TWI412363B - 5-(3,4-二氯苯基)-n-(2-羥基環己基)-6-(2,2,2-三氟乙氧基)-菸鹼醯胺及其鹽 - Google Patents

5-(3,4-二氯苯基)-n-(2-羥基環己基)-6-(2,2,2-三氟乙氧基)-菸鹼醯胺及其鹽 Download PDF

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Publication number
TWI412363B
TWI412363B TW099130367A TW99130367A TWI412363B TW I412363 B TWI412363 B TW I412363B TW 099130367 A TW099130367 A TW 099130367A TW 99130367 A TW99130367 A TW 99130367A TW I412363 B TWI412363 B TW I412363B
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Taiwan
Prior art keywords
compound
formula
treatment
acid
medicament
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TW099130367A
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English (en)
Chinese (zh)
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TW201114427A (en
Inventor
Stephan Roever
Matthew Wright
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Hoffmann La Roche
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Publication of TW201114427A publication Critical patent/TW201114427A/zh
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Publication of TWI412363B publication Critical patent/TWI412363B/zh

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    • 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • 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
    • A61K31/465—Nicotine; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A61P39/02—Antidotes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • A61P9/12—Antihypertensives

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Toxicology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
TW099130367A 2009-09-11 2010-09-08 5-(3,4-二氯苯基)-n-(2-羥基環己基)-6-(2,2,2-三氟乙氧基)-菸鹼醯胺及其鹽 TWI412363B (zh)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP09170097 2009-09-11

Publications (2)

Publication Number Publication Date
TW201114427A TW201114427A (en) 2011-05-01
TWI412363B true TWI412363B (zh) 2013-10-21

Family

ID=42830122

Family Applications (1)

Application Number Title Priority Date Filing Date
TW099130367A TWI412363B (zh) 2009-09-11 2010-09-08 5-(3,4-二氯苯基)-n-(2-羥基環己基)-6-(2,2,2-三氟乙氧基)-菸鹼醯胺及其鹽

Country Status (34)

Country Link
US (1) US8227491B2 (enExample)
EP (1) EP2475645B1 (enExample)
JP (1) JP5604520B2 (enExample)
KR (1) KR101382871B1 (enExample)
CN (1) CN102639506B (enExample)
AR (2) AR078352A1 (enExample)
AU (1) AU2010294277B2 (enExample)
BR (1) BR112012005511B8 (enExample)
CA (1) CA2771493C (enExample)
CL (1) CL2012000611A1 (enExample)
CO (1) CO6491033A2 (enExample)
CR (1) CR20120089A (enExample)
CY (1) CY1114377T1 (enExample)
DK (1) DK2475645T3 (enExample)
EC (1) ECSP12011723A (enExample)
ES (1) ES2423821T3 (enExample)
HR (1) HRP20130869T1 (enExample)
IL (1) IL217920A (enExample)
IN (1) IN2012DN00763A (enExample)
MA (1) MA33563B1 (enExample)
MX (1) MX2012002254A (enExample)
MY (1) MY161103A (enExample)
NZ (1) NZ597514A (enExample)
PE (1) PE20120863A1 (enExample)
PL (1) PL2475645T3 (enExample)
PT (1) PT2475645E (enExample)
RS (1) RS52987B (enExample)
RU (1) RU2541475C2 (enExample)
SG (1) SG179035A1 (enExample)
SI (1) SI2475645T1 (enExample)
TW (1) TWI412363B (enExample)
UA (1) UA107088C2 (enExample)
WO (1) WO2011029827A1 (enExample)
ZA (1) ZA201201599B (enExample)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012031817A1 (en) 2010-09-09 2012-03-15 F. Hoffmann-La Roche Ag Determination of abca1 protein levels in cells
US8410107B2 (en) 2010-10-15 2013-04-02 Hoffmann-La Roche Inc. N-pyridin-3-yl or N-pyrazin-2-yl carboxamides
US20120101282A1 (en) * 2010-10-22 2012-04-26 Pascal Dott Process for the preparation of nicotinamide derivatives
US8669254B2 (en) 2010-12-15 2014-03-11 Hoffman-La Roche Inc. Pyridine, pyridazine, pyrimidine or pyrazine carboxamides as HDL-cholesterol raising agents
WO2014180741A1 (en) * 2013-05-06 2014-11-13 F. Hoffmann-La Roche Ag Methods of identifying modulators of osbpl7 and the use of such modulators for treatment of diseases associated with osbpl7
US20200085810A1 (en) * 2018-07-26 2020-03-19 Hoffmann-La Roche Inc. Compounds for use in treating kidney disorders
US11814354B2 (en) * 2021-09-08 2023-11-14 River 3 Renal Corp. Solid forms

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW200640867A (en) * 2005-04-06 2006-12-01 Hoffmann La Roche Pyridine-3-carboxamide derivatives as CB1 inverse agonists

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI259180B (en) * 2000-08-08 2006-08-01 Hoffmann La Roche 4-Phenyl-pyridine derivatives
EP2074096B1 (en) 2006-10-04 2012-06-27 F. Hoffmann-La Roche AG 3-pyridinecarboxamide and 2-pyrazinecarboxamide derivatives as hdl-cholesterol raising agents

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW200640867A (en) * 2005-04-06 2006-12-01 Hoffmann La Roche Pyridine-3-carboxamide derivatives as CB1 inverse agonists

Also Published As

Publication number Publication date
CA2771493A1 (en) 2011-03-17
CL2012000611A1 (es) 2012-09-07
AR114032A2 (es) 2020-07-15
ES2423821T3 (es) 2013-09-24
SG179035A1 (en) 2012-04-27
US8227491B2 (en) 2012-07-24
DK2475645T3 (da) 2013-07-22
NZ597514A (en) 2013-10-25
KR101382871B1 (ko) 2014-04-08
TW201114427A (en) 2011-05-01
IL217920A (en) 2015-11-30
MY161103A (en) 2017-04-14
CO6491033A2 (es) 2012-07-31
PE20120863A1 (es) 2012-07-23
CN102639506B (zh) 2014-09-03
JP5604520B2 (ja) 2014-10-08
BR112012005511B8 (pt) 2021-05-25
EP2475645A1 (en) 2012-07-18
PT2475645E (pt) 2013-08-05
AU2010294277B2 (en) 2015-07-09
JP2013504534A (ja) 2013-02-07
RU2012113924A (ru) 2013-10-20
UA107088C2 (xx) 2014-11-25
AR078352A1 (es) 2011-11-02
RS52987B (sr) 2014-02-28
BR112012005511A2 (pt) 2016-04-19
HK1172021A1 (en) 2013-04-12
MX2012002254A (es) 2012-03-16
MA33563B1 (fr) 2012-09-01
RU2541475C2 (ru) 2015-02-20
IN2012DN00763A (enExample) 2015-06-26
CY1114377T1 (el) 2016-08-31
CA2771493C (en) 2017-08-29
AU2010294277A1 (en) 2012-02-09
PL2475645T3 (pl) 2013-12-31
BR112012005511B1 (pt) 2021-03-02
CN102639506A (zh) 2012-08-15
SI2475645T1 (sl) 2013-10-30
WO2011029827A1 (en) 2011-03-17
ZA201201599B (en) 2012-11-28
US20110065759A1 (en) 2011-03-17
HRP20130869T1 (hr) 2013-10-25
EP2475645B1 (en) 2013-07-03
CR20120089A (es) 2012-03-22
IL217920A0 (en) 2012-03-29
ECSP12011723A (es) 2012-04-30
KR20120048040A (ko) 2012-05-14

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