JP5850952B2 - セリン／スレオニンキナーゼ阻害剤としての新しいアザインドリルフェニルスルホンアミド - Google Patents
セリン／スレオニンキナーゼ阻害剤としての新しいアザインドリルフェニルスルホンアミド Download PDFInfo
- Publication number
- JP5850952B2 JP5850952B2 JP2013552207A JP2013552207A JP5850952B2 JP 5850952 B2 JP5850952 B2 JP 5850952B2 JP 2013552207 A JP2013552207 A JP 2013552207A JP 2013552207 A JP2013552207 A JP 2013552207A JP 5850952 B2 JP5850952 B2 JP 5850952B2
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- independently
- cycloalkyl
- heterocyclyl
- nhc
- 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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Links
- 0 Cc1cc(O*)cnc1 Chemical compound Cc1cc(O*)cnc1 0.000 description 3
- HDFWVJAQABCYDP-UHFFFAOYSA-N CC(C)C1=CCCC1 Chemical compound CC(C)C1=CCCC1 HDFWVJAQABCYDP-UHFFFAOYSA-N 0.000 description 1
- QGOAVYUHMIPPOD-UHFFFAOYSA-N CC(C)C1=CCCC1C Chemical compound CC(C)C1=CCCC1C QGOAVYUHMIPPOD-UHFFFAOYSA-N 0.000 description 1
- XCYJPXQACVEIOS-UHFFFAOYSA-N CC(C)c1cccc(C)c1 Chemical compound CC(C)c1cccc(C)c1 XCYJPXQACVEIOS-UHFFFAOYSA-N 0.000 description 1
- WWRCMNKATXZARA-UHFFFAOYSA-N CC(C)c1ccccc1C Chemical compound CC(C)c1ccccc1C WWRCMNKATXZARA-UHFFFAOYSA-N 0.000 description 1
- WTCPAFWUNFLPEW-UHFFFAOYSA-N CC1=CC=C(C)CC1 Chemical compound CC1=CC=C(C)CC1 WTCPAFWUNFLPEW-UHFFFAOYSA-N 0.000 description 1
- QDLJTKFLNSIMOX-UHFFFAOYSA-N CCC(C1CC1)=N Chemical compound CCC(C1CC1)=N QDLJTKFLNSIMOX-UHFFFAOYSA-N 0.000 description 1
- KWKAWSQYCXSIML-UHFFFAOYSA-N CCC1C=CC(C)C1 Chemical compound CCC1C=CC(C)C1 KWKAWSQYCXSIML-UHFFFAOYSA-N 0.000 description 1
- WEPJHIJXYRZXRB-UHFFFAOYSA-N CCCS(Nc(c(F)c1-[n](cc2-c3cc(OC)cnc3)c(cc3)c2nc3N2CCN(C)CC2)ccc1F)(=O)=O Chemical compound CCCS(Nc(c(F)c1-[n](cc2-c3cc(OC)cnc3)c(cc3)c2nc3N2CCN(C)CC2)ccc1F)(=O)=O WEPJHIJXYRZXRB-UHFFFAOYSA-N 0.000 description 1
- CEZSIPIJAQVIOX-UHFFFAOYSA-N CCCS(Nc(c(F)c1-[n](cc2-c3cc(OC)cnc3)c(cc3)c2nc3N2CCNCC2)ccc1F)(=O)=O Chemical compound CCCS(Nc(c(F)c1-[n](cc2-c3cc(OC)cnc3)c(cc3)c2nc3N2CCNCC2)ccc1F)(=O)=O CEZSIPIJAQVIOX-UHFFFAOYSA-N 0.000 description 1
- REQSQBUKCBFQGN-UHFFFAOYSA-N CCc1cc2ccccc2c(C(C)C)c1 Chemical compound CCc1cc2ccccc2c(C(C)C)c1 REQSQBUKCBFQGN-UHFFFAOYSA-N 0.000 description 1
- LRQYSMQNJLZKPS-UHFFFAOYSA-N Cc(cc1)cc2c1ccc(C)c2 Chemical compound Cc(cc1)cc2c1ccc(C)c2 LRQYSMQNJLZKPS-UHFFFAOYSA-N 0.000 description 1
- VLPWXHZDGMUMBR-UHFFFAOYSA-N Cc1cc(OC)cnc1 Chemical compound Cc1cc(OC)cnc1 VLPWXHZDGMUMBR-UHFFFAOYSA-N 0.000 description 1
- QIMMUPPBPVKWKM-UHFFFAOYSA-N Cc1cc2ccccc2cc1 Chemical compound Cc1cc2ccccc2cc1 QIMMUPPBPVKWKM-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11153087 | 2011-02-02 | ||
| EP11153087.9 | 2011-02-02 | ||
| EP11181258.2 | 2011-09-14 | ||
| EP11181258 | 2011-09-14 | ||
| PCT/EP2012/051796 WO2012104388A1 (en) | 2011-02-02 | 2012-02-02 | New azaindolylphenyl sulfonamides as serine/threonine kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014504622A JP2014504622A (ja) | 2014-02-24 |
| JP2014504622A5 JP2014504622A5 (enExample) | 2015-03-19 |
