AR083595A1 - Derivados de indol y el proceso para su preparacion - Google Patents

Derivados de indol y el proceso para su preparacion

Info

Publication number
AR083595A1
AR083595A1 ARP110103997A ARP110103997A AR083595A1 AR 083595 A1 AR083595 A1 AR 083595A1 AR P110103997 A ARP110103997 A AR P110103997A AR P110103997 A ARP110103997 A AR P110103997A AR 083595 A1 AR083595 A1 AR 083595A1
Authority
AR
Argentina
Prior art keywords
hydrogen
alkyl
nhr
cycloalkyl
alkenyl
Prior art date
Application number
ARP110103997A
Other languages
English (en)
Original Assignee
Merz Pharma Gmbh & Co Kgaa
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Merz Pharma Gmbh & Co Kgaa filed Critical Merz Pharma Gmbh & Co Kgaa
Publication of AR083595A1 publication Critical patent/AR083595A1/es

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Classifications

    • 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
    • A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34—Tobacco-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • A61P27/16—Otologicals
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D209/20—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals substituted additionally by nitrogen atoms, e.g. tryptophane
    • 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
    • C07D405/06—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 carbon chain containing only aliphatic carbon atoms

Abstract

Los compuestos son inhibidores potentes de la polimerización del péptido Ab y se pueden utilizar para el tratamiento de por ejemplo la enfermedad de Alzheimer o trastornos oculares.Reivindicación 1: Un compuesto de la fórmula (1) en donde R1 es hidrógeno, alquilo C1-6, cicloalquilo C3-12, -C(O)-R o -C(O)OR; R2 es hidrógeno, alquilo C1-6 o cicloalquilo C3-12; R3 es-OR, -NHR o -NR2; R4 es hidrógeno, halógeno, ciano, trifluorometilo, alquilo C1-6, arilo C6-10, heteroarilo, -OR, -NHR, -NRR, -C(O)-R o -C(O)-NHR; R5 es hidrógeno, alquilo C1-6 o alquenilo C2-6; R6 es hidrógeno, alquilo C1-6 o alquenilo C2-6; o R5 y R6 conjuntamente con los átomos de carbono que los portan forman un sistema cíclico con 3 a 6 átomos de carbono; R es hidrógeno, alquilo C1-6, o arilo C6-10; X es un grupo -C(O)CH2-, -CH(OH)CH2-, -CH=CH- o -CH2-NH-C(O)-; R7 es hidrógeno, metilo, etilo, propilo o ciclopropilo; o un isómero óptico, sal farmacéuticamente aceptable, hidrato, solvato, o polimorfo de los mismos.
ARP110103997A 2010-10-29 2011-10-28 Derivados de indol y el proceso para su preparacion AR083595A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US40792410P 2010-10-29 2010-10-29
EP10189377 2010-10-29

Publications (1)

Publication Number Publication Date
AR083595A1 true AR083595A1 (es) 2013-03-06

Family

ID=43768707

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110103997A AR083595A1 (es) 2010-10-29 2011-10-28 Derivados de indol y el proceso para su preparacion

Country Status (13)

