JP2016513660A5 - - Google Patents
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- JP2016513660A5 JP2016513660A5 JP2016502187A JP2016502187A JP2016513660A5 JP 2016513660 A5 JP2016513660 A5 JP 2016513660A5 JP 2016502187 A JP2016502187 A JP 2016502187A JP 2016502187 A JP2016502187 A JP 2016502187A JP 2016513660 A5 JP2016513660 A5 JP 2016513660A5
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- pharmaceutically acceptable
- acceptable salt
- pharmaceutical composition
- composition according
- 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.)
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- 150000003839 salts Chemical class 0.000 claims 40
- 150000001875 compounds Chemical class 0.000 claims 39
- 239000008194 pharmaceutical composition Substances 0.000 claims 37
- 206010028980 Neoplasm Diseases 0.000 claims 36
- 201000011510 cancer Diseases 0.000 claims 36
- 125000000217 alkyl group Chemical group 0.000 claims 22
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 11
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 8
- 125000005843 halogen group Chemical group 0.000 claims 8
- 125000001424 substituent group Chemical group 0.000 claims 7
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 6
- 125000004076 pyridyl group Chemical group 0.000 claims 6
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 4
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 4
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 4
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 4
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 4
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 4
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 2
- 208000003950 B-cell lymphoma Diseases 0.000 claims 2
- 208000011691 Burkitt lymphomas Diseases 0.000 claims 2
- 208000017604 Hodgkin disease Diseases 0.000 claims 2
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims 2
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 2
- 206010025323 Lymphomas Diseases 0.000 claims 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 2
- PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical compound OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 claims 2
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 2
- 206010041067 Small cell lung cancer Diseases 0.000 claims 2
- 206010042971 T-cell lymphoma Diseases 0.000 claims 2
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 208000005017 glioblastoma Diseases 0.000 claims 2
- 201000010536 head and neck cancer Diseases 0.000 claims 2
- 208000014829 head and neck neoplasm Diseases 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 2
- 201000008968 osteosarcoma Diseases 0.000 claims 2
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 2
- 125000000335 thiazolyl group Chemical group 0.000 claims 2
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
- GOYFACGYNALWDU-HYHFPRINSA-N 2-[[(2r,5r,6r)-4-[(1s)-2-tert-butylsulfonyl-1-cyclopropylethyl]-5-(4-chloro-3-fluorophenyl)-6-(3-chlorophenyl)-2-methyl-3-oxomorpholin-2-yl]methyl]-1,3-thiazole-5-carboxylic acid Chemical compound C1([C@@H](CS(=O)(=O)C(C)(C)C)N2C([C@@](C)(CC=3SC(=CN=3)C(O)=O)O[C@@H]([C@H]2C=2C=C(F)C(Cl)=CC=2)C=2C=C(Cl)C=CC=2)=O)CC1 GOYFACGYNALWDU-HYHFPRINSA-N 0.000 claims 1
