JPWO2018049861A5 - - Google Patents
Download PDFInfo
- Publication number
- JPWO2018049861A5 JPWO2018049861A5 JP2019515307A JP2019515307A JPWO2018049861A5 JP WO2018049861 A5 JPWO2018049861 A5 JP WO2018049861A5 JP 2019515307 A JP2019515307 A JP 2019515307A JP 2019515307 A JP2019515307 A JP 2019515307A JP WO2018049861 A5 JPWO2018049861 A5 JP WO2018049861A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- pharmaceutically acceptable
- cancer
- acceptable salt
- hydrogen
- 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.)
- Pending
Links
- 150000001875 compounds Chemical class 0.000 claims description 13
- 150000001335 aliphatic alkanes Chemical class 0.000 claims description 9
- 229910052739 hydrogen Inorganic materials 0.000 claims description 9
- 239000001257 hydrogen Substances 0.000 claims description 9
- 150000001924 cycloalkanes Chemical group 0.000 claims description 8
- 150000002431 hydrogen Chemical group 0.000 claims description 7
- 229910052736 halogen Inorganic materials 0.000 claims description 6
- 150000002367 halogens Chemical class 0.000 claims description 6
- 150000003839 salts Chemical class 0.000 claims description 6
- 125000003545 alkoxy group Chemical group 0.000 claims description 4
- 238000004519 manufacturing process Methods 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 102100033177 Vascular endothelial growth factor receptor 2 Human genes 0.000 claims 2
- 239000002260 anti-inflammatory agent Substances 0.000 claims 2
- 229940124599 anti-inflammatory drug Drugs 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 229940121358 tyrosine kinase inhibitor Drugs 0.000 claims 2
- 239000005483 tyrosine kinase inhibitor Substances 0.000 claims 2
- 150000004917 tyrosine kinase inhibitor derivatives Chemical class 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 102100021435 Macrophage-stimulating protein receptor Human genes 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 claims 1
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 108091008605 VEGF receptors Proteins 0.000 claims 1
- 239000012830 cancer therapeutic Substances 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 208000029824 high grade glioma Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 201000011614 malignant glioma Diseases 0.000 claims 1
- 102000009076 src-Family Kinases Human genes 0.000 claims 1
- 108010087686 src-Family Kinases Proteins 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 3
- 150000001336 alkenes Chemical group 0.000 description 2
- 125000002355 alkine group Chemical group 0.000 description 2
- 125000000000 cycloalkoxy group Chemical group 0.000 description 2
- 125000004414 alkyl thio group Chemical group 0.000 description 1
- 150000002576 ketones Chemical class 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 229910052717 sulfur Inorganic materials 0.000 description 1
- 125000003396 thiol group Chemical group [H]S* 0.000 description 1
Description
上記のような技術的課題を解決するために、本発明は、下記のような技術的解決手段によって実現される。
本発明の一態様において、一般式（Ｉ）を有する化合物またはその薬学的に許容可能な塩を提供する。
In order to solve the above technical problems, the present invention is realized by the following technical solutions.
In one aspect of the invention, a compound having general formula (I) or a pharmaceutically acceptable salt thereof is provided.
前記式で、
Ｋは： シクロアルカン基
ハロゲン化アルカン基
またはＮ－Ｒ６のラジカルから選択され、前記ｂ、ｄは、数字１、２、３または４であり、Ｅ、Ｇは、水素、ハロゲン、ヒドロキシ基、アルコキシ基、ケトン、メルカプト基、アルキルメルカプト基中の１つであるが、Ｅ、Ｇが異なる場合、水素であり、Ｒ６は、水素、低級ハロゲン化アルカン基、低級ハロゲン化シクロアルカン基、低級アルカン基、低級シクロアルカン基中の１つである。
In the above formula,
K is: cycloalkane group
halogenated alkane group
or NR6 radical, b and d are numbers 1, 2, 3 or 4, and E and G are hydrogen, halogen, hydroxy group, alkoxy group, ketone, mercapto group, alkylmercapto group If E and G are different, it is hydrogen, and R6 is one of hydrogen, a lower halogenated alkane group, a lower halogenated cycloalkane group, a lower alkane group, a lower cycloalkane group. be.
