HRP20120330T1 - Sukristali i farmaceutski pripravci koji ih sadrže - Google Patents
Sukristali i farmaceutski pripravci koji ih sadrže Download PDFInfo
- Publication number
- HRP20120330T1 HRP20120330T1 HRP20120330AT HRP20120330T HRP20120330T1 HR P20120330 T1 HRP20120330 T1 HR P20120330T1 HR P20120330A T HRP20120330A T HR P20120330AT HR P20120330 T HRP20120330 T HR P20120330T HR P20120330 T1 HRP20120330 T1 HR P20120330T1
- Authority
- HR
- Croatia
- Prior art keywords
- image
- compound
- hydroxybenzoic acid
- molar ratio
- approximately
- Prior art date
Links
- 239000013078 crystal Substances 0.000 title claims 16
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- FJKROLUGYXJWQN-UHFFFAOYSA-N 4-hydroxybenzoic acid Chemical compound OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 claims abstract 38
- 150000001875 compounds Chemical class 0.000 claims abstract 23
- 229940090248 4-hydroxybenzoic acid Drugs 0.000 claims abstract 19
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims 24
- 239000000825 pharmaceutical preparation Substances 0.000 claims 9
- 239000002904 solvent Substances 0.000 claims 7
- 239000000126 substance Substances 0.000 claims 5
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims 3
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 claims 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 3
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims 3
- 230000000704 physical effect Effects 0.000 claims 3
- BZLVMXJERCGZMT-UHFFFAOYSA-N Methyl tert-butyl ether Chemical compound COC(C)(C)C BZLVMXJERCGZMT-UHFFFAOYSA-N 0.000 claims 2
- 239000002585 base Substances 0.000 claims 2
- 238000001938 differential scanning calorimetry curve Methods 0.000 claims 2
- 239000003085 diluting agent Substances 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 238000000634 powder X-ray diffraction Methods 0.000 claims 2
- 238000002425 crystallisation Methods 0.000 claims 1
- 230000008025 crystallization Effects 0.000 claims 1
- 238000000227 grinding Methods 0.000 claims 1
- 238000010438 heat treatment Methods 0.000 claims 1
- 238000002844 melting Methods 0.000 claims 1
- 230000008018 melting Effects 0.000 claims 1
- 239000007790 solid phase Substances 0.000 claims 1
- 238000000859 sublimation Methods 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
-
- 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
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/07—Tetrapeptides
-
- 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
-
- 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
-
- 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
- C07D403/12—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 chain containing hetero atoms as chain links
Abstract
Sukristal, naznačen time što sadrži spoj sa strukturomi 4-hidroksibenzojevu kiselinu. Patent sadrži još 17 patentnih zahtjeva.
Claims (18)
1. Sukristal, naznačen time što sadrži spoj sa strukturom
[image]
i 4-hidroksibenzojevu kiselinu.
2. Sukristal u skladu s patentnim zahtjevom 1, naznačen time što je molarni odnos između spoja sa strukturom
[image]
i 4-hidroksibenzojeve kiseline u rasponu od otprilike 5:1 do otprilike 1:5, ili gdje molarni odnos između spoja sa strukturom
[image]
i 4-hidroksibenzojeve kiseline iznosi otprilike 1:1.
3. Sukristal u skladu s patentnim zahtjevom 2, naznačen time što molarni odnos između spoja sa strukturom
[image]
i 4-hidroksibenzojeve kiseline iznosi otprilike 1:1, gdje sukristal ima najmanje dva od pet signala difrakcije rendgenskih zraka na prahu na otprilike 17,61, 18,07, 18,87, 19,68, te 20,75 °2θ, od kojih svaki ima standardnu devijaciju od otprilike ± 0,3 °2θ; ili gdje molarni odnos između spoja sa strukturom
[image]
i 4-hidroksibenzojeve kiseline iznosi otprilike 1:1, te gdje sukristal ima signal u svom DSC termogramu na otprilike 191,19 °C, uz standardnu devijaciju od otprilike ± 5 °C.
4. Sukristal, naznačen time što sadrži spoj sa strukturom
[image]
4-hidroksibenzojevu kiselinu, te otapalo koja se bira iz skupine koju čine acetonitril, etil-acetat, etanol, aceton, diklormetan i metil-tert-butil-eter.
5. Sukristal u skladu s patentnim zahtjevom 4, naznačen time što je otapalo acetonitril.
6. Sukristal u skladu s patentnim zahtjevom 5, naznačen time što je molarni odnos između spoja sa strukturom
[image]
i 4-hidroksibenzojeve kiseline u rasponu od otprilike 5:1 do otprilike 1:5, ili gdje molarni odnos između spoja sa strukturom
[image]
i 4-hidroksibenzojeva kiselina iznosi otprilike 1:1, te gdje, izborno, molarni odnos između spoja sa strukturom
[image]
i acetonitrila iznosi otprilike 1:0,05 do otprilike 1:0,5, ili gdje molarni odnos između spoja sa strukturom
[image]
i acetonitrila iznosi otprilike 1:0,14.
