JP2004509941A5 - - Google Patents
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- JP2004509941A5 JP2004509941A5 JP2002531082A JP2002531082A JP2004509941A5 JP 2004509941 A5 JP2004509941 A5 JP 2004509941A5 JP 2002531082 A JP2002531082 A JP 2002531082A JP 2002531082 A JP2002531082 A JP 2002531082A JP 2004509941 A5 JP2004509941 A5 JP 2004509941A5
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- Prior art keywords
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- leader group
- alkylene
- acid leader
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- 150000001875 compounds Chemical class 0.000 description 101
- -1 chloro, bromo, iodo, methyl Chemical group 0.000 description 59
- 239000002253 acid Substances 0.000 description 37
- 125000002947 alkylene group Chemical group 0.000 description 31
- 125000003118 aryl group Chemical group 0.000 description 26
- 125000004432 carbon atom Chemical group C* 0.000 description 19
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 17
- 125000001153 fluoro group Chemical group F* 0.000 description 16
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 16
- 150000001408 amides Chemical group 0.000 description 15
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 15
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 15
- 125000000732 arylene group Chemical group 0.000 description 11
- 238000000034 method Methods 0.000 description 11
- 239000000203 mixture Substances 0.000 description 11
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 11
- 150000002148 esters Chemical class 0.000 description 9
- 150000002170 ethers Chemical class 0.000 description 9
- 150000003839 salts Chemical class 0.000 description 9
- 239000012453 solvate Substances 0.000 description 9
- MHJROHFILMZTFC-UHFFFAOYSA-N CCN(CC)NN1CCOC(C1)(N)N(C)C Chemical compound CCN(CC)NN1CCOC(C1)(N)N(C)C MHJROHFILMZTFC-UHFFFAOYSA-N 0.000 description 8
- 125000004093 cyano group Chemical group *C#N 0.000 description 8
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 8
- 241001465754 Metazoa Species 0.000 description 5
- 229920006395 saturated elastomer Polymers 0.000 description 4
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 description 3
- 125000001931 aliphatic group Chemical group 0.000 description 3
- 125000000217 alkyl group Chemical group 0.000 description 3
- 239000011203 carbon fibre reinforced carbon Substances 0.000 description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
- 229910052739 hydrogen Inorganic materials 0.000 description 3
- 239000001257 hydrogen Substances 0.000 description 3
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 description 3
- JWZZKOKVBUJMES-UHFFFAOYSA-N (+-)-Isoprenaline Chemical group CC(C)NCC(O)C1=CC=C(O)C(O)=C1 JWZZKOKVBUJMES-UHFFFAOYSA-N 0.000 description 2
- FCEHBMOGCRZNNI-UHFFFAOYSA-N 1-benzothiophene Chemical compound C1=CC=C2SC=CC2=C1 FCEHBMOGCRZNNI-UHFFFAOYSA-N 0.000 description 2
- UJOBWOGCFQCDNV-UHFFFAOYSA-N 9H-carbazole Chemical compound C1=CC=C2C3=CC=CC=C3NC2=C1 UJOBWOGCFQCDNV-UHFFFAOYSA-N 0.000 description 2
- YLQBMQCUIZJEEH-UHFFFAOYSA-N Furan Chemical compound C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 2
- 102000003964 Histone deacetylase Human genes 0.000 description 2
- 108090000353 Histone deacetylase Proteins 0.000 description 2
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical compound C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 description 2
- UFWIBTONFRDIAS-UHFFFAOYSA-N Naphthalene Chemical compound C1=CC=CC2=CC=CC=C21 UFWIBTONFRDIAS-UHFFFAOYSA-N 0.000 description 2
- 206010028980 Neoplasm Diseases 0.000 description 2
- 201000004681 Psoriasis Diseases 0.000 description 2
