AR111983A1 - ANILLOS 6 - 5 FUSIONADOS COMO INHIBIDORES DE C5a - Google Patents
ANILLOS 6 - 5 FUSIONADOS COMO INHIBIDORES DE C5aInfo
- Publication number
- AR111983A1 AR111983A1 ARP180101449A ARP180101449A AR111983A1 AR 111983 A1 AR111983 A1 AR 111983A1 AR P180101449 A ARP180101449 A AR P180101449A AR P180101449 A ARP180101449 A AR P180101449A AR 111983 A1 AR111983 A1 AR 111983A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- haloalkyl
- independently selected
- ring
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- 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
-
- 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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Immunology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Liquid Crystal Substances (AREA)
- Glass Compositions (AREA)
Abstract
Reivindicación 1: Un compuesto caracterizado porque es de la fórmula (1), o una sal farmacéuticamente aceptable del mismo, en donde: el vértice del anillo A⁰ es NH o C(O); cada uno de los vértices del anillo A¹ y A³ se seleccionan independientemente entre el grupo que consiste en N, NH, CH, C(O) y C(R⁴); cada uno de los vértices del anillo A², A⁵ y A⁶ se selecciona independientemente entre el grupo que consiste en N, CH, y C(R⁴); el vértice del anillo A⁴ se selecciona entre el grupo que consiste en N, N(alquilo C₁₋₄), CH, Y C(R⁴); y no más de dos de A³, A⁴, A⁵ y A⁶ son N; cada uno de los enlaces en líneas discontinuas es independientemente un enlace simple o doble; R¹ se selecciona entre el grupo que consiste en heteroarilo, arilo C₆₋₁₀, -alquileno C₁₋₈-heteroarilo, -alquilen C₁₋₈-arilo C₆₋₁₀, cicloalquilo C₃₋₈, heterocicloalquilo de cuatro a ocho miembros, alquilo C₁₋₈, haloalquilo C₁₋₈, -C(O)NR¹ᵃR¹ᵇ, y -CO₂R¹ᵃ; en donde el grupo heterocicloalquilo es un anillo de 4 a 8 miembros que tiene desde 1 hasta 3 heteroátomos como vértices del anillo seleccionados entre N, O y S; y el grupo heteroarilo es un anillo aromático de 5 a 10 miembros que tiene desde 1 hasta 3 heteroátomos como vértices del anillo seleccionados entre N, O y S; en donde R¹ᵃ y R¹ᵇ se seleccionan, cada uno independientemente, entre el grupo que consiste en hidrógeno, alquilo C₁₋₈, arilo C₆₋₁₀, y -alquilen C₁₋₆-arilo C₆₋₁₀; en donde R¹ está opcionalmente sustituido con 1 a 5 sustituyentes R⁵; R²ᵃ y R²ᵉ se seleccionan, cada uno independientemente, entre el grupo que consiste en alquilo C₁₋₆, alcoxi C₁₋₆, haloalquilo C₁₋₆,-O-haloalquilo C₁₋₆, -S-alquilo C₁₋₆, -alquil C₁₋₆-O-alquilo C₁₋₆, -alquil C₁₋₆-S-alquilo C₁₋₆, CN, y halógeno; R²ᵇ, R²ᶜ, y R²ᵈ se seleccionan, cada uno independientemente, entre el grupo que consiste en hidrógeno, alquilo C₁₋₆, alcoxi C₁₋₆, haloalquilo C₁₋₆, -O-haloalquilo C₁₋₆, -S-alquilo C₁₋₆, -alquil C₁₋₆-O-alquilo C₁₋₆, -alquil C₁₋₆-S-alquilo C₁₋₆, ciano, y halógeno; cada R³ se selecciona independientemente entre el grupo que consiste en alquilo C₁₋₄, haloalquilo C₁₋₄ e hidroxilo, y opcionalmente dos grupos R³ en el mismo átomo de carbono se combinan para formar oxo (=O); cada R⁴ se selecciona independientemente entre el grupo que consiste en alquilo C₁₋₆, alcoxi C₁₋₆, hidroxialquilo C₁₋₆, haloalquilo C₁₋₆, haloalcoxi C₁₋₆, -O-haloalquilo C₁₋₆, halógeno, ciano, hidroxilo, -S-alquilo C₁₋₆, -alquil C₁₋₆-O-alquilo C₁₋₆, -alquil C₁₋₆-S-alquilo C₁₋₆, -NR⁴ᵃR⁴ᵇ, -CONR⁴ᵃR⁴ᵇ, -CO₂R⁴ᵃ, -COR⁴ᵃ, -OC(O)NR⁴ᵃR⁴ᵇ, -NR⁴ᵃC(O)R⁴ᵇ, -NR⁴ᵃC(O)₂R⁴ᵇ, y -NR⁴ᵃ-C(O)NR⁴ᵃR⁴ᵇ; cada R⁴ᵃ y R⁴ᵇ se selecciona independientemente entre el grupo que consiste en hidrógeno, alquilo C₁₋₄, y haloalquilo C₁₋₄; cada R⁵ se selecciona independientemente entre el grupo que consiste en alquilo C₁₋₈, alcoxi C₁₋₈, haloalquilo C₁₋₈, haloalcoxi C₁₋₈, hidroxialquilo C₁₋₈, -alquil C₁₋₈-heterocicloalquilo, -alquil C₁₋₈-cicloalquilo C₃₋₈, cicloalquilo C₃₋₆, heterocicloalquilo, halógeno, OH, alquenilo C₂₋₈, alquinilo C₂₋₈, CN, C(O)R⁵ᵃ, -NR⁵ᵇC(O)R⁵ᵃ, -CONR⁵ᵃR⁵ᵇ, -NR⁵ᵃR⁵ᵇ, -alquilen C₁₋₈-NR⁵ᵃR⁵ᵇ, -S-alquilo C₁₋₆, -alquil C₁₋₆-O-alquilo C₁₋₆, -alquil C₁₋₆-S-alquilo C₁₋₆, -OC(O)NR⁵ᵃR⁵ᵇ, -NR⁵ᵃC(O)₂R⁵ᵇ, -NR⁵ᵃ-C(O)NR⁵ᵃR⁵ᵇ y CO₂R⁵ᵃ; en donde el grupo heterocicloalquilo es un anillo de 4 a 8 miembros que tiene desde 1 hasta 3 heteroátomos como vértices del anillo seleccionados entre N, O y S; en donde cada R⁵ᵃ y R⁵ᵇ se selecciona independientemente entre el grupo que consiste en hidrógeno, alquilo C₁₋₄, y haloalquilo C₁₋₄ o, cuando se unen al mismo átomo de carbono, R⁵ᵃ y R⁵ᵇ se combinan con el átomo de nitrógeno para formar un anillo de cinco o seis miembros que tiene entre 0 y 1 heteroátomos adicionales como vértices del anillo seleccionados entre N, O, o S; y el subíndice n es 0, 1, 2 ó 3.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762513010P | 2017-05-31 | 2017-05-31 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR111983A1 true AR111983A1 (es) | 2019-09-11 |
Family
ID=64456009
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP180101449A AR111983A1 (es) | 2017-05-31 | 2018-05-31 | ANILLOS 6 - 5 FUSIONADOS COMO INHIBIDORES DE C5a |
Country Status (14)
| Country | Link |
|---|---|
| US (3) | US10562896B2 (es) |
| EP (1) | EP3630775B1 (es) |
| JP (1) | JP7141130B2 (es) |
| KR (1) | KR102638253B1 (es) |
| CN (1) | CN110997674B (es) |
| AR (1) | AR111983A1 (es) |
| AU (1) | AU2018277520B2 (es) |
| BR (1) | BR112019025049A2 (es) |
| CA (1) | CA3064017A1 (es) |
| IL (1) | IL270828B2 (es) |
| MA (1) | MA48803A (es) |
| TW (1) | TWI781177B (es) |
| WO (1) | WO2018222598A1 (es) |
| ZA (1) | ZA201907746B (es) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112019025049A2 (pt) | 2017-05-31 | 2020-06-16 | Chemocentryx, Inc. | Anéis 6- 5 fundidos como inibidores de c5a |
| MX2019014292A (es) | 2017-05-31 | 2022-04-07 | Chemocentryx Inc | Anillos 5-5 fusionados como inhibidores c5a. |
| MX2020006459A (es) | 2017-12-22 | 2020-11-06 | Chemocentryx Inc | Compuestos de anillos fusionados 6,5 diaril sustituidos como inhibidores de c5ar. |
| KR20200110656A (ko) | 2017-12-22 | 2020-09-24 | 케모센트릭스, 인크. | C5aR 억제제로서의 디아릴 치환된 5,5-융합 고리 화합물 |
| MX2020010390A (es) | 2018-04-02 | 2021-01-15 | Chemocentryx Inc | Profarmacos de antagonistas de c5ar biciclicos fusionados. |
| BR112021025888A2 (pt) | 2019-07-10 | 2022-04-26 | Chemocentryx Inc | Indanos como inibidores de pd-l1 |
| CN112625036A (zh) * | 2019-10-08 | 2021-04-09 | 上海海和药物研究开发股份有限公司 | 一类具有brd4抑制活性的化合物、其制备方法及用途 |
| US20220047592A1 (en) * | 2020-08-13 | 2022-02-17 | Chemocentryx, Inc. | METHODS OF TREATING RESPIRATORY DISEASES USING C5a INHIBITORS |
| US11351149B2 (en) | 2020-09-03 | 2022-06-07 | Pfizer Inc. | Nitrile-containing antiviral compounds |
| US11844790B2 (en) | 2020-10-28 | 2023-12-19 | Chemocentryx, Inc. | Methods of treating hidradenitis suppurativa |
| CN112979646B (zh) * | 2021-03-08 | 2022-01-14 | 北京富龙康泰生物技术有限公司 | 一种咪唑并吡啶类衍生物 |
