PE20231502A1 - Acidos pirazolo piperidin carboxilicos sustituidos - Google Patents
Acidos pirazolo piperidin carboxilicos sustituidosInfo
- Publication number
- PE20231502A1 PE20231502A1 PE2023001810A PE2023001810A PE20231502A1 PE 20231502 A1 PE20231502 A1 PE 20231502A1 PE 2023001810 A PE2023001810 A PE 2023001810A PE 2023001810 A PE2023001810 A PE 2023001810A PE 20231502 A1 PE20231502 A1 PE 20231502A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- increase
- guanylate cyclase
- soluble guanylate
- hypertension
- Prior art date
Links
- CXVWVEAHZKABIU-UHFFFAOYSA-N piperidine;1h-pyrazole Chemical class C=1C=NNC=1.C1CCNCC1 CXVWVEAHZKABIU-UHFFFAOYSA-N 0.000 title 1
- 208000008960 Diabetic foot Diseases 0.000 abstract 2
- 206010020772 Hypertension Diseases 0.000 abstract 2
- 208000005764 Peripheral Arterial Disease Diseases 0.000 abstract 2
- 102000007637 Soluble Guanylyl Cyclase Human genes 0.000 abstract 2
- 108010007205 Soluble Guanylyl Cyclase Proteins 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 208000020832 chronic kidney disease Diseases 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 208000002815 pulmonary hypertension Diseases 0.000 abstract 2
- 208000007056 sickle cell anemia Diseases 0.000 abstract 2
- 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 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 abstract 1
- 206010019280 Heart failures Diseases 0.000 abstract 1
- 208000034189 Sclerosis Diseases 0.000 abstract 1
- 201000009594 Systemic Scleroderma Diseases 0.000 abstract 1
- 206010042953 Systemic sclerosis Diseases 0.000 abstract 1
- 230000004913 activation Effects 0.000 abstract 1
- 239000012190 activator Substances 0.000 abstract 1
- 230000036772 blood pressure Effects 0.000 abstract 1
- 150000001735 carboxylic acids Chemical class 0.000 abstract 1
- 230000001684 chronic effect Effects 0.000 abstract 1
- 208000033679 diabetic kidney disease Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 150000003278 haem Chemical class 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 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
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 230000003834 intracellular effect Effects 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 230000003389 potentiating effect Effects 0.000 abstract 1
- 230000008327 renal blood flow Effects 0.000 abstract 1
- 208000010110 spontaneous platelet aggregation Diseases 0.000 abstract 1
- 230000001196 vasorelaxation Effects 0.000 abstract 1
Classifications
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- 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
Esta referido a derivados de acidos carboxilicos pirazolo piperidinicos sustituidos de Formula I, en donde: R1 y R2 son H, o halogeno; R3 es Cl, CF3; R4 es H, alquilo; R5 es alquilo, X1 y X2 son N, C. Los compuestos preferidos son como se detalla a continuacion. Estos compuestos son potentes activadores de la guanilato ciclasa soluble, conducen a vasorrelajacion, inhibicion de la agregacion plaquetaria y disminucion de la presion arterial y aumento del flujo sanguineo coronario y renal. Estos efectos estan mediados por la activacion directa independiente del hemo de la guanilato ciclasa soluble y un aumento de cGMP intracelular. Se emplean en el tratamiento de diversas enfermedades, como insuficiencia cardiaca con fraccion de eyeccion reducida y conservada (ICFEr, ICFEp e ICFErm), hipertension (HTA), enfermedades arteriales perifericas (EAP, EAPO), enfermedad renal cronica y diabetica (ERC y ERD), hipertension pulmonar (HP), esclerosis sistemica (ES), enfermedad de celula falciforme (SCD), ulceras del pie diabetico (UPD), entre otras.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP20213016.7A EP4011873A1 (en) | 2020-12-10 | 2020-12-10 | Substituted pyrazolo piperidine carboxylic acids |
| PCT/EP2021/084980 WO2022122910A1 (en) | 2020-12-10 | 2021-12-09 | Substituted pyrazolo piperidine carboxylic acids |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20231502A1 true PE20231502A1 (es) | 2023-09-26 |
Family
ID=73793021
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2023001810A PE20231502A1 (es) | 2020-12-10 | 2021-12-09 | Acidos pirazolo piperidin carboxilicos sustituidos |
