AR044974A1 - Derivados duales de nk1/nk3, su uso, procedimiento de preparacion y medicamento para el tratamiento de la esquizofrenia - Google Patents
Derivados duales de nk1/nk3, su uso, procedimiento de preparacion y medicamento para el tratamiento de la esquizofreniaInfo
- Publication number
- AR044974A1 AR044974A1 ARP040102313A ARP040102313A AR044974A1 AR 044974 A1 AR044974 A1 AR 044974A1 AR P040102313 A ARP040102313 A AR P040102313A AR P040102313 A ARP040102313 A AR P040102313A AR 044974 A1 AR044974 A1 AR 044974A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- unsubstituted
- halogen
- substituted
- lower alkyl
- Prior art date
Links
- 230000009977 dual effect Effects 0.000 title 1
- 229940126601 medicinal product Drugs 0.000 title 1
- 238000000034 method Methods 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 21
- 229910052736 halogen Inorganic materials 0.000 abstract 8
- 150000002367 halogens Chemical class 0.000 abstract 8
- 125000001424 substituent group Chemical group 0.000 abstract 6
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 5
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 4
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- 150000002431 hydrogen Chemical class 0.000 abstract 2
- 239000002253 acid Substances 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004786 difluoromethoxy group Chemical group [H]C(F)(F)O* 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000004785 fluoromethoxy group Chemical group [H]C([H])(F)O* 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000002883 imidazolyl group Chemical group 0.000 abstract 1
- 125000002971 oxazolyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 201000000980 schizophrenia Diseases 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
-
- 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
-
- 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
- A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
-
- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
-
- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4995—Pyrazines or piperazines forming part of bridged ring systems
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
-
- 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
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/541—Non-condensed thiazines containing further heterocyclic 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
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/547—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame spiro-condensed or forming part of bridged ring systems
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/554—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D417/04—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 directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D419/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms
- C07D419/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D419/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D451/04—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 with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D497/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having oxygen and sulfur atoms as the only ring hetero atoms