7. Sukristal u skladu s patentnim zahtjevom 6, naznačen time što molarni odnos između spoja sa strukturom
[image]
i 4-hidroksibenzojeve kiseline iznosi otprilike 1:1, a molarni odnos između spoja sa strukturom
[image]
i acetonitrila iznosi otprilike 1:0,14 i ima najmanje dva od četiri signala difrakcije rendgenskih zraka na prahu na otprilike 7,684, 8,599, 9,605, 9,938 °2θ, od kojih svaki ima standardnu devijaciju od otprilike ± 0,3 °2θ, ili ima DSC signal u svom DSC termogramu na otprilike 190,78 °C, uz standardnu devijaciju od otprilike ± 5 °C.
8. Farmaceutski pripravak, naznačen time što sadrži sukristal u skladu s patentnim zahtjevom 1.
9. Farmaceutski pripravak u skladu s patentnim zahtjevom 8, naznačen time što je molarni odnos između spoja sa strukturom
[image]
i 4-hidroksibenzojeve kiseline u rasponu od otprilike 5:1 do otprilike 1:5, ili gdje molarni odnos između spoja sa strukturom
[image]
i 4-hidroksibenzojeve kiseline iznosi otprilike 1:1.
10. Farmaceutski pripravak, naznačen time što sadrži sukristal u skladu s patentnim zahtjevom 4.
11. Farmaceutski pripravak u skladu s patentnim zahtjevom 10, naznačen time što je otapalo acetonitril.
12. Farmaceutski pripravak u skladu s patentnim zahtjevom 11, naznačen time što je molarni odnos između spoja sa strukturom
[image]
i 4-hidroksibenzojeve kiseline u rasponu od otprilike 5:1 do otprilike 1:5, ili gdje molarni odnos između spoja sa strukturom
[image]
i 4-hidroksibenzojeve kiseline iznosi otprilike 1:1.
13. Farmaceutski pripravak u skladu s patentnim zahtjevom 12, naznačen time što molarni odnos između spoja sa strukturom
[image]
i 4-hidroksibenzojeve kiseline iznosi otprilike 1:1, a molarni odnos između spoja sa strukturom
[image]
i acetonitrila je u rasponu od otprilike 1:0,01 do otprilike 1:1.
14. Farmaceutski pripravak u skladu s patentnim zahtjevom 13, naznačen time što molarni odnos između spoja sa strukturom
[image]
i acetonitrila iznosi otprilike 1:0,14.
15. Farmaceutski pripravak u skladu s patentnim zahtjevom 10, naznačen time što dodatno sadrži drugo otapalo, razrjeđivač, pomoćnu tvar, podlogu ili solubilizacijsko sredstvo.
16. Farmaceutski pripravak u skladu s patentnim zahtjevom 8, naznačen time što dodatno sadrži otapalo, razrjeđivač, pomoćnu tvar, podlogu ili solubilizacijsko sredstvo.
17. Postupak dobivanja sukristala u skladu s bilo kojim od patentnih zahtjeva 1-7, naznačen time što se sastoji u:
a) osiguravanju spoja sa strukturom
[image]
b) osiguravanju 4-hidroksibenzojeve kiseline,
c) mljevenju, grijanju, susublimiranju, sutaljenju ili stavljanju u kontakt u otopini spoja sa strukturom
[image]
s 4-hidroksibenzojevom kiselinom u uvjetima kristaliziranja, tako da nastane sukristal u čvrstoj fazi, i
d) izborno izdvajanju sukristala nastalog u koraku (c).
18. Postupak mijenjanja kemijskog ili fizičkog svojstva od interesa sukristala u skladu s bilo kojim od patentnih zahtjeva 1-7, naznačen time što se sastoji u:
a) mjerenju kemijskog ili fizičkog svojstva od interesa spoja sa strukturom
[image]
i 4-hidroksibenzojeve kiseline,
b) određivanju molarnog udjela spoja sa strukturom
[image]
i 4-hidroksibenzojeve kiseline koji će rezultirati željenom promjenom kemijskog ili fizičkog svojstva od interesa, i
c) dobivanju sukristala s molarnim udjelom određenim u koraku (b).