| JP5850952B2 true JP5850952B2 (ja) | 2016-02-03 |
Family
ID=45558742
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013552207A Active JP5850952B2 (ja) | 2011-02-02 | 2012-02-02 | セリン／スレオニンキナーゼ阻害剤としての新しいアザインドリルフェニルスルホンアミド |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US8889684B2 (enExample) |
| EP (1) | EP2670749B1 (enExample) |
| JP (1) | JP5850952B2 (enExample) |
| KR (1) | KR20140014149A (enExample) |
| CN (1) | CN103476773A (enExample) |
| AU (1) | AU2012213390A1 (enExample) |
| BR (1) | BR112013019714A2 (enExample) |
| CA (1) | CA2825279A1 (enExample) |
| CL (1) | CL2013002063A1 (enExample) |
| EA (1) | EA201300874A1 (enExample) |
| IL (1) | IL227399A0 (enExample) |
| MX (1) | MX2013008868A (enExample) |
| PH (1) | PH12013501618A1 (enExample) |
| UY (1) | UY33890A (enExample) |
| WO (1) | WO2012104388A1 (enExample) |
Families Citing this family (65)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CL2008001943A1 (es) | 2007-07-02 | 2009-09-11 | Boehringer Ingelheim Int | Compuestos derivados de fenil-triazol, inhibidores de enzimas de señales especificas que participan del control de la proliferacion celular; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar cancer, infecciones, enfermedades inflamatorias y autoinmunes. |
| TW201014860A (en) | 2008-09-08 | 2010-04-16 | Boehringer Ingelheim Int | New chemical compounds |
| EP2350052B1 (en) | 2008-09-29 | 2014-08-13 | Boehringer Ingelheim International GmbH | Antiproliferative compounds |
| EP2398797B1 (en) | 2009-02-17 | 2013-11-06 | Boehringer Ingelheim International GmbH | Pyrimido[5,4-d]pyrimidine derivatives for the inhibition of tyrosine kinases |
| ES2835553T3 (es) | 2009-08-10 | 2021-06-22 | Biosplice Therapeutics Inc | Inhibidores de indazol de la vía de señalización de Wnt y sus usos terapéuticos |
| SMT201700581T1 (it) | 2009-12-21 | 2018-01-11 | Samumed Llc | 1h-pirazolo[3,4-b]piridine e loro usi terapeutici |
| EP2552907B1 (en) | 2010-03-26 | 2014-10-22 | Boehringer Ingelheim International GmbH | Pyridyltriazoles |
| US9290507B2 (en) | 2010-03-26 | 2016-03-22 | Boehringer Ingelheim International Gmbh | B-RAF kinase inhibitors |
| EP2571361A4 (en) | 2010-05-19 | 2013-11-13 | Univ North Carolina | PYRAZOLOPYRIMIDINE COMPOUNDS FOR CANCER TREATMENT |
| US8710055B2 (en) | 2010-12-21 | 2014-04-29 | Boehringer Ingelheim International Gmbh | Triazolylphenyl sulfonamides as serine/threonine kinase inhibitors |
| US8889684B2 (en) | 2011-02-02 | 2014-11-18 | Boehringer Ingelheim International Gmbh | Azaindolylphenyl sulfonamides as serine/threonine kinase inhibitors |
| HUE041576T2 (hu) | 2011-09-14 | 2019-05-28 | Samumed Llc | Indazol-3-karboxamid-származékok és alkalmazásuk Wnt/b-katenin szignalizáló útvonal inhibitorokként |
| PH12017500997A1 (en) | 2012-04-04 | 2018-02-19 | Samumed Llc | Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof |
| SG11201407148XA (en) | 2012-05-04 | 2014-11-27 | Samumed Llc | 1h-pyrazolo[3,4-b]pyridines and therapeutic uses thereof |
