, optionally having an alkyl chain interrupted by at least one etheric oxygen atom, or hydrogen; N1, N2, N3 and N4 are nitrogen atoms capable of protonation at physiological pH's; a and b may be the same or different and are integers from 1 to 4; A, B and C may be the same or different and are bridging groups which effectively maintain the distance between the nitrogen atoms such that the polyamines: (i) are capable of uptake by a target cell upon administration thereof to a human or non-human animal; and (ii) upon uptake by the target cell, competitively bind via an electrostatic interaction between the positively charged nitrogen atoms to substantially the same biological counter-anions as the intracellular natural polyamines in the target cell; the polyamines, upon binding to the biological counter-anion in the cell, function in a manner biologically different than the intracellular polyamines, the polyamines not occurring in nature; as well as pharmaceutical compositions embodying the polyamines and methods of treating patients requiring anti-neoplastic therapy.
대표청구항▼
I claim: 1. An article of manufacture comprising packaging material and a pharmaceutical agent contained within said packaging material, wherein said pharmaceutical agent is effective for the treatment of a subject suffering from neoplasm, and wherein said packaging material comprises a label which
I claim: 1. An article of manufacture comprising packaging material and a pharmaceutical agent contained within said packaging material, wherein said pharmaceutical agent is effective for the treatment of a subject suffering from neoplasm, and wherein said packaging material comprises a label which indicates that said pharmaceutical agent can be used for treating neoplasm, and wherein said pharmaceutical agent is a polyamine having the formula: R1--N1(R2)-A-[N2(R3)-B]a-[N 3(R4)-C]b-N4(R5)--R6 or a salt thereof with a pharmaceutically acceptable acid wherein: R1-R6 may be the same or different and are alkyl, aryl, aryl alkyl, or cycloalkyl, optionally having an alkyl chains interrupted by at least one etheric oxygen atom, or hydrogen; N1, N2, N3 and N4 are nitrogen atoms capable of protonation at physiological pH's; a and b may be the same or different and are integers from 1 to 4; A, B and C may be the same or different and are bridging groups which effectively maintain the distance between said nitrogen atoms such that said polyamine: (i) is capable of uptake by a target cell upon administration of said polyamine to a human or non-human animal; and (ii) upon uptake by said target cell, competitively binds via an electrostatic interaction between the positively charged nitrogen atoms to substantially the same biological counter-anions as the intra-cellular natural polyamines in the target cell; said polyamine, upon binding to said biological counter-anion in the cell, functions in a manner biologically different than said intracellular polyamines, said polyamine not occurring in nature. 2. The article of manufacture of claim 1, wherein, in said formula, A, B and C may be the same or different and are alkylene, branched alkylene, cycloalkylene, arylalkylene or a heterocyclic bridging group wherein one of said N1, N2, N3 or N4 atoms is incorporated in the ring as the heteroatom. 3. The article of manufacture of claim 2 wherein, in said formula, A and C are pyridinyl.
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이 특허에 인용된 특허 (16)
Kluger Edward W. (Pauline SC) Miley John W. (Inman SC) Su Tien K. (Spartanburg SC), Additives for lubricants and fuels.
Bergeron Raymond J. (Gainesville FL), Anti-neoplastic, anti-viral and ribonucleotide reductase activity affecting pharmaceutical compositions and methods of t.
Bergeron Raymond J. (Gainesville FL), Anti-neoplastic, anti-viral and ribonucleotide reductase activity affecting pharmaceutical compositions and methods of t.
Amundsen Alan R. (Somerville NJ) Stern Eric W. (Mountainside NJ), Pharmaceutical composition containing cis-platinum (II) amine lactate and a method of using same.
Prakash Nellikunja (Cincinnati OH) Stemerick David M. (Fairfield OH) Edwards Michael L. (Cincinnati OH) Bowlin Terry L. (Maineville OH), Polyamine derivatives as antineoplastic agents.
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