AR065376A1 - Formulacion de pastillas de liberacion sostenida de antagonistas y agonistas de piperazina - piperidina del receptor 5 ht1a que tienen disolucion instestinal mejorada - Google Patents
Formulacion de pastillas de liberacion sostenida de antagonistas y agonistas de piperazina - piperidina del receptor 5 ht1a que tienen disolucion instestinal mejoradaInfo
- Publication number
- AR065376A1 AR065376A1 ARP080100662A ARP080100662A AR065376A1 AR 065376 A1 AR065376 A1 AR 065376A1 AR P080100662 A ARP080100662 A AR P080100662A AR P080100662 A ARP080100662 A AR P080100662A AR 065376 A1 AR065376 A1 AR 065376A1
- Authority
- AR
- Argentina
- Prior art keywords
- piperidin
- piperazin
- quinoline
- fluoro
- methoxy
- Prior art date
Links
- 238000009472 formulation Methods 0.000 title abstract 4
- 239000000203 mixture Substances 0.000 title abstract 4
- 230000002459 sustained effect Effects 0.000 title abstract 2
- 239000000556 agonist Substances 0.000 title 1
- 238000004090 dissolution Methods 0.000 title 1
- NQRYJNQNLNOLGT-UHFFFAOYSA-N tetrahydropyridine hydrochloride Natural products C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 title 1
- -1 1-quinolin-8-yl-piperidin-4-yl Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
- CTAGQKIJWQYQRN-UHFFFAOYSA-N 2,5-difluoro-8-[4-[4-(6-methoxyquinolin-8-yl)piperazin-1-yl]piperidin-1-yl]quinoline Chemical compound N1=CC=CC2=CC(OC)=CC(N3CCN(CC3)C3CCN(CC3)C=3C4=NC(F)=CC=C4C(F)=CC=3)=C21 CTAGQKIJWQYQRN-UHFFFAOYSA-N 0.000 abstract 1
- IOUVTAYJFBQRDZ-UHFFFAOYSA-N 2-methyl-8-[4-(1-quinolin-8-ylpiperidin-4-yl)piperazin-1-yl]quinoline Chemical compound C1=CN=C2C(N3CCC(CC3)N3CCN(CC3)C3=CC=CC4=CC=C(N=C43)C)=CC=CC2=C1 IOUVTAYJFBQRDZ-UHFFFAOYSA-N 0.000 abstract 1
- BOKOMGLCFUOPFS-UHFFFAOYSA-N 4,5-difluoro-8-[4-[4-(6-methoxyquinolin-8-yl)piperazin-1-yl]piperidin-1-yl]quinoline Chemical compound N1=CC=CC2=CC(OC)=CC(N3CCN(CC3)C3CCN(CC3)C=3C4=NC=CC(F)=C4C(F)=CC=3)=C21 BOKOMGLCFUOPFS-UHFFFAOYSA-N 0.000 abstract 1
- VHDGYUCLNQWJJC-UHFFFAOYSA-N 4-methoxy-7-[4-[4-(6-methoxyquinolin-8-yl)piperazin-1-yl]piperidin-1-yl]-2-(trifluoromethyl)quinoline Chemical compound N1=CC=CC2=CC(OC)=CC(N3CCN(CC3)C3CCN(CC3)C=3C=C4N=C(C=C(OC)C4=CC=3)C(F)(F)F)=C21 VHDGYUCLNQWJJC-UHFFFAOYSA-N 0.000 abstract 1
- PIUQVNKFONMZAS-UHFFFAOYSA-N 4-methoxy-8-[4-[4-(6-methoxyquinolin-8-yl)piperazin-1-yl]piperidin-1-yl]-2-(trifluoromethyl)quinoline Chemical compound N1=CC=CC2=CC(OC)=CC(N3CCN(CC3)C3CCN(CC3)C=3C4=NC(=CC(OC)=C4C=CC=3)C(F)(F)F)=C21 PIUQVNKFONMZAS-UHFFFAOYSA-N 0.000 abstract 1
