RU2019107667A - Спироциклические соединения - Google Patents
Спироциклические соединения Download PDFInfo
- Publication number
- RU2019107667A RU2019107667A RU2019107667A RU2019107667A RU2019107667A RU 2019107667 A RU2019107667 A RU 2019107667A RU 2019107667 A RU2019107667 A RU 2019107667A RU 2019107667 A RU2019107667 A RU 2019107667A RU 2019107667 A RU2019107667 A RU 2019107667A
- Authority
- RU
- Russia
- Prior art keywords
- cancer
- pharmaceutically acceptable
- acceptable salt
- compound according
- group
- Prior art date
Links
- 150000003839 salts Chemical class 0.000 claims 57
- 150000001875 compounds Chemical class 0.000 claims 55
- 206010028980 Neoplasm Diseases 0.000 claims 41
- -1 methylbenzoxazolyl Chemical group 0.000 claims 34
- 201000011510 cancer Diseases 0.000 claims 33
- 210000004027 cell Anatomy 0.000 claims 25
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 14
- 125000004093 cyano group Chemical group *C#N 0.000 claims 11
- 125000001153 fluoro group Chemical group F* 0.000 claims 10
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 10
- 125000001424 substituent group Chemical group 0.000 claims 10
- 239000008194 pharmaceutical composition Substances 0.000 claims 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 8
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 8
- 208000001446 Anaplastic Thyroid Carcinoma Diseases 0.000 claims 7
- 206010002240 Anaplastic thyroid cancer Diseases 0.000 claims 7
- 208000003174 Brain Neoplasms Diseases 0.000 claims 7
- 206010006187 Breast cancer Diseases 0.000 claims 7
- 208000026310 Breast neoplasm Diseases 0.000 claims 7
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 7
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 7
- 208000034578 Multiple myelomas Diseases 0.000 claims 7
- 206010029260 Neuroblastoma Diseases 0.000 claims 7
- 208000009905 Neurofibromatoses Diseases 0.000 claims 7
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 7
- 206010033128 Ovarian cancer Diseases 0.000 claims 7
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 7
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 7
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 7
- 206010060862 Prostate cancer Diseases 0.000 claims 7
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 7
- 206010038389 Renal cancer Diseases 0.000 claims 7
- 206010039491 Sarcoma Diseases 0.000 claims 7
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 7
- 201000010536 head and neck cancer Diseases 0.000 claims 7
- 208000014829 head and neck neoplasm Diseases 0.000 claims 7
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 7
- 201000010982 kidney cancer Diseases 0.000 claims 7
- 201000005202 lung cancer Diseases 0.000 claims 7
- 208000020816 lung neoplasm Diseases 0.000 claims 7
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 7
- 201000001441 melanoma Diseases 0.000 claims 7
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 7
- 208000025113 myeloid leukemia Diseases 0.000 claims 7
- 201000004931 neurofibromatosis Diseases 0.000 claims 7
- 201000002528 pancreatic cancer Diseases 0.000 claims 7
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 7
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 7
- 201000002510 thyroid cancer Diseases 0.000 claims 7
- 208000019179 thyroid gland undifferentiated (anaplastic) carcinoma Diseases 0.000 claims 7
- 206010005003 Bladder cancer Diseases 0.000 claims 6
