CA2776849A1 - Novel heterocyclic acrylamides and their use as pharmaceuticals - Google Patents

Novel heterocyclic acrylamides and their use as pharmaceuticals Download PDF

Info

Publication number
CA2776849A1
CA2776849A1 CA2776849A CA2776849A CA2776849A1 CA 2776849 A1 CA2776849 A1 CA 2776849A1 CA 2776849 A CA2776849 A CA 2776849A CA 2776849 A CA2776849 A CA 2776849A CA 2776849 A1 CA2776849 A1 CA 2776849A1
Authority
CA
Canada
Prior art keywords
naphthyridin
dihydro
mmol
azetidin
oxo
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Abandoned
Application number
CA2776849A
Other languages
English (en)
French (fr)
Inventor
Vincent Gerusz
Sonia Escaich
Mayalen Oxoby
Alexis Denis
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
FAB PHARMA Sas
Original Assignee
FAB PHARMA Sas
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by FAB PHARMA Sas filed Critical FAB PHARMA Sas
Publication of CA2776849A1 publication Critical patent/CA2776849A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • 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
    • A61K31/435—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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A61P31/06—Antibacterial agents for tuberculosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06—Antimalarials
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D207/12—Oxygen or sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/20—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
    • C07D211/22—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms by oxygen atoms
    • 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
    • C07D213/73—Unsubstituted amino or imino radicals
    • 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
    • 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
    • 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
    • C07D333/12—Radicals substituted by halogen atoms or nitro or nitroso radicals
    • 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
    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/20—Spiro-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Pulmonology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
CA2776849A 2009-11-18 2010-11-17 Novel heterocyclic acrylamides and their use as pharmaceuticals Abandoned CA2776849A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US26230909P 2009-11-18 2009-11-18
US61/262,309 2009-11-18
PCT/EP2010/067647 WO2011061214A1 (en) 2009-11-18 2010-11-17 Novel heterocyclic acrylamides and their use as pharmaceuticals

Publications (1)

Publication Number Publication Date
CA2776849A1 true CA2776849A1 (en) 2011-05-26

Family

ID=44059228

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2776849A Abandoned CA2776849A1 (en) 2009-11-18 2010-11-17 Novel heterocyclic acrylamides and their use as pharmaceuticals

Country Status (16)

Country Link
US (3) US8846711B2 (enExample)
EP (1) EP2501693B1 (enExample)
JP (1) JP5816629B2 (enExample)
KR (1) KR20130010456A (enExample)
CN (1) CN102656158B (enExample)
AU (1) AU2010320963B2 (enExample)
BR (1) BR112012011793A2 (enExample)
CA (1) CA2776849A1 (enExample)
DK (1) DK2501693T3 (enExample)
ES (1) ES2526567T3 (enExample)
IL (1) IL218934A0 (enExample)
MX (1) MX2012005759A (enExample)
NZ (1) NZ599444A (enExample)
PL (1) PL2501693T3 (enExample)
WO (1) WO2011061214A1 (enExample)
ZA (1) ZA201202489B (enExample)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013190384A1 (en) * 2012-06-19 2013-12-27 Affinium Pharmaceuticals, Inc. Prodrug derivatives of (e)-n-methyl-n-((3-methylbenzofuran-2-yl)methyl)-3-(7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)acrylamide
US8895545B2 (en) 2006-07-20 2014-11-25 Debiopharm International Sa Acrylamide derivatives as Fab I inhibitors
US10751351B2 (en) 2016-02-26 2020-08-25 Debiopharm International S.A. Medicament for treatment of diabetic foot infections
US12403131B2 (en) 2019-02-14 2025-09-02 Debiopharm International S.A. Afabicin formulation, method for making the same and uses thereof
US12414958B2 (en) 2019-06-14 2025-09-16 Debiopharm International S.A. Medicament and use thereof for treating bacterial infections involving biofilm

