JP2016520118A5 - - Google Patents
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- JP2016520118A5 JP2016520118A5 JP2016516280A JP2016516280A JP2016520118A5 JP 2016520118 A5 JP2016520118 A5 JP 2016520118A5 JP 2016516280 A JP2016516280 A JP 2016516280A JP 2016516280 A JP2016516280 A JP 2016516280A JP 2016520118 A5 JP2016520118 A5 JP 2016520118A5
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- pyrazol
- chlorophenyl
- cyclopropyl
- dihydropyrrolo
- 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
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- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims description 32
- 150000003839 salts Chemical class 0.000 claims description 29
- 150000001875 compounds Chemical class 0.000 claims description 27
- SEMXWBFSIDIGPO-UHFFFAOYSA-N 1,5-dihydropyrazol-4-one Chemical compound O=C1CNN=C1 SEMXWBFSIDIGPO-UHFFFAOYSA-N 0.000 claims description 20
- -1 3,8-dimethyl- [1,2,4] triazolo [4,3-a] pyridin-6-yl Chemical group 0.000 claims description 13
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 10
- 206010028980 Neoplasm Diseases 0.000 claims description 6
- 125000000217 alkyl group Chemical group 0.000 claims description 6
- 201000011510 cancer Diseases 0.000 claims description 6
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 6
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims description 6
- 125000001153 fluoro group Chemical group F* 0.000 claims description 6
- 239000003814 drug Substances 0.000 claims description 4
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- XMRBIQDRTZCVGG-OAQYLSRUSA-N (6r)-6-(4-chlorophenyl)-3-cyclopropyl-5-(3,7-dimethylbenzotriazol-5-yl)-1-methyl-6h-pyrrolo[3,4-c]pyrazol-4-one Chemical compound N=1N(C)C([C@H](N(C2=O)C=3C=C(C=4N=NN(C)C=4C=3)C)C=3C=CC(Cl)=CC=3)=C2C=1C1CC1 XMRBIQDRTZCVGG-OAQYLSRUSA-N 0.000 claims description 2
- AVVWKDYUXSFEJL-LJQANCHMSA-N (6r)-6-(4-chlorophenyl)-3-cyclopropyl-5-(3,8-dimethyl-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-1-methyl-6h-pyrrolo[3,4-c]pyrazol-4-one Chemical compound N=1N(C)C([C@H](N(C2=O)C=3C=C(C)C4=NN=C(N4N=3)C)C=3C=CC(Cl)=CC=3)=C2C=1C1CC1 AVVWKDYUXSFEJL-LJQANCHMSA-N 0.000 claims description 2
- MVAYDDZVYGANLI-HXUWFJFHSA-N (6r)-6-(4-chlorophenyl)-3-cyclopropyl-5-(8-methoxy-3-methyl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)-1-methyl-6h-pyrrolo[3,4-c]pyrazol-4-one Chemical compound N=1N(C)C([C@H](N(C2=O)C=3C=C(C4=NN=C(C)N4C=3)OC)C=3C=CC(Cl)=CC=3)=C2C=1C1CC1 MVAYDDZVYGANLI-HXUWFJFHSA-N 0.000 claims description 2
- 239000013543 active substance Substances 0.000 claims description 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 230000004952 protein activity Effects 0.000 claims description 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 3
