EA032094B1 - Дейтерированный палбоциклиб - Google Patents
Дейтерированный палбоциклиб Download PDFInfo
- Publication number
- EA032094B1 EA032094B1 EA201591628A EA201591628A EA032094B1 EA 032094 B1 EA032094 B1 EA 032094B1 EA 201591628 A EA201591628 A EA 201591628A EA 201591628 A EA201591628 A EA 201591628A EA 032094 B1 EA032094 B1 EA 032094B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- pops
- snz
- compound
- deuterium
- same
- Prior art date
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- AHJRHEGDXFFMBM-UHFFFAOYSA-N palbociclib Chemical class N1=C2N(C3CCCC3)C(=O)C(C(=O)C)=C(C)C2=CN=C1NC(N=C1)=CC=C1N1CCNCC1 AHJRHEGDXFFMBM-UHFFFAOYSA-N 0.000 title 1
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- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims description 55
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- 239000001257 hydrogen Substances 0.000 claims description 28
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- YGSDEFSMJLZEOE-UHFFFAOYSA-M salicylate Chemical compound OC1=CC=CC=C1C([O-])=O YGSDEFSMJLZEOE-UHFFFAOYSA-M 0.000 description 1
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- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
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- DPKBAXPHAYBPRL-UHFFFAOYSA-M tetrabutylazanium;iodide Chemical compound [I-].CCCC[N+](CCCC)(CCCC)CCCC DPKBAXPHAYBPRL-UHFFFAOYSA-M 0.000 description 1
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- 230000000699 topical effect Effects 0.000 description 1
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- 125000005270 trialkylamine group Chemical group 0.000 description 1
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- 125000005580 triphenylene group Chemical group 0.000 description 1
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- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical class [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61K31/66—Phosphorus compounds
- A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
-
- 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
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/06—Phosphorus compounds without P—C bonds
- C07F9/062—Organo-phosphoranes without P-C bonds
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361787540P | 2013-03-15 | 2013-03-15 | |
| PCT/US2014/024564 WO2014150925A2 (en) | 2013-03-15 | 2014-03-12 | Deuterated palbociclib |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201591628A1 EA201591628A1 (ru) | 2016-03-31 |
| EA032094B1 true EA032094B1 (ru) | 2019-04-30 |
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| EA201591628A EA032094B1 (ru) | 2013-03-15 | 2014-03-12 | Дейтерированный палбоциклиб |
| EA201892726A EA201892726A1 (ru) | 2013-03-15 | 2014-03-12 | Дейтерированный палбоциклиб |
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| Application Number | Title | Priority Date | Filing Date |
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| EA201892726A EA201892726A1 (ru) | 2013-03-15 | 2014-03-12 | Дейтерированный палбоциклиб |
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| US (3) | US20160024084A1 (enExample) |
| EP (2) | EP2970209B1 (enExample) |
| JP (1) | JP2016512831A (enExample) |
| AU (1) | AU2014235462C1 (enExample) |
| CA (1) | CA2904054A1 (enExample) |
| EA (2) | EA032094B1 (enExample) |
| MX (1) | MX2015012741A (enExample) |
