AR124196A1 - Ácidos pirazolo piperidin carboxílicos sustituidos - Google Patents
Ácidos pirazolo piperidin carboxílicos sustituidosInfo
- Publication number
- AR124196A1 AR124196A1 ARP210103423A ARP210103423A AR124196A1 AR 124196 A1 AR124196 A1 AR 124196A1 AR P210103423 A ARP210103423 A AR P210103423A AR P210103423 A ARP210103423 A AR P210103423A AR 124196 A1 AR124196 A1 AR 124196A1
- Authority
- AR
- Argentina
- Prior art keywords
- diseases
- represents hydrogen
- carboxylic acids
- solvates
- halogen
- Prior art date
Links
- CANSPPZTVXEOJH-UHFFFAOYSA-N 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-b]pyridine-3-carboxylic acid Chemical class C1CCNC2=C1NN=C2C(=O)O CANSPPZTVXEOJH-UHFFFAOYSA-N 0.000 title abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 4
- 201000010099 disease Diseases 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 150000003839 salts Chemical class 0.000 abstract 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 2
- 208000008960 Diabetic foot Diseases 0.000 abstract 2
- 206010020772 Hypertension Diseases 0.000 abstract 2
- 208000005764 Peripheral Arterial Disease Diseases 0.000 abstract 2
- 201000009594 Systemic Scleroderma Diseases 0.000 abstract 2
- 206010042953 Systemic sclerosis Diseases 0.000 abstract 2
- 229910052799 carbon Chemical group 0.000 abstract 2
- 208000020832 chronic kidney disease Diseases 0.000 abstract 2
- 208000033679 diabetic kidney disease Diseases 0.000 abstract 2
- 229910052736 halogen Chemical group 0.000 abstract 2
- 150000002367 halogens Chemical group 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 2
- 208000002815 pulmonary hypertension Diseases 0.000 abstract 2
- 208000007056 sickle cell anemia Diseases 0.000 abstract 2
- 239000012453 solvate Substances 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 201000006306 Cor pulmonale Diseases 0.000 abstract 1
- 206010012289 Dementia Diseases 0.000 abstract 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 abstract 1
- 206010019280 Heart failures Diseases 0.000 abstract 1
- 208000019693 Lung disease Diseases 0.000 abstract 1
- 229910052801 chlorine Inorganic materials 0.000 abstract 1
- 239000000460 chlorine Substances 0.000 abstract 1
- 125000001309 chloro group Chemical group Cl* 0.000 abstract 1
- 230000001684 chronic effect Effects 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 230000002526 effect on cardiovascular system Effects 0.000 abstract 1
- 230000003176 fibrotic effect Effects 0.000 abstract 1
- 208000019622 heart disease Diseases 0.000 abstract 1
- 208000038003 heart failure with preserved ejection fraction Diseases 0.000 abstract 1
- 208000038002 heart failure with reduced ejection fraction Diseases 0.000 abstract 1
- 208000017169 kidney disease Diseases 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 230000004770 neurodegeneration Effects 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 238000011282 treatment Methods 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
- 230000029663 wound healing Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic 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
- C07D401/14—Heterocyclic 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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic 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
- C07D401/02—Heterocyclic 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
