PE20091032A1 - Composicion que contiene n-(3-metoxi-5-metilpirazin-2-il)-2-(4-[1,3,4-oxadiazol-2-il]fenil)piridin-3-sulfonamida (zibotentan) - Google Patents
Composicion que contiene n-(3-metoxi-5-metilpirazin-2-il)-2-(4-[1,3,4-oxadiazol-2-il]fenil)piridin-3-sulfonamida (zibotentan)Info
- Publication number
- PE20091032A1 PE20091032A1 PE2008001750A PE2008001750A PE20091032A1 PE 20091032 A1 PE20091032 A1 PE 20091032A1 PE 2008001750 A PE2008001750 A PE 2008001750A PE 2008001750 A PE2008001750 A PE 2008001750A PE 20091032 A1 PE20091032 A1 PE 20091032A1
- Authority
- PE
- Peru
- Prior art keywords
- zibotentan
- methylpyrazin
- oxadiazol
- sulfonamide
- pyridin
- Prior art date
Links
- 229950003684 zibotentan Drugs 0.000 title abstract 3
- FJHHZXWJVIEFGJ-UHFFFAOYSA-N N-(3-methoxy-5-methyl-2-pyrazinyl)-2-[4-(1,3,4-oxadiazol-2-yl)phenyl]-3-pyridinesulfonamide Chemical compound COC1=NC(C)=CN=C1NS(=O)(=O)C1=CC=CN=C1C1=CC=C(C=2OC=NN=2)C=C1 FJHHZXWJVIEFGJ-UHFFFAOYSA-N 0.000 title abstract 2
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical class [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 title abstract 2
- NKFLEFWUYAUDJV-UHFFFAOYSA-N pyridine-3-sulfonamide Chemical compound NS(=O)(=O)C1=CC=CN=C1 NKFLEFWUYAUDJV-UHFFFAOYSA-N 0.000 title abstract 2
- 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
- 102000002045 Endothelin Human genes 0.000 abstract 1
- 108050009340 Endothelin Proteins 0.000 abstract 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 abstract 1
- 229930195725 Mannitol Natural products 0.000 abstract 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 abstract 1
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- -1 ZIBOTENTAN COMPOUND Chemical class 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 239000011230 binding agent Substances 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 239000007884 disintegrant Substances 0.000 abstract 1
- ZUBDGKVDJUIMQQ-UBFCDGJISA-N endothelin-1 Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(O)=O)NC(=O)[C@H]1NC(=O)[C@H](CC=2C=CC=CC=2)NC(=O)[C@@H](CC=2C=CC(O)=CC=2)NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CSSC[C@@H](C(N[C@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@H](CC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(O)=O)C(=O)N2)=O)NC(=O)[C@@H](CO)NC(=O)[C@H](N)CSSC1)C1=CNC=N1 ZUBDGKVDJUIMQQ-UBFCDGJISA-N 0.000 abstract 1
- 239000000594 mannitol Substances 0.000 abstract 1
- 235000010355 mannitol Nutrition 0.000 abstract 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 abstract 1
- 239000008108 microcrystalline cellulose Substances 0.000 abstract 1
- 229940016286 microcrystalline cellulose Drugs 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 abstract 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 abstract 1
- 229940069328 povidone Drugs 0.000 abstract 1
- 229910052708 sodium Inorganic materials 0.000 abstract 1
- 239000011734 sodium 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
- A61K9/2013—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
- 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
-
- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
- A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
REFERIDA A UNA COMPOSICION FARMACEUTICA QUE CONTIENE N-(3-METOXI-5-METILPIRAZIN-2-IL)-2-(4-[1,3,4-OXADIAZOL-2-IL]FENIL)PIRIDIN-3-SULFONAMIDA (I) (ZIBOTENTAN) EN UNA CANTIDAD DE 2 A 20% EN PESO, MANITOL EN UNA CANTIDAD DE 65% A 75% EN PESO Y/O CELULOSA MICROCRISTALINA EN UNA CANTIDAD DE 10% A 15% EN PESO. TAMBIEN CONTIENE UNO O MAS AGLUTINANTES TAL COMO POVIDONA, UNO O MAS DESINTEGRANTES TAL COMO CROSCAMELOSA SODICA. EL COMPUESTO ZIBOTENTAN ES UN ANTAGONISTA DE LA ENDOTELINA Y ES UTIL EN EL TRATAMIENTO DEL CANCER
