JP2009541260A5 - - Google Patents
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- Publication number
- JP2009541260A5 JP2009541260A5 JP2009515860A JP2009515860A JP2009541260A5 JP 2009541260 A5 JP2009541260 A5 JP 2009541260A5 JP 2009515860 A JP2009515860 A JP 2009515860A JP 2009515860 A JP2009515860 A JP 2009515860A JP 2009541260 A5 JP2009541260 A5 JP 2009541260A5
- Authority
- JP
- Japan
- Prior art keywords
- phenyl
- piperazin
- propenone
- benzyl
- chloro
- 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
- -1 2,6-difluoro-phenyl Chemical group 0.000 claims 28
- 150000001875 compounds Chemical class 0.000 claims 23
- 125000004182 2-chlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(*)C([H])=C1[H] 0.000 claims 14
- 239000008194 pharmaceutical composition Substances 0.000 claims 8
- 230000001225 therapeutic effect Effects 0.000 claims 8
- 229910052736 halogen Inorganic materials 0.000 claims 7
- 150000002367 halogens Chemical class 0.000 claims 7
- 238000011321 prophylaxis Methods 0.000 claims 7
- 125000004176 4-fluorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1F)C([H])([H])* 0.000 claims 5
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 239000001257 hydrogen Substances 0.000 claims 5
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 125000004847 2-fluorobenzyl group Chemical group [H]C1=C([H])C(F)=C(C([H])=C1[H])C([H])([H])* 0.000 claims 3
- 125000006509 3,4-difluorobenzyl group Chemical group [H]C1=C(F)C(F)=C([H])C(=C1[H])C([H])([H])* 0.000 claims 3
- 125000006180 3-methyl benzyl group Chemical group [H]C1=C([H])C(=C([H])C(=C1[H])C([H])([H])[H])C([H])([H])* 0.000 claims 3
- 125000006283 4-chlorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1Cl)C([H])([H])* 0.000 claims 3
- 125000006181 4-methyl benzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1C([H])([H])[H])C([H])([H])* 0.000 claims 3
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 125000004198 2-fluorophenyl group Chemical group [H]C1=C([H])C(F)=C(*)C([H])=C1[H] 0.000 claims 2
- 125000006179 2-methyl benzyl group Chemical group [H]C1=C([H])C(=C(C([H])=C1[H])C([H])([H])*)C([H])([H])[H] 0.000 claims 2
- 125000003852 3-chlorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C(Cl)=C1[H])C([H])([H])* 0.000 claims 2
- 206010003658 Atrial Fibrillation Diseases 0.000 claims 2
- 101000783577 Dendroaspis angusticeps Thrombostatin Proteins 0.000 claims 2
- 101000783578 Dendroaspis jamesoni kaimosae Dendroaspin Proteins 0.000 claims 2
- 108010070519 PAR-1 Receptor Proteins 0.000 claims 2
- 102100037136 Proteinase-activated receptor 1 Human genes 0.000 claims 2
- 150000001412 amines Chemical class 0.000 claims 2
- 229940127218 antiplatelet drug Drugs 0.000 claims 2
- 239000002327 cardiovascular agent Substances 0.000 claims 2
- 229940125692 cardiovascular agent Drugs 0.000 claims 2
- 229910052801 chlorine Inorganic materials 0.000 claims 2
- 239000000460 chlorine Substances 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 239000000106 platelet aggregation inhibitor Substances 0.000 claims 2
- 239000000047 product Substances 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 210000000329 smooth muscle myocyte Anatomy 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- BLYXTWCMEQUPJI-UHFFFAOYSA-N 2-[3-[4-(cyclohexylmethyl)piperazin-1-yl]-3-oxoprop-1-enyl]benzonitrile Chemical compound C1CN(CC2CCCCC2)CCN1C(=O)C=CC1=CC=CC=C1C#N BLYXTWCMEQUPJI-UHFFFAOYSA-N 0.000 claims 1
- 125000006276 2-bromophenyl group Chemical group [H]C1=C([H])C(Br)=C(*)C([H])=C1[H] 0.000 claims 1
- 125000006282 2-chlorobenzyl group Chemical group [H]C1=C([H])C(Cl)=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000006185 3,4-dimethyl benzyl group Chemical group [H]C1=C(C([H])=C(C(=C1[H])C([H])([H])[H])C([H])([H])[H])C([H])([H])* 0.000 claims 1
