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 composicionInfo
- 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
Links
- 150000001875 compounds Chemical class 0.000 title abstract 5
- 239000000203 mixture Substances 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 8
- 125000000623 heterocyclic group Chemical group 0.000 abstract 6
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 5
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 abstract 5
- 125000003545 alkoxy group Chemical group 0.000 abstract 5
- 125000004448 alkyl carbonyl group Chemical group 0.000 abstract 5
- 125000001118 alkylidene group Chemical group 0.000 abstract 5
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 150000002367 halogens Chemical group 0.000 abstract 4
- 125000001424 substituent group Chemical group 0.000 abstract 4
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- SILNNFMWIMZVEQ-UHFFFAOYSA-N 1,3-dihydrobenzimidazol-2-one Chemical compound C1=CC=C2NC(O)=NC2=C1 SILNNFMWIMZVEQ-UHFFFAOYSA-N 0.000 abstract 2
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 abstract 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 abstract 2
- 125000000304 alkynyl group Chemical group 0.000 abstract 2
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000003107 substituted aryl group Chemical group 0.000 abstract 2
- DGGKXQQCVPAUEA-UHFFFAOYSA-N 8-azabicyclo[3.2.1]octane Chemical compound C1CCC2CCC1N2 DGGKXQQCVPAUEA-UHFFFAOYSA-N 0.000 abstract 1
- NOWKCMXCCJGMRR-UHFFFAOYSA-N Aziridine Chemical compound C1CN1 NOWKCMXCCJGMRR-UHFFFAOYSA-N 0.000 abstract 1
- 102000017927 CHRM1 Human genes 0.000 abstract 1
- 102000017924 CHRM4 Human genes 0.000 abstract 1
- 101150073075 Chrm1 gene Proteins 0.000 abstract 1
- 208000028017 Psychotic disease Diseases 0.000 abstract 1
- 101100107916 Xenopus laevis chrm4 gene Proteins 0.000 abstract 1
- OIPILFWXSMYKGL-UHFFFAOYSA-N acetylcholine Chemical compound CC(=O)OCC[N+](C)(C)C OIPILFWXSMYKGL-UHFFFAOYSA-N 0.000 abstract 1
- 229960004373 acetylcholine Drugs 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- ZSIQJIWKELUFRJ-UHFFFAOYSA-N azepane Chemical compound C1CCCNCC1 ZSIQJIWKELUFRJ-UHFFFAOYSA-N 0.000 abstract 1
- HONIICLYMWZJFZ-UHFFFAOYSA-N azetidine Chemical compound C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 abstract 1
- QXNDZONIWRINJR-UHFFFAOYSA-N azocane Chemical compound C1CCCNCCC1 QXNDZONIWRINJR-UHFFFAOYSA-N 0.000 abstract 1
- -1 benzimidazolidinone derivative compound Chemical class 0.000 abstract 1
- 210000004556 brain Anatomy 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 239000000472 muscarinic agonist Substances 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 230000011664 signaling Effects 0.000 abstract 1
- 125000006850 spacer group Chemical group 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
-
- 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
-
- C—CHEMISTRY; METALLURGY
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Ophthalmology & Optometry (AREA)
- Psychology (AREA)
- Pain & Pain Management (AREA)
- Anesthesiology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
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.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US32675401P | 2001-10-02 | 2001-10-02 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR036716A1 true AR036716A1 (es) | 2004-09-29 |
Family
ID=23273560
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP020103714A AR036716A1 (es) | 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 |
Country Status (17)
| Country | Link |
|---|---|
| US (6) | US7087593B2 (es) |
| EP (1) | EP1432420B1 (es) |
| JP (1) | JP4347047B2 (es) |
| KR (2) | KR100809569B1 (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 (46)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1432420B1 (en) * | 2001-10-02 | 2011-07-13 | 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 |
