Water soluble tetrapyrollic photosensitizers for photodynamic therapy
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
C07B-047/00
C09D-048/22
출원번호
US-0452511
(2006-06-14)
등록번호
US-7501509
(2009-03-10)
발명자
/ 주소
Pandey,Ravindra K.
Gryshuk,Amy
Goswami,Lalit
Potter,William
Oseroff,Allan
출원인 / 주소
Health Research, Inc.
대리인 / 주소
Dunn,Michael L.
인용정보
피인용 횟수 :
4인용 특허 :
254
초록▼
A tetrapyrollic photosensitizer compound having at least one pendant--CH2CH2CON(CH2CON(CH2COOH)2) 2 or--N(CH2COOH)2 group or esters thereof said tetrapyrollic compound being a chlorin, bacteriochlorin, porphyrin, pyropheophorbide, purpurinimide, or bacteriopurpurinimide. Desirably the compound has t
A tetrapyrollic photosensitizer compound having at least one pendant--CH2CH2CON(CH2CON(CH2COOH)2) 2 or--N(CH2COOH)2 group or esters thereof said tetrapyrollic compound being a chlorin, bacteriochlorin, porphyrin, pyropheophorbide, purpurinimide, or bacteriopurpurinimide. Desirably the compound has the formula: or a phamaceutically acceptable derivative thereof, wherein R1-R8 and R10 are various substituents and R9 is substituted or unsubstituted--CH2CH2CON(CH2CON(CH2COOH)2) 2; or--N(CH2COOH)2. The invention also includes a method of treatment by photodynamic therapy by treatment with light after injecting the compound and a method of imaging by fluorescence after injection of the compound.
대표청구항▼
What is claimed is: 1. A tetrapyrollic photosensitizer compound having at least one pendant--CH2CH2CON(CH2CON(CH2COOH)2) 2 or--N(CH2COOH)2 group or esters thereof said tetrapyrollic compound being a chlorin, bacteriochlorin, porphyrin, pyropheophorbide, purpurinimide, or bacteriopurpurinimide. 2.
What is claimed is: 1. A tetrapyrollic photosensitizer compound having at least one pendant--CH2CH2CON(CH2CON(CH2COOH)2) 2 or--N(CH2COOH)2 group or esters thereof said tetrapyrollic compound being a chlorin, bacteriochlorin, porphyrin, pyropheophorbide, purpurinimide, or bacteriopurpurinimide. 2. A compound of the formula: or a phamaceutically acceptable derivative thereof, wherein: R1 and R2 are each independently substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl,--C(O)Ra or--COORa or--CH(CH3)(OR) or--CH(CH3)(O(CH2)nXR) where Ra is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, or substituted or unsubstituted cycloalkyl where R2 may be CH═CH2, CH(OR20)CH3, C(O)Me, C(═NR21)CH3 or CH(NHR21)CH3; where X is an aryl or heteroaryl group; n is an integer of 0 to 6; R and R' are independently H or lower alkyl of 1 through 8 carbon atoms; where R20 is methyl, butyl, heptyl, docecyl or 3,5-bis(trifluoromethyl)-benzyl; and R21 is 3,5,-bis(trifluoromethyl)benzyl; R1a and R2a are each independently hydrogen or substituted or unsubstituted alkyl, or together form a covalent bond; R3 and R4 are each independently hydrogen or substituted or unsubstituted alkyl; R3a and R4a are each independently hydrogen or substituted or unsubstituted alkyl, or together form a covalent bond; R5 is hydrogen or substituted or unsubstituted alkyl; R6 and R6aare each independently hydrogen or substituted or unsubstituted alkyl, or together form ═O ; R7 is a covalent bond, alkylene, azaalkyl, or azaaraalkyl or ═NR20 where R20 is hydrogen or lower alkyl of 1 through 8 carbon atoms or--CH2-3,5-bis(tri-fluoromethyl) benzyl or--CH2X-R1 or--YR1 where Y is an aryl or heteroaryl group; R8 and R8a are each independently hydrogen or substituted or unsubstituted alkyl or together form ═O; R9 is--CH2CH2CON(CH2CON(CH2COOH)2) 2; or--N(CH2COOH)2 R10 is hydrogen, or substituted or unsubstituted alkyl and; each of R1-R10, when substituted, is substituted with one or more substituents each independently selected from Q, where Q is alkyl, haloalkyl, halo, pseudohalo, or--COORb where Rb is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, araalkyl, or ORc where Rc is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, or aryl or CONRdRe where Rd and Re are each independently hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, or aryl, or NRfRg where Rf and Rg are each