- GOYFACGYNALWDU-PHSVCASQSA-N 2-[[(2s,5r,6r)-4-[(1s)-2-tert-butylsulfonyl-1-cyclopropylethyl]-5-(4-chloro-3-fluorophenyl)-6-(3-chlorophenyl)-2-methyl-3-oxomorpholin-2-yl]methyl]-1,3-thiazole-5-carboxylic acid Chemical compound C1([C@@H](CS(=O)(=O)C(C)(C)C)N2C([C@](C)(CC=3SC(=CN=3)C(O)=O)O[C@@H]([C@H]2C=2C=C(F)C(Cl)=CC=2)C=2C=C(Cl)C=CC=2)=O)CC1 GOYFACGYNALWDU-PHSVCASQSA-N 0.000 claims 1
- 125000004179 3-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(Cl)=C1[H] 0.000 claims 1
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 1
- ILRYIEMVGUAAAV-OZLMZZSTSA-N 6-[[(2r,5r,6r)-4-[(1s)-2-tert-butylsulfonyl-1-cyclopropylethyl]-5-(4-chloro-3-fluorophenyl)-6-(3-chlorophenyl)-2-methyl-3-oxomorpholin-2-yl]methyl]pyridine-3-carboxylic acid Chemical compound C1([C@@H](CS(=O)(=O)C(C)(C)C)N2C([C@@](C)(CC=3N=CC(=CC=3)C(O)=O)O[C@@H]([C@H]2C=2C=C(F)C(Cl)=CC=2)C=2C=C(Cl)C=CC=2)=O)CC1 ILRYIEMVGUAAAV-OZLMZZSTSA-N 0.000 claims 1
- UFMQNHQVIXKCIT-OZLMZZSTSA-N 6-[[(2r,5r,6r)-4-[(1s)-2-tert-butylsulfonyl-1-cyclopropylethyl]-6-(3-chlorophenyl)-5-(4-chlorophenyl)-2-methyl-3-oxomorpholin-2-yl]methyl]-1-oxidopyridin-1-ium-3-carboxylic acid Chemical compound C1([C@@H](CS(=O)(=O)C(C)(C)C)N2C([C@@](C)(CC=3[N+](=CC(=CC=3)C(O)=O)[O-])O[C@@H]([C@H]2C=2C=CC(Cl)=CC=2)C=2C=C(Cl)C=CC=2)=O)CC1 UFMQNHQVIXKCIT-OZLMZZSTSA-N 0.000 claims 1
- OTQRFDJHHZHHNT-OZLMZZSTSA-N 6-[[(2r,5r,6r)-4-[(1s)-2-tert-butylsulfonyl-1-cyclopropylethyl]-6-(3-chlorophenyl)-5-(4-chlorophenyl)-2-methyl-3-oxomorpholin-2-yl]methyl]pyridine-3-carboxylic acid Chemical compound C1([C@@H](CS(=O)(=O)C(C)(C)C)N2C([C@@](C)(CC=3N=CC(=CC=3)C(O)=O)O[C@@H]([C@H]2C=2C=CC(Cl)=CC=2)C=2C=C(Cl)C=CC=2)=O)CC1 OTQRFDJHHZHHNT-OZLMZZSTSA-N 0.000 claims 1
- UFMQNHQVIXKCIT-LNHQPZRBSA-N 6-[[(2s,5r,6r)-4-[(1s)-2-tert-butylsulfonyl-1-cyclopropylethyl]-6-(3-chlorophenyl)-5-(4-chlorophenyl)-2-methyl-3-oxomorpholin-2-yl]methyl]-1-oxidopyridin-1-ium-3-carboxylic acid Chemical compound C1([C@@H](CS(=O)(=O)C(C)(C)C)N2C([C@](C)(CC=3[N+](=CC(=CC=3)C(O)=O)[O-])O[C@@H]([C@H]2C=2C=CC(Cl)=CC=2)C=2C=C(Cl)C=CC=2)=O)CC1 UFMQNHQVIXKCIT-LNHQPZRBSA-N 0.000 claims 1
- OTQRFDJHHZHHNT-LNHQPZRBSA-N 6-[[(2s,5r,6r)-4-[(1s)-2-tert-butylsulfonyl-1-cyclopropylethyl]-6-(3-chlorophenyl)-5-(4-chlorophenyl)-2-methyl-3-oxomorpholin-2-yl]methyl]pyridine-3-carboxylic acid Chemical compound C1([C@@H](CS(=O)(=O)C(C)(C)C)N2C([C@](C)(CC=3N=CC(=CC=3)C(O)=O)O[C@@H]([C@H]2C=2C=CC(Cl)=CC=2)C=2C=C(Cl)C=CC=2)=O)CC1 OTQRFDJHHZHHNT-LNHQPZRBSA-N 0.000 claims 1
- 125000006164 6-membered heteroaryl group Chemical group 0.000 claims 1
- 206010005003 Bladder cancer 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
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 208000022072 Gallbladder Neoplasms Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 150000001204 N-oxides Chemical class 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
