FI106961B - Förfarande för framställning av terapeutiskt användbara bis-indolyl-1H-pyrrol-2,5-dionderivat - Google Patents
Förfarande för framställning av terapeutiskt användbara bis-indolyl-1H-pyrrol-2,5-dionderivat Download PDFInfo
- Publication number
- FI106961B FI106961B FI942158A FI942158A FI106961B FI 106961 B FI106961 B FI 106961B FI 942158 A FI942158 A FI 942158A FI 942158 A FI942158 A FI 942158A FI 106961 B FI106961 B FI 106961B
- Authority
- FI
- Finland
- Prior art keywords
- formula
- tetrahydropyrido
- indolyl
- pyrrole
- methyl
- Prior art date
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/08—Bronchodilators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
-
- 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
- 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
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/08—Vasodilators for multiple indications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Heart & Thoracic Surgery (AREA)
- Virology (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Pulmonology (AREA)
- Emergency Medicine (AREA)
- Obesity (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Urology & Nephrology (AREA)
- Molecular Biology (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Vascular Medicine (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyrrole Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Saccharide Compounds (AREA)
- Cephalosporin Compounds (AREA)
Claims (8)
1. Förfarande för framställning av terapeutiskt användbara bis-indolyl-lH-pyrrol-2,5-dionderivat med den 5 allmänna formeIn A H o=^ n=o oö~co / (CH2)m | (CH^n R2 CH R1 CH'' 15 1 HNR30 A var R1 är en lägre alkyl, R2 är en lägre alkyl, R30 är väte eller en uretanskyddsgrupp, m är 1 och n är 2 samt för framställning av farmaceutiskt godtagbara salter därav, 20 som syraföreningarna enligt formel A, var R30 är väte, bil-dar med baserna och som basföreningarna enligt formel A, var R30 är väte, bildar med syrorna, kännetecknat av a) hydrolysering och dehydrering av hydroxipyrro-linon med den allmänna formeln VI 25 Ό==\ η—on4 Coct^O 30 / (pH,)m ¥ VI (¾¾. | Ra CH R1 HN—R3 35 var R1, R2, m och n är sä som ovan definierats, R3 är en uretanskyddsgrupp och R4 är en lägre alkyl eller 106961 40 b) behandling av en substituerad furandion med den allmänna formeln VIII O / vm (CH2)n I R2
10 CH R* HN—R* var R1, R2, R3, m och n är sä som ovan definierats, med 15 hexametyldisilazan i närvaro av en alkanol och därefter för att erhalla en förening med formeln A, var R30 är väte, spjälks skyddsgruppen som är betecknad med R3 frän den erhällna föreningen med den allmänna formeln II 20 1 X / Ϊ, ^ 11 (CHj)n I Ra CH R1 HN-R3 30 var R1, R2, R3, m och n är sä som ovan definierats och • om sä önskas ändras syraföreningen enligt formel A med en bas till ett farmaceutiskt godtagbart salt eller ändras basföreningen enligt formel A med en syra till ett farmaceutiskt godtagbart salt. 35
2 . Förfarande enligt patentkrav 1, känneteck- nat av att man framställer 3-[8(S)-[l(R eller S)-amino- 106961 41 propyl] -6,7,8,9 -1 e t rahydropyr ido[l, 2 - a] indol -10 -yl] -4-(1-metyl-3 -indolyl) -ΙΗ-pyrrol-2,5-dion.
3. Förfarande enligt patentkrav 1, känneteck-nat av . att man framställer 3-[8 (S)-[l (S)-amino-2-metyl- 5 propyl]-6,7,8,9-tetrahydropyrido[l, 2-a]indol-10-yl]-4- (1-metyl-3 -indolyl) -ΙΗ-pyrrol-2,5-dion.
4. Förfarande enligt patentkrav 1, känneteck-nat av att man framställer 3-[8(R eller S)-1(R eller S)-aminoetyl]-6,7,8,9-tetrahydropyrido[l, 2-a]indol-10-yl]-4- (1- 10 metyl-3-indolyl)-lH-pyrrol-2,5-dion.