- C07D497/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having oxygen and sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D497/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/08—Bridged systems
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Emergency Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Pyridine Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Reivindicación 1: El uso de compuestos de la fórmula general (1), en donde: R1 es arilo, sin sustituir o sustituido por uno o más sustituyentes, seleccionados del grupo, consistente en alquilo inferior, alcoxilo inferior, halógeno, -(CH2)oOH, -C(O)H, CF3, CN, S-alquilo inferior, -S(O)-alquilo inferior, -C(O)NR'R'', -NR'R'', -NR'C(O)-alquilo inferior, -NR'S(O)2-alquilo inferior, o es heteroarilo, seleccionados de los grupos, consistentes en piridin-2- ó 3-ilo, imidazolilo u oxazolilo, sin sustituir o sustituido por alquilo inferior, halógeno o alcoxilo; R2 y R3 son independientemente el uno del otro hidrógeno, halógeno, alquilo, alcoxilo, OCHF2, OCH2F, OCF3 ó CF3; R4, R5 son independientemente el uno del otro hidrógeno, -(CR'R'')1-(CR'R'')1-(CR'R'')0,1-OH ó -(CR'R'')1-(CR'R'')1-(CR'R'')0,1-alquilo inferior, en donde R' y R'' en cada átomo de carbono puede ser el mismo o diferente el uno del otro, -C1,2-alquilo; -C(O)H; -(CH)2ocicloalquilo, sin sustituir o sustituido por hidroxilo; -(CH2)1,2,3NR'R''; -(CH2)1,2,3NR'C(O)-alquilo inferior; -(CH2)1,2,3NR'S(O)2-alquilo inferior; -(CH2)oS(O)-alquilo inferior; R' es hidrógeno, alquilo inferior, -(CH2)oOH, -C(O)H, -C(O)-alquilo inferior, -C(O)-cicloalquilo, -S(O)2-alquilo inferior; R'' es hidrógeno o alquilo inferior; o R4 y R5 forman junto con el átomo N al que están unidos un anillo con: -(CH2)3-5-, que está sin sustituir o sustituido por uno o más sustituyentes, seleccionados del grupo consistente en alquilo, halógeno, -(CR'R'')oOH, =O, -CHO, -NR'R'', en donde R' y R'' pueden formar junto con el átomo N al que están unidos un anillo con -(CH2)3-5, o mediante -(CH2)oNR'-C(O)-alquilo, -(CH2)o-C(O)-alquilo inferior, -(CH2)o-C(O)-cicloalquilo, -(CH2)oOC-(O)NR'R'', -(CH2)o-S(O)2-alquilo, -(CH2)o-S(O)-alquilo inferior, -(CH2)o-S-alquilo inferior, -(CH2)o-S(O)2-NR'R'', -(CH2)o-pirrolidinilo, o -C(O)NR'R'', o con -(CH2)1,2,3-NR'-(CH2)2-, que está sin sustituir o sustituido por uno o más sustituyentes, seleccionados del grupo consistente en alquilo inferior, halógeno, CF3, -(CR'R'')oOH, =O, -CHO, -NR'R'', en donde R' y R'' pueden formar junto con el átomo N al que están unidos un anillo con -(CH2)3-5, o mediante -(CH2)oNR'-C(O)-alquilo inferior, -(CH2)o-C(O)-alquilo inferior, -(CH2)o-C(O)-cicloalquilo, -(CH2)oOC(O)NR'R'', -(CH2)o-S(O)2-alquilo inferior, -(CH2)o-pirrolidinilo o -C(O)NR'R'', o con -(CH2)1,2,3-O-(CH2)2-, que está sin sustituir o sustituido por uno o más sustituyentes, seleccionados del grupo consistente en alquilo, halógeno, -(CR'R'')oOH, =O, -CHO, -NR'R'', en donde R' puede formar junto con el átomo N al que están unidos un anillo con -(CH2)3-5, o mediante -(CH2)oNR'-C(O)-alquilo inferior , -(CH2)o-C(O)-alquilo inferior, -(CH2)o-C(O)-cicloalquilo, -(CH2)oOC(O)NR'R'', -(CH2)o-S(O)2-alquilo inferior, -(CH2)o-pirrolidinilo o -C(O)NR'R'', o con -(CH2)1,2,3-S(O)0,1,2-(CH2)1,2,3-, que