HRP20161674T1 - 4-(8-METOKSI-1-((1-METOKSIPROPAN-2-IL)-2-(TETRAHIDRO-2H-PIRAN-4-IL)-1H-IMIDAZO[4,5-c]KINOLIN-7-IL)-3,5-DIMETILIZOKSAZOL I NJEGOVA UPOTREBA KAO INHIBITORA BROMODOMENE - Google Patents
4-(8-METOKSI-1-((1-METOKSIPROPAN-2-IL)-2-(TETRAHIDRO-2H-PIRAN-4-IL)-1H-IMIDAZO[4,5-c]KINOLIN-7-IL)-3,5-DIMETILIZOKSAZOL I NJEGOVA UPOTREBA KAO INHIBITORA BROMODOMENE Download PDFInfo
- Publication number
- HRP20161674T1 HRP20161674T1 HRP20161674TT HRP20161674T HRP20161674T1 HR P20161674 T1 HRP20161674 T1 HR P20161674T1 HR P20161674T T HRP20161674T T HR P20161674TT HR P20161674 T HRP20161674 T HR P20161674T HR P20161674 T1 HRP20161674 T1 HR P20161674T1
- Authority
- HR
- Croatia
- Prior art keywords
- compound
- pharmaceutically acceptable
- cancer
- acceptable salt
- dimethylisoxazole
- Prior art date
Links
- 229940125763 bromodomain inhibitor Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 13
- 150000003839 salts Chemical class 0.000 claims 10
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 239000000825 pharmaceutical preparation Substances 0.000 claims 2
- HYPXHDJBILNWLI-UHFFFAOYSA-N 4-[8-methoxy-1-(1-methoxypropan-2-yl)-2-(oxan-4-yl)imidazo[4,5-c]quinolin-7-yl]-3,5-dimethyl-1,2-oxazole Chemical compound COC1=CC2=C3N(C(C)COC)C(C4CCOCC4)=NC3=CN=C2C=C1C=1C(C)=NOC=1C HYPXHDJBILNWLI-UHFFFAOYSA-N 0.000 claims 1
- HYPXHDJBILNWLI-CQSZACIVSA-N 4-[8-methoxy-1-[(2r)-1-methoxypropan-2-yl]-2-(oxan-4-yl)imidazo[4,5-c]quinolin-7-yl]-3,5-dimethyl-1,2-oxazole Chemical compound COC1=CC2=C3N([C@H](C)COC)C(C4CCOCC4)=NC3=CN=C2C=C1C=1C(C)=NOC=1C HYPXHDJBILNWLI-CQSZACIVSA-N 0.000 claims 1
- HYPXHDJBILNWLI-AWEZNQCLSA-N 4-[8-methoxy-1-[(2s)-1-methoxypropan-2-yl]-2-(oxan-4-yl)imidazo[4,5-c]quinolin-7-yl]-3,5-dimethyl-1,2-oxazole Chemical compound COC1=CC2=C3N([C@@H](C)COC)C(C4CCOCC4)=NC3=CN=C2C=C1C=1C(C)=NOC=1C HYPXHDJBILNWLI-AWEZNQCLSA-N 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 208000011691 Burkitt lymphomas Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 206010029260 Neuroblastoma 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
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 230000001363 autoimmune Effects 0.000 claims 1
- 239000002585 base Substances 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- YKGMKSIHIVVYKY-UHFFFAOYSA-N dabrafenib mesylate Chemical class CS(O)(=O)=O.S1C(C(C)(C)C)=NC(C=2C(=C(NS(=O)(=O)C=3C(=CC=CC=3F)F)C=CC=2)F)=C1C1=CC=NC(N)=N1 YKGMKSIHIVVYKY-UHFFFAOYSA-N 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 239000012458 free base Substances 0.000 claims 1
- 230000004968 inflammatory condition Effects 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 229940127557 pharmaceutical product Drugs 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Immunology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Transplantation (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Claims (12)
1. Spoj formule (I), naznačen time što je 4-(8-metoksi-1-(1-metoksipropan-2-il)-2-(tetrahidro-2H-piran-4-il)-1H-imidazo[4,5-c]kinolin-7-il)-3,5-dimetilizoksazol,
[image]
,
ili njegova sol.
