AR083579A1 - Inhibidor de cetp de oxazodilinona sustituida con amina ciclica - Google Patents

Inhibidor de cetp de oxazodilinona sustituida con amina ciclica

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Publication number
AR083579A1
AR083579A1 ARP110103977A ARP110103977A AR083579A1 AR 083579 A1 AR083579 A1 AR 083579A1 AR P110103977 A ARP110103977 A AR P110103977A AR P110103977 A ARP110103977 A AR P110103977A AR 083579 A1 AR083579 A1 AR 083579A1
Authority
AR
Argentina
Prior art keywords
alkyl
optionally substituted
independently
halogens
halogen
Prior art date
Application number
ARP110103977A
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English (en)
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Merck Sharp & Dohme
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Publication date
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Publication of AR083579A1 publication Critical patent/AR083579A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08—Bridged 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • 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
    • 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
    • A61K31/44—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
    • A61K31/4965—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
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine 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
    • 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
    • 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
    • C07D413/06—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 only aliphatic carbon atoms
    • 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
    • C07D417/14—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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Son inhibidores de CETP y son útiles para elevar el colesterol HDL, reducir el colesterol LDL y para tratar o prevenir aterosclerosis. En los compuestos de fórmula (1), A3 es un grupo indanil o grupo fenil sustituido.Reivindicación 1: Un compuesto de fórmula (1), o una sal farmacéuticamente aceptable del mismo, en la que A3 se representa por la fórmula (2) o fórmula (3), en la que Y es N o CH, en la que CH puede estar sustituido con Rc1 si Rc1 está presente en la estructura; R1 es H, CF3, o alquilo C1-3; cada Ra es independientemente alquilo C1-3 opcionalmente sustituido con 1 - 5 halógenos, -O-alquilo C1-3 opcionalmente sustituido con 1 - 5 halógenos, halógeno, -CN o cicloalquilo C3-4 opcionalmente sustituido con 1 - 3 halógenos; Rc es (a) es un heterociclo monocíclico de 4 - 7 miembros que comprende un N que está unido al anillo heteroaromático al que Rc está conectado, en el que el heterocíclico monocíclico comprende opcionalmente 1 - 3 dobles enlaces, un carbonilo y 1 - 3 grupos heteroátomo adicionales que son cada uno, independientemente, N, O, S, S(O), o S(O)2 o (b) un heterociclo bicíclico de 5 - 8 miembros que comprende un N que está unido al anillo heteroaromático al que está conectado Rc, donde el heterociclo bicíclico comprende opcionalmente 1 - 3 dobles enlaces, un carbonilo y 1 - 3 grupos heteroátomo adicionales que son cada uno, independientemente, N, O, S, S(O), o S(O)2, donde Rc como se ha definido en (a) o (b) está opcionalmente sustituido con 1 - 3 grupos sustituyentes que son independientemente halógeno, -OH, -CN, alquilo C1-3 o -O-alquilo C1-3, donde el alquilo C1-3 y el -O-alquilo C1-3 están opcionalmente sustituidos con 1 - 3 halógenos; cada Rc1 es independientemente alquilo C1-3, -O-alquilo C1-3 o halógeno, donde el alquilo, en cualquier caso, está opcionalmente sustituido con 1 - 5 halógenos; Rb es H, alquilo C1-3, -O-alquilo C1-3, -O-cicloalquilo C3-6, halógeno, -CN, -NO2, o -OH, donde el alquilo C1-3 y el -O-alquilo C1-3 están opcionalmente sustituidos con 1 - 5 halógenos, y -O-cicloalquilo C3-6 está opcionalmente sustituido con 1 - 3 halógenos; cada Rb1 es independientemente alquilo C1-3, -O-alquilo C1-3 o halógeno, donde el alquilo C1-3 y el -O-alquilo C1-3 están opcionalmente sustituidos con 1 - 5 halógenos; X es: (a) (i) halógeno, (ii) -alquilo C1-4, (iii) -cicloalquil C3-6-Y o alquil C1-3-Y, donde Y es -CN, -OH o -OCH3, o (iv) -fenilo que está sustituido con 1 - 3 grupos que son independientemente halógeno, -CN, -OH, -alquilo C1-4, -O-alquilo C1-4, o -C(=O)alquilo C1-2, donde el alquilo y el cicloalquilo en todos los usos están opcionalmente sustituidos con 1 - 3 halógenos; (b) D1, donde D1 es -CO2H, -CO2-alquilo C1-4, o -C(=O)NR2R3; (c) -alquil C1-4-D1, donde el alquilo está opcionalmente sustituido con 1 - 3 halógenos; (d) -cicloalquil C3-6-D1, donde el cicloalquilo está opcionalmente sustituido con 1 - 2 grupos que son independientemente -alquilo C1-2 o halógeno, donde el -alquilo C1-2 está opcionalmente sustituido con 1 - 3 halógenos; (e) -cicloalquil C3-6-CH2-D1, donde el cicloalquilo está opcionalmente sustituido con 1 - 2 grupos que son independientemente -alquilo C1-2 o halógeno, donde el -alquilo C1-2 está opcionalmente sustituido con 1 - 3 halógenos; (f) -fenil-D1, donde el fenilo está opcionalmente sustituido con 1 - 3 sustituyentes que son independientemente halógeno, -CN, -OH, -CH3, -CF3, -OCR3 o -OCF3; (g) -Het-D1, donde Het es un anillo heteroaromático de 5 - 6 miembros que tiene 1 - 4 grupos heteroátomo que son cada uno, independientemente, N, O, S, S(O), o S(O)2, donde Het está opcionalmente sustituido con 1 - 3 grupos que son independientemente halógeno, -CH3, -CF3, -OCH3 o -OCF3; o (h) -alquil C1-2-Het, donde Het está opcionalmente sustituido con 1 - 3 grupos que son independientemente -CH3, -CF3, -OCH3, -OCF3 o halógeno; cada uno de R2 y R3 es independientemente H o -alquilo C1-3, o R2 y R3 se unen opcionalmente para formar un grupo de unión que tiene 3 - 5 carbonos, produciendo de esta manera un grupo amida cíclica de 4 - 6 miembros; d es un número entero de 0 - 2; e es un número entero de 0 - 3; y f es un número entero de 0 - 2.
ARP110103977A 2010-10-29 2011-10-27 Inhibidor de cetp de oxazodilinona sustituida con amina ciclica AR083579A1 (es)

