JP2014531436A5 - - Google Patents
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- JP2014531436A5 JP2014531436A5 JP2014529985A JP2014529985A JP2014531436A5 JP 2014531436 A5 JP2014531436 A5 JP 2014531436A5 JP 2014529985 A JP2014529985 A JP 2014529985A JP 2014529985 A JP2014529985 A JP 2014529985A JP 2014531436 A5 JP2014531436 A5 JP 2014531436A5
- Authority
- JP
- Japan
- Prior art keywords
- atoms
- cancer
- hal
- group
- phenyl
- 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
- 125000000217 alkyl group Chemical group 0.000 claims 33
- 125000004432 carbon atom Chemical group C* 0.000 claims 20
- 125000000753 cycloalkyl group Chemical group 0.000 claims 16
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 12
- 150000003839 salts Chemical class 0.000 claims 12
- 150000001875 compounds Chemical class 0.000 claims 11
- 239000012453 solvate Substances 0.000 claims 11
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 9
- 125000004076 pyridyl group Chemical group 0.000 claims 9
- 125000004429 atom Chemical group 0.000 claims 8
- 125000000623 heterocyclic group Chemical group 0.000 claims 8
- -1 isopropyloxy, ethyl Chemical group 0.000 claims 8
- 125000004430 oxygen atom Chemical group O* 0.000 claims 8
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 7
- 229910052760 oxygen Inorganic materials 0.000 claims 7
- 206010028980 Neoplasm Diseases 0.000 claims 6
- 201000011510 cancer Diseases 0.000 claims 5
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 5
- 125000003118 aryl group Chemical group 0.000 claims 4
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 4
- 125000002950 monocyclic group Chemical group 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000006413 ring segment Chemical group 0.000 claims 4
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 238000002360 preparation method Methods 0.000 claims 3
- 239000004215 Carbon black (E152) Substances 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 2
- 206010038389 Renal cancer Diseases 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 229930195733 hydrocarbon Natural products 0.000 claims 2
- 150000002430 hydrocarbons Chemical class 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 201000010982 kidney cancer Diseases 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 125000004434 sulfur atom Chemical group 0.000 claims 2
- SKBGXGJACXJIHW-UHFFFAOYSA-N 4-amino-6-[4-[1-[2-(azetidin-1-yl)ethyl]-4-(3-chloro-4-fluorophenyl)imidazol-2-yl]piperidin-1-yl]pyrimidine-5-carboxamide Chemical compound NC(=O)C1=C(N)N=CN=C1N1CCC(C=2N(C=C(N=2)C=2C=C(Cl)C(F)=CC=2)CCN2CCC2)CC1 SKBGXGJACXJIHW-UHFFFAOYSA-N 0.000 claims 1
- WNBFWWDKYZWYOX-UHFFFAOYSA-N 4-amino-6-[4-[1-[2-(azetidin-1-yl)ethyl]-4-[4-fluoro-3-(trifluoromethyl)phenyl]imidazol-2-yl]piperidin-1-yl]pyrimidine-5-carboxamide Chemical compound NC(=O)C1=C(N)N=CN=C1N1CCC(C=2N(C=C(N=2)C=2C=C(C(F)=CC=2)C(F)(F)F)CCN2CCC2)CC1 WNBFWWDKYZWYOX-UHFFFAOYSA-N 0.000 claims 1
- HFKGXBIBYCUDKG-UHFFFAOYSA-N 4-amino-6-[4-[1-[2-(azetidin-1-yl)ethyl]-4-cyclohexylimidazol-2-yl]piperidin-1-yl]pyrimidine-5-carbonitrile Chemical compound NC1=NC=NC(N2CCC(CC2)C=2N(C=C(N=2)C2CCCCC2)CCN2CCC2)=C1C#N HFKGXBIBYCUDKG-UHFFFAOYSA-N 0.000 claims 1
