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 RIPK2

Info

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
Authority
AR
Argentina
Prior art keywords
alkyl
halo
alkoxy
substituted
independently
Prior art date
Application number
ARP200100803A
Other languages
Spanish (es)
Original Assignee
Takeda Pharmaceuticals Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Takeda Pharmaceuticals Co filed Critical Takeda Pharmaceuticals Co
Publication of AR118471A1 publication Critical patent/AR118471A1/en

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
    • 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
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • 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
    • 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
    • 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

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.

ARP200100803A 2019-03-22 2020-03-20 DERIVATIVES OF PIRROL AND IMIDAZOLE FUSED WITH PYRIDINE AS INHIBITORS OF RIPK2 AR118471A1 (en)

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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN117500778A (en) * 2021-02-22 2024-02-02 普林斯顿大学保管委员会 2-substituted bicyclo [1.1.1] pentanes

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR0166088B1 (en) 1990-01-23 1999-01-15 . Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof
US5376645A (en) 1990-01-23 1994-12-27 University Of Kansas Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use 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
ES2816003T3 (en) * 2016-09-15 2021-03-31 Boehringer Ingelheim Int Heteroaryl carboxamide compounds as RIPK2 inhibitors

Also Published As

Publication number Publication date
TW202102498A (en) 2021-01-16
WO2020198053A1 (en) 2020-10-01

Similar Documents

Publication Publication Date Title
PE20220931A1 (en) PYRAZOLO[3,4-B]PYRAZINE-TYPE SHP2 PHOSPHATASE INHIBITORS
AR107714A1 (en) DERIVATIVES OF PIRAZOLO [1,5-A] PIRAZIN-4-ILO
AR119424A1 (en) 3-OXO-4H-QUINOXALINE AND OXO-1H-NAPHTHYRIDINE DERIVATIVES AS PARP INHIBITORS
AR113964A1 (en) CARBAMOIL CYCLOHEXYL N-LINKED ACIDS OF TRIAZOLE AS ANTAGONISTS OF LPA
AR120080A1 (en) BRANCH-TAIL LIPID COMPOUNDS AND COMPOSITIONS FOR INTRACELLULAR DELIVERY OF THERAPEUTIC AGENTS
AR112834A1 (en) RAPAMYCIN DERIVATIVES
AR119018A1 (en) DNA-DEPENDENT PROTEIN KINASE INHIBITORS
AR119657A1 (en) PYRIMIDINE COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS FOR PREVENTING OR TREATING CANCERS INCLUDING THE SAME
AR117139A1 (en) DERIVATIVES OF PYRIDOOXAZINONE AS INHIBITORS OF MONOACILGLICEROL LIGASE (MAGL)
AR109709A1 (en) 3-QUINASA PHOSFATIDYLINOSITOL INHIBITORS
AR100438A1 (en) PIRAZOLOPIRIDINAS AND PIRAZOLOPIRIMIDINAS
AR099228A1 (en) FXIA MACROCYCLIC INHIBITORS THAT HAVE HETEROCYCLIC GROUPS
AR114793A1 (en) MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES OF THEM
AR114369A1 (en) CYCLIC DINUCLEOTIDES AS ANTINEOPLASTIC AGENTS
AR121078A1 (en) ARILAMIDE DERIVATIVES WITH ANTI-TUMOR ACTIVITY
AR117424A1 (en) INHIBITORS OF ERBB RECEPTORS
AR098666A1 (en) BIARILACETAMIDE COMPOUNDS AND THEIR METHODS OF USE
AR106301A1 (en) PIRROLPIRIMIDINE COMPOSITIONS AS KINASE INHIBITORS
AR087607A1 (en) DERIVATIVES OF PIRIDAZINONA
AR119728A1 (en) 3-AMINO-4H-BENZO[E][1,2,4]THIADAZINE 1,1-DIOXIDE DERIVATIVES AS MRGX2 INHIBITORS
AR103232A1 (en) TGFbR ANTAGONISTS
AR104878A1 (en) ROR GAMMA MODULATORS (RORg)
AR096846A1 (en) DIHYDROCHINOXALINONES AND MODIFIED DIHYDROPIRIDOPIRAZINONES AS INHIBITORS OF BET PROTEIN
AR116464A1 (en) N-SUBSTITUTED DIOXOCYCLOBUTENYLAMINE-3-HYDROXY-PICOLINAMIDES USEFUL AS INHIBITORS OF CCR6
AR090835A1 (en) DERIVATIVES OF QUINAZOLINDIONA

Legal Events

Date Code Title Description
FB Suspension of granting procedure