WO2006080412A3 - Cyanopyrrolidine derivative-containing composition for solid pharmaceutical preparations, solid pharmaceutical preparation containing the composition, and process for producing the solid pharmaceutical preparation - Google Patents
Cyanopyrrolidine derivative-containing composition for solid pharmaceutical preparations, solid pharmaceutical preparation containing the composition, and process for producing the solid pharmaceutical preparation Download PDFInfo
- Publication number
- WO2006080412A3 WO2006080412A3 PCT/JP2006/301258 JP2006301258W WO2006080412A3 WO 2006080412 A3 WO2006080412 A3 WO 2006080412A3 JP 2006301258 W JP2006301258 W JP 2006301258W WO 2006080412 A3 WO2006080412 A3 WO 2006080412A3
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- group
- solid pharmaceutical
- composition
- pharmaceutical preparation
- atom
- Prior art date
Links
- 239000000825 pharmaceutical preparation Substances 0.000 title abstract 4
- 239000007787 solid Substances 0.000 title abstract 4
- 239000000203 mixture Substances 0.000 title abstract 3
- QJRYYOWARFCJQZ-UHFFFAOYSA-N pyrrolidine-1-carbonitrile Chemical class N#CN1CCCC1 QJRYYOWARFCJQZ-UHFFFAOYSA-N 0.000 title abstract 2
- 238000000034 method Methods 0.000 title 1
- 125000005843 halogen group Chemical group 0.000 abstract 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 150000001413 amino acids Chemical class 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 1
- 239000004615 ingredient Substances 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 230000000087 stabilizing effect Effects 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 235000000346 sugar Nutrition 0.000 abstract 1
- 150000005846 sugar alcohols Chemical class 0.000 abstract 1
- 150000008163 sugars Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 125000004434 sulfur atom Chemical group 0.000 abstract 1
- 125000003396 thiol group Chemical group [H]S* 0.000 abstract 1
Classifications
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- 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
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
A composition for solid pharmaceutical preparations, essentially consisting of a cyanopyrrolidine derivative represented by the following general formula (1) or a pharmaceutically acceptable salt thereof, and at least one stabilizing ingredient selected from the group consisting of sugars and sugar alcohols, [Formula 1] [wherein R1 represents, for example, a halogen atom or a hydroxyl group, R3 and R4 may be the same or different, each represents, for example, a hydrogen atom or a halogen atom, X represents an oxygen atom or a sulfur atom, Y represents, for example, a group represented by -CR5R6- (wherein R5 and R6 may be the same or different, each represents, for example, a hydrogen atom or a halogen atom), W represents, for example, a hydrogen atom or an acyl group derived from naturally occurring amino acids, and Z represents, for example, a hydrogen atom or an alkyl group of 1 to 10 carbon atoms which may be substituted with one or more substituents selected from the group consisting of a halogen atom, a hydroxyl group, a hydroxylalkyl group of 1 to 5 carbon atoms, a carboxyl group, a mercapto group and the like].
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2005022193A JP2008024592A (en) | 2005-01-28 | 2005-01-28 | Cyanopyrrolidine derivative-containing composition for solid preparation, solid preparation containing the composition and process for producing the solid preparation |
| JP2005-022193 | 2005-01-28 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| WO2006080412A2 WO2006080412A2 (en) | 2006-08-03 |
| WO2006080412A3 true WO2006080412A3 (en) | 2006-09-21 |
Family
ID=36570928
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/JP2006/301258 WO2006080412A2 (en) | 2005-01-28 | 2006-01-20 | Cyanopyrrolidine derivative-containing composition for solid pharmaceutical preparations, solid pharmaceutical preparation containing the composition, and process for producing the solid pharmaceutical preparation |
Country Status (6)
| Country | Link |
|---|---|
| JP (1) | JP2008024592A (en) |
| AR (1) | AR052197A1 (en) |
| DO (1) | DOP2006000019A (en) |
| PE (1) | PE20061199A1 (en) |
| TW (1) | TW200637815A (en) |
| WO (1) | WO2006080412A2 (en) |
Citations (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0280999A2 (en) * | 1987-02-24 | 1988-09-07 | Warner-Lambert Company | Stabilized pharmaceutical compositions containing angiotensin-converting enzyme inhibitors |
