AR088565A1 - Inhibidor de cetp de oxazolidinona biciclico fusionado - Google Patents
Inhibidor de cetp de oxazolidinona biciclico fusionadoInfo
- Publication number
- AR088565A1 AR088565A1 ARP120104037A ARP120104037A AR088565A1 AR 088565 A1 AR088565 A1 AR 088565A1 AR P120104037 A ARP120104037 A AR P120104037A AR P120104037 A ARP120104037 A AR P120104037A AR 088565 A1 AR088565 A1 AR 088565A1
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- alkyl
- alkynyl
- alkenyl
- optionally substituted
- halogens
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
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- 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
- A61K31/424—Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
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- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
- A61P9/10—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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Obesity (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Reivindicación 1: Un compuesto de fórmula (1), o una sal farmacéuticamente aceptable del mismo, en la que R¹ es H, -alquilo C₁₋₅, -O-alquilo C₁₋₅, -alquenilo C₂₋₅, -O-alquenilo C₂₋₅, -alquinilo C₂₋₅, -O-alquinilo C₂₋₅, -OH, halógeno, -CN, -NR⁶R⁷, -CO₂R⁸, -C(O)NR⁶R⁷, -SO₂NR⁶R⁷, HET⁽³⁾, o cicloalquilo C₃₋₆ que tiene opcionalmente 1 - 2 dobles enlaces, en la que -alquilo C₁₋₅, -O-alquilo C₁₋₅, -alquenilo C₂₋₅, -O-alquenilo C₂₋₅, -alquinilo C₂₋₅ y -O-alquinilo C₂₋₅ están cada uno opcionalmente sustituido con 1 - 7 halógenos, y en la que HET⁽³⁾ y cicloalquilo C₃₋₆ que tiene opcionalmente 1 - 2 dobles enlaces están opcionalmente sustituidos con 1 - 3 grupos de sustituyentes que son cada uno independientemente halógeno, -alquilo C₁₋₃, -O-alquilo C₁₋₃, -alquenilo C₂₋₃, -O-alquenilo C₂₋₃, -alquinilo C₂₋₃ o -O-alquinilo C₂₋₃, en la que -alquilo C₁₋₃, -O-alquilo C₁₋₃, -alquenilo C₂₋₃, -O-alquenilo C₂₋₃, -alquinilo C₂₋₃ y -O-alquinilo C₂₋₃ están cada uno opcionalmente sustituido con 1 - 7 halógenos; cada uno de R⁶ y R⁷ es independientemente H o -alquilo C₁₋₅; R⁸ es H o -alquilo C₁₋₅ opcionalmente sustituido con 1 - 7 halógenos; HET⁽³⁾ es un anillo heterocíclico de 3 - 6 miembros que tiene 1 - 3 grupos de heteroátomos que son cada uno independientemente N, NH, O, S, S(O) o S(O)₂ y que tiene opcionalmente 1 - 3 dobles enlaces; x es 0 ó 1; las líneas discontinuas en la fórmula (1) representan un doble enlace opcional entre 2 átomos de carbono adyacentes; D¹ es N o CR²; D² es N o CR³; D³ es N o CR⁴; cada uno de R², R³ y R⁴ es independientemente H, -alquilo C₁₋₅, -O-alquilo C₁₋₅, -alquenilo C₂₋₅, -O-alquenilo C₂₋₅, -alquinilo C₂₋₅, -O-alquinilo C₂₋₅, -OH, halógeno, -CN, -NR⁶R⁷, -CO₂R⁸, -C(O)NR⁶R⁷ o -SO₂NR⁶R⁷, donde -alquilo C₁₋₅, -O-alquilo C₁₋₅, -alquenilo C₂₋₅, -O-alquenilo C₂₋₅, -alquinilo C₂₋₅ y -O-alquinilo C₂₋₅ están opcionalmente sustituidos con 1 - 7 halógenos; cada R⁵ es independientemente -alquilo C₁₋₅, -O-alquilo C₁₋₅, -alquenilo C₂₋₅, -O-alquenilo C₂₋₅, -alquinilo C₂₋₅, -O-alquinilo C₂₋₅, -OH, halógeno, -CN, -NR⁶R⁷, -CO₂R⁸, -C(O)NR⁶R⁷ o -SONR⁶R⁷, donde -alquilo C₁₋₅, -O-alquilo C₁₋₅, -alquenilo C₂₋₅, -O-alquenilo C₂₋₅, -alquinilo C₂₋₅ y -O-alquinilo C₂₋₅ están opcionalmente sustituidos con 1 - 7 halógenos; A¹ es fenilo, HET⁽¹⁾, o cicloalquilo C₃₋₈ que tiene opcionalmente 1 - 2 dobles enlaces, donde A¹ está opcionalmente sustituido con un grupo sustituyente Z y está opcionalmente sustituido con 1 - 3 grupos que son cada uno independientemente -alquilo C₁₋₅, -O-alquilo