RU2500679C2 - Кристаллические противогрибковые соединения - Google Patents
Кристаллические противогрибковые соединения Download PDFInfo
- Publication number
- RU2500679C2 RU2500679C2 RU2009104959/04A RU2009104959A RU2500679C2 RU 2500679 C2 RU2500679 C2 RU 2500679C2 RU 2009104959/04 A RU2009104959/04 A RU 2009104959/04A RU 2009104959 A RU2009104959 A RU 2009104959A RU 2500679 C2 RU2500679 C2 RU 2500679C2
- Authority
- RU
- Russia
- Prior art keywords
- hfa
- characteristic
- ray powder
- powder diffraction
- theta
- Prior art date
Links
- 230000000843 anti-fungal effect Effects 0.000 title abstract 2
- 229940121375 antifungal agent Drugs 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 238000000634 powder X-ray diffraction Methods 0.000 claims abstract 28
- UHIXWHUVLCAJQL-MPBGBICISA-N albaconazole Chemical group C([C@@](O)([C@H](N1C(C2=CC=C(Cl)C=C2N=C1)=O)C)C=1C(=CC(F)=CC=1)F)N1C=NC=N1 UHIXWHUVLCAJQL-MPBGBICISA-N 0.000 claims abstract 11
- 238000002329 infrared spectrum Methods 0.000 claims abstract 11
- 238000000034 method Methods 0.000 claims abstract 5
- 230000003595 spectral effect Effects 0.000 claims 10
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 9
- 239000000725 suspension Substances 0.000 claims 5
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 3
- 239000003960 organic solvent Substances 0.000 claims 3
- QMNUDYFKZYBWQX-UHFFFAOYSA-N 1H-quinazolin-4-one Chemical compound C1=CC=C2C(=O)N=CNC2=C1 QMNUDYFKZYBWQX-UHFFFAOYSA-N 0.000 claims 2
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims 2
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 2
- 125000004215 2,4-difluorophenyl group Chemical group [H]C1=C([H])C(*)=C(F)C([H])=C1F 0.000 claims 1
- 239000003125 aqueous solvent Substances 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 238000002425 crystallisation Methods 0.000 claims 1
- 230000008025 crystallization Effects 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 230000000845 anti-microbial effect Effects 0.000 abstract 1
- 238000004090 dissolution Methods 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 239000012535 impurity Substances 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
Images
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 (9)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US83586306P | 2006-08-07 | 2006-08-07 | |
US60/835,863 | 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 |
US92940807P | 2007-06-26 | 2007-06-26 | |
EP07380186.2 | 2007-06-26 | ||
EP07380186A EP2009009A1 (en) | 2007-06-26 | 2007-06-26 | Crystalline antifungal compounds |
US60/929,408 | 2007-06-26 | ||
PCT/US2007/017476 WO2008021049A2 (en) | 2006-08-07 | 2007-08-06 | Crystalline antifungal compounds |
Publications (2)
Publication Number | Publication Date |
---|---|
RU2009104959A RU2009104959A (ru) | 2010-08-20 |
RU2500679C2 true RU2500679C2 (ru) | 2013-12-10 |
Family
ID=39082545
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
RU2009104959/04A RU2500679C2 (ru) | 2006-08-07 | 2007-08-06 | Кристаллические противогрибковые соединения |
Country Status (17)
Country | Link |
---|---|
US (2) | US7879867B2 (en, 2012) |
EP (2) | EP2049504A4 (en, 2012) |
JP (3) | JP2010513222A (en, 2012) |
KR (1) | KR20090053903A (en, 2012) |
CN (1) | CN103232442B (en, 2012) |
AR (1) | AR062232A1 (en, 2012) |
AU (1) | AU2007284851B2 (en, 2012) |
BR (1) | BRPI0716026A2 (en, 2012) |
CA (1) | CA2658843A1 (en, 2012) |
DK (1) | DK2650291T3 (en, 2012) |
ES (1) | ES2652670T3 (en, 2012) |
IL (2) | IL196722A (en, 2012) |
IN (1) | IN2014MN01560A (en, 2012) |
MX (1) | MX2009001208A (en, 2012) |
RU (1) | RU2500679C2 (en, 2012) |
TW (1) | TWI426073B (en, 2012) |
WO (1) | WO2008021049A2 (en, 2012) |
Families Citing this family (13)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2006018853A2 (en) | 2004-08-19 | 2006-02-23 | Hetero Drugs Limited | Novel polymorphs of efavirenz |
PE20142329A1 (es) * | 2006-04-05 | 2015-01-30 | Opko Health Inc | Sales de hidrocloruro de 8-[{1-(3,5-bis-(trifluorometil)fenil)-etoxi}-metil]-8-fenil-1,7-diazaspiro[4.5]decan-2-ona |
ITMI20062449A1 (it) * | 2006-12-19 | 2008-06-20 | Dipharma Spa | Forma cristallina di rabeprazolo sodico |
WO2010138674A1 (en) * | 2009-05-29 | 2010-12-02 | Stiefel Laboratories, Inc. | Azole antifungal compositions |
CA2767785A1 (en) * | 2009-07-10 | 2011-01-13 | Evolva Ag | Diyne compositions |
