RS54850B1 - Novi tienopirimidin derivati, procesi za pripremu istih i terapijska korišćenja toga - Google Patents
Novi tienopirimidin derivati, procesi za pripremu istih i terapijska korišćenja togaInfo
- Publication number
- RS54850B1 RS54850B1 RS20160436A RSP20160436A RS54850B1 RS 54850 B1 RS54850 B1 RS 54850B1 RS 20160436 A RS20160436 A RS 20160436A RS P20160436 A RSP20160436 A RS P20160436A RS 54850 B1 RS54850 B1 RS 54850B1
- Authority
- RS
- Serbia
- Prior art keywords
- group
- alkyl
- heterocycloalkyl
- hydrogen atom
- independently
- Prior art date
Links
Classifications
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- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
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- 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
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Professional, Industrial, Or Sporting Protective Garments (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Jedinjenje sa formulom (I):naznačeno time što:R6 je -CONH2 ili -C(Ra)(Rp)(OH) grupa u kojoj Ra i Rp su, nezavisno jedanod drugoga, atom vodonika ili (C1-C6) alkil grupa ili zajedno grade, sa atomom ugljenika koji ih nosi, 3- do 5-člani karbocikal;R je fenil ili heteroaril grupa supstituisana sa R1, R'1, R2 i R3;R1 je atom vodonika ili je odabran iz sledećih grupa: (C1-C6)alkil, (C1-C6)alkoksi, (C3-C7)cikloalkil i aril, pomenute grupe su po izboru supstituisane sa jednim ili više supstituenata koji su izabrani, svaki puta nezavisno, od:amino, hidroksila, tiola, halogena, (C1-C6)alkil, (C1-C6)alkoksi, (C1-C6)alkiltio, (C1-C6)alkilamino, ariloksi, aril(C1-C6)alkoksi, cijano, halo(C1-C6)alkil, karboksila i karboksi(C1-C6)alkil;R'1 je atom vodonika ili (C1-C6)alkoksi grupa;R2 je odabran od:- atoma vodonika, atoma halogena, ili (C1-C6)alkil, (C3-C7)cikloalkil ili (C1-C6)alkoksi grupa;- heterocikloalkil, heterocikloalkil-CH2- ili heteroaril grupe;gde svaka navedena heterocikloalkil, heterocikloalkil-CH2- i heteroaril grupaje po izboru supstituisana sa jednim ili više supstituenata koji su izabrani,svaki puta nezavisno, od: (C1-C6)alkil, (C3-C7)cikloalkil, (C1-C6)alkoksi, heterocikloalkila, karboksi(C1-C6)alkil, NR4R5 i OR4;navedena (C1-C6)alkil grupa je po izboru supstituisana sa atomom halogena ili (C1-C6)alkoksi, heterocikloalkil, NH2 ili OH grupom; iR4 i R5 su svaki, nezavisno jedan od drugoga, atom vodonika, (C1-C6)alkil grupa ili heterocikloalkil grupa;ili pored toga R4 i R5 zajedno grade, sa atomom azota koji ih nosi, 4- do 7-člani prsten;- grupe NRaRb, gde su Ra i Rb, nezavisno jedan od drugoga: atom vodonika; heterocikloalkil grupa, navedena heterocikloalkil grupa je po izboru supstituisana sa grupom (C1-C6)alkil; ili (C1-C6)alkil grupa, navedena alkil grupa je po izboru supstituisana sa grupom NR4R5;R4 i R5 su svaki, nezavisno jedan od drugoga, atom vodonika, (C1-C6)alkil grupa ili heterocikloalkil grupa;ili pored toga R4 i R5 zajedno grade, sa atomom azota koji ih nosi, 4- do 7-člani prsten;R3 je atom vodonika, atom halogena ili (C1-C6)alkil grupa; gde kada R je fenilna grupa, dva susedna supstituenta na fenilnoj grupi mogu zajedno graditi heterocikloalkilni prsten kondenzovan sa fenilom