AR004413A1 - Compuestos de tiol que poseen actividad inhibitoria de metalopeptidasa; proceso para preparar dichos derivados; composiciones farmaceuticas que loscontienen - Google Patents
Compuestos de tiol que poseen actividad inhibitoria de metalopeptidasa; proceso para preparar dichos derivados; composiciones farmaceuticas que loscontienenInfo
- Publication number
- AR004413A1 AR004413A1 ARP960105957A ARP960105957A AR004413A1 AR 004413 A1 AR004413 A1 AR 004413A1 AR P960105957 A ARP960105957 A AR P960105957A AR P960105957 A ARP960105957 A AR P960105957A AR 004413 A1 AR004413 A1 AR 004413A1
- Authority
- AR
- Argentina
- Prior art keywords
- group
- groups
- alkyl
- phenyl
- branched
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 230000002401 inhibitory effect Effects 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 239000001301 oxygen Chemical group 0.000 abstract 2
- 229910052717 sulfur Chemical group 0.000 abstract 2
- 239000011593 sulfur Chemical group 0.000 abstract 2
- 125000003396 thiol group Chemical group [H]S* 0.000 abstract 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 1
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 239000004480 active ingredient Substances 0.000 abstract 1
- 125000004442 acylamino group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 abstract 1
- 125000004414 alkyl thio group Chemical group 0.000 abstract 1
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 125000004473 dialkylaminocarbonyl group Chemical group 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 125000001153 fluoro group Chemical group F* 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/26—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
- C07D213/24—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 substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/55—Acids; Esters
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D241/12—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D277/30—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- 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
- C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D307/38—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D307/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
- C07D333/24—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 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)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Treatment Of Fiber Materials (AREA)
- Preliminary Treatment Of Fibers (AREA)
- Heterocyclic Compounds Containing Sulfur Atoms (AREA)
- Furan Compounds (AREA)
- Pyridine Compounds (AREA)
- Medicines Containing Plant Substances (AREA)
Abstract
El invento se refiere a fórmula (I), donde R es un grupo mercapto o un grupo R4COS convertible en el organismo a un grupo mercapto; R1 es un grupoalquilo C2-C4 recto o ramificado o un grupo arilo o arilalquilo que tiene entre 1 y 6 átomosde carbono en la fracción alquilo donde el arilo es unfenilo o un heterociclo aromático de 5 ó 6 miembros con uno o dos heteroátomos seleccionados del grupo consistente en nitrógeno, oxígeno y azufre, sustituidooptativamente con uno o mássustituyen tes, los mismos o diferentes, seleccionados del grupo formado por átomos de halógeno, grupos hidroxi, alcoxi,alquilo, alquiltio, alquilsulfonilo o alcoxicarbonilo que tienen entre 1 y 6 átomos de carbono en la fracciónalquilo, grupos alquilo C1-C3 que contienenuno o más átomos de fluor, grupos carboxi, grupos nitro, grupos