RU2005131937A - Макролидные конъюгаты, с противовоспалительной активностью - Google Patents
Макролидные конъюгаты, с противовоспалительной активностью Download PDFInfo
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- RU2005131937A RU2005131937A RU2005131937/04A RU2005131937A RU2005131937A RU 2005131937 A RU2005131937 A RU 2005131937A RU 2005131937/04 A RU2005131937/04 A RU 2005131937/04A RU 2005131937 A RU2005131937 A RU 2005131937A RU 2005131937 A RU2005131937 A RU 2005131937A
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- inflammatory
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- 239000003120 macrolide antibiotic agent Substances 0.000 title claims 2
- 150000001875 compounds Chemical class 0.000 claims 37
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- 238000000034 method Methods 0.000 claims 6
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- UPSPUYADGBWSHF-UHFFFAOYSA-N tolmetin Chemical compound C1=CC(C)=CC=C1C(=O)C1=CC=C(CC(O)=O)N1C UPSPUYADGBWSHF-UHFFFAOYSA-N 0.000 claims 1
- UCCJWNPWWPJKGL-UHFFFAOYSA-N tropesin Chemical compound CC1=C(CC(=O)OCC(C(O)=O)C=2C=CC=CC=2)C2=CC(OC)=CC=C2N1C(=O)C1=CC=C(Cl)C=C1 UCCJWNPWWPJKGL-UHFFFAOYSA-N 0.000 claims 1
- 229950002470 tropesin Drugs 0.000 claims 1
- IYEPZNKOJZOGJG-UHFFFAOYSA-N xenbucin Chemical compound C1=CC(C(C(O)=O)CC)=CC=C1C1=CC=CC=C1 IYEPZNKOJZOGJG-UHFFFAOYSA-N 0.000 claims 1
- 229950005298 xenbucin Drugs 0.000 claims 1
- 229950000707 ximoprofen Drugs 0.000 claims 1
- FVANAXVFEXRXSV-JMBQMWJUSA-N CCCC([C@](C)([C@@H]([C@@H](C)N(CCCCCCNC(Cc(c1c2)c(C)[n](C(c(cc3)ccc3Cl)=O)c1ccc2OC)=O)C[C@H](C)C[C@H](C[C@@H](C)[C@@H]([C@H]1C)O)[O]=C)O)O)OC1=O Chemical compound CCCC([C@](C)([C@@H]([C@@H](C)N(CCCCCCNC(Cc(c1c2)c(C)[n](C(c(cc3)ccc3Cl)=O)c1ccc2OC)=O)C[C@H](C)C[C@H](C[C@@H](C)[C@@H]([C@H]1C)O)[O]=C)O)O)OC1=O FVANAXVFEXRXSV-JMBQMWJUSA-N 0.000 description 1
- 0 C[C@](CC(C)(C)C[C@@](C)[C@@]([C@](C)C(OC[C@@]1(C)O)=O)O)CN(CCCNC([C@@](CC2)([C@@](C)(C[C@@]3O)C2C(CCC([C@]2(C)C=C4)=CC4=O)[C@]32F)O*)=O)[C@](C)[C@]1O Chemical compound C[C@](CC(C)(C)C[C@@](C)[C@@]([C@](C)C(OC[C@@]1(C)O)=O)O)CN(CCCNC([C@@](CC2)([C@@](C)(C[C@@]3O)C2C(CCC([C@]2(C)C=C4)=CC4=O)[C@]32F)O*)=O)[C@](C)[C@]1O 0.000 description 1
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Claims (38)
1. Соединение согласно формуле I
где М представляет собой макролидную субъединицу с субструктурой II
где R1, R2, R3, R4 и R5 независимо выбирают из группы, включающей водород, C1-С4 алкил, алканоил, алкоксикарбонил, арилметоксикарбонил, ароил, арилалкил, алкилсилил и алкилсилилалкоксиалкил;
RN представляет собой ковалентную связь с X1 цепи L;
L представляет собой цепь субструктуры III
где X1 представляет собой -СН2- или -С(O)-;
X2 представляет собой -NH- или -O-;
Q представляет собой -NH- или -СН2-;
символы m и n независимо представляют собой целые числа от 0 до 4;
если Q=NH, то n не может быть равным 0;
D представляет собой нестероидную противовоспалительную субъединицу или
а стероидную субъединицу,
а также фармацевтически допустимые соли вышеуказанных соединений и фармацевтически допустимые составы, содержащие вышеуказанные соединения.
