HUP0002682A1 - VLA-4 által közvetített leukocita adhéziót gátló dipeptidszármazékok - Google Patents
VLA-4 által közvetített leukocita adhéziót gátló dipeptidszármazékokInfo
- Publication number
- HUP0002682A1 HUP0002682A1 HU0002682A HUP0002682A HUP0002682A1 HU P0002682 A1 HUP0002682 A1 HU P0002682A1 HU 0002682 A HU0002682 A HU 0002682A HU P0002682 A HUP0002682 A HU P0002682A HU P0002682 A1 HUP0002682 A1 HU P0002682A1
- Authority
- HU
- Hungary
- Prior art keywords
- group
- substituted
- aryl
- alkyl
- cycloalkyl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 108010016626 Dipeptides Proteins 0.000 title 1
- 230000023404 leukocyte cell-cell adhesion Effects 0.000 title 1
- 230000001404 mediated effect Effects 0.000 title 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 9
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 8
- 125000001072 heteroaryl group Chemical group 0.000 abstract 7
- 125000003118 aryl group Chemical group 0.000 abstract 6
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 6
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- -1 hydroxyl- Chemical group 0.000 abstract 3
- 125000005325 aryloxy aryl group Chemical group 0.000 abstract 2
- 125000004104 aryloxy group Chemical group 0.000 abstract 2
- 125000004429 atom Chemical group 0.000 abstract 2
- 125000003107 substituted aryl group Chemical group 0.000 abstract 2
- 125000005346 substituted cycloalkyl group Chemical group 0.000 abstract 2
- 125000004442 acylamino group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000004181 carboxyalkyl group Chemical group 0.000 abstract 1
- 125000005026 carboxyaryl group Chemical group 0.000 abstract 1
- 125000005352 carboxycycloalkyl group Chemical group 0.000 abstract 1
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000005415 substituted alkoxy group Chemical group 0.000 abstract 1
- 125000005338 substituted cycloalkoxy group Chemical group 0.000 abstract 1
- 229910052717 sulfur Chemical group 0.000 abstract 1
- 125000004434 sulfur atom Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06139—Dipeptides with the first amino acid being heterocyclic
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06139—Dipeptides with the first amino acid being heterocyclic
- C07K5/06165—Dipeptides with the first amino acid being heterocyclic and Pro-amino acid; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Rheumatology (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Peptides Or Proteins (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
A találmány tárgya (I) és (IA) általános képletű vegyületekgyógyászati szempontból elfogadható sóik, és ezeket tartalmazógyógyászati készítmények. A képletekben R1 jelentése adott esetbenszubsztituált alkil-, aril-, cikloalkil-, heterociklusos- ésheteroarilcsoport; R2 jelentése hidrogénatom, adott esetbenszubsztituált alkil-, cikloalkil-, cikloalkenil-, heterociklusosaril-és heteroarilcsoport; vagy R1 és R2 jelentése a kapcsolódó atomokkalegyütt adott esetben szubsztituált heterociklusos csoport; R3jelentése hidrogénatom, adott esetben szubsztituált alkil-,cikloalkil-, aril-, heteroarilcsoport és heterociklusos csoport; vagyR2 és R3 jelentése a kapcsolódó atomokkal együtt adott esetbenszubsztituált telített heterociklusos csoport; R4 jelentése adottesetben szubsztituált alkil-, aril- vagy heteroarilcsoport, vagy ha R3és