DK2925761T3 - Triazolpyraziner som BRD4-hæmmere til anvendelse i behandling af cancer - Google Patents
Triazolpyraziner som BRD4-hæmmere til anvendelse i behandling af cancer Download PDFInfo
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- DK2925761T3 DK2925761T3 DK13789833.4T DK13789833T DK2925761T3 DK 2925761 T3 DK2925761 T3 DK 2925761T3 DK 13789833 T DK13789833 T DK 13789833T DK 2925761 T3 DK2925761 T3 DK 2925761T3
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- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
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- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- C07C211/44—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having amino groups bound to only one six-membered aromatic ring
- C07C211/49—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having amino groups bound to only one six-membered aromatic ring having at least two amino groups bound to the carbon skeleton
- C07C211/50—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having amino groups bound to only one six-membered aromatic ring having at least two amino groups bound to the carbon skeleton with at least two amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
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- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
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- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
- C07D295/135—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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Claims (30)
1. Forbindelse med formlen (I)
(I) hvor R1 er -Ci-3-alkyl eller -Ci-3-haloalkyl; R2 er udvalgt blandt -NHR4, -Ci-5-alkyl, -Ci-5-haloalkyl, halogen og -S-Ci-3-alkyl; R3 er en 5-12-leddet heteroaryl, hvilken gruppe er substitueret med -X-R10 og eventuelt yderligere substitueret med en eller flere grupper uafhængigt udvalgt blandt R9; R4 er udvalgt blandt -Ci-5-alkyl og 5-12-leddet heterocykloalkyl, hvilken heterocykloalkyl eventuelt kan være substitueret med en eller flere grupper uafhængigt udvalgt blandt R5; R5 er udvalgt blandt -Ci-5-alkyl, -Ci-5-haloalkyl og -Ci-3-alkylen-0-Ci-3-alkyl; R9 er udvalgt blandt -Ci-5-alkyl, -O-Ci-5-alkyl, -N(Ci-5-alkyl)2, halogen, -Ci-3-alkylen-0-Ci-3-alkyl, -Ci-5-alkylen-N(-Ci-5-alkyl,-Ci-5-alkyl), 5-12-leddet heterocykloalkyl, hvor heterocykloalkylgruppen eventuelt kan være substitueret med en eller flere grupper uafhængigt udvalgt blandt =0, -Ci-3-alkyl, eller R9 er udvalgt blandt -C6-io-aryl og 5-12-leddet heteroaryl, hvor aryl- og heteroarylgrupperne eventuelt og uafhængigt kan være substituerede med en eller flere grupper udvalgt blandt halogen, -Ci-3-alkyl, -O-Ci-3-alkyl, -Ci-3-haloalkyl, -O-Ci-3-haloalkyl, -N(Ci-5-alkyl, Ci-5-alkyl) og -NH-Ci-5-alkyl; X er -Ci-3-alkylen- eller -0-; R10 er -C6-io-aryl eller 5-12-leddet heteroaryl, idet hver enkelt gruppe eventuelt kan være substitueret med en eller flere grupper udvalgt blandt halogen, -Ci-3-alkyl, -O-Ci-3-alkyl, -Ci-3-haloalkyl, -O-Ci-3-haloalkyl; hvor forbindelserne med formlen (I) eventuelt kan være til stede i form af salte.
2. Forbindelse ifølge krav 1, hvor R1 er -CH3.
3. Forbindelse ifølge krav 1 eller 2, hvor R2 er -NFIR4, og R4 er en 5-6-leddet heterocykloalkyl, eventuelt substitueret som defineret i krav 1.
4. Forbindelse ifølge krav 3, hvor R4 er tetrahydrofuran eller piperidin, hvor piperidinen er substitueret med én gruppe udvalgt blandt -CFI3, -CH2CH3,-CH2CH2CH3 og -(CH2)2-0-CH3.