| WO (1) | WO2014150925A2 (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN105294682B (zh) | 2014-07-26 | 2017-07-07 | 广东东阳光药业有限公司 | Cdk类小分子抑制剂的化合物及其用途 |
| CN105111201B (zh) * | 2014-10-16 | 2017-01-11 | 上海页岩科技有限公司 | 5-甲基-2-(吡啶-2-基氨基)-8H-吡啶并[2,3-d]嘧啶-7-酮化合物 |
| WO2016092442A1 (en) * | 2014-12-08 | 2016-06-16 | Sun Pharmaceutical Industries Limited | Processes for the preparation of crystalline forms of palbociclib acetate |
| CN104892604B (zh) * | 2015-06-19 | 2016-08-24 | 北京康立生医药技术开发有限公司 | 一种cdk4抑制剂的合成方法 |
| CN105153149B (zh) * | 2015-07-29 | 2017-09-19 | 江苏中邦制药有限公司 | 一种选择性激酶抑制剂Palbociclib的制备方法 |
| CN108699055B (zh) * | 2015-12-13 | 2020-10-23 | 杭州英创医药科技有限公司 | 用作抗癌药物的杂环化合物 |
| CN106986871B (zh) * | 2017-03-29 | 2019-02-26 | 浙江同源康医药股份有限公司 | 一种氘代Palbociclib的晶型及其制备方法和应用 |
| CN106967064B (zh) * | 2017-03-29 | 2018-03-23 | 郑州泰基鸿诺医药股份有限公司 | 氘代Palbociclib的衍生物、制备方法及其应用 |
| MX2021000895A (es) | 2018-07-27 | 2021-08-24 | California Inst Of Techn | Inhibidores de cinasas dependientes de ciclinas (cdk) y usos de los mismos. |
| CN113166148B (zh) * | 2018-12-07 | 2024-04-12 | 杭州英创医药科技有限公司 | 作为cdk-hdac双通路抑制剂的杂环化合物 |
| WO2021113595A1 (en) * | 2019-12-06 | 2021-06-10 | Beta Pharma, Inc. | Phosphorus derivatives as kras inhibitors |
| LV15575A (lv) | 2019-12-20 | 2021-06-20 | Latvijas Organiskās Sintēzes Institūts | Selenofēnhromēnu deiterēti analogi, to iegūšana un izmantošana |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5304121A (en) | 1990-12-28 | 1994-04-19 | Boston Scientific Corporation | Drug delivery system making use of a hydrogel polymer coating |
| US5716981A (en) | 1993-07-19 | 1998-02-10 | Angiogenesis Technologies, Inc. | Anti-angiogenic compositions and methods of use |
| US6099562A (en) | 1996-06-13 | 2000-08-08 | Schneider (Usa) Inc. | Drug coating with topcoat |
| TW354293B (en) | 1995-06-06 | 1999-03-11 | Bristol Myers Squibb Co | Prodrugs of paclitaxel derivatives |
| GB9925962D0 (en) | 1999-11-02 | 1999-12-29 | Novartis Ag | Organic compounds |
| NZ528689A (en) | 2001-05-03 | 2005-03-24 | F | Pharmaceutical dosage form of amorphous nelfinavir mesylate |
| JP2005503425A (ja) | 2001-05-24 | 2005-02-03 | アレックザ モレキュラー デリヴァリー コーポレイション | 所定の吸入ルートによる薬剤エステルの送出 |
| GEP20063909B (en) * | 2002-01-22 | 2006-08-25 | Warner Lambert Co | 2-(PYRIDIN-2-YLAMINO)-PYRIDO[2,3d] PYRIMIDIN-7-ONES |
| DE602004017474D1 (de) * | 2003-07-11 | 2008-12-11 | Warner Lambert Co | Isethionat salz eines selektiven cdk4 inhibitors |
| WO2006039237A1 (en) | 2004-09-29 | 2006-04-13 | Cordis Corporation | Pharmaceutical dosage forms of stable amorphous rapamycin like compounds |
| WO2007050732A1 (en) | 2005-10-28 | 2007-05-03 | Abbott Laboratories | INDAZOLE DERIVATIVES THAT INHIBIT TRPVl RECEPTOR |
| WO2008032157A2 (en) * | 2006-09-08 | 2008-03-20 | Pfizer Products Inc. | Synthesis of 2-(pyridin-2-ylamino)-pyrido[2,3-d]pyrimidin-7-ones |
| US20080182853A1 (en) | 2006-12-14 | 2008-07-31 | Inna Kruman | Methods of neuroprotection by cyclin-dependent kinase inhibition |
| US20090030005A1 (en) | 2007-07-19 | 2009-01-29 | Amgen Inc. | Combinations for the treatment of cancer |
| US9259399B2 (en) | 2007-11-07 | 2016-02-16 | Cornell University | Targeting CDK4 and CDK6 in cancer therapy |
| JP2011510079A (ja) * | 2008-01-22 | 2011-03-31 | コンサート ファーマシューティカルズ インコーポレイテッド | ゲフィチニブ誘導体 |
