AR033945A1 - Antagonistas del receptor de bradiquinina, proceso para su produccion, su uso para la fabricacion de un medicamento para el tratamiento o prevencion de una enfermedad o condicion en que juega un rol la activacion del receptor de bradiquinina b1 y una composicion farmaceutica que comprende dichos ant - Google Patents
Antagonistas del receptor de bradiquinina, proceso para su produccion, su uso para la fabricacion de un medicamento para el tratamiento o prevencion de una enfermedad o condicion en que juega un rol la activacion del receptor de bradiquinina b1 y una composicion farmaceutica que comprende dichos antInfo
- Publication number
- AR033945A1 AR033945A1 ARP000102710A ARP000102710A AR033945A1 AR 033945 A1 AR033945 A1 AR 033945A1 AR P000102710 A ARP000102710 A AR P000102710A AR P000102710 A ARP000102710 A AR P000102710A AR 033945 A1 AR033945 A1 AR 033945A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- bradiquinine
- receiver
- treatment
- formula
- Prior art date
Links
- 238000004519 manufacturing process Methods 0.000 title 2
- 239000005557 antagonist Substances 0.000 title 1
- 229940126601 medicinal product Drugs 0.000 title 1
- 238000000034 method Methods 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 230000002265 prevention Effects 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 2
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 abstract 2
- 239000005977 Ethylene Substances 0.000 abstract 2
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000000304 alkynyl group Chemical group 0.000 abstract 2
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 210000002345 respiratory system Anatomy 0.000 abstract 2
- 101800004538 Bradykinin Proteins 0.000 abstract 1
- QXZGBUJJYSLZLT-UHFFFAOYSA-N H-Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg-OH Natural products NC(N)=NCCCC(N)C(=O)N1CCCC1C(=O)N1C(C(=O)NCC(=O)NC(CC=2C=CC=CC=2)C(=O)NC(CO)C(=O)N2C(CCC2)C(=O)NC(CC=2C=CC=CC=2)C(=O)NC(CCCN=C(N)N)C(O)=O)CCC1 QXZGBUJJYSLZLT-UHFFFAOYSA-N 0.000 abstract 1
- 102100035792 Kininogen-1 Human genes 0.000 abstract 1
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical group C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 abstract 1
- 208000005392 Spasm Diseases 0.000 abstract 1
- 230000004913 activation Effects 0.000 abstract 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 abstract 1
- 230000003042 antagnostic effect Effects 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- QXZGBUJJYSLZLT-FDISYFBBSA-N bradykinin Chemical compound NC(=N)NCCC[C@H](N)C(=O)N1CCC[C@H]1C(=O)N1[C@H](C(=O)NCC(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CO)C(=O)N2[C@@H](CCC2)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CCCNC(N)=N)C(O)=O)CCC1 QXZGBUJJYSLZLT-FDISYFBBSA-N 0.000 abstract 1
- 125000004181 carboxyalkyl group Chemical group 0.000 abstract 1
- 210000001035 gastrointestinal tract Anatomy 0.000 abstract 1
- 125000004475 heteroaralkyl group Chemical group 0.000 abstract 1
- 230000035874 hyperreactivity Effects 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 230000002757 inflammatory effect Effects 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 230000000144 pharmacologic effect Effects 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000003884 phenylalkyl group Chemical group 0.000 abstract 1
- QQONPFPTGQHPMA-UHFFFAOYSA-N propylene Natural products CC=C QQONPFPTGQHPMA-UHFFFAOYSA-N 0.000 abstract 1
- 125000004805 propylene group Chemical group [H]C([H])([H])C([H])([*:1])C([H])([H])[*:2] 0.000 abstract 1
- 210000004291 uterus Anatomy 0.000 abstract 1
Classifications
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- C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
- C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
- C07D295/182—Radicals derived from carboxylic acids
- C07D295/192—Radicals derived from carboxylic acids from aromatic carboxylic acids
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- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/37—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
- C07C311/38—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton
- C07C311/44—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
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Abstract
