AR106040A1 - Moduladores de la proteína core de la hepatitis b - Google Patents
Moduladores de la proteína core de la hepatitis bInfo
- Publication number
- AR106040A1 AR106040A1 ARP160102819A ARP160102819A AR106040A1 AR 106040 A1 AR106040 A1 AR 106040A1 AR P160102819 A ARP160102819 A AR P160102819A AR P160102819 A ARP160102819 A AR P160102819A AR 106040 A1 AR106040 A1 AR 106040A1
- Authority
- AR
- Argentina
- Prior art keywords
- 6alkyl
- group
- optionally substituted
- halogen
- hydroxyl
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/554—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
- A61P31/22—Antivirals for DNA viruses for herpes viruses
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
- C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
- C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
- C07D243/38—[b, e]- or [b, f]-condensed with six-membered rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D267/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D267/02—Seven-membered rings
- C07D267/08—Seven-membered rings having the hetero atoms in positions 1 and 4
- C07D267/12—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
- C07D267/16—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with two six-membered rings
- C07D267/20—[b, f]-condensed
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D281/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one sulfur atom as the only ring hetero atoms
- C07D281/02—Seven-membered rings
- C07D281/04—Seven-membered rings having the hetero atoms in positions 1 and 4
- C07D281/08—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
- C07D281/12—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with two six-membered rings
- C07D281/16—[b, f]-condensed
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
- C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
Abstract
Reivindicación 1: Un compuesto caracterizado porque representado mediante la fórmula (1), donde Y se selecciona del grupo que consiste en S(O)ʸ, C=O, C(R¹¹)₂, NRY y O donde y es 0, 1 ó 2; R¹¹, en cada caso, se selecciona del grupo que consiste en H, halógeno, y C₁₋₆alquilo (opcionalmente sustituido con uno, dos o tres halógenos); RY se selecciona del grupo que consiste en H, metilo, etilo, propilo, propenilo, butilo, fenilo y bencilo, donde RY, cuando no es H, puede estar opcionalmente sustituido con hidroxilo; RZ se selecciona del grupo que consiste en H, metilo, etilo, propilo, fenilo y bencilo; Rᵐ y Rᵐ se seleccionan en forma independiente entre sí del grupo que consiste en H, C₁₋₆alquilo (opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados cada uno de forma independiente entre halógeno e hidroxilo), y C₂₋₆alquenilo (opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados cada uno de forma independiente entre halógeno e hidroxilo); Rᶜ se selecciona del grupo que consiste en H, C₁₋₆alquilo y C₂₋₆alquenilo; R⁷⁷ se selecciona del grupo que consiste en H, halógeno, ciano, y C₁₋₆alquilo; R⁷⁸ se selecciona del grupo que consiste en H, halógeno, ciano, C₁₋₆alquilo, carboxi, -C(O)-O-C₁₋₆alquilo; C₃₋₆cicloalquilo, -NRR; fenilo (opcionalmente sustituido con uno, dos, tres o cuatro sustituyentes seleccionados cada uno de forma independiente del grupo que consiste en R⁷³); bencilo (opcionalmente sustituido con uno o más sustituyentes seleccionados cada uno de forma independiente del grupo que consiste en R⁷³), heterociclo de 4 - 7 miembros (opcionalmente sustituido con uno o más sustituyentes seleccionados cada uno de forma independiente del grupo que consiste en R⁷³); heteroarilo monocíclico de 4 - 7 miembros (opcionalmente sustituido con uno o más sustituyentes seleccionados cada uno de forma independiente del grupo que