PE20220167A1 - COMPUESTOS PIPERIDINIL BICICLICOS FUSIONADOS Y RELACIONADOS COMO MODULADORES DEL RECEPTOR C5a - Google Patents
COMPUESTOS PIPERIDINIL BICICLICOS FUSIONADOS Y RELACIONADOS COMO MODULADORES DEL RECEPTOR C5aInfo
- Publication number
- PE20220167A1 PE20220167A1 PE2021001484A PE2021001484A PE20220167A1 PE 20220167 A1 PE20220167 A1 PE 20220167A1 PE 2021001484 A PE2021001484 A PE 2021001484A PE 2021001484 A PE2021001484 A PE 2021001484A PE 20220167 A1 PE20220167 A1 PE 20220167A1
- Authority
- PE
- Peru
- Prior art keywords
- heteroaryl
- aryl
- compounds
- alkyl
- fused
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
- C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
- C07D215/54—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
- C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/451—Non condensed piperidines, e.g. piperocaine having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Neurosurgery (AREA)
- Virology (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Oncology (AREA)
- Heart & Thoracic Surgery (AREA)
- Molecular Biology (AREA)
- AIDS & HIV (AREA)
- Communicable Diseases (AREA)
- Psychiatry (AREA)
- Cardiology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Hospice & Palliative Care (AREA)
- Transplantation (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente invencion se refiere a compuestos derivados de piperidinil biciclico fusionados, piperidinilo sustituido en meta, de formula general (XXI) caracterizado porque C1 se selecciona del grupo que consiste de arilo y heteroarilo, en donde el heteroarilo tiene de 1-3 heteroatomos seleccionados de N, O y S; y en donde dichos arilo y heteroarilo estan sustituidos de manera opcional con 1- 3 sustituyentes R1; C2 se selecciona de arilo y heteroarilo, en donde el heteroarilo tiene de 1-3 heteroatomos seleccionados de N, O y S; y en donde dichos grupos arilo y heteroarilo estan sustituidos de manera opcional con de 1-3 sustituyentes R2; C3 se selecciona del grupo de alquilo o heteroalquilo de C1-8, cicloalquilo de C3-8, cicloalquilo de C3-8-alquilo de C1-4, arilo, arilo-alquilo de C1-4, heteroarilo, entre otros; X es hidrogeno o CH3; R8 y R9 se seleccionan independientemente de hidrogeno, halogeno, alquilo de C1-C8, haloalquilo de C1-C8, y alcoxi de C1-C8; o R8 y R9 se combinan para formar un carbociclo mono o multiple saturado o no saturado fusionado en el cual uno o mas de los atomos de carbono en el anillo puede remplazarse por N, S, u O, con la condicion de que al menos uno de R8 y R9 no es hidrogeno. Dichos compuestos modulan la actividad del receptor C5a de mamifero que se une directamente al receptor C5a. Tambien se refiere a composiciones farmaceuticas que contienen tales compuestos y su uso en el tratamiento de una enfermedad o trastorno que implica la activacion patogena de los receptores C5a.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962816726P | 2019-03-11 | 2019-03-11 | |
| EP19177349 | 2019-05-29 | ||
| US201962873612P | 2019-07-12 | 2019-07-12 | |
| PCT/EP2020/053171 WO2020182384A1 (en) | 2019-03-11 | 2020-02-07 | Fused piperidinyl bicyclic and related compounds as modulators of c5a receptor |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20220167A1 true PE20220167A1 (es) | 2022-01-28 |