Un compuesto de la fórmula (1) en donde: R5A es -XA-R6A o -N(R7A)R8A, en donde: XA es piperidinileno o piperazinileno; R6A es H, alquilo C1-4, alquenilo C3-4, alquinilo C3-4, (alcoxialquilo) C1-4, (carboxialquilo) C1-4, un grupo heterocíclico C5-7, o fenilalquilo C1-4; R7A es aminoalquilo C2-4, o mono- o di- (alquilo C1-5) aminoalquilo C2-5; y R8A es H, alquilo C1-4, o tiene los significados dados para R7A; X1 es un grupo divalente de la fórmula (2) en donde: n es 0 o 1; X3 es CH o N; (a) X4 es un enlace directo, R3A y R4A son juntos etileno, y m es 2; o (b) X4 es un enlace directo, R3A es H, alquilo C1-4, cicloalquilo C3-6, alquenilo C3-6, alquinilo C3-6, aralquilo C7-10, o heteroaralquilo C6-9, R4A es H, y m es 1 o 2 o 3; o (c) X4 es -CH(R12)-, R3A es H, y R4A y R12 son juntos propileno, y m es 1 o etileno y m es 2; X2 es un grupo divalente de la fórmula (3) en donde: X3 es CH o N; y R11 es alquilo C1-4, cicloalquilo C3-6, o -NR1AR2A, en donde: R1A y R2A son independientemente alquilo C1-4, o junto con el átomo de N con el que están unidos, representan un anillo heterocíclico de 5 a 7 miembros; y R9 y R10 son independientemente un anillo de fenilo o piridina; y sales del mismo. Los compuestos de fórmula (1) tienen actividad farmacológica, en particular exhiben actividad antagonista de bradiquinina y son útiles, por ejemplo para el tratamiento de enfermedades y condiciones en que la activación del receptor B1 juega un rol o está implicado, en particular en el dolor, enfermedades inflamatorias, espasmo del tracto gastrointestinal o útero, hiperreactividad de las vías respiratorias así como para el tratamiento de eventos inflamatorios asociados con enfermedades de las vías respiratorias, en particular asma.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB9913079.1A GB9913079D0 (en) | 1999-06-04 | 1999-06-04 | Organic compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR033945A1 true AR033945A1 (es) | 2004-01-21 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP000102710A AR033945A1 (es) | 1999-06-04 | 2000-06-01 | Antagonistas del receptor de bradiquinina, proceso para su produccion, su uso para la fabricacion de un medicamento para el tratamiento o prevencion de una enfermedad o condicion en que juega un rol la activacion del receptor de bradiquinina b1 y una composicion farmaceutica que comprende dichos ant |
Country Status (28)
| Country | Link |
|---|---|
| US (1) | US6958331B1 (es) |
| EP (1) | EP1183233B1 (es) |
| JP (1) | JP3820148B2 (es) |
| KR (1) | KR100479896B1 (es) |
| CN (1) | CN1165522C (es) |
| AR (1) | AR033945A1 (es) |
| AT (1) | ATE305920T1 (es) |
| AU (1) | AU765628B2 (es) |
| BR (1) | BR0011329A (es) |
| CA (1) | CA2372575C (es) |
| CZ (1) | CZ20014302A3 (es) |
| DE (1) | DE60022999T2 (es) |
| ES (1) | ES2250144T3 (es) |
| GB (1) | GB9913079D0 (es) |
| HK (1) | HK1045834A1 (es) |
| HU (1) | HUP0201524A3 (es) |
| IL (1) | IL146112A0 (es) |
| MX (1) | MXPA01012473A (es) |
| NO (1) | NO20015779D0 (es) |
| NZ (1) | NZ515304A (es) |
| PE (1) | PE20010215A1 (es) |
| PL (1) | PL352056A1 (es) |
| RU (1) | RU2001135802A (es) |
| SK (1) | SK17492001A3 (es) |
| TR (1) | TR200103108T2 (es) |
| TW (1) | TWI227224B (es) |
| WO (1) | WO2000075107A2 (es) |
| ZA (1) | ZA200109891B (es) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7141609B2 (en) * | 1992-08-25 | 2006-11-28 | G.D. Searle & Co. | α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors |
| ES2123065T3 (es) | 1992-08-25 | 1999-01-01 | Searle & Co | Hidroxietilamino-sulfonamidas utiles como inhibidores de proteasas retroviricas. |
| CN1268610C (zh) * | 2001-05-14 | 2006-08-09 | 诺瓦提斯公司 | 磺酰胺衍生物 |
| FR2840897B1 (fr) * | 2002-06-14 | 2004-09-10 | Fournier Lab Sa | Nouveaux derives d'arylsulfonamides et leur utilisation en therapeutique |
| US7211566B2 (en) | 2003-04-01 | 2007-05-01 | Universite De Sherbrooke | Selective bradykinin (BK) B1 peptidic receptor antagonists and uses thereof |
| CA2522084A1 (en) | 2003-04-10 | 2004-10-28 | Amgen Inc. | Cyclic amine derivatives and their use in the treatment of inflammation-related disorders mediated by bradykinin |
| GB0525068D0 (en) | 2005-12-08 | 2006-01-18 | Novartis Ag | Organic compounds |