5. Förfarande enligt patentkrav 1, känneteck-nat av att man framställer 3-[8(R eller S)-1(R eller S)-aminopropyl]-6,7, 8,9-tetrahydropyrido[l,2-a]indol-10-yl]-4-(1-metyl-3-indolyl)-lH-pyrrol-2,5-dion. 15
6. Förfarande enligt patentkrav 1, känneteck- nat av att man framställer 3-[8(R eller S)-1(R eller S) -aminobutyl]-6,7,8,9-tetrahydropyrido[l, 2-a]indol-10-yl]-4-(1-metyl-3-indolyl)-lH-pyrrol-2,5-dion.
7. Förfarande enligt patentkrav 1, känneteck- 20 nat av att man framställer 3-[8(R eller S)-1(R eller S) - amino-2-metylpropyl]-6,7,8,9-tetrahydropyrido[l, 2-a]indol-10-yl]-4-(1-metyl-3-indolyl)-lH-pyrrol-2,5-dion.
8. Förfarande enligt patentkrav 1, känneteck-nat av att man framställer 3-[8 (S)-1 (R) -amino-2-metyl- 25 propyl]-6,7,8,9-tetrahydropyrido[l,2-a]indol-10-yl]-4-(1-metyl-3-indolyl)-lH-pyrrol-2,5-dion.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB939309602A GB9309602D0 (en) | 1993-05-10 | 1993-05-10 | Substituted pyrroles |
| GB9309602 | 1993-05-10 | ||
| GB9403249A GB9403249D0 (en) | 1993-05-10 | 1994-02-21 | Substituted pyrroles |
| GB9403249 | 1994-02-21 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| FI942158A0 FI942158A0 (sv) | 1994-05-10 |
| FI942158A7 FI942158A7 (sv) | 1994-11-11 |
| FI106961B true FI106961B (sv) | 2001-05-15 |
Family
ID=26302877
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| FI942158A FI106961B (sv) | 1993-05-10 | 1994-05-10 | Förfarande för framställning av terapeutiskt användbara bis-indolyl-1H-pyrrol-2,5-dionderivat |
Country Status (25)
| Country | Link |
|---|---|
| EP (1) | EP0624586B1 (sv) |
| JP (1) | JP2668818B2 (sv) |
| CN (1) | CN1048014C (sv) |
| AT (1) | ATE184007T1 (sv) |
| AU (1) | AU678435B2 (sv) |
| BG (1) | BG98761A (sv) |
| BR (1) | BR9401935A (sv) |
| CA (1) | CA2121567A1 (sv) |
| CZ (1) | CZ112894A3 (sv) |
| DE (1) | DE69420310T2 (sv) |
| DK (1) | DK0624586T3 (sv) |
| ES (1) | ES2137281T3 (sv) |
| FI (1) | FI106961B (sv) |
| GR (1) | GR3031901T3 (sv) |
| HR (1) | HRP940287B1 (sv) |
| HU (1) | HU215954B (sv) |
| IL (1) | IL109547A (sv) |
| IS (1) | IS1690B (sv) |
| LT (1) | LT3288B (sv) |
| LV (1) | LV11173B (sv) |
| NO (1) | NO301230B1 (sv) |
| NZ (1) | NZ260475A (sv) |
| RU (1) | RU2141960C1 (sv) |
| SI (1) | SI0624586T1 (sv) |
| SK (1) | SK53594A3 (sv) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG63570A1 (en) * | 1993-12-07 | 1999-03-30 | Lilly Co Eli | Protein kinase c inhibitors |
| US5624949A (en) * | 1993-12-07 | 1997-04-29 | Eli Lilly And Company | Protein kinase C inhibitors |
| US5843935A (en) * | 1993-12-07 | 1998-12-01 | Eli Lilly And Company | Protein kinase C inhibitors |
| US5723456A (en) * | 1993-12-07 | 1998-03-03 | Eli Lilly & Company | Therapeutic treatment for cardiovascular diseases |
| EP1449529B1 (en) * | 1993-12-23 | 2010-01-27 | Eli Lilly And Company | Protein Kinase C Inhibitors |
| EP0695755B1 (en) * | 1994-08-04 | 1998-10-21 | F. Hoffmann-La Roche AG | Pyrrolocarbazole |
| CN1225634A (zh) * | 1996-03-20 | 1999-08-11 | 伊莱利利公司 | 吲哚马来酰亚胺的合成 |
| KR100499190B1 (ko) * | 1996-03-29 | 2006-04-17 | 교와 핫꼬 고교 가부시끼가이샤 | 육모제 |
| US5859261A (en) * | 1997-03-20 | 1999-01-12 | Eli Lilly And Company | Synthesis of indolylmaleimides |
