JP2012522759A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2012522759A5 JP2012522759A5 JP2012502778A JP2012502778A JP2012522759A5 JP 2012522759 A5 JP2012522759 A5 JP 2012522759A5 JP 2012502778 A JP2012502778 A JP 2012502778A JP 2012502778 A JP2012502778 A JP 2012502778A JP 2012522759 A5 JP2012522759 A5 JP 2012522759A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally
- independently
- substituted
- alkyl
- substituents selected
- 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.)
- Granted
Links
- 125000001424 substituent group Chemical group 0.000 claims 28
- 150000001875 compounds Chemical class 0.000 claims 22
- 125000000217 alkyl group Chemical group 0.000 claims 19
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 13
- 229910052739 hydrogen Inorganic materials 0.000 claims 13
- 239000001257 hydrogen Substances 0.000 claims 13
- 125000003118 aryl group Chemical group 0.000 claims 11
- 201000010099 disease Diseases 0.000 claims 11
- 125000001072 heteroaryl group Chemical group 0.000 claims 11
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 9
- 150000001408 amides Chemical class 0.000 claims 9
- 150000002148 esters Chemical class 0.000 claims 9
- 150000003839 salts Chemical class 0.000 claims 9
- 239000012453 solvate Substances 0.000 claims 9
- 125000005842 heteroatom Chemical group 0.000 claims 8
- 125000005843 halogen group Chemical group 0.000 claims 7
- 238000000034 method Methods 0.000 claims 7
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 6
- 125000001153 fluoro group Chemical group F* 0.000 claims 5
- 201000001320 Atherosclerosis Diseases 0.000 claims 4
- 208000020084 Bone disease Diseases 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 239000002671 adjuvant Substances 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 239000003085 diluting agent Substances 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 3
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 3
- 230000005764 inhibitory process Effects 0.000 claims 3
- 239000001301 oxygen Substances 0.000 claims 3
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 238000002360 preparation method Methods 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 239000011593 sulfur Substances 0.000 claims 3
- 208000012124 AIDS-related disease Diseases 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 2
- 201000003883 Cystic fibrosis Diseases 0.000 claims 2
- 206010018364 Glomerulonephritis Diseases 0.000 claims 2
- 206010019842 Hepatomegaly Diseases 0.000 claims 2
- 206010062016 Immunosuppression Diseases 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 2
- 208000009905 Neurofibromatoses Diseases 0.000 claims 2
- 208000031481 Pathologic Constriction Diseases 0.000 claims 2
- 208000004403 Prostatic Hyperplasia Diseases 0.000 claims 2
- 201000004681 Psoriasis Diseases 0.000 claims 2
- 208000006011 Stroke Diseases 0.000 claims 2
- 230000006044 T cell activation Effects 0.000 claims 2
- 108090000190 Thrombin Proteins 0.000 claims 2
- 208000036142 Viral infection Diseases 0.000 claims 2
- 208000026935 allergic disease Diseases 0.000 claims 2
- 206010003246 arthritis Diseases 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 230000030833 cell death Effects 0.000 claims 2
- 230000004663 cell proliferation Effects 0.000 claims 2
- 208000015114 central nervous system disease Diseases 0.000 claims 2
- 239000013066 combination product Substances 0.000 claims 2
- 229940127555 combination product Drugs 0.000 claims 2
- 230000001066 destructive effect Effects 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 230000004064 dysfunction Effects 0.000 claims 2
- 230000002124 endocrine Effects 0.000 claims 2
- 239000005556 hormone Substances 0.000 claims 2
- 229940088597 hormone Drugs 0.000 claims 2
