PE20190711A1 - N-(fenils ulfonil) benzamidas y compuestos relacionados como inhibidores de bcl-2 - Google Patents
N-(fenils ulfonil) benzamidas y compuestos relacionados como inhibidores de bcl-2Info
- Publication number
- PE20190711A1 PE20190711A1 PE2019000335A PE2019000335A PE20190711A1 PE 20190711 A1 PE20190711 A1 PE 20190711A1 PE 2019000335 A PE2019000335 A PE 2019000335A PE 2019000335 A PE2019000335 A PE 2019000335A PE 20190711 A1 PE20190711 A1 PE 20190711A1
- Authority
- PE
- Peru
- Prior art keywords
- bcl
- inhibitors
- dotted line
- ulfonil
- fenils
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 239000012664 BCL-2-inhibitor Substances 0.000 title 1
- 229940123711 Bcl2 inhibitor Drugs 0.000 title 1
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 108010090931 Proto-Oncogene Proteins c-bcl-2 Proteins 0.000 abstract 1
- 102000013535 Proto-Oncogene Proteins c-bcl-2 Human genes 0.000 abstract 1
- 150000003936 benzamides Chemical class 0.000 abstract 1
- 230000006806 disease prevention Effects 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000004404 heteroalkyl group Chemical group 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 102000004169 proteins and genes Human genes 0.000 abstract 1
- 108090000623 proteins and genes Proteins 0.000 abstract 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 abstract 1
Classifications
-
- 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
- A61K31/435—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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Hydrogenated Pyridines (AREA)
Abstract
Se refiere a compuestos de derivados de benzamida de formula I-A, donde A es (A-1, (A-2), entre otros; E es un atomo de carbono y la linea punteada es un enlace doble o E es un -C(H)- y la linea punteada es un enlace simple, o E es un atomo de nitrogeno y la linea punteada es un enlace simple; X1, X2 y X3 son -N= y -CR8; R1a y R1b junto al atomo de carbono al que estan unidos forman un cicloalquilo o un heterociclo opcionalmente sustituidos; R2 es -NO2, -SO2CH3, y -SO2CF3.; R2a y R8 son hidrogeno o halogeno; R3 es hidrogeno, -CN, entre otros; R5 es heterociclo, heteroalquilo, entre otros. Tambien se refiere a composiciones farmaceuticas. Dichos compuestos son inhibidores de la proteina Bcl-2 y son utiles en el tratamiento o prevencion de enfermedades mediadas por dicha proteina
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662371504P | 2016-08-05 | 2016-08-05 | |
| US201762454101P | 2017-02-03 | 2017-02-03 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20190711A1 true PE20190711A1 (es) | 2019-05-17 |
Family
ID=59677319
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2019000335A PE20190711A1 (es) | 2016-08-05 | 2017-08-04 | N-(fenils ulfonil) benzamidas y compuestos relacionados como inhibidores de bcl-2 |
Country Status (28)
| Country | Link |
|---|---|
| US (3) | US10829488B2 (es) |
| EP (3) | EP3494115B1 (es) |
| JP (2) | JP6651180B2 (es) |
| KR (2) | KR102376764B1 (es) |
| CN (2) | CN110483501B (es) |
| AU (2) | AU2017305508B2 (es) |
| BR (1) | BR112019001666A2 (es) |
| CA (1) | CA3031419C (es) |
| CY (1) | CY1123859T1 (es) |
| DK (1) | DK3494115T3 (es) |
| ES (1) | ES2849959T3 (es) |
| HR (1) | HRP20202073T1 (es) |
| HU (1) | HUE053414T2 (es) |
| IL (2) | IL264059B (es) |
| LT (1) | LT3494115T (es) |
| MX (2) | MX381588B (es) |
| MY (1) | MY199409A (es) |
| PE (1) | PE20190711A1 (es) |
| PH (1) | PH12019500231A1 (es) |
| PT (1) | PT3494115T (es) |
| RS (1) | RS61821B1 (es) |
| RU (2) | RU2722560C1 (es) |
| SA (1) | SA519401020B1 (es) |
| SG (2) | SG10201913643YA (es) |
| SI (1) | SI3494115T1 (es) |
