PE20171318A1 - Ciclopropabenzofuranil-piridopirazindionas novedosas - Google Patents
Ciclopropabenzofuranil-piridopirazindionas novedosasInfo
- Publication number
- PE20171318A1 PE20171318A1 PE2017001310A PE2017001310A PE20171318A1 PE 20171318 A1 PE20171318 A1 PE 20171318A1 PE 2017001310 A PE2017001310 A PE 2017001310A PE 2017001310 A PE2017001310 A PE 2017001310A PE 20171318 A1 PE20171318 A1 PE 20171318A1
- Authority
- PE
- Peru
- Prior art keywords
- halogen
- methyl
- hydrogen
- dihydro
- cyano
- Prior art date
Links
- 229910052736 halogen Inorganic materials 0.000 abstract 7
- 150000002367 halogens Chemical group 0.000 abstract 7
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 5
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 3
- HCMJWOGOISXSDL-UHFFFAOYSA-N (2-isothiocyanato-1-phenylethyl)benzene Chemical compound C=1C=CC=CC=1C(CN=C=S)C1=CC=CC=C1 HCMJWOGOISXSDL-UHFFFAOYSA-N 0.000 abstract 1
- VHNYOQKVZQVBLC-RTCGXNAVSA-N (4r,7e,9as)-7-[[3-methoxy-4-(4-methylimidazol-1-yl)phenyl]methylidene]-4-(3,4,5-trifluorophenyl)-1,3,4,8,9,9a-hexahydropyrido[2,1-c][1,4]oxazin-6-one Chemical compound C1([C@@H]2COC[C@@H]3CC\C(C(N32)=O)=C/C=2C=C(C(=CC=2)N2C=C(C)N=C2)OC)=CC(F)=C(F)C(F)=C1 VHNYOQKVZQVBLC-RTCGXNAVSA-N 0.000 abstract 1
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 201000010374 Down Syndrome Diseases 0.000 abstract 1
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
- 229910018482 SF5 Inorganic materials 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- 230000000626 neurodegenerative effect Effects 0.000 abstract 1
- 125000004043 oxo group Chemical group O=* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 229940124648 γ-Secretase Modulator Drugs 0.000 abstract 1
Classifications
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- 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
-
- 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
- A61K31/495—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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- C—CHEMISTRY; METALLURGY
- 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
- C07D487/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hospice & Palliative Care (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychiatry (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Se refiere a un compuesto de formula I, donde: X es un heteroarilo de 5 a 14 miembros que contiene 1 a 3 heteroatomos; R1 es hidrogeno, halogeno, entre otros; R2a y R2b son hidrogeno, halogeno, ciano, entre otros; R4a y R4b son hidrogeno, halogeno, oxo, entre otros; R5a y R5b son hidrogeno, halogeno, SF5, entre otros; R6 y R7 son hidrogeno, halogeno, entre otros; R10 es halogeno, ciano, entre otros; R11 es halogeno, ciano, entre otros; y es un numero entero de 1, 2, 3 o 4. Son compuestos preferidos: 2-{[(1aS, 6bR)-4-fluoro-1a-metil-5-(trifluorometoxi)-1,1a-dihidro-6bH-ciclopropa[b][1]benzofuran-6b-il]metil}-7-(4-metil-1H-imidazol-1-il)-3,4-dihidro-2H-pirido[1,2-a]pirazin-1,6-diona; 2-{[(1aS, 6bR)-3-fluoro-1a-metil-5-(trifluorometoxi)-1,1a-dihidro-6bH-ciclopropa[b][1]benzofuran-6b-il]metil}-7-(4-metil-1H-imidazol-1-il)-3,4-dihidro-2H-pirido[1,2-a]pirazin-1,6-diona; entre otros. Tambien se refiere a una composicion farmaceutica. Dichos compuestos son moduladores de gamma-secretasa, siendo utiles en el tratamiento de trastornos neurodegenerativos y neurologicos, tales como la enfermedad de Alzheimer y sindrome de Down.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201562111222P | 2015-02-03 | 2015-02-03 |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20171318A1 true PE20171318A1 (es) | 2017-09-07 |
Family
ID=55299692
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2017001310A PE20171318A1 (es) | 2015-02-03 | 2016-01-26 | Ciclopropabenzofuranil-piridopirazindionas novedosas |
Country Status (22)
Country | Link |
---|---|
US (2) | US20160222007A1 (es) |
EP (1) | EP3253755B1 (es) |
