HRP20120160T1 - Supstituirani fenoksi n-alkilirani tiazoldindion kao modulatori estrogen srodnih alfa-receptora - Google Patents
Supstituirani fenoksi n-alkilirani tiazoldindion kao modulatori estrogen srodnih alfa-receptora Download PDFInfo
- Publication number
- HRP20120160T1 HRP20120160T1 HR20120160T HRP20120160T HRP20120160T1 HR P20120160 T1 HRP20120160 T1 HR P20120160T1 HR 20120160 T HR20120160 T HR 20120160T HR P20120160 T HRP20120160 T HR P20120160T HR P20120160 T1 HRP20120160 T1 HR P20120160T1
- Authority
- HR
- Croatia
- Prior art keywords
- phenoxy
- benzonitrile
- trifluoromethyl
- ethyl
- ylidenemethyl
- Prior art date
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- 102100036832 Steroid hormone receptor ERR1 Human genes 0.000 title claims 7
- 108091008559 estrogen-related receptor alpha Proteins 0.000 title 1
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 39
- 125000005843 halogen group Chemical group 0.000 claims abstract 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims abstract 5
- 125000000217 alkyl group Chemical group 0.000 claims abstract 4
- 125000003118 aryl group Chemical group 0.000 claims abstract 4
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims abstract 4
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims abstract 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims abstract 3
- 230000003287 optical effect Effects 0.000 claims abstract 3
- 150000003839 salts Chemical class 0.000 claims abstract 3
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 13
- 239000003795 chemical substances by application Substances 0.000 claims 7
- 208000035475 disorder Diseases 0.000 claims 7
- 101710205336 Steroid hormone receptor ERR1 Proteins 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 6
- 239000000825 pharmaceutical preparation Substances 0.000 claims 5
- 230000001404 mediated effect Effects 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- KSJUANLHNRPXBN-UHFFFAOYSA-N 4-[2-fluoro-4-[[3-(2-morpholin-4-ylethyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenoxy]-3-(trifluoromethyl)benzonitrile Chemical compound C=1C=C(OC=2C(=CC(=CC=2)C#N)C(F)(F)F)C(F)=CC=1C=C(C1=O)SC(=O)N1CCN1CCOCC1 KSJUANLHNRPXBN-UHFFFAOYSA-N 0.000 claims 2
- XLBKWGNFYDARLD-UHFFFAOYSA-N 4-[2-methoxy-4-[[3-(2-morpholin-4-ylethyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenoxy]-3-(trifluoromethyl)benzonitrile Chemical group C=1C=C(OC=2C(=CC(=CC=2)C#N)C(F)(F)F)C(OC)=CC=1C=C(C1=O)SC(=O)N1CCN1CCOCC1 XLBKWGNFYDARLD-UHFFFAOYSA-N 0.000 claims 2
- GZXPHSJMYNSXAR-UHFFFAOYSA-N 4-[2-methoxy-4-[[3-[2-(4-methylpiperazin-1-yl)ethyl]-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenoxy]-3-(trifluoromethyl)benzonitrile Chemical compound C=1C=C(OC=2C(=CC(=CC=2)C#N)C(F)(F)F)C(OC)=CC=1C=C(C1=O)SC(=O)N1CCN1CCN(C)CC1 GZXPHSJMYNSXAR-UHFFFAOYSA-N 0.000 claims 2
- NPUNYRATWGPIJY-UHFFFAOYSA-N 4-[4-[[2,4-dioxo-3-(2-piperidin-1-ylethyl)-1,3-thiazolidin-5-ylidene]methyl]-2-methoxyphenoxy]-3-(trifluoromethyl)benzonitrile Chemical compound C=1C=C(OC=2C(=CC(=CC=2)C#N)C(F)(F)F)C(OC)=CC=1C=C(C1=O)SC(=O)N1CCN1CCCCC1 NPUNYRATWGPIJY-UHFFFAOYSA-N 0.000 claims 2
- FSSNIIAXIOXWHQ-UHFFFAOYSA-N 4-[4-[[2,4-dioxo-3-(2-pyrazol-1-ylethyl)-1,3-thiazolidin-5-ylidene]methyl]-2-methoxyphenoxy]-3-(trifluoromethyl)benzonitrile Chemical compound C=1C=C(OC=2C(=CC(=CC=2)C#N)C(F)(F)F)C(OC)=CC=1C=C(C1=O)SC(=O)N1CCN1C=CC=N1 FSSNIIAXIOXWHQ-UHFFFAOYSA-N 0.000 claims 2
