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 (OSRAM) | 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 (OSRAM) |
| EP (1) | EP2448935B1 (OSRAM) |
| JP (1) | JP2012531456A (OSRAM) |
| KR (1) | KR20120092552A (OSRAM) |
| CN (1) | CN102471332A (OSRAM) |
| AR (1) | AR077367A1 (OSRAM) |
| AU (1) | AU2010268019A1 (OSRAM) |
| BR (1) | BRPI1015909A2 (OSRAM) |
| CA (1) | CA2766855A1 (OSRAM) |
| EA (1) | EA201200086A1 (OSRAM) |
| MX (1) | MX2012000177A (OSRAM) |
| TW (1) | TW201105666A (OSRAM) |
| UY (1) | UY32747A (OSRAM) |
| WO (1) | WO2011000905A1 (OSRAM) |
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 |
| WO2009080694A1 (en) * | 2007-12-20 | 2009-07-02 | Novartis Ag | Thiazole derivatives used as pi 3 kinase inhibitors |
| RU2014149145A (ru) | 2012-05-23 | 2016-07-20 | Ф. Хоффманн-Ля Рош Аг | Композиции и способы получения и применения эндодермальных клеток и гепатоцитов |
| ES2686689T3 (es) * | 2012-09-20 | 2018-10-19 | Novartis Ag | Combinación farmacéutica que comprende un inhibidor de fosfatidilinositol 3-quinasa y un inhibidor de aromatasa |
| EP2948447B1 (en) | 2013-01-23 | 2016-09-21 | Astrazeneca AB | Chemical compounds |
| TW202214254A (zh) | 2013-03-01 | 2022-04-16 | 美商英塞特控股公司 | 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 |
| WO2020072892A1 (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 JP JP2012518092A patent/JP2012531456A/ja active Pending
- 2010-07-01 KR KR1020127002827A patent/KR20120092552A/ko not_active Withdrawn
- 2010-07-01 TW TW099121705A patent/TW201105666A/zh unknown
- 2010-07-01 WO PCT/EP2010/059352 patent/WO2011000905A1/en not_active Ceased
- 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 AR ARP100102354A patent/AR077367A1/es unknown
- 2010-07-01 CN CN2010800300379A patent/CN102471332A/zh active Pending
- 2010-07-01 EA EA201200086A patent/EA201200086A1/ru unknown
- 2010-07-01 EP EP10730435.4A patent/EP2448935B1/en not_active Not-in-force
- 2010-07-01 BR BRPI1015909A patent/BRPI1015909A2/pt not_active IP Right Cessation
- 2010-07-01 AU AU2010268019A patent/AU2010268019A1/en not_active Abandoned
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