consiste en R⁷³); heteroarilo bicíclico de 9 - 10 miembros (opcionalmente sustituido con uno o más sustituyentes seleccionados cada uno de forma independiente del grupo que consiste en R⁷³), X²-R⁷⁹, y X²-C₁₋₆alquilen-R⁷⁹; X² se selecciona del grupo que consiste en S(O)ʷ (donde w es 0, 1, ó 2), O, -C(O)- y NR; R⁷⁹ se selecciona del grupo que consiste en H, hidroxilo, halógeno, C₁₋₆alquilo, -C(O)-O-C₁₋₆alquilo, heterociclo (opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo que consiste en halógeno, NRR, -C(O)-O-C₁₋₆alquilo, carboxi y C₁₋₆alquilo), -C(O)-NRR, -C(=NH)-NRR, heteroarilo, fenilo (opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo que consiste en halógeno, NRR, -C(O)-O-C₁₋₆alquilo, carboxi, C₁₋₆alcoxi, y C₁₋₆alquilo), C₂₋₆alquenilo, C₂₋₆alquinilo, C₁₋₆alcoxi, carboxi, NRR, -C(O)-C₁₋₆alquilo, C₃₋₆cicloalquilo, -NR-C(O)-C₁₋₆alquilo, NR-C(O)-O-C₁₋₆alquilo, -S(O)ʷ-C₁₋₆alquilo (donde w es 0, 1 ó 2), -S(O)ʷ-NRR (donde w es 0, 1 ó 2), y -NR-S(O)ʷ-C₁₋₆alquilo (donde w es 0, 1 ó 2)); R⁷³ se selecciona del grupo que consiste en H, halógeno, hidroxilo, nitro, ciano, carboxi, oxo, C₁₋₆alquilo, -C(O)-O-C₁₋₆alquilo, heterociclo (opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo que consiste en halógeno, hidroxilo, oxo, NRR, -C(O)-O-C₁₋₆alquilo, carboxi y C₁₋₆alquilo), -C(O)-NR-C₁₋₆alquilo, -C(=NH)-NRR, heteroarilo, fenilo, C₂₋₆alquenilo, C₂₋₆alquinilo, C₁₋₆alcoxi, carboxi, oxo, NRR, -C(O)-C₁₋₆alquilo, -C₃₋₆cicloalquilo, NR-C(O)-C₁₋₆alquilo, NR-C(O)-O-C₁₋₆alquilo, -S(O)ʷ-C₁₋₆alquilo (donde w es 0, 1 ó 2), -S(O)ʷ-NRR (donde w es 1, 2 ó 3), -NR-S(O)ʷ-C₁₋₆alquilo (donde w es 0, 1 ó 2), C(O)-NR-C₁₋₆alquilo, C(O)-C₁₋₃alquilen-NR-C(O)-O-C₁₋₆alquilo, X²-R⁷⁹; y X²-C₁₋₆alquilen-R⁷⁹; R se selecciona, en forma independiente en cada caso, entre H, metilo, etilo, ciclopropilo, ciclobutilo, y propilo; R se selecciona, en forma independiente en cada caso, entre H, metilo, etilo, propilo (opcionalmente sustituido con hidroxilo), butilo (opcionalmente sustituido con hidroxilo), -C(O)-metilo y -C(O)-etilo, o R y R tomados junto con el nitrógeno al cual están unidos pueden formar un heterociclo de 4 - 7 miembros opcionalmente sustituido con uno, dos o más sustituyentes seleccionados del grupo que consiste en halógeno, hidroxilo, NH₂, -C(O)-O-C₁₋₃alquilo, -C(O)-C₁₋₃alquilo, carboxi, oxo, y C₁₋₃alquilo; cada una de las porciones R⁴, R⁵, R⁶, R⁷, R⁸, R⁹, y R¹⁰ se selecciona en forma independiente en cada caso entre el grupo que consiste en hidrógeno, C₁₋₆alquilo, C₁₋₆alcoxi, C₂₋₆alquinilo, C₂₋₆alquenilo, halógeno, hidroxilo, nitro, ciano, y NRR; donde en cada caso, C₁₋₆alquilo, C₂₋₆alquenilo o C₂₋₆alquinilo puede estar opcionalmente sustituido con uno, dos, tres o más sustituyentes seleccionados del grupo que consiste en halógeno, hidroxilo, nitro, ciano, carboxi, C₃₋₆cicloalquilo, C₂₋₄alquenilo, C₂₋₄alquinilo, C₁₋₃alcoxi, NRR, -NR-S(O)ʷ-C₁₋₂alquilo (donde w es 0, 1 ó 2), NR-C(O)-C₁₋₃alquilo, NR-C(O)-O-C₁₋₃alquilo, y S(O)ʷ-NRR (donde w es 0, 1 ó 2); C₁₋₆alcoxi puede estar opcionalmente sustituido con uno, dos, tres o más sustituyentes seleccionados del grupo que consiste en halógeno, hidroxilo, nitro, ciano, carboxi, C₁₋₃alquilo, NRR, -NR-S(O)ʷ-C₁₋₂alquilo (donde w es 0, 1 ó 2), y S(O)ʷ-NRR (donde w es 0, 1 ó 2); C₁₋₆alquileno puede estar opcionalmente sustituido con un sustituyente seleccionado entre el grupo que consiste en C₃₋₆ cicloalquilo, hidroxilo, ciano, y halógeno; y sales aceptables farmacéuticamente y N-óxidos del mismo.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201562218815P | 2015-09-15 | 2015-09-15 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR106040A1 true AR106040A1 (es) | 2017-12-06 |
Family
ID=58289869
