JP2008504301A5 - - Google Patents
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- Publication number
- JP2008504301A5 JP2008504301A5 JP2007518379A JP2007518379A JP2008504301A5 JP 2008504301 A5 JP2008504301 A5 JP 2008504301A5 JP 2007518379 A JP2007518379 A JP 2007518379A JP 2007518379 A JP2007518379 A JP 2007518379A JP 2008504301 A5 JP2008504301 A5 JP 2008504301A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- alkyl
- aryl
- heteroalkyl
- heteroaryl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 150000001875 compounds Chemical class 0.000 claims 54
- 125000004404 heteroalkyl group Chemical group 0.000 claims 32
- 125000003118 aryl group Chemical group 0.000 claims 26
- 125000001072 heteroaryl group Chemical group 0.000 claims 21
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims 19
- 229910052739 hydrogen Inorganic materials 0.000 claims 11
- 239000001257 hydrogen Substances 0.000 claims 11
- 229910052736 halogen Inorganic materials 0.000 claims 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 9
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 239000000651 prodrug Substances 0.000 claims 5
- 229940002612 prodrug Drugs 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 125000003837 (C1-C20) alkyl group Chemical group 0.000 claims 4
- 102100028990 C-X-C chemokine receptor type 3 Human genes 0.000 claims 4
- 201000004624 Dermatitis Diseases 0.000 claims 4
- 101000916050 Homo sapiens C-X-C chemokine receptor type 3 Proteins 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 125000004474 heteroalkylene group Chemical group 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 230000002757 inflammatory effect Effects 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 3
- 201000004681 Psoriasis Diseases 0.000 claims 3
- 125000002947 alkylene group Chemical group 0.000 claims 3
- 208000006673 asthma Diseases 0.000 claims 3
- 201000006417 multiple sclerosis Diseases 0.000 claims 3
- 210000000056 organ Anatomy 0.000 claims 3
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 3
- 125000003107 substituted aryl group Chemical group 0.000 claims 3
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 2
- 201000001320 Atherosclerosis Diseases 0.000 claims 2
- 208000035143 Bacterial infection Diseases 0.000 claims 2
- 208000027496 Behcet disease Diseases 0.000 claims 2
- 208000009137 Behcet syndrome Diseases 0.000 claims 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 2
- 206010009900 Colitis ulcerative Diseases 0.000 claims 2
- 206010010741 Conjunctivitis Diseases 0.000 claims 2
- 208000011231 Crohn disease Diseases 0.000 claims 2
- 201000005569 Gout Diseases 0.000 claims 2
- 208000009329 Graft vs Host Disease Diseases 0.000 claims 2
- 201000009906 Meningitis Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 208000005141 Otitis Diseases 0.000 claims 2
- 206010039085 Rhinitis allergic Diseases 0.000 claims 2
- 206010040047 Sepsis Diseases 0.000 claims 2
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 2
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 2
- 208000024780 Urticaria Diseases 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 201000010105 allergic rhinitis Diseases 0.000 claims 2