- IWTFOFMTUOBLHG-UHFFFAOYSA-N 2-methoxypyridine Chemical compound COC1=CC=CC=N1 IWTFOFMTUOBLHG-UHFFFAOYSA-N 0.000 claims 2
- 125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 claims 2
- SCOGYYPZUPWMLU-JOCHJYFZSA-N (6r)-6-(4-chlorophenyl)-3-cyclopropyl-5-(3,8-dimethyl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)-1-(2-methoxyethyl)-6h-pyrrolo[3,4-c]pyrazol-4-one Chemical compound C=1([C@H](N(C(=O)C=11)C2=CN3C(C)=NN=C3C(C)=C2)C=2C=CC(Cl)=CC=2)N(CCOC)N=C1C1CC1 SCOGYYPZUPWMLU-JOCHJYFZSA-N 0.000 claims 1
- NCLGWTFZOQZNIS-GHTZIAJQSA-N (6r)-6-(4-chlorophenyl)-3-cyclopropyl-5-(3,8-dimethyl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)-1-[(2s)-3,3,3-trifluoro-2-hydroxypropyl]-6h-pyrrolo[3,4-c]pyrazol-4-one Chemical compound N=1N(C[C@H](O)C(F)(F)F)C([C@H](N(C2=O)C=3C=C(C)C4=NN=C(N4C=3)C)C=3C=CC(Cl)=CC=3)=C2C=1C1CC1 NCLGWTFZOQZNIS-GHTZIAJQSA-N 0.000 claims 1
- ZBIYSSHSZQVNSP-GOSISDBHSA-N (6r)-6-(4-chlorophenyl)-3-cyclopropyl-5-[3-(difluoromethyl)-8-methyl-[1,2,4]triazolo[4,3-a]pyridin-6-yl]-1-methyl-6h-pyrrolo[3,4-c]pyrazol-4-one Chemical compound N=1N(C)C([C@H](N(C2=O)C=3C=C(C4=NN=C(N4C=3)C(F)F)C)C=3C=CC(Cl)=CC=3)=C2C=1C1CC1 ZBIYSSHSZQVNSP-GOSISDBHSA-N 0.000 claims 1
- JBWFCYLPISSKIG-HXUWFJFHSA-N (6r)-6-(4-chlorophenyl)-3-cyclopropyl-5-[3-(fluoromethyl)-8-methyl-[1,2,4]triazolo[4,3-a]pyridin-6-yl]-1-methyl-6h-pyrrolo[3,4-c]pyrazol-4-one Chemical compound N=1N(C)C([C@H](N(C2=O)C=3C=C(C4=NN=C(CF)N4C=3)C)C=3C=CC(Cl)=CC=3)=C2C=1C1CC1 JBWFCYLPISSKIG-HXUWFJFHSA-N 0.000 claims 1
- XZYFNQNYLMTZIS-JOCHJYFZSA-N (6r)-6-(4-chlorophenyl)-5-(3,8-dimethyl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)-3-(2-methoxypyridin-3-yl)-1-methyl-6h-pyrrolo[3,4-c]pyrazol-4-one Chemical compound COC1=NC=CC=C1C1=NN(C)C2=C1C(=O)N(C1=CN3C(C)=NN=C3C(C)=C1)[C@@H]2C1=CC=C(Cl)C=C1 XZYFNQNYLMTZIS-JOCHJYFZSA-N 0.000 claims 1
- FRDVUWTYVBTBSE-UHFFFAOYSA-N 5-(8-amino-3-methyl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)-6-(4-chlorophenyl)-3-cyclopropyl-1-methyl-6h-pyrrolo[3,4-c]pyrazol-4-one Chemical compound C=1N2C(C)=NN=C2C(N)=CC=1N(C1=O)C(C=2C=CC(Cl)=CC=2)C(N(N=2)C)=C1C=2C1CC1 FRDVUWTYVBTBSE-UHFFFAOYSA-N 0.000 claims 1
- ADWUQOKWKQHUJB-FTYDEUEMSA-N 5-[(2R,4E)-4-[amino(cyclopropyl)methylidene]-2-(4-chlorophenyl)-3-methylimino-5-oxopyrrolidin-1-yl]-1,3-dimethylpyridin-2-one Chemical compound CC1=CC(=CN(C1=O)C)N2[C@@H](C(=NC)/C(=C(/C3CC3)\N)/C2=O)C4=CC=C(C=C4)Cl ADWUQOKWKQHUJB-FTYDEUEMSA-N 0.000 claims 1
- SNIKOFNWYKITGY-UHFFFAOYSA-N 6-(4-chlorophenyl)-3-cyclopropyl-5-(3,7-dimethylbenzotriazol-5-yl)-1-(2-methylpyrazol-3-yl)-6h-pyrrolo[3,4-c]pyrazol-4-one Chemical compound C=1C=2N(C)N=NC=2C(C)=CC=1N(C1=O)C(C=2C=CC(Cl)=CC=2)C2=C1C(C1CC1)=NN2C1=CC=NN1C SNIKOFNWYKITGY-UHFFFAOYSA-N 0.000 claims 1