| US7378526B2 (en) | 2002-05-07 | 2008-05-27 | Neurosearch A/S | Azacyclic ethynyl derivatives |
| RU2358735C2 (ru) * | 2003-03-28 | 2009-06-20 | Акадиа Фармасьютикалз Инк. | Агонисты м1 мускариновых рецепторов для противоболевой терапии |
| US7157471B2 (en) * | 2003-08-25 | 2007-01-02 | Boehringer Ingelheim International Gmbh | Haloalkyl- and piperidine-substituted benzimidazole-derivatives |
| AR045843A1 (es) * | 2003-10-03 | 2005-11-16 | Solvay Pharm Bv | Derivados de bencimidazolonas y quinazolinonas sustituidas con hidronopol como agonistas en receptores orl 1 humanos |
| CA2620333A1 (en) * | 2005-08-26 | 2007-03-01 | Braincells, Inc. | Neurogenesis by muscarinic receptor modulation |
| EP2258357A3 (en) | 2005-08-26 | 2011-04-06 | Braincells, Inc. | Neurogenesis with acetylcholinesterase inhibitor |
| KR20130091791A (ko) * | 2005-09-30 | 2013-08-19 | 글락소 그룹 리미티드 | M1 수용체에서 활성을 갖는 화합물 및 그의 의약적 용도 |
| US8288413B2 (en) * | 2005-09-30 | 2012-10-16 | Glaxo Group Limited | Benzimidazolones which have activity at M1 receptor |
| ES2391107T3 (es) * | 2005-09-30 | 2012-11-21 | Glaxo Group Limited | Compuestos que tienen actividad en el receptor M1 y sus usos en medicina |
| WO2007047978A2 (en) | 2005-10-21 | 2007-04-26 | Braincells, Inc. | Modulation of neurogenesis by pde inhibition |
| EP1942879A1 (en) | 2005-10-31 | 2008-07-16 | 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 |
| WO2007134077A2 (en) | 2006-05-09 | 2007-11-22 | Braincells, Inc. | 5 ht receptor mediated neurogenesis |
| JP2009536669A (ja) | 2006-05-09 | 2009-10-15 | ブレインセルス,インコーポレイティド | アンジオテンシン調節による神経新生 |
| TW200813018A (en) * | 2006-06-09 | 2008-03-16 | Astrazeneca Ab | Novel compounds |
| KR20090064418A (ko) | 2006-09-08 | 2009-06-18 | 브레인셀즈 인코퍼레이션 | 4-아실아미노피리딘 유도체 포함 조합물 |
| US20100184806A1 (en) | 2006-09-19 | 2010-07-22 | Braincells, Inc. | Modulation of neurogenesis by ppar agents |
| WO2008045564A2 (en) * | 2006-10-12 | 2008-04-17 | Epix Delaware, Inc. | Carboxamide compounds and their use as antagonists of the chemokine ccr2 receptor |
| EP2194982A1 (en) * | 2007-09-20 | 2010-06-16 | Glaxo Group Limited | Compounds which have activity at m1 receptor and their uses in medicine |
| US8299257B2 (en) * | 2007-09-20 | 2012-10-30 | Glaxo Group Limited | Compounds which have activity at M1receptor and their uses in medicine |
| GB0718415D0 (en) * | 2007-09-20 | 2007-10-31 | Glaxo Group Ltd | Compounds |
| CA2708364A1 (en) | 2007-12-11 | 2009-06-18 | Efrat Ben-Zeev | Carboxamide compounds and their use as chemokine receptor agonists |
| EP2296471A4 (en) | 2008-05-15 | 2012-03-14 | Univ Toledo | MUSCARIC ACID 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 |
| US20130196990A1 (en) | 2010-10-06 | 2013-08-01 | Junya Qu | Benzimidazole Derivatives As PI3 Kinase Inhibitors |
| 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 |
| HUE055763T2 (hu) | 2015-07-20 | 2021-12-28 | Acadia Pharm Inc | Eljárás N-(4-fluorbenzil)-N-(1-metilpiperidin-4-il)-N'-(4-(2-metil-propil-oxi)fenil-metil)karbamid vagy ennek tartarát-sója és C polimorf formája elõállítására |
| 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 |
| US20210077479A1 (en) | 2017-08-30 | 2021-03-18 | Acadia Pharmaceuticals Inc. | Formulations of pimavanserin |
| WO2020113094A1 (en) | 2018-11-30 | 2020-06-04 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
| CN115836054B (zh) * | 2020-05-06 | 2024-12-10 | 默沙东有限责任公司 | Il4i1抑制剂和使用方法 |
| WO2023114224A1 (en) | 2021-12-13 | 2023-06-22 | Sage Therapeutics, Inc. | Combination of muscarinic receptor positive modulators and nmda positive allosteric modulators |
| WO2024138108A2 (en) * | 2022-12-22 | 2024-06-27 | University Of Florida Research Foundation, Incorporated | Metabolically stable sigma receptor ligands |
Family Cites Families (24)
