JP2015534975A5 - - Google Patents
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- JP2015534975A5 JP2015534975A5 JP2015537355A JP2015537355A JP2015534975A5 JP 2015534975 A5 JP2015534975 A5 JP 2015534975A5 JP 2015537355 A JP2015537355 A JP 2015537355A JP 2015537355 A JP2015537355 A JP 2015537355A JP 2015534975 A5 JP2015534975 A5 JP 2015534975A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- nitrile
- substituted
- hydroxyl
- hydroxy
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 125000000217 alkyl group Chemical group 0.000 claims 62
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 39
- 125000001424 substituent group Chemical group 0.000 claims 25
- 150000002825 nitriles Chemical class 0.000 claims 19
- 150000001875 compounds Chemical class 0.000 claims 18
- 206010028980 Neoplasm Diseases 0.000 claims 16
- 125000003545 alkoxy group Chemical group 0.000 claims 15
- 229910052757 nitrogen Inorganic materials 0.000 claims 14
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 claims 13
- 125000004432 carbon atom Chemical group C* 0.000 claims 12
- 125000003226 pyrazolyl group Chemical group 0.000 claims 12
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 11
- 229910052799 carbon Inorganic materials 0.000 claims 10
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 10
- 125000001475 halogen functional group Chemical group 0.000 claims 9
- 229910052736 halogen Inorganic materials 0.000 claims 8
- 150000002367 halogens Chemical class 0.000 claims 8
- -1 methoxy, monofluoromethyl Chemical group 0.000 claims 8
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 7
- 150000001204 N-oxides Chemical class 0.000 claims 5
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 5
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 5
- 230000002265 prevention Effects 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 239000012453 solvate Substances 0.000 claims 5
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 5
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 4
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 229910052801 chlorine Inorganic materials 0.000 claims 4
- 239000000460 chlorine Substances 0.000 claims 4
- 229910052731 fluorine Inorganic materials 0.000 claims 4
- 239000011737 fluorine Substances 0.000 claims 4
- 125000002883 imidazolyl group Chemical group 0.000 claims 4
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 4
- 208000024891 symptom Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- 238000006467 substitution reaction Methods 0.000 claims 3
- 208000011580 syndromic disease Diseases 0.000 claims 3
- 229940124597 therapeutic agent Drugs 0.000 claims 3
- 125000006507 2,4-difluorobenzyl group Chemical group [H]C1=C(F)C([H])=C(F)C(=C1[H])C([H])([H])* 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 2
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
- 108091007065 BIRCs Proteins 0.000 claims 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 2
- 201000008808 Fibrosarcoma Diseases 0.000 claims 2
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims 2
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 2
- 208000033833 Myelomonocytic Chronic Leukemia Diseases 0.000 claims 2
- 206010039491 Sarcoma Diseases 0.000 claims 2
- 108700031544 X-Linked Inhibitor of Apoptosis Proteins 0.000 claims 2
- 102000050257 X-Linked Inhibitor of Apoptosis Human genes 0.000 claims 2
- 208000009956 adenocarcinoma Diseases 0.000 claims 2
- 239000002246 antineoplastic agent Substances 0.000 claims 2
- 210000004027 cell Anatomy 0.000 claims 2
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 2
- 201000010902 chronic myelomonocytic leukemia Diseases 0.000 claims 2
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 2
- 208000032839 leukemia Diseases 0.000 claims 2
- 230000003211 malignant effect Effects 0.000 claims 2
- 230000002071 myeloproliferative effect Effects 0.000 claims 2
- 125000001425 triazolyl group Chemical group 0.000 claims 2
- 125000004176 4-fluorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1F)C([H])([H])* 0.000 claims 1
- 208000003200 Adenoma Diseases 0.000 claims 1