| WO2010039997A2 (en) | 2008-10-01 | 2010-04-08 | The University Of North Carolina At Chapel Hill | Hematopoietic protection against chemotherapeutic compounds using selective cyclin-dependent kinase 4/6 inhibitors |
| CA2738909A1 (en) | 2008-10-01 | 2010-05-06 | The University Of North Carolina At Chapel Hill | Hematopoietic protection against ionizing radiation using selective cyclin-dependent kinase 4/6 inhibitors |
| US20120100100A1 (en) | 2009-05-13 | 2012-04-26 | Sharpless Norman E | Cyclin dependent kinase inhibitors and methods of use |
| UY33226A (es) * | 2010-02-19 | 2011-09-30 | Novartis Ag | Compuestos de pirrolopirimidina deuterada como inhibidores de la cdk4/6 |
| KR101830455B1 (ko) | 2010-04-13 | 2018-02-20 | 노파르티스 아게 | 시클린 의존성 키나제 ４ 또는 시클린 의존성 키나제 （ｃｄｋ４／６） 억제제 및 ｍｔｏｒ 억제제를 포함하는 암 치료를 위한 조합물 |
| CN101973989B (zh) * | 2010-05-17 | 2012-07-18 | 苏州波锐生物医药科技有限公司 | 一种噻唑酰胺类化合物及其在治疗恶性肿瘤中的药物用途 |
| WO2012068381A2 (en) | 2010-11-17 | 2012-05-24 | The University Of North Carolina At Chapel Hill | Protection of renal tissues from schema through inhibition of the proliferative kisses cdk4 and cdk6 |
-
2014
- 2014-03-12 CA CA2904054A patent/CA2904054A1/en not_active Abandoned
- 2014-03-12 WO PCT/US2014/024564 patent/WO2014150925A2/en not_active Ceased
- 2014-03-12 US US14/775,854 patent/US20160024084A1/en not_active Abandoned
- 2014-03-12 EP EP14769343.6A patent/EP2970209B1/en active Active
- 2014-03-12 EP EP18205631.7A patent/EP3492470A1/en not_active Withdrawn
- 2014-03-12 JP JP2016501574A patent/JP2016512831A/ja active Pending
- 2014-03-12 EA EA201591628A patent/EA032094B1/ru not_active IP Right Cessation
- 2014-03-12 MX MX2015012741A patent/MX2015012741A/es unknown
- 2014-03-12 AU AU2014235462A patent/AU2014235462C1/en not_active Ceased
- 2014-03-12 EA EA201892726A patent/EA201892726A1/ru unknown
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2017
- 2017-06-29 US US15/636,976 patent/US20180051022A1/en not_active Abandoned
-
2018
- 2018-11-13 US US16/189,304 patent/US20190225605A1/en not_active Abandoned
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| DAVID W. ERY, et al., Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Mole cular Cancer Therapeutics. November 2004, 3(11), pp.1427-1438, see abstract, figure 1 * |
| RICHARD S FINN, et al., PD 0332991, a selective cyclin D kinase 4/6 inhibitor, preferentially inhibits proliferation of luminal estrogen receptor-positive human breast cancer cell lines in vitro. Breast Cancer Research. 2009, 1 5(5):R77. doi: 10.1186/bcr2419, pp.1-13, see abstract * |
Also Published As
| Publication number | Publication date |
|---|---|
| AU2014235462C1 (en) | 2018-11-01 |
| US20190225605A1 (en) | 2019-07-25 |
| AU2014235462A1 (en) | 2015-09-17 |
| AU2014235462B2 (en) | 2018-05-17 |
| EP3492470A1 (en) | 2019-06-05 |
| MX2015012741A (es) | 2016-02-19 |
| US20160024084A1 (en) | 2016-01-28 |
| EA201591628A1 (ru) | 2016-03-31 |
| EA201892726A1 (ru) | 2019-04-30 |
| EP2970209A2 (en) | 2016-01-20 |
| WO2014150925A3 (en) | 2014-12-04 |
| US20180051022A1 (en) | 2018-02-22 |
| WO2014150925A2 (en) | 2014-09-25 |
| JP2016512831A (ja) | 2016-05-09 |
| CA2904054A1 (en) | 2014-09-25 |
| EP2970209A4 (en) | 2016-08-31 |
| EP2970209B1 (en) | 2018-12-26 |
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| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
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