- OVEZCVVQVWPPPN-UHFFFAOYSA-N 5-chloro-8-[4-(1-quinolin-8-ylpiperidin-4-yl)piperazin-1-yl]quinoline Chemical compound C12=NC=CC=C2C(Cl)=CC=C1N1CCN(C2CCN(CC2)C=2C3=NC=CC=C3C=CC=2)CC1 OVEZCVVQVWPPPN-UHFFFAOYSA-N 0.000 abstract 1
- SZPYUJIVXAFIMH-UHFFFAOYSA-N 5-fluoro-4-methoxy-8-[4-[4-(6-methoxyquinolin-8-yl)piperazin-1-yl]piperidin-1-yl]-2-(trifluoromethyl)quinoline Chemical compound N1=CC=CC2=CC(OC)=CC(N3CCN(CC3)C3CCN(CC3)C=3C4=NC(=CC(OC)=C4C(F)=CC=3)C(F)(F)F)=C21 SZPYUJIVXAFIMH-UHFFFAOYSA-N 0.000 abstract 1
- VLSKWFJXIRXMRF-UHFFFAOYSA-N 5-fluoro-8-[4-(1-quinolin-8-ylpiperidin-4-yl)piperazin-1-yl]quinoline Chemical compound C12=NC=CC=C2C(F)=CC=C1N1CCN(C2CCN(CC2)C=2C3=NC=CC=C3C=CC=2)CC1 VLSKWFJXIRXMRF-UHFFFAOYSA-N 0.000 abstract 1
- WNQHGRRIAUIHQT-UHFFFAOYSA-N 5-fluoro-8-[4-(4-quinolin-8-ylpiperazin-1-yl)piperidin-1-yl]quinoline Chemical compound C12=NC=CC=C2C(F)=CC=C1N1CCC(N2CCN(CC2)C=2C3=NC=CC=C3C=CC=2)CC1 WNQHGRRIAUIHQT-UHFFFAOYSA-N 0.000 abstract 1
- AQKJNURRIWKPDW-UHFFFAOYSA-N 5-fluoro-8-[4-[4-(6-fluoroquinolin-8-yl)piperazin-1-yl]piperidin-1-yl]quinoline Chemical compound N1=CC=CC2=CC(F)=CC(N3CCN(CC3)C3CCN(CC3)C=3C4=NC=CC=C4C(F)=CC=3)=C21 AQKJNURRIWKPDW-UHFFFAOYSA-N 0.000 abstract 1
- GNNYYPQOLAQITN-UHFFFAOYSA-N 5-fluoro-8-[4-[4-(6-methoxyquinolin-8-yl)piperazin-1-yl]piperidin-1-yl]-2,4-dimethylquinoline Chemical compound N1=CC=CC2=CC(OC)=CC(N3CCN(CC3)C3CCN(CC3)C=3C4=NC(C)=CC(C)=C4C(F)=CC=3)=C21 GNNYYPQOLAQITN-UHFFFAOYSA-N 0.000 abstract 1
- NTADQIOJOYLPAR-UHFFFAOYSA-N 5-fluoro-8-[4-[4-(6-methoxyquinolin-8-yl)piperazin-1-yl]piperidin-1-yl]-2-(trifluoromethyl)quinoline Chemical compound N1=CC=CC2=CC(OC)=CC(N3CCN(CC3)C3CCN(CC3)C=3C4=NC(=CC=C4C(F)=CC=3)C(F)(F)F)=C21 NTADQIOJOYLPAR-UHFFFAOYSA-N 0.000 abstract 1
- OSRWFGCIJIRBCM-UHFFFAOYSA-N 5-fluoro-8-[4-[4-(6-methoxyquinolin-8-yl)piperazin-1-yl]piperidin-1-yl]-3-(trifluoromethyl)quinoline Chemical compound N1=CC=CC2=CC(OC)=CC(N3CCN(CC3)C3CCN(CC3)C=3C4=NC=C(C=C4C(F)=CC=3)C(F)(F)F)=C21 OSRWFGCIJIRBCM-UHFFFAOYSA-N 0.000 abstract 1
- RATHBIMJMPZRTE-UHFFFAOYSA-N 5-fluoro-8-[4-[4-(6-methoxyquinolin-8-yl)piperazin-1-yl]piperidin-1-yl]-4-(trifluoromethyl)quinoline Chemical compound N1=CC=CC2=CC(OC)=CC(N3CCN(CC3)C3CCN(CC3)C=3C4=NC=CC(=C4C(F)=CC=3)C(F)(F)F)=C21 RATHBIMJMPZRTE-UHFFFAOYSA-N 0.000 abstract 1
- XPHZCOLHJWNPNX-UHFFFAOYSA-N 5-fluoro-8-[4-[4-(6-methoxyquinolin-8-yl)piperazin-1-yl]piperidin-1-yl]quinoline Chemical compound N1=CC=CC2=CC(OC)=CC(N3CCN(CC3)C3CCN(CC3)C=3C4=NC=CC=C4C(F)=CC=3)=C21 XPHZCOLHJWNPNX-UHFFFAOYSA-N 0.000 abstract 1
