TWI597276B - 胺基甲酸酯/尿素衍生物 - Google Patents

胺基甲酸酯/尿素衍生物 Download PDF

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Publication number
TWI597276B
TWI597276B TW102125975A TW102125975A TWI597276B TW I597276 B TWI597276 B TW I597276B TW 102125975 A TW102125975 A TW 102125975A TW 102125975 A TW102125975 A TW 102125975A TW I597276 B TWI597276 B TW I597276B
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TW
Taiwan
Prior art keywords
compound
ester
piperidin
carboxylic acid
salt
Prior art date
Application number
TW102125975A
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English (en)
Chinese (zh)
Other versions
TW201408656A (zh
Inventor
尹維 歐柏森
馬克 蓋瑞 博客
達利歐 伯格
馬可 克茲
史蒂芬妮 凱 達德
史塔法偌 魯卡 吉亞法瑞達
姜海洋
派崔 卡賓斯基
湯瑪斯J 崔斯勒
王泰霖
王曉陽
張肅臣
Original Assignee
諾華公司
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Application filed by 諾華公司 filed Critical 諾華公司
Publication of TW201408656A publication Critical patent/TW201408656A/zh
Application granted granted Critical
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    • 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
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13—Dicarboxylic acids
    • C07C57/15—Fumaric acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235—Saturated compounds containing more than one carboxyl group
    • C07C59/245—Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
    • C07C59/265—Citric acid
    • 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
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D403/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Hydrogenated Pyridines (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
TW102125975A 2012-07-20 2013-07-19 胺基甲酸酯/尿素衍生物 TWI597276B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN2012078933 2012-07-20
CN2013078309 2013-06-28

Publications (2)

Publication Number Publication Date
TW201408656A TW201408656A (zh) 2014-03-01
TWI597276B true TWI597276B (zh) 2017-09-01

Family

ID=49263333

Family Applications (1)

Application Number Title Priority Date Filing Date
TW102125975A TWI597276B (zh) 2012-07-20 2013-07-19 胺基甲酸酯/尿素衍生物

Country Status (41)

Country Link
US (4) US9034874B2 (enExample)
EP (1) EP2875016B1 (enExample)
JP (1) JP6203841B2 (enExample)
KR (1) KR102150739B1 (enExample)
CN (1) CN104470911B (enExample)
AP (1) AP3710A (enExample)
AR (1) AR092354A1 (enExample)
AU (1) AU2013291617B2 (enExample)
BR (1) BR112015001207B1 (enExample)
CA (1) CA2878006C (enExample)
CL (1) CL2015000056A1 (enExample)
CO (1) CO7170173A2 (enExample)
CR (1) CR20150019A (enExample)
CU (1) CU24248B1 (enExample)
CY (1) CY1119492T1 (enExample)
DK (1) DK2875016T3 (enExample)
EA (1) EA026091B1 (enExample)
ES (1) ES2648512T3 (enExample)
GT (1) GT201500012A (enExample)
HR (1) HRP20171692T1 (enExample)
HU (1) HUE035592T2 (enExample)
IL (1) IL236656A (enExample)
IN (1) IN2014DN10449A (enExample)
JO (1) JO3439B1 (enExample)
LT (1) LT2875016T (enExample)
MX (1) MX362059B (enExample)
MY (1) MY168752A (enExample)
NO (1) NO2875016T3 (enExample)
NZ (1) NZ702346A (enExample)
PE (1) PE20151155A1 (enExample)
PH (1) PH12014502743B1 (enExample)
PL (1) PL2875016T3 (enExample)
PT (1) PT2875016T (enExample)
RS (1) RS56479B1 (enExample)
SG (2) SG11201408020RA (enExample)
SI (1) SI2875016T1 (enExample)
TN (1) TN2014000497A1 (enExample)
TW (1) TWI597276B (enExample)
UY (1) UY34921A (enExample)
WO (1) WO2014013469A1 (enExample)
ZA (1) ZA201408805B (enExample)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW201321353A (zh) 2011-10-08 2013-06-01 Novartis Ag 胺基甲酸酯/尿素衍生物
US9034874B2 (en) 2012-07-20 2015-05-19 Novartis Ag Carbamate/urea derivatives
EP3391886A1 (en) * 2017-04-19 2018-10-24 Novartis AG The use of a h3r inverse agonist for the treatment of shift work disorder
WO2019245975A1 (en) 2018-06-17 2019-12-26 Axsome Therapeutics, Inc. Compositions for delivery of reboxetine
CN112789038A (zh) 2018-10-11 2021-05-11 诺华股份有限公司 H3r反向激动剂用于治疗与帕金森病(pd)相关的日间过度嗜睡的用途
US20200147093A1 (en) 2018-10-15 2020-05-14 Axsome Therapeutics, Inc. Use of esreboxetine to treat nervous system disorders such as fibromyalgia
US11020402B2 (en) 2018-10-15 2021-06-01 Axsome Therapeutics, Inc. Use of reboxetine to treat narcolepsy
US12616702B2 (en) 2019-12-03 2026-05-05 Axsome Therapeutics, Inc. Use of reboxetine to treat narcolepsy
EP4251148A1 (en) 2020-11-27 2023-10-04 Richter Gedeon Nyrt. Histamine h3 receptor antagonists/inverse agonists for the treatment of autism spectrum disorder
US12565478B1 (en) 2025-01-21 2026-03-03 Axsome Therapeutics, Inc. (S)-2-((S)-(2-ethoxyphenoxy)(phenyl)methyl)-4-nitrosomorpholine

