AR079226A1 - Espiroindolinona- pirrolidinas, procesos de preparacion y uso de los mismos para el tratamiento y profilaxis del cancer - Google Patents
Espiroindolinona- pirrolidinas, procesos de preparacion y uso de los mismos para el tratamiento y profilaxis del cancerInfo
- Publication number
- AR079226A1 AR079226A1 ARP100104410A ARP100104410A AR079226A1 AR 079226 A1 AR079226 A1 AR 079226A1 AR P100104410 A ARP100104410 A AR P100104410A AR P100104410 A ARP100104410 A AR P100104410A AR 079226 A1 AR079226 A1 AR 079226A1
- Authority
- AR
- Argentina
- Prior art keywords
- substituted
- chosen
- heteroaryl
- aryl
- group
- Prior art date
Links
- 206010028980 Neoplasm Diseases 0.000 title 1
- 201000011510 cancer Diseases 0.000 title 1
- 238000002360 preparation method Methods 0.000 title 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 125000001072 heteroaryl group Chemical group 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 125000003107 substituted aryl group Chemical group 0.000 abstract 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 239000002246 antineoplastic agent Substances 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 abstract 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 abstract 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 abstract 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 150000002431 hydrogen Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 abstract 1
Classifications
-
- 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
- C07D487/10—Spiro-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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Indole Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
Las sales farmacéuticamente aceptables y los ésteres de los mismos. Estos compuestos son utiles como agentes anticancerosos. Reivindicacion 1: Un compuesto de la formula (1), en la que X se elige entre el grupo formado por F, Cl y Br; Y se elige entre el grupo formado por F, Cl y Br; R1 es un alquilo inferior sustituido, elegido entre el compuesto de formula (2) en el que R9 y R10 son, ambos, metilo, o están unidos para formar un grupo ciclopropilo, ciclobutilo, ciclopentilo o ciclohexilo; R11 es (CH2)q-R12 y R12 se elige entre hidrogeno, hidroxilo, alquilo inferior, alcoxi inferior, cicloalquenilo inferior, cicloalquenilo sustituido, cicloalquilo inferior, cicloalquilo sustituido, arilo, arilo sustituido, heteroarilo, heteroarilo sustituido; heterociclo o heterociclo sustituido; q es el numero 0, 1 o 2; R2 se elige entre el grupo formado por arilo, arilo sustituido, heteroarilo y heteroarilo sustituido; R3, R4 y R5 se eligen entre H o F con la condicion de que por lo menos dos de R3, R4 y R5 sean hidrogeno; R6, R7 y R8 se eligen entre H o F con la condicion de que por lo menos dos de R6, R7 y R8 sean hidrogeno; o las sales y enantiomeros farmacéuticamente aceptables del mismo.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US26579209P | 2009-12-02 | 2009-12-02 | |
| US38805410P | 2010-09-30 | 2010-09-30 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR079226A1 true AR079226A1 (es) | 2012-01-04 |
Family
ID=43608656
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100104410A AR079226A1 (es) | 2009-12-02 | 2010-11-30 | Espiroindolinona- pirrolidinas, procesos de preparacion y uso de los mismos para el tratamiento y profilaxis del cancer |
Country Status (26)
| Country | Link |
|---|---|
| US (1) | US8088815B2 (es) |
| EP (1) | EP2507243B1 (es) |
| JP (1) | JP5647262B2 (es) |
| KR (1) | KR101418191B1 (es) |
| CN (1) | CN102741257B (es) |
| AR (1) | AR079226A1 (es) |
| AU (1) | AU2010326855B2 (es) |
| BR (1) | BR112012012872A2 (es) |
| CA (1) | CA2781823A1 (es) |
| CL (1) | CL2012001405A1 (es) |
| CO (1) | CO6541606A2 (es) |
| CR (1) | CR20120259A (es) |
| EC (1) | ECSP12011945A (es) |
| ES (1) | ES2543468T3 (es) |
| IL (1) | IL220010A (es) |
| MA (1) | MA33976B1 (es) |
| MX (1) | MX2012006260A (es) |
| MY (1) | MY160596A (es) |
| NZ (1) | NZ600024A (es) |
| PE (1) | PE20121334A1 (es) |
| PH (1) | PH12012501029A1 (es) |
| RU (1) | RU2571100C2 (es) |
| SG (1) | SG181465A1 (es) |
| TW (1) | TW201129571A (es) |
| WO (1) | WO2011067185A1 (es) |
| ZA (1) | ZA201204036B (es) |
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| JP2013510860A (ja) | 2009-11-12 | 2013-03-28 | ザ、リージェンツ、オブ、ザ、ユニバーシティ、オブ、ミシガン | スピロ−オキシインドールｍｄｍ２アンタゴニスト |
| US20110118283A1 (en) * | 2009-11-17 | 2011-05-19 | Qingjie Ding | Substituted Pyrrolidine-2-Carboxamides |
