AR034547A1 - Derivados de indolin-2-ona, su utilizacion, procedimiento para su preparacion, composicion farmaceutica que lo contiene, medicamento que consiste en dicho derivado, y un producto que contiene dicho derivado y un antagonista de los receptores de la vasopresina - Google Patents
Derivados de indolin-2-ona, su utilizacion, procedimiento para su preparacion, composicion farmaceutica que lo contiene, medicamento que consiste en dicho derivado, y un producto que contiene dicho derivado y un antagonista de los receptores de la vasopresinaInfo
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- AR034547A1 AR034547A1 ARP010101541A ARP010101541A AR034547A1 AR 034547 A1 AR034547 A1 AR 034547A1 AR P010101541 A ARP010101541 A AR P010101541A AR P010101541 A ARP010101541 A AR P010101541A AR 034547 A1 AR034547 A1 AR 034547A1
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- alkyl
- atom
- alkoxy
- pyrrolidinyl
- piperidinyl
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Abstract
Derivado de indolin-2-ona en forma de enantiómero puro o de mezcla de enantiómeros de fórmula (1) en la cual: R0 representa un grupo elegido entre fórmula (2) en la cual: Z1 representa un átomo de cloro, bromo, yodo o flúor, alquilo C1-4, alcoxi C1-4 o trifluorometilo; Z2 representa un átomo de hidrógeno, de cloro, bromo, yodo o flúor, alquilo C1-4, cicloalquilo C3-5, alcoxi C1-4, cicloalcoxi C3-5, o polifluoroalquilo C1-4; R5 representa T1W en el cual T1 representa -(CH2)m, m puede ser igual a 0 o 1; W representa un átomo de hidrógeno, hidroxicarbonilo (o carboxilo), alcoxicarbonilo C1-4, 1,3-dioxolan-2-ilo, 1,3-dioxan-2-ilo, o bien W representa un grupo -NR6R7 en el cual R6 y R7 representan independientemente entre sí, un átomo de hidrógeno, alquilo C1-4, alquilsulfonilo C1-4 o fenilsulfonilo en el cual fenilo puede ser mono, di o trisustituido por Z5; o bien R6 y R7 forman con el átomo de nitrógeno al cual están unidos morfolinilo eventualmente sustituido por alquilo o un oxo, o bien R6 y R7 forman con el átomo de nitrógeno al cual están unidos piperazinilo eventualmente sustituido en posición 4 por un sustituyente Z3; o bien R6 y R7 forman con el átomo de nitrógeno al cual están unidos pirrolidinilo o piperidinilo, y dichos pirrolidinilo y piperidinilo están eventualmente sustituidos por Z4; o bien W representa un grupo -NR8COR9 en el cual R8 representa un átomo de hidrógeno o alquilo C1-4 y R9 representa un átomo de hidrógeno, alquilo C1-4, bencilo, piridilo, fenilo, y dicho fenilo puede ser mono, di o trisustituido por Z5; o bien R9 representa un grupo -NR10R11 en el cual R10 y R11 representan independientemente entre sí, un átomo de hidrógeno o un alquilo C1-4, o bien R10 y R11 forman con el átomo de nitrógeno al cual están unidos, pirrolidinilo, piperidinilo, o morfolinilo eventualmente sustituido por alquilo C1-4, o bien R9 representa pirrolidin-2-ilo o 3-ilo, piperidin-2-ilo, 3-ilo o 4-ilo, dichos pirrolidinilo y piperidinilo están eventualmente sustituidos por Z7; o bien R9 representa un grupo -T2-R12 o -T2-COR12 en el cual T2 representa -(CH2)n-, n puede ser igual a 1, 2, 3 y 4 y R12 representan alcoxi C1-4 o -NR10R11, R10 y R11 son tal como se los ha definido anteriormente; o bien W representa un grupo -CONR13R14 en el cual R13 