- LBTKEPYWOLJQQB-UHFFFAOYSA-N 4-amino-6-[4-[1-[2-(cyclopentylamino)ethyl]-4-(4-fluoro-3-methylphenyl)imidazol-2-yl]piperidin-1-yl]pyrimidine-5-carboxamide Chemical compound C1=C(F)C(C)=CC(C=2N=C(N(CCNC3CCCC3)C=2)C2CCN(CC2)C=2C(=C(N)N=CN=2)C(N)=O)=C1 LBTKEPYWOLJQQB-UHFFFAOYSA-N 0.000 claims 1
- PIVDYIBVDVOUTC-UHFFFAOYSA-N 4-amino-6-[4-[1-[2-(cyclopropylmethylamino)ethyl]-4-(4-fluoro-3-methylphenyl)imidazol-2-yl]piperidin-1-yl]pyrimidine-5-carboxamide Chemical compound C1=C(F)C(C)=CC(C=2N=C(N(CCNCC3CC3)C=2)C2CCN(CC2)C=2C(=C(N)N=CN=2)C(N)=O)=C1 PIVDYIBVDVOUTC-UHFFFAOYSA-N 0.000 claims 1
- MRYHAUHEHQAMRQ-UHFFFAOYSA-N 4-amino-6-[4-[4-(4-fluoro-3-methylphenyl)-1-[2-(methylamino)ethyl]imidazol-2-yl]piperidin-1-yl]pyrimidine-5-carboxamide Chemical compound CNCCN1C=C(C=2C=C(C)C(F)=CC=2)N=C1C(CC1)CCN1C1=NC=NC(N)=C1C(N)=O MRYHAUHEHQAMRQ-UHFFFAOYSA-N 0.000 claims 1
- WTXODCJICMVXLA-UHFFFAOYSA-N 4-amino-6-[4-[4-[4-fluoro-3-(trifluoromethyl)phenyl]-1-[2-(2-methoxyethylamino)ethyl]imidazol-2-yl]piperidin-1-yl]pyrimidine-5-carbonitrile Chemical compound COCCNCCN1C=C(C=2C=C(C(F)=CC=2)C(F)(F)F)N=C1C(CC1)CCN1C1=NC=NC(N)=C1C#N WTXODCJICMVXLA-UHFFFAOYSA-N 0.000 claims 1
- MOQRMWMUHUDDJL-UHFFFAOYSA-N 4-amino-6-[4-[4-[4-fluoro-3-(trifluoromethyl)phenyl]-1-[2-(propan-2-ylamino)ethyl]imidazol-2-yl]piperidin-1-yl]pyrimidine-5-carboxamide Chemical compound CC(C)NCCN1C=C(C=2C=C(C(F)=CC=2)C(F)(F)F)N=C1C(CC1)CCN1C1=NC=NC(N)=C1C(N)=O MOQRMWMUHUDDJL-UHFFFAOYSA-N 0.000 claims 1
- GAYRMKRSQCSTHF-UHFFFAOYSA-N 4-amino-6-[4-[4-[4-fluoro-3-(trifluoromethyl)phenyl]-1-pyrrolidin-3-ylimidazol-2-yl]piperidin-1-yl]pyrimidine-5-carboxamide Chemical compound NC(=O)C1=C(N)N=CN=C1N1CCC(C=2N(C=C(N=2)C=2C=C(C(F)=CC=2)C(F)(F)F)C2CNCC2)CC1 GAYRMKRSQCSTHF-UHFFFAOYSA-N 0.000 claims 1
- GNOBRAMAIHJFOP-UHFFFAOYSA-N 5-chloro-6-[4-[1-[2-(cyclopropylamino)ethyl]-4-[2-(trifluoromethyl)pyridin-4-yl]imidazol-2-yl]piperidin-1-yl]pyrimidin-4-amine Chemical compound NC1=NC=NC(N2CCC(CC2)C=2N(C=C(N=2)C=2C=C(N=CC=2)C(F)(F)F)CCNC2CC2)=C1Cl GNOBRAMAIHJFOP-UHFFFAOYSA-N 0.000 claims 1
- MGYJNZHGAIGKBJ-UHFFFAOYSA-N 5-ethoxy-6-[4-[4-[4-fluoro-3-(trifluoromethyl)phenyl]-1-[2-(propan-2-ylamino)ethyl]imidazol-2-yl]piperidin-1-yl]pyrimidin-4-amine Chemical compound CCOC1=C(N)N=CN=C1N1CCC(C=2N(C=C(N=2)C=2C=C(C(F)=CC=2)C(F)(F)F)CCNC(C)C)CC1 MGYJNZHGAIGKBJ-UHFFFAOYSA-N 0.000 claims 1
- JNWSILMDEXPLAM-UHFFFAOYSA-N 5-ethyl-6-[4-[4-[4-fluoro-3-(trifluoromethyl)phenyl]-1-piperidin-4-ylimidazol-2-yl]piperidin-1-yl]pyrimidin-4-amine Chemical compound CCC1=C(N)N=CN=C1N1CCC(C=2N(C=C(N=2)C=2C=C(C(F)=CC=2)C(F)(F)F)C2CCNCC2)CC1 JNWSILMDEXPLAM-UHFFFAOYSA-N 0.000 claims 1
- YOXMBPVKSDWRAV-UHFFFAOYSA-N 6-[4-[1-(2-aminoethyl)-4-[4-fluoro-3-(trifluoromethyl)phenyl]imidazol-2-yl]piperidin-1-yl]-5-ethylpyrimidin-4-amine Chemical compound CCC1=C(N)N=CN=C1N1CCC(C=2N(C=C(N=2)C=2C=C(C(F)=CC=2)C(F)(F)F)CCN)CC1 YOXMBPVKSDWRAV-UHFFFAOYSA-N 0.000 claims 1
- BZOAWHFCLQZEIR-UHFFFAOYSA-N 6-[4-[1-(azetidin-3-ylmethyl)-4-(4-fluoro-3-methylphenyl)imidazol-2-yl]cyclohexyl]-5-propan-2-ylpyrimidin-4-amine Chemical compound CC(C)C1=C(N)N=CN=C1C1CCC(C=2N(C=C(N=2)C=2C=C(C)C(F)=CC=2)CC2CNC2)CC1 BZOAWHFCLQZEIR-UHFFFAOYSA-N 0.000 claims 1
