JP2012524731A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2012524731A5 JP2012524731A5 JP2012506333A JP2012506333A JP2012524731A5 JP 2012524731 A5 JP2012524731 A5 JP 2012524731A5 JP 2012506333 A JP2012506333 A JP 2012506333A JP 2012506333 A JP2012506333 A JP 2012506333A JP 2012524731 A5 JP2012524731 A5 JP 2012524731A5
- Authority
- JP
- Japan
- Prior art keywords
- hydrogen
- compound according
- triazin
- pharmaceutically acceptable
- acceptable salt
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- -1 1,3-oxazol-2-yl Chemical group 0.000 claims description 76
- 150000001875 compounds Chemical class 0.000 claims description 49
- 230000003287 optical effect Effects 0.000 claims description 48
- 229910052739 hydrogen Inorganic materials 0.000 claims description 34
- 239000001257 hydrogen Substances 0.000 claims description 34
- 239000000203 mixture Substances 0.000 claims description 34
- 150000003839 salts Chemical class 0.000 claims description 24
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 22
- 206010028980 Neoplasm Diseases 0.000 claims description 20
- 239000003814 drug Substances 0.000 claims description 12
- 150000002431 hydrogen Chemical class 0.000 claims description 12
- 235000011178 triphosphate Nutrition 0.000 claims description 12
- 239000001226 triphosphate Substances 0.000 claims description 12
- UNXRWKVEANCORM-UHFFFAOYSA-N triphosphoric acid Chemical compound OP(O)(=O)OP(O)(=O)OP(O)(O)=O UNXRWKVEANCORM-UHFFFAOYSA-N 0.000 claims description 12
- 125000004414 alkyl thio group Chemical group 0.000 claims description 10
- 229910052736 halogen Chemical group 0.000 claims description 10
- 150000002367 halogens Chemical group 0.000 claims description 10
- 125000001072 heteroaryl group Chemical group 0.000 claims description 10
- 125000001424 substituent group Chemical group 0.000 claims description 10
- 125000001766 1,2,4-oxadiazol-3-yl group Chemical group [H]C1=NC(*)=NO1 0.000 claims description 8
- 125000002941 2-furyl group Chemical group O1C([*])=C([H])C([H])=C1[H] 0.000 claims description 8
- 125000003118 aryl group Chemical group 0.000 claims description 8
- 201000011510 cancer Diseases 0.000 claims description 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 8
- 125000003545 alkoxy group Chemical group 0.000 claims description 6
- 125000000217 alkyl group Chemical group 0.000 claims description 6
- 230000002401 inhibitory effect Effects 0.000 claims description 6
- 230000005907 cancer growth Effects 0.000 claims description 5
- 201000010099 disease Diseases 0.000 claims description 5
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 4
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims description 4
- 125000000304 alkynyl group Chemical group 0.000 claims description 4
- 239000012627 chemopreventive agent Substances 0.000 claims description 4
- 229940124443 chemopreventive agent Drugs 0.000 claims description 4
- 239000003937 drug carrier Substances 0.000 claims description 4
- 230000001613 neoplastic effect Effects 0.000 claims description 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 4
- 230000002062 proliferating effect Effects 0.000 claims description 4