representa un átomo de hidrógeno, alquilo C1-4, cicloalquilo C3-7, un mono- o polifluoro C1-4 alquilo, y R14 representa un átomo de hidrógeno, alquilo C1-4, fenilo eventualmente sustituido por Z5, -T4-R15 en el cual T4 represente -(CH2)q- con q igual a 1, 2, 3 o 4 y R15 representa hidroxilo, alcoxi C1-4, alcoxicarbonilo C1-4, alcoxicarbonilamino C1-4, fenilo eventualmente mono-, disustituido por Z5, un pirid-2-ilo, 3-ilo o 4-ilo, -NR16R17 en el cual R16 y R17 representan independientemente entre sí, un átomo de hidrógeno, o un alquilo C1-4, o bien R16 y R17 forman con el átomo de nitrógeno al cual están unidos morfolinilo eventualmente mono o disustituido por alquilo C1-4, o bien R16 y R17 forman con el átomo de nitrógeno al cual están unidos piperazinilo eventualmente sustituido en posición 4 por un sustituyente Z3, o bien R16 y R17 forman con el átomo de nitrógeno al cual están unidos pirrolidinilo o piperidinilo, dichos pirrolidinilo y piperidinilo están eventualmente sustituidos por Z5 y se entiende que cuando q = 1, R15 es diferente de hidroxilo, alcoxi C1-4, alcoxicarbonilamino C1-4, -NR16R17; o bien R13 y R14 forman con el átomo de nitrógeno al cual están unidos un grupo morfolinilo eventualmente mono o disustituido por un grupo alquilo C1-4, piperazinilo eventualmente sustituido en posición 4 por un sustituyente Z3; o bien R13 y R14 forman con el átomo de nitrógeno al cual están unidos azetidinilo, pirrolidinilo o piperidinilo, hexahidroazepinilo, dichos grupos pirrolidinilo, piperidinilo y hexahidroazepinilo están eventualmente mono o disustituidos por Z8; o bien W representa un grupo OR18, en el cual R18 representa un átomo de hidrógeno, alquilo C1-4, alcoxi C1-4 alquilo C1-4 o -T3-R19 en el cual T3 representa -(CH2)p-, p puede ser igual a 2, 3 y R19 se elige entre los grupos hidroxilo, trifenilmetoxi, -NR20R21 en el cual R20 representa un átomo de hidrógeno o alquilo C1-4 y R21 representa un átomo de hidrógeno, alquilo C1-4, tetrahidrofuranilmetilo o tetrahidropiranilmetilo, o bien R20 y R21 forman con el átomos de nitrógeno al cual están unidos, morfolinilo eventualmente mono o disustituido por alquilo C1-4, piperazinilo eventualmente sustituido en posición 4 por un sustituyente Z3 o bien R20 y R21 forman con el átomo de nitrógeno al cual están unidos, pirrolidinilo o piperidinilo, dichos pirrolidinilo y piperidinilo están eventualmente sustituidos por Z5; Z3 representa alquilo, piridilo o fenilo C1-4, alquilcarbonilo C1-4, alcoxicarbonilo C1-4; Z4 representa un oxo, un átomo de flúor, hidroxilo, alquilo C1-4, bencilo, amino, alquilamino C1-4, di C1-4 alquilamino, alcoxi C1-4, alcoxicarbonilo C1-4, alcoxicarbonilamino C1-4; Z5 representa un átomo de cloro, bromo, yodo o flúor, hidroxilo alquilo C1-4, o alcoxi C1-4; Z7 representa un átomo de flúor, hidroxilo, hidroxialquilo C1-4, alquilo C1-4, alcoxi C1-4, alquilcarbonilo C1-4; Z8 representa un átomo de flúor, hidroxilo alquilo C1-4, cicloalquilo C3-6, bencilo, amino, alquilamino C1-4, dialquilamino C1-4, alcoxicarbonilo C1-4, alcoxicarbonilamino C1-4, cicloalcoxi C3-6, hidroxicarbonilo, hidroxialquilo C1-4 o alcoxi C1-4 alquilo C1-4, alcoxi C1-4, -CONR23R24 en el cual R23 y R24 representan independientemente entre sí, un átomo de hidrógeno, alquilo C1-4, mono o