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 mismosInfo
- 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
Links
Classifications
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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 System
- 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
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.
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)
Publication Number | Publication Date |
---|---|
PE20220937A1 true PE20220937A1 (es) | 2022-05-31 |
Family
ID=72422197
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2022000120A PE20220937A1 (es) | 2019-07-22 | 2020-07-22 | Compuestos macrociclicos como agonistas de sting y metodos y usos de los mismos |
Country Status (17)
Country | Link |
---|---|
US (1) | US20220289763A1 (es) |
EP (1) | EP4004002A1 (es) |
JP (1) | JP2022541330A (es) |
KR (1) | KR20220035955A (es) |
CN (1) | CN114174303A (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) |
IL (1) | IL289740A (es) |
MX (1) | MX2022000939A (es) |
PE (1) | PE20220937A1 (es) |
WO (1) | WO2021014365A1 (es) |
ZA (1) | ZA202201375B (es) |
Families Citing this family (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US11155567B2 (en) | 2019-08-02 | 2021-10-26 | Mersana Therapeutics, Inc. | Sting agonist compounds and methods of use |
WO2021206158A1 (ja) | 2020-04-10 | 2021-10-14 | 小野薬品工業株式会社 | がん治療方法 |
EP4277904A1 (en) * | 2021-01-15 | 2023-11-22 | Seagen Inc. | Immunomodulatory antibody-drug conjugates |
UY39705A (es) * | 2021-03-30 | 2022-10-31 | Jacobio Pharmaceuticals Co Ltd | Novedosos compuestos útiles como agonistas de sting y sus usos |
Family Cites Families (27)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ITMI20010395A1 (it) | 2001-02-27 | 2002-08-27 | Dompe Spa | Omega-amminoalchilammidi di acidi r-2-aril-propionici come inibitori della chemiotassi di cellule polimorfonucleate e mononucleate |
AR046959A1 (es) | 2003-12-18 | 2006-01-04 | Tibotec Pharm Ltd | Morfolinilo que contiene bencimidazoles como inhibidores de la replicacion del virus sincitial respiratorio |
US7488736B2 (en) | 2004-05-17 | 2009-02-10 | Epix Delaware, Inc. | Thienopyridinone compounds and methods of treatment |
NZ567140A (en) | 2005-10-07 | 2011-09-30 | Exelixis Inc | Azetidines as MEK inhibitors for the treatment of proliferative diseases |
CN101506175A (zh) | 2006-06-15 | 2009-08-12 | 贝林格尔·英格海姆国际有限公司 | 作为蛋白激酶C-α抑制剂的2-苯氨基-4-(杂环基)氨基-嘧啶 |
WO2008090570A1 (en) | 2007-01-25 | 2008-07-31 | Panacea Biotec Ltd | Novel antimicrobials |
TW201000447A (en) | 2008-05-30 | 2010-01-01 | Astrazeneca Ab | New compounds useful in pain therapy |
WO2011091446A1 (en) * | 2010-01-22 | 2011-07-28 | Glaxosmithkline Llc | Chemical compounds |
WO2012083053A2 (en) * | 2010-12-15 | 2012-06-21 | Abbott Laboratories | Anti-viral compounds |
AU2013366974B2 (en) | 2012-12-28 | 2017-11-02 | Nippon Zoki Pharmaceutical Co., Ltd. | Cinnamic acid amide derivative |
ES2692226T3 (es) * | 2014-06-04 | 2018-11-30 | Glaxosmithkline Intellectual Property Development Limited | Dinucleótidos cíclicos como moduladores de STING |
US20180147187A1 (en) | 2015-01-12 | 2018-05-31 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for increasing cftr activity |
WO2017011920A1 (en) | 2015-07-22 | 2017-01-26 | The Royal Institution For The Advancement Of Learning/Mcgill University | Compounds and uses thereof in the treatment of cancers and other medical conditions |
