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ECSP13012704A - Moduladores del receptor gpr119 y el tratamiento de trastornos relacionados con este - Google Patents

Moduladores del receptor gpr119 y el tratamiento de trastornos relacionados con este

Info

Publication number
ECSP13012704A
ECSP13012704A ECSP13012704A ECSP13012704A EC SP13012704 A ECSP13012704 A EC SP13012704A EC SP13012704 A ECSP13012704 A EC SP13012704A EC SP13012704 A ECSP13012704 A EC SP13012704A
Authority
EC
Ecuador
Prior art keywords
fluoro
fluoropropan
oxadiazol
pyrimidin
piperidin
Prior art date
Application number
Other languages
English (en)
Inventor
M Jones Robert
Lehmann Juerg
Chen Weichao
Edwards Jeffrey
Marquez Glen
e morgan Michael
J M Sadeque Abu
Hee Kim Sun
Original Assignee
Arena Pharmaceuticals
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 Arena Pharmaceuticals filed Critical Arena Pharmaceuticals
Publication of ECSP13012704A publication Critical patent/ECSP13012704A/es

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    • 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
    • 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
    • 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
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
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    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • 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
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
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    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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    • A—HUMAN NECESSITIES
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
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    • A61P27/00—Drugs for disorders of the senses
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P27/02—Ophthalmic agents
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P3/04—Anorexiants; Antiobesity agents
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    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • 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
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00—Drugs for disorders of the cardiovascular system
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    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
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  • Obesity (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Psychology (AREA)
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  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Child & Adolescent Psychology (AREA)
  • Immunology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La presente invención se refiere a los agonistas del receptor GPR119: 3-fluoro-4-(5-fluoro-6-(4-(3-(2-fluoropropan-2-il)-1,2,4-oxadiazol-5-il)piperidin-1-il)pirimidin-4-ilamino)-N,N-dimetilbenzamida; 3-fluoro-4-(5-fluoro-6-(4-(3-(2-fluoropropan-2-il)-1,2,4-oxadiazol-5-il)piperidin-1-il)pirimidin-4-ilamino)-N-metilbenzamida; y 3-fluoro-4-(5-fluoro-6-(4-(3-(2-fluoropropan-2-il)-1,2,4-oxadiazol-5-il)piperidin-1-il)pirimidin-4-ilamino)benzamida, y a sales, solvatos e hidratos farmacéuticamente aceptables de estos, que son útiles como un agente farmacéutico único o combinados con uno o más agentes farmacéuticos adicionales tales como un inhibidor de DPP-IV, una biguanida, un inhibidor de alfa-glucosidasa, un análogo de insulina, una sulfonilurea, un inhibidor de SGLT2, una meglitinida, una tiazolidinodiona, o un análogo peptídico antidiabético, en el tratamiento de, por ejemplo, un trastorno seleccionado entre: un trastorno relacionado con el receptor GPR119, una afección mejorada al incrementar la secreción de una incretina, una afección mejorada al incrementar el nivel de incretina en sangre, una afección caracterizada por una masa ósea baja, un trastorno neurológico, un trastorno relacionado con el metabolismo, diabetes de tipo 2, obesidad, y complicaciones relacionadas con estos.
ECSP13012704 2010-09-22 2013-06-19 Moduladores del receptor gpr119 y el tratamiento de trastornos relacionados con este ECSP13012704A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US38541010P 2010-09-22 2010-09-22
US201161478262P 2011-04-22 2011-04-22

Publications (1)

Publication Number Publication Date
ECSP13012704A true ECSP13012704A (es) 2013-08-30

Family

ID=44721104

Family Applications (1)

Application Number Title Priority Date Filing Date
ECSP13012704 ECSP13012704A (es) 2010-09-22 2013-06-19 Moduladores del receptor gpr119 y el tratamiento de trastornos relacionados con este

Country Status (22)

Country Link
US (2) US10894787B2 (es)
EP (2) EP2619198A1 (es)
JP (1) JP5941916B2 (es)
KR (1) KR101871011B1 (es)
CN (2) CN103221410B (es)
AU (2) AU2011305525B2 (es)
BR (1) BR112013008100A2 (es)
CA (1) CA2812061A1 (es)
CL (1) CL2013000785A1 (es)
CO (1) CO6700841A2 (es)
CR (1) CR20130145A (es)
DO (1) DOP2013000061A (es)
EA (1) EA201390421A1 (es)
EC (1) ECSP13012704A (es)
GT (1) GT201300075A (es)
HK (1) HK1254745A1 (es)
MX (1) MX2013003184A (es)
NI (1) NI201300030A (es)
PE (1) PE20131371A1 (es)
PH (1) PH12013500547A1 (es)
SG (1) SG188548A1 (es)
WO (1) WO2012040279A1 (es)

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JP5856980B2 (ja) 2010-01-27 2016-02-10 アリーナ ファーマシューティカルズ， インコーポレイテッド （Ｒ）−２−（７−（４−シクロペンチル−３−（トリフルオロメチル）ベンジルオキシ）−１，２，３，４−テトラヒドロシクロペンタ［ｂ］インドール−３−イル）酢酸およびその塩の調製のためのプロセス
CN103221410B (zh) * 2010-09-22 2017-09-15 艾尼纳制药公司 Gpr119受体调节剂和对与其相关的障碍的治疗
ES2602813T3 (es) 2011-06-09 2017-02-22 Rhizen Pharmaceuticals S.A. Nuevos compuestos como moduladores de GPR-119
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WO2014074668A1 (en) 2012-11-08 2014-05-15 Arena Pharmaceuticals, Inc. Modulators of gpr119 and the treatment of disorders related thereto
EP4445956A3 (en) 2015-01-06 2024-12-04 Arena Pharmaceuticals, Inc. Compound for use in treating conditions related to the s1p1 receptor
PL3310760T3 (pl) 2015-06-22 2023-03-06 Arena Pharmaceuticals, Inc. Krystaliczna sól L-argininy kwasu (R)-2-(7-(4-cyklopentylo-3-(trifluorometylo)benzyloksy)- 1,2,3,4-tetrahydrocyklo-penta[b]indol-3-ilo)octowego do zastosowania w zaburzeniach związanych z receptorem S1P1
MA47504A (fr) 2017-02-16 2019-12-25 Arena Pharm Inc Composés et méthodes de traitement de l'angiocholite biliaire primitive
ES2987794T3 (es) 2018-06-06 2024-11-18 Arena Pharm Inc Procedimientos de tratamiento de afecciones relacionadas con el receptor S1P1
RS64972B1 (sr) 2019-06-10 2024-01-31 Lupin Ltd Inhibitori prmt5
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