PE20121805A1 - Derivados de 6-oxo-1,6-dihidropiridazin-4-carboxamida n-sustituidas con anilino-(bencil o piridinilmetil)-carbamoilo como antagonistas del receptor de bradiquinina 1 (b1) - Google Patents
Derivados de 6-oxo-1,6-dihidropiridazin-4-carboxamida n-sustituidas con anilino-(bencil o piridinilmetil)-carbamoilo como antagonistas del receptor de bradiquinina 1 (b1)Info
- Publication number
- PE20121805A1 PE20121805A1 PE2012001250A PE2012001250A PE20121805A1 PE 20121805 A1 PE20121805 A1 PE 20121805A1 PE 2012001250 A PE2012001250 A PE 2012001250A PE 2012001250 A PE2012001250 A PE 2012001250A PE 20121805 A1 PE20121805 A1 PE 20121805A1
- Authority
- PE
- Peru
- Prior art keywords
- oxo
- alkyl
- bradiquinin
- dihydropyridazine
- pyridinylmethyl
- Prior art date
Links
- SLRMQYXOBQWXCR-UHFFFAOYSA-N 2154-56-5 Chemical class [CH2]C1=CC=CC=C1 SLRMQYXOBQWXCR-UHFFFAOYSA-N 0.000 title 1
- WHZFQZPLYVKTAE-UHFFFAOYSA-N 6-oxo-1h-pyridazine-4-carboxamide Chemical compound NC(=O)C1=CN=NC(O)=C1 WHZFQZPLYVKTAE-UHFFFAOYSA-N 0.000 title 1
- -1 PYRIDINYLMETHYL Chemical class 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 208000002193 Pain Diseases 0.000 abstract 2
- CVINWVPRKDIGLL-UHFFFAOYSA-N 4-chloro-2-(trifluoromethyl)aniline Chemical compound NC1=CC=C(Cl)C=C1C(F)(F)F CVINWVPRKDIGLL-UHFFFAOYSA-N 0.000 abstract 1
- LRCQLCWUUBSUOY-UHFFFAOYSA-N 4-fluoro-2-(trifluoromethyl)aniline Chemical compound NC1=CC=C(F)C=C1C(F)(F)F LRCQLCWUUBSUOY-UHFFFAOYSA-N 0.000 abstract 1
- JNCMHMUGTWEVOZ-UHFFFAOYSA-N F[CH]F Chemical compound F[CH]F JNCMHMUGTWEVOZ-UHFFFAOYSA-N 0.000 abstract 1
- 108010081348 HRT1 protein Hairy Proteins 0.000 abstract 1
- 102100021881 Hairy/enhancer-of-split related with YRPW motif protein 1 Human genes 0.000 abstract 1
- 206010019233 Headaches Diseases 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 208000005298 acute pain Diseases 0.000 abstract 1
- 230000002757 inflammatory effect Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 abstract 1
- 208000004296 neuralgia Diseases 0.000 abstract 1
- 208000021722 neuropathic pain Diseases 0.000 abstract 1
- 230000001173 tumoral effect Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/06—Antimigraine agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C211/00—Compounds containing amino groups bound to a carbon skeleton
- C07C211/43—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
- C07C211/54—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having amino groups bound to two or three six-membered aromatic rings
- C07C211/56—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having amino groups bound to two or three six-membered aromatic rings the carbon skeleton being further substituted by halogen atoms or by nitro or nitroso groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/72—Nitrogen atoms
- C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
- C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having 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
- C07D237/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
- C07D307/04—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D307/18—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no 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
- C07D307/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Pain & Pain Management (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Rheumatology (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