2. Соединение по п.1, отличающееся тем, что D представляет собой стероид субструктуры IV
где Ra, Rb независимо выбирают из группы, включающей водород и галоген,
Rf выбирают из группы, включающей водород, гидроксильную группу, галоген, или Rf образует (С=О) карбонильную группу с атомом углерода, с которым оно связано;
Rc представляет собой ковалентную связь с X2 цепи L;
Rd и Re независимо выбирают из группы, включающей водород, гидрокси, метил или C1-C4 алкокси, или совместно с соответствующими атомами углерода они представляют собой 1,3-диоксалановое ядро, которое может дополнительно содержать одно или два алкильных или алкенильных замещения; и
Rj выбирают из группы, включающей водород или хлор.
3. Соединение по п.2, отличающееся тем, что R1, R2, R3, R4 и R5 независимо выбирают из группы, включающей водород и C1-C4 алкил.
4. Соединение по п.2, отличающееся тем, что R1, R2, R3, R4 и R5 независимо выбирают из группы, включающей водород и метил.
5. Соединение по п.2, отличающееся тем, что X1 представляет собой CH2, a X2 представляет собой NH.
6. Соединение по п.5, отличающееся тем, что m=1, n=1, a Q=CH2 субструктуры III.
20. Соединение по п.1, отличающееся тем, что указанное D представляет собой нестероидную противовоспалительную (NSAID) субъединицу.
21. Соединение по п.20, отличающееся тем, что указанную субъединицу NSAID выбирают из группы, включающей субъединицы ацеклофенака, ацеметацина, ацетминофена, ацетаминосалола, ацетилсалициловой кислоты, ацетилсалициловой-2-амино-4-пиколиновой кислоты, 5-аминоацетилсалициловой кислоты, алклофенака, аминопрофена амфенака, ампирона, ампироксикама, анилеридина, бензадака, беноксалрофена, бермопрофена, а-бизаболола, бромфенака, 5-бромосилициловой кислоты, бромосалигенина, bucloxic** (4-(3-хлоро-4-циклогексилфенил)-4-оксомасляной) кислоты, бутибуфена, карпрофена, целекоксиба, хромогликата, цинметацина, клинданака, клопирака, натрия диклофенака, дифлунисала, дитазола, дроксикама, энфенамовой (N-фениленэтилантраниловой) кислоты, этодолака, этофенамата, фелбинака, фенбуфена, fenclozic** кислоты, фендосала, фенопрофена, фентиазака, фепрадинола, флуфенака, флуфенамовой кислоты, флуниксина, флуноксапрофена, флубипрофена, глутаметацина, гликольсалицилата, ибуфенака, ибупрофена, ибупроксама, индометацина, индопрофена, изофецолака, изоксепака, изоксикама, кетопрофена, кеторолака, лорноксикама, локсопрофена, меклофенамовой кислоты, мефенамовой кислоты, мелоксикама, месаламина, метиациновой кислоты, мофецолака, монтелукаста, микофеноловой кислоты, набуметона, напроксена, нифлумовой кислоты, нимесульфида, олсалацина, оксацепрола, оксапрозина, оксифенбутазона, парацетамола, парсалмида, перисоксала, фенилацетилсалицилата, фенилбутазона, фенилсалицилата, пиразолака, пироксикама, пирпрофена, прапопрофена, протизиновой кислоты, резервератола, салацетамида, салициламида, салициламид-O-ацетиловой кислоты, салицилсерной кислоты, салицина, салициламида, сальсалата, сулиндака, супрофена, суксибутазона, тамоксифена, теноксикама, теофиллина, тиапрофеновой кислоты, тиарамида, тиклопридина, тиноридина, толфенамовой кислоты, толметина, тропесина, ксенбуцина, ксимопрофена, залтопрофена, зомепирака, томоксипрола, зафирлукаста и циклоспорина.
