JP2012531456A5 - - Google Patents
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- Publication number
- JP2012531456A5 JP2012531456A5 JP2012518092A JP2012518092A JP2012531456A5 JP 2012531456 A5 JP2012531456 A5 JP 2012531456A5 JP 2012518092 A JP2012518092 A JP 2012518092A JP 2012518092 A JP2012518092 A JP 2012518092A JP 2012531456 A5 JP2012531456 A5 JP 2012531456A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- amide
- methyl
- dicarboxylic acid
- pyrrolidine
- 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.)
- Pending
Links
- 150000001875 compounds Chemical class 0.000 claims description 18
- 108091007960 PI3Ks Proteins 0.000 claims description 13
- 239000003814 drug Substances 0.000 claims description 3
- 239000008194 pharmaceutical composition Substances 0.000 claims description 3
- 239000004480 active ingredient Substances 0.000 claims description 2
- 230000005764 inhibitory process Effects 0.000 claims description 2
- 206010028980 Neoplasm Diseases 0.000 claims 14
- 102000038030 PI3Ks Human genes 0.000 claims 12
- -1 2-tert-butyl-pyrimidin-4-yl Chemical group 0.000 claims 11
- 201000010099 disease Diseases 0.000 claims 11
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 11
- 229910052736 halogen Inorganic materials 0.000 claims 9
- 150000002367 halogens Chemical class 0.000 claims 9
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 150000002632 lipids Chemical class 0.000 claims 7
- LFEUADMCDRWDRA-UHNVWZDZSA-N (2s,3r)-3-methylpyrrolidine-1,2-dicarboxylic acid Chemical compound C[C@@H]1CCN(C(O)=O)[C@@H]1C(O)=O LFEUADMCDRWDRA-UHNVWZDZSA-N 0.000 claims 6
- 201000011510 cancer Diseases 0.000 claims 6
- 230000001419 dependent effect Effects 0.000 claims 6
- 108091000080 Phosphotransferase Proteins 0.000 claims 4
- 210000004556 brain Anatomy 0.000 claims 4
- 208000035269 cancer or benign tumor Diseases 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 201000001441 melanoma Diseases 0.000 claims 4
- 102000020233 phosphotransferase Human genes 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- 210000002784 stomach Anatomy 0.000 claims 4
- 102000001253 Protein Kinase Human genes 0.000 claims 3
- 239000003795 chemical substances by application Substances 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 125000001475 halogen functional group Chemical group 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 108060006633 protein kinase Proteins 0.000 claims 3
- TVWSZMXMMPFCMN-IUCAKERBSA-N (2S,3S)-3-(morpholin-4-ylmethyl)pyrrolidine-1,2-dicarboxylic acid Chemical compound N1(CCOCC1)C[C@H]1[C@H](N(CC1)C(=O)O)C(=O)O TVWSZMXMMPFCMN-IUCAKERBSA-N 0.000 claims 2
- NMKJZOUSNLUCPS-UHFFFAOYSA-N 3,3-dimethylpyrrolidine-1,2-dicarboxylic acid Chemical compound CC1(C(N(CC1)C(=O)O)C(=O)O)C NMKJZOUSNLUCPS-UHFFFAOYSA-N 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 2
- 208000003200 Adenoma Diseases 0.000 claims 2
- 206010001233 Adenoma benign Diseases 0.000 claims 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
- 206010004146 Basal cell carcinoma Diseases 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- HYZWWZBFPUNNHZ-BQBZGAKWSA-N C(C)(=O)NC[C@H]1[C@H](N(CC1)C(=O)O)C(=O)O Chemical compound C(C)(=O)NC[C@H]1[C@H](N(CC1)C(=O)O)C(=O)O HYZWWZBFPUNNHZ-BQBZGAKWSA-N 0.000 claims 2
- 201000009030 Carcinoma Diseases 0.000 claims 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 2
- 208000012609 Cowden disease Diseases 0.000 claims 2
- 201000002847 Cowden syndrome Diseases 0.000 claims 2
- 208000032027 Essential Thrombocythemia Diseases 0.000 claims 2
- 208000032612 Glial tumor Diseases 0.000 claims 2
- 206010018338 Glioma Diseases 0.000 claims 2
- 208000028018 Lymphocytic leukaemia Diseases 0.000 claims 2
- 206010025323 Lymphomas Diseases 0.000 claims 2
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 2
- 208000008770 Multiple Hamartoma Syndrome Diseases 0.000 claims 2