- 230000004614 tumor growth Effects 0.000 claims description 4
- 230000004663 cell proliferation Effects 0.000 claims description 3
- 239000008194 pharmaceutical composition Substances 0.000 claims description 3
- 102000004127 Cytokines Human genes 0.000 claims description 2
- 108090000695 Cytokines Proteins 0.000 claims description 2
- 239000012625 DNA intercalator Substances 0.000 claims description 2
- 229940123780 DNA topoisomerase I inhibitor Drugs 0.000 claims description 2
- 229940124087 DNA topoisomerase II inhibitor Drugs 0.000 claims description 2
- 101000904173 Homo sapiens Progonadoliberin-1 Proteins 0.000 claims description 2
- 102100024028 Progonadoliberin-1 Human genes 0.000 claims description 2
- 101000996723 Sus scrofa Gonadotropin-releasing hormone receptor Proteins 0.000 claims description 2
- 239000000365 Topoisomerase I Inhibitor Substances 0.000 claims description 2
- 239000000317 Topoisomerase II Inhibitor Substances 0.000 claims description 2
- 239000000556 agonist Substances 0.000 claims description 2
- 229930013930 alkaloid Natural products 0.000 claims description 2
- 150000003797 alkaloid derivatives Chemical class 0.000 claims description 2
- 229940100198 alkylating agent Drugs 0.000 claims description 2
- 239000002168 alkylating agent Substances 0.000 claims description 2
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 claims description 2
- 239000002870 angiogenesis inducing agent Substances 0.000 claims description 2
- 239000005557 antagonist Substances 0.000 claims description 2
- 229940045799 anthracyclines and related substance Drugs 0.000 claims description 2
- 230000002280 anti-androgenic effect Effects 0.000 claims description 2
- 230000001772 anti-angiogenic effect Effects 0.000 claims description 2
- 239000000051 antiandrogen Substances 0.000 claims description 2
- 229940030495 antiandrogen sex hormone and modulator of the genital system Drugs 0.000 claims description 2
- 239000003080 antimitotic agent Substances 0.000 claims description 2
- 229940034982 antineoplastic agent Drugs 0.000 claims description 2
- 239000002246 antineoplastic agent Substances 0.000 claims description 2
- 239000003886 aromatase inhibitor Substances 0.000 claims description 2
- 229940046844 aromatase inhibitors Drugs 0.000 claims description 2
- 230000022131 cell cycle Effects 0.000 claims description 2
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 claims description 2
- XLXSAKCOAKORKW-UHFFFAOYSA-N gonadorelin Chemical compound C1CCC(C(=O)NCC(N)=O)N1C(=O)C(CCCN=C(N)N)NC(=O)C(CC(C)C)NC(=O)CNC(=O)C(NC(=O)C(CO)NC(=O)C(CC=1C2=CC=CC=C2NC=1)NC(=O)C(CC=1NC=NC=1)NC(=O)C1NC(=O)CC1)CC1=CC=C(O)C=C1 XLXSAKCOAKORKW-UHFFFAOYSA-N 0.000 claims description 2
- 239000003102 growth factor Substances 0.000 claims description 2
- 239000003112 inhibitor Substances 0.000 claims description 2
- 229940124597 therapeutic agent Drugs 0.000 claims description 2
- 230000010261 cell growth Effects 0.000 claims 1
- 230000001413 cellular effect Effects 0.000 claims 1
- 229940125697 hormonal agent Drugs 0.000 claims 1
- 239000002777 nucleoside Substances 0.000 claims 1
- 150000003833 nucleoside derivatives Chemical class 0.000 claims 1
- 238000000034 method Methods 0.000 description 6
