HUP0101586A2 - Az 1S-[1 alfa(2S*, 3R*),9alfa]-6,10-dioxo-N-(2-etoxi-5-oxo-tetrahidro-3-furanil)-9-{[(1-izokinolil)-karbonil]-amino}-oktahidro-6H-piridazino[1,2-a][1,2]diazepin-1-karboxamid új kristályos formái, előállításuk és gyógyszerkészítmények - Google Patents
Az 1S-[1 alfa(2S*, 3R*),9alfa]-6,10-dioxo-N-(2-etoxi-5-oxo-tetrahidro-3-furanil)-9-{[(1-izokinolil)-karbonil]-amino}-oktahidro-6H-piridazino[1,2-a][1,2]diazepin-1-karboxamid új kristályos formái, előállításuk és gyógyszerkészítményekInfo
- Publication number
- HUP0101586A2 HUP0101586A2 HU0101586A HUP0101586A HUP0101586A2 HU P0101586 A2 HUP0101586 A2 HU P0101586A2 HU 0101586 A HU0101586 A HU 0101586A HU P0101586 A HUP0101586 A HU P0101586A HU P0101586 A2 HUP0101586 A2 HU P0101586A2
- Authority
- HU
- Hungary
- Prior art keywords
- crystalline forms
- following
- formula
- octahydro
- isoquinolyl
- Prior art date
Links
- -1 1-isoquinolyl Chemical group 0.000 title abstract 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 title abstract 2
- 238000002360 preparation method Methods 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 3
- 238000010521 absorption reaction Methods 0.000 abstract 2
- 238000002329 infrared spectrum Methods 0.000 abstract 2
- 238000004519 manufacturing process Methods 0.000 abstract 2
- 238000002844 melting Methods 0.000 abstract 2
- 230000008018 melting Effects 0.000 abstract 2
- 239000003960 organic solvent Substances 0.000 abstract 2
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- 230000018044 dehydration Effects 0.000 abstract 1
- 238000006297 dehydration reaction Methods 0.000 abstract 1
- 238000010586 diagram Methods 0.000 abstract 1
- AUHBCNJHXCDLMK-UHFFFAOYSA-N diazepine-1-carboxamide Chemical compound NC(=O)N1C=CC=CC=N1 AUHBCNJHXCDLMK-UHFFFAOYSA-N 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 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
- C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
- C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- 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
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Biochemistry (AREA)
- Immunology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Crystallography & Structural Chemistry (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Peptides Or Proteins (AREA)
Abstract
A találmány az (I) képletű 1S-[l...(2S*,3R*),9...]- -6,10-dioxo-N-(2-etoxi-5-oxo-tetrahidro-3-furanil)-9-{[(1-izokinolil)-karbonil]-amino}-oktahidro-6H-piridazino[ 1,2-a][1,2]diazepin-1-karboxamid két újkristályos - vízmentes és hidratált - formájára, azok előállítására ésalkalmazására, valamint ilyen kristályos formákat tartalmazógyógyszerkészítményekre vonatkozik. A vízmentes (I) képletű vegyületkristályos formája, az A-forma a következő tulajdonságok közüllegalább eggyel rendelkezik: a) endoterm olvadáspont 168 °C-tól; b)infravörös spektrum, amely körülbelül a következő hullámhosszúságoknálmutat jellemző abszorpciót (nujol, cm-1): 3253; 1789; 1702; 1681 és1644, valamint c) XR-diffrakciós diagram a következő jellemzőrácsállandókkal (d, A): 17,73; 8,87; 8,11; 7,50; 7,17;6,31; 6,09 és5,81. A hidratált (I) képletű vegyület kristályos formája, a B-forma akövetkező tulajdonságok közül legalább eggyel rendelkezik: a) endotermdehidratálódás 50 °C és 110 °C, valamint 110 °C és 130 °C között,továbbá endoterm olvadáspont 162 °C-tól; b) infravörös spektrum, amelyközelítőleg a következő hullámhosszúságoknál