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US97973607P | 2007-10-12 | 2007-10-12 | |
| US8911808P | 2008-08-15 | 2008-08-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20091032A1 true PE20091032A1 (es) | 2009-08-15 |
Family
ID=40534840
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2008001750A PE20091032A1 (es) | 2007-10-12 | 2008-10-10 | Composicion que contiene n-(3-metoxi-5-metilpirazin-2-il)-2-(4-[1,3,4-oxadiazol-2-il]fenil)piridin-3-sulfonamida (zibotentan) |
Country Status (34)
| Country | Link |
|---|---|
| US (2) | US8168221B2 (es) |
| EP (2) | EP2209501B1 (es) |
| JP (1) | JP2011500548A (es) |
| KR (1) | KR20100099113A (es) |
| CN (1) | CN101896210A (es) |
| AR (1) | AR068845A1 (es) |
| AT (1) | ATE536893T1 (es) |
| AU (1) | AU2008309385B2 (es) |
| BR (1) | BRPI0818323A2 (es) |
| CA (1) | CA2701385A1 (es) |
| CL (1) | CL2008003022A1 (es) |
| CO (1) | CO6270344A2 (es) |
| CR (1) | CR11363A (es) |
| CU (1) | CU20100064A7 (es) |
| CY (1) | CY1112433T1 (es) |
| DK (1) | DK2209501T3 (es) |
| DO (1) | DOP2010000105A (es) |
| EA (1) | EA201000545A1 (es) |
| ES (1) | ES2377426T3 (es) |
| HR (1) | HRP20120085T1 (es) |
| IL (1) | IL204953A0 (es) |
| MX (1) | MX2010003989A (es) |
| NI (1) | NI201000052A (es) |
| NZ (1) | NZ585310A (es) |
| PE (1) | PE20091032A1 (es) |
| PL (1) | PL2209501T3 (es) |
| PT (1) | PT2209501E (es) |
| SG (1) | SG182138A1 (es) |
| SI (1) | SI2209501T1 (es) |
| SV (1) | SV2010003529A (es) |
| TW (1) | TW200924768A (es) |
| UY (1) | UY31385A1 (es) |
| WO (1) | WO2009047565A2 (es) |
| ZA (1) | ZA201002477B (es) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE602004031114D1 (de) | 2003-06-06 | 2011-03-03 | Fibrogen Inc | Stickstoffhaltige heteroarylverbindungen und deren verwendungen zur erhoehung des gehaltes von endogenem erythropoietin |
| MX2010003989A (es) | 2007-10-12 | 2010-04-27 | Astrazeneca Ab | Composicion zibotentan que contiene mannitol y/o celulosa microcristalina. |
| CN101822796B (zh) * | 2010-03-17 | 2012-01-04 | 山西仟源制药有限公司 | 一种银冰含片及制备方法和应用 |
| WO2011143347A2 (en) * | 2010-05-11 | 2011-11-17 | Sensient Colors Llc | Film coating composition and methods of making and using the same |
| JO3753B1 (ar) * | 2011-10-14 | 2021-01-31 | Otsuka Pharma Co Ltd | قرص يتألف من 7-[4-(4-بينزو[بي]ثيوفين-4-ايل-ببرازين-1-1ايل)بوتكسيل]-1اتش-كوينولين-2-وان أو ملح منه |
| EP2844234B1 (de) * | 2012-04-27 | 2020-01-08 | Merck Patent GmbH | Tabletten mit überzug und deren herstellung |
| US8883823B2 (en) | 2012-07-16 | 2014-11-11 | Fibrogen, Inc. | Crystalline forms of a prolyl hydroxylase inhibitor |
| BR112015001101A2 (pt) | 2012-07-16 | 2017-06-27 | Fibrogen Inc | formas cristalinas de um inibidor de prolil hidroxilase |
| KR20220164069A (ko) * | 2013-06-06 | 2022-12-12 | 피브로겐, 인크. | Hif 하이드록실라제 억제자의 약학적 제형 |
| WO2021200767A1 (ja) * | 2020-03-31 | 2021-10-07 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 錠剤、医薬及びそれらの製造方法並びにキット |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3674794A (en) * | 1970-03-18 | 1972-07-04 | Ciba Geigy Corp | Certain-3-pyridine-sulfonamide derivatives |
| UA58494C2 (uk) * | 1995-06-07 | 2003-08-15 | Зенека Лімітед | Похідні n-гетероарилпіридинсульфонаміду, фармацевтична композиція, спосіб одержання та спосіб протидії впливам ендотеліну |
| ID25921A (id) * | 1997-04-28 | 2000-11-09 | Texas Biotechnology Corp | Sulfonamida-sulfonamida untuk pengobatan penyakit-penyakit yang dimediakan endotelin |
| US5783705A (en) * | 1997-04-28 | 1998-07-21 | Texas Biotechnology Corporation | Process of preparing alkali metal salys of hydrophobic sulfonamides |
| WO2000078292A1 (en) * | 1999-06-18 | 2000-12-28 | Takeda Chemical Industries, Ltd. | Quickly disintegrating solid preparations |