- 0 *C1(C([n]2c3ncnc(N)c3c(*)c2)OC(CO)C1O)O Chemical compound *C1(C([n]2c3ncnc(N)c3c(*)c2)OC(CO)C1O)O 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 1
- 229940088597 hormone Drugs 0.000 description 1
- 239000005556 hormone Substances 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 229940127073 nucleoside analogue Drugs 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US17165609P | 2009-04-22 | 2009-04-22 | |
| US61/171,656 | 2009-04-22 | ||
| PCT/CZ2010/000050 WO2010121576A2 (en) | 2009-04-22 | 2010-04-19 | Novel 7-deazapurine nucleosides for therapeutic uses |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014213410A Division JP6087889B2 (ja) | 2009-04-22 | 2014-10-20 | 治療的使用のための新規７−デアザプリンヌクレオシド |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2012524731A JP2012524731A (ja) | 2012-10-18 |
| JP2012524731A5 true JP2012524731A5 (https=) | 2013-05-30 |
| JP5721275B2 JP5721275B2 (ja) | 2015-05-20 |
Family
ID=42768153
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012506333A Active JP5721275B2 (ja) | 2009-04-22 | 2010-04-19 | 治療的使用のための新規７−デアザプリンヌクレオシド |
| JP2014213410A Active JP6087889B2 (ja) | 2009-04-22 | 2014-10-20 | 治療的使用のための新規７−デアザプリンヌクレオシド |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014213410A Active JP6087889B2 (ja) | 2009-04-22 | 2014-10-20 | 治療的使用のための新規７−デアザプリンヌクレオシド |
Country Status (15)
| Country | Link |
|---|---|
| US (3) | US9321800B2 (https=) |
| EP (1) | EP2421879B1 (https=) |
| JP (2) | JP5721275B2 (https=) |
| CN (2) | CN104497084B (https=) |
| AU (3) | AU2010238985B2 (https=) |
| CA (2) | CA2759131C (https=) |
| DK (1) | DK2421879T3 (https=) |
| ES (1) | ES2437917T3 (https=) |
| HR (1) | HRP20131021T1 (https=) |
| MX (1) | MX2011011160A (https=) |
| NZ (2) | NZ700583A (https=) |
| PL (1) | PL2421879T3 (https=) |
| PT (1) | PT2421879E (https=) |
| SI (1) | SI2421879T1 (https=) |
| WO (1) | WO2010121576A2 (https=) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT2421879E (pt) * | 2009-04-22 | 2013-12-09 | Acad Of Science Czech Republic | Novos 7-deazapurina nucleósidos para utilizações terapêuticas |
| KR20120113228A (ko) * | 2009-12-18 | 2012-10-12 | 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 | 베타 세포 복제 촉진 화합물 및 그 사용 방법 |
| CN102319254B (zh) * | 2011-07-20 | 2013-06-19 | 上海交通大学 | 5-碘代杀菌核素在制备抗肿瘤药物中的应用 |
| CZ305466B6 (cs) * | 2013-11-04 | 2015-10-14 | Ústav organické chemie a biochemie Akademie věd České republiky, v. v. i. | Substituované 7-deazapurinové ribonukleosidy pro terapeutické použití |
| KR102562866B1 (ko) | 2014-11-14 | 2023-08-04 | 네르비아노 메디칼 사이언시스 에스.알.엘. | 단백질 키나아제 억제제로서의 6-아미노-7-바이사이클로-7-데아자-퓨린 유도체 |
| EP3454856B1 (en) | 2016-05-10 | 2024-09-11 | C4 Therapeutics, Inc. | Heterocyclic degronimers for target protein degradation |
| CN109790143A (zh) | 2016-05-10 | 2019-05-21 | C4医药公司 | 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体 |
| ES2990061T3 (es) | 2016-05-10 | 2024-11-28 | C4 Therapeutics Inc | Degronímeros espirocíclicos para la degradación de proteínas diana |
| CN109641874A (zh) | 2016-05-10 | 2019-04-16 | C4医药公司 | 用于靶蛋白降解的c3-碳连接的戊二酰亚胺降解决定子体 |
