AR036716A1 - Un compuesto derivado de bencimidazolidinona, metodos que lo utilizan, una composicion farmaceutica que lo comprende y uso de dicho compuesto o composicion - Google Patents

Un compuesto derivado de bencimidazolidinona, metodos que lo utilizan, una composicion farmaceutica que lo comprende y uso de dicho compuesto o composicion

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Publication number
AR036716A1
AR036716A1 ARP020103714A ARP020103714A AR036716A1 AR 036716 A1 AR036716 A1 AR 036716A1 AR P020103714 A ARP020103714 A AR P020103714A AR P020103714 A ARP020103714 A AR P020103714A AR 036716 A1 AR036716 A1 AR 036716A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
group
cycloalkyl
alkyl
alkylidene
Prior art date
Application number
ARP020103714A
Other languages
English (en)
Inventor
Nicholas Michael Kelly
Kristian Norup Koch
Bo-Ragnar Tolf
Original Assignee
Acadia Pharm Inc
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 Acadia Pharm Inc filed Critical Acadia Pharm Inc
Publication of AR036716A1 publication Critical patent/AR036716A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/423—Oxazoles condensed with carbocyclic rings
    • 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
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • A61P25/14—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
    • A61P25/24—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
    • A61P27/00—Drugs for disorders of the senses
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • 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
    • C07D209/30—Indoles; 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
    • C07D209/32—Oxygen atoms
    • C07D209/34—Oxygen atoms in position 2
    • 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
    • C07D209/30—Indoles; 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
    • C07D209/32—Oxygen atoms
    • C07D209/38—Oxygen atoms in positions 2 and 3, e.g. isatin
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • C07D235/26—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/58—Benzoxazoles; Hydrogenated benzoxazoles 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 in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/68—Benzothiazoles 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 in position 2
    • 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
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    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Abstract

Un compuesto derivado de bencimidazolidinona de Fórmula (1), o una sal farmacéuticamente aceptable o prodroga de la misma, donde: X se selecciona entre el grupo que consiste en C, O, N y S; Z se selecciona entre el grupo que consiste en CH y N; Y se selecciona entre el grupo que consiste en =O, =N y =S o tautómeros de los mismos; SPU es una unidad espaciadora que provee una distancia d entre Z y N, donde -SPU- es un bi-radical seleccionado entre el grupo que consiste en -(CR6R7)n-A- y cicloalquilo C3-8, donde n está comprendido entre 1 y 5, como ser 1, 2, 3, 4 ó 5 y A está ausente o es un cicloalquilo C3-8 opcionalmente sustituido; N, junto con R1 y R2, forman un anillo heterocíclico donde dicho anillo heterocíclico se selecciona entre el grupo que consiste en perhidroazocina, perhidroazepina, piperidina, pirrolidina, azetidina, aziridina y 8-azabiciclo[3.2.1]-octano y donde el anillo heterocíclico está sustituido por uno o más sustituyentes R4 seleccionados entre el grupo que consiste en halógeno, alquilo C1-8, cicloalquilo C3-8, alcoxi C1-8, alquilcarbonilo C1-8, alquilideno C1-8, alquenilo C2-8, alquinilo C2-8, alquiloxi-imino C1-6, y alquiloxiamino C1-6, cada uno de los cuales puede ser opcionalmente sustituido por un sustituyente R5 y donde al menos uno de dichos sustituyentes R4 es R4' que se selecciona entre el grupo que consiste en alquilo C1-8, cicloalquilo C3-8, alcoxi C1-8, alquilcarbonilo C1-8, alquilideno C1-8, cada uno de los cuales puede ser opcionalmente sustituido por un sustituyente R5; R5 se selecciona entre el grupo que consiste en hidrógeno, halógeno, hidroxi, alquilo C1-8, alcoxi C1-8, cicloalquilo C3-8, heterociclilo C3-8, alquilcarbonilo C1-8, alquilideno C1-8, alquenilo C2-8 y alquinilo C2-8; Rx puede estar ausente o seleccionarse entre el grupo que consiste en hidrógeno, alquilo C1-8 opcionalmente sustituido, cicloalquilo C3-8 opcionalmente sustituido, alquenilo C2-8 opcionalmente sustituido, alquinilo C2-8 opcionalmente sustituido, -CH2-N(R5)(R5), CH2-OR5, CH2-SR5, CH2-O-C(=O)R5, CH2-O-C(=S)R5; R3 puede estar presente entre 0 y 4 veces y seleccionarse entre el grupo que consiste en halógeno, hidroxi, alquilo C1-8 opcionalmente sustituido, alcoxi C1-8, alquilideno C1-8 opcionalmente sustituido, alquenilo C2-8 opcionalmente sustituido, alquinilo C2-8 opcionalmente sustituido, arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, cicloalquilo C3-8 opcionalmente sustituido, heterociclilo C3-8 opcionalmente sustituido y alquilcarbonilo C1-8 opcionalmente sustituido; cada R6 y cada R7 se seleccionan opcional e independientemente, entre el grupo que consiste en hidrógeno, halógeno, hidroxi, alquilo C1-8 opcionalmente sustituido, alcoxi C1-8, alquilideno C1-8 opcionalmente sustituido, alquenilo C2-8 opcionalmente sustituido, alquinilo C2-8 opcionalmente sustituido, arilo opcionalmente sustituido, heteroarilo, opcionalmente sustituido, cicloalquilo C3-8 opcionalmente sustituido, heterociclilo C3-8 opcionalmente sustituido y alquilcarbonilo C1-8 opcionalmente sustituido. Métodos que lo utilizan, una composición farmacéutica que lo comprende y uso del compuesto y de la composición. El compuesto derivado de bencimidazolidinona aumenta la senalización de acetilcolina o el efecto en el cerebro. Es un agonista muscarínico altamente selectivo, particularmente para los sub-tipos receptores M1 y/o M4. El compuesto derivado de bencimidazolidinona es útil para el tratamiento de por ejemplo psicosis.
ARP020103714A 2001-10-02 2002-10-02 Un compuesto derivado de bencimidazolidinona, metodos que lo utilizan, una composicion farmaceutica que lo comprende y uso de dicho compuesto o composicion AR036716A1 (es)

