RU2020112117A - Кристаллическое вещество - Google Patents
Кристаллическое вещество Download PDFInfo
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- RU2020112117A RU2020112117A RU2020112117A RU2020112117A RU2020112117A RU 2020112117 A RU2020112117 A RU 2020112117A RU 2020112117 A RU2020112117 A RU 2020112117A RU 2020112117 A RU2020112117 A RU 2020112117A RU 2020112117 A RU2020112117 A RU 2020112117A
- Authority
- RU
- Russia
- Prior art keywords
- crystalline substance
- diphenylpyrazin
- butyloxy
- isopropylamino
- acetic acid
- Prior art date
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- 239000000126 substance Substances 0.000 title claims 9
- OJQMKCBWYCWFPU-UHFFFAOYSA-N ACT-333679 Chemical compound C=1C=CC=CC=1C1=NC(N(CCCCOCC(O)=O)C(C)C)=CN=C1C1=CC=CC=C1 OJQMKCBWYCWFPU-UHFFFAOYSA-N 0.000 claims 6
- 239000004480 active ingredient Substances 0.000 claims 3
- 238000010521 absorption reaction Methods 0.000 claims 2
- 238000000862 absorption spectrum Methods 0.000 claims 2
- 238000000113 differential scanning calorimetry Methods 0.000 claims 2
- 238000000634 powder X-ray diffraction Methods 0.000 claims 2
- 230000005855 radiation Effects 0.000 claims 2
- 238000001228 spectrum Methods 0.000 claims 2
- 206010002383 Angina Pectoris Diseases 0.000 claims 1
- 208000031104 Arterial Occlusive disease Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 1
- 206010012665 Diabetic gangrene Diseases 0.000 claims 1
- 102000009079 Epoprostenol Receptors Human genes 0.000 claims 1
- 108010073099 Epoprostenol Receptors Proteins 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 206010022562 Intermittent claudication Diseases 0.000 claims 1
- 208000029523 Interstitial Lung disease Diseases 0.000 claims 1
- 206010039710 Scleroderma Diseases 0.000 claims 1
- 208000007536 Thrombosis Diseases 0.000 claims 1
- 206010048302 Tubulointerstitial nephritis Diseases 0.000 claims 1
- 208000021328 arterial occlusion Diseases 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 239000002178 crystalline material Substances 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 230000003383 glomerulonephritic effect Effects 0.000 claims 1
- 230000001771 impaired effect Effects 0.000 claims 1
- 208000021156 intermittent vascular claudication Diseases 0.000 claims 1
- 201000006334 interstitial nephritis Diseases 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 201000008383 nephritis Diseases 0.000 claims 1
- 230000003836 peripheral circulation Effects 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 1
- 208000002815 pulmonary hypertension Diseases 0.000 claims 1
- 239000000018 receptor agonist Substances 0.000 claims 1
- 229940044601 receptor agonist Drugs 0.000 claims 1
- 208000005198 spinal stenosis Diseases 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D241/20—Nitrogen atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- 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
-
- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/14—Antitussive agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
- A61P9/08—Vasodilators for multiple indications
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D241/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
-
- 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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pulmonology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Vascular Medicine (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Analysing Materials By The Use Of Radiation (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Steroid Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Cephalosporin Compounds (AREA)
Claims (9)
1. Кристаллическое вещество формы-I 2-{4-[N-(5,6-дифенилпиразин-2-ил)-N-изопропиламино]бутилокси}уксусной кислоты, которое показывает дифракционные пики при углах дифракции (2θ) 6,4, 8,1, 9,5, 10,9, 13,2, 15,7, 17,0, 19,5, 20,3, 21,0 и 22,8 в спектре порошковой рентгеновской дифракции, полученном с использованием Cu-Kα-излучения (λ=1,54 Å).
2. Кристаллическое вещество формы-I 2-{4-[N-(5,6-дифенилпиразин-2-ил)-N-изопропиламино]бутилокси}уксусной кислоты, которое показывает пики поглощения при волновых числах 2874 см-1, 1736 см-1 1558 см-1, 1375 см-1, 1126 см-1 и 696 см-1 в инфракрасном спектре поглощения.
3. Кристаллическое вещество формы-I 2-{4-[N-(5,6-дифенилпиразин-2-ил)-N-изопропиламино]бутилокси}уксусной кислоты, которое имеет эндотермический пик при 127°С в дифференциальной сканирующей калориметрии.
4. Кристаллическое вещество формы-II 2-{4-[N-(5,6-дифенилпиразин-2-ил)-N-изопропиламино]бутилокси}уксусной кислоты, которое показывает дифракционные пики при углах дифракции (2θ) 9,6, 11,4, 11,7, 16,3, 17,5, 18,5, 18,7, 19,9, 20,1, 21,0 и 24,6 в спектре порошковой рентгеновской дифракции, полученном с использованием Cu-Kα-излучения (λ=1,54 Å).
5. Кристаллическое вещество формы-II 2-{4-[N-(5,6-дифенилпиразин-2-ил)-N-изопропиламино]бутилокси}уксусной кислоты, которое показывает пики поглощения при волновых числах 2867 см-1, 1749 см-1 1568 см-1, 1382 см-1, 1131 см-1 и 701 см-1 в инфракрасном спектре поглощения.
6. Кристаллическое вещество формы-II 2-{4-[N-(5,6-дифенилпиразин-2-ил)-N-изопропиламино]бутилокси}уксусной кислоты, которое имеет эндотермический пик при 147°С в дифференциальной сканирующей калориметрии.
7. Фармацевтическая композиция, содержащая кристаллическое вещество по любому одному из пп. 1-6 в качестве активного ингредиента.
8. Агонист рецептора PGI2, содержащий кристаллическое вещество по любому одному из пп. 1-6 в качестве активного ингредиента.
9. Терапевтическое средство для лечения симптомов, связанных с диабетической невропатией, диабетической гангреной, нарушением периферического кровообращения, хронической артериальной окклюзией, перемежающейся хромотой, склеродермией, тромбозом, легочной гипертензией, инфарктом миокарда, стенокардией, гломерулонефритом, диабетической нефропатией, хронической почечной недостаточностью, бронхиальной астмой, интерстициальной пневмонией (легочным фиброзом), хронической обструктивной болезнью легких, тубулоинтерстициальным нефритом, воспалительным заболеванием кишечника или стенозом позвоночного канала, включающее кристаллическое вещество по любому одному из пп. 1-6 в качестве активного ингредиента.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2017-187296 | 2017-09-28 | ||
| JP2017187296 | 2017-09-28 | ||
| PCT/JP2018/035828 WO2019065792A1 (ja) | 2017-09-28 | 2018-09-27 | 結晶 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2020112117A true RU2020112117A (ru) | 2021-10-28 |
| RU2834293C2 RU2834293C2 (ru) | 2025-02-05 |
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