CN104995188B - 2-((1r,4r)-4-(4-(5-(苯并噁唑-2-基氨基)吡啶-2-基)苯基)环己基)乙酸的葡甲胺盐形式和它们作为dgat1抑制剂的用途 - Google Patents

2-((1r,4r)-4-(4-(5-(苯并噁唑-2-基氨基)吡啶-2-基)苯基)环己基)乙酸的葡甲胺盐形式和它们作为dgat1抑制剂的用途 Download PDF

Info

Publication number
CN104995188B
CN104995188B CN201480003867.0A CN201480003867A CN104995188B CN 104995188 B CN104995188 B CN 104995188B CN 201480003867 A CN201480003867 A CN 201480003867A CN 104995188 B CN104995188 B CN 104995188B
Authority
CN
China
Prior art keywords
phenyl
pyridin
crystal form
ylamino
cyclohexyl
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.)
Expired - Fee Related
Application number
CN201480003867.0A
Other languages
English (en)
Chinese (zh)
Other versions
CN104995188A (zh
Inventor
C·卡帕茨-丹尼尔
M·德拉克鲁兹
B·宫
A·贾殷
Y·陆
L·张
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.)
Novartis AG
Original Assignee
Novartis AG
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 Novartis AG filed Critical Novartis AG
Publication of CN104995188A publication Critical patent/CN104995188A/zh
Application granted granted Critical
Publication of CN104995188B publication Critical patent/CN104995188B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric 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
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • 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

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201480003867.0A 2013-01-11 2014-01-10 2-((1r,4r)-4-(4-(5-(苯并噁唑-2-基氨基)吡啶-2-基)苯基)环己基)乙酸的葡甲胺盐形式和它们作为dgat1抑制剂的用途 Expired - Fee Related CN104995188B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361751443P 2013-01-11 2013-01-11
US61/751,443 2013-01-11
PCT/US2014/011005 WO2014110344A1 (en) 2013-01-11 2014-01-10 Meglumine salt forms of 2-((1 r,4r)-4-(4-(5-(benzoxazol-2-ylamino)pyridin-2-yl)phenyl)cyclohexyl) acetic acid and their use as dgat1 inhibitors

Publications (2)

Publication Number Publication Date
CN104995188A CN104995188A (zh) 2015-10-21
CN104995188B true CN104995188B (zh) 2018-09-14

Family

ID=50001335

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201480003867.0A Expired - Fee Related CN104995188B (zh) 2013-01-11 2014-01-10 2-((1r,4r)-4-(4-(5-(苯并噁唑-2-基氨基)吡啶-2-基)苯基)环己基)乙酸的葡甲胺盐形式和它们作为dgat1抑制剂的用途

Country Status (16)

Country Link
US (2) US8987459B2 (enExample)
EP (1) EP2943488B1 (enExample)
JP (1) JP6302937B2 (enExample)
KR (1) KR20150103747A (enExample)
CN (1) CN104995188B (enExample)
AR (1) AR101523A1 (enExample)
AU (1) AU2014205276B2 (enExample)
BR (1) BR112015016370A2 (enExample)
CA (1) CA2896861A1 (enExample)
EA (1) EA027688B1 (enExample)
ES (1) ES2675398T3 (enExample)
MX (1) MX2015008978A (enExample)
PL (1) PL2943488T3 (enExample)
PT (1) PT2943488T (enExample)
TR (1) TR201808198T4 (enExample)
WO (1) WO2014110344A1 (enExample)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104995188B (zh) * 2013-01-11 2018-09-14 诺华股份有限公司 2-((1r,4r)-4-(4-(5-(苯并噁唑-2-基氨基)吡啶-2-基)苯基)环己基)乙酸的葡甲胺盐形式和它们作为dgat1抑制剂的用途
KR101684053B1 (ko) * 2015-01-20 2016-12-08 씨제이헬스케어 주식회사 벤즈이미다졸 유도체의 신규 결정형 및 이의 제조방법
US10822346B2 (en) * 2018-04-17 2020-11-03 Cardurion Pharmaceuticals, Llc Meglumine salts of thienopyrimidines
MX2023005447A (es) * 2020-11-10 2023-09-25 Unity Biotechnology Inc Inhibidor de sales sólidas cristalinas de meglumina de bcl y métodos de elaboración y uso de estos.

