ES2479718T3 - Nuevos derivados de tetrahidroquinolina - Google Patents

Nuevos derivados de tetrahidroquinolina Download PDF

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Publication number
ES2479718T3
ES2479718T3 ES11730935.1T ES11730935T ES2479718T3 ES 2479718 T3 ES2479718 T3 ES 2479718T3 ES 11730935 T ES11730935 T ES 11730935T ES 2479718 T3 ES2479718 T3 ES 2479718T3
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Spain
Prior art keywords
alkyl
carbon
alone
hydrogen
combination
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Active
Application number
ES11730935.1T
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English (en)
Inventor
Li Chen
Lichun Feng
Yun He
Mengwei Huang
Yongfu Liu
Hongying Yun
Mingwei Zhou
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F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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Publication of ES2479718T3 publication Critical patent/ES2479718T3/es
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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • 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
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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 two hetero rings
    • C07D401/06—Heterocyclic 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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/12—Heterocyclic 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 chain containing hetero atoms as chain links
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Quinoline Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Un compuesto de la fórmula (I) en donde, A1, se encuentra ausente, o es -CH2-, A2, es nitrógeno ó -CH-; A3, se encuentra ausente ó es -C(CH3)2; R1, es hidroxilo ó NR11R12; R1 y R2, se seleccionan, de una forma independiente, de entre alquilo, alquenilo y fenilo; ó R1 y R2, conjuntamente con el átomo de carbono al cual se encuentran éstas unidas, forman cicloalquilo; R4, R5, R6, R7 y R8, se seleccionan, de una forma independiente, de entre hidrógeno, alquilo, alcoxi, halógeno, alquilsufonilo, morfolinilo, piperazinilo y alquilpiperazinilo; R9, es hidrógeno, alquilo, bencilo ó alquilaminocarbonilo; R10, es hidrógeno ó halógeno R11 y R12, se seleccionan, de una forma independiente, de entre hidrógeno, alquilo, cicloalquilo, hidroxialquilo, oxetanilo, alquilpiperidinilo, 1,1-dioxotiaminomorfolinilalquilo ó bencilpiperidinilo; ó R11 y R12, conjuntamente con el átomo de nitrógeno al cual se encuentran éstas unidas, forman morfolinilo, piperazinilo, alquilpiperazinilo, alquilsulfonilpiperazinilo, alquilhidroxipirrolidinilo, ó hidroxialquilpirrolidinilo, o una sal o un éster de éste, farmacéuticamente aceptable. en donde, "alquilo", solo o en combinación, es un significa un grupo alquilo de cadena lineal o ramificada, saturado, el cual contiene de 1 a 8 átomos de carbono. "alquenilo", solo o en combinación, es un grupo alquilo, tal y como éste se ha definido anteriormente, arriba, en donde, uno o más eslabones individuales carbono - carbono, se encuentra reemplazado por un doble enlace carbono >= carbono. "alcoxi", solo o en combinación, significa un grupo alquilo-O-, en donde, "alquilo", es tal y como éste se define anteriormente, arriba. "cicloalquilo", solo o en combinación, es un anillo de carbono, saturado, el cual contiene de 3 a 7 átomos de carbono, conteniendo, de una forma preferible, de 3 a 6 átomos de carbono, como por ejemplo, ciclopropilo, ciclobutilo, ciclopentilo, ciclohexilo, cicloheptilo, y por el estilo. Los grupos cicloalquilo preferidos, son ciclopropilo, ciclopentilo y ciclohexilo.

Description

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E11730935
09-07-2014
Ejemplo 16
8,61
Ejemplo 17
4,54
Ejemplo 18
4,58
Ejemplo 19
2,13
Ejemplo 20
3,31
Ejemplo 22
5,35
Ejemplo 23
7,02
Ejemplo 25
4,83
Ejemplo 26
2,1
Ejemplo 27
1,49
Ejemplo 28
11,36
Ejemplo 30
2,47
Ejemplo 31
2,58
Ejemplo 32
1,24
Ejemplo 33
13,58
Ejemplo 34
2,71
Ejemplo 35
6,88
Ejemplo 36
5,63
Ejemplo 37
13,91
Ejemplo 38
2,38
Ejemplo 39
4,95
Ejemplo 40
3,69
Ejemplo 41
5,17
Ejemplo 42
3,77
Ejemplo 43
5,86
Ejemplo 44
3,02
Ejemplo 45
1,76
Ejemplo 46
7,62
Ejemplo 47
11,41
Ejemplo 48
2,1
Ejemplo 49
3,23
Ejemplo 52
4,84
40
imagen39

Claims (1)

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ES11730935.1T 2010-07-02 2011-06-29 Nuevos derivados de tetrahidroquinolina Active ES2479718T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
WOPCT/CN2010/074931 2010-07-02
CN2010074931 2010-07-02
PCT/EP2011/060864 WO2012001020A1 (en) 2010-07-02 2011-06-29 Novel tetrahydroquinoline derivatives

Publications (1)

Publication Number Publication Date
ES2479718T3 true ES2479718T3 (es) 2014-07-24

Family

ID=44583531

Family Applications (1)

Application Number Title Priority Date Filing Date
ES11730935.1T Active ES2479718T3 (es) 2010-07-02 2011-06-29 Nuevos derivados de tetrahidroquinolina

Country Status (10)

Country Link
US (1) US8592594B2 (es)
EP (1) EP2588458B1 (es)
JP (1) JP2013534928A (es)
KR (1) KR20130088843A (es)
BR (1) BR112012033599A2 (es)
CA (1) CA2803478A1 (es)
ES (1) ES2479718T3 (es)
MX (1) MX2012014647A (es)
RU (1) RU2013102031A (es)
WO (1) WO2012001020A1 (es)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8889730B2 (en) 2012-04-10 2014-11-18 Pfizer Inc. Indole and indazole compounds that activate AMPK
CA2905242C (en) 2013-03-15 2016-11-29 Pfizer Inc. Indole compounds that activate ampk
WO2015103480A1 (en) 2014-01-02 2015-07-09 Massachusetts Eye & Ear Infirmary Treating ocular neovascularization
BR112022023359A2 (pt) 2020-05-19 2023-04-18 Kallyope Inc Ativadores de ampk
EP4172162A1 (en) 2020-06-26 2023-05-03 Kallyope, Inc. Ampk activators
US20240182468A1 (en) * 2022-10-18 2024-06-06 Pfizer Inc. Compounds for the activation of ampk

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP3209568B2 (ja) 1991-04-16 2001-09-17 杏林製薬株式会社 新規環状アミノフェニル酢酸誘導体、その製造法及びそれらを有効成分とする免疫応答の修飾剤
US7138412B2 (en) 2003-03-11 2006-11-21 Bristol-Myers Squibb Company Tetrahydroquinoline derivatives useful as serine protease inhibitors
US8344137B2 (en) * 2010-04-14 2013-01-01 Hoffman-La Roche Inc. 3,3-dimethyl tetrahydroquinoline derivatives

Also Published As

Publication number Publication date
MX2012014647A (es) 2013-02-07
US20120004218A1 (en) 2012-01-05
EP2588458A1 (en) 2013-05-08
JP2013534928A (ja) 2013-09-09
BR112012033599A2 (pt) 2016-11-29
EP2588458B1 (en) 2014-06-04
CA2803478A1 (en) 2012-01-05
RU2013102031A (ru) 2014-08-10
KR20130088843A (ko) 2013-08-08
WO2012001020A1 (en) 2012-01-05
US8592594B2 (en) 2013-11-26

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