| CA3029170C (en) | 2016-06-29 | 2021-02-16 | Ustav Organicke Chemie A Biochemie Av Cr, V.V.I. | Substituted thienopyrrolopyrimidine ribonucleosides for therapeutic use |
| CZ307334B6 (cs) | 2016-08-02 | 2018-06-13 | Ăšstav organickĂ© chemie a biochemie AV ÄŚR, v.v.i. | Substituované heteropentadieno-pyrrolopyrimidinové ribonukleosidy pro terapeutické použití |
| WO2018136661A1 (en) | 2017-01-18 | 2018-07-26 | Andrews Steven W | SUBSTITUTED PYRAZOLO[1,5-a]PYRAZINE COMPOUNDS AS RET KINASE INHIBITORS |
| CN110769822A (zh) | 2017-06-20 | 2020-02-07 | C4医药公司 | 用于蛋白降解的n/o-连接的降解决定子和降解决定子体 |
| EP3697800A1 (en) | 2017-10-19 | 2020-08-26 | Universiteit Gent | Nucleoside analogues for the treatment of parasitic infections |
| EP3740490A1 (en) | 2018-01-18 | 2020-11-25 | Array Biopharma, Inc. | Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors |
| JP7060694B2 (ja) * | 2018-01-18 | 2022-04-26 | アレイ バイオファーマ インコーポレイテッド | Ｒｅｔキナーゼ阻害剤としての置換ピロロ［２，３－ｄ］ピリミジン化合物 |
| US11472802B2 (en) | 2018-01-18 | 2022-10-18 | Array Biopharma Inc. | Substituted pyrazolyl[4,3-c]pyridine compounds as RET kinase inhibitors |
| CZ308104B6 (cs) | 2018-03-12 | 2020-01-08 | Ăšstav organickĂ© chemie a biochemie AV ÄŚR, v. v. i. | Pyridinopyrrolopyrimidinové ribonukleosidy pro terapeutické použití |
| US12173026B2 (en) | 2018-08-07 | 2024-12-24 | Merck Sharp & Dohme Llc | PRMT5 inhibitors |
| CN112996794A (zh) | 2018-09-10 | 2021-06-18 | 阿雷生物药品公司 | 作为ret激酶抑制剂的稠合杂环化合物 |
| CN114008064A (zh) * | 2019-06-18 | 2022-02-01 | 大鹏药品工业株式会社 | 具有吡咯并嘧啶骨架的新型的磷酸酯化合物或其药学上可接受的盐 |
| CN115515593A (zh) * | 2020-02-17 | 2022-12-23 | 勒芬天主教大学 | 作为药物的新的6-取代的7-脱氮嘌呤和相应的核苷 |
| KR102639275B1 (ko) * | 2021-06-08 | 2024-02-21 | 퓨쳐메디신 주식회사 | 다중 표적 인산화효소 저해 활성을 갖는 뉴클레오사이드 유도체 및 이를 포함하는 암의 예방 및 치료용 약학적 조성물 |
| CN118355022A (zh) | 2021-09-28 | 2024-07-16 | 安特卫普大学 | 用于治疗寄生虫感染的核苷类似物 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL108523A0 (en) * | 1993-02-03 | 1994-05-30 | Gensia Inc | Pharmaceutical compositions containing adenosine kinase inhibitors for preventing or treating conditions involving inflammatory responses and pain |
| SK286630B6 (sk) * | 2001-01-22 | 2009-02-05 | Merck & Co., Inc. | Nukleozidové deriváty, farmaceutický prostriedok s ich obsahom a ich použitie |
| WO2003051899A1 (en) * | 2001-12-17 | 2003-06-26 | Ribapharm Inc. | Deazapurine nucleoside libraries and compounds |
| US20040063658A1 (en) * | 2002-05-06 | 2004-04-01 | Roberts Christopher Don | Nucleoside derivatives for treating hepatitis C virus infection |
| US20040157892A1 (en) | 2003-02-12 | 2004-08-12 | Crompton Co./Cie | Pesticidal fluoroethyl pyrazoles |
| CA2542776A1 (en) * | 2003-10-27 | 2005-05-12 | Genelabs Technologies, Inc. | Nucleoside compounds for treating viral infections |
| US7202223B2 (en) * | 2003-10-27 | 2007-04-10 | Genelabs Technologies, Inc. | Nucleoside compounds for treating viral infections |
| CA2543116A1 (en) * | 2003-10-27 | 2005-05-19 | Genelabs Technologies, Inc. | Methods for preparing 7-(2'-substituted-.szlig.-d-ribofuranosyl)-4-(nr2r3)-5-(substituted ethyn-1-yl)-pyrrolo[2,3-d]pyrimidine derivatives |
| WO2006033709A2 (en) * | 2004-07-29 | 2006-03-30 | Metabasis Therapeutics, Inc. | Novel nucleoside derivatives |
