JP2014514317A5 - - Google Patents
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- JP2014514317A5 JP2014514317A5 JP2014505721A JP2014505721A JP2014514317A5 JP 2014514317 A5 JP2014514317 A5 JP 2014514317A5 JP 2014505721 A JP2014505721 A JP 2014505721A JP 2014505721 A JP2014505721 A JP 2014505721A JP 2014514317 A5 JP2014514317 A5 JP 2014514317A5
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- JP
- Japan
- Prior art keywords
- cancer
- alkyl
- compound
- formula
- pharmaceutical composition
- 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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- 150000001875 compounds Chemical class 0.000 claims 65
- 125000000217 alkyl group Chemical group 0.000 claims 41
- 125000000623 heterocyclic group Chemical group 0.000 claims 31
- 206010028980 Neoplasm Diseases 0.000 claims 28
- 239000008194 pharmaceutical composition Substances 0.000 claims 26
- 201000011510 cancer Diseases 0.000 claims 19
- 125000004452 carbocyclyl group Chemical group 0.000 claims 17
- 229910052739 hydrogen Inorganic materials 0.000 claims 15
- 239000001257 hydrogen Substances 0.000 claims 15
- 229910052736 halogen Inorganic materials 0.000 claims 10
- 150000002367 halogens Chemical class 0.000 claims 10
- 150000002431 hydrogen Chemical class 0.000 claims 9
- 229910052799 carbon Inorganic materials 0.000 claims 7
- 125000004093 cyano group Chemical group *C#N 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 7
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 6
- 206010006187 Breast cancer Diseases 0.000 claims 6
- 208000026310 Breast neoplasm Diseases 0.000 claims 6
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 6
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 6
- 150000001204 N-oxides Chemical class 0.000 claims 6
- 201000001441 melanoma Diseases 0.000 claims 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 6
- 230000002265 prevention Effects 0.000 claims 6
- 125000006239 protecting group Chemical group 0.000 claims 6
- 239000012453 solvate Substances 0.000 claims 6
- 206010033128 Ovarian cancer Diseases 0.000 claims 5
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 5
- 125000005843 halogen group Chemical group 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- -1 2 -Piperidinyl Chemical group 0.000 claims 4
- 206010009944 Colon cancer Diseases 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 4
- 125000003342 alkenyl group Chemical group 0.000 claims 4
- 208000029742 colonic neoplasm Diseases 0.000 claims 4
- 229910052731 fluorine Inorganic materials 0.000 claims 4
- 239000011737 fluorine Substances 0.000 claims 4
- 201000005202 lung cancer Diseases 0.000 claims 4
- 208000020816 lung neoplasm Diseases 0.000 claims 4
- 208000011580 syndromic disease Diseases 0.000 claims 4
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 3
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 3
- 206010060862 Prostate cancer Diseases 0.000 claims 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 3
- 206010038389 Renal cancer Diseases 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 150000001721 carbon Chemical group 0.000 claims 3
- 238000010511 deprotection reaction Methods 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 230000002757 inflammatory effect Effects 0.000 claims 3
- 201000010982 kidney cancer Diseases 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 229940124597 therapeutic agent Drugs 0.000 claims 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 2
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims 2
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 2
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 2
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 2
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 2
- 208000003950 B-cell lymphoma Diseases 0.000 claims 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
- 108091007065 BIRCs Proteins 0.000 claims 2