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| JO2998B1 (ar) | 2010-06-04 | 2016-09-05 | Amgen Inc | مشتقات بيبيريدينون كمثبطات mdm2 لعلاج السرطان |
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| US20120046306A1 (en) * | 2010-08-18 | 2012-02-23 | David Joseph Bartkovitz | Substituted Heteroaryl Spiropyrrolidine MDM2 Antagonists |
| KR101929188B1 (ko) | 2010-11-12 | 2018-12-17 | 사노피 | 스피로옥신돌 ｍｄｍ２ 길항제 |
| CA2829188C (en) * | 2011-03-10 | 2016-10-18 | Daiichi Sankyo Company, Limited | Dispiropyrrolidine derivatives |
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| BR112014009418A2 (pt) | 2011-10-18 | 2017-04-18 | Aileron Therapeutics Inc | macrociclos peptidomiméticos |
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| CN103342672B (zh) * | 2013-07-02 | 2015-12-23 | 扬州大学 | 取代吡咯烷-2-酮的新合成方法 |
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| EA038071B1 (ru) | 2014-08-21 | 2021-07-01 | Бёрингер Ингельхайм Интернациональ Гмбх | СОЕДИНЕНИЕ СПИРО[3H-ИНДОЛ-3,2'-ПИРРОЛИДИН]-2(1H)-ОНА И ЕГО ПРОИЗВОДНЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ MDM2-p53 |
| MX389354B (es) | 2014-09-24 | 2025-03-20 | Aileron Therapeutics Inc | Macrociclos peptidomimeticos y formulaciones de los mismos. |
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| CA2979847A1 (en) | 2015-03-20 | 2016-09-29 | Aileron Therapeutics, Inc. | Peptidomimetic macrocycles and uses thereof |
| RU2629750C2 (ru) * | 2015-04-09 | 2017-09-01 | Ян Андреевич Иваненков | НОВЫЕ ДИСПИРО-ИНДОЛИНОНЫ, ИНГИБИТОРЫ MDM2/p53 ВЗАИМОДЕЙСТВИЯ, СПОСОБ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ |
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| US7553833B2 (en) * | 2007-05-17 | 2009-06-30 | Hoffmann-La Roche Inc. | 3,3-spiroindolinone derivatives |
| US7776875B2 (en) | 2007-12-19 | 2010-08-17 | Hoffman-La Roche Inc. | Spiroindolinone derivatives |
| US8258134B2 (en) | 2008-04-16 | 2012-09-04 | Hoffmann-La Roche Inc. | Pyridazinone glucokinase activators |
| US8354444B2 (en) * | 2008-09-18 | 2013-01-15 | Hoffmann-La Roche Inc. | Substituted pyrrolidine-2-carboxamides |
| KR101380013B1 (ko) * | 2008-09-18 | 2014-04-10 | 에프. 호프만-라 로슈 아게 | 치환 피롤리딘-2-카르복사미드 |
| JP2013510860A (ja) * | 2009-11-12 | 2013-03-28 | ザ、リージェンツ、オブ、ザ、ユニバーシティ、オブ、ミシガン | スピロ−オキシインドールｍｄｍ２アンタゴニスト |
| AU2011237782A1 (en) * | 2010-04-09 | 2012-10-25 | The Regents Of The University Of Michigan | Biomarkers for MDM2 inhibitors for use in treating disease |
-
2010
- 2010-11-04 US US12/939,234 patent/US8088815B2/en not_active Expired - Fee Related
- 2010-11-29 KR KR1020127016926A patent/KR101418191B1/ko not_active Expired - Fee Related
- 2010-11-29 MA MA34939A patent/MA33976B1/fr unknown
- 2010-11-29 SG SG2012040341A patent/SG181465A1/en unknown
- 2010-11-29 RU RU2012125763/04A patent/RU2571100C2/ru not_active IP Right Cessation
- 2010-11-29 PH PH1/2012/501029A patent/PH12012501029A1/en unknown
- 2010-11-29 JP JP2012541424A patent/JP5647262B2/ja not_active Expired - Fee Related
- 2010-11-29 TW TW099141297A patent/TW201129571A/zh unknown
- 2010-11-29 PE PE2012000748A patent/PE20121334A1/es not_active Application Discontinuation
- 2010-11-29 AU AU2010326855A patent/AU2010326855B2/en not_active Ceased
- 2010-11-29 WO PCT/EP2010/068353 patent/WO2011067185A1/en not_active Ceased
- 2010-11-29 EP EP10793189.1A patent/EP2507243B1/en not_active Not-in-force
- 2010-11-29 MY MYPI2012002434A patent/MY160596A/en unknown
- 2010-11-29 MX MX2012006260A patent/MX2012006260A/es active IP Right Grant
- 2010-11-29 ES ES10793189.1T patent/ES2543468T3/es active Active
- 2010-11-29 BR BR112012012872A patent/BR112012012872A2/pt not_active Application Discontinuation
- 2010-11-29 CA CA2781823A patent/CA2781823A1/en not_active Abandoned
- 2010-11-29 CN CN201080062931.4A patent/CN102741257B/zh not_active Expired - Fee Related
- 2010-11-29 NZ NZ600024A patent/NZ600024A/en not_active IP Right Cessation
- 2010-11-30 AR ARP100104410A patent/AR079226A1/es unknown
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2012
- 2012-05-18 CR CR20120259A patent/CR20120259A/es unknown
- 2012-05-24 IL IL220010A patent/IL220010A/en not_active IP Right Cessation
- 2012-05-24 CO CO12086101A patent/CO6541606A2/es not_active Application Discontinuation
- 2012-05-30 CL CL2012001405A patent/CL2012001405A1/es unknown
- 2012-06-01 ZA ZA2012/04036A patent/ZA201204036B/en unknown
- 2012-06-01 EC ECSP12011945 patent/ECSP12011945A/es unknown
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