Ｒ１、Ｒ２、Ｒ３、Ｒ４、Ｒ５は、それぞれ水素、ハロゲン、低級ハロゲン化アルカン基、低級ハロゲン化シクロアルカン基、低級アルカン基、低級シクロアルカン基、ヒドロキシ基、低級アルコキシ基、低級シクロアルコキシ基、低級オレフィン基、低級アルキン基中の１つまたは複数である。 R1, R2, R3, R4, and R5 are hydrogen, halogen, lower halogenated alkane group, lower halogenated cycloalkane group, lower alkane group, lower cycloalkane group, hydroxy group, lower alkoxy group, lower cycloalkoxy group, One or more of lower olefin groups and lower alkyne groups.
Ｘは、Ｃ－Ｒ、Ｃ－（ＣＮ）、Ｎ中の１つであり、前記Ｒは水素、ハロゲン、低級ハロゲン化アルカン基、低級ハロゲン化シクロアルカン基、低級アルカン基、低級シクロアルカン基、ヒドロキシ基、低級アルコキシ基、低級シクロアルコキシ、低級オレフィン基、低級アルキン基中の１つであり、
Ｙは、Ｏ、Ｓ、Ｎ－Ｒ６中の１つまたは空であり、Ｍは、Ｏまたは空であり、
ａ、ｃは、それぞれ数字０、１、２、または３であり、ｅは、数字１または２である。
X is one of CR, C-(CN), and N, and the R is hydrogen, halogen, lower halogenated alkane group, lower halogenated cycloalkane group, lower alkane group, lower cycloalkane group, One of hydroxy group, lower alkoxy group, lower cycloalkoxy, lower olefin group, lower alkyne group,
Y is one of O, S, NR6 or empty, M is O or empty,
a, c are the numbers 0, 1, 2, or 3, respectively, and e is the number 1 or 2.
好ましくは、前記Ｅ及びＧのうちの少なくとも１つは、ハロゲンＦである。 Preferably, at least one of E and G is halogen F.
好ましくは、前記Ｙは、Ｏまたは空である。 Preferably, said Y is O or empty.
好ましくは、前記一般式（Ｉ）化合物は、下記の具体的な構造の化合物を含む。 Preferably, the compound of general formula (I) includes a compound having the following specific structure.
Claims (12)
前記式で、
Ｋは、
ハロゲン化アルカン基（ｈａｌｏｇｅｎａｔｅｄ ａｌｋａｎｅ ｇｒｏｕｐ）である
、またはＮ－Ｒ６のラジカルから選択され、
ここで、前記シクロアルカン基、前記ハロゲン化アルカン基を表す部分構造式において、前記ｂ、ｄは、数字１、または２であり、Ｅ、Ｇは、水素、またはハロゲン（ｈａｌｏｇｅｎ）であり、前記Ｎ－Ｒ６におけるＲ６は、水素であり、
Ｒ１、Ｒ２、Ｒ５は、それぞれ水素、またはハロゲンであり、Ｒ３は水素であり、Ｒ４は低級アルコキシ基であり、
Ｘは、Ｃ－Ｈであり、
Ｙは、Ｏ、または空であり、Ｍは、Ｏまたは空であり、
ａ、ｃは、それぞれ数字０、１、２、または３であり、ｅは、数字１または２である、前記一般式（Ｉ）を有する化合物またはその薬学的に許容可能な塩。 A compound having general formula (I) or a pharmaceutically acceptable salt thereof,
In the above formula,
K is
is a halogenated alkane group
, or a radical of NR6,
Here, in the partial structural formula representing the cycloalkane group or the halogenated alkane group, b and d are numbers 1 or 2, E and G are hydrogen or halogen, and R6 in NR6 is hydrogen,
R1, R2, R5 are each hydrogen or halogen, R3 is hydrogen, R4 is a lower alkoxy group,
X is CH;
Y is O or empty, M is O or empty,
A compound having the general formula (I) or a pharmaceutically acceptable salt thereof, wherein a and c are each a number 0, 1, 2, or 3, and e is a number 1 or 2.