- PVXFJWVGSDXSON-UHFFFAOYSA-N 5-methoxy-8-[4-(1-quinolin-8-ylpiperidin-4-yl)piperazin-1-yl]quinoline Chemical compound C12=NC=CC=C2C(OC)=CC=C1N1CCN(C2CCN(CC2)C=2C3=NC=CC=C3C=CC=2)CC1 PVXFJWVGSDXSON-UHFFFAOYSA-N 0.000 abstract 1
- POCSVEHDZIFYRI-UHFFFAOYSA-N 6-bromo-8-[4-[4-(6-methoxyquinolin-8-yl)piperazin-1-yl]piperidin-1-yl]quinoline Chemical compound N1=CC=CC2=CC(OC)=CC(N3CCN(CC3)C3CCN(CC3)C=3C4=NC=CC=C4C=C(Br)C=3)=C21 POCSVEHDZIFYRI-UHFFFAOYSA-N 0.000 abstract 1
- JGBPYUBROZGGEG-UHFFFAOYSA-N 6-chloro-8-[4-(1-quinolin-8-ylpiperidin-4-yl)piperazin-1-yl]quinoline Chemical compound N1=CC=CC2=CC(Cl)=CC(N3CCN(CC3)C3CCN(CC3)C=3C4=NC=CC=C4C=CC=3)=C21 JGBPYUBROZGGEG-UHFFFAOYSA-N 0.000 abstract 1
- RLLMNBTUILNGRU-UHFFFAOYSA-N 6-fluoro-8-[4-(1-quinolin-8-ylpiperidin-4-yl)piperazin-1-yl]quinoline Chemical compound N1=CC=CC2=CC(F)=CC(N3CCN(CC3)C3CCN(CC3)C=3C4=NC=CC=C4C=CC=3)=C21 RLLMNBTUILNGRU-UHFFFAOYSA-N 0.000 abstract 1
- QOUCORNJMQHBDT-UHFFFAOYSA-N 6-fluoro-8-[4-[1-(2-methylquinolin-8-yl)piperidin-4-yl]piperazin-1-yl]quinoline Chemical compound C1=CN=C2C(N3CCN(CC3)C3CCN(CC3)C3=CC=CC4=CC=C(N=C43)C)=CC(F)=CC2=C1 QOUCORNJMQHBDT-UHFFFAOYSA-N 0.000 abstract 1
- RJQPUAHYXSLVGW-UHFFFAOYSA-N 6-fluoro-8-[4-[1-(7-fluoroquinolin-8-yl)piperidin-4-yl]piperazin-1-yl]quinoline Chemical compound N1=CC=CC2=CC(F)=CC(N3CCN(CC3)C3CCN(CC3)C=3C4=NC=CC=C4C=CC=3F)=C21 RJQPUAHYXSLVGW-UHFFFAOYSA-N 0.000 abstract 1
- PYGVLCWDSXKWJV-UHFFFAOYSA-N 6-fluoro-8-[4-[1-(8-fluoroquinolin-7-yl)piperidin-4-yl]piperazin-1-yl]quinoline Chemical compound N1=CC=CC2=CC(F)=CC(N3CCN(CC3)C3CCN(CC3)C=3C(=C4N=CC=CC4=CC=3)F)=C21 PYGVLCWDSXKWJV-UHFFFAOYSA-N 0.000 abstract 1
- GYNZCUUXCASQNQ-UHFFFAOYSA-N 6-fluoro-8-[4-[4-(6-methoxyquinolin-8-yl)piperazin-1-yl]piperidin-1-yl]quinoline Chemical compound N1=CC=CC2=CC(OC)=CC(N3CCN(CC3)C3CCN(CC3)C=3C4=NC=CC=C4C=C(F)C=3)=C21 GYNZCUUXCASQNQ-UHFFFAOYSA-N 0.000 abstract 1
- GORYJXZWFPJTLB-UHFFFAOYSA-N 6-methoxy-8-[4-(1-quinolin-8-ylpiperidin-4-yl)piperazin-1-yl]quinoline Chemical compound N1=CC=CC2=CC(OC)=CC(N3CCN(CC3)C3CCN(CC3)C=3C4=NC=CC=C4C=CC=3)=C21 GORYJXZWFPJTLB-UHFFFAOYSA-N 0.000 abstract 1
- AGKQMEJGGYUHPL-UHFFFAOYSA-N 6-methoxy-8-[4-[1-(2-methylquinolin-8-yl)piperidin-4-yl]piperazin-1-yl]quinoline Chemical compound N1=CC=CC2=CC(OC)=CC(N3CCN(CC3)C3CCN(CC3)C=3C4=NC(C)=CC=C4C=CC=3)=C21 AGKQMEJGGYUHPL-UHFFFAOYSA-N 0.000 abstract 1
- AZWXAFUKSVZQEG-UHFFFAOYSA-N 6-methoxy-8-[4-[1-(4-methylquinolin-8-yl)piperidin-4-yl]piperazin-1-yl]quinoline Chemical compound N1=CC=CC2=CC(OC)=CC(N3CCN(CC3)C3CCN(CC3)C=3C4=NC=CC(C)=C4C=CC=3)=C21 AZWXAFUKSVZQEG-UHFFFAOYSA-N 0.000 abstract 1
