[go: up one dir, main page]

CY1120066T1 - Ενωση κινολονης - Google Patents

Ενωση κινολονης

Info

Publication number
CY1120066T1
CY1120066T1 CY20181100309T CY181100309T CY1120066T1 CY 1120066 T1 CY1120066 T1 CY 1120066T1 CY 20181100309 T CY20181100309 T CY 20181100309T CY 181100309 T CY181100309 T CY 181100309T CY 1120066 T1 CY1120066 T1 CY 1120066T1
Authority
CY
Cyprus
Prior art keywords
alkyl
optionally substituted
clostridium difficile
halogen atoms
hydrogen atom
Prior art date
Application number
CY20181100309T
Other languages
English (en)
Inventor
Mamuti ABUDUSAIMI
Fangguo YE
Jiangqin SUN
Hisashi Miyamoto
Jay-Fei CHENG
Daisuke Oka
Original Assignee
Otsuka Pharmaceutical Co., Ltd.
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 Otsuka Pharmaceutical Co., Ltd. filed Critical Otsuka Pharmaceutical Co., Ltd.
Publication of CY1120066T1 publication Critical patent/CY1120066T1/el

Links

Classifications

    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12—Antidiarrhoeals
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/54—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
    • C07D215/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3 with oxygen atoms in position 4
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D401/10—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 carbon chain containing aromatic rings
    • 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
    • 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
    • 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
    • C07D409/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • 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
    • C07D413/10—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 linked by a carbon chain containing aromatic rings
    • 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
    • C07D413/12—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 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D417/04—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
    • 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
    • C07D417/14—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 three or more hetero rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/06—Peri-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/06—Peri-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Quinoline Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Η παρούσα εφεύρεση παρέχει μια ένωση η οποία αντιπροσωπεύεται από τον τύπο (Ι) όπου Χ είναι ένα άτομο υδρογόνου ή ένα άτομο φθορίου˙ R είναι ένα άτομο υδρογόνου ή αλκύλιο˙ R1 είναι (1) κυκλοπροπύλιο κατ' επιλογή υποκατεστημένο με 3 άτομα αλογόνου ή (2) φαινύλιο κατ' επιλογή υποκατεστημένο με 1 έως 3 άτομα αλογόνου˙ R2 είναι αλκύλιο, αλκοξύλιο, αλογονοαλκοξυ, ένα άτομο αλογόνου, κυανο, κλπ.˙ και R3 είναι 7-οξο-7,8-διυδρο-1,8-ναφθυριδινύλιο, 3-πυριδύλιο, κλπ., ή ένα άλας αυτής. Η ένωση της παρούσας εφεύρεσης έχει εξαιρετική αντιμικροβιακή δραστικότητα έναντι του Clostridium difficile και είναι χρήσιμη για την πρόληψη ή αντιμετώπιση εντερικής μόλυνσης όπως διάρροιας η οποία σχετίζεται με Clostridium difficile.
CY20181100309T 2011-08-31 2018-03-14 Ενωση κινολονης CY1120066T1 (el)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2011001477 2011-08-31
CN2012001044 2012-08-06
PCT/CN2012/080753 WO2013029548A1 (en) 2011-08-31 2012-08-30 Quinolone compound

Publications (1)

Publication Number Publication Date
CY1120066T1 true CY1120066T1 (el) 2018-12-12

Family

ID=47755336

Family Applications (1)

Application Number Title Priority Date Filing Date
CY20181100309T CY1120066T1 (el) 2011-08-31 2018-03-14 Ενωση κινολονης

Country Status (30)