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 description 2
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 description 2
- SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical compound N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 description 2
- DZBUGLKDJFMEHC-UHFFFAOYSA-N acridine Chemical compound C1=CC=CC2=CC3=CC=CC=C3N=C21 DZBUGLKDJFMEHC-UHFFFAOYSA-N 0.000 description 2
- 125000002723 alicyclic group Chemical group 0.000 description 2
- 201000011510 cancer Diseases 0.000 description 2
- 208000035475 disorder Diseases 0.000 description 2
- NIHNNTQXNPWCJQ-UHFFFAOYSA-N fluorene Chemical compound C1=CC=C2CC3=CC=CC=C3C2=C1 NIHNNTQXNPWCJQ-UHFFFAOYSA-N 0.000 description 2
- 125000004435 hydrogen atom Chemical class [H]* 0.000 description 2
- 230000002519 immonomodulatory effect Effects 0.000 description 2
- 208000027866 inflammatory disease Diseases 0.000 description 2
- 206010025135 lupus erythematosus Diseases 0.000 description 2
- 230000002062 proliferating effect Effects 0.000 description 2
- 206010039073 rheumatoid arthritis Diseases 0.000 description 2
- HYZJCKYKOHLVJF-UHFFFAOYSA-N 1H-benzimidazole Chemical compound C1=CC=C2NC=NC2=C1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 description 1
- 208000024827 Alzheimer disease Diseases 0.000 description 1
- 201000001320 Atherosclerosis Diseases 0.000 description 1
- 208000035143 Bacterial infection Diseases 0.000 description 1
- 206010008025 Cerebellar ataxia Diseases 0.000 description 1
- 206010012438 Dermatitis atopic Diseases 0.000 description 1
- 206010012689 Diabetic retinopathy Diseases 0.000 description 1
- 206010017533 Fungal infection Diseases 0.000 description 1
- 208000015336 Helminthic disease Diseases 0.000 description 1
- 208000023105 Huntington disease Diseases 0.000 description 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 1
- 206010020751 Hypersensitivity Diseases 0.000 description 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 description 1
- 208000031888 Mycoses Diseases 0.000 description 1
- ABDMQSFNJPYOLA-UHFFFAOYSA-N NS(=O)(=O)[N+]([O-])=O Chemical compound NS(=O)(=O)[N+]([O-])=O ABDMQSFNJPYOLA-UHFFFAOYSA-N 0.000 description 1
- 208000030852 Parasitic disease Diseases 0.000 description 1
- 208000018737 Parkinson disease Diseases 0.000 description 1
- 206010039085 Rhinitis allergic Diseases 0.000 description 1
- 208000010112 Spinocerebellar Degenerations Diseases 0.000 description 1
- 208000002903 Thalassemia Diseases 0.000 description 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 description 1
- 208000036142 Viral infection Diseases 0.000 description 1
- 125000002252 acyl group Chemical group 0.000 description 1
- 208000026935 allergic disease Diseases 0.000 description 1
- 201000010105 allergic rhinitis Diseases 0.000 description 1
- 230000007815 allergy Effects 0.000 description 1
- 208000007502 anemia Diseases 0.000 description 1
- 230000033115 angiogenesis Effects 0.000 description 1
- 208000006673 asthma Diseases 0.000 description 1
- 201000008937 atopic dermatitis Diseases 0.000 description 1
- 208000022362 bacterial infectious disease Diseases 0.000 description 1
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 description 1
- 125000005488 carboaryl group Chemical group 0.000 description 1
- CREMABGTGYGIQB-UHFFFAOYSA-N carbon carbon Chemical compound C.C CREMABGTGYGIQB-UHFFFAOYSA-N 0.000 description 1
- 208000019425 cirrhosis of liver Diseases 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 230000000893 fibroproliferative effect Effects 0.000 description 1
- 125000002541 furyl group Chemical group 0.000 description 1
- 125000005843 halogen group Chemical group 0.000 description 1
