EA201891303A1 - ПРОИЗВОДНЫЕ 4-АМИНО-2-(1H-ПИРАЗОЛО[3,4-b]ПИРИДИН-3-ИЛ)-6-ОКСО-6,7-ДИГИДРО-5H-ПИРРОЛО[2,3-d]ПИРИМИДИНА И СООТВЕТСТВУЮЩИЕ ПРОИЗВОДНЫЕ (1H-ИНДАЗОЛ-3-ИЛА) В КАЧЕСТВЕ МОДУЛЯТОРОВ cGMP ДЛЯ ЛЕЧЕНИЯ СЕРДЕЧНО-СОСУДИСТЫХ ЗАБОЛЕВАНИЙ - Google Patents
ПРОИЗВОДНЫЕ 4-АМИНО-2-(1H-ПИРАЗОЛО[3,4-b]ПИРИДИН-3-ИЛ)-6-ОКСО-6,7-ДИГИДРО-5H-ПИРРОЛО[2,3-d]ПИРИМИДИНА И СООТВЕТСТВУЮЩИЕ ПРОИЗВОДНЫЕ (1H-ИНДАЗОЛ-3-ИЛА) В КАЧЕСТВЕ МОДУЛЯТОРОВ cGMP ДЛЯ ЛЕЧЕНИЯ СЕРДЕЧНО-СОСУДИСТЫХ ЗАБОЛЕВАНИЙInfo
- Publication number
- EA201891303A1 EA201891303A1 EA201891303A EA201891303A EA201891303A1 EA 201891303 A1 EA201891303 A1 EA 201891303A1 EA 201891303 A EA201891303 A EA 201891303A EA 201891303 A EA201891303 A EA 201891303A EA 201891303 A1 EA201891303 A1 EA 201891303A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- compounds
- pharmaceutically acceptable
- acceptable salts
- derivatives
- pulmonary
- Prior art date
Links
- 208000024172 Cardiovascular disease Diseases 0.000 title abstract 2
- 238000011282 treatment Methods 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 4
- 150000003839 salts Chemical class 0.000 abstract 4
- ZOOGRGPOEVQQDX-UUOKFMHZSA-N 3',5'-cyclic GMP Chemical compound C([C@H]1O2)OP(O)(=O)O[C@H]1[C@@H](O)[C@@H]2N1C(N=C(NC2=O)N)=C2N=C1 ZOOGRGPOEVQQDX-UUOKFMHZSA-N 0.000 abstract 3
- 206010020772 Hypertension Diseases 0.000 abstract 2
- 230000001154 acute effect Effects 0.000 abstract 2
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 abstract 1
- 206010002383 Angina Pectoris Diseases 0.000 abstract 1
- 201000001320 Atherosclerosis Diseases 0.000 abstract 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 abstract 1
- 201000003883 Cystic fibrosis Diseases 0.000 abstract 1
- 206010012689 Diabetic retinopathy Diseases 0.000 abstract 1
- 206010052337 Diastolic dysfunction Diseases 0.000 abstract 1
- 206010048554 Endothelial dysfunction Diseases 0.000 abstract 1
- 208000010228 Erectile Dysfunction Diseases 0.000 abstract 1
- 206010016654 Fibrosis Diseases 0.000 abstract 1
- 206010019280 Heart failures Diseases 0.000 abstract 1
- 208000029523 Interstitial Lung disease Diseases 0.000 abstract 1
- 208000003782 Raynaud disease Diseases 0.000 abstract 1
- 208000012322 Raynaud phenomenon Diseases 0.000 abstract 1
- 206010039710 Scleroderma Diseases 0.000 abstract 1
- 208000006011 Stroke Diseases 0.000 abstract 1
- 208000007536 Thrombosis Diseases 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- 230000000747 cardiac effect Effects 0.000 abstract 1
- 208000020832 chronic kidney disease Diseases 0.000 abstract 1
- 208000022831 chronic renal failure syndrome Diseases 0.000 abstract 1
- 208000019425 cirrhosis of liver Diseases 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 230000006806 disease prevention Effects 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 230000008694 endothelial dysfunction Effects 0.000 abstract 1
- 230000004761 fibrosis Effects 0.000 abstract 1
- 230000001771 impaired effect Effects 0.000 abstract 1
