TWI565703B - 2-(1,2,3-三唑-2-基)苯甲醯胺及3-(1,2,3-三唑-2-基)吡啶醯胺衍生物 - Google Patents

2-(1,2,3-三唑-2-基)苯甲醯胺及3-(1,2,3-三唑-2-基)吡啶醯胺衍生物 Download PDF

Info

Publication number
TWI565703B
TWI565703B TW105118634A TW105118634A TWI565703B TW I565703 B TWI565703 B TW I565703B TW 105118634 A TW105118634 A TW 105118634A TW 105118634 A TW105118634 A TW 105118634A TW I565703 B TWI565703 B TW I565703B
Authority
TW
Taiwan
Prior art keywords
triazol
benzyl
phenyl
methyl
morpholin
Prior art date
Application number
TW105118634A
Other languages
English (en)
Chinese (zh)
Other versions
TW201632517A (zh
Inventor
馬汀 波利
克里斯多夫 博斯
克利斯汀 布洛奇
畢比雅 海曼
賽瑞 席佛林
喬帝T 威廉斯
Original Assignee
艾克泰聯製藥有限公司
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 艾克泰聯製藥有限公司 filed Critical 艾克泰聯製藥有限公司
Publication of TW201632517A publication Critical patent/TW201632517A/zh
Application granted granted Critical
Publication of TWI565703B publication Critical patent/TWI565703B/zh

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/26Psychostimulants, e.g. nicotine, cocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/10Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
TW105118634A 2011-11-08 2012-11-07 2-(1,2,3-三唑-2-基)苯甲醯胺及3-(1,2,3-三唑-2-基)吡啶醯胺衍生物 TWI565703B (zh)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
IB2011054976 2011-11-08

Publications (2)

Publication Number Publication Date
TW201632517A TW201632517A (zh) 2016-09-16
TWI565703B true TWI565703B (zh) 2017-01-11

Family

ID=47258050

Family Applications (2)

Application Number Title Priority Date Filing Date
TW105118634A TWI565703B (zh) 2011-11-08 2012-11-07 2-(1,2,3-三唑-2-基)苯甲醯胺及3-(1,2,3-三唑-2-基)吡啶醯胺衍生物
TW101141421A TWI555747B (zh) 2011-11-08 2012-11-07 2-(1,2,3-三唑-2-基)苯甲醯胺及3-(1,2,3-三唑-2-基)吡啶醯胺衍生物

Family Applications After (1)

Application Number Title Priority Date Filing Date
TW101141421A TWI555747B (zh) 2011-11-08 2012-11-07 2-(1,2,3-三唑-2-基)苯甲醯胺及3-(1,2,3-三唑-2-基)吡啶醯胺衍生物

Country Status (28)