polifluoroalquilo C1-4 o bien R23 y R24 forman con el átomo de nitrógeno al cual están unidos, pirrolidinilo o piperidinilo, dichos grupos pirrolidinilo o piperidinilo están eventualmente sustituidos por Z3, difluorometilideno; o R0 representa un grupo elegido entre fórmula (3)Z6 representa un átomo de cloro o alquilo C1-4 o alcoxi C1-4; R1 representa alquilo C1-4 que presenta eventualmente un doble o un triple enlace, alcoxicarbonilo C1-4; feniloxicarbonilo o un grupo T1-R22 en el cual T1 es tal como se ha definido anteriormente y R22 representa un grupo hidroxilo o alcoxi C1-4; R2 y R4 representan independientemente entre sí, un átomo de hidrógeno, de cloro o de flúor, alquilo C1-4 o alcoxi C1-4; R3 representa un átomo de cloro o de flúor, hidroxilo, alquilo C1-4, alcoxi C1-4, carbamoílo C1-4, alquilcarbonilamino C1-4, nitro, ciano, trifluorometilo, amino, cicloalquilamino C3-6, alquilamino C1-4, dialquilamino C1-4, trialquilamonio C1-4, A-, A- son un anión; pirrolidin-1-ilo, piperidin-1-ilo, piperazin-1-ilo, morfolin-4-ilo o hexahidroazepin-1-ilo; X e Y representan independientemente entre sí, un átomo de hidrógeno, de cloro, bromo, yodo o flúor o alcoxi C1-4 o trifluorometoxi; así como sus sales farmacéuticamente aceptables, solvatos e hidratos. El compuesto de fórmula (1) es afín con los receptores de la oxitocina. Su utilización, procedimiento para su preparación, composición farmacéutica que lo contiene, medicamento que consiste en el compuesto de fórmula (1), y un producto que contiene el compuesto de fórmula (1), y un producto que contiene el compuesto de fórmula (1) antagonista de los receptores de la oxitocina y un antagonista de los receptores de la vasopresina.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
FR0004193A FR2807038B1 (fr) | 2000-04-03 | 2000-04-03 | Nouveaux derives d'indolin-2-one, leur preparation et les compositions pharmaceutiques les contenant |
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AR034547A1 true AR034547A1 (es) | 2004-03-03 |
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ARP010101541A AR034547A1 (es) | 2000-04-03 | 2001-03-30 | Derivados de indolin-2-ona, su utilizacion, procedimiento para su preparacion, composicion farmaceutica que lo contiene, medicamento que consiste en dicho derivado, y un producto que contiene dicho derivado y un antagonista de los receptores de la vasopresina |
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US (2) | US20040059132A1 (es) |
EP (1) | EP1272468B1 (es) |
JP (1) | JP2003529586A (es) |
KR (1) | KR100765028B1 (es) |
CN (1) | CN1224614C (es) |
AR (1) | AR034547A1 (es) |
AT (1) | ATE282593T1 (es) |
AU (2) | AU2001246671B2 (es) |
BR (1) | BR0109814A (es) |
CA (1) | CA2404592A1 (es) |
CZ (1) | CZ20023297A3 (es) |
DE (1) | DE60107221T2 (es) |
DK (1) | DK1272468T3 (es) |
EA (1) | EA005093B1 (es) |
EE (1) | EE05002B1 (es) |
ES (1) | ES2232610T3 (es) |
FR (1) | FR2807038B1 (es) |
HK (1) | HK1050004A1 (es) |
HU (1) | HUP0303109A3 (es) |
IL (1) | IL152085A0 (es) |
IS (1) | IS2458B (es) |
ME (1) | MEP24308A (es) |
MX (1) | MXPA02009773A (es) |
NO (1) | NO324314B1 (es) |
NZ (1) | NZ521617A (es) |
PL (1) | PL358222A1 (es) |
PT (1) | PT1272468E (es) |
SI (1) | SI1272468T1 (es) |
SK (1) | SK14272002A3 (es) |
TR (1) | TR200202288T2 (es) |