- XMRBIQDRTZCVGG-UHFFFAOYSA-N 6-(4-chlorophenyl)-3-cyclopropyl-5-(3,7-dimethylbenzotriazol-5-yl)-1-methyl-6h-pyrrolo[3,4-c]pyrazol-4-one Chemical compound C=1C=2N(C)N=NC=2C(C)=CC=1N(C1=O)C(C=2C=CC(Cl)=CC=2)C(N(N=2)C)=C1C=2C1CC1 XMRBIQDRTZCVGG-UHFFFAOYSA-N 0.000 claims 1
- YTFVGFPLAOYSNF-UHFFFAOYSA-N 6-(4-chlorophenyl)-3-cyclopropyl-5-(3,8-dimethyl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)-1-(2-methylpyrazol-3-yl)-6h-pyrrolo[3,4-c]pyrazol-4-one Chemical compound C=1N2C(C)=NN=C2C(C)=CC=1N(C1=O)C(C=2C=CC(Cl)=CC=2)C2=C1C(C1CC1)=NN2C1=CC=NN1C YTFVGFPLAOYSNF-UHFFFAOYSA-N 0.000 claims 1
- ZRAGYVAOZMZDPY-UHFFFAOYSA-N 6-(4-chlorophenyl)-3-cyclopropyl-5-(3,8-dimethyl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)-1-methyl-6h-pyrrolo[3,4-c]pyrazol-4-one Chemical compound C=1N2C(C)=NN=C2C(C)=CC=1N(C1=O)C(C=2C=CC(Cl)=CC=2)C(N(N=2)C)=C1C=2C1CC1 ZRAGYVAOZMZDPY-UHFFFAOYSA-N 0.000 claims 1
- MLMDKPAWBXFXNA-UHFFFAOYSA-N 6-(4-chlorophenyl)-3-cyclopropyl-5-(3,8-dimethyl-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-1-(2-methylpyrazol-3-yl)-6h-pyrrolo[3,4-c]pyrazol-4-one Chemical compound N=1N2C(C)=NN=C2C(C)=CC=1N(C1=O)C(C=2C=CC(Cl)=CC=2)C2=C1C(C1CC1)=NN2C1=CC=NN1C MLMDKPAWBXFXNA-UHFFFAOYSA-N 0.000 claims 1
- AVVWKDYUXSFEJL-UHFFFAOYSA-N 6-(4-chlorophenyl)-3-cyclopropyl-5-(3,8-dimethyl-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-1-methyl-6h-pyrrolo[3,4-c]pyrazol-4-one Chemical compound N=1N2C(C)=NN=C2C(C)=CC=1N(C1=O)C(C=2C=CC(Cl)=CC=2)C(N(N=2)C)=C1C=2C1CC1 AVVWKDYUXSFEJL-UHFFFAOYSA-N 0.000 claims 1
- MDJXFKRWSHUIHK-YMOXTTMHSA-N COc1ncccc1C1NNC2C1C(=O)N([C@@H]2c1ccc(Cl)cc1)c1cc(C)c2nnc(C)n2c1 Chemical compound COc1ncccc1C1NNC2C1C(=O)N([C@@H]2c1ccc(Cl)cc1)c1cc(C)c2nnc(C)n2c1 MDJXFKRWSHUIHK-YMOXTTMHSA-N 0.000 claims 1
- 150000004657 carbamic acid derivatives Chemical class 0.000 claims 1
- OYDMPDMTZYTSSQ-UHFFFAOYSA-N tert-butyl n-[6-[6-(4-chlorophenyl)-3-cyclopropyl-1-methyl-4-oxo-6h-pyrrolo[3,4-c]pyrazol-5-yl]-3-methyl-[1,2,4]triazolo[4,3-a]pyridin-8-yl]carbamate Chemical compound C=1N2C(C)=NN=C2C(NC(=O)OC(C)(C)C)=CC=1N(C1=O)C(C=2C=CC(Cl)=CC=2)C(N(N=2)C)=C1C=2C1CC1 OYDMPDMTZYTSSQ-UHFFFAOYSA-N 0.000 claims 1
- PQIOSYKVBBWRRI-UHFFFAOYSA-N methylphosphonyl difluoride Chemical group CP(F)(F)=O PQIOSYKVBBWRRI-UHFFFAOYSA-N 0.000 description 3
- 125000004939 6-pyridyl group Chemical group N1=CC=CC=C1* 0.000 description 2
- 125000005843 halogen group Chemical group 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 description 1
