UA78975C2 - Basic linear compounds with activity of tachykinin antagonists and their dosage forms - Google Patents
Basic linear compounds with activity of tachykinin antagonists and their dosage forms Download PDFInfo
- Publication number
- UA78975C2 UA78975C2 UA20040504087A UA20040504087A UA78975C2 UA 78975 C2 UA78975 C2 UA 78975C2 UA 20040504087 A UA20040504087 A UA 20040504087A UA 20040504087 A UA20040504087 A UA 20040504087A UA 78975 C2 UA78975 C2 UA 78975C2
- Authority
- UA
- Ukraine
- Prior art keywords
- carboxylic acid
- amide
- group
- ethylcarbamoyl
- phenyl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract description 47
- 239000005557 antagonist Substances 0.000 title abstract description 9
- 102000003141 Tachykinin Human genes 0.000 title abstract description 7
- 108060008037 tachykinin Proteins 0.000 title abstract description 7
- 230000000694 effects Effects 0.000 title description 5
- 239000002552 dosage form Substances 0.000 title description 4
- HEAUFJZALFKPBA-YRVBCFNBSA-N Neurokinin A Chemical compound C([C@@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(N)=O)C(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@@H](NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CC=1NC=NC=1)C(C)O)C1=CC=CC=C1 HEAUFJZALFKPBA-YRVBCFNBSA-N 0.000 abstract description 9
- 239000008194 pharmaceutical composition Substances 0.000 abstract description 9
- 102400000097 Neurokinin A Human genes 0.000 abstract description 8
- 101800000399 Neurokinin A Proteins 0.000 abstract description 8
- 238000000034 method Methods 0.000 description 160
- -1 cyanomethyl Chemical group 0.000 description 126
- 238000001819 mass spectrum Methods 0.000 description 106
- 150000001408 amides Chemical class 0.000 description 80
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 76
- 125000005605 benzo group Chemical group 0.000 description 72
- 239000000243 solution Substances 0.000 description 58
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 48
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 description 42
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- 239000000047 product Substances 0.000 description 38
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- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 29
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ITFI20010203 ITFI20010203A1 (it) | 2001-10-29 | 2001-10-29 | Composti lineari con caratteristiche basiche ad attivita' nk-2 antagonista,loro processi di sintesi e formulazioni che li contengono |
| ITFI20020104 ITFI20020104A1 (it) | 2002-06-14 | 2002-06-14 | Composti lineari con caratteristiche basiche ed attivita' nk-2 antagonista, loro processi di sintesi e formulazioni che li contengono |
| PCT/EP2002/012022 WO2003037916A2 (en) | 2001-10-29 | 2002-10-28 | Linear basic compounds having nk-2 antagonist activity and formulations thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| UA78975C2 true UA78975C2 (en) | 2007-05-10 |
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| UA20040504087A UA78975C2 (en) | 2001-10-29 | 2002-10-28 | Basic linear compounds with activity of tachykinin antagonists and their dosage forms |
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| CA2564207A1 (en) * | 2004-05-13 | 2005-11-24 | Boehringer Ingelheim International Gmbh | Novel substituted thiophenecarboxamides, their production and their use as medicaments |
| ITFI20040221A1 (it) * | 2004-10-27 | 2005-01-27 | Guidotti & C Spa | Composizioni farmaceutiche a base di nk2 antagonisti per uso pediatrico |
