BRPI0513932A - derivados de indol-2-carboxamidina como antagonistas de receptores de nmda - Google Patents

derivados de indol-2-carboxamidina como antagonistas de receptores de nmda

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Publication number
BRPI0513932A
BRPI0513932A BRPI0513932-5A BRPI0513932A BRPI0513932A BR PI0513932 A BRPI0513932 A BR PI0513932A BR PI0513932 A BRPI0513932 A BR PI0513932A BR PI0513932 A BRPI0513932 A BR PI0513932A
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BR
Brazil
Prior art keywords
atom
carboxamidine derivatives
formula
nmda receptor
indole
Prior art date
Application number
BRPI0513932-5A
Other languages
English (en)
Inventor
Istvan Borza
Csilla Horvath
Sandor Farkas
Jozsef Nagy
Sandor Kolok
Original Assignee
Richter Gedeon Vegyeszet
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 Richter Gedeon Vegyeszet filed Critical Richter Gedeon Vegyeszet
Publication of BRPI0513932A publication Critical patent/BRPI0513932A/pt

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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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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 chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic 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
    • A61K31/403Heterocyclic 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
    • A61K31/404Indoles, e.g. pindolol
    • A61K31/405Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • AHUMAN NECESSITIES
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00Drugs for disorders of the nervous system
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00Drugs for disorders of the nervous system
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
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    • AHUMAN NECESSITIES
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    • A61P27/00Drugs for disorders of the senses
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    • 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
    • C07D209/30Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • C07D405/12Heterocyclic 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

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Abstract

DERIVADOS DE INDOL-2-CARBOXAMIDINA COMO ANTAGONISTAS DE RECEPTORES DE NMDA A presente invenção se refere, portanto, primeiro a novos derivados de indol-2-carboxamidina da fórmula (I): em que o significado de: x é átomo de hidrogênio ou de halogênio, C~ 1~-C~ 4~ alquila, C~ 1~-C~ 4~ alcóxi, grupo trifluorometila; Y, V e Z independentemente são átomo de hidrogênio ou átomo de halogênio, hidróxi, ciano, C~ 1~-C~ 4~ alquilsulfonamido opcionalmente é substituído por um átomo halogênio ou átomos de halogênio, C~1 ~-C~ 4~ alcanoilamido opcionalmente substituído por um átomo de halogênio ou átomos de halogênio, trifluorometila, trifluorometóxi, C~ 1-~C~ 4~ alquila, grupo C~ 1~-C~ 4~ alcóxi ou grupos V e Z vizinhos, em dado caso junto com um ou mais hétero átomo idêntico ou diferente e -CH= e/ou grupos -CH~ 2~- podem formar um anel homo- ou heterocíclico com 4-7 elementos opcionalmente substituído, de preferência anel de dioxalano, benzeno, anel de dioxolano, A, B e C, independentemente, são átomo de carbono substituído ou um deles é átomo de nitrogênio e os seus sais. Outros objetivos da invenção são os processos para produção de derivados de indol-2-carboxamidina da fórmula (I) e a fabricação farmacêutica de medicamentos contendo esses compostos, bem como o processo de tratamentos com esses compostos o que significa administração, a um mamífero a ser tratado - incluindo um ser humano - de uma quantidade/quantidades eficazes de novos derivados de indol-2-carboxamidina da fórmula (I) da presente invenção como tal ou como um medicamento. Os novos derivados indol-2-carboxamidina da fórmula (1) da presente invenção são antagonistas altamente eficazes e seletivos do receptor de NMDA e, além disso, a maioria dos compostos são antagonistas seletivos do subtipo NR2B de receptor de NMDA.
BRPI0513932-5A 2004-07-29 2005-07-21 derivados de indol-2-carboxamidina como antagonistas de receptores de nmda BRPI0513932A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
HU0401523A HUP0401523A3 (en) 2004-07-29 2004-07-29 Indole-2-carboxamide derivatives, pharmaceutical compositions containing them and process for producing them
PCT/HU2005/000078 WO2006010965A1 (en) 2004-07-29 2005-07-21 Indole-2 -carboxamidine derivatives as nmda receptor antagonists

Publications (1)

Publication Number Publication Date
BRPI0513932A true BRPI0513932A (pt) 2008-05-20

Family

ID=89985408

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0513932-5A BRPI0513932A (pt) 2004-07-29 2005-07-21 derivados de indol-2-carboxamidina como antagonistas de receptores de nmda

Country Status (21)

