AU2018388302B2 - GPCR heteromer inhibitors and uses thereof - Google Patents

GPCR heteromer inhibitors and uses thereof Download PDF

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Publication number
AU2018388302B2
AU2018388302B2 AU2018388302A AU2018388302A AU2018388302B2 AU 2018388302 B2 AU2018388302 B2 AU 2018388302B2 AU 2018388302 A AU2018388302 A AU 2018388302A AU 2018388302 A AU2018388302 A AU 2018388302A AU 2018388302 B2 AU2018388302 B2 AU 2018388302B2
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cxcr4
inhibitor
gpcrx
group
cxcl12
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AU2018388302A1 (en
Inventor
Won Ki Huh
Jae Yeon Jeong
Eun Hee Kim
So Hui Kim
Ji Yeong Lee
Mi Lim Lee
Chul O Park
Hye Ryung Park
Dong Seung Seen
Yong Bhum Song
Chang Soo Yang
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GPCR Therapeutics Inc
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GPCR Therapeutics Inc
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/19Cytokines; Lymphokines; Interferons
    • A61K38/195Chemokines, e.g. RANTES
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • A61K31/135Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/138Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/222Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having aromatic groups, e.g. dipivefrine, ibopamine
    • AHUMAN NECESSITIES
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • AHUMAN NECESSITIES
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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    • A61K31/33Heterocyclic compounds
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    • A61K31/435Heterocyclic 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
    • A61K31/439Heterocyclic 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 the ring forming part of a bridged ring system, e.g. quinuclidine
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    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/451Non condensed piperidines, e.g. piperocaine having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
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    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic 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
    • A61K31/5415Heterocyclic 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 ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
    • AHUMAN NECESSITIES
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    • A61K38/12Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
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    • A61K39/39533Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/3955Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
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    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
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    • C07K16/18Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/286Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against neuromediator receptors, e.g. serotonin receptor, dopamine receptor
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    • C07K16/28Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2866Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against receptors for cytokines, lymphokines, interferons
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/575Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G01N33/5758Immunoassay; Biospecific binding assay; Materials therefor for cancer involving compounds serving as markers for tumours, cancers or neoplasias, e.g. cellular determinants, receptors, heat shock/stress proteins, A-protein, oligosaccharides or metabolites
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    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/68Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids
    • G01N33/6893Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids related to diseases not provided for elsewhere
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    • C07K2317/76Antagonist effect on antigen, e.g. neutralization or inhibition of binding
    • GPHYSICS
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    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
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AU2018388302A 2017-12-19 2018-12-18 GPCR heteromer inhibitors and uses thereof Active AU2018388302B2 (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201762607876P 2017-12-19 2017-12-19
US62/607,876 2017-12-19
US201862679598P 2018-06-01 2018-06-01
US62/679,598 2018-06-01
US201862732946P 2018-09-18 2018-09-18
US62/732,946 2018-09-18
PCT/KR2018/016166 WO2019124951A1 (en) 2017-12-19 2018-12-18 Gpcr heteromer inhibitors and uses thereof

Publications (2)

Publication Number Publication Date
AU2018388302A1 AU2018388302A1 (en) 2020-07-02
AU2018388302B2 true AU2018388302B2 (en) 2024-10-31

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AU2018388302A Active AU2018388302B2 (en) 2017-12-19 2018-12-18 GPCR heteromer inhibitors and uses thereof

Country Status (10)

Country Link
US (3) US10709763B2 (https=)
EP (2) EP3727371A4 (https=)
JP (2) JP7517986B2 (https=)
KR (2) KR20260035212A (https=)
CN (1) CN111741752A (https=)
AU (1) AU2018388302B2 (https=)
BR (1) BR112020012075A2 (https=)
CA (1) CA3086337A1 (https=)
TW (1) TWI818938B (https=)
WO (1) WO2019124951A1 (https=)

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EP3727371A4 (en) 2017-12-19 2021-10-27 GPCR Therapeutics, Inc. GPCR HETEROMER INHIBITORS AND THEIR USES
MX2020009286A (es) 2018-03-05 2020-12-11 Teon Therapeutics Inc Antagonistas del receptor de adenosina y usos de los mismos.
CA3129314A1 (en) * 2019-03-06 2020-09-10 Vikramaditya Ganapati Yadav Compositions and methods for biosynthesis of terpenoids or cannabinoids in a heterologous system
BR112021022887A2 (pt) * 2019-05-17 2022-01-18 Gpcr Therapeutics Inc Inibidores de heterômero gpcr e usos dos mesmos
KR102268983B1 (ko) * 2019-09-11 2021-06-24 경북대학교 산학협력단 엔도테린 수용체 억제제에 의한 엑소좀 분비 억제 또는 pd-l1 발현 억제 용도
CN110755431B (zh) * 2019-11-08 2023-02-28 暨南大学 地氯雷他定在制备抗肝癌药物中的应用
WO2022025168A1 (ja) * 2020-07-30 2022-02-03 国立大学法人広島大学 凝固・線溶系と補体を介したマスト細胞および好塩基球の活性化の制御ならびにその医薬用途
CN116057185A (zh) 2020-08-15 2023-05-02 雷杰纳荣制药公司 治疗具有编码降钙素受体(calcr)的变体核酸分子的受试者的肥胖症
CN112807425A (zh) * 2021-01-14 2021-05-18 南方医科大学深圳医院 一种tTIM融合蛋白疫苗、制备方法及应用
WO2023010330A1 (zh) * 2021-08-04 2023-02-09 杭州浙大迪迅生物基因工程有限公司 一种人组胺受体HRH1 mRNA检测引物探针组、试剂盒和检测方法
CN114574580B (zh) * 2022-02-14 2022-11-29 山东大学 靶向a2br联合化疗在三阴性乳腺癌治疗中的应用
WO2023211779A1 (en) * 2022-04-25 2023-11-02 Kallyope, Inc. Treatment of headache disorders with nk3 modulators
CA3258771A1 (en) * 2022-06-10 2023-12-14 Gpcr Therapeutics, Inc. GPCR INHIBITORS AND THEIR USES
CN114891742B (zh) * 2022-06-23 2024-06-04 杭州中赢生物医疗科技有限公司 一种强杀伤性nk细胞的培养基及体外扩增方法
CN116298305B (zh) * 2023-01-03 2024-05-28 郑州大学 一种抗nt5c1a自身抗体检测方法及体外诊断试剂盒
EP4698530A1 (en) 2023-04-18 2026-02-25 Kallyope, Inc. Nk3 modulators and uses thereof
AU2024334309A1 (en) * 2023-08-30 2026-03-05 Josephine Cardarelli Gpcr inhibitors and uses thereof
CN119345201B (zh) * 2024-12-25 2025-03-18 中国人民解放军总医院第三医学中心 治疗tfe3基因重排性肾细胞癌的药物或药物组合物及用途

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