CY1118112T1 - Διυποκατεστημενες βενζοθειενυλ-πυρρολοτριαζινες και η χρηση τους ως αναστολεις κινασης υποδοχεα του αυξητικου παραγοντα των ινοβλαστων (fgfr) - Google Patents
Διυποκατεστημενες βενζοθειενυλ-πυρρολοτριαζινες και η χρηση τους ως αναστολεις κινασης υποδοχεα του αυξητικου παραγοντα των ινοβλαστων (fgfr)Info
- Publication number
- CY1118112T1 CY1118112T1 CY20161100853T CY161100853T CY1118112T1 CY 1118112 T1 CY1118112 T1 CY 1118112T1 CY 20161100853 T CY20161100853 T CY 20161100853T CY 161100853 T CY161100853 T CY 161100853T CY 1118112 T1 CY1118112 T1 CY 1118112T1
- Authority
- CY
- Cyprus
- Prior art keywords
- hydrogen
- compounds
- differentialized
- benzothythenyl
- pyrrolotriazines
- Prior art date
Links
Classifications
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- 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
-
- 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/541—Non-condensed thiazines containing further heterocyclic rings
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Treatment Of Liquids With Adsorbents In General (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
Αυτή η εφεύρεση αναφέρεται σε νέα υποκατεστημένο παράγωγο της 5-(1-βενζοθειοφαιν-2-υλο) πυρρολο[2,1-f][1,2,4]τριαζιν-4-αμίνης του τύπου (I) όπου το R1 είναι υδρογόνο, χλώριο, μεθύλιο ή μεθοξύ, το R2 είναι υδρογόνο ή μεθοξύ, με την προϋπόθεση ότι τουλάχιστον ένα εκ των R1 και R2 είναι άλλο εκτός από υδρογόνο, το G1 είναι χλώριο, (C1-C4)-αλκύλιο, (C1-C4)-αλκοξυκαρβονυλιο, 5-μελές αζα-ετεροαρύλιο, ή η ομάδα -CH2-OR3, -CH2-NR4R5 ή -C(=0)- NR4R6, και το G2 είναι χλώριο, κυάνιο, (C1-C4)-αλκύλιο ή η ομάδα - CR8AR8B-OH, -CH2-NR9R10, -C(=0)-NR11R12 ή -CH2-OR15, που έχουν ανασταλτικές δράσεις της πρωτεϊνικής κινάσης τυροσίνης, σε διαδικασίες για την παρασκευή τέτοιων ενώσεων, σε φαρμακευτικές συνθέσεις που περιέχουν τέτοιες ενώσεις, και στη χρήση τέτοιων ενώσεων ή συνθέσεων για την θεραπεία νεοπλαστικών διαταραχών, ιδιαίτερα των παθήσεων καρκίνου και όγκου.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11193841 | 2011-12-15 | ||
| EP12798738.6A EP2791140B1 (en) | 2011-12-15 | 2012-12-10 | Disubstituted benzothienyl-pyrrolotriazines and their use as fgfr kinase inhibitors |
| PCT/EP2012/074977 WO2013087578A1 (en) | 2011-12-15 | 2012-12-10 | Disubstituted benzothienyl-pyrrolotriazines and their use as fgfr kinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CY1118112T1 true CY1118112T1 (el) | 2017-06-28 |
Family
ID=47326168
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CY20161100853T CY1118112T1 (el) | 2011-12-15 | 2016-08-31 | Διυποκατεστημενες βενζοθειενυλ-πυρρολοτριαζινες και η χρηση τους ως αναστολεις κινασης υποδοχεα του αυξητικου παραγοντα των ινοβλαστων (fgfr) |
Country Status (43)
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| US10388493B2 (en) | 2011-09-16 | 2019-08-20 | Lam Research Corporation | Component of a substrate support assembly producing localized magnetic fields |
| UY34484A (es) * | 2011-12-15 | 2013-07-31 | Bayer Ip Gmbh | Benzotienilo-pirrolotriazinas disustituidas y sus usos |
| JP6084292B2 (ja) | 2013-07-18 | 2017-02-22 | 大鵬薬品工業株式会社 | Ｆｇｆｒ阻害剤耐性癌の治療薬 |
| US20160193210A1 (en) | 2013-07-18 | 2016-07-07 | Taiho Pharmaceutical Co., Ltd. | Antitumor drug for intermittent administration of fgfr inhibitor |
| JP6434506B2 (ja) * | 2013-10-21 | 2018-12-05 | ジェノスコ | 置換ピリミジン化合物およびｓｙｋ阻害剤としてのそれらの使用 |
| AU2015359538A1 (en) * | 2014-12-11 | 2017-06-08 | Bayer Pharma Aktiengesellschaft | Use of pan FGFR inhibitors and method of identifying patients with cancer eligible for treatment with a pan FGFR inhibitor |