5. Forbindelse ifølge et hvilket som helst af kravene 1 eller 2, hvor R2 er -NFIR4, og R4 er -Ci-3-alkyl.
5. Forbindelse ifølge krav 5, hvor R2 er -NHR4, og R4 er -CH3 eller -CH(CH3)2.
7. Forbindelse ifølge et hvilket som helst af kravene 1 eller 2, hvor R2 er -Ci-3-alkyl.
8. Forbindelse ifølge et hvilket som helst af kravene 1 til 7, hvor R3 er en 5-9-leddet heteroaryl substitueret med -X-R10 og eventuelt yderligere substitueret med en eller flere grupper uafhængigt udvalgt blandt R9, hvor R9, X og R10 er definerede som i krav 1.
9. Forbindelse ifølge et hvilket som helst af kravene 1 til 8, hvor -X-R10 er udvalgt blandt -CH2-phenyl, -CH(CH3)-phenyl, -CH2-pyridyl, -CH(CH3)-pyridyl, -O-phenyl, idet hver enkelt af disse phenyl- eller pyridylgrupper eventuelt er substitueret med -F eller -CH3.
10. Forbindelse ifølge krav 9, hvor -X-R10 er udvalgt blandt -CFI2-phenyl, -CH2-pyridyl, -CFI(CFI3)-phenyl, -CH(CH3)-pyridyl, idet hver enkelt af disse pyridyl- eller phenylgrupper eventuelt er substitueret med -F eller -CH3.
11. Forbindelse ifølge krav 8, hvor R3 er udvalgt blandt pyrazolyl, imidazol, benzimidazolyl, imidazopyridin og imidazopyrimidin, og R3 er substitueret med -X-R10, og R3 er eventuelt yderligere substitueret med en eller flere grupper uafhængigt udvalgt blandt R9, hvor R9, X og R10 er defineret som i krav 1.
12. Forbindelse ifølge et hvilket som helst af kravene 1 til 11, hvor R9 er uafhængigt udvalgt blandt -Ci-3-alkyl, -0-Ci-3-alkyl, -N(Ci-3-alkyl)2, phenyl og 6-leddet heterocykloalkyl, hvilken heterocykloalkyl eventuelt kan være substitueret med en eller flere grupper uafhængigt udvalgt blandt =0 og -Ci-3-alkyl.
13. Forbindelse ifølge krav 11, hvor R3 er imidazopyridin eller benzimidazol substitueret med -CFb-phenyl eller -CFh-pyridyl, -CH(CH3)-pyridyl og eventuelt yderligere substitueret med -Ci-3-alkyl eller 5-12-leddet heterocykloalkyl, hvor heterocykloalkylgruppen eventuelt kan være substitueret med en eller flere grupper uafhængigt udvalgt blandt -Ci-3-alkyl.
14. Forbindelse ifølge krav 13, hvor R3 er imidazopyridin eller benzimidazol substitueret med -CFl2-phenyl, -CH(CH3)-pyridyl eller -CH2-pyridyl og med -CFI(CFl3)2 eller morpholinyl eller piperazinyl, hvor morpholinyl- eller piperazinylgrupperne eventuelt er substitueret med en eller flere grupper udvalgt blandt -Ci-3-alkyl.
15. Forbindelse ifølge krav 1 udvalgt blandt
h
I hvor forbindelsen eventuelt kan være til stede i form af et salt deraf. 16.
Forbindelse ifølge krav 1 eller 15 (III-13), hvor forbindelsen eventuelt kan være til stede i form af et salt deraf.
17. Forbindelse ifølge krav 1 eller 15 (III-8),
hvor forbindelsen eventuelt kan være til stede i form af et salt deraf.
18. Forbindelse ifølge krav 1 eller 15 (III-40),
hvor forbindelsen eventuelt kan være til stede i form af et salt deraf.
19. Forbindelse ifølge krav 1 eller 15 (III-26),
hvor forbindelsen eventuelt kan være til stede i form af et salt deraf.
20. Forbindelse ifølge krav 1 eller 15 (III-19),
hvor forbindelsen eventuelt kan være til stede i form af et salt deraf.
