RU2021107754A - ТЕТРАГИДРО-1H-ПИРИДО[3,4-b]ИНДОЛЬНЫЕ АНТИЭСТРОГЕННЫЕ ЛЕКАРСТВЕННЫЕ СРЕДСТВА - Google Patents
ТЕТРАГИДРО-1H-ПИРИДО[3,4-b]ИНДОЛЬНЫЕ АНТИЭСТРОГЕННЫЕ ЛЕКАРСТВЕННЫЕ СРЕДСТВА Download PDFInfo
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- RU2021107754A RU2021107754A RU2021107754A RU2021107754A RU2021107754A RU 2021107754 A RU2021107754 A RU 2021107754A RU 2021107754 A RU2021107754 A RU 2021107754A RU 2021107754 A RU2021107754 A RU 2021107754A RU 2021107754 A RU2021107754 A RU 2021107754A
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- compound
- cancer
- hydrogen
- pharmaceutically acceptable
- acceptable salt
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- 230000001833 anti-estrogenic effect Effects 0.000 title 1
- 239000003814 drug Substances 0.000 title 1
- 229940079593