- GTLGKZJPNAWIBT-UHFFFAOYSA-N ethyl n-[6-[6-(4-chlorophenyl)-3-cyclopropyl-1-methyl-4-oxo-6h-pyrrolo[3,4-c]pyrazol-5-yl]-3-methyl-[1,2,4]triazolo[4,3-a]pyridin-8-yl]carbamate Chemical compound C=1N2C(C)=NN=C2C(NC(=O)OCC)=CC=1N(C1=O)C(C=2C=CC(Cl)=CC=2)C(N(N=2)C)=C1C=2C1CC1 GTLGKZJPNAWIBT-UHFFFAOYSA-N 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13169441.6 | 2013-05-28 | ||
| EP13169441 | 2013-05-28 | ||
| PCT/IB2014/061736 WO2014191906A1 (en) | 2013-05-28 | 2014-05-27 | Pyrazolo-pyrrolidin-4-one derivatives as bet inhibitors and their use in the treatment of disease |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016520118A JP2016520118A (ja) | 2016-07-11 |
| JP2016520118A5 true JP2016520118A5 (https=) | 2017-06-29 |
Family
ID=48470849
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016516280A Pending JP2016520118A (ja) | 2013-05-28 | 2014-05-27 | Ｂｅｔ阻害剤としてのピラゾロ−ピロリジン−４−オン誘導体および疾患の処置におけるその使用 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US9624247B2 (https=) |
| EP (1) | EP3004108B1 (https=) |
| JP (1) | JP2016520118A (https=) |
| KR (1) | KR20160012195A (https=) |
| CN (1) | CN105263934B (https=) |
| AU (1) | AU2014272695B2 (https=) |
| BR (1) | BR112015029401A8 (https=) |
| CA (1) | CA2912986A1 (https=) |
| EA (1) | EA028175B1 (https=) |
| ES (1) | ES2656471T3 (https=) |
| MX (1) | MX2015016421A (https=) |
| PL (1) | PL3004108T3 (https=) |
| PT (1) | PT3004108T (https=) |
| WO (1) | WO2014191906A1 (https=) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG11201506924YA (en) | 2013-03-15 | 2015-09-29 | Incyte Corp | Tricyclic heterocycles as bet protein inhibitors |
| MX2015016421A (es) | 2013-05-28 | 2016-03-03 | Novartis Ag | Derivados de pirazolo-pirrolidin-4-ona como inhibidores de bet y su uso en el tratamiento de enfermedades. |
| EP3019502B1 (en) | 2013-07-08 | 2017-05-17 | Incyte Holdings Corporation | Tricyclic heterocycles as bet protein inhibitors |
| US9399640B2 (en) | 2013-11-26 | 2016-07-26 | Incyte Corporation | Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors |
| WO2015081189A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| WO2015095492A1 (en) | 2013-12-19 | 2015-06-25 | Incyte Corporation | Tricyclic heterocycles as bet protein inhibitors |
| PL3134403T3 (pl) | 2014-04-23 | 2020-07-13 | Incyte Corporation | 1H-pirolo[2,3-c]pirydyn-7(6H)-ony i pirazolo[3,4-c]pirydyn-7(6H)-ony jako inhibitory białek BET |
| JP6599979B2 (ja) | 2014-09-15 | 2019-10-30 | インサイト・コーポレイション | Ｂｅｔタンパク質阻害剤として用いるための三環式複素環化合物 |
| GB201504694D0 (en) | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Covalent conjugates |
| WO2017075377A1 (en) | 2015-10-29 | 2017-05-04 | Incyte Corporation | Amorphous solid form of a bet protein inhibitor |
| KR20180134860A (ko) | 2016-02-15 | 2018-12-19 | 체엠엠 - 포르슝스첸트룸 퓨어 몰레쿨라레 메디친 게엠베하 | 암의 치료를 위한 taf1 억제제 |
| CA3028689A1 (en) | 2016-06-20 | 2017-12-28 | Incyte Corporation | Crystalline solid forms of a bet inhibitor |