amino o aminocarbonilo, grupos acilamino, grupos aminosulfonilo, grupos mono- ódi-alquilamino o mono- ó dialquilaminocarbonilo quetienen entre 1 y 6 á tomos en la fracción alquilo; R2 es un átomo de hidrógeno, un alquilo C1-C4 recto oramificado o un grupo bencilo; R3 es un grupo fenilo sustituido con un heterociclo aromático de 5 ó 6 miembros con uno o dosheteroátomosseleccionados del g rupo consistente en nitrógeno, oxígeno y azufre, estando los grupos fenilo y heterocíclico sustituidos optativamente con uno o mássustituyentes, los mismos o diferentes, según se indica para R1; R4 es un grupoalquilo C1-C4 recto o ramificado o un grupo fenilo; procedimiento para supreparación y composiciones farmacéuticas que los contiene como ingredientes activos. Los compuestos de fórmula (I) están dotados de una actividad mixtainhibitoria de ACE yNEP y son útiles en el tratamiento de enfermedades cardiovasculares.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IT95MI002773A IT1277737B1 (it) | 1995-12-28 | 1995-12-28 | Derivati tiolici ad attivita' inibitrice delle metallopeptidasi |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR004413A1 true AR004413A1 (es) | 1998-11-04 |
Family
ID=11372827
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP960105957A AR004413A1 (es) | 1995-12-28 | 1996-12-27 | Compuestos de tiol que poseen actividad inhibitoria de metalopeptidasa; proceso para preparar dichos derivados; composiciones farmaceuticas que loscontienen |
Country Status (30)
| Country | Link |
|---|---|
| EP (1) | EP0877740B1 (es) |
| JP (1) | JP2000502687A (es) |
| KR (1) | KR19990076809A (es) |
| CN (1) | CN1071325C (es) |
| AP (1) | AP1186A (es) |
| AR (1) | AR004413A1 (es) |
| AT (1) | ATE292123T1 (es) |
| AU (1) | AU713156B2 (es) |
| BG (1) | BG63942B1 (es) |
| BR (1) | BR9612373A (es) |
| CA (1) | CA2241414A1 (es) |
| CZ (1) | CZ204698A3 (es) |
| DE (1) | DE69634543D1 (es) |
| EA (1) | EA000991B1 (es) |
| EE (1) | EE03766B1 (es) |
| GE (1) | GEP19991871B (es) |
| IL (1) | IL124915A (es) |
| IS (1) | IS1885B (es) |
| IT (1) | IT1277737B1 (es) |
| NO (1) | NO310914B1 (es) |
| NZ (1) | NZ325785A (es) |
| OA (1) | OA10704A (es) |
| PL (1) | PL188151B1 (es) |
| RO (1) | RO119882B1 (es) |
| SK (1) | SK282977B6 (es) |
| TR (1) | TR199801229T2 (es) |
| UA (1) | UA62923C2 (es) |
| UY (1) | UY24425A1 (es) |
| WO (1) | WO1997024342A1 (es) |
| ZA (1) | ZA9610891B (es) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IT1289522B1 (it) * | 1996-12-24 | 1998-10-15 | Zambon Spa | Processo per la preparazione di eteroaril-fenilalanine |
| MY153569A (en) | 1998-01-20 | 2015-02-27 | Mitsubishi Tanabe Pharma Corp | Inhibitors of ?4 mediated cell adhesion |
| US8168616B1 (en) | 2000-11-17 | 2012-05-01 | Novartis Ag | Combination comprising a renin inhibitor and an angiotensin receptor inhibitor for hypertension |
| GB0203665D0 (en) * | 2002-02-15 | 2002-04-03 | Glaxo Group Ltd | Process |
| MY140707A (en) | 2002-02-28 | 2010-01-15 | Mitsubishi Tanabe Pharma Corp | Process for preparing a phenylalanine derivative and intermediates thereof |
| WO2003074478A1 (en) | 2002-03-05 | 2003-09-12 | Sumitomo Chemical Company, Limited | Process for the preparation of biaryl compounds |
| GB0213122D0 (en) * | 2002-06-07 | 2002-07-17 | Glaxo Group Ltd | Compounds |
| WO2003104200A1 (en) * | 2002-06-07 | 2003-12-18 | Glaxo Group Limited | N-mercaptoacyl phenyalanine derivatives, process for their preparation, and pharmaceutical compositions containing them |
