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 | |
| GBGB1106817.8A GB201106817D0 (en) | 2011-04-21 | 2011-04-21 | New compound |
| US61/477,726 | 2011-04-21 | ||
| GB1106817.8 | 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 (https=) | 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 (https=) |
| EP (2) | EP2699562B1 (https=) |
| JP (1) | JP6100238B2 (https=) |
| KR (1) | KR101896134B1 (https=) |
| CN (1) | CN103492376B (https=) |
| AR (2) | AR086468A1 (https=) |
| AU (1) | AU2012246081B2 (https=) |
| BR (1) | BR112013027121B8 (https=) |
| CA (1) | CA2831346C (https=) |
| CY (1) | CY1123991T1 (https=) |
| DK (1) | DK2699562T3 (https=) |
| ES (1) | ES2855171T3 (https=) |
| GB (1) | GB201106817D0 (https=) |
| HR (1) | HRP20210450T1 (https=) |
| HU (1) | HUE053688T2 (https=) |
| IL (1) | IL228923A (https=) |
| LT (1) | LT2699562T (https=) |
| MX (1) | MX352564B (https=) |
| MY (1) | MY168159A (https=) |
| NZ (1) | NZ615572A (https=) |
| PH (1) | PH12013502002A1 (https=) |
| PL (1) | PL2699562T3 (https=) |
| PT (1) | PT2699562T (https=) |
| RU (1) | RU2662827C2 (https=) |
| SG (1) | SG193542A1 (https=) |
| SI (1) | SI2699562T1 (https=) |
| TW (1) | TWI558698B (https=) |
| WO (1) | WO2012143726A1 (https=) |
| ZA (1) | ZA201307797B (https=) |
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 |
| 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 |
| GB201218862D0 (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 |
| BR122022015241B1 (pt) * | 2013-12-20 | 2023-09-26 | Astex Therapeutics Limited | Compostos heterocíclicos bicíclicos intermediários para a preparação de um composto de fórmula (i) |
| MX374574B (es) | 2014-05-22 | 2025-03-06 | Hoffmann La Roche | Derivados indolin-2-ona y 1,3-dihidro-pirrol[3,2-c]piridin-2-ona. |
| AU2015279377B2 (en) | 2014-06-26 | 2019-09-12 | F. Hoffmann-La Roche Ag | Indolin-2-one or pyrrolo-pyridin-2-one derivatives |
| 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 |
| 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 |
| 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 |
| EP3226915B1 (en) | 2014-12-03 | 2019-02-20 | Janssen Pharmaceutica NV | Radiolabelled mglur2 pet ligands |
| RU2711382C2 (ru) | 2014-12-03 | 2020-01-16 | Янссен Фармацевтика Нв | 6,7-ДИГИДРОПИРАЗОЛО[1,5-a]ПИРАЗИН-4(5H)-ОНОВЫЕ СОЕДИНЕНИЯ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ОТРИЦАТЕЛЬНЫХ АЛЛОСТЕРИЧЕСКИХ МОДУЛЯТОРОВ РЕЦЕПТОРОВ MGLUR2 |
| EP3317269B1 (en) * | 2015-07-02 | 2022-09-21 | F. Hoffmann-La Roche AG | Bicyclic lactams as receptor-interacting protein-1 (rip1) kinase inhibitors for treating e.g. inflammatory diseases |
| RS60981B1 (sr) | 2015-12-18 | 2020-11-30 | Janssen Pharmaceutica Nv | Radiooznačeni mglur2/3 pet ligandi |
| JP6929285B2 (ja) | 2015-12-18 | 2021-09-01 | ヤンセン ファーマシューティカ エヌ．ベー． | 放射性標識ｍＧｌｕＲ２／３ＰＥＴリガンド |
| 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 |
| 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 |
| CN113365998B (zh) * | 2019-02-02 | 2023-04-14 | 正大天晴药业集团股份有限公司 | 用于parp抑制剂的吲哚并七元酰肟类似物 |
| JP7764027B2 (ja) | 2019-07-31 | 2025-11-05 | ファイメクス株式会社 | 複素環化合物 |
| 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 |
| AR125043A1 (es) * | 2021-03-10 | 2023-05-31 | 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 (https=) * | 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 |
| WO2024258988A2 (en) * | 2023-06-13 | 2024-12-19 | Delix Therapeutics, Inc. | Serotonin releasing compounds and uses thereof |
Family Cites Families (85)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR901228A (fr) | 1943-01-16 | 1945-07-20 | Deutsche Edelstahlwerke Ag | Système d'aimant à entrefer annulaire |
| US4080330A (en) | 1975-06-23 | 1978-03-21 | Delmar Chemicals Limited | Phenylindolines and process for their production |
| US4666828A (en) | 1984-08-15 | 1987-05-19 | The General Hospital Corporation | Test for Huntington's disease |
| US4683202A (en) | 1985-03-28 | 1987-07-28 | Cetus Corporation | Process for amplifying nucleic acid sequences |
| US4801531A (en) | 1985-04-17 | 1989-01-31 | Biotechnology Research Partners, Ltd. | Apo AI/CIII genomic polymorphisms predictive of atherosclerosis |
| DE3822792C2 (de) | 1987-07-11 | 1997-11-27 | Sandoz Ag | Neue Verwendung von 5HT¶3¶-Antagonisten |