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US (1) US9221834B2 (es)
EP (1) EP2632269B1 (es)
JP (1) JP5852662B2 (es)
CN (1) CN103269592B (es)
AR (1) AR083579A1 (es)
AU (1) AU2011320665B2 (es)
CA (1) CA2814846A1 (es)
ES (1) ES2623759T3 (es)
TW (1) TW201305146A (es)
WO (1) WO2012058187A1 (es)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JO3210B1 (ar) 2011-10-28 2018-03-08 Merck Sharp & Dohme مثبط منصهر لبروتين نقل الكوليسترليستير اوكسازوليدينون ثمائي الحلقة
EP2844252B1 (en) * 2012-05-02 2016-11-30 Merck Sharp & Dohme Corp. Cyclic amine substituted heterocyclic compounds as cetp inhibitors
CN103958484B (zh) * 2012-07-19 2015-11-25 上海恒瑞医药有限公司 噁唑烷酮类衍生物、其制备方法及其在医药上的应用
CN102977044A (zh) * 2012-11-26 2013-03-20 盛世泰科生物医药技术(苏州)有限公司 一种3-(4-甲氧基苯基)-异噁唑-5-羧酸的制备方法
EP2934518B1 (en) 2012-12-19 2020-02-19 Merck Sharp & Dohme Corp. Spirocyclic cetp inhibitors
EP2934519B1 (en) 2012-12-20 2021-05-12 Merck Sharp & Dohme Corp. Therapeutic thiazolidinone compounds
CN105143193B (zh) * 2013-01-31 2017-12-15 株式会社钟根堂 作为cetp抑制剂的联芳基或杂环联芳基取代的环己烯衍生化合物
WO2015017302A2 (en) 2013-07-30 2015-02-05 Merck Sharp & Dohme Corp. Bicyclic ureas and thiadiazolidine-1,1-dioxides as cetp inhibitors
US9688630B2 (en) 2013-10-10 2017-06-27 Merck Sharp & Dohme Corp. 3,3′-disubstituted indolines as inhibitors of cholesterol ester transfer protein
CN105814064A (zh) 2013-12-17 2016-07-27 默沙东公司 作为胆固醇酯转运蛋白的抑制剂的稠合双环异噁唑啉类
US10011572B2 (en) 2014-07-29 2018-07-03 Merck Sharp & Dohme Corp. Monocyclic isoxazolines as inhibitors of cholesterol ester transfer protein
WO2016040223A1 (en) * 2014-09-09 2016-03-17 Bristol-Myers Squibb Company Cyclobutane containing carboxylic acid gpr120 modulators
EP3322420B1 (en) 2015-07-13 2021-12-29 Merck Sharp & Dohme Corp. Bicyclic heterocycles as inhibitors of cholesterol ester transfer protein
EP3687992A1 (en) * 2017-09-27 2020-08-05 Meiji Seika Pharma Co., Ltd. Crystalline forms of diazabicyclooctane derivatives and production process thereof