21. Forbindelse ifølge krav 1 eller 15 (III-30),
hvor forbindelsen eventuelt kan være til stede i form af et salt deraf.
22. Forbindelse ifølge krav 1 eller 15 (III-20),
hvor forbindelsen eventuelt kan være til stede i form af et salt deraf.
23. Forbindelse ifølge krav 1 eller 15 (III-21),
5 hvor forbindelsen eventuelt kan være til stede i form af et salt deraf.
->λ FnrhinHeice ifølge krav 1 eller 15 (III-l), < hvor forbindelsen eventuelt kan være til stede i form af et salt deraf.
25. Forbindelse ifølge krav 1 eller 15 (III-27),
hvor forbindelsen eventuelt kan være til stede i form af et salt deraf.
26. Forbindelse med den almene formel (I) ifølge et hvilket som helst af kravene 1 til 25 - eller et farmaceutisk acceptabelt salt deraf - til anvendelse i behandling og/eller forebyggelse af cancer.
27. Forbindelse med den almene formel (I) ifølge et hvilket som helst af kravene 1 til 26 eller et salt deraf i form af hydrater, solvater eller polymorfer.
28. Farmaceutisk præparat omfattende som virksom bestanddel en eller flere forbindelser med den almene formel (I) ifølge et hvilket som helst af kravene 1 til 25 eventuelt i kombination med gængse excipienser og/eller bærestoffer.
29. Farmaceutisk præparat omfattende en forbindelse med den almene formel (I) ifølge et hvilket som helst af kravene 1 til 25 - eller et af de farmaceutisk acceptable salte deraf- og mindst ét andet cytostatisk eller cytotoksisk aktivt stof, der adskiller sig fra formel (I)·
30. Forbindelse med den almene formel (I) ifølge et hvilket som helst af kravene 1 til 25 - eller de farmaceutisk acceptable salte deraf - til anvendelse som lægemidler.
31. Forbindelse med den almene formel (I) ifølge et hvilket som helst af kravene 1 til 25 - eller de farmaceutisk acceptable salte deraf - til anvendelse i behandlingen af hæmatopoietiske lidelser.
32. Forbindelse med den almene formel (I) ifølge et hvilket som helst af kravene 1 til 25 - eller de farmaceutisk acceptable salte deraf - til anvendelse i behandling af akut myeoloid leukæmi eller multipelt myelom.
33. Forbindelse med den almene formel (I) ifølge et hvilket som helst af kravene 1 til 25 - eller de farmaceutisk acceptable salte deraf - til anvendelse i behandling af lunge-, lever-, tyktarms-, hjerne-, skjoldbruskkirtel, bugspytkirtel-, bryst-, æggestok- og blærehalskirtelcancer.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
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EP12192987 | 2012-11-16 | ||
PCT/EP2013/073946 WO2014076237A1 (en) | 2012-11-16 | 2013-11-15 | Triazolopyrazine |
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Publication Number | Publication Date |
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DK2925761T3 true DK2925761T3 (da) | 2017-09-18 |
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Application Number | Title | Priority Date | Filing Date |
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DK13789833.4T DK2925761T3 (da) | 2012-11-16 | 2013-11-15 | Triazolpyraziner som BRD4-hæmmere til anvendelse i behandling af cancer |
Country Status (38)
Country | Link |