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms 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
- 230000001154 acute effect Effects 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 210000004027 cell Anatomy 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 210000003679 cervix uteri Anatomy 0.000 claims 1
- 125000000068 chlorophenyl group Chemical group 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 1
- 210000004696 endometrium Anatomy 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 210000003238 esophagus Anatomy 0.000 claims 1
- 210000000232 gallbladder Anatomy 0.000 claims 1
- 201000010175 gallbladder cancer Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 210000002768 hair cell Anatomy 0.000 claims 1
- -1 halophenyl compound Chemical class 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 229960003512 nicotinic acid Drugs 0.000 claims 1
- 235000001968 nicotinic acid Nutrition 0.000 claims 1
- 239000011664 nicotinic acid Substances 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 210000001672 ovary Anatomy 0.000 claims 1
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 1
- 210000000496 pancreas Anatomy 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- ILVXOBCQQYKLDS-UHFFFAOYSA-N pyridine N-oxide Chemical compound [O-][N+]1=CC=CC=C1 ILVXOBCQQYKLDS-UHFFFAOYSA-N 0.000 claims 1
- 206010038038 rectal cancer Diseases 0.000 claims 1
- 210000000664 rectum Anatomy 0.000 claims 1
- 201000001275 rectum cancer Diseases 0.000 claims 1
- 210000003491 skin Anatomy 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 210000002784 stomach Anatomy 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 210000001685 thyroid gland Anatomy 0.000 claims 1
- 210000003932 urinary bladder Anatomy 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361784230P | 2013-03-14 | 2013-03-14 | |
| US61/784,230 | 2013-03-14 | ||
| PCT/US2014/026584 WO2014151863A1 (en) | 2013-03-14 | 2014-03-13 | Heteroaryl acid morpholinone compounds as mdm2 inhibitors for the treatment of cancer |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016513660A JP2016513660A (ja) | 2016-05-16 |
| JP2016513660A5 true JP2016513660A5 (enExample) | 2017-03-30 |
| JP6377123B2 JP6377123B2 (ja) | 2018-08-22 |
Family
ID=50442720
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016502187A Active JP6377123B2 (ja) | 2013-03-14 | 2014-03-13 | 癌の治療のためのｍｄｍ２阻害剤としてのヘテロアリール酸モルホリノン化合物 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US9758495B2 (enExample) |
| EP (1) | EP2970237B1 (enExample) |
| JP (1) | JP6377123B2 (enExample) |
| AU (1) | AU2014236812B2 (enExample) |
| CA (1) | CA2906538C (enExample) |
| MX (1) | MX374513B (enExample) |
| WO (1) | WO2014151863A1 (enExample) |
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JO2998B1 (ar) | 2010-06-04 | 2016-09-05 | Amgen Inc | مشتقات بيبيريدينون كمثبطات mdm2 لعلاج السرطان |
| WO2013049250A1 (en) | 2011-09-27 | 2013-04-04 | Amgen Inc. | Heterocyclic compounds as mdm2 inhibitors for the treatment of cancer |
| US11407721B2 (en) | 2013-02-19 | 2022-08-09 | Amgen Inc. | CIS-morpholinone and other compounds as MDM2 inhibitors for the treatment of cancer |