| JP2015517574A (ja) | 2012-05-22 | 2015-06-22 | ザ・ユニヴァーシティ・オヴ・ノース・キャロライナ・アト・チャペル・ヒル | がん治療のためのピリミジン化合物 |
| WO2014062774A1 (en) | 2012-10-17 | 2014-04-24 | The University Of North Carolina At Chapel Hill | Pyrazolopyrimidine compounds for the treatment of cancer |
| WO2014085225A1 (en) | 2012-11-27 | 2014-06-05 | The University Of North Carolina At Chapel Hill | Pyrimidine compounds for the treatment of cancer |
| US9908867B2 (en) | 2013-01-08 | 2018-03-06 | Samumed, Llc | 3-(benzoimidazol-2-yl)-indazole inhibitors of the Wnt signaling pathway and therapeutic uses thereof |
| US11021752B2 (en) | 2013-03-15 | 2021-06-01 | Myriad Genetics, Inc. | Genes and gene signatures for diagnosis and treatment of melanoma |
| US9649309B2 (en) | 2014-04-11 | 2017-05-16 | The University Of North Carolina At Chapel Hill | Therapeutic uses of selected pyrimidine compounds with anti-Mer tyrosine kinase activity |
| EP3164508B1 (en) | 2014-07-02 | 2023-06-07 | Myriad myPath, LLC | Genes and gene signatures for diagnosis and treatment of melanoma |
| WO2016040181A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof |
| WO2016040184A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof |
| WO2016040185A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 2-(1h-indazol-3-yl)-3h-imidazo[4,5-b]pyridine and therapeutic uses thereof |
| WO2016040182A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 2-(1h-indazol-3-yl)-1h-imidazo[4,5-c]pyridine and therapeutic uses thereof |
| WO2016040193A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine and therapeutic uses thereof |
| WO2016040180A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(1h-benzo[d]imidazol-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof |
| WO2016040188A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(3h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof |
| WO2016040190A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine and therapeutic uses thereof |
| CN107454899B (zh) * | 2014-10-27 | 2020-05-29 | 大学健康网络 | Ripk2抑制剂及用其治疗癌症的方法 |
| WO2017024026A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc | 3-(1h-indol-2-yl)-1h-pyrazolo[3,4-c]pyridines and therapeutic uses thereof |
| US10195185B2 (en) | 2015-08-03 | 2019-02-05 | Samumed, Llc | 3-(1H-imidazo[4,5-C]pyridin-2-yl)-1H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof |
| US10350199B2 (en) | 2015-08-03 | 2019-07-16 | Samumed, Llc | 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-indazoles and therapeutic uses thereof |
| US10206908B2 (en) | 2015-08-03 | 2019-02-19 | Samumed, Llc | 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof |
| WO2017023989A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-benzo[d]imidazol-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof |
| US10604512B2 (en) | 2015-08-03 | 2020-03-31 | Samumed, Llc | 3-(1H-indol-2-yl)-1H-indazoles and therapeutic uses thereof |
| WO2017023980A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridines and therapeutic uses thereof |
