PE20211207A1 - Formas solidas de 3-((1r,3r)-1-(2,6-difluoro-4-((1- (3-fluoropropil)azetidin-3-il)amino)fenil)-3-metil-1,3,4,9-tetrahidro-2h-pirido[3,4-b]indol-2-il)-2,2-difluoropropan-1-ol y procesos para preparar compuestos triciclicos fusionados que comprenden un resto fenilo o piridinilo sustituido, incluidos metodos para su uso - Google Patents
Formas solidas de 3-((1r,3r)-1-(2,6-difluoro-4-((1- (3-fluoropropil)azetidin-3-il)amino)fenil)-3-metil-1,3,4,9-tetrahidro-2h-pirido[3,4-b]indol-2-il)-2,2-difluoropropan-1-ol y procesos para preparar compuestos triciclicos fusionados que comprenden un resto fenilo o piridinilo sustituido, incluidos metodos para su usoInfo
- Publication number
- PE20211207A1 PE20211207A1 PE2020001888A PE2020001888A PE20211207A1 PE 20211207 A1 PE20211207 A1 PE 20211207A1 PE 2020001888 A PE2020001888 A PE 2020001888A PE 2020001888 A PE2020001888 A PE 2020001888A PE 20211207 A1 PE20211207 A1 PE 20211207A1
- Authority
- PE
- Peru
- Prior art keywords
- phenyl
- difluoropropan
- fluoropropyl
- indol
- difluoro
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 238000000034 method Methods 0.000 title abstract 3
- -1 AMINO Chemical class 0.000 title abstract 2
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical class [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 title 2
- HNEGJTWNOOWEMH-UHFFFAOYSA-N 1-fluoropropane Chemical class [CH2]CCF HNEGJTWNOOWEMH-UHFFFAOYSA-N 0.000 title 1
- FIULGFJIHJJXMT-UHFFFAOYSA-N [C]1[N]C=CC=C1 Chemical class [C]1[N]C=CC=C1 FIULGFJIHJJXMT-UHFFFAOYSA-N 0.000 title 1
- 239000007787 solid Substances 0.000 title 1
- GQCXHIKRWBIQMD-AKJBCIBTSA-N 3-[(1R,3R)-1-[2,6-difluoro-4-[[1-(3-fluoropropyl)azetidin-3-yl]amino]phenyl]-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-2-yl]-2,2-difluoropropan-1-ol Chemical compound FC1=C(C(=CC(=C1)NC1CN(C1)CCCF)F)[C@H]1N([C@@H](CC2=C1NC1=CC=CC=C21)C)CC(CO)(F)F GQCXHIKRWBIQMD-AKJBCIBTSA-N 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 238000000634 powder X-ray diffraction Methods 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
Classifications
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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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
- C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
- C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Abstract
La presente invencion se refiere al compuesto (2R,3R)-2,3-dihidroxisuccinato de 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropil)azetidin-3-il)amino)fenil)-3-metil-1,3,4,9-tetrahidro-2H-pirido[3,4-b]indol-2-il)-2,2-difluoropropan-1-ol (compuesto B) o una forma cristalina del mismo que tiene un patron de difraccion de polvo de rayos X que comprende picos en 19,32, 20,26, 21,63, 23,28 o 24,81 ±0,1º 2 theta (± 0,1 °2 theta). Tambien se refiere a composiciones farmaceuticas y procesos de sintesis. Dichos compuestos son utiles en el tratamiento del cancer.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201862687930P | 2018-06-21 | 2018-06-21 | |
US201862719896P | 2018-08-20 | 2018-08-20 | |
PCT/US2019/037492 WO2019245974A1 (en) | 2018-06-21 | 2019-06-17 | Solid forms of 3-((1r,3r)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2h-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol and processes for preparing fused tricyclic compounds comprising a substituted phenyl or pyridinyl moiety, including methods of their use |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20211207A1 true PE20211207A1 (es) | 2021-07-05 |