C₁₋₅, -alquenilo C₂₋₅, -O-alquenilo C₂₋₅, -alquinilo C₂₋₅, -O-alquinilo C₂₋₅, halógeno, -OH o -CN, donde -alquilo C₁₋₅, -O-alquilo C₁₋₅, -alquenilo C₂₋₅, -O-alquenilo C₂₋₅, -alquinilo C₂₋₅ y -O-alquinilo C₂₋₅ están opcionalmente sustituidos con 1 - 7 halógenos; cada HET⁽¹⁾ es un anillo heteroaromático de 5 ó 6 miembros que tiene 1 - 4 grupos de heteroátomos que son cada uno independientemente -N-, -NH-, -S-, -O-, -S(O)- o -S(O)₂-, que tiene opcionalmente un grupo -C(=O)-, y que tiene opcionalmente 1 - 3 dobles enlaces; Z es A³, -alquileno C₁₋₃-CO₂R⁸, -alquileno C₁₋₃-C(O)NR⁶R⁷, -alquileno C₁₋₃-SO₂NR⁶R⁷, -CO₂R⁸, -C(O)NR⁶R⁷, -SO₂NR⁶R⁷ o -alquileno C₁₋₃-HET⁽²⁾, donde -alquileno C₁₋₃ en todos los usos está opcionalmente sustituido con 1 - 7 halógenos, y HET⁽²⁾ está opcionalmente sustituido con 1 - 3 sustituyentes que son independientemente -alquilo C₁₋₃ opcionalmente sustituido con 1 - 5 halógenos, -O-alquilo C₁₋₃ opcionalmente sustituido con 1 - 5 halógenos, halógeno o NR⁶R⁷; A³ es fenilo, cicloalquilo C₃₋₆ que tiene opcionalmente 1 - 2 dobles enlaces, o HET⁽¹⁾, donde A³ está opcionalmente sustituido con 1 - 3 grupos que son cada uno independientemente -alquilo C₁₋₅, -O-alquilo C₁₋₅, -alquenilo C₂₋₅, -O-alquenilo C₂₋₅, -alquinilo C₂₋₅, -O-alquinilo C₂₋₅, halógeno, -OH, o -CN, donde -alquilo C₁₋₅, -O-alquilo C₁₋₅, -alquenilo C₂₋₅, -O-alquenilo C₂₋₅, -alquinilo C₂₋₅ y -O-alquinilo C₂₋₅ están opcionalmente sustituidos con 1 - 7 halógenos; y A³ está opcionalmente sustituido con un grupo que es HET⁽²⁾, -alquileno C₁₋₄-CO₂R⁸, -alquileno C₁₋₄-C(O)NR⁶R⁷, -alquileno C₁₋₄-SO₂NR⁶R⁷, -CO₂R⁸, -C(O)NR⁶R⁷ o -SO₂NR⁶R⁷, donde -alquileno C₁₋₄ en todos los usos está opcionalmente sustituido con 1 - 7 halógenos; y donde HET⁽²⁾ está opcionalmente sustituido con 1 - 3 grupos que son cada uno independientemente halógeno, -alquilo C₁₋₅ opcionalmente sustituido con 1 - 7 halógenos, -O-alquilo C₁₋₅ opcionalmente sustituido con 1 - 7 halógenos, o NR⁶R⁷; HET⁽²⁾ es un anillo heterocíclico de 5 - 6 miembros que tiene 1 - 3 grupos de heteroátomos que son cada uno independientemente N, NH, O ó S, que tiene opcionalmente un grupo -C(=O), y que tiene opcionalmente 1 - 3 dobles enlaces; A² es fenilo o HET⁽¹⁾, donde A² está opcionalmente sustituido con 1 - 3 grupos de sustituyentes que son cada uno independientemente -alquilo C₁₋₅, -O-alquilo C₁₋₅, -alquenilo C₂₋₅, -O-alquenilo C₂₋₅, -alquinilo C₂₋₅, -O-alquinilo C₂₋₅, halógeno, -CN, -OH o cicloalquilo C₃₋₆, donde -alquilo C₁₋₅, -O-alquilo C₁₋₅, -alquenilo C₂₋₅, -O-alquenilo C₂₋₅, -alquinilo C₂₋₅ y -O-alquinilo C₂₋₅ están opcionalmente sustituidos con 1 - 7 halógenos, y cicloalquilo C₃₋₆ está opcionalmente sustituido con 1 - 3 sustituyentes que son cada uno independientemente halógeno, -alquilo C₁₋₃ o -O-alquilo C₁₋₃, donde -alquilo C₁₋₃ y -O-alquilo C₁₋₃ están cada uno opcionalmente sustituido con 1 - 7 halógenos; y a es 0 o un número entero de 1 - 3.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161552592P | 2011-10-28 | 2011-10-28 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR088565A1 true AR088565A1 (es) | 2014-06-18 |
Family
ID=47143312
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120104037A AR088565A1 (es) | 2011-10-28 | 2012-10-26 | Inhibidor de cetp de oxazolidinona biciclico fusionado |
Country Status (41)
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201007286D0 (en) | 2010-04-30 | 2010-06-16 | Astex Therapeutics Ltd | New compounds |
| WO2012058187A1 (en) | 2010-10-29 | 2012-05-03 | Merck Sharp & Dohme Corp. | Cyclic amine substituted oxazolidinone cetp inhibitor |