Country Link
US (7) US9067887B2 (el)
EP (2) EP3318557A3 (el)
JP (4) JP6106174B2 (el)
KR (3) KR101560073B1 (el)
CN (3) CN105017151B (el)
AR (1) AR087747A1 (el)
AU (2) AU2012303954B2 (el)
BR (1) BR112014000665B8 (el)
CA (1) CA2845459C (el)
CO (1) CO6920292A2 (el)
CY (1) CY1120066T1 (el)
DK (1) DK2751083T3 (el)
EA (2) EA030867B1 (el)
ES (1) ES2660973T3 (el)
HK (4) HK1198828A1 (el)
HR (1) HRP20180483T1 (el)
HU (1) HUE036301T2 (el)
IL (1) IL230559B (el)
LT (1) LT2751083T (el)
MX (3) MX371361B (el)
MY (1) MY165004A (el)
NO (1) NO2751083T3 (el)
PH (1) PH12014500130B1 (el)
PL (1) PL2751083T3 (el)
PT (1) PT2751083T (el)
SG (3) SG2014004162A (el)
SI (1) SI2751083T1 (el)
TW (3) TW201718506A (el)
WO (1) WO2013029548A1 (el)
ZA (1) ZA201402326B (el)

Families Citing this family (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9403818B2 (en) * 2011-02-01 2016-08-02 Emergent Product Development Gaithersburg Inc. Antimicrobial 4-oxoquinolizines
PH12014500130B1 (en) * 2011-08-31 2018-07-04 Otsuka Pharmaceutical Co Ltd Quinolone compound
UA119848C2 (uk) 2013-03-15 2019-08-27 Інсайт Холдинґс Корпорейшн Трициклічні гетероцикли як інгібітори білків бет
AR096135A1 (es) 2013-05-02 2015-12-09 Actelion Pharmaceuticals Ltd Derivados de la quinolona
WO2015006193A1 (en) 2013-07-08 2015-01-15 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
CN104513253A (zh) 2013-10-01 2015-04-15 南京波尔泰药业科技有限公司 用于治疗增殖性疾病的大环化合物
WO2015081203A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
US9315501B2 (en) 2013-11-26 2016-04-19 Incyte Corporation Bicyclic heterocycles as BET protein inhibitors
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
EP3674302B1 (en) 2014-04-23 2023-03-01 Incyte Holdings Corporation 1h-pyrrolo[2,3-c]pyridin-7(6h)-ones and pyrazolo[3,4-c]pyridin-7(6h)-ones as inhibitors of bet proteins
ES2855225T3 (es) 2014-09-15 2021-09-23 Incyte Corp Heterociclos tricíclicos para su uso como inhibidores de proteínas BET
US10456379B2 (en) 2014-12-04 2019-10-29 Procomcure Biotech Gmbh Imidazole-based antimicrobial agents
WO2016087615A1 (en) 2014-12-04 2016-06-09 Procomcure Biotech Gmbh Novel imidazole-based heterocyclic compounds
WO2017017631A2 (en) * 2015-07-28 2017-02-02 Vyome Biosciences Pvt. Ltd. Antibacterial therapeutics and prophylactics
AR106520A1 (es) 2015-10-29 2018-01-24 Incyte Corp Forma sólida amorfa de un inhibidor de proteína bet
CN109153683A (zh) * 2015-12-29 2019-01-04 免疫目标公司 作为NF-κB抑制剂的2H-色烯并[2,3-D]嘧啶-2,4(3H)-二酮
KR102643344B1 (ko) 2016-06-20 2024-03-07 인사이트 코포레이션 Bet 저해제의 결정질 고체 형태
WO2018013430A2 (en) 2016-07-12 2018-01-18 Arisan Therapeutics Inc. Heterocyclic compounds for the treatment of arenavirus infection
KR102537749B1 (ko) 2017-06-14 2023-05-26 산요 시키소 가부시키가이샤 안료 분산체 및 그것을 포함하는 착색 조성물
CN107964020B (zh) * 2018-01-11 2019-07-05 河南大学 1-(n-左氧氟沙星酰胺基)-6-氟-7-哌嗪萘啶酮酸化合物及其制备方法和应用
CN108191889B (zh) * 2018-01-11 2019-06-07 河南大学 1-(n-氧氟沙星酰胺基)-6-氟-7-哌嗪萘啶酮酸化合物及其制备方法和应用
KR20210046015A (ko) 2018-08-13 2021-04-27 오츠카 세이야쿠 가부시키가이샤 염증성 장 질환의 치료를 위한 신규 의약
WO2020163816A1 (en) * 2019-02-08 2020-08-13 Frequency Therapeutics, Inc. Quinolin-4-one and 4(1h)-cinnolinone compounds and methods of using same
CN110551124B (zh) * 2019-06-14 2021-01-08 山东省联合农药工业有限公司 一种喹诺酮类化合物或其农药学上可接受的盐及其制备方法与用途
CN112624970B (zh) * 2019-09-24 2022-10-28 南开大学 8位芳基取代喹啉氮氧化物在抗植物病毒及杀菌方面的应用
CN112939860B (zh) * 2019-11-11 2022-11-11 山东畜牧兽医职业学院 一种治疗耐药性革兰阴阳性菌的化合物及其制备方法
JP2023012559A (ja) 2020-02-10 2023-01-26 大塚製薬株式会社 新規炎症性疾患治療剤
JP2023012557A (ja) 2020-02-10 2023-01-26 大塚製薬株式会社 新規肝性脳症治療剤
JP2023012558A (ja) 2020-02-10 2023-01-26 大塚製薬株式会社 腸内細菌叢構成比率調整剤
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
IL316564A (en) * 2022-04-29 2024-12-01 Beigene Ltd 7-(Pyrimidine-4-yl)quinolin-4-(1H)-one compounds are being developed as cyclin-dependent kinase inhibitors.
CN119343138A (zh) * 2022-07-11 2025-01-21 大塚制药株式会社 包含喹诺酮类化合物的肠易激综合征用药物组合物
WO2024128235A1 (ja) * 2022-12-13 2024-06-20 大塚製薬株式会社 キノロン化合物の製造方法
WO2024138292A1 (zh) * 2022-12-26 2024-07-04 深圳阿尔法分子科技有限责任公司 一种新型具有抗菌和抗癌功能的苯基喹诺酮类化合物及其制备
CN118255716A (zh) * 2022-12-26 2024-06-28 深圳阿尔法分子科技有限责任公司 一种新型具有抗菌和抗癌功能的苯基喹诺酮类化合物及其制备

