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CR20200643A - Nuev0s compuestos de piridina y pirazina com0 inhibidores del receptor connabinoide 2 - Google Patents

Nuev0s compuestos de piridina y pirazina com0 inhibidores del receptor connabinoide 2

Info

Publication number
CR20200643A
CR20200643A CR20200643A CR20200643A CR20200643A CR 20200643 A CR20200643 A CR 20200643A CR 20200643 A CR20200643 A CR 20200643A CR 20200643 A CR20200643 A CR 20200643A CR 20200643 A CR20200643 A CR 20200643A
Authority
CR
Costa Rica
Prior art keywords
inhibitors
cannabinoid receptor
pyrazine compounds
novel pyridine
sup
Prior art date
Application number
CR20200643A
Other languages
English (en)
Inventor
Uwe Grether
Luca Gobbi
Julian Kretz
Simon M Ametamey
Original Assignee
Eth Zuerich
Hoffmann La Roche
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 Eth Zuerich, Hoffmann La Roche filed Critical Eth Zuerich
Publication of CR20200643A publication Critical patent/CR20200643A/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P23/00Anaesthetics
    • A61P23/02Local anaesthetics
    • 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
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Cardiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Anesthesiology (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Vascular Medicine (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Transplantation (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Neurology (AREA)
  • Hospice & Palliative Care (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)