- 206010005003 Bladder cancer Diseases 0.000 claims 2
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 claims 2
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 claims 2
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 2
- 206010017993 Gastrointestinal neoplasms 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
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 2
- 208000007097 Urinary Bladder Neoplasms 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
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
- 210000004027 cell Anatomy 0.000 claims 2
- 229910052801 chlorine Inorganic materials 0.000 claims 2
- 239000000460 chlorine Substances 0.000 claims 2
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 2
- 201000010902 chronic myelomonocytic leukemia Diseases 0.000 claims 2
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 201000005787 hematologic cancer Diseases 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 208000032839 leukemia Diseases 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 229940127084 other anti-cancer agent Drugs 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 238000002560 therapeutic procedure Methods 0.000 claims 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims 2
- 125000006553 (C3-C8) cycloalkenyl group Chemical group 0.000 claims 1
- 125000004485 2-pyrrolidinyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])([H])C1([H])* 0.000 claims 1
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 1
- 208000036762 Acute promyelocytic leukaemia Diseases 0.000 claims 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 1
- 208000011691 Burkitt lymphomas Diseases 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 201000009030 Carcinoma Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 206010010356 Congenital anomaly Diseases 0.000 claims 1
- 206010058314 Dysplasia Diseases 0.000 claims 1
- 208000001976 Endocrine Gland Neoplasms Diseases 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 206010014950 Eosinophilia Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 201000001342 Fallopian tube cancer Diseases 0.000 claims 1
- 208000013452 Fallopian tube neoplasm Diseases 0.000 claims 1
- 208000022072 Gallbladder Neoplasms 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
- 208000005726 Inflammatory Breast Neoplasms Diseases 0.000 claims 1
- 206010021980 Inflammatory carcinoma of the breast Diseases 0.000 claims 1
- 206010025280 Lymphocytosis Diseases 0.000 claims 1
- 208000032271 Malignant tumor of penis Diseases 0.000 claims 1
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 claims 1
- 206010027406 Mesothelioma Diseases 0.000 claims 1
- 206010060880 Monoclonal gammopathy Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 208000014767 Myeloproliferative disease Diseases 0.000 claims 1
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 208000002471 Penile Neoplasms Diseases 0.000 claims 1
- 206010034299 Penile cancer Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 208000007452 Plasmacytoma Diseases 0.000 claims 1
- 208000015634 Rectal Neoplasms Diseases 0.000 claims 1
- XUIMIQQOPSSXEZ-UHFFFAOYSA-N Silicon Chemical group [Si] XUIMIQQOPSSXEZ-UHFFFAOYSA-N 0.000 claims 1
- 208000000453 Skin Neoplasms 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
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 208000006593 Urologic Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 208000004354 Vulvar Neoplasms Diseases 0.000 claims 1
- 208000009956 adenocarcinoma Diseases 0.000 claims 1
- 210000004100 adrenal gland Anatomy 0.000 claims 1
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 201000009036 biliary tract cancer Diseases 0.000 claims 1
- 208000020790 biliary tract neoplasm Diseases 0.000 claims 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 1
- 229910052794 bromium Inorganic materials 0.000 claims 1
- 201000007455 central nervous system cancer Diseases 0.000 claims 1