| US20190262355A1 (en) | 2016-11-14 | 2019-08-29 | Cemm-Forschungszentrum Für Molekulare Medizin Gmbh | Combination of a brd4 inhibitor and an antifolate for the therapy of cancer |
| JP7840635B2 (ja) | 2017-12-20 | 2026-04-06 | 貝達薬業股▲ふん▼有限公司 | ブロモドメインタンパク質阻害剤である化合物、および組成物 |
| KR20210031852A (ko) * | 2018-03-05 | 2021-03-23 | 클리니쿰 레히츠 데어 이자르 데어 테크니쉔 우니베르지테트 뮌헨 | 종양 세포 붕괴성 아데노바이러스와 cdk4/6 억제제의 조합물에 의한 종양의 치료 |
| MX2022000521A (es) * | 2019-07-12 | 2022-06-14 | Scenic Immunology B V | Compuestos n-sustituidos-3,4-(5-anillo fusionado)-5-fenil-pirrolid in-2-ona como inhibidores de la enzima isoqc y/o qc. |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
Family Cites Families (75)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3829420A (en) | 1970-07-13 | 1974-08-13 | Sumitomo Chemical Co | 3,4-dihydro-2(1h)-quinazolinones and preparation thereof |
| US4099002A (en) | 1970-12-23 | 1978-07-04 | Sumitomo Chemical Company, Limited | Quinazolinone derivatives and a process for production thereof |
| JPS4822715B1 (https=) | 1970-12-28 | 1973-07-07 | ||
| JPS5427356B2 (https=) | 1972-03-31 | 1979-09-10 | ||
| US4258187A (en) | 1977-06-16 | 1981-03-24 | E. I. Du Pont De Nemours And Company | Process for preparing quinazolinone oxides |
| US4335127A (en) | 1979-01-08 | 1982-06-15 | Janssen Pharmaceutica, N.V. | Piperidinylalkyl quinazoline compounds, composition and method of use |
| JPS5721388A (en) | 1980-07-11 | 1982-02-04 | Nippon Nohyaku Co Ltd | Condensed pyrazole derivative |
| DE3420799A1 (de) | 1984-06-04 | 1985-12-05 | Bayer Ag, 5090 Leverkusen | Chromogene 4,4-diaryl-dihydrochinazolone, ihre herstellung und verwendung |
| AU2436792A (en) | 1991-08-16 | 1993-03-16 | Merck & Co., Inc. | Quinazoline derivatives as inhibitors of hiv reverse transcriptase |
| US5508300A (en) | 1994-01-14 | 1996-04-16 | Pfizer Inc. | Dihydro pyrazolopyrroles, compositions and use |
| EP0958305B1 (en) | 1996-07-05 | 2008-06-04 | Cancer Research Technology Limited | Inhibitions of the interaction between p53 and mdm2 |
| HRP980143A2 (en) | 1997-04-09 | 1999-02-28 | Soo Sung Ko | 4,4-disubstituted-3,4-dihydro-2 (1h)-quinazolinones useful as hiv reverse transcriptase inhibitors |
| WO2000066560A1 (en) | 1999-05-04 | 2000-11-09 | American Home Products Corporation | Quinazolinone and benzoxazine derivatives as progesterone receptor modulators |
| JP2001302515A (ja) | 2000-04-18 | 2001-10-31 | Sumitomo Pharmaceut Co Ltd | ポリ（ａｄｐ−リボース）ポリメラーゼ阻害剤 |
| US6479499B1 (en) | 2000-06-28 | 2002-11-12 | National Science Council | 2-phenyl-4-quinazolinone compounds, 2-phenyl-4-alkoxy-quinazoline compounds and their pharmaceutical compositions |
