LV10961B - Novel colon- or ileum-specific steroid derivatives - Google Patents
Novel colon- or ileum-specific steroid derivatives Download PDFInfo
- Publication number
- LV10961B LV10961B LVP-95-207A LV950207A LV10961B LV 10961 B LV10961 B LV 10961B LV 950207 A LV950207 A LV 950207A LV 10961 B LV10961 B LV 10961B
- Authority
- LV
- Latvia
- Prior art keywords
- compound according
- epimer
- gcs
- sugar
- formula
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
- C07J71/0005—Oxygen-containing hetero ring
- C07J71/0026—Oxygen-containing hetero ring cyclic ketals
- C07J71/0031—Oxygen-containing hetero ring cyclic ketals at positions 16, 17
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- 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]
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
- Medicines Containing Plant Substances (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Claims (20)
- LV 10961 JAUNI STEROĪDU ATVASINĀJUMI LOKZARNAS VAI LĪKUMAINĀS ZARNAS ĀRSTĒŠANAI Patenta formula 1. Savienojums ar vispārīgo formulu GCS1 - 0 - Cukurs1 kurā GCS1 ir glikokortikosteroīds (GCS’-OH) ar augstu pirmējās metaboliskās pārvēršanās pakāpi aknās, izvēlēts no grupas ar formulu I c=o*2 kā epimēru maisījums vai ka atbilstošs tīrs 22R-epimērs vai 22S-epimērs, vai no savienojumiem ar formulu II, -2- ch2— ΟΧ3 ο (22ΓχΗ3 pie kam minētajās formulās Xi un Χ2 aizvietotāji ir vienādi vai dažādi -ūdeņradis, fluors, hlors vai broms, Xs aizvietotāji ir fluors, hlors vai broms, R ir ogļūdeņraža virkne ar Cm, un pozīcija 1,2 ir piesātināta vai dubultsaite, Cukurs1 ir monosaharida, disaharida vai oligosahanda atlikums, GCS ir 21. pozīcijā ar glikozīda saiti piesaistīts cukuram, kā arī to farmaceitiski un farmakoloģiski pieņemami sāļi.
- 2. Savienojums saskaņā ar 1.p., kurā GCS1 ir 22R-epimērs ar formulu I.
- 3. Savienojums saskaņā ar 1.p., kurā GCS1 ir budesonīda daļas 22-epimers CH2“O ‘3 - LV 10961 vai savienojuma IV 22R-epimērs ar formuluvai savienojuma V 22R-epimērs ar formulu
- 4. Savienojums saskaņā ar jebkuru p. 1.-3., kurā Cukurs’-OH ir D-glikoze, D-galaktoze, D-celobioze vai D-laktoze.
- 5. Savienojums saskaņā ar jebkuru p.1 .-3., kurā Cukurs’-OH ir D-glukuronskābe vai D-galaktouronskābe. 6. Savienojums saskaņā ar 1.p., kurā Cukurs’-OH ir /3-D-glikoze. -4-
- 7. Savienojums saskaņā ar 1.p., kurā Cukurs1-OH ir /3-D-glukuronskābe.
- 8. Savienojums saskaņā ar 2.p., kurā Cukurs1-OH ir /3-D-glikoze.
- 9. Savienojums saskaņā ar 2.p.f kurā Cukurs1-OH ir /3- D-gluku ronskābe.
- 10. Savienojums saskaņā ar 3.p., kurā Cukurs’-OH ir /3-D-glikoze.
- 11. Savienojums saskaņā ar 3.p., kurā Cukurs1-OH ir /3-D-glukuronskābe.
- 12. Savienojums saskaņā ar 2.p., kas ir (22R) - 16a,17a -butilidēndioksi - 6a - 9a - difluor -11/3 - hidroksi -4- pregnīn - 3,20 - dion - 21-il /3-D-glikopiranozīds.
- 13. Savienojums saskaņā ar 2.p., kas ir (22R) - 16a,17a -butilidēndioksi -11/3 - hidroksipregna -1,4 - dien - 3,20 - dion - 21 - il /3-D-glikopiranozīds.