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2776849A1 (en) 2009-11-18 2011-05-26 Fab Pharma S.A.S. Novel heterocyclic acrylamides and their use as pharmaceuticals
JO3611B1 (ar) * 2011-08-10 2020-08-27 Janssen Sciences Ireland Uc سايكلو بنتا (سي (بيرول 4,3 ثاني هيدرو 1 hمستبدله [8,1] نافثيريدينونات مضادة للجراثيم
CN104039782A (zh) * 2011-08-10 2014-09-10 爱尔兰詹森研发公司 抗菌的高哌啶基取代的3,4二氢1h[1,8]萘啶酮类
WO2013021052A1 (en) * 2011-08-10 2013-02-14 Janssen R&D Ireland Antibacterial piperidinyl substituted 3,4-dihydro-1h-[1,8]naphthyridinones
EP2758376A4 (en) 2011-09-19 2015-04-29 Vitas Pharma Res Private Ltd HETEROCYCLIC COMPOUNDS AS INHIBITORS OF FATTY ACID BIOSYNTHESIS FOR BACTERIAL INFECTIONS
US9062075B2 (en) 2011-12-02 2015-06-23 Aurigene Discovery Technologies Limited Tetrahydropyridine derivatives as FabI inhibitors
SG11201402409UA (en) 2011-12-02 2014-10-30 Aurigene Discovery Tech Ltd Substituted pyridine derivatives as fabi inhibitors
AR090880A1 (es) 2012-04-30 2014-12-10 Janssen R & D Ireland Derivados de pirimidina
WO2014023814A1 (en) * 2012-08-10 2014-02-13 Janssen R&D Ireland New antibacterial compounds
JP6250668B2 (ja) * 2012-08-10 2017-12-20 ヤンセン・サイエンシズ・アイルランド・ユーシー 新しい抗菌化合物
WO2014072930A2 (en) * 2012-11-09 2014-05-15 Aurigene Discovery Technologies Limited Fused pyridine derivatives as antibacterial agents
MY187891A (en) * 2013-06-04 2021-10-27 Aurigene Discovery Tech Ltd Tetrahydropyridine derivatives as fabi inhibitors
CN104292142B (zh) * 2013-07-17 2019-05-14 天津大地康和医药技术有限公司 一种n-芳基杂环丁烷脱芳基方法
WO2015071780A1 (en) * 2013-11-12 2015-05-21 Aurigene Discovery Technologies Limited Alkylidine substituted heterocyclyl derivatives as anti-bacterial agents
CN104529854B (zh) * 2015-01-14 2016-10-05 武汉金联药业有限公司 一种取代氮杂环丁烷类医药中间体化合物的合成方法
RU2766579C2 (ru) 2015-07-02 2022-03-15 ХОРАЙЗОН ОРФАН ЭлЭлСи Цистеаминдиоксигеназа-резистентные аналоги цистеамина и их применение
CN108440523A (zh) * 2018-04-23 2018-08-24 爱斯特（成都）生物制药股份有限公司 一种合成6-溴-3,4-二氢-1h-[1,8]萘啶-2-酮的新方法
CN114351128B (zh) * 2021-12-10 2022-12-13 江阴纳力新材料科技有限公司 镀铜液添加剂、镀铜液、镀铜薄膜及其制备方法、负极集流体、锂电池