| US10285983B2 (en) | 2015-08-03 | 2019-05-14 | Samumed, Llc | 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[3,4-B] pyridines and therapeutic uses thereof |
| WO2017023987A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridines and therapeutic uses thereof |
| US10231956B2 (en) | 2015-08-03 | 2019-03-19 | Samumed, Llc | 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1 H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof |
| US10188634B2 (en) | 2015-08-03 | 2019-01-29 | Samumed, Llc | 3-(3H-imidazo[4,5-C]pyridin-2-yl)-1 H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof |
| WO2017024025A1 (en) | 2015-08-03 | 2017-02-09 | Sunil Kumar Kc | 3-(1h-pyrrolo[2,3-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof |
| US10329309B2 (en) | 2015-08-03 | 2019-06-25 | Samumed, Llc | 3-(3H-imidazo[4,5-B]pyridin-2-yl)-1H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof |
| US10206909B2 (en) | 2015-08-03 | 2019-02-19 | Samumed, Llc | 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof |
| US10463651B2 (en) | 2015-08-03 | 2019-11-05 | Samumed, Llc | 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1H-indazoles and therapeutic uses thereof |
| WO2017023993A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-indol-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof |
| US10383861B2 (en) | 2015-08-03 | 2019-08-20 | Sammumed, LLC | 3-(1H-pyrrolo[2,3-C]pyridin-2-yl)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof |
| KR102048719B1 (ko) * | 2015-08-13 | 2019-11-26 | 베이징 한미 파마슈티컬 컴퍼니 리미티드 | Irak4억제제 및 이의 용도 |
| WO2017079759A1 (en) | 2015-11-06 | 2017-05-11 | Samumed, Llc | 2-(1h-indazol-3-yl)-3h-imidazo[4,5-c]pyridines and their anti-inflammatory uses thereof |
| US10709708B2 (en) | 2016-03-17 | 2020-07-14 | The University Of North Carolina At Chapel Hill | Method of treating cancer with a combination of MER tyrosine kinase inhibitor and an epidermal growth factor receptor (EGFR) inhibitor |
| AR108325A1 (es) | 2016-04-27 | 2018-08-08 | Samumed Llc | Isoquinolin-3-il carboxamidas y preparación y uso de las mismas |
| MY199242A (en) | 2016-06-01 | 2023-10-22 | Samumed Llc | Process for preparing n-(5-(3-(7-(3-fluorophenyl)-3h-imidazo[4,5-c]pyridin-2-yl)-1h-indazol-5-yl)pyridin-3-yl)-3-methylbutanamide |
| BR112019008061A2 (pt) | 2016-10-21 | 2019-09-17 | Samumed Llc | métodos de uso de indazol-3-carboxamidas e seu uso como inibidores da via de sinalização de wnt/b-catenina |
| MA46696A (fr) | 2016-11-07 | 2019-09-11 | Samumed Llc | Formulations injectables à dose unique prêtes à l'emploi |
| IL266842B (en) | 2016-12-01 | 2022-09-01 | Arvinas Operations Inc | History of tetrahydronaphthalene and tetrahydroisoquinoline as estrogen receptor antagonists |
| IL325835A (en) * | 2016-12-23 | 2026-03-01 | Univ Yale | Compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides |
| US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides |
| ES2947411T3 (es) | 2017-10-26 | 2023-08-08 | Xynomic Pharmaceuticals Inc | Sales cristalinas de un campo inhibidor de quinasa B-RAF |
| WO2021041348A1 (en) | 2019-08-26 | 2021-03-04 | Arvinas Operations, Inc. | Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders |
| WO2022047145A1 (en) | 2020-08-28 | 2022-03-03 | Arvinas Operations, Inc. | Rapidly accelerating fibrosarcoma protein degrading compounds and associated methods of use |
| AU2021342287A1 (en) | 2020-09-14 | 2023-04-13 | Arvinas Operations, Inc. | Crystalline forms of a compound for the targeted degradation of estrogen receptor |
| TW202329937A (zh) | 2021-12-03 | 2023-08-01 | 美商英塞特公司 | 雙環胺ｃｋ１２抑制劑 |
| US12084453B2 (en) | 2021-12-10 | 2024-09-10 | Incyte Corporation | Bicyclic amines as CDK12 inhibitors |
| CN115010574B (zh) * | 2022-06-06 | 2024-01-05 | 爱斯特（成都）生物制药股份有限公司 | 1-溴-2-氯-4-氟-2碘苯的合成方法 |
| EP4584258A1 (en) | 2022-09-07 | 2025-07-16 | Arvinas Operations, Inc. | Rapidly accelerated fibrosarcoma (raf) degrading compounds and associated methods of use |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CZ2001959A3 (cs) * | 1998-09-18 | 2001-12-12 | Basf Aktiengesellschaft | 4-Aminopyrrolopyrimidiny jako inhibitory kinasy |
| KR20020088406A (ko) * | 1999-09-17 | 2002-11-27 | 애보트 게엠베하 운트 콤파니 카게 | 치료제로서의 피라졸로피리미딘 |
| ATE329909T1 (de) | 2002-11-27 | 2006-07-15 | Boehringer Ingelheim Pharma | 1,2,3-triazolamid-derivate als cytokininhibitoren |
| BRPI0413746A (pt) * | 2003-08-21 | 2006-10-24 | Osi Pharm Inc | composto ou um seu n-óxido ou seu sal farmaceuticamente aceitável, composição, e, método de tratamento de distúrbio hiperproliferativo |
| US7511042B2 (en) | 2003-12-03 | 2009-03-31 | Boehringer Ingelheim Pharmaceuticals, Inc. | Triazole compounds |
| ES2389203T3 (es) * | 2004-01-12 | 2012-10-24 | Ym Biosciences Australia Pty Ltd | Inhibidores de quinasa selectivos |
| EP1725544B1 (en) | 2004-03-09 | 2009-05-27 | Boehringer Ingelheim Pharmaceuticals Inc. | 3-[4-heterocyclyl-1,2,3-triazol-1-yl]-n-aryl-benzamides as inhibitors of the cytokines production for the treatment of chronic inflammatory diseases |
| US7485657B2 (en) | 2004-05-12 | 2009-02-03 | Boehringer Ingelheim Pharmaceuticals, Inc. | Anti-cytokine heterocyclic compounds |
| US20060004197A1 (en) * | 2004-07-02 | 2006-01-05 | Thomas Thrash | Sulfonamide-based compounds as protein tyrosine kinase inhibitors |
| US7531560B2 (en) | 2004-11-10 | 2009-05-12 | Boehringer Ingelheim Pharmaceuticals, Inc. | Anti-cytokine heterocyclic compounds |
| JP2007076376A (ja) | 2005-09-09 | 2007-03-29 | Yanmar Co Ltd | トラクタ |
| GB0526246D0 (en) * | 2005-12-22 | 2006-02-01 | Novartis Ag | Organic compounds |
| JP2009536618A (ja) | 2006-04-18 | 2009-10-15 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ４−及び５−イミダゾリル環を含むサイトカイン阻害化合物の製造方法及びその中間体 |
| PE20080401A1 (es) | 2006-07-07 | 2008-06-23 | Boehringer Ingelheim Int | DERIVADOS DE HETEROARIL-FENIL SUSTITUIDOS COMO INHIBIDORES DE B-Raf-QUINASAS |