- XDCFPLHPOOPKGK-UHFFFAOYSA-N 6-[4-[1-[2-(azetidin-1-yl)ethyl]-4-(2-propan-2-ylpyridin-4-yl)imidazol-2-yl]piperidin-1-yl]-5-ethenylpyrimidin-4-amine Chemical compound C1=NC(C(C)C)=CC(C=2N=C(N(CCN3CCC3)C=2)C2CCN(CC2)C=2C(=C(N)N=CN=2)C=C)=C1 XDCFPLHPOOPKGK-UHFFFAOYSA-N 0.000 claims 1
- MERNKFHEABWVHR-UHFFFAOYSA-N 6-[4-[1-[2-(azetidin-1-yl)ethyl]-4-[2-(trifluoromethyl)pyridin-4-yl]imidazol-2-yl]piperidin-1-yl]-5-chloropyrimidin-4-amine Chemical compound NC1=NC=NC(N2CCC(CC2)C=2N(C=C(N=2)C=2C=C(N=CC=2)C(F)(F)F)CCN2CCC2)=C1Cl MERNKFHEABWVHR-UHFFFAOYSA-N 0.000 claims 1
- XYZFWUNBADWKLH-UHFFFAOYSA-N 6-[4-[1-[2-(azetidin-1-yl)ethyl]-4-[4-fluoro-3-(trifluoromethyl)phenyl]imidazol-2-yl]piperidin-1-yl]-5-propan-2-yloxypyrimidin-4-amine Chemical compound CC(C)OC1=C(N)N=CN=C1N1CCC(C=2N(C=C(N=2)C=2C=C(C(F)=CC=2)C(F)(F)F)CCN2CCC2)CC1 XYZFWUNBADWKLH-UHFFFAOYSA-N 0.000 claims 1
- NUPWMMJWFAYJED-UHFFFAOYSA-N 6-[4-[1-[2-(dimethylamino)ethyl]-4-(4-fluoro-3-methylphenyl)imidazol-2-yl]piperidin-1-yl]-5-(1h-pyrazol-4-yl)pyrimidin-4-amine Chemical compound CN(C)CCN1C=C(C=2C=C(C)C(F)=CC=2)N=C1C(CC1)CCN1C1=NC=NC(N)=C1C=1C=NNC=1 NUPWMMJWFAYJED-UHFFFAOYSA-N 0.000 claims 1
- RGZTUPDJESIZJE-UHFFFAOYSA-N 6-[4-[1-[2-(ethylamino)ethyl]-4-[4-fluoro-3-(trifluoromethyl)phenyl]imidazol-2-yl]piperidin-1-yl]-5-propan-2-yloxypyrimidin-4-amine Chemical compound CCNCCN1C=C(C=2C=C(C(F)=CC=2)C(F)(F)F)N=C1C(CC1)CCN1C1=NC=NC(N)=C1OC(C)C RGZTUPDJESIZJE-UHFFFAOYSA-N 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 206010066476 Haematological malignancy Diseases 0.000 claims 1
- 208000002250 Hematologic Neoplasms Diseases 0.000 claims 1
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 208000015634 Rectal Neoplasms Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000024313 Testicular Neoplasms Diseases 0.000 claims 1
- 206010057644 Testis cancer Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 1
- 125000002619 bicyclic group Chemical group 0.000 claims 1
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 claims 1
- 210000001185 bone marrow Anatomy 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 210000002615 epidermis Anatomy 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000000543 intermediate Substances 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 210000000066 myeloid cell Anatomy 0.000 claims 1
- 238000010534 nucleophilic substitution reaction Methods 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 206010038038 rectal cancer Diseases 0.000 claims 1
- 201000001275 rectum cancer Diseases 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 1
- 208000017572 squamous cell neoplasm Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 201000003120 testicular cancer Diseases 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 206010046766 uterine cancer Diseases 0.000 claims 1
- 0 *C(C=C)=C(*)C(N)=NC=* Chemical compound *C(C=C)=C(*)C(N)=NC=* 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161533601P | 2011-09-12 | 2011-09-12 | |
| US61/533,601 | 2011-09-12 | ||