- 208000018706 hematopoietic system disease Diseases 0.000 description 1
- 125000001072 heteroaryl group Chemical group 0.000 description 1
- 125000000623 heterocyclic group Chemical group 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 description 1
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 description 1
- 125000001041 indolyl group Chemical group 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 201000010901 lateral sclerosis Diseases 0.000 description 1
- 201000004792 malaria Diseases 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 1
- 208000005264 motor neuron disease Diseases 0.000 description 1
- 201000006417 multiple sclerosis Diseases 0.000 description 1
- 125000001624 naphthyl group Chemical group 0.000 description 1
- 230000004770 neurodegeneration Effects 0.000 description 1
- 208000015122 neurodegenerative disease Diseases 0.000 description 1
- 201000008482 osteoarthritis Diseases 0.000 description 1
- 230000036281 parasite infection Effects 0.000 description 1
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 description 1
- 208000028172 protozoa infectious disease Diseases 0.000 description 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 1
- 208000037803 restenosis Diseases 0.000 description 1
- 208000007056 sickle cell anemia Diseases 0.000 description 1
- 210000002460 smooth muscle Anatomy 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 125000001544 thienyl group Chemical group 0.000 description 1
- JSPLKZUTYZBBKA-UHFFFAOYSA-N trioxidane Chemical group OOO JSPLKZUTYZBBKA-UHFFFAOYSA-N 0.000 description 1
- 201000002311 trypanosomiasis Diseases 0.000 description 1
- 230000009385 viral infection Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0023985A GB0023985D0 (en) | 2000-09-29 | 2000-09-29 | Therapeutic compounds |
| US29778501P | 2001-06-14 | 2001-06-14 | |
| PCT/GB2001/004329 WO2002026696A1 (en) | 2000-09-29 | 2001-09-27 | Carbamic acid compounds comprising an amide linkage as hdac inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2004509941A JP2004509941A (ja) | 2004-04-02 |
| JP2004509941A5 true JP2004509941A5 (https=) | 2008-10-23 |
Family
ID=26245083
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002531082A Pending JP2004509941A (ja) | 2000-09-29 | 2001-09-27 | Hdacインヒビターとしてのアミド結合を含むカルバミン酸化合物 |
Country Status (10)
| Country | Link |
|---|---|
| US (3) | US7569724B2 (https=) |
| EP (3) | EP1335898B1 (https=) |
| JP (1) | JP2004509941A (https=) |
| AT (2) | ATE310719T1 (https=) |
| AU (1) | AU2001290134A1 (https=) |
| CA (1) | CA2423868C (https=) |
| DE (2) | DE60115279T2 (https=) |
| DK (1) | DK1335898T3 (https=) |
| ES (1) | ES2257441T3 (https=) |
| WO (1) | WO2002026696A1 (https=) |
Families Citing this family (154)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6777217B1 (en) | 1996-03-26 | 2004-08-17 | President And Fellows Of Harvard College | Histone deacetylases, and uses related thereto |
| FR2758459B1 (fr) * | 1997-01-17 | 1999-05-07 | Pharma Pass | Composition pharmaceutique de fenofibrate presentant une biodisponibilite elevee et son procede de preparation |
| US20030129724A1 (en) | 2000-03-03 | 2003-07-10 | Grozinger Christina M. | Class II human histone deacetylases, and uses related thereto |
| US7244853B2 (en) | 2001-05-09 | 2007-07-17 | President And Fellows Of Harvard College | Dioxanes and uses thereof |
| US6706686B2 (en) | 2001-09-27 | 2004-03-16 | The Regents Of The University Of Colorado | Inhibition of histone deacetylase as a treatment for cardiac hypertrophy |
| EP1443928B1 (en) | 2001-10-16 | 2011-07-27 | Sloan-Kettering Institute For Cancer Research | Treatment of neurodegenerative diseases and cancer of the brain |