Family Cites Families (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK27383A (da) | 1982-02-17 | 1983-08-18 | Lepetit Spa | Fremgangsmaade til fremstilling af pyrazol(4,3-c)pyridiner |
| GB8613591D0 (en) | 1986-06-04 | 1986-07-09 | Roussel Lab Ltd | Chemical compounds |
| FR2761266B1 (fr) | 1997-03-28 | 1999-07-02 | Sanofi Sa | Composition pharmaceutique formee par granulation humide pour l'administration orale d'un derive du n-piperidino-3- pyrazolecarboxamide, de ses sels et de leurs solvates |
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| DE60039921D1 (de) | 2000-09-29 | 2008-09-25 | Neurogen Corp | Hochaffine kleinmolekülige c5a-rezeptor-modulatoren |
| SE524438C2 (sv) | 2000-10-05 | 2004-08-10 | Magnus Georg Goertz | Fjärrstyrt dörrelaterat låsarrangemang, första och andra datorpogramprodukt, bärande medium och ett datorlösbart medium |
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| WO2003082828A1 (en) | 2002-03-28 | 2003-10-09 | Neurogen Corporation | Substituted tetrahydroisoquinolines as c5a receptor modulators |
| CA2479928A1 (en) | 2002-03-28 | 2003-10-09 | Neurogen Corporation | Substituted biaryl amides as c5a receptor modulators |
| WO2003084524A1 (en) | 2002-03-29 | 2003-10-16 | Neurogen Corporation | Combination therapy for the treatment of conditions with pathogenic inflammatory components |
| WO2004016592A1 (en) * | 2002-08-14 | 2004-02-26 | Ppd Discovery, Inc. | Prenylation inhibitors and methods of their synthesis and use |
| WO2004018460A1 (en) | 2002-08-21 | 2004-03-04 | Neurogen Corporation | Amino methyl imidazoles as c5a receptor modulators |
| CA2504941C (en) | 2002-11-08 | 2012-06-26 | Neurogen Corporation | 3-substituted-6-aryl pyridines |
| US7145012B2 (en) | 2003-04-23 | 2006-12-05 | Pfizer Inc. | Cannabinoid receptor ligands and uses thereof |
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| AU2003902354A0 (en) | 2003-05-15 | 2003-05-29 | Harkin, Denis W. | Treatment of haemorrhagic shock |
| US20060154917A1 (en) | 2003-07-03 | 2006-07-13 | Neurogen Corporation | Substituted (heterocycloalkyl)methyl azole derivatives as c5a receptor modulators |
| US7906528B2 (en) | 2004-10-05 | 2011-03-15 | Novartis International Pharmaceutical Ltd. | Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds |
| AU2006278759B2 (en) | 2005-08-04 | 2012-08-16 | Janssen Pharmaceutica N.V. | Pyrimidine compounds as serotonin receptor modulators |
| US7598255B2 (en) | 2005-08-04 | 2009-10-06 | Janssen Pharmaceutica Nv | Pyrimidine compounds as serotonin receptor modulators |
| US20070112015A1 (en) | 2005-10-28 | 2007-05-17 | Chemocentryx, Inc. | Substituted dihydropyridines and methods of use |
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| PE20110063A1 (es) | 2008-06-20 | 2011-02-16 | Genentech Inc | DERIVADOS DE [1, 2, 4]TRIAZOLO[1, 5-a]PIRIDINA COMO INHIBIDORES DE JAK |
| CA2965223C (en) | 2008-12-22 | 2019-09-24 | Chemocentryx, Inc. | C5ar antagonists |
| US20110275639A1 (en) | 2008-12-22 | 2011-11-10 | Chemocentryx, Inc. | C5aR ANTAGONISTS |
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| JP2013529647A (ja) | 2010-06-24 | 2013-07-22 | ケモセントリックス，インコーポレイティド | Ｃ５ａＲアンタゴニスト |
| US8846656B2 (en) | 2011-07-22 | 2014-09-30 | Novartis Ag | Tetrahydropyrido-pyridine and tetrahydropyrido-pyrimidine compounds and use thereof as C5a receptor modulators |
