Modified oligonucleotides for telomerase inhibition
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-031/7052
C12N-005/00
C07H-021/00
C12N-015/113
A61K-047/48
C07H-021/02
C07H-021/04
C07C-233/18
출원번호
US-0720467
(2015-05-22)
등록번호
US-9388416
(2016-07-12)
발명자
/ 주소
Gryaznov, Sergei
Pongracz, Krisztina
출원인 / 주소
Gryaznov, Sergei
대리인 / 주소
Francis, Carol L.
인용정보
피인용 횟수 :
1인용 특허 :
49
초록▼
Compounds comprising an oligonucleotide moiety covalently linked to a lipid moiety are disclosed. The oligonucleotide moiety comprises a sequence that is complementary to the RNA component of human telomerase. The compounds inhibit telomerase activity in cells with a high potency and have superior c
Compounds comprising an oligonucleotide moiety covalently linked to a lipid moiety are disclosed. The oligonucleotide moiety comprises a sequence that is complementary to the RNA component of human telomerase. The compounds inhibit telomerase activity in cells with a high potency and have superior cellular uptake characteristics.
대표청구항▼
1. A method of inhibiting the proliferation of a cancer cell comprising contacting the cancer cell with a compound having the following structure: wherein “nps” represents a thiophosphoramidate linkage,—NH—P(═O)(SH)—O—, connecting the 3′-carbon of one nucleoside to the 5′-carbon of the adjacent nucl
1. A method of inhibiting the proliferation of a cancer cell comprising contacting the cancer cell with a compound having the following structure: wherein “nps” represents a thiophosphoramidate linkage,—NH—P(═O)(SH)—O—, connecting the 3′-carbon of one nucleoside to the 5′-carbon of the adjacent nucleoside;or a pharmaceutically acceptable salt thereof. 2. The method of claim 1, wherein the cancer is skin cancer, connective tissue cancer, adipose cancer, breast cancer, lung cancer, stomach cancer, pancreas cancer, ovary cancer, cervix cancer, uterus cancer, kidney cancer, bladder cancer, colon cancer, prostate cancer, central nervous system (CNS) cancer, retina cancer, or a hematologic cancer. 3. The method of claim 2, wherein the cancer is lung cancer. 4. The method of claim 2, wherein the cancer is a hematologic cancer. 5. The method of claim 4, wherein the hematologic cancer is myeloma, leukemia, or lymphoma. 6. The method of claim 2, wherein the cancer is breast cancer. 7. A method of treating cancer comprising contacting the cancer with a compound having the structure: wherein “nps” represents a thiophosphoramidate linkage,—NH—P(═O)(SH)—O—, connecting the 3′-carbon of one nucleoside to the 5′-carbon of the adjacent nucleoside; or a pharmaceutically acceptable salt thereof; andwherein the cancer is skin cancer, connective tissue cancer, adipose cancer, breast cancer, lung cancer, stomach cancer, pancreas cancer, ovary cancer, cervix cancer, uterus cancer, kidney cancer, bladder cancer, colon cancer, prostate cancer, central nervous system (CNS) cancer, retina cancer, or a hematologic cancer. 8. The method of claim 7, wherein the cancer is lung cancer. 9. The method of claim 7, wherein the cancer is a hematologic cancer. 10. The method of claim 9, wherein the hematologic cancer is myeloma, leukemia, or lymphoma. 11. The method of claim 7, wherein the cancer is breast cancer. 12. A method of inhibiting the proliferation of a cancer in a patient comprising administering to the patient a pharmaceutical composition comprising a compound having the structure: wherein “nps” represents a thiophosphoramidate linkage,—NH—P(═O)(SH)—O—, connecting the 3′-carbon of one nucleoside to the 5′-carbon of the adjacent nucleoside;or a pharmaceutically acceptable salt thereof; andwherein the cancer is skin cancer, connective tissue cancer, adipose cancer, breast cancer, lung cancer, stomach cancer, pancreas cancer, ovary cancer, cervix cancer, uterus cancer, kidney cancer, bladder cancer, colon cancer, prostate cancer, central nervous system (CNS) cancer, retina cancer, or a hematologic cancer. 13. The method of claim 12, wherein the cancer is lung cancer. 14. The method of claim 12, wherein the cancer is a hematologic cancer. 15. The method of claim 14, wherein the hematologic cancer is myeloma, leukemia, or lymphoma. 16. The method of claim 12, wherein the cancer is breast cancer. 17. A method of treating cancer in a patient comprising administering to the patient a pharmaceutical composition comprising a compound having the structure: wherein “nps” represents a thiophosphoramidate linkage,—NH—P(═O)(SH)—O—, connecting the 3′-carbon of one nucleoside to the 5′-carbon of the adjacent nucleoside;or a pharmaceutically acceptable salt thereof; andwherein the cancer is skin cancer, connective tissue cancer, adipose cancer, breast cancer, lung cancer, stomach cancer, pancreas cancer, ovary cancer, cervix cancer, uterus cancer, kidney cancer, bladder cancer, colon cancer, prostate cancer, central nervous system (CNS) cancer, retina cancer, or a hematologic cancer. 18. The method of claim 17, wherein the cancer is lung cancer. 19. The method of claim 17, wherein the cancer is a hematologic cancer. 20. The method of claim 19, wherein the hematologic cancer is myeloma, leukemia, or lymphoma. 21. The method of claim 17, wherein the cancer is breast cancer.