Family
ID=69526272
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2021001484A PE20220167A1 (es) | 2019-03-11 | 2020-02-07 | COMPUESTOS PIPERIDINIL BICICLICOS FUSIONADOS Y RELACIONADOS COMO MODULADORES DEL RECEPTOR C5a |
Country Status (15)
| Country | Link |
|---|---|
| US (3) | US11149009B2 (es) |
| EP (1) | EP3938351A1 (es) |
| JP (1) | JP7360745B2 (es) |
| KR (1) | KR102702654B1 (es) |
| CN (2) | CN113784955B (es) |
| AU (1) | AU2020234859B2 (es) |
| BR (1) | BR112021017756A2 (es) |
| CA (1) | CA3129019A1 (es) |
| CL (1) | CL2021002357A1 (es) |
| IL (2) | IL312955B1 (es) |
| MX (2) | MX2021011008A (es) |
| PE (1) | PE20220167A1 (es) |
| PH (1) | PH12021552171A1 (es) |
| SG (1) | SG11202108957RA (es) |
| WO (1) | WO2020182384A1 (es) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL261809B2 (en) | 2017-04-03 | 2024-04-01 | Inflarx Gmbh | Treatment of inflammatory diseases with inhibitors of C5A activity |
| US10376595B2 (en) | 2017-04-03 | 2019-08-13 | Inflarx Gmbh | Treatment of inflammatory diseases with inhibitors of C5a activity |
| AU2020234859B2 (en) | 2019-03-11 | 2025-03-13 | Inflarx Gmbh | Fused piperidinyl bicyclic and related compounds as modulators of C5a receptor |
| CN118908883A (zh) * | 2019-11-08 | 2024-11-08 | 凯莫森特里克斯股份有限公司 | 补体成分c5a受体的盐形式 |
| IL292383A (en) | 2019-11-08 | 2022-06-01 | Chemocentryx Inc | Amorphous form of complement component c5a receptor |
| AU2021321901A1 (en) * | 2020-08-07 | 2023-03-09 | Kira Pharmaceuticals (Suzhou) Ltd. | Compounds as C5ar inhibitors |
| WO2024245527A1 (en) | 2023-05-26 | 2024-12-05 | Inflarx Gmbh | Treatment of pneumonia and ards with inhibitors of c5a and il-6 activity |
| US12180274B2 (en) | 2023-05-26 | 2024-12-31 | Inflarx Gmbh | Treatment of pneumonia and ARDS with inhibitors of C5a and IL-6 activity |
| AU2024324780A1 (en) | 2023-08-16 | 2026-02-05 | Inflarx Gmbh | Fused piperidinyl bicyclic and related compounds for use in the treatment of diseases |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4704355A (en) | 1985-03-27 | 1987-11-03 | New Horizons Diagnostics Corporation | Assay utilizing ATP encapsulated within liposome particles |
| CA2025907A1 (en) | 1989-09-21 | 1991-03-22 | Franklin D. Collins | Method of transporting compositions across the blood brain barrier |
| US20070112015A1 (en) | 2005-10-28 | 2007-05-17 | Chemocentryx, Inc. | Substituted dihydropyridines and methods of use |
| CN102264227B (zh) * | 2008-12-22 | 2014-07-23 | 凯莫森特里克斯股份有限公司 | C5aR拮抗剂 |
| JP7339733B2 (ja) | 2016-01-14 | 2023-09-06 | ケモセントリックス，インコーポレイティド | Ｃ３腎症を処置する方法 |
| IL261809B2 (en) | 2017-04-03 | 2024-04-01 | Inflarx Gmbh | Treatment of inflammatory diseases with inhibitors of C5A activity |
| US10376595B2 (en) | 2017-04-03 | 2019-08-13 | Inflarx Gmbh | Treatment of inflammatory diseases with inhibitors of C5a activity |
| CN108558844A (zh) * | 2018-05-16 | 2018-09-21 | 张玉叶 | 一种甲酰胺类衍生物及其在抗肿瘤药物中的应用 |
| CN108727354A (zh) * | 2018-05-16 | 2018-11-02 | 张玉叶 | 一种甲酰胺类衍生物及其在抗肿瘤药物中的应用 |
| CN108727355A (zh) * | 2018-05-16 | 2018-11-02 | 张玉叶 | 一种甲酰胺类衍生物、制备方法及其在抗肿瘤药物中的应用 |