Family Cites Families (41)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5781486A (en) * 1980-11-10 1982-05-21 Otsuka Pharmaceut Co Ltd Benzo(ij)quinolidine-2-carboxylic acid derivative
JPS5872589A (ja) * 1981-10-28 1983-04-30 Dai Ichi Seiyaku Co Ltd ピリド〔１，２，３−ｄｅ〕〔１，４〕ベンゾオキサジン誘導体
US4443447A (en) 1982-10-25 1984-04-17 Riker Laboratories, Inc. Phenyl-substituted tricyclic antibacterial agents
ZA859283B (en) 1984-12-06 1987-07-29 Pfizer Substituted dihydroquinolone carboxylic acids and anti-bacterial compositions containing them
US4623650A (en) * 1984-12-06 1986-11-18 Pfizer Inc. Antibiotic derivatives of 7-phenyl-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids
US4636506A (en) * 1984-12-06 1987-01-13 Pfizer, Inc. 7-heterocyclic-1,4-dihydroquinolones
US4797490A (en) * 1984-12-06 1989-01-10 Pfizer Inc. Process for the preparation of 3-(2'-fluorophenyl)pyridine
JPS62228063A (ja) * 1985-12-27 1987-10-06 Sankyo Co Ltd キノリンカルボン酸誘導体
IT1197841B (it) * 1986-10-14 1988-12-06 Mediolanum Farmaceutici Srl Derivati pirido-benzotiazinici ad attivita' antibatterica ed a lunga durata di azione
US4929613A (en) 1987-08-26 1990-05-29 Warner-Lambert Company Antibacterial agents
US5081254A (en) 1987-08-26 1992-01-14 Warner-Lambert Company Antibacterial agents
US5075319A (en) * 1987-09-08 1991-12-24 Sterling Drug Inc. Pyridinyl-quinolone compounds, their preparation and use
US4839355A (en) * 1987-09-09 1989-06-13 Sterling Drug Inc. Tricyclic-pyridinylquinoline compounds, their preparation and use
WO1989005643A1 (en) * 1987-12-18 1989-06-29 Pfizer Inc. Heterocyclic-substituted quinoline-carboxylic acids
DE3816119A1 (de) * 1988-05-11 1989-11-23 Bayer Ag 7-substituierte chinolon- und naphthyridoncarbonsaeure-derivate
JPH0366301A (ja) 1989-08-03 1991-03-22 Asahi Corp 靴底射出成形金型
KR910009333B1 (ko) * 1989-10-23 1991-11-11 재단법인 한국화학연구소 항균작용을 갖는 퀴놀린계 화합물과 그의 제조방법
JP2613139B2 (ja) * 1990-07-19 1997-05-21 エスエス製薬 株式会社 キノロンカルボン酸誘導体
US5308843A (en) * 1990-09-11 1994-05-03 Sterling Drug Inc. Method of inhibiting mammalian topoisomerase II and malignant cell growth in mammals, with substituted (S)-3-methyl-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4 ]-benzoxazine(and-benzothiazine)-6-carboxylic acids
CA2099591C (en) 1990-12-05 2002-11-12 Rajeshwar Singh 7-substituted-6-fluoro-1,4-dihydro-4-oxo-quinoline-3- carboxylic acid compounds useful as antibacterial agents