- IYEMIKGUZSTPNV-UHFFFAOYSA-N 6-methoxy-8-[4-[1-(quinolin-8-ylmethyl)piperidin-4-yl]piperazin-1-yl]quinoline Chemical compound N1=CC=CC2=CC(OC)=CC(N3CCN(CC3)C3CCN(CC=4C5=NC=CC=C5C=CC=4)CC3)=C21 IYEMIKGUZSTPNV-UHFFFAOYSA-N 0.000 abstract 1
- FOYUBTQMQRUAHU-UHFFFAOYSA-N 6-methoxy-8-[4-[1-[2-(trifluoromethyl)quinolin-8-yl]piperidin-4-yl]piperazin-1-yl]quinoline Chemical compound N1=CC=CC2=CC(OC)=CC(N3CCN(CC3)C3CCN(CC3)C=3C4=NC(=CC=C4C=CC=3)C(F)(F)F)=C21 FOYUBTQMQRUAHU-UHFFFAOYSA-N 0.000 abstract 1
- YMMDYYYQPNEQIT-UHFFFAOYSA-N 6-methoxy-8-[4-[1-[3-(trifluoromethyl)quinolin-8-yl]piperidin-4-yl]piperazin-1-yl]quinoline Chemical compound N1=CC=CC2=CC(OC)=CC(N3CCN(CC3)C3CCN(CC3)C=3C4=NC=C(C=C4C=CC=3)C(F)(F)F)=C21 YMMDYYYQPNEQIT-UHFFFAOYSA-N 0.000 abstract 1
- QZUWVQMRRZIPEG-UHFFFAOYSA-N 7-fluoro-8-[4-[4-(6-methoxyquinolin-8-yl)piperazin-1-yl]piperidin-1-yl]quinoline Chemical compound N1=CC=CC2=CC(OC)=CC(N3CCN(CC3)C3CCN(CC3)C=3C4=NC=CC=C4C=CC=3F)=C21 QZUWVQMRRZIPEG-UHFFFAOYSA-N 0.000 abstract 1
- VCZUIKWAOYYMFS-UHFFFAOYSA-N 8-[4-[4-(6-methoxyquinolin-8-yl)piperazin-1-yl]piperidin-1-yl]-2,4-dimethylquinoline Chemical compound N1=CC=CC2=CC(OC)=CC(N3CCN(CC3)C3CCN(CC3)C=3C4=NC(C)=CC(C)=C4C=CC=3)=C21 VCZUIKWAOYYMFS-UHFFFAOYSA-N 0.000 abstract 1
- WFRPBQPVVYMYFV-UHFFFAOYSA-N 8-fluoro-7-[4-[4-(6-methoxyquinolin-8-yl)piperazin-1-yl]piperidin-1-yl]quinoline Chemical compound N1=CC=CC2=CC(OC)=CC(N3CCN(CC3)C3CCN(CC3)C=3C(=C4N=CC=CC4=CC=3)F)=C21 WFRPBQPVVYMYFV-UHFFFAOYSA-N 0.000 abstract 1
- RZCAPXWCMUAQBL-UHFFFAOYSA-N COC=1C=C2C=CC=NC2=C(C=1)N1CCN(CC1)C1CCN(CC1)C1=NC2=CC=CC=C2C=C1 Chemical compound COC=1C=C2C=CC=NC2=C(C=1)N1CCN(CC1)C1CCN(CC1)C1=NC2=CC=CC=C2C=C1 RZCAPXWCMUAQBL-UHFFFAOYSA-N 0.000 abstract 1
- XRZGGPWRYYFFEY-UHFFFAOYSA-N butanedioic acid;5-fluoro-8-[4-[4-(6-methoxyquinolin-8-yl)piperazin-1-yl]piperidin-1-yl]quinoline Chemical compound OC(=O)CCC(O)=O.OC(=O)CCC(O)=O.OC(=O)CCC(O)=O.N1=CC=CC2=CC(OC)=CC(N3CCN(CC3)C3CCN(CC3)C=3C4=NC=CC=C4C(F)=CC=3)=C21 XRZGGPWRYYFFEY-UHFFFAOYSA-N 0.000 abstract 1
- 210000003169 central nervous system Anatomy 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 239000000945 filler Substances 0.000 abstract 1
- 125000001188 haloalkyl group Chemical group 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 239000000314 lubricant Substances 0.000 abstract 1
- 150000007524 organic acids Chemical class 0.000 abstract 1
- XSXHWVKGUXMUQE-UHFFFAOYSA-N osmium dioxide Inorganic materials O=[Os]=O XSXHWVKGUXMUQE-UHFFFAOYSA-N 0.000 abstract 1
- LMRCKXYHPYNEJV-UHFFFAOYSA-N piperazine;piperidine Chemical class C1CCNCC1.C1CNCCN1 LMRCKXYHPYNEJV-UHFFFAOYSA-N 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000007939 sustained release tablet Substances 0.000 abstract 1