- 208000010668 atopic eczema Diseases 0.000 claims 2
- 208000022362 bacterial infectious disease Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 208000019258 ear infection Diseases 0.000 claims 2
- 206010014599 encephalitis Diseases 0.000 claims 2
- 208000024908 graft versus host disease Diseases 0.000 claims 2
- 208000006454 hepatitis Diseases 0.000 claims 2
- 231100000283 hepatitis Toxicity 0.000 claims 2
- 125000005114 heteroarylalkoxy group Chemical group 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 201000008383 nephritis Diseases 0.000 claims 2
- 230000004770 neurodegeneration Effects 0.000 claims 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 201000000306 sarcoidosis Diseases 0.000 claims 2
- 201000009890 sinusitis Diseases 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 2
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 1
- 125000006833 (C1-C5) alkylene group Chemical group 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- -1 NH 2 Inorganic materials 0.000 claims 1
- 208000036142 Viral infection Diseases 0.000 claims 1
- 241000700605 Viruses Species 0.000 claims 1
- 125000002877 alkyl aryl group Chemical group 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000004802 cyanophenyl group Chemical group 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 230000009385 viral infection Effects 0.000 claims 1
- 0 C*[C@](C)C*(*(C)C)=*(C)c1c(*)*cc*1C Chemical compound C*[C@](C)C*(*(C)C)=*(C)c1c(*)*cc*1C 0.000 description 4
- LNSGIYHTBZBJHU-UHFFFAOYSA-N CC(Cc(cc1)ccc1OC(F)(F)F)=O Chemical compound CC(Cc(cc1)ccc1OC(F)(F)F)=O LNSGIYHTBZBJHU-UHFFFAOYSA-N 0.000 description 2
- UIPDPUXNQIWJLF-UHFFFAOYSA-N CC(Cc1ccc(C(F)(F)F)cc1)=O Chemical compound CC(Cc1ccc(C(F)(F)F)cc1)=O UIPDPUXNQIWJLF-UHFFFAOYSA-N 0.000 description 2
- AUDJPOKCCLAMKC-XGOROQTFSA-N CC(CC/C=C\C(\C(F)(F)F)=C(/C#C)\F)=O Chemical compound CC(CC/C=C\C(\C(F)(F)F)=C(/C#C)\F)=O AUDJPOKCCLAMKC-XGOROQTFSA-N 0.000 description 1
- FKQYECMKLWYTCQ-UHFFFAOYSA-N CC(Cc1cc(F)c(C(F)(F)F)cc1)=O Chemical compound CC(Cc1cc(F)c(C(F)(F)F)cc1)=O FKQYECMKLWYTCQ-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US58390104P | 2004-06-28 | 2004-06-28 | |
| PCT/US2005/023251 WO2006004915A1 (en) | 2004-06-28 | 2005-06-28 | Fused pyrimidine derivatives and compositions thereof as cxcr3 receptor modulators, useful in prevention and treatment of inflammatory and immunoregulatory disorders and diseases |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2008504301A JP2008504301A (ja) | 2008-02-14 |
| JP2008504301A5 true JP2008504301A5 (enExample) | 2008-08-14 |
Family
ID=35197976
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007518379A Pending JP2008504301A (ja) | 2004-06-28 | 2005-06-28 | 炎症性及び免疫調節性の障害及び疾患の予防及び治療に有用である、ｃｘｃｒ３受容体モジュレーターとしての縮合ピリミジン誘導体及びその組成物 |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US7939538B2 (enExample) |
| EP (1) | EP1771447A1 (enExample) |
| JP (1) | JP2008504301A (enExample) |
| KR (1) | KR20070045203A (enExample) |
| CN (1) | CN101006088A (enExample) |
| AR (1) | AR049558A1 (enExample) |
| AU (1) | AU2005260620A1 (enExample) |
| BR (1) | BRPI0512703A (enExample) |
| CA (1) | CA2572083A1 (enExample) |
