PE20181289A1 - 3-azabiciclo[3.1.0]hexanos sustituidos como inhibidores de cetohexoquinasa - Google Patents
3-azabiciclo[3.1.0]hexanos sustituidos como inhibidores de cetohexoquinasaInfo
- Publication number
- PE20181289A1 PE20181289A1 PE2018001204A PE2018001204A PE20181289A1 PE 20181289 A1 PE20181289 A1 PE 20181289A1 PE 2018001204 A PE2018001204 A PE 2018001204A PE 2018001204 A PE2018001204 A PE 2018001204A PE 20181289 A1 PE20181289 A1 PE 20181289A1
- Authority
- PE
- Peru
- Prior art keywords
- inhibitors
- cetohexoquinase
- hexans
- azabicycle
- substituted
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- HGWUUOXXAIISDB-UHFFFAOYSA-N 3-azabicyclo[3.1.0]hexane Chemical compound C1NCC2CC21 HGWUUOXXAIISDB-UHFFFAOYSA-N 0.000 abstract 1
- 125000003341 7 membered heterocyclic group Chemical group 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- 102000004190 Enzymes Human genes 0.000 abstract 1
- RFSUNEUAIZKAJO-ARQDHWQXSA-N Fructose Chemical compound OC[C@H]1O[C@](O)(CO)[C@@H](O)[C@@H]1O RFSUNEUAIZKAJO-ARQDHWQXSA-N 0.000 abstract 1
- 229930091371 Fructose Natural products 0.000 abstract 1
- 239000005715 Fructose Substances 0.000 abstract 1
- 206010022489 Insulin Resistance Diseases 0.000 abstract 1
- 102100023418 Ketohexokinase Human genes 0.000 abstract 1
- 108010062852 Ketohexokinase Proteins 0.000 abstract 1
- 230000010014 adipocyte dysfunction Effects 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 abstract 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 208000017169 kidney disease Diseases 0.000 abstract 1
- 230000004060 metabolic process Effects 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 abstract 1
Classifications
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- 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
- C07D403/14—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 three or more hetero rings
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- 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
- C07D401/14—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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- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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- 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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- 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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- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
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- Health & Medical Sciences (AREA)
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- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
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- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
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- Engineering & Computer Science (AREA)
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- Diabetes (AREA)
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- Neurology (AREA)
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- Obesity (AREA)
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- Heart & Thoracic Surgery (AREA)
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- Physical Education & Sports Medicine (AREA)
- Psychiatry (AREA)
- Rheumatology (AREA)
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- Urology & Nephrology (AREA)
- Dermatology (AREA)
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- Pain & Pain Management (AREA)
- Child & Adolescent Psychology (AREA)
- Gynecology & Obstetrics (AREA)
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Abstract
