ES2639757T3 - Síntesis de 2-(1H-indazol-6-il)espiro[ciclopropan-1,3'-indolin]-2'-onas quirales - Google Patents
Síntesis de 2-(1H-indazol-6-il)espiro[ciclopropan-1,3'-indolin]-2'-onas quirales Download PDFInfo
- Publication number
- ES2639757T3 ES2639757T3 ES11764989T ES11764989T ES2639757T3 ES 2639757 T3 ES2639757 T3 ES 2639757T3 ES 11764989 T ES11764989 T ES 11764989T ES 11764989 T ES11764989 T ES 11764989T ES 2639757 T3 ES2639757 T3 ES 2639757T3
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- Prior art keywords
- alkyl
- amino
- group
- halogen
- phenyl
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- -1 2- (1H-indazol-6-yl) spiro [cyclopropan-1,3'-indolin] Chemical compound 0.000 title abstract 10
- 230000015572 biosynthetic process Effects 0.000 title 1
- 238000003786 synthesis reaction Methods 0.000 title 1
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 17
- 229910052736 halogen Inorganic materials 0.000 abstract 14
- 150000002367 halogens Chemical class 0.000 abstract 14
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 13
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 12
- 125000001424 substituent group Chemical group 0.000 abstract 11
- 125000004438 haloalkoxy group Chemical group 0.000 abstract 10
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 9
- 125000001188 haloalkyl group Chemical group 0.000 abstract 7
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 6
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 4
- 125000000027 (C1-C10) alkoxy group Chemical group 0.000 abstract 3
- 125000006708 (C5-C14) heteroaryl group Chemical group 0.000 abstract 3
- 125000005915 C6-C14 aryl group Chemical group 0.000 abstract 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 3
- 125000001931 aliphatic group Chemical group 0.000 abstract 3
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 3
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 2
- 125000004448 alkyl carbonyl group Chemical group 0.000 abstract 2
- 125000005196 alkyl carbonyloxy group Chemical group 0.000 abstract 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 1
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 abstract 1
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 abstract 1
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- MDFFNEOEWAXZRQ-UHFFFAOYSA-N aminyl Chemical compound [NH2] MDFFNEOEWAXZRQ-UHFFFAOYSA-N 0.000 abstract 1
- 125000006615 aromatic heterocyclic group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 150000002431 hydrogen Chemical group 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- 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
- A61K31/40—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
- A61K31/404—Indoles, e.g. pindolol
-
- 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
- A61K31/415—1,2-Diazoles
- A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
-
- 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
- A61K31/535—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
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- 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
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
- C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
-
- 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
- C07D403/02—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
-
- 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
- C07D403/02—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
- C07D403/10—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 linked by a carbon chain containing aromatic rings
-
- 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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pulmonology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Indole Compounds (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US32132910P | 2010-04-06 | 2010-04-06 | |
| US32133210P | 2010-04-06 | 2010-04-06 | |
| PCT/CA2010/000518 WO2010115279A1 (en) | 2009-04-06 | 2010-04-06 | Kinase inhibitors and method of treating cancer with same |
| PCT/CA2011/000387 WO2011123947A1 (en) | 2010-04-06 | 2011-04-06 | Synthesis of chiral 2-(1h-indazol-6-yl)-spiro[cyclopropane-1,3'- indolin]-2'-ones |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2639757T3 true ES2639757T3 (es) | 2017-10-30 |
Family
ID=44761967
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES11764989T Active ES2639757T3 (es) | 2010-04-06 | 2011-04-06 | Síntesis de 2-(1H-indazol-6-il)espiro[ciclopropan-1,3'-indolin]-2'-onas quirales |
| ES11764988.9T Active ES2603613T3 (es) | 2010-04-06 | 2011-04-06 | Inhibidores de quinasa y su uso en el tratamiento del cáncer |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES11764988.9T Active ES2603613T3 (es) | 2010-04-06 | 2011-04-06 | Inhibidores de quinasa y su uso en el tratamiento del cáncer |
