PE20160880A1 - Compuestos de triazolona y usos de los mismos - Google Patents
Compuestos de triazolona y usos de los mismosInfo
- Publication number
- PE20160880A1 PE20160880A1 PE2016000323A PE2016000323A PE20160880A1 PE 20160880 A1 PE20160880 A1 PE 20160880A1 PE 2016000323 A PE2016000323 A PE 2016000323A PE 2016000323 A PE2016000323 A PE 2016000323A PE 20160880 A1 PE20160880 A1 PE 20160880A1
- Authority
- PE
- Peru
- Prior art keywords
- compounds
- alkyl
- ppar
- heteroaryl
- cycloalkyl
- Prior art date
Links
- FFSJPOPLSWBGQY-UHFFFAOYSA-N triazol-4-one Chemical class O=C1C=NN=N1 FFSJPOPLSWBGQY-UHFFFAOYSA-N 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 125000001072 heteroaryl group Chemical group 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 abstract 1
- 208000031886 HIV Infections Diseases 0.000 abstract 1
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 abstract 1
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical compound O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 abstract 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 abstract 1
- 102100038831 Peroxisome proliferator-activated receptor alpha Human genes 0.000 abstract 1
- 102100038824 Peroxisome proliferator-activated receptor delta Human genes 0.000 abstract 1
- 208000036142 Viral infection Diseases 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 210000000481 breast Anatomy 0.000 abstract 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 abstract 1
- 210000001072 colon Anatomy 0.000 abstract 1
- 230000009977 dual effect Effects 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 208000015181 infectious disease Diseases 0.000 abstract 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 abstract 1
- 201000001441 melanoma Diseases 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 201000002528 pancreatic cancer Diseases 0.000 abstract 1
- 208000008443 pancreatic carcinoma Diseases 0.000 abstract 1
- 108091008725 peroxisome proliferator-activated receptors alpha Proteins 0.000 abstract 1
- 108091008765 peroxisome proliferator-activated receptors β/δ Proteins 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 210000002307 prostate Anatomy 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
- 230000009385 viral infection Effects 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
- C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D249/12—Oxygen or sulfur atoms
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4196—1,2,4-Triazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- 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
-
- 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
- A61P31/14—Antivirals for RNA 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
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D401/04—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
-
- 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
- C07D401/10—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 carbon chain containing aromatic rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Virology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Communicable Diseases (AREA)
- Hematology (AREA)
- Molecular Biology (AREA)
- Epidemiology (AREA)
- AIDS & HIV (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Gastroenterology & Hepatology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Se refiere a compuestos de formulas Ia y Ib, y sales farmaceuticamente aceptables de los mismos, en los cuales A1 es fenilo o piridilo; A2 es fenilo, un anillo heteroaromatico de 6 miembros conteniendo 1, 2 o 3 atomos de N, o un anillo heteroaromatico de 5 miembros conteniendo 1, 2, 3 o 4 heteroatomos independiente seleccionados de O, S y N, entre otros; X es (CH2)m o (CH2)mNH(CH2)n, en donde m y n son independientemente 0, 1, 2, 3 o 4, y m + n es 2, 3 o 4; R1 y R2 son independientemente H, halogeno, CN, CF3, alquilo C16 o cicloalquilo C36, entre otros; R5 es alquilo C16, arilo, heteroarilo, cicloalquilo C36 o alquenilo C26, entre otros; y R6 es arilo o heteroarilo, cada uno de ellos opcionalmente sustituido con 1 o 2 sustituyentes independientemente seleccionados entre halogeno, NO2, CF3, OCF3, alquilo C16 o CN, entre otros. Tambien se refiere a composiciones farmaceuticas que comprenden dichos compuestos de formula Ia o Ib, o sales de los mismos. Los compuestos de la invencion son antagonistas duales de PPAR-alfa y PPAR-delta, por lo cual son utiles en el tratamiento de canceres de prostata, mama, colon, pancreatico, leucemia linfocitica cronica humana, melanoma y otros. Asimismo, tambien son utiles en el tratamiento de infecciones virales, tales como infecciones por HCV e infecciones por VIH.