AU2004278276B2 - New 2-substituted, 4-amino-thiazolo(4,5-d) pyrimidines, useful as chemokine receptor antagonists, esp. CX3CR1 - Google Patents
New 2-substituted, 4-amino-thiazolo(4,5-d) pyrimidines, useful as chemokine receptor antagonists, esp. CX3CR1 Download PDFInfo
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- AU2004278276B2 AU2004278276B2 AU2004278276A AU2004278276A AU2004278276B2 AU 2004278276 B2 AU2004278276 B2 AU 2004278276B2 AU 2004278276 A AU2004278276 A AU 2004278276A AU 2004278276 A AU2004278276 A AU 2004278276A AU 2004278276 B2 AU2004278276 B2 AU 2004278276B2
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- 230000001590 oxidative effect Effects 0.000 description 1
- 208000012111 paraneoplastic syndrome Diseases 0.000 description 1
- 230000007170 pathology Effects 0.000 description 1
- 239000008188 pellet Substances 0.000 description 1
- 229940049954 penicillin Drugs 0.000 description 1
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 description 1
- 239000000137 peptide hydrolase inhibitor Substances 0.000 description 1
- 230000002085 persistent effect Effects 0.000 description 1
- DDBREPKUVSBGFI-UHFFFAOYSA-N phenobarbital Chemical compound C=1C=CC=CC=1C1(CC)C(=O)NC(=O)NC1=O DDBREPKUVSBGFI-UHFFFAOYSA-N 0.000 description 1
- 239000008363 phosphate buffer Substances 0.000 description 1
- 201000006380 plexopathy Diseases 0.000 description 1
- 230000007824 polyneuropathy Effects 0.000 description 1
- 239000004810 polytetrafluoroethylene Substances 0.000 description 1
- 229920001343 polytetrafluoroethylene Polymers 0.000 description 1
- 239000002243 precursor Substances 0.000 description 1
- 238000012746 preparative thin layer chromatography Methods 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 1
- 235000008160 pyridoxine Nutrition 0.000 description 1
- 239000011677 pyridoxine Substances 0.000 description 1
- 125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 description 1
- 229940083082 pyrimidine derivative acting on arteriolar smooth muscle Drugs 0.000 description 1
- 238000011002 quantification Methods 0.000 description 1
- 238000010791 quenching Methods 0.000 description 1
- 239000000376 reactant Substances 0.000 description 1
- 238000001953 recrystallisation Methods 0.000 description 1
- 238000012216 screening Methods 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 239000012279 sodium borohydride Substances 0.000 description 1
- 229910000033 sodium borohydride Inorganic materials 0.000 description 1
- AKHNMLFCWUSKQB-UHFFFAOYSA-L sodium thiosulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=S AKHNMLFCWUSKQB-UHFFFAOYSA-L 0.000 description 1
- 235000019345 sodium thiosulphate Nutrition 0.000 description 1
- SUBJHSREKVAVAR-UHFFFAOYSA-N sodium;methanol;methanolate Chemical compound [Na+].OC.[O-]C SUBJHSREKVAVAR-UHFFFAOYSA-N 0.000 description 1
- 238000007921 solubility assay Methods 0.000 description 1
- 238000001228 spectrum Methods 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 230000010473 stable expression Effects 0.000 description 1
- 238000010561 standard procedure Methods 0.000 description 1
- 239000012258 stirred mixture Substances 0.000 description 1
- 239000011550 stock solution Substances 0.000 description 1
- 229960005322 streptomycin Drugs 0.000 description 1
- 125000001174 sulfone group Chemical group 0.000 description 1
- 208000011580 syndromic disease Diseases 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- CZDYPVPMEAXLPK-UHFFFAOYSA-N tetramethylsilane Chemical compound C[Si](C)(C)C CZDYPVPMEAXLPK-UHFFFAOYSA-N 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- VLLMWSRANPNYQX-UHFFFAOYSA-N thiadiazole Chemical compound C1=CSN=N1.C1=CSN=N1 VLLMWSRANPNYQX-UHFFFAOYSA-N 0.000 description 1
- 229930192474 thiophene Natural products 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 239000012096 transfection reagent Substances 0.000 description 1