| WO2014151863A1 (en) | 2013-03-14 | 2014-09-25 | Amgen Inc. | Heteroaryl acid morpholinone compounds as mdm2 inhibitors for the treatment of cancer |
| JOP20200296A1 (ar) | 2013-06-10 | 2017-06-16 | Amgen Inc | عمليات صنع وأشكال بلورية من mdm2 مثبط |
| GB201311888D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201311891D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compound |
| PT3068393T (pt) | 2013-11-11 | 2022-06-14 | Amgen Inc | Terapia de combinação, incluindo um inibidor de mdm2 e um ou mais agentes farmaceuticamente ativos adicionais para o tratamento de cancros |
| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| US12312316B2 (en) | 2015-01-20 | 2025-05-27 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| HK1247204A1 (zh) | 2015-01-20 | 2018-09-21 | Arvinas Operations, Inc. | 用於雄激素受体的靶向降解的化合物和方法 |
| EP3302482A4 (en) | 2015-06-05 | 2018-12-19 | Arvinas, Inc. | Tank-binding kinase-1 protacs and associated methods of use |
| US10772962B2 (en) | 2015-08-19 | 2020-09-15 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of bromodomain-containing proteins |
| CN109152843A (zh) | 2016-05-20 | 2019-01-04 | 豪夫迈·罗氏有限公司 | Protac抗体缀合物及其使用方法 |
| JP7286539B2 (ja) | 2016-11-01 | 2023-06-05 | アルビナス・オペレーションズ・インコーポレイテッド | タウタンパク質標的化ｐｒｏｔａｃ、および関連使用方法 |
| DK3689868T3 (da) | 2016-12-01 | 2024-01-02 | Arvinas Operations Inc | Tetrahydronaphthalen- og tetrahydroisoquinolinderivater som østrogenreceptordegraderende midler |
| CN110753693A (zh) | 2016-12-23 | 2020-02-04 | 阿尔维纳斯运营股份有限公司 | Egfr蛋白水解靶向嵌合分子和相关使用方法 |
| AU2017382436C1 (en) | 2016-12-23 | 2021-05-27 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of Rapidly Accelerated Fibrosarcoma polypeptides |
| US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides |
| US10806737B2 (en) | 2016-12-23 | 2020-10-20 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of fetal liver kinase polypeptides |
| US11191741B2 (en) | 2016-12-24 | 2021-12-07 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide |
| EP3573977A4 (en) | 2017-01-26 | 2020-12-23 | Arvinas Operations, Inc. | Modulators of estrogen receptor proteolysis and associated methods of use |
| US20200231556A1 (en) * | 2017-07-28 | 2020-07-23 | Basf Se | Preparation of substituted 3-aryl-5-trifluoromethyl-1,2,4-oxadiazoles |
| WO2019025250A1 (en) | 2017-08-04 | 2019-02-07 | Basf Se | SUBSTITUTED TRIFLUOROMETHYLOXADIAZOLES FOR COMBATING PHYTOPATHOGENIC FUNGI |
| WO2019038042A1 (en) | 2017-08-21 | 2019-02-28 | Basf Se | SUBSTITUTED TRIFLUOROMETHYLOXADIAZOLES FOR THE CONTROL OF PHYTOPATHOGENIC FUNGI |
| WO2019099926A1 (en) | 2017-11-17 | 2019-05-23 | Arvinas, Inc. | Compounds and methods for the targeted degradation of interleukin-1 receptor-associated kinase 4 polypeptides |
| CN119569702A (zh) | 2018-04-04 | 2025-03-07 | 阿尔维纳斯运营股份有限公司 | 蛋白水解调节剂及相关使用方法 |
| WO2019219464A1 (en) | 2018-05-15 | 2019-11-21 | Basf Se | Substituted trifluoromethyloxadiazoles for combating phytopathogenic fungi |