| CA2692379A1 (en) | 2007-07-02 | 2009-01-08 | Boehringer Ingelheim International Gmbh | Antiproliferative compounds based on 5-membered heterocycles |
| CL2008001943A1 (es) | 2007-07-02 | 2009-09-11 | Boehringer Ingelheim Int | Compuestos derivados de fenil-triazol, inhibidores de enzimas de señales especificas que participan del control de la proliferacion celular; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar cancer, infecciones, enfermedades inflamatorias y autoinmunes. |
| JP2010533729A (ja) | 2007-07-17 | 2010-10-28 | プレキシコン，インコーポレーテッド | キナーゼ調節のための化合物と方法、及びそのための適応 |
| SI2215094T1 (sl) * | 2007-11-15 | 2016-05-31 | Ym Biosciences Australia Pty Ltd | N vsebujoče heterociklične spojine |
| EP2350052B1 (en) | 2008-09-29 | 2014-08-13 | Boehringer Ingelheim International GmbH | Antiproliferative compounds |
| WO2010042337A1 (en) | 2008-10-07 | 2010-04-15 | Merck Sharp & Dohme Corp. | Novel 6-azaindole aminopyrimidine derivatives having nik inhibitory activity |
| TW201041888A (en) * | 2009-05-06 | 2010-12-01 | Plexxikon Inc | Compounds and methods for kinase modulation, and indications therefor |
| EP2470538A1 (en) * | 2009-08-28 | 2012-07-04 | Array Biopharma, Inc. | Raf inhibitor compounds and methods of use thereof |
| US9290507B2 (en) | 2010-03-26 | 2016-03-22 | Boehringer Ingelheim International Gmbh | B-RAF kinase inhibitors |
| US8710055B2 (en) | 2010-12-21 | 2014-04-29 | Boehringer Ingelheim International Gmbh | Triazolylphenyl sulfonamides as serine/threonine kinase inhibitors |
| US8546443B2 (en) | 2010-12-21 | 2013-10-01 | Boehringer Ingelheim International Gmbh | Benzylic oxindole pyrimidines |
| US20130023531A1 (en) | 2011-01-27 | 2013-01-24 | Boehringer Ingelheim International Gmbh | Pyrimido[5,4-d]pyrimidylamino phenyl sulfonamides as serine/threonine kinase inhibitors |
| US8889684B2 (en) | 2011-02-02 | 2014-11-18 | Boehringer Ingelheim International Gmbh | Azaindolylphenyl sulfonamides as serine/threonine kinase inhibitors |
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- 2012-02-02 AU AU2012213390A patent/AU2012213390A1/en not_active Abandoned
- 2012-02-02 JP JP2013552207A patent/JP5850952B2/ja active Active
- 2012-02-02 CN CN2012800157100A patent/CN103476773A/zh active Pending
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Also Published As
| Publication number | Publication date |
|---|---|
| JP2014504622A (ja) | 2014-02-24 |
| WO2012104388A1 (en) | 2012-08-09 |
| EA201300874A1 (ru) | 2014-02-28 |
| EP2670749B1 (en) | 2016-01-27 |
| CL2013002063A1 (es) | 2013-12-27 |
| CN103476773A (zh) | 2013-12-25 |
| BR112013019714A2 (pt) | 2016-10-18 |
| AU2012213390A1 (en) | 2013-08-01 |
| PH12013501618A1 (en) | 2013-09-30 |
| MX2013008868A (es) | 2013-08-14 |
| US20130029993A1 (en) | 2013-01-31 |
| KR20140014149A (ko) | 2014-02-05 |
| US8889684B2 (en) | 2014-11-18 |
| CA2825279A1 (en) | 2012-08-09 |
| IL227399A0 (en) | 2013-09-30 |
| EP2670749A1 (en) | 2013-12-11 |
| UY33890A (es) | 2012-08-31 |
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