Abstract

La invención se refiere a un compuesto de fórmula (I) <img src="data:image/png;base64,iVBORw0KGgoAAAANSUhEUgAAAUcAAABhCAYAAABFy2P0AAAAAXNSR0IArs4c6QAAAARnQU1BAACxjwv8YQUAAAAJcEhZcwAADsMAAA7DAcdvqGQAAB70SURBVHhe7Z0JvE3VHsdXGgwhQ+a8SMaSFyLTe5XCiz5RhjRIhicZylMqeoU0iBClUhLqGVNPmZ5ClCmVnjLkEZJSGUIayH77+79r37vPce6559x7z3Cv//fzOZ979trn3r3v2Xv/1n9aa53muBhFURQlgDz2p6IoiuJDxVFRFCUEKo6KoighUHFUFEUJgYqjoihKCFQcFUVRQqClPErCOX78uHn++efN999/b+rUqWNat25t98SOZ5991uzdu9c0atTItGjRwrYqShpqOSoJ5ciRI6Zly5Zm3bp1pkSJEmbgwIFmzJgxdm/2c+LECdO2bVszZ84cOV6fPn3MlClT7F5FSUPFUUko//vf/8yxY8fM5MmTTd++fc0LL7xgZsyYYfdmP4cOHTLFixc38+fPl+PdeeedZvz48XavoqShbrVyEn/88YeZNWuWWbBggbi8VatWNR07djSVK1e2n4gdw4YNMx9++KEcO5b8/vvvZvny5eahhx4y/fv3N+3atbN7FCUFtRyVADZt2mSqV69uevXqZX744Qdz9tlnmwkTJpgqVaqY119/3X4qNkydOtU8/PDDZsSIEbYldmCxDh8+3Bw4cMAUKVLEtipKGmo5KqkcPXrU1KpVyxQsWNAsXbo0VTSI0yFYDzzwgFmxYoVp3LixtGcEv8ffxBL132Z58uQxhQsXtlspEPe7++67zezZs03Tpk1ta3Skd7zTTz/dFCpUyG4Fwv9z1113Scwzb968tlVRXBBHRYHp06ejKM7WrVttSyANGzZ0Lr74YscVIdsSnm3btjmlS5d2ypUr55x33nmpL1cYnbZt2zo//vijfO5f//qXU6lSJWf37t2ynVk+/fRTp1SpUgHH4uWKveMKruNaic7PP//s/OMf/7C/4TiHDx92qlWr5hw5csS2KEoKajkqqdx6661iSe3cudO2BEL5C9Ydrmiw5ReKzZs3i4vuip+pXbu2bTVmw4YNEsPs0qWLGTx4sClbtqxp3769lNVg+RUoUMD06NEjaktu5cqV8jdItlxwwQW21Zi1a9eaTp06mW7duknypWLFiqZNmzZyTFzrYsWKSULotNNOs7+hKBpzVHysX7/euNah3ToZ3G1c140bN9qW8HhiQ0LH/6KUBqF69dVXza5du8xNN90kiR9EbdmyZZKQwTWOFu94NWrUCDjebbfdZgYNGmRefvllc8YZZxjXwjS//PKLZMYbNGggLr0KoxKMWo5KKgjFWWedZd5//33bEsgrr7xiunfvLoLmusq2NX22bNliXJdVxBQL0oPSHSxJYoEIcnaxatUqEXeKyalh9NOkSRMRRKxIYp6KkhEqjkoqTz/9tCRd9u/fHzKBgdu9aNEiEZ9ILK0vv/xSxLFVq1amZMmSYrXxevfdd6X4+6233jJ169a1n846a9asMZdffrlYpuecc46IILf3xx9/bPbt2yfJnssuu8x+WlHCo12okgquLtbcvffea1vSWL16tZTyDBkyJGoXlL+JKBLLfO6550ylSpWklMYvjFiXWHbZgSfCBw8eFFeaou8dO3aoMCrRgeUYLWQZ27Rp47iWgW1RcguuADpnnnmm07x5c+fFF1903nnnHadTp06Sxb7xxhvtpyJj8+bN8nuu8NkWx3Fdc8cVV2fu3Lm2JYX69es7rijbrcyxcuVKOZ5r2doWx3n77belbcqUKbZFUSIjU+I4aNAgueFuv/1226LkJjZt2uR07NhRymAqVqzo1KlTx3nhhRfs3sjxxBHR8nPzzTeLQPpLdxCxfPnyOd9++61tiR5PHDmuH0/c9+zZY1sUJWOiFkesANdlcaZOnSoWxrvvvmv3KEogiCyi9MEHH9iWFKgtLFq0qHPNNdcE1Ew2aNDAad26td2KHo7D8Tiun0OHDjnFihVzWrVqZVsUJWOijjmSrbzuuuskON+5c2cZvO/+HbtXyQ389ttvMu6Ysh2g9pDtaK+z23lKDaNrEdqWFCgJonyGkhr+rsdrr70mSZolS5bYlujgOByP4/ohuUSNJnWQlAopSkSIREYI8Sd+Ze/evbLNaAOsx+eff162ldzB+vXrnXPPPTd11Mh//vMfcbEjHRnjwee5R/744w/bEgh/HyvSD6NXatasabeiI73jeHAuOhJGiZSILUesCbKZjzzyiJRlACMZGHN7//33m59++knalJwPFmP+/PlTs9LufRKwHSl8nnskvbpCJrXAivTDrDzUR7744ou2JXI4ztatW9O9FzkXjqkokRCxOOKWMIqBkQZ+GE5GqQTDwJTcAaLmF8Lg7ViCCDMLUO/evaXeMhr27Nkj5UHM8K0oWSUicfzuu++k9m3SpEknxXOAsbPM3kyvrShZ5fbbb5cROEOHDrUtkdG1a1dTv359mV5NUbJKROLIhKD16tWTkQ6hYFRCs2bNxIpUlOxg+vTp5plnnpH5JSOBYYgLFy6UUT6Kkh1kKI5kFCdOnChWYziYRIDZmxcvXmxbFCXz0OEyO3ekHS7x8J49e5qaNWvaFkXJGhmKI6U6uDnMdBKOMmXKmH79+qn1qGQbY8eOlc523rx5tiU0LJbF+Olo3XBFCUdYcXzjjTfMBx98YEaPHm1bwvPUU0/J+FmSN4qSVUqXLm0effRRmYsxvSnMqMHEYkRIzz33XNuqKFknXXHkpmMy0lGjRpmiRYva1vAw2H/cuHGyDgi/n6wwwUEynB+LPIWCUhr2UUJzqjNgwAApv+E+DAVxSa4nqwgmA1wzJuj45z//KbF6itqZoi2ZoCzPK/CH//73vzJN3eHDh21LCnRIfJZnxXv5fy8cv/76q32Xg6HYMRRuj+0UL17cOX78uG2JnAsvvNC566677FbyMH78eKd69epOmTJlnD/96U9O+fLlHdfKzbB4OFYwVK5x48aOK4S2JYVVq1bJ+e3atcu2xBeWG+D4FE0DReBVqlSR94nAFRgZfOCfUAL27dsnSyC4Ho5tSSxr1qxxqlat6hQoUMC5/PLLnSZNmsgY8ho1ajjffPON/VRiWbFihdOtWzd5z3WtXbu2U7ZsWVnOgufd9f5kH7z66qtyH5x//vmpL56Z4cOH20+kD0ttdOjQwXHF1bbkPEKK49dffy034/z5821LdDDGlfHXrCGSLNx3333yP7kWhrN06VLn448/dtze3TnrrLNkBhpGc8QbHh7OybUwbEsK7733nrQn6vtLNnGEv/zlLydNdMI2a9okAzwziGKzZs0CRJxrWLlyZTEYvO8zUWDoMPpo8eLFco25x4YNGyYj3hg5xFo+tA0dOlQ+/+STT8oIOEZMffbZZ/LCmPB+LyNYJ2jgwIF2K+cRUhyZkaVu3bp2K3MgOFdeeaXdSizcDFzQ1157zbaksW7dOtnHVF3xhu8Hy4fjf/TRR7bVEfGmbfv27bYlviSjOPJg8p3QqYHrCopVxs9kgE6XyS1CdbLMPsS5440lkgkTJji1atWS93gs119/vbz3M2LEiFSvDyuS/ymYZ555Rr57FiwLx9q1a51ChQo5P/zwg23JWZwkjqtXr5YLGTztU7TQk2I9JsOsPfRg9NzpcdVVV2V6PG9WwKXp0qWLWJCIj+deqziG5u9//3vqeTRq1Cjq+SVjxbFjx0REunfvbltO5uqrr3YuvfRSu5UYLrroIufBBx+U++zss892/v3vf9s9oUEcmT0pWPAR+7x580oYIRz8Hi77qFGjbEvOIiAh426bPn36yBBBFibKCuedd55xL4RkEhMNs1iHW2uZFet (***)
CR20200643A 2018-06-27 2019-06-25 Nuev0s compuestos de piridina y pirazina com0 inhibidores del receptor connabinoide 2 CR20200643A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP18180137 2018-06-27
PCT/EP2019/066811 WO2020002320A1 (en) 2018-06-27 2019-06-25 Novel pyridine and pyrazine compounds as inhibitors of cannabinoid receptor 2