US10981901B1 (en) * | 2016-04-07 | 2021-04-20 | Glaxosmithkline Intellectual Property Development Limited | Heterocyclic amides useful as protein modulators |
AU2017247806B2 (en) | 2016-04-07 | 2019-11-14 | Glaxosmithkline Intellectual Property Development Limited | Heterocyclic amides useful as protein modulators |
CN109153678B (zh) | 2016-05-27 | 2020-04-14 | 石药集团中奇制药技术(石家庄)有限公司 | 作为fgfr4抑制剂的杂环化合物 |
EA037671B1 (ru) * | 2017-02-22 | 2021-04-29 | Глэксосмитклайн Интеллекчуал Проперти Девелопмент Лимитед | Гетероциклические амиды, пригодные в качестве модуляторов белков |
JP2020524717A (ja) | 2017-06-22 | 2020-08-20 | キュラデブ・ファーマ・リミテッドCuradev Pharma Limited | ヒトstingの小分子調節因子 |
JP2020524718A (ja) | 2017-06-22 | 2020-08-20 | キュラデブ・ファーマ・リミテッドCuradev Pharma Limited | ヒトstingの複素環式小分子調節因子 |
AU2018288018C1 (en) | 2017-06-22 | 2022-10-20 | Curadev Pharma Limited | Small molecule modulators of human STING |
CN111615388B (zh) | 2017-07-27 | 2023-11-14 | 斯汀格瑞治疗股份有限公司 | 癌症免疫治疗剂 |
WO2019027857A1 (en) | 2017-08-04 | 2019-02-07 | Merck Sharp & Dohme Corp. | COMBINATIONS OF PD-1 ANTAGONISTS AND STING BENZO [B] THIOPHENIC AGONISTS FOR THE TREATMENT OF CANCER |
EP3661498A4 (en) | 2017-08-04 | 2021-04-21 | Merck Sharp & Dohme Corp. | BENZO [B] THIOPHEN STING ANTAGONISTS FOR CANCER TREATMENT |
US11377440B2 (en) * | 2017-10-05 | 2022-07-05 | Glaxosmithkline Intellectual Property Development Limited | Modulators of stimulator of interferon genes (STING) |
TW201927771A (zh) * | 2017-10-05 | 2019-07-16 | 英商葛蘭素史密斯克藍智慧財產發展有限公司 | 可作為蛋白質調節劑之雜環醯胺及其使用方法 |
WO2020132582A1 (en) * | 2018-12-21 | 2020-06-25 | Nimbus Titan, Inc. | Sting agonists and uses thereof |
EP3946610A1 (en) * | 2019-03-28 | 2022-02-09 | Lupin Limited | Macrocyclic compounds as sting agonists |
-
2020
- 2020-07-22 BR BR112022001125A patent/BR112022001125A2/pt unknown
- 2020-07-22 CR CR20220029A patent/CR20220029A/es unknown
- 2020-07-22 PE PE2022000120A patent/PE20220937A1/es unknown
- 2020-07-22 EP EP20768090.1A patent/EP4004002A1/en active Pending
- 2020-07-22 CN CN202080053237.XA patent/CN114174303A/zh active Pending
- 2020-07-22 CA CA3147397A patent/CA3147397A1/en active Pending
- 2020-07-22 AU AU2020319058A patent/AU2020319058A1/en active Pending
- 2020-07-22 US US17/628,619 patent/US20220289763A1/en active Pending
- 2020-07-22 WO PCT/IB2020/056875 patent/WO2021014365A1/en unknown
- 2020-07-22 JP JP2022504707A patent/JP2022541330A/ja active Pending
- 2020-07-22 MX MX2022000939A patent/MX2022000939A/es unknown
- 2020-07-22 KR KR1020227005943A patent/KR20220035955A/ko unknown
-
2022
- 2022-01-10 IL IL289740A patent/IL289740A/en unknown
- 2022-01-21 EC ECSENADI20225485A patent/ECSP22005485A/es unknown
- 2022-01-21 CL CL2022000145A patent/CL2022000145A1/es unknown
- 2022-01-28 ZA ZA2022/01375A patent/ZA202201375B/en unknown
- 2022-02-21 CO CONC2022/0001814A patent/CO2022001814A2/es unknown
Also Published As
Publication number | Publication date |
---|---|
CL2022000145A1 (es) | 2022-09-09 |
CO2022001814A2 (es) | 2022-04-29 |
ZA202201375B (en) | 2022-09-28 |
MX2022000939A (es) | 2022-04-06 |
US20220289763A1 (en) | 2022-09-15 |
AU2020319058A1 (en) | 2022-02-17 |
KR20220035955A (ko) | 2022-03-22 |
JP2022541330A (ja) | 2022-09-22 |
CN114174303A (zh) | 2022-03-11 |
IL289740A (en) | 2022-03-01 |
ECSP22005485A (es) | 2022-02-25 |
CR20220029A (es) | 2022-03-14 |
WO2021014365A1 (en) | 2021-01-28 |
BR112022001125A2 (pt) | 2022-03-15 |
CA3147397A1 (en) | 2021-01-28 |
EP4004002A1 (en) | 2022-06-01 |
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