| JP2001058944A (ja) * | 1999-06-18 | 2001-03-06 | Takeda Chem Ind Ltd | 速崩壊性固形製剤 |
| US20030100595A1 (en) * | 2001-11-13 | 2003-05-29 | Aziz Karim | Oral dosage form of a sulfonamide prodrug |
| GB0219660D0 (en) * | 2002-08-23 | 2002-10-02 | Astrazeneca Ab | Therapeutic use |
| EP1551401A4 (en) * | 2002-09-20 | 2006-03-22 | Merck & Co Inc | MANNITOL FORMULATION FOR AN INTEGRIN RECEPTOR ANTAGONIST |
| GB0223854D0 (en) * | 2002-10-12 | 2002-11-20 | Astrazeneca Ab | Therapeutic treatment |
| GB0320806D0 (en) | 2003-09-05 | 2003-10-08 | Astrazeneca Ab | Therapeutic treatment |
| US7772232B2 (en) | 2004-04-15 | 2010-08-10 | Bristol-Myers Squibb Company | Quinazolinyl compounds as inhibitors of potassium channel function |
| GB0425854D0 (en) | 2004-11-25 | 2004-12-29 | Astrazeneca Ab | Therapeutic treatment |
| CN101032464A (zh) * | 2007-04-01 | 2007-09-12 | 杨喜鸿 | 含有利莫那班和聚乙烯吡咯烷酮的组合物、固体分散体及其制备和药物应用 |
| MX2010003989A (es) | 2007-10-12 | 2010-04-27 | Astrazeneca Ab | Composicion zibotentan que contiene mannitol y/o celulosa microcristalina. |
-
2008
- 2008-10-09 MX MX2010003989A patent/MX2010003989A/es active IP Right Grant
- 2008-10-09 SG SG2012039327A patent/SG182138A1/en unknown
- 2008-10-09 EA EA201000545A patent/EA201000545A1/ru unknown
- 2008-10-09 EP EP08806744A patent/EP2209501B1/en not_active Not-in-force
- 2008-10-09 JP JP2010528486A patent/JP2011500548A/ja active Pending
- 2008-10-09 PL PL08806744T patent/PL2209501T3/pl unknown
- 2008-10-09 TW TW097139020A patent/TW200924768A/zh unknown
- 2008-10-09 CN CN2008801210391A patent/CN101896210A/zh active Pending
- 2008-10-09 EP EP11187017A patent/EP2433620A1/en not_active Withdrawn
- 2008-10-09 NZ NZ585310A patent/NZ585310A/en not_active IP Right Cessation
- 2008-10-09 DK DK08806744.2T patent/DK2209501T3/da active
- 2008-10-09 AU AU2008309385A patent/AU2008309385B2/en not_active Ceased
- 2008-10-09 ES ES08806744T patent/ES2377426T3/es active Active
- 2008-10-09 PT PT08806744T patent/PT2209501E/pt unknown
- 2008-10-09 AT AT08806744T patent/ATE536893T1/de active
- 2008-10-09 SI SI200830529T patent/SI2209501T1/sl unknown
- 2008-10-09 HR HR20120085T patent/HRP20120085T1/hr unknown
- 2008-10-09 WO PCT/GB2008/050928 patent/WO2009047565A2/en not_active Ceased
- 2008-10-09 CA CA2701385A patent/CA2701385A1/en not_active Abandoned
- 2008-10-09 BR BRPI0818323A patent/BRPI0818323A2/pt not_active IP Right Cessation
- 2008-10-09 KR KR1020107010484A patent/KR20100099113A/ko not_active Withdrawn
- 2008-10-10 PE PE2008001750A patent/PE20091032A1/es not_active Application Discontinuation
- 2008-10-10 CL CL2008003022A patent/CL2008003022A1/es unknown
- 2008-10-10 UY UY31385A patent/UY31385A1/es not_active Application Discontinuation
- 2008-10-10 US US12/249,157 patent/US8168221B2/en not_active Expired - Fee Related
- 2008-10-10 AR ARP080104448A patent/AR068845A1/es not_active Application Discontinuation
-
2010
- 2010-04-08 ZA ZA2010/02477A patent/ZA201002477B/en unknown
- 2010-04-08 IL IL204953A patent/IL204953A0/en unknown
- 2010-04-12 SV SV2010003529A patent/SV2010003529A/es not_active Application Discontinuation
- 2010-04-12 DO DO2010000105A patent/DOP2010000105A/es unknown
- 2010-04-12 CR CR11363A patent/CR11363A/es not_active Application Discontinuation
- 2010-04-12 NI NI201000052A patent/NI201000052A/es unknown
- 2010-04-12 CU CU20100064A patent/CU20100064A7/es unknown
- 2010-05-07 CO CO10054830A patent/CO6270344A2/es not_active Application Discontinuation
-
2012
- 2012-02-09 CY CY20121100136T patent/CY1112433T1/el unknown
- 2012-03-21 US US13/425,474 patent/US20120177705A1/en not_active Abandoned
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