| PT2231689T (pt) * | 2008-01-18 | 2016-10-07 | Inst Of Organic Chemistry And Biochemistry Of The Acad Of Sciences Of The Czech Republic | Novos nucleósidos 7-deazapurina citostáticos |
| MX2010014501A (es) * | 2008-06-23 | 2011-02-25 | Janssen Pharmaceutica Nv | Antagonistas de piperidil acrilamida de receptor 2 de citocina quimioatrayente. |
| GB0815968D0 (en) * | 2008-09-03 | 2008-10-08 | Angeletti P Ist Richerche Bio | Antiviral agents |
| PT2421879E (pt) * | 2009-04-22 | 2013-12-09 | Acad Of Science Czech Republic | Novos 7-deazapurina nucleósidos para utilizações terapêuticas |
-
2010
- 2010-04-19 PT PT107344335T patent/PT2421879E/pt unknown
- 2010-04-19 EP EP10734433.5A patent/EP2421879B1/en active Active
- 2010-04-19 JP JP2012506333A patent/JP5721275B2/ja active Active
- 2010-04-19 SI SI201030450T patent/SI2421879T1/sl unknown
- 2010-04-19 ES ES10734433.5T patent/ES2437917T3/es active Active
- 2010-04-19 CN CN201410643709.3A patent/CN104497084B/zh active Active
- 2010-04-19 WO PCT/CZ2010/000050 patent/WO2010121576A2/en not_active Ceased
- 2010-04-19 DK DK10734433.5T patent/DK2421879T3/da active
- 2010-04-19 CA CA2759131A patent/CA2759131C/en active Active
- 2010-04-19 CN CN201080027802.1A patent/CN102459300B/zh active Active
- 2010-04-19 NZ NZ700583A patent/NZ700583A/en active IP Right Revival
- 2010-04-19 NZ NZ596301A patent/NZ596301A/en unknown
- 2010-04-19 HR HRP20131021AT patent/HRP20131021T1/hr unknown
- 2010-04-19 CA CA2966647A patent/CA2966647A1/en not_active Abandoned
- 2010-04-19 AU AU2010238985A patent/AU2010238985B2/en active Active
- 2010-04-19 MX MX2011011160A patent/MX2011011160A/es active IP Right Grant
- 2010-04-19 PL PL10734433T patent/PL2421879T3/pl unknown
- 2010-04-19 US US14/394,262 patent/US9321800B2/en active Active
-
2014
- 2014-10-20 JP JP2014213410A patent/JP6087889B2/ja active Active
-
2015
- 2015-07-22 AU AU2015205885A patent/AU2015205885B2/en active Active
-
2016
- 2016-03-17 US US15/073,502 patent/US9624257B2/en active Active
-
2017
- 2017-03-08 US US15/453,702 patent/US10294262B2/en active Active
- 2017-06-19 AU AU2017204148A patent/AU2017204148B2/en active Active
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2012524731A5 (https=) | ||
| CN105683166B (zh) | 取代的嘧啶Bmi-1抑制剂 | |
| CN111423417B (zh) | 取代的反向嘧啶Bmi-1抑制剂 | |
| JP2007529421A5 (https=) | ||
| JP2008535902A5 (https=) | ||
| JP2017528498A5 (https=) | ||
| JP2011509949A5 (https=) | ||
| JP2017528524A5 (https=) | ||
| JP2001522842A5 (https=) | ||
| JP2014518266A5 (https=) | ||
| US12350265B2 (en) | Pharmaceutical composition for treating acute myeloid leukemia, containing FLT3 inhibitor and chemotherapeutic agents | |
| JP2016513737A5 (https=) | ||
| JP2020506951A5 (https=) | ||
| JP2013501731A5 (https=) | ||
| JP2009538897A5 (https=) | ||
| JP2021530487A5 (https=) | ||
| JP2019501197A5 (ja) | 腫瘍を処置するための抗ｈｅｒ２組み合わせ | |
| JP2006506443A5 (https=) | ||
| JP2011526917A5 (https=) | ||
| JP2017535600A5 (https=) | ||
| JP2014144962A5 (https=) | ||
| JP2018525425A5 (https=) | ||
| SI3174881T1 (en) | (1,2,4) triazolo (4,3-B) pyridazines for use in the treatment of proliferative diseases | |
| RU2015101702A (ru) | Фармацевтически активные соединения | |
| AU2012336154B2 (en) | Combination therapy for ovarian cancer |