SE REFIERE A UN COMPUESTO DE FORMULA I, DONDE R1 ES 6-OXO-5,6-DIHIDRO-PIRIDAZIN-4IL; R2 ES H, CH3; R3 Y R4 JUNTO AL ATOMO DE C AL QUE ESTAN UNIDOS FORMAN CICLOALQUILENO C3-C6; R5 ES H, CH3; R6 ES H, F, Cl, METILO; R7 ES H, F, Cl, Br,-CN, ALQUILO C1-C4, CF3, CHF2; R8 ES H, R9 ES F, Cl, Br, ALQUILO C1-C4, O-ALQUILO C1-C4, S-(ALQUILO C1-C4); R10 ES H; R11 ES F, Cl, Br, -CN, ALQUILO C1-C4, CF3, ENTRE OTROS; X ES CH, N. SON COMPUESTOS PREFERIDOS: (1-{[5-(4-CLORO-2-TRIFLUOROMETIL-FENILAMINO)-PIRIDIN-2-ILMETIL]-CARBAMOIL}-CICLOPROPIL)-AMIDA DEL ACIDO 6-OXO-1,6-DIHIDRO-PIRIDAZIN-4-CARBOXILICO; {3-[2-FLUORO-4-(4-FLUORO-2-TRIFLUOROMETIL-FENILAMINO)-BENCILCARBAMOIL]-TETRAHIDROFURAN-3-IL}-AMIDA DEL ACIDO (S)-6-OXO-1,6-DIHIDRO-PIRIDAZIN-4-CARBOXILICO; ENTRE OTROS. REFERIDA ADEMAS A UN PROCEDIMIENTO DE PREPARACION. DICHOS COMPUESTOS SON UTILES EN EL TRATAMIENTO DE DOLORES AGUDOS, DOLORES VICERALES, NEUROPATICOS, INFLAMATORIOS, TUMORALES ASI COMO DOLORES DE CABEZA
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/EP2010/052232 WO2010097372A1 (de) | 2009-02-26 | 2010-02-23 | Verbindungen als bradykinin-b1-antagonisten |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20121805A1 true PE20121805A1 (es) | 2013-01-23 |
Family
ID=43981434
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2012001250A PE20121805A1 (es) | 2010-02-23 | 2011-02-21 | Derivados de 6-oxo-1,6-dihidropiridazin-4-carboxamida n-sustituidas con anilino-(bencil o piridinilmetil)-carbamoilo como antagonistas del receptor de bradiquinina 1 (b1) |
Country Status (22)
| Country | Link |
|---|---|
| EP (1) | EP2539323B3 (es) |
| JP (1) | JP5603955B2 (es) |
| KR (1) | KR101843341B1 (es) |
| CN (2) | CN103980258B (es) |
| AP (1) | AP3218A (es) |
| AR (1) | AR080249A1 (es) |
| AU (1) | AU2011219885C1 (es) |
| CA (1) | CA2790952C (es) |
| CY (1) | CY1116182T1 (es) |
| DK (1) | DK2539323T6 (es) |
| ES (1) | ES2531663T7 (es) |
| IL (1) | IL220680A (es) |
| MA (1) | MA34008B1 (es) |
| MX (1) | MX2012009224A (es) |
| NZ (1) | NZ601194A (es) |
| PE (1) | PE20121805A1 (es) |
| PL (1) | PL2539323T6 (es) |
| PT (1) | PT2539323E (es) |
| SG (1) | SG183336A1 (es) |
| SI (1) | SI2539323T1 (es) |
| TW (1) | TWI499589B (es) |
| WO (1) | WO2011104203A1 (es) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102007034620A1 (de) | 2007-07-25 | 2009-01-29 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue B1-Antagonisten |
| WO2009027450A1 (de) | 2007-08-29 | 2009-03-05 | Boehringer Ingelheim International Gmbh | Neue bradykinin b1-antagonisten |
| PE20121805A1 (es) | 2010-02-23 | 2013-01-23 | Boehringer Ingelheim Int | Derivados de 6-oxo-1,6-dihidropiridazin-4-carboxamida n-sustituidas con anilino-(bencil o piridinilmetil)-carbamoilo como antagonistas del receptor de bradiquinina 1 (b1) |
| US8937073B2 (en) * | 2010-08-20 | 2015-01-20 | Boehringer Ingelheim International Gmbh | Disubstituted tetrahydrofuranyl compounds and their use as B1-receptor antagonists |
| US8901127B2 (en) | 2010-08-20 | 2014-12-02 | Boehringer Ingelheim International Gmbh | Pyridazin derivatives as antagonists of the bradykinin B1 receptor |
| JP7376582B2 (ja) * | 2018-10-22 | 2023-11-08 | イーオーイー オレオ ゲーエムベーハー | 成形体への圧縮を目的とした粉末材料用添加剤 |
| EP3907218A4 (en) * | 2019-01-04 | 2022-09-21 | Jiangsu Hengrui Medicine Co., Ltd. | 6-OXO-1,6-DIHYDROPYRIDAZINE DERIVATIVE, METHOD FOR PREPARATION AND MEDICAL USE |
| KR20210131357A (ko) * | 2019-02-20 | 2021-11-02 | 지앙수 헨그루이 메디슨 컴퍼니 리미티드 | 6-옥소-1,6-디하이드로피리다진 프로드러그 유도체, 이의 제조 방법, 및 의약에서의 이의 응용 |