- 201000003076 Angiosarcoma Diseases 0.000 claims 1
- 206010003571 Astrocytoma Diseases 0.000 claims 1
- 208000003950 B-cell lymphoma Diseases 0.000 claims 1
- 206010004146 Basal cell carcinoma Diseases 0.000 claims 1
- 206010004272 Benign hydatidiform mole Diseases 0.000 claims 1
- 208000011691 Burkitt lymphomas Diseases 0.000 claims 1
- 201000009030 Carcinoma Diseases 0.000 claims 1
- 206010039499 Cartilage sarcomas Diseases 0.000 claims 1
- 208000005243 Chondrosarcoma Diseases 0.000 claims 1
- 208000006332 Choriocarcinoma Diseases 0.000 claims 1
- 206010010356 Congenital anomaly Diseases 0.000 claims 1
- 208000000471 Dysplastic Nevus Syndrome Diseases 0.000 claims 1
- 206010014967 Ependymoma Diseases 0.000 claims 1
- 201000005231 Epithelioid sarcoma Diseases 0.000 claims 1
- 208000032027 Essential Thrombocythemia Diseases 0.000 claims 1
- 208000006168 Ewing Sarcoma Diseases 0.000 claims 1
- 206010053717 Fibrous histiocytoma Diseases 0.000 claims 1
- 208000004463 Follicular Adenocarcinoma Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 208000001258 Hemangiosarcoma Diseases 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 1
- 208000006937 Hydatidiform mole Diseases 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 206010048643 Hypereosinophilic syndrome Diseases 0.000 claims 1
- 208000019758 Hypergammaglobulinemia Diseases 0.000 claims 1
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 1
- 208000018142 Leiomyosarcoma Diseases 0.000 claims 1
- 208000028018 Lymphocytic leukaemia Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 claims 1
- 208000009018 Medullary thyroid cancer Diseases 0.000 claims 1
- 208000000172 Medulloblastoma Diseases 0.000 claims 1
- 206010027406 Mesothelioma Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 206010033963 Parathyroid tumour Diseases 0.000 claims 1
- 208000007913 Pituitary Neoplasms Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 208000007452 Plasmacytoma Diseases 0.000 claims 1
- 201000000582 Retinoblastoma Diseases 0.000 claims 1
- 201000010208 Seminoma Diseases 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 claims 1
- 208000000389 T-cell leukemia Diseases 0.000 claims 1
- 208000028530 T-cell lymphoblastic leukemia/lymphoma Diseases 0.000 claims 1
- 206010042971 T-cell lymphoma Diseases 0.000 claims 1
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 0.000 claims 1
- 206010043276 Teratoma Diseases 0.000 claims 1
- 208000008383 Wilms tumor Diseases 0.000 claims 1
- 206010048218 Xeroderma Diseases 0.000 claims 1
- 210000001015 abdomen Anatomy 0.000 claims 1
- 208000017733 acquired polycythemia vera Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 210000004100 adrenal gland Anatomy 0.000 claims 1
- 208000024447 adrenal gland neoplasm Diseases 0.000 claims 1
- 210000000436 anus Anatomy 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 210000003445 biliary tract Anatomy 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000000988 bone and bone Anatomy 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 208000002458 carcinoid tumor Diseases 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 210000003679 cervix uteri Anatomy 0.000 claims 1
- 230000001886 ciliary effect Effects 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 230000002500 effect on skin Effects 0.000 claims 1
- 210000004696 endometrium Anatomy 0.000 claims 1
- 210000003238 esophagus Anatomy 0.000 claims 1
- 210000003020 exocrine pancreas Anatomy 0.000 claims 1
- 201000003444 follicular lymphoma Diseases 0.000 claims 1
- 210000000232 gallbladder Anatomy 0.000 claims 1
- 230000002496 gastric effect Effects 0.000 claims 1
- 210000001035 gastrointestinal tract Anatomy 0.000 claims 1
- 210000004602 germ cell Anatomy 0.000 claims 1
- 201000007116 gestational trophoblastic neoplasm Diseases 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 210000003128 head Anatomy 0.000 claims 1
- 201000005787 hematologic cancer Diseases 0.000 claims 1
- 208000014951 hematologic disease Diseases 0.000 claims 1
- 230000002489 hematologic effect Effects 0.000 claims 1
