AR107154A1 - Estimuladores de guanilato ciclasa soluble - Google Patents
Estimuladores de guanilato ciclasa solubleInfo
- Publication number
- AR107154A1 AR107154A1 ARP160103930A ARP160103930A AR107154A1 AR 107154 A1 AR107154 A1 AR 107154A1 AR P160103930 A ARP160103930 A AR P160103930A AR P160103930 A ARP160103930 A AR P160103930A AR 107154 A1 AR107154 A1 AR 107154A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- formula
- cycloalkyl
- ring
- subscript
- Prior art date
Links
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
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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
- A61P9/00—Drugs for disorders of the cardiovascular system
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- 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
Los compuestos o sus sales farmacéuticamente aceptables pueden modular la producción corporal de guanosín monofosfato cíclico (GMPc) y son generalmente adecuados para el tratamiento y la prevención de enfermedades que están asociadas con un equilibrio de GMPc perturbado. También proporciona composiciones farmacéuticas que comprenden compuestos de fórmula (1) o sales farmacéuticamente aceptables de los mismos. También se refiere a procedimientos para el uso de los compuestos o sus sales farmacéuticamente aceptables en el tratamiento y la prevención de las enfermedades mencionadas anteriormente y para la preparación de productos farmacéuticos para este fin. Reivindicación 1: Un compuesto de la fórmula (1), o una sal farmacéuticamente aceptable del mismo, en la que: X es C(H) o N; cada R¹ es independientemente halo, hidroxilo, alquilo C₁₋₃, cicloalquilo C₃₋₆ u -O-alquilo C₁₋₃; R² es: (a) alquilo C₁₋₆, estando dicho alquilo C₁₋₆ de R² sin sustituir o sustituido con 1 a 6 restos seleccionados independientemente de fluoro u -O-alquilo C₁₋₃; (b) anillo C², siendo el anillo C²: (i) cicloalquilo C₃₋₁₂; (ii) fenilo; (iii) un heteroarilo monocíclico de 5 ó 6 miembros que contiene de 1 a 2 heteroátomos seleccionados de N, O ó S; o (iv) un heterociclilo monocíclico de 5 ó 6 miembros que contiene de 1 a 2 heteroátomos seleccionados de N, O ó S; estando el anillo C² sin sustituir o sustituido con 1 a 3 restos seleccionados independientemente de halo, ciano, alquilo C₁₋₃, -O-alquilo C₁₋₃ u oxo; R⁴ es alquilo C₁₋₆, CF₃ o cicloalquilo C₃₋₆; el anillo C³ es: (a) fenilo; (b) un heteroarilo monocíclico de 5 ó 6 miembros o un heteroarilo bicíclico de 9 a 10 miembros que contiene de 1 a 3 heteroátomos seleccionados de N, O ó S; (c) un heterociclilo monocíclico de 5 ó 6 miembros que contiene de 1 a 3 heteroátomos seleccionados de N, O ó S; (d) cicloalquilo C₃₋₆; seleccionándose cada Rᵃ independientemente de halo, ciano, alquilo C₁₋₃, -O-alquilo C₁₋₃, oxo o hidroxilo; Y es: (a) un enlace; (b) representa un grupo de la fórmula (2), en la que RY¹ y RY² son independientemente H, alquilo C₁₋₃, hidroxilo, fluoro, hidroxialquilo C₁₋₃ o amino; o como alternativa RY¹ y RY², conjuntamente con el átomo de carbono al que están unidos forman un cicloalquilo C₃₋₆; RY³ y RY⁴ son independientemente H, alquilo C₁₋₃, hidroxilo, fluoro o hidroxialquilo C₁₋₃ ; o como alternativa RY³ y RY⁴, conjuntamente con el átomo de carbono al que están unidos, forman un cicloalquilo C₃₋₆; (c) un