IPC분류정보
국가/구분 |
United States(US) Patent
등록
|
국제특허분류(IPC7판) |
|
출원번호 |
US-0177129
(2002-06-21)
|
발명자
/ 주소 |
- Pandey,Ravindra K.
- Grossman,Zachary
- Kanter,Peter
- Dougherty,Thomas J.
|
출원인 / 주소 |
|
인용정보 |
피인용 횟수 :
3 인용 특허 :
32 |
초록
▼
A compound comprising a chemical combination of a photodynamic tetra-pyrrolic compound with a plurality of radionuclide element atoms such that the compound may be used to enhance MR imaging and also be used as a photodynamic compound for use in photodynamic therapy to treat hyperproliferative tissu
A compound comprising a chemical combination of a photodynamic tetra-pyrrolic compound with a plurality of radionuclide element atoms such that the compound may be used to enhance MR imaging and also be used as a photodynamic compound for use in photodynamic therapy to treat hyperproliferative tissue. The preferred compounds have the structural formula: where R1, R2, R2a R3, R3a R4, R5, R5a R6, R7, R 7a, and R8 cumulatively contain at least two functional groups that will complex or combine with an MR imaging enhancing element or ion. The compound is intended to include such complexes and combinations and includes the use of such compounds for MR imaging and photodynamic therapy treatment of tumors and other hyperproliferative tissue.
대표청구항
▼
The invention claimed is: 1. A composition comprising a chemical combination of a photodynamic tetra-pyrrolic compound having a porphyrin or chlorin structure having four pendant groups attached to at least one pyrolle ring, said compound being provided with a plurality of radionuclide element atom
The invention claimed is: 1. A composition comprising a chemical combination of a photodynamic tetra-pyrrolic compound having a porphyrin or chlorin structure having four pendant groups attached to at least one pyrolle ring, said compound being provided with a plurality of radionuclide element atoms connected to a plurality of functional groups that will complex or combine with an MR imaging enhancing element or ion selected from the group consisting of--(CH2)2CONHphenyleneCH 2DTPA;--CH2CH2CON(CONHphenylene-CH2DTPA) 2 such that the compound may be used to enhance MR imaging wherein--CH2CH2CON(CONHphenylene-CH2DTPA) 2 counts as two such functional groups. 2. The composition of claim 1 wherein the radionuclide element is selected from the group consisting of Technetium99, Indium111, radioactive iodine and a Lanthanum series element including Gadolinium. 3. The composition of claim 1 wherein the radionuclide element forms cations and the compound is a chelate of the radionuclide element with the porphyrin or chlorin structure. 4. The composition of claim 1 wherein the radionuclide element forms anions and the compound is a direct chemical combination of the radionuclide element with a porphyrin or chlorin structure. 5. A compound having the structural formula: where R1, R2, R2a R3, R3a R4, R5, R5a R6, R 7, R7a, and R8 cumulatively contain at least two functional groups that complex or combine with an MR imaging enhancing element or ion; R1 is--CH═CH2,--CHO, COOH, where R9=--OR10 where R10 is lower alkyl of 1 through 8 carbon atoms,--((CH2)2O)n CH3 where n is 0 through 3, or--(CH2)2 CONHphenyleneCH2DTPA; R2, R2a, R3, R3a, R4, R5, R5a, R7, and R7a are independently hydrogen, lower alkyl or substituted lower alkyl so as to contain a functional group that will combine with a radionuclide element selected from the group consisting of Technetium 99, Indium111, radioactive iodine and a Lanthanum series element including Gadolinium or two R2, R2a, R3 , R3a, R5, R5a, R7, and R7a groups on adjacent carbon atoms may be taken together to form a covalent bond or two R2, R2a, R3, R3a, R 5, R5a, R7, and R7a groups on the same carbon atom may form a double bond to a divalent pendant group; R2 and R3 may together form a 5 or 6 membered heterocyclic ring containing oxygen, nitrogen or sulfur; R6 is--CH2--,--NR11--or a covalent bond; R8 is--(CH2) 2CO2CH3,--(CH2)2 CONHphenyleneCH2DTPA,--CH2CH2 CON(CONHphenyleneCH2DTPA)2,--CH2R11 or where R11 is and polynuclide complexes thereof; wherein the functional groups that will complex or combine with an MR imaging enhancing element or ion are selected from the group consisting of--(CH2) 2CONHphenyleneCH2DTPA;--CH2CH2 CON(CONHphenyleneCH2DTPA)2; wherein--CH2CH2CON(CONHphenylene-CH 2DTPA)2 counts as two such functional groups. 