| HU230518B1 (hu) | 2005-12-20 | 2016-10-28 | Richter Gedeon Nyrt. | Bradykinin B1 receptor szelektív antagonista hatással rendelkező új fenatridin származékok, eljárás előállításukra, és az ezeket tartalmazó gyógyszerkészítmények |
| HUP0600808A3 (en) | 2006-10-27 | 2008-09-29 | Richter Gedeon Nyrt | New benzamide derivatives as bradykinin antagonists, process for their preparation and pharmaceutical compositions containing them |
| HUP0600810A3 (en) | 2006-10-27 | 2008-09-29 | Richter Gedeon Nyrt | New sulfonamide derivatives as bradykinin antagonists, process and intermediates for their preparation and pharmaceutical compositions containing them |
| TWI407960B (zh) | 2007-03-23 | 2013-09-11 | Jerini Ag | 小分子緩激肽b2受體調節劑 |
| WO2008153967A1 (en) * | 2007-06-08 | 2008-12-18 | Contec Therapeutics, Inc. | Bk1 antagonist conjugates |
| EP2316820A1 (en) | 2009-10-28 | 2011-05-04 | Dompe S.p.A. | 2-aryl-propionamide derivatives useful as bradykinin receptor antagonists and pharmaceutical compositions containing them |
| US8394858B2 (en) | 2009-12-03 | 2013-03-12 | Novartis Ag | Cyclohexane derivatives and uses thereof |
| UY34094A (es) | 2011-05-27 | 2013-01-03 | Novartis Ag | Derivados de la piperidina 3-espirocíclica como agonistas de receptores de la ghrelina |
| EA201491990A1 (ru) | 2012-05-03 | 2015-02-27 | Новартис Аг | L-малатная соль 2,7-диазаспиро[4.5]дец-7-иловых производных и их кристаллические формы в качестве агонистов грелиновых рецепторов |
| LT3713928T (lt) | 2017-11-24 | 2022-05-10 | Pharvaris Netherlands B.V. | Nauji bradikinino b2 receptoriaus antagonistai |
| AR118982A1 (es) | 2019-05-23 | 2021-11-17 | Pharvaris Gmbh | Antagonistas cíclicos del receptor b2 de bradiquinina |
| UY38707A (es) | 2019-05-23 | 2020-12-31 | Pharvaris Gmbh | Nuevos antagonistas cíclicos del receptor b2 de bradiquinina |
| KR102825097B1 (ko) | 2022-06-21 | 2025-06-24 | 정인호 | 균일한 고기 익힘 상태를 제공하는 숯불 고기 구이기 |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2743562B1 (fr) | 1996-01-11 | 1998-04-03 | Sanofi Sa | Derives de n-(arylsulfonyl) aminoacides, leur preparation, les compositions pharmaceutiques en contenant |
-
1999
- 1999-06-04 GB GBGB9913079.1A patent/GB9913079D0/en not_active Ceased
-
2000
- 2000-05-29 TW TW089110384A patent/TWI227224B/zh not_active IP Right Cessation
- 2000-06-01 AR ARP000102710A patent/AR033945A1/es not_active Application Discontinuation
- 2000-06-02 JP JP2001501588A patent/JP3820148B2/ja not_active Expired - Fee Related
- 2000-06-02 KR KR10-2001-7015416A patent/KR100479896B1/ko not_active Expired - Fee Related
- 2000-06-02 TR TR2001/03108T patent/TR200103108T2/xx unknown
- 2000-06-02 NZ NZ515304A patent/NZ515304A/xx unknown
- 2000-06-02 US US10/009,009 patent/US6958331B1/en not_active Expired - Fee Related
- 2000-06-02 PL PL00352056A patent/PL352056A1/xx not_active Application Discontinuation
- 2000-06-02 AT AT00940304T patent/ATE305920T1/de not_active IP Right Cessation
- 2000-06-02 CZ CZ20014302A patent/CZ20014302A3/cs unknown
- 2000-06-02 MX MXPA01012473A patent/MXPA01012473A/es unknown
- 2000-06-02 ES ES00940304T patent/ES2250144T3/es not_active Expired - Lifetime
- 2000-06-02 AU AU55282/00A patent/AU765628B2/en not_active Ceased
- 2000-06-02 WO PCT/EP2000/005059 patent/WO2000075107A2/en not_active Ceased
- 2000-06-02 IL IL14611200A patent/IL146112A0/xx unknown
- 2000-06-02 DE DE60022999T patent/DE60022999T2/de not_active Expired - Fee Related
- 2000-06-02 CA CA2372575A patent/CA2372575C/en not_active Expired - Fee Related
- 2000-06-02 EP EP00940304A patent/EP1183233B1/en not_active Expired - Lifetime
- 2000-06-02 PE PE2000000549A patent/PE20010215A1/es not_active Application Discontinuation
- 2000-06-02 HU HU0201524A patent/HUP0201524A3/hu unknown
- 2000-06-02 RU RU2001135802/04A patent/RU2001135802A/ru not_active Application Discontinuation
- 2000-06-02 SK SK1749-2001A patent/SK17492001A3/sk unknown
- 2000-06-02 CN CNB008082405A patent/CN1165522C/zh not_active Expired - Fee Related
- 2000-06-02 BR BR0011329-8A patent/BR0011329A/pt not_active IP Right Cessation
- 2000-06-02 HK HK02105567.0A patent/HK1045834A1/zh unknown
-
2001
- 2001-11-27 NO NO20015779A patent/NO20015779D0/no not_active Application Discontinuation
- 2001-11-30 ZA ZA200109891A patent/ZA200109891B/en unknown
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