CN103232442B - 一水合物的晶体形式及其药物组合物和应用以及制备工艺 - Google Patents
一水合物的晶体形式及其药物组合物和应用以及制备工艺 Download PDFInfo
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- CN103232442B CN103232442B CN201210396409.0A CN201210396409A CN103232442B CN 103232442 B CN103232442 B CN 103232442B CN 201210396409 A CN201210396409 A CN 201210396409A CN 103232442 B CN103232442 B CN 103232442B
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- methyl
- triazol
- chloro
- quinazoline
- difluorophenyl
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- 235000019333 sodium laurylsulphate Nutrition 0.000 description 1
- 159000000000 sodium salts Chemical class 0.000 description 1
- XNRNJIIJLOFJEK-UHFFFAOYSA-N sodium;1-oxidopyridine-2-thione Chemical compound [Na+].[O-]N1C=CC=CC1=S XNRNJIIJLOFJEK-UHFFFAOYSA-N 0.000 description 1
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- 229940118172 sucrets Drugs 0.000 description 1
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- DHCDFWKWKRSZHF-UHFFFAOYSA-N sulfurothioic S-acid Chemical compound OS(O)(=O)=S DHCDFWKWKRSZHF-UHFFFAOYSA-N 0.000 description 1
- 239000002511 suppository base Substances 0.000 description 1
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- 238000003786 synthesis reaction Methods 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 239000007885 tablet disintegrant Substances 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- 229940111630 tea tree oil Drugs 0.000 description 1
- 239000010677 tea tree oil Substances 0.000 description 1
- 229960002722 terbinafine Drugs 0.000 description 1
- DOMXUEMWDBAQBQ-WEVVVXLNSA-N terbinafine Chemical compound C1=CC=C2C(CN(C\C=C\C#CC(C)(C)C)C)=CC=CC2=C1 DOMXUEMWDBAQBQ-WEVVVXLNSA-N 0.000 description 1
- 229960000580 terconazole Drugs 0.000 description 1
- 229940063650 terramycin Drugs 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 229940073455 tetraethylammonium hydroxide Drugs 0.000 description 1
- LRGJRHZIDJQFCL-UHFFFAOYSA-M tetraethylazanium;hydroxide Chemical compound [OH-].CC[N+](CC)(CC)CC LRGJRHZIDJQFCL-UHFFFAOYSA-M 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- WJCNZQLZVWNLKY-UHFFFAOYSA-N thiabendazole Chemical compound S1C=NC(C=2NC3=CC=CC=C3N=2)=C1 WJCNZQLZVWNLKY-UHFFFAOYSA-N 0.000 description 1
- CWERGRDVMFNCDR-UHFFFAOYSA-N thioglycolic acid Chemical compound OC(=O)CS CWERGRDVMFNCDR-UHFFFAOYSA-N 0.000 description 1
- 229960002010 ticlatone Drugs 0.000 description 1
- POPOYOKQQAEISW-UHFFFAOYSA-N ticlatone Chemical compound ClC1=CC=C2C(=O)NSC2=C1 POPOYOKQQAEISW-UHFFFAOYSA-N 0.000 description 1
- 229960004214 tioconazole Drugs 0.000 description 1
- 229960004880 tolnaftate Drugs 0.000 description 1
- FUSNMLFNXJSCDI-UHFFFAOYSA-N tolnaftate Chemical compound C=1C=C2C=CC=CC2=CC=1OC(=S)N(C)C1=CC=CC(C)=C1 FUSNMLFNXJSCDI-UHFFFAOYSA-N 0.000 description 1
- 239000012049 topical pharmaceutical composition Substances 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
- 150000003852 triazoles Chemical class 0.000 description 1
- IMFACGCPASFAPR-UHFFFAOYSA-N tributylamine Chemical compound CCCCN(CCCC)CCCC IMFACGCPASFAPR-UHFFFAOYSA-N 0.000 description 1
- ICUTUKXCWQYESQ-UHFFFAOYSA-N triclocarban Chemical compound C1=CC(Cl)=CC=C1NC(=O)NC1=CC=C(Cl)C(Cl)=C1 ICUTUKXCWQYESQ-UHFFFAOYSA-N 0.000 description 1
- 229960001325 triclocarban Drugs 0.000 description 1
- 229960003500 triclosan Drugs 0.000 description 1
- GZXOHHPYODFEGO-UHFFFAOYSA-N triglycine sulfate Chemical compound NCC(O)=O.NCC(O)=O.NCC(O)=O.OS(O)(=O)=O GZXOHHPYODFEGO-UHFFFAOYSA-N 0.000 description 1
- 229960004418 trolamine Drugs 0.000 description 1
- 238000002211 ultraviolet spectrum Methods 0.000 description 1
- 210000001215 vagina Anatomy 0.000 description 1
- 229910052720 vanadium Inorganic materials 0.000 description 1
- 239000002966 varnish Substances 0.000 description 1
- 235000013311 vegetables Nutrition 0.000 description 1