- 201000001881 impotence Diseases 0.000 abstract 1
- 208000010125 myocardial infarction Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 230000002685 pulmonary effect Effects 0.000 abstract 1
- 208000005069 pulmonary fibrosis Diseases 0.000 abstract 1
- 208000002815 pulmonary hypertension Diseases 0.000 abstract 1
- 208000037803 restenosis Diseases 0.000 abstract 1
- 208000007056 sickle cell anemia Diseases 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—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
- A61K31/495—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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Cardiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Heart & Thoracic Surgery (AREA)
- Epidemiology (AREA)
- Hospice & Palliative Care (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Изобретение относится к соединениям формулы (I) или их фармацевтически приемлемым солям, где X, Y, Z, R, R, R, Rи нижние индексы m, p и q представляют собой то, что раскрыто в настоящем описании. Соединения или их фармацевтически приемлемые соли могут модулировать в организме продуцирование циклического гуанозинмонофосфата ("cGMP") и в целом подходят для терапии и профилактики заболеваний, которые связаны с нарушенным балансом cGMP, таких как сердечно-сосудистое заболевание, нарушение эндотелиальной функции, нарушение диастолической функции, атеросклероз, гипертензия, сердечная недостаточность, легочная гипертензия (группы I, II, III, IV по WHO), стенокардия, тромбоз, рестеноз, инфаркт миокарда, инсульт, сердечная декомпенсация, фиброз, легочная гипертония, нарушение эректильной функции, астма, острый респираторный дистресс синдром (ARDS), хроническая почечная недостаточность, кистозный фиброз, серповидноклеточная анемия, склеродермия, синдром Рейно, диабет, диабетическая ретинопатия, цирроз печени, хроническое обструктивное заболевание легких (COPD), острое повреждение легких, фиброз легких или интерстициальное заболевание легких. Изобретение также относится к фармацевтическим композициям, которые содержат соединения формулы (I) или их фармацевтически приемлемые соли. Изобретение также относится к соединениям или их фармацевтически приемлемым солям для использования в терапии и профилактике вышеуказанных заболеваний и для получения фармацевтических средств с этой целью.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/CN2015/098251 WO2017107052A1 (en) | 2015-12-22 | 2015-12-22 | Soluble guanylate cyclase stimulators |
| PCT/US2016/067654 WO2017112617A1 (en) | 2015-12-22 | 2016-12-20 | 4-amino-2-(1h-pyrazolo[3,4-b]pyridin-3-yl)-6-oxo-6,7-dihydro-5h-pyrrolo[2,3-d]pyrimidine derivatives and the respective (1h-indazol-3-yl) derivatives as cgmp modulators for treating cardiovascular diseases |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201891303A1 true EA201891303A1 (ru) | 2018-11-30 |
| EA036445B1 EA036445B1 (ru) | 2020-11-11 |
Family
ID=57758775
