AR074499A1 - Carboxamidas heterobiciclicas como inhibidoras de cinasas - Google Patents
Carboxamidas heterobiciclicas como inhibidoras de cinasasInfo
- Publication number
- AR074499A1 AR074499A1 ARP090104731A ARP090104731A AR074499A1 AR 074499 A1 AR074499 A1 AR 074499A1 AR P090104731 A ARP090104731 A AR P090104731A AR P090104731 A ARP090104731 A AR P090104731A AR 074499 A1 AR074499 A1 AR 074499A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- amino
- hydrogen
- mono
- group
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/18—Sulfonamides
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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
- A61K31/40—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
- A61K31/403—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 carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
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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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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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
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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
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- C07D487/04—Ortho-condensed systems
-
- 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
- C07D487/08—Bridged systems
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Urology & Nephrology (AREA)
- Pulmonology (AREA)
- Hematology (AREA)
- Heart & Thoracic Surgery (AREA)
- Dermatology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Oncology (AREA)
- Immunology (AREA)
- Ophthalmology & Optometry (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Composiciones farmacéuticas que comprenden un compuesto de la fórmula (1), y al uso de un compuesto de la fórmula (1) para la preparación de composiciones farmacéuticas para utilizarse en el tratamiento de enfermedades dependientes de la cinasa de proteína, en especial de enfermedades proliferativas, tal como en el tratamiento de enfermedades tumorales y enfermedades neovasculares oculares. Reivindicación 1: Un compuesto de la fórmula (1) o una sal del mismo, en donde R1 es hidrógeno o alquilo C1-6; R2 es hidrógeno o alquilo C1-6; R3 es hidrógeno o alquilo C1-6; R4 es hidrógeno o alquilo C1-6; o R2 y R4, tomados en combinación, forman un enlace; R5 es hidrógeno, alquilo C1-6, o halógeno; R6 representa 0, 1 o 2 residuos independientemente seleccionados en cada presentación a partir de halógeno, o alquilo C1-6; R7 es hidrógeno o alquilo C1-6; X es O o S; Z1 y Z2 se seleccionan independientemente a partir del grupo que consiste en N y CR8; R8 y R10 se seleccionan independientemente a partir del grupo que consiste en hidrógeno y alquilo C1-6; R9 se selecciona a partir del grupo que consisto en (CR11R12)nNR13R14, (CR11R12)nheterociclo, (CR11R12)nOR15, (CR11R12)nC(O)ER13, y (CR11R12)nS(O)mR17; o R8 y R9, tomados en combinación, junto con los átomos con los que están unidos, forman un anillo heterocíclico saturado de 4 a 7 miembros que tiene 1 ó 2 heteroátomos del anillo seleccionados a partir de N, O o S, cuyo anillo heterocíclico está sustituido con 0, 1 o 2 residuos seleccionados independientemente a partir del grupo que consiste en oxo, alquilo C1-6, halo-alquilo C1-6, alcoxilo C1-6, halo-alcoxilo C1-6, halógeno, hidroxilo, amino, hidroxi-alquilo C1-6, amino-alquilo C1-6, mono- y di-alquilo C1-6-amino-alquilo C1-6, cicloalquilo C3-7-alquilo C1-4, hetero-cicloalquilo C1-4, alcanoílo C1-6, mono- y di-alquilo C1-6-amino, amino-carbonilo, mono- y di-alquilo C1-6-amino-carbonilo, alcoxilo C1-6-carbonilo, alquilo C1-6-sulfonilo, amino-sulfonilo, y mono- y di-alquilo C1-6-amino-sulfonilo; Ar2 se selecciona a partir del grupo que consiste en fenilo, naftilo, un heteroarilo monocíclico o bicíclico, y heterociclo bicíclico o tricíclico, en donde cada residuo de heteroarilo o heterociclo tiene 1, 2, 3 o 4 heteroátomos del anillo seleccionados a partir de N, O o S, y en donde el grupo fenilo, naftilo, heteroarilo o heterociclo está insustituido o sustituido por 1, 2, o 3 grupos independientemente seleccionados a partir de alquilo C1-8, halo-alquilo C1-8, hidroxi-alquilo C1-6, alcoxilo C1-8, halo-alcoxilo C1-8, halógeno, hidroxilo, amino, amino-alquilo C1-6, mono- y di-alquilo C1-6-amino-alquilo C1-6, mono- y di-alquilo C1-6-amino, CO2-alquilo C1-6, fenil-alquilo C0-4, cicloalquilo C3-7-alquilo C0-4, cicloalquilo espirocíclico C3-7, amino-sulfonilo, y mono- y di-alquilo C1-6-amino-sulfonilo; m es 0, 1, o 2; n es 0, 1, 2, o 3; E está ausente, o es O o NR18: R11, R12, y R18 son iguales o diferentes, y se seleccionan independientemente en cada presentación a partir del grupo que consiste en hidrógeno y alquilo C1-4; y R13, R14, R15, R16 y R17 se seleccionan independientemente en cada presentación a partir del grupo que consiste en hidrógeno, alquilo C1-6, alcanoílo C1-6, cicloalquilo C3-6, fenilo y heterociclo, cada uno de los cuales está sustituido con 0, 1 o 2 residuos seleccionados independientemente a partir de alquilo C1-4, alcoxilo C1-4, halógeno, hidroxilo, amino, y mono- y di-alquilo C1-6-amino.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US20124308P | 2008-12-09 | 2008-12-09 | |