| US5272057A (en) | 1988-10-14 | 1993-12-21 | Georgetown University | Method of detecting a predisposition to cancer by the use of restriction fragment length polymorphism of the gene for human poly (ADP-ribose) polymerase |
| US5192659A (en) | 1989-08-25 | 1993-03-09 | Genetype Ag | Intron sequence analysis method for detection of adjacent and remote locus alleles as haplotypes |
| TW218875B (https=) | 1992-03-09 | 1994-01-11 | Takeda Pharm Industry Co Ltd | |
| EP0951541B1 (en) | 1995-07-31 | 2005-11-30 | Urocor, Inc. | Biomarkers and targets for diagnosis, prognosis and management of prostate disease |
| US6218529B1 (en) | 1995-07-31 | 2001-04-17 | Urocor, Inc. | Biomarkers and targets for diagnosis, prognosis and management of prostate, breast and bladder cancer |
| 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 |
| AU7526798A (en) | 1997-04-18 | 1998-11-27 | Smithkline Beecham Plc | Acetamide and urea derivatives, process for their preparation and their use in the treatment of cns disorders |
| US6557977B1 (en) | 1997-07-15 | 2003-05-06 | Silverbrook Research Pty Ltd | Shape memory alloy ink jet printing mechanism |
| US6084098A (en) | 1999-02-26 | 2000-07-04 | Neurogen Corporation | Benzylpiperazinyl and piperidinyl ethanone derivatives: dopamine receptor subtype specific ligands |
| IL137930A0 (en) | 1998-02-26 | 2001-10-31 | Neurogen Corp | Benzylpiperazinyl and benzylpiperidinyl ethanone derivatives, their preparation and their use as a dopamine d4 receptor antagonists |
| 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 |
| TW200402417A (en) | 2002-06-21 | 2004-02-16 | Akzo Nobel Nv | 1-[(Indol-3-yl)carbonyl]piperazine derivatives |
| BRPI0408136A (pt) | 2003-03-07 | 2006-03-01 | Astellas Pharma Inc | derivados heterocìclicos contendo nitrogênio tendo estirila 2,6-dissubstituìda |
| GB0307891D0 (en) * | 2003-04-04 | 2003-05-14 | Angeletti P Ist Richerche Bio | Chemical compounds,compositions and uses |
| 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 |
| DK2253614T3 (da) | 2004-04-07 | 2013-01-07 | Novartis Ag | IAP-inhibitorer |
| KR100984459B1 (ko) | 2004-07-02 | 2010-09-29 | 제넨테크, 인크. | Ｉａｐ의 억제제 |
| 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. |
| MX2007010371A (es) | 2005-02-25 | 2008-01-11 | Tetralogic Pharmaceuticals | Inhibidores dimericos iap. |
| JP4955009B2 (ja) | 2005-11-11 | 2012-06-20 | エフ．ホフマン−ラ ロシュ アーゲー | 凝固因子Ｘａの阻害剤としての炭素環式縮合環アミン |
| CN101374829A (zh) | 2005-12-19 | 2009-02-25 | 健泰科生物技术公司 | Iap的抑制剂 |
| 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 |
| JP2009534456A (ja) | 2006-04-25 | 2009-09-24 | アステックス、セラピューティックス、リミテッド | 医薬化合物 |
| GB0608184D0 (en) * | 2006-04-25 | 2006-06-07 | Astex Therapeutics Ltd | Pharmaceutical compounds |
| NZ572531A (en) * | 2006-05-05 | 2011-09-30 | Univ Michigan | Bivalent smac mimetics and the uses thereof |
| 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 |
| WO2008128171A2 (en) * | 2007-04-13 | 2008-10-23 | The Regents Of The University Of Michigan | Diazo bicyclic smac mimetics and the uses thereof |
| ES2424977T3 (es) | 2007-08-08 | 2013-10-10 | Glaxosmithkline Intellectual Property Development Limited | Derivados de 2-[(2-{fenilamino}-1H-pirrolo[2,3-D]pirimidin-4-il)amino]benzamida como inhibidores de IGF-1R para el tratamiento del cáncer |
| WO2009067233A1 (en) | 2007-11-20 | 2009-05-28 | Millennium Pharmaceuticals, Inc. | Beta carbolines and uses thereof |
| 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 |
| DE102008059578A1 (de) | 2008-11-28 | 2010-06-10 | Merck Patent Gmbh | Benzo-Naphtyridin Verbindungen |
| RU2544010C2 (ru) | 2009-02-27 | 2015-03-10 | Энанта Фармасьютикалс, Инк. | Ингибиторы вируса гепатита с |
| 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 |
| UY33794A (es) | 2010-12-13 | 2012-07-31 | Novartis Ag | Inhibidores diméricos de las iap |
| 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 |
| 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 |
| 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 |
| EP4146617B8 (en) | 2020-05-04 | 2025-10-15 | Taiho Pharmaceutical Co., Ltd. | Methods for synthesizing anhydrous lactic acid |
| EP4146648A1 (en) | 2020-05-04 | 2023-03-15 | Otsuka Pharmaceutical Co., Ltd. | Iap antagonist compounds and intermediates and methods for synthesizing the same |
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