Se refiere a un compuesto derivado de 3-azabiciclo[3.1.0]hexano de formula I, donde R1 es cicloalquilo C3-C7 o una porcion heterociclica de 4 a 7 miembros, donde la porcion heterociclica contiene 1 a 2 atomos de N, O y S; R2 es -(L)m-CON(RN2), -(L)m-SO2RS, entre otros; R4 es ciclopropilo, ciclobutilo, entre otros; Y es N o C-CN; Z es N o CH; X es CR3 donde R3 es H, -CN, halogeno, entre otros.; m y n son 0 o 1; RN y RS son H o -C1-3alquilo, L es CH2, CHF, entre otros. Tambien se refiere a una composicion farmaceutica. Dichos compuestos son inhibidores de cetohexoquinasa, principal enzima en el metabolismo de fructosa, y son utiles para el tratamiento de enfermedades tales como la resistencia a la insulina, enfermedad renal, disfuncion del adipocito, entre otras
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562272598P | 2015-12-29 | 2015-12-29 | |
| US201662423549P | 2016-11-17 | 2016-11-17 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20181289A1 true PE20181289A1 (es) | 2018-08-07 |
Family
ID=57755415
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2018001204A PE20181289A1 (es) | 2015-12-29 | 2016-12-16 | 3-azabiciclo[3.1.0]hexanos sustituidos como inhibidores de cetohexoquinasa |
Country Status (38)
| Country | Link |
|---|---|
| US (6) | US9809579B2 (es) |
| EP (1) | EP3397631B1 (es) |
| JP (1) | JP6503515B2 (es) |
| KR (1) | KR102073048B1 (es) |
| CN (1) | CN108473469B (es) |
| AU (1) | AU2016380920B2 (es) |
| CA (1) | CA2952466C (es) |
| CL (1) | CL2018001667A1 (es) |
| CO (1) | CO2018006714A2 (es) |
| CU (1) | CU24540B1 (es) |
| CY (1) | CY1124389T1 (es) |
| DK (1) | DK3397631T3 (es) |
| EC (1) | ECSP18048517A (es) |
| ES (1) | ES2871251T3 (es) |
| GE (1) | GEP20207147B (es) |
| HR (1) | HRP20210769T1 (es) |
| HU (1) | HUE054380T2 (es) |
| IL (1) | IL260330B (es) |
| LT (1) | LT3397631T (es) |
| MA (1) | MA43518B1 (es) |
| MD (1) | MD3397631T2 (es) |
| MX (1) | MX376072B (es) |
| NI (1) | NI201800072A (es) |
| PE (1) | PE20181289A1 (es) |
| PH (1) | PH12018501375A1 (es) |
| PL (1) | PL3397631T3 (es) |
| PT (1) | PT3397631T (es) |
| RS (1) | RS61896B1 (es) |
| RU (1) | RU2696269C1 (es) |
| SG (1) | SG11201804363UA (es) |
| SI (1) | SI3397631T1 (es) |
| SV (1) | SV2018005709A (es) |
| TN (1) | TN2018000198A1 (es) |
| TW (1) | TWI653232B (es) |
| UA (1) | UA121271C2 (es) |
| UY (1) | UY37051A (es) |
| WO (1) | WO2017115205A1 (es) |
| ZA (1) | ZA201803449B (es) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9809579B2 (en) * | 2015-12-29 | 2017-11-07 | Pfizer Inc. | Substituted 3-azabicyclo[3.1.0]hexanes as ketohexokinase inhibitors |
| EP3872080B1 (en) | 2016-09-02 | 2023-08-16 | Cyclerion Therapeutics, Inc. | Fused bicyclic sgc stimulators |
| US10558874B1 (en) | 2017-01-19 | 2020-02-11 | State Farm Mutual Automobile Insurance Company | Apparatuses, systems and methods for generation and transmission of vehicle operation mode data |
| CN109316601B (zh) * | 2017-07-31 | 2021-11-09 | 武汉朗来科技发展有限公司 | 药物组合物及其用途 |
| TWI707683B (zh) | 2018-06-13 | 2020-10-21 | 美商輝瑞股份有限公司 | Ｇｌｐ－１受體促效劑及其用途 |
| TWI718644B (zh) * | 2018-08-31 | 2021-02-11 | 美商輝瑞股份有限公司 | 用於治療ｎａｓｈ／ｎａｆｌｄ和相關疾病之組合 |
| TWI714231B (zh) * | 2018-09-04 | 2020-12-21 | 美商美國禮來大藥廠 | 2,6-二胺基吡啶化合物 |
| KR102558308B1 (ko) * | 2018-09-27 | 2023-07-24 | 주식회사 엘지화학 | 3-아자바이사이클로[3,1,1]헵탄 유도체 및 이를 포함하는 약제학적 조성물 |
| CN113412260B (zh) * | 2019-01-29 | 2022-08-02 | 山东轩竹医药科技有限公司 | 己酮糖激酶抑制剂及其用途 |
| US20220184172A1 (en) * | 2019-04-19 | 2022-06-16 | The Regents Of The University Of California | Ampk/caspase-6 axis controls liver damage in nonalcoholic steatohepatitis |
| EP3972596B1 (en) * | 2019-05-20 | 2025-07-16 | Pfizer Inc. | Combinations comprising benzodioxol as glp-1r agonists for use in the treatment of nash/nafld and related diseases |
| CN111978296A (zh) * | 2019-05-22 | 2020-11-24 | 山东轩竹医药科技有限公司 | 己酮糖激酶抑制剂及其用途 |
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