PE20091886A1 - PIPERAZINE-BASED CCR5 ANTAGONIST TABLET DOSAGE FORM - Google Patents
PIPERAZINE-BASED CCR5 ANTAGONIST TABLET DOSAGE FORMInfo
- Publication number
- PE20091886A1 PE20091886A1 PE2009000552A PE2009000552A PE20091886A1 PE 20091886 A1 PE20091886 A1 PE 20091886A1 PE 2009000552 A PE2009000552 A PE 2009000552A PE 2009000552 A PE2009000552 A PE 2009000552A PE 20091886 A1 PE20091886 A1 PE 20091886A1
- Authority
- PE
- Peru
- Prior art keywords
- receptor
- piperazine
- influenza
- hiv
- tablet
- Prior art date
Links
- 239000003067 chemokine receptor CCR5 antagonist Substances 0.000 title 1
- 239000002552 dosage form Substances 0.000 title 1
- 239000000203 mixture Substances 0.000 abstract 4
- 102000005962 receptors Human genes 0.000 abstract 3
- 108020003175 receptors Proteins 0.000 abstract 3
- -1 4,6-DIMETHYL-5-PYRIMIDINYL Chemical class 0.000 abstract 2
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 abstract 2
- 206010022000 influenza Diseases 0.000 abstract 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 abstract 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 abstract 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 abstract 2
- 239000008109 sodium starch glycolate Substances 0.000 abstract 2
- 229940079832 sodium starch glycolate Drugs 0.000 abstract 2
- 229920003109 sodium starch glycolate Polymers 0.000 abstract 2
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 abstract 1
- 102100035875 C-C chemokine receptor type 5 Human genes 0.000 abstract 1
- 101710149870 C-C chemokine receptor type 5 Proteins 0.000 abstract 1
- UGFAIRIUMAVXCW-UHFFFAOYSA-N Carbon monoxide Chemical compound [O+]#[C-] UGFAIRIUMAVXCW-UHFFFAOYSA-N 0.000 abstract 1
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 abstract 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 abstract 1
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 abstract 1
- 239000001828 Gelatine Substances 0.000 abstract 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 abstract 1
- 229930195725 Mannitol Natural products 0.000 abstract 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 abstract 1
- 239000002202 Polyethylene glycol Substances 0.000 abstract 1
- 229920002472 Starch Polymers 0.000 abstract 1
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 abstract 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical compound [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 239000011230 binding agent Substances 0.000 abstract 1
- 239000007884 disintegrant Substances 0.000 abstract 1
- QUPDWYMUPZLYJZ-UHFFFAOYSA-N ethyl Chemical compound C[CH2] QUPDWYMUPZLYJZ-UHFFFAOYSA-N 0.000 abstract 1
- 229920000159 gelatin Polymers 0.000 abstract 1
- 235000019322 gelatine Nutrition 0.000 abstract 1
- 239000008187 granular material Substances 0.000 abstract 1
- 229920000591 gum Polymers 0.000 abstract 1
- 239000008101 lactose Substances 0.000 abstract 1
- 229960001375 lactose Drugs 0.000 abstract 1
- 235000019359 magnesium stearate Nutrition 0.000 abstract 1
- 229940057948 magnesium stearate Drugs 0.000 abstract 1
- 239000000594 mannitol Substances 0.000 abstract 1
- 235000010355 mannitol Nutrition 0.000 abstract 1
- 229960001855 mannitol Drugs 0.000 abstract 1
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 abstract 1
- 239000008108 microcrystalline cellulose Substances 0.000 abstract 1
- 229940016286 microcrystalline cellulose Drugs 0.000 abstract 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 abstract 1
- 239000000546 pharmaceutical excipient Substances 0.000 abstract 1
- 229920001223 polyethylene glycol Polymers 0.000 abstract 1
- 229940069328 povidone Drugs 0.000 abstract 1
- 239000000600 sorbitol Substances 0.000 abstract 1
- 229960002920 sorbitol Drugs 0.000 abstract 1
- 235000010356 sorbitol Nutrition 0.000 abstract 1
- 239000008107 starch Substances 0.000 abstract 1
- 229940032147 starch Drugs 0.000 abstract 1
- 235000019698 starch Nutrition 0.000 abstract 1
- 239000000811 xylitol Substances 0.000 abstract 1
- 235000010447 xylitol Nutrition 0.000 abstract 1