- 208000026278 immune system disease Diseases 0.000 claims 2
- 230000001506 immunosuppresive effect Effects 0.000 claims 2
- 208000033065 inborn errors of immunity Diseases 0.000 claims 2
- 208000015181 infectious disease Diseases 0.000 claims 2
- 208000027866 inflammatory disease Diseases 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 208000019423 liver disease Diseases 0.000 claims 2
- 230000002503 metabolic effect Effects 0.000 claims 2
- 201000004931 neurofibromatosis Diseases 0.000 claims 2
- 201000001119 neuropathy Diseases 0.000 claims 2
- 230000007823 neuropathy Effects 0.000 claims 2
- 230000000414 obstructive effect Effects 0.000 claims 2
- 210000000056 organ Anatomy 0.000 claims 2
- 230000001575 pathological effect Effects 0.000 claims 2
- 208000033808 peripheral neuropathy Diseases 0.000 claims 2
- 208000015768 polyposis Diseases 0.000 claims 2
- 230000002980 postoperative effect Effects 0.000 claims 2
- 208000028529 primary immunodeficiency disease Diseases 0.000 claims 2
- 230000002062 proliferating effect Effects 0.000 claims 2
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 2
- 208000023504 respiratory system disease Diseases 0.000 claims 2
- 208000037803 restenosis Diseases 0.000 claims 2
- 208000010110 spontaneous platelet aggregation Diseases 0.000 claims 2
- 230000036262 stenosis Effects 0.000 claims 2
- 208000037804 stenosis Diseases 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- 229960004072 thrombin Drugs 0.000 claims 2
- 210000004509 vascular smooth muscle cell Anatomy 0.000 claims 2
- 230000009385 viral infection Effects 0.000 claims 2
- 125000006582 (C5-C6) heterocycloalkyl group Chemical group 0.000 claims 1
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 239000000047 product Substances 0.000 claims 1
- 0 *c(nc1[s]c(*)n[n]11)c1I Chemical compound *c(nc1[s]c(*)n[n]11)c1I 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09380069.6 | 2009-04-02 | ||
| EP09380069 | 2009-04-02 | ||
| PCT/GB2010/000674 WO2010112874A1 (en) | 2009-04-02 | 2010-04-01 | Imidazo [2, 1-b] [ 1, 3, 4 ] thiadiazole derivatives |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2012522759A JP2012522759A (ja) | 2012-09-27 |
| JP2012522759A5 true JP2012522759A5 (enExample) | 2013-05-16 |
| JP5615902B2 JP5615902B2 (ja) | 2014-10-29 |
Family
ID=40750794
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012502778A Expired - Fee Related JP5615902B2 (ja) | 2009-04-02 | 2010-04-01 | イミダゾ［２，１−ｂ］［１，３，４］チアジアゾール誘導体 |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US8815918B2 (enExample) |
| EP (1) | EP2414369B1 (enExample) |
| JP (1) | JP5615902B2 (enExample) |
| KR (1) | KR101727264B1 (enExample) |
| CN (1) | CN102388055B (enExample) |
| AU (1) | AU2010231162B2 (enExample) |
| BR (1) | BRPI1015367B8 (enExample) |
| CA (1) | CA2756873C (enExample) |
| CY (1) | CY1116880T1 (enExample) |
| DK (1) | DK2414369T3 (enExample) |
| EA (1) | EA022753B1 (enExample) |
| ES (1) | ES2548571T3 (enExample) |
| HR (1) | HRP20151126T1 (enExample) |
| HU (1) | HUE027964T2 (enExample) |
| IL (1) | IL215158A (enExample) |
| MX (1) | MX2011010372A (enExample) |
| NZ (1) | NZ595674A (enExample) |
| PL (1) | PL2414369T3 (enExample) |
| PT (1) | PT2414369E (enExample) |
| SG (1) | SG175001A1 (enExample) |
| SI (1) | SI2414369T1 (enExample) |
| WO (1) | WO2010112874A1 (enExample) |
| ZA (1) | ZA201107350B (enExample) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0821913D0 (en) | 2008-12-02 | 2009-01-07 | Price & Co | Antibacterial compounds |
| WO2011121317A1 (en) | 2010-04-01 | 2011-10-06 | Centro Nacional De Investigaciones Oncologicas (Cnio) | Imidazo [2,1-b] [1,3,4] thiadiazoles as protein or lipid kinase inhibitors |
| GB2480815A (en) * | 2010-06-01 | 2011-12-07 | Summit Corp Plc | Compounds for the treatment of clostridium difficile-associated disease |