| SG11201501133WA (en) | 2012-08-16 | 2015-04-29 | Janssen Pharmaceutica Nv | Pyrrolopyrazoles as n-type calcium channel blockers |
| CN103421006B (zh) * | 2013-08-18 | 2016-06-22 | 上海师范大学 | 2,3,5,7-四取代二氢吡唑并六氢吡啶衍生物及其制备方法和应用 |
| GB201321746D0 (en) | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic agents |
| RU2748260C2 (ru) | 2016-04-04 | 2021-05-21 | Кемосентрикс, Инк. | РАСТВОРИМЫЕ С5аR АНТАГОНИСТЫ |
| BR112019025049A2 (pt) | 2017-05-31 | 2020-06-16 | Chemocentryx, Inc. | Anéis 6- 5 fundidos como inibidores de c5a |
| MX2019014292A (es) | 2017-05-31 | 2022-04-07 | Chemocentryx Inc | Anillos 5-5 fusionados como inhibidores c5a. |
| US10589871B2 (en) | 2017-09-25 | 2020-03-17 | Hamilton Sundstrand Corporation | Prognostic health monitoring and jam detection for use with an aircraft |
| MX2020006459A (es) | 2017-12-22 | 2020-11-06 | Chemocentryx Inc | Compuestos de anillos fusionados 6,5 diaril sustituidos como inhibidores de c5ar. |
| KR20200110656A (ko) | 2017-12-22 | 2020-09-24 | 케모센트릭스, 인크. | C5aR 억제제로서의 디아릴 치환된 5,5-융합 고리 화합물 |
| MX2020010390A (es) | 2018-04-02 | 2021-01-15 | Chemocentryx Inc | Profarmacos de antagonistas de c5ar biciclicos fusionados. |
-
2018
- 2018-05-29 BR BR112019025049-2A patent/BR112019025049A2/pt active Search and Examination
- 2018-05-29 US US15/991,703 patent/US10562896B2/en active Active
- 2018-05-29 JP JP2019565833A patent/JP7141130B2/ja active Active
- 2018-05-29 MA MA048803A patent/MA48803A/fr unknown
- 2018-05-29 KR KR1020197038669A patent/KR102638253B1/ko active IP Right Grant
- 2018-05-29 WO PCT/US2018/034905 patent/WO2018222598A1/en active Application Filing
- 2018-05-29 CN CN201880036662.0A patent/CN110997674B/zh active Active
- 2018-05-29 AU AU2018277520A patent/AU2018277520B2/en active Active
- 2018-05-29 EP EP18809537.6A patent/EP3630775B1/en active Active
- 2018-05-29 CA CA3064017A patent/CA3064017A1/en active Pending
- 2018-05-31 TW TW107118601A patent/TWI781177B/zh active
- 2018-05-31 AR ARP180101449A patent/AR111983A1/es unknown
-
2019
- 2019-11-21 IL IL270828A patent/IL270828B2/en unknown
- 2019-11-22 ZA ZA2019/07746A patent/ZA201907746B/en unknown
- 2019-12-20 US US16/723,433 patent/US11384079B2/en active Active
-
2022
- 2022-05-03 US US17/735,283 patent/US11773091B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| US20180370967A1 (en) | 2018-12-27 |
| US10562896B2 (en) | 2020-02-18 |
| CN110997674A (zh) | 2020-04-10 |
| KR102638253B1 (ko) | 2024-02-16 |
| CA3064017A1 (en) | 2018-12-06 |
| TWI781177B (zh) | 2022-10-21 |
| RU2019142942A3 (es) | 2021-09-03 |
| AU2018277520B2 (en) | 2022-03-17 |
| US20230151002A1 (en) | 2023-05-18 |
| EP3630775A1 (en) | 2020-04-08 |
| US20200347049A1 (en) | 2020-11-05 |
| RU2019142942A (ru) | 2021-06-30 |
| US11384079B2 (en) | 2022-07-12 |
| JP2020522484A (ja) | 2020-07-30 |
| IL270828B (en) | 2022-12-01 |
| BR112019025049A2 (pt) | 2020-06-16 |
| KR20200015604A (ko) | 2020-02-12 |
| AU2018277520A1 (en) | 2019-12-12 |
| WO2018222598A1 (en) | 2018-12-06 |
| MA48803A (fr) | 2020-04-08 |
| CN110997674B (zh) | 2022-12-20 |
| US11773091B2 (en) | 2023-10-03 |
| ZA201907746B (en) | 2023-10-25 |
| EP3630775A4 (en) | 2020-10-07 |
| EP3630775B1 (en) | 2022-12-14 |
| JP7141130B2 (ja) | 2022-09-22 |
| IL270828B2 (en) | 2023-04-01 |
| IL270828A (en) | 2020-01-30 |
| TW201902895A (zh) | 2019-01-16 |
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