| JP4012239B2 (ja) * | 2006-01-11 | 2007-11-21 | 生化学工業株式会社 | オキサゾロン誘導体 |
| US20080227823A1 (en) * | 2007-03-12 | 2008-09-18 | Hassan Pajouhesh | Amide derivatives as calcium channel blockers |
| IT1394304B1 (it) * | 2009-05-21 | 2012-06-06 | Malesci Sas | Processo per la preparazione di ibodutant (men15596) e relativi intermedi |
| JP5929483B2 (ja) | 2011-05-10 | 2016-06-08 | 住友化学株式会社 | 植物の生長を促進する方法 |
| WO2012177893A2 (en) | 2011-06-24 | 2012-12-27 | Amgen Inc. | Trpm8 antagonists and their use in treatments |
| JP2014517074A (ja) | 2011-06-24 | 2014-07-17 | アムジエン・インコーポレーテツド | Ｔｒｐｍ８アンタゴニストおよび治療におけるそれらの使用 |
| EP2671575A1 (en) * | 2012-06-04 | 2013-12-11 | Universität Regensburg | Ras inhibitors |
| US8952009B2 (en) | 2012-08-06 | 2015-02-10 | Amgen Inc. | Chroman derivatives as TRPM8 inhibitors |
| IL309232A (en) | 2021-06-14 | 2024-02-01 | Scorpion Therapeutics Inc | History of urea which can be used to treat cancer |
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| DE3711335A1 (de) * | 1987-04-03 | 1988-10-20 | Merck Patent Gmbh | Aminosaeurederivate |
| US5164372A (en) | 1989-04-28 | 1992-11-17 | Fujisawa Pharmaceutical Company, Ltd. | Peptide compounds having substance p antagonism, processes for preparation thereof and pharmaceutical composition comprising the same |
| CA2140640A1 (en) | 1992-08-13 | 1994-03-03 | David C. Horwell | Tachykinin antagonists |
| ITFI940009A1 (it) * | 1994-01-19 | 1995-07-19 | Menarini Farma Ind | Antagonisti delle tachichinine, loro preparazione e formulazioni farmaceutiche che li contengono. |
| TW385308B (en) * | 1994-03-04 | 2000-03-21 | Merck & Co Inc | Prodrugs of morpholine tachykinin receptor antagonists |
| JPH10501228A (ja) * | 1994-06-06 | 1998-02-03 | ワーナー−ランバート・コンパニー | タキキニン（ｎｋ▲下１▼）受容体アンタゴニスト |
| US5483070A (en) * | 1994-08-02 | 1996-01-09 | Packard Instrument Company | Scintillation counter |
| IT1291776B1 (it) | 1997-02-07 | 1999-01-21 | Menarini Ricerche Spa | Composti monociclici a quattro residui bifunzionali, aventi azione nk-2 antagonista |
| IT1291823B1 (it) | 1997-04-08 | 1999-01-21 | Menarini Ricerche Spa | Composti pseudo-peptidici, loro preparazione ed uso in formulazioni farmaceutiche |
| AU729995B2 (en) * | 1997-06-30 | 2001-02-22 | Nippon Kayaku Kabushiki Kaisha | Novel naphthyridine derivatives or salts thereof |
| US6740682B2 (en) * | 1997-08-29 | 2004-05-25 | Tularik Limited | Meta-benzamidine derivatives as serine protease inhibitors |
| DE69830410T2 (de) * | 1997-08-29 | 2006-01-26 | Tularik Ltd. | Meta-benzamidinderivate als serinprotease-inhibitoren |
| IT1304898B1 (it) * | 1998-09-08 | 2001-04-05 | Menarini Ricerche Spa | Prodotti con caratteristiche basiche aventi attivita' antagonista sulrecettore nk-1 e loro impiego in preparazioni farmaceutiche |
| ES2248084T3 (es) * | 1999-06-14 | 2006-03-16 | Eli Lilly And Company | Inhibidores de serinproteasa. |
| IT1307809B1 (it) | 1999-10-21 | 2001-11-19 | Menarini Ricerche Spa | Composti monociclici basici ad azione nk-2 antagonista, processi difabbricazione e formulazioni che li contengono. |
| GB0030305D0 (en) * | 2000-12-13 | 2001-01-24 | Lilly Co Eli | Compounds |
| GB0030303D0 (en) * | 2000-12-13 | 2001-01-24 | Lilly Co Eli | Compounds |
| US20050038692A1 (en) | 2003-08-14 | 2005-02-17 | Kane John Michael | System and method for facilitating centralized candidate selection and monitoring subject participation in clinical trial studies |
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