化合物またはその薬学的に許容可能な塩。 characterized by being either
A compound or a pharmaceutically acceptable salt thereof .
化合物またはその薬学的に許容可能な塩。 characterized by being either
A compound or a pharmaceutically acceptable salt thereof .
であることを特徴とする
請求項１に記載の化合物またはその薬学的に許容可能な塩。 The compound of the general formula (I) is
The compound according to claim 1 or a pharmaceutically acceptable salt thereof .
請求項６に記載のチロシンキナーゼ阻害剤。 The tyrosine kinase inhibitor according to claim 6, wherein the tyrosine kinase includes C-MET, VEGFR, KDR, RON, KIT, PDGF, FGF, and SRC kinase.
請求項８に記載の使用。 The use according to claim 8, wherein the cancer includes lung cancer, gastric cancer, ovarian cancer, colon cancer , and malignant glioma.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610822529.0A CN107235896B (en) | 2016-09-13 | 2016-09-13 | Tyrosine kinase inhibitor and its application |
| CN201610822529.0 | 2016-09-13 | ||
| PCT/CN2017/089501 WO2018049861A1 (en) | 2016-09-13 | 2017-06-22 | Tyrosine kinase inhibitor and application thereof |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2019529435A JP2019529435A (en) | 2019-10-17 |
| JP2019529435A5 JP2019529435A5 (en) | 2020-11-12 |
| JPWO2018049861A5 true JPWO2018049861A5 (en) | 2024-03-06 |
| JP7487921B2 JP7487921B2 (en) | 2024-05-21 |
Family
ID=59982910
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019515307A Active JP7487921B2 (en) | 2016-09-13 | 2017-06-22 | Tyrosine kinase inhibitors and their applications |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US10882853B2 (en) |
| EP (1) | EP3511327B1 (en) |
| JP (1) | JP7487921B2 (en) |
| KR (2) | KR102382039B1 (en) |
| CN (2) | CN107235896B (en) |
| AU (1) | AU2017325641B2 (en) |
| ES (1) | ES2902549T3 (en) |
| WO (1) | WO2018049861A1 (en) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11427578B1 (en) | 2017-07-18 | 2022-08-30 | Bayer Pharma Aktiengesellschaft | Substituted pyrrolopyridine-derivatives |
| JP7307733B2 (en) | 2018-01-26 | 2023-07-12 | エグゼリクシス， インコーポレイテッド | Compounds for treating kinase dependent disorders |
| AU2019212800B2 (en) | 2018-01-26 | 2024-05-23 | Exelixis, Inc. | Compounds for the treatment of kinase-dependent disorders |
| CR20200358A (en) * | 2018-01-26 | 2021-02-22 | Exelixis Inc | Compounds for the treatment of kinase-dependent disorders |
| AR119069A1 (en) * | 2019-06-04 | 2021-11-24 | Exelixis Inc | COMPOUNDS FOR THE TREATMENT OF KINASE-DEPENDENT DISORDERS |
| CN112358469A (en) * | 2020-03-18 | 2021-02-12 | 北京康辰药业股份有限公司 | Angiogenesis inhibitor, preparation method and application thereof |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI2213661T1 (en) * | 2003-09-26 | 2011-11-30 | Exelixis Inc | c-Met Modulators and Methods of Use |
| UY31800A (en) * | 2008-05-05 | 2009-11-10 | Smithkline Beckman Corp | CANCER TREATMENT METHOD USING A CMET AND AXL INHIBITOR AND AN ERBB INHIBITOR |
| KR20110075016A (en) * | 2008-10-14 | 2011-07-05 | 닝 시 | Compounds and methods of use |
| EP2408300B1 (en) * | 2009-03-21 | 2016-05-11 | Sunshine Lake Pharma Co., Ltd. | Amino ester derivatives, salts thereof and methods of use |
| US8664244B2 (en) | 2010-09-12 | 2014-03-04 | Advenchen Pharmaceuticals, LLC | Compounds as c-Met kinase inhibitors |
| CN105884695B (en) * | 2015-02-13 | 2019-02-26 | 山东轩竹医药科技有限公司 | Heterocyclic derivatives species tyrosine kinase inhibitor |
