HUP9801805A2 - Diglikozilezett 1,2-diolok mint szialil-Lewis X és szialil-Lewis A mimetikumok - Google Patents
Diglikozilezett 1,2-diolok mint szialil-Lewis X és szialil-Lewis A mimetikumokInfo
- Publication number
- HUP9801805A2 HUP9801805A2 HU9801805A HUP9801805A HUP9801805A2 HU P9801805 A2 HUP9801805 A2 HU P9801805A2 HU 9801805 A HU9801805 A HU 9801805A HU P9801805 A HUP9801805 A HU P9801805A HU P9801805 A2 HUP9801805 A2 HU P9801805A2
- Authority
- HU
- Hungary
- Prior art keywords
- alkyl
- aryl
- heteroaryl
- alkenyl
- heterocyclicalkyl
- Prior art date
Links
- NIGUVXFURDGQKZ-UQTBNESHSA-N alpha-Neup5Ac-(2->3)-beta-D-Galp-(1->4)-[alpha-L-Fucp-(1->3)]-beta-D-GlcpNAc Chemical compound O[C@H]1[C@H](O)[C@H](O)[C@H](C)O[C@H]1O[C@H]1[C@H](O[C@H]2[C@@H]([C@@H](O[C@]3(O[C@H]([C@H](NC(C)=O)[C@@H](O)C3)[C@H](O)[C@H](O)CO)C(O)=O)[C@@H](O)[C@@H](CO)O2)O)[C@@H](CO)O[C@@H](O)[C@@H]1NC(C)=O NIGUVXFURDGQKZ-UQTBNESHSA-N 0.000 title abstract 2
- 150000000180 1,2-diols Chemical class 0.000 title 1
- XBSNXOHQOTUENA-KRAHZTDDSA-N alpha-Neu5Ac-(2->3)-beta-D-Gal-(1->3)-[alpha-L-Fuc-(1->4)]-D-GlcNAc Chemical compound O[C@H]1[C@H](O)[C@H](O)[C@H](C)O[C@H]1O[C@H]1[C@H](O[C@H]2[C@@H]([C@@H](O[C@]3(O[C@H]([C@H](NC(C)=O)[C@@H](O)C3)[C@H](O)[C@H](O)CO)C(O)=O)[C@@H](O)[C@@H](CO)O2)O)[C@@H](NC(C)=O)C(O)O[C@@H]1CO XBSNXOHQOTUENA-KRAHZTDDSA-N 0.000 title 1
- 125000003118 aryl group Chemical group 0.000 abstract 7
- 125000000217 alkyl group Chemical group 0.000 abstract 6
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 6
- 239000000843 powder Substances 0.000 abstract 6
- 125000001072 heteroaryl group Chemical group 0.000 abstract 5
- 125000005343 heterocyclic alkyl group Chemical group 0.000 abstract 5
- -1 nitro, amino Chemical group 0.000 abstract 5
- 125000003342 alkenyl group Chemical group 0.000 abstract 4
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 4
- 125000004447 heteroarylalkenyl group Chemical group 0.000 abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000005018 aryl alkenyl group Chemical group 0.000 abstract 2
- 125000004104 aryloxy group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000005553 heteroaryloxy group Chemical group 0.000 abstract 2
- 229910052751 metal Inorganic materials 0.000 abstract 2
- 239000002184 metal Substances 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- XSQUKJJJFZCRTK-UHFFFAOYSA-N urea group Chemical group NC(=O)N XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 abstract 2
- KXDHJXZQYSOELW-UHFFFAOYSA-N Carbamic acid Chemical compound NC(O)=O KXDHJXZQYSOELW-UHFFFAOYSA-N 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 229910052791 calcium Inorganic materials 0.000 abstract 1
- 239000011575 calcium Substances 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000000467 secondary amino group Chemical group [H]N([*:1])[*:2] 0.000 abstract 1
- 125000000565 sulfonamide group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
- C07H15/20—Carbocyclic rings
- C07H15/207—Cyclohexane rings not substituted by nitrogen atoms, e.g. kasugamycins
-
- 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
- A61P11/16—Central respiratory analeptics
-