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US (3) | US9266891B2 (da) |
EP (1) | EP2925761B1 (da) |
JP (1) | JP5959754B2 (da) |
KR (1) | KR102190087B1 (da) |
CN (2) | CN107266455B (da) |
AP (1) | AP2015008418A0 (da) |
AR (1) | AR093515A1 (da) |
AU (1) | AU2013346809B9 (da) |
BR (1) | BR112015011158B1 (da) |
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Families Citing this family (26)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US9266891B2 (en) * | 2012-11-16 | 2016-02-23 | Boehringer Ingelheim International Gmbh | Substituted [1,2,4]triazolo[4,3-A]pyrazines that are BRD4 inhibitors |
US9428513B2 (en) | 2013-11-07 | 2016-08-30 | Boehringer Ingelheim International Gmbh | Triazolopyrazine |
GB201321737D0 (en) * | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic Agents |
GB201504694D0 (en) | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Covalent conjugates |
CN105669733A (zh) * | 2016-01-29 | 2016-06-15 | 上海毕路得医药科技有限公司 | 一种1-甲基-1h-吡唑-3-硼酸频哪醇酯的合成方法 |
KR20190103154A (ko) * | 2016-11-14 | 2019-09-04 | 체엠엠 - 포르슝스첸트룸 퓨어 몰레쿨라레 메디친 게엠베하 | 암의 치료법을 위한 brd4 억제제 및 항폴레이트의 조합 |
CN109111437B (zh) * | 2017-06-22 | 2022-03-04 | 中国科学院广州生物医药与健康研究院 | 一种苯并[d]异恶唑类化合物及其制备方法和应用 |
KR20200040764A (ko) | 2017-07-18 | 2020-04-20 | 누베이션 바이오 인크. | 1,8-나프티리디논 화합물 및 그의 용도 |
MX2020000690A (es) | 2017-07-18 | 2020-07-29 | Nuvation Bio Inc | Compuestos heterociclicos como antagonistas de adenosina. |
US20210038602A1 (en) * | 2018-01-25 | 2021-02-11 | Boehringer Ingelheim International Gmbh | Combination treatment of acute myeloid leukemia |
AU2019256534A1 (en) | 2018-04-19 | 2020-10-22 | Ember Technologies, Inc. | Portable cooler with active temperature control |
CN108794484B (zh) * | 2018-04-28 | 2020-04-24 | 北京施安泰医药技术开发有限公司 | [1,2,4]三唑并[4,3-a]吡嗪衍生物、其药物组合物、制备方法和应用 |
BR112021007982A2 (pt) | 2018-10-30 | 2021-08-03 | Nuvation Bio Inc. | compostos heterocíclicos como inibidores de bet |
KR20210113233A (ko) | 2019-01-11 | 2021-09-15 | 엠버 테크놀로지스 인코포레이티드 | 능동적 온도 제어 기능을 가진 휴대용 쿨러 |
US11306071B2 (en) | 2019-01-18 | 2022-04-19 | Nuvation Bio Inc. | Heterocyclic compounds as adenosine antagonists |
JP2022523473A (ja) | 2019-01-18 | 2022-04-25 | ニューベイション・バイオ・インコーポレイテッド | 1,8-ナフチリジジノン化合物およびそれらの使用 |
KR20220027144A (ko) | 2019-06-25 | 2022-03-07 | 엠버 테크놀로지스 인코포레이티드 | 휴대용 쿨러 |
US11668508B2 (en) | 2019-06-25 | 2023-06-06 | Ember Technologies, Inc. | Portable cooler |
US11162716B2 (en) | 2019-06-25 | 2021-11-02 | Ember Technologies, Inc. | Portable cooler |
CA3145827A1 (en) | 2019-07-02 | 2021-01-07 | Nuvation Bio Inc. | Heterocyclic compounds as bet inhibitors |
EP4035124A4 (en) * | 2019-09-25 | 2023-10-11 | Subtle Medical, Inc. | SYSTEMS AND METHODS FOR IMPROVING LOW-DOSE VOLUMETRIC CONTRAST-ENHANCED MRI |
KR20220077138A (ko) | 2019-09-30 | 2022-06-08 | 쿄와 기린 가부시키가이샤 | Bet 분해제 |
WO2021175432A1 (en) | 2020-03-04 | 2021-09-10 | Boehringer Ingelheim International Gmbh | Method for administration of an anti cancer agent |
CN115769034A (zh) | 2020-04-03 | 2023-03-07 | 恩伯生命科学有限公司 | 具有主动温度控制的便携式冷却器 |
WO2022184664A1 (en) * | 2021-03-02 | 2022-09-09 | Boehringer Ingelheim International Gmbh | Anticancer combination therapy |