| WO2021198534A1 (en) | 2020-04-04 | 2021-10-07 | Oxurion NV | Plasma kallikrein inhibitors for use in the treatment of coronaviral disease |
| WO2023148016A1 (en) | 2022-02-04 | 2023-08-10 | Oxurion NV | Biomarker for plasma kallikrein inhibitor therapy response |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR038377A1 (es) * | 2002-02-08 | 2005-01-12 | Merck & Co Inc | Derivados de n-bifenil-aminocicloalcancarboxamida (con sustitucion con metilo) |
| CA2495914A1 (en) * | 2002-08-29 | 2004-03-11 | Merck & Co., Inc. | N-biarylmethyl aminocycloalkanecarboxamide derivatives |
| EP1654232A4 (en) * | 2003-08-07 | 2008-11-12 | Merck & Co Inc | SULPHONYL SUBSTITUTED N- (BIARYLMETHYL) AMINOCYCLOPROPANCARBOXYLIC ACID AMIDE |
| EP1723143B1 (en) * | 2004-03-02 | 2009-02-18 | Merck & Co., Inc. | Amino cyclopropane carboxamide derivatives as bradykinin antagonists |
| MX2007013766A (es) | 2005-05-11 | 2008-01-28 | Nycomed Gmbh | Combinacion de inhibidor pde4 de roflumilast y un derivado de tetrahidrobiopterina. |
| HUP0600809A3 (en) * | 2006-10-27 | 2008-09-29 | Richter Gedeon Nyrt | New phenylsulfamoyl-benzamide derivatives as bradykinin antagonists, process and intermediates for their preparation and pharmaceutical compositions containing them |
| JP5629274B2 (ja) * | 2009-02-26 | 2014-11-19 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ブラジキニンｂ１アンタゴニストとしての化合物 |
| PE20121805A1 (es) | 2010-02-23 | 2013-01-23 | Boehringer Ingelheim Int | Derivados de 6-oxo-1,6-dihidropiridazin-4-carboxamida n-sustituidas con anilino-(bencil o piridinilmetil)-carbamoilo como antagonistas del receptor de bradiquinina 1 (b1) |
-
2011
- 2011-02-21 PE PE2012001250A patent/PE20121805A1/es not_active Application Discontinuation
- 2011-02-21 CN CN201410206948.2A patent/CN103980258B/zh not_active Expired - Fee Related
- 2011-02-21 WO PCT/EP2011/052512 patent/WO2011104203A1/de not_active Ceased
- 2011-02-21 PL PL11705858T patent/PL2539323T6/pl unknown
- 2011-02-21 JP JP2012553341A patent/JP5603955B2/ja active Active
- 2011-02-21 AU AU2011219885A patent/AU2011219885C1/en not_active Ceased
- 2011-02-21 DK DK11705858.6T patent/DK2539323T6/en active
- 2011-02-21 MA MA35153A patent/MA34008B1/fr unknown
- 2011-02-21 EP EP11705858.6A patent/EP2539323B3/de active Active
- 2011-02-21 KR KR1020127021929A patent/KR101843341B1/ko not_active Expired - Fee Related
- 2011-02-21 AP AP2012006330A patent/AP3218A/xx active
- 2011-02-21 NZ NZ601194A patent/NZ601194A/en not_active IP Right Cessation
- 2011-02-21 CA CA2790952A patent/CA2790952C/en not_active Expired - Fee Related
- 2011-02-21 SG SG2012060620A patent/SG183336A1/en unknown
- 2011-02-21 ES ES11705858.6T patent/ES2531663T7/es active Active
- 2011-02-21 SI SI201130402T patent/SI2539323T1/sl unknown
- 2011-02-21 CN CN201180009563.1A patent/CN102781916B/zh not_active Expired - Fee Related
- 2011-02-21 MX MX2012009224A patent/MX2012009224A/es active IP Right Grant
- 2011-02-21 PT PT117058586T patent/PT2539323E/pt unknown
- 2011-02-22 AR ARP110100542A patent/AR080249A1/es not_active Application Discontinuation
- 2011-02-22 TW TW100105851A patent/TWI499589B/zh active
-
2012
- 2012-06-28 IL IL220680A patent/IL220680A/en not_active IP Right Cessation
-
2015
- 2015-03-02 CY CY20151100211T patent/CY1116182T1/el unknown
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| FD | Application declared void or lapsed |