6. The compound of claim 5 wherein the compound is a dinuclide complex of gadolinium III. 7. The compound of claim 6 where R8 is--CH2 CH2CON(CONHphenyleneCH2DTPA)2. 8. The compound of claim 7 wherein R2, R2a, R3, R3a, R4, R5, R5a, R 7, and R7a are independently hydrogen or lower alkyl of 1 through 4 carbon atoms, R1 is and R9 is--O-hexyl. 9. A compound of the formula: where R1 is--CH═CH2,--CHO, COOH, or where R9=--OR10 where R10 is lower alkyl of 1 through 8 carbon atoms,--((CH2)2O)n CH3 where n is 0 through 3, or--(CH2)2 CONHphenyleneCH2DTPA; R2, R2a, R3, R3a, R7, and R7a are independently hydrogen, lower alkyl or substituted lower alkyl so as to contain a functional group that will combine with a radionuclide element is selected from the group consisting of Technetium99, Indium111, radioactive iodine and a Lanthanum series element including Gadolinium or two R2, R2a, R3, R3a, R7, and R7a groups on adjacent carbon atoms may be taken together to form a covalent bond or two R2, R2a, R3, R 3a, R7, and R7a groups on the same carbon atom may form a double bond to a divalent pendant group; and R6 is--CH2--,--NR11--or a covalent bond where R11 is lower alkyl of 1 through 6 carbon atoms; and R12 is--COORa where Ra is hydrogen or lower alkyl of 1 through 8 carbon atoms; and dinuclide complexes thereof; wherein the functional groups that will complex or combine with an MR imaging enhancing element or ion are selected from the group consisting of--(CH2)2 CONHphenyleneCH2DTPA;--CH2CH2 CON(CONHphenylene-CH2 DTPA)2; and 10. The compound of claim 9 where the compound is a digadolinium III complex. 11. The compound of claim 9 where R2 is--CH3 and R3 is--CH2CH3. 12. The compound or complex of claim 9 where R6 is--NR11--where R11 is hexyl. 13. A di-technetium99m complex of the compound of claim 1. 14. A di-indium111 complex of the compound of claim 1. 15. The compound of claim 1 that is a di-99mTc complex of a bisaminoethanethiol derivative of HPPH. 16. The compound of claim 1 that is HPPH-di-Gd(III)di-aminophenylDTPA. 17. The compound of claim 1 that is purpurin 18 imide-di-Gd(III)di-aminophenylDTPA. 18. The compound of claim 1 that is a di-Gd(III)di-aminophenylDTPA derivative of bacteriochlorin. 19. The compound of claim 5 wherein the compound is a dicomplex of radionuclide element technetium99m, indium111 or gadolinium III. 20. A method for the detection of tumors that comprises injecting from about 5 to about 20 μmol/kg of body weight of the compound of claim 1 into a mammal followed by MR imaging of the mammal to locate and visualize the tumors. 21. The method of claim 20 wherein the tumor is exposed to light at the absorption frequency of the compound after MR imaging at a sufficient intensity to cause tumor necrosis. 22. A method for the detection of tumors that comprises injecting from about 5 to about 20 μmol/kg of body weight of the compound of claim 3 into a mammal followed by MR imaging of the mammal to locate and visualize the tumors. 23. The method of claim 22 wherein the tumor is exposed to light at the absorption frequency of the compound after MR imaging at a sufficient intensity to cause tumor necrosis. 24. A method for the detection of tumors that comprises injecting from about 5 to about 20 μmol/kg of body weight of the compound of claim 5 into a mammal followed by MR imaging of the mammal to locate and visualize the tumors. 25. The method of claim 24 wherein the tumor is exposed to light at the absorption frequency of the compound after MR imaging at a sufficient intensity to cause tumor necrosis. 26. A method for the detection of tumors that comprises injecting from about 5 to about 20 μmol/kg of body weight of the compound of claim 6 into a mammal followed by MR imaging of the mammal to locate and visualize the tumors. 27. The method of claim 26 wherein the tumor is exposed to light at the absorption frequency of the compound after MR imaging at a sufficient intensity to cause tumor necrosis. 