JP2013533879A5 - - Google Patents
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- JP2013533879A5 JP2013533879A5 JP2013518581A JP2013518581A JP2013533879A5 JP 2013533879 A5 JP2013533879 A5 JP 2013533879A5 JP 2013518581 A JP2013518581 A JP 2013518581A JP 2013518581 A JP2013518581 A JP 2013518581A JP 2013533879 A5 JP2013533879 A5 JP 2013533879A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- halo
- substituted
- unsubstituted
- independently
- 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
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- 125000000217 alkyl group Chemical group 0.000 claims 33
- 125000005843 halogen group Chemical group 0.000 claims 26
- 150000001875 compounds Chemical class 0.000 claims 22
- 229910052739 hydrogen Inorganic materials 0.000 claims 21
- 239000001257 hydrogen Substances 0.000 claims 20
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 14
- 150000003839 salts Chemical class 0.000 claims 11
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 10
- 125000004093 cyano group Chemical group *C#N 0.000 claims 10
- 229910052757 nitrogen Inorganic materials 0.000 claims 9
- 125000000623 heterocyclic group Chemical group 0.000 claims 8
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 7
- 125000003118 aryl group Chemical group 0.000 claims 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 208000035475 disorder Diseases 0.000 claims 6
- 125000001072 heteroaryl group Chemical group 0.000 claims 6
- 150000002431 hydrogen Chemical class 0.000 claims 6
- 125000003545 alkoxy group Chemical group 0.000 claims 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 125000004076 pyridyl group Chemical group 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- -1 amino, hydroxyl Chemical group 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 230000002062 proliferating effect Effects 0.000 claims 3
- 125000003373 pyrazinyl group Chemical group 0.000 claims 3
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 210000004027 cell Anatomy 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 1
- 206010004146 Basal cell carcinoma Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 208000005243 Chondrosarcoma Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 206010058202 Cystoid macular oedema Diseases 0.000 claims 1
- 241001481760 Erethizon dorsatum Species 0.000 claims 1
- 208000006168 Ewing Sarcoma Diseases 0.000 claims 1
- 206010016654 Fibrosis Diseases 0.000 claims 1
- 208000002260 Keloid Diseases 0.000 claims 1
- 206010023330 Keloid scar Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 208000001344 Macular Edema Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 208000017442 Retinal disease Diseases 0.000 claims 1
- 201000000582 Retinoblastoma Diseases 0.000 claims 1
- 206010038923 Retinopathy Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 208000000102 Squamous Cell Carcinoma of Head and Neck Diseases 0.000 claims 1
- 208000036765 Squamous cell carcinoma of the esophagus Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 208000008383 Wilms tumor Diseases 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 201000010206 cystoid macular edema Diseases 0.000 claims 1
- 229940127089 cytotoxic agent Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000007276 esophageal squamous cell carcinoma Diseases 0.000 claims 1
- 230000004761 fibrosis Effects 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 201000000459 head and neck squamous cell carcinoma Diseases 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 210000001117 keloid Anatomy 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 208000002780 macular degeneration Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 150000007522 mineralic acids Chemical group 0.000 claims 1