| CN108440514A (zh) * | 2018-05-16 | 2018-08-24 | 张玉叶 | 一种甲酰胺类衍生物、制备方法及其在抗肿瘤药物中的应用 |
| CN108440513A (zh) * | 2018-05-16 | 2018-08-24 | 张玉叶 | 一种甲酰胺类衍生物及其在抗肿瘤药物中的应用 |
| PE20211644A1 (es) | 2018-09-18 | 2021-08-24 | Terns Inc | Compuestos para tratar ciertas leucemias |
| UY38423A (es) | 2018-10-19 | 2021-02-26 | Servier Lab | Nuevos derivados amino-pirimidonil-piperidinilo, un proceso para su preparación y composiciones farmacéuticas que los contienen |
| AU2020234859B2 (en) | 2019-03-11 | 2025-03-13 | Inflarx Gmbh | Fused piperidinyl bicyclic and related compounds as modulators of C5a receptor |
| GB201907616D0 (en) | 2019-05-29 | 2019-07-10 | Galapagos Nv | Novel compounds and pharmaceutical compositons thereof for the treatment of diseases |
-
2020
- 2020-02-07 AU AU2020234859A patent/AU2020234859B2/en active Active
- 2020-02-07 PE PE2021001484A patent/PE20220167A1/es unknown
- 2020-02-07 JP JP2021554679A patent/JP7360745B2/ja active Active
- 2020-02-07 EP EP20704284.7A patent/EP3938351A1/en active Pending
- 2020-02-07 SG SG11202108957RA patent/SG11202108957RA/en unknown
- 2020-02-07 CN CN202080034858.3A patent/CN113784955B/zh active Active
- 2020-02-07 IL IL312955A patent/IL312955B1/en unknown
- 2020-02-07 CA CA3129019A patent/CA3129019A1/en active Pending
- 2020-02-07 MX MX2021011008A patent/MX2021011008A/es unknown
- 2020-02-07 BR BR112021017756A patent/BR112021017756A2/pt unknown
- 2020-02-07 PH PH1/2021/552171A patent/PH12021552171A1/en unknown
- 2020-02-07 US US16/784,951 patent/US11149009B2/en active Active
- 2020-02-07 KR KR1020217032491A patent/KR102702654B1/ko active Active
- 2020-02-07 CN CN202510075819.2A patent/CN119874606A/zh active Pending
- 2020-02-07 WO PCT/EP2020/053171 patent/WO2020182384A1/en not_active Ceased
-
2021
- 2021-08-15 IL IL285630A patent/IL285630A/en unknown
- 2021-09-09 CL CL2021002357A patent/CL2021002357A1/es unknown
- 2021-09-09 US US17/470,980 patent/US11999698B2/en active Active
- 2021-09-10 MX MX2024014462A patent/MX2024014462A/es unknown
-
2024
- 2024-05-15 US US18/665,214 patent/US20240300898A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| BR112021017756A2 (pt) | 2021-11-16 |
| EP3938351A1 (en) | 2022-01-19 |
| AU2020234859B2 (en) | 2025-03-13 |
| JP2022524544A (ja) | 2022-05-06 |
| IL285630A (en) | 2021-09-30 |
| SG11202108957RA (en) | 2021-09-29 |
| US20200290969A1 (en) | 2020-09-17 |
| AU2020234859A1 (en) | 2021-09-16 |
| NZ779253A (en) | 2024-09-27 |
| MX2021011008A (es) | 2021-10-13 |
| KR102702654B1 (ko) | 2024-09-04 |
| KR20210137157A (ko) | 2021-11-17 |
| CN113784955B (zh) | 2025-02-14 |
| CN113784955A (zh) | 2021-12-10 |
| PH12021552171A1 (en) | 2022-09-12 |
| JP7360745B2 (ja) | 2023-10-13 |
| CN119874606A (zh) | 2025-04-25 |
| WO2020182384A1 (en) | 2020-09-17 |
| US20240300898A1 (en) | 2024-09-12 |
| MX2024014462A (es) | 2025-01-09 |
| US11149009B2 (en) | 2021-10-19 |
| US20210403433A1 (en) | 2021-12-30 |
| IL312955A (en) | 2024-07-01 |
| IL312955B1 (en) | 2026-01-01 |
| CA3129019A1 (en) | 2020-09-17 |
| CL2021002357A1 (es) | 2022-04-22 |
| US11999698B2 (en) | 2024-06-04 |
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