koji ih nosi, navedeni heterocikloalkil je po izboru supstituisan sajednim ili više supstituenata koji su izabrani, svaki puta nezavisno, od: okso grupe i (C1-C6)alkil grupe;R7 je aril grupa ili heteroaril grupa, ova grupa je po izboru supstituisana sa jednim ili više supstituenata koji su izabrani, svaki puta nezavisno, od: cijano, halogena, (C1-C6)alkila, OR'4, CH2OH, CH2NH2, S(0)nR4, R8 i OR8; gde:R'4 je atom vodonika ili (C1-C6)alkil ili aril grupa, pomenute alkil i aril grupe su po izboru supstituisane sa atomom halogena ili NH2 ili OH grupom;n je 1 ili 2; iR8 je halo(C1-C6)alkil grupa;gde svaki od atoma azota za jedinjenja sa formulom (I) može biti, nezavisno jedan od drugoga, po izboru u oksidovanom obliku (N-oksid);ili njegova farmaceutski prihvatljiva so.Prijava sadrži još 20 patentnih zahteva.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR1253044A FR2988722B1 (fr) | 2012-04-03 | 2012-04-03 | Nouveaux derives de thienopyrimidines, leurs procedes de preparation et leurs utilisations therapeutiques |
| EP13716241.8A EP2834248B1 (en) | 2012-04-03 | 2013-04-02 | Novel thienopyrimidine derivatives, processes for the preparation thereof and therapeutic uses thereof |
| PCT/EP2013/056958 WO2013150036A1 (en) | 2012-04-03 | 2013-04-02 | Novel thienopyrimidine derivatives, processes for the preparation thereof and therapeutic uses thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RS54850B1 true RS54850B1 (sr) | 2016-10-31 |
Family
ID=48095815
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RS20160436A RS54850B1 (sr) | 2012-04-03 | 2013-04-02 | Novi tienopirimidin derivati, procesi za pripremu istih i terapijska korišćenja toga |
Country Status (38)
| Country | Link |
|---|---|
| US (6) | US9115140B2 (sr) |
| EP (1) | EP2834248B1 (sr) |
| JP (1) | JP6096278B2 (sr) |
| KR (1) | KR102039764B1 (sr) |
| CN (2) | CN107652303B (sr) |
| AR (1) | AR090572A1 (sr) |
| AU (1) | AU2013244992B2 (sr) |
| BR (1) | BR112014024489B1 (sr) |
| CA (1) | CA2868685C (sr) |
| CL (1) | CL2014002661A1 (sr) |
| CO (1) | CO7091179A2 (sr) |
| CR (1) | CR20140435A (sr) |
| CY (1) | CY1117843T1 (sr) |
| DK (1) | DK2834248T3 (sr) |
| DO (1) | DOP2014000216A (sr) |
| EA (1) | EA025558B1 (sr) |
| ES (1) | ES2577382T3 (sr) |
| FR (1) | FR2988722B1 (sr) |
| HK (2) | HK1201263A1 (sr) |
| HR (1) | HRP20160649T1 (sr) |
| HU (1) | HUE027895T2 (sr) |
| IL (1) | IL234960A (sr) |
| MA (1) | MA37384B1 (sr) |
| MX (1) | MX355104B (sr) |
| MY (1) | MY166151A (sr) |
| PE (1) | PE20150289A1 (sr) |
| PH (1) | PH12014502180B1 (sr) |
| PL (1) | PL2834248T3 (sr) |
| PT (1) | PT2834248E (sr) |
| RS (1) | RS54850B1 (sr) |
| SG (1) | SG11201406091RA (sr) |
| SI (1) | SI2834248T1 (sr) |
| TN (1) | TN2014000415A1 (sr) |
| TW (1) | TWI579288B (sr) |
| UA (1) | UA112685C2 (sr) |
| UY (1) | UY34725A (sr) |
| WO (1) | WO2013150036A1 (sr) |
| ZA (1) | ZA201407021B (sr) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2988722B1 (fr) | 2012-04-03 | 2014-05-09 | Sanofi Sa | Nouveaux derives de thienopyrimidines, leurs procedes de preparation et leurs utilisations therapeutiques |
| US10087195B2 (en) * | 2014-05-28 | 2018-10-02 | Shanghai Fochon Pharmaceutical Co., Ltd. | Certain protein kinase inhibitors |