- 230000004304 visual acuity Effects 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 239000000230 xanthan gum Substances 0.000 description 1
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- 150000003751 zinc Chemical class 0.000 description 1
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- PICXIOQBANWBIZ-UHFFFAOYSA-N zinc;1-oxidopyridine-2-thione Chemical compound [Zn+2].[O-]N1C=CC=CC1=S.[O-]N1C=CC=CC1=S PICXIOQBANWBIZ-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/88—Oxygen atoms
- C07D239/90—Oxygen atoms with acyclic radicals attached in position 2 or 3
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and 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
- A61K31/495—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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
-
- 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
- A61P31/04—Antibacterial agents
-
- 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
- A61P31/10—Antimycotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Epidemiology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (8)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US83586306P | 2006-08-07 | 2006-08-07 | |
| EP06380225.0 | 2006-08-07 | ||
| EP06380225A EP1887004A1 (en) | 2006-08-07 | 2006-08-07 | Crystalline forms of (1R,2R)-7-Chloro-3-[2-(2,4-difluorophenyl)-2-hydroxy-1-methyl-3-(1H-1,2,4-triazol-1-yl)propyl]quinazolin-4(3H)-one |
| US60/835,863 | 2006-08-07 | ||
| US92940807P | 2007-06-26 | 2007-06-26 | |
| EP07380186A EP2009009A1 (en) | 2007-06-26 | 2007-06-26 | Crystalline antifungal compounds |
| US60/929,408 | 2007-06-26 | ||
| EP07380186.2 | 2007-06-26 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2007800357074A Division CN101516858B (zh) | 2006-08-07 | 2007-08-06 | 晶体抗真菌化合物 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103232442A CN103232442A (zh) | 2013-08-07 |
| CN103232442B true CN103232442B (zh) | 2015-01-21 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201210396409.0A Expired - Fee Related CN103232442B (zh) | 2006-08-07 | 2007-08-06 | 一水合物的晶体形式及其药物组合物和应用以及制备工艺 |
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| EP (2) | EP2650291B1 (enExample) |
| JP (3) | JP2010513222A (enExample) |
| KR (1) | KR20090053903A (enExample) |
| CN (1) | CN103232442B (enExample) |
| AR (1) | AR062232A1 (enExample) |
| AU (1) | AU2007284851B2 (enExample) |
| BR (1) | BRPI0716026A2 (enExample) |
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| RU (1) | RU2500679C2 (enExample) |
| TW (1) | TWI426073B (enExample) |
| WO (1) | WO2008021049A2 (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20060235008A1 (en) | 2004-08-19 | 2006-10-19 | Hetero Drugs Limited | Novel polymorphs of efavirenz |
| PL2004646T3 (pl) | 2006-04-05 | 2016-12-30 | Chlorowodorek 8-[{l-(3,5-bis(trifluorometylo)fenylo)-etoksy}-metylol-8-fenylo-1,7-diaza-spiro[4.5]dekan-2-onu i sposób jego otrzymywania | |
| ITMI20062449A1 (it) * | 2006-12-19 | 2008-06-20 | Dipharma Spa | Forma cristallina di rabeprazolo sodico |
| ES2548998T3 (es) * | 2009-05-29 | 2015-10-22 | Palau Pharma, S.A. | Composiciones antifúngicas de azol |
| KR20120079054A (ko) * | 2009-07-10 | 2012-07-11 | 에볼바 아게 | 디인 조성물 |
| WO2011019911A1 (en) * | 2009-08-14 | 2011-02-17 | Opko Health, Inc. | Intravenous formulations of neurokinin-1 antagonists |
| US9435692B2 (en) | 2014-02-05 | 2016-09-06 | Lam Research Corporation | Calculating power input to an array of thermal control elements to achieve a two-dimensional temperature output |
| US9622483B2 (en) | 2014-02-19 | 2017-04-18 | Corning Incorporated | Antimicrobial glass compositions, glasses and polymeric articles incorporating the same |
| US11039620B2 (en) | 2014-02-19 | 2021-06-22 | Corning Incorporated | Antimicrobial glass compositions, glasses and polymeric articles incorporating the same |
| US11039621B2 (en) | 2014-02-19 | 2021-06-22 | Corning Incorporated | Antimicrobial glass compositions, glasses and polymeric articles incorporating the same |