está sin sustituir o sustituido por uno o más sustituyentes, seleccionados del grupo consistente en alquilo inferior, halógeno, CF3, -(CR'R'')oOH, =O, -NR'R'', en donde R' y R'' pueden formar junto con el átomo N- al que están unidos un anillo con -(CH2)3-5, o -(CH2)oNR'-C(O)-alquilo inferior, -(CH2)o-C(O)-alquilo, -(CH2)o-C(O)-cicloalquilo, -(CH2)oOC(O)NR'R'', -(CH2)o-S(O)2-alquilo inferior, -(CH2)o-pirrolidi-nilo o -C(O)NR'R'', o con -CH2CH=CH-CH2-, que está sin sustituir o sustituido por uno o más sustituyentes, seleccionados del grupo consistente en alquilo, halógeno, -(CR'R'')oOH, =O, -CHO, -NR'R'', en donde R' y R'' pueden formar junto con el átomo N al que está unido un anillo con -(CH2)3-5, o mediante -(CH2)oNR'-C(O)-alquilo inferior, -(CH2)o-C(O)-alquilo inferior, -(CH2)o-C(O)-cicloalquilo, -(CH2)oOC(O)NR'R'', -(CH2)o-S(O)2-alquilo inferior, -(CH2)o-pirrolidinilo o -C(O)NR'R'', o es 0, 1, 2, ó 3 o sales de adición ácida farmacéuticamente activas de los mismos, para la preparación de medicamentos para el tratamiento de esquizofrenia.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP03014513 | 2003-07-03 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR044974A1 true AR044974A1 (es) | 2005-10-12 |
Family
ID=33560750
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP040102313A AR044974A1 (es) | 2003-07-03 | 2004-07-01 | Derivados duales de nk1/nk3, su uso, procedimiento de preparacion y medicamento para el tratamiento de la esquizofrenia |
Country Status (27)
Country | Link |
---|---|
US (3) | US20050090533A1 (es) |
EP (1) | EP1643998B1 (es) |
JP (1) | JP4490421B2 (es) |
KR (1) | KR100744859B1 (es) |
CN (1) | CN1852712B (es) |
AR (1) | AR044974A1 (es) |
AT (1) | ATE371451T1 (es) |
AU (1) | AU2004253267B2 (es) |
BR (1) | BRPI0412291A (es) |
CA (1) | CA2530886C (es) |
CO (1) | CO5650234A2 (es) |
DE (1) | DE602004008631T2 (es) |
DK (1) | DK1643998T3 (es) |
ES (1) | ES2291891T3 (es) |
HR (1) | HRP20070471T3 (es) |
IL (1) | IL172614A (es) |
MX (1) | MXPA06000192A (es) |
MY (1) | MY137156A (es) |
NO (1) | NO20056007L (es) |
NZ (1) | NZ544244A (es) |
PL (1) | PL1643998T3 (es) |
PT (1) | PT1643998E (es) |
RU (1) | RU2347777C2 (es) |
SI (1) | SI1643998T1 (es) |
TW (1) | TW200502230A (es) |
WO (1) | WO2005002577A1 (es) |
ZA (1) | ZA200510453B (es) |
Families Citing this family (32)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE102004034619A1 (de) * | 2004-07-16 | 2006-02-23 | Grünenthal GmbH | Substituierte Aminoverbindungen als 5-HT/NA Uptakehemmer |
US20060030600A1 (en) * | 2004-08-06 | 2006-02-09 | Patrick Schnider | Dual NK1/NK3 receptor antagonists for the treatment of schizophrenia |
DE102004039789A1 (de) * | 2004-08-16 | 2006-03-02 | Sanofi-Aventis Deutschland Gmbh | Arylsubstituierte polycyclische Amine, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
ES2540966T3 (es) | 2005-02-16 | 2015-07-15 | Anacor Pharmaceuticals, Inc. | Compuestos biocidas de boronoftalida |
ES2329827T3 (es) * | 2005-02-22 | 2009-12-01 | F. Hoffmann-La Roche Ag | Antagonistas de nk1. |
CN101146775B (zh) * | 2005-03-23 | 2012-07-18 | 弗·哈夫曼-拉罗切有限公司 | 用于呕吐的用作nk-i拮抗剂的代谢物 |
WO2006119390A1 (en) * | 2005-05-04 | 2006-11-09 | Vertex Pharmaceuticals Incorporated | Pyridines useful as modulators of ion channels |