| JP6966423B2 (ja) * | 2015-04-24 | 2021-11-17 | グアンジョウ マキシノベル ファーマシューティカルズ カンパニー リミテッド | 縮合環ピリミジンアミノ誘導体、その製造方法、中間体、薬学的組成物及び応用 |
| CN108779117B (zh) * | 2015-12-27 | 2021-08-31 | 重庆复创医药研究有限公司 | 一类激酶抑制剂 |
| WO2017193872A1 (en) * | 2016-05-07 | 2017-11-16 | Shanghai Fochon Pharmaceutical Co., Ltd. | Certain protein kinase inhibitors |
| AU2018333913B2 (en) | 2017-09-14 | 2022-11-17 | Daiichi Sankyo Company, Limited | Compound having cyclic structure |
| SI3762368T1 (sl) | 2018-03-08 | 2022-06-30 | Incyte Corporation | Aminopirazin diolne spojine kot zaviralci PI3K-y |
| CN110551142B (zh) | 2018-05-31 | 2023-05-12 | 上海再极医药科技有限公司 | 一种稠环嘧啶类化合物的盐、晶型及其制备方法和应用 |
| US11046658B2 (en) | 2018-07-02 | 2021-06-29 | Incyte Corporation | Aminopyrazine derivatives as PI3K-γ inhibitors |
| WO2020113094A1 (en) | 2018-11-30 | 2020-06-04 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
| CN110922421B (zh) * | 2019-12-17 | 2023-05-05 | 安徽英特美科技有限公司 | 一种n-甲基-1,2,5,6-四氢吡啶-4-硼酸频哪醇酯的合成方法 |
| US20230192653A1 (en) * | 2020-03-13 | 2023-06-22 | Guangzhou Maxinovel Pharmaceuticals Co., Ltd. | Novel Therapeutic Methods |
| CN116731035A (zh) * | 2022-03-08 | 2023-09-12 | 广州再极医药科技有限公司 | 一种噻吩并嘧啶类化合物、中间体、其制备方法、组合物和应用 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE1470356A1 (de) * | 1964-01-15 | 1970-04-30 | Thomae Gmbh Dr K | Neue Thieno[3,2-d]pyrimidine und Verfahren zu ihrer Herstellung |
| EP1028964A1 (en) * | 1997-11-11 | 2000-08-23 | Pfizer Products Inc. | Thienopyrimidine and thienopyridine derivatives useful as anticancer agents |
| EP1181296A1 (en) | 1999-06-03 | 2002-02-27 | Abbott Laboratories | Cell adhesion-inhibiting antiinflammatory compounds |
| DE10042997A1 (de) | 2000-09-01 | 2002-03-14 | Merck Patent Gmbh | Thienopyrimidine |
| WO2007084815A2 (en) | 2006-01-19 | 2007-07-26 | Janssen Pharmaceutica, N.V. | Substituted thienopyrimidine kinase inhibitors |
| KR101402474B1 (ko) * | 2006-04-26 | 2014-06-19 | 제넨테크, 인크. | 포스포이노시티드 3-키나제 억제제 화합물 및 이를 포함하는 약학적 조성물 |
| MX2009006081A (es) | 2006-12-08 | 2009-06-17 | Irmc Llc | Compuestos y composiciones como inhibidores de cinasa de proteina. |
| EP2215094B1 (en) * | 2007-11-15 | 2016-01-27 | YM BioSciences Australia Pty Ltd | N-containing heterocyclic compounds |
| DE102008017853A1 (de) | 2008-04-09 | 2009-10-15 | Merck Patent Gmbh | Thienopyrimidine |
| KR101147550B1 (ko) * | 2009-10-22 | 2012-05-17 | 한국과학기술연구원 | 단백질 키나아제 저해활성을 가지는 2,7-치환된 티에노［3,2-ｄ］피리미딘 화합물 |
| KR101094446B1 (ko) * | 2009-11-19 | 2011-12-15 | 한국과학기술연구원 | 단백질 키나아제 저해활성을 가지는 2,4,7-치환된 티에노［3,2-ｄ］피리미딘 화합물 |
| WO2012004900A1 (en) | 2010-07-09 | 2012-01-12 | Aska Pharmaceutical Co., Ltd. | Thienopyrimidine compounds |
| FR2988722B1 (fr) * | 2012-04-03 | 2014-05-09 | Sanofi Sa | Nouveaux derives de thienopyrimidines, leurs procedes de preparation et leurs utilisations therapeutiques |
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2012
- 2012-04-03 FR FR1253044A patent/FR2988722B1/fr active Active
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2013
- 2013-02-04 UA UAA201411826A patent/UA112685C2/uk unknown
- 2013-04-02 SI SI201330203A patent/SI2834248T1/sl unknown
- 2013-04-02 CN CN201710950612.0A patent/CN107652303B/zh active Active