| DK1320531T3 (da) | 2000-08-10 | 2011-01-03 | Pfizer Italia Srl | Bicyclo-pyrazoler, der er aktive som kinase inhibitorer, fremgangsmåde til fremstilling deraf og farmaceutiske sammensætninger, der indeholder disse |
| PL370823A1 (en) | 2001-12-18 | 2005-05-30 | F.Hoffmann-La Roche Ag | Cis-2,4,5- triphenyl-imidazolines and their use in the treatment of tumors |
| CA2473740A1 (en) | 2002-01-18 | 2003-07-31 | David Solow-Cordero | Methods of treating conditions associated with an edg receptor |
| US20060189511A1 (en) | 2002-05-13 | 2006-08-24 | Koblish Holly K | Method for cytoprotection through mdm2 and hdm2 inhibition |
| US7119111B2 (en) | 2002-05-29 | 2006-10-10 | Amgen, Inc. | 2-oxo-1,3,4-trihydroquinazolinyl derivatives and methods of use |
| AU2003253165A1 (en) | 2002-08-13 | 2004-02-25 | Warner-Lambert Company Llc | Pyrimidine fused bicyclic metalloproteinase inhibitors |
| JP2007524596A (ja) | 2003-02-28 | 2007-08-30 | トランスフォーム・ファーマシューティカルズ・インコーポレイテッド | 共結晶医薬組成物 |
| US20040214856A1 (en) | 2003-04-23 | 2004-10-28 | Pfizer Inc | Cannabinoid receptor ligands and uses thereof |
| US7145012B2 (en) | 2003-04-23 | 2006-12-05 | Pfizer Inc. | Cannabinoid receptor ligands and uses thereof |
| US20040213264A1 (en) | 2003-04-25 | 2004-10-28 | Nortel Networks Limited | Service class and destination dominance traffic management |
| EP1657238A4 (en) | 2003-08-22 | 2008-12-03 | Takeda Pharmaceutical | CONDENSATE PYRIMIDINE DERIVATIVE AND ITS USE |
| WO2005027882A1 (en) | 2003-09-22 | 2005-03-31 | Bionetworks Gmbh | Prevention and treatment of inflammation-induced and/or immune-mediated bone loss |
| KR20060127413A (ko) | 2003-11-25 | 2006-12-12 | 카이론 코포레이션 | 항암제로서의 퀴나졸리논 화합물 |
| 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 |
| EP1750706B1 (en) | 2004-06-01 | 2016-10-05 | University Of Virginia Patent Foundation | Dual small molecule inhibitors of cancer and angiogenesis |
| GB0419481D0 (en) | 2004-09-02 | 2004-10-06 | Cancer Rec Tech Ltd | Isoindolin-1-one derivatives |
| US20060069085A1 (en) | 2004-09-28 | 2006-03-30 | Rulin Zhao | Preparation of 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones |
| WO2006074262A1 (en) | 2005-01-05 | 2006-07-13 | Rigel Pharmaceuticals, Inc. | Ubiquitin ligase inhibitors |
| US20080153791A1 (en) | 2005-03-18 | 2008-06-26 | Onpharm Gmbh | 11Beta -Hydroxysteroid Dehydrogenases |
| WO2006100038A1 (en) | 2005-03-23 | 2006-09-28 | Syngenta Participations Ag | Triazolopyrimidine derivatives useful as fungicides |
| US7576082B2 (en) | 2005-06-24 | 2009-08-18 | Hoffman-La Roche Inc. | Oxindole derivatives |
| JP5222731B2 (ja) | 2005-12-12 | 2013-06-26 | ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ | キナーゼ阻害薬として活性な置換ピロロ−ピラゾール誘導体 |