| SI2575968T1 (sl) | 2010-06-01 | 2016-06-30 | Summit Therapeutics Plc | Spojine za zdravljenje bolezni, ki je povezana s clostridium difficile |
| WO2012020217A1 (en) | 2010-08-09 | 2012-02-16 | Centro Nacional De Investigaciones Oncológicas (Cnio) | Amino- imidazolothiadiazoles for use as protein or lipid kinase inhibitors |
| WO2012020215A1 (en) | 2010-08-09 | 2012-02-16 | Centro Nacional De Investigaciones Oncológicas (Cnio) | Amino- imidazolothiadiazoles for use as protein or lipid kinase inhibitors |
| PT2624696T (pt) | 2010-10-06 | 2017-03-21 | Glaxosmithkline Llc | Derivados de benzimidazole como inibidores da cinase pi3 |
| TWI617559B (zh) | 2010-12-22 | 2018-03-11 | 江蘇恆瑞醫藥股份有限公司 | ２－芳基咪唑并［１，２－ｂ］嗒．２－苯基咪唑并［１，２－ａ］吡啶，和２－苯基咪唑并［１，２－ａ］吡衍生物 |
| US9284334B2 (en) | 2011-05-19 | 2016-03-15 | Fundación Centro Nacional De Investigaciones Oncologicas Carlos Iii | Macrocyclic compounds as protein kinase inhibitors |
| KR101399484B1 (ko) | 2011-07-14 | 2014-05-29 | 한국화학연구원 | 허피스바이러스 엑소뉴클리에이즈 활성 억제 물질을 유효성분으로 함유하는 항허피스바이러스용 약학적 조성물 |
| HRP20211778T1 (hr) | 2014-08-29 | 2022-03-18 | Chdi Foundation, Inc. | Kontrastna sredstva za slikovnu dijagnostiku huntingtin proteina |
| BR112017004134A2 (pt) * | 2014-08-29 | 2017-12-12 | Chdi Foundation Inc | ?sondas para imageamento de proteína de huntingtina? |
| CN118084937A (zh) * | 2018-08-21 | 2024-05-28 | 杏林制药株式会社 | 双环杂芳族环衍生物 |
| WO2020061103A1 (en) | 2018-09-18 | 2020-03-26 | Nikang Therapeutics, Inc. | Fused tricyclic ring derivatives as src homology-2 phosphatase inhibitors |
| CN114787167B (zh) | 2019-10-21 | 2024-06-21 | 诺华股份有限公司 | 用于治疗寄生虫病的化合物及组合物 |
| WO2022053838A1 (en) * | 2020-09-14 | 2022-03-17 | The University Of Sussex | Small molecule inhibitors of lemur tyrosine kinase 3 |
Family Cites Families (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1464259A (en) | 1975-10-03 | 1977-02-09 | Pfizer Ltd | Imidazo-thiazole and -thiadiazole sulphonamides and their use as therapeutic agents |
| NO811630L (no) | 1980-05-29 | 1981-11-30 | Bayer Ag | Imidazoazolalkensyreamider, nye mellomprodukter for deres fremstilling, deres fremstilling og deres anvendelse som legemiddel |
| DE3208437A1 (de) | 1982-03-09 | 1983-09-15 | Bayer Ag, 5090 Leverkusen | Imidazothiadiazolalkencarbonsaeureamide, neue zwischenprodukte zu ihrer herstellung, ihre herstellung und ihre verwendung in arzneimitteln |
| IT1269176B (it) | 1994-01-11 | 1997-03-21 | Isagro Srl | Eterobicicli ad attivita' fungicida |
| AU7001396A (en) | 1995-09-22 | 1997-04-09 | Takeda Chemical Industries Ltd. | Triazole compounds, their production and use |
| MXPA03001189A (es) * | 2000-08-09 | 2004-05-14 | Agouron Pharma | Compuestos de pirazol-tiazol, composiciones farmaceuticas que los contienen y su uso para inhibir las cinasas dependientes de ciclinas. |
| CA2364985A1 (en) * | 2001-12-14 | 2003-06-14 | John W. Gillard | Imidazo(2,1-b)thiadiazole sulfonamides |
| NZ541151A (en) | 2002-12-18 | 2008-09-26 | Vertex Pharma | Triazolopyridazines as protein kinase inhibitors |
| PA8595001A1 (es) | 2003-03-04 | 2004-09-28 | Pfizer Prod Inc | Nuevos compuestos heteroaromaticos condensados que son inhibidores del factor de crecimiento transforante (tgf) |
| WO2004111060A1 (en) * | 2003-06-13 | 2004-12-23 | Aegera Therapeutics Inc. | IMIDAZO[2,1-b]-1,3,4-THIADIAZOLE SULFOXIDES AND SULFONES |
| CA2527906A1 (en) | 2003-06-13 | 2004-12-23 | Aegera Therapeutics, Inc. | Acylated imidazo[2,1-b]-1,3,4,-thiadiazole-2-sulfonamides and uses thereof |
| SE0402735D0 (sv) | 2004-11-09 | 2004-11-09 | Astrazeneca Ab | Novel compounds |
| WO2006128693A2 (en) | 2005-06-01 | 2006-12-07 | Ucb Pharma, S.A. | 2 -oxo-i -pyrrolidine derivatives/ processes for preparing them and their therapeutic use on the central nervous system |