- 208000025997 central nervous system neoplasm Diseases 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 125000000596 cyclohexenyl group Chemical group C1(=CCCCC1)* 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 201000011523 endocrine gland cancer Diseases 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 230000001605 fetal effect Effects 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 201000003444 follicular lymphoma Diseases 0.000 claims 1
- 239000012458 free base Substances 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 210000000232 gallbladder Anatomy 0.000 claims 1
- 201000010175 gallbladder cancer Diseases 0.000 claims 1
- 210000004602 germ cell Anatomy 0.000 claims 1
- 210000002768 hair cell Anatomy 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 208000014951 hematologic disease Diseases 0.000 claims 1
- 208000019691 hematopoietic and lymphoid cell neoplasm 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
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 1
- 201000004653 inflammatory breast carcinoma Diseases 0.000 claims 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 210000003574 melanophore Anatomy 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 1
- 230000002071 myeloproliferative effect Effects 0.000 claims 1
- 210000000754 myometrium Anatomy 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 230000007170 pathology Effects 0.000 claims 1
- 201000005528 peripheral nervous system neoplasm Diseases 0.000 claims 1
- 201000002628 peritoneum cancer Diseases 0.000 claims 1
- 125000004437 phosphorous atom Chemical group 0.000 claims 1
- 229910052698 phosphorus Chemical group 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000002098 pyridazinyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 206010038038 rectal cancer Diseases 0.000 claims 1
- 201000001275 rectum cancer Diseases 0.000 claims 1
- 229910052710 silicon Inorganic materials 0.000 claims 1
- 239000010703 silicon Substances 0.000 claims 1
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 210000000278 spinal cord Anatomy 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- 125000003831 tetrazolyl group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 206010046885 vaginal cancer Diseases 0.000 claims 1
- 208000013139 vaginal neoplasm Diseases 0.000 claims 1
- 201000005102 vulva cancer Diseases 0.000 claims 1
- 0 *C(C(N1C(C*(*)CC*(*)C2)C2C(*)(*)C1)=O)N1C(*)(*)C(*)NC(*)C1 Chemical compound *C(C(N1C(C*(*)CC*(*)C2)C2C(*)(*)C1)=O)N1C(*)(*)C(*)NC(*)C1 0.000 description 2
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161477726P | 2011-04-21 | 2011-04-21 | |
| GB1106817.8 | 2011-04-21 | ||
| GBGB1106817.8A GB201106817D0 (en) | 2011-04-21 | 2011-04-21 | New compound |
| US61/477,726 | 2011-04-21 | ||
| PCT/GB2012/050867 WO2012143726A1 (en) | 2011-04-21 | 2012-04-20 | Bicyclic heterocycle compounds and their uses in therapy |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014514317A JP2014514317A (ja) | 2014-06-19 |
| JP2014514317A5 true JP2014514317A5 (enExample) | 2015-06-11 |
| JP6100238B2 JP6100238B2 (ja) | 2017-03-22 |
Family
ID=44147398
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014505721A Active JP6100238B2 (ja) | 2011-04-21 | 2012-04-20 | 二環式複素環化合物および治療法におけるその使用 |
Country Status (29)
| Country | Link |
|---|---|
| US (6) | US9018214B2 (enExample) |
| EP (2) | EP3868747A1 (enExample) |
| JP (1) | JP6100238B2 (enExample) |
| KR (1) | KR101896134B1 (enExample) |
| CN (1) | CN103492376B (enExample) |
| AR (2) | AR086468A1 (enExample) |
| AU (1) | AU2012246081B2 (enExample) |
| BR (1) | BR112013027121B8 (enExample) |
| CA (1) | CA2831346C (enExample) |
| CY (1) | CY1123991T1 (enExample) |
| DK (1) | DK2699562T3 (enExample) |
| ES (1) | ES2855171T3 (enExample) |
| GB (1) | GB201106817D0 (enExample) |
| HR (1) | HRP20210450T1 (enExample) |
| HU (1) | HUE053688T2 (enExample) |
| IL (1) | IL228923A (enExample) |
| LT (1) | LT2699562T (enExample) |
| MX (1) | MX352564B (enExample) |
| MY (1) | MY168159A (enExample) |
| NZ (1) | NZ615572A (enExample) |
| PH (1) | PH12013502002A1 (enExample) |
| PL (1) | PL2699562T3 (enExample) |
| PT (1) | PT2699562T (enExample) |
| RU (1) | RU2662827C2 (enExample) |
| SG (1) | SG193542A1 (enExample) |
| SI (1) | SI2699562T1 (enExample) |
| TW (1) | TWI558698B (enExample) |
| WO (1) | WO2012143726A1 (enExample) |
| ZA (1) | ZA201307797B (enExample) |
Families Citing this family (34)
| 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 |
| 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 |
| US9980973B2 (en) | 2012-10-19 | 2018-05-29 | Astex Therapeutics Limited | 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 |
| JO3368B1 (ar) | 2013-06-04 | 2019-03-13 | Janssen Pharmaceutica Nv | مركبات 6، 7- ثاني هيدرو بيرازولو [5،1-a] بيرازين- 4 (5 يد)- اون واستخدامها بصفة منظمات تفارغية سلبية لمستقبلات ميجلور 2 |
| SG10201808102WA (en) * | 2013-12-20 | 2018-10-30 | Astex Therapeutics Ltd | Bicyclic heterocycle compounds and their uses in therapy |
| CA2943882A1 (en) | 2014-05-22 | 2015-11-26 | F. Hoffmann-La Roche Ag | Indolin-2-one and 1,3-dihydro-pyrrolo[3,2-c]pyridin-2-one derivatives |
| AU2015279377B2 (en) | 2014-06-26 | 2019-09-12 | F. Hoffmann-La Roche Ag | Indolin-2-one or pyrrolo-pyridin-2-one derivatives |
| JOP20150177B1 (ar) | 2014-08-01 | 2021-08-17 | Janssen Pharmaceutica Nv | مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2 |
| JOP20150179B1 (ar) | 2014-08-01 | 2021-08-17 | Janssen Pharmaceutica Nv | مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2 |
| EP3180312B1 (en) | 2014-08-12 | 2019-10-16 | Loyola University Of Chicago | Indoline sulfonamide inhibitors of dape and ndm-1 and use of the same |
| JP6861154B2 (ja) | 2014-12-03 | 2021-04-21 | ヤンセン ファーマシューティカ エヌ．ベー． | 放射標識されたｍＧｌｕＲ２ ＰＥＴリガンド |
| JP6689856B2 (ja) | 2014-12-03 | 2020-04-28 | ヤンセン ファーマシューティカ エヌ．ベー． | ６，７−ジヒドロピラゾロ［１，５−ａ］ピラジン−４（５Ｈ）−オン化合物およびＭＧＬＵＲ２受容体の負のアロステリック調節因子としてのそれらの使用 |
| CA3094197C (en) * | 2015-07-02 | 2023-02-28 | F. Hoffmann-La Roche Ag | Bicyclic lactams and methods of use thereof |
| US11045562B2 (en) | 2015-12-18 | 2021-06-29 | Janssen Pharmaceutica Nv | Radiolabelled mGluR2/3 PET ligands |
| CA3003998A1 (en) | 2015-12-18 | 2017-06-22 | Janssen Pharmaceutica Nv | Radiolabelled mglur2/3 pet ligands |
| JP2019514878A (ja) * | 2016-04-20 | 2019-06-06 | グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ | Ｒｉｐｋ２阻害剤を含むコンジュゲート |
| JP6953435B2 (ja) * | 2016-05-09 | 2021-10-27 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | 二量体化合物 |
| CN108690005B (zh) * | 2018-06-26 | 2021-08-24 | 兰州大学 | 含硝基天然产物chrysamides B合成方法及其非对映异构体-化合物 |
| WO2020027225A1 (ja) | 2018-07-31 | 2020-02-06 | ファイメクス株式会社 | 複素環化合物 |
| CN111072549A (zh) * | 2018-10-19 | 2020-04-28 | 中国科学院兰州化学物理研究所苏州研究院 | 一种手性氧化吲哚螺环茚酮化合物及其合成方法 |
| JP2022519268A (ja) * | 2019-02-02 | 2022-03-22 | チア タイ ティエンチン ファーマシューティカル グループ カンパニー リミテッド | Ｐａｒｐ阻害剤としてのインドロヘプタアシルオキシム類似体 |
| JP7764027B2 (ja) | 2019-07-31 | 2025-11-05 | ファイメクス株式会社 | 複素環化合物 |
| JP7690493B2 (ja) * | 2020-05-04 | 2025-06-10 | 大鵬薬品工業株式会社 | Ｉａｐアンタゴニスト化合物及びその中間体、並びにそれを合成する方法 |
| IL298645A (en) * | 2020-06-04 | 2023-01-01 | Beigene Ltd | Pyrido[2,3-b][1,4]oxazines or tetrahydropyrido[2,3-b][1,4]oxazines as iap antagonists |
| MX2023010590A (es) * | 2021-03-10 | 2023-09-22 | Acondicionamiento Tarrasense | Nuevos derivados de 2,3-dihidro-1h-pirrolo[3,2-b]piridina como ligandos sigma. |
| EP4490159A4 (en) * | 2022-03-11 | 2025-08-20 | Ascentage Pharma Suzhou Co Ltd | TRICYCLIC HETEROCYCLIC COMPOUNDS AS IAP ANTAGONISTS |
| JPWO2024071371A1 (enExample) * | 2022-09-30 | 2024-04-04 | ||
| CN118027138A (zh) * | 2022-11-07 | 2024-05-14 | 南京中澳转化医学研究院有限公司 | 吡啶酮类化合物及其制备方法、药物组合物和应用 |
| CN120752233A (zh) * | 2023-02-28 | 2025-10-03 | 上海海雁医药科技有限公司 | 取代的三环衍生物及其药物组合物和用途 |
| CN116253756B (zh) * | 2023-05-11 | 2023-07-18 | 北京元延医药科技股份有限公司 | 克立硼罗的制备方法 |
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