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US32675401P 2001-10-02 2001-10-02

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US (6) US7087593B2 (es)
EP (1) EP1432420B1 (es)
JP (1) JP4347047B2 (es)
KR (2) KR20040047877A (es)
CN (1) CN1561212A (es)
AR (1) AR036716A1 (es)
AT (1) ATE516030T1 (es)
AU (1) AU2002327810B2 (es)
BR (1) BR0213611A (es)
CA (1) CA2457647A1 (es)
MX (1) MXPA04003103A (es)
NO (1) NO20041317L (es)
NZ (1) NZ531550A (es)
RU (1) RU2288919C2 (es)
TW (1) TWI310034B (es)
WO (1) WO2003028650A2 (es)
ZA (1) ZA200402609B (es)

Families Citing this family (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7087593B2 (en) * 2001-10-02 2006-08-08 Acadia Pharmaceuticals Inc. Benzimidazolidinone derivatives as muscarinic agents
US6951849B2 (en) * 2001-10-02 2005-10-04 Acadia Pharmaceuticals Inc. Benzimidazolidinone derivatives as muscarinic agents
WO2004089942A2 (en) * 2001-10-02 2004-10-21 Acadia Pharmaceuticals Inc. Benzimidazolidinone derivatives as muscarinic agents
MXPA04010965A (es) * 2002-05-07 2005-01-25 Neurosearch As Derivados de etinilo azaciclico novedoso.
US20050130961A1 (en) * 2003-03-28 2005-06-16 Davis Robert E. Muscarinic M1 receptor agonists for pain management
US7157471B2 (en) * 2003-08-25 2007-01-02 Boehringer Ingelheim International Gmbh Haloalkyl- and piperidine-substituted benzimidazole-derivatives
JP2009506069A (ja) 2005-08-26 2009-02-12 ブレインセルス，インコーポレイティド ムスカリン性受容体調節による神経発生
EP2258357A3 (en) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenesis with acetylcholinesterase inhibitor
ATE492537T1 (de) * 2005-09-30 2011-01-15 Glaxo Group Ltd Verbindungen mit aktivität am m1-rezeptor und ihre verwendung in der medizin
EP1937670A1 (en) * 2005-09-30 2008-07-02 Glaxo Group Limited Benzimidazolones which have activity at m1 receptor
EP1960389B1 (en) * 2005-09-30 2012-08-15 Glaxo Group Limited Compounds which have activity at m1 receptor and their uses in medicine
AU2006304787A1 (en) 2005-10-21 2007-04-26 Braincells, Inc. Modulation of neurogenesis by PDE inhibition
US20070112017A1 (en) 2005-10-31 2007-05-17 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
US20090012101A1 (en) * 2005-12-27 2009-01-08 University Of Toledo Mucarinic Agonists and Methods of Use Thereof
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
GB0607949D0 (en) * 2006-04-21 2006-05-31 Minster Res The Ltd Mono and combination therapy
JP2009536667A (ja) 2006-05-09 2009-10-15 ブレインセルス，インコーポレイティド ５ｈｔ受容体介在性の神経新生
EP2021000A2 (en) 2006-05-09 2009-02-11 Braincells, Inc. Neurogenesis by modulating angiotensin
TW200813018A (en) * 2006-06-09 2008-03-16 Astrazeneca Ab Novel compounds
US7998971B2 (en) 2006-09-08 2011-08-16 Braincells Inc. Combinations containing a 4-acylaminopyridine derivative
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
US20100210633A1 (en) * 2006-10-12 2010-08-19 Epix Delaware, Inc. Carboxamide compounds and their use