JP (1) | JP6628805B2 (es) |
KR (1) | KR102000382B1 (es) |
CN (1) | CN107406445B (es) |
AR (1) | AR103582A1 (es) |
AU (1) | AU2016214102B2 (es) |
BR (1) | BR112017015693A2 (es) |
CA (1) | CA2919338A1 (es) |
DK (1) | DK3253755T3 (es) |
EA (1) | EA033423B1 (es) |
EC (1) | ECSP17050310A (es) |
ES (1) | ES2818806T3 (es) |
IL (1) | IL253635A0 (es) |
MX (1) | MX368391B (es) |
PE (1) | PE20171318A1 (es) |
PH (1) | PH12017501369A1 (es) |
SG (1) | SG11201705780PA (es) |
TN (1) | TN2017000342A1 (es) |
TW (1) | TWI616445B (es) |
UY (1) | UY36546A (es) |
WO (1) | WO2016125048A1 (es) |
Families Citing this family (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR102271305B1 (ko) | 2020-05-21 | 2021-06-30 | 주식회사 아리바이오 | 치매 예방 및 치료용 조성물 |
CN111978324A (zh) * | 2020-08-28 | 2020-11-24 | 开封康诺药业有限公司 | 一种多索茶碱的晶型及其制备方法 |
KR102272907B1 (ko) | 2020-11-05 | 2021-07-05 | 주식회사 아리바이오 | 치매 예방 및 치료용 조성물 |
KR102272910B1 (ko) | 2021-01-28 | 2021-07-06 | 주식회사 아리바이오 | 당뇨병을 동반한 치매 예방 및 치료용 조성물 |
KR102311224B1 (ko) | 2021-04-23 | 2021-10-13 | 주식회사 아리바이오 | Pde5 억제제와 글루코코르티코이드 수용체 길항제 병용투여를 통한 치매 예방 및 치료용 조성물 |
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2016
- 2016-01-26 EA EA201700356A patent/EA033423B1/ru unknown
- 2016-01-26 JP JP2017540574A patent/JP6628805B2/ja not_active Expired - Fee Related
- 2016-01-26 MX MX2017010019A patent/MX368391B/es active IP Right Grant
- 2016-01-26 EP EP16702810.9A patent/EP3253755B1/en active Active
- 2016-01-26 ES ES16702810T patent/ES2818806T3/es active Active
- 2016-01-26 TN TNP/2017/000342A patent/TN2017000342A1/en unknown
- 2016-01-26 DK DK16702810.9T patent/DK3253755T3/da active
- 2016-01-26 PE PE2017001310A patent/PE20171318A1/es not_active Application Discontinuation
- 2016-01-26 AU AU2016214102A patent/AU2016214102B2/en not_active Ceased
- 2016-01-26 CN CN201680008557.7A patent/CN107406445B/zh not_active Expired - Fee Related
- 2016-01-26 KR KR1020177024302A patent/KR102000382B1/ko active IP Right Grant
- 2016-01-26 BR BR112017015693A patent/BR112017015693A2/pt active Search and Examination
- 2016-01-26 WO PCT/IB2016/050384 patent/WO2016125048A1/en active Application Filing
- 2016-01-26 SG SG11201705780PA patent/SG11201705780PA/en unknown
- 2016-01-29 CA CA2919338A patent/CA2919338A1/en not_active Abandoned
- 2016-02-01 UY UY0001036546A patent/UY36546A/es not_active Application Discontinuation
- 2016-02-01 AR ARP160100286A patent/AR103582A1/es unknown
- 2016-02-01 TW TW105103193A patent/TWI616445B/zh not_active IP Right Cessation
- 2016-02-02 US US15/012,954 patent/US20160222007A1/en not_active Abandoned
- 2016-12-19 US US15/382,778 patent/US9765073B2/en active Active
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2017
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- 2017-07-28 PH PH12017501369A patent/PH12017501369A1/en unknown
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EP3253755A1 (en) | 2017-12-13 |
AU2016214102A1 (en) | 2017-07-27 |
KR102000382B1 (ko) | 2019-07-15 |
MX2017010019A (es) | 2017-10-24 |
TWI616445B (zh) | 2018-03-01 |
ECSP17050310A (es) | 2017-11-30 |
EP3253755B1 (en) | 2020-08-26 |
JP2018508494A (ja) | 2018-03-29 |
EA201700356A1 (ru) | 2018-01-31 |
JP6628805B2 (ja) | 2020-01-15 |
EA033423B1 (ru) | 2019-10-31 |
TN2017000342A1 (en) | 2019-01-16 |
PH12017501369A1 (en) | 2017-12-18 |
CA2919338A1 (en) | 2016-08-03 |
CN107406445B (zh) | 2019-12-24 |
US9765073B2 (en) | 2017-09-19 |
CN107406445A (zh) | 2017-11-28 |
US20170096428A1 (en) | 2017-04-06 |
KR20170113603A (ko) | 2017-10-12 |
MX368391B (es) | 2019-09-30 |
ES2818806T3 (es) | 2021-04-14 |
DK3253755T3 (da) | 2020-09-28 |
US20160222007A1 (en) | 2016-08-04 |
WO2016125048A1 (en) | 2016-08-11 |
TW201630913A (zh) | 2016-09-01 |
UY36546A (es) | 2016-08-31 |
AU2016214102B2 (en) | 2018-09-27 |
SG11201705780PA (en) | 2017-08-30 |
BR112017015693A2 (pt) | 2018-03-20 |
IL253635A0 (en) | 2017-09-28 |
AR103582A1 (es) | 2017-05-17 |
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