| BR112017019188A2 (pt) * | 2015-03-09 | 2018-04-24 | Bayer Pharma Aktiengesellschaft | Combinações contendo 2,3-di-hidroimidazo[1,2-c] quinazolina substituídas |
| US10221191B2 (en) | 2015-12-22 | 2019-03-05 | SHY Therapeutics LLC | Compounds for the treatment of cancer and inflammatory disease |
| US11883404B2 (en) | 2016-03-04 | 2024-01-30 | Taiho Pharmaceuticals Co., Ltd. | Preparation and composition for treatment of malignant tumors |
| KR20240014585A (ko) | 2016-03-04 | 2024-02-01 | 다이호야쿠힌고교 가부시키가이샤 | 악성 종양 치료용 제제 및 조성물 |
| MD3436461T2 (ro) | 2016-03-28 | 2024-05-31 | Incyte Corp | Compuși pirolotriazină ca inhibitori TAM |
| CN107513068A (zh) * | 2016-06-16 | 2017-12-26 | 中国科学院上海药物研究所 | 一种具有fgfr抑制活性的新型化合物及其制备和应用 |
| AU2017378324B2 (en) | 2016-12-16 | 2021-09-02 | Cystic Fibrosis Foundation | Bycyclic heteroaryl derivatives as CFTR potentiators |
| SG11201911929XA (en) | 2017-06-21 | 2020-01-30 | SHY Therapeutics LLC | Compounds that interact with the ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease |
| AU2018317153B2 (en) * | 2017-08-15 | 2021-12-23 | Cspc Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd. | FGFR inhibitor and medical application thereof |
| WO2019034075A1 (zh) * | 2017-08-15 | 2019-02-21 | 南京明德新药研发股份有限公司 | Fgfr和egfr抑制剂 |
| MX2020003375A (es) | 2017-09-27 | 2020-08-03 | Incyte Corp | Sales de inhibidores de macrofagos asociados a tumores (tam). |
| WO2019081346A1 (en) | 2017-10-25 | 2019-05-02 | Bayer Pharma Aktiengesellschaft | PROCESS FOR THE PREPARATION OF BENZOTHIOPHEN-2YL BORONATE |
| WO2019105734A1 (en) | 2017-11-28 | 2019-06-06 | Bayer Consumer Care Ag | Combinations of copanlisib |
| DK3769765T3 (da) | 2018-03-19 | 2024-05-13 | Taiho Pharmaceutical Co Ltd | Farmaceutisk sammensætning indeholdende natriumalkylsulfat |
| WO2019180141A1 (en) | 2018-03-23 | 2019-09-26 | Bayer Aktiengesellschaft | Combinations of rogaratinib |
| EA202192133A1 (ru) * | 2019-01-31 | 2022-02-09 | Байер Акциенгезельшафт | Моногидрат гидрохлорида рогаратиниба и его твердые состояния |
| CA3130247C (en) * | 2019-02-15 | 2024-02-13 | Cspc Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd | Fgfr inhibitor compound in solid form and preparation method therefor |
| WO2020170355A1 (ja) * | 2019-02-20 | 2020-08-27 | 大鵬薬品工業株式会社 | Ｆｇｆｒ１変異腫瘍の治療方法 |
| CN109928976A (zh) * | 2019-02-26 | 2019-06-25 | 泰州亿腾景昂药业有限公司 | 一种工业化生产eoc317的方法 |
| CN114641293B (zh) * | 2019-11-08 | 2024-05-31 | 石药集团中奇制药技术（石家庄）有限公司 | 一种fgfr抑制剂的用途 |
| CN111004234A (zh) * | 2019-11-28 | 2020-04-14 | 湖南农业大学 | 一种2-苯基咪唑并[1,2-α]吡啶类化合物的C3位卤化方法 |
| JP2023516441A (ja) | 2020-03-06 | 2023-04-19 | インサイト・コーポレイション | Ａｘｌ／ｍｅｒ阻害剤及びｐｄ－１／ｐｄ－ｌ１阻害剤を含む併用療法 |
| JP7563752B2 (ja) | 2021-03-31 | 2024-10-08 | 川上産業株式会社 | 空間仕切りパネル、及び組立式個室 |
| CN117402161A (zh) * | 2022-07-06 | 2024-01-16 | 上海科恩泰生物医药科技有限公司 | 一种具有fgfr抑制作用的亚砜亚胺类化合物、包含其的药物组合物及其用途 |
| WO2024206858A1 (en) | 2023-03-30 | 2024-10-03 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
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| AU2006320440B2 (en) | 2005-12-02 | 2012-04-05 | Bayer Healthcare Llc | Substituted 4-amino-pyrrolotriazine derivatives useful for treating hyper-proliferative disorders and diseases associated with angiogenesis |
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2012
- 2012-12-03 UY UY0001034484A patent/UY34484A/es unknown
- 2012-12-10 ES ES12798738.6T patent/ES2591203T3/es active Active
- 2012-12-10 HU HUE12798738A patent/HUE029582T2/en unknown