- 14. Savienojums saskaņā ar 2.p., kas ir nātrija [ (22R)- 16a, 17a - butilidēndioksi - 6a,9a - difluor -11/3 - hidroksi - 4 - pregnīn - 3,20 -dion - 21 - il /3-D-glikopiranozīd 3 ] uronāts.
- 15. Savienojums saskaņā ar 2.p., kas ir nātrija [ (22R) - 16a, 17a - butilidēndioksi -11/3 - hidroksipregna -1,4 - diēn - 3,20 - dion - 21 - il -5- LV 10961 β-D-glikopiranozīd ] uronāts.
- 16. Savienojuma saskaņā ar 1.p. iegūšanas paņēmiens, kurā cukuru kondensē ar GCS1-OH ar formulu VI, VI A, VI B vai VII, pie kam X-, X2, X3, R un Ci - C2 saistībai ir tās pašas 1.p. definētās nozīmes. CH2OHCHR *2 VI ch2ohVIA -6- CH2OHX2 c.: " H VI B CH2OHΧ3 CH3 ch3 VII 17. saskaņā » 18. jebkuru 19. Paņēmiens saskaņā ar 16.p., ar kuru iegūst savienojumu ar jebkuru p.2.-15. Farmaceitisks preparāts, kas satur savienojumu saskaņā ar p. 1.-15. kā aktīvo sastāvdaļu. Farmaceitisks preparāts saskaņā ar 1 8.p. dozētā formā. -7- LV 10961
- 20. Farmaceitisks preparāts saskaņā ar jebkuru p.18.-19., kas satur aktīvo sastāvdaļu kopā ar farmaceitiski pieņemamu nesēju.
- 21. Savienojums saskaņā ar 1.p. lietošanai terāpijā.
- 22. Savienojuma saskaņā ar 1.p. lietošana, ražojot no tā ārstniecības līdzekli zarnu gļotādu iekaisumu ārstēšanai.
- 23. Savienojuma saskaņā ar 22.p. lietošana, ražojot no tā ārstniecības līdzekli čūlainā kolīta ārstēšanai.
- 24. Savienojuma saskaņā ar 22.p. lietošana, ražojot no tā ārstniecības līdzekli Krona slimības ārstēšanai.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
SE9300030A SE9300030D0 (sv) | 1993-01-08 | 1993-01-08 | Novel colon- or ileum-specific steroid derivatives |
SE9300082A SE9300082D0 (sv) | 1993-01-14 | 1993-01-14 | Novel colon- or ileum-specific steroid derivatives |
PCT/SE1993/001081 WO1994015947A1 (en) | 1993-01-08 | 1993-12-17 | Novel colon- or ileum-specific steroid derivatives |
Publications (2)
Publication Number | Publication Date |
---|---|
LV10961A LV10961A (lv) | 1995-12-20 |
LV10961B true LV10961B (en) | 1996-08-20 |
Family
ID=26661623
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
LVP-95-207A LV10961B (en) | 1993-01-08 | 1995-07-05 | Novel colon- or ileum-specific steroid derivatives |
Country Status (22)
Country | Link |
---|---|
US (2) | US5908833A (lv) |
EP (1) | EP0678097B1 (lv) |
JP (1) | JP3366640B2 (lv) |
KR (1) | KR960700266A (lv) |
AT (1) | ATE183192T1 (lv) |
BR (1) | BR9307746A (lv) |
CA (1) | CA2152374A1 (lv) |
CZ (1) | CZ171095A3 (lv) |
DK (1) | DK0678097T3 (lv) |
ES (1) | ES2137353T3 (lv) |
FI (1) | FI953358A (lv) |
GR (1) | GR3031789T3 (lv) |
HU (1) | HU221584B (lv) |
IS (1) | IS4111A (lv) |
LV (1) | LV10961B (lv) |
NO (1) | NO305367B1 (lv) |
NZ (1) | NZ259596A (lv) |
PL (1) | PL178307B1 (lv) |
RU (1) | RU95115547A (lv) |
SK (1) | SK87295A3 (lv) |
TW (1) | TW261615B (lv) |
WO (1) | WO1994015947A1 (lv) |
Families Citing this family (19)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
HU221584B (hu) * | 1993-01-08 | 2002-11-28 | Aktiebolaget Astra | Új vastagbél- (colon) vagy csípőbél- (ileum) specifikus, cukortartalmú szteroidszármazékok, ezeket tartalmazó gyógyszerkészítmények és előállításuk |