| CN104817497B (en) * | 2015-03-20 | 2017-03-08 | 南京众睿缘生物科技有限公司 | A kind of alkynes is for quinoline and its production and use |
| CN105017163A (en) * | 2015-08-25 | 2015-11-04 | 佛山市赛维斯医药科技有限公司 | Bis(ethoxy) benzo quinazoline tyrosine kinase inhibitor as well as preparation method and application thereof |
| CN105001168A (en) * | 2015-08-25 | 2015-10-28 | 佛山市赛维斯医药科技有限公司 | Tri-alkoxy-substituted benzo quinazoline type tyrosine kinase inhibitor and application thereof |
| CN105085416A (en) * | 2015-08-25 | 2015-11-25 | 佛山市赛维斯医药科技有限公司 | Nitro-substituted bisalcoxylbenzoquinazoline tyrosine kinase inhibitor and application |
| CN105218445B (en) * | 2015-08-25 | 2018-05-22 | 江苏中邦制药有限公司 | A kind of preparation method of tyrosine kinase inhibitor Foretinib |
-
2016
- 2016-09-13 CN CN201610822529.0A patent/CN107235896B/en active Active
- 2016-09-13 CN CN201910822704.XA patent/CN110437145A/en active Pending
-
2017
- 2017-06-22 JP JP2019515307A patent/JP7487921B2/en active Active
- 2017-06-22 AU AU2017325641A patent/AU2017325641B2/en active Active
- 2017-06-22 ES ES17850066T patent/ES2902549T3/en active Active
- 2017-06-22 EP EP17850066.6A patent/EP3511327B1/en active Active
- 2017-06-22 KR KR1020217037589A patent/KR102382039B1/en active IP Right Grant
- 2017-06-22 KR KR1020197010451A patent/KR20190045354A/en active Application Filing
- 2017-06-22 US US16/333,050 patent/US10882853B2/en active Active
- 2017-06-22 WO PCT/CN2017/089501 patent/WO2018049861A1/en unknown
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| TWI520950B (en) | Crystalline form of an inhibitor of mdm2/4 and p53 interaction | |
| JP2020007311A5 (en) | ||
| EP2678336B1 (en) | Thiazolylphenyl-benzenesulfonamido derivatives as kinase inhibitors | |
| JP5852678B2 (en) | Antitumor agent effect enhancer | |
| CN103153980B (en) | The derivative of pyrazolo phenyl benzenesulfonamides compound and the purposes as antitumour drug thereof | |
| Nowak‐Sliwinska et al. | Angiostatic kinase inhibitors to sustain photodynamic angio‐occlusion | |
| JP2007511504A5 (en) | ||
| JP2005536526A (en) | Bicyclo-pyrazoles active as kinase inhibitors, process for producing the same, and pharmaceutical compositions containing the same | |
| JP2019529435A5 (en) | ||
| EP1427708A1 (en) | Amino-phthalazinone derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions containing them | |
| CN107406438A (en) | The inhibitor of bromine domain | |
| CN111051300B (en) | Novel heteroaryl amide derivatives as selective inhibitors of histone deacetylase 1 and/or 2 (HDAC 1-2) | |
| JP2009537546A5 (en) | ||
| WO2014171464A1 (en) | Novel use for pai-1 inhibitor | |
| JPWO2018049861A5 (en) | ||
| US20040010027A1 (en) | Hydroxphenyl-pyrazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical comositions comprising them | |
| JPWO2019195124A5 (en) | ||
| WO2018136935A1 (en) | 2-arylsulfonamido-n-arylacetamide derivatized stat3 inhibitors | |
| JP2019520344A5 (en) | ||
| CN109928972A (en) | A kind of matrine derivative and its application in drug | |
| JP2004502755A5 (en) | ||
| JP2020111571A5 (en) | ||
| TWI225062B (en) | Pentacyclic taxan compound | |
| CN103159674A (en) | 2-benzene alkyl amid compound and preparation method, medical composition and use thereof | |
| DK2930167T3 (en) | INDOLINO DERIVATIVE AS A TYROSINKINASE INHIBITOR |