- 206010009944 Colon cancer Diseases 0.000 claims 6
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 6
- 125000001309 chloro group Chemical group Cl* 0.000 claims 6
- 208000029742 colonic neoplasm Diseases 0.000 claims 6
- 201000005112 urinary bladder cancer Diseases 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- 125000001072 heteroaryl group Chemical group 0.000 claims 5
- 125000000623 heterocyclic group Chemical group 0.000 claims 5
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 239000001257 hydrogen Substances 0.000 claims 5
- 125000004076 pyridyl group Chemical group 0.000 claims 5
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 4
- 229910052805 deuterium Inorganic materials 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 4
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 230000015572 biosynthetic process Effects 0.000 claims 3
- 125000005043 dihydropyranyl group Chemical group O1C(CCC=C1)* 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 125000005059 halophenyl group Chemical group 0.000 claims 3
- 230000002401 inhibitory effect Effects 0.000 claims 3
- 125000006645 (C3-C4) cycloalkyl group Chemical group 0.000 claims 2
- 125000005036 alkoxyphenyl group Chemical group 0.000 claims 2
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 2
- 210000004907 gland Anatomy 0.000 claims 2
- 125000003253 isopropoxy group Chemical group [H]C([H])([H])C([H])(O*)C([H])([H])[H] 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 230000010076 replication Effects 0.000 claims 2
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 2
- 125000000335 thiazolyl group Chemical group 0.000 claims 2
- 125000001425 triazolyl group Chemical group 0.000 claims 2
- 125000004205 trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims 2
- WIRWAVLHCQROQG-ZCQIMEDXSA-N (5S)-7-[1,1-dideuterio-2-[4-[4-(1-methyl-1,2,4-triazol-3-yl)phenyl]-3,6-dihydro-2H-pyridin-1-yl]-2-oxoethyl]-2-[3-(5-fluoropyridin-2-yl)-1H-indazol-5-yl]-2,7-diazaspiro[4.4]nonan-1-one Chemical compound FC=1C=CC(=NC=1)C1=NNC2=CC=C(C=C12)N1C([C@@]2(CC1)CN(CC2)C(C(=O)N1CCC(=CC1)C1=CC=C(C=C1)C1=NN(C=N1)C)([2H])[2H])=O WIRWAVLHCQROQG-ZCQIMEDXSA-N 0.000 claims 1
- BPGVSQWUBDBBAJ-OZOQSGKISA-N (5S)-7-[1,1-dideuterio-2-[4-[4-(1-methyl-1,2,4-triazol-3-yl)phenyl]-3,6-dihydro-2H-pyridin-1-yl]-2-oxoethyl]-2-[3-(oxan-4-yl)-2H-indazol-5-yl]-2,7-diazaspiro[4.4]nonan-1-one Chemical compound CN1N=C(N=C1)C1=CC=C(C=C1)C=1CCN(CC=1)C(C([2H])([2H])N1C[C@@]2(CCN(C2=O)C=2C=C3C(=NNC3=CC=2)C2CCOCC2)CC1)=O BPGVSQWUBDBBAJ-OZOQSGKISA-N 0.000 claims 1
- FWOPJXVQGMZKEP-UHFFFAOYSA-N 3-methyl-2h-indazole Chemical compound C1=CC=CC2=C(C)NN=C21 FWOPJXVQGMZKEP-UHFFFAOYSA-N 0.000 claims 1
- 101000876610 Dictyostelium discoideum Extracellular signal-regulated kinase 2 Proteins 0.000 claims 1
- 101001052493 Homo sapiens Mitogen-activated protein kinase 1 Proteins 0.000 claims 1
- 108040008097 MAP kinase activity proteins Proteins 0.000 claims 1
- 102000019149 MAP kinase activity proteins Human genes 0.000 claims 1
- 102100024193 Mitogen-activated protein kinase 1 Human genes 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 125000001207 fluorophenyl group Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 230000003211 malignant effect Effects 0.000 claims 1
- 210000000066 myeloid cell Anatomy 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
Classifications