| EA (1) | EA011439B1 (enExample) |
| EC (1) | ECSP077212A (enExample) |
| IL (1) | IL180327A0 (enExample) |
| MA (1) | MA28755B1 (enExample) |
| MX (1) | MX2007000051A (enExample) |
| NO (1) | NO20070484L (enExample) |
| TN (1) | TNSN06430A1 (enExample) |
| TW (1) | TW200611699A (enExample) |
| WO (1) | WO2006004915A1 (enExample) |
| ZA (1) | ZA200700752B (enExample) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9506197D0 (en) | 1995-03-27 | 1995-05-17 | Hoffmann La Roche | Inhibition of tau-tau association. |
| JP2003007697A (ja) * | 2001-06-21 | 2003-01-10 | Hitachi Kokusai Electric Inc | 半導体装置の製造方法、基板処理方法および基板処理装置 |
| US7491794B2 (en) * | 2003-10-14 | 2009-02-17 | Intermune, Inc. | Macrocyclic compounds as inhibitors of viral replication |
| US7939538B2 (en) | 2004-06-28 | 2011-05-10 | Amgen Inc. | Compounds, compositions and methods for prevention and treatment of inflammatory and immunoregulatory disorders and diseases |
| TW200714610A (en) * | 2005-02-16 | 2007-04-16 | Univ Maryland | CXCR3 is a gliadin receptor |
| EP1917250B1 (en) | 2005-06-27 | 2010-07-21 | Amgen, Inc | Anti-inflammatory aryl nitrile compounds |
| EP2305696A3 (en) * | 2005-07-25 | 2011-10-12 | Intermune, Inc. | Macrocyclic inhibitors of Hepatitis C virus replication |
| JP2009511595A (ja) * | 2005-10-11 | 2009-03-19 | インターミューン・インコーポレーテッド | Ｃ型肝炎ウイルスの複製を阻害する化合物および方法 |
| KR20090024834A (ko) * | 2006-07-05 | 2009-03-09 | 인터뮨, 인크. | Ｃ형 간염 바이러스 복제의 신규 억제제 |
| KR101129868B1 (ko) * | 2006-10-04 | 2012-04-12 | 화이자 프로덕츠 인코포레이티드 | 칼슘 수용체 길항제로서의 피리도［4,3-ｄ］피리미딘-4(3Ｈ)-온 유도체 |
| BRPI0811020A2 (pt) * | 2007-05-03 | 2015-07-21 | Intermune Inc | Composto, composição farmacêutica e métodos de inibição da atividade da protease ns3/ns4, de tratamento da fibrose hepática, de intensificação da função hepática em indivíduo com infecção do vírus da hepatite c e métodos de síntese de compostos, de administração de inibidor da infecção do vírus da hepatite c (hcv) e de distribuição de forma de dosagem oral. |
| KR20100027134A (ko) | 2007-05-10 | 2010-03-10 | 인터뮨, 인크. | Ｃ형 간염 바이러스 복제의 신규 펩티드 억제제 |
| WO2009094168A1 (en) * | 2008-01-22 | 2009-07-30 | Amgen Inc. | Cxcr3 antagonists |
| EP2282762A2 (en) * | 2008-04-15 | 2011-02-16 | Intermune, Inc. | Novel macrocyclic inhibitors of hepatitis c virus replication |
| AR075584A1 (es) * | 2009-02-27 | 2011-04-20 | Intermune Inc | COMPOSICIONES TERAPEUTICAS QUE COMPRENDEN beta-D-2'-DESOXI-2'-FLUORO-2'-C-METILCITIDINA Y UN DERIVADO DE ACIDO ISOINDOL CARBOXILICO Y SUS USOS. COMPUESTO. |
| WO2011038293A1 (en) * | 2009-09-28 | 2011-03-31 | Intermune, Inc. | Cyclic peptide inhibitors of hepatitis c virus replication |
| JPWO2012011591A1 (ja) * | 2010-07-23 | 2013-09-09 | 武田薬品工業株式会社 | 縮合複素環化合物およびその用途 |
| US8940742B2 (en) | 2012-04-10 | 2015-01-27 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| BR112015014592A2 (pt) | 2012-12-21 | 2017-07-11 | Gilead Calistoga Llc | composto, composição farmacêutica, e, método para o tratamento de um humano |
| CA2895782C (en) | 2012-12-21 | 2017-08-22 | Gilead Calistoga Llc | Substituted pyrimidine aminoalkyl-quinazolones as phosphatidylinositol 3-kinase inhibitors |