- 239000003826 tablet Substances 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
- 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
- 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
- A61P25/22—Anxiolytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
Landscapes
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Addiction (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
Formulaciones de pastillas de liberacion sostenida de compuestos DE piperazina-piperidina, los cuales pueden ser utiles en el tratamiento de trastornos del sistema nervioso central: a procesos para su preparacion: y para métodos de su uso.Reivindicacion 1: Una formulacion de pastillas de liberacion sostenida para administracion oral caracterizada porque comprende: (a) un compuesto de la formula (1), o una sal farmacéuticamente aceptable del mismo, en donde R1, R2, R3, R4, R5, R6, R7,R8, R9, R10, R11, R12, R13, R14, R15, y R16, son cada uno independientemerte -H, alquilo-(C1-6), haloalquilo(C1-6), alquenilo-(C2-6), o alquinilo-(C2-6) , halogeno, -CF3, -NO2, -CN, -OR25, -OSO2,R25, SR25, -SO2R25, -SO2N(R25)2, -N(R25)2, C(O), -COR25, -CO2R25, -NR25CO2R25, -NR25COR25, -NR25CON(R25)2, o -CON(R25)2 Ra y Rb son cada uno independientemente -H o -CH3; y R25 es -H, alquilo- (C1-6) recto o ramificado, haloalquilo- (C1-6) alquenilo-(C2-6), o alquinilo- (C2-6); (b) al menos unácido orgánico; (c) al menos un controlador de la liberacion; (d) al menos un relleno; y (e) al menos un lubricante. Reivindicacion 4: La formulacion de una de cualesquiera de las reivindicaciones 1 hasta 3, caracterizada porque el compuesto de laformula (1) se selecciona del grupo que consiste de: 6-metoxi-8-[4-(1-quinolin-8-il-piperidin-4-il)-piperazin-1-il]-quinolina; 6-fluoro-8-[4-(1-quinolin-8-il-piperidin-4-il)-piperazin1-il]-quinolina; 5-fluoro-8-[4-(1-quinolin-8-il-piperidin-4-il)-piperazin-1-il]-quinolina; 7-fluoro-8-(4-(4-(6-metoxiquinolin-8-il)piperazin-1- il)piperidin-1-il)quinolina; 6-fluoro-8-{4-[1-(8-fluoroquinolin-7-il)piperidin-4-il]piperazin-1-il)quinolina; 3-trifluorometil-8-(4-(4-(6-metoxiquinolin-8-il)piperazin-1-il)piperidin-1-il)quinolina; 6-metoxi-8-(4-(1-(quinolin-8-ilmetil)piperidin-4-il)piperazin-1-il)quinolina; 5-fluoro-4-metoxi-8-(4-(4-(6-metoxiquinolin-8-il)piperazin-1-il)piperidin-1-il)-2-(trifluorometil)quinolina; 5-fluoro-8-(4-(4-(6-metoxiquinolin-8-il)piperazin-1-il)piperidin-1-il)quinolina; trisuccinato de 5-fluoro-8-(4-(4-(6-metoxiquinolin-8-il)piperazin-1-il)piperidin-1-il)quinolina; 