independently hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, or aryl, or ═NRh where Rh is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, or aryl, or is an amino acid residue; each Q is independently unsubstituted or is substituted with one or more substituents each independently selected from Q1, where Q1 is alkyl, haloalkyl, halo, pseudohalo, or--COORb where Rb is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, araalkyl, or ORc where Rc is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, or aryl or CONRdRe where Rd and Re are each independently hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, or aryl, or NRfRg where Rf and Rg are each independently hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, or aryl, or ═NRh where Rh is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, or aryl, or is an amino acid residue. 3. A compound according to claim 2 having the formula: 4. A compound according to claim 2 having the formula: 5. A compound according to claim 2 having the formula: 6. The compound of claim 2, wherein: R1 is substituted or unsubstituted alkyl; R2 is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or--C(O)Ra, where Ra is substituted or unsubstituted alkyl; R1a and R2a together form a covalent bond; R3 and R4 are each independently substituted or unsubstituted alkyl; R3a and R4a are each independently hydrogen, or together form a covalent bond; R5 is substituted or unsubstituted alkyl; R6 and R6a together form ═O; R7 is azaalkyl, or azaaralkyl; R8 and R8a together form ═O; R9 and R10 are each independently substituted or unsubstituted alkyl; each of R1-R10, when substituted, is substituted with one or more substituents each independently selected from Q, where Q is halo, pseudohalo, haloalkyl, COORb where Rb is hydrogen or alkyl, ORc where Rc is alkyl or aralkyl, NRfRg where Rf and Rg are each independently hydrogen, alkyl or aralkyl, or ═NRh where Rh is aralkyl; each Q is independently unsubstituted or is substituted with one or more substituents each independently selected from Q1, where Q1 is halo, pseudohalo, or haloalkyl. 7. The compound of claim 2, wherein: R1 is unsubstituted alkyl; R2 is substituted or unsubstituted alkyl, unsubstituted alkenyl, or--C(O)Ra, where Ra is unsubstituted alkyl; R1a and R2a together form a covalent bond; R3 and R4 are each independently unsubstituted alkyl; R3a and R4a are each independently hydrogen, or together form a covalent bond; R5 is unsubstituted alkyl; R6 and R6a together form ═O; R7 is azaalkyl, or azaaralkyl; R8 and R8a together form ═O; R10 is unsubstituted alkyl; each of R1-R10, when substituted, is substituted with one or more substituents each independently selected from Q, where Q is halo, pseudohalo, haloalkyl, COORb where Rb is hydrogen or alkyl, ORc where Rc is alkyl or aralkyl, NRfRg where Rf and Rg are each independently hydrogen, alkyl or aralkyl, or ═NRh where Rh is aralkyl; each Q is independently unsubstituted or is substituted with one or more substituents each independently selected from Q1, where Q1 is halo, pseudohalo, or haloalkyl. 8. The compound of claim 2, wherein: R1 is methyl; R1a and R2a together form a covalent bond; R3 is methyl; R4 is ethyl; R3a and R4a are each independently hydrogen, or together form a covalent bond; R5 is methyl; and R10 is methyl. 9. The compound claim 2, wherein: R2 is CH═CH2, CH(OR20)CH3, C(O)Me, C(═NR21)CH3 or CH(NHR21)CH3; where R20 is methyl, butyl, heptyl, dodecyl or 3,5-bis(trifluoromethyl)-benzyl; and R21 is 3,5-bis(trifluoromethyl)benzyl. 10. The compound of claim 2, wherein: R7 is ═NR20, where R20 is methyl, butyl, heptyl, dodecyl or 3,5-bis(trifluoromethyl)-benzyl. 11. A pharmaceutical composition, comprising a compound of claim 1 or a pharmaceutically acceptable derivative thereof in a pharmaceutically acceptable carrier. 12. A pharmaceutical composition, comprising a compound of claim 2 or a pharmaceutically acceptable derivative thereof in a pharmaceutically acceptable carrier.
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