| EP3008053B1 (en) | 2013-06-14 | 2018-03-21 | Gilead Calistoga LLC | Phosphatidylinositol 3-kinase inhibitors |
| UY35675A (es) | 2013-07-24 | 2015-02-27 | Novartis Ag | Derivados sustituidos de quinazolin-4-ona |
| US9359365B2 (en) | 2013-10-04 | 2016-06-07 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| WO2015051241A1 (en) | 2013-10-04 | 2015-04-09 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| CN106456628A (zh) | 2014-03-19 | 2017-02-22 | 无限药品股份有限公司 | 用于治疗PI3K‑γ介导的障碍的杂环化合物 |
| US9708348B2 (en) | 2014-10-03 | 2017-07-18 | Infinity Pharmaceuticals, Inc. | Trisubstituted bicyclic heterocyclic compounds with kinase activities and uses thereof |
| CA2998469C (en) | 2015-09-14 | 2025-12-09 | Twelve Therapeutics, Inc. | Solid forms of isoquinolinones, and process of making, composition comprising, and methods of using the same |
| WO2017161116A1 (en) | 2016-03-17 | 2017-09-21 | Infinity Pharmaceuticals, Inc. | Isotopologues of isoquinolinone and quinazolinone compounds and uses thereof as pi3k kinase inhibitors |
| WO2017214269A1 (en) | 2016-06-08 | 2017-12-14 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| TW201815787A (zh) | 2016-09-23 | 2018-05-01 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
| TW201825465A (zh) | 2016-09-23 | 2018-07-16 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
| TW201813963A (zh) | 2016-09-23 | 2018-04-16 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
Family Cites Families (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0481614A1 (en) | 1990-10-01 | 1992-04-22 | Merck & Co. Inc. | Substituted pyridopyrimidinones and related heterocycles as angiotensin II antagonists |
| US5202322A (en) * | 1991-09-25 | 1993-04-13 | Merck & Co., Inc. | Quinazolinone and pyridopyrimidine a-II antagonists |
| US5256667A (en) * | 1991-09-25 | 1993-10-26 | Merck & Co., Inc. | Quinazolinones and pyridopyrimidinones |
| US5756502A (en) * | 1994-08-08 | 1998-05-26 | Warner-Lambert Company | Quinazolinone derivatives as cholyecystokinin (CCK) ligands |
| US5719144A (en) * | 1995-02-22 | 1998-02-17 | Merck & Co., Inc. | Fibrinogen receptor antagonists |
| US5908930A (en) * | 1995-03-15 | 1999-06-01 | Pfizer Inc. | 5,10-dihydropyrimdo 4,5-b!quinolin-4(1H)-one tyrosine kinase inhibitors |
| US6140064A (en) * | 1996-09-10 | 2000-10-31 | Theodor-Kocher Institute | Method of detecting or identifying ligands, inhibitors or promoters of CXC chemokine receptor 3 |
| AU5380398A (en) | 1996-12-17 | 1998-07-15 | E.I. Du Pont De Nemours And Company | Fungicidal quinazolinones |
| FR2778662B1 (fr) * | 1998-05-12 | 2000-06-16 | Adir | Nouveaux composes cycliques substitues, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| WO2001016114A2 (en) | 1999-08-27 | 2001-03-08 | Chemocentryx, Inc. | Heterocyclic compounds and methods for modulating cxcr3 function |
| ATE286033T1 (de) | 1999-09-16 | 2005-01-15 | Curis Inc | Vermittler von igel signalwegen, deren zusammenstellungen und verwendungen |
| US6545004B1 (en) | 1999-10-27 | 2003-04-08 | Cytokinetics, Inc. | Methods and compositions utilizing quinazolinones |
| PL203998B1 (pl) | 1999-10-27 | 2009-11-30 | Cytokinetics Inc | Nowy związek chinazolinowy, zastosowanie związku chinazolinowego, sposób jego otrzymywania i kompozycja farmaceutyczna zawierająca związek chinazolinowy |