8-[4-(1-quinolin-8-il-piperidin-4-il)-piperazin-1-jl]-quinolina; 6-cloro-8-[4-(4-(6-cloro)-quinolin-8-il-piperidin-1-il)-piperazin-1-il]-quinolina; 6-fluoro-8-[4-(4-(6-cloro)-quinolin-8-il-piperidin-1-jl)-piperazin-1-il]-quinolina; 5-cloro-8-[4-(1-quinolin-8-il-piperidin-4-il)-piperazin-1-il]-quinolina; 2-metil-8-[4-(1-quinolin-8-il-piperidin-4-il)-piperazin-1-il]-quinolina; 6-cloro-8-[4-(1-quinolin-8-il-piperidin-4-il)-piperazin-1-il]-quinolina; 8-[4-(1-quinolin-8-il-piperidin-4-il)-pjperazin-1-il]-5-trifluorometil-quinolina; 5-metoxi-8-[4-(1-quinolin-8-il-piperidin-4-il)-piperazin-1-il]-quinolina; 5-fluoro-8-[4-(4-quinolin-8-il-piperazin-1-il)piperidin-1-il]-quinolina; 6-metoxi-8-[4-(2-metilquinolin-8-il-piperidin-4-il)-piperazin-1-il]-quinolina; 6-fluoro-8-(4-(1-(2-metilquinolin-8-il)piperidin-4-il)piperazin-1-il)quinolina; 6-metoxi-8-[4-(3-netilquinolin-8-il-piperidin-4-il)-piperazin-1-il]-quinolina; 6-metoxi-8-(4-(1-(4-metilquinolin-8-il)piperidin-4-il)piperazin-1-il)quinolina; 6-metoxi-8-(4-(1-(2,4-dimetilquinolin-8-il)piperidin-4-il)piperazin-1-il)quinolina; 6-metoxi-8-(4-(1-(2,4-dimetil-5-fluoroquinolin-8-il)piperidin-4-il)piperazin-1-il)quinolina; 6-metoxi-8-(4-(1-(2-(trifluorometil)quinolin-8-il)piperidin-4-il)piperazin-1-il)quinolina; 6-fluoro-8-(4-(1-(5-fluoroquinolin-8-il)piperidin-4-il)piperazin-1-il)quinolina; 6-metoxi-8-(4-(1-(6-bromoquinolin-8-il)piperidin-4-il)piperazin-1-il)quinolina; 6-metoxi-8-(4-(1-(6-fluoroquinolin-8-il)piperidin-4-il)piperazin-1-il)quinolina; 6-fluoro-8-(4-(1-(7-fluoroquinolin-8-il)piperidin-4-il)piperazin-1-il)quinolina; 6-metoxi-8-{4-[1-(8-fluoroquinolin-7-il)piperidin-4-il]piperazin-il}quinolina; 6-metoxi-8-{4-[1-(2-trifluorometil-4-metoxiquinolin-7-il)piperidin-4-il]piperazin-1-il}quinolina; 6-metoxi-8-(4-(1-(2-trifluorometil-4-metoxiquinolin-8-il)piperidin-4-il)piperazin-1-il)quinolina; 5-fluoro-8-(4-(4-(6-metoxiquinolin-8-il)piperazin-1-il)piperidin-1-il)-2-trifluorometilquinolina; 5-fluoro-8-(4-(4-(6-metoxiquinolin-8-il)piperazin-1-il)piperidin-1-il)-3-trifluorometilquinolina; 5-fluoro-8-(4-(4-(6-metoxiquinolin-8-il)piperazin-1-il)piperidin-1-il)-4-trifluorometilquinolina; 2,5-difluoro-8-(4-(4-(6-metoxiquinolin-8-il)piperazin-1-il)piperidin-1-il)quinolina; 3,5-difluoro-8-(4-(4-(6-metoxiquinolin-8-il)piperazin-1-il)piperidin-1-il)quinolina; y 4,5-difluoro-8-(4-(4-(6-metoxiquinolin-8-il)piperazin-1-il)piperidin-1-il)quinolina.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US90191207P | 2007-02-16 | 2007-02-16 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR065376A1 true AR065376A1 (es) | 2009-06-03 |