- 208000034578 Multiple myelomas Diseases 0.000 claims 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 2
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- 206010039491 Sarcoma Diseases 0.000 claims 2
- 208000017733 acquired polycythemia vera Diseases 0.000 claims 2
- 208000009621 actinic keratosis Diseases 0.000 claims 2
- 210000004100 adrenal gland Anatomy 0.000 claims 2
- 210000001185 bone marrow Anatomy 0.000 claims 2
- 210000000481 breast Anatomy 0.000 claims 2
- 210000000621 bronchi Anatomy 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 210000003679 cervix uteri Anatomy 0.000 claims 2
- 210000001072 colon Anatomy 0.000 claims 2
- 201000002758 colorectal adenoma Diseases 0.000 claims 2
- 210000004696 endometrium Anatomy 0.000 claims 2
- 210000003238 esophagus Anatomy 0.000 claims 2
- 208000005017 glioblastoma Diseases 0.000 claims 2
- 210000003494 hepatocyte Anatomy 0.000 claims 2
- 210000003228 intrahepatic bile duct Anatomy 0.000 claims 2
- 208000032839 leukemia Diseases 0.000 claims 2
- 210000004185 liver Anatomy 0.000 claims 2
- 210000004072 lung Anatomy 0.000 claims 2
- 208000003747 lymphoid leukemia Diseases 0.000 claims 2
- 206010028537 myelofibrosis Diseases 0.000 claims 2
- 208000025113 myeloid leukemia Diseases 0.000 claims 2
- 210000004798 organs belonging to the digestive system Anatomy 0.000 claims 2
- 210000001672 ovary Anatomy 0.000 claims 2
- 210000000496 pancreas Anatomy 0.000 claims 2
- 208000037244 polycythemia vera Diseases 0.000 claims 2
- 210000002307 prostate Anatomy 0.000 claims 2
- 201000010700 sporadic breast cancer Diseases 0.000 claims 2
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 2
- 125000000335 thiazolyl group Chemical group 0.000 claims 2
- 210000001685 thyroid gland Anatomy 0.000 claims 2
- 210000004291 uterus Anatomy 0.000 claims 2
- 210000001215 vagina Anatomy 0.000 claims 2
- ZXNDWVDSVLPGNK-WDCZJNDASA-N (1r,2s,5s)-3-azabicyclo[3.1.0]hexane-2,3-dicarboxylic acid Chemical compound C1N(C(O)=O)[C@H](C(=O)O)[C@@H]2C[C@@H]21 ZXNDWVDSVLPGNK-WDCZJNDASA-N 0.000 claims 1
- WKVGKBOIHYVALB-WDSKDSINSA-N (2S,3R)-3-(methoxymethyl)pyrrolidine-1,2-dicarboxylic acid Chemical compound COC[C@@H]1CCN([C@@H]1C(O)=O)C(O)=O WKVGKBOIHYVALB-WDSKDSINSA-N 0.000 claims 1
- VDCGXJHBHIABJG-BQBZGAKWSA-N (2S,3S)-3-[(dimethylamino)methyl]pyrrolidine-1,2-dicarboxylic acid Chemical compound CN(C)C[C@H]1[C@H](N(CC1)C(=O)O)C(=O)O VDCGXJHBHIABJG-BQBZGAKWSA-N 0.000 claims 1
- AWXDDXPSAPKTTK-DMTCNVIQSA-N (2s,3r)-3-hydroxypyrrolidine-1,2-dicarboxylic acid Chemical compound O[C@@H]1CCN(C(O)=O)[C@@H]1C(O)=O AWXDDXPSAPKTTK-DMTCNVIQSA-N 0.000 claims 1
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 208000003476 primary myelofibrosis Diseases 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000000020 sulfo group Chemical group O=S(=O)([*])O[H] 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 238000000034 method Methods 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 229920006395 saturated elastomer Polymers 0.000 description 2
- 102000010400 1-phosphatidylinositol-3-kinase activity proteins Human genes 0.000 description 1
- OMWOCSIQOUVUFY-UHFFFAOYSA-N 2-(1-methylcyclopropyl)-1h-pyridin-4-one Chemical compound C=1C(=O)C=CNC=1C1(C)CC1 OMWOCSIQOUVUFY-UHFFFAOYSA-N 0.000 description 1
- MTCUFGSMUDIWDV-UHFFFAOYSA-N 4-bromo-2-(1-methylcyclopropyl)pyridine Chemical compound C=1C(Br)=CC=NC=1C1(C)CC1 MTCUFGSMUDIWDV-UHFFFAOYSA-N 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 238000001816 cooling Methods 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 238000004128 high performance liquid chromatography Methods 0.000 description 1
- 238000004895 liquid chromatography mass spectrometry Methods 0.000 description 1
- 239000012074 organic phase Substances 0.000 description 1
- 239000011541 reaction mixture Substances 0.000 description 1