grupo de la fórmula (3); o (d) un anillo AH, siendo el anillo AH cicloalquilo C₃₋₆ o fenilo, en lo que el anillo AH está sin sustituir o sustituido con 1 a 3 restos seleccionados independientemente de halo o alquilo C₁₋₃; (e) un grupo -CH=CH-; o (f) un grupo de fórmula (4); Z es: (a) -CO₂H; (b) -C(O)N(H)OH; (c) un resto de fórmula (5); (d) un resto de fórmula (6); (e) un resto de fórmula (7); (f) -SO₃H; (g) -P(=O)(OH)₂ o (h) -C(O)N(H)S(O)₂CH₃; el subíndice m es 0, 1 ó 2; el subíndice p es 0, 1, 2 ó 3; el subíndice q es 0 ó 1; el subíndice r1 es 0, 1, 2, 3 ó 4; y el subíndice r2 es 0 ó 1.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/CN2015/098251 WO2017107052A1 (en) | 2015-12-22 | 2015-12-22 | Soluble guanylate cyclase stimulators |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR107154A1 true AR107154A1 (es) | 2018-03-28 |
Family
ID=57758775
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP160103930A AR107154A1 (es) | 2015-12-22 | 2016-12-20 | Estimuladores de guanilato ciclasa soluble |
Country Status (39)
| Country | Link |
|---|---|
| US (2) | US10030027B2 (es) |
| EP (1) | EP3394067B1 (es) |
| JP (1) | JP6454448B2 (es) |
| KR (1) | KR102191312B1 (es) |
| CN (1) | CN108738320B (es) |
| AR (1) | AR107154A1 (es) |
| AU (1) | AU2016377364B2 (es) |
| BR (1) | BR112018012579B8 (es) |
| CA (1) | CA3009193C (es) |
| CL (1) | CL2018001671A1 (es) |
| CO (1) | CO2018006300A2 (es) |
| CR (1) | CR20180330A (es) |
| CY (1) | CY1123173T1 (es) |
| DK (1) | DK3394067T3 (es) |
| DO (1) | DOP2018000153A (es) |
| EA (1) | EA036445B1 (es) |
| EC (1) | ECSP18054606A (es) |
| ES (1) | ES2794654T3 (es) |
| GE (1) | GEP20207205B (es) |
| HR (1) | HRP20200857T1 (es) |
| HU (1) | HUE049941T2 (es) |
| IL (1) | IL260020B (es) |
| LT (1) | LT3394067T (es) |
| ME (1) | ME03748B (es) |
| MX (2) | MX376256B (es) |
| MY (1) | MY194021A (es) |
| NI (1) | NI201800069A (es) |
| PE (1) | PE20181802A1 (es) |
| PH (1) | PH12018501342B1 (es) |
| PL (1) | PL3394067T3 (es) |
| PT (1) | PT3394067T (es) |
| RS (1) | RS60344B1 (es) |
| SG (1) | SG11201805272XA (es) |
| SI (1) | SI3394067T1 (es) |
| SV (1) | SV2018005715A (es) |
| TN (1) | TN2018000219A1 (es) |
| TW (1) | TWI724079B (es) |
| UA (1) | UA122264C2 (es) |
| WO (2) | WO2017107052A1 (es) |
Families Citing this family (37)
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| EP3303342B1 (en) | 2015-05-27 | 2021-03-17 | Merck Sharp & Dohme Corp. | Imidazo-pyrazinyl derivatives useful as soluble guanylate cyclase activators |
| WO2016191335A1 (en) | 2015-05-28 | 2016-12-01 | 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 |
| SG10202004618TA (en) | 2015-11-19 | 2020-06-29 | Incyte Corp | Heterocyclic compounds as immunomodulators |
| US20170174671A1 (en) | 2015-12-17 | 2017-06-22 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| SI3394033T1 (sl) | 2015-12-22 | 2021-03-31 | Incyte Corporation | Heterociklične spojine kot imunomodulatorji |
| WO2017107052A1 (en) | 2015-12-22 | 2017-06-29 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase stimulators |
| AR108396A1 (es) | 2016-05-06 | 2018-08-15 | 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 |
| WO2017200857A1 (en) | 2016-05-18 | 2017-11-23 | Merck Sharp & Dohme Corp. | Methods for using triazolo-pyrazinyl soluble guanylate cyclase activators in fibrotic disorders |