mutat jellemzőabszorpciót (nujol, cm-1): 356; 3447; 3322; 1778; 1682 és 1660,valamint c) XR-diffrakciós diagram a következő jellemzőrácsállandókkal (d, A): 11,34; 10,80; 10,06; 7,59; 7,16; 6,71; 6,41;6,11 és 5,44. A találmány szerinti kristályos formákat úgy állítjákelő, hogy amorf (I) képletű vegyületet belekevernek megfelelő szervesoldószerbe vagy szerves oldószerek elegyébe, és kikristályosítják akívánt A- vagy B-formát. A találmány szerinti kristályos formákat azICE (1b-inter-leukin konverziós enzim) aktivitásának gátlására szántgyógyszerek előállítására használják fel. Ó
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR9804367A FR2777279B1 (fr) | 1998-04-08 | 1998-04-08 | Nouvelles formes cristallines du 1s-[1alpha(2s*,3r*), 9 alpha] 6,10-dioxo-n-(2-ethoxy-5-oxo-tetrahydro-3-furanyl) -9[[(1-isoquinolyl)carbonyl]amino]octohydro-6h-pyridazino [1,2-a][1,2]diazepine-1-carboxamide |
| PCT/FR1999/000799 WO1999052935A1 (fr) | 1998-04-08 | 1999-04-07 | Formes cristallines du 1s-[1alpha (2s*,3r*),9alpha]-6, 10-dioxo-n- (2-ethoxy-5 -oxo-tetrahydro-3 -furanyl) -9-[[(1-isoquinolyl) carbonyl]-amino] octahydro-6h -piridazino[1, 2-a][1,2] diazepine-1- carboxamide |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| HUP0101586A2 true HUP0101586A2 (hu) | 2001-11-28 |
| HUP0101586A3 HUP0101586A3 (en) | 2002-11-28 |
| HU227561B1 HU227561B1 (en) | 2011-08-29 |
Family
ID=9524993
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0101586A HU227561B1 (en) | 1998-04-08 | 1999-04-07 | Crystalline forms of 1s-[1alpha (2s*,3r*), 9alpha]-6,10-dioxo-n-(2-ethoxy-5-oxo-tetrahydro-3 -furanyl)-9-[[(1-isoquinolyl) carbonyl]-amino] octahydro-6h-pyridazino[1,2-a][1,2]diazepin-1-carboxamide and pharmaceutical compositions containing them |
Country Status (38)
| Country | Link |
|---|---|
| US (2) | US6544977B1 (hu) |
| EP (1) | EP1070083B1 (hu) |
| JP (1) | JP2002511485A (hu) |
| KR (1) | KR100582981B1 (hu) |
| CN (1) | CN1202123C (hu) |
| AP (1) | AP1734A (hu) |
| AR (1) | AR018328A1 (hu) |
| AT (1) | ATE315044T1 (hu) |
| AU (1) | AU758042B2 (hu) |
| BG (1) | BG64736B1 (hu) |
| BR (1) | BR9909549A (hu) |
| CA (1) | CA2325629C (hu) |
| CU (1) | CU23055A3 (hu) |
| CZ (1) | CZ299744B6 (hu) |
| DE (1) | DE69929315T2 (hu) |
| DK (1) | DK1070083T3 (hu) |
| EA (1) | EA002761B1 (hu) |
| EE (1) | EE04467B1 (hu) |
| ES (1) | ES2253880T3 (hu) |
| FR (1) | FR2777279B1 (hu) |
| GE (1) | GEP20032974B (hu) |
| HK (1) | HK1038575B (hu) |
| HR (1) | HRP20000665B1 (hu) |
| HU (1) | HU227561B1 (hu) |
| ID (1) | ID26290A (hu) |
| IL (2) | IL138818A (hu) |
| ME (1) | ME01627B (hu) |
| NO (1) | NO327995B1 (hu) |
| NZ (1) | NZ507199A (hu) |
| PL (1) | PL197016B1 (hu) |
| RS (1) | RS49916B (hu) |
| SI (1) | SI1070083T1 (hu) |
| SK (1) | SK286267B6 (hu) |
| TR (1) | TR200002914T2 (hu) |
| TW (1) | TW522152B (hu) |
| UA (1) | UA71563C2 (hu) |
| WO (1) | WO1999052935A1 (hu) |
| ZA (1) | ZA200005438B (hu) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT2044025E (pt) * | 2006-06-30 | 2012-12-17 | Novartis Ag | Derivados de quinolinona e suas composições farmacêuticas |
| AU2014277867B2 (en) * | 2007-12-04 | 2016-11-03 | Arbutus Biopharma Corporation | Targeting lipids |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6204261B1 (en) * | 1995-12-20 | 2001-03-20 | Vertex Pharmaceuticals Incorporated | Inhibitors of interleukin-1β Converting enzyme inhibitors |