| PCT/US2012/054900 WO2013040059A1 (en) | 2011-09-12 | 2012-09-12 | Novel imidazole amines as modulators of kinase activity |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014531436A JP2014531436A (ja) | 2014-11-27 |
| JP2014531436A5 true JP2014531436A5 (enExample) | 2016-06-09 |
| JP5964974B2 JP5964974B2 (ja) | 2016-08-03 |
Family
ID=46881179
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014529985A Expired - Fee Related JP5964974B2 (ja) | 2011-09-12 | 2012-09-12 | キナーゼ活性のモジュレーターとしての新規イミダゾールアミン |
Country Status (24)
| Country | Link |
|---|---|
| US (2) | US9145392B2 (enExample) |
| EP (1) | EP2755965B1 (enExample) |
| JP (1) | JP5964974B2 (enExample) |
| KR (1) | KR101995605B1 (enExample) |
| CN (1) | CN104080782B (enExample) |
| AU (1) | AU2012308696B2 (enExample) |
| BR (1) | BR112014005554A2 (enExample) |
| CA (1) | CA2844830C (enExample) |
| DK (1) | DK2755965T3 (enExample) |
| EA (1) | EA025098B1 (enExample) |
| ES (1) | ES2644536T3 (enExample) |
| HR (1) | HRP20171554T1 (enExample) |
| HU (1) | HUE035019T2 (enExample) |
| IL (1) | IL231383A (enExample) |
| LT (1) | LT2755965T (enExample) |
| MX (1) | MX346095B (enExample) |
| NO (1) | NO2791461T3 (enExample) |
| PL (1) | PL2755965T3 (enExample) |
| PT (1) | PT2755965T (enExample) |
| RS (1) | RS56534B1 (enExample) |
| SG (2) | SG2014009278A (enExample) |
| SI (1) | SI2755965T1 (enExample) |
| WO (1) | WO2013040059A1 (enExample) |
| ZA (1) | ZA201401013B (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6082011B2 (ja) * | 2011-09-12 | 2017-02-15 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ | キナーゼ活性のモジュレーターとして使用するためのアミノピリミジン誘導体 |
| EA027277B1 (ru) | 2012-10-16 | 2017-07-31 | Альмираль, С.А. | Производные пирроллотриазинона в качестве ингибиторов pi3k |
| AU2013344549B2 (en) | 2012-11-16 | 2018-03-08 | Xiaoling Chen | Novel imidazol-piperidinyl derivatives as modulators of kinase activity |
| HK1218756A1 (zh) | 2013-03-11 | 2017-03-10 | 默克专利有限公司 | 用作激酶活性调节剂的6-[4-(1h-咪唑-2-基)哌啶-1-基]嘧啶-4-胺衍生物 |
| SG11201605121VA (en) * | 2014-02-11 | 2016-07-28 | Merck Patent Gmbh | Pyrimidine imidazole amines as modulators of kinase activity |
| JP6529085B2 (ja) | 2014-04-18 | 2019-06-12 | 武田薬品工業株式会社 | 複素環化合物 |
| CN109467538A (zh) | 2017-09-07 | 2019-03-15 | 和记黄埔医药（上海）有限公司 | 环烯烃取代的杂芳环类化合物及其用途 |
| KR20200093159A (ko) | 2019-01-28 | 2020-08-05 | 주식회사 링크모션 | 스마트 팜 모듈 구조물 |
| PH12022551379A1 (en) | 2019-12-06 | 2023-05-03 | Vertex Pharma | Substituted tetrahydrofurans as modulators of sodium channels |
| US11866421B2 (en) | 2021-05-31 | 2024-01-09 | Epigen Biosciences, Inc. | Pyrimidine and pyridine amine compounds and usage thereof in disease treatment |
| DK4347031T3 (da) | 2021-06-04 | 2025-12-01 | Vertex Pharma | N-(hydroxyalkyl-(hetero)aryl)-tetrahydrofuran-carboxamider som modulatorer af natriumkanaler |
| CN117567435A (zh) * | 2022-01-30 | 2024-02-20 | 上海市第十人民医院 | 谷氨酰胺环化酶抑制剂及其应用 |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW200306819A (en) | 2002-01-25 | 2003-12-01 | Vertex Pharma | Indazole compounds useful as protein kinase inhibitors |
| AU2004230841A1 (en) | 2003-04-03 | 2004-10-28 | Vertex Pharmaceuticals Incorporated | Compositions useful as inhibitors of protein kinases |