| GB2359551A (en) | 2000-02-23 | 2001-08-29 | Astrazeneca Uk Ltd | Pharmaceutically active pyrimidine derivatives |
| SK8752003A3 (en) * | 2000-12-11 | 2003-11-04 | Tularik Inc | CXCR3 antagonists, pharmaceutical composition comprising same and use thereof |
| ITMI20010808A1 (it) | 2001-04-13 | 2002-10-13 | Ilpea Ind Spa | Procedimento per ottenere una pelle sintetica adatta in particolare arivestire plance portastrumenti in autoveicoli e pelle cosi' ottenuta |
| US6794379B2 (en) * | 2001-06-06 | 2004-09-21 | Tularik Inc. | CXCR3 antagonists |
| DE60336901D1 (de) | 2002-03-07 | 2011-06-09 | X Ceptor Therapeutics Inc | Chinazolinon modulatoren von nukleinrezeptoren |
| JP2006508030A (ja) * | 2002-05-09 | 2006-03-09 | サイトキネティクス・インコーポレーテッド | ピリミジノン化合物、組成物および方法 |
| EP1513820A4 (en) * | 2002-05-23 | 2006-09-13 | Cytokinetics Inc | COMPOUNDS, COMPOSITIONS AND METHODS |
| US20040242498A1 (en) | 2003-02-27 | 2004-12-02 | Collins Tassie L. | CXCR3 antagonists |
| US7939538B2 (en) | 2004-06-28 | 2011-05-10 | Amgen Inc. | Compounds, compositions and methods for prevention and treatment of inflammatory and immunoregulatory disorders and diseases |
| US7271271B2 (en) * | 2004-06-28 | 2007-09-18 | Amgen Sf, Llc | Imidazolo-related compounds, compositions and methods for their use |
| US7375102B2 (en) * | 2004-06-28 | 2008-05-20 | Amgen Sf, Llc | Tetrahydroquinazolin-4(3H)-one-related and tetrahydropyrido[2,3-D]pyrimidin-4(3H)-one-related compounds, compositions and methods for their use |
| WO2006023381A1 (en) * | 2004-08-16 | 2006-03-02 | Taigen Biotechnology | Pyrimidinone compounds |
| EP1917250B1 (en) * | 2005-06-27 | 2010-07-21 | Amgen, Inc | Anti-inflammatory aryl nitrile compounds |
-
2005
- 2005-06-27 US US11/168,005 patent/US7939538B2/en not_active Expired - Fee Related
- 2005-06-28 KR KR1020077002012A patent/KR20070045203A/ko not_active Withdrawn
- 2005-06-28 AU AU2005260620A patent/AU2005260620A1/en not_active Abandoned
- 2005-06-28 AR ARP050102670A patent/AR049558A1/es not_active Application Discontinuation
- 2005-06-28 JP JP2007518379A patent/JP2008504301A/ja active Pending
- 2005-06-28 WO PCT/US2005/023251 patent/WO2006004915A1/en not_active Ceased
- 2005-06-28 MX MX2007000051A patent/MX2007000051A/es not_active Application Discontinuation
- 2005-06-28 CN CNA2005800277780A patent/CN101006088A/zh active Pending
- 2005-06-28 ZA ZA200700752A patent/ZA200700752B/xx unknown
- 2005-06-28 TW TW094121708A patent/TW200611699A/zh unknown
- 2005-06-28 EA EA200700169A patent/EA011439B1/ru not_active IP Right Cessation
- 2005-06-28 BR BRPI0512703-3A patent/BRPI0512703A/pt not_active IP Right Cessation
- 2005-06-28 CA CA002572083A patent/CA2572083A1/en not_active Abandoned
- 2005-06-28 EP EP05789126A patent/EP1771447A1/en not_active Withdrawn
-
2006
- 2006-12-25 IL IL180327A patent/IL180327A0/en unknown
- 2006-12-26 TN TNP2006000430A patent/TNSN06430A1/en unknown
-
2007
- 2007-01-25 NO NO20070484A patent/NO20070484L/no not_active Application Discontinuation
- 2007-01-29 EC EC2007007212A patent/ECSP077212A/es unknown
- 2007-01-29 MA MA29639A patent/MA28755B1/fr unknown