- LLFZCNABZILTOV-UHFFFAOYSA-N 4-[4-[[2,4-dioxo-3-(2-pyrrol-1-ylethyl)-1,3-thiazolidin-5-ylidene]methyl]-2-methoxyphenoxy]-3-(trifluoromethyl)benzonitrile Chemical compound C=1C=C(OC=2C(=CC(=CC=2)C#N)C(F)(F)F)C(OC)=CC=1C=C(C1=O)SC(=O)N1CCN1C=CC=C1 LLFZCNABZILTOV-UHFFFAOYSA-N 0.000 claims 2
- ARUVXYQPNZWEOM-UHFFFAOYSA-N 4-[4-[[2,4-dioxo-3-(2-pyrrolidin-1-ylethyl)-1,3-thiazolidin-5-ylidene]methyl]-2-fluorophenoxy]-3-(trifluoromethyl)benzonitrile Chemical compound C=1C=C(OC=2C(=CC(=CC=2)C#N)C(F)(F)F)C(F)=CC=1C=C(C1=O)SC(=O)N1CCN1CCCC1 ARUVXYQPNZWEOM-UHFFFAOYSA-N 0.000 claims 2
- RLKRQUKOVSDPPY-UHFFFAOYSA-N 4-[4-[[2,4-dioxo-3-(2-pyrrolidin-1-ylethyl)-1,3-thiazolidin-5-ylidene]methyl]-2-methoxyphenoxy]-3-(trifluoromethyl)benzonitrile Chemical compound C=1C=C(OC=2C(=CC(=CC=2)C#N)C(F)(F)F)C(OC)=CC=1C=C(C1=O)SC(=O)N1CCN1CCCC1 RLKRQUKOVSDPPY-UHFFFAOYSA-N 0.000 claims 2
- JQRBXJURGODTQK-UHFFFAOYSA-N 4-[4-[[3-(2-imidazol-1-ylethyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]-2-methoxyphenoxy]-3-(trifluoromethyl)benzonitrile Chemical compound C=1C=C(OC=2C(=CC(=CC=2)C#N)C(F)(F)F)C(OC)=CC=1C=C(C1=O)SC(=O)N1CCN1C=CN=C1 JQRBXJURGODTQK-UHFFFAOYSA-N 0.000 claims 2
- BABRIBMDAFGENJ-UHFFFAOYSA-N 4-[4-[[3-[2-(azepan-1-yl)ethyl]-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]-2-methoxyphenoxy]-3-(trifluoromethyl)benzonitrile Chemical compound C=1C=C(OC=2C(=CC(=CC=2)C#N)C(F)(F)F)C(OC)=CC=1C=C(C1=O)SC(=O)N1CCN1CCCCCC1 BABRIBMDAFGENJ-UHFFFAOYSA-N 0.000 claims 2
- XMFPEECIPIYBQW-UHFFFAOYSA-N 4-[4-[[3-[2-(diethylamino)ethyl]-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]-2-methoxyphenoxy]-3-(trifluoromethyl)benzonitrile Chemical compound O=C1N(CCN(CC)CC)C(=O)SC1=CC(C=C1OC)=CC=C1OC1=CC=C(C#N)C=C1C(F)(F)F XMFPEECIPIYBQW-UHFFFAOYSA-N 0.000 claims 2
- IPXOBBOQEHQQQX-UHFFFAOYSA-N 4-[4-[[3-[2-(dimethylamino)ethyl]-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]-2-fluorophenoxy]-3-(trifluoromethyl)benzonitrile Chemical compound O=C1N(CCN(C)C)C(=O)SC1=CC(C=C1F)=CC=C1OC1=CC=C(C#N)C=C1C(F)(F)F IPXOBBOQEHQQQX-UHFFFAOYSA-N 0.000 claims 2
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- CAKOHXXVOIJVTM-UHFFFAOYSA-N 4-[4-[[2,4-dioxo-3-[2-(1,2,4-triazol-1-yl)ethyl]-1,3-thiazolidin-5-ylidene]methyl]-2-methoxyphenoxy]-3-(trifluoromethyl)benzonitrile Chemical compound C=1C=C(OC=2C(=CC(=CC=2)C#N)C(F)(F)F)C(OC)=CC=1C=C(C1=O)SC(=O)N1CCN1C=NC=N1 CAKOHXXVOIJVTM-UHFFFAOYSA-N 0.000 claims 1
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- 229940124802 CB1 antagonist Drugs 0.000 claims 1
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- 208000005243 Chondrosarcoma Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 208000012514 Cumulative Trauma disease Diseases 0.000 claims 1
- 229940123900 Direct thrombin inhibitor Drugs 0.000 claims 1
- 102000030595 Glucokinase Human genes 0.000 claims 1
- 108010021582 Glucokinase Proteins 0.000 claims 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 1
- 206010018429 Glucose tolerance impaired Diseases 0.000 claims 1
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- 229940127470 Lipase Inhibitors Drugs 0.000 claims 1
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- 125000003545 alkoxy group Chemical group 0.000 claims 1