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TW301607B (enExample) 1993-03-09 1997-04-01 Takeda Pharm Industry Co Ltd
IL150650A0 (en) 2000-01-20 2003-02-12 Eisai Co Ltd Piperidine derivatives and pharmaceutical compositions containing the same
JP4522651B2 (ja) 2001-03-13 2010-08-11 シェーリング コーポレイション 新規非イミダゾール化合物
WO2004078163A2 (en) 2003-02-28 2004-09-16 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
HRP20080541T3 (en) 2003-04-23 2008-12-31 Glaxo Group Limited Piperazine derivatives and their use for the treatment of neurological and psychiatric diseases
BRPI0507629A (pt) 2004-02-13 2007-07-03 Banyu Pharma Co Ltd composto, antagonista do receptor e agonista inverso do receptor da histamina h3, agente profilático ou terapêutico para uma doença metabólica, uma doença circulatória ou uma doença do sistema nervoso, ou um seu sal farmaceuticamente aceitável
SE0401971D0 (sv) * 2004-08-02 2004-08-02 Astrazeneca Ab Piperidne derivatives
KR20090102883A (ko) 2004-09-02 2009-09-30 테바 파마슈티컬 인더스트리즈 리미티드 올메살탄 메독소밀의 정제
WO2006029056A1 (en) 2004-09-02 2006-03-16 Teva Pharmaceutical Industries Ltd. Preparation of olmesartan medoxomil
WO2007016496A2 (en) 2005-08-02 2007-02-08 Neurogen Corporation Dipiperazinyl ketones and related analogues
JP2009514846A (ja) 2005-11-04 2009-04-09 ファイザー・リミテッド テトラヒドロナフチリジン誘導体
WO2007063934A1 (ja) 2005-12-02 2007-06-07 Mitsubishi Tanabe Pharma Corporation 脂環式複素環化合物
US8093248B2 (en) * 2007-12-05 2012-01-10 Astrazeneca Ab (Publ) Compounds useful for the treatment of conditions associated with weight gain
TWI498115B (zh) * 2007-12-27 2015-09-01 Daiichi Sankyo Co Ltd 咪唑羰基化合物
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TW201321353A (zh) * 2011-10-08 2013-06-01 Novartis Ag 胺基甲酸酯/尿素衍生物
US9034874B2 (en) 2012-07-20 2015-05-19 Novartis Ag Carbamate/urea derivatives

Also Published As

Publication number Publication date
TN2014000497A1 (en) 2016-03-30
MX2015000903A (es) 2015-04-10
MX362059B (es) 2019-01-07
IL236656A (en) 2017-12-31
IL236656A0 (en) 2015-02-26
CL2015000056A1 (es) 2015-03-20
PH12014502743A1 (en) 2015-02-02
CN104470911B (zh) 2018-04-06
MY168752A (en) 2018-11-30
PH12014502743B1 (en) 2015-02-02
CY1119492T1 (el) 2018-03-07
AP2014008109A0 (en) 2014-12-31
AR092354A1 (es) 2015-04-15
JP6203841B2 (ja) 2017-09-27
HRP20171692T1 (hr) 2017-12-15
JO3439B1 (ar) 2019-10-20
CA2878006A1 (en) 2014-01-23
US9273026B2 (en) 2016-03-01
AU2013291617A1 (en) 2015-01-15
PE20151155A1 (es) 2015-08-05
BR112015001207A8 (pt) 2018-01-16
HUE035592T2 (en) 2018-05-28
NZ702346A (en) 2017-06-30
CA2878006C (en) 2020-10-27
US9624192B2 (en) 2017-04-18
KR102150739B1 (ko) 2020-09-02
IN2014DN10449A (enExample) 2015-08-21
US9034874B2 (en) 2015-05-19
PL2875016T3 (pl) 2018-01-31
ZA201408805B (en) 2016-08-31
CR20150019A (es) 2015-05-04
CO7170173A2 (es) 2015-01-28
US20170275264A1 (en) 2017-09-28
US20140163036A1 (en) 2014-06-12
AU2013291617B2 (en) 2015-10-01
PT2875016T (pt) 2017-11-30
US20160244426A1 (en) 2016-08-25
RS56479B1 (sr) 2018-01-31
GT201500012A (es) 2017-11-09
EP2875016B1 (en) 2017-08-23
BR112015001207A2 (pt) 2017-08-01
EP2875016A1 (en) 2015-05-27
US20150218127A1 (en) 2015-08-06
UY34921A (es) 2014-02-28
KR20150036081A (ko) 2015-04-07
EA026091B1 (ru) 2017-02-28
EA201590250A1 (ru) 2015-05-29
ES2648512T3 (es) 2018-01-03
SI2875016T1 (sl) 2017-11-30
HK1204609A1 (en) 2015-11-27
LT2875016T (lt) 2017-11-10
CU24248B1 (es) 2017-02-02
NO2875016T3 (enExample) 2018-01-20
BR112015001207B1 (pt) 2022-08-09
WO2014013469A1 (en) 2014-01-23
CU20150006A7 (es) 2016-02-29
SG11201408020RA (en) 2015-03-30
JP2015522606A (ja) 2015-08-06
DK2875016T3 (da) 2017-11-27
TW201408656A (zh) 2014-03-01
CN104470911A (zh) 2015-03-25
SG10201700188PA (en) 2017-02-27
AP3710A (en) 2016-05-31

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