AR099768A1 - Inhibidores de diacilglicerol aciltransferasa 2 - Google Patents
Inhibidores de diacilglicerol aciltransferasa 2Info
- Publication number
- AR099768A1 AR099768A1 ARP150100790A ARP150100790A AR099768A1 AR 099768 A1 AR099768 A1 AR 099768A1 AR P150100790 A ARP150100790 A AR P150100790A AR P150100790 A ARP150100790 A AR P150100790A AR 099768 A1 AR099768 A1 AR 099768A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- cooh
- heteroaryl
- aryl
- cycloalkyl
- Prior art date
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- 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
- C07D401/14—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 three or more hetero rings
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- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K31/60—Salicylic acid; Derivatives thereof
- A61K31/606—Salicylic acid; Derivatives thereof having amino groups
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- 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
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- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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- C07—ORGANIC CHEMISTRY
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- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/08—Bridged systems
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Abstract
Compuestos que inhiben la actividad de la diacilglicerol aciltransferasa 2 (DGAT2) y sus usos en el tratamiento de enfermedades relacionadas con estos en animales. Reivindicación 1: Un compuesto, caracterizado porque tiene la fórmula (1) en donde D es N, CH o CF; R¹ es C₁₋₄ alquilo opcionalmente sustituido con 1, 2 ó 3 sustituyentes cada uno seleccionado independientemente de fluoro y C₃₋₆ cicloalquilo; R² es fluoro o C₁₋₄ alquilo; R³ es H, C₁₋₄ alquilo o C₃₋₆ cicloalquilo; R⁴ es H, -C₁₋₄ alquilo, -(C₁₋₄ alquil)ₚ-C₃₋₆ cicloalquilo, -(C₁₋₄ alquil)ₚ-C₃₋₆ heterociclilo, -(C₁₋₄ alquil)ₚ-arilo o -(C₁₋₄ alquil)ₚ-heteroarilo, en donde R⁴ se sustituye opcionalmente con 1, 2, 3 ó 4 sustituyentes seleccionados de halo, ciano, oxo, aminilo, iminilo, -OH, -C₁₋₄ alquilo, -C₁₋₄ fluoroalquilo, -C₁₋₄ alcoxi, -C₃₋₆ cicloalcoxi, -C₁₋₄ fluoroalcoxi, -(C₁₋₄ alquil)q-COOH, -(C₁₋₄ alquil)q-C₃₋₆ cicloalquil-COOH, -(C₁₋₄ alquil)q-C₃₋₆ heterociclil-COOH, -(C₁₋₄ alquil)q-aril-COOH, -(C₁₋₄ alquil)q-heteroaril-COOH, -O-(C₁₋₄ alquil)q-COOH, -O-(C₁₋₄ alquil)q-aril-COOH, -O-(C₁₋₄ alquil)q-heteroaril-COOH, -(C₁₋₄ alquil)q-C₃₋₆ cicloalquilo, -(C₁₋₄ alquil)q-C₃₋₆ heterociclilo, -(C₁₋₄ alquil)q-arilo, -(C₁₋₄ alquil)q-heteroarilo, -C(O)-C₁₋₄ alquilo, -C(O)-C₁₋₄ alcoxi, -C(O)-C₃₋₆ cicloalquilo, -C(O)-C₃₋₆ heterociclilo, -C(O)-NR⁶R⁷, -C(O)-(C₁₋₄ alquil)q-arilo, -C(O)-(C₁₋₄ alquil)q-heteroarilo, -NR⁶R⁷, -NR⁶-C(O)-R⁷, -(C₁₋₄ alquil)q-O-arilo, -(C₁₋₄ alquil)q-O-heteroarilo, -S(O)₂-R⁷ y -S(O)₂-NR⁶R⁷; o R³ y R⁴ juntos se pueden unir para formar un sistema de anillos totalmente saturados o parcialmente saturados de 4 a 10 miembros opcionalmente sustituidos con 1, 2, 3 ó 4 sustituyentes seleccionados de halo, ciano, -OH, -C₁₋₄ alquilo, -C₁₋₄ fluoroalquilo, -C₁₋₄ alcoxi, -C₃₋₆ cicloalcoxi, -C₁₋₄ fluoroalcoxi, -(C₁₋₄ alquil)q-COOH, -(C₁₋₄ alquil)q-C₃₋₆ cicloalquil-COOH, -(C₁₋₄ alquil)q-C₃₋₆ heterociclil-COOH, -(C₁₋₄ alquil)q-aril-COOH, -(C₁₋₄ alquil)q-heteroaril-COOH, -O-(C₁₋₄ alquil)q-COOH, -O-(C₁₋₄ alquil)q-aril-COOH, -O-(C₁₋₄ alquil)q-heteroaril-COOH, -(C₁₋₄ alquil)q-C₃₋₆ cicloalquilo, -(C₁₋₄ alquil)q-C₃₋₆ heterociclilo, -(C₁₋₄ alquil)q-arilo, -(C₁₋₄ alquil)q-heteroarilo, -C(O)-C₁₋₄ alquilo, -C(O)-C₃₋₆ cicloalquilo, -C(O)-C₃₋₆ heterociclilo, -C(O)-arilo, -C(O)-heteroarilo, -C(O)-NR⁶R⁷, -C(O)-C₁₋₄ alquil-arilo, -C(O)-C₁₋₄ alquil-heteroarilo, -NR⁶R⁷, -NR⁶-C(O)-R⁷, -O-arilo, -O-heteroarilo, -C₁₋₄ alquil-O-arilo, -C₁₋₄ alquil-O-heteroarilo, -O-C₁₋₄ alquil-arilo y -O-C₁₋₄ alquil-heteroarilo; R⁵ es H, F o ciano; R⁶ es H, C₁₋₄ alquilo o -S(O)₂-R⁷; R⁷ es H, C₁₋₄ alquilo, -C₃₋₆ cicloalquilo, -C₃₋₆ heterociclilo, arilo o heteroarilo; n es 0, 1, 2 ó 3; p es 0 ó 1; y q es 0 ó 1; o una sal de aquel aceptable desde el punto de vista farmacéutico.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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US201461954351P | 2014-03-17 | 2014-03-17 |
Publications (1)
Publication Number | Publication Date |
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AR099768A1 true AR099768A1 (es) | 2016-08-17 |
Family
ID=52682788
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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ARP150100790A AR099768A1 (es) | 2014-03-17 | 2015-03-16 | Inhibidores de diacilglicerol aciltransferasa 2 |
Country Status (39)
Country | Link |
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US (3) | US9440949B2 (es) |
EP (1) | EP3119757B1 (es) |
JP (1) | JP6152229B2 (es) |
KR (1) | KR101772836B1 (es) |
CN (1) | CN106103425A (es) |
AP (1) | AP2016009407A0 (es) |
AR (1) | AR099768A1 (es) |
AU (1) | AU2015233094B2 (es) |
CA (1) | CA2942759C (es) |
CL (1) | CL2016002169A1 (es) |
CR (1) | CR20160405A (es) |
CU (1) | CU24395B1 (es) |
CY (1) | CY1120354T1 (es) |
DK (1) | DK3119757T3 (es) |
DO (1) | DOP2016000248A (es) |
EA (1) | EA032356B1 (es) |
EC (1) | ECSP16072034A (es) |
ES (1) | ES2674240T3 (es) |
GE (1) | GEP20186864B (es) |
HR (1) | HRP20180992T1 (es) |
HU (1) | HUE039446T2 (es) |
IL (1) | IL247809A0 (es) |
LT (1) | LT3119757T (es) |
MA (1) | MA39753B1 (es) |
MD (1) | MD20160099A2 (es) |
MX (1) | MX2016012008A (es) |
NI (1) | NI201600129A (es) |
PE (1) | PE20161368A1 (es) |
PH (1) | PH12016501654A1 (es) |
PL (1) | PL3119757T3 (es) |
PT (1) | PT3119757T (es) |
RS (1) | RS57384B1 (es) |
SG (1) | SG11201606779RA (es) |
SI (1) | SI3119757T1 (es) |
SV (1) | SV2016005279A (es) |
TR (1) | TR201809388T4 (es) |
TW (1) | TWI551596B (es) |
UY (1) | UY36033A (es) |
WO (1) | WO2015140658A1 (es) |
Families Citing this family (16)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
SI3119757T1 (en) * | 2014-03-17 | 2018-08-31 | Pfizer Inc. | DIACILGLICEROL-ACILTRANSFERAZE 2 BINDERS FOR THE USE IN THE TREATMENT OF PRECIOUS AND RELATED DISEASES |
AR109179A1 (es) * | 2016-08-19 | 2018-11-07 | Pfizer | Inhibidores de diacilglicerol aciltransferasa 2 |
KR102218042B1 (ko) * | 2016-10-17 | 2021-02-18 | 각고호우징 게이오기주크 | 미분화 줄기세포 제거제, 및 미분화 줄기세포 제거 방법 |
CA3043308A1 (en) * | 2016-11-11 | 2018-05-17 | 3-V Biosciences, Inc. | Heterocyclic modulators of lipid synthesis |
GB201815018D0 (en) * | 2018-09-14 | 2018-10-31 | Univ Oxford Innovation Ltd | Enantiomeric compounds |
CN110305966B (zh) * | 2019-06-18 | 2023-03-28 | 广西壮族自治区水产科学研究院 | 一种罗非鱼肝脏dgat2基因表达的调控方法 |
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