| GB201410407D0 (en) * | 2014-06-11 | 2014-07-23 | Univ Dundee And Syngene Internat Ltd Plc And Consejo Superior De Investigaciones Cientificas And Med | Treatment of chagas disease |
| EA025187B1 (ru) * | 2015-04-17 | 2016-11-30 | Тагир Аббасели оглы Сулейманов | Производное дитиокарбамата 2-((4-(4-метилпиперазин-1-ил)фенил)амино)-2-оксоетил4-этилпиперазин-1-карбодитиоат, обладающее антифунгальной активностью |
| EP4452232A1 (en) | 2021-12-22 | 2024-10-30 | Palau Pharma, S.L.U. | Multiparticulate albaconazole composition |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1997005130A1 (en) * | 1995-08-02 | 1997-02-13 | J. Uriach & Cia. S.A. | New pyrimidone derivatives with antifungal activity |
| EP1282084A2 (en) * | 2000-03-07 | 2003-02-05 | J. Uriach & Cia. S.A. | Method for preparing pyrimidone derivatives with antifungal activity |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0293500A1 (en) | 1987-06-01 | 1988-12-07 | American Cyanamid Company | 3-heteroalkyl-2,4.quinzaoline-diones |
| GB8819308D0 (en) | 1988-08-13 | 1988-09-14 | Pfizer Ltd | Triazole antifungal agents |
| TW218017B (enExample) | 1992-04-28 | 1993-12-21 | Takeda Pharm Industry Co Ltd | |
| TW297813B (enExample) * | 1993-09-24 | 1997-02-11 | Takeda Pharm Industry Co Ltd | |
| CA2134417A1 (en) | 1993-12-22 | 1995-06-23 | Katsumi Itoh | Optically active azole derivatives, their production and use |
| WO1998039305A1 (en) * | 1997-03-05 | 1998-09-11 | Takeda Chemical Industries, Ltd. | Crystalline form of a bis 1,2,4-triazole compound |
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2007
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- 2007-08-06 IN IN1560MUN2014 patent/IN2014MN01560A/en unknown
- 2007-08-06 MX MX2009001208A patent/MX2009001208A/es active IP Right Grant
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- 2007-08-06 EP EP20070836538 patent/EP2049504A4/en not_active Withdrawn
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- 2007-08-06 CA CA002658843A patent/CA2658843A1/en not_active Abandoned
- 2007-08-06 CN CN201210396409.0A patent/CN103232442B/zh not_active Expired - Fee Related
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2013
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2015
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2016
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Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1997005130A1 (en) * | 1995-08-02 | 1997-02-13 | J. Uriach & Cia. S.A. | New pyrimidone derivatives with antifungal activity |
| EP1282084A2 (en) * | 2000-03-07 | 2003-02-05 | J. Uriach & Cia. S.A. | Method for preparing pyrimidone derivatives with antifungal activity |
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| IN2014MN01560A (enExample) | 2015-05-08 |
| EP2650291A1 (en) | 2013-10-16 |
| US20080076787A1 (en) | 2008-03-27 |
| CA2658843A1 (en) | 2008-02-21 |
| US8258296B2 (en) | 2012-09-04 |
| AU2007284851A1 (en) | 2008-02-21 |
| IL196722A (en) | 2016-10-31 |
| EP2049504A2 (en) | 2009-04-22 |
| TW200823197A (en) | 2008-06-01 |
| RU2500679C2 (ru) | 2013-12-10 |
| CN103232442A (zh) | 2013-08-07 |
| DK2650291T3 (en) | 2017-10-23 |
| AU2007284851B2 (en) | 2013-05-09 |
| WO2008021049A3 (en) | 2008-12-31 |
| WO2008021049A9 (en) | 2008-10-30 |
| JP2010513222A (ja) | 2010-04-30 |
| EP2049504A4 (en) | 2010-09-22 |
| BRPI0716026A2 (pt) | 2013-08-06 |
| JP2014012673A (ja) | 2014-01-23 |
| ES2652670T3 (es) | 2018-02-05 |
| RU2009104959A (ru) | 2010-08-20 |
| IL196722A0 (en) | 2009-11-18 |
| WO2008021049A2 (en) | 2008-02-21 |
| US7879867B2 (en) | 2011-02-01 |
| IL248216B (en) | 2018-03-29 |
| AR062232A1 (es) | 2008-10-22 |
| KR20090053903A (ko) | 2009-05-28 |
| EP2650291B1 (en) | 2017-10-04 |
| JP2015193642A (ja) | 2015-11-05 |
| MX2009001208A (es) | 2009-04-14 |
| US20110092702A1 (en) | 2011-04-21 |
| TWI426073B (zh) | 2014-02-11 |
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