| WO2020041331A1 (en) | 2018-08-20 | 2020-02-27 | Arvinas Operations, Inc. | Proteolysis targeting chimeric (protac) compound with e3 ubiquitin ligase binding activity and targeting alpha-synuclein protein for treating neurodegenerative diseases |
| IL290789B2 (en) | 2019-08-26 | 2025-09-01 | Arvinas Operations Inc | Methods for treating breast cancer with a history of tetrahydronaphthalene as estrogen receptor-disrupting agents |
| CN114761387A (zh) | 2019-12-05 | 2022-07-15 | 巴斯夫欧洲公司 | 取代的芳族羧酰胺的制备 |
| WO2021219424A1 (en) | 2020-04-29 | 2021-11-04 | Basf Se | Preparation of aromatic carboxyamides by a palladium-catalyzed carbonylation reaction |
| WO2021219418A1 (en) | 2020-04-29 | 2021-11-04 | Basf Se | Preparation of aromatic carboxyamides by palladium-catalyzed carbonylation reaction |
| JP2023539663A (ja) | 2020-08-28 | 2023-09-15 | アルビナス・オペレーションズ・インコーポレイテッド | 急速進行性線維肉腫タンパク質分解化合物及び関連する使用方法 |
| CN116390916A (zh) | 2020-09-14 | 2023-07-04 | 阿尔维纳斯运营股份有限公司 | 用于靶向降解雌激素受体的化合物的结晶形式 |
| WO2023056069A1 (en) | 2021-09-30 | 2023-04-06 | Angiex, Inc. | Degrader-antibody conjugates and methods of using same |
| US11957759B1 (en) | 2022-09-07 | 2024-04-16 | Arvinas Operations, Inc. | Rapidly accelerated fibrosarcoma (RAF) degrading compounds and associated methods of use |
| WO2024159164A2 (en) | 2023-01-26 | 2024-08-02 | Arvinas Operations, Inc. | Cereblon-based kras degrading protacs ans uses related thereto |
| WO2024240858A1 (en) | 2023-05-23 | 2024-11-28 | Valerio Therapeutics | Protac molecules directed against dna damage repair system and uses thereof |
Family Cites Families (82)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1016828A (en) | 1961-11-13 | 1966-01-12 | Mcneilab Inc | Substituted morpholines and process for preparing same |
| US3518236A (en) | 1967-07-20 | 1970-06-30 | Uniroyal Inc | Acceleration of sulfur-vulcanization of rubber with sulfinic acids and derivatives |
| DE3246148A1 (de) | 1982-12-14 | 1984-06-14 | Troponwerke GmbH & Co KG, 5000 Köln | Pyrazolo(4.3-b)(1.4)oxazine, verfahren zu ihrer herstellung und ihre verwendung als arzneimittel |
| JP2604472B2 (ja) | 1989-07-12 | 1997-04-30 | 株式会社クラレ | 重合性組成物 |
| US5334720A (en) | 1991-03-07 | 1994-08-02 | Fisons Corporation | Diphenyl-1-(aminoalkyl)-2-piperidinone and -2-pyrrolidinone derivatives having anticonvulsant properties |
| WO1995023135A1 (en) | 1991-03-07 | 1995-08-31 | Fisons Corporation | Diphenyl-2-piperidinone and -2-pyrrolidinone derivatives having anti-convulsant and neuroprotective activity |
| EP0776324B1 (en) | 1994-08-19 | 2002-06-12 | Abbott Laboratories | Endothelin antagonists |
| EP0885215B1 (en) | 1996-02-13 | 2006-04-19 | Abbott Laboratories | Novel benzo-1,3-dioxolyl- and benzofuranyl substituted pyrrolidine derivatives as endothelin antagonists |
| AUPO527597A0 (en) * | 1997-02-24 | 1997-03-20 | Fujisawa Pharmaceutical Co., Ltd. | Novel heterocyclic compounds |
| US6159990A (en) | 1997-06-18 | 2000-12-12 | Synaptic Pharmaceutical Corporation | Oxazolidinones as α1A receptor antagonists |
| TR200101234T2 (tr) | 1997-08-04 | 2002-06-21 | Abbott Laboratories | Endotelin antagonistleri. |
