EA201290720A1 - Двузамещенные производные пиридина в качестве противораковых средств - Google Patents
Двузамещенные производные пиридина в качестве противораковых средствInfo
- Publication number
- EA201290720A1 EA201290720A1 EA201290720A EA201290720A EA201290720A1 EA 201290720 A1 EA201290720 A1 EA 201290720A1 EA 201290720 A EA201290720 A EA 201290720A EA 201290720 A EA201290720 A EA 201290720A EA 201290720 A1 EA201290720 A1 EA 201290720A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- phenylene
- lower alkylene
- facilities
- cancer
- double
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/62—Oxygen or sulfur atoms
- C07D213/69—Two or more oxygen atoms
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Abstract
Настоящее изобретение относится к новому соединению, имеющему превосходный противоопухолевый эффект. Соединение согласно настоящему изобретению представлено следующей общей формулой (1)в которой Rи Rобозначают арил или подобное; А обозначает низший алкилен; кольцо Х обозначает в случае необходимости замещенный арилен; Е обозначает связь или низший алкенилен; кольцо Y обозначает в случае необходимости замещенный гетероциклоалкилен, содержащий один или более атомов азота, один из которых присоединен к смежной карбонильной группе; G обозначает -NH-G-, -N(низший алкил)-G-, -NH-CH-G-, -N(низший алкил)-CH-G- или -CH-G- [причем Gсвязывается с R, G-Rобозначает связь-R, фенилен-G-R, фенилен-G-O-R, фенилен-G-NH-R, фенилен-G-N(низший алкил)-Rили хинолиндиил-O-R, причем фенилен указанных фениленсодержащих групп может быть замещен одним или более заместителями; С-Rобозначает -O-низший алкилен-Rили подобное; G-O- обозначает низший алкилен -О- или подобное; Gобозначает низший алкилен; Gобозначает низший алкилен].
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US29963110P | 2010-01-29 | 2010-01-29 | |
| US35972910P | 2010-06-29 | 2010-06-29 | |
| PCT/JP2011/052302 WO2011093524A1 (en) | 2010-01-29 | 2011-01-28 | Di - substituted pyridine derivatives as anticancers |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201290720A1 true EA201290720A1 (ru) | 2013-02-28 |
| EA026042B1 EA026042B1 (ru) | 2017-02-28 |
Family
ID=43797869
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201290720A EA026042B1 (ru) | 2010-01-29 | 2011-01-28 | Двузамещенные производные пиридина в качестве противораковых средств |
Country Status (27)
| Country | Link |
|---|---|
| US (1) | US8722663B2 (ru) |
| EP (1) | EP2528897B9 (ru) |
| JP (1) | JP5335932B2 (ru) |
| KR (1) | KR101411030B1 (ru) |
| CN (1) | CN102791690B (ru) |
| AR (1) | AR080057A1 (ru) |
| AU (1) | AU2011211306B2 (ru) |
| CA (1) | CA2788073A1 (ru) |
| CO (1) | CO6561817A2 (ru) |
| DK (1) | DK2528897T3 (ru) |
| EA (1) | EA026042B1 (ru) |
| ES (1) | ES2521016T3 (ru) |
| HK (1) | HK1178523A1 (ru) |
| HR (1) | HRP20141190T1 (ru) |
| IL (1) | IL221146A (ru) |
| MX (1) | MX2012008391A (ru) |
| MY (1) | MY160875A (ru) |
| NZ (1) | NZ601794A (ru) |
| PL (1) | PL2528897T3 (ru) |
| PT (1) | PT2528897E (ru) |
| RS (1) | RS53705B1 (ru) |
| SG (1) | SG182663A1 (ru) |
| SI (1) | SI2528897T1 (ru) |
| SM (1) | SMT201500007B (ru) |
| TW (1) | TWI404713B (ru) |
| UA (1) | UA107692C2 (ru) |
| WO (1) | WO2011093524A1 (ru) |
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2013047223A (ja) * | 2011-07-28 | 2013-03-07 | Otsuka Pharmaceut Co Ltd | 医薬 |
| KR102334260B1 (ko) | 2013-03-14 | 2021-12-02 | 스미토모 다이니폰 파마 온콜로지, 인크. | Ｊａｋ2 및 ａｌｋ2 억제제 및 이들의 사용 방법 |
| US9227978B2 (en) | 2013-03-15 | 2016-01-05 | Araxes Pharma Llc | Covalent inhibitors of Kras G12C |
| US9745319B2 (en) | 2013-03-15 | 2017-08-29 | Araxes Pharma Llc | Irreversible covalent inhibitors of the GTPase K-Ras G12C |