| WO2000034241A1 (en) * | 1998-12-10 | 2000-06-15 | Novartis Ag | N-substituted 2-cyanopyrrolidines |
| WO2001068603A2 (en) * | 2000-03-10 | 2001-09-20 | Bristol-Myers Squibb Co. | Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl iv, processes for their preparation, and their use |
| WO2001096295A2 (en) * | 2000-06-13 | 2001-12-20 | Novartis Ag | 2-cyanopyrrolidine derivatives and their use as medicaments |
| WO2003057144A2 (en) * | 2001-12-26 | 2003-07-17 | Guilford Pharmaceuticals | Change inhibitors of dipeptidyl peptidase iv |
| EP1333025A1 (en) * | 2000-11-10 | 2003-08-06 | Taisho Pharmaceutical Co., Ltd | Cyanopyrrolidine derivatives |
| WO2003074500A2 (en) * | 2002-03-06 | 2003-09-12 | Sanofi-Aventis | N-aminoacetyl-pyrrolidine-2-carbonitriles and their use as ddp-iv inhibitors |
| WO2004009544A1 (en) * | 2002-07-23 | 2004-01-29 | Yamanouchi Pharmaceutical Co., Ltd. | 2-cyano-4-fluoropyrrolidine derivative or its salt |
| WO2004020407A1 (en) * | 2002-08-29 | 2004-03-11 | Taisho Pharmaceutical Co.,Ltd. | Benzenesulfonate of 4-fluoro-2-cyanopyrrolidine derivative |
| US20040235752A1 (en) * | 2001-06-25 | 2004-11-25 | Pitt Gary Robert William | 3-fluoro-pyrrolidines as antidiabetic agents |
| WO2005021536A2 (en) * | 2003-08-29 | 2005-03-10 | Sanofi-Aventis | Adamantane and azabicyclo-octane and nonane derivatives, process of their preparation and their use as dpp-iv inhibitors |
| WO2005067976A2 (en) * | 2004-01-20 | 2005-07-28 | Novartis Ag | Direct compression formulation and process |
-
2005
- 2005-01-28 JP JP2005022193A patent/JP2008024592A/en active Pending
-
2006
- 2006-01-20 WO PCT/JP2006/301258 patent/WO2006080412A2/en not_active Application Discontinuation
- 2006-01-24 DO DO2006000019A patent/DOP2006000019A/en unknown
- 2006-01-24 PE PE2006000103A patent/PE20061199A1/en not_active Application Discontinuation
- 2006-01-24 AR ARP060100263A patent/AR052197A1/en not_active Application Discontinuation
- 2006-01-25 TW TW095102875A patent/TW200637815A/en unknown
Patent Citations (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0280999A2 (en) * | 1987-02-24 | 1988-09-07 | Warner-Lambert Company | Stabilized pharmaceutical compositions containing angiotensin-converting enzyme inhibitors |
| WO2000034241A1 (en) * | 1998-12-10 | 2000-06-15 | Novartis Ag | N-substituted 2-cyanopyrrolidines |
| WO2001068603A2 (en) * | 2000-03-10 | 2001-09-20 | Bristol-Myers Squibb Co. | Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl iv, processes for their preparation, and their use |
| WO2001096295A2 (en) * | 2000-06-13 | 2001-12-20 | Novartis Ag | 2-cyanopyrrolidine derivatives and their use as medicaments |
| EP1333025A1 (en) * | 2000-11-10 | 2003-08-06 | Taisho Pharmaceutical Co., Ltd | Cyanopyrrolidine derivatives |
| US20040235752A1 (en) * | 2001-06-25 | 2004-11-25 | Pitt Gary Robert William | 3-fluoro-pyrrolidines as antidiabetic agents |
| WO2003057144A2 (en) * | 2001-12-26 | 2003-07-17 | Guilford Pharmaceuticals | Change inhibitors of dipeptidyl peptidase iv |
| WO2003074500A2 (en) * | 2002-03-06 | 2003-09-12 | Sanofi-Aventis | N-aminoacetyl-pyrrolidine-2-carbonitriles and their use as ddp-iv inhibitors |
| WO2004009544A1 (en) * | 2002-07-23 | 2004-01-29 | Yamanouchi Pharmaceutical Co., Ltd. | 2-cyano-4-fluoropyrrolidine derivative or its salt |
| EP1541551A1 (en) * | 2002-07-23 | 2005-06-15 | Yamanouchi Pharmaceutical Co. Ltd. | 2-cyano-4-fluoropyrrolidine derivative or its salt |
| WO2004020407A1 (en) * | 2002-08-29 | 2004-03-11 | Taisho Pharmaceutical Co.,Ltd. | Benzenesulfonate of 4-fluoro-2-cyanopyrrolidine derivative |
| EP1535907A1 (en) * | 2002-08-29 | 2005-06-01 | Taisho Pharmaceutical Co., Ltd | Benzenesulfonate of 4-fluoro-2-cyanopyrrolidine derivative |
| WO2005021536A2 (en) * | 2003-08-29 | 2005-03-10 | Sanofi-Aventis | Adamantane and azabicyclo-octane and nonane derivatives, process of their preparation and their use as dpp-iv inhibitors |
| WO2005067976A2 (en) * | 2004-01-20 | 2005-07-28 | Novartis Ag | Direct compression formulation and process |
Also Published As
| Publication number | Publication date |
|---|---|
| DOP2006000019A (en) | 2006-07-15 |
| AR052197A1 (en) | 2007-03-07 |
| JP2008024592A (en) | 2008-02-07 |
| TW200637815A (en) | 2006-11-01 |
| WO2006080412A2 (en) | 2006-08-03 |
| PE20061199A1 (en) | 2006-11-18 |
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