公开(公告)号：US20200323827A1

公开(公告)日：2020-10-15

申请号：US16908583

申请日：2020-06-22

申请人： Ariagen, Inc.

发明人： Jiasheng Song

IPC分类号： A61K31/427 ,  A61K31/40 ,  A61K31/425 ,  A61K31/475 ,  A61K45/06 ,  C07D417/06

摘要： A method of cancer intervention or eradication by administering an effective amount of an endogenous ligand for the aryl hydrocarbon (Ah) receptor (AhR) named ITE or one of its analogs (the active ingredient) to a subject with cancer is disclosed. An effective dose and dosing frequency of the active ingredient are determined by measuring its blood levels of the subject after dosing. The active ingredient formulated with a carrier system is applied topically, enterally, or parenterally to the subject. The formulated drug can also be administered together with one or more of other cancer therapeutic agents. A maintenance dosing is provided after the subject is free of cancer to insure the cancer eradication. Subjects with cancers of prostate, liver, lung, ovarian, and breast are preferably accepted for treatment.

公开(公告)号：US20190134009A1

公开(公告)日：2019-05-09

申请号：US16047805

申请日：2018-07-27

申请人： Ariagen, Inc.

发明人： Jiasheng Song

IPC分类号： A61K31/427 ,  C07D417/06 ,  A61K45/06 ,  A61K31/40 ,  A61K31/425 ,  A61K31/475

摘要： Provided herein are methods of cancer treatment by administering an effective amount of an endogenous ligand for the aryl hydrocarbon (Ah) receptor (AhR) named ITE or one of its structural analogs to a patient with cancer, for example, prostate, liver, lung, ovarian, breast, skin, colon (or rectum), stomach, pancreatic, kidney, bladder, soft tissue, or cervical cancer.

公开(公告)号：US20190084948A1

公开(公告)日：2019-03-21

申请号：US15998528

申请日：2018-08-16

申请人： Ariagen, Inc.

发明人： Jiasheng Song ,  Suoming Zhang ,  Guodong Li ,  Luqing Yang

IPC分类号： C07D277/20

摘要： Methods of synthesizing 2−(1′H-indole-3′-carbonyl)-thiazole-4-carboxylic acid methyl ester (ITE) and structural analogs thereof. The methods include condensation reactions or condensation and oxidation reactions to form the thiazoline or thiazole moiety of ITE or its structural analogs.

公开(公告)号：US20230054194A1

公开(公告)日：2023-02-23

申请号：US17295132

申请日：2019-11-19

申请人： ARIAGEN, INC.

发明人： Peter Colabuono

IPC分类号： A61K31/426 ,  A61K31/4245 ,  A61P35/00

摘要： The present disclosure relates to methods of treating cancer in a patient using a combination of an inhibitor of an immune checkpoint protein and an indole compound or its phosphate derivative.

公开(公告)号：US11547698B2

公开(公告)日：2023-01-10

申请号：US16473616

申请日：2017-12-22

申请人： ARIAGEN, INC.

发明人： Luqing Yang ,  Guodong Li ,  Suoming Zhang

IPC分类号： C07H19/044 ,  C07D401/06 ,  C07D403/06 ,  C07D409/06 ,  C07D413/06 ,  C07D417/06 ,  C07D417/10 ,  C07D417/14 ,  A61K31/4245 ,  A61P35/04 ,  A61K31/404 ,  A61K31/4196 ,  A61K31/427 ,  A61K31/433 ,  A61K31/437 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/7056 ,  A61K31/506 ,  A61K31/4025 ,  A61P35/00 ,  C07D209/12 ,  A61K31/4178 ,  A61K31/4439 ,  C07D419/14

摘要： The disclosure discloses an aryl hydrocarbon receptor modulators of formula (I), and pharmaceutically acceptable salts, R′ is H, CN, CH2(OH)R0, CmH2m+1, CnH2n-1, CnH2n-3, two Ra is independently H, or two Ra together form ═O or ═N—W3—R1; A is a C6 to C10 aromatic ring, or a C2 to C10 heteroaromatic ring containing 1 to 5 heteroatom from N, O and S, or 4 to 7 membered non-aromatic heterocyclic ring containing 1 to 3 heteroatom from N, O and S and C═N, which are with no substituent or substituted by 1 or 3 R; Q is R, or a C6 to C10 aromatic ring or a C2 to C10 heteroaromatic ring containing 1 to 5 heteroatom selected from N, O and S, which are with no substituent or substituted by 1 or 3 R; R is Rc connected with C or RN connected with N.

公开(公告)号：US20190307731A1

公开(公告)日：2019-10-10

申请号：US16229408

申请日：2018-12-21

申请人： Ariagen, Inc.