- C07D401/04—Heterocyclic 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
-
- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- 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
- 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
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Psychiatry (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
La invención se refiere a ácidos pirazolo piperidin carboxílicos sustituidos, sus sales y a procesos para su preparación, y también a su uso para la preparación de medicamentos para el tratamiento y/o la profilaxis de enfermedades, en particular enfermedades cardiovasculares y cardíacas, preferiblemente insuficiencia cardíaca con fracción de eyección reducida y conservada (HFrEF, HFmrEF y HFpEF), hipertensión (HTN), enfermedades de arterias periféricas (PAD, PAOD), enfermedades cardiorrenales y renales, preferiblemente enfermedad renal crónica y diabética (CKD y DKD), enfermedades cardiopulmonares y pulmonares, preferiblemente hipertensión pulmonar (PH), y otras enfermedades, preferiblemente enfermedades neurodegenerativas y diferentes formas de demencias, enfermedades fibróticas, esclerosis sistémica (SSc), enfermedad de células falciformes (SCD), trastornos de cicatrización de heridas como la úlcera del pie diabético (DFU). Reivindicación 1: Un compuesto de fórmula (1), en la cual R¹ representa hidrógeno o halógeno, R² representa hidrógeno o halógeno, R³ representa cloro o trifluorometilo, R⁴ representa hidrógeno o alquilo C₁-C₄, R⁵ representa alquilo C₁-C₆, X¹ representa nitrógeno o carbono, X² representa nitrógeno o carbono, o una de sus sales, sus solvatos o solvatos de sus sales.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP20213016.7A EP4011873A1 (en) | 2020-12-10 | 2020-12-10 | Substituted pyrazolo piperidine carboxylic acids |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR124196A1 true AR124196A1 (es) | 2023-02-22 |
Family
ID=73793021
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP210103423A AR124196A1 (es) | 2020-12-10 | 2021-12-09 | Ácidos pirazolo piperidin carboxílicos sustituidos |
Country Status (19)
| Country | Link |
|---|---|
| US (3) | US20220274958A1 (es) |
| EP (2) | EP4011873A1 (es) |
| JP (1) | JP7451700B2 (es) |
| KR (1) | KR20230118145A (es) |
| CN (3) | CN118791463A (es) |
| AR (1) | AR124196A1 (es) |
| AU (2) | AU2021393987A1 (es) |
| CA (1) | CA3204491A1 (es) |
| CL (1) | CL2023001633A1 (es) |
| CO (1) | CO2023007334A2 (es) |
| CR (2) | CR20250266A (es) |
| DO (1) | DOP2023000114A (es) |
| EC (1) | ECSP23041151A (es) |
| GE (2) | GEAP202316286A (es) |
| IL (1) | IL303299A (es) |
| MX (2) | MX2023006904A (es) |
| PE (1) | PE20231502A1 (es) |
| TW (1) | TW202237588A (es) |
| WO (1) | WO2022122910A1 (es) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP4011874A1 (en) * | 2020-12-10 | 2022-06-15 | Bayer Aktiengesellschaft | Substituted pyrazolo piperidine carboxylic acids |
| CN116829545A (zh) * | 2020-12-10 | 2023-09-29 | 拜耳公司 | 取代的吡唑基哌啶羧酸 |
| EP4011873A1 (en) * | 2020-12-10 | 2022-06-15 | Bayer Aktiengesellschaft | Substituted pyrazolo piperidine carboxylic acids |
| JP2025518350A (ja) | 2022-06-09 | 2025-06-12 | バイエル・アクチエンゲゼルシヤフト | 女性における駆出率が維持された心不全の治療に使用するための可溶性グアニル酸シクラーゼアクチベーター |
| WO2024163561A1 (en) * | 2023-01-31 | 2024-08-08 | Invivosciences, Inc. | Systems and methods for treating heart failure with preserved ejection fraction |