US5935952A (en) 1994-08-12 1999-08-10 Toyama Chemical Co., Ltd. Quinolone- or naphthylidone-carboxylic acid derivates or their salts
WO1999000393A1 (en) 1997-06-26 1999-01-07 Dong Wha Pharmaceutical Industrial Co., Ltd. Quinolone carboxylic acid derivatives
WO1999003465A1 (fr) 1997-07-16 1999-01-28 Eisai Co., Ltd. Antibiotiques contenant des derives indole
JP4370002B2 (ja) 1997-08-08 2009-11-25 富山化学工業株式会社 キノロンカルボン酸誘導体またはその塩
DE69841563D1 (de) 1997-10-27 2010-04-29 Toyama Chemical Co Ltd Salz eines 7-isoindolinchinoloncarbonsäure-derivats, sein monohydrat und zusammensetzungen die diese als wirksamen bestandteil enthalten
US6335447B1 (en) 1998-04-06 2002-01-01 Toyama Chemical Co., Ltd. Quinolonecarboxylic acid derivatives or salts thereof
JP2000229946A (ja) * 1998-12-10 2000-08-22 Toyama Chem Co Ltd キノロンカルボン酸の製造法およびその中間体
AU2325300A (en) * 1999-02-05 2000-08-25 Toyama Chemical Co. Ltd. Tricyclic quinolonecarboxylic acid derivatives or salts thereof
US20020049223A1 (en) * 1999-11-05 2002-04-25 Elmore Steven W. Quinoline and naphthyridine carboxylic acid antibacterials
DE10026903A1 (de) * 2000-06-03 2002-01-10 Cpc Cellular Process Chemistry Verfahren zur Herstellung von Chinolon-3-carbonsäuren
WO2002009758A2 (en) * 2000-08-01 2002-02-07 Wockhardt Limited Inhibitors of cellular efflux pumps of microbes
JP2003104988A (ja) * 2001-09-28 2003-04-09 Sato Pharmaceutical Co Ltd 抗菌剤として有用なキノロン誘導体
US7012144B2 (en) 2001-12-31 2006-03-14 Korea Research Institute Of Chemical Technology Quinolone carboxylic acid derivatives
JP3885679B2 (ja) * 2002-06-28 2007-02-21 株式会社日立製作所 電子機器
US20070224282A1 (en) * 2005-03-28 2007-09-27 Toyama Chemical Co., Ltd. Fine Dispersion of Sparingly Soluble Drug and Process for Producing the Same
CN101341249B (zh) * 2006-02-17 2013-07-24 森永乳业株式会社 用于检测微生物的方法和用于检测微生物的试剂盒
CN101168541A (zh) * 2006-10-26 2008-04-30 孙飘扬 喹诺酮羧酸类衍生物及其制备方法和药物用途
US8124623B2 (en) * 2006-11-10 2012-02-28 Actelion Pharmaceuticals Ltd. 5-hydroxymethyl-oxazolidin-2-one-derivatives and their uses as antibacterials
US20090270379A1 (en) * 2008-04-23 2009-10-29 Macielag Mark J Quinolone derivatives useful as antibacterial agents
EP2177214A1 (en) 2008-10-17 2010-04-21 Ferrer Internacional, S.A. Solid Oral Dosage Forms and Uses
PH12014500130B1 (en) * 2011-08-31 2018-07-04 Otsuka Pharmaceutical Co Ltd Quinolone compound