| BR0112965A (pt) | 2000-07-27 | 2003-07-08 | Hoffmann La Roche | Derivados de 3-indolil-4-fenil-1h-pirrol-2,5-diona como inibidores de glocogênio sintase cinase-3beta |
| PL211461B1 (pl) * | 2001-10-30 | 2012-05-31 | Dana Farber Cancer Inst Inc | Zastosowanie pochodnych staurosporyny do wytwarzania kompozycji farmaceutycznej do leczenia lub zapobiegania białaczkom i zespołom mielodysplastycznym, preparat farmaceutyczny do leczenia białaczek i zestaw farmaceutyczny |
| CA2393720C (en) | 2002-07-12 | 2010-09-14 | Eli Lilly And Company | Crystalline 2,5-dione-3-(1-methyl-1h-indol-3-yl)-4-[1-(pyridin-2-ylmethyl)piperidin-4-yl]-1h-indol-3-yl]-1h-pyrrole mono-hydrochloride |
| MXPA06001524A (es) | 2003-08-08 | 2006-05-15 | Novartis Ag | Combinaciones que comprenden estaurosporinas. |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3803620A1 (de) * | 1988-02-06 | 1989-08-17 | Goedecke Ag | Indolocarbazol-derivate, verfahren zu deren herstellung und diese enthaltende arzneimittel |
| IL89167A (en) * | 1988-02-10 | 1994-02-27 | Hoffmann La Roche | Substituted pyrroles, their manufacture and pharmaceutical compositions containing them |
| DE3833008A1 (de) * | 1988-09-29 | 1990-04-05 | Goedecke Ag | Pyrrolocarbozol-derivate, verfahren zu deren herstellung und deren verwendung als arzneimittel |
| MC2096A1 (fr) * | 1989-02-23 | 1991-02-15 | Hoffmann La Roche | Pyrroles substitues |
| CA2046801C (en) * | 1990-08-07 | 2002-02-26 | Peter D. Davis | Substituted pyrroles |
-
1994
- 1994-04-15 AU AU60555/94A patent/AU678435B2/en not_active Ceased
- 1994-04-26 CA CA002121567A patent/CA2121567A1/en not_active Abandoned
- 1994-05-02 EP EP94106812A patent/EP0624586B1/en not_active Expired - Lifetime
- 1994-05-02 AT AT94106812T patent/ATE184007T1/de not_active IP Right Cessation
- 1994-05-02 DK DK94106812T patent/DK0624586T3/da active
- 1994-05-02 DE DE69420310T patent/DE69420310T2/de not_active Expired - Fee Related
- 1994-05-02 ES ES94106812T patent/ES2137281T3/es not_active Expired - Lifetime
- 1994-05-02 SI SI9430273T patent/SI0624586T1/xx unknown
- 1994-05-04 HU HU9401298A patent/HU215954B/hu not_active IP Right Cessation
- 1994-05-04 IL IL10954794A patent/IL109547A/en not_active IP Right Cessation
- 1994-05-05 RU RU94015830A patent/RU2141960C1/ru active
- 1994-05-05 HR HR9309602.2A patent/HRP940287B1/xx not_active IP Right Cessation
- 1994-05-06 NO NO941682A patent/NO301230B1/no not_active IP Right Cessation
- 1994-05-06 CZ CZ941128A patent/CZ112894A3/cs unknown
- 1994-05-06 NZ NZ260475A patent/NZ260475A/en unknown
- 1994-05-09 CN CN94105846A patent/CN1048014C/zh not_active Expired - Fee Related
- 1994-05-09 LV LVP-94-100A patent/LV11173B/en unknown
- 1994-05-09 LT LTIP1927A patent/LT3288B/lt not_active IP Right Cessation
- 1994-05-09 SK SK535-94A patent/SK53594A3/sk unknown
- 1994-05-09 IS IS4162A patent/IS1690B/is unknown
- 1994-05-09 BR BR9401935A patent/BR9401935A/pt not_active Application Discontinuation
- 1994-05-09 JP JP6119542A patent/JP2668818B2/ja not_active Expired - Fee Related
- 1994-05-10 FI FI942158A patent/FI106961B/sv not_active IP Right Cessation
- 1994-05-10 BG BG98761A patent/BG98761A/xx unknown
-
1999
- 1999-11-18 GR GR990402995T patent/GR3031901T3/el unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MA | Patent expired |