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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- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
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- 230000000699 topical effect Effects 0.000 description 1
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- 125000005580 triphenylene group Chemical group 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)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (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)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
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| 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 |
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| 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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| EA201892726A EA201892726A1 (ru) | 2013-03-15 | 2014-03-12 | Дейтерированный палбоциклиб |
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|---|---|
| US (3) | US20160024084A1 (enExample) |
| EP (2) | EP3492470A1 (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) |
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| KR20170032244A (ko) | 2014-07-26 | 2017-03-22 | 선샤인 레이크 파르마 컴퍼니 리미티드 | Cdk 저해제로서 2-아미노-피리도[2,3-d]피리미딘-7(8h)-온 유도체 및 그 용도 |
| 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 |
| EP3386981B1 (en) * | 2015-12-13 | 2021-10-13 | Hangzhou Innogate Pharma Co., Ltd. | Heterocycles useful as anti-cancer agents |
| 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. |
| US12358911B2 (en) | 2018-12-07 | 2025-07-15 | Hangzhou Innogate Pharma Co., Ltd. | Heterocyclic comipound as CDK-HDAC dual pathway inhibitor |
| 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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| US5304121A (en) | 1990-12-28 | 1994-04-19 | Boston Scientific Corporation | Drug delivery system making use of a hydrogel polymer coating |
| US5994341A (en) | 1993-07-19 | 1999-11-30 | Angiogenesis Technologies, Inc. | Anti-angiogenic Compositions and methods for the treatment of arthritis |
| 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 |
| EP1390063B1 (en) | 2001-05-03 | 2004-11-17 | F. Hoffmann-La Roche Ag | Pharmaceutical dosage form of amorphous nelfinavir mesylate |
| CA2446904A1 (en) | 2001-05-24 | 2003-04-03 | Alexza Molecular Delivery Corporation | Delivery of drug esters through an inhalation route |
| DK1470124T3 (da) * | 2002-01-22 | 2006-04-18 | Warner Lambert Co | 2-(Pyridin-2-yl amino)-pyrido[2,3]pyrimidin-7-oner |
| WO2005005426A1 (en) * | 2003-07-11 | 2005-01-20 | Warner-Lambert Company Llc | Isethionate salt of a selective cdk4 inhibitor |
| CA2581169A1 (en) | 2004-09-29 | 2006-04-13 | Cordis Corporation | Pharmaceutical dosage forms of stable amorphous rapamycin like compounds |
| CN102516176A (zh) | 2005-10-28 | 2012-06-27 | 雅培制药有限公司 | 抑制trpv1受体的吲唑衍生物 |
| KR20090052385A (ko) * | 2006-09-08 | 2009-05-25 | 화이자 프로덕츠 인크. | 2-（피리딘-2-일아미노）-피리도［2,3-ｄ］피리미딘-7-온의합성 |
| 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 |
| WO2009061345A2 (en) | 2007-11-07 | 2009-05-14 | Cornell Research Foundation, Inc. | Targeting cdk4 and cdk6 in cancer therapy |
| US7855204B2 (en) * | 2008-01-22 | 2010-12-21 | Concert Pharmaceuticals Inc. | Derivatives of gefitinib |
| JP2012504645A (ja) | 2008-10-01 | 2012-02-23 | ザ ユニバーシティ オブ ノース カロライナ アット チャペル ヒル | 健康な細胞に対する電離放射線の影響を低下させる又は防止するための医薬組成物 |
| CN102231984A (zh) | 2008-10-01 | 2011-11-02 | 北卡罗来纳大学查珀尔希尔分校 | 使用选择性细胞周期蛋白依赖性激酶4/6抑制剂对抗化疗化合物的造血防护 |
| WO2010132725A2 (en) | 2009-05-13 | 2010-11-18 | The University Of North Carolina At Chapel Hill | 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 |
| ES2689177T3 (es) | 2010-04-13 | 2018-11-08 | Novartis Ag | Combinación que comprende un inhibidor de cinasa 4 dependiente de ciclina o cinasa dependiente de ciclina (CDK4/6) y un inhibidor de mTOR para tratar cáncer |
| 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 |
| CN103501789A (zh) | 2010-11-17 | 2014-01-08 | 北卡罗来纳大学查珀尔希尔分校 | 通过抑制增殖性激酶cdk4和cdk6保护肾组织免于局部缺血 |
-
2014
- 2014-03-12 EP EP18205631.7A patent/EP3492470A1/en not_active Withdrawn
- 2014-03-12 CA CA2904054A patent/CA2904054A1/en not_active Abandoned
- 2014-03-12 AU AU2014235462A patent/AU2014235462C1/en not_active Ceased
- 2014-03-12 WO PCT/US2014/024564 patent/WO2014150925A2/en not_active Ceased
- 2014-03-12 EA EA201591628A patent/EA032094B1/ru not_active IP Right Cessation
- 2014-03-12 JP JP2016501574A patent/JP2016512831A/ja active Pending
- 2014-03-12 MX MX2015012741A patent/MX2015012741A/es unknown
- 2014-03-12 EA EA201892726A patent/EA201892726A1/ru unknown
- 2014-03-12 US US14/775,854 patent/US20160024084A1/en not_active Abandoned
- 2014-03-12 EP EP14769343.6A patent/EP2970209B1/en active Active
-
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 |
|---|---|
| EP2970209A4 (en) | 2016-08-31 |
| AU2014235462B2 (en) | 2018-05-17 |
| EP3492470A1 (en) | 2019-06-05 |
| CA2904054A1 (en) | 2014-09-25 |
| US20180051022A1 (en) | 2018-02-22 |
| EP2970209A2 (en) | 2016-01-20 |
| US20160024084A1 (en) | 2016-01-28 |
| AU2014235462A1 (en) | 2015-09-17 |
| WO2014150925A3 (en) | 2014-12-04 |
| MX2015012741A (es) | 2016-02-19 |
| US20190225605A1 (en) | 2019-07-25 |
| AU2014235462C1 (en) | 2018-11-01 |
| EA201892726A1 (ru) | 2019-04-30 |
| EP2970209B1 (en) | 2018-12-26 |
| WO2014150925A2 (en) | 2014-09-25 |
| JP2016512831A (ja) | 2016-05-09 |
| EA201591628A1 (ru) | 2016-03-31 |
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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) |
Designated state(s): AM AZ BY KZ KG TJ TM RU |