2. Spoj formule (IA) u skladu s patentnim zahtjevom 1, naznačen time što je 4-(8-metoksi-1-((R)-1-metoksipropan-2-il)-2-(tetrahidro-2H-piran-4-il)-1H-imidazo[4,5-c]kinolin-7-il)-3,5-dimetilizoksazol,
[image]
,
ili njegova sol.
3. Spoj formule (IB) u skladu s patentnim zahtjevom 1, naznačen time što je 4-(8-metoksi-1-((S)-1-metoksipropan-2-il)-2-(tetrahidro-2H-piran-4-il)-1H-imidazo[4,5-c]kinolin-7-il)-3,5-dimetilizoksazol,
[image]
,
ili njegova sol.
4. Spoj, naznačen time što je spoj u skladu s bilo kojim od patentnih zahtjeva 1-3, ili njegova farmaceutski prihvatljiva sol.
5. Spoj u skladu s patentnim zahtjevom 4, naznačen time što je u obliku slobodne baze.
6. Spoj u skladu s patentnim zahtjevom 4, naznačen time što je u obliku metansulfonatne soli.
7. Farmaceutski pripravak, naznačen time što sadrži spoj, ili njegovu farmaceutski prihvatljivu sol, u skladu s patentnim zahtjevom 4, kao i jednu ili više farmaceutski prihvatljivih podloga, razrjeđivača ili pomoćnih tvari.
8. Kombinirani farmaceutski proizvod, naznačen time što sadrži spoj, ili njegovu farmaceutski prihvatljivu sol, u skladu s patentnim zahtjevom 4, uz jedno ili više drugih terapijski aktivnih sredstava.
9. Spoj, ili njegova farmaceutski prihvatljiva sol, u skladu s patentnim zahtjevom 4, naznačen time što je namijenjen upotrebi u terapiji.
10. Spoj, ili njegova farmaceutski prihvatljiva sol, u skladu s patentnim zahtjevom 4, naznačen time što je namijenjen upotrebi u liječenju kroničnog autoimunog i/ili upalnog stanja.
11. Spoj, ili njegova farmaceutski prihvatljiva sol, u skladu s patentnim zahtjevom 4, naznačen time što je namijenjen upotrebi u liječenju raka.
12. Spoj, ili njegova farmaceutski prihvatljiva sol, namijenjen upotrebi u skladu s patentnim zahtjevom 11, naznačen time što se rak bira između leukemije, NUT karcinoma središnje linije, multiplog mijeloma, neuroblastoma, Burkittovog limfoma, raka vrata maternice, raka jednjaka, raka jajnika, raka dojke i kolorektalnog raka.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1114103.3A GB201114103D0 (en) | 2011-08-17 | 2011-08-17 | Novel compounds |
| EP12748028.3A EP2744809B1 (en) | 2011-08-17 | 2012-08-15 | 4-(8-methoxy-1-((1-methoxypropan-2-yl)-2-(tetrahydro-2h-pyran-4-yl)-1 h-imidazo[4,5-c]quinolin-7-yl)-3,5-dimethylisoxazole and its use as bromodomain inhibitor |
| PCT/EP2012/065918 WO2013024104A1 (en) | 2011-08-17 | 2012-08-15 | 4-(8-methoxy-1-((1-methoxypropan-2-yl)-2-(tetrahydro-2h-pyran-4-yl)-1 h-imidazo[4,5-c]quinolin-7-yl)-3,5-dimethylisoxazole and its use as bromodomain inhibitor |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20161674T1 true HRP20161674T1 (hr) | 2017-01-27 |
Family
ID=44764570
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20161674TT HRP20161674T1 (hr) | 2011-08-17 | 2016-12-08 | 4-(8-METOKSI-1-((1-METOKSIPROPAN-2-IL)-2-(TETRAHIDRO-2H-PIRAN-4-IL)-1H-IMIDAZO[4,5-c]KINOLIN-7-IL)-3,5-DIMETILIZOKSAZOL I NJEGOVA UPOTREBA KAO INHIBITORA BROMODOMENE |