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 abstract 1
- 229960002675 xylitol Drugs 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
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- 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
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Virology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- AIDS & HIV (AREA)
- Molecular Biology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Communicable Diseases (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Oncology (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
SE REFIERE A UNA TABLETA PARA ADMINISTRACION ORAL QUE COMPRENDE UN GRANULADO QUE COMPRENDE: A) 1-[(4,6-DIMETIL-5-PIRIMIDINIL)CARBONIL]-4-[4-[2-METOXI-1(R)-[4-(TRIFLUORMETIL)FENIL]ETIL]-3-(S)-METIL-1-PIPERAZINIL]-4-METIL-PIPERIDINA, ENTRE 10% A 20% EN PESO DE LA TABLETA; B) UN AGLUTINANTE SELECCIONADO DE GELATINA, POLIETILENGLICOL, GOMA, POVIDONA (PVP), ENTRE OTROS O MEZCLAS DE LOS MISMOS; C) UN DESINTEGRANTE SELECCIONADO DE GLICOLATO DE ALMIDON DE SODIO, CARBOXIMETILCELULOSA, ENTRE OTROS O MEZCLA DE LOS MISMOS; C) UN DILUYENTE SELECCIONADO DE LACTOSA, MANITOL, XILITOL, CELULOSA MICROCRISTALINA, ENTRE OTROS O MEZCLA DE LOS MISMOS. DICHA COMPOSICION COMPRENDE ADEMAS UN EXCIPIENTE EXTRAGRANULAR SELECCIONADO DE GLICOLATO DE ALMIDON DE SODIO, ALMIDON, SORBITOL, ESTEARATO DE MAGNESIO, ENTRE OTROS, SIENDO ANTAGONISTA DE CCR5 (RECEPTOR 5 QUIMIOCINA), UTIL EN EL TRATAMIENTO DE HIV ASI COMO ENFERMEDADES INFLAMATORIASREFERS TO A TABLET FOR ORAL ADMINISTRATION INCLUDING A GRANULATE COMPARING: A) 1 - [(4,6-DIMETHYL-5-PYRIMIDINYL) CARBONYL] -4- [4- [2-METOXY-1 (R) - [ 4- (TRIFLUORMETHYL) PHENYL] ETHYL] -3- (S) -MEthyl-1-PIPERAZINYL] -4-METHYL-PIPERIDINE, BETWEEN 10% TO 20% BY WEIGHT OF THE TABLET; B) A BINDER SELECTED FROM GELATINE, POLYETHYLENE GLYCOL, GUM, POVIDONE (PVP), AMONG OTHERS OR MIXTURES OF THE SAME; C) A DISINTEGRANT SELECTED FROM SODIUM STARCH GLYCOLATE, CARBOXIMETHYLCELLULOSE, AMONG OTHERS OR A MIXTURE OF THE SAME; C) A THINNER SELECTED FROM LACTOSE, MANNITOL, XYLITOL, MICROCRYSTALLINE CELLULOSE, AMONG OTHERS, OR A MIXTURE OF THEM. SUCH COMPOSITION ALSO INCLUDES A SELECTED EXTRAGRANULAR EXCIPIENT OF SODIUM STARCH GLYCOLATE, STARCH, SORBITOL, MAGNESIUM STEARATE, AMONG OTHERS, BEING ANTAGONIST OF CCR5 (RECEPTOR 5-ASFAMEDIATIVE INFLUENZA IN HIVMEDIUM ENDYMEDIATION 5 RECEPTOR, HIV INFLUENZA-CHEMEDIACIN 5 RECEPTOR IN HIVMEDIACYMEDIUM TRIALS IN HIV
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US4841108P | 2008-04-28 | 2008-04-28 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20091886A1 true PE20091886A1 (en) | 2009-12-19 |
Family
ID=40910997
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2009000552A PE20091886A1 (en) | 2008-04-28 | 2009-04-21 | PIPERAZINE-BASED CCR5 ANTAGONIST TABLET DOSAGE FORM |
Country Status (5)
| Country | Link |
|---|---|
| AR (1) | AR071394A1 (en) |
| CL (1) | CL2009000965A1 (en) |
| PE (1) | PE20091886A1 (en) |
| TW (1) | TW200948363A (en) |
| WO (1) | WO2009134637A1 (en) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2020033283A1 (en) * | 2018-08-09 | 2020-02-13 | Merck Sharp & Dohme Corp. | Compositions and methods for treating cancer with a combination of programmed death receptor (pd-1) antibodies and vicriviroc |
| CN113855640B (en) * | 2021-11-21 | 2023-09-26 | 湖南洞庭药业股份有限公司 | Solid pharmaceutical composition for treating mental diseases |
-
2009
- 2009-04-21 WO PCT/US2009/041196 patent/WO2009134637A1/en not_active Ceased
- 2009-04-21 PE PE2009000552A patent/PE20091886A1/en not_active Application Discontinuation
- 2009-04-22 TW TW098113335A patent/TW200948363A/en unknown
- 2009-04-22 AR ARP090101419A patent/AR071394A1/en not_active Application Discontinuation
- 2009-04-22 CL CL2009000965A patent/CL2009000965A1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| TW200948363A (en) | 2009-12-01 |
| WO2009134637A1 (en) | 2009-11-05 |
| CL2009000965A1 (en) | 2010-04-16 |
| AR071394A1 (en) | 2010-06-16 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FD | Application declared void or lapsed |