- 2013-04-02 CN CN201380029174.4A patent/CN104540834B/zh active Active
- 2013-04-02 PT PT137162418T patent/PT2834248E/pt unknown
- 2013-04-02 AU AU2013244992A patent/AU2013244992B2/en active Active
- 2013-04-02 ES ES13716241.8T patent/ES2577382T3/es active Active
- 2013-04-02 MY MYPI2014002724A patent/MY166151A/en unknown
- 2013-04-02 KR KR1020147030322A patent/KR102039764B1/ko active IP Right Grant
- 2013-04-02 EP EP13716241.8A patent/EP2834248B1/en active Active
- 2013-04-02 PE PE2014001523A patent/PE20150289A1/es active IP Right Grant
- 2013-04-02 SG SG11201406091RA patent/SG11201406091RA/en unknown
- 2013-04-02 MA MA37384A patent/MA37384B1/fr unknown
- 2013-04-02 WO PCT/EP2013/056958 patent/WO2013150036A1/en active Application Filing
- 2013-04-02 CA CA2868685A patent/CA2868685C/en active Active
- 2013-04-02 JP JP2015503860A patent/JP6096278B2/ja active Active
- 2013-04-02 BR BR112014024489-8A patent/BR112014024489B1/pt not_active IP Right Cessation
- 2013-04-02 US US13/855,246 patent/US9115140B2/en active Active
- 2013-04-02 MX MX2014011921A patent/MX355104B/es active IP Right Grant
- 2013-04-02 DK DK13716241.8T patent/DK2834248T3/en active
- 2013-04-02 RS RS20160436A patent/RS54850B1/sr unknown
- 2013-04-02 EA EA201491820A patent/EA025558B1/ru not_active IP Right Cessation
- 2013-04-02 PL PL13716241.8T patent/PL2834248T3/pl unknown
- 2013-04-02 HU HUE13716241A patent/HUE027895T2/en unknown
- 2013-04-03 AR ARP130101067A patent/AR090572A1/es active IP Right Grant
- 2013-04-03 TW TW102112260A patent/TWI579288B/zh active
- 2013-04-03 UY UY0001034725A patent/UY34725A/es not_active Application Discontinuation
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2014
- 2014-09-22 CR CR20140435A patent/CR20140435A/es unknown
- 2014-09-25 DO DO2014000216A patent/DOP2014000216A/es unknown
- 2014-09-26 ZA ZA2014/07021A patent/ZA201407021B/en unknown
- 2014-09-29 PH PH12014502180A patent/PH12014502180B1/en unknown
- 2014-09-30 TN TNP2014000415A patent/TN2014000415A1/fr unknown
- 2014-10-02 IL IL234960A patent/IL234960A/en active IP Right Grant
- 2014-10-02 CL CL2014002661A patent/CL2014002661A1/es unknown
- 2014-10-03 CO CO14219119A patent/CO7091179A2/es unknown
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2015
- 2015-02-17 HK HK15101753.8A patent/HK1201263A1/zh unknown
- 2015-07-08 US US14/794,574 patent/US9744176B2/en active Active
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2016
- 2016-06-10 HR HRP20160649TT patent/HRP20160649T1/hr unknown
- 2016-06-15 CY CY20161100522T patent/CY1117843T1/el unknown
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2017
- 2017-07-26 US US15/660,694 patent/US10220044B2/en active Active
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2018
- 2018-06-08 HK HK18107478.6A patent/HK1248214A1/zh unknown
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2019
- 2019-01-10 US US16/245,131 patent/US10500212B2/en active Active
- 2019-10-30 US US16/668,555 patent/US10736904B2/en active Active
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2020
- 2020-06-29 US US16/915,782 patent/US10980816B2/en active Active
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