US7880008B2 (en) * | 2005-05-31 | 2011-02-01 | Vertex Pharmaceuticals Incorporated | Heterocycles useful as modulators of ion channels |
DK1928886T3 (da) * | 2005-09-09 | 2011-07-11 | Glaxosmithkline Llc | Pyridin-derivater og deres anvendelse i behandlingen af psykotiske lidelser |
GB0518472D0 (en) * | 2005-09-09 | 2005-10-19 | Glaxo Group Ltd | Novel compounds |
WO2007039123A2 (en) * | 2005-09-22 | 2007-04-12 | Smithkline Beecham Corporation | Combination therapy comprising an nk-3 antagonist and an antipsychotic agent |
BRPI0621279B1 (pt) | 2005-12-30 | 2021-07-20 | Anacor Pharmaceuticals, Inc | Moléculas pequenas contendo boro |
CN102532180B (zh) * | 2005-12-30 | 2016-06-29 | 安纳考尔医药公司 | 含硼的小分子 |
EP2007726B1 (en) | 2006-02-07 | 2011-03-02 | F. Hoffmann-La Roche AG | Benzamide and heteroarene derivatives as cetp inhibitors |
CA2682506C (en) * | 2007-04-20 | 2016-05-24 | F. Hoffmann-La Roche Ag | Pyrrolidine derivatives as dual nk1/nk3 receptor antagonists |
CN101778837A (zh) | 2007-08-07 | 2010-07-14 | 弗·哈夫曼-拉罗切有限公司 | 作为nk3受体拮抗剂的吡咯烷芳基-醚 |
GB0808747D0 (en) * | 2008-05-14 | 2008-06-18 | Glaxo Wellcome Mfg Pte Ltd | Novel compounds |
GB0814340D0 (en) | 2008-08-05 | 2008-09-10 | Smithkline Beecham Corp | Anhydrous crystol form fo a pyridine derivative |
CA2772168C (en) * | 2009-08-27 | 2019-01-08 | Glaxosmithkline Llc | Anhydrate forms of a pyridine derivative |
WO2011054773A1 (en) | 2009-11-03 | 2011-05-12 | Glaxosmithkline Llc | Novel lactam compounds |
US20110144081A1 (en) * | 2009-12-15 | 2011-06-16 | Henner Knust | Pyrrolidine derivatives |
US8487102B2 (en) | 2010-04-20 | 2013-07-16 | Hoffmann-La Roche Inc. | Pyrrazolopyridine compounds as dual NK1/NK3 receptor antagonists |
US8987307B2 (en) | 2011-03-03 | 2015-03-24 | Hoffmann-La Roche Inc. | 3-amino-pyridines as GPBAR1 agonists |
CA2930008A1 (en) * | 2013-11-08 | 2015-05-14 | Kissei Pharmaceutical Co., Ltd. | Carboxymethyl piperidine derivative |
TWI649307B (zh) | 2014-05-07 | 2019-02-01 | 日商橘生藥品工業股份有限公司 | Cyclohexylpyridine derivative |
CN114306347A (zh) | 2015-05-18 | 2022-04-12 | 康堤医疗有限公司 | 用于治疗性激素依赖性疾病的双重nk-1/nk-3受体拮抗剂 |
HUE049979T2 (hu) | 2017-03-20 | 2020-11-30 | Forma Therapeutics Inc | Pirrolopirrol készítmények piruvát-kináz (PKR) aktivátorokként |
MX2020009438A (es) | 2018-03-14 | 2022-05-11 | Kandy Therapeutics Ltd | Formulacion farmaceutica novedosa que comprende antagonistas del receptor dual nk-1/nk-3. |
BR112021005188A2 (pt) | 2018-09-19 | 2021-06-08 | Forma Therapeutics, Inc. | tratamento de anemia falciforme com um composto de ativação de piruvato cinase r |
CN113226356A (zh) | 2018-09-19 | 2021-08-06 | 福马治疗股份有限公司 | 活化丙酮酸激酶r |
CN114728906B (zh) | 2019-11-15 | 2024-08-20 | 康堤医疗有限公司 | 制备nt-814的关键中间体6-氯-4-(4-氟-2-甲基苯基)吡啶-3-胺的新化学方法 |
EP4431512A1 (en) | 2023-03-16 | 2024-09-18 | Bayer Consumer Care AG | Novel dual nk-1/nk-3 receptor antagonists |
Family Cites Families (15)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
IL111960A (en) | 1993-12-17 | 1999-12-22 | Merck & Co Inc | Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them |
SG52217A1 (en) | 1993-12-29 | 1998-09-28 | Merck Sharp & Dohme | Substituted morpholine derivatives and their use as therapeutic agents |