- 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
- A61P17/06—Antipsoriatics
-
- 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
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
- C07H17/02—Heterocyclic radicals containing only nitrogen as ring hetero atoms
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Genetics & Genomics (AREA)
- Biotechnology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pulmonology (AREA)
- Oncology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Diabetes (AREA)
- Dermatology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Hydrogenated Pyridines (AREA)
- Cosmetics (AREA)
Abstract
A találmány (I) általánős képletű szialil-Lewis X és szialil-Lewis Amimetikűmőkra és élettanileg elfőgadható sóikra, a vegyületekelőállítási eljárásaira, gyógyászati eljárásőkban történőalkalmazására, valamint a vegyületeket tartalmazógyógyszerkészítményekre vőnatkőzik. Az (I) általánős képletben X egynemglikőzidős alifás 1,2-diől maradéka, R1 egy karbőxilcsőpőrttal ésegy másik szűbsztitűenssel szűbsztitűált, S-kőnfigűrációjúmetilcsőpőrt, és R2 hidrőgénatőm, alkil- vagy arilcsőpőrt, ahől azalkil- és az arilcsőpőrt adőtt esetben egy vagy több, a következőkközül kiválasztőtt atőmmal és/vagy csőpőrttal szűbsztitűált,hidrőxilcsőpőrt, halőgénatőm, -C(O)ORs1, -OC(O)Rs4, -C(O)Rs2 általánősképletű csőpőrt, nitrő-, aminő-, cianőcsőpőrt, -SO3My, -OSO3My, -NR5SO3My általánős képletű csőpőrt, alkil-, alkenil-, alkőxi-,ciklőalkil-, ciklőalkenil-, heterőciklőalkil-, heterőciklőalkenil-,aril-, arilőxi-, heterőaril-, heterőaril-őxi-, aril-alkil-, (aril-alkil)-őxi-, heterőaril-alkil-, aril-alkenil-, heterőaril-alkenil-,primer vagy szekűnder aminő-, szűlfőnil-, szűlfőnamid-, karbamid-,karbamát-, szűlfőn-hidrazid-, karbhidrazid-, karbőhidrőxámsav- ésaminő-karbőnil-amidcsőpőrt, ahől Rs1 hidrőgénatőm, My, alkil-,alkenil-, ciklőalkil-, heterőciklőalkil-, aril-, heterőaril-, aril-alkil- vagy heterőaril-alkil-csőpőrt, Rs4 hidrőgénatőm, alkil-,alkenil-, ciklőalkil-, heterőaciklőalkil-, aril-, heterőaril-, aril-alkil- vagy heterőaril-alkil-csőpőrt, valamint Rs2 és R20hidrőgénatőm, alkil-, alkenil-, ciklőalkil-, ciklőalkenil-,heterőciklőalkil-, heterőciklőalkenil-, aril-, heterőaril-, aril-alkil-, heterőaril-alkil-, aril-alkenil- vagy heterőaril-alkenil-csőpőrt, ahől az alkil-, alkenil-, alkőxi-, ciklőalkil-,ciklőalkenil-, heterőciklőalkil-, heterőciklőalkenil-, aril-, aril-őxi-, heterőaril-, heterőaril-őxi-, aril-alkil-, (aril-alkil)-őxi-,heterőaril-alkil-, aril-alkenil- és heterőaril-alkenil-csőpőrt adőttesetben a fentiekben említett szűbsztitűensek egyikével szűbsztitűáltlehet, Y 1, és M egyvegyértékű fém, vagy y 1/2, és M kétvegyértékűfém. ŕ
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CH191495 | 1995-06-29 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP9801805A2 true HUP9801805A2 (hu) | 1998-12-28 |
| HUP9801805A3 HUP9801805A3 (en) | 2002-01-28 |
Family
ID=4221546
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU9801805A HUP9801805A3 (en) | 1995-06-29 | 1996-06-26 | Diglycosylated 1,2-diols as mimetics of sialyl-lewis x and sialyl-lewis a |
Country Status (19)
| Country | Link |