GB0718415D0 (en) * 2007-09-20 2007-10-31 Glaxo Group Ltd Compounds
JP2010539217A (ja) * 2007-09-20 2010-12-16 グラクソ グループ リミテッド Ｍ１受容体にて活性を有する化合物および医薬としてのそれらの使用
AR068480A1 (es) * 2007-09-20 2009-11-18 Glaxo Group Ltd Compuesto de 4-heteroaril-piperidinil-n-substituido su uso para la preparacion de un medicamento util para el tratamiento de una afeccion en el que seria beneficioso el agonismo de un receptor muscarinico m1 y composicion farmaceutica que lo comprende
US8569282B2 (en) 2007-12-11 2013-10-29 Cytopathfinder, Inc. Carboxamide compounds and their use
US20110294835A1 (en) 2008-05-15 2011-12-01 The Board Of Trustees Of The University Of Illinois Muscarinic Agonists as Cognitive Enhancers
US20100158829A1 (en) * 2008-12-24 2010-06-24 Conopco, Inc., D/B/A Unilever Method and Composition for Color Modulation
WO2010099217A1 (en) 2009-02-25 2010-09-02 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
US20100286136A1 (en) * 2009-05-08 2010-11-11 Simon Jones Dihydronaphthyridinyl and related compounds for use in treating ophthalmological disorders
ES2714384T3 (es) 2010-10-06 2019-05-28 Glaxosmithkline Llc Derivados de bencimidazol como inhibidores de PI3 quinasa
US9549928B2 (en) 2011-04-29 2017-01-24 The University Of Toledo Muscarinic agonists as enhancers of cognitive flexibility
JP6393524B2 (ja) * 2014-06-05 2018-09-19 ロート製薬株式会社 保湿剤
WO2016022644A1 (en) * 2014-08-06 2016-02-11 Merck Sharp & Dohme Corp. Heterocyclic cgrp receptor antagonists
WO2017015272A1 (en) 2015-07-20 2017-01-26 Acadia Pharmaceuticals Inc. Methods for preparing n-(4-fluorobenzyl)-n-(1-methylpiperidin-4-yl)-n'-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and polymorphic form c
US10953000B2 (en) 2016-03-25 2021-03-23 Acadia Pharmaceuticals Inc. Combination of pimavanserin and cytochrome P450 modulators
WO2017165635A1 (en) 2016-03-25 2017-09-28 Acadia Pharmaceuticals Inc. Combination of pimavanserin and cytochrome p450 modulators
US20190117636A1 (en) * 2016-03-29 2019-04-25 Acadia Pharmaceuticals Inc. 5-ht2a serotonin receptor inverse agonists or antagonists for use in reducing amyloid-beta peptides and accumulation of amyloid plaques
EP3558311A1 (en) 2016-12-20 2019-10-30 Acadia Pharmaceuticals Inc. Pimavanserin alone or in combination for use in the treatment of alzheimer's disease psychosis
EP3615028A1 (en) 2017-04-28 2020-03-04 Acadia Pharmaceuticals Inc. Pimavanserin for treating impulse control disorder
WO2019046167A1 (en) 2017-08-30 2019-03-07 Acadia Pharmaceuticals Inc. PIMAVANSERIN FORMULATIONS
US11034669B2 (en) 2018-11-30 2021-06-15 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
TW202202493A (zh) * 2020-05-06 2022-01-16 美商默沙東藥廠 Il4i1抑制劑及使用方法
WO2023114224A1 (en) 2021-12-13 2023-06-22 Sage Therapeutics, Inc. Combination of muscarinic receptor positive modulators and nmda positive allosteric modulators