Country Status (25)
| Country | Link |
|---|---|
| US (9) | US8263596B2 (enExample) |
| EP (2) | EP2556070B1 (enExample) |
| JP (1) | JP5442906B2 (enExample) |
| KR (1) | KR101782668B1 (enExample) |
| CN (1) | CN102892766B (enExample) |
| AU (1) | AU2011238384B2 (enExample) |
| BR (1) | BR112012025496B1 (enExample) |
| CY (1) | CY1118610T1 (enExample) |
| DK (1) | DK2556071T3 (enExample) |
| EA (1) | EA023173B1 (enExample) |
| ES (2) | ES2639757T3 (enExample) |
| HR (1) | HRP20161498T1 (enExample) |
| HU (1) | HUE030651T2 (enExample) |
| IL (1) | IL221556A (enExample) |
| LT (1) | LT2556071T (enExample) |
| ME (1) | ME02545B (enExample) |
| MX (1) | MX2012011516A (enExample) |
| NZ (1) | NZ602350A (enExample) |
| PL (1) | PL2556071T3 (enExample) |
| PT (1) | PT2556071T (enExample) |
| SG (1) | SG183875A1 (enExample) |
| SI (1) | SI2556071T1 (enExample) |
| SM (1) | SMT201600430B (enExample) |
| TW (1) | TWI516262B (enExample) |
| WO (2) | WO2011123947A1 (enExample) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2235004A4 (en) * | 2007-12-21 | 2011-05-04 | Univ Health Network | INDAZOLYL, BENZIMIDAZOLYL, BENZOTRIAZOLYL-SUBSTITUTED INDOLUND DERIVATIVES AS A KINASE-HEMMER FOR CANCER TREATMENT |
| WO2010115279A1 (en) | 2009-04-06 | 2010-10-14 | University Health Network | Kinase inhibitors and method of treating cancer with same |
| TWI516262B (zh) | 2010-04-06 | 2016-01-11 | 健康網路大學 | 激酶抑制劑及以其治療癌症的方法 |
| CA2803446C (en) | 2010-07-02 | 2019-06-04 | University Health Network | Use of plk4 antagonists for treating pten mutant diseases |
| WO2012048411A1 (en) * | 2010-10-13 | 2012-04-19 | University Health Network | Plk-4 inhibitors and method of treating cancer with same |
| WO2014017643A1 (ja) * | 2012-07-27 | 2014-01-30 | 佐藤製薬株式会社 | ジフルオロメチレン化合物 |
| EA030089B1 (ru) * | 2013-10-18 | 2018-06-29 | Юниверсити Хелс Нетуорк | Лечение рака поджелудочной железы |
| TR201902875T4 (tr) * | 2013-10-18 | 2019-03-21 | Univ Health Network | Plk-4 inhibitörünün tuz ve kristal formları. |
| CN104130175A (zh) * | 2014-06-13 | 2014-11-05 | 天津科技大学 | 不同位置取代吲哚酮类衍生物及其应用 |
| US11608334B2 (en) | 2017-02-08 | 2023-03-21 | The National Institutes of Pharmaceutical R&D Co., Ltd. | Pyrrolo-aromatic heterocyclic compound, preparation method therefor, and medical use thereof |
| CN108947961B (zh) * | 2017-05-18 | 2021-06-04 | 四川大学 | 吲唑类衍生物及其制备方法和用途 |
| JP7343483B2 (ja) * | 2017-09-08 | 2023-09-12 | ユニバーシティー ヘルス ネットワーク | Ｐｏｌｏ様キナーゼ４の阻害のための併用療法 |
| WO2020097396A1 (en) | 2018-11-07 | 2020-05-14 | Dana-Farber Cancer Institute, Inc. | Benzimidazole derivatives and aza-benzimidazole derivatives as janus kinase 2 inhibitors and uses thereof |
| US12509455B2 (en) | 2018-11-07 | 2025-12-30 | Dana-Farber Cancer Institute, Inc. | Imidazopyridine derivatives and aza-imidazopyridine derivatives as Janus kinase 2 inhibitors and uses thereof |
| EP3876939A4 (en) | 2018-11-07 | 2022-08-10 | Dana-Farber Cancer Institute, Inc. | Benzothiazole derivatives and 7-aza-benzothiazole derivatives as janus kinase 2 inhibitors and uses thereof |
| EP3959209A4 (en) | 2019-04-24 | 2022-12-28 | University Health Network | S4 CRYSTALLINE FORM OF A PLK4 INHIBITOR (1R,2S)-(E)-2-(3-(4-((CIS-2,6-DIMETHYLMORPHOLINO)METHYL)STYRYL)-1H-IMIDAZOL-6-YL )-5'-METHOXYSPIRO[CYCLOPROPANE-L,3'-INDOLIN]-2'-ONE FUMARATE |
| CA3156828A1 (en) | 2019-10-03 | 2021-04-08 | Dana-Farber Cancer Institute, Inc. | Tricyclic kinase inhibitors and uses thereof |
| KR20220124177A (ko) * | 2019-12-06 | 2022-09-13 | 유니버시티 헬스 네트워크 | 급성 골수성 백혈병 또는 골수형성이상증후군의 치료방법 |
| TW202204350A (zh) | 2020-05-06 | 2022-02-01 | 美商雅捷可斯治療公司 | 作為ｊａｋ２抑制劑之６－雜芳基氧基苯并咪唑及氮雜苯并咪唑 |
| CN112250614B (zh) | 2020-10-20 | 2022-02-01 | 苏州大学 | 3-螺三元环吲哚酮衍生物的合成方法 |
| EP4267574B1 (en) | 2020-12-23 | 2025-04-23 | Ajax Therapeutics, Inc. | 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors |
| TW202300485A (zh) * | 2021-03-02 | 2023-01-01 | 大陸商上海齊魯製藥研究中心有限公司 | Plk4抑制劑及其用途 |
| TWI926033B (zh) | 2021-05-11 | 2026-05-21 | 美商歐瑞克製藥公司 | 類ｐｏｌｏ激酶４抑制劑 |
| CN115677682B (zh) * | 2021-07-30 | 2023-07-18 | 上海齐鲁制药研究中心有限公司 | 螺环类plk4抑制剂及其用途 |
| CA3234638A1 (en) | 2021-11-09 | 2023-05-19 | Ajax Therapeutics, Inc. | 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors |
| US12162881B2 (en) | 2021-11-09 | 2024-12-10 | Ajax Therapeutics, Inc. | Forms and compositions of inhibitors of JAK2 |
| US20260015351A1 (en) * | 2022-06-30 | 2026-01-15 | Axonis Therapeutics, Inc. | Methods and compounds for inhibiting mkk7 enzymes |
| WO2024209363A1 (en) | 2023-04-06 | 2024-10-10 | Pfizer Inc. | Substituted indazole propionic acid derivative compounds and uses thereof as ampk activators |
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