JP2002053577A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2002053577A5 JP2002053577A5 JP2001224792A JP2001224792A JP2002053577A5 JP 2002053577 A5 JP2002053577 A5 JP 2002053577A5 JP 2001224792 A JP2001224792 A JP 2001224792A JP 2001224792 A JP2001224792 A JP 2001224792A JP 2002053577 A5 JP2002053577 A5 JP 2002053577A5
- Authority
- JP
- Japan
- Prior art keywords
- lower alkyl
- alkyl
- hetero
- twice
- phenyl
- 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
- 125000000217 alkyl group Chemical group 0.000 description 116
- 125000005842 heteroatom Chemical group 0.000 description 37
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 28
- 125000003545 alkoxy group Chemical group 0.000 description 27
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 19
- 229910052739 hydrogen Inorganic materials 0.000 description 16
- 239000001257 hydrogen Substances 0.000 description 16
- 125000004453 alkoxycarbonyl group Chemical group 0.000 description 15
- 150000001875 compounds Chemical class 0.000 description 15
- 125000006413 ring segment Chemical group 0.000 description 14
- 229910052736 halogen Inorganic materials 0.000 description 13
- 150000002367 halogens Chemical class 0.000 description 13
- 229910052757 nitrogen Inorganic materials 0.000 description 11
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 9
- 229910052799 carbon Inorganic materials 0.000 description 9
- 150000002431 hydrogen Chemical class 0.000 description 9
- 239000002253 acid Substances 0.000 description 8
- 125000003282 alkyl amino group Chemical group 0.000 description 8
- 150000003839 salts Chemical class 0.000 description 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 7
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 description 7
- 125000002947 alkylene group Chemical group 0.000 description 6
- 125000004429 atom Chemical group 0.000 description 6
- 238000000034 method Methods 0.000 description 6
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical group C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 description 5
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical group C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 description 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 4
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 3
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 description 3
- 239000001301 oxygen Chemical group 0.000 description 3
- 229910052760 oxygen Inorganic materials 0.000 description 3
- 125000006239 protecting group Chemical group 0.000 description 3
- 125000000980 1H-indol-3-ylmethyl group Chemical group [H]C1=C([H])C([H])=C2N([H])C([H])=C(C([H])([H])[*])C2=C1[H] 0.000 description 2
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical group C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 description 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical group C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 description 2
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 description 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 2
- 0 *N(*)Cc1n[n]nc1CN(CC1)CC(Cc2c[n](*)c3c2cccc3)N1C(c1cc(C(F)(F)F)cc(C(F)(F)F)c1)=O Chemical compound *N(*)Cc1n[n]nc1CN(CC1)CC(Cc2c[n](*)c3c2cccc3)N1C(c1cc(C(F)(F)F)cc(C(F)(F)F)c1)=O 0.000 description 1
- FQXWSUOMZGXWNB-UHFFFAOYSA-N 1-(2h-triazol-4-ylmethyl)piperazine Chemical class C=1NN=NC=1CN1CCNCC1 FQXWSUOMZGXWNB-UHFFFAOYSA-N 0.000 description 1
- -1 1H-indol-3-yl-methyl group Chemical group 0.000 description 1
- ZOWMTYKIOFIWJW-UHFFFAOYSA-N 2-(piperazin-2-ylmethyl)-1h-indole Chemical class C=1C2=CC=CC=C2NC=1CC1CNCCN1 ZOWMTYKIOFIWJW-UHFFFAOYSA-N 0.000 description 1
- JVQIKJMSUIMUDI-UHFFFAOYSA-N 3-pyrroline Chemical group C1NCC=C1 JVQIKJMSUIMUDI-UHFFFAOYSA-N 0.000 description 1
- 102000009493 Neurokinin receptors Human genes 0.000 description 1
- 108050000302 Neurokinin receptors Proteins 0.000 description 1
- 102000002002 Neurokinin-1 Receptors Human genes 0.000 description 1
- 108010040718 Neurokinin-1 Receptors Proteins 0.000 description 1
- 230000003042 antagnostic effect Effects 0.000 description 1