| EP3816155A1 (en) * | 2013-08-23 | 2021-05-05 | Virginia Commonwealth University | Ester nitrates derivatives of aromatic aldehydes with multiple pharmalogic properties to treat sickle cell disease |
| TWI659021B (zh) | 2013-10-10 | 2019-05-11 | 亞瑞克西斯製藥公司 | Ｋｒａｓ ｇ１２ｃ之抑制劑 |
| JO3556B1 (ar) | 2014-09-18 | 2020-07-05 | Araxes Pharma Llc | علاجات مدمجة لمعالجة السرطان |
| AR102094A1 (es) * | 2014-09-25 | 2017-02-01 | Araxes Pharma Llc | Inhibidores de proteínas kras con una mutación g12c |
| WO2016049568A1 (en) | 2014-09-25 | 2016-03-31 | Araxes Pharma Llc | Methods and compositions for inhibition of ras |
| ES2898765T3 (es) | 2015-04-10 | 2022-03-08 | Araxes Pharma Llc | Compuestos de quinazolina sustituidos y métodos de uso de los mismos |
| EP3283462B1 (en) | 2015-04-15 | 2020-12-02 | Araxes Pharma LLC | Fused-tricyclic inhibitors of kras and methods of use thereof |
| US10144724B2 (en) | 2015-07-22 | 2018-12-04 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
| US10875842B2 (en) | 2015-09-28 | 2020-12-29 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| WO2017058768A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| US10858343B2 (en) | 2015-09-28 | 2020-12-08 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| WO2017058915A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| WO2017058805A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| US10882847B2 (en) | 2015-09-28 | 2021-01-05 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| WO2017058902A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| JP2018533939A (ja) | 2015-10-19 | 2018-11-22 | アラクセス ファーマ エルエルシー | Ｒａｓの阻害剤をスクリーニングするための方法 |
| EA038635B9 (ru) | 2015-11-16 | 2021-10-26 | Араксис Фарма Ллк | 2-замещенные соединения хиназолина, содержащие замещенную гетероциклическую группу, и способы их применения |
| US9988357B2 (en) | 2015-12-09 | 2018-06-05 | Araxes Pharma Llc | Methods for preparation of quinazoline derivatives |
| WO2017172979A1 (en) | 2016-03-30 | 2017-10-05 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use |
| US10646488B2 (en) | 2016-07-13 | 2020-05-12 | Araxes Pharma Llc | Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof |
| CN110036010A (zh) | 2016-09-29 | 2019-07-19 | 亚瑞克西斯制药公司 | Kras g12c突变蛋白的抑制剂 |
| EP3523289A1 (en) | 2016-10-07 | 2019-08-14 | Araxes Pharma LLC | Heterocyclic compounds as inhibitors of ras and methods of use thereof |
| EP3573954A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | Fused bicyclic benzoheteroaromatic compounds and methods of use thereof |
| EP3573970A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | 1-(6-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)azetidin-1-yl)prop-2-en-1-one derivatives and similar compounds as kras g12c inhibitors for the treatment of cancer |
| EP3573971A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer |
| WO2018140600A1 (en) | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | Fused hetero-hetero bicyclic compounds and methods of use thereof |
| US11358959B2 (en) | 2017-01-26 | 2022-06-14 | Araxes Pharma Llc | Benzothiophene and benzothiazole compounds and methods of use thereof |
| EP3630746A1 (en) | 2017-05-25 | 2020-04-08 | Araxes Pharma LLC | Compounds and methods of use thereof for treatment of cancer |
| WO2018218069A1 (en) | 2017-05-25 | 2018-11-29 | Araxes Pharma Llc | Quinazoline derivatives as modulators of mutant kras, hras or nras |
| TW201900633A (zh) | 2017-05-25 | 2019-01-01 | 美商亞瑞克西斯製藥公司 | Kras之共價抑制劑 |
| BR112020020246A8 (pt) | 2018-04-05 | 2022-10-18 | Sumitomo Dainippon Pharma Oncology Inc | Inibidores de cinase axl e uso dos mesmos |