- 230000008733 trauma Effects 0.000 description 1
- 150000003852 triazoles Chemical class 0.000 description 1
- 229940011671 vitamin b6 Drugs 0.000 description 1
- 239000011534 wash buffer Substances 0.000 description 1
- 229910052725 zinc Inorganic materials 0.000 description 1
- 239000011701 zinc Substances 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
-
- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- 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
- A61P11/06—Antiasthmatics
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D475/00—Heterocyclic compounds containing pteridine ring systems
- C07D475/06—Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4
-
- 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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pulmonology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Immunology (AREA)
- Urology & Nephrology (AREA)
- Cardiology (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SE0302667-1 | 2003-10-07 | ||
| SE0302667A SE0302667D0 (sv) | 2003-10-07 | 2003-10-07 | Novel Compounds |
| SE0302666-3 | 2003-10-07 | ||
| SE0302666A SE0302666D0 (sv) | 2003-10-07 | 2003-10-07 | Novel Compounds |
| PCT/SE2004/001421 WO2005033115A1 (en) | 2003-10-07 | 2004-10-05 | New 2-substituted, 4-amino-thiazolo[4,5-d] pyrimidines, useful as chemokine receptor antagonists, esp. cx3cr1 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2004278276A1 AU2004278276A1 (en) | 2005-04-14 |
| AU2004278276B2 true AU2004278276B2 (en) | 2007-10-18 |
Family
ID=34425473
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2004278276A Ceased AU2004278276B2 (en) | 2003-10-07 | 2004-10-05 | New 2-substituted, 4-amino-thiazolo(4,5-d) pyrimidines, useful as chemokine receptor antagonists, esp. CX3CR1 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20070142386A1 (enExample) |
| EP (1) | EP1675862A1 (enExample) |
| JP (1) | JP2007507494A (enExample) |
| KR (1) | KR20060120014A (enExample) |
| AU (1) | AU2004278276B2 (enExample) |
| BR (1) | BRPI0415050A (enExample) |
| CA (1) | CA2541533A1 (enExample) |
| IL (1) | IL174508A0 (enExample) |
| MX (1) | MXPA06003792A (enExample) |
| NO (1) | NO20062061L (enExample) |
| WO (1) | WO2005033115A1 (enExample) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE9903544D0 (sv) | 1999-10-01 | 1999-10-01 | Astra Pharma Prod | Novel compounds |
| GB2359551A (en) | 2000-02-23 | 2001-08-29 | Astrazeneca Uk Ltd | Pharmaceutically active pyrimidine derivatives |
| GB0221828D0 (en) | 2002-09-20 | 2002-10-30 | Astrazeneca Ab | Novel compound |
| GB0328243D0 (en) | 2003-12-05 | 2004-01-07 | Astrazeneca Ab | Methods |
| WO2006046739A1 (ja) | 2004-10-29 | 2006-05-04 | Eisai R & D Management Co., Ltd. | 炎症性疾患治療剤 |
| US20090239882A1 (en) * | 2004-12-17 | 2009-09-24 | Astrazeneca Ab | Thiazolopyramidine Compounds for the Modulation of Chemokine Receptor Activity |
| AR053347A1 (es) | 2005-04-06 | 2007-05-02 | Astrazeneca Ab | Derivados de [1,3]tiazolo[4,5-d]pirimidin-2(3h)-ona 5,7-sustituidos |
| UA90707C2 (en) | 2005-04-06 | 2010-05-25 | Астразенека Аб | Novel 5-substituted 7-amino-[1,3]thiazolo[4,5-d]pyrimidine derivatives |
| PE20080145A1 (es) | 2006-03-21 | 2008-02-11 | Janssen Pharmaceutica Nv | Tetrahidro-pirimidoazepinas como moduladores de trpv1 |
| WO2008005303A2 (en) * | 2006-06-30 | 2008-01-10 | Janssen Pharmaceutica N.V. | Thiazolopyrimidine modulators of trpv1 |
| CA2664930A1 (en) * | 2006-09-29 | 2008-04-03 | Astrazeneca Ab | Novel 5,7-disubstituted[1,3]thiazolo[4,5-d]pyrimidin-2(3h)-amine derivatives and their use in therapy |
| TW200820973A (en) * | 2006-09-29 | 2008-05-16 | Astrazeneca Ab | Novel compounds 480 |
| WO2009078999A1 (en) | 2007-12-17 | 2009-06-25 | Janssen Pharmaceutica N.V. | Imidazolo-, oxazolo-, and thiazolopyrimidine modulators of trpv1 |