| US5552400A (en) * | 1994-06-08 | 1996-09-03 | Sterling Winthrop Inc. | Fused-bicyclic lactams as interleukin-1β converting enzyme inhibitors |
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1998
- 1998-04-08 FR FR9804367A patent/FR2777279B1/fr not_active Expired - Lifetime
-
1999
- 1999-03-15 TW TW088103966A patent/TW522152B/zh not_active IP Right Cessation
- 1999-03-30 AR ARP990101432A patent/AR018328A1/es active IP Right Grant
- 1999-04-07 ES ES99911890T patent/ES2253880T3/es not_active Expired - Lifetime
- 1999-04-07 RS YUP-608/00A patent/RS49916B/sr unknown
- 1999-04-07 BR BR9909549-1A patent/BR9909549A/pt not_active Application Discontinuation
- 1999-04-07 EE EEP200000586A patent/EE04467B1/xx unknown
- 1999-04-07 CZ CZ20003678A patent/CZ299744B6/cs not_active IP Right Cessation
- 1999-04-07 SK SK1488-2000A patent/SK286267B6/sk not_active IP Right Cessation
- 1999-04-07 CA CA2325629A patent/CA2325629C/fr not_active Expired - Fee Related
- 1999-04-07 KR KR1020007011159A patent/KR100582981B1/ko not_active IP Right Cessation
- 1999-04-07 AT AT99911890T patent/ATE315044T1/de active
- 1999-04-07 GE GEAP19995614A patent/GEP20032974B/en unknown
- 1999-04-07 DE DE69929315T patent/DE69929315T2/de not_active Expired - Lifetime
- 1999-04-07 DK DK99911890T patent/DK1070083T3/da active
- 1999-04-07 TR TR2000/02914T patent/TR200002914T2/xx unknown
- 1999-04-07 JP JP2000543491A patent/JP2002511485A/ja active Pending
- 1999-04-07 SI SI9930877T patent/SI1070083T1/sl unknown
- 1999-04-07 HU HU0101586A patent/HU227561B1/hu not_active IP Right Cessation
- 1999-04-07 CU CU20000213A patent/CU23055A3/es unknown
- 1999-04-07 ID IDW20002015A patent/ID26290A/id unknown
- 1999-04-07 US US09/647,858 patent/US6544977B1/en not_active Expired - Lifetime
- 1999-04-07 EP EP99911890A patent/EP1070083B1/fr not_active Expired - Lifetime
- 1999-04-07 WO PCT/FR1999/000799 patent/WO1999052935A1/fr active IP Right Grant
- 1999-04-07 ME MEP-2000-608A patent/ME01627B/me unknown
- 1999-04-07 AP APAP/P/2000/001939A patent/AP1734A/en active
- 1999-04-07 EA EA200001047A patent/EA002761B1/ru not_active IP Right Cessation
- 1999-04-07 PL PL343350A patent/PL197016B1/pl unknown
- 1999-04-07 CN CNB998071455A patent/CN1202123C/zh not_active Expired - Fee Related
- 1999-04-07 AU AU30416/99A patent/AU758042B2/en not_active Ceased
- 1999-04-07 NZ NZ507199A patent/NZ507199A/xx not_active IP Right Cessation
- 1999-07-04 UA UA2000116295A patent/UA71563C2/uk unknown
-
2000
- 2000-10-02 IL IL138818A patent/IL138818A/en not_active IP Right Cessation
- 2000-10-05 ZA ZA200005438A patent/ZA200005438B/en unknown
- 2000-10-06 NO NO20005060A patent/NO327995B1/no not_active IP Right Cessation
- 2000-10-06 BG BG104829A patent/BG64736B1/bg unknown
- 2000-10-09 HR HR20000665A patent/HRP20000665B1/xx not_active IP Right Cessation
-
2002
- 2002-01-07 HK HK02100107.8A patent/HK1038575B/zh not_active IP Right Cessation
- 2002-11-18 US US10/299,242 patent/US6946459B2/en not_active Expired - Lifetime
-
2005
- 2005-04-14 IL IL168047A patent/IL168047A/en not_active IP Right Cessation
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| HUP0101586A2 (hu) | Az 1S-[1 alfa(2S*, 3R*),9alfa]-6,10-dioxo-N-(2-etoxi-5-oxo-tetrahidro-3-furanil)-9-{[(1-izokinolil)-karbonil]-amino}-oktahidro-6H-piridazino[1,2-a][1,2]diazepin-1-karboxamid új kristályos formái, előállításuk és gyógyszerkészítmények | |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Lapse of definitive patent protection due to non-payment of fees |