JP6771464B2 - Cbpおよび/またはep300インヒビターとしての、4,5,6,7−テトラヒドロ−1h−ピラゾロ[4,3−c]ピリジン−3−アミン化合物 - Google Patents
Cbpおよび/またはep300インヒビターとしての、4,5,6,7−テトラヒドロ−1h−ピラゾロ[4,3−c]ピリジン−3−アミン化合物 Download PDFInfo
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- JP6771464B2 JP6771464B2 JP2017528520A JP2017528520A JP6771464B2 JP 6771464 B2 JP6771464 B2 JP 6771464B2 JP 2017528520 A JP2017528520 A JP 2017528520A JP 2017528520 A JP2017528520 A JP 2017528520A JP 6771464 B2 JP6771464 B2 JP 6771464B2
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- alkyl
- optionally substituted
- independently selected
- oxo
- halo
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- 0 C*=C(C)C(C1)=C(*)C=C*1C(C)=O Chemical compound C*=C(C)C(C1)=C(*)C=C*1C(C)=O 0.000 description 11
- XREKNSPXHOTFAJ-IBGZPJMESA-N CC(N(CC1)Cc2c1[n]([C@@H]1COCC1)nc2N(CCC1)c2c1cc(-c1c[n](C)nc1)c(OC(F)(F)F)c2)=O Chemical compound CC(N(CC1)Cc2c1[n]([C@@H]1COCC1)nc2N(CCC1)c2c1cc(-c1c[n](C)nc1)c(OC(F)(F)F)c2)=O XREKNSPXHOTFAJ-IBGZPJMESA-N 0.000 description 1
- WDKUXUZYKCXAHC-UHFFFAOYSA-N CC1(C)COCC1 Chemical compound CC1(C)COCC1 WDKUXUZYKCXAHC-UHFFFAOYSA-N 0.000 description 1
- XQIUBXUYYNBTAU-UHFFFAOYSA-N CNC(N(CC1)Cc2c1[n](C1CCOCC1)nc2N(CCCc1c2)c1cnc2-c1c[n](C)nc1)=O Chemical compound CNC(N(CC1)Cc2c1[n](C1CCOCC1)nc2N(CCCc1c2)c1cnc2-c1c[n](C)nc1)=O XQIUBXUYYNBTAU-UHFFFAOYSA-N 0.000 description 1
- JCTPCIJTMOZBIZ-UHFFFAOYSA-N C[n]1ncc(-c(cc2CCC3)ncc2N3c2n[n](C3CCOCC3)c3c2CNCC3)c1 Chemical compound C[n]1ncc(-c(cc2CCC3)ncc2N3c2n[n](C3CCOCC3)c3c2CNCC3)c1 JCTPCIJTMOZBIZ-UHFFFAOYSA-N 0.000 description 1
- LCAVOMDTLTZXIN-BIXGBWIQSA-N C[n]1ncc(C(C=C2)=CC(CCC3)C2N3c2n[n]([C@@H]3COCC3)c(CC3)c2CN3C(N)=O)c1 Chemical compound C[n]1ncc(C(C=C2)=CC(CCC3)C2N3c2n[n]([C@@H]3COCC3)c(CC3)c2CN3C(N)=O)c1 LCAVOMDTLTZXIN-BIXGBWIQSA-N 0.000 description 1
- WJXOZTLEJLFKOV-UHFFFAOYSA-N Cc(c(-c1c[n](C)nc1)c1)ccc1N Chemical compound Cc(c(-c1c[n](C)nc1)c1)ccc1N WJXOZTLEJLFKOV-UHFFFAOYSA-N 0.000 description 1
- IXXDRIBSFYQWRM-UHFFFAOYSA-N Cc(c(-c1c[n](C)nc1)c1)ccc1[N+]([O-])=O Chemical compound Cc(c(-c1c[n](C)nc1)c1)ccc1[N+]([O-])=O IXXDRIBSFYQWRM-UHFFFAOYSA-N 0.000 description 1
- ZOLQDQKZTCTWMX-UHFFFAOYSA-N Cc1cccc(NC2=NCCCCC3=C2CNCC3)c1 Chemical compound Cc1cccc(NC2=NCCCCC3=C2CNCC3)c1 ZOLQDQKZTCTWMX-UHFFFAOYSA-N 0.000 description 1
Classifications
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- A—HUMAN NECESSITIES
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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
- A61K31/4353—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
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—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
- A61K31/4375—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 six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
-
- A—HUMAN NECESSITIES
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
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- A—HUMAN NECESSITIES
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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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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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
- A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
