CA2970864C - Solid state forms of fused heteroaromatic pyrrolidinones - Google Patents
Solid state forms of fused heteroaromatic pyrrolidinones Download PDFInfo
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- CA2970864C CA2970864C CA2970864A CA2970864A CA2970864C CA 2970864 C CA2970864 C CA 2970864C CA 2970864 A CA2970864 A CA 2970864A CA 2970864 A CA2970864 A CA 2970864A CA 2970864 C CA2970864 C CA 2970864C
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- HZEVBBFYOHEJSR-NEPJUHHUSA-N tert-butyl (3aR,7aS)-3-(4-chloro-7-fluoro-3-oxo-1,2-dihydropyrrolo[3,4-c]pyridin-6-yl)-3a,4,5,6,7,7a-hexahydro-2H-benzimidazole-1-carboxylate Chemical compound ClC1=NC(=C(C2=C1C(NC2)=O)F)N1CN([C@@H]2[C@H]1CCCC2)C(=O)OC(C)(C)C HZEVBBFYOHEJSR-NEPJUHHUSA-N 0.000 description 1
- DLFJYFPTJVIHJL-KGLIPLIRSA-N tert-butyl (3aR,7aS)-3-(6-chloro-5-cyano-3-fluoropyridin-2-yl)-3a,4,5,6,7,7a-hexahydro-2H-benzimidazole-1-carboxylate Chemical compound ClC1=C(C=C(C(=N1)N1CN([C@@H]2[C@H]1CCCC2)C(=O)OC(C)(C)C)F)C#N DLFJYFPTJVIHJL-KGLIPLIRSA-N 0.000 description 1
- HABPUQRAKKBZJJ-UHFFFAOYSA-N tert-butyl 4,6-dichloro-7-fluoro-3-oxo-1h-pyrrolo[3,4-c]pyridine-2-carboxylate Chemical compound ClC1=NC(Cl)=C(F)C2=C1C(=O)N(C(=O)OC(C)(C)C)C2 HABPUQRAKKBZJJ-UHFFFAOYSA-N 0.000 description 1
- SOGZIWVEABFBEY-UHFFFAOYSA-N tert-butyl 4-chloro-6,7-difluoro-3-oxo-1h-pyrrolo[3,4-c]pyridine-2-carboxylate Chemical compound ClC1=NC(F)=C(F)C2=C1C(=O)N(C(=O)OC(C)(C)C)C2 SOGZIWVEABFBEY-UHFFFAOYSA-N 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- MHXBHWLGRWOABW-UHFFFAOYSA-N tetradecyl octadecanoate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCCCCCCCCCCCCCC MHXBHWLGRWOABW-UHFFFAOYSA-N 0.000 description 1
- 210000001685 thyroid gland Anatomy 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 230000000451 tissue damage Effects 0.000 description 1
- 231100000827 tissue damage Toxicity 0.000 description 1
- 238000004448 titration Methods 0.000 description 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
- 125000003944 tolyl group Chemical group 0.000 description 1
- 238000011200 topical administration Methods 0.000 description 1
- 239000012049 topical pharmaceutical composition Substances 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 238000000844 transformation Methods 0.000 description 1
- WLPUWLXVBWGYMZ-UHFFFAOYSA-N tricyclohexylphosphine Chemical compound C1CCCCC1P(C1CCCCC1)C1CCCCC1 WLPUWLXVBWGYMZ-UHFFFAOYSA-N 0.000 description 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 description 1
- 230000009959 type I hypersensitivity Effects 0.000 description 1
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 description 1
- ZDPHROOEEOARMN-UHFFFAOYSA-N undecanoic acid Chemical compound CCCCCCCCCCC(O)=O ZDPHROOEEOARMN-UHFFFAOYSA-N 0.000 description 1
- 210000003932 urinary bladder Anatomy 0.000 description 1
- 235000013311 vegetables Nutrition 0.000 description 1
- 239000003981 vehicle Substances 0.000 description 1
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Classifications
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (7)
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| US201562115223P | 2015-02-12 | 2015-02-12 | |
| US62/115,223 | 2015-02-12 | ||
| US201562180222P | 2015-06-16 | 2015-06-16 | |
| US62/180,222 | 2015-06-16 | ||
| PCT/IB2015/002489 WO2016097862A2 (en) | 2014-12-18 | 2015-12-17 | Solid state forms of fused heteroaromatic pyrrolidinones |
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| CA2970864A1 CA2970864A1 (en) | 2016-06-23 |
| CA2970864C true CA2970864C (en) | 2020-04-14 |
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|---|---|---|---|
| CA2970864A Active CA2970864C (en) | 2014-12-18 | 2015-12-17 | Solid state forms of fused heteroaromatic pyrrolidinones |