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 201000000284 histiocytoma Diseases 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 206010021198 ichthyosis Diseases 0.000 claims 1
- 210000004153 islets of langerhan Anatomy 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 210000000867 larynx Anatomy 0.000 claims 1
- 206010024627 liposarcoma Diseases 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 210000004324 lymphatic system Anatomy 0.000 claims 1
- 208000003747 lymphoid leukemia Diseases 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 208000023356 medullary thyroid gland carcinoma Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 206010027191 meningioma Diseases 0.000 claims 1
- 201000008806 mesenchymal cell neoplasm Diseases 0.000 claims 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
- 210000000214 mouth Anatomy 0.000 claims 1
- 206010028537 myelofibrosis Diseases 0.000 claims 1
- 208000025113 myeloid leukemia Diseases 0.000 claims 1
- 210000000754 myometrium Anatomy 0.000 claims 1
- 210000003928 nasal cavity Anatomy 0.000 claims 1
- 210000001989 nasopharynx Anatomy 0.000 claims 1
- 201000008026 nephroblastoma Diseases 0.000 claims 1
- 208000004649 neutrophil actin dysfunction Diseases 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- 210000001672 ovary Anatomy 0.000 claims 1
- 210000003101 oviduct Anatomy 0.000 claims 1
- 210000002741 palatine tonsil Anatomy 0.000 claims 1
- 210000003695 paranasal sinus Anatomy 0.000 claims 1
- 210000003899 penis Anatomy 0.000 claims 1
- 210000001428 peripheral nervous system Anatomy 0.000 claims 1
- 210000004303 peritoneum Anatomy 0.000 claims 1
- 210000003800 pharynx Anatomy 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 208000037244 polycythemia vera Diseases 0.000 claims 1
- 208000017805 post-transplant lymphoproliferative disease Diseases 0.000 claims 1
- 208000003476 primary myelofibrosis Diseases 0.000 claims 1
- 208000029340 primitive neuroectodermal tumor Diseases 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 210000000664 rectum Anatomy 0.000 claims 1
- 210000003079 salivary gland Anatomy 0.000 claims 1
- 210000004116 schwann cell Anatomy 0.000 claims 1
- 210000003491 skin Anatomy 0.000 claims 1
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 210000000813 small intestine Anatomy 0.000 claims 1
- 210000004872 soft tissue Anatomy 0.000 claims 1
- 210000002784 stomach Anatomy 0.000 claims 1
- 210000003699 striated muscle Anatomy 0.000 claims 1
- 206010042863 synovial sarcoma Diseases 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 210000001685 thyroid gland Anatomy 0.000 claims 1
- 208000030901 thyroid gland follicular carcinoma Diseases 0.000 claims 1
- 210000002105 tongue Anatomy 0.000 claims 1
- 206010044412 transitional cell carcinoma Diseases 0.000 claims 1
- 208000017997 tumor of parathyroid gland Diseases 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 210000003932 urinary bladder Anatomy 0.000 claims 1
- 210000001635 urinary tract Anatomy 0.000 claims 1
- 210000001215 vagina Anatomy 0.000 claims 1
- 230000002861 ventricular Effects 0.000 claims 1
- 230000000007 visual effect Effects 0.000 claims 1
- 210000003905 vulva Anatomy 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261716089P | 2012-10-19 | 2012-10-19 | |
| US61/716,089 | 2012-10-19 | ||
| GB1218864.5 | 2012-10-19 | ||
| GBGB1218864.5A GB201218864D0 (en) | 2012-10-19 | 2012-10-19 | Bicyclic heterocycle compounds and their uses in therapy |
| PCT/GB2013/052721 WO2014060768A1 (en) | 2012-10-19 | 2013-10-18 | Bicyclic heterocycle compounds and their uses in therapy |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015534975A JP2015534975A (ja) | 2015-12-07 |
| JP2015534975A5 true JP2015534975A5 (https=) | 2016-12-08 |
| JP6324976B2 JP6324976B2 (ja) | 2018-05-16 |
Family
ID=47359191
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015537355A Active JP6324976B2 (ja) | 2012-10-19 | 2013-10-18 | 二環式複素環化合物およびそれらの治療での使用 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US9663512B2 (https=) |
| EP (1) | EP2909197B1 (https=) |
| JP (1) | JP6324976B2 (https=) |
| KR (1) | KR102299832B1 (https=) |