IL112778A0 (en) | 1994-03-04 | 1995-05-26 | Merck & Co Inc | Substituted heterocycles, their preparation and pharmaceutical compositions containing them |
FR2719311B1 (fr) * | 1994-03-18 | 1998-06-26 | Sanofi Sa | Composés antagonistes sélectifs du récepteur NK3 humain et leur utilisation comme médicaments et outils de diagnostic. |
WO1998024445A1 (en) * | 1996-12-02 | 1998-06-11 | Merck Sharp & Dohme Limited | Use of nk-1 receptor antagonists for treating schizophrenic disorders |
US5972938A (en) * | 1997-12-01 | 1999-10-26 | Merck & Co., Inc. | Method for treating or preventing psychoimmunological disorders |
WO2000050398A2 (en) | 1999-02-24 | 2000-08-31 | F. Hoffmann-La Roche Ag | Phenyl- and pyridinyl derivatives as neurokinin 1 antagonists |
EP1035115B1 (en) * | 1999-02-24 | 2004-09-29 | F. Hoffmann-La Roche Ag | 4-Phenylpyridine derivatives and their use as NK-1 receptor antagonists |
PT1103545E (pt) | 1999-11-29 | 2004-03-31 | Hoffmann La Roche | 2-(3,5-bis-trifluorometil-fenil)-n-metil-n-(6-morfolin-4-il-4-o-totil-piridin-3-il)-isobutiramida |
KR100501608B1 (ko) * | 2000-07-14 | 2005-07-18 | 에프. 호프만-라 로슈 아게 | 4-페닐-피리딘 유도체의 nk1 수용체의 길항성선구약물로서의 n-산화물 |
TWI287003B (en) * | 2000-07-24 | 2007-09-21 | Hoffmann La Roche | 4-phenyl-pyridine derivatives |
TWI259180B (en) * | 2000-08-08 | 2006-08-01 | Hoffmann La Roche | 4-Phenyl-pyridine derivatives |
EP1192952A3 (en) | 2000-09-28 | 2003-03-26 | Pfizer Products Inc. | Combination, for treating depression and anxiety, containing an NK-3 receptor antagonist and a CNS penetrant NK-1 receptor antagonist |
KR100599134B1 (ko) * | 2001-04-23 | 2006-07-12 | 에프. 호프만-라 로슈 아게 | 양성 전립선 비대증에 대한 nk-1 수용체 길항물질의 용도 |
US20030083345A1 (en) * | 2001-07-10 | 2003-05-01 | Torsten Hoffmann | Method of treatment and/or prevention of brain, spinal or nerve injury |
-
2004
- 2004-06-25 NZ NZ544244A patent/NZ544244A/xx unknown
- 2004-06-25 WO PCT/EP2004/006929 patent/WO2005002577A1/en active IP Right Grant
- 2004-06-25 AU AU2004253267A patent/AU2004253267B2/en not_active Ceased
- 2004-06-25 PT PT04740337T patent/PT1643998E/pt unknown
- 2004-06-25 DE DE602004008631T patent/DE602004008631T2/de not_active Expired - Lifetime
- 2004-06-25 JP JP2006518043A patent/JP4490421B2/ja not_active Expired - Fee Related
- 2004-06-25 BR BRPI0412291-7A patent/BRPI0412291A/pt not_active Application Discontinuation
- 2004-06-25 DK DK04740337T patent/DK1643998T3/da active
- 2004-06-25 CA CA2530886A patent/CA2530886C/en not_active Expired - Fee Related
- 2004-06-25 ES ES04740337T patent/ES2291891T3/es not_active Expired - Lifetime
- 2004-06-25 KR KR1020067000167A patent/KR100744859B1/ko not_active IP Right Cessation
- 2004-06-25 EP EP04740337A patent/EP1643998B1/en not_active Expired - Lifetime
- 2004-06-25 AT AT04740337T patent/ATE371451T1/de active
- 2004-06-25 PL PL04740337T patent/PL1643998T3/pl unknown
- 2004-06-25 CN CN2004800253601A patent/CN1852712B/zh not_active Expired - Fee Related
- 2004-06-25 SI SI200430471T patent/SI1643998T1/sl unknown
- 2004-06-25 RU RU2006103010/04A patent/RU2347777C2/ru not_active IP Right Cessation
- 2004-06-25 MX MXPA06000192A patent/MXPA06000192A/es active IP Right Grant
- 2004-06-30 TW TW093119675A patent/TW200502230A/zh unknown