Family Applications (3)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP160102819A AR106040A1 (es) | 2015-09-15 | 2016-09-15 | Moduladores de la proteína core de la hepatitis b |
ARP160102816A AR106037A1 (es) | 2015-09-15 | 2016-09-15 | Moduladores de la proteína core de la hepatitis b |
ARP160102820A AR106041A1 (es) | 2015-09-15 | 2016-09-15 | Moduladores de la proteína core de la hepatitis b |
Family Applications After (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP160102816A AR106037A1 (es) | 2015-09-15 | 2016-09-15 | Moduladores de la proteína core de la hepatitis b |
ARP160102820A AR106041A1 (es) | 2015-09-15 | 2016-09-15 | Moduladores de la proteína core de la hepatitis b |
Country Status (28)
Country | Link |
---|---|
US (6) | US10377748B2 (es) |
EP (4) | EP3349580B1 (es) |
JP (4) | JP2018531919A (es) |
KR (3) | KR20180053363A (es) |
CN (4) | CN108347942B (es) |
AR (3) | AR106040A1 (es) |
AU (4) | AU2016323297A1 (es) |
CA (3) | CA2998803A1 (es) |
CL (2) | CL2018000684A1 (es) |
CY (1) | CY1123570T1 (es) |
DK (1) | DK3349580T3 (es) |
DO (1) | DOP2018000074A (es) |
EA (3) | EA201890736A1 (es) |
ES (2) | ES2831333T3 (es) |
HK (3) | HK1258761A1 (es) |
HR (1) | HRP20201812T1 (es) |
HU (1) | HUE051872T2 (es) |
IL (3) | IL258099A (es) |
LT (1) | LT3349580T (es) |
MX (4) | MX2018003207A (es) |
PH (3) | PH12018500572A1 (es) |
PT (1) | PT3349580T (es) |
RS (1) | RS61064B1 (es) |
SG (1) | SG10202011103UA (es) |
SI (1) | SI3349580T1 (es) |
TW (4) | TW201720802A (es) |
WO (3) | WO2017048950A1 (es) |
ZA (1) | ZA201802456B (es) |
Families Citing this family (60)
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TW201720802A (zh) * | 2015-09-15 | 2017-06-16 | 艾森伯利生物科學公司 | B型肝炎核心蛋白質調節劑 |
US10987360B2 (en) | 2016-09-15 | 2021-04-27 | Assembly Biosciences, Inc. | Hepatitis B core protein modulators |
AU2017342536A1 (en) | 2016-10-14 | 2019-05-02 | Precision Biosciences, Inc. | Engineered meganucleases specific for recognition sequences in the Hepatitis B virus genome |
CA3040919A1 (en) | 2016-11-07 | 2018-05-11 | Arbutus Biopharma Corporation | Substituted pyridinone-containing tricyclic compounds, and methods using same |
BR112019017603A2 (pt) * | 2017-02-23 | 2020-03-24 | Fujian Cosunter Pharmaceutical Co., Ltd. | Composto de tri-ciclo e aplicações do mesmo |
SG11201908012SA (en) | 2017-03-02 | 2019-09-27 | Assembly Biosciences Inc | Cyclic sulfamide compounds and methods of using same |
CN110612300B (zh) | 2017-03-13 | 2023-10-20 | 组装生物科学股份有限公司 | 制备乙型肝炎核心蛋白调节剂的方法 |
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KR20200083551A (ko) | 2017-11-02 | 2020-07-08 | 아이쿠리스 게엠베하 운트 코. 카게 | B형 간염 바이러스 (hbv)에 활성인 신규 고활성 아미노-티아졸 치환된 인돌-2-카르복스아미드 |
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AU2018392212B9 (en) | 2017-12-20 | 2021-03-18 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 2'3' cyclic dinucleotides with phosphonate bond activating the STING adaptor protein |
KR102492187B1 (ko) | 2017-12-20 | 2023-01-27 | 인스티튜트 오브 오가닉 케미스트리 앤드 바이오케미스트리 에이에스 씨알 브이.브이.아이. | Sting 어댑터 단백질을 활성화하는 포스포네이트 결합을 가진 3'3' 사이클릭 다이뉴클레오티드 |
CN111788204B (zh) | 2018-02-26 | 2023-05-05 | 吉利德科学公司 | 作为hbv复制抑制剂的取代吡咯嗪化合物 |
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TW202005654A (zh) | 2018-04-06 | 2020-02-01 | 捷克科學院有機化學與生物化學研究所 | 2,2,─環二核苷酸 |
TWI818007B (zh) | 2018-04-06 | 2023-10-11 | 捷克科學院有機化學與生物化學研究所 | 2'3'-環二核苷酸 |
KR20200140867A (ko) | 2018-04-06 | 2020-12-16 | 인스티튜트 오브 오가닉 케미스트리 앤드 바이오케미스트리 에이에스 씨알 브이.브이.아이. | 3'3'-사이클릭 다이뉴클레오티드 |
TW201945388A (zh) | 2018-04-12 | 2019-12-01 | 美商精密生物科學公司 | 對b型肝炎病毒基因體中之識別序列具有特異性之最佳化之經工程化巨核酸酶 |
CA3099138A1 (en) * | 2018-05-03 | 2019-11-07 | Emory University | Modulators of orphan nuclear receptors for nash and other metabolic disorders |
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