| WO2025067414A1 (zh) * | 2023-09-27 | 2025-04-03 | 海思科医药集团股份有限公司 | 吡唑羧酸衍生物及其在医药上的应用 |
| TW202535380A (zh) * | 2024-01-30 | 2025-09-16 | 大陸商海思科醫藥集團股份有限公司 | 吡唑羧酸衍生物及其在醫藥上的應用 |
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| DE19830431A1 (de) | 1998-07-08 | 2000-01-13 | Hoechst Marion Roussel De Gmbh | Sulfonylamino-carbonsäure-N-arylamide als Guanylatcyclase-Aktivatoren |
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| DE19834044A1 (de) | 1998-07-29 | 2000-02-03 | Bayer Ag | Neue substituierte Pyrazolderivate |
| DE19834047A1 (de) | 1998-07-29 | 2000-02-03 | Bayer Ag | Substituierte Pyrazolderivate |
| DE19836697A1 (de) | 1998-08-13 | 2000-02-17 | Hoechst Marion Roussel De Gmbh | Substituierte 4-Amino-2-aryl-pyrimidine, ihre Herstellung, ihre Verwendung und sie enthaltende pharmazeutische Präparate |
| GB9824310D0 (en) | 1998-11-05 | 1998-12-30 | Univ London | Activators of soluble guanylate cyclase |
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| WO2020245342A1 (en) | 2019-06-07 | 2020-12-10 | Bayer Aktiengesellschaft | The use of sgc activators for the treatment of ophthalmologic diseases |
| EP4011873A1 (en) | 2020-12-10 | 2022-06-15 | Bayer Aktiengesellschaft | Substituted pyrazolo piperidine carboxylic acids |
| WO2022122914A1 (en) | 2020-12-10 | 2022-06-16 | Bayer Aktiengesellschaft | Substituted pyrazolo piperidine carboxylic acids |
| CN116829545A (zh) | 2020-12-10 | 2023-09-29 | 拜耳公司 | 取代的吡唑基哌啶羧酸 |
| EP4011874A1 (en) | 2020-12-10 | 2022-06-15 | Bayer Aktiengesellschaft | Substituted pyrazolo piperidine carboxylic acids |
| KR20230118143A (ko) | 2020-12-10 | 2023-08-10 | 바이엘 악티엔게젤샤프트 | 안과 질환의 치료를 위한 sGC 활성화제의 용도 |
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2020
- 2020-12-10 EP EP20213016.7A patent/EP4011873A1/en not_active Ceased
-
2021
- 2021-12-09 KR KR1020237022819A patent/KR20230118145A/ko active Pending
- 2021-12-09 CA CA3204491A patent/CA3204491A1/en active Pending
- 2021-12-09 AU AU2021393987A patent/AU2021393987A1/en active Pending
- 2021-12-09 CR CR20250266A patent/CR20250266A/es unknown
- 2021-12-09 CN CN202410784385.9A patent/CN118791463A/zh active Pending
- 2021-12-09 CN CN202180008063.XA patent/CN114981257B/zh active Active
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| ECSP23041151A (es) | 2023-07-31 |
| JP7451700B2 (ja) | 2024-03-18 |
| KR20230118145A (ko) | 2023-08-10 |
| US20230265072A1 (en) | 2023-08-24 |
| EP4259615A1 (en) | 2023-10-18 |
| DOP2023000114A (es) | 2023-07-09 |
| US20250026737A1 (en) | 2025-01-23 |
| CR20250266A (es) | 2025-08-27 |
| TW202237588A (zh) | 2022-10-01 |
| IL303299A (en) | 2023-07-01 |
| CN118787643A (zh) | 2024-10-18 |
| CN114981257B (zh) | 2024-07-05 |
| US20220274958A1 (en) | 2022-09-01 |
| AU2021393987A1 (en) | 2023-06-22 |
| WO2022122910A1 (en) | 2022-06-16 |
| CL2023001633A1 (es) | 2023-11-10 |
| CN118791463A (zh) | 2024-10-18 |
| EP4011873A1 (en) | 2022-06-15 |
| AU2021393987A9 (en) | 2025-04-03 |
| GEAP202316286A (en) | 2023-09-11 |
| CR20230238A (es) | 2023-07-19 |
| PE20231502A1 (es) | 2023-09-26 |
| CN114981257A (zh) | 2022-08-30 |
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| MX2023006904A (es) | 2023-06-26 |
| CO2023007334A2 (es) | 2023-06-09 |
| AU2025279820A1 (en) | 2026-01-15 |
| JP2023543646A (ja) | 2023-10-18 |
| CA3204491A1 (en) | 2022-06-16 |
| US12195448B2 (en) | 2025-01-14 |
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