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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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- 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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- 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
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/5415—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 sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
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- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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- Health & Medical Sciences (AREA)
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- Public Health (AREA)
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2014/092380 | 2014-11-27 | ||
| CN2014092380 | 2014-11-27 | ||
| CNPCT/CN2015/092965 | 2015-10-27 | ||
| CN2015092965 | 2015-10-27 | ||
| PCT/US2015/062794 WO2016086200A1 (en) | 2014-11-27 | 2015-11-25 | 4,5,6,7-tetrahydro-1 h-pyrazolo[4,3-c]pyridin-3-amine compounds as cbp and/or ep300 inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017537100A JP2017537100A (ja) | 2017-12-14 |
| JP2017537100A5 JP2017537100A5 (enExample) | 2019-01-10 |
| JP6771464B2 true JP6771464B2 (ja) | 2020-10-21 |
Family
ID=55024234
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017528520A Active JP6771464B2 (ja) | 2014-11-27 | 2015-11-25 | Cbpおよび/またはep300インヒビターとしての、4,5,6,7−テトラヒドロ−1h−ピラゾロ[4,3−c]ピリジン−3−アミン化合物 |
Country Status (5)
| Country | Link |
|---|---|
| US (2) | US9763922B2 (enExample) |
| EP (2) | EP3632915A1 (enExample) |
| JP (1) | JP6771464B2 (enExample) |
| CN (1) | CN107531690B (enExample) |
| WO (1) | WO2016086200A1 (enExample) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2019516759A (ja) * | 2016-05-24 | 2019-06-20 | ジェネンテック, インコーポレイテッド | がんの処置のためのピラゾロピリジン誘導体 |
| JP2024517496A (ja) * | 2021-05-14 | 2024-04-22 | 武漢朗来科技発展有限公司 | Rock阻害剤の酸付加塩及び塩の結晶形、組成物並びに薬物用途 |
Families Citing this family (49)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016077375A1 (en) | 2014-11-10 | 2016-05-19 | Genentech, Inc. | Bromodomain inhibitors and uses thereof |
| MA40943A (fr) | 2014-11-10 | 2017-09-19 | Constellation Pharmaceuticals Inc | Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines |
| MA40940A (fr) * | 2014-11-10 | 2017-09-19 | Constellation Pharmaceuticals Inc | Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines |
| SG11201704089UA (en) * | 2014-12-05 | 2017-06-29 | H Lee Moffitt Cancer Ct & Res | Bromodomain inhibitor as adjuvant in cancer immunotherapy |
| CN107531692B (zh) | 2015-01-29 | 2020-12-25 | 基因泰克公司 | 治疗化合物及其用途 |
| AR104259A1 (es) | 2015-04-15 | 2017-07-05 | Celgene Quanticel Res Inc | Inhibidores de bromodominio |
| JP7160688B2 (ja) * | 2016-05-24 | 2022-10-25 | ジェネンテック, インコーポレイテッド | Cbp/ep300の複素環式インヒビターおよびがんの処置におけるそれらの使用 |
| CN109715790A (zh) | 2016-07-25 | 2019-05-03 | 埃皮兹姆公司 | Crebbp相关的癌症疗法 |
| GB201617630D0 (en) * | 2016-10-18 | 2016-11-30 | Cellcentric Ltd | Pharmaceutical compounds |
| GB201617627D0 (en) * | 2016-10-18 | 2016-11-30 | Cellcentric Ltd | Pharmaceutical compounds |
| MX393780B (es) | 2017-01-17 | 2025-03-24 | Heparegenix Gmbh | Inhibidores de proteina cinasa para promover la regeneracion hepatica o reducir o prevenir la muerte de hepatocitos |