| WO2007025090A2 (en) | 2005-08-25 | 2007-03-01 | Kalypsys, Inc. | Heterobicyclic and - tricyclic inhibitors of mapk/erk kinase |
| US7750000B2 (en) | 2005-09-02 | 2010-07-06 | Bayer Schering Pharma Ag | Substituted imidazo[1,2b]pyridazines as kinase inhibitors, their preparation and use as medicaments |
| KR20080080584A (ko) | 2005-11-30 | 2008-09-04 | 버텍스 파마슈티칼스 인코포레이티드 | ｃ-Ｍｅｔ의 억제제 및 이의 용도 |
| CA2584745A1 (en) | 2006-04-13 | 2007-10-13 | Aegera Therapeutics Inc. | Use of imidazo(2,1-b) -1,3,4-thiadiazole-2-sulfonamide compounds to treat neuropathic pain |
| CN101484452A (zh) | 2006-05-03 | 2009-07-15 | 阿斯利康(瑞典)有限公司 | 噻唑衍生物及其作为抗肿瘤药物的用途 |
| WO2007136736A2 (en) | 2006-05-19 | 2007-11-29 | Codon Devices, Inc. | Methods for nucleic acid sorting and synthesis |
| US20090306126A1 (en) | 2006-05-22 | 2009-12-10 | Astrazeneca Ab | Indole Derivatives |
| MX2009002171A (es) | 2006-08-30 | 2009-05-28 | Cellzome Ltd | Derivados de triazol como inhibidores de cinasas. |
| JP2010502716A (ja) * | 2006-09-07 | 2010-01-28 | バイオジェン・アイデック・エムエイ・インコーポレイテッド | インターロイキン１受容体関連キナーゼの調節物質 |
| WO2008060578A2 (en) * | 2006-11-15 | 2008-05-22 | Cytovia, Inc. | 3-aryl-6-aryl-[1,2,4] triazolo[3,4-b][1,3,4] thiadiazoles and related compounds as activators of caspases and inducers of apoptosis and the use thereof |
| CN101037445A (zh) | 2007-04-14 | 2007-09-19 | 西北师范大学 | 一种具有潜在生物活性的咪唑并[2，1－b]－1，3，4－噻二唑衍生物及其合成方法 |
| US20100305113A1 (en) | 2007-05-09 | 2010-12-02 | Hans-Georg Capraro | Substituted Imidazopyridazines as Lipid Kinase Inhibitors |
| PE20090717A1 (es) | 2007-05-18 | 2009-07-18 | Smithkline Beecham Corp | Derivados de quinolina como inhibidores de la pi3 quinasa |
| CN101678014B (zh) * | 2007-05-21 | 2012-12-12 | Sgx药品公司 | 杂环激酶调节剂 |
| EP2180893B1 (en) * | 2007-08-09 | 2014-11-12 | Urifer Ltd | Pharmaceutical compositions and methods for the treatment of cancer |
| CN101878219B (zh) | 2007-09-27 | 2014-04-02 | 西班牙国家癌症研究中心 | 用于作为蛋白激酶抑制剂使用的咪唑并噻二唑类 |
| JP2011500823A (ja) | 2007-10-22 | 2011-01-06 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー | Ｐｉ３キナーゼ阻害物質としてのピリドスルホンアミド誘導体 |
| CA2732186A1 (en) | 2008-07-29 | 2010-02-04 | Merck Patent Gmbh | Imidazothiadiazole derivatives |
-
2010
- 2010-04-01 HU HUE10715318A patent/HUE027964T2/en unknown
- 2010-04-01 ES ES10715318.1T patent/ES2548571T3/es active Active
- 2010-04-01 CN CN201080015246.6A patent/CN102388055B/zh not_active Expired - Fee Related
- 2010-04-01 EP EP10715318.1A patent/EP2414369B1/en active Active
- 2010-04-01 SI SI201031054T patent/SI2414369T1/sl unknown
- 2010-04-01 BR BRPI1015367A patent/BRPI1015367B8/pt not_active IP Right Cessation
- 2010-04-01 NZ NZ595674A patent/NZ595674A/xx not_active IP Right Cessation
- 2010-04-01 KR KR1020117026103A patent/KR101727264B1/ko not_active Expired - Fee Related
- 2010-04-01 WO PCT/GB2010/000674 patent/WO2010112874A1/en not_active Ceased
- 2010-04-01 US US13/262,183 patent/US8815918B2/en active Active
- 2010-04-01 MX MX2011010372A patent/MX2011010372A/es active IP Right Grant
- 2010-04-01 EA EA201101435A patent/EA022753B1/ru not_active IP Right Cessation
- 2010-04-01 DK DK10715318.1T patent/DK2414369T3/en active
- 2010-04-01 SG SG2011071412A patent/SG175001A1/en unknown
- 2010-04-01 PL PL10715318T patent/PL2414369T3/pl unknown
- 2010-04-01 HR HRP20151126TT patent/HRP20151126T1/hr unknown
- 2010-04-01 PT PT107153181T patent/PT2414369E/pt unknown
- 2010-04-01 CA CA2756873A patent/CA2756873C/en active Active
- 2010-04-01 AU AU2010231162A patent/AU2010231162B2/en not_active Ceased
- 2010-04-01 JP JP2012502778A patent/JP5615902B2/ja not_active Expired - Fee Related
-
2011
- 2011-09-15 IL IL215158A patent/IL215158A/en active IP Right Grant
- 2011-10-07 ZA ZA2011/07350A patent/ZA201107350B/en unknown
-
2015
- 2015-11-03 CY CY20151100981T patent/CY1116880T1/el unknown