DE69425439D1 (de) * | 1993-09-29 | 2000-09-07 | Nissin Food Products Ltd | In stellung 21 substituierte steroide |
US6028190A (en) | 1994-02-01 | 2000-02-22 | The Regents Of The University Of California | Probes labeled with energy transfer coupled dyes |
US6166024A (en) | 1995-03-30 | 2000-12-26 | Mayo Foundation For Medical Education And Research | Use of topical azathioprine and thioguanine to treat colorectal adenomas |
WO1999047541A1 (fr) * | 1998-03-19 | 1999-09-23 | Nissin Food Products Co., Ltd. | Composes steroides glycosyles a substitution en position 21 |
US20030083231A1 (en) * | 1998-11-24 | 2003-05-01 | Ahlem Clarence N. | Blood cell deficiency treatment method |
JP5005127B2 (ja) | 1999-05-04 | 2012-08-22 | ストラカン・インターナショナル・リミテッド | アンドロゲングリコシド及びそのアンドロゲン作用活性 |
US7431943B1 (en) | 1999-06-14 | 2008-10-07 | Cosmo Technologies Limited | Controlled release and taste masking oral pharmaceutical compositions |
US8895064B2 (en) | 1999-06-14 | 2014-11-25 | Cosmo Technologies Limited | Controlled release and taste masking oral pharmaceutical composition |
WO2001051057A2 (en) * | 2000-01-14 | 2001-07-19 | Strakan Limited | Glycosides and orthoester glycosides of glucocorticoids and uses thereof |
SE0101220D0 (sv) * | 2001-04-04 | 2001-04-04 | Astrazeneca Ab | New use |
ES2315600T3 (es) * | 2004-08-09 | 2009-04-01 | Deutsches Krebsforschungszentrum Stiftung Des Offentlichen Rechts | Conjugados de albumina que contienen un ligador glucuronico. |
WO2008100560A2 (en) * | 2007-02-14 | 2008-08-21 | University Of Southern California | Estrogen receptor modulators, associated pharmaceutical compositions and methods of use |
US10154964B2 (en) | 2011-09-07 | 2018-12-18 | Cosmo Technologies Limited | Controlled release and taste masking oral pharmaceutical composition |
AU2017359043B2 (en) | 2016-11-08 | 2022-06-16 | Regeneron Pharmaceuticals, Inc. | Steroids and protein-conjugates thereof |
WO2018177381A1 (zh) | 2017-03-30 | 2018-10-04 | 合肥合源药业有限公司 | 乳果糖糖苷化合物、其制备方法及其用途 |
MX2019013690A (es) | 2017-05-18 | 2020-01-27 | Regeneron Pharma | Conjugados de farmaco-proteina con ciclodextrina. |
US20190209702A1 (en) * | 2018-01-08 | 2019-07-11 | Regeneron Pharmaceuticals, Inc. | Steroids and antibody-conjugates thereof |
CA3098453A1 (en) | 2018-05-09 | 2019-11-14 | Regeneron Pharmaceuticals, Inc. | Anti-msr1 antibodies and methods of use thereof |
Family Cites Families (32)
Publication number | Priority date | Publication date | Assignee | Title |
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US3992534A (en) * | 1972-05-19 | 1976-11-16 | Ab Bofors | Compositions and method of treating with component B of stereoisomeric mixtures of 2'-unsymmetrical 16,17-methylenedioxy steriods |
SE378110B (lv) * | 1972-05-19 | 1975-08-18 | Bofors Ab | |
US3996359A (en) * | 1972-05-19 | 1976-12-07 | Ab Bofors | Novel stereoisomeric component A of stereoisomeric mixtures of 2'-unsymmetrical 16,17-methylenedioxy steroid 21-acylates, compositions thereof, and method of treating therewith |
SE378109B (lv) * | 1972-05-19 | 1975-08-18 | Bofors Ab | |
US3938233A (en) * | 1974-08-12 | 1976-02-17 | Cannon Robert B | Heat transfer apparatus |