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1020864C (zh) * 1988-09-14 1993-05-26 中国科学院上海有机化学研究所 醛的烯基化反应的催化剂及其应用
TW224042B (enExample) * 1992-04-04 1994-05-21 Basf Ag
WO1997033870A1 (en) * 1996-03-15 1997-09-18 Ss Pharmaceutical Co., Ltd. Novel pyridine derivatives and medicines containing the same as active ingredient
ES2320316T3 (es) * 1996-05-01 2009-05-21 Ortho-Mcneil Pharmaceutical, Inc. Derivados carboxamida de pirrolidina, piperidina y hexahidroazepina utiles en el tratamiento de trastornos tromboticos.
ES2231275T3 (es) 1999-10-08 2005-05-16 Affinium Pharmaceuticals, Inc. Inhibidores de fab i.
JP4387804B2 (ja) 2001-04-06 2009-12-24 アフィニアム・ファーマシューティカルズ・インコーポレイテッド ＦａｂＩ阻害剤
JP2004099499A (ja) * 2002-09-09 2004-04-02 Sanei Gen Ffi Inc 抗微生物剤
PT1575951E (pt) 2002-12-06 2014-09-15 Debiopharm Int Sa Compostos heterocíclicos, métodos para os preparar e sua utilização em terapia
US8450307B2 (en) 2004-06-04 2013-05-28 Affinium Pharmaceuticals, Inc. Therapeutic agents, and methods of making and using the same
PL383715A1 (pl) * 2005-01-26 2008-05-12 Allergan, Inc. Amidy kwasu 3-arylo-3-hydroksy-2-amino-propionowego, amidy kwasu 3-heteroarylo-3-hydroksy-2-amino-propionowego i ich związki pokrewne posiadające aktywność przeciwbólową i/lub pobudzającą odporność
US20090156578A1 (en) 2005-12-05 2009-06-18 PAULS Henry 3-Heterocyclylacrylamide Compounds as Fab I Inhibitors and Antibacterial Agents
WO2007086584A1 (ja) * 2006-01-30 2007-08-02 Meiji Seika Kaisha, Ltd. 新規ＦａｂＫおよびＦａｂＩ／Ｋ阻害剤
EP1845087A1 (en) 2006-04-14 2007-10-17 Mutabilis SA Hydroxyphenyl derivatives and biological applications thereof
EP2054422B1 (en) 2006-07-20 2017-06-14 Debiopharm International SA Acrylamide derivatives as fab i inhibitors
EP1942104A1 (en) 2006-12-20 2008-07-09 sanofi-aventis Heteroarylcyclopropanecarboxamides and their use as pharmaceuticals
EP1939180A1 (en) 2006-12-20 2008-07-02 sanofi-aventis Heteroarylacrylamides and their use as pharmaceuticals for the stimulation of the expression of endothelial NO synthase
WO2008098374A1 (en) 2007-02-16 2008-08-21 Affinium Pharmaceuticals, Inc. Salts, prodrugs and polymorphs of fab i inhibitors
WO2009110002A1 (en) * 2008-03-05 2009-09-11 Council Of Scientific & Industrial Research Novel efflux pump inhibitors
JP2012102018A (ja) * 2009-03-03 2012-05-31 Astellas Pharma Inc アミド化合物
CA2776849A1 (en) 2009-11-18 2011-05-26 Fab Pharma S.A.S. Novel heterocyclic acrylamides and their use as pharmaceuticals

Cited By (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8895545B2 (en) 2006-07-20 2014-11-25 Debiopharm International Sa Acrylamide derivatives as Fab I inhibitors
WO2013190384A1 (en) * 2012-06-19 2013-12-27 Affinium Pharmaceuticals, Inc. Prodrug derivatives of (e)-n-methyl-n-((3-methylbenzofuran-2-yl)methyl)-3-(7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)acrylamide
US8901105B2 (en) 2012-06-19 2014-12-02 Debiopharm International Sa Prodrug derivatives of (E)-N-methyl-N-((3-M ethylbenzofuran-2-yl)methyl)-3-(7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)acrylamide
CN104684922A (zh) * 2012-06-19 2015-06-03 德彪药业国际股份公司 (e)-n-甲基-n-((3-甲基苯并呋喃-2-基)甲基)-3-(7-氧代-5,6,7,8-四氢-1,8-萘啶-3-基)丙烯酰胺的前药衍生物
AU2013279021B2 (en) * 2012-06-19 2016-09-08 Debiopharm International Sa Prodrug derivatives of (E)-N-methyl-N-((3-methylbenzofuran-2-yl)methyl)-3-(7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)acrylamide
CN104684922B (zh) * 2012-06-19 2016-10-26 德彪药业国际股份公司 (e)-n-甲基-n-((3-甲基苯并呋喃-2-基)甲基)-3-(7-氧代-5,6,7,8-四氢-1,8-萘啶-3-基)丙烯酰胺的前药衍生物
AU2013279021C1 (en) * 2012-06-19 2017-03-16 Debiopharm International Sa Prodrug derivatives of (E)-N-methyl-N-((3-methylbenzofuran-2-yl)methyl)-3-(7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)acrylamide
EA028136B1 (ru) * 2012-06-19 2017-10-31 Дибиофарм Интернешнл Са Пролекарственные производные (е)-n-метил-n-((3-метилбензофуран-2-ил)метил)-3-(7-оксо-5,6,7,8-тетрагидро-1,8-нафтиридин-3-ил)акриламида
US10035813B2 (en) 2012-06-19 2018-07-31 Debiopharm International Sa Prodrug derivatives of (E)-N-methyl-N-((3-methylbenzofuran-2-yl)methyl)-3-(7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)acrylamide
US10751351B2 (en) 2016-02-26 2020-08-25 Debiopharm International S.A. Medicament for treatment of diabetic foot infections
US12403131B2 (en) 2019-02-14 2025-09-02 Debiopharm International S.A. Afabicin formulation, method for making the same and uses thereof
US12414958B2 (en) 2019-06-14 2025-09-16 Debiopharm International S.A. Medicament and use thereof for treating bacterial infections involving biofilm