- 125000004432 carbon atom Chemical group C* 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 125000004122 cyclic group Chemical group 0.000 description 1
- AAOVKJBEBIDNHE-UHFFFAOYSA-N diazepam Chemical group N=1CC(=O)N(C)C2=CC=C(Cl)C=C2C=1C1=CC=CC=C1 AAOVKJBEBIDNHE-UHFFFAOYSA-N 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 239000000543 intermediate Substances 0.000 description 1
- 239000013067 intermediate product Substances 0.000 description 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 description 1
- CWWARWOPSKGELM-SARDKLJWSA-N methyl (2s)-2-[[(2s)-2-[[2-[[(2s)-2-[[(2s)-2-[[(2s)-5-amino-2-[[(2s)-5-amino-2-[[(2s)-1-[(2s)-6-amino-2-[[(2s)-1-[(2s)-2-amino-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoyl]amino]-5 Chemical compound C([C@@H](C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)OC)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CCCCN)NC(=O)[C@H]1N(CCC1)C(=O)[C@@H](N)CCCN=C(N)N)C1=CC=CC=C1 CWWARWOPSKGELM-SARDKLJWSA-N 0.000 description 1
- 150000004885 piperazines Chemical class 0.000 description 1
- 125000004193 piperazinyl group Chemical group 0.000 description 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 description 1
- 229940066771 systemic antihistamines piperazine derivative Drugs 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10036818.2 | 2000-07-28 | ||
| DE10036818A DE10036818A1 (de) | 2000-07-28 | 2000-07-28 | Neue N-Triazolylmethyl-Piperazinderivate als Neurokininrezeptor-Antagonisten |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2002053577A JP2002053577A (ja) | 2002-02-19 |
| JP2002053577A5 true JP2002053577A5 (enExample) | 2008-06-19 |
Family
ID=7650544
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2001224792A Pending JP2002053577A (ja) | 2000-07-28 | 2001-07-25 | 新規ｎ−トリアゾリルメチル−ピペラジン誘導体、その製造方法および中間生成物、および前記誘導体を含有する医薬品 |
Country Status (27)
| Country | Link |
|---|---|
| US (1) | US6407106B1 (enExample) |
| EP (1) | EP1176144B1 (enExample) |
| JP (1) | JP2002053577A (enExample) |
| KR (1) | KR100924405B1 (enExample) |
| CN (1) | CN1167698C (enExample) |
| AR (1) | AR028743A1 (enExample) |
| AT (1) | ATE244716T1 (enExample) |
| AU (1) | AU779318B2 (enExample) |
| BR (1) | BR0103048A (enExample) |
| CA (1) | CA2354213C (enExample) |
| CZ (1) | CZ301695B6 (enExample) |
| DE (2) | DE10036818A1 (enExample) |
| DK (1) | DK1176144T3 (enExample) |
| DZ (1) | DZ3119A1 (enExample) |
| ES (1) | ES2201007T3 (enExample) |
| HU (1) | HU226687B1 (enExample) |
| IL (1) | IL144299A (enExample) |
| IN (1) | IN191021B (enExample) |
| NO (1) | NO323233B1 (enExample) |
| NZ (1) | NZ513041A (enExample) |
| PL (1) | PL210436B1 (enExample) |
| PT (1) | PT1176144E (enExample) |
| RU (1) | RU2288918C2 (enExample) |
| SK (1) | SK284802B6 (enExample) |
| TW (1) | TWI304403B (enExample) |
| UA (1) | UA73728C2 (enExample) |
| ZA (1) | ZA200105737B (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA77515C2 (en) * | 2002-04-04 | 2006-12-15 | Diazabicyclo alkane derivatives possessing neuroldnin-nk1 receptor antagonistic activity | |
| DK1501808T3 (da) * | 2002-04-26 | 2008-10-13 | Lilly Co Eli | Tachykininreceptor-antagonister |
| MXPA04010622A (es) * | 2002-04-26 | 2005-01-25 | Lilly Co Eli | Derivados de triazol como antagonistas de receptor de taquicinina. |
| US20060160794A1 (en) * | 2003-06-12 | 2006-07-20 | Amegadzie Albert K | Tachykinin receptor antagonists |
| US20070082905A1 (en) * | 2005-05-27 | 2007-04-12 | De Vries Michiel H | Pharmaceutical compositions comprising n-triazolymethyl-piperazine compounds and methods of using same |
| CN101228137B (zh) * | 2005-07-25 | 2010-09-29 | 弗·哈夫曼-拉罗切有限公司 | 被取代的三唑衍生物和它们作为神经激肽3受体拮抗剂的用途 |
| PE20081229A1 (es) * | 2006-12-01 | 2008-08-28 | Merck & Co Inc | Antagonistas de receptor de orexina de diazepam sustituido |
| WO2008090114A1 (en) | 2007-01-24 | 2008-07-31 | Glaxo Group Limited | Pharmaceutical compositions comprising 2-methoxy-5- (5-trifluoromethyl-tetrazol-i-yl-benzyl) - (2s-phenyl-piperidin-3s-yl-) |
| WO2011020874A1 (en) | 2009-08-20 | 2011-02-24 | Inserm (Institut National De La Sante Et De La Recherche Medicale) | Vla-4 as a biomarker for prognosis and target for therapy in duchenne muscular dystrophy |