-
- 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
- C07D487/10—Spiro-condensed systems
-
- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- 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)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662404668P | 2016-10-05 | 2016-10-05 | |
| US62/404,668 | 2016-10-05 | ||
| PCT/US2017/054865 WO2018067512A1 (en) | 2016-10-05 | 2017-10-03 | Spirocyclic compounds |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2019107667A true RU2019107667A (ru) | 2020-11-06 |
| RU2019107667A3 RU2019107667A3 (https=) | 2021-01-27 |
Family
ID=61831517
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2019107667A RU2019107667A (ru) | 2016-10-05 | 2017-10-03 | Спироциклические соединения |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US10934304B2 (https=) |
| EP (1) | EP3523306A4 (https=) |
| JP (2) | JP6949952B2 (https=) |
| KR (1) | KR20190075931A (https=) |
| CN (1) | CN109890827A (https=) |
| AU (1) | AU2017339890A1 (https=) |
| BR (1) | BR112019005305A2 (https=) |
| CA (1) | CA3037064A1 (https=) |
| IL (1) | IL265752A (https=) |
| MX (1) | MX2019003938A (https=) |
| RU (1) | RU2019107667A (https=) |
| TW (1) | TW201817732A (https=) |
| WO (1) | WO2018067512A1 (https=) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RS58514B1 (sr) | 2012-06-13 | 2019-04-30 | Incyte Holdings Corp | Supstituisana triciklična jedinjenja kao inhibitori fgfr |
| PH12015502383B1 (en) | 2013-04-19 | 2023-02-03 | Incyte Holdings Corp | Bicyclic heterocycles as fgfr inhibitors |
| TWI712601B (zh) | 2015-02-20 | 2020-12-11 | 美商英塞特公司 | 作為fgfr抑制劑之雙環雜環 |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| MX379622B (es) | 2015-04-03 | 2025-03-11 | Recurium Ip Holdings Llc | Compuestos espirociclicos |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| HRP20241288T1 (hr) | 2018-05-04 | 2024-12-06 | Incyte Corporation | Čvrsti oblici fgfr inhibitora i postupci za njihovu proizvodnju |
| AU2019262579B2 (en) | 2018-05-04 | 2024-09-12 | Incyte Corporation | Salts of an FGFR inhibitor |
| CN112654396B (zh) * | 2018-09-07 | 2025-07-01 | 默克专利股份公司 | 5-吗啉-4-基-吡唑并[4,3-b]吡啶衍生物 |
| US11628162B2 (en) | 2019-03-08 | 2023-04-18 | Incyte Corporation | Methods of treating cancer with an FGFR inhibitor |
| US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| CA3157361A1 (en) | 2019-10-14 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| JP7832891B2 (ja) | 2019-12-04 | 2026-03-18 | インサイト・コーポレイション | Ｆｇｆｒ阻害剤の誘導体 |
| CA3163875A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| CN110922421B (zh) * | 2019-12-17 | 2023-05-05 | 安徽英特美科技有限公司 | 一种n-甲基-1,2,5,6-四氢吡啶-4-硼酸频哪醇酯的合成方法 |
| US12012409B2 (en) | 2020-01-15 | 2024-06-18 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2022221170A1 (en) | 2021-04-12 | 2022-10-20 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| CA3220155A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| US11939331B2 (en) | 2021-06-09 | 2024-03-26 | Incyte Corporation | Tricyclic heterocycles as FGFR inhibitors |
| AU2024374279A1 (en) * | 2023-10-31 | 2026-03-12 | C4 Therapeutics, Inc. | Compounds for the degradation of mutant braf |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA84930C2 (ru) | 2004-05-14 | 2008-12-10 | Вертекс Фармасьютикалс Инкорпорейтед | Пиррольные соединения как ингибиторы протеинкиназ erk, их синтез и соответствующие промежуточные соединения |