28. A method for the detection of tumors that comprises injecting from about 5 to about 20 μmol/kg of body weight of the compound of claim 7 into a mammal followed by MR imaging of the mammal to locate and visualize the tumors. 29. The method of claim 28 wherein the tumor is exposed to light at the absorption frequency of the compound after MR imaging at a sufficient intensity to cause tumor necrosis. 30. A method for the detection of tumors that comprises injecting from about 5 to about 20 μmol/kg of body weight of the compound of claim 8 into a mammal followed by MR imaging of the mammal to locate and visualize the tumors. 31. The method of claim 30 wherein the tumor is exposed to light at the absorption frequency of the compound after MR imaging at a sufficient intensity to cause tumor necrosis. 32. A method for the detection of tumors that comprises injecting from about 5 to about 20 μmol/kg of body weight of the compound of claim 9 into a mammal followed by MR imaging of the mammal to locate and visualize the tumors. 33. The method of claim 32 wherein the tumor is exposed to light at the absorption frequency of the compound after MR imaging at a sufficient intensity to cause tumor necrosis. 34. A method for the detection of tumors that comprises injecting from about 5 to about 20 μmol/kg of body weight of the compound of claim 10 into a mammal followed by MR imaging of the mammal to locate and visualize the tumors. 35. The method of claim 34 wherein the tumor is exposed to light at the absorption frequency of the compound after MR imaging at a sufficient intensity to cause tumor necrosis. 36. A method for the detection of tumors that comprises injecting from about 5 to about 20 μmol/kg of body weight of the compound of claim 11 into a mammal followed by MR imaging of the mammal to locate and visualize the tumors. 37. The method of claim 36 wherein the tumor is exposed to light at the absorption frequency of the compound after MR imaging at a sufficient intensity to cause tumor necrosis. 38. A method for the detection of tumors that comprises injecting from about 5 to about 20 μmol/kg of body weight of the compound of claim 11 into a mammal followed by MR imaging of the mammal to locate and visualize the tumors. 39. The method of claim 38 wherein the tumor is exposed to light at the absorption frequency of the compound after MR imaging at a sufficient intensity to cause tumor necrosis. 40. A method for the detection of tumors that comprises injecting from about 5 to about 20 μmol/kg of body weight of the compound of claim 12 into a mammal followed by MR imaging of the mammal to locate and visualize the tumors. 41. The method of claim 40 wherein the tumor is exposed to light at the absorption frequency of the compound after MR imaging at a sufficient intensity to cause tumor necrosis. 42. A method for the detection of tumors that comprises injecting from about 5 to about 20 μmol/kg of body weight of the compound of claim 16 into a mammal followed by MR imaging of the mammal to locate and visualize the tumors. 43. The method of claim 42 wherein the tumor is exposed to light at the absorption frequency of the compound after MR imaging at a sufficient intensity to cause tumor necrosis. 44. A method for the detection of tumors that comprises injecting from about 5 to about 20 μmol/kg of body weight of the compound of claim 17 into a mammal followed by MR imaging of the mammal to locate and visualize the tumors. 45. The method of claim 44 wherein the tumor is exposed to light at the absorption frequency of the compound after MR imaging at a sufficient intensity to cause tumor necrosis. 46. A method for the detection of tumors that comprises injecting from about 5 to about 20 μmol/kg of body weight of the compound of claim 18 into a mammal followed by MR imaging of the mammal to locate and visualize the tumors. 47. The method of claim 46 wherein the tumor is exposed to light at the absorption frequency of the compound after MR imaging at a sufficient intensity to cause tumor necrosis. 48. The compound of claim 1 where the compound is a digadolinium III complex.
※ AI-Helper는 부적절한 답변을 할 수 있습니다.