US23334109P | 2009-08-12 | 2009-08-12 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR074499A1 true AR074499A1 (es) | 2011-01-19 |
Family
ID=42034535
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP090104731A AR074499A1 (es) | 2008-12-09 | 2009-12-07 | Carboxamidas heterobiciclicas como inhibidoras de cinasas |
Country Status (39)
Country | Link |
---|---|
US (6) | US8242125B2 (es) |
EP (1) | EP2376478B1 (es) |
JP (1) | JP5580330B2 (es) |
KR (1) | KR101345956B1 (es) |
CN (2) | CN102307870B (es) |
AR (1) | AR074499A1 (es) |
AU (1) | AU2009326110B9 (es) |
BR (1) | BRPI0922552A2 (es) |
CA (1) | CA2745922C (es) |
CL (1) | CL2011001378A1 (es) |
CO (1) | CO6382119A2 (es) |
CR (1) | CR20110270A (es) |
CU (1) | CU24097B1 (es) |
CY (1) | CY1119091T1 (es) |
DK (1) | DK2376478T3 (es) |
EA (1) | EA019681B1 (es) |
EC (1) | ECSP11011113A (es) |
ES (1) | ES2633959T3 (es) |
HN (1) | HN2011001593A (es) |
HR (1) | HRP20171075T1 (es) |
HU (1) | HUE035292T2 (es) |
IL (1) | IL213068A (es) |
JO (1) | JO3265B1 (es) |
LT (1) | LT2376478T (es) |
MX (1) | MX2011006093A (es) |
MY (1) | MY155649A (es) |
NZ (2) | NZ593030A (es) |
PE (1) | PE20110835A1 (es) |
PL (1) | PL2376478T3 (es) |
PT (1) | PT2376478T (es) |
RS (1) | RS56076B1 (es) |
SG (1) | SG171784A1 (es) |
SI (1) | SI2376478T1 (es) |
SV (1) | SV2011003939A (es) |
TN (1) | TN2011000263A1 (es) |
TW (1) | TWI429640B (es) |
UY (1) | UY32302A (es) |
WO (1) | WO2010066684A2 (es) |
ZA (1) | ZA201103759B (es) |
Families Citing this family (63)
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PT2350075E (pt) | 2008-09-22 | 2014-06-09 | Array Biopharma Inc | Compostos imidazo[1,2b]piridazina substituídos como inibidores da trk cinase |
AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
ES2547145T3 (es) * | 2010-10-27 | 2015-10-02 | Novartis Ag | Regímenes de dosificación para el tratamiento de enfermedad vascular ocular |
CN102786469B (zh) * | 2011-05-18 | 2016-09-14 | 中国医学科学院药物研究所 | 邻吡啶酰肼衍生物及其制法和药物组合物与用途 |
US9056874B2 (en) | 2012-05-04 | 2015-06-16 | Novartis Ag | Complement pathway modulators and uses thereof |
KR20150003903A (ko) * | 2012-05-04 | 2015-01-09 | 노파르티스 아게 | 보체 경로 조절제 및 그의 용도 |
KR101315227B1 (ko) * | 2012-05-30 | 2013-10-07 | 엘지디스플레이 주식회사 | 터치스크린 일체형 표시장치 및 그 구동 방법 |
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US9388199B2 (en) * | 2012-06-28 | 2016-07-12 | Novartis Ag | Pyrrolidine derivatives and their use as complement pathway modulators |
US9468661B2 (en) * | 2012-06-28 | 2016-10-18 | Novartis Ag | Pyrrolidine derivatives and their use as complement pathway modulators |
CN104640855B (zh) * | 2012-06-28 | 2017-08-29 | 诺华股份有限公司 | 补体途经调节剂及其用途 |
CN104379579B (zh) * | 2012-06-28 | 2017-03-08 | 诺华股份有限公司 | 吡咯烷衍生物及其作为补体途径调节剂的用途 |
EA201590118A1 (ru) * | 2012-06-28 | 2015-04-30 | Новартис Аг | Производные пирролидина и их применение в качестве модуляторов пути активации комплемента |
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CN103570616B (zh) * | 2012-07-18 | 2017-10-20 | 中国医学科学院药物研究所 | N′‑直链烷酰基邻吡啶酰肼衍生物及其制法和药物组合物与用途 |
WO2014143638A1 (en) | 2013-03-14 | 2014-09-18 | Novartis Ag | 2-(1h-indol-4-ylmethyl)-3h-imidazo[4,5-b]pyridine-6-carbonitrile derivatives as complement factor b inhibitors useful for the treatment of ophthalmic diseases |
CN104072481B (zh) * | 2013-03-28 | 2016-08-17 | 宁波市方昌医药有限公司 | 一种抗血管新生化合物 |
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US10174006B2 (en) * | 2013-06-06 | 2019-01-08 | Novartis Ag | Topical aqueous ophthalmic compositions containing a 1H-indole-1-carboxamide derivative and use thereof for treatment of ophthalmic disease |
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JP6816100B2 (ja) | 2015-07-16 | 2021-01-20 | アレイ バイオファーマ、インコーポレイテッド | RETキナーゼ阻害物質としての置換ピラゾロ[1,5−a]ピリジン化合物 |
AU2016344058A1 (en) | 2015-10-26 | 2018-05-17 | Array Biopharma Inc. | Point mutations in Trk inhibitor-resistant cancer and methods relating to the same |
EP3371170B1 (en) | 2015-11-06 | 2019-07-31 | H. Hoffnabb-La Roche Ag | Indolin-2-one derivatives useful in the treatment of cns diseases |
JP6857653B2 (ja) | 2015-11-06 | 2021-04-14 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | Cns及び関連障害の治療において使用するためのインドリン−2−オン誘導体 |
EP3371174B1 (en) | 2015-11-06 | 2021-03-17 | H. Hoffnabb-La Roche Ag | Indolin-2-one derivatives |
DK3371168T3 (da) | 2015-11-06 | 2020-08-03 | Hoffmann La Roche | Indolin-2-on-derivater |
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