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361874956P | 2013-09-06 | 2013-09-06 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20160880A1 true PE20160880A1 (es) | 2016-09-22 |
Family
ID=52628929
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2016000323A PE20160880A1 (es) | 2013-09-06 | 2014-09-04 | Compuestos de triazolona y usos de los mismos |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US9776976B2 (es) |
| EP (1) | EP3041826A4 (es) |
| JP (1) | JP2016529311A (es) |
| KR (1) | KR20160048988A (es) |
| CN (1) | CN105579440A (es) |
| AU (1) | AU2014315151A1 (es) |
| CA (1) | CA2921420A1 (es) |
| EA (1) | EA201690230A1 (es) |
| IL (1) | IL244383A0 (es) |
| MX (1) | MX2016002795A (es) |
| PE (1) | PE20160880A1 (es) |
| SG (1) | SG11201601066VA (es) |
| WO (1) | WO2015035059A1 (es) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9676754B2 (en) | 2012-12-20 | 2017-06-13 | Inception 2, Inc. | Triazolone compounds and uses thereof |
| US20180194769A1 (en) | 2015-07-06 | 2018-07-12 | Rodin Therapeutics, Inc. | Hetero-halo inhibitors of histone deacetylase |
| EP3319968A1 (en) | 2015-07-06 | 2018-05-16 | Rodin Therapeutics, Inc. | Heterobicyclic n-aminophenyl-amides as inhibitors of histone deacetylase |
| JP2019522671A (ja) | 2016-07-12 | 2019-08-15 | バイエル・クロップサイエンス・アクチェンゲゼルシャフト | 殺虫剤としての二環式化合物 |
| JP6756925B2 (ja) | 2017-01-11 | 2020-09-16 | ロダン・セラピューティクス,インコーポレーテッド | ヒストンデアセチラーゼの二環式阻害剤 |
| SMT202200232T1 (it) | 2017-08-07 | 2022-07-21 | Alkermes Inc | Inibitori biciclici di istone deacetilasi |
| CN112168820B (zh) * | 2019-07-05 | 2023-09-29 | 中国科学院生物物理研究所 | SRCAP ATPase抑制剂在结直肠癌治疗中的应用 |
| GB201910037D0 (en) | 2019-07-12 | 2019-08-28 | Syngenta Crop Protection Ag | Microbiocidal compounds |
| CN114853686B (zh) * | 2021-08-23 | 2023-06-20 | 中国药科大学 | 三氮唑酮类化合物及其医药用途 |
| CN115894379B (zh) * | 2022-01-20 | 2025-06-27 | 哈尔滨三联药业股份有限公司 | 海因类化合物及其医药用途 |
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-
2014
- 2014-09-04 EA EA201690230A patent/EA201690230A1/ru unknown
- 2014-09-04 US US14/916,860 patent/US9776976B2/en not_active Expired - Fee Related
- 2014-09-04 CN CN201480048882.7A patent/CN105579440A/zh active Pending
- 2014-09-04 PE PE2016000323A patent/PE20160880A1/es not_active Application Discontinuation
- 2014-09-04 EP EP14842357.7A patent/EP3041826A4/en not_active Withdrawn
- 2014-09-04 AU AU2014315151A patent/AU2014315151A1/en not_active Abandoned
- 2014-09-04 MX MX2016002795A patent/MX2016002795A/es unknown
- 2014-09-04 SG SG11201601066VA patent/SG11201601066VA/en unknown
- 2014-09-04 JP JP2016540386A patent/JP2016529311A/ja active Pending
- 2014-09-04 WO PCT/US2014/054108 patent/WO2015035059A1/en not_active Ceased
- 2014-09-04 CA CA2921420A patent/CA2921420A1/en not_active Abandoned
- 2014-09-04 KR KR1020167008627A patent/KR20160048988A/ko not_active Withdrawn
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2016
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| WO2015035059A1 (en) | 2015-03-12 |
| EP3041826A1 (en) | 2016-07-13 |
| AU2014315151A1 (en) | 2016-03-03 |
| US9776976B2 (en) | 2017-10-03 |
| SG11201601066VA (en) | 2016-03-30 |
| EP3041826A4 (en) | 2017-02-15 |
| EA201690230A1 (ru) | 2016-07-29 |
| KR20160048988A (ko) | 2016-05-04 |
| US20160194292A1 (en) | 2016-07-07 |
| MX2016002795A (es) | 2016-05-26 |
| IL244383A0 (en) | 2016-04-21 |
| CA2921420A1 (en) | 2015-03-12 |
| JP2016529311A (ja) | 2016-09-23 |
| CN105579440A (zh) | 2016-05-11 |
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