Country Status (37)
| Country | Link |
|---|---|
| US (4) | US9067936B2 (hr) |
| EP (2) | EP3150601A1 (hr) |
| JP (1) | JP6059723B2 (hr) |
| KR (1) | KR20140064878A (hr) |
| CN (1) | CN103889984B (hr) |
| AR (1) | AR087545A1 (hr) |
| AU (1) | AU2012296914B2 (hr) |
| BR (1) | BR112014003681A8 (hr) |
| CA (1) | CA2843537A1 (hr) |
| CL (1) | CL2014000365A1 (hr) |
| CO (1) | CO6862151A2 (hr) |
| CR (1) | CR20140076A (hr) |
| CY (1) | CY1118370T1 (hr) |
| DK (1) | DK2744809T3 (hr) |
| DO (1) | DOP2014000031A (hr) |
| EA (1) | EA023374B1 (hr) |
| ES (1) | ES2609857T3 (hr) |
| GB (1) | GB201114103D0 (hr) |
| HR (1) | HRP20161674T1 (hr) |
| HU (1) | HUE030106T2 (hr) |
| IL (1) | IL230489A (hr) |
| IN (1) | IN2014CN00568A (hr) |
| JO (1) | JO3187B1 (hr) |
| LT (1) | LT2744809T (hr) |
| ME (1) | ME02589B (hr) |
| MX (1) | MX350597B (hr) |
| MY (1) | MY170729A (hr) |
| PE (1) | PE20141406A1 (hr) |
| PL (1) | PL2744809T3 (hr) |
| PT (1) | PT2744809T (hr) |
| RS (1) | RS55560B1 (hr) |
| SI (1) | SI2744809T1 (hr) |
| SM (1) | SMT201700005B (hr) |
| TW (1) | TWI558704B (hr) |
| UA (1) | UA110838C2 (hr) |
| UY (1) | UY34264A (hr) |
| WO (1) | WO2013024104A1 (hr) |
Families Citing this family (56)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9249161B2 (en) | 2010-12-02 | 2016-02-02 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| AR084070A1 (es) | 2010-12-02 | 2013-04-17 | Constellation Pharmaceuticals Inc | Inhibidores del bromodominio y usos de los mismos |
| EP2705039B1 (en) | 2011-05-04 | 2017-07-26 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| EP2721031B1 (en) | 2011-06-17 | 2016-01-20 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| GB201114103D0 (en) * | 2011-08-17 | 2011-09-28 | Glaxosmithkline Llc | Novel compounds |
| WO2013184878A1 (en) | 2012-06-06 | 2013-12-12 | Constellation Pharmaceuticals, Inc. | Benzo [b] isoxazoloazepine bromodomain inhibitors and uses thereof |
| TWI602820B (zh) | 2012-06-06 | 2017-10-21 | 星宿藥物公司 | 溴域抑制劑及其用途 |
| US9765039B2 (en) | 2012-11-21 | 2017-09-19 | Zenith Epigenetics Ltd. | Biaryl derivatives as bromodomain inhibitors |
| US9073878B2 (en) | 2012-11-21 | 2015-07-07 | Zenith Epigenetics Corp. | Cyclic amines as bromodomain inhibitors |
| US9271978B2 (en) | 2012-12-21 | 2016-03-01 | Zenith Epigenetics Corp. | Heterocyclic compounds as bromodomain inhibitors |
| CN105164127A (zh) * | 2013-03-11 | 2015-12-16 | 艾伯维公司 | 溴结构域抑制剂 |
| WO2014164596A1 (en) | 2013-03-11 | 2014-10-09 | The Regents Of The University Of Michigan | Bet bromodomain inhibitors and therapeutic methods using the same |
| MX2015012158A (es) | 2013-03-11 | 2015-12-01 | Abbvie Inc | Inhibidores de bomodominio tetraciclicos fusionados. |
| EP3581576B1 (en) | 2013-03-15 | 2022-01-26 | Incyte Holdings Corporation | Tricyclic heterocycles as bet protein inhibitors for use in the treatment of a proliferative disease in combination with a janus kinase inhibitor |