Also Published As

Publication number Publication date
CN105017151B (zh) 2019-04-02
EA034787B1 (ru) 2020-03-20
JP6106174B2 (ja) 2017-03-29
BR112014000665B1 (pt) 2020-02-18
KR101560073B1 (ko) 2015-10-13
US20170362180A1 (en) 2017-12-21
SG2014004162A (en) 2014-03-28
EP3318557A3 (en) 2018-07-11
CN105712976A (zh) 2016-06-29
CN105017151A (zh) 2015-11-04
EA030867B1 (ru) 2018-10-31
AU2012303954B2 (en) 2017-06-22
MY165004A (en) 2018-02-28
EA201490530A1 (ru) 2014-06-30
NO2751083T3 (el) 2018-05-26
KR20130095831A (ko) 2013-08-28
ZA201402326B (en) 2016-06-29
US20200055823A1 (en) 2020-02-20
TW201630900A (zh) 2016-09-01
PH12014500130B1 (en) 2018-07-04
EA201890098A2 (ru) 2018-05-31
ES2660973T3 (es) 2018-03-26
MX2019010100A (es) 2019-10-15
CO6920292A2 (es) 2014-04-10
EP2751083A1 (en) 2014-07-09
PT2751083T (pt) 2018-03-05
HK1252389A1 (zh) 2019-05-24
BR112014000665B8 (pt) 2020-03-10
US20210032207A1 (en) 2021-02-04
TWI606044B (zh) 2017-11-21
US9440951B2 (en) 2016-09-13
SG10201606932TA (en) 2016-10-28
US20190077762A1 (en) 2019-03-14
NZ620447A (en) 2016-02-26
JP2017039733A (ja) 2017-02-23
MX371361B (es) 2020-01-27
BR112014000665A2 (pt) 2017-01-10
IL230559B (en) 2019-03-31
JP2016027046A (ja) 2016-02-18
CA2845459A1 (en) 2013-03-07
CA2845459C (en) 2019-08-27
SI2751083T1 (en) 2018-04-30
HRP20180483T1 (hr) 2018-05-04
AU2017203756A1 (en) 2017-06-22
JP2014525420A (ja) 2014-09-29
EP2751083B1 (en) 2017-12-27
CN103764631B (zh) 2017-02-15
US20140179675A1 (en) 2014-06-26
TW201319053A (zh) 2013-05-16
LT2751083T (lt) 2018-03-26
AR087747A1 (es) 2014-04-16
KR20140139132A (ko) 2014-12-04
EP2751083A4 (en) 2015-06-10
PH12014500130A1 (en) 2014-02-24
HK1216528A1 (zh) 2016-11-18
US9067887B2 (en) 2015-06-30
TWI583680B (zh) 2017-05-21
KR101996697B1 (ko) 2019-07-04
AU2012303954A1 (en) 2014-02-20
KR20140087059A (ko) 2014-07-08
TW201718506A (zh) 2017-06-01
HUE036301T2 (hu) 2018-06-28
DK2751083T3 (en) 2018-02-26
US20150005287A2 (en) 2015-01-01
IL230559A0 (en) 2014-03-31
JP2018150324A (ja) 2018-09-27
WO2013029548A1 (en) 2013-03-07
US20160340314A1 (en) 2016-11-24
SG10201505811QA (en) 2015-09-29
JP6039025B2 (ja) 2016-12-07
PL2751083T3 (pl) 2018-08-31
MX2014002338A (es) 2014-03-27
EP3318557A2 (en) 2018-05-09
HK1198828A1 (en) 2015-06-12
HK1226077A1 (zh) 2017-09-22
CN103764631A (zh) 2014-04-30
US20150239865A1 (en) 2015-08-27
MX376109B (es) 2025-03-07
AU2017203756B2 (en) 2019-02-07
EA201890098A3 (ru) 2018-09-28