| 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 |
| GB8718345D0 (en) * | 1987-08-03 | 1987-09-09 | Fordonal Sa | N-substituted benzamides |
| 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 |
| US5707798A (en) | 1993-07-13 | 1998-01-13 | Novo Nordisk A/S | 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 |
| AU701127B2 (en) | 1994-10-27 | 1999-01-21 | Merck & Co., Inc. | Muscarine antagonists |
| CA2215951A1 (en) * | 1995-03-22 | 1996-09-26 | Taisho Pharmaceutical Co., Ltd. | Thiazole derivatives |
| AU7528696A (en) | 1995-10-31 | 1997-05-22 | Merck & Co., Inc. | Muscarine antagonists |
| WO1997016187A1 (en) | 1995-10-31 | 1997-05-09 | Merck & Co., Inc. | Muscarine antagonists |
| US5756508A (en) | 1995-10-31 | 1998-05-26 | Merck & Co., Inc. | Muscarine antagonists |
| AU7478396A (en) | 1995-10-31 | 1997-05-22 | Merck & Co., Inc. | Muscarine agonists |
| 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 |
| WO2001083472A1 (en) | 2000-04-28 | 2001-11-08 | Acadia Pharmaceuticals, Inc. | Muscarinic agonists |
| ATE341538T1 (de) * | 2000-09-19 | 2006-10-15 | Boehringer Ingelheim Pharma | Benzimidazolonderivate mit affinität zu serotonin-und dopaminrezeptoren |
| US6586435B2 (en) * | 2000-09-19 | 2003-07-01 | Boehringer Ingelheim Pharma Kg | Benzimidazolone derivatives displaying affinity at the serotonin and dopamine receptors |
| EP1432420B1 (en) * | 2001-10-02 | 2011-07-13 | Acadia Pharmaceuticals Inc. | Benzimidazolidinone derivatives as muscarinic agents |
| US6951849B2 (en) * | 2001-10-02 | 2005-10-04 | Acadia Pharmaceuticals Inc. | Benzimidazolidinone derivatives as muscarinic agents |
-
2002
- 2002-09-30 EP EP02763824A patent/EP1432420B1/en not_active Expired - Lifetime
- 2002-09-30 CA CA002457647A patent/CA2457647A1/en not_active Abandoned
- 2002-09-30 KR KR1020067025160A patent/KR100809569B1/ko not_active Expired - Fee Related
- 2002-09-30 BR BR0213611-2A patent/BR0213611A/pt not_active IP Right Cessation
- 2002-09-30 RU RU2004113451/04A patent/RU2288919C2/ru not_active IP Right Cessation
- 2002-09-30 AU AU2002327810A patent/AU2002327810B2/en not_active Ceased
- 2002-09-30 CN CNA028194446A patent/CN1561212A/zh active Pending
- 2002-09-30 AT AT02763824T patent/ATE516030T1/de not_active IP Right Cessation
- 2002-09-30 NZ NZ531550A patent/NZ531550A/en not_active IP Right Cessation
- 2002-09-30 WO PCT/US2002/031308 patent/WO2003028650A2/en not_active Ceased
- 2002-09-30 TW TW091122574A patent/TWI310034B/zh not_active IP Right Cessation
- 2002-09-30 JP JP2003531986A patent/JP4347047B2/ja not_active Expired - Fee Related
- 2002-09-30 US US10/262,517 patent/US7087593B2/en not_active Expired - Fee Related
- 2002-09-30 KR KR10-2004-7004720A patent/KR20040047877A/ko not_active Ceased
- 2002-09-30 MX MXPA04003103A patent/MXPA04003103A/es active IP Right Grant
- 2002-10-02 AR ARP020103714A patent/AR036716A1/es unknown
-
2004
- 2004-03-30 NO NO20041317A patent/NO20041317L/no not_active Application Discontinuation
- 2004-04-01 ZA ZA200402609A patent/ZA200402609B/en unknown
-
2006
- 2006-05-03 US US11/418,342 patent/US7273857B2/en not_active Expired - Fee Related
- 2006-07-19 US US11/490,416 patent/US20060258707A1/en not_active Abandoned
-
2007
- 2007-09-20 US US11/858,828 patent/US20080009520A1/en not_active Abandoned
- 2007-11-27 US US11/945,857 patent/US20080070948A1/en not_active Abandoned
-
2010
- 2010-05-07 US US12/776,096 patent/US20100216840A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| KR100809569B1 (ko) | 2008-03-04 |
| KR20040047877A (ko) | 2004-06-05 |
| TWI310034B (en) | 2009-05-21 |
| US7087593B2 (en) | 2006-08-08 |
| CA2457647A1 (en) | 2003-04-10 |
| US20060205785A1 (en) | 2006-09-14 |
| WO2003028650A2 (en) | 2003-04-10 |
| KR20060130271A (ko) | 2006-12-18 |
| WO2003028650A3 (en) | 2003-06-19 |
| EP1432420A4 (en) | 2005-11-09 |
| NZ531550A (en) | 2006-12-22 |