| CN (1) | CN104870440B (https=) |
| CA (1) | CA2888112C (https=) |
| DK (1) | DK2909197T3 (https=) |
| ES (1) | ES2794009T3 (https=) |
| GB (1) | GB201218864D0 (https=) |
| WO (1) | WO2014060768A1 (https=) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201106817D0 (en) | 2011-04-21 | 2011-06-01 | Astex Therapeutics Ltd | New compound |
| GB201106814D0 (en) | 2011-04-21 | 2011-06-01 | Astex Therapeutics Ltd | New compounds |
| US9980973B2 (en) | 2012-10-19 | 2018-05-29 | Astex Therapeutics Limited | Bicyclic heterocycle compounds and their uses in therapy |
| GB201218862D0 (en) | 2012-10-19 | 2012-12-05 | Astex Therapeutics Ltd | Bicyclic heterocycle compounds and their uses in therapy |
| GB201218850D0 (en) | 2012-10-19 | 2012-12-05 | Astex Therapeutics Ltd | Bicyclic heterocycle compounds and their uses in therapy |
| GB201218864D0 (en) | 2012-10-19 | 2012-12-05 | Astex Therapeutics Ltd | Bicyclic heterocycle compounds and their uses in therapy |
| BR122022015241B1 (pt) | 2013-12-20 | 2023-09-26 | Astex Therapeutics Limited | Compostos heterocíclicos bicíclicos intermediários para a preparação de um composto de fórmula (i) |
| WO2016079527A1 (en) | 2014-11-19 | 2016-05-26 | Tetralogic Birinapant Uk Ltd | Combination therapy |
| WO2016097773A1 (en) | 2014-12-19 | 2016-06-23 | Children's Cancer Institute | Therapeutic iap antagonists for treating proliferative disorders |
| GB201506871D0 (en) | 2015-04-22 | 2015-06-03 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| AU2017253560B2 (en) | 2016-04-20 | 2019-03-21 | Glaxosmithkline Intellectual Property Development Limited | Conjugates comprising RIPK2 inhibitors |
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| WO2010121212A2 (en) | 2009-04-17 | 2010-10-21 | H. Lee Moffit Cancer Center And Research Institute, Inc. | Indoline scaffold shp-2 inhibitors and method of treating cancer |
| CA2761009A1 (en) | 2009-05-04 | 2010-11-11 | Plexxikon, Inc. | Compounds and methods for inhibition of renin, and indications therefor |
| AU2010254056A1 (en) | 2009-05-28 | 2011-12-15 | Tetralogic Pharmaceuticals Corp. | IAP inhibitors |
| GB201106817D0 (en) | 2011-04-21 | 2011-06-01 | Astex Therapeutics Ltd | New compound |
| GB201106814D0 (en) | 2011-04-21 | 2011-06-01 | Astex Therapeutics Ltd | New compounds |
| CA2850757A1 (en) | 2011-10-03 | 2013-04-11 | The Trustees Of Columbia University In The City Of New York | Novel molecules that selectively inhibit histone deacetylase 6 relative to histone deacetylase 1 |
| ES2802251T3 (es) | 2012-01-06 | 2021-01-18 | Novartis Ag | Compuestos heterocíclicos y métodos para su uso |
| GB201218864D0 (en) | 2012-10-19 | 2012-12-05 | Astex Therapeutics Ltd | Bicyclic heterocycle compounds and their uses in therapy |
| GB201218862D0 (en) | 2012-10-19 | 2012-12-05 | Astex Therapeutics Ltd | Bicyclic heterocycle compounds and their uses in therapy |
| GB201218850D0 (en) | 2012-10-19 | 2012-12-05 | Astex Therapeutics Ltd | Bicyclic heterocycle compounds and their uses in therapy |
| BR122022015241B1 (pt) | 2013-12-20 | 2023-09-26 | Astex Therapeutics Limited | Compostos heterocíclicos bicíclicos intermediários para a preparação de um composto de fórmula (i) |
| US10087151B2 (en) | 2014-01-09 | 2018-10-02 | The J. David Gladstone Institutes, A Testimentary Trust Established Under The Will Of J. David Gladstone | Substituted benzoxazine and related compounds |
-
2012
- 2012-10-19 GB GBGB1218864.5A patent/GB201218864D0/en not_active Ceased
-
2013
- 2013-10-18 JP JP2015537355A patent/JP6324976B2/ja active Active
- 2013-10-18 WO PCT/GB2013/052721 patent/WO2014060768A1/en not_active Ceased
- 2013-10-18 CA CA2888112A patent/CA2888112C/en active Active
- 2013-10-18 KR KR1020157012697A patent/KR102299832B1/ko active Active
- 2013-10-18 DK DK13780388.8T patent/DK2909197T3/da active
- 2013-10-18 ES ES13780388T patent/ES2794009T3/es active Active
- 2013-10-18 US US14/436,364 patent/US9663512B2/en active Active
- 2013-10-18 EP EP13780388.8A patent/EP2909197B1/en active Active
- 2013-10-18 CN CN201380066425.6A patent/CN104870440B/zh active Active
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