PE20160998A1 - Derivados de n-((3-(n-hidroxiformamido)propanamido)metil)furan-2-carboxamida - Google Patents
Derivados de n-((3-(n-hidroxiformamido)propanamido)metil)furan-2-carboxamidaInfo
- Publication number
- PE20160998A1 PE20160998A1 PE2016001113A PE2016001113A PE20160998A1 PE 20160998 A1 PE20160998 A1 PE 20160998A1 PE 2016001113 A PE2016001113 A PE 2016001113A PE 2016001113 A PE2016001113 A PE 2016001113A PE 20160998 A1 PE20160998 A1 PE 20160998A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- compounds
- formula
- hydroxiformide
- propanamide
- Prior art date
Links
- TVFIYRKPCACCNL-UHFFFAOYSA-N furan-2-carboxamide Chemical compound NC(=O)C1=CC=CO1 TVFIYRKPCACCNL-UHFFFAOYSA-N 0.000 title 1
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 title 1
- QLNJFJADRCOGBJ-UHFFFAOYSA-N propionamide Chemical compound CCC(N)=O QLNJFJADRCOGBJ-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 206010016654 Fibrosis Diseases 0.000 abstract 2
- 125000000896 monocarboxylic acid group Chemical group 0.000 abstract 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 102000004152 Bone morphogenetic protein 1 Human genes 0.000 abstract 1
- 108090000654 Bone morphogenetic protein 1 Proteins 0.000 abstract 1
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 abstract 1
- 101000637851 Homo sapiens Tolloid-like protein 1 Proteins 0.000 abstract 1
- 101000637850 Homo sapiens Tolloid-like protein 2 Proteins 0.000 abstract 1
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 abstract 1
- 102100031996 Tolloid-like protein 1 Human genes 0.000 abstract 1
- 102100031997 Tolloid-like protein 2 Human genes 0.000 abstract 1
- 125000005037 alkyl phenyl group Chemical group 0.000 abstract 1
- MDFFNEOEWAXZRQ-UHFFFAOYSA-N aminyl Chemical compound [NH2] MDFFNEOEWAXZRQ-UHFFFAOYSA-N 0.000 abstract 1
- 206010003119 arrhythmia Diseases 0.000 abstract 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 1
- 208000020832 chronic kidney disease Diseases 0.000 abstract 1
- 208000022831 chronic renal failure syndrome Diseases 0.000 abstract 1
- 230000007882 cirrhosis Effects 0.000 abstract 1
- 208000019425 cirrhosis of liver Diseases 0.000 abstract 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000004761 fibrosis Effects 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 208000036971 interstitial lung disease 2 Diseases 0.000 abstract 1
- 201000006938 muscular dystrophy Diseases 0.000 abstract 1
- 208000010125 myocardial infarction Diseases 0.000 abstract 1
- 125000004043 oxo group Chemical group O=* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- 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
- C07D307/56—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 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
- C07D307/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
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- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
- A61K31/341—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
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- 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
- A61K31/415—1,2-Diazoles
- A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
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- 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
- A61K31/428—Thiazoles condensed with carbocyclic rings
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/443—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
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- A61K31/66—Phosphorus compounds
- A61K31/665—Phosphorus compounds having oxygen as a ring hetero atom, e.g. fosfomycin
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- 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
- C07D307/10—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 substituted hydrocarbon radicals attached to ring carbon atoms
- C07D307/12—Radicals substituted by oxygen atoms
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- 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
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- C—CHEMISTRY; METALLURGY
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- 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
- C07D405/04—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 directly linked by a ring-member-to-ring-member bond
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- C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
- C07D407/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- 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
- C07D417/04—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 directly linked by a ring-member-to-ring-member bond
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- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/655—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms
- C07F9/65515—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms the oxygen atom being part of a five-membered ring