| GB201020179D0 (en) | 2010-11-29 | 2011-01-12 | Astex Therapeutics Ltd | New compounds |
| GB201118656D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118675D0 (en) | 2011-10-28 | 2011-12-14 | Astex Therapeutics Ltd | New compounds |
| GB201118654D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118652D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201209613D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| GB201209609D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| WO2014099836A1 (en) | 2012-12-19 | 2014-06-26 | Merck Sharp & Dohme Corp. | Spirocyclic cetp inhibitors |
| WO2014099834A1 (en) | 2012-12-20 | 2014-06-26 | Merck Sharp & Dohme Corp. | Therapeutic thiazolidinone compounds |
| EP2943474B1 (en) * | 2013-01-31 | 2017-07-05 | Chong Kun Dang Pharmaceutical Corp. | Biaryl- or heterocyclic biaryl-substituted cyclohexene derivative compounds as cetp inhibitors |
| GB201307577D0 (en) | 2013-04-26 | 2013-06-12 | Astex Therapeutics Ltd | New compounds |
| WO2015017302A2 (en) | 2013-07-30 | 2015-02-05 | Merck Sharp & Dohme Corp. | Bicyclic ureas and thiadiazolidine-1,1-dioxides as cetp inhibitors |
| US9937153B2 (en) * | 2013-08-30 | 2018-04-10 | Merck Sharp & Dohme Ltd. | Oral pharmaceutical formulation of omarigliptin |
| EP3054945B1 (en) | 2013-10-10 | 2018-08-15 | Merck Sharp & Dohme Corp. | 3,3'-disubstituted indolines as inhibitors of cholesterol ester transfer protein |
| US9663534B2 (en) | 2013-12-17 | 2017-05-30 | Merck Sharp & Dohme Corp. | Fused bicyclic isoxazolines as inhibitors of cholesterol ester transfer protein |
| EA032689B1 (ru) | 2014-02-05 | 2019-07-31 | Дезима Фарма Б.В. | Ингибитор белка-переносчика эфира холестерина (cetp) и фармацевтические композиции, содержащие указанный ингибитор для применения для лечения или предотвращения сердечно-сосудистых заболеваний |
| HUE053653T2 (hu) | 2014-03-26 | 2021-07-28 | Astex Therapeutics Ltd | FGFR inhibitor és IGF1R inhibitor kombinációi |
| AU2015238301B2 (en) | 2014-03-26 | 2020-06-25 | Astex Therapeutics Ltd | Combinations |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| WO2016018729A1 (en) | 2014-07-29 | 2016-02-04 | Merck Sharp & Dohme Corp. | Monocyclic isoxazolines as inhibitors of cholesterol ester transfer protein |
| WO2016067194A1 (en) * | 2014-10-27 | 2016-05-06 | Sun Pharmaceutical Industries Limited | Process for the preparation of anacetrapib and an intermediate thereof |
| JPWO2016084949A1 (ja) * | 2014-11-28 | 2017-09-07 | 興和株式会社 | 医薬 |
| JOP20200201A1 (ar) | 2015-02-10 | 2017-06-16 | Astex Therapeutics Ltd | تركيبات صيدلانية تشتمل على n-(3.5- ثنائي ميثوكسي فينيل)-n'-(1-ميثيل إيثيل)-n-[3-(ميثيل-1h-بيرازول-4-يل) كينوكسالين-6-يل]إيثان-1.2-ثنائي الأمين |
| US10478494B2 (en) | 2015-04-03 | 2019-11-19 | Astex Therapeutics Ltd | FGFR/PD-1 combination therapy for the treatment of cancer |
| CN109996757A (zh) * | 2015-06-12 | 2019-07-09 | 罗地亚经营管理公司 | 含枝状体的混合纳米粒子、生产此类混合纳米粒子的方法以及它们的用途 |
| EP3322420B1 (en) | 2015-07-13 | 2021-12-29 | Merck Sharp & Dohme Corp. | Bicyclic heterocycles as inhibitors of cholesterol ester transfer protein |
| KR102703498B1 (ko) | 2015-09-23 | 2024-09-04 | 얀센 파마슈티카 엔브이 | 신규 화합물 |
| CA2996989C (en) | 2015-09-23 | 2023-10-03 | Janssen Pharmaceutica Nv | Bi-heteroaryl substituted 1,4-benzodiazepines and uses thereof for the treatment of cancer |
| CN106432058A (zh) * | 2016-09-17 | 2017-02-22 | 青岛云天生物技术有限公司 | 一种Niraparib中间体4‑（3S‑哌啶‑3‑基）苯胺的制备方法 |
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