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101415683A (zh) * 2006-03-31 2009-04-22 诺瓦提斯公司 新化合物
WO2013169648A1 (en) * 2012-05-07 2013-11-14 Novartis Ag Pharmaceutical combinations comprising a dgat1 inhibtor and a triglyceride lowering drug

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW200303742A (en) 2001-11-21 2003-09-16 Novartis Ag Organic compounds
CN104995188B (zh) * 2013-01-11 2018-09-14 诺华股份有限公司 2-((1r,4r)-4-(4-(5-(苯并噁唑-2-基氨基)吡啶-2-基)苯基)环己基)乙酸的葡甲胺盐形式和它们作为dgat1抑制剂的用途

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101415683A (zh) * 2006-03-31 2009-04-22 诺瓦提斯公司 新化合物
WO2013169648A1 (en) * 2012-05-07 2013-11-14 Novartis Ag Pharmaceutical combinations comprising a dgat1 inhibtor and a triglyceride lowering drug

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
A counter ion that fulfils all needs;Steffen Denzinger;《World Pharmaceutical Frontier》;20111231;第2卷;第90页 *

Also Published As

Publication number Publication date
KR20150103747A (ko) 2015-09-11
CA2896861A1 (en) 2014-07-17
EA201591300A1 (ru) 2015-11-30
AU2014205276A1 (en) 2015-07-16
EP2943488A1 (en) 2015-11-18
MX2015008978A (es) 2015-09-29
WO2014110344A1 (en) 2014-07-17
AU2014205276B2 (en) 2016-10-20
CN104995188A (zh) 2015-10-21
ES2675398T3 (es) 2018-07-11
PL2943488T3 (pl) 2018-09-28
US8987459B2 (en) 2015-03-24
JP6302937B2 (ja) 2018-03-28
EA027688B1 (ru) 2017-08-31
PT2943488T (pt) 2018-06-12
EP2943488B1 (en) 2018-03-28
BR112015016370A2 (pt) 2017-07-11
JP2016505017A (ja) 2016-02-18
US20150166522A1 (en) 2015-06-18
US9242971B2 (en) 2016-01-26
AR101523A1 (es) 2016-12-28
TR201808198T4 (tr) 2018-07-23
US20140200246A1 (en) 2014-07-17

Similar Documents

Publication Publication Date Title
US9023882B2 (en) 5-membered nitrogen containing heterocyclic derivatives and pharmaceutical compositions comprising the same
CN104395309B (zh) 环状桥头醚dgat1抑制剂
WO2007097403A1 (ja) 消化管潰瘍治療又は予防薬
KR20100071048A (ko) Dgat1 억제제로서의 옥사디아졸- 및 옥사졸-치환된 벤즈이미다졸- 및 인돌-유도체
TW201124400A (en) Conpounds and compositions as modulators of GPR119 activity
US20140343102A1 (en) Crystalline forms of the sodium salt of (4--cyclohexyl)-acetic acid
JP5314037B2 (ja) 縮合環誘導体及びその医薬用途
JP6302937B2 (ja) 2−((1r,4r)−4−(4−(5−(ベンゾオキサゾール−2−イルアミノ)ピリジン−2−イル)フェニル)シクロヘキシル)酢酸のメグルミン塩形態、およびdgat1阻害剤としてのそれらの使用
HK1183485B (en) New crystalline forms of the sodium salt of (4- {4- [5- ( 6 - trifluoromethyl - pyridin- 3 - ylamino ) - pyridin- 2 -yl]-phenyl} - cyclohexyl) -acetic acid
HK1183485A (en) New crystalline forms of the sodium salt of (4- {4- [5- ( 6 - trifluoromethyl - pyridin- 3 - ylamino ) - pyridin- 2 -yl]-phenyl} - cyclohexyl) -acetic acid

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant
CF01 Termination of patent right due to non-payment of annual fee
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20180914

Termination date: 20200110