- 201000008026 nephroblastoma Diseases 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 150000007524 organic acids Chemical group 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- 125000005476 oxopyrrolidinyl group Chemical group 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 201000001474 proteinuria Diseases 0.000 claims 1
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims 1
- 230000011664 signaling Effects 0.000 claims 1
- 230000007781 signaling event Effects 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US35956910P | 2010-06-29 | 2010-06-29 | |
| US61/359,569 | 2010-06-29 | ||
| PCT/US2011/042215 WO2012003189A1 (en) | 2010-06-29 | 2011-06-28 | Compositions and methods for modulating the wnt signaling pathway |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013533879A JP2013533879A (ja) | 2013-08-29 |
| JP2013533879A5 true JP2013533879A5 (enExample) | 2014-07-03 |
| JP5778270B2 JP5778270B2 (ja) | 2015-09-16 |
Family
ID=44514972
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013518581A Active JP5778270B2 (ja) | 2010-06-29 | 2011-06-28 | Ｗｎｔシグナル伝達経路調節のための組成物および方法 |
Country Status (27)
| Country | Link |
|---|---|
| US (1) | US9181235B2 (enExample) |
| EP (1) | EP2588453B1 (enExample) |
| JP (1) | JP5778270B2 (enExample) |
| KR (1) | KR20130131290A (enExample) |
| CN (1) | CN102958917B (enExample) |
| AR (1) | AR082029A1 (enExample) |
| AU (1) | AU2011271479B2 (enExample) |
| BR (1) | BR112012033350A2 (enExample) |
| CA (1) | CA2803879A1 (enExample) |
| CL (1) | CL2012003604A1 (enExample) |
| CO (1) | CO6650353A2 (enExample) |
| CU (1) | CU20120174A7 (enExample) |
| DO (1) | DOP2012000329A (enExample) |
| EA (1) | EA201390032A1 (enExample) |
| EC (1) | ECSP13012410A (enExample) |
| ES (1) | ES2536216T3 (enExample) |
| MA (1) | MA34388B1 (enExample) |
| MX (1) | MX2012015092A (enExample) |
| NI (1) | NI201200190A (enExample) |
| PE (1) | PE20130311A1 (enExample) |
| PH (1) | PH12012502571A1 (enExample) |
| SG (1) | SG186473A1 (enExample) |
| TN (1) | TN2012000575A1 (enExample) |
| TW (1) | TW201206921A (enExample) |
| UY (1) | UY33469A (enExample) |
| WO (1) | WO2012003189A1 (enExample) |
| ZA (1) | ZA201300319B (enExample) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7723477B2 (en) | 2005-10-31 | 2010-05-25 | Oncomed Pharmaceuticals, Inc. | Compositions and methods for inhibiting Wnt-dependent solid tumor cell growth |
| SG190568A1 (en) | 2008-09-26 | 2013-06-28 | Oncomed Pharm Inc | Frizzled-binding agents and uses thereof |
| UA103918C2 (en) | 2009-03-02 | 2013-12-10 | Айерем Элелси | N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as wnt signaling modulators |
| TWI535445B (zh) | 2010-01-12 | 2016-06-01 | 安可美德藥物股份有限公司 | Ｗｎｔ拮抗劑及治療和篩選方法 |
| NZ602700A (en) | 2010-04-01 | 2014-10-31 | Oncomed Pharm Inc | Frizzled-binding agents and uses thereof |
| UY33469A (es) * | 2010-06-29 | 2012-01-31 | Irm Llc Y Novartis Ag | Composiciones y metodos para modular la via de señalizacion de wnt |
| TWI567061B (zh) * | 2011-07-01 | 2017-01-21 | 吉李德科學股份有限公司 | 用於治療成癮之化合物 |
| RU2486859C1 (ru) * | 2012-02-02 | 2013-07-10 | Федеральное государственное бюджетное учреждение "Московский научно-исследовательский институт глазных болезней имени Гельмгольца" Министерства здравоохранения и социального развития Российской Федерации | Способ оценки эффективности комбинированного органосохраняющего лечения первичной начальной ретинобластомы у детей |
| JP6081582B2 (ja) * | 2012-06-15 | 2017-02-15 | キュアジェニックス インコーポレイテッド | Ｗｎｔシグナリング阻害剤、組成物およびその用途としての化合物 |
| US9266959B2 (en) | 2012-10-23 | 2016-02-23 | Oncomed Pharmaceuticals, Inc. | Methods of treating neuroendocrine tumors using frizzled-binding agents |
| HK1211887A1 (en) | 2013-02-04 | 2016-06-03 | Oncomed Pharmaceuticals, Inc. | Methods and monitoring of treatment with a wnt pathway inhibitor |
