CA2960280A1 - Substituted piperidine compounds - Google Patents
Substituted piperidine compounds Download PDFInfo
- Publication number
- CA2960280A1 CA2960280A1 CA2960280A CA2960280A CA2960280A1 CA 2960280 A1 CA2960280 A1 CA 2960280A1 CA 2960280 A CA2960280 A CA 2960280A CA 2960280 A CA2960280 A CA 2960280A CA 2960280 A1 CA2960280 A1 CA 2960280A1
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- Prior art keywords
- cancer
- carboxamide
- cell
- tumor
- alkyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Abandoned
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- 150000003053 piperidines Chemical class 0.000 title claims abstract description 13
- 150000001875 compounds Chemical class 0.000 claims abstract description 306
- 150000003839 salts Chemical class 0.000 claims abstract description 169
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- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 44
- 108090000623 proteins and genes Proteins 0.000 claims abstract description 40
- 102000004169 proteins and genes Human genes 0.000 claims abstract description 38
- -1 amino-substituted piperidine Chemical class 0.000 claims description 499
- 125000000217 alkyl group Chemical group 0.000 claims description 418
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 195
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 108
- 125000003282 alkyl amino group Chemical group 0.000 claims description 87
- 229910052739 hydrogen Inorganic materials 0.000 claims description 83
- 239000001257 hydrogen Substances 0.000 claims description 79
- 125000004663 dialkyl amino group Chemical group 0.000 claims description 69
- NQRYJNQNLNOLGT-UHFFFAOYSA-N tetrahydropyridine hydrochloride Natural products C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims description 69
- 125000005843 halogen group Chemical group 0.000 claims description 64
- 125000001072 heteroaryl group Chemical group 0.000 claims description 60
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 55
- 150000002431 hydrogen Chemical class 0.000 claims description 55
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
- C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
-
- 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
- A61K31/42—Oxazoles
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4453—Non condensed piperidines, e.g. piperocaine only substituted in position 1, e.g. propipocaine, diperodon
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- C07D487/08—Bridged systems
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462048771P | 2014-09-10 | 2014-09-10 | |
| US62/048,771 | 2014-09-10 | ||
| US201462078845P | 2014-11-12 | 2014-11-12 | |
| US62/078,845 | 2014-11-12 | ||
| US201562146790P | 2015-04-13 | 2015-04-13 | |
| US62/146,790 | 2015-04-13 | ||
| PCT/US2015/049235 WO2016040515A1 (en) | 2014-09-10 | 2015-09-09 | Substituted piperidine compounds |
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| AU2015315180A1 (en) * | 2014-09-10 | 2017-03-16 | Epizyme, Inc. | Isoxazole carboxamides as irreversible SMYD inhibitors |
| CA2960275A1 (en) | 2014-09-10 | 2016-03-17 | Epizyme, Inc. | Smyd inhibitors |
| JP2017526706A (ja) | 2014-09-10 | 2017-09-14 | エピザイム，インコーポレイティド | イソオキサゾールカルボキサミド化合物 |
| EP3190891B1 (en) | 2014-09-10 | 2020-01-15 | Epizyme, Inc. | Isoxazolecarboxamide substituted by a cyclohexylamine as smyd protein inhibitors |
| WO2016136963A1 (ja) * | 2015-02-27 | 2016-09-01 | 彰彦 石川 | カケロマイシンおよびその誘導体の製造方法 |
| HUE062019T2 (hu) * | 2016-07-28 | 2023-09-28 | Idorsia Pharmaceuticals Ltd | Piperidin CXCR7 receptor modulátorok |
| WO2018151678A1 (en) * | 2017-02-15 | 2018-08-23 | Agency For Science, Technology And Research | Compounds for treatment of cancer and epigenetics |