| TWI530499B (zh) * | 2013-03-28 | 2016-04-21 | 吉李德科學股份有限公司 | 作為溴結構域（ｂｒｏｍｏｄｏｍａｉｎ）抑制劑之苯並咪唑酮衍生物類 |
| EP3010503B1 (en) | 2013-06-21 | 2020-03-11 | Zenith Epigenetics Ltd. | Novel bicyclic bromodomain inhibitors |
| CA2915561C (en) | 2013-06-21 | 2020-09-22 | Zenith Epigenetics Corp. | Novel substituted bicyclic compounds as bromodomain inhibitors |
| JP2016523964A (ja) | 2013-07-08 | 2016-08-12 | インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ | Ｂｅｔタンパク質阻害剤としての三環式複素環 |
| US9855271B2 (en) | 2013-07-31 | 2018-01-02 | Zenith Epigenetics Ltd. | Quinazolinones as bromodomain inhibitors |
| WO2015049629A1 (en) * | 2013-10-01 | 2015-04-09 | Piramal Enterprises Limited | Imidazoquinoline compounds as bromodomain inhibitors |
| WO2015081189A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| WO2015081203A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| US9309246B2 (en) | 2013-12-19 | 2016-04-12 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| EP3110818B1 (en) | 2014-02-28 | 2019-10-23 | The Regents of The University of Michigan | 9h-pyrimido[4,5-b]indoles and related analogs as bet bromodomain inhibitors |
| AR100160A1 (es) | 2014-04-23 | 2016-09-14 | Incyte Corp | 1H-PIRROLO[2,3-c]PIRIDIN-7(6H)-ONAS Y PIRAZOLO[3,4-c]PIRIDIN-7(6H)-ONAS COMO INHIBIDORES DE PROTEÍNAS BET |
| JP6682522B2 (ja) | 2014-06-20 | 2020-04-15 | コンステレーション・ファーマシューティカルズ・インコーポレイテッドＣｏｎｓｔｅｌｌａｔｉｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． | ２−（（４ｓ）−６−（４−クロロフェニル）−１−メチル−４ｈ−ベンゾ［ｃ］イソオキサゾロ［４，５−ｅ］アゼピン−４−イル）アセトアミドの結晶形態 |
| EP3194406B8 (en) | 2014-09-15 | 2021-03-31 | Incyte Corporation | Tricyclic heterocycles for use as bet protein inhibitors |
| WO2016087942A1 (en) | 2014-12-01 | 2016-06-09 | Zenith Epigenetics Corp. | Substituted pyridines as bromodomain inhibitors |
| CA2966298A1 (en) | 2014-12-01 | 2016-06-09 | Zenith Epigenetics Ltd. | Substituted pyridinones as bromodomain inhibitors |
| EP3230277B1 (en) | 2014-12-11 | 2019-09-18 | Zenith Epigenetics Ltd. | Substituted heterocycles as bromodomain inhibitors |
| CN107406438B (zh) | 2014-12-17 | 2021-05-14 | 恒翼生物医药科技(上海)有限公司 | 溴结构域的抑制剂 |
| CA2974153A1 (en) * | 2015-02-03 | 2016-08-11 | Trillium Therapeutics Inc. | Fluorinated imidazo[4,5-c]quinoline derivatives as inhibitors of bromodomain containing proteins |
| US10307407B2 (en) | 2015-02-27 | 2019-06-04 | The Regents Of The University Of Michigan | 9H-pyrimido [4,5-B] indoles as BET bromodomain inhibitors |
| GB201504694D0 (en) | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Covalent conjugates |
| GB201504689D0 (en) * | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Chemical compounds |
| WO2016186453A1 (en) * | 2015-05-20 | 2016-11-24 | Kainos Medicine, Inc. | Quinoline derivatives as bromodomain inhibitors |
| WO2016196065A1 (en) | 2015-05-29 | 2016-12-08 | Genentech, Inc. | Methods and compositions for assessing responsiveness of cancers to bet inhibitors |
| WO2016199943A1 (en) * | 2015-06-11 | 2016-12-15 | Takeda Pharmaceutical Company Limited | Heterocyclic compounds |