- 125000006284 3-fluorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C(F)=C1[H])C([H])([H])* 0.000 claims 1
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 1
- 208000004476 Acute Coronary Syndrome Diseases 0.000 claims 1
- 206010003178 Arterial thrombosis Diseases 0.000 claims 1
- BSYNRYMUTXBXSQ-UHFFFAOYSA-N Aspirin Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 claims 1
- 208000032845 Atrial Remodeling Diseases 0.000 claims 1
- 239000005552 B01AC04 - Clopidogrel Substances 0.000 claims 1
- 239000005528 B01AC05 - Ticlopidine Substances 0.000 claims 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
- 108010056764 Eptifibatide Proteins 0.000 claims 1
- 206010016654 Fibrosis Diseases 0.000 claims 1
- 208000018522 Gastrointestinal disease Diseases 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 208000019693 Lung disease Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 229940098892 Protease-activated receptor-1 antagonist Drugs 0.000 claims 1
- 208000007718 Stable Angina Diseases 0.000 claims 1
- 206010047249 Venous thrombosis Diseases 0.000 claims 1
- 229960000446 abciximab Drugs 0.000 claims 1
- 229960001138 acetylsalicylic acid Drugs 0.000 claims 1
- 230000004913 activation Effects 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 229910052794 bromium Inorganic materials 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 210000001054 cardiac fibroblast Anatomy 0.000 claims 1
- 210000004027 cell Anatomy 0.000 claims 1
- 230000004663 cell proliferation Effects 0.000 claims 1
- 208000026106 cerebrovascular disease Diseases 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 239000003153 chemical reaction reagent Substances 0.000 claims 1
- GKTWGGQPFAXNFI-HNNXBMFYSA-N clopidogrel Chemical compound C1([C@H](N2CC=3C=CSC=3CC2)C(=O)OC)=CC=CC=C1Cl GKTWGGQPFAXNFI-HNNXBMFYSA-N 0.000 claims 1
- 229960003009 clopidogrel Drugs 0.000 claims 1
- 239000013066 combination product Substances 0.000 claims 1
- 229940127555 combination product Drugs 0.000 claims 1
- 238000010511 deprotection reaction Methods 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 230000002526 effect on cardiovascular system Effects 0.000 claims 1
- 210000002889 endothelial cell Anatomy 0.000 claims 1
- 229960004468 eptifibatide Drugs 0.000 claims 1
- GLGOPUHVAZCPRB-LROMGURASA-N eptifibatide Chemical compound N1C(=O)[C@H](CC(O)=O)NC(=O)CNC(=O)[C@H](CCCCNC(=N)N)NC(=O)CCSSC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]1CC1=CN=C2[C]1C=CC=C2 GLGOPUHVAZCPRB-LROMGURASA-N 0.000 claims 1
- 210000002950 fibroblast Anatomy 0.000 claims 1
- 230000004761 fibrosis Effects 0.000 claims 1
- 125000002485 formyl group Chemical class [H]C(*)=O 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 229910052740 iodine Inorganic materials 0.000 claims 1
- 208000019423 liver disease Diseases 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 210000004498 neuroglial cell Anatomy 0.000 claims 1
- 230000035755 proliferation Effects 0.000 claims 1
- 230000000069 prophylactic effect Effects 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 208000017520 skin disease Diseases 0.000 claims 1
- 238000013268 sustained release Methods 0.000 claims 1
- 239000012730 sustained-release form Substances 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 239000003856 thrombin receptor antagonist Substances 0.000 claims 1
- PHWBOXQYWZNQIN-UHFFFAOYSA-N ticlopidine Chemical compound ClC1=CC=CC=C1CN1CC(C=CS2)=C2CC1 PHWBOXQYWZNQIN-UHFFFAOYSA-N 0.000 claims 1
- 229960005001 ticlopidine Drugs 0.000 claims 1
- 229960003425 tirofiban Drugs 0.000 claims 1
