ES2190221T3 - Derivados de indol y su uso para el tratamiento de enfermedades malignas y otras, que se basan en proliferaciones celulares patologicas. - Google Patents

Derivados de indol y su uso para el tratamiento de enfermedades malignas y otras, que se basan en proliferaciones celulares patologicas.

Info

Publication number
ES2190221T3
ES2190221T3 ES99927711T ES99927711T ES2190221T3 ES 2190221 T3 ES2190221 T3 ES 2190221T3 ES 99927711 T ES99927711 T ES 99927711T ES 99927711 T ES99927711 T ES 99927711T ES 2190221 T3 ES2190221 T3 ES 2190221T3
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ES
Spain
Prior art keywords
alkyl
formula
atom
substituted
general formula
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Lifetime
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ES99927711T
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English (en)
Inventor
Siavosh Mahboobi
Wall Sabine De
Herwig Pongratz
Alfred Popp
Harald Hufsky
Frank-D Bohmer
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Aeterna Zentaris GmbH
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Zentaris AG
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Filing date
Publication date
Priority claimed from DE19838506A external-priority patent/DE19838506C2/de
Application filed by Zentaris AG filed Critical Zentaris AG
Application granted granted Critical
Publication of ES2190221T3 publication Critical patent/ES2190221T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/02Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
    • A61P5/04Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin for decreasing, blocking or antagonising the activity of the hypothalamic hormones
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/14Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/54Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C07D333/56Radicals substituted by oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12Heterocyclic 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 three hetero rings
    • C07D487/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/14Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Saccharide Compounds (AREA)

Abstract

Compuestos de fórmula general I: **(Fórmula)** en la que Z es un grupo de fórmula general (II) **(Fórmula)** en la que B, B¿ pueden ser un átomo de carbono, nitrógeno, oxígeno o azufre y los sistemas de anillo F y G pueden ser, independientemente entre sí, anillos penta y hexagonales tanto saturados como insaturados, X representa un grupo de fórmula general III o IV, **(Fórmula)** en la que A puede ser un átomo de N, O, S, l y n pueden tomar los números de 0 a 6, m los números 1 y 2, así como R14 y R15 conjuntamente forman un átomo de oxígeno o R14 significa un grupo hidroxilo y R15 un átomo de hidrógeno, o R14 y R15 significan átomos de hidrógeno, y en la que R16 significa un átomo de hidrógeno, un resto alquilo o arilo, un resto alquilo o arilo sustituido con halógeno, amino o azido, un resto alquiloximetilo o alquiloximetilo sustituido, R2 y R13 forman conjuntamente una unión de fórmula general V o VI **(Fórmula)** en las que el enlace de trazos discontínuos significa un enlace doble o sencillo, A y R16 poseen los mismos significados que anteriormente y o puede adoptar los números 1 y 2, R2 y R13 significan restos iguales o distintos de fórmula general VII o átomos de hidrógeno, **(Fórmula)** en la que el enlace de trazos discontínuos significa un enlace doble o sencillo, A y R16 poseen los mismos significados que anteriormente y R17 significa un átomo de halógeno o un resto de fórmula general VIII **(Fórmula)** de modo que puede ser igual a 0, 1 ó 2 (cuando p=0, se trata entonces de una amina acíclica primaria e Y porta un átomo de hidrógeno adicional), Y puede ser un átomo de carbono, oxígeno o nitrógeno y cuando Y es un átomo de carbono o nitrógeno, R18 significa un átomo de hidrógeno o un resto alquilo o **(Fórmula)** arilo, un resto alquilo o arilo sustituido, heterociclo, un resto alcoxicarbonilo, un resto aminocarbonilmetilo saturado o insaturado, o un resto aminocarbonilmetilo sustituido, R2 y R13 forman conjuntamente una unión de fórmula general IX o X **(Fórmula)** en las que W representa un átomo de carbono o nitrógeno, q puede adoptar un número entre 0 y 6 y R10 y R20 pueden significar átomos de hidrógeno, restos alquilo o alquilo sustituido, en las que R1, R7 y R12 son iguales o distintos y significan átomos de hidrógeno, restos alquilo y aminoalquilo, restos fenilsulfonilo, restos alquilsililmetoximetilo, un azúcar o un azúcar sustituido, en las que R3, R4, R5, R6, R8, R9, R10 y R11 son iguales o distintos y representan respectivamente un átomo de hidrógeno, un grupo alquilo, alcoxi, alcoximetilo sustituido con alcoxi, amino, halógeno, cicloalquilo, cicloheteroalquilo, arilo o heteroarilo, un grupo nitro, un átomo de halógeno o un grupo O-alcoxi de fórmula general -O-(C=O)-R21, en la que R21 significa un grupo alquilo, alcoxi o alcoximetilo sustituido con alcoxi, amino, halógeno, cicloalquilo, cicloheteroalquilo, arilo o heteroarilo.
ES99927711T 1998-05-04 1999-04-22 Derivados de indol y su uso para el tratamiento de enfermedades malignas y otras, que se basan en proliferaciones celulares patologicas. Expired - Lifetime ES2190221T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19819835 1998-05-04
DE19838506A DE19838506C2 (de) 1998-05-04 1998-08-25 Indolderivate und deren Verwendung zur Behandlung von malignen und anderen, auf pathologischen Zellproliferationen beruhenden Erkrankungen

Publications (1)

Publication Number Publication Date
ES2190221T3 true ES2190221T3 (es) 2003-07-16

Family

ID=26045937

Family Applications (1)

Application Number Title Priority Date Filing Date
ES99927711T Expired - Lifetime ES2190221T3 (es) 1998-05-04 1999-04-22 Derivados de indol y su uso para el tratamiento de enfermedades malignas y otras, que se basan en proliferaciones celulares patologicas.