| WO1999031507A1 (en) | 1997-12-18 | 1999-06-24 | Eli Lilly And Company | Peptidomimetic template-based combinatorial libraries |
| US6770658B2 (en) | 1998-09-09 | 2004-08-03 | Inflazyme Pharmaceuticals Ltd. | Substituted γ-phenyl-Δ-lactams and uses related thereto |
| US7214540B2 (en) | 1999-04-06 | 2007-05-08 | Uab Research Foundation | Method for screening crystallization conditions in solution crystal growth |
| US6630006B2 (en) | 1999-06-18 | 2003-10-07 | The Regents Of The University Of California | Method for screening microcrystallizations for crystal formation |
| US7052545B2 (en) | 2001-04-06 | 2006-05-30 | California Institute Of Technology | High throughput screening of crystallization of materials |
| US7195670B2 (en) | 2000-06-27 | 2007-03-27 | California Institute Of Technology | High throughput screening of crystallization of materials |
| WO2002017912A1 (en) | 2000-08-31 | 2002-03-07 | Abbott Laboratories | Endothelin antagonists |
| AU2002228598A1 (en) | 2000-11-20 | 2002-06-03 | Parallel Synthesis Technologies, Inc. | Methods and devices for high throughput crystallization |
| JP2004518688A (ja) | 2001-01-30 | 2004-06-24 | ブリストル−マイヤーズ スクイブ カンパニー | ファクターＸａ阻害剤のスルホンアミドラクタムおよびその方法 |
| DE60229059D1 (de) | 2001-05-08 | 2008-11-06 | Univ Yale | Proteomimetische verbindungen und verfahren |
| WO2002094787A1 (en) | 2001-05-23 | 2002-11-28 | Ucb, S.A. | 2-oxo-piperidinyl- and 2-oxo-azepanyl alkanoic acid derivativ es for the treatment of epilepsy and other neurological disorders |
| AU2002366278B2 (en) | 2001-12-18 | 2007-07-19 | F. Hoffmann-La Roche Ag | CIS-2,4,5- triphenyl-imidazolines and their use in the treatment of tumors |
| US6860940B2 (en) | 2002-02-11 | 2005-03-01 | The Regents Of The University Of California | Automated macromolecular crystallization screening |
| US7425638B2 (en) | 2003-06-17 | 2008-09-16 | Hoffmann-La Roche Inc. | Cis-imidazolines |
| JP4814228B2 (ja) | 2004-05-18 | 2011-11-16 | エフ．ホフマン−ラ ロシュ アーゲー | 新規ｃｉｓ−イミダゾリン |
| US7893278B2 (en) | 2004-06-17 | 2011-02-22 | Hoffman-La Roche Inc. | CIS-imidazolines |
| MX2007004551A (es) | 2004-10-18 | 2007-05-23 | Amgen Inc | Compuestos tiadiazol y metodos de uso. |
| CN101155784A (zh) | 2005-03-16 | 2008-04-02 | 霍夫曼-拉罗奇有限公司 | 顺式-2,4,5-三芳基-咪唑啉类化合物及其作为抗癌药物的应用 |
| HRP20110524T1 (hr) | 2005-04-04 | 2011-08-31 | Eisai R&D Management Co. | Spojevi dihidropiridina za neurodegenerativne bolesti i demenciju |
| EP2130822A1 (en) | 2005-12-01 | 2009-12-09 | F. Hoffmann-La Roche AG | 2,4,5-triphenyl imidazoline derivatives as inhibitors of the interaction between p53 and mdm2 proteins for use as anticancer agents |
| EP1981884B1 (en) | 2006-01-18 | 2012-06-13 | Amgen, Inc | Thiazole compounds as protein kinase b (pkb) inhibitors |
| US20070213341A1 (en) | 2006-03-13 | 2007-09-13 | Li Chen | Spiroindolinone derivatives |
| KR20090042779A (ko) | 2006-06-30 | 2009-04-30 | 쉐링 코포레이션 | Ｐ53 활성을 증가시키는 치환된 피페리딘 및 이의 사용 |
| WO2008010953A2 (en) | 2006-07-19 | 2008-01-24 | University Of Georgia Research Foundation, Inc. | Pyridinone diketo acids: inhibitors of hiv replication in combination therapy |