| US9168300B2 (en) | 2013-03-14 | 2015-10-27 | Oncomed Pharmaceuticals, Inc. | MET-binding agents and uses thereof |
| GB201309333D0 (en) | 2013-05-23 | 2013-07-10 | Agency Science Tech & Res | Purine diones as WNT pathway modulators |
| CU24425B1 (es) * | 2013-11-01 | 2019-06-04 | Novartis Ag | Amino-heteroaril-benzamidas como inhibidores de cinasa |
| AU2015329784C1 (en) * | 2014-10-08 | 2020-10-15 | Redx Pharma Plc | N-pyridinyl acetamide derivatives as inhibitors of the Wnt signalling pathway |
| LT3204381T (lt) * | 2014-10-08 | 2022-08-25 | Redx Pharma Plc | N-piridinilo acetamido dariniai kaip wnt signalinio kelio inhibitoriai |
| CN104557862B (zh) * | 2014-12-15 | 2017-05-17 | 苏州云轩医药科技有限公司 | 具有Wnt信号通路抑制活性的杂环化合物 |
| WO2016126860A1 (en) | 2015-02-03 | 2016-08-11 | Kadmon Pharmaceuticals, Llc | Stable trientine formulations |
| US20180092866A1 (en) * | 2015-04-15 | 2018-04-05 | University Of Utah Research Foundation | Substituted n-([1,1'-biphenyl]-3-yl)-[1,1'-biphenyl]-3-carboxamide analogs as inhibitors for beta-catenin/b-cell lymphoma 9 interactions |
| US20180112273A1 (en) * | 2015-05-26 | 2018-04-26 | Curegenix Corporation | Tumor biomarkers and use thereof |
| CN107759584B (zh) * | 2016-08-16 | 2021-06-01 | 苏州云轩医药科技有限公司 | 一种具有Wnt信号通路抑制活性的氨基五元杂环化合物及其应用 |
| US10821104B2 (en) * | 2015-12-07 | 2020-11-03 | Suzhou Sinovent Pharmaceuticals Co., Ltd. | Five-membered heterocyclic amides WNT pathway inhibitor |
| WO2017097215A1 (zh) * | 2015-12-07 | 2017-06-15 | 杭州雷索药业有限公司 | 内嵌脲类结构的wnt通路抑制剂 |
| US11542254B2 (en) | 2016-03-25 | 2023-01-03 | Universisity Of Utah Research Foundation | Methods and composition of 4-substituted benzoylpiperazine-1-substituted carbonyls as beta-catenin/B-cell lymphoma 9 inhibitors |
| WO2018045182A1 (en) * | 2016-09-01 | 2018-03-08 | The Board Of Regents Of Hte University Of Texas System | Disubstituted and trisubtituted 1,2,3-triazoles as wnt inhibitors |
| EP3717465A1 (en) * | 2017-11-30 | 2020-10-07 | Step Pharma S.A.S. | Compounds |
| EP3717459A1 (en) | 2017-11-30 | 2020-10-07 | Step Pharma S.A.S. | Compounds |
| WO2019124603A1 (ko) * | 2017-12-22 | 2019-06-27 | 경상대학교병원 | Iwr-1을 유효성분으로 함유하는 켈로이드 예방 또는 치료용 조성물 |
| LT3762368T (lt) | 2018-03-08 | 2022-06-10 | Incyte Corporation | Aminopirazindiolio junginiai, kaip pi3k-γ inhibitoriai |
| US11046658B2 (en) | 2018-07-02 | 2021-06-29 | Incyte Corporation | Aminopyrazine derivatives as PI3K-γ inhibitors |
| CN111662228B (zh) * | 2019-03-07 | 2023-07-28 | 中国医学科学院药物研究所 | 吡啶酮酰联芳基胺类化合物及其用途 |
| WO2020245664A1 (en) | 2019-06-04 | 2020-12-10 | Step Pharma S.A.S. | N-(5-(6-ethoxypyrazin-2-yl)pyridin-2-yl)-4-(2-(methylsulfonamido)pyrimidin-4-yl) tetrahydro-2h-pyran-4-carboxamide derivatives and related compounds as human ctps1 inhibitors for the treatment of proliferative diseases |
| CN118234726A (zh) | 2021-11-25 | 2024-06-21 | 江苏恒瑞医药股份有限公司 | 一种用于雄激素受体蛋白靶向降解的嵌合体化合物、其制备方法及其在医药上的应用 |
| EP4540228A1 (en) * | 2022-06-14 | 2025-04-23 | Amygdala Neurosciences, Inc. | Aldh-2 inhibitor compounds and methods of use |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT72878B (en) | 1980-04-24 | 1983-03-29 | Merck & Co Inc | Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents |
| US6602677B1 (en) | 1997-09-19 | 2003-08-05 | Promega Corporation | Thermostable luciferases and methods of production |
| GB0124931D0 (en) * | 2001-10-17 | 2001-12-05 | Glaxo Group Ltd | Chemical compounds |
| WO2004078163A2 (en) | 2003-02-28 | 2004-09-16 | Transform Pharmaceuticals, Inc. | Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen |
| AU2003234464B2 (en) * | 2002-05-03 | 2009-06-04 | Exelixis, Inc. | Protein kinase modulators and methods of use |
| FR2847253B1 (fr) | 2002-11-19 | 2007-05-18 | Aventis Pharma Sa | Nouveaux derives de pyridazinones a titre de medicaments et compositions pharmaceutiques les renfermant |