Country Link
US (2) US9309196B2 (es)
EP (1) EP2632897B1 (es)
JP (1) JP5848768B2 (es)
KR (1) KR20130132829A (es)
CN (1) CN103282349A (es)
AR (1) AR083595A1 (es)
AU (1) AU2011322565A1 (es)
BR (1) BR112013010549A2 (es)
CA (1) CA2814905A1 (es)
IL (1) IL225771A0 (es)
MX (1) MX2013004760A (es)
RU (1) RU2013124827A (es)
WO (1) WO2012055945A1 (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2044951A1 (en) 2007-10-02 2009-04-08 Merz Pharma GmbH & Co. KGaA The use of substances for the treatment of loss of eyesight in humans with glaucoma and other degenerative eye diseases
EP2632897B1 (en) 2010-10-29 2014-10-01 Merz Pharma GmbH & Co. KGaA Indole derivatives and process for their preparation
TW201412325A (zh) 2012-06-20 2014-04-01 梅茲製藥有限兩合公司 用於治療患有青光眼及其他退化性眼疾之人類視力喪失的間隔醫療
WO2017218697A1 (en) * 2016-06-17 2017-12-21 The Trustees Columbia University In The City Of New York Identification of compounds that target the rna-binding protein tia-1 an important regulator of stress vulnerability in both mice and humans
EP3774722A1 (en) * 2018-04-04 2021-02-17 Epiodyne, Inc. Opioid receptor modulators and products and methods related thereto
BR112021021267A2 (pt) 2019-04-24 2021-12-21 Galimedix Therapeutics Inc Compostos de indol para uso na neurorrestauração
EP4000623A1 (en) 2020-11-11 2022-05-25 Consejo Superior De Investigaciones Científicas 5-(2-(1h-indol-3-yl))-ethyl)- piperazin-2-one derivatives for use in the treatment of viral infections by viruses of the family coronaviridae

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH603545A5 (es) 1972-04-20 1978-08-31 Merz & Co
DE2856393C2 (de) 1978-12-27 1983-04-28 Merz + Co GmbH & Co, 6000 Frankfurt Arzneimittel zur Behandlung von Morbus Parkinson
US4743585A (en) * 1986-11-21 1988-05-10 Warner-Lambert Company Renin inhibitors
DE10299048I2 (de) 1989-04-14 2006-07-13 Merz Pharma Gmbh & Co Kgaa Verwendung von Adamantan-Derivaten zur Pr{vention und Behandlung der cerebralen Isch{mie
US7384910B2 (en) 1997-10-08 2008-06-10 Castillo Gerardo M Small peptides for the treatment of Alzheimer's disease and other beta-amyloid protein fibrillogenesis disorders
WO2005000193A2 (en) 2003-06-30 2005-01-06 Tel Aviv University Future Technology Development L.P. Peptides antibodies directed thereagainst and methods using same for diagnosing and treating amyloid-associated diseases
EP1534310A4 (en) 2002-01-31 2006-05-31 Univ Tel Aviv Future Tech Dev PEPTIDES, ANTIBODIES AGAINST DISEASES ASSOCIATED WITH AMYLOID AND METHODS USING SAID PEPTIDES AND ANTIBODIES TO DIAGNOSE AND TREAT THESE DISEASES
US20040072806A1 (en) 2002-03-15 2004-04-15 Zhi-Xing Yao Neuroprotective spirostenol pharmaceutical compositions
DE60327565D1 (de) 2003-12-19 2009-06-18 Ericsson Telefon Ab L M Relaisstation und verfahren zur ermöglichung einer zuverlässigen digitalen kommunikation zwischen zwei knoten in einem drahtlosen netzwerk auf relais-basis
EP2044951A1 (en) 2007-10-02 2009-04-08 Merz Pharma GmbH & Co. KGaA The use of substances for the treatment of loss of eyesight in humans with glaucoma and other degenerative eye diseases
EP2632897B1 (en) 2010-10-29 2014-10-01 Merz Pharma GmbH & Co. KGaA Indole derivatives and process for their preparation

Also Published As

Publication number Publication date
EP2632897B1 (en) 2014-10-01
US9629824B2 (en) 2017-04-25
US20160220535A1 (en) 2016-08-04
CN103282349A (zh) 2013-09-04
US20130289090A1 (en) 2013-10-31
BR112013010549A2 (pt) 2017-10-24
JP2013540796A (ja) 2013-11-07
AU2011322565A1 (en) 2013-05-30
JP5848768B2 (ja) 2016-01-27
WO2012055945A1 (en) 2012-05-03
MX2013004760A (es) 2013-07-02
IL225771A0 (en) 2013-06-27
RU2013124827A (ru) 2014-12-10
EP2632897A1 (en) 2013-09-04
US9309196B2 (en) 2016-04-12
KR20130132829A (ko) 2013-12-05
CA2814905A1 (en) 2012-05-03

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