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AU1856997A (en) 1996-02-02 1997-08-22 Merck & Co., Inc. Method for raising hdl cholesterol levels
HN2005000340A (es) * 2004-07-02 2009-11-06 Merck Sharp & Dohme Inhibidores de cetp
DOP2005000123A (es) * 2004-07-02 2011-07-15 Merck Sharp & Dohme Inhibidores de cetp
KR20140107671A (ko) * 2005-12-30 2014-09-04 머크 샤프 앤드 돔 코포레이션 Ｃｅｔｐ 억제제로서 유용한 1,3-옥사졸리딘-2-온 유도체
JP5199121B2 (ja) 2005-12-30 2013-05-15 メルク・シャープ・エンド・ドーム・コーポレイション Ｃｅｔｐ阻害剤
US7910592B2 (en) 2005-12-30 2011-03-22 Merck Sharp & Dohme Corp. CETP inhibitors
WO2011028395A1 (en) * 2009-08-24 2011-03-10 Merck Sharp & Dohme Corp. Pyridyl oxazolidinone cetp inhibitor
JO3210B1 (ar) 2011-10-28 2018-03-08 Merck Sharp & Dohme مثبط منصهر لبروتين نقل الكوليسترليستير اوكسازوليدينون ثمائي الحلقة
EP2844252B1 (en) 2012-05-02 2016-11-30 Merck Sharp & Dohme Corp. Cyclic amine substituted heterocyclic compounds as cetp inhibitors

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CN103269592B (zh) 2016-05-11
EP2632269A1 (en) 2013-09-04
US9221834B2 (en) 2015-12-29
AU2011320665B2 (en) 2015-09-03
JP2013544805A (ja) 2013-12-19
WO2012058187A1 (en) 2012-05-03
CA2814846A1 (en) 2012-05-03
TW201305146A (zh) 2013-02-01
EP2632269B1 (en) 2017-03-15
JP5852662B2 (ja) 2016-02-03
ES2623759T3 (es) 2017-07-12
CN103269592A (zh) 2013-08-28
US20130331372A1 (en) 2013-12-12
AU2011320665A1 (en) 2013-05-09
EP2632269A4 (en) 2015-01-21

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