|---|---|
| EP (1) | EP0836610A1 (hu) |
| JP (1) | JPH11508548A (hu) |
| KR (1) | KR19990028543A (hu) |
| CN (1) | CN1196731A (hu) |
| AU (1) | AU707474B2 (hu) |
| BR (1) | BR9609285A (hu) |
| CA (1) | CA2224346A1 (hu) |
| CZ (1) | CZ419797A3 (hu) |
| EA (1) | EA001356B1 (hu) |
| HU (1) | HUP9801805A3 (hu) |
| IL (1) | IL118740A0 (hu) |
| MX (1) | MX9800218A (hu) |
| NO (1) | NO976065L (hu) |
| NZ (1) | NZ311686A (hu) |
| PL (1) | PL324258A1 (hu) |
| SI (1) | SI9620099A (hu) |
| SK (1) | SK177897A3 (hu) |
| TR (1) | TR199701728T1 (hu) |
| WO (1) | WO1997001569A1 (hu) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002036587A2 (en) | 2000-11-01 | 2002-05-10 | Cor Therapeutics, Inc. | Process for the production of 4-quinazolinylpiperazin-1-carboxylic acid phenylamides |
| EP1577289A1 (en) | 2004-03-18 | 2005-09-21 | Revotar Biopharmaceuticals AG | Non-glycosylated/-glycosidic/-peptidic small molecule selectin inhibitors for the treament of inflammatory disorders |
| LT2264043T (lt) | 2005-09-02 | 2017-12-11 | Glycomimetics, Inc. | Heterobifunkciniai pan-selektino inhibitoriai |
| EP1764095A1 (en) | 2005-09-20 | 2007-03-21 | Revotar Biopharmaceuticals AG | Novel nitrocatechol derivatives having selectin ligand activity |
| EP1764096A1 (en) | 2005-09-20 | 2007-03-21 | Revotar Biopharmaceuticals AG | Novel phloroglucinol derivatives having selectin ligand activity |
| EP1764093A1 (en) | 2005-09-20 | 2007-03-21 | Revotar Biopharmaceuticals AG | Novel aromatic compounds and their use in medical applications |
| JP5298020B2 (ja) * | 2006-10-12 | 2013-09-25 | グリコミメティクス， インコーポレイテッド | ヘキソースおよびｎ−アセチルヘキソサミンの糖模倣体置換 |
| NZ598863A (en) * | 2007-02-09 | 2013-11-29 | Glycomimetics Inc | Methods of use of glycomimetics with replacements for hexoses and n-acetyl hexosamines |
| WO2009126556A1 (en) | 2008-04-08 | 2009-10-15 | Glycomimetics, Inc. | Pan-selectin inhibitor with enhanced pharmacokinetic activity |
| US8921328B2 (en) | 2010-09-14 | 2014-12-30 | Glycomimetics, Inc. | E-selectin antagonists |
| AU2012358150B2 (en) | 2011-12-22 | 2017-07-20 | Glycomimetics, Inc. | E-selectin antagonist compounds, compositions, and methods of use |
| CN104837492B (zh) | 2012-12-07 | 2018-04-27 | 糖模拟物有限公司 | 使用e-选择素拮抗剂动员造血细胞的化合物、组合物和方法 |
| EP3227310B1 (en) | 2014-12-03 | 2019-07-31 | GlycoMimetics, Inc. | Heterobifunctional inhibitors of e-selectins and cxcr4 chemokine receptors |
| US11045485B2 (en) | 2016-01-22 | 2021-06-29 | Glycomimetics, Inc. | Glycomimetic inhibitors of PA-IL and PA-IIL lectins |
| US11291678B2 (en) | 2016-03-02 | 2022-04-05 | Glycomimetics, Inc | Methods for the treatment and/or prevention of cardiovascular disease by inhibition of E-selectin |
| JP2019524791A (ja) | 2016-08-08 | 2019-09-05 | グリコミメティクス， インコーポレイテッド | Ｅ−セレクチンの阻害剤もしくはｃｘｃｒ４の阻害剤との、またはｅ−セレクチンおよびｃｘｃｒ４両方のヘテロ二機能性阻害剤とのｔ細胞チェックポイント阻害剤の組み合わせ |
| US11072625B2 (en) | 2016-10-07 | 2021-07-27 | Glycomimetics, Inc. | Highly potent multimeric e-selectin antagonists |
| EP3596096A1 (en) | 2017-03-15 | 2020-01-22 | GlycoMimetics, Inc. | Galactopyranosyl-cyclohexyl derivatives as e-selectin antagonists |