- 2004-07-01 AR ARP040102313A patent/AR044974A1/es not_active Application Discontinuation
- 2004-07-02 MY MYPI20042647A patent/MY137156A/en unknown
- 2004-07-02 US US10/884,707 patent/US20050090533A1/en not_active Abandoned
-
2005
- 2005-12-15 IL IL172614A patent/IL172614A/en not_active IP Right Cessation
- 2005-12-16 NO NO20056007A patent/NO20056007L/no not_active Application Discontinuation
- 2005-12-22 ZA ZA200510453A patent/ZA200510453B/en unknown
- 2005-12-29 CO CO05131296A patent/CO5650234A2/es not_active Application Discontinuation
-
2007
- 2007-10-10 HR HR20070471T patent/HRP20070471T3/xx unknown
-
2009
- 2009-01-29 US US12/361,569 patent/US7939533B2/en not_active Expired - Fee Related
-
2011
- 2011-03-31 US US13/076,891 patent/US8404708B2/en not_active Expired - Fee Related
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
AR044974A1 (es) | Derivados duales de nk1/nk3, su uso, procedimiento de preparacion y medicamento para el tratamiento de la esquizofrenia | |
AR029717A1 (es) | Derivados del pro-farmaco de 4-fenil-piridina | |
UY26043A1 (es) | Acidos oxamicos y derivados como ligandos de receptores tiroideos | |
JPS62126168A (ja) | 新規化合物、その製法及びそれを含む医薬組成物 | |
AR045859A1 (es) | Derivados de dibenzoazepina y de benzodiazepinas sustitudos, procesos de preparacion y usos | |
AR037489A1 (es) | Quinolinas sustituidas y proceso para su preparacion | |
AR052903A1 (es) | Compuestos de bis arilo y heteroarilo sustituidos como antagonistas selectivos de 5ht2a, composiciones farmaceuticas que los contienen y su empleo en el tratamiento de trastornos del sueno. | |
AU2003212305A1 (en) | Cyclic amides | |
AR059328A1 (es) | Derivados de antranilamida-2-amino-heteroareno-carboxamida, un proceso para su obtencion, composiciones farmaceuticas que los contienen y el uso de estos compuestos para la fabricacion de un medicamento para el tratamiento de enfermedades mediadas por cetp | |
AR050282A1 (es) | Antagonistas duales nk1/nk3 contra la esquizofrenia | |
MX2009011051A (es) | Derivados de pirrolidina como antagonistas del receptor nk1/nk3 doble. | |
PT736525E (pt) | Benzonitrilos e fluoretos como agonistas e antagonistas de 5-ht | |
AR041079A1 (es) | Derivados de 2-ariltiazol como agonistas de receptores activados proliferadores de peroxisomas alfa y gamma (ppar alfa y gamma) | |
CN114025847B (zh) | 作为tlr信号传导的调节剂的化合物和组合物 | |
CZ288787B6 (cs) | N-Substituovaný azabicyklo[3,2,0]heptanový derivát a jeho použití | |
JPS62267270A (ja) | 新規化合物、その製法及びそれを含む医薬組成物 | |
KR20080044273A (ko) | 아실구아니딘 유도체 또는 그의 염 | |
SE7501365L (es) | ||
US3769274A (en) | Aminophenyl-cycloamidines | |
ES2821962T3 (es) | Bloqueador de canales de sodio | |
SE435374B (sv) | Terapeutiskt aktiva derivat av 4-(2-hydroxi-3-amino-propoxi)-indol, deras framstellning och anvendning. | |
HUP0203187A2 (hu) | Izoxazolszármazékok mint foszfodiészteráz VII inhibitorok és ezeket tartalmazó gyógyszerkészítmények | |
MXPA02011464A (es) | Derivados 1,4-diazepan-2,5-diona y su uso como antagonistas del receptor de la nk-1. | |
NO160445B (no) | Analogifremgangsmaate for fremstilling av terapeutisk aktive heterocykliske forbindelser. | |
US3897443A (en) | Pharmacologically active anilinobenzothiazoles |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
FA | Abandonment or withdrawal |