| DE10306250A1 (de) | 2003-02-14 | 2004-09-09 | Aventis Pharma Deutschland Gmbh | Substituierte N-Arylheterozyklen, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
| US20080275062A1 (en) * | 2004-01-30 | 2008-11-06 | David Harold Drewry | Chemical Compounds |
| US20090099184A1 (en) * | 2006-02-16 | 2009-04-16 | Boehringer Ingelheim International Gmbh | Substituted pyridineamide compounds useful as soluble epoxide hydrolase inhibitors |
| BRPI0714751A2 (pt) * | 2006-09-08 | 2014-06-24 | Genentech Inc | "antagonistas wnt , composição , ácido nucléico , vetor , célula hospedeira , artigo manufaturado , método de inibição da sinalização wnt , método para detectar a presença de uam proteina wnt , método para modular a expressão de um gene wnt alvo em uma célula , método para tratar terapeuticamente um câncer mediado por wnt e usos de uns antagonistas wnt na manufatura de um medicamento " |
| JP2011502148A (ja) | 2007-10-31 | 2011-01-20 | メルク・シャープ・エンド・ドーム・コーポレイション | 疼痛の治療用としてのｐ２ｘ３受容体アンタゴニスト |
| AU2008335709A1 (en) | 2007-12-13 | 2009-06-18 | Amgen Inc. | Gamma secretase modulators |
| WO2009117269A1 (en) * | 2008-03-18 | 2009-09-24 | Merck & Co., Inc. | Substituted 4-hydroxypyrimidine-5-carboxamides |
| BRPI0913119A2 (pt) * | 2008-05-27 | 2015-07-28 | Univ Texas | Inibidores de sinalização de proteína wnt |
| US8384140B2 (en) | 2008-07-29 | 2013-02-26 | International Business Machines Corporation | Structure for dual contact trench capacitor and structure thereof |
| UA103918C2 (en) | 2009-03-02 | 2013-12-10 | Айерем Элелси | N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as wnt signaling modulators |
| UY33469A (es) * | 2010-06-29 | 2012-01-31 | Irm Llc Y Novartis Ag | Composiciones y metodos para modular la via de señalizacion de wnt |
-
2011
- 2011-06-27 UY UY0001033469A patent/UY33469A/es not_active Application Discontinuation
- 2011-06-28 SG SG2012095980A patent/SG186473A1/en unknown
- 2011-06-28 CN CN201180032354.9A patent/CN102958917B/zh active Active
- 2011-06-28 PE PE2012002648A patent/PE20130311A1/es not_active Application Discontinuation
- 2011-06-28 PH PH1/2012/502571A patent/PH12012502571A1/en unknown
- 2011-06-28 US US13/701,982 patent/US9181235B2/en active Active
- 2011-06-28 CA CA2803879A patent/CA2803879A1/en not_active Abandoned
- 2011-06-28 EP EP11733945.7A patent/EP2588453B1/en active Active
- 2011-06-28 JP JP2013518581A patent/JP5778270B2/ja active Active
- 2011-06-28 ES ES11733945.7T patent/ES2536216T3/es active Active
- 2011-06-28 WO PCT/US2011/042215 patent/WO2012003189A1/en not_active Ceased
- 2011-06-28 KR KR1020137002280A patent/KR20130131290A/ko not_active Withdrawn
- 2011-06-28 BR BR112012033350A patent/BR112012033350A2/pt not_active IP Right Cessation
- 2011-06-28 AU AU2011271479A patent/AU2011271479B2/en not_active Expired - Fee Related
- 2011-06-28 MA MA35576A patent/MA34388B1/fr unknown
- 2011-06-28 EA EA201390032A patent/EA201390032A1/ru unknown
- 2011-06-28 MX MX2012015092A patent/MX2012015092A/es not_active Application Discontinuation
- 2011-06-29 TW TW100122939A patent/TW201206921A/zh unknown
- 2011-06-29 AR ARP110102283A patent/AR082029A1/es not_active Application Discontinuation
-
2012
- 2012-12-05 TN TNP2012000575A patent/TN2012000575A1/en unknown
- 2012-12-20 CU CU2012000174A patent/CU20120174A7/es unknown
- 2012-12-20 NI NI201200190A patent/NI201200190A/es unknown
- 2012-12-20 CL CL2012003604A patent/CL2012003604A1/es unknown
- 2012-12-27 DO DO2012000329A patent/DOP2012000329A/es unknown
- 2012-12-27 CO CO12234891A patent/CO6650353A2/es unknown
-
2013
- 2013-01-14 ZA ZA2013/00319A patent/ZA201300319B/en unknown
- 2013-01-29 EC ECSP13012410 patent/ECSP13012410A/es unknown
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