Publications (1)

Publication Number Publication Date
CR20200643A true CR20200643A (es) 2021-05-11

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CR20200643A CR20200643A (es) 2018-06-27 2019-06-25 Nuev0s compuestos de piridina y pirazina com0 inhibidores del receptor connabinoide 2

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US (2) US12071420B2 (es)
EP (1) EP3814329B1 (es)
JP (1) JP7445610B2 (es)
CN (2) CN112262132A (es)
AU (2) AU2019294256B2 (es)
BR (1) BR112020025013A2 (es)
CA (1) CA3096777A1 (es)
CL (1) CL2020003331A1 (es)
CO (1) CO2020011855A2 (es)
CR (1) CR20200643A (es)
IL (1) IL279725B2 (es)
MA (1) MA53002A (es)
MX (1) MX2020012760A (es)
PE (1) PE20210368A1 (es)
PH (1) PH12020552152A1 (es)
SG (1) SG11202009103WA (es)
WO (1) WO2020002320A1 (es)

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WO2020002270A1 (en) 2018-06-27 2020-01-02 F. Hoffmann-La Roche Ag Pyridine and pyrazine derivatives as preferential cannabinoid 2 agonists
MA53002A (fr) 2018-06-27 2021-05-05 Eth Zuerich Nouveaux composés de pyridine et de pyrazine en tant qu'inhibiteurs du récepteur cannabinoïde 2
EP3995155A1 (en) 2018-06-27 2022-05-11 F. Hoffmann-La Roche AG Radiolabeled cannabinoid receptor 2 ligand
EP3814328A1 (en) 2018-06-27 2021-05-05 F. Hoffmann-La Roche AG Novel azetidine-substituted pyridine and pyrazine compounds as inhibitors of cannabinoid receptor 2
JP2024541968A (ja) 2021-10-28 2024-11-13 ジェネンテック, インコーポレイテッド 治療的介入のためにmhc関連抗原を同定するためのシステムおよび方法

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