- COKMIXFXJJXBQG-NRFANRHFSA-N tirofiban Chemical compound C1=CC(C[C@H](NS(=O)(=O)CCCC)C(O)=O)=CC=C1OCCCCC1CCNCC1 COKMIXFXJJXBQG-NRFANRHFSA-N 0.000 claims 1
- 238000011282 treatment Methods 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR0605419A FR2902426B1 (fr) | 2006-06-19 | 2006-06-19 | Derives de cinnamoyl-piperazine |
| FR0605419 | 2006-06-19 | ||
| PCT/EP2007/056086 WO2007147824A1 (en) | 2006-06-19 | 2007-06-19 | Cinnamoyl-piperazine derivatives and their use as par- i antagonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2009541260A JP2009541260A (ja) | 2009-11-26 |
| JP2009541260A5 true JP2009541260A5 (enExample) | 2010-07-22 |
| JP5356222B2 JP5356222B2 (ja) | 2013-12-04 |
Family
ID=37846050
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009515860A Expired - Fee Related JP5356222B2 (ja) | 2006-06-19 | 2007-06-19 | シンナモイル−ピペラジン誘導体およびｐａｒ−１拮抗薬としてのそれらの使用 |
Country Status (31)
| Country | Link |
|---|---|
| US (2) | US8217046B2 (enExample) |
| EP (1) | EP2041104B1 (enExample) |
| JP (1) | JP5356222B2 (enExample) |
| KR (1) | KR101468752B1 (enExample) |
| CN (1) | CN101472907B (enExample) |
| AR (1) | AR061520A1 (enExample) |
| AT (1) | ATE478059T1 (enExample) |
| AU (1) | AU2007263051B2 (enExample) |
| BR (1) | BRPI0713132B8 (enExample) |
| CA (1) | CA2655527C (enExample) |
| CR (1) | CR10509A (enExample) |
| DE (1) | DE602007008572D1 (enExample) |
| EC (1) | ECSP099065A (enExample) |
| ES (1) | ES2349324T3 (enExample) |
| FR (1) | FR2902426B1 (enExample) |
| GE (1) | GEP20115201B (enExample) |
| IL (1) | IL195972A (enExample) |
| MA (1) | MA30756B1 (enExample) |
| MX (1) | MX2008016447A (enExample) |
| MY (1) | MY144461A (enExample) |
| NO (1) | NO341389B1 (enExample) |
| NZ (1) | NZ573764A (enExample) |
| PL (1) | PL2041104T3 (enExample) |
| PT (1) | PT2041104E (enExample) |
| RU (1) | RU2440997C2 (enExample) |
| SA (1) | SA07280330B1 (enExample) |
| TN (1) | TNSN08522A1 (enExample) |
| TW (1) | TWI404710B (enExample) |
| UA (1) | UA96947C2 (enExample) |
| WO (1) | WO2007147824A1 (enExample) |
| ZA (1) | ZA200900303B (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR3014693B1 (fr) | 2013-12-16 | 2016-01-08 | Pf Medicament | Utilisation de la 3-(2-chloro-phenyl)-1-[4-(4-fluoro-benzyl)-piperazin-1-yl]-propenone pour la prevention et/ou le traitement des pathologies fonctionnelles pelvi-perineales |
| EP3143036B1 (en) | 2014-05-11 | 2023-08-02 | Tel Hashomer Medical Research Infrastructure and Services Ltd. | Par-1 based therapeutic conjugates and uses thereof |
| WO2016066789A1 (fr) * | 2014-10-31 | 2016-05-06 | Pierre Fabre Medicament | Utilisation d'antagonistes par-1 pour la prevention et/ou le traitement des pathologies fonctionnelles pelvi-perineales |
| CN104496922B (zh) * | 2015-01-13 | 2016-04-06 | 佛山市赛维斯医药科技有限公司 | 腈基苯二烯四氮唑类化合物、其制备方法和用途 |
| CN104496924B (zh) * | 2015-01-13 | 2016-04-13 | 佛山市赛维斯医药科技有限公司 | 卤苯二烯四氮唑类化合物、其制备方法和用途 |
| CN104529860B (zh) * | 2015-01-13 | 2016-06-01 | 佛山市赛维斯医药科技有限公司 | 一种含硝基苯和二烯氟代金刚烷结构的化合物及制备方法 |
| CN104496879A (zh) * | 2015-01-13 | 2015-04-08 | 佛山市赛维斯医药科技有限公司 | 一种含腈基苯和二烯氟代金刚烷结构的化合物和用途 |
| CN105949116A (zh) * | 2016-06-08 | 2016-09-21 | 青岛理工大学 | 酰基哌嗪类化合物及其制备方法和用途 |
| EP3278802A1 (en) | 2016-08-04 | 2018-02-07 | Metabolys | New treatment for the non alcoholic steatohepatitis and fibrosis |
| RU2662308C1 (ru) * | 2017-12-25 | 2018-07-25 | Феркат Адельзянович Халиуллин | Средство для лечения и профилактики тромбоза |
| IL278311B2 (en) | 2018-05-02 | 2024-02-01 | Tel Hashomer Medical Res Infrastructure & Services Ltd | Preparations and methods for the treatment of glioblastoma |