发明人： Luqing YANG ,  Guodong LI ,  Suoming ZHANG

IPC分类号： A61K31/4245 ,  A61K31/433 ,  A61K31/4196 ,  A61K31/427 ,  A61K31/404 ,  A61K31/437 ,  A61K31/7056 ,  A61K31/497 ,  A61K31/5377 ,  A61P35/04

摘要： Disclosed is an aryl hydrocarbon receptor modulator of formula (I), and a pharmaceutically acceptable salt thereof, wherein R′ is H, CN, CH2(OH)R0, CmH2m+1, CnH2n-1, CnH2n-3, two Ra are independently H or two Ra together form ═O or ═N—W3—R1; A is a C6 to C10 aromatic ring unsubstituted or substituted with 1 to 3 R, or a C2-C10 heteroaromatic ring interrupted by 1 to 5 heteroatoms selected from N, O, and S or a 4 to 7 membered nonaromatic heterocyclic ring containing C═N and interrupted by 1 to 3 heteroatoms selected from N, O, and S, with either one unsubstituted or substituted with 1 to 3 R; Q is R, or is a C6 to C10 aromatic ring or a C2 to C10 heteroaromatic ring unsubstituted or substituted with 1 to 3 R and interrupted by 1 to 5 heteroatoms selected from N, O, and S; and R is Rc which is C-attached or RN which is N-attached. The compounds of formula (I) of the present invention can regulate AhR activity, and can be used to inhibit the growth of cancer cells and inhibit the metastasis and invasion of tumor cells.

公开(公告)号：US20170333401A1

公开(公告)日：2017-11-23

申请号：US15613808

申请日：2017-06-05

申请人： Ariagen, Inc.

发明人： Jiasheng Song

IPC分类号： A61K31/427 ,  A61K31/475 ,  A61K31/40 ,  A61K31/425 ,  C07D417/06 ,  A61K45/06

CPC分类号： A61K31/427 ,  A61K31/40 ,  A61K31/425 ,  A61K31/475 ,  A61K45/06 ,  C07D417/06

摘要： A method of cancer intervention or eradication by administering an effective amount of an endogenous ligand for the aryl hydrocarbon (Ah) receptor (AhR) named ITE or one of its analogs (the active ingredient) to a subject with cancer is disclosed. An effective dose and dosing frequency of the active ingredient are determined by measuring its blood levels of the subject after dosing. The active ingredient formulated with a carrier system is applied topically, enterally, or parenterally to the subject. The formulated drug can also be administered together with one or more of other cancer therapeutic agents. A maintenance dosing is provided after the subject is free of cancer to insure the cancer eradication. Subjects with cancers of prostate, liver, lung, ovarian, and breast are preferably accepted for treatment.

公开(公告)号：US11427576B2

公开(公告)日：2022-08-30

申请号：US17179286

申请日：2021-02-18

申请人： ARIAGEN, INC.

发明人： Peter Colabuono ,  Graham Johnson ,  David Douglas Manning ,  Mark Allan Wolf

IPC分类号： C07D417/14 ,  A61P35/00 ,  C07D209/12 ,  C07D209/26 ,  C07D401/06 ,  C07D403/06 ,  C07D413/14 ,  C07D417/06

摘要： The present disclosure relates to indole compounds and pharmaceutical compositions thereof, and their use in stimulating the immune system of patients in need thereof and in treating cancer.

公开(公告)号：US20190275011A1

公开(公告)日：2019-09-12

申请号：US16210765

申请日：2018-12-05

申请人： Ariagen, Inc.

发明人： Jiasheng Song

IPC分类号： A61K31/427 ,  C07D417/06 ,  A61K45/06 ,  A61K31/40 ,  A61K31/425 ,  A61K31/475

摘要： A method of cancer intervention or eradication by administering an effective amount of an endogenous ligand for the aryl hydrocarbon (Ah) receptor (AhR) named ITE or one of its analogs (the active ingredient) to a subject with cancer is disclosed. An effective dose and dosing frequency of the active ingredient are determined by measuring its blood levels of the subject after dosing. The active ingredient formulated with a carrier system is applied topically, enterally, or parenterally to the subject. The formulated drug can also be administered together with one or more of other cancer therapeutic agents. A maintenance dosing is provided after the subject is free of cancer to insure the cancer eradication. Subjects with cancers of prostate, liver, lung, ovarian, and breast are preferably accepted for treatment.

公开(公告)号：US10195182B2

公开(公告)日：2019-02-05

申请号：US15613808

申请日：2017-06-05

申请人： Ariagen, Inc.

发明人： Jiasheng Song

IPC分类号： A61K31/427 ,  A61P35/00 ,  A61K31/40 ,  A61K31/425 ,  A61K31/475 ,  A61K45/06 ,  C07D417/06

摘要： A method of cancer intervention or eradication by administering an effective amount of an endogenous ligand for the aryl hydrocarbon (Ah) receptor (AhR) named ITE or one of its analogs (the active ingredient) to a subject with cancer is disclosed. An effective dose and dosing frequency of the active ingredient are determined by measuring its blood levels of the subject after dosing. The active ingredient formulated with a carrier system is applied topically, enterally, or parenterally to the subject. The formulated drug can also be administered together with one or more of other cancer therapeutic agents. A maintenance dosing is provided after the subject is free of cancer to insure the cancer eradication. Subjects with cancers of prostate, liver, lung, ovarian, and breast are preferably accepted for treatment.