Country Link
US (1) US20090048303A1 (pt)
EP (1) EP1773770B1 (pt)
JP (1) JP2008508248A (pt)
KR (1) KR20070038502A (pt)
CN (1) CN1989103A (pt)
AP (1) AP2006003840A0 (pt)
AT (1) ATE427299T1 (pt)
AU (1) AU2005266160A1 (pt)
BR (1) BRPI0513932A (pt)
CA (1) CA2574155A1 (pt)
DE (1) DE602005013675D1 (pt)
EA (1) EA009981B1 (pt)
GE (1) GEP20094606B (pt)
HU (1) HUP0401523A3 (pt)
IL (1) IL179485A0 (pt)
MA (1) MA28815B1 (pt)
MX (1) MX2007001052A (pt)
NO (1) NO20071109L (pt)
TN (1) TNSN07016A1 (pt)
WO (1) WO2006010965A1 (pt)
ZA (1) ZA200700325B (pt)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7732162B2 (en) 2003-05-05 2010-06-08 Probiodrug Ag Inhibitors of glutaminyl cyclase for treating neurodegenerative diseases
EP2089383B1 (en) 2006-11-09 2015-09-16 Probiodrug AG 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases
US9126987B2 (en) 2006-11-30 2015-09-08 Probiodrug Ag Inhibitors of glutaminyl cyclase
AU2008220785B2 (en) 2007-03-01 2013-02-21 Vivoryon Therapeutics N.V. New use of glutaminyl cyclase inhibitors
US9656991B2 (en) 2007-04-18 2017-05-23 Probiodrug Ag Inhibitors of glutaminyl cyclase
PL2475428T3 (pl) 2009-09-11 2015-12-31 Probiodrug Ag Pochodne heterocykliczne jako inhibitory cyklazy glutaminowej
EP2536713A1 (en) 2010-02-16 2012-12-26 Pfizer Inc. (r)-4-((4-((4-(tetrahydrofuran-3-yloxy)benzo[d]isoxazol-3-yloxy)methyl)piperidin-1-yl)methyl)tetrahydro-2h-pyran-4-ol, a partial agonist of 5-ht4 receptors
US9181233B2 (en) 2010-03-03 2015-11-10 Probiodrug Ag Inhibitors of glutaminyl cyclase
DK2545047T3 (da) 2010-03-10 2014-07-28 Probiodrug Ag Heterocycliske inhibitorer af glutaminylcyclase (QC, EC 2.3.2.5)
WO2011131748A2 (en) 2010-04-21 2011-10-27 Probiodrug Ag Novel inhibitors
US9562038B2 (en) * 2010-11-18 2017-02-07 Yale University Bifunctional molecules with antibody-recruiting and entry inhibitory activity against the human immunodeficiency virus
EP2686313B1 (en) 2011-03-16 2016-02-03 Probiodrug AG Benzimidazole derivatives as inhibitors of glutaminyl cyclase
US9669030B2 (en) * 2012-05-22 2017-06-06 Autifony Therapeutics Limited Hydantoin derivatives as Kv3 inhibitors
JO3579B1 (ar) 2014-09-26 2020-07-05 Luc Therapeutics Inc مُعدِلات تفاغرية سالبة لمستقبل nr2b من المركب n-ألكيل أريل-5-أوكسي أريل-ثامن هيدرو-خماسي الحلقة [c] بيرول
WO2019022179A1 (ja) * 2017-07-28 2019-01-31 武田薬品工業株式会社 複素環化合物
PL3461819T3 (pl) 2017-09-29 2020-11-30 Probiodrug Ag Inhibitory cyklazy glutaminylowej
JP2021050161A (ja) 2019-09-25 2021-04-01 武田薬品工業株式会社 複素環化合物及びその用途

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9726388D0 (en) * 1997-12-12 1998-02-11 Cerebrus Ltd Chemical compounds
US6319944B1 (en) * 1999-05-10 2001-11-20 Merck & Co., Inc. Aryl amidines, compositions containing such compounds and methods of use
US6376530B1 (en) * 1999-05-10 2002-04-23 Merck & Co., Inc. Cyclic amidines useful as NMDA NR2B antagonists
GB0015488D0 (en) * 2000-06-23 2000-08-16 Merck Sharp & Dohme Therapeutic agents
HU227197B1 (en) * 2000-10-24 2010-10-28 Richter Gedeon Nyrt Nmda receptor antagonist carboxylic acid amide derivatives and pharmaceutical compositions containing them
JP2004253425A (ja) * 2003-02-18 2004-09-09 Tdk Corp 積層コンデンサ

Also Published As

Publication number Publication date
KR20070038502A (ko) 2007-04-10
WO2006010965A1 (en) 2006-02-02
US20090048303A1 (en) 2009-02-19
IL179485A0 (en) 2007-05-15
HUP0401523A2 (en) 2006-11-28
CA2574155A1 (en) 2006-02-02
ZA200700325B (en) 2008-05-28
HU0401523D0 (en) 2004-09-28
EA200700365A1 (ru) 2007-06-29
HUP0401523A3 (en) 2007-05-02
JP2008508248A (ja) 2008-03-21
MA28815B1 (fr) 2007-08-01
EA009981B1 (ru) 2008-04-28
DE602005013675D1 (de) 2009-05-14
AP2006003840A0 (en) 2006-12-31
AU2005266160A1 (en) 2006-02-02
NO20071109L (no) 2007-02-27
TNSN07016A1 (en) 2008-06-02
EP1773770B1 (en) 2009-04-01
ATE427299T1 (de) 2009-04-15
MX2007001052A (es) 2007-04-16
CN1989103A (zh) 2007-06-27
EP1773770A1 (en) 2007-04-18
GEP20094606B (en) 2009-02-10

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B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2158 DE 15/05/2012.