TW (1) | TWI225860B (es) |
UA (1) | UA73163C2 (es) |
WO (1) | WO2001074775A1 (es) |
YU (1) | YU80902A (es) |
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CN1711101A (zh) * | 2002-10-03 | 2005-12-21 | Pr药品有限公司 | 孤独症及相似障碍的治疗 |
TWI289141B (en) | 2003-03-11 | 2007-11-01 | Hoffmann La Roche F. Ag. | Quinolinone derivatives and uses thereof |
FR2875499B1 (fr) * | 2004-09-20 | 2006-10-27 | Sanofi Aventis Sa | Nouveaux derives pyridiniques d'indolin-2-one, leur preparation et leur application en therapeutique |
MY145694A (en) | 2005-04-11 | 2012-03-30 | Xenon Pharmaceuticals Inc | Spiroheterocyclic compounds and their uses as therapeutic agents |
MY144968A (en) | 2005-04-11 | 2011-11-30 | Xenon Pharmaceuticals Inc | Spiro-oxindole compounds and their uses as therapeutic agents |
AR056317A1 (es) * | 2005-04-20 | 2007-10-03 | Xenon Pharmaceuticals Inc | Compuestos de oxindol y composicion farmaceutica |
CA2605923C (en) * | 2005-05-10 | 2012-07-24 | Ferring International Center Sa. | Use of antagonists of oxytocin and/or vasopressin |
WO2007063123A1 (de) * | 2005-12-02 | 2007-06-07 | Abbott Gmbh & Co. Kg | Substituierte oxindol-derivate, diese enthaltende arzneimittel und deren verwendung |
US7855194B2 (en) | 2006-03-27 | 2010-12-21 | Hoffmann-La Roche Inc. | Pyrimidine, quinazoline, pteridine and triazine derivatives |
WO2007120102A1 (en) * | 2006-04-19 | 2007-10-25 | Astrazeneca Ab | New substituted oxindole derivatives |
JP5460324B2 (ja) | 2006-10-12 | 2014-04-02 | ゼノン・ファーマシューティカルズ・インコーポレイテッド | 治療剤としてのスピロ−オキシインドール化合物の使用 |
WO2008046083A2 (en) * | 2006-10-12 | 2008-04-17 | Xenon Pharmaceuticals Inc. | Use of oxindole compounds as therapeutic agents |
FR2909668B1 (fr) * | 2006-12-12 | 2009-01-23 | Sanofi Aventis Sa | Derives de 5-alkyloxy-indolin-2-one,leur preparation et leurs applications en therapeutique |
DK2350090T3 (en) | 2008-10-17 | 2015-09-07 | Xenon Pharmaceuticals Inc | Spiro-oxindole compounds and their use as therapeutic agents |
EP2350091B1 (en) | 2008-10-17 | 2015-06-03 | Xenon Pharmaceuticals Inc. | Spiro-oxindole compounds and their use as therapeutic agents |
AR077252A1 (es) | 2009-06-29 | 2011-08-10 | Xenon Pharmaceuticals Inc | Enantiomeros de compuestos de espirooxindol y sus usos como agentes terapeuticos |
WO2011047174A1 (en) | 2009-10-14 | 2011-04-21 | Xenon Pharmaceuticals Inc. | Synthetic methods for spiro-oxindole compounds |
US9504671B2 (en) | 2010-02-26 | 2016-11-29 | Xenon Pharmaceuticals Inc. | Pharmaceutical compositions of spiro-oxindole compound for topical administration and their use as therapeutic agents |
CN103623268B (zh) * | 2013-12-04 | 2015-07-15 | 张国显 | 神经康复再造丸及其制备方法 |
CN103830666B (zh) * | 2014-02-14 | 2016-02-10 | 孔祥英 | 一种治疗高血压的中药足浴组合物 |
CN104402886B (zh) * | 2014-09-18 | 2017-01-25 | 陕西科技大学 | 一种具有抗肿瘤活性的7‑氮杂靛红类双螺环化合物及其合成方法 |
CN104230786B (zh) * | 2014-09-26 | 2017-03-22 | 陕西科技大学 | 一种具有抗肿瘤活性的含吲哚结构的化合物及其合成方法 |
US9682033B2 (en) | 2015-02-05 | 2017-06-20 | Teva Pharmaceuticals International Gmbh | Methods of treating postherpetic neuralgia with a topical formulation of a spiro-oxindole compound |
CN108349944B (zh) | 2015-11-06 | 2021-03-30 | 豪夫迈·罗氏有限公司 | 二氢吲哚-2-酮衍生物 |
CN108698991B (zh) * | 2016-01-20 | 2022-08-23 | 凯莫森特里克斯股份有限公司 | 2-氧代吲哚化合物 |
CN109232290A (zh) * | 2018-11-07 | 2019-01-18 | 陕西科技大学 | 一种含氟酰胺及其制备方法 |