| RS65594B1 (sr) | 2018-01-26 | 2024-06-28 | Idorsia Pharmaceuticals Ltd | Kristalni oblici antagonista cxcr7 receptora (1-pirimidin-2-il-ciklopropil)-amida (3s,4s)-1-ciklopropilmetil-4-{[5-(2,4-difluoro-fenil)-izoksazol-3-karbonil]-amino}-piperidin-3-karboksilne kiseline |
| WO2020089026A1 (en) | 2018-10-29 | 2020-05-07 | Boehringer Ingelheim International Gmbh | Pyridinyl sulfonamide derivatives, pharmaceutical compositions and uses thereof |
| JP7425793B2 (ja) | 2018-10-29 | 2024-01-31 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ピリジニルスルホンアミド誘導体、医薬組成物およびそれらの使用 |
| JP7678756B2 (ja) | 2019-09-30 | 2025-05-16 | 日本ケミファ株式会社 | アゼパン誘導体 |
| CN114702552B (zh) * | 2022-03-11 | 2024-05-31 | 苏州思萃免疫技术研究所有限公司 | mTORC2抑制剂 |
| WO2024067708A1 (zh) * | 2022-09-30 | 2024-04-04 | 苏州阿尔脉生物科技有限公司 | 草酸胺类衍生物、包含其的药物组合物及其医药用途 |
| WO2025133989A1 (en) * | 2023-12-20 | 2025-06-26 | Alt-Bio Pte. Ltd. | Smyd modulators and uses thereof |
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| SE0403106D0 (sv) * | 2004-12-20 | 2004-12-20 | Astrazeneca Ab | Chemical compounds |
| WO2008137834A2 (en) * | 2007-05-04 | 2008-11-13 | Osi Pharmaceuticals, Inc. | Crystal structure of smyd3 protein |
| PE20091093A1 (es) * | 2007-12-03 | 2009-08-25 | Takeda Pharmaceutical | Compuesto heterociclico que contiene nitrogeno y su uso |
| TWI535712B (zh) * | 2010-08-06 | 2016-06-01 | 阿斯特捷利康公司 | 化合物 |
| JP5927201B2 (ja) * | 2010-12-16 | 2016-06-01 | カルチャン リミテッド | Ａｓｋ１阻害ピロロピリミジン誘導体 |
| AU2015315180A1 (en) * | 2014-09-10 | 2017-03-16 | Epizyme, Inc. | Isoxazole carboxamides as irreversible SMYD inhibitors |
| EP3190891B1 (en) | 2014-09-10 | 2020-01-15 | Epizyme, Inc. | Isoxazolecarboxamide substituted by a cyclohexylamine as smyd protein inhibitors |
| CA2960273A1 (en) | 2014-09-10 | 2016-03-17 | Epizyme, Inc. | Substituted pyrrolidine compounds |
| CA2960275A1 (en) | 2014-09-10 | 2016-03-17 | Epizyme, Inc. | Smyd inhibitors |
| WO2016040508A1 (en) | 2014-09-10 | 2016-03-17 | Epizyme, Inc. | Substituted pyrrolidine carboxamide compounds |
| JP2017526706A (ja) * | 2014-09-10 | 2017-09-14 | エピザイム，インコーポレイティド | イソオキサゾールカルボキサミド化合物 |
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- 2015-09-09 EA EA201790327A patent/EA201790327A1/ru unknown
- 2015-09-09 JP JP2017513207A patent/JP2017528464A/ja active Pending
- 2015-09-09 BR BR112017004589A patent/BR112017004589A2/pt not_active Application Discontinuation
- 2015-09-09 CN CN201580060918.8A patent/CN107072207A/zh active Pending
- 2015-09-09 MX MX2017002986A patent/MX2017002986A/es unknown
- 2015-09-09 WO PCT/US2015/049235 patent/WO2016040515A1/en not_active Ceased
- 2015-09-09 KR KR1020177009316A patent/KR20170047397A/ko not_active Withdrawn
- 2015-09-09 US US15/510,588 patent/US10577363B2/en active Active
- 2015-09-09 EP EP15840497.0A patent/EP3193605A4/en not_active Withdrawn
- 2015-09-09 SG SG11201701597RA patent/SG11201701597RA/en unknown
- 2015-09-09 SG SG10201901189SA patent/SG10201901189SA/en unknown
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2017
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| US20170362217A1 (en) | 2017-12-21 |
| IL250888A0 (en) | 2017-04-30 |
| EA201790327A1 (ru) | 2017-10-31 |
| AU2015315182A1 (en) | 2017-03-16 |
| SG11201701597RA (en) | 2017-03-30 |
| JP2017528464A (ja) | 2017-09-28 |
| MX2017002986A (es) | 2017-10-24 |
| EP3193605A1 (en) | 2017-07-26 |
| US10577363B2 (en) | 2020-03-03 |
| BR112017004589A2 (pt) | 2018-01-23 |
| KR20170047397A (ko) | 2017-05-04 |
| WO2016040515A1 (en) | 2016-03-17 |
| EP3193605A4 (en) | 2018-04-18 |
| SG10201901189SA (en) | 2019-03-28 |
| CN107072207A (zh) | 2017-08-18 |
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