| EP2729147B1 (en) | 2011-07-04 | 2017-09-06 | IRBM - Science Park S.p.A. | Nk-1 receptor antagonists for treating corneal neovascularisation |
| WO2019162519A1 (en) | 2018-02-26 | 2019-08-29 | Ospedale San Raffaele S.R.L. | Nk-1 antagonists for use in the treatment of ocular pain |
| US20230134843A1 (en) | 2020-03-11 | 2023-05-04 | Ospedale San Raffaele S.R.L. | Treatment of stem cell deficiency |
| CN115184498B (zh) * | 2022-07-15 | 2023-02-21 | 山东京卫制药有限公司 | N-Boc-哌嗪中有关物质哌嗪的检测方法 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL111730A (en) | 1993-11-29 | 1998-12-06 | Fujisawa Pharmaceutical Co | Piperazine derivatives processes for the preparation thereof and pharmaceutical compositions containing the same |
| US5883098A (en) | 1993-11-29 | 1999-03-16 | Fujisawa Pharmaceutical Co., Ltd. | Piperazine derivatives |
| US5637592A (en) * | 1994-07-12 | 1997-06-10 | Janssen Pharmaceutica N.V. | Acyl derivatives of azolones |
| HUP9900822A3 (en) * | 1995-05-25 | 1999-11-29 | Fujisawa Pharmaceutical Co | Piperazine derivatives, process for producing them, pharmaceutical compositions containing them and method for treating tachykinin-mediated diseases |
| GB9513118D0 (en) * | 1995-06-28 | 1995-08-30 | Merck Sharp & Dohme | Therapeutic agents |
| EP0873320B1 (en) * | 1995-12-18 | 2002-06-12 | Fujisawa Pharmaceutical Co., Ltd. | Piperazine derivatives as tachykinin antagonists |
| KR100458346B1 (ko) * | 1996-03-29 | 2005-06-21 | 듀파 인터내셔날 리서치 베 파우 | 피페라진및피페리딘화합물 |
| AUPO735997A0 (en) * | 1997-06-17 | 1997-07-10 | Fujisawa Pharmaceutical Co., Ltd. | Piperazine derivatives |
| DE59814233D1 (de) * | 1997-08-27 | 2008-07-03 | Solvay Pharm Gmbh | Indolmethyl-N,N'-bisacylpiperazine als Neurokininrezeptorantagonisten |
| DE19824865A1 (de) | 1997-08-27 | 1999-03-04 | Solvay Pharm Gmbh | Neue Harnstoffderivate |
| ES2162731B1 (es) * | 1999-06-04 | 2003-02-16 | Faes Fabrica Espanola De Produ | Nuevas arilpiperacilnilalquil-3(2h)-piridacinonas. |
-
2000
- 2000-07-28 DE DE10036818A patent/DE10036818A1/de not_active Withdrawn
-
2001
- 2001-05-23 CZ CZ20011813A patent/CZ301695B6/cs not_active IP Right Cessation
- 2001-06-01 SK SK757-2001A patent/SK284802B6/sk not_active IP Right Cessation
- 2001-06-21 AR ARP010102959A patent/AR028743A1/es active IP Right Grant
- 2001-07-10 CN CNB011228261A patent/CN1167698C/zh not_active Expired - Fee Related
- 2001-07-11 HU HU0102931A patent/HU226687B1/hu not_active IP Right Cessation
- 2001-07-12 IL IL14429901A patent/IL144299A/en not_active IP Right Cessation
- 2001-07-12 ZA ZA200105737A patent/ZA200105737B/xx unknown
- 2001-07-12 TW TW090117136A patent/TWI304403B/zh not_active IP Right Cessation
- 2001-07-16 IN IN672MU2001 patent/IN191021B/en unknown
- 2001-07-18 NZ NZ513041A patent/NZ513041A/xx not_active IP Right Cessation
- 2001-07-18 KR KR1020010043215A patent/KR100924405B1/ko not_active Expired - Fee Related
- 2001-07-19 ES ES01117433T patent/ES2201007T3/es not_active Expired - Lifetime
- 2001-07-19 PT PT01117433T patent/PT1176144E/pt unknown
- 2001-07-19 DE DE50100358T patent/DE50100358D1/de not_active Expired - Lifetime
- 2001-07-19 AT AT01117433T patent/ATE244716T1/de active
- 2001-07-19 DK DK01117433T patent/DK1176144T3/da active
- 2001-07-19 EP EP01117433A patent/EP1176144B1/de not_active Expired - Lifetime
- 2001-07-25 JP JP2001224792A patent/JP2002053577A/ja active Pending
- 2001-07-26 AU AU57675/01A patent/AU779318B2/en not_active Ceased
- 2001-07-26 CA CA2354213A patent/CA2354213C/en not_active Expired - Fee Related
- 2001-07-26 BR BR0103048-5A patent/BR0103048A/pt not_active IP Right Cessation
- 2001-07-27 RU RU2001121084/04A patent/RU2288918C2/ru not_active IP Right Cessation
- 2001-07-27 PL PL348946A patent/PL210436B1/pl not_active IP Right Cessation
- 2001-07-27 NO NO20013709A patent/NO323233B1/no not_active IP Right Cessation
- 2001-07-27 US US09/915,558 patent/US6407106B1/en not_active Expired - Lifetime
- 2001-07-27 UA UA2001075403A patent/UA73728C2/uk unknown
- 2001-07-28 DZ DZ010054A patent/DZ3119A1/xx active