- 2012-12-10 WO PCT/EP2012/074977 patent/WO2013087578A1/en active Application Filing
- 2012-12-10 EP EP12798738.6A patent/EP2791140B1/en active Active
- 2012-12-10 UA UAA201407930A patent/UA116768C2/uk unknown
- 2012-12-10 AU AU2012350750A patent/AU2012350750B2/en not_active Ceased
- 2012-12-10 LT LTEP12798738.6T patent/LT2791140T/lt unknown
- 2012-12-10 BR BR112014014531-8A patent/BR112014014531B1/pt not_active IP Right Cessation
- 2012-12-10 PL PL12798738T patent/PL2791140T3/pl unknown
- 2012-12-10 ME MEP-2016-181A patent/ME02517B/me unknown
- 2012-12-10 IN IN4310CHN2014 patent/IN2014CN04310A/en unknown
- 2012-12-10 JP JP2014546445A patent/JP6050829B2/ja not_active Expired - Fee Related
- 2012-12-10 CA CA2859133A patent/CA2859133C/en active Active
- 2012-12-10 CU CU2016000039A patent/CU24426B1/es unknown
- 2012-12-10 MX MX2014006905A patent/MX367158B/es active IP Right Grant
- 2012-12-10 CN CN201280069882.6A patent/CN104245700B/zh not_active Expired - Fee Related
- 2012-12-10 RS RS20160733A patent/RS55144B1/sr unknown
- 2012-12-10 PT PT127987386T patent/PT2791140T/pt unknown
- 2012-12-10 EA EA201400707A patent/EA029556B1/ru not_active IP Right Cessation
- 2012-12-10 DK DK12798738.6T patent/DK2791140T3/en active
- 2012-12-10 US US14/365,424 patent/US20140336173A1/en not_active Abandoned
- 2012-12-10 SG SG11201402325QA patent/SG11201402325QA/en unknown
- 2012-12-10 PE PE2014000926A patent/PE20141855A1/es active IP Right Grant
- 2012-12-10 MY MYPI2014701550A patent/MY178660A/en unknown
- 2012-12-10 KR KR1020147019406A patent/KR102057444B1/ko not_active Expired - Fee Related
- 2012-12-10 SI SI201230702A patent/SI2791140T1/sl unknown
- 2012-12-12 JO JOP/2012/0377A patent/JO3295B1/ar active
- 2012-12-12 AR ARP120104679A patent/AR089207A1/es active Pending
- 2012-12-14 TW TW101147336A patent/TWI567076B/zh not_active IP Right Cessation
- 2012-12-14 US US13/715,553 patent/US9206184B2/en active Active
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2014
- 2014-05-14 IL IL232611A patent/IL232611A/en active IP Right Grant
- 2014-06-09 CO CO14123802A patent/CO7030961A2/es unknown
- 2014-06-09 CU CUP2014000065A patent/CU20140065A7/es unknown
- 2014-06-10 DO DO2014000127A patent/DOP2014000127A/es unknown
- 2014-06-11 TN TNP2014000255A patent/TN2014000255A1/en unknown
- 2014-06-12 EC ECIEPI20144722A patent/ECSP14004722A/es unknown
- 2014-06-12 CL CL2014001547A patent/CL2014001547A1/es unknown
- 2014-06-13 GT GT201400113A patent/GT201400113A/es unknown
- 2014-06-13 PH PH12014501355A patent/PH12014501355A1/en unknown
- 2014-06-17 CR CR20140288A patent/CR20140288A/es unknown
- 2014-07-14 ZA ZA2014/05140A patent/ZA201405140B/en unknown
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2015
- 2015-06-22 HK HK15105900.1A patent/HK1205123A1/xx not_active IP Right Cessation
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2016
- 2016-08-31 CY CY20161100853T patent/CY1118112T1/el unknown
- 2016-09-02 HR HRP20161130TT patent/HRP20161130T1/hr unknown
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2017
- 2017-07-17 AU AU2017206140A patent/AU2017206140A1/en not_active Abandoned
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2018
- 2018-02-20 US US15/900,725 patent/US20190016724A1/en not_active Abandoned
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2019
- 2019-06-18 AU AU2019204255A patent/AU2019204255A1/en not_active Abandoned
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2021
- 2021-11-01 US US17/516,542 patent/US20220153745A1/en not_active Abandoned
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