R2 jelentése együtt nem heterociklusos csoport, akkor R3 és R4jelentése a kapcsolódó szénatommal együtt adott esetben szubsztituáltcikioalkil- vagy heterociklusos csoport; R5 jelentéseizopropilcsoport, -CH2X vagy =CH-X általános képletű csoport, ahol Xjelentése hidrogénatom, hidroxil-, acilamino-, alkil-, alkoxi-,ariloxi-, aril-, ariloxiaril-, karboxil-, karboxialkil-, karboxi-(szubsztituált alkil)-, karboxicikloalkil-, karboxi-(szubsztituáltcikloalkil)-, karboxiaril-, karboxi-(szubsztituált aril)-,karboxiheteroaril-, karboxi-(szubsztituált heteroaril)-,karboxiheterociklusos, karboxi-(szubsztituált heterociklusos)-,cikloalkil-, szubsztituált alkil-, szubsztituált alkoxi-,szubsztituált aril-, szubsztituált ariloxi-, szubsztituáltariloxiaril-, szubsztituált cikloalkil-, heteroaril-, szubsztituáltheteroaril-, heterociklusos vagy szubsztituált heterociklusos csoport,azzal a megszorítással, hogy ha R5 jelentése =CH-X általános képletűcsoport, akkor (H) hiányzik a képletből és X jelentésehidroxilcsoporttól eltérő; R6 jelentése 2,4-dioxo-tetrahidrofurán-3-yl(3,4-enol)-, amino-, alkoxi-, szubsztituált alkoxi-, cikloalkoxi-,szubsztituált cikloalkoxi-, -O-(N-szukcinimidil)-, -NH-adamantil-, -O-koleszt-5-en-3-<-il-csoport, -NHOY általános képletű csoport, ahol Yjelentése hidrogénatom, alkil-, szubsztituált alkil-, aril- vagyszubsztituált arilcsoport, -NH(CH2)PCOOY, ahol Y jelentése a fenti, pértéke 1-8, -OCH2NR9R10 általános képletű csoport, ahol R9 jelentése -C(O)-aril- vagy -C(O)-(szubsztituált aril)csoport és R10 jelentésehidrogénatom vagy -CH2COOR11 általános képletű csoport, ahol R11jelentése alkilcsoport, és -NHSO2Z< általános képletű csoport, ahol Z<jelentése egyenként adott esetben szubsztituált alkil-, cikloalkil-,aril-, heteroaril- vagy heterociklusos csoport; Q jelentése -C(X)NR7-általános képletű csoport, ahol R7 jelentése hidrogénatom vagyalkilcsoport és X jelentése oxigénatom vagy kénatom.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US90441597A | 1997-07-31 | 1997-07-31 | |
| PCT/US1998/015314 WO1999006435A1 (en) | 1997-07-31 | 1998-07-30 | Dipeptide compounds which inhibit leukocyte adhesion mediated by vla-4 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP0002682A1 true HUP0002682A1 (hu) | 2001-07-30 |
| HUP0002682A3 HUP0002682A3 (en) | 2001-12-28 |
Family
ID=25419114
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0002682A HUP0002682A3 (en) | 1997-07-31 | 1998-07-30 | Dipeptide compounds which inhibit leukocyte adhesion mediated by vla-4 |
Country Status (14)
| Country | Link |
|---|---|
| EP (1) | EP0994895A1 (hu) |
| JP (1) | JP2001512137A (hu) |
| KR (1) | KR20010022412A (hu) |
| CN (1) | CN1265673A (hu) |
| AR (1) | AR016387A1 (hu) |
| AU (1) | AU8661298A (hu) |
| BR (1) | BR9811599A (hu) |
| CA (1) | CA2291475A1 (hu) |
| HU (1) | HUP0002682A3 (hu) |
| IL (1) | IL133642A0 (hu) |
| NO (1) | NO20000412L (hu) |
| PL (1) | PL338554A1 (hu) |
| WO (1) | WO1999006435A1 (hu) |
| ZA (1) | ZA986834B (hu) |
Families Citing this family (45)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6903075B1 (en) | 1997-05-29 | 2005-06-07 | Merck & Co., Inc. | Heterocyclic amide compounds as cell adhesion inhibitors |
| CA2291708A1 (en) * | 1997-05-29 | 1998-12-03 | Merck & Co., Inc. | Sulfonamides as cell adhesion inhibitors |
| US6221888B1 (en) | 1997-05-29 | 2001-04-24 | Merck & Co., Inc. | Sulfonamides as cell adhesion inhibitors |