Family
ID=67441580
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2020001888A PE20211207A1 (es) | 2018-06-21 | 2019-06-17 | Formas solidas de 3-((1r,3r)-1-(2,6-difluoro-4-((1- (3-fluoropropil)azetidin-3-il)amino)fenil)-3-metil-1,3,4,9-tetrahidro-2h-pirido[3,4-b]indol-2-il)-2,2-difluoropropan-1-ol y procesos para preparar compuestos triciclicos fusionados que comprenden un resto fenilo o piridinilo sustituido, incluidos metodos para su uso |
Country Status (29)
Country | Link |
---|---|
US (2) | US10954234B2 (es) |
EP (2) | EP3810283B1 (es) |
JP (4) | JP6916969B1 (es) |
KR (2) | KR20230117761A (es) |
CN (1) | CN112437685A (es) |
AU (3) | AU2019290545B2 (es) |
BR (1) | BR112020024073A2 (es) |
CA (1) | CA3098203A1 (es) |
CL (1) | CL2020003022A1 (es) |
CO (1) | CO2020014604A2 (es) |
CR (2) | CR20200621A (es) |
DK (1) | DK3810283T3 (es) |
ES (1) | ES2951829T3 (es) |
FI (1) | FI3810283T3 (es) |
HR (1) | HRP20230859T1 (es) |
HU (1) | HUE064542T2 (es) |
IL (1) | IL278063A (es) |
LT (1) | LT3810283T (es) |
MX (3) | MX2020011531A (es) |
PE (1) | PE20211207A1 (es) |
PH (1) | PH12020500676A1 (es) |
PL (1) | PL3810283T3 (es) |
PT (1) | PT3810283T (es) |
RS (1) | RS64429B1 (es) |
SG (1) | SG11202012171SA (es) |
SI (1) | SI3810283T1 (es) |
TW (1) | TW202016098A (es) |
UA (1) | UA128114C2 (es) |
WO (1) | WO2019245974A1 (es) |
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RS64429B1 (sr) | 2018-06-21 | 2023-09-29 | Hoffmann La Roche | Čvrsti oblici soli tartarata 3-((1r,3r)-1-(2,6-difluor-4-((1-(3-fluorpropil)azetidin-3-il)amino)fenil)-3-metil-1,3,4,9-tetrahidro-2h-pirido[3,4-b]indol-2-il)-2,2-difluorpropan-1-ola, proces za njihovu pripremu i postupci za njihovu upotrebu u lečenju kancera |
KR20230007360A (ko) * | 2020-05-07 | 2023-01-12 | 리커리엄 아이피 홀딩스, 엘엘씨 | 복합제 |
CA3182018A1 (en) | 2020-05-12 | 2021-11-18 | Genentech, Inc. | Treatment of breast cancer using combination therapies comprising gdc-9545 and a cdk4/6 inhibitor |
WO2021228210A1 (zh) | 2020-05-15 | 2021-11-18 | 江苏先声药业有限公司 | 吡咯烷类化合物及其应用 |
WO2022001971A1 (zh) | 2020-06-28 | 2022-01-06 | 南京明德新药研发有限公司 | 并环吲唑类化合物 |
AU2021299200A1 (en) | 2020-06-30 | 2023-02-23 | F. Hoffmann-La Roche Ag | Processes for making SERD tricyclic compounds having a substituted phenyl or pyridinyl moiety |
WO2022140744A1 (en) | 2020-12-23 | 2022-06-30 | Recurium Ip Holdings, Llc | Estrogen receptor modulators |
IL304911A (en) * | 2021-02-16 | 2023-10-01 | Genentech Inc | Breast cancer treatment using combination therapies including GDC-9545 and abemciclib or ribociclib |
WO2022177835A1 (en) * | 2021-02-16 | 2022-08-25 | Genentech, Inc. | Treatment of breast cancer using combination therapies comprising gdc-9545 and ipatasertib |
CN117813288A (zh) | 2021-07-15 | 2024-04-02 | 西藏海思科制药有限公司 | 芳氨基衍生物雌激素受体调节剂及其用途 |
CN114656444A (zh) * | 2022-03-04 | 2022-06-24 | 河北松辰医药科技有限公司 | 一种2,2-二氟-1,3-丙基磺酸内酯的合成方法 |
TW202400141A (zh) | 2022-04-28 | 2024-01-01 | 瑞士商赫孚孟拉羅股份公司 | 3-((1r,3r)-1-(2,6-二氟-4-((1-(3-氟丙基)四氫吖唉-3-基)胺基)苯基)-3-甲基-1,3,4,9-四氫-2h-吡啶并[3,4-b]吲哚-2-基)-2,2-二氟丙-1-醇酒石酸鹽之固體形式 |
CN115872996B (zh) * | 2023-02-21 | 2023-05-05 | 山东绿叶制药有限公司 | 一种雌激素受体降解剂化合物及其制备方法和应用 |
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2019
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