| US20090156598A1 (en) * | 2007-12-17 | 2009-06-18 | Lebsack Alec D | Imidazolopyrimidine modulators of TRPV1 |
| WO2009109616A2 (en) | 2008-03-07 | 2009-09-11 | Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.P.A. | Novel 1-benzil-3-hydroxymethylindazole derivatives and use thereof in the treatment of diseases based on the expression of mcp-1, cx3cr1 and p40 |
| PT2254869T (pt) * | 2008-03-07 | 2017-07-18 | Acraf | Novos derivados de 1-benzil-3-hidroximetilindazole e suas utilizações no tratamento de doenças com base na expressão de cx3cr1 e p40 |
| CN101959866B (zh) | 2008-03-07 | 2013-10-02 | 方济各安吉利克化学联合股份有限公司 | 1-苄基-3-羟基甲基吲唑衍生物及其在治疗基于mcp-1和cx3cr1表达的疾病中的用途 |
| JO3437B1 (ar) | 2009-10-30 | 2019-10-20 | Esai R & D Man Co Ltd | أجسام مضادة محسنة مضادة للفراكتالكين البشري واستخداماتها |
| WO2012078633A2 (en) * | 2010-12-07 | 2012-06-14 | Philadelphia Health And Education Corporation, D/B/A Drexel University College Of Medicene | Methods of inhibiting metastasis from cancer |
| US8476301B2 (en) | 2011-09-13 | 2013-07-02 | Eisai R&D Management Co., Ltd. | Pyrrolidin-3-ylacetic acid derivative |
| TWI543975B (zh) * | 2011-09-13 | 2016-08-01 | Eisai R&D Man Co Ltd | Pyrrolidin-3-yl acetic acid derivatives |
| JP5872105B2 (ja) | 2013-03-12 | 2016-03-01 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | ピロリジン−３−イル酢酸誘導体の塩およびその結晶 |
| WO2014142086A1 (ja) * | 2013-03-13 | 2014-09-18 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | ピロリジン－３－イル酢酸誘導体およびピペリジン－３－イル酢酸誘導体 |
| US11267817B2 (en) | 2017-05-02 | 2022-03-08 | Drexel University | Substituted pyrrolo[1,2-a]quinoxalin-4(5H)-ones as CX3CR1 antagonists |
| GB201811169D0 (en) | 2018-07-06 | 2018-08-29 | Kancera Ab | New compounds |
| KR20250086780A (ko) | 2022-10-19 | 2025-06-13 | 아스트라제네카 아베 | Cx3cr1 조절제로서의 2,4,6-삼중치환된 1,3,5-트리아진 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE9802729D0 (sv) * | 1998-08-13 | 1998-08-13 | Astra Pharma Prod | Novel Compounds |
| SE9903544D0 (sv) * | 1999-10-01 | 1999-10-01 | Astra Pharma Prod | Novel compounds |
| SE0101082D0 (sv) * | 2001-03-27 | 2001-03-27 | Astrazeneca Ab | Novel use |
| SE0101322D0 (sv) * | 2001-04-12 | 2001-04-12 | Astrazeneca Ab | Novel compounds |
-
2004
- 2004-10-05 MX MXPA06003792A patent/MXPA06003792A/es unknown
- 2004-10-05 KR KR1020067006638A patent/KR20060120014A/ko not_active Withdrawn
- 2004-10-05 JP JP2006532235A patent/JP2007507494A/ja active Pending
- 2004-10-05 CA CA002541533A patent/CA2541533A1/en not_active Abandoned
- 2004-10-05 WO PCT/SE2004/001421 patent/WO2005033115A1/en not_active Ceased
- 2004-10-05 BR BRPI0415050-3A patent/BRPI0415050A/pt not_active IP Right Cessation
- 2004-10-05 US US10/575,534 patent/US20070142386A1/en not_active Abandoned
- 2004-10-05 EP EP04775512A patent/EP1675862A1/en not_active Withdrawn
- 2004-10-05 AU AU2004278276A patent/AU2004278276B2/en not_active Ceased
-
2006
- 2006-03-23 IL IL174508A patent/IL174508A0/en unknown
- 2006-05-08 NO NO20062061A patent/NO20062061L/no not_active Application Discontinuation
Non-Patent Citations (1)
| Title |
|---|
| Pfleiderer, W. et al., Chemische Berichte, 1963, 96, 2964-2976 * |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2005033115A1 (en) | 2005-04-14 |
| IL174508A0 (en) | 2006-08-01 |
| EP1675862A1 (en) | 2006-07-05 |
| US20070142386A1 (en) | 2007-06-21 |
| JP2007507494A (ja) | 2007-03-29 |
| AU2004278276A1 (en) | 2005-04-14 |
| MXPA06003792A (es) | 2006-06-14 |
| KR20060120014A (ko) | 2006-11-24 |
| NO20062061L (no) | 2006-07-03 |
| CA2541533A1 (en) | 2005-04-14 |
| BRPI0415050A (pt) | 2006-11-28 |
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| Date | Code | Title | Description |
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| FGA | Letters patent sealed or granted (standard patent) | ||
| MK14 | Patent ceased section 143(a) (annual fees not paid) or expired |