| KR20210038906A (ko) | 2018-07-26 | 2021-04-08 | 스미토모 다이니폰 파마 온콜로지, 인크. | 비정상적 acvr1 발현과 연관된 질환을 치료하는 방법 및 그에 사용하기 위한 acvr1 억제제 |
| CN112812781B (zh) * | 2021-01-21 | 2023-09-29 | 西安瑞联新材料股份有限公司 | 一种基于双哌嗪类苯并噁唑液晶化合物及其制备方法 |
| CN116903587B (zh) * | 2023-06-01 | 2024-03-22 | 三峡大学 | 一种角鲨烯环氧酶抑制剂及其用途 |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| JPS63301880A (ja) * | 1985-09-03 | 1988-12-08 | Otsuka Pharmaceut Co Ltd | ５−フルオロウラシル誘導体 |
| AR015733A1 (es) * | 1998-03-25 | 2001-05-16 | Otsuka Pharma Co Ltd | DERIVADO DE PIRIDINA, EL PRODUCTO Y LA COMPOSICIoN FARMACEUTICA QUE CONTIENE DICHO DERIVADO. |
| US6262088B1 (en) * | 1998-11-19 | 2001-07-17 | Berlex Laboratories, Inc. | Polyhydroxylated monocyclic N-heterocyclic derivatives as anti-coagulants |
| JP2001089450A (ja) * | 1999-09-22 | 2001-04-03 | Otsuka Pharmaceut Co Ltd | ピリジン誘導体含有医薬製剤 |
| JP2001089412A (ja) * | 1999-09-22 | 2001-04-03 | Otsuka Pharmaceut Co Ltd | ベンゼン誘導体またはその医薬的に許容される塩 |
| JP2002226429A (ja) * | 2001-02-06 | 2002-08-14 | Fuji Photo Film Co Ltd | アクリル酸エステル化合物の製造方法 |
| GB0224917D0 (en) * | 2002-10-25 | 2002-12-04 | Novartis Ag | Organic compounds |
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| DE202009007345U1 (de) * | 2009-05-22 | 2009-09-10 | Schebo (R) . Biotech Ag | Neue Pharmazeutika und Arzneimittelzubereitungen |
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2011
- 2011-01-28 MY MYPI2012003367A patent/MY160875A/en unknown
- 2011-01-28 NZ NZ601794A patent/NZ601794A/en not_active IP Right Cessation
- 2011-01-28 CA CA2788073A patent/CA2788073A1/en not_active Abandoned
- 2011-01-28 WO PCT/JP2011/052302 patent/WO2011093524A1/en active Application Filing
- 2011-01-28 US US13/318,053 patent/US8722663B2/en not_active Expired - Fee Related
- 2011-01-28 EA EA201290720A patent/EA026042B1/ru not_active IP Right Cessation
- 2011-01-28 UA UAA201209216A patent/UA107692C2/ru unknown
- 2011-01-28 KR KR1020117025212A patent/KR101411030B1/ko not_active IP Right Cessation
- 2011-01-28 AU AU2011211306A patent/AU2011211306B2/en not_active Ceased
- 2011-01-28 DK DK11705048.4T patent/DK2528897T3/en active
- 2011-01-28 PT PT117050484T patent/PT2528897E/pt unknown
- 2011-01-28 SI SI201130359T patent/SI2528897T1/sl unknown
- 2011-01-28 RS RS20140688A patent/RS53705B1/en unknown
- 2011-01-28 CN CN201180007162.2A patent/CN102791690B/zh not_active Expired - Fee Related
- 2011-01-28 JP JP2011545133A patent/JP5335932B2/ja not_active Expired - Fee Related
- 2011-01-28 ES ES11705048.4T patent/ES2521016T3/es active Active
- 2011-01-28 SG SG2012054243A patent/SG182663A1/en unknown
- 2011-01-28 EP EP11705048.4A patent/EP2528897B9/en active Active
- 2011-01-28 TW TW100103410A patent/TWI404713B/zh not_active IP Right Cessation
- 2011-01-28 PL PL11705048T patent/PL2528897T3/pl unknown
- 2011-01-28 AR ARP110100297A patent/AR080057A1/es unknown
- 2011-01-28 MX MX2012008391A patent/MX2012008391A/es active IP Right Grant
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2012
- 2012-07-19 CO CO12121461A patent/CO6561817A2/es unknown
- 2012-07-26 IL IL221146A patent/IL221146A/en not_active IP Right Cessation
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2013
- 2013-05-06 HK HK13105398.2A patent/HK1178523A1/xx not_active IP Right Cessation
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2014
- 2014-12-09 HR HRP20141190AT patent/HRP20141190T1/hr unknown
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2015
- 2015-01-09 SM SM201500007T patent/SMT201500007B/xx unknown
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| Date | Code | Title | Description |
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| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ BY KZ KG MD TJ TM RU |