22. Соединение по п.21, отличающееся тем, что указанная субъединица NSAID не является ацетилсилициловой кислотой или микофеноловой кислотой.
23. Соединение по п.21, отличающееся тем, что указанную субъединицу NSAID выбирают из группы, включающей субъединицы индометацина, флуфенамовой кислоты, флуниксина и теофиллина.
24. Соединение по п.23, отличающееся тем, что указанная субъединица NSAID представляет собой субъединицу индометацина.
32. Фармацевтический состав, содержащий соединение по пп.1, 2 или 20 или их фармацевтически допустимые соли или сольват, а также фармацевтически допустимый разбавитель или носитель.
33. Способ олечения воспалительных заболеваний, нарушений и состояний, характеризующихся или связанных с нежелательной воспалительной иммунной реакцией, а также всех заболеваний и состояний, индуцированных или связанных с чрезмерной секрецией TNF (tumour necrosis factor, фактор некроза опухолей)-α и IL (interleukin, интрелейкин)-1, который включает введение субъекту терапевтически эффективной дозы соединения по пп.1, 2 или 20.
34. Способ лечения воспалительных состояний и иммунных или анафилактических нарушений, связанных с инфильтрацией лекоцитов в ткань воспаления, у субъекта, нуждающегося в лечении, который включает введение указанному субъекту терапевтически эффективной дозы соединения по пп.1, 2 или 20.
35. Способ по п.33, отличающийся тем, что воспалительные состояния и иммунные нарушения выбирают из группы, включающей астму, синдром расстройства дыхания у взрослых, хронические обструктивные легочные заболевания, воспаление кишечника, болезнь Крона, бронхит и кистозный фиброз.
36. Способ по п.33, отличающийся тем, что указанные воспалительные состояния и иммунные нарушения выбирают из группы, включающей воспалительные состояния или иммунные нарушения легких, суставов, глаз, кишечника, кожи и сердца.
37. Способ по п.33, отличающийся тем, что указанные воспалительные состояния и иммунные нарушения выбирают из группы, включающей астму, синдром расстройства дыхания у взрослых, бронхит, кистозный фиброз, ревматоидный артрит, ревматоидный спондилит, остеоартрит, подагрический артрит, увеит, конъюнктивит, воспаление кишечника, болезнь Крона, язвенный колит, дистальный проктит, псориаз, экзему, дерматит, коронарный инфаркт, хроническое воспаление, эндотоксемию и пролиферативные нарушения гладких мышц.
38. Способ лечения воспалительных заболеваний, нарушений и состояний, характеризующийся или связанный с чрезмерным нерегулируемым образованием цитокинов или медиаторов воспаления, и включающий введение субъекту терапевтически эффективной дозы соединения по пп.1, 2 или 20.