| US20080045560A1 (en) | 2006-08-15 | 2008-02-21 | Wyeth | Pyrrolidine and related derivatives useful as PR modulators |
| US7618989B2 (en) | 2006-08-15 | 2009-11-17 | Wyeth | Tricyclic oxazolidone derivatives useful as PR modulators |
| TW200831080A (en) | 2006-12-15 | 2008-08-01 | Irm Llc | Compounds and compositions as inhibitors of cannabinoid receptor 1 activity |
| GB0722769D0 (en) | 2007-11-21 | 2008-01-02 | Biolipox Ab | New compounds |
| US7705018B2 (en) | 2007-03-23 | 2010-04-27 | Amgen Inc. | Substituted quinolines and their uses in treatment of inflammatory and related conditions |
| PL2137186T3 (pl) | 2007-03-23 | 2016-09-30 | Związki heterocykliczne i ich zastosowania | |
| AU2008231384B2 (en) | 2007-03-23 | 2011-09-15 | Amgen Inc. | Heterocyclic compounds and their use |
| US7625895B2 (en) | 2007-04-12 | 2009-12-01 | Hoffmann-Le Roche Inc. | Diphenyl-dihydro-imidazopyridinones |
| WO2008130614A2 (en) | 2007-04-20 | 2008-10-30 | University Of Pittsburg-Of The Commonwealth System Of Higher Education | Selective and dual-action p53/mdm2/mdm4 antagonists |
| US7834179B2 (en) | 2007-05-23 | 2010-11-16 | Hoffmann-La Roche Inc. | Spiroindolinone derivatives |
| WO2009004430A1 (en) | 2007-06-29 | 2009-01-08 | Pfizer Inc. | N-benzyl oxazolidinones and related heterocycleic compounds as potentiators of glutamate receptors |
| CA2692720A1 (en) | 2007-07-09 | 2009-01-15 | Astrazeneca Ab | Morpholino pyrimidine derivatives used in diseases linked to mtor kinase and/or pi3k |
| AU2008276521B2 (en) | 2007-07-17 | 2011-11-03 | Amgen Inc. | Heterocyclic modulators of PKB |
| AU2008276512A1 (en) | 2007-07-17 | 2009-01-22 | Amgen Inc. | Thiadiazole modulators of PKB |
| ES2401557T3 (es) | 2007-08-02 | 2013-04-22 | Amgen, Inc | Moduladores de Pl3 cinasas y métodos de uso |
| RU2487127C2 (ru) | 2007-10-09 | 2013-07-10 | Ф.Хоффманн-Ля Рош Аг | Хиральные цис-имидазолины |
| US7776875B2 (en) | 2007-12-19 | 2010-08-17 | Hoffman-La Roche Inc. | Spiroindolinone derivatives |
| US7820665B2 (en) | 2007-12-19 | 2010-10-26 | Amgen Inc. | Imidazopyridazine inhibitors of PI3 kinase for cancer treatment |
| CA2709202C (en) | 2007-12-19 | 2013-04-23 | Amgen Inc. | Fused pyridine, pyrimidine and triazine compounds as cell cycle inhibitors |
| EP2222296A2 (en) | 2007-12-26 | 2010-09-01 | Eisai R&D Management Co., Ltd. | Ampa receptor antagonists and zonisamide for epilepsy |
| WO2009114950A1 (en) | 2008-03-21 | 2009-09-24 | Chlorion Pharma, Inc. | Substituted pyrrolidine and piperidine compounds, derivatives thereof, and methods for treating pain |
| WO2009126584A1 (en) | 2008-04-07 | 2009-10-15 | Amgen Inc. | Gem-disubstituted and spirocyclic amino pyridines/pyrimidines as cell cycle inhibitors |
| WO2009155121A2 (en) | 2008-05-30 | 2009-12-23 | Amgen Inc. | Inhibitors of pi3 kinase |
| GB0811643D0 (en) | 2008-06-25 | 2008-07-30 | Cancer Rec Tech Ltd | New therapeutic agents |
| TW201011009A (en) | 2008-09-15 | 2010-03-16 | Priaxon Ag | Novel pyrrolidin-2-ones |
| KR101380013B1 (ko) | 2008-09-18 | 2014-04-10 | 에프. 호프만-라 로슈 아게 | 치환 피롤리딘-2-카르복사미드 |