| US10501438B2 (en) | 2015-08-11 | 2019-12-10 | Neomed Institute | Aryl-substituted dihydroquinolinones, their preparation and their use as pharmaceuticals |
| US10836742B2 (en) | 2015-08-11 | 2020-11-17 | Neomed Institute | N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals |
| KR20180039669A (ko) | 2015-08-12 | 2018-04-18 | 네오메드 인스티튜트 | 치환된 벤즈이미다졸, 그의 제조법 및 제약으로서의 그의 용도 |
| WO2017066876A1 (en) | 2015-10-21 | 2017-04-27 | Neomed Institute | Substituted imidazopyridines, their preparation and their use as pharmaceuticals |
| TW201722966A (zh) | 2015-10-29 | 2017-07-01 | 英塞特公司 | Bet蛋白質抑制劑之非晶固體形式 |
| US10519151B2 (en) | 2016-01-28 | 2019-12-31 | Neomed Institute | Substituted [1,2,4]triazolo[4,3-A]pyridines, their preparation and their use as pharmaceuticals |
| JP6967522B2 (ja) | 2016-02-15 | 2021-11-17 | ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン | Ｂｅｔブロモドメイン阻害剤としての融合１，４−オキサゼピンおよび関連類似体 |
| JP7001614B2 (ja) | 2016-04-06 | 2022-02-03 | ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン | リガンド依存性の標的タンパク質分解のための単官能性中間体 |
| RU2021102253A (ru) | 2016-04-06 | 2021-03-03 | Дзе Риджентс Оф Дзе Юниверсити Оф Мичиган | Деструкторы белка mdm2 |
| SG11201808729WA (en) | 2016-04-12 | 2018-11-29 | Univ Michigan Regents | Bet protein degraders |
| PT3472157T (pt) | 2016-06-20 | 2023-05-30 | Incyte Corp | Formas sólidas cristalinas de um inibidor bet |
| AU2017326175B2 (en) | 2016-09-13 | 2022-01-27 | The Regents Of The University Of Michigan | Fused 1,4-diazepines as BET protein degraders |
| JP6961684B2 (ja) | 2016-09-13 | 2021-11-05 | ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン | Ｂｅｔタンパク質分解物質としての縮合１，４−オキサゼピン |
| US11046709B2 (en) | 2017-02-03 | 2021-06-29 | The Regents Of The University Of Michigan | Fused 1,4-diazepines as BET bromodomain inhibitors |
| US11267822B2 (en) | 2017-09-13 | 2022-03-08 | The Regents Of The University Of Michigan | BET bromodomain protein degraders with cleavable linkers |
| CN108033957A (zh) * | 2018-01-09 | 2018-05-15 | 中国药科大学 | 一种喹啉类BET bromodomain抑制剂及其制备方法和用途 |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| WO2022132049A1 (en) * | 2020-12-17 | 2022-06-23 | National University Of Singapore | Treating cancers using bet inhibitors |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9004781D0 (en) | 1990-03-02 | 1990-04-25 | Glaxo Group Ltd | Device |
| GB0211649D0 (en) | 2002-05-21 | 2002-07-03 | Novartis Ag | Organic compounds |
| CA2510375A1 (en) | 2002-12-20 | 2004-07-15 | 3M Innovative Properties Company | Aryl / hetaryl substituted imidazoquinolines |
| DK1699512T3 (da) | 2003-11-03 | 2012-09-17 | Glaxo Group Ltd | Fluiddispenseringsindretning |
| ATE400573T1 (de) | 2003-11-21 | 2008-07-15 | Novartis Pharma Gmbh | 1h-imidazochinolinderivate als proteinkinaseinhibitoren |
| AU2006216997A1 (en) | 2005-02-11 | 2006-08-31 | Coley Pharmaceutical Group, Inc. | Substituted imidazoquinolines and imidazonaphthyridines |
