AR118471A1 - DERIVATIVES OF PIRROL AND IMIDAZOLE FUSED WITH PYRIDINE AS INHIBITORS OF RIPK2 - Google Patents
DERIVATIVES OF PIRROL AND IMIDAZOLE FUSED WITH PYRIDINE AS INHIBITORS OF RIPK2Info
- Publication number
- AR118471A1 AR118471A1 ARP200100803A ARP200100803A AR118471A1 AR 118471 A1 AR118471 A1 AR 118471A1 AR P200100803 A ARP200100803 A AR P200100803A AR P200100803 A ARP200100803 A AR P200100803A AR 118471 A1 AR118471 A1 AR 118471A1
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- Argentina
- Prior art keywords
- alkyl
- halo
- alkoxy
- substituted
- independently
- Prior art date
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- 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
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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
- A61K31/435—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
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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
- A61P11/00—Drugs for disorders of the respiratory system
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- 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
- A61P11/02—Nasal agents, e.g. decongestants
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- 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
- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- 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
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- 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]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
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- 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
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- 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
- A61P37/08—Antiallergic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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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
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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
- A61P9/10—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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Dermatology (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Physical Education & Sports Medicine (AREA)
- Neurosurgery (AREA)
- Otolaryngology (AREA)
- Transplantation (AREA)
- Hospice & Palliative Care (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pain & Pain Management (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Se describen compuestos de fórmula (1), y sales farmacéuticamente aceptables de estos, donde a, b, R², R³, R⁴, R⁵, R⁸, R⁹, X¹, X⁶ y X⁷ se definen en la memoria descriptiva. Esta descripción también hace referencia a materiales y métodos para la preparación de compuestos de fórmula (1), a composiciones farmacéuticas que los contienen y a su uso para el tratamiento de enfermedades, trastornos y afecciones asociados con RIPK2. Reivindicación 1: Un compuesto de fórmula (1), o una sal farmacéuticamente aceptable este donde: a es un enlace simple, b es un enlace doble, X¹ es NR¹N y R² es oxo; o a es un enlace doble, b es un enlace simple, X¹ se selecciona de N y CR¹C y R² se selecciona de hidrógeno, alquilo C₁₋₄ y alcoxi C₁₋₄; R¹C se selecciona de hidrógeno, halo y alquilo C₁₋₆ que se sustituye con 0 a 3 sustituyentes opcionales que se seleccionan independientemente de halo, hidroxi, ciano, alcoxi C₁₋₄ y amino que se sustituye opcionalmente con uno o dos alquilos C₁₋₄; R¹N se selecciona de alquilo C₁₋₄, cicloalquilo C₃₋₈-(CH₂)ₙ, heterociclilo C₂₋₈-(CH₂)ₙ y heteroarilo C₁₋₉-(CH₂)ₙ, donde cada uno de los restos de alquilo C₁₋₄, cicloalquilo C₃₋₈, heterociclilo C₂₋₈ y heteroarilo C₁₋₉ se sustituye con 0 a 3 sustituyentes opcionales que se seleccionan independientemente de halo, hidroxi, ciano, alquilo C₁₋₄, alcoxi C₁₋₄ y amino que se sustituye opcionalmente con uno o dos alquilos C₁₋₄, y donde cada uno de los sustituyentes opcionales de alquilo C₁₋₄ y alcoxi C₁₋₄ se sustituye independientemente con 0 a 3 sustituyentes opcionales que se seleccionan independientemente de halo; n se selecciona de 0, 1, 2 y 3; R³ es alquilo C₁₋₆ que se sustituye con 0 a 3 sustituyentes opcionales que se seleccionan independientemente de halo, hidroxi, ciano, alcoxi C₁₋₄ que se sustituye opcionalmente con alcoxi C₁₋₄, y de amino que se sustituye opcionalmente con uno o dos alquilos C₁₋₄, donde uno o más de los átomos de hidrógeno de R³ pueden ser opcionalmente deuterio; cada uno de R⁴ y R⁵ se selecciona independientemente de hidrógeno, halo y alquilo C₁₋₄; X⁶ se selecciona de N y C(R⁶); X⁷ se selecciona de N y C(R⁷); cada uno de R⁶ y R⁷ es independientemente hidrógeno, halo, alquilo C₁₋₄ y alcoxi C₁₋₄; R⁸ se selecciona de hidrógeno, halo, alquilo C₁₋₄ y alcoxi C₁₋₄, donde los sustituyentes de alquilo C₁₋₄ y alcoxi C₁₋₄ se sustituyen con 0 a 3 sustituyentes opcionales que se seleccionan independientemente de halo; y R⁹ se selecciona de alquilo C₁₋₆, cicloalquilo C₃₋₈, heterociclilo C₂₋₈ y heteroarilo C₁₋₉, cada uno sustituido con 0 a 3 sustituyentes opcionales que se seleccionan independientemente de halo, hidroxi, ciano, oxo, alquilo C₁₋₄, alcoxi C₁₋₄ y amino