| DE69820614T2 (de) * | 1997-05-30 | 2004-09-30 | Celltech Therapeutics Ltd., Slough | Entzündungshemmende tyrosin-derivate |
| PT991619E (pt) | 1997-06-23 | 2004-02-27 | Upjohn Co | Inibidores da adesao celular mediada pela alfa4beta1 |
| US6455550B1 (en) | 1997-08-22 | 2002-09-24 | Hoffmann-La Roche Inc. | N-alkanoylphenylalanine derivatives |
| MY153569A (en) | 1998-01-20 | 2015-02-27 | Mitsubishi Tanabe Pharma Corp | Inhibitors of ?4 mediated cell adhesion |
| US6329372B1 (en) | 1998-01-27 | 2001-12-11 | Celltech Therapeutics Limited | Phenylalanine derivatives |
| DE69919334T2 (de) | 1998-02-26 | 2005-08-04 | Celltech Therapeutics Ltd., Slough | Phenylalaninderivate als inhibitoren von alpha4 integrinen |
| US6521626B1 (en) | 1998-03-24 | 2003-02-18 | Celltech R&D Limited | Thiocarboxamide derivatives |
| GB9811159D0 (en) | 1998-05-22 | 1998-07-22 | Celltech Therapeutics Ltd | Chemical compounds |
| GB9811969D0 (en) * | 1998-06-03 | 1998-07-29 | Celltech Therapeutics Ltd | Chemical compounds |
| GB9812088D0 (en) * | 1998-06-05 | 1998-08-05 | Celltech Therapeutics Ltd | Chemical compounds |
| US6685617B1 (en) | 1998-06-23 | 2004-02-03 | Pharmacia & Upjohn Company | Inhibitors of α4β1 mediated cell adhesion |
| GB9814414D0 (en) | 1998-07-03 | 1998-09-02 | Celltech Therapeutics Ltd | Chemical compounds |
| US6333340B1 (en) * | 1998-08-14 | 2001-12-25 | Gpi Nil Holdings, Inc. | Small molecule sulfonamides for vision and memory disorders |
| US6339101B1 (en) * | 1998-08-14 | 2002-01-15 | Gpi Nil Holdings, Inc. | N-linked sulfonamides of N-heterocyclic carboxylic acids or isosteres for vision and memory disorders |
| GB9821061D0 (en) | 1998-09-28 | 1998-11-18 | Celltech Therapeutics Ltd | Chemical compounds |
| GB9821222D0 (en) | 1998-09-30 | 1998-11-25 | Celltech Therapeutics Ltd | Chemical compounds |
| GB9825652D0 (en) | 1998-11-23 | 1999-01-13 | Celltech Therapeutics Ltd | Chemical compounds |
| GB9826174D0 (en) | 1998-11-30 | 1999-01-20 | Celltech Therapeutics Ltd | Chemical compounds |
| PT1154993E (pt) * | 1999-02-18 | 2005-01-31 | Hoffmann La Roche | Derivados de tioamida |
| US6518283B1 (en) | 1999-05-28 | 2003-02-11 | Celltech R&D Limited | Squaric acid derivatives |
| CN1377268A (zh) * | 1999-08-13 | 2002-10-30 | 比奥根公司 | 细胞粘合抑制剂 |
| IL148544A0 (en) * | 1999-09-24 | 2002-09-12 | Genentech Inc | Tyrosine derivatives |
| US6534513B1 (en) | 1999-09-29 | 2003-03-18 | Celltech R&D Limited | Phenylalkanoic acid derivatives |
| US6455539B2 (en) | 1999-12-23 | 2002-09-24 | Celltech R&D Limited | Squaric acid derivates |
| JP2003519697A (ja) | 1999-12-28 | 2003-06-24 | ファイザー・プロダクツ・インク | 炎症性疾患、自己免疫疾患および呼吸器疾患の処置に有用な非ペプチド系のｖｌａ−４依存性細胞結合阻害薬 |
| JP2003531141A (ja) | 2000-04-17 | 2003-10-21 | セルテック アール アンド ディ リミテッド | エナミン誘導体 |
| US6545013B2 (en) | 2000-05-30 | 2003-04-08 | Celltech R&D Limited | 2,7-naphthyridine derivatives |
| US6403608B1 (en) | 2000-05-30 | 2002-06-11 | Celltech R&D, Ltd. | 3-Substituted isoquinolin-1-yl derivatives |
| US6960597B2 (en) | 2000-06-30 | 2005-11-01 | Orth-Mcneil Pharmaceutical, Inc. | Aza-bridged-bicyclic amino acid derivatives as α4 integrin antagonists |
| US6740654B2 (en) | 2000-07-07 | 2004-05-25 | Celltech R & D Limited | Squaric acid derivatives |