| FR3090317B1 (fr) | 2018-12-19 | 2021-05-07 | Cvasthera | Utilisation d’un antagoniste de par-1 pour le traitement d’une maladie inflammatoire chronique intestinale |
| KR102791326B1 (ko) * | 2021-09-29 | 2025-04-04 | 주성수 | 피페론구민계 화합물을 유효성분으로 포함하는 혈관질환 예방 또는 치료용 약학적 조성물 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS61106564A (ja) * | 1984-10-30 | 1986-05-24 | Terumo Corp | 不飽和脂肪酸アミド誘導体およびこれを含有する血小板凝集抑制剤 |
| JPS6219577A (ja) * | 1985-07-16 | 1987-01-28 | Kanebo Ltd | 新規なベンジルピペラジン誘導体および該化合物を有効成分とする医薬組成物 |
| SE9201956D0 (sv) * | 1992-06-25 | 1992-06-25 | Kabi Pharmacia Ab | Novel nicotinicacid esters |
| US6207665B1 (en) * | 1997-06-12 | 2001-03-27 | Schering Aktiengesellschaft | Piperazine derivatives and their use as anti-inflammatory agents |
| WO2002076965A1 (en) * | 2001-03-23 | 2002-10-03 | John Matsoukas | Non peptide mimetics based on the active sequence s42fllr46 of the thrombin receptor for the treatment of thrombosis and cancer |
| GB0224917D0 (en) * | 2002-10-25 | 2002-12-04 | Novartis Ag | Organic compounds |
| CA2504735C (en) * | 2002-11-07 | 2009-06-23 | Merck & Co., Inc. | Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
| CN1775762A (zh) * | 2005-12-06 | 2006-05-24 | 山东大学 | 川芎嗪酰基哌嗪衍生物、制备方法和药物组合物与应用 |
| FR2917622B1 (fr) * | 2007-06-19 | 2009-10-23 | Pierre Fabre Medicament Sa | Utilisation d'un antagoniste par1 dans le traitement de la fibrillation atriale. |
-
2006
- 2006-06-19 FR FR0605419A patent/FR2902426B1/fr not_active Expired - Fee Related
-
2007
- 2007-06-19 MX MX2008016447A patent/MX2008016447A/es active IP Right Grant
- 2007-06-19 DE DE602007008572T patent/DE602007008572D1/de active Active
- 2007-06-19 AU AU2007263051A patent/AU2007263051B2/en not_active Ceased
- 2007-06-19 EP EP07786761A patent/EP2041104B1/en active Active
- 2007-06-19 CA CA2655527A patent/CA2655527C/en not_active Expired - Fee Related
- 2007-06-19 GE GEAP200711058A patent/GEP20115201B/en unknown
- 2007-06-19 BR BRPI0713132A patent/BRPI0713132B8/pt not_active IP Right Cessation
- 2007-06-19 UA UAA200900373A patent/UA96947C2/ru unknown
- 2007-06-19 US US12/305,584 patent/US8217046B2/en not_active Expired - Fee Related
- 2007-06-19 SA SA07280330A patent/SA07280330B1/ar unknown
- 2007-06-19 AT AT07786761T patent/ATE478059T1/de not_active IP Right Cessation
- 2007-06-19 PL PL07786761T patent/PL2041104T3/pl unknown
- 2007-06-19 PT PT07786761T patent/PT2041104E/pt unknown
- 2007-06-19 AR ARP070102685A patent/AR061520A1/es active IP Right Grant
- 2007-06-19 ES ES07786761T patent/ES2349324T3/es active Active
- 2007-06-19 NZ NZ573764A patent/NZ573764A/en not_active IP Right Cessation
- 2007-06-19 JP JP2009515860A patent/JP5356222B2/ja not_active Expired - Fee Related
- 2007-06-19 CN CN200780022674XA patent/CN101472907B/zh not_active Expired - Fee Related
- 2007-06-19 KR KR1020097000946A patent/KR101468752B1/ko not_active Expired - Fee Related
- 2007-06-19 WO PCT/EP2007/056086 patent/WO2007147824A1/en not_active Ceased
- 2007-06-19 RU RU2008152247/04A patent/RU2440997C2/ru active
- 2007-06-19 MY MYPI20085203A patent/MY144461A/en unknown
- 2007-06-20 TW TW096122073A patent/TWI404710B/zh not_active IP Right Cessation
-
2008
- 2008-12-16 TN TNP2008000522A patent/TNSN08522A1/en unknown
- 2008-12-16 CR CR10509A patent/CR10509A/es unknown
- 2008-12-16 IL IL195972A patent/IL195972A/en active IP Right Grant
-
2009
- 2009-01-09 MA MA31560A patent/MA30756B1/fr unknown
- 2009-01-13 EC EC2009009065A patent/ECSP099065A/es unknown
- 2009-01-14 ZA ZA2009/00303A patent/ZA200900303B/en unknown
- 2009-01-16 NO NO20090270A patent/NO341389B1/no not_active IP Right Cessation
-
2012
- 2012-05-21 US US13/476,487 patent/US8513258B2/en not_active Expired - Fee Related
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