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- 150000002632 lipids Chemical class 0.000 claims 1
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- UNAANXDKBXWMLN-UHFFFAOYSA-N sibutramine Chemical compound C=1C=C(Cl)C=CC=1C1(C(N(C)C)CC(C)C)CCC1 UNAANXDKBXWMLN-UHFFFAOYSA-N 0.000 claims 1
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Classifications
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- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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US89345807P | 2007-03-07 | 2007-03-07 | |
PCT/US2008/056018 WO2008109731A2 (en) | 2007-03-07 | 2008-03-06 | Substituted phenoxy n-alkylated thiazoledinedione as estrogen related receptor-alpha modulators |
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HR20120160T HRP20120160T1 (hr) | 2007-03-07 | 2012-02-17 | Supstituirani fenoksi n-alkilirani tiazoldindion kao modulatori estrogen srodnih alfa-receptora |
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US (2) | US8119669B2 (pl) |
EP (1) | EP2132188B1 (pl) |
JP (1) | JP2010520307A (pl) |
KR (1) | KR20090118103A (pl) |
CN (1) | CN101679326B (pl) |
AR (1) | AR065656A1 (pl) |
AT (1) | ATE537157T1 (pl) |
AU (1) | AU2008222749A1 (pl) |
BR (1) | BRPI0808662B8 (pl) |
CA (1) | CA2679965A1 (pl) |
CL (1) | CL2008000669A1 (pl) |
CY (1) | CY1112778T1 (pl) |
DK (1) | DK2132188T3 (pl) |
EA (1) | EA200970838A1 (pl) |
ES (1) | ES2377165T3 (pl) |
HR (1) | HRP20120160T1 (pl) |
IL (1) | IL200758A0 (pl) |
MX (1) | MX2009009519A (pl) |
NZ (1) | NZ579418A (pl) |
PL (1) | PL2132188T3 (pl) |
PT (1) | PT2132188E (pl) |
RS (1) | RS52247B (pl) |
SI (1) | SI2132188T1 (pl) |
TW (1) | TW200902507A (pl) |
WO (1) | WO2008109731A2 (pl) |
ZA (1) | ZA200906953B (pl) |
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RU2012139463A (ru) * | 2010-02-17 | 2014-03-27 | Янссен Фармацевтика Нв | Аминотиазолоны как модуляторы активности белков, родственных рецептору эстрогена альфа |
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JP6014816B2 (ja) * | 2011-05-10 | 2016-10-26 | 国立大学法人神戸大学 | Ras機能阻害作用を有するチオキソチアゾリジン誘導体 |
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KR102199273B1 (ko) | 2012-03-26 | 2021-01-06 | 닛뽕 케미파 가부시키가이샤 | 뼈 및 연부에 발생하는 거대 세포성 종양 또는 연골 육종의 예방 및 치료제 |
EP2909333A1 (en) * | 2012-10-17 | 2015-08-26 | Institut National de la Santé et de la Recherche Médicale (INSERM) | Methods for predicting and treating bone metastases in prostate cancer patients |
JO3368B1 (ar) | 2013-06-04 | 2019-03-13 | Janssen Pharmaceutica Nv | مركبات 6، 7- ثاني هيدرو بيرازولو [5،1-a] بيرازين- 4 (5 يد)- اون واستخدامها بصفة منظمات تفارغية سلبية لمستقبلات ميجلور 2 |
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JP6527822B2 (ja) | 2013-09-25 | 2019-06-05 | 日本ケミファ株式会社 | 骨・軟部に発生する巨細胞性腫瘍、軟骨肉腫または骨肉腫の予防、治療または転移の予防のための薬剤、動脈塞栓術用局所注入剤、および、人工骨 |
UA121965C2 (uk) | 2014-01-21 | 2020-08-25 | Янссен Фармацевтика Нв | Комбінації, які містять позитивні алостеричні модулятори або ортостеричні агоністи метаботропного глутаматергічного рецептора 2 підтипу, та їх застосування |
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EP1398029A1 (en) | 2002-09-10 | 2004-03-17 | LION Bioscience AG | NR3B1 nuclear receptor binding 3-substituted pyrazole derivatives |
US20080313061A1 (en) | 2004-06-30 | 2008-12-18 | Paysetter Pte Ltd | System and Method for Facilitating Transfer of Physical Money and/or Credit |