DE2803660A1 (de) * | 1978-01-25 | 1979-07-26 | Schering Ag | Neue in 17-position substituierte steroide der pregnanreihe, ihre herstellung und verwendung |
EP0003341B1 (de) * | 1978-01-25 | 1984-06-27 | Schering Aktiengesellschaft | 11,17-substituierte Pregnane, ihre Herstellung und Verwendung zur Herstellung von pharmazeutischen Präparaten |
US4221787A (en) * | 1978-03-28 | 1980-09-09 | Interx Research Corporation | Esteramide prodrugs of anti-inflammatory corticosteroids |
SE8008524L (sv) * | 1980-12-04 | 1982-06-05 | Draco Ab | 4-pregnen-derivat, ett forfarande for deras framstellning, beredning och metod for behandling av inflammatoriska tillstand |
US4456602A (en) * | 1982-08-23 | 1984-06-26 | The Upjohn Company | Amine containing ester prodrugs of corticosteroids |
US4443440A (en) * | 1982-08-30 | 1984-04-17 | The Upjohn Company | Amine containing ester prodrugs of corticosteroids |
US4472392A (en) * | 1983-01-21 | 1984-09-18 | The Upjohn Company | Sulfonate containing ester prodrugs of corticosteroids |
US4469689A (en) * | 1983-03-30 | 1984-09-04 | The Upjohn Company | Sulfonate containing ester prodrugs of corticosteroids |
WO1984004041A1 (en) * | 1983-04-14 | 1984-10-25 | Univ California | Colon-specific drug delivery system |
US4959358A (en) * | 1983-06-06 | 1990-09-25 | Beth Israel Hospital Assn. | Drug administration |
US4548922A (en) * | 1983-06-06 | 1985-10-22 | Beth Israel Hospital | Drug administration |
SE8306370D0 (sv) * | 1983-11-18 | 1983-11-18 | Draco Ab | Novel androstane-17beta-carboxylic acid esters, a process and intermediates for their preparation, compositions and method for the treatment of inflammatory conditions |
US4588718A (en) * | 1984-03-28 | 1986-05-13 | The Upjohn Company | Carboxy containing ester prodrugs of corticosteroids |
SE8403905D0 (sv) * | 1984-07-30 | 1984-07-30 | Draco Ab | Liposomes and steroid esters |
US5215979A (en) * | 1985-12-19 | 1993-06-01 | Aktiebolaget Draco | 16,17-acetalsubstituted pregnane 21-oic acid derivatives |
GB8600489D0 (en) * | 1986-01-09 | 1986-02-12 | Erba Farmitalia | Aminoglycoside steroids |
GB8600490D0 (en) * | 1986-01-09 | 1986-02-12 | Erba Farmitalia | Aminoglycoside norcholanic acid lactams |
GB8600491D0 (en) * | 1986-01-09 | 1986-02-12 | Erba Farmitalia | Aminoglycoside norcholanic acid derivatives |
HU198216B (en) * | 1986-05-12 | 1989-08-28 | Kanto Ishi Pharma Co Ltd | Process for producing sialosyl-cholesterin and pharmaceutical compositions containing them as active components |
CA1299653C (en) * | 1988-07-07 | 1992-04-28 | Markwell Medical Institute, Inc. | Biological fluid measuring device |
US5643602A (en) * | 1989-11-22 | 1997-07-01 | Astra Aktiebolag | Oral composition for the treatment of inflammatory bowel disease |
SE8903914D0 (sv) * | 1989-11-22 | 1989-11-22 | Draco Ab | Oral composition for the treatment of inflammatory bowel diseases |
SE9100342D0 (sv) * | 1991-02-04 | 1991-02-04 | Astra Ab | Novel steroid esters |
US5888995A (en) * | 1991-02-04 | 1999-03-30 | Astra Aktiebolag | Steroid esters |
SE9100341D0 (sv) * | 1991-02-04 | 1991-02-04 | Astra Ab | Novel steroids |