Country Link
US (1) US9150566B2 (enExample)
EP (1) EP2776430B1 (enExample)
JP (1) JP5718535B2 (enExample)
KR (1) KR101676930B1 (enExample)
CN (1) CN103917538B (enExample)
AR (1) AR088692A1 (enExample)
AU (1) AU2012335194B2 (enExample)
BR (1) BR112014010617B1 (enExample)
CA (1) CA2846568C (enExample)
CL (1) CL2014000659A1 (enExample)
CY (1) CY1117638T1 (enExample)
DK (1) DK2776430T3 (enExample)
EA (1) EA024106B1 (enExample)
ES (1) ES2572703T3 (enExample)
HR (1) HRP20160678T1 (enExample)
HU (1) HUE029239T2 (enExample)
IL (1) IL232462A (enExample)
IN (1) IN2014CN04127A (enExample)
MX (1) MX343837B (enExample)
MY (1) MY167791A (enExample)
PH (1) PH12014500852A1 (enExample)
PL (1) PL2776430T3 (enExample)
SG (1) SG11201401665WA (enExample)
SI (1) SI2776430T1 (enExample)
TW (2) TWI565703B (enExample)
UA (1) UA112317C2 (enExample)
WO (1) WO2013068935A1 (enExample)
ZA (1) ZA201404189B (enExample)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9440982B2 (en) 2012-02-07 2016-09-13 Eolas Therapeutics, Inc. Substituted prolines/piperidines as orexin receptor antagonists
HK1204955A1 (zh) 2012-02-07 2015-12-11 Eolas Therapeutics Inc. 取代的脯氨酸/哌啶用作食慾素受體拮抗劑
KR101689093B1 (ko) 2012-06-04 2016-12-22 액테리온 파마슈티칼 리미티드 벤즈이미다졸-프롤린 유도체
CN105051040A (zh) 2013-03-12 2015-11-11 埃科特莱茵药品有限公司 作为食欲素受体拮抗剂的氮杂环丁烷酰胺衍生物
WO2015083070A1 (en) 2013-12-03 2015-06-11 Actelion Pharmaceuticals Ltd Crystalline form of (s)-(2-(6-chloro-7-methyl-1h-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1 -yl)(5-methoxy-2-(2h-1,2,3-triazol-2-yl)phenyl)methanone and its use as orexin receptor antagonists
UA119151C2 (uk) 2013-12-03 2019-05-10 Ідорсія Фармасьютікалз Лтд КРИСТАЛІЧНА СОЛЬОВА ФОРМА (S)-(2-(6-ХЛОР-7-МЕТИЛ-1H-БЕНЗО[d]ІМІДАЗОЛ-2-ІЛ)-2-МЕТИЛПІРОЛІДИН-1-ІЛ)(5-МЕТОКСИ-2-(2H-1,2,3-ТРИАЗОЛ-2-ІЛ)ФЕНІЛ)МЕТАНОНУ ЯК АНТАГОНІСТ ОРЕКСИНОВОГО РЕЦЕПТОРА
MX366642B (es) 2013-12-04 2019-07-17 Idorsia Pharmaceuticals Ltd Uso de derivados de bencimidazol-prolina.
JP2017024990A (ja) * 2013-12-13 2017-02-02 大正製薬株式会社 オキサゾリジン及びオキサジナン誘導体
JP5907310B2 (ja) * 2013-12-13 2016-04-26 大正製薬株式会社 オキサジナン化合物の結晶形及びその製造方法
EP3143999A4 (en) 2014-05-16 2017-12-20 The University of Tokyo Depression treatment agent
US10221170B2 (en) 2014-08-13 2019-03-05 Eolas Therapeutics, Inc. Difluoropyrrolidines as orexin receptor modulators
WO2016095205A1 (en) 2014-12-19 2016-06-23 Merck Sharp & Dohme Corp. Heteroaryl orexin receptor antagonists
CN104557744B (zh) * 2014-12-23 2017-04-12 广东东阳光药业有限公司 一种三氮唑化合物的制备方法
AU2016360245B2 (en) 2015-11-23 2020-07-09 Sunshine Lake Pharma Co., Ltd. Octahydropyrrolo [3, 4-c] pyrrole derivatives and uses thereof
SMT202200323T1 (it) 2016-02-12 2022-09-14 Astrazeneca Ab Piperidine alo-sostituite come modulatori del recettore di oressina
RS62357B1 (sr) 2017-05-03 2021-10-29 Idorsia Pharmaceuticals Ltd Dobijanje derivata 2-([1,2,3]triazol-2-il)-benzojeve kiseline
WO2020099511A1 (en) * 2018-11-14 2020-05-22 Idorsia Pharmaceuticals Ltd Benzimidazole-2-methyl-morpholine derivatives
GB201901142D0 (en) 2019-01-28 2019-03-20 Heptares Therapeutics Ltd OX1 Antagonists
US20240116913A1 (en) * 2021-02-02 2024-04-11 Idorsia Pharmaceuticals Ltd A crystalline form of (4-methyl-2-[1,2,3]triazol-2-yl-phenyl)-[(r)-3-(3-[1,2,3]triazol-2-yl-benzyl)-morpholin-4-yl]-methanone
TW202400149A (zh) * 2022-05-13 2024-01-01 瑞士商愛杜西亞製藥有限公司 經噻唑并芳基-甲基取代之環狀肼-n-甲醯胺衍生物
CN115947697A (zh) * 2022-12-28 2023-04-11 苏州汉德创宏生化科技有限公司 一种3-氧代吗啉-4-羧酸叔丁酯的合成方法
WO2024214321A1 (ja) * 2023-04-10 2024-10-17 三菱瓦斯化学株式会社 化合物、組成物、増感効果を発現する方法および製造方法
GB202311280D0 (en) 2023-07-21 2023-09-06 Bial Portela & Ca Sa Orexin receptor antagonists
GB202311281D0 (en) 2023-07-21 2023-09-06 Bial Portela & Ca Sa Orexin receptor antagonists