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- Orthopedic Medicine & Surgery (AREA)
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- Dermatology (AREA)
- Rheumatology (AREA)
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Abstract
Se refiere a compuestos de Formula (I) o sales de los mismos, donde R1 es H, alquilo C1C4 o hidroxialquilo C1C4; R2 es H, alquilo C1C11, alquil (C1C3)cicloalquilo (C3C6), alquil (C1C3)fenilo, entre otros; y R3 es: (a) fenilo opcionalmente sustituido con 1 a 3 grupos seleccionados independientemente entre alquilo C1C6, ciclopropilo, CONH2, NH2, SH, COOH, entre otros; o (b) heteroarilo opcionalmente sustituido con 1 o 2 grupos seleccionados independientemente entre alquilo C1C4, alcoxi C1C4, oxo, COOH, entre otros. Tambien se refiere a composiciones y combinaciones farmaceuticas comprendiendo dichos compuestos de Formula (I). Dichos compuestos de Formula (I) son inhibidores de BMP1, TLL1 o TLL2, por lo cual son utiles en el tratamiento de enfermedades asociadas con fibrosis (infarto de miocardio, arritmias cardiacas, insuficiencia renal cronica, fibrosis pulmonar idiopatica, cirrosis, entre otros), distrofias musculares, entre otras
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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US201461925848P | 2014-01-10 | 2014-01-10 |
Publications (1)
Publication Number | Publication Date |
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PE20160998A1 true PE20160998A1 (es) | 2016-10-26 |
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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PE2016001113A PE20160998A1 (es) | 2014-01-10 | 2015-01-09 | Derivados de n-((3-(n-hidroxiformamido)propanamido)metil)furan-2-carboxamida |
Country Status (21)
Country | Link |
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US (2) | US10450288B2 (es) |
EP (1) | EP3092233A1 (es) |
JP (2) | JP2017507915A (es) |
KR (1) | KR20160106684A (es) |
CN (2) | CN106103431B (es) |
AU (1) | AU2015205370B2 (es) |
BR (1) | BR112016016130A2 (es) |
CA (1) | CA2936467A1 (es) |
CL (1) | CL2016001746A1 (es) |
CR (1) | CR20160316A (es) |
DO (1) | DOP2016000170A (es) |
EA (1) | EA031654B1 (es) |
IL (1) | IL246653A0 (es) |
MA (1) | MA39171A1 (es) |
MX (1) | MX2016009064A (es) |
PE (1) | PE20160998A1 (es) |
PH (1) | PH12016501349A1 (es) |
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JP2017507915A (ja) * | 2014-01-10 | 2017-03-23 | グラクソスミスクライン、インテレクチュアル、プロパティー、(ナンバー2)、リミテッドGlaxosmithkline Intellectual Property (No.2) Limited | ヒドロキシホルムアミド誘導体およびそれらの使用 |
WO2017006295A1 (en) * | 2015-07-08 | 2017-01-12 | Glaxosmithkline Intellectual Property (No.2) Limited | Hydroxy formamide derivatives and their use |
JP2018525353A (ja) | 2015-07-09 | 2018-09-06 | グラクソスミスクライン、インテレクチュアル、プロパティー、(ナンバー2)、リミテッドGlaxosmithkline Intellectual Property (No.2) Limited | Bmp1、tll1および/またはtll2の阻害剤としての使用するための、n−ヒドロキシホルムアミド化合物およびそれらを含んでなる組成物 |
CN106699604B (zh) * | 2017-01-09 | 2019-01-01 | 四川同晟生物医药有限公司 | 一种沙库比曲及其中间体的制备方法 |
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CN114195638B (zh) * | 2021-12-28 | 2023-07-14 | 青岛科技大学 | 一种邻羟基苯甲酸苯酯的制备方法 |
CN114230463B (zh) * | 2021-12-28 | 2024-06-21 | 青岛科技大学 | 一种邻羟基苯甲酸苯酯的后处理方法 |
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- 2015-01-09 CN CN201580013152.8A patent/CN106103431B/zh not_active Expired - Fee Related
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- 2015-01-09 AU AU2015205370A patent/AU2015205370B2/en not_active Ceased
- 2015-01-09 UA UAA201608690A patent/UA118278C2/uk unknown
- 2015-01-09 EP EP15702008.2A patent/EP3092233A1/en not_active Withdrawn
- 2015-01-09 MA MA39171A patent/MA39171A1/fr unknown
- 2015-01-09 CN CN201910119933.5A patent/CN109970797A/zh active Pending
- 2015-01-09 KR KR1020167021496A patent/KR20160106684A/ko not_active Application Discontinuation
- 2015-01-09 BR BR112016016130A patent/BR112016016130A2/pt not_active Application Discontinuation
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Also Published As
Publication number | Publication date |
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SG11201605539SA (en) | 2016-08-30 |
KR20160106684A (ko) | 2016-09-12 |
TW201620887A (zh) | 2016-06-16 |
UA118278C2 (uk) | 2018-12-26 |
CR20160316A (es) | 2016-09-19 |
MA39171A1 (fr) | 2017-07-31 |
IL246653A0 (en) | 2016-08-31 |
US20200095217A1 (en) | 2020-03-26 |
PH12016501349A1 (en) | 2016-08-15 |
MX2016009064A (es) | 2017-01-23 |
CN106103431A (zh) | 2016-11-09 |
DOP2016000170A (es) | 2016-10-30 |
WO2015104684A1 (en) | 2015-07-16 |
AU2015205370A1 (en) | 2016-07-21 |
CL2016001746A1 (es) | 2017-06-02 |
EA201691412A1 (ru) | 2016-12-30 |
BR112016016130A2 (pt) | 2017-08-08 |
JP2017507915A (ja) | 2017-03-23 |
AU2015205370B2 (en) | 2017-11-30 |
CA2936467A1 (en) | 2015-07-16 |
CN109970797A (zh) | 2019-07-05 |
JP2020011968A (ja) | 2020-01-23 |
CN106103431B (zh) | 2019-03-15 |
EA031654B1 (ru) | 2019-02-28 |
US10450288B2 (en) | 2019-10-22 |
US20160340328A1 (en) | 2016-11-24 |
EP3092233A1 (en) | 2016-11-16 |
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