BR112012003263A2 (pt) * | 2009-08-14 | 2015-09-22 | Opko Health Inc | formulações intravenosas de antagonistas de neuroquinina-1 |
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 |
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 |
US9622483B2 (en) | 2014-02-19 | 2017-04-18 | 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 |
CN118695852A (zh) | 2021-12-22 | 2024-09-24 | 帕劳制药有限公司 | 多颗粒阿巴康唑组合物 |
Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5807854A (en) * | 1995-08-02 | 1998-09-15 | J. Uriah & Cia. S.A. | Pyrimidone derivatives with antifungal activity |
RU2131417C1 (ru) * | 1993-09-24 | 1999-06-10 | Такеда Кемикал Индастриз, Лтд. | Производные азола, способы их получения и антигрибковое средство |
US6653475B2 (en) * | 2000-03-07 | 2003-11-25 | J. Uriach & Cia, S.A. | Method for preparing pyrimidone derivatives with antifungal activity |
Family Cites Families (5)
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 (en, 2012) | 1992-04-28 | 1993-12-21 | 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 |
-
2007
- 2007-08-06 IN IN1560MUN2014 patent/IN2014MN01560A/en unknown
- 2007-08-06 TW TW096128916A patent/TWI426073B/zh not_active IP Right Cessation
- 2007-08-06 US US11/882,892 patent/US7879867B2/en active Active
- 2007-08-06 CA CA002658843A patent/CA2658843A1/en not_active Abandoned
- 2007-08-06 MX MX2009001208A patent/MX2009001208A/es active IP Right Grant
- 2007-08-06 KR KR1020097004839A patent/KR20090053903A/ko not_active Ceased
- 2007-08-06 CN CN201210396409.0A patent/CN103232442B/zh not_active Expired - Fee Related
- 2007-08-06 EP EP20070836538 patent/EP2049504A4/en not_active Withdrawn
- 2007-08-06 EP EP13167750.2A patent/EP2650291B1/en active Active
- 2007-08-06 AU AU2007284851A patent/AU2007284851B2/en not_active Ceased
- 2007-08-06 ES ES13167750.2T patent/ES2652670T3/es active Active
- 2007-08-06 WO PCT/US2007/017476 patent/WO2008021049A2/en active Application Filing
- 2007-08-06 BR BRPI0716026-7A patent/BRPI0716026A2/pt not_active Application Discontinuation
- 2007-08-06 RU RU2009104959/04A patent/RU2500679C2/ru active
- 2007-08-06 JP JP2009523811A patent/JP2010513222A/ja active Pending
- 2007-08-06 DK DK13167750.2T patent/DK2650291T3/en active
- 2007-08-07 AR ARP070103473A patent/AR062232A1/es not_active Application Discontinuation
-
2009
- 2009-01-26 IL IL196722A patent/IL196722A/en active IP Right Grant
-
2010
- 2010-12-16 US US12/970,297 patent/US8258296B2/en not_active Expired - Fee Related
-
2013
- 2013-07-25 JP JP2013154163A patent/JP2014012673A/ja active Pending
-
2015
- 2015-07-09 JP JP2015137404A patent/JP2015193642A/ja active Pending
-
2016
- 2016-10-06 IL IL248216A patent/IL248216B/en active IP Right Grant
Patent Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
RU2131417C1 (ru) * | 1993-09-24 | 1999-06-10 | Такеда Кемикал Индастриз, Лтд. | Производные азола, способы их получения и антигрибковое средство |
US5807854A (en) * | 1995-08-02 | 1998-09-15 | J. Uriah & Cia. S.A. | Pyrimidone derivatives with antifungal activity |
US6653475B2 (en) * | 2000-03-07 | 2003-11-25 | J. Uriach & Cia, S.A. | Method for preparing pyrimidone derivatives with antifungal activity |
Non-Patent Citations (1)
Title |
---|
BARTROLI, Journal of Medicinal Chemistry, 1998, 41, 1869-1882. * |
Also Published As
Publication number | Publication date |
---|---|
MX2009001208A (es) | 2009-04-14 |
EP2650291B1 (en) | 2017-10-04 |
JP2014012673A (ja) | 2014-01-23 |
US7879867B2 (en) | 2011-02-01 |
TWI426073B (zh) | 2014-02-11 |
US20080076787A1 (en) | 2008-03-27 |
JP2015193642A (ja) | 2015-11-05 |
RU2009104959A (ru) | 2010-08-20 |
AU2007284851B2 (en) | 2013-05-09 |
TW200823197A (en) | 2008-06-01 |
IN2014MN01560A (en, 2012) | 2015-05-08 |
IL196722A (en) | 2016-10-31 |
CA2658843A1 (en) | 2008-02-21 |
CN103232442A (zh) | 2013-08-07 |
AU2007284851A1 (en) | 2008-02-21 |
WO2008021049A2 (en) | 2008-02-21 |
US20110092702A1 (en) | 2011-04-21 |
IL248216B (en) | 2018-03-29 |
CN103232442B (zh) | 2015-01-21 |
WO2008021049A9 (en) | 2008-10-30 |
ES2652670T3 (es) | 2018-02-05 |
KR20090053903A (ko) | 2009-05-28 |
IL196722A0 (en) | 2009-11-18 |
EP2049504A2 (en) | 2009-04-22 |
AR062232A1 (es) | 2008-10-22 |
EP2650291A1 (en) | 2013-10-16 |
US8258296B2 (en) | 2012-09-04 |
EP2049504A4 (en) | 2010-09-22 |
JP2010513222A (ja) | 2010-04-30 |
BRPI0716026A2 (pt) | 2013-08-06 |
WO2008021049A3 (en) | 2008-12-31 |
DK2650291T3 (en) | 2017-10-23 |
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