- 238000010898 silica gel chromatography Methods 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 230000002459 sustained effect Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US27002909P | 2009-07-02 | 2009-07-02 | |
| US61/270,029 | 2009-07-02 | ||
| PCT/EP2010/059352 WO2011000905A1 (en) | 2009-07-02 | 2010-07-01 | Substituted 2-carboxamide cycloamino ureas |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2012531456A JP2012531456A (ja) | 2012-12-10 |
| JP2012531456A5 true JP2012531456A5 (enExample) | 2013-08-01 |
Family
ID=42727680
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012518092A Pending JP2012531456A (ja) | 2009-07-02 | 2010-07-01 | 置換２−カルボキサミドシクロアミノウレア類 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US8293753B2 (enExample) |
| EP (1) | EP2448935B1 (enExample) |
| JP (1) | JP2012531456A (enExample) |
| KR (1) | KR20120092552A (enExample) |
| CN (1) | CN102471332A (enExample) |
| AR (1) | AR077367A1 (enExample) |
| AU (1) | AU2010268019A1 (enExample) |
| BR (1) | BRPI1015909A2 (enExample) |
| CA (1) | CA2766855A1 (enExample) |
| EA (1) | EA201200086A1 (enExample) |
| MX (1) | MX2012000177A (enExample) |
| TW (1) | TW201105666A (enExample) |
| UY (1) | UY32747A (enExample) |
| WO (1) | WO2011000905A1 (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW200519106A (en) * | 2003-05-02 | 2005-06-16 | Novartis Ag | Organic compounds |
| EA201000947A1 (ru) * | 2007-12-20 | 2011-02-28 | Новартис Аг | Производные тиазола, применимые в качестве ингибиторов киназы pi3 |
| JP6301316B2 (ja) | 2012-05-23 | 2018-03-28 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | 内胚葉細胞および肝実質細胞の組成物ならびにそれらの細胞を入手および使用する方法 |
| AU2013318205B2 (en) * | 2012-09-20 | 2016-05-19 | Novartis Ag | Pharmaceutical combination comprising a phosphatidylinositol 3-kinase inhibitor|and an aromatase inhibitor |
| ES2608395T3 (es) | 2013-01-23 | 2017-04-10 | Astrazeneca Ab | Compuestos químicos |
| TWI657090B (zh) | 2013-03-01 | 2019-04-21 | 英塞特控股公司 | 吡唑并嘧啶衍生物治療PI3Kδ 相關病症之用途 |
| TW201726140A (zh) | 2015-09-17 | 2017-08-01 | 瑞典商阿斯特捷利康公司 | 治療癌症之新型生物標記及方法 |
| CA3115103A1 (en) | 2018-10-05 | 2020-04-09 | Sloan-Kettering Institute For Cancer Research | Pi3k inhibitors and uses thereof |
| AU2023366352A1 (en) * | 2022-10-28 | 2025-05-08 | Assistance Publique – Hopitaux De Paris (Aphp) | New inhibitors of phosphatidylinositol 3-kinase |
| CN116239591B (zh) * | 2023-02-14 | 2025-09-23 | 嘉兴大学 | 一种(4r)-磺酰氨基-l-脯氨酰胺类化合物、制备方法、应用及其药物组合 |
| CN116987072A (zh) * | 2023-07-27 | 2023-11-03 | 武汉呈瑞生物医药科技有限公司 | 化合物及其应用 |
| EP4643858A1 (en) * | 2024-04-29 | 2025-11-05 | Institut National de la Santé et de la Recherche Médicale | Methods and pharmaceutical composition for the treatment of uterine disease |
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2010
- 2010-06-28 US US12/824,461 patent/US8293753B2/en active Active
- 2010-06-30 UY UY0001032747A patent/UY32747A/es not_active Application Discontinuation
- 2010-07-01 TW TW099121705A patent/TW201105666A/zh unknown
- 2010-07-01 KR KR1020127002827A patent/KR20120092552A/ko not_active Withdrawn
- 2010-07-01 BR BRPI1015909A patent/BRPI1015909A2/pt not_active IP Right Cessation
- 2010-07-01 WO PCT/EP2010/059352 patent/WO2011000905A1/en not_active Ceased
- 2010-07-01 EA EA201200086A patent/EA201200086A1/ru unknown
- 2010-07-01 AU AU2010268019A patent/AU2010268019A1/en not_active Abandoned
- 2010-07-01 AR ARP100102354A patent/AR077367A1/es unknown
- 2010-07-01 JP JP2012518092A patent/JP2012531456A/ja active Pending
- 2010-07-01 CA CA2766855A patent/CA2766855A1/en not_active Abandoned
- 2010-07-01 MX MX2012000177A patent/MX2012000177A/es not_active Application Discontinuation
- 2010-07-01 CN CN2010800300379A patent/CN102471332A/zh active Pending
- 2010-07-01 EP EP10730435.4A patent/EP2448935B1/en not_active Not-in-force
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