PE20220937A1 - Compuestos macrociclicos como agonistas de sting y metodos y usos de los mismos - Google Patents

Compuestos macrociclicos como agonistas de sting y metodos y usos de los mismos

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Publication number
PE20220937A1
PE20220937A1 PE2022000120A PE2022000120A PE20220937A1 PE 20220937 A1 PE20220937 A1 PE 20220937A1 PE 2022000120 A PE2022000120 A PE 2022000120A PE 2022000120 A PE2022000120 A PE 2022000120A PE 20220937 A1 PE20220937 A1 PE 20220937A1
Authority
PE
Peru
Prior art keywords
optionally substituted
ring
carboxamido
compound
heteroaryl
Prior art date
Application number
PE2022000120A
Other languages
English (en)
Inventor
Navnath Popat Karche
Moloy Banerjee
Nishant Ramnivasji Gupta
Ganesh Rajaram Jadhav
Vinod Popatrao Vyavahare
Amit Kumar Das
Deepak Sahebrao Walke
Vaibhav Madhukar Kalhapure
Smita Aditya Bhoskar
Vidya Ramdas
Venkata P Palle
Rajender Kumar Kamboj
Original Assignee
Lupin Ltd
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Filing date
Publication date
Application filed by Lupin Ltd filed Critical Lupin Ltd
Publication of PE20220937A1 publication Critical patent/PE20220937A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/16—Peri-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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/39—Medicinal preparations containing antigens or antibodies characterised by the immunostimulating additives, e.g. chemical adjuvants
    • 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
    • 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
    • A61P31/04—Antibacterial agents
    • 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
    • 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
    • A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6581—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms
    • C07F9/6584—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms having one phosphorus atom as ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K2039/555—Medicinal preparations containing antigens or antibodies characterised by a specific combination antigen/adjuvant
    • A61K2039/55511—Organic adjuvants

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Mycology (AREA)
  • Microbiology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Pulmonology (AREA)
  • Biochemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

La presente invencion se refiere a un compuesto de formula general (I), su forma tautomerica, su estereoisomero, su sal farmaceuticamente aceptable, donde: G1 es -CH2- o -CH(CH2)n-anillo A-; G2 es -CH=CH-; el anillo A es heterociclilo o heteroarilo opcionalmente sustituido; el anillo B es un anillo aromatico; el anillo C es heteroarilo de cinco miembros opcionalmente sustituido; R1 es heteroarilo opcionalmente sustituido, entre otros; R2 es hidrogeno, alquilo C1-C6 opcionalmente sustituido y cicloalquilo C3-C5 monociclico opcionalmente sustituido; o y m son 1; p es 0 a 2. Son compuestos especificos: acido (1S,4S)-4-((E)-12-carbamoil-1,15-bis(1-etil-3-metil-1H-pirazol-5-carboxamido)-8,9,16,19-tetrahidro-7H-6,10-dioxa-2,14,15a,19a-tetraazaciclopentadeca[3,2,1-cd:8,9,10-c'd']diinden-4-carboxamido)ciclohexano-1-carboxilico (Compuesto 1); acido (1R,4R)-4-((E)-12-carbamoil-1,15-bis(1-etil-3-metil-1H-pirazol-5-carboxamido)-8,9,16,19-tetrahidro-7H-6,10-dioxa-2,14,15a,19a-tetraazaciclopentadeca[3,2,1-cd:8,9,10-c'd']diinden-4-carboxamido)ciclohexano-1-carboxilico (Compuesto 2); entre otros. Tambien se refiere a una composicion farmaceutica. Dicho compuesto es un modulador de una proteina estimulador de genes de interferon (STING) y/o un complejo proteico STING, siendo util en el tratamiento del cancer y enfermedades infecciosas.
PE2022000120A 2019-07-22 2020-07-22 Compuestos macrociclicos como agonistas de sting y metodos y usos de los mismos PE20220937A1 (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
IN201921029556 2019-07-22
IN201921051086 2019-12-10
IN202021003961 2020-01-29
PCT/IB2020/056875 WO2021014365A1 (en) 2019-07-22 2020-07-22 Macrocyclic compounds as sting agonists and methods and uses thereof

Publications (1)

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PE20220937A1 true PE20220937A1 (es) 2022-05-31

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Country Status (18)

Country Link
US (1) US20220289763A1 (es)
EP (1) EP4004002B1 (es)
JP (1) JP2022541330A (es)
KR (1) KR20220035955A (es)
CN (1) CN114174303B (es)
AU (1) AU2020319058A1 (es)
BR (1) BR112022001125A2 (es)
CA (1) CA3147397A1 (es)
CL (1) CL2022000145A1 (es)
CO (1) CO2022001814A2 (es)
CR (1) CR20220029A (es)
EC (1) ECSP22005485A (es)
GE (1) GEP20247627B (es)
IL (1) IL289740A (es)
MX (1) MX2022000939A (es)
PE (1) PE20220937A1 (es)
WO (1) WO2021014365A1 (es)
ZA (1) ZA202201375B (es)

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TW202246242A (zh) * 2021-01-15 2022-12-01 美商西健公司 免疫調節抗體藥物結合物
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WO2024130341A1 (en) * 2022-12-22 2024-06-27 Aculeus Therapeutics Pty Ltd Benzimidazole derivatives for the modulation of sting

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CL2022000145A1 (es) 2022-09-09
MX2022000939A (es) 2022-04-06
IL289740A (en) 2022-03-01
ZA202201375B (en) 2022-09-28
KR20220035955A (ko) 2022-03-22
AU2020319058A1 (en) 2022-02-17
JP2022541330A (ja) 2022-09-22
CN114174303A (zh) 2022-03-11
WO2021014365A1 (en) 2021-01-28
GEP20247627B (en) 2024-05-27
CN114174303B (zh) 2024-06-25
BR112022001125A2 (pt) 2022-03-15
CR20220029A (es) 2022-03-14
EP4004002A1 (en) 2022-06-01
ECSP22005485A (es) 2022-02-25
US20220289763A1 (en) 2022-09-15
CA3147397A1 (en) 2021-01-28
CO2022001814A2 (es) 2022-04-29
EP4004002B1 (en) 2024-07-10

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