Also Published As

Publication number Publication date
US20150232466A1 (en) 2015-08-20
CN102656158A (zh) 2012-09-05
KR20130010456A (ko) 2013-01-28
ZA201202489B (en) 2013-02-27
EP2501693B1 (en) 2014-09-17
CN102656158B (zh) 2015-02-11
US8846711B2 (en) 2014-09-30
AU2010320963B2 (en) 2015-07-09
JP2013511486A (ja) 2013-04-04
BR112012011793A2 (pt) 2019-09-24
EP2501693A1 (en) 2012-09-26
US9051321B2 (en) 2015-06-09
US20120277207A1 (en) 2012-11-01
DK2501693T3 (en) 2014-12-08
IL218934A0 (en) 2012-07-31
MX2012005759A (es) 2012-10-03
WO2011061214A1 (en) 2011-05-26
JP5816629B2 (ja) 2015-11-18
ES2526567T3 (es) 2015-01-13
US20140357617A1 (en) 2014-12-04
US9321769B2 (en) 2016-04-26
AU2010320963A1 (en) 2012-05-03
HK1176358A1 (en) 2013-07-26
NZ599444A (en) 2014-02-28
PL2501693T3 (pl) 2015-03-31

Similar Documents

Publication Publication Date Title
AU2010320963B2 (en) Novel heterocyclic acrylamides and their use as pharmaceuticals
CN114867727B (zh) Tau蛋白靶向化合物及相关使用方法
CN110234646B (zh) 靶向PROTAC的Tau蛋白及相关使用方法
CN112805067B (zh) Pad酶的吲哚及氮杂吲哚抑制剂
AU2008254270B2 (en) Spiroindalones
CN110869360A (zh) 作为rock抑制剂的苯乙酰胺类
US9062002B2 (en) Substituted pyridine derivatives as FabI inhibitors
AU2006287976A1 (en) Novel diazaspiroalkanes and their use for treatment of CCR8 mediated diseases
MX2010007430A (es) Piridoindoles (1-azinona)-sustituidos como antagonistas de la hormona de concentracion melanina humana.
JP2022527679A (ja) インターフェロン遺伝子の刺激因子（ｓｔｉｎｇ）の次世代モジュレーター
US10000501B2 (en) Inhibitors of HIF prolyl hydroxylase
AU2010333024B2 (en) MK2 inhibitors
CN105492434A (zh) Rorc2抑制剂及其使用方法
CN117126231A (zh) 拟肽类stat蛋白降解剂、组合物及其应用
TW201833113A (zh) 作為Ｐ１３Ｋδ抑制劑之咪唑并［１，５－Ａ］吡衍生物
CN117321046A (zh) 基于吲唑的化合物和相关使用方法
WO2014072930A2 (en) Fused pyridine derivatives as antibacterial agents
CN114805341B (zh) 一类芳杂环类化合物及其制备方法和用途
HK1176358B (en) Aza heterocyclic acrylamides and their use as bactericides
CN120957981A (zh) 基于2,4-二苯胺嘧啶的Aurora-A激酶选择性降解诱导化合物
CN117813086A (zh) 作为ccr6抑制剂的芳基磺酰基(羟基)哌啶
HK1219093B (en) Heterobicycloaryl rorc2 inhibitors and methods of use thereof

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20151117

FZDE Discontinued

Effective date: 20180313