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003002559A2 (en) * 2001-06-28 2003-01-09 Smithkline Beecham P.L.C. Piperidine compounds for use as orexin receptor antagonist

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5130432A (en) 1990-12-21 1992-07-14 Syntex (U.S.A.) Inc. Process for preparing cyclic amines and intermediate products thereof
AU676993B2 (en) 1991-06-27 1997-04-10 Virginia Commonwealth University Sigma receptor ligands and the use thereof
EP1435955A2 (en) * 2001-05-05 2004-07-14 SmithKline Beecham P.L.C. N-aroyl cyclic amine derivatives as orexin receptor antagonists
MXPA03011706A (es) * 2001-06-28 2004-03-19 Smithkline Beecham Plc Derivados de n-aroil-amina ciclica como antagonistas del receptor de orexina.
GB0124463D0 (en) * 2001-10-11 2001-12-05 Smithkline Beecham Plc Compounds
GB0130335D0 (en) * 2001-12-19 2002-02-06 Smithkline Beecham Plc Compounds
RU2378257C2 (ru) 2004-03-01 2010-01-10 Актелион Фармасьютиклз Лтд Замещенные производные 1,2,3,4-тетрагидроизохинолина
UA93903C2 (ru) 2006-03-15 2011-03-25 Актелион Фармасьютикалз Лтд Производные тетрагидроизохинолина для повышения функции памяти
AU2007272854B2 (en) 2006-07-14 2013-08-01 Merck Sharp & Dohme Corp. Bridged diazepan orexin receptor antagonists
GB0620818D0 (en) 2006-10-19 2006-11-29 Ucb Sa Therapeutic agents
PE20081229A1 (es) 2006-12-01 2008-08-28 Merck & Co Inc Antagonistas de receptor de orexina de diazepam sustituido
WO2009040730A2 (en) 2007-09-24 2009-04-02 Actelion Pharmaceuticals Ltd Pyrrolidines and piperidines as orexin receptor antagonists
PE20091010A1 (es) 2007-10-10 2009-08-08 Actelion Pharmaceuticals Ltd Derivados de tetrahidroquinolina
AU2009307913A1 (en) * 2008-10-21 2010-04-29 Merck Sharp & Dohme Corp. 2,5-disubstituted piperidine orexin receptor antagonists
EP2349269A4 (en) 2008-10-21 2012-04-25 Merck Sharp & Dohme 2,5-DISUBSTITUTED PIPERIDINOREXINE RECEPTOR ANTAGONISTS
US8466281B2 (en) * 2008-10-21 2013-06-18 Merck Sharp & Dohme Corp. 2,5-disubstituted morpholine orexin receptor antagonists
WO2010063662A1 (en) 2008-12-02 2010-06-10 Glaxo Group Limited N-{[(ir,4s,6r-3-(2-pyridinylcarbonyl)-3-azabicyclo [4.1.0] hept-4-yl] methyl}-2-heteroarylamine derivatives and uses thereof
EP2370426A1 (en) 2008-12-02 2011-10-05 Glaxo Group Limited N-{[(ir,4s,6r-3-(2-pyridinylcarbonyl)-3-azabicyclo [4.1.0]hept-4-yl]methyl}-2-heteroarylamine derivatives and uses thereof
SI2491038T1 (sl) 2009-10-23 2016-08-31 Janssen Pharmaceutica N.V. Disubstituirani oktahil-dropirolo(3,4-c)piroli kot modulatorji oreksinskega receptorja
JP5848251B2 (ja) 2009-10-23 2016-01-27 ヤンセン ファーマシューティカ エヌ.ベー. オレキシン受容体調節因子としての縮合複素環式化合物
WO2011050200A1 (en) 2009-10-23 2011-04-28 Janssen Pharmaceutica Nv Fused heterocyclic compounds as orexin receptor modulators