Similar Documents

Publication Publication Date Title
CY1120066T1 (el) Ενωση κινολονης
CY1121549T1 (el) Ενωσεις 1-αρυλκαρβονυλ-4-oξυ-πιπεριδινης χρησιμες για την αγωγη νευροεκφυλιστικων παθησεων
CY1124537T1 (el) Παραγωγο πυριδονης που εχει τετραϋδροπυρανυλ μεθυλ ομαδα
EA033294B1 (ru) Пиридазиноновые гербициды
PE20160523A1 (es) Derivados de arilo o heteroarilo como inhibidores de moleculas pequenas de fibrosis
BR112015006439A2 (pt) compostos de tetrazolinona e seu uso como pesticidas
PH12014500584A1 (en) New bicyclic dihydroquinoline-2-one derivatives
EA201390884A1 (ru) Азабензимидазолы в качестве противовирусных средств в отношении респираторного синцитиального вируса
UA110647C2 (uk) Похідне азолу, спосіб його одержання, проміжна сполука і хімічний агент, призначений для застосування в сільському господарстві і садівництві, і агент для захисту промислових матеріалів
PH12013501873A1 (en) Novel imidazo-oxazine compound or salt thereof
JO3509B1 (ar) معدلات p2x7
BR112015023829A2 (pt) composto de amidina e seu uso
JO3143B1 (ar) مركبات تتراهيدرو بيرولو ثيازين
MX2016017405A (es) Compuestos derivados de 2-(3-piridinil)-1h-benzimidazol y medicamentos que los contienen.
RS54248B1 (en) NEW UNITS AS LISTS OF HISTAMINE H3 RECEPTORS
BR112015011897A2 (pt) novos moduladores seletivos do receptor de andrógeno
EP2602254A4 (en) HETEROCYCLIC CONNECTION
EA201590315A1 (ru) Средства и способ лечения солидных опухолей
UA111950C2 (uk) Гетероциклічні сполуки для лікування або профілактики розладів, викликаних зниженою нейротрансмісією серотоніну, норепінефрину або допаміну
BR112018008885A8 (pt) composto heterocíclico condensado
MX2015015010A (es) Nuevos compuestos de 3,4-dihidro-2h-isoquinolin-1-ona y 2,3-dihidro-isoindol-1-ona.
MX2015002705A (es) Compuestos de piridinona para usarse en terapia fotodinamica.
MX2015015058A (es) Nuevos compuestos de 3,4-dihidro-2h-isoquinolin-1-ona y 2,3-dihidro-isoindol-1-ona.
BR112014020610B8 (pt) composto, métodos para produzir e para purificar a forma (z) de um composto, e para produzir a forma (z) de um derivado de tetrazoliloxima
BR112013021121A2 (pt) microbiocidas de carboxamida