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201891303A EA036445B1 (ru) | 2015-12-22 | 2016-12-20 | ПРОИЗВОДНЫЕ 4-АМИНО-2-(1H-ПИРАЗОЛО[3,4-b]ПИРИДИН-3-ИЛ)-6-ОКСО-6,7-ДИГИДРО-5H-ПИРРОЛО[2,3-d]ПИРИМИДИНА И СООТВЕТСТВУЮЩИЕ ПРОИЗВОДНЫЕ (1H-ИНДАЗОЛ-3-ИЛА) В КАЧЕСТВЕ МОДУЛЯТОРОВ cGMP ДЛЯ ЛЕЧЕНИЯ СЕРДЕЧНО-СОСУДИСТЫХ ЗАБОЛЕВАНИЙ |
Country Status (39)
| Country | Link |
|---|---|
| US (2) | US10030027B2 (ru) |
| EP (1) | EP3394067B1 (ru) |
| JP (1) | JP6454448B2 (ru) |
| KR (1) | KR102191312B1 (ru) |
| CN (1) | CN108738320B (ru) |
| AR (1) | AR107154A1 (ru) |
| AU (1) | AU2016377364B2 (ru) |
| BR (1) | BR112018012579B8 (ru) |
| CA (1) | CA3009193C (ru) |
| CL (1) | CL2018001671A1 (ru) |
| CO (1) | CO2018006300A2 (ru) |
| CR (1) | CR20180330A (ru) |
| CY (1) | CY1123173T1 (ru) |
| DK (1) | DK3394067T3 (ru) |
| DO (1) | DOP2018000153A (ru) |
| EA (1) | EA036445B1 (ru) |
| EC (1) | ECSP18054606A (ru) |
| ES (1) | ES2794654T3 (ru) |
| GE (1) | GEP20207205B (ru) |
| HR (1) | HRP20200857T1 (ru) |
| HU (1) | HUE049941T2 (ru) |
| IL (1) | IL260020B (ru) |
| LT (1) | LT3394067T (ru) |
| ME (1) | ME03748B (ru) |
| MX (2) | MX376256B (ru) |
| MY (1) | MY194021A (ru) |
| NI (1) | NI201800069A (ru) |
| PE (1) | PE20181802A1 (ru) |
| PH (1) | PH12018501342B1 (ru) |
| PL (1) | PL3394067T3 (ru) |
| PT (1) | PT3394067T (ru) |
| RS (1) | RS60344B1 (ru) |
| SG (1) | SG11201805272XA (ru) |
| SI (1) | SI3394067T1 (ru) |
| SV (1) | SV2018005715A (ru) |
| TN (1) | TN2018000219A1 (ru) |
| TW (1) | TWI724079B (ru) |
| UA (1) | UA122264C2 (ru) |
| WO (2) | WO2017107052A1 (ru) |
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| US10245264B2 (en) | 2015-05-27 | 2019-04-02 | Merck Sharp & Dohme Corp. | Substituted imidazo[1,2-a]pyrazines as soluble guanylate cyclase activators |
| US10213429B2 (en) | 2015-05-28 | 2019-02-26 | Merck Sharp & Dohme Corp. | Imidazo-pyrazinyl derivatives useful as soluble guanylate cyclase activators |
| TW201718581A (zh) | 2015-10-19 | 2017-06-01 | 英塞特公司 | 作為免疫調節劑之雜環化合物 |
| SMT202200369T1 (it) | 2015-11-19 | 2022-11-18 | Incyte Corp | Composti eterociclici come immunomodulatori |
| MA44075A (fr) | 2015-12-17 | 2021-05-19 | Incyte Corp | Dérivés de n-phényl-pyridine-2-carboxamide et leur utilisation en tant que modulateurs des interactions protéine/protéine pd-1/pd-l1 |
| WO2017107052A1 (en) | 2015-12-22 | 2017-06-29 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase stimulators |
| SG10202005790VA (en) | 2015-12-22 | 2020-07-29 | Incyte Corp | Heterocyclic compounds as immunomodulators |
| ES2906460T3 (es) | 2016-05-06 | 2022-04-18 | Incyte Corp | Compuestos heterocíclicos como inmunomoduladores |
| WO2017197555A1 (en) | 2016-05-16 | 2017-11-23 | Merck Sharp & Dohme Corp. | Fused pyrazine derivatives useful as soluble guanylate cyclase stimulators |
| EP3458063A4 (en) | 2016-05-18 | 2020-02-26 | Merck Sharp & Dohme Corp. | METHOD FOR USE OF TRIAZOLO-PYRAZINYL-SOLUBLE GUANYLATE CYCLASE ACTIVATORS IN FIBROTIC DISEASES |
| TW201808902A (zh) | 2016-05-26 | 2018-03-16 | 美商英塞特公司 | 作為免疫調節劑之雜環化合物 |