| AU2004278413B2 (en) | 2003-09-30 | 2008-07-31 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| AU2004283751B2 (en) | 2003-10-24 | 2011-05-19 | Exelixis, Inc. | p70S6 kinase modulators and method of use |
| WO2005054237A1 (en) | 2003-11-21 | 2005-06-16 | Novartis Ag | 1h-imidazoquinoline derivatives as protein kinase inhibitors |
| CN1889958A (zh) | 2003-12-09 | 2007-01-03 | 美国政府健康及人类服务部 | 抑制免疫应答或治疗增生性疾病的方法 |
| WO2005117909A2 (en) | 2004-04-23 | 2005-12-15 | Exelixis, Inc. | Kinase modulators and methods of use |
| CA2590961C (en) | 2004-12-28 | 2013-11-26 | Exelixis, Inc. | [1h-pyrazolo[3,4-d]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-threonine kinase modulators (p70s6k, atk1 and atk2) for the treatment of immunological, inflammatory and proliferative diseases |
| AU2006206246A1 (en) * | 2005-01-19 | 2006-07-27 | Neurogen Corporation | Heteroaryl substituted piperazinyl-pyridine analogues |
| GB0501999D0 (en) | 2005-02-01 | 2005-03-09 | Sentinel Oncology Ltd | Pharmaceutical compounds |
| US8343953B2 (en) | 2005-06-22 | 2013-01-01 | Astex Therapeutics Limited | Pharmaceutical compounds |
| AR064416A1 (es) * | 2006-12-21 | 2009-04-01 | Cancer Rec Tech Ltd | Derivados de purina, piridina y pirimidina condensadas con heterociclos, moduladores de pka y/o pkb, composiciones farmaceuticas que los contienen, y usos para el tratamiento de enfermedades hiperproliferativas. |
| UA99284C2 (ru) * | 2007-05-11 | 2012-08-10 | Елі Ліллі Енд Компані | ИНГИБИТОРЫ р70 S6-КИНАЗЫ |
| AR074072A1 (es) | 2008-11-11 | 2010-12-22 | Lilly Co Eli | Compuesto de imidazol -piperidin -pirrol-pirimidin-6-ona, composicion farmaceutica que lo comprende y su uso para preparar un medicamento util para tratar el glioblastoma multiforme |
| EP2396307B1 (en) | 2009-02-11 | 2014-10-15 | Merck Patent GmbH | Novel amino azaheterocyclic carboxamides |
| UA110113C2 (xx) | 2010-07-29 | 2015-11-25 | Біциклічні азагетероциклічні карбоксаміди | |
| CA2803387C (en) | 2010-07-29 | 2017-12-05 | Bayard R. Huck | Cyclic amine azaheterocyclic carboxamides |
| WO2012069146A1 (en) | 2010-11-24 | 2012-05-31 | Merck Patent Gmbh | Quinazoline carboxamide azetidines |
-
2012
- 2012-09-12 LT LTEP12761865.0T patent/LT2755965T/lt unknown
- 2012-09-12 SG SG2014009278A patent/SG2014009278A/en unknown
- 2012-09-12 MX MX2014002832A patent/MX346095B/es active IP Right Grant
- 2012-09-12 HR HRP20171554TT patent/HRP20171554T1/hr unknown
- 2012-09-12 AU AU2012308696A patent/AU2012308696B2/en not_active Ceased
- 2012-09-12 CA CA2844830A patent/CA2844830C/en not_active Expired - Fee Related
- 2012-09-12 DK DK12761865.0T patent/DK2755965T3/en active
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- 2012-09-12 RS RS20171075A patent/RS56534B1/sr unknown
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- 2012-09-12 ES ES12761865.0T patent/ES2644536T3/es active Active
- 2012-09-12 SI SI201231104T patent/SI2755965T1/sl unknown
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2014
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2015
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