| US7045653B2 (en) | 2002-12-23 | 2006-05-16 | Pfizer, Inc. | Pharmaceuticals |
| GB0327839D0 (en) | 2003-12-01 | 2003-12-31 | Novartis Ag | Organic compounds |
| EP1977741A3 (en) | 2004-03-17 | 2009-10-14 | Novartis AG | Use of renin inhibitors in therapy |
| CA2757650C (en) | 2009-04-03 | 2016-06-07 | Statoil Asa | Equipment and method for reinforcing a borehole of a well while drilling |
| CA2826623A1 (en) * | 2010-02-03 | 2011-08-11 | Meh Associates, Inc | Multiple substituted fluoromethanes as selective and bioactive isosteres |
| WO2011116115A1 (en) | 2010-03-16 | 2011-09-22 | Novartis Ag | Aliskiren composition comprising a medium chain fatty acid, their process of manufacturing |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4401677A (en) * | 1981-10-09 | 1983-08-30 | E. R. Squibb & Sons, Inc. | Enkephalinase inhibitors |
| FR2652087B1 (fr) * | 1989-09-15 | 1993-10-15 | Bioprojet Ste Civile | Derives d'amino-acides, leur procede de preparation et leurs applications therapeutiques. |
| FR2682952B1 (fr) * | 1991-10-25 | 1993-12-03 | Institut Nal Sante Recherc Medic | Nouveaux n-(mercaptoacyl) amino-acides, leur preparation et les compositions pharmaceutiques qui les contiennent. |
| IT1273455B (it) * | 1995-01-27 | 1997-07-08 | Zambon Spa | Derivati tiolici ad attivita' inibitrice delle metallopeptidasi |
-
1995
- 1995-12-28 IT IT95MI002773A patent/IT1277737B1/it active IP Right Grant
-
1996
- 1996-12-17 CN CN96199354A patent/CN1071325C/zh not_active Expired - Fee Related
- 1996-12-17 EA EA199800544A patent/EA000991B1/ru not_active IP Right Cessation
- 1996-12-17 EP EP96944583A patent/EP0877740B1/en not_active Expired - Lifetime
- 1996-12-17 NZ NZ325785A patent/NZ325785A/en unknown
- 1996-12-17 BR BR9612373A patent/BR9612373A/pt not_active Application Discontinuation
- 1996-12-17 SK SK889-98A patent/SK282977B6/sk unknown
- 1996-12-17 JP JP09524001A patent/JP2000502687A/ja not_active Ceased
- 1996-12-17 CZ CZ982046A patent/CZ204698A3/cs unknown
- 1996-12-17 KR KR1019980704934A patent/KR19990076809A/ko not_active Ceased
- 1996-12-17 DE DE69634543T patent/DE69634543D1/de not_active Expired - Lifetime
- 1996-12-17 TR TR1998/01229T patent/TR199801229T2/xx unknown
- 1996-12-17 PL PL96327580A patent/PL188151B1/pl not_active IP Right Cessation
- 1996-12-17 IL IL12491596A patent/IL124915A/en not_active IP Right Cessation
- 1996-12-17 RO RO98-01109A patent/RO119882B1/ro unknown
- 1996-12-17 EE EE9800192A patent/EE03766B1/xx not_active IP Right Cessation
- 1996-12-17 AU AU13018/97A patent/AU713156B2/en not_active Ceased
- 1996-12-17 CA CA002241414A patent/CA2241414A1/en not_active Abandoned
- 1996-12-17 GE GEAP19964406A patent/GEP19991871B/en unknown
- 1996-12-17 AT AT96944583T patent/ATE292123T1/de not_active IP Right Cessation
- 1996-12-17 WO PCT/EP1996/005663 patent/WO1997024342A1/en not_active Ceased
- 1996-12-17 AP APAP/P/1998/001264A patent/AP1186A/en active
- 1996-12-17 UA UA98074090A patent/UA62923C2/uk unknown
- 1996-12-23 ZA ZA9610891A patent/ZA9610891B/xx unknown
- 1996-12-27 UY UY24425A patent/UY24425A1/es not_active IP Right Cessation
- 1996-12-27 AR ARP960105957A patent/AR004413A1/es not_active Application Discontinuation
-
1998
- 1998-06-18 BG BG102553A patent/BG63942B1/bg unknown
- 1998-06-22 IS IS4780A patent/IS1885B/is unknown
- 1998-06-26 NO NO19982977A patent/NO310914B1/no unknown
- 1998-06-26 OA OA9800094A patent/OA10704A/en unknown
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