| WO2007096334A1 (en) | 2006-02-24 | 2007-08-30 | Pfizer Italia Srl | Pyrrolopyrrolones active as kinase inhibitors |
| DE102006016426A1 (de) | 2006-04-07 | 2007-10-11 | Merck Patent Gmbh | Neuartige Cyclobutyl-Verbindungen als Kinase-Inhibitoren |
| WO2007144384A1 (en) | 2006-06-14 | 2007-12-21 | 4Sc Ag | Pyrazolopyrimidones |
| US8222288B2 (en) | 2006-08-30 | 2012-07-17 | The Regents Of The University Of Michigan | Small molecule inhibitors of MDM2 and the uses thereof |
| WO2008034039A2 (en) | 2006-09-15 | 2008-03-20 | Nexuspharma Inc. | Novel tetrahydro-isoquinolines |
| WO2008045529A1 (en) | 2006-10-12 | 2008-04-17 | Serenex, Inc. | Purine and pyrimidine derivatives for treatment of cancer and inflammatory diseases |
| TW200843739A (en) | 2007-03-30 | 2008-11-16 | Shionogi & Co | Novel pyrrolinone derivative and composition containing the same |
| 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 |
| WO2009086303A2 (en) | 2007-12-21 | 2009-07-09 | University Of Rochester | Method for altering the lifespan of eukaryotic organisms |
| UY31982A (es) | 2008-07-16 | 2010-02-26 | Boehringer Ingelheim Int | Derivados de 1,2-dihidropiridin-3-carboxamidas n-sustituidas |
| TW201016702A (en) | 2008-09-25 | 2010-05-01 | Shionogi & Co | Novel pyrrolinone derivative and pharmaceutical composition comprising the same |
| CN102272135A (zh) | 2008-10-08 | 2011-12-07 | 百时美施贵宝公司 | 唑并吡咯酮黑色素浓集激素受体-1拮抗剂 |
| JP5752601B2 (ja) | 2008-12-08 | 2015-07-22 | ブイエム ファーマ エルエルシー | タンパク質受容体チロシンキナーゼ阻害薬の組成物 |
| WO2010141738A2 (en) | 2009-06-03 | 2010-12-09 | President And Fellows Of Harvard College | Compositions and method for inhibiting tumor growth |
| GB0919423D0 (en) * | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| CU24130B1 (es) | 2009-12-22 | 2015-09-29 | Novartis Ag | Isoquinolinonas y quinazolinonas sustituidas |
| US8440693B2 (en) | 2009-12-22 | 2013-05-14 | Novartis Ag | Substituted isoquinolinones and quinazolinones |
| JP5844358B2 (ja) | 2010-06-22 | 2016-01-13 | グラクソスミスクライン エルエルシー | ベンゾトリアゾロジアゼピン化合物を含むブロモドメイン阻害剤 |
| US20120065210A1 (en) | 2010-09-15 | 2012-03-15 | Xin-Jie Chu | Substituted hexahydropyrrolo[1,2-c]imidazolones |
| GB201016880D0 (en) | 2010-10-07 | 2010-11-17 | Riotech Pharmaceuticals Ltd | Phosphodiesterase inhibitors |
| JP2014500870A (ja) | 2010-11-12 | 2014-01-16 | ザ、リージェンツ、オブ、ザ、ユニバーシティ、オブ、ミシガン | スピロ−オキシインドールｍｄｍ２アンタゴニスト |
| AR084070A1 (es) * | 2010-12-02 | 2013-04-17 | Constellation Pharmaceuticals Inc | Inhibidores del bromodominio y usos de los mismos |
| US9422292B2 (en) | 2011-05-04 | 2016-08-23 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| WO2012174487A2 (en) * | 2011-06-17 | 2012-12-20 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| WO2012175520A1 (en) | 2011-06-20 | 2012-12-27 | Novartis Ag | Hydroxy substituted isoquinolinone derivatives |