| JP7134173B2 (ja) * | 2017-06-21 | 2022-09-09 | 第一三共株式会社 | Ep300/crebbp阻害剤 |
| TWI846350B (zh) * | 2017-09-15 | 2024-06-21 | 美商佛瑪治療公司 | 作為CBP/p300抑制劑之四氫-咪唑並喹啉化合物 |
| CN111527087A (zh) | 2017-11-02 | 2020-08-11 | 艾库里斯有限及两合公司 | 具有抗乙型肝炎病毒(hbv)活性的新的高活性的吡唑并-哌啶取代的吲哚-2-甲酰胺 |
| BR112020019824A2 (pt) * | 2018-03-29 | 2021-01-05 | Board Of Regents, The University Of Texas System | Composto de fórmula estrutural i ou um sal do mesmo, composição farmacêutica, método de inibição de cbp, método de inibição de p300, método de tratamento de uma doença mediada por cbp, método de tratamento de uma doença mediada por p300 e método para alcançar um efeito em um paciente |
| WO2019195846A1 (en) | 2018-04-06 | 2019-10-10 | Board Of Regents, The University Of Texas System | Imidazopiperazinone inhibitors of transcription activating proteins |
| GB201806320D0 (en) * | 2018-04-18 | 2018-05-30 | Cellcentric Ltd | Process |
| GB201809295D0 (en) | 2018-06-06 | 2018-07-25 | Institute Of Cancer Res Royal Cancer Hospital | Lox inhibitors |
| EP3587418B1 (en) * | 2018-06-29 | 2021-09-01 | Forma Therapeutics, Inc. | Inhibitors of creb binding protein (cbp) |
| MX2023013508A (es) * | 2018-06-29 | 2023-12-13 | Forma Therapeutics Inc | Inhibicion de la proteina de union a creb (cbp). |
| CN109187832B (zh) * | 2018-09-30 | 2021-07-30 | 华润三九医药股份有限公司 | Lc-ms/ms测定去氧肾上腺素浓度的方法及样品的前处理方法 |
| GB201818750D0 (en) | 2018-11-16 | 2019-01-02 | Institute Of Cancer Res Royal Cancer Hospital | Lox inhibitors |
| CN111320621B (zh) * | 2018-12-14 | 2022-10-04 | 中国科学院广州生物医药与健康研究院 | 一种吲嗪类化合物及其制备方法和应用 |
| TWI850342B (zh) * | 2019-02-27 | 2024-08-01 | 美商星座製藥公司 | P300/cbp hat抑制劑及其使用方法 |
| CN119330963A (zh) * | 2019-02-27 | 2025-01-21 | 上海睿跃生物科技有限公司 | 环amp反应元件结合蛋白(cbp)和/或300kda腺病毒e1a结合蛋白(p300)降解化合物和使用方法 |
| EP3938365A4 (en) * | 2019-03-15 | 2023-01-25 | Forma Therapeutics, Inc. | COMPOSITIONS AND METHODS OF TREATMENT OF ANDROGEN RECEPTOR POSITIVE FORMS OF CANCER |
| US12351577B2 (en) | 2019-03-15 | 2025-07-08 | Forma Therapeutics, Inc. | Inhibiting cyclic AMP-responsive element-binding protein (CREB) |
| JP2022535743A (ja) * | 2019-05-29 | 2022-08-10 | アイエフエム デュー インコーポレイテッド | Sting活性に関連する状態を治療するための化合物および組成物 |
| CN110170052B (zh) * | 2019-06-21 | 2020-07-10 | 复旦大学 | Cbp-p300抑制剂在肠道损伤疾病中的应用 |
| TW202120095A (zh) * | 2019-08-05 | 2021-06-01 | 美商美國禮來大藥廠 | 7,8-二氫-4H-吡唑并[4,3-c]氮呯-6-酮化合物 |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2019516759A (ja) * | 2016-05-24 | 2019-06-20 | ジェネンテック, インコーポレイテッド | がんの処置のためのピラゾロピリジン誘導体 |
| JP7014736B2 (ja) | 2016-05-24 | 2022-02-01 | ジェネンテック, インコーポレイテッド | がんの処置のためのピラゾロピリジン誘導体 |
| JP2024517496A (ja) * | 2021-05-14 | 2024-04-22 | 武漢朗来科技発展有限公司 | Rock阻害剤の酸付加塩及び塩の結晶形、組成物並びに薬物用途 |
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| EP3224258A1 (en) | 2017-10-04 |
| CN107531690A (zh) | 2018-01-02 |
| US20160158207A1 (en) | 2016-06-09 |
| WO2016086200A1 (en) | 2016-06-02 |
| CN107531690B (zh) | 2020-11-06 |
| US20170333406A1 (en) | 2017-11-23 |
| WO2016086200A9 (en) | 2016-06-23 |
| HK1248695A1 (zh) | 2018-10-19 |
| US9763922B2 (en) | 2017-09-19 |
| JP2017537100A (ja) | 2017-12-14 |
| EP3224258B1 (en) | 2019-08-14 |
| EP3632915A1 (en) | 2020-04-08 |
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