| BRPI0616338A2 (pt) | 2005-09-23 | 2011-06-14 | Coley Pharm Group Inc | mÉtodo para 1h-imidazo[4,5-c] piridinas e anÁlogos da mesma |
| EP1968587A1 (en) | 2005-12-16 | 2008-09-17 | Coley Pharmaceutical, Inc. | Substituted imidazoquinolines, imidazonaphthyridines, and imidazopyridines, compositions, and methods |
| JP2008156311A (ja) | 2006-12-26 | 2008-07-10 | Institute Of Physical & Chemical Research | Ｂｒｄ２ブロモドメイン結合剤 |
| KR101600634B1 (ko) * | 2007-12-28 | 2016-03-07 | 미쓰비시 타나베 파마 코퍼레이션 | 항암제 |
| GB0919432D0 (en) * | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Use |
| HUE026967T2 (en) * | 2009-11-05 | 2016-07-28 | Glaxosmithkline Llc | Benzodiazepine Bromodomain inhibitor |
| GB0919434D0 (en) * | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919423D0 (en) * | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB201106799D0 (en) | 2011-04-21 | 2011-06-01 | Glaxosmithkline Llc | Novel compounds |
| GB201114103D0 (en) * | 2011-08-17 | 2011-09-28 | Glaxosmithkline Llc | Novel compounds |
-
2011
- 2011-08-17 GB GBGB1114103.3A patent/GB201114103D0/en not_active Ceased
-
2012
- 2012-08-15 CN CN201280040092.5A patent/CN103889984B/zh not_active Expired - Fee Related
- 2012-08-15 UA UAA201400590A patent/UA110838C2/uk unknown
- 2012-08-15 MY MYPI2014700328A patent/MY170729A/en unknown
- 2012-08-15 US US14/237,905 patent/US9067936B2/en not_active Expired - Fee Related
- 2012-08-15 SI SI201230818A patent/SI2744809T1/sl unknown
- 2012-08-15 HU HUE12748028A patent/HUE030106T2/en unknown
- 2012-08-15 PL PL12748028T patent/PL2744809T3/pl unknown
- 2012-08-15 JP JP2014525437A patent/JP6059723B2/ja not_active Expired - Fee Related
- 2012-08-15 EA EA201490200A patent/EA023374B1/ru not_active IP Right Cessation
- 2012-08-15 IN IN568CHN2014 patent/IN2014CN00568A/en unknown
- 2012-08-15 ES ES12748028.3T patent/ES2609857T3/es active Active
- 2012-08-15 KR KR1020147007082A patent/KR20140064878A/ko not_active Application Discontinuation
- 2012-08-15 CA CA2843537A patent/CA2843537A1/en not_active Abandoned
- 2012-08-15 EP EP16192662.1A patent/EP3150601A1/en not_active Withdrawn
- 2012-08-15 WO PCT/EP2012/065918 patent/WO2013024104A1/en active Application Filing
- 2012-08-15 JO JOP/2012/0229A patent/JO3187B1/ar active
- 2012-08-15 RS RS20170014A patent/RS55560B1/sr unknown
- 2012-08-15 PT PT127480283T patent/PT2744809T/pt unknown
- 2012-08-15 LT LTEP12748028.3T patent/LT2744809T/lt unknown
- 2012-08-15 AU AU2012296914A patent/AU2012296914B2/en not_active Ceased
- 2012-08-15 AR ARP120102987A patent/AR087545A1/es unknown
- 2012-08-15 EP EP12748028.3A patent/EP2744809B1/en active Active
- 2012-08-15 ME MEP-2016-288A patent/ME02589B/me unknown
- 2012-08-15 UY UY0001034264A patent/UY34264A/es not_active Application Discontinuation
- 2012-08-15 BR BR112014003681A patent/BR112014003681A8/pt not_active Application Discontinuation
- 2012-08-15 PE PE2014000167A patent/PE20141406A1/es not_active Application Discontinuation