| US8859586B2 (en) | 2011-06-20 | 2014-10-14 | Novartis Ag | Cyclohexyl isoquinolinone compounds |
| WO2013027168A1 (en) | 2011-08-22 | 2013-02-28 | Pfizer Inc. | Novel heterocyclic compounds as bromodomain inhibitors |
| WO2013033268A2 (en) | 2011-08-29 | 2013-03-07 | Coferon, Inc. | Bivalent bromodomain ligands, and methods of using same |
| WO2013080141A1 (en) * | 2011-11-29 | 2013-06-06 | Novartis Ag | Pyrazolopyrrolidine compounds |
| WO2013097052A1 (en) | 2011-12-30 | 2013-07-04 | Abbott Laboratories | Bromodomain inhibitors |
| UY34591A (es) | 2012-01-26 | 2013-09-02 | Novartis Ag | Compuestos de imidazopirrolidinona |
| US20130281396A1 (en) | 2012-04-19 | 2013-10-24 | Rvx Therapeutics Inc. | Treatment of diseases by epigenetic regulation |
| US20130281399A1 (en) | 2012-04-19 | 2013-10-24 | Rvx Therapeutics Inc. | Treatment of diseases by epigenetic regulation |
| US20130281397A1 (en) | 2012-04-19 | 2013-10-24 | Rvx Therapeutics Inc. | Treatment of diseases by epigenetic regulation |
| CA2870931A1 (en) | 2012-04-20 | 2013-10-24 | Abbvie Inc. | Isoindolone derivatives |
| EP2855483B1 (en) | 2012-05-24 | 2017-10-25 | Novartis AG | Pyrrolopyrrolidinone compounds |
| US8975417B2 (en) * | 2013-05-27 | 2015-03-10 | Novartis Ag | Pyrazolopyrrolidine derivatives and their use in the treatment of disease |
| MX2015016421A (es) | 2013-05-28 | 2016-03-03 | Novartis Ag | Derivados de pirazolo-pirrolidin-4-ona como inhibidores de bet y su uso en el tratamiento de enfermedades. |
-
2014
- 2014-05-27 MX MX2015016421A patent/MX2015016421A/es unknown
- 2014-05-27 EP EP14728350.1A patent/EP3004108B1/en not_active Not-in-force
- 2014-05-27 ES ES14728350.1T patent/ES2656471T3/es active Active
- 2014-05-27 EA EA201592255A patent/EA028175B1/ru not_active IP Right Cessation
- 2014-05-27 CA CA2912986A patent/CA2912986A1/en not_active Abandoned
- 2014-05-27 CN CN201480030590.0A patent/CN105263934B/zh not_active Expired - Fee Related
- 2014-05-27 PT PT147283501T patent/PT3004108T/pt unknown
- 2014-05-27 JP JP2016516280A patent/JP2016520118A/ja active Pending
- 2014-05-27 US US14/892,623 patent/US9624247B2/en not_active Expired - Fee Related
- 2014-05-27 AU AU2014272695A patent/AU2014272695B2/en not_active Ceased
- 2014-05-27 WO PCT/IB2014/061736 patent/WO2014191906A1/en not_active Ceased
- 2014-05-27 BR BR112015029401A patent/BR112015029401A8/pt not_active Application Discontinuation
- 2014-05-27 KR KR1020157036224A patent/KR20160012195A/ko not_active Withdrawn
- 2014-05-27 PL PL14728350T patent/PL3004108T3/pl unknown
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