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH407121A (de) 1962-03-30 1966-02-15 Geigy Ag J R Verfahren zur Herstellung von neuen Piperidinderivaten
US4371388A (en) * 1980-01-25 1983-02-01 Monsanto Company 3-Substituted aminoalkyl-2-benzothiazolinones as plant growth regulants
US4254127A (en) 1980-04-03 1981-03-03 Janssen Pharmaceutica, N.V. 1,3-Dihydro-1-[(1-piperidinyl)alkyl]-2H-benzimidazol-2-one derivatives
US4943580A (en) * 1987-03-09 1990-07-24 Janssen Pharmaceutica N.V. Anti-histaminic benzimidazole, imidazopyridine and purine derivatives
US4861889A (en) * 1988-03-14 1989-08-29 Hoechst-Roussel Pharmaceuticals, Inc. 3-(2,3,4,5,6-pentafluorophenoxy)-8-azabicyclo[3.2.1]octanes
IL110298A (en) 1993-07-13 1999-04-11 Brann Mark Robert Identification of ligands by selective amplification of cells transfected with receptors
JP3916092B2 (ja) 1993-09-17 2007-05-16 杏林製薬株式会社 イミダゾリジノン誘導体とその酸付加塩及び老年性痴呆症の治療薬
JP3916093B2 (ja) 1993-09-17 2007-05-16 杏林製薬株式会社 光学活性イミダゾリジノン誘導体とその製造方法
JP2002515008A (ja) 1994-10-27 2002-05-21 メルク エンド カンパニー インコーポレーテッド ムスカリン・アンタゴニスト
EP0816362A4 (en) * 1995-03-22 1998-07-08 Taisho Pharmaceutical Co Ltd THIAZOLE DERIVATIVES
AU7528696A (en) 1995-10-31 1997-05-22 Merck & Co., Inc. Muscarine antagonists
AU7478496A (en) 1995-10-31 1997-05-22 Merck & Co., Inc. Muscarine antagonists
AU7478396A (en) 1995-10-31 1997-05-22 Merck & Co., Inc. Muscarine agonists
US5756508A (en) 1995-10-31 1998-05-26 Merck & Co., Inc. Muscarine antagonists
US5718912A (en) 1996-10-28 1998-02-17 Merck & Co., Inc. Muscarine agonists
AU2307999A (en) 1997-12-23 1999-07-12 Alcon Laboratories, Inc. Muscarinic agents and use thereof to treat glaucoma, myopia and various other conditions
US6569956B1 (en) * 1999-12-22 2003-05-27 Basf Corporation Hyperbranched polyol macromolecule, method of making same, and coating composition including same
JP4664564B2 (ja) * 2000-03-06 2011-04-06 アカディア ファーマシューティカルズ，インコーポレーテッド セロトニン関連疾患の治療に使用する含窒素環式化合物
DE60109148T2 (de) 2000-04-28 2006-01-05 Acadia Pharmaceuticals Inc., San Diego Muscarinrezeptoren
WO2002024662A1 (en) 2000-09-19 2002-03-28 Boehringer Ingelheim Pharma Gmbh & Ko. Kg New benzimidazolone derivatives displaying affinity at the serotonin and dopamine receptors
US6586435B2 (en) 2000-09-19 2003-07-01 Boehringer Ingelheim Pharma Kg Benzimidazolone derivatives displaying affinity at the serotonin and dopamine receptors
US7087593B2 (en) * 2001-10-02 2006-08-08 Acadia Pharmaceuticals Inc. Benzimidazolidinone derivatives as muscarinic agents
US6951849B2 (en) * 2001-10-02 2005-10-04 Acadia Pharmaceuticals Inc. Benzimidazolidinone derivatives as muscarinic agents

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