Country Status (22)

Country Link
US (2) US6407102B1 (es)
EP (1) EP1109785B1 (es)
JP (1) JP2002514572A (es)
CN (1) CN1151127C (es)
AT (1) ATE230394T1 (es)
AU (1) AU752464B2 (es)
BG (1) BG104996A (es)
BR (1) BR9911017A (es)
CA (1) CA2330756C (es)
CZ (1) CZ20003960A3 (es)
DE (1) DE59903921D1 (es)
DK (1) DK1109785T3 (es)
ES (1) ES2190221T3 (es)
HK (1) HK1038354A1 (es)
HU (1) HUP0102563A3 (es)
IL (1) IL139056A0 (es)
NO (1) NO317261B1 (es)
NZ (1) NZ507735A (es)
PL (1) PL346840A1 (es)
SK (1) SK16352000A3 (es)
TR (1) TR200003206T2 (es)
WO (1) WO1999057117A2 (es)

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TW557298B (en) * 2000-08-14 2003-10-11 Ciba Sc Holding Ag A compound, a photopolymerizible composition, a process for producing coatings and a method for causing a photoinitiator to accumulate at the surface of coatings
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DE10143079A1 (de) * 2001-09-03 2003-05-15 Zentaris Ag Cyclische Indol- und Heteroindolderivate, deren Herstellung und Verwendung als Arzneimittel
US20050267303A1 (en) * 2001-09-04 2005-12-01 Zentaris Ag Cyclic indole and heteroindole derivatives and methods for making and using as pharmaceuticals
JPWO2003063861A1 (ja) * 2002-01-30 2005-05-26 住友製薬株式会社 線維化抑制剤
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US9062055B2 (en) 2010-06-21 2015-06-23 Incyte Corporation Fused pyrrole derivatives as PI3K inhibitors
WO2012087881A1 (en) 2010-12-20 2012-06-28 Incyte Corporation N-(1-(substituted-phenyl)ethyl)-9h-purin-6-amines as pi3k inhibitors
US9108984B2 (en) 2011-03-14 2015-08-18 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as PI3K inhibitors
US9126948B2 (en) 2011-03-25 2015-09-08 Incyte Holdings Corporation Pyrimidine-4,6-diamine derivatives as PI3K inhibitors
ES2722524T3 (es) 2011-09-02 2019-08-13 Incyte Holdings Corp Heterociclaminas como inhibidores de pi3k
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
WO2015191677A1 (en) 2014-06-11 2015-12-17 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
MD3831833T2 (ro) 2015-02-27 2023-04-30 Incyte Holdings Corp Procedee pentru prepararea unui inhibitor PI3K
US9988401B2 (en) 2015-05-11 2018-06-05 Incyte Corporation Crystalline forms of a PI3K inhibitor
US9732097B2 (en) 2015-05-11 2017-08-15 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
CN106317169B (zh) * 2015-06-23 2019-07-02 首都医科大学 双吲哚-二肽衍生物,其合成,抗血栓活性和制备抗血栓剂的应用
CN109790191B (zh) * 2016-08-05 2022-04-08 香港大学 铂配合物及其使用方法
CN114364798A (zh) 2019-03-21 2022-04-15 欧恩科斯欧公司 用于治疗癌症的Dbait分子与激酶抑制剂的组合
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KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
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Also Published As

Publication number Publication date
DK1109785T3 (da) 2003-04-22
CA2330756A1 (en) 1999-11-11
CN1310705A (zh) 2001-08-29
WO1999057117A2 (de) 1999-11-11
NZ507735A (en) 2003-04-29
HUP0102563A3 (en) 2003-04-28
PL346840A1 (en) 2002-02-25
IL139056A0 (en) 2001-11-25
EP1109785A2 (de) 2001-06-27
CN1151127C (zh) 2004-05-26
US6812243B2 (en) 2004-11-02
HUP0102563A2 (hu) 2001-11-28
WO1999057117A3 (de) 2001-04-12
HK1038354A1 (en) 2002-03-15
CA2330756C (en) 2007-10-02
SK16352000A3 (sk) 2002-07-02
AU752464B2 (en) 2002-09-19
CZ20003960A3 (cs) 2002-04-17
EP1109785B1 (de) 2003-01-02
NO20005448L (no) 2000-10-27
AU4497599A (en) 1999-11-23
NO317261B1 (no) 2004-09-27
BR9911017A (pt) 2001-02-06
TR200003206T2 (tr) 2001-07-23
US20030008898A1 (en) 2003-01-09
BG104996A (en) 2001-07-31
US6407102B1 (en) 2002-06-18
DE59903921D1 (de) 2003-02-06
NO20005448D0 (no) 2000-10-27
JP2002514572A (ja) 2002-05-21
ATE230394T1 (de) 2003-01-15

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