Family
ID=39596364
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP080100662A AR065376A1 (es) | 2007-02-16 | 2008-02-15 | Formulacion de pastillas de liberacion sostenida de antagonistas y agonistas de piperazina - piperidina del receptor 5 ht1a que tienen disolucion instestinal mejorada |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20080226714A1 (es) |
| AR (1) | AR065376A1 (es) |
| PA (1) | PA8769901A1 (es) |
| TW (1) | TW200846032A (es) |
| WO (1) | WO2008101139A1 (es) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113559074B (zh) * | 2020-06-28 | 2023-04-21 | 海创药业股份有限公司 | 一种喹啉类化合物缓释片及其制备方法 |
| CA3232088A1 (en) * | 2021-09-17 | 2023-03-23 | Hinova Pharmaceuticals Inc. | Quinoline compound sustained-release tablet and preparation method thereof |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7276603B2 (en) * | 2003-05-02 | 2007-10-02 | Wyeth | Benzofuranyl-and benzothienyl-piperazinyl quinolines and methods of their use |
| US20050215561A1 (en) * | 2004-03-19 | 2005-09-29 | Krishnendu Ghosh | Pharmaceutical dosage forms and compositions |
| TWI391387B (zh) * | 2004-05-12 | 2013-04-01 | Eisai R&D Man Co Ltd | 具有哌啶環之吲哚衍生物 |
| TW200800959A (en) * | 2005-06-10 | 2008-01-01 | Wyeth Corp | Piperazine-piperidine antagonists and agonists of the 5-HT1a receptor |
| TW200808740A (en) * | 2006-06-09 | 2008-02-16 | Wyeth Corp | Succinate salts of 6-methoxy-8-[4-(1-(5-fluoro)-quinolin-8-yl-piperidin-4-yl)-piperazin-1-yl]-quinoline and crystalline forms thereof |
| TW200808741A (en) * | 2006-06-09 | 2008-02-16 | Wyeth Corp | 6-methoxy-8-[4-(1-(5-fluoro)-quinolin-8-yl-piperidin-4-yl)-piperazin-1-yl]-quinoline hydrochloric acid salts |
| CL2007003409A1 (es) * | 2006-11-28 | 2008-04-11 | Wyeth Corp | Perla de liberacion controlada que comprende una unidad de nucleo central, una primera capa con un agente farmacologico que es un compuesto derivado de piperazina-piperidina, un acidificante, una segunda capa; procedimiento de preparacion; formulacio |
-
2008
- 2008-02-15 WO PCT/US2008/054044 patent/WO2008101139A1/en active Application Filing
- 2008-02-15 TW TW097105307A patent/TW200846032A/zh unknown
- 2008-02-15 US US12/032,003 patent/US20080226714A1/en not_active Abandoned
- 2008-02-15 PA PA20088769901A patent/PA8769901A1/es unknown
- 2008-02-15 AR ARP080100662A patent/AR065376A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| TW200846032A (en) | 2008-12-01 |
| US20080226714A1 (en) | 2008-09-18 |
| WO2008101139A1 (en) | 2008-08-21 |
| PA8769901A1 (es) | 2008-11-19 |
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