| SM (1) | SMT202100025T1 (es) |
| WO (1) | WO2018027097A1 (es) |
| ZA (2) | ZA201900240B (es) |
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| CN110483501B (zh) * | 2016-08-05 | 2022-07-01 | 密歇根大学董事会 | 作为bcl-2抑制剂的n-(苯基磺酰基)苯甲酰胺及相关化合物 |
| US11053239B2 (en) | 2017-01-07 | 2021-07-06 | Fochon Pharmaceuticals, Ltd. | Compounds as BLC-2-selective apoptosis-inducing agents |
| JP7085566B2 (ja) | 2017-04-18 | 2022-06-16 | シャンハイ フォチョン ファーマシューティカル カンパニー リミテッド | アポトーシス誘発剤 |
| CN117683029A (zh) | 2018-04-29 | 2024-03-12 | 百济神州有限公司 | Bcl-2抑制剂 |
| EP3672595B1 (en) * | 2018-07-31 | 2021-07-21 | Ascentage Pharma (Suzhou) Co., Ltd. | Combination product of bcl-2 inhibitor and chemotherapeutic agent and use thereof in the prevention and/or treatment of diseases |
| CN110772521A (zh) | 2018-07-31 | 2020-02-11 | 苏州亚盛药业有限公司 | Bcl-2抑制剂或Bcl-2/Bcl-xL抑制剂与BTK抑制剂的组合产品及其用途 |
| US11554127B2 (en) * | 2018-07-31 | 2023-01-17 | Ascentage Pharma (Suzhou) Co., Ltd. | Synergistic antitumor effect of Bcl-2 inhibitor combined with rituximab and/or bendamustine or Bcl-2 inhibitor combined with CHOP |
| MX2020009757A (es) * | 2018-07-31 | 2020-10-08 | Ascentage Pharma Suzhou Co Ltd | Producto combinado de inhibidor de bcl-2 e inhibidor de mdm2 y uso de este en la prevencion y/o tratamiento de enfermedades. |
| AU2019385458A1 (en) * | 2018-11-23 | 2021-01-07 | Ascentage Pharma (Suzhou) Co., Ltd. | Pharmaceutical composition and use thereof |
| TWI770503B (zh) * | 2019-05-13 | 2022-07-11 | 大陸商蘇州亞盛藥業有限公司 | 用於預測bcl-2/bcl-xl抑制劑對癌症的功效的方法和組合物 |
| CN112168830B (zh) * | 2019-07-02 | 2022-01-25 | 苏州亚盛药业有限公司 | 一种含有mTOR抑制剂的药物组合及其应用 |
| JP2021535129A (ja) * | 2019-07-31 | 2021-12-16 | アセンテージ ファーマ（スーチョウ）カンパニー，リミティド | Ｂｃｌ−２／Ｂｃｌ−ｘＬ阻害剤及び化学療法剤の組み合わせ製品、並びに疾患の予防及び／又は治療におけるその使用 |
| US12287338B2 (en) | 2019-11-27 | 2025-04-29 | Ascentage Pharma (Suzhou) Co., Ltd. | Method and compositions for predicting anti-cancer efficacy of compounds targeting apoptosis pathway |
| CN112898295A (zh) * | 2019-12-03 | 2021-06-04 | 苏州亚盛药业有限公司 | 作为bcl-2抑制剂的n-(苯基磺酰基)苯甲酰胺及相关化合物 |
| CN112891353B (zh) * | 2019-12-04 | 2024-01-30 | 苏州亚盛药业有限公司 | 药物组合及其用途 |
| WO2021113497A1 (en) | 2019-12-06 | 2021-06-10 | Loxo Oncology, Inc. | Dosing of a bruton's tyrosine kinase inhibitor |
| TWI777438B (zh) * | 2020-03-06 | 2022-09-11 | 大陸商蘇州亞盛藥業有限公司 | N- (苯基磺醯基) 苯甲醯胺類化合物的結晶形式 |
| CN115244051B (zh) * | 2020-03-12 | 2024-10-18 | 南京明德新药研发有限公司 | 苯并五元环类化合物 |
| KR20230002419A (ko) | 2020-04-15 | 2023-01-05 | 베이진 엘티디 | Bcl-2 억제제 |
| WO2021227763A1 (en) * | 2020-05-14 | 2021-11-18 | Ascentage Pharma (Suzhou) Co., Ltd. | Hplc analysis method for n- (phenylsulfonyl) benzamide compound |
| CN113880834B (zh) * | 2020-07-01 | 2023-01-20 | 苏州亚盛药业有限公司 | N-(苯基磺酰基)苯甲酰胺类化合物及其中间体的合成方法 |
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| CN114057728A (zh) * | 2020-08-06 | 2022-02-18 | 北京诺诚健华医药科技有限公司 | 作为bcl-2抑制剂的杂环化合物 |
| US20230398110A1 (en) * | 2020-08-21 | 2023-12-14 | Ascentage Pharma (Suzhou) Co., Ltd. | Compositions and methods for treating non-alcoholic steatohepatitis |
| EP4199924A4 (en) * | 2020-08-21 | 2024-08-28 | Ascentage Pharma (Suzhou) Co., Ltd. | COMPOSITIONS AND METHODS FOR TREATING SYSTEMIC LUPUS ERYTHEMATOSUS |
| CN114533677A (zh) * | 2020-11-25 | 2022-05-27 | 苏州亚盛药业有限公司 | 固体分散体、制剂、其制备方法及其应用 |
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| CN114835704B (zh) * | 2021-02-01 | 2023-10-27 | 苏州亚盛药业有限公司 | 作为bcl-2抑制剂的磺酰基苯甲酰胺衍生物 |
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| CN110483501B (zh) | 2016-08-05 | 2022-07-01 | 密歇根大学董事会 | 作为bcl-2抑制剂的n-(苯基磺酰基)苯甲酰胺及相关化合物 |
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2017
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