| WO2002008206A1 (en) * | 2000-07-21 | 2002-01-31 | Elan Pharmaceuticals, Inc. | 3-amino-2-(4-aminocarbonyloxy)phenyl-propionic acid derivatives as alpha-4- integrin inhibitors |
| WO2002010136A1 (en) | 2000-08-02 | 2002-02-07 | Celltech R & D Limited | 3-substituted isoquinolin-1-yl derivatives |
| MY129000A (en) | 2000-08-31 | 2007-03-30 | Tanabe Seiyaku Co | INHIBITORS OF a4 MEDIATED CELL ADHESION |
| JP2004526733A (ja) | 2001-03-20 | 2004-09-02 | メルク エンド カムパニー インコーポレーテッド | 強力な細胞接着阻害剤としての置換ｎ−アリールスルホニル−プロリン誘導体 |
| MY140707A (en) | 2002-02-28 | 2010-01-15 | Mitsubishi Tanabe Pharma Corp | Process for preparing a phenylalanine derivative and intermediates thereof |
| CA2561164A1 (en) * | 2004-04-01 | 2005-10-20 | Elan Pharmaceuticals, Inc. | Steroid sparing agents and their use |
| EP2124996A4 (en) | 2007-02-20 | 2010-03-24 | Merrimack Pharmaceuticals Inc | METHODS OF TREATING MULTIPLE SCLEROSIS BY ADMINISTERING ALPHA-FETOPROTEIN COMBINED WITH INTEGRIN ANTAGONIST |
| CA2721093A1 (en) | 2008-04-11 | 2009-10-15 | Merrimack Pharmaceuticals, Inc. | Human serum albumin linkers and conjugates thereof |
| EP2774919A1 (en) * | 2013-03-06 | 2014-09-10 | Pharmeste S.R.L. In Liquidazione | Novel sulfonamide TRPA1 receptor antagonists |
| US9834520B2 (en) | 2013-03-14 | 2017-12-05 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
| EP3018126A4 (en) * | 2013-07-03 | 2016-12-07 | Takeda Pharmaceuticals Co | HETEROCYCLIC COMPOUND |
| EP3018123B1 (en) | 2013-07-03 | 2023-05-10 | Takeda Pharmaceutical Company Limited | Amide compound |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1995015973A1 (en) * | 1993-12-06 | 1995-06-15 | Cytel Corporation | Cs-1 peptidomimetics, compositions and methods of using the same |
| US6306840B1 (en) * | 1995-01-23 | 2001-10-23 | Biogen, Inc. | Cell adhesion inhibitors |
-
1998
- 1998-07-30 CA CA002291475A patent/CA2291475A1/en not_active Abandoned
- 1998-07-30 EP EP98937991A patent/EP0994895A1/en not_active Withdrawn
- 1998-07-30 JP JP2000505190A patent/JP2001512137A/ja not_active Withdrawn
- 1998-07-30 CN CN98807762A patent/CN1265673A/zh active Pending
- 1998-07-30 PL PL98338554A patent/PL338554A1/xx unknown
- 1998-07-30 AU AU86612/98A patent/AU8661298A/en not_active Abandoned
- 1998-07-30 KR KR1020007000992A patent/KR20010022412A/ko not_active Application Discontinuation
- 1998-07-30 AR ARP980103776A patent/AR016387A1/es unknown
- 1998-07-30 WO PCT/US1998/015314 patent/WO1999006435A1/en not_active Application Discontinuation
- 1998-07-30 IL IL13364298A patent/IL133642A0/xx unknown
- 1998-07-30 BR BR9811599-5A patent/BR9811599A/pt not_active Application Discontinuation
- 1998-07-30 HU HU0002682A patent/HUP0002682A3/hu unknown
- 1998-07-30 ZA ZA9806834A patent/ZA986834B/xx unknown
-
2000
- 2000-01-27 NO NO20000412A patent/NO20000412L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| AR016387A1 (es) | 2001-07-04 |
| ZA986834B (en) | 2000-05-02 |
| CA2291475A1 (en) | 1999-02-11 |
| CN1265673A (zh) | 2000-09-06 |
| NO20000412L (no) | 2000-03-24 |
| BR9811599A (pt) | 2000-09-19 |
| NO20000412D0 (no) | 2000-01-27 |
| WO1999006435A1 (en) | 1999-02-11 |
| HUP0002682A3 (en) | 2001-12-28 |
| AU8661298A (en) | 1999-02-22 |
| PL338554A1 (en) | 2000-11-06 |
| EP0994895A1 (en) | 2000-04-26 |
| IL133642A0 (en) | 2001-04-30 |
| KR20010022412A (ko) | 2001-03-15 |
| JP2001512137A (ja) | 2001-08-21 |
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