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이 특허에 인용된 특허 (49)
Fung Steven (Palo Alto CA) Woo Sam L. (Redwood City CA) Smith Lloyd M. (South Pasadena CA), Amino-derivatized phosphite and phosphate linking agents, phosphoramidite precursors, and useful conjugates thereof.
McKay Robert ; Dean Nicholas ; Monia Brett P. ; Nero Pamela Scott ; Gaarde William A., Antisense oligonucleotide compositions and methods for the modulation of JNK proteins.
Hostetler Karl Y. (Del Mar CA) Kumar Raj (San Diego CA), Method of converting a drug to an orally available form by covalently bonding a lipid to the drug.
Shay Jerry W. ; Wright Woodring E. ; Piatyszek Mieczyslaw A. ; Corey David R. ; Norton James C., Modulation of mammalian telomerase by peptide nucleic acids.
Hanecak,Ronnie C.; Anderson,Kevin P.; Bennett,C. Frank; Chiang,Ming Yi; Brown Driver,Vickie L.; Ecker,David J.; Vickers,Timothy A.; Wyatt,Jacqueline R., Modulation of telomere length by oligonucleotides having a G-core sequence.
Letsinger Robert L. (Wilmette IL) Gryaznov Sergei M. (San Mateo CA), Oligodeoxyribonucleotides including 3′-aminonucleoside-phosphoramidate linkages and terminal 3′-amino groups.
Gryaznov Sergei M. (San Mateo CA) Schultz Ronald G. (Fremont CA) Chen Jer-kang (Palo Alto CA), Oligonucleotide N3′-P5′phosphoramidates: hybridization and nuclease resistance properties.
Gryaznov Sergei M. (San Mateo CA) Schultz Ronald G. (Fremont CA) Chen Jer-Kang (Palo Alto CA), Oligonucleotide N3′→P5′phosphoramidates: hybridization and nuclease resistance properties.
Gryaznov Sergei M. (San Mateo CA) Schultz Ronald G. (Fremont CA) Chen Jer-kang (Palo Alto CA), Oligonucleotide N3→P5′phosphoramidates: triplex DNA formation.
Bischofberger Norbert ; Kent Ken ; Wagner Rick ; Buhr Chris ; Lin Kuei-Ying, Oligonucleotides and their analogs capable of passive cell membrane permeation.
Hanecak Ronnie C. ; Anderson Kevin P. ; Bennett C. Frank ; Chiang Ming-Yi ; Brown-Driver Vickie L. ; Ecker David J. ; Vickers Timothy A. ; Wyatt Jacqueline R. ; Imbach Jean Louis,FRX, Oligonucleotides having a conserved G4 core sequence.
Letsinger Robert L. (316 3rd St. Wilmette IL 60091) Gryaznov Sergei M. (2 Clark Dr. San Mateo CA 94401), Oligonucleotides having modified internucleoside linkages.
Hirschbein Bernard L. ; Fearon Karen L. ; Gryaznov Sergei M. ; McCurdy Sarah N. ; Nelson Jeffery S. ; Schultz Ronald G., Solid phase synthesis of oligonucleotide N3'-P5' phosphoramidates.
Hirschbein Bernard L. ; Fearon Karen L. ; Gryaznov Sergei M. ; McCurdy Sarah N. ; Nelson Jeffrey S. ; Schultz Ronald G., Synthons for synthesis of oligonucleotide N3-P5 phosphoramidates.
Matsuo, Kazunori; Suzuki, Yasutaka; Takahashi, Masakazu; Nishio, Yoshimichi; Watarihana, Hideaki; Goto, Hiroki; Takahashi, Teruo; Furukawa, Kiyoshi; Kobayashi, Hiroyuki; Kubota, Hidetsugu; Abe, Takuy, System for reproducing information recorded on an information recording medium.
Summerton James E. (Corvallis OR) Weller Dwight D. (Corvallis OR), Uncharged morpolino-based polymers having phosphorous containing chiral intersubunit linkages.
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