- 2012-08-15 TW TW101129613A patent/TWI558704B/zh not_active IP Right Cessation
- 2012-08-15 DK DK12748028.3T patent/DK2744809T3/en active
- 2012-08-15 MX MX2014001834A patent/MX350597B/es active IP Right Grant
-
2014
- 2014-01-16 IL IL230489A patent/IL230489A/en active IP Right Grant
- 2014-01-21 CO CO14011125A patent/CO6862151A2/es not_active Application Discontinuation
- 2014-02-13 CL CL2014000365A patent/CL2014000365A1/es unknown
- 2014-02-17 CR CR20140076A patent/CR20140076A/es unknown
- 2014-02-17 DO DO2014000031A patent/DOP2014000031A/es unknown
-
2015
- 2015-05-28 US US14/723,556 patent/US9416130B2/en active Active
-
2016
- 2016-07-08 US US15/205,372 patent/US9610284B2/en not_active Expired - Fee Related
- 2016-12-08 HR HRP20161674TT patent/HRP20161674T1/hr unknown
- 2016-12-16 CY CY20161101310T patent/CY1118370T1/el unknown
-
2017
- 2017-01-04 SM SM201700005T patent/SMT201700005B/it unknown
- 2017-02-17 US US15/435,697 patent/US9861627B2/en not_active Expired - Fee Related
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| HRP20161674T1 (hr) | 4-(8-METOKSI-1-((1-METOKSIPROPAN-2-IL)-2-(TETRAHIDRO-2H-PIRAN-4-IL)-1H-IMIDAZO[4,5-c]KINOLIN-7-IL)-3,5-DIMETILIZOKSAZOL I NJEGOVA UPOTREBA KAO INHIBITORA BROMODOMENE | |
| JP2014521735A5 (hr) | ||
| JP2014513139A5 (hr) | ||
| HRP20120918T1 (hr) | Aminopirazolski spoj | |
| HRP20200836T1 (hr) | Liječenje bolesti povezanih s imunitetom i upalnih bolesti | |
| JP2014511893A5 (hr) | ||
| HRP20201949T1 (hr) | 7-benzil-4-(4-(trifluorometil)benzil)-1,2,6,7,8,9-heksahidroimidazo[1,2-a]pirido[3,4-e]pirimidin-5(4h)-on i njegove soli i njihova primjena u terapiji | |
| JP2013510124A5 (hr) | ||
| WO2011113802A3 (en) | Imidazopyridine and purine compounds, compositions and methods of use | |
| MY164705A (en) | Imidazo [4,5-c] quinolin - 2 - one compound and its use as pi3 kinase / mtor dual inhibitor | |
| JP2012512158A5 (hr) | ||
| JP2014505735A5 (hr) | ||
| JP2013542247A5 (hr) | ||
| GEP20156417B (en) | Pyrrolo [2,3-d] pyrimidine derivatives as inhibitors of tropomyosin-related kinases | |
| MY180666A (en) | Substituted pyrazolo [3,4-b] pyridines as medicaments | |
| MX345928B (es) | Composiciones terapeuticamente activas y metodos de uso de las mismas. | |
| GB2495676A (en) | Use of binders for manufacturing storage stable formulations | |
| RU2017105353A (ru) | Соединения | |
| WO2013004995A8 (en) | Pyrimidinone compounds and their use | |
| WO2011128407A3 (en) | Substituted 2,3-dihydroimidazo[1,2-c]quinazoline-containing combinations | |
| MA37455A1 (fr) | Utilisation d'un dérivé de pyrazole dans le traitement d'exacerbations aigues d'une maladie pulmonaire obstructive chronique | |
| EP3412668A3 (en) | A selective inhibitor of phosphatidylinositol 3-kinase-gamma | |
| WO2015116856A3 (en) | Farnesoid x receptor antagonists | |
| NZ608375A (en) | Pharmaceutical combination of an mtor catalytic inhibitor and an allosteric mtor inhibitor | |
| HRP20180386T1 (hr) | Farmaceutski aktivni spojevi |