que se sustituye opcionalmente con uno o dos alquilos C₁₋₄, donde cada uno de los sustituyentes opcionales de alquilo C₁₋₄ y alcoxi C₁₋₄ se sustituye independientemente con 0 a 3 sustituyentes opcionales que se seleccionan independientemente de halo; y donde cada uno de los restos de heterociclilo y heteroarilo tiene independientemente de 1 a 4 miembros anulares que son heteroátomos, y cada uno de los heteroátomos se selecciona independientemente de N, O y S.Compounds of formula (1), and pharmaceutically acceptable salts thereof, are described, where a, b, R², R³, R⁴, R⁵, R⁸, R⁹, X¹, X⁶ and X⁷ are defined in the specification. This description also refers to materials and methods for the preparation of compounds of formula (1), to pharmaceutical compositions containing them and to their use for the treatment of diseases, disorders and conditions associated with RIPK2. Claim 1: A compound of formula (1), or a pharmaceutically acceptable salt, wherein: a is a single bond, b is a double bond, X¹ is NR¹N and R² is oxo; or a is a double bond, b is a single bond, X¹ is selected from N and CR¹C and R² is selected from hydrogen, C₁₋₄ alkyl, and C₁₋₄ alkoxy; R¹C is selected from hydrogen, halo, and C₁₋₆ alkyl which is substituted with 0 to 3 optional substituents which are independently selected from halo, hydroxy, cyano, C₁₋₄ alkoxy, and amino which is optionally substituted with one or two C₁₋₄ alkyls. ; R¹N is selected from C₁₋₄ alkyl, C₃₋₈- (CH₂) ₙ cycloalkyl, C₂₋₈- (CH₂) ₙ heterocyclyl, and C₁₋₉- (CH₂) ₙ heteroaryl, where each of the C₁₋₄ alkyl moieties , C₃₋₈ cycloalkyl, C₂₋₈ heterocyclyl, and C₁₋₉ heteroaryl is substituted with 0 to 3 optional substituents which are independently selected from halo, hydroxy, cyano, C₁₋₄ alkyl, C₁₋₄ alkoxy, and amino which is optionally substituted with one or two C₁₋₄ alkyls, and wherein each of the optional C₁₋₄ alkyl and C₁₋₄ alkoxy substituents is independently substituted with 0 to 3 optional substituents independently selected from halo; n is selected from 0, 1, 2, and 3; R³ is C₁₋₆ alkyl which is substituted with 0 to 3 optional substituents which are independently selected from halo, hydroxy, cyano, C₁₋₄ alkoxy which is optionally substituted with C₁₋₄ alkoxy, and from amino which is optionally substituted with one or two C₁₋₄ alkyls, where one or more of the hydrogen atoms of R³ may optionally be deuterium; R⁴ and R⁵ are each independently selected from hydrogen, halo, and C₁₋₄ alkyl; X⁶ is selected from N and C (R⁶); X⁷ is selected from N and C (R⁷); R⁶ and R⁷ are each independently hydrogen, halo, C₁₋₄ alkyl, and C₁₋₄ alkoxy; R⁸ is selected from hydrogen, halo, C₁₋₄ alkyl, and C₁₋₄ alkoxy, where the C₁₋₄ alkyl and C₁₋₄ alkoxy substituents are substituted with 0 to 3 optional substituents which are independently selected from halo; and R⁹ is selected from C₁₋₆ alkyl, C₃₋₈ cycloalkyl, C₂₋₈ heterocyclyl, and C₁₋₉ heteroaryl, each substituted with 0 to 3 optional substituents which are independently selected from halo, hydroxy, cyano, oxo, C₁₋ alkyl. ₄, C₁₋₄ alkoxy, and amino that is optionally substituted with one or two C₁₋₄ alkyls, where each of the optional C₁₋₄ alkyl and C₁₋₄ alkoxy substituents is independently substituted with 0 to 3 optional substituents that are selected regardless of halo; and where each of the heterocyclyl and heteroaryl moieties independently has 1 to 4 ring members that are heteroatoms, and each of the heteroatoms is independently selected from N, O, and S.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962822734P | 2019-03-22 | 2019-03-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR118471A1 true AR118471A1 (en) | 2021-10-06 |
Family
ID=70285980
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP200100803A AR118471A1 (en) | 2019-03-22 | 2020-03-20 | DERIVATIVES OF PIRROL AND IMIDAZOLE FUSED WITH PYRIDINE AS INHIBITORS OF RIPK2 |
Country Status (3)
| Country | Link |
|---|---|
| AR (1) | AR118471A1 (en) |
| TW (1) | TW202102498A (en) |
| WO (1) | WO2020198053A1 (en) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20240360125A9 (en) * | 2021-02-22 | 2024-10-31 | The Trustees Of Princeton University | 2-substituted bicyclo[1.1.1]pentanes |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5376645A (en) | 1990-01-23 | 1994-12-27 | University Of Kansas | Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof |
| KR0166088B1 (en) | 1990-01-23 | 1999-01-15 | . | Cyclodextrin derivatives with increased water solubility and uses thereof |
| GB9518953D0 (en) | 1995-09-15 | 1995-11-15 | Pfizer Ltd | Pharmaceutical formulations |
| GB9711643D0 (en) | 1997-06-05 | 1997-07-30 | Janssen Pharmaceutica Nv | Glass thermoplastic systems |
| JP6733050B2 (en) * | 2016-09-15 | 2020-07-29 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Heteroaryl carboxamide compounds as inhibitors of RIPK2 |
-
2020
- 2020-03-20 AR ARP200100803A patent/AR118471A1/en unknown
- 2020-03-20 WO PCT/US2020/023984 patent/WO2020198053A1/en active Application Filing
- 2020-03-20 TW TW109109361A patent/TW202102498A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2020198053A1 (en) | 2020-10-01 |
| TW202102498A (en) | 2021-01-16 |
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