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HRP20030324 | 2003-04-24 | ||
HR20030324A HRP20030324A2 (en) | 2003-04-24 | 2003-04-24 | Compounds of antiinflammatory effect |
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US (1) | US7579334B2 (ru) |
EP (2) | EP2070940B1 (ru) |
JP (1) | JP4613366B2 (ru) |
KR (1) | KR101107336B1 (ru) |
CN (1) | CN100393741C (ru) |
AR (1) | AR044083A1 (ru) |
AT (1) | ATE518876T1 (ru) |
AU (1) | AU2004232546B2 (ru) |
BR (1) | BRPI0410490A (ru) |
CA (1) | CA2523081C (ru) |
CL (1) | CL2004000872A1 (ru) |
CY (2) | CY1109491T1 (ru) |
DE (1) | DE602004022047D1 (ru) |
DK (2) | DK1633771T3 (ru) |
ES (2) | ES2370371T3 (ru) |
HR (3) | HRP20030324A2 (ru) |
IS (2) | IS2736B (ru) |
ME (1) | MEP34708A (ru) |
MX (1) | MXPA05011359A (ru) |
NO (2) | NO333909B1 (ru) |
PL (2) | PL1633771T3 (ru) |
PT (2) | PT1633771E (ru) |
RS (1) | RS52621B (ru) |
RU (1) | RU2355699C2 (ru) |
SI (2) | SI1633771T1 (ru) |
WO (1) | WO2004094449A1 (ru) |
ZA (1) | ZA200508388B (ru) |
Families Citing this family (16)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AR043050A1 (es) | 2002-09-26 | 2005-07-13 | Rib X Pharmaceuticals Inc | Compuestos heterociclicos bifuncionales y metodos para preparar y usar los mismos |
HRP20030324A2 (en) | 2003-04-24 | 2005-02-28 | Pliva-Istra�iva�ki institut d.o.o. | Compounds of antiinflammatory effect |
US8202843B2 (en) | 2004-02-27 | 2012-06-19 | Rib-X Pharmaceuticals, Inc. | Macrocyclic compounds and methods of making and using the same |
EP1778292A2 (en) * | 2004-08-12 | 2007-05-02 | GlaxoSmithKline istrazivacki centar Zagreb d.o.o. | Use of cell-specific conjugates for treatment of inflammatory diseases of the gastrointestinal tract |
US20060183696A1 (en) * | 2004-08-12 | 2006-08-17 | Pliva-Istrazivacki Institut D.O.O. | Use of immune cell specific conjugates for treatment of inflammatory diseases of gastrointestinal tract |
AU2005298312A1 (en) * | 2004-10-27 | 2006-05-04 | Glaxosmithkline Istrazivacki Centar Zagreb D.O.O. | Conjugates with anti-inflammatory activity |
AU2006327181A1 (en) * | 2005-12-22 | 2007-06-28 | Hydra Biosciences, Inc. | TRPA1 inhibitors for treating pain |
WO2007093840A2 (en) * | 2006-02-15 | 2007-08-23 | Glaxosmithkline Istrazivacki Centar Zagreb D.O.O. | Use of cell-specific conjugates for treatment of inflammatory diseases of the gastrointestinal tract |
CA2717456A1 (en) * | 2008-03-05 | 2009-09-11 | Panacea Biotec Limited | Modified release pharmaceutical compositions comprising mycophenolate and processes thereof |
CN102838660B (zh) * | 2011-06-23 | 2016-11-02 | 上海市第一人民医院 | 一种抑制炎症免疫反应的小肽及其应用 |
WO2014115167A2 (en) * | 2013-01-23 | 2014-07-31 | Sphaera Pharma Pvt. Ltd. | Novel compounds of 11beta-hydroxy-steroids for use in mitochondria biogenesis and diseases associated with mitochondrial dysfunction or depletion |
US20140256666A1 (en) * | 2013-03-08 | 2014-09-11 | Allergan, Inc. | Antibiotic conjugates with nonsteroidal anti-inflammatory drugs |
JP2016510753A (ja) * | 2013-03-08 | 2016-04-11 | アラーガン、インコーポレイテッドAllergan,Incorporated | ステロイド薬と結合した抗生物質共役体 |
WO2014138437A1 (en) | 2013-03-08 | 2014-09-12 | Allergan, Inc. | Steroid conjugates |