EP4313308A1 (en) * | 2021-03-26 | 2024-02-07 | Cedilla Therapeutics, Inc. | Tead inhibitors and uses thereof |
Family Cites Families (24)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3915968A (en) | 1973-09-21 | 1975-10-28 | Lepetit Spa | Triazolopyridazines |
BR9814628A (pt) | 1997-11-11 | 2001-11-27 | Ono Pharmaceutical Co | Derivados de pirazina fundidos |
RS55630B1 (sr) | 2005-12-21 | 2017-06-30 | Janssen Pharmaceutica Nv | Triazolopiridazini kao modulatori tirozin kinaze |
WO2008109104A1 (en) | 2007-03-07 | 2008-09-12 | The Regents Of The University Of California | Bivalent inhibitors of akt protein kinase |
WO2008130951A1 (en) | 2007-04-17 | 2008-10-30 | Bristol-Myers Squibb Company | Fused heterocyclic 11-beta-hydroxysteroid dehydrogenase type i inhibitors |
BRPI0821676A2 (pt) | 2007-12-21 | 2015-06-16 | Astrazeneca Ab | Composto, composição farmacêutica, e, processo para a preparação dos compostos. |
EP2239264A4 (en) * | 2007-12-28 | 2012-01-11 | Mitsubishi Tanabe Pharma Corp | ANTITUMOR AGENT |
GB0919423D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
AU2010314395B2 (en) | 2009-11-05 | 2015-04-09 | Glaxosmithkline Llc | Benzodiazepine bromodomain inhibitor |
EP2526102B1 (en) | 2010-01-22 | 2017-03-08 | Fundación Centro Nacional de Investigaciones Oncológicas Carlos III | Inhibitors of PI3 kinase |
TW201200518A (en) | 2010-03-10 | 2012-01-01 | Kalypsys Inc | Heterocyclic inhibitors of histamine receptors for the treatment of disease |
WO2011161031A1 (en) | 2010-06-22 | 2011-12-29 | Glaxosmithkline Llc | Benzotriazolodiazepine compounds inhibitors of bromodomains |
EP2705039B1 (en) | 2011-05-04 | 2017-07-26 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
US9328117B2 (en) | 2011-06-17 | 2016-05-03 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
DE102011082013A1 (de) * | 2011-09-01 | 2013-03-07 | Bayer Pharma AG | 6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine |
AU2013259344A1 (en) | 2012-05-11 | 2014-11-13 | Abbvie Inc. | Nampt inhibitors |
AU2013340483B2 (en) * | 2012-09-28 | 2018-01-18 | Oncoethix Gmbh | Pharmaceutical formulation containing thienotriazolodiazepine compounds |
US9422290B2 (en) | 2012-11-13 | 2016-08-23 | Boehringer Ingelheim International Gmbh | Triazolopyridazine |
US9266891B2 (en) | 2012-11-16 | 2016-02-23 | Boehringer Ingelheim International Gmbh | Substituted [1,2,4]triazolo[4,3-A]pyrazines that are BRD4 inhibitors |
EP2978757B1 (en) | 2013-03-27 | 2017-02-08 | Boehringer Ingelheim International GmbH | Indolinone analogues as brd4 inhibitors |
US9199988B2 (en) | 2013-03-27 | 2015-12-01 | Boehringer Ingelheim International Gmbh | Dihydroquinazolinone analogues |
US20150051208A1 (en) | 2013-08-14 | 2015-02-19 | Boehringer Ingelheim International Gmbh | Pyridinones |
US9428513B2 (en) | 2013-11-07 | 2016-08-30 | Boehringer Ingelheim International Gmbh | Triazolopyrazine |
US9428515B2 (en) | 2014-05-09 | 2016-08-30 | Boehringer Ingelheim International Gmbh | Benzimidazole derivatives |
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