WO2006019741A1 (en) * | 2004-07-14 | 2006-02-23 | Janssen Pharmaceutica N.V. | Arylidenes for the treatment of estrogen related receptor-alpha mediated diseases |
US7977489B2 (en) | 2004-10-22 | 2011-07-12 | Exelixis, Inc. | Benzylthiazolone inhibitors of estrogen-related receptors (ERR) |
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2008
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- 2008-03-06 CA CA002679965A patent/CA2679965A1/en not_active Abandoned
- 2008-03-06 AU AU2008222749A patent/AU2008222749A1/en not_active Abandoned
- 2008-03-06 EA EA200970838A patent/EA200970838A1/ru unknown
- 2008-03-06 EP EP08731517A patent/EP2132188B1/en active Active
- 2008-03-06 JP JP2009552883A patent/JP2010520307A/ja active Pending
- 2008-03-06 DK DK08731517.2T patent/DK2132188T3/da active
- 2008-03-06 CL CL2008000669A patent/CL2008000669A1/es unknown
- 2008-03-06 PT PT08731517T patent/PT2132188E/pt unknown
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- 2008-03-06 ES ES08731517T patent/ES2377165T3/es active Active
- 2008-03-06 SI SI200830561T patent/SI2132188T1/sl unknown
- 2008-03-06 AT AT08731517T patent/ATE537157T1/de active
- 2008-03-06 BR BRPI0808662A patent/BRPI0808662B8/pt not_active IP Right Cessation
- 2008-03-06 PL PL08731517T patent/PL2132188T3/pl unknown
- 2008-03-06 CN CN2008800153616A patent/CN101679326B/zh not_active Expired - Fee Related
- 2008-03-06 NZ NZ579418A patent/NZ579418A/en not_active IP Right Cessation
- 2008-03-06 TW TW097107936A patent/TW200902507A/zh unknown
- 2008-03-06 US US12/043,291 patent/US8119669B2/en not_active Expired - Fee Related
- 2008-03-06 KR KR1020097020832A patent/KR20090118103A/ko not_active Application Discontinuation
- 2008-03-06 RS RS20120106A patent/RS52247B/en unknown
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2009
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- 2009-10-06 ZA ZA2009/06953A patent/ZA200906953B/en unknown
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2012
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Also Published As
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EP2132188A2 (en) | 2009-12-16 |
ATE537157T1 (de) | 2011-12-15 |
ZA200906953B (en) | 2010-12-29 |
CN101679326B (zh) | 2012-12-12 |
JP2010520307A (ja) | 2010-06-10 |
MX2009009519A (es) | 2009-11-18 |
PL2132188T3 (pl) | 2012-05-31 |
US8119669B2 (en) | 2012-02-21 |
CA2679965A1 (en) | 2008-09-12 |
SI2132188T1 (sl) | 2012-04-30 |
CL2008000669A1 (es) | 2008-11-03 |
EA200970838A1 (ru) | 2010-02-26 |
BRPI0808662B8 (pt) | 2021-05-25 |
KR20090118103A (ko) | 2009-11-17 |
BRPI0808662B1 (pt) | 2020-09-29 |
WO2008109731A3 (en) | 2008-11-27 |
AR065656A1 (es) | 2009-06-24 |
EP2132188B1 (en) | 2011-12-14 |
US9034852B2 (en) | 2015-05-19 |
CN101679326A (zh) | 2010-03-24 |
IL200758A0 (en) | 2010-05-17 |
AU2008222749A1 (en) | 2008-09-12 |
ES2377165T3 (es) | 2012-03-23 |
US20120108571A1 (en) | 2012-05-03 |
PT2132188E (pt) | 2012-02-13 |
CY1112778T1 (el) | 2016-02-10 |
NZ579418A (en) | 2012-01-12 |
DK2132188T3 (da) | 2012-02-27 |
TW200902507A (en) | 2009-01-16 |
WO2008109731A2 (en) | 2008-09-12 |
US20080286265A1 (en) | 2008-11-20 |
BRPI0808662A2 (pt) | 2014-08-26 |
RS52247B (en) | 2012-10-31 |
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