WO2014138350A1 (en) | 2013-03-08 | 2014-09-12 | Allergan, Inc. | Antibiotic conjugates directly linked with steroid drugs |
CN106714770B (zh) | 2014-07-23 | 2024-04-19 | 斯法尔制药私人有限公司 | 羟基类固醇化合物、其中间体、制备方法、组合物及其用途 |
Family Cites Families (22)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE3779221D1 (de) | 1986-08-19 | 1992-06-25 | Genentech Inc | Einrichtung und dispersion zum intrapulmonalen eingeben von polypeptidwuchsstoffen und -zytokinen. |
DE3860503D1 (de) * | 1987-09-03 | 1990-10-04 | Pliva Pharm & Chem Works | 10-dihydro-10-deoxo-11-azaerythronolid-a-verbindungen,verfahren und zwischenprodukte zu ihrer herstellung und ihre verwendung in arzneimitteln und in deren herstellung. |
SE9100341D0 (sv) | 1991-02-04 | 1991-02-04 | Astra Ab | Novel steroids |
SE9100342D0 (sv) | 1991-02-04 | 1991-02-04 | Astra Ab | Novel steroid esters |
GB9225923D0 (en) | 1992-12-11 | 1993-02-03 | Rhone Poulenc Rorer Ltd | New compositions of matter |
FI953130A0 (fi) | 1992-12-24 | 1995-06-22 | Rhone Poulenc Rorer Ltd | Uudet steroidit |
CN1159757A (zh) | 1994-08-12 | 1997-09-17 | 大正制药株式会社 | 抑制白细胞介素5产生的抑制剂 |
EP0775489A4 (en) | 1994-08-12 | 1998-05-06 | Taisho Pharmaceutical Co Ltd | INTERLEUKIN-5 PRODUCTION INHIBITOR |
DE19616573C2 (de) | 1996-04-25 | 1999-03-04 | Pari Gmbh | Verwendung unterkritischer Treibmittelmischungen und Aerosole für die Mikronisierung von Arzneimitteln mit Hilfe dichter Gase |
JP3530004B2 (ja) | 1998-02-06 | 2004-05-24 | 株式会社日立ユニシアオートモティブ | 吸入式投薬器 |
EP1126838A4 (en) | 1998-10-30 | 2005-02-16 | Nitromed Inc | NITROSIS AND NITROSYAL NON-STEROID ANTI-INFLAMMATORY COMPOUNDS, COMPOSITIONS AND METHODS OF USE |
IT1306205B1 (it) | 1999-01-15 | 2001-05-30 | Zambon Spa | Macrolidi ad attivita' antiinfiammatoria. |
HRP20000310A2 (en) | 2000-05-17 | 2002-02-28 | Pliva Farmaceutska Ind Dioniko | New dibenzoazulene compounds as tumor necrosis factor inhibitors |
FI110835B (fi) | 2000-07-11 | 2003-03-31 | Radiolinja Ab | Menetelmä palvelunumeropuhelun tarjoamiseksi matkaviestintilaajalle ennalta määrätyllä taksalla |
HRP20010018A2 (en) | 2001-01-09 | 2002-12-31 | Pliva D D | Novel anti-inflammatory compounds |
US20040186063A1 (en) | 2002-02-15 | 2004-09-23 | Hans-Jurgen Gutke | Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof |
WO2003070174A2 (en) | 2002-02-15 | 2003-08-28 | Sympore Gmbh | Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof |
HRP20040849A2 (en) | 2002-02-15 | 2005-08-31 | Synovo Gmbh | Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof |
ATE429441T1 (de) | 2002-07-08 | 2009-05-15 | Glaxosmithkline Zagreb | Hybridmoleküle von makroliden mit steroidalen/nicht-steroidalen antientzündlich aktiven molekülen |
JP4790263B2 (ja) | 2002-07-08 | 2011-10-12 | グラクソ グループ リミテッド | 炎症性の疾患および病態を治療する新規な化合物、組成物および方法 |
AU2003255849A1 (en) | 2002-07-08 | 2004-01-23 | Glaxosmithkline Istrazivacki Centar Zagreb D.O.O. | Novel nonsteroidal anti-inflammatory substances, compositions and methods for their use |
HRP20030324A2 (en) | 2003-04-24 | 2005-02-28 | Pliva-Istra�iva�ki institut d.o.o. | Compounds of antiinflammatory effect |
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2003
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