| US20110263647A1 (en) | 2009-01-15 | 2011-10-27 | Amgen Inc. | Fluoroisoquinoline substituted thiazole compounds and methods of use |
| CA2752527C (en) | 2009-02-18 | 2014-09-23 | Amgen Inc. | Indole/benzimidazole compounds as mtor kinase inhibitors |
| MX2011009796A (es) | 2009-03-20 | 2011-12-14 | Amgen Inc | Inhibidores de la cinasa pi3. |
| US8076482B2 (en) | 2009-04-23 | 2011-12-13 | Hoffmann-La Roche Inc. | 3,3′-spiroindolinone derivatives |
| UY32582A (es) | 2009-04-28 | 2010-11-30 | Amgen Inc | Inhibidores de fosfoinositida 3 cinasa y/u objetivo mamífero |
| JP2012526836A (ja) | 2009-05-13 | 2012-11-01 | アムジエン・インコーポレーテツド | Ｐｉｋｋ阻害薬としてのヘテロアリール化合物 |
| WO2010151791A1 (en) | 2009-06-25 | 2010-12-29 | Amgen Inc. | Heterocyclic compounds and their uses |
| SG176986A1 (en) | 2009-06-25 | 2012-02-28 | Amgen Inc | Polycyclic derivatives of pyridine and their use in the treatment of (inter alia) rheumatoid arthritis and similar diseases |
| CA2765819A1 (en) | 2009-06-25 | 2010-12-29 | Amgen Inc. | Heterocyclic compounds and their uses as inhibitors of pi3 k activity |
| US8754089B2 (en) | 2009-06-25 | 2014-06-17 | Amgen Inc. | Heterocyclic compounds and their uses |
| EA201200321A1 (ru) | 2009-08-26 | 2012-09-28 | Новартис Аг | Тетразамещенные гетероарильные соединения и их применение в качестве модуляторов mdm2 и/или mdm4 |
| US8088815B2 (en) | 2009-12-02 | 2012-01-03 | Hoffman-La Roche Inc. | Spiroindolinone pyrrolidines |
| US8440693B2 (en) | 2009-12-22 | 2013-05-14 | Novartis Ag | Substituted isoquinolinones and quinazolinones |
| JO2998B1 (ar) | 2010-06-04 | 2016-09-05 | Amgen Inc | مشتقات بيبيريدينون كمثبطات mdm2 لعلاج السرطان |
| CN102153557B (zh) | 2011-01-21 | 2013-03-20 | 中国科学院上海有机化学研究所 | 具有乙二胺骨架的多手性中心氮杂环卡宾前体盐、合成方法及用途 |
| WO2013049250A1 (en) | 2011-09-27 | 2013-04-04 | Amgen Inc. | Heterocyclic compounds as mdm2 inhibitors for the treatment of cancer |
| EP2958902B1 (en) | 2013-02-19 | 2017-11-15 | Amgen Inc. | Cis-morpholinone and other compounds as mdm2 inhibitors for the treatment of cancer |
| CN105121407B (zh) | 2013-02-28 | 2017-07-18 | 美国安进公司 | 用于治疗癌症的苯甲酸衍生物mdm2抑制剂 |
| WO2014151863A1 (en) | 2013-03-14 | 2014-09-25 | Amgen Inc. | Heteroaryl acid morpholinone compounds as mdm2 inhibitors for the treatment of cancer |
| JOP20200296A1 (ar) | 2013-06-10 | 2017-06-16 | Amgen Inc | عمليات صنع وأشكال بلورية من mdm2 مثبط |
| PT3068393T (pt) | 2013-11-11 | 2022-06-14 | Amgen Inc | Terapia de combinação, incluindo um inibidor de mdm2 e um ou mais agentes farmaceuticamente ativos adicionais para o tratamento de cancros |
-
2014
- 2014-03-13 WO PCT/US2014/026584 patent/WO2014151863A1/en not_active Ceased
- 2014-03-13 EP EP14716176.4A patent/EP2970237B1/en active Active
- 2014-03-13 CA CA2906538A patent/CA2906538C/en active Active
- 2014-03-13 MX MX2015012427A patent/MX374513B/es active IP Right Grant
- 2014-03-13 US US14/774,645 patent/US9758495B2/en active Active
- 2014-03-13 JP JP2016502187A patent/JP6377123B2/ja active Active
- 2014-03-13 AU AU2014236812A patent/AU2014236812B2/en active Active
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