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003002559A2 (en) * 2001-06-28 2003-01-09 Smithkline Beecham P.L.C. Piperidine compounds for use as orexin receptor antagonist

Also Published As

Publication number Publication date
KR101676930B1 (ko) 2016-11-16
MY167791A (en) 2018-09-26
SI2776430T1 (sl) 2016-06-30
MX2014005635A (es) 2014-06-23
EP2776430A1 (en) 2014-09-17
CN103917538B (zh) 2016-08-24
PL2776430T3 (pl) 2016-09-30
WO2013068935A1 (en) 2013-05-16
UA112317C2 (uk) 2016-08-25
HK1199022A1 (zh) 2015-06-19
IL232462A (en) 2016-11-30
TW201323421A (zh) 2013-06-16
TWI555747B (zh) 2016-11-01
PH12014500852A1 (en) 2016-03-02
IN2014CN04127A (enExample) 2015-07-10
EA201400553A1 (ru) 2014-10-30
KR20140096338A (ko) 2014-08-05
US9150566B2 (en) 2015-10-06
CA2846568C (en) 2020-01-14
EP2776430B1 (en) 2016-03-16
JP2014532753A (ja) 2014-12-08
US20150158855A1 (en) 2015-06-11
NZ625896A (en) 2016-04-29
ZA201404189B (en) 2017-08-30
BR112014010617A2 (pt) 2017-04-25
ES2572703T3 (es) 2016-06-01
MX343837B (es) 2016-11-24
AR088692A1 (es) 2014-06-25
BR112014010617A8 (pt) 2017-12-26
HUE029239T2 (en) 2017-02-28
TW201632517A (zh) 2016-09-16
IL232462A0 (en) 2014-06-30
AU2012335194A1 (en) 2014-07-03
EA024106B1 (ru) 2016-08-31
HRP20160678T1 (hr) 2016-07-15
CN103917538A (zh) 2014-07-09
AU2012335194B2 (en) 2017-05-25
DK2776430T3 (en) 2016-05-09
CA2846568A1 (en) 2013-05-16
SG11201401665WA (en) 2014-09-26
CL2014000659A1 (es) 2014-08-18
BR112014010617B1 (pt) 2021-12-14
CY1117638T1 (el) 2017-04-26
JP5718535B2 (ja) 2015-05-13

Similar Documents

Publication Publication Date Title
TWI565703B (zh) 2-(1,2,3-三唑-2-基)苯甲醯胺及3-(1,2,3-三唑-2-基)吡啶醯胺衍生物
US11040966B2 (en) Benzimidazole-proline derivatives
CN104703980B (zh) 属于[邻双(杂)芳基]‑[2‑(间双(杂)芳基)吡咯烷‑1‑基]甲酮衍生物的食欲素受体拮抗剂
TWI639595B (zh) 作為LRRK2(富含白胺酸重複激酶2)抑制劑之新穎咪唑並[4,5-c]喹啉和咪唑並[4,5-c][1,5]萘啶衍生物
CN106117193B (zh) 新的杂环衍生物及其在神经性疾病治疗中的应用
MX2008014796A (es) Derivados de aril-4-etinil-isoxazol.
TW201639851A (zh) 雙環咪唑衍生物
KR20140051922A (ko) 페닐-3-아자-바이사이클로[3.1.0]헥스-3일-메타논 및 약제로서의 이의 용도
US9403813B2 (en) Azetidine amide derivatives as orexin receptor antagonists
WO2020007964A1 (en) 2-(2-azabicyclo[3.1.0]hexan-1-yl)-1h-benzimidazole derivatives
HK1199022B (en) 2-(1,2,3-triazol-2-yl)benzamide and 3-(1,2,3-triazol-2-yl)picolinamide derivatives as orexin receptor antagonists
WO2023218023A1 (en) Thiazoloaryl-methyl substituted cyclic hydrazine-n-carboxamide derivatives
NZ625896B2 (en) 2-(1,2,3-triazol-2-yl)benzamide and 3-(1,2,3-triazol-2-yl)picolinamide derivatives as orexin receptor antagonists

Legal Events

Date Code Title Description
MM4A Annulment or lapse of patent due to non-payment of fees