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US90358707P | 2007-02-27 | 2007-02-27 | |
PCT/US2008/002568 WO2008106151A2 (en) | 2007-02-27 | 2008-02-27 | Co-crystals and pharmaceutical compositions comprising the same |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20120330T1 true HRP20120330T1 (hr) | 2012-05-31 |
Family
ID=39672669
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20120330AT HRP20120330T1 (hr) | 2007-02-27 | 2012-04-13 | Sukristali i farmaceutski pripravci koji ih sadrže |
Country Status (28)
Country | Link |
---|---|
US (1) | US8759353B2 (hr) |
EP (3) | EP2463285A1 (hr) |
JP (1) | JP2010519330A (hr) |
KR (1) | KR20090115970A (hr) |
CN (1) | CN101687856A (hr) |
AP (1) | AP2009004960A0 (hr) |
AR (1) | AR065498A1 (hr) |
AT (1) | ATE542815T1 (hr) |
AU (1) | AU2008219607B2 (hr) |
BR (1) | BRPI0807907A2 (hr) |
CA (1) | CA2679312A1 (hr) |
CO (1) | CO6220963A2 (hr) |
CY (1) | CY1112865T1 (hr) |
DK (1) | DK2114924T3 (hr) |
EA (1) | EA200970806A1 (hr) |
EC (1) | ECSP099600A (hr) |
ES (1) | ES2379905T3 (hr) |
GE (1) | GEP20125645B (hr) |
HR (1) | HRP20120330T1 (hr) |
IL (1) | IL200616A0 (hr) |
MX (1) | MX2009009182A (hr) |
NZ (1) | NZ579442A (hr) |
PL (1) | PL2114924T3 (hr) |
PT (1) | PT2114924E (hr) |
RS (1) | RS52306B (hr) |
SI (1) | SI2114924T1 (hr) |
TW (1) | TW200846343A (hr) |
WO (1) | WO2008106151A2 (hr) |
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US8399615B2 (en) | 2005-08-19 | 2013-03-19 | Vertex Pharmaceuticals Incorporated | Processes and intermediates |
WO2007098270A2 (en) * | 2006-02-27 | 2007-08-30 | Vertex Pharmaceuticals Incorporated | Co-crystals comprising vx-950 and pharmaceutical compositions comprising the same |
JP2012501971A (ja) * | 2008-09-03 | 2012-01-26 | バーテックス ファーマシューティカルズ インコーポレイテッド | 共結晶および共結晶を含む薬学的処方物 |
WO2010093843A2 (en) | 2009-02-12 | 2010-08-19 | Vertex Pharmaceuticals Incorporated | Hcv combination therapies |
EP2496077B1 (en) * | 2009-11-06 | 2014-08-20 | Basf Se | Crystalline complexes of 4-hydroxy benzoic acid and selected pesticides |
JP2013518124A (ja) | 2010-01-29 | 2013-05-20 | バーテックス ファーマシューティカルズ インコーポレイテッド | C型肝炎ウイルス感染の処置のための治療法 |
WO2011112922A2 (en) * | 2010-03-11 | 2011-09-15 | Vertex Pharmaceuticals Incorporated | Co-crystals and pharmaceutical formulations comprising the same |
WO2011156545A1 (en) | 2010-06-09 | 2011-12-15 | Vertex Pharmaceuticals Incorporated | Viral dynamic model for hcv combination therapy |
WO2012009503A1 (en) | 2010-07-14 | 2012-01-19 | Vertex Pharmaceuticals Incorporated | Palatable pharmaceutical composition comprising vx-950 |
EP2630499A2 (en) | 2010-10-21 | 2013-08-28 | Vertex Pharmaceuticals Incorporated | Biomarkers for hcv infected patients |
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FR2976284B1 (fr) * | 2011-06-09 | 2013-05-24 | Servier Lab | Nouveaux co-cristaux d'agomelatine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent. |
US8466159B2 (en) | 2011-10-21 | 2013-06-18 | Abbvie Inc. | Methods for treating HCV |
US8492386B2 (en) | 2011-10-21 | 2013-07-23 | Abbvie Inc. | Methods for treating HCV |
EP2583680A3 (en) | 2011-10-21 | 2013-06-12 | Abbvie Inc. | Mono (PSI-7977) or combination treatment of DAAs for use in treating HCV |
ES2572328B1 (es) | 2011-10-21 | 2017-08-24 | Abbvie Inc. | Combinación de al menos dos agentes antivirales de acción directa y ribavirina pero no interferón, para su uso en el tratamiento del vhc |
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WO2014015217A1 (en) | 2012-07-19 | 2014-01-23 | Vertex Pharmaceuticals Incorporated | Biomarkers for hcv infected patients |
US9556216B2 (en) * | 2012-08-31 | 2017-01-31 | Novartis Ag | 2′-Ethynyl nucleoside derivatives for treatment of viral infections |