| KR101417136B1 (ko) * | 2005-12-13 | 2014-08-07 | 머크 샤프 앤드 돔 코포레이션 | Ｅｒｋ 억제제인 폴리사이클릭 인다졸 유도체 및 이를 포함하는 약제학적 조성물 |
| WO2008063609A2 (en) | 2006-11-17 | 2008-05-29 | Polyera Corporation | Diimide-based semiconductor materials and methods of preparing and using the same |
| CA2691417A1 (en) * | 2007-06-18 | 2008-12-24 | Schering Corporation | Heterocyclic compounds and use thereof as erk inhibitors |
| EP2318388A2 (en) | 2008-07-23 | 2011-05-11 | Schering Corporation | Tricyclic spirocycle derivatives and methods of use thereof |
| EP3296398A1 (en) | 2009-12-07 | 2018-03-21 | Arbutus Biopharma Corporation | Compositions for nucleic acid delivery |
| US8664213B2 (en) * | 2011-08-29 | 2014-03-04 | Bristol-Myers Squibb Company | Spiro bicyclic diamine derivatives as HIV attachment inhibitors |
| CN103130775B (zh) | 2011-11-22 | 2015-09-30 | 山东亨利医药科技有限责任公司 | 作为酪氨酸激酶抑制剂的吲哚满酮衍生物 |
| US8987264B2 (en) | 2012-11-09 | 2015-03-24 | Bristol-Myers Squibb Company | 1,3,5-triazine derivatives of spiro bicyclic oxalamide-compounds for treatment of hepatitis C |
| US9447026B2 (en) | 2013-03-14 | 2016-09-20 | Kalyra Pharmaceuticals, Inc. | Bicyclic analgesic compounds |
| US9879029B2 (en) | 2014-12-22 | 2018-01-30 | Eli Lilly And Company | ERK inhibitors |
| CN105732636B (zh) * | 2014-12-30 | 2020-04-21 | 广东东阳光药业有限公司 | 杂芳化合物及其在药物中的应用 |
| MX379622B (es) | 2015-04-03 | 2025-03-11 | Recurium Ip Holdings Llc | Compuestos espirociclicos |
-
2017
- 2017-10-03 AU AU2017339890A patent/AU2017339890A1/en not_active Abandoned
- 2017-10-03 EP EP17858989.1A patent/EP3523306A4/en not_active Withdrawn
- 2017-10-03 CN CN201780067175.6A patent/CN109890827A/zh active Pending
- 2017-10-03 KR KR1020197012021A patent/KR20190075931A/ko not_active Ceased
- 2017-10-03 BR BR112019005305A patent/BR112019005305A2/pt not_active Application Discontinuation
- 2017-10-03 US US16/336,854 patent/US10934304B2/en not_active Expired - Fee Related
- 2017-10-03 MX MX2019003938A patent/MX2019003938A/es unknown
- 2017-10-03 JP JP2019518440A patent/JP6949952B2/ja not_active Expired - Fee Related
- 2017-10-03 RU RU2019107667A patent/RU2019107667A/ru not_active Application Discontinuation
- 2017-10-03 WO PCT/US2017/054865 patent/WO2018067512A1/en not_active Ceased
- 2017-10-03 CA CA3037064A patent/CA3037064A1/en not_active Abandoned
- 2017-10-05 TW TW106134299A patent/TW201817732A/zh unknown
-
2019
- 2019-04-01 IL IL265752A patent/IL265752A/en unknown
-
2020
- 2020-12-18 US US17/127,710 patent/US20210115058A1/en not_active Abandoned
-
2021
- 2021-09-22 JP JP2021154677A patent/JP2021193138A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| CA3037064A1 (en) | 2018-04-12 |
| TW201817732A (zh) | 2018-05-16 |
| CN109890827A (zh) | 2019-06-14 |
| EP3523306A1 (en) | 2019-08-14 |
| JP2021193138A (ja) | 2021-12-23 |
| EP3523306A4 (en) | 2020-05-06 |
| US20210115058A1 (en) | 2021-04-22 |
| WO2018067512A1 (en) | 2018-04-12 |
| MX2019003938A (es) | 2019-06-10 |
| NZ751398A (en) | 2021-03-26 |
| AU2017339890A1 (en) | 2019-04-11 |
| WO2018067512A8 (en) | 2018-11-01 |
| US10934304B2 (en) | 2021-03-02 |
| IL265752A (en) | 2019-06-30 |
| JP2019534261A (ja) | 2019-11-28 |
| KR20190075931A (ko) | 2019-07-01 |
| RU2019107667A3 (https=) | 2021-01-27 |
| JP6949952B2 (ja) | 2021-10-13 |
| US20200207776A1 (en) | 2020-07-02 |
| BR112019005305A2 (pt) | 2019-07-02 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20220110 |