WO1993022334A1 (en) * | 1992-05-04 | 1993-11-11 | Sri International | Pharmaceutical compositions and methods for colonic delivery of corticosteroids |
HU221584B (hu) * | 1993-01-08 | 2002-11-28 | Aktiebolaget Astra | Új vastagbél- (colon) vagy csípőbél- (ileum) specifikus, cukortartalmú szteroidszármazékok, ezeket tartalmazó gyógyszerkészítmények és előállításuk |
-
1993
- 1993-12-17 HU HU9502087A patent/HU221584B/hu not_active IP Right Cessation
- 1993-12-17 DK DK94904364T patent/DK0678097T3/da active
- 1993-12-17 CA CA002152374A patent/CA2152374A1/en not_active Abandoned
- 1993-12-17 JP JP51591394A patent/JP3366640B2/ja not_active Expired - Lifetime
- 1993-12-17 RU RU95115547/04A patent/RU95115547A/ru unknown
- 1993-12-17 EP EP94904364A patent/EP0678097B1/en not_active Expired - Lifetime
- 1993-12-17 CZ CZ951710A patent/CZ171095A3/cs unknown
- 1993-12-17 NZ NZ259596A patent/NZ259596A/xx unknown
- 1993-12-17 AT AT94904364T patent/ATE183192T1/de not_active IP Right Cessation
- 1993-12-17 WO PCT/SE1993/001081 patent/WO1994015947A1/en not_active Application Discontinuation
- 1993-12-17 BR BR9307746A patent/BR9307746A/pt not_active Application Discontinuation
- 1993-12-17 KR KR1019950702801A patent/KR960700266A/ko not_active Application Discontinuation
- 1993-12-17 ES ES94904364T patent/ES2137353T3/es not_active Expired - Lifetime
- 1993-12-17 PL PL93309777A patent/PL178307B1/pl unknown
- 1993-12-17 SK SK872-95A patent/SK87295A3/sk unknown
- 1993-12-22 IS IS4111A patent/IS4111A/is unknown
-
1994
- 1994-07-04 TW TW083106090A patent/TW261615B/zh active
-
1995
- 1995-07-05 LV LVP-95-207A patent/LV10961B/en unknown
- 1995-07-06 NO NO952683A patent/NO305367B1/no unknown
- 1995-07-07 FI FI953358A patent/FI953358A/fi unknown
-
1996
- 1996-12-13 US US08/764,985 patent/US5908833A/en not_active Expired - Lifetime
-
1999
- 1999-03-03 US US09/261,247 patent/US6140308A/en not_active Expired - Lifetime
- 1999-11-09 GR GR990402882T patent/GR3031789T3/el unknown
Also Published As
Publication number | Publication date |
---|---|
FI953358A0 (fi) | 1995-07-07 |
BR9307746A (pt) | 1995-11-14 |
JPH08505616A (ja) | 1996-06-18 |
WO1994015947A1 (en) | 1994-07-21 |
ES2137353T3 (es) | 1999-12-16 |
KR960700266A (ko) | 1996-01-19 |
SK87295A3 (en) | 1996-04-03 |
CA2152374A1 (en) | 1994-07-21 |
LV10961A (lv) | 1995-12-20 |
IS4111A (is) | 1994-07-09 |
PL309777A1 (en) | 1995-11-13 |
RU95115547A (ru) | 1997-06-10 |
ATE183192T1 (de) | 1999-08-15 |
HU9502087D0 (en) | 1995-09-28 |
EP0678097B1 (en) | 1999-08-11 |
AU678803B2 (en) | 1997-06-12 |
JP3366640B2 (ja) | 2003-01-14 |
NO305367B1 (no) | 1999-05-18 |
HUT73227A (en) | 1996-07-29 |
CZ171095A3 (en) | 1996-01-17 |
US5908833A (en) | 1999-06-01 |
FI953358A (fi) | 1995-07-07 |
HU221584B (hu) | 2002-11-28 |
PL178307B1 (pl) | 2000-04-28 |
TW261615B (lv) | 1995-11-01 |
NO952683L (no) | 1995-07-06 |
GR3031789T3 (en) | 2000-02-29 |
EP0678097A1 (en) | 1995-10-25 |
AU5844794A (en) | 1994-08-15 |
NZ259596A (en) | 1997-04-24 |
DK0678097T3 (da) | 2000-02-07 |
US6140308A (en) | 2000-10-31 |
NO952683D0 (no) | 1995-07-06 |
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