ITMI20131839A1 (it) * | 2013-11-06 | 2015-05-07 | Dipharma Francis Srl | Co-cristallo di un farmaco antidepressivo |
CN103819379A (zh) * | 2014-02-18 | 2014-05-28 | 中国科学院上海药物研究所 | 维生素d3的胆甾烷醇共结晶及其制备方法和应用 |
CN105696066B (zh) * | 2015-10-26 | 2018-07-03 | 西北大学 | 一种压片法制备共晶的方法 |
EP3448392A4 (en) | 2016-04-28 | 2020-01-15 | Emory University | ALCYNE-CONTAINING NUCLEOTIDES AND NUCLEOSIDES THERAPEUTIC COMPOSITIONS AND USES THEREOF |
CN113295723B (zh) * | 2021-07-27 | 2021-09-28 | 西南石油大学 | 一种岩石中粘土矿物的分子模拟表征方法 |
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-
2008
- 2008-02-27 PT PT08726147T patent/PT2114924E/pt unknown
- 2008-02-27 US US12/528,977 patent/US8759353B2/en not_active Expired - Fee Related
- 2008-02-27 JP JP2009551708A patent/JP2010519330A/ja active Pending
- 2008-02-27 SI SI200830602T patent/SI2114924T1/sl unknown
- 2008-02-27 AR ARP080100809A patent/AR065498A1/es not_active Application Discontinuation
- 2008-02-27 NZ NZ579442A patent/NZ579442A/en not_active IP Right Cessation
- 2008-02-27 GE GEAP200811488A patent/GEP20125645B/en unknown
- 2008-02-27 AP AP2009004960A patent/AP2009004960A0/xx unknown
- 2008-02-27 WO PCT/US2008/002568 patent/WO2008106151A2/en active Application Filing
- 2008-02-27 AT AT08726147T patent/ATE542815T1/de active
- 2008-02-27 CA CA002679312A patent/CA2679312A1/en not_active Abandoned
- 2008-02-27 KR KR1020097020031A patent/KR20090115970A/ko not_active Application Discontinuation
- 2008-02-27 TW TW097106897A patent/TW200846343A/zh unknown
- 2008-02-27 EP EP11195294A patent/EP2463285A1/en not_active Withdrawn
- 2008-02-27 EP EP11195217A patent/EP2463284A1/en not_active Withdrawn
- 2008-02-27 MX MX2009009182A patent/MX2009009182A/es active IP Right Grant
- 2008-02-27 DK DK08726147.5T patent/DK2114924T3/da active
- 2008-02-27 ES ES08726147T patent/ES2379905T3/es active Active
- 2008-02-27 AU AU2008219607A patent/AU2008219607B2/en not_active Ceased
- 2008-02-27 RS RS20120160A patent/RS52306B/en unknown
- 2008-02-27 BR BRPI0807907A patent/BRPI0807907A2/pt not_active IP Right Cessation
- 2008-02-27 CN CN200880013606A patent/CN101687856A/zh active Pending
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- 2008-02-27 EA EA200970806A patent/EA200970806A1/ru unknown
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2009
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- 2009-08-27 IL IL200616A patent/IL200616A0/en unknown
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Also Published As
Publication number | Publication date |
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BRPI0807907A2 (pt) | 2017-05-16 |
KR20090115970A (ko) | 2009-11-10 |
SI2114924T1 (sl) | 2012-06-29 |
CO6220963A2 (es) | 2010-11-19 |
ATE542815T1 (de) | 2012-02-15 |
GEP20125645B (en) | 2012-09-25 |
RS52306B (en) | 2012-12-31 |
MX2009009182A (es) | 2009-09-04 |
TW200846343A (en) | 2008-12-01 |
EP2463285A1 (en) | 2012-06-13 |
CN101687856A (zh) | 2010-03-31 |
ECSP099600A (es) | 2009-09-29 |
WO2008106151A2 (en) | 2008-09-04 |
CY1112865T1 (el) | 2016-04-13 |
AP2009004960A0 (en) | 2009-08-31 |
US8759353B2 (en) | 2014-06-24 |
AU2008219607B2 (en) | 2013-09-12 |
NZ579442A (en) | 2012-02-24 |
AR065498A1 (es) | 2009-06-10 |
DK2114924T3 (da) | 2012-04-10 |
EP2463284A1 (en) | 2012-06-13 |
WO2008106151A3 (en) | 2008-11-06 |
EP2114924B1 (en) | 2012-01-25 |
CA2679312A1 (en) | 2008-09-04 |
EP2114924A2 (en) | 2009-11-11 |
JP2010519330A (ja) | 2010-06-03 |
US20110059987A1 (en) | 2011-03-10 |
IL200616A0 (en) | 2010-05-17 |
ES2379905T3 (es) | 2012-05-04 |
AU2008219607A1 (en) | 2008-09-04 |
PL2114924T3 (pl) | 2012-07-31 |
EA200970806A1 (ru) | 2010-08-30 |
PT2114924E (pt) | 2012-04-03 |
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