| MA45116A (fr) | 2016-05-26 | 2021-06-02 | Incyte Corp | Composés hétérocycliques comme immunomodulateurs |
| ES2927984T3 (es) | 2016-06-20 | 2022-11-14 | Incyte Corp | Compuestos heterocíclicos como inmunomoduladores |
| ES2930092T3 (es) | 2016-07-14 | 2022-12-07 | Incyte Corp | Compuestos heterocíclicos como inmunomoduladores |
| US20180057486A1 (en) | 2016-08-29 | 2018-03-01 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| ES2929193T3 (es) | 2016-12-22 | 2022-11-25 | Incyte Corp | Derivados de tetrahidro imidazo[4,5-c]piridina como inductores de la internalización de PD-L1 |
| EP3558963B1 (en) | 2016-12-22 | 2022-03-23 | Incyte Corporation | Bicyclic heteroaromatic compounds as immunomodulators |
| WO2018119236A1 (en) | 2016-12-22 | 2018-06-28 | Incyte Corporation | Triazolo[1,5-a]pyridine derivatives as immunomodulators |
| MX391981B (es) | 2016-12-22 | 2025-03-21 | Incyte Corp | Derivados de benzooxazol como inmunomoduladores. |
| WO2018119221A1 (en) | 2016-12-22 | 2018-06-28 | Incyte Corporation | Pyridine derivatives as immunomodulators |
| ES2924359T3 (es) * | 2017-04-11 | 2022-10-06 | Sunshine Lake Pharma Co Ltd | Compuestos de indazol sustituidos con flúor y usos de los mismos |
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| SMT202300065T1 (it) | 2018-03-30 | 2023-05-12 | Incyte Corp | Composti eterociclici come immunomodulatori |
| WO2019211081A1 (en) | 2018-04-30 | 2019-11-07 | Bayer Aktiengesellschaft | The use of sgc activators and sgc stimulators for the treatment of cognitive impairment |
| PL3790877T3 (pl) | 2018-05-11 | 2023-06-12 | Incyte Corporation | Pochodne tetrahydroimidazo[4,5-c]pirydyny jako immunomodulatory pd-l1 |
| US11508483B2 (en) | 2018-05-30 | 2022-11-22 | 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 |
| WO2020148379A1 (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 |
| IL291471B2 (en) | 2019-09-30 | 2025-04-01 | Incyte Corp | Pyrimido[3,2–D]pyrimidine compounds as immunomodulators |
| CN114829366A (zh) | 2019-11-11 | 2022-07-29 | 因赛特公司 | Pd-1/pd-l1抑制剂的盐及结晶形式 |
| US11866434B2 (en) | 2020-11-06 | 2024-01-09 | Incyte Corporation | Process for making a PD-1/PD-L1 inhibitor and salts and crystalline forms thereof |
| TW202233615A (zh) | 2020-11-06 | 2022-09-01 | 美商英塞特公司 | Ｐｄ—１／ｐｄ—ｌ１抑制劑之結晶形式 |
| WO2022099018A1 (en) | 2020-11-06 | 2022-05-12 | Incyte Corporation | Process of preparing a pd-1/pd-l1 inhibitor |
| TW202448469A (zh) * | 2023-06-09 | 2024-12-16 | 大陸商西藏海思科製藥有限公司 | 吡咯並[2,3-d]嘧啶-4-胺衍生物及其在醫藥上的應用 |
| WO2025006294A2 (en) * | 2023-06-26 | 2025-01-02 | Merck Sharp & Dohme Llc | Processes for preparing crystalline soluble guanylate cyclase stimulators |
| WO2025006295A1 (en) * | 2023-06-26 | 2025-01-02 | Merck Sharp & Dohme Llc | Processes for preparing soluble guanylate cyclase stimulators |
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| EP2729476B1 (de) | 2011-07-06 | 2017-08-23 | Bayer Intellectual Property GmbH | Heteroaryl-substituierte pyrazolopyridine und ihre verwendung als stimulatoren der löslichen guanylatcyclase |
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| JP7098214B2 (ja) | 2016-02-01 | 2022-07-11 | サイクレリオン・セラピューティクス，インコーポレーテッド | 非アルコール性脂肪性肝炎（ＮＡＳＨ）の処置のためのｓＧＣ刺激物質の使用 |
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