| WO2003048114A2 (en) * | 2001-12-04 | 2003-06-12 | De Novo Pharmaceuticals Limited | Bacterial enzyme inhibitors |
| CA2479906C (en) | 2002-04-03 | 2011-02-08 | Topotarget Uk Limited | Carbamic acid compounds comprising a piperazine linkage as hdac inhibitors |
| PL374970A1 (en) * | 2002-08-02 | 2005-11-14 | Argenta Discovery Limited | Substituted thienyl-hydroxamic acids as histone deacetylase inhibitors |
| US7154002B1 (en) | 2002-10-08 | 2006-12-26 | Takeda San Diego, Inc. | Histone deacetylase inhibitors |
| US7250514B1 (en) | 2002-10-21 | 2007-07-31 | Takeda San Diego, Inc. | Histone deacetylase inhibitors |
| US7465719B2 (en) | 2003-01-17 | 2008-12-16 | Topotarget Uk Limited | Carbamic acid compounds comprising an ester or ketone linkage as HDAC inhibitors |
| AU2003900608A0 (en) * | 2003-02-11 | 2003-02-27 | Fujisawa Pharmaceutical Co., Ltd. | Hdac inhibitor |
| US7244751B2 (en) | 2003-02-14 | 2007-07-17 | Shenzhen Chipscreen Biosciences Ltd. | Histone deacetylase inhibitors of novel benzamide derivatives with potent differentiation and anti-proliferation activity |
| US7652036B2 (en) | 2003-02-25 | 2010-01-26 | Topotarget Uk Limited | Carbamic acid compounds comprising a bicyclic heteroaryl group as HDAC inhibitors |
| CA2518318A1 (en) | 2003-03-17 | 2004-09-30 | Takeda San Diego, Inc. | Histone deacetylase inhibitors |
| US7842835B2 (en) | 2003-07-07 | 2010-11-30 | Georgetown University | Histone deacetylase inhibitors and methods of use thereof |
| EP1644323B1 (en) * | 2003-07-07 | 2015-03-18 | Georgetown University | Histone deacetylase inhibitors and methods of use thereof |
| JP4799408B2 (ja) * | 2003-07-15 | 2011-10-26 | コリア リサーチ インスティテュート オブ バイオサイエンス アンド バイオテクノロジー | 新規な2−オキソ複素環化合物およびそれを含有する薬剤組成物の使用 |
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| DK1696898T3 (en) * | 2003-12-02 | 2016-02-22 | Univ Ohio State Res Found | ZN2 + -CHELATING DESIGN-BASED SHORT-CHAIN FAT ACIDS AS AN UNKNOWN CLASS OF HISTONDEACETYLASE INHIBITORS |
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| KR100620488B1 (ko) | 2004-08-13 | 2006-09-08 | 연세대학교 산학협력단 | 신규한 히스톤 디아세틸라아제 억제제 및 이의 제조방법 |
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| US20090005344A1 (en) * | 2004-11-01 | 2009-01-01 | Nkuada, Llc | Compounds and Methods of Use Thereof |
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| CN101495116A (zh) | 2005-03-22 | 2009-07-29 | 哈佛大学校长及研究员协会 | 蛋白降解病症的治疗 |
| US8580752B2 (en) * | 2005-03-31 | 2013-11-12 | Council Of Scientitic And Industrial Research | Aromatic amides as potentiators of bioefficacy of anti-infective drugs |
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| JP5377968B2 (ja) * | 2005-11-10 | 2013-12-25 | トポターゲット ユーケー リミテッド | 癌治療のために単独で用いるまたは化学療法薬と併用するヒストンデアセチラーゼ(hdac)阻害剤 |
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- 2001-09-27 DK DK01970014T patent/DK1335898T3/da active
- 2001-09-27 AT AT01970014T patent/ATE310719T1/de active
- 2001-09-27 ES ES01970014T patent/ES2257441T3/es not_active Expired - Lifetime
- 2001-09-27 AT AT05015737T patent/ATE430567T1/de not_active IP Right Cessation
- 2001-09-27 AU AU2001290134A patent/AU2001290134A1/en not_active Abandoned
- 2001-09-27 DE DE60115279T patent/DE60115279T2/de not_active Expired - Lifetime
- 2001-09-27 US US10/381,791 patent/US7569724B2/en not_active Expired - Fee Related
- 2001-09-27 WO PCT/GB2001/004329 patent/WO2002026696A1/en not_active Ceased
- 2001-09-27 CA CA2423868A patent/CA2423868C/en not_active Expired - Fee Related
- 2001-09-27 EP EP09004388A patent/EP2083005A1/en not_active Withdrawn
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2009
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