| CN1561212A (zh) | 2005-01-05 |
| AU2002327810B2 (en) | 2006-11-02 |
| US20100216840A1 (en) | 2010-08-26 |
| JP4347047B2 (ja) | 2009-10-21 |
| US20080009520A1 (en) | 2008-01-10 |
| EP1432420B1 (en) | 2011-07-13 |
| US20030100545A1 (en) | 2003-05-29 |
| EP1432420A2 (en) | 2004-06-30 |
| JP2005510473A (ja) | 2005-04-21 |
| US7273857B2 (en) | 2007-09-25 |
| ATE516030T1 (de) | 2011-07-15 |
| ZA200402609B (en) | 2005-05-09 |
| US20060258707A1 (en) | 2006-11-16 |
| RU2288919C2 (ru) | 2006-12-10 |
| BR0213611A (pt) | 2005-12-20 |
| NO20041317L (no) | 2004-06-29 |
| US20080070948A1 (en) | 2008-03-20 |
| MXPA04003103A (es) | 2004-07-27 |
| RU2004113451A (ru) | 2005-09-10 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR036716A1 (es) | Un compuesto derivado de bencimidazolidinona, metodos que lo utilizan, una composicion farmaceutica que lo comprende y uso de dicho compuesto o composicion | |
| AR061564A1 (es) | Derivados de isoindoles, composiciones farmaceuticas y usos | |
| AR037983A1 (es) | Derivados de pirido [2,1-a] isoquinolina | |
| PE20080841A1 (es) | Derivados de quinazolinona e isoquinolinona y su uso para el tratamiento o prevencion de trastornos relacionados con el estres o la depresion | |
| RU2014120210A (ru) | (гетеро)арилциклопропиламины в качестве ингибиторов lsd1 | |
| AR079553A1 (es) | Derivados de diaza-espiro-[5,5]-undecanos, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de trastornos del snc, tales como trastornos del sueno y de la dependencia,entre otros. | |
| AR059905A1 (es) | Pirrolidina-3-ilaminas n-substituidas como antagonistas del receptor histamina-3, composicion farmaceutica y proceso para preparar el compuesto | |
| AR089568A1 (es) | Compuestos heterociclicos y sus metodos de usos | |
| AR066562A1 (es) | Derivados de pirrol condensados; una formulacion farmaceutica en base al compuesto y su uso para preparar medicamentos | |
| AR081577A1 (es) | Derivados de aminopirimidina como moduladores de la lrrk2 | |
| AR044795A1 (es) | Derivados de pirido [2,1-a] isoquinolina como inhibidores de la dpp-iv | |
| AR054560A1 (es) | Espiropiperidina como inhibidores de beta-secretasa para el tratamiento de la enfermedad de alzheimer | |
| AR064608A1 (es) | Derivados de pirazolo-quinazolina sustituidos, composiciones farmaceuticas que los contienen. proceso para su preparacion y uso de los mismos como agentes anticancer. | |
| AR037731A1 (es) | Uso de ureas de benzotiazoles | |
| AR077328A1 (es) | Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos | |
| ECSP066688A (es) | Polimorfo cristalino de una sal de bisulfato de underivados de azepinoindol como agentes farmaceuticos antagonista del receptor de trombina | |
| AR057769A1 (es) | Pirazolo pirimidinas como inhibidores de map quinasa p38, metodos para utilizarlos y composiciones farmaceuticas | |
| PE20071100A1 (es) | Derivados de azepinoindol como agentes farmaceuticos | |
| AR038172A1 (es) | Compuesto de ciclohexano y ciclohexeno, su uso para preparar una composicion farmaceutica, dicha composicion farmaceutica, procedimiento para preparar el compuesto y compuestos intermediarios en dicho procedimiento | |
| AR064547A1 (es) | Derivados de azaspiro como antagonistas del receptor v1a | |
| CO5700774A2 (es) | Derivados de triazol como inhibidores de 11-beta-hidroxiesteroide deshidrogenasa-1 | |
| AR074052A1 (es) | Compuestos pirazolo{1,5-a}pirimidina sustituida como inhibidores de trk cinasa | |
| AR071763A1 (es) | Pirazoles trisustituidos, composiciones farmaceuticas que los contienen, y usos de los mismos en el tratamiento de trastornos neurologicos y psiquiatricos | |
| PE20190446A1 (es) | Moduladores alostericos positivos del receptor muscarinico de acetilcolina m4 | |
| AR047098A1 (es) | Derivados de arilanilina como agonistas del receptor adrenergico beta2 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |