JP2016500684A5 - - Google Patents
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- JP2016500684A5 JP2016500684A5 JP2015537354A JP2015537354A JP2016500684A5 JP 2016500684 A5 JP2016500684 A5 JP 2016500684A5 JP 2015537354 A JP2015537354 A JP 2015537354A JP 2015537354 A JP2015537354 A JP 2015537354A JP 2016500684 A5 JP2016500684 A5 JP 2016500684A5
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- Prior art keywords
- alkyl
- hydrogen
- tumors
- nitrogen
- hydroxyl
- 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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- 125000000217 alkyl group Chemical group 0.000 claims 37
- 229910052739 hydrogen Inorganic materials 0.000 claims 28
- 239000001257 hydrogen Substances 0.000 claims 28
- 206010028980 Neoplasm Diseases 0.000 claims 16
- 150000001875 compounds Chemical class 0.000 claims 15
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 15
- 150000002431 hydrogen Chemical class 0.000 claims 14
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 13
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 10
- 229910052757 nitrogen Inorganic materials 0.000 claims 10
- 150000002825 nitriles Chemical class 0.000 claims 7
- 229910052760 oxygen Inorganic materials 0.000 claims 7
- 229910052736 halogen Inorganic materials 0.000 claims 6
- 150000002367 halogens Chemical class 0.000 claims 6
- -1 methoxy, cyclopropyl Chemical group 0.000 claims 6
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 5
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 claims 5
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 5
- 230000002265 prevention Effects 0.000 claims 5
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 4
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 229910052731 fluorine Inorganic materials 0.000 claims 4
- 239000011737 fluorine Substances 0.000 claims 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 125000003566 oxetanyl group Chemical group 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 208000011580 syndromic disease Diseases 0.000 claims 4
- 150000001204 N-oxides Chemical class 0.000 claims 3
- 210000004027 cell Anatomy 0.000 claims 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 208000032839 leukemia Diseases 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- 208000024891 symptom 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
- 208000018142 Leiomyosarcoma Diseases 0.000 claims 2
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 2
- 206010025323 Lymphomas 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
- 229910052799 carbon Inorganic materials 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
- 125000001475 halogen functional group Chemical group 0.000 claims 2
- 201000005787 hematologic cancer Diseases 0.000 claims 2
- 230000003211 malignant effect Effects 0.000 claims 2
- 230000002071 myeloproliferative effect Effects 0.000 claims 2
- 125000004076 pyridyl 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
- 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
- 206010062805 Dysplastic naevus Diseases 0.000 claims 1
- 206010014950 Eosinophilia 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
- 208000019758 Hypergammaglobulinemia Diseases 0.000 claims 1
- 208000007766 Kaposi sarcoma 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
- 208000009277 Neuroectodermal Tumors Diseases 0.000 claims 1
- 206010033963 Parathyroid tumour Diseases 0.000 claims 1
- OAICVXFJPJFONN-UHFFFAOYSA-N Phosphorus Chemical compound [P] OAICVXFJPJFONN-UHFFFAOYSA-N 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
- 210000001185 bone marrow Anatomy 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 208000002458 carcinoid tumor Diseases 0.000 claims 1
- 210000000845 cartilage Anatomy 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
- 125000000753 cycloalkyl group Chemical group 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
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000000816 ethylene group Chemical group [H]C([H])([*:1])C([H])([H])[*:2] 0.000 claims 1
- 210000003020 exocrine pancreas Anatomy 0.000 claims 1
- 239000000835 fiber Substances 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
- 208000014951 hematologic disease Diseases 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
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 1
- 206010021198 ichthyosis Diseases 0.000 claims 1
- 210000004153 islets of langerhan Anatomy 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 210000000867 larynx Anatomy 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
- 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
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims 1
- 210000000214 mouth Anatomy 0.000 claims 1
- 206010028537 myelofibrosis 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
- 229910052698 phosphorus Inorganic materials 0.000 claims 1
- 239000011574 phosphorus Substances 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
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 210000000664 rectum Anatomy 0.000 claims 1
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims 1
- 210000003079 salivary gland Anatomy 0.000 claims 1
- 210000004116 schwann cell Anatomy 0.000 claims 1
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- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 210000000813 small intestine Anatomy 0.000 claims 1
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- 206010042863 synovial sarcoma Diseases 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 210000001685 thyroid gland Anatomy 0.000 claims 1
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- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 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
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Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261716086P | 2012-10-19 | 2012-10-19 | |
| GB1218862.9 | 2012-10-19 | ||
| US61/716,086 | 2012-10-19 | ||
| GBGB1218862.9A GB201218862D0 (en) | 2012-10-19 | 2012-10-19 | Bicyclic heterocycle compounds and their uses in therapy |
| PCT/GB2013/052720 WO2014060767A1 (en) | 2012-10-19 | 2013-10-18 | Bicyclic heterocycle compounds and their uses in therapy |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016500684A JP2016500684A (ja) | 2016-01-14 |
| JP2016500684A5 true JP2016500684A5 (https=) | 2016-12-08 |
| JP6381534B2 JP6381534B2 (ja) | 2018-08-29 |
Family
ID=47359189
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015537354A Active JP6381534B2 (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) | US9617283B2 (https=) |
| EP (1) | EP2909196B1 (https=) |
| JP (1) | JP6381534B2 (https=) |
| KR (1) | KR102299834B1 (https=) |
| CN (1) | CN104870441B (https=) |
| CA (1) | CA2888107C (https=) |
| DK (1) | DK2909196T3 (https=) |
| ES (1) | ES2847897T3 (https=) |
| GB (1) | GB201218862D0 (https=) |
| WO (1) | WO2014060767A1 (https=) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201106814D0 (en) | 2011-04-21 | 2011-06-01 | Astex Therapeutics Ltd | New compounds |
| GB201106817D0 (en) | 2011-04-21 | 2011-06-01 | Astex Therapeutics Ltd | New compound |
| 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 |
| 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 |
| 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 |
| WO2017194390A1 (en) * | 2016-05-09 | 2017-11-16 | F. Hoffmann-La Roche Ag | Dimeric compounds |
| CN118436801A (zh) | 2016-05-20 | 2024-08-06 | 豪夫迈·罗氏有限公司 | Protac抗体缀合物及其使用方法 |
| GB201610147D0 (en) | 2016-06-10 | 2016-07-27 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| CN106265764B (zh) | 2016-08-18 | 2018-03-16 | 广州威溶特医药科技有限公司 | Iap抑制剂和溶瘤病毒在制备抗肿瘤药物中的应用 |
| US20210361774A1 (en) | 2018-10-16 | 2021-11-25 | Dana-Farber Cancer Institute, Inc. | Degraders of wild-type and mutant forms of lrrk2 |
| WO2020133092A1 (zh) | 2018-12-27 | 2020-07-02 | 青岛清原化合物有限公司 | 吡啶氧基羧酸酯衍生物及其制备方法、除草组合物和应用 |
| CN109535070B (zh) * | 2018-12-27 | 2022-03-29 | 青岛清原化合物有限公司 | 吡啶氧基羧酸酯衍生物及其制备方法、除草组合物和应用 |
| EP3947368B1 (en) | 2019-04-04 | 2025-09-03 | Dana-Farber Cancer Institute, Inc. | Bifunctional compounds comprising a cdk2/5 ligand, a linker and a e3 ubiquitin ligase binding degron for the treatment of cancer |
| WO2021026349A1 (en) | 2019-08-08 | 2021-02-11 | Institute For Cancer Research D/B/A The Research Institute Of Fox Chase Cancer Center | Combination therapy for treatment of cancer |
| CN110483509B (zh) * | 2019-09-04 | 2020-08-25 | 温州大学 | 一种合成含氮杂环衍生物的方法 |
| CN110627785B (zh) * | 2019-09-19 | 2021-06-25 | 温州大学 | 一种1,5-四氢萘啶衍生物的制备方法 |
| EP4146648A1 (en) * | 2020-05-04 | 2023-03-15 | Otsuka Pharmaceutical Co., Ltd. | Iap antagonist compounds and intermediates and methods for synthesizing the same |
| TWI894285B (zh) * | 2020-06-04 | 2025-08-21 | 英屬開曼群島商百濟神州有限公司 | 作為IAP拮抗劑的吡啶並[2,3-b][1,4]噁嗪或四氫吡啶並[2,3-b][1,4]氧氮呯 |
| WO2023056069A1 (en) | 2021-09-30 | 2023-04-06 | Angiex, Inc. | Degrader-antibody conjugates and methods of using same |
| EP4490159A4 (en) * | 2022-03-11 | 2025-08-20 | Ascentage Pharma Suzhou Co Ltd | TRICYCLIC HETEROCYCLIC COMPOUNDS AS IAP ANTAGONISTS |
| WO2024240858A1 (en) | 2023-05-23 | 2024-11-28 | Valerio Therapeutics | Protac molecules directed against dna damage repair system and uses thereof |
Family Cites Families (56)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4080330A (en) | 1975-06-23 | 1978-03-21 | Delmar Chemicals Limited | Phenylindolines and process for their production |
| DE3822792C2 (de) | 1987-07-11 | 1997-11-27 | Sandoz Ag | Neue Verwendung von 5HT¶3¶-Antagonisten |
| TW218875B (https=) | 1992-03-09 | 1994-01-11 | Takeda Pharm Industry Co Ltd | |
| NZ321575A (en) | 1995-10-30 | 1999-05-28 | Janssen Pharmaceutica Nv | 1-(1,2-disubstituted piperidinyl)-4- substituted piperazine derivatives |
| PT778277E (pt) | 1995-12-08 | 2003-11-28 | Pfizer | Derivados heterociclicos substituidos como antagonistas do crf |
| PT892780E (pt) | 1996-02-22 | 2003-02-28 | Bristol Myers Squibb Pharma Co | Analogos de m-amidino fenilo como inibidores do factor xa |
| EP0944388A4 (en) | 1996-04-03 | 2001-08-16 | Merck & Co Inc | INHIBITORS OF FARNESYL PROTEIN TRANSFERASE |
| JP2000513375A (ja) | 1996-06-28 | 2000-10-10 | メルク エンド カンパニー インコーポレーテッド | フィブリノーゲンレセプター拮抗薬プロドラッグ |
| US5977134A (en) | 1996-12-05 | 1999-11-02 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| EP0975593A1 (en) | 1997-04-18 | 2000-02-02 | Smithkline Beecham Plc | Indole derivatives having combined 5ht1a, 5ht1b and 5ht1d receptor antagonist activity |
| US6084098A (en) | 1999-02-26 | 2000-07-04 | Neurogen Corporation | Benzylpiperazinyl and piperidinyl ethanone derivatives: dopamine receptor subtype specific ligands |
| US6528529B1 (en) | 1998-03-31 | 2003-03-04 | Acadia Pharmaceuticals Inc. | Compounds with activity on muscarinic receptors |
| BR9909277A (pt) | 1998-03-31 | 2001-10-16 | Acadia Pharm Inc | Compostos com atividade em receptores muscarìnicos |
| US6608084B1 (en) | 1998-08-26 | 2003-08-19 | Aventis Pharma Ltd. | Aza-bicycles which modulate the inhibition of cell adhesion |
| GB9905010D0 (en) | 1999-03-04 | 1999-04-28 | Merck Sharp & Dohme | Therapeutic agents |
| AU3555200A (en) | 1999-03-17 | 2000-10-04 | F. Hoffmann-La Roche Ag | Oxazolone derivatives and their use as alpha-1 adrenoreceptor modulators |
| GB9929552D0 (en) | 1999-12-14 | 2000-02-09 | Proteus Molecular Design | Compounds |
| US6534535B1 (en) | 1999-08-12 | 2003-03-18 | Millennium Pharmaceuticals, Inc. | Inhibitors of factor Xa |
| US6878712B1 (en) | 1999-09-04 | 2005-04-12 | Astrazeneca Ab | Amides as inhibitors for pyruvate dehydrogenase |
| GB0031088D0 (en) | 2000-12-20 | 2001-01-31 | Smithkline Beecham Plc | Medicaments |
| CA2433090A1 (en) | 2000-12-27 | 2002-07-04 | Kyowa Hakko Kogyo Co., Ltd. | Dipeptidyl peptidase iv inhibitor |
| WO2002080853A2 (en) | 2001-04-09 | 2002-10-17 | Bristol-Myers Squibb Company | Fused heterocyclic inhibitors of factor xa |
| EP1389194A2 (en) | 2001-04-27 | 2004-02-18 | Vertex Pharmaceuticals Incorporated | Inhibitors of bace |
| US20050245537A1 (en) | 2002-04-24 | 2005-11-03 | Noboru Tsuchimori | Use of compounds having ccr antagonism |
| BRPI0408136A (pt) | 2003-03-07 | 2006-03-01 | Astellas Pharma Inc | derivados heterocìclicos contendo nitrogênio tendo estirila 2,6-dissubstituìda |
| TWI372050B (en) | 2003-07-03 | 2012-09-11 | Astex Therapeutics Ltd | (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles |
| AU2004266233A1 (en) | 2003-08-13 | 2005-03-03 | Amgen, Inc. | Melanin concentrating hormone receptor antagonist |
| TW200524887A (en) | 2003-10-27 | 2005-08-01 | Lundbeck & Co As H | N-thiazol-2-yl-benzamide derivatives |
| WO2006010118A2 (en) | 2004-07-09 | 2006-01-26 | The Regents Of The University Of Michigan | Conformationally constrained smac mimetics and the uses thereof |
| WO2006032987A1 (en) | 2004-09-23 | 2006-03-30 | Pfizer Products Inc. | Indoline compounds and their use in the treatment of arteriosclerosis |
| DK1836201T4 (da) | 2004-12-20 | 2013-11-11 | Genentech Inc | Pyrrolidininhibitorer af IAP. |
| CN101128425B (zh) * | 2005-02-25 | 2012-12-26 | 泰特拉洛吉克药业公司 | Iap二聚体抑制剂 |
| CA2634699A1 (en) | 2005-12-21 | 2007-06-28 | Decode Genetics Ehf | N-linked aryl heteroaryl inhibitors of lta4h for treating inflammation |
| FR2896504B1 (fr) | 2006-01-23 | 2012-07-13 | Aventis Pharma Sa | Nouveaux derives d'uree cyclique, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de kinases |
| GB0602335D0 (en) | 2006-02-07 | 2006-03-15 | Remynd Nv | Thiadiazole Derivatives For The Treatment Of Neurodegenerative Diseases |
| JP5452223B2 (ja) * | 2006-07-24 | 2014-03-26 | テトラロジック ファーマシューティカルズ コーポレーション | Ｉａｐ阻害剤 |
| WO2008045905A1 (en) * | 2006-10-12 | 2008-04-17 | Novartis Ag | Pyrrolydine derivatives as iap inhibitors |
| KR20090086244A (ko) * | 2006-12-07 | 2009-08-11 | 노파르티스 아게 | 증식성 질환의 치료에서의 6-옥소-1,6-디히드로피리미딘-2-일 |
| JP2010520293A (ja) | 2007-03-07 | 2010-06-10 | アラントス・フアーマシユーテイカルズ・ホールデイング・インコーポレイテツド | 複素環式部分を含有するメタロプロテアーゼ阻害剤 |
| US8173645B2 (en) | 2007-03-21 | 2012-05-08 | Takeda San Diego, Inc. | Glucokinase activators |
| CA2712604A1 (en) | 2008-01-24 | 2009-07-30 | Tetralogic Pharmaceutical Corporation | Iap inhibitors |
| WO2009147476A1 (en) | 2008-06-02 | 2009-12-10 | Matrix Laboratories Ltd. | Novel pde inhibitors, pharmaceutical compositions containing them and processes for their preparation |
| WO2010011666A2 (en) | 2008-07-21 | 2010-01-28 | University Of South Florida | Indoline scaffold shp-2 inhibitors and cancer treatment method |
| WO2010048149A2 (en) | 2008-10-20 | 2010-04-29 | Kalypsys, Inc. | Heterocyclic modulators of gpr119 for treatment of disease |
| 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 |
| GB201106814D0 (en) | 2011-04-21 | 2011-06-01 | Astex Therapeutics Ltd | New compounds |
| GB201106817D0 (en) | 2011-04-21 | 2011-06-01 | Astex Therapeutics Ltd | New compound |
| 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 |
| GB201218850D0 (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 |
| 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) |
| 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 GBGB1218862.9A patent/GB201218862D0/en not_active Ceased
-
2013
- 2013-10-18 KR KR1020157012696A patent/KR102299834B1/ko active Active
- 2013-10-18 WO PCT/GB2013/052720 patent/WO2014060767A1/en not_active Ceased
- 2013-10-18 ES ES13780387T patent/ES2847897T3/es active Active
- 2013-10-18 DK DK13780387.0T patent/DK2909196T3/da active
- 2013-10-18 US US14/436,345 patent/US9617283B2/en active Active
- 2013-10-18 JP JP2015537354A patent/JP6381534B2/ja active Active
- 2013-10-18 CN CN201380066428.XA patent/CN104870441B/zh active Active
- 2013-10-18 EP EP13780387.0A patent/EP2909196B1/en active Active
- 2013-10-18 CA CA2888107A patent/CA2888107C/en active Active
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