Country Status (19)
| Country | Link |
|---|---|
| US (3) | US20220274958A1 (es) |
| EP (2) | EP4011873A1 (es) |
| JP (1) | JP7451700B2 (es) |
| KR (1) | KR20230118145A (es) |
| CN (3) | CN118787643A (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 |
| EP4011873A1 (en) * | 2020-12-10 | 2022-06-15 | Bayer Aktiengesellschaft | Substituted pyrazolo piperidine carboxylic acids |
| WO2022122916A1 (en) * | 2020-12-10 | 2022-06-16 | Bayer Aktiengesellschaft | Substituted pyrazolyl 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 |
| WO2025162280A1 (zh) * | 2024-01-30 | 2025-08-07 | 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 |
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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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| 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 |
| DE19853278A1 (de) | 1998-11-19 | 2000-05-25 | Aventis Pharma Gmbh | Substituierte 4-Amino-2-aryl-cyclopenta[d]pyrimidine, ihre Herstellung, ihre Verwendung und sie enthaltende pharmazeutische Präparate |
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| WO2022122916A1 (en) * | 2020-12-10 | 2022-06-16 | Bayer Aktiengesellschaft | Substituted pyrazolyl piperidine carboxylic acids |
| EP4011874A1 (en) * | 2020-12-10 | 2022-06-15 | Bayer Aktiengesellschaft | Substituted pyrazolo piperidine carboxylic acids |
| EP4011873A1 (en) * | 2020-12-10 | 2022-06-15 | Bayer Aktiengesellschaft | Substituted pyrazolo piperidine carboxylic acids |
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-
2020
- 2020-12-10 EP EP20213016.7A patent/EP4011873A1/en not_active Ceased
-
2021
- 2021-12-09 CA CA3204491A patent/CA3204491A1/en active Pending
- 2021-12-09 MX MX2023006904A patent/MX2023006904A/es unknown
- 2021-12-09 GE GEAP202316286A patent/GEAP202316286A/en unknown
- 2021-12-09 GE GEAP202116286A patent/GEP20247635B/en unknown
- 2021-12-09 KR KR1020237022819A patent/KR20230118145A/ko active Pending
- 2021-12-09 AR ARP210103423A patent/AR124196A1/es unknown
- 2021-12-09 CR CR20250266A patent/CR20250266A/es unknown
- 2021-12-09 PE PE2023001810A patent/PE20231502A1/es unknown
- 2021-12-09 WO PCT/EP2021/084980 patent/WO2022122910A1/en not_active Ceased
- 2021-12-09 JP JP2022526369A patent/JP7451700B2/ja active Active
- 2021-12-09 IL IL303299A patent/IL303299A/en unknown
- 2021-12-09 CN CN202410784381.0A patent/CN118787643A/zh active Pending
- 2021-12-09 AU AU2021393987A patent/AU2021393987A1/en active Pending
- 2021-12-09 CN CN202410784385.9A patent/CN118791463A/zh active Pending
- 2021-12-09 CN CN202180008063.XA patent/CN114981257B/zh active Active
- 2021-12-09 TW TW110146018A patent/TW202237588A/zh unknown
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- 2021-12-09 EP EP21820285.1A patent/EP4259615A1/en active Pending
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2022
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2023
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2024
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| Publication number | Publication date |
|---|---|
| CN118787643A (zh) | 2024-10-18 |
| GEP20247635B (en) | 2024-06-25 |
| AU2021393987A9 (en) | 2025-04-03 |
| MX2023006904A (es) | 2023-06-26 |
| CO2023007334A2 (es) | 2023-06-09 |
| US12195448B2 (en) | 2025-01-14 |
| IL303299A (en) | 2023-07-01 |
| GEAP202316286A (en) | 2023-09-11 |
| EP4011873A1 (en) | 2022-06-15 |
| KR20230118145A (ko) | 2023-08-10 |
| AU2021393987A1 (en) | 2023-06-22 |
| CR20230238A (es) | 2023-07-19 |
| WO2022122910A1 (en) | 2022-06-16 |
| AU2025279820A1 (en) | 2026-01-15 |
| CR20250266A (es) | 2025-08-27 |
| TW202237588A (zh) | 2022-10-01 |
| US20220274958A1 (en) | 2022-09-01 |
| MX2025009051A (es) | 2025-09-02 |
| JP7451700B2 (ja) | 2024-03-18 |
| DOP2023000114A (es) | 2023-07-09 |
| US20230265072A1 (en) | 2023-08-24 |
| CA3204491A1 (en) | 2022-06-16 |
| CN114981257A (zh) | 2022-08-30 |
| EP4259615A1 (en) | 2023-10-18 |
| CN118791463A (zh) | 2024-10-18 |
| JP2023543646A (ja) | 2023-10-18 |
| CN114981257B (zh) | 2024-07-05 |
| CL2023001633A1 (es) | 2023-11-10 |
| US20250026737A1 (en) | 2025-01-23 |
| AR124196A1 (es) | 2023-02-22 |
| ECSP23041151A (es) | 2023-07-31 |
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