CN109678781B (zh) * | 2018-12-20 | 2022-03-29 | 苏州麦迪耐斯医药科技有限公司 | 一种刺猬通路抑制剂 |
EP3912625A1 (en) | 2020-05-20 | 2021-11-24 | Kaerus Bioscience Limited | Novel maxi-k potassium channel openers for the treatment of fragile x associated disorders |
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DE3529994A1 (de) * | 1985-08-22 | 1987-02-26 | Hoechst Ag | Indolinonderivate, verfahren zu ihrer herstellung, sie enthaltende arzneimittel und deren verwendung |
CA2037923C (en) * | 1989-07-25 | 1996-08-06 | Akihiro Kawaguchi | Oxindole derivative |
US5686624A (en) * | 1992-01-30 | 1997-11-11 | Sanofi | 1-benzenesulfonyl-1,3-dihydro-indol-2-one derivatives, their preparation and pharmaceutical compositions in which they are present |
FR2708605A1 (fr) * | 1993-07-30 | 1995-02-10 | Sanofi Sa | Dérivés du N-sulfonylindol-2-one, leur préparation, les compositions pharmaceutiques en contenant. |
FR2714378B1 (fr) * | 1993-12-24 | 1996-03-15 | Sanofi Sa | Dérivés de l'indol-2-one substitués en 3 par un groupe azoté, leur préparation, les compositions pharmaceutiques en contenant. |
JPH10338672A (ja) * | 1996-07-16 | 1998-12-22 | Takeda Chem Ind Ltd | 排尿調節剤および2環性化合物 |
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2000
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2001
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- 2001-04-02 CA CA002404592A patent/CA2404592A1/fr not_active Abandoned
- 2001-04-02 CZ CZ20023297A patent/CZ20023297A3/cs unknown
- 2001-04-02 AT AT01919610T patent/ATE282593T1/de active
- 2001-04-02 YU YU80902A patent/YU80902A/sh unknown
- 2001-04-02 MX MXPA02009773A patent/MXPA02009773A/es active IP Right Grant
- 2001-04-02 AU AU2001246671A patent/AU2001246671B2/en not_active Ceased
- 2001-04-02 TR TR2002/02288T patent/TR200202288T2/xx unknown
- 2001-04-02 DK DK01919610T patent/DK1272468T3/da active
- 2001-04-02 KR KR1020027013217A patent/KR100765028B1/ko not_active IP Right Cessation
- 2001-04-02 ES ES01919610T patent/ES2232610T3/es not_active Expired - Lifetime
- 2001-04-02 JP JP2001572470A patent/JP2003529586A/ja active Pending
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- 2001-04-02 IL IL15208501A patent/IL152085A0/xx not_active IP Right Cessation
- 2001-04-02 PT PT01919610T patent/PT1272468E/pt unknown
- 2001-04-02 SI SI200130294T patent/SI1272468T1/xx unknown
- 2001-04-02 AU AU4667101A patent/AU4667101A/xx active Pending
- 2001-04-02 BR BR0109814-4A patent/BR0109814A/pt not_active IP Right Cessation
- 2001-04-02 EP EP01919610A patent/EP1272468B1/fr not_active Expired - Lifetime
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- 2001-04-02 EE EEP200200573A patent/EE05002B1/xx not_active IP Right Cessation
- 2001-04-02 PL PL01358222A patent/PL358222A1/xx not_active Application Discontinuation
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- 2001-04-02 CN CNB018090303A patent/CN1224614C/zh not_active Expired - Fee Related
- 2001-04-02 WO PCT/FR2001/000980 patent/WO2001074775A1/fr active IP Right Grant
- 2001-04-02 SK SK1427-2002A patent/SK14272002A3/sk unknown
- 2001-04-02 DE DE60107221T patent/DE60107221T2/de not_active Expired - Lifetime
- 2001-04-03 TW TW090107916A patent/TWI225860B/zh not_active IP Right Cessation
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