| SG11201811414TA (en) | 2016-06-20 | 2019-01-30 | Incyte Corp | Heterocyclic compounds as immunomodulators |
| MA45669A (fr) | 2016-07-14 | 2019-05-22 | Incyte Corp | Composés hétérocycliques utilisés comme immunomodulateurs |
| MA46045A (fr) | 2016-08-29 | 2021-04-28 | Incyte Corp | Composés hétérocycliques utilisés comme immunomodulateurs |
| MX391981B (es) | 2016-12-22 | 2025-03-21 | Incyte Corp | Derivados de benzooxazol como inmunomoduladores. |
| WO2018119236A1 (en) | 2016-12-22 | 2018-06-28 | Incyte Corporation | Triazolo[1,5-a]pyridine derivatives as immunomodulators |
| US20180179179A1 (en) | 2016-12-22 | 2018-06-28 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| PL3558990T3 (pl) | 2016-12-22 | 2022-12-19 | Incyte Corporation | Pochodne tetrahydroimidazo[4,5-c]pirydyny jako induktory internalizacji pd-l1 |
| MA47099A (fr) | 2016-12-22 | 2021-05-12 | Incyte Corp | Composés hétéroaromatiques bicycliques utilisés en tant qu'immunomodulateurs |
| JP7090639B2 (ja) * | 2017-04-11 | 2022-06-24 | サンシャイン・レイク・ファーマ・カンパニー・リミテッド | フッ素置換されたインダゾール化合物及びその使用 |
| WO2019081456A1 (en) | 2017-10-24 | 2019-05-02 | Bayer Aktiengesellschaft | USE OF SGC ACTIVATORS AND STIMULATORS COMPRISING A BETA2 SUBUNIT |
| EP3498298A1 (en) | 2017-12-15 | 2019-06-19 | Bayer AG | The use of sgc stimulators and sgc activators alone or in combination with pde5 inhibitors for the treatment of bone disorders including osteogenesis imperfecta (oi) |
| UA128453C2 (uk) | 2018-03-30 | 2024-07-17 | Інсайт Корпорейшн | Гетероциклічні сполуки як імуномодулятори |
| JP7314173B2 (ja) | 2018-04-30 | 2023-07-25 | バイエル アクチェンゲゼルシャフト | 認知障害の治療のためのｓＧＣ活性化薬及びｓＧＣ刺激薬の使用 |
| PL3790877T3 (pl) | 2018-05-11 | 2023-06-12 | Incyte Corporation | Pochodne tetrahydroimidazo[4,5-c]pirydyny jako immunomodulatory pd-l1 |
| EP3574905A1 (en) | 2018-05-30 | 2019-12-04 | Adverio Pharma GmbH | Method of identifying a subgroup of patients suffering from dcssc which benefits from a treatment with sgc stimulators and sgc activators in a higher degree than a control group |
| CA3126778A1 (en) | 2019-01-17 | 2020-07-23 | Bayer Aktiengesellschaft | Methods to determine whether a subject is suitable of being treated with an agonist of soluble guanylyl cyclase (sgc) |
| WO2021030162A1 (en) | 2019-08-09 | 2021-02-18 | Incyte Corporation | Salts of a pd-1/pd-l1 inhibitor |
| CN115175734B (zh) | 2019-09-30 | 2024-04-19 | 因赛特公司 | 作为免疫调节剂的吡啶并[3,2-d]嘧啶化合物 |
| CA3160131A1 (en) | 2019-11-11 | 2021-05-20 | Incyte Corporation | Salts and crystalline forms of a pd-1/pd-l1 inhibitor |
| MX2023005362A (es) | 2020-11-06 | 2023-06-22 | Incyte Corp | Proceso para hacer un inhibidor de proteina de muerte programada 1 (pd-1)/ligando de muerte programada 1 (pd-l1) y sales y formas cristalinas del mismo. |
| US11760756B2 (en) | 2020-11-06 | 2023-09-19 | Incyte Corporation | Crystalline form of a PD-1/PD-L1 inhibitor |
| WO2022099018A1 (en) | 2020-11-06 | 2022-05-12 | Incyte Corporation | Process of preparing a pd-1/pd-l1 inhibitor |
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