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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- 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 |
|---|---|---|---|
| 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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| EA201892726A EA201892726A1 (ru) | 2013-03-15 | 2014-03-12 | Дейтерированный палбоциклиб |
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|---|---|
| US (3) | US20160024084A1 (OSRAM) |
| EP (2) | EP2970209B1 (OSRAM) |
| JP (1) | JP2016512831A (OSRAM) |
| AU (1) | AU2014235462C1 (OSRAM) |
| CA (1) | CA2904054A1 (OSRAM) |
| EA (2) | EA032094B1 (OSRAM) |
| MX (1) | MX2015012741A (OSRAM) |
| WO (1) | WO2014150925A2 (OSRAM) |
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| AU2015296322B2 (en) | 2014-07-26 | 2019-09-19 | Sunshine Lake Pharma Co., Ltd. | 2-amino-pyrido[2,3-d]pyrimidin-7(8h)-one derivatives as CDK inhibitors and uses thereof |
| 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 |
| SG11202100429TA (en) | 2018-07-27 | 2021-02-25 | California Inst Of Techn | Cdk inhibitors and uses thereof |
| WO2020114519A1 (zh) * | 2018-12-07 | 2020-06-11 | 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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| 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 |
| CN1255185C (zh) | 2001-05-03 | 2006-05-10 | 弗·哈夫曼-拉罗切有限公司 | 无定形甲磺酸奈非那韦的药物剂型 |
| CA2446904A1 (en) | 2001-05-24 | 2003-04-03 | Alexza Molecular Delivery Corporation | Delivery of drug esters through an inhalation route |
| JP4291696B2 (ja) * | 2002-01-22 | 2009-07-08 | ワーナー−ランバート カンパニー リミテッド ライアビリティー カンパニー | ２−（ピリジン−２−イルアミノ）−ピリド［２，３−ｄ］ピリミジン−７−オン |
| JP4053073B2 (ja) * | 2003-07-11 | 2008-02-27 | ワーナー−ランバート カンパニー リミテッド ライアビリティー カンパニー | 選択的ｃｄｋ４阻害剤のイセチオン酸塩 |
| WO2006039237A1 (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 |
| AU2007297286A1 (en) * | 2006-09-08 | 2008-03-20 | Pfizer Products Inc. | Synthesis of 2-(pyridin-2-ylamino)-pyrido[2,3-d]pyrimidin-7-ones |
| JP2010513317A (ja) | 2006-12-14 | 2010-04-30 | パナシー ファーマシューティカルズ インコーポレーティッド | サイクリン依存性キナーゼの阻害による神経保護方法 |
| 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 |
| EP2242493B1 (en) * | 2008-01-22 | 2013-06-05 | Concert Pharmaceuticals Inc. | Derivatives of gefitinib |
| CA2738925A1 (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 |
| 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 |
| EP3718560A3 (en) | 2009-05-13 | 2020-12-09 | 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 |
| US20130035336A1 (en) | 2010-04-13 | 2013-02-07 | Novartis Ag | Combination comprising a cyclin dependent kinase 4 or cyclin dependent kinase (cdk4/6) inhibitor for treating cancer |
| CN101967142B (zh) * | 2010-05-17 | 2012-05-30 | 苏州波锐生物医药科技有限公司 | 噻唑酰胺类化合物及其在治疗恶性肿瘤中的药物用途 |
| US9808461B2 (en) | 2010-11-17 | 2017-11-07 | The University Of North Carolina At Chapel Hill | Protection of renal tissues from ischemia through inhibition of the proliferative kinases CDK4 and CDK6 |
-
2014
- 2014-03-12 JP JP2016501574A patent/JP2016512831A/ja active Pending
- 2014-03-12 WO PCT/US2014/024564 patent/WO2014150925A2/en not_active Ceased
- 2014-03-12 EP EP14769343.6A patent/EP2970209B1/en active Active
- 2014-03-12 MX MX2015012741A patent/MX2015012741A/es unknown
- 2014-03-12 EA EA201591628A patent/EA032094B1/ru not_active IP Right Cessation
- 2014-03-12 EA EA201892726A patent/EA201892726A1/ru unknown
- 2014-03-12 AU AU2014235462A patent/AU2014235462C1/en not_active Ceased
- 2014-03-12 CA CA2904054A patent/CA2904054A1/en not_active Abandoned
- 2014-03-12 US US14/775,854 patent/US20160024084A1/en not_active Abandoned
- 2014-03-12 EP EP18205631.7A patent/EP3492470A1/en not_active Withdrawn
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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 |
|---|---|
| EP2970209A2 (en) | 2016-01-20 |
| AU2014235462C1 (en) | 2018-11-01 |
| US20190225605A1 (en) | 2019-07-25 |
| WO2014150925A2 (en) | 2014-09-25 |
| EA201892726A1 (ru) | 2019-04-30 |
| EP2970209A4 (en) | 2016-08-31 |
| MX2015012741A (es) | 2016-02-19 |
| EP3492470A1 (en) | 2019-06-05 |
| US20180051022A1 (en) | 2018-02-22 |
| EP2970209B1 (en) | 2018-12-26 |
| EA201591628A1 (ru) | 2016-03-31 |
| WO2014150925A3 (en) | 2014-12-04 |
| AU2014235462B2 (en) | 2018-05-17 |
| AU2014235462A1 (en) | 2015-09-17 |
| CA2904054A1 (en) | 2014-09-25 |
| US20160024084A1 (en) | 2016-01-28 |
| JP2016512831A (ja) | 2016-05-09 |
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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 |