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| PL3233857T3 (pl) * | 2014-12-18 | 2020-07-27 | Takeda Pharmaceutical Company Limited | Stałe postacie skondensowanych heteroaromatycznych pirolidynonów |
| JP2019520419A (ja) * | 2016-07-13 | 2019-07-18 | 武田薬品工業株式会社 | 脾臓チロシンキナーゼ阻害剤と他の治療薬の併用 |
| SG11202002475TA (en) | 2017-10-19 | 2020-04-29 | Bayer Animal Health Gmbh | Use of fused heteroaromatic pyrrolidones for treatment and prevention of diseases in animals |
| WO2019088039A1 (en) | 2017-10-30 | 2019-05-09 | Takeda Pharmaceutical Company Limited | Treatment of acute myeloid leukemia |
| EP3896063B1 (en) * | 2018-12-14 | 2024-01-24 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Crystalline forms of the syk inhibitor 5-fluoro-1-methyl-3-[[5-[4-(3-oxetanyl)-1-piperazinyl]-2-pyridinyl]amino]-6-(1h-pyrazol-3-yl)-2(1h)-quinolinone hydrochloride salt (1:1) |
| US20220081422A1 (en) | 2019-02-07 | 2022-03-17 | Janssen Biotech, Inc. | Dihydroorotate dehydrogenase inhibitors |
| TW202104207A (zh) | 2019-04-17 | 2021-02-01 | 美商健生生物科技公司 | 二氫乳清酸脫氫酶抑制劑 |
| AU2020363021A1 (en) | 2019-10-10 | 2022-04-07 | Janssen Biotech, Inc. | Bi-aryl dihydroorotate dehydrogenase inhibitors |
| IL293965A (en) | 2019-12-19 | 2022-08-01 | Janssen Pharmaceutica Nv | History of Spiro straight chain transformed |
| WO2022074534A1 (en) | 2020-10-05 | 2022-04-14 | Janssen Biotech, Inc. | Combinations of dihydroorotate dehydrogenase inhibitors and hypomethylating agents |
| CN115698005B (zh) * | 2020-12-18 | 2024-02-06 | 山东轩竹医药科技有限公司 | 稠环类AhR抑制剂 |
| WO2022237720A1 (en) | 2021-05-11 | 2022-11-17 | Janssen Pharmaceutica Nv | Combination therapies |
| EP4337215A1 (en) | 2021-05-11 | 2024-03-20 | JANSSEN Pharmaceutica NV | Combination therapies |
| CN120282784A (zh) | 2022-11-30 | 2025-07-08 | 詹森药业有限公司 | 包含多发性内分泌癌蛋白-mll抑制剂和bcl-2抑制剂的组合 |
| EP4626426A1 (en) | 2022-11-30 | 2025-10-08 | JANSSEN Pharmaceutica NV | Combinations comprising a menin-mll inhibitor and at least one other therapeutic agent |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| WO2007070872A1 (en) * | 2005-12-15 | 2007-06-21 | Rigel Pharmaceuticals, Inc. | Kinase inhibitors and their uses |
| SG181857A1 (en) * | 2009-12-23 | 2012-07-30 | Takeda Pharmaceutical | Fused heteroaromatic pyrrolidinones as syk inhibitors |
| US9056873B2 (en) | 2011-06-22 | 2015-06-16 | Takeda Pharmaceutical Company Limited | Substituted 6-aza-isoindolin-1-one derivatives |
| WO2016048982A2 (en) * | 2014-09-24 | 2016-03-31 | Millennium Pharmaceuticals, Inc. | COMBINATION TREATMENT WITH PI3Kα INHIBITORS AND TAXANES |
| PL3233857T3 (pl) * | 2014-12-18 | 2020-07-27 | Takeda Pharmaceutical Company Limited | Stałe postacie skondensowanych heteroaromatycznych pirolidynonów |
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2015
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- 2015-12-17 WO PCT/IB2015/002489 patent/WO2016097862A2/en not_active Ceased
- 2015-12-17 BR BR112017013149-8A patent/BR112017013149B1/pt not_active IP Right Cessation
- 2015-12-17 KR KR1020177019929A patent/KR102037502B1/ko active Active
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- 2015-12-17 EP EP15831150.6A patent/EP3233857B1/en active Active
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- 2015-12-17 UA UAA201707489A patent/UA120632C2/uk unknown
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2017
- 2017-03-13 ZA ZA2017/01800A patent/ZA201701800B/en unknown
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- 2017-06-15 CL CL2017001561A patent/CL2017001561A1/es unknown
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2020
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2021
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2022
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Effective date: 20170804 |