| EP3717013A1 (en) | 2017-11-30 | 2020-10-07 | GlycoMimetics, Inc. | Methods of mobilizing marrow infiltrating lymphocytes and uses thereof |
| EP3732186A1 (en) | 2017-12-29 | 2020-11-04 | GlycoMimetics, Inc. | Heterobifunctional inhibitors of e-selectin and galectin-3 |
| EP3761994A1 (en) | 2018-03-05 | 2021-01-13 | GlycoMimetics, Inc. | Methods for treating acute myeloid leukemia and related conditions |
| WO2020139962A1 (en) | 2018-12-27 | 2020-07-02 | Glycomimetics, Inc. | Heterobifunctional inhibitors of e-selectin and galectin-3 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5326752A (en) * | 1991-11-27 | 1994-07-05 | Glycomed Incorporated | Substituted lactose and lactosamine derivatives as cell adhesion inhibitors |
| WO1993023031A1 (en) * | 1992-05-08 | 1993-11-25 | The Biomembrane Institute | Multivalent mimetics and peptide mimetics for blocking carbohydrate-dependent cellular interaction and for eliciting anticarbohydrate t-cell response |
| CA2100412A1 (en) * | 1992-07-15 | 1994-01-16 | Yutaka Yamada | Glycolipid derivatives |
-
1996
- 1996-06-26 SI SI9620099A patent/SI9620099A/sl unknown
- 1996-06-26 EP EP96922034A patent/EP0836610A1/en not_active Ceased
- 1996-06-26 WO PCT/EP1996/002785 patent/WO1997001569A1/en not_active Application Discontinuation
- 1996-06-26 KR KR1019970709861A patent/KR19990028543A/ko not_active Application Discontinuation
- 1996-06-26 CN CN96196452A patent/CN1196731A/zh active Pending
- 1996-06-26 IL IL11874096A patent/IL118740A0/xx unknown
- 1996-06-26 AU AU63053/96A patent/AU707474B2/en not_active Ceased
- 1996-06-26 JP JP9504171A patent/JPH11508548A/ja active Pending
- 1996-06-26 CA CA002224346A patent/CA2224346A1/en not_active Abandoned
- 1996-06-26 CZ CZ974197A patent/CZ419797A3/cs unknown
- 1996-06-26 NZ NZ311686A patent/NZ311686A/xx unknown
- 1996-06-26 PL PL96324258A patent/PL324258A1/xx unknown
- 1996-06-26 EA EA199800103A patent/EA001356B1/ru not_active IP Right Cessation
- 1996-06-26 HU HU9801805A patent/HUP9801805A3/hu unknown
- 1996-06-26 BR BR9609285A patent/BR9609285A/pt not_active Application Discontinuation
- 1996-06-26 TR TR97/01728T patent/TR199701728T1/xx unknown
- 1996-06-26 SK SK1778-97A patent/SK177897A3/sk unknown
-
1997
- 1997-12-23 NO NO976065A patent/NO976065L/no not_active Application Discontinuation
-
1998
- 1998-01-07 MX MX9800218A patent/MX9800218A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA2224346A1 (en) | 1997-01-16 |
| AU707474B2 (en) | 1999-07-08 |
| SI9620099A (sl) | 1998-08-31 |
| MX9800218A (es) | 1998-07-31 |
| WO1997001569A1 (en) | 1997-01-16 |
| NZ311686A (en) | 2000-01-28 |
| EP0836610A1 (en) | 1998-04-22 |
| TR199701728T1 (xx) | 1998-03-21 |
| CN1196731A (zh) | 1998-10-21 |
| KR19990028543A (ko) | 1999-04-15 |
| IL118740A0 (en) | 1996-10-16 |
| EA199800103A1 (ru) | 1998-08-27 |
| PL324258A1 (en) | 1998-05-11 |
| HUP9801805A3 (en) | 2002-01-28 |
| CZ419797A3 (cs) | 1998-06-17 |
| BR9609285A (pt) | 1999-05-11 |
| JPH11508548A (ja) | 1999-07-27 |
| AU6305396A (en) | 1997-01-30 |
| EA001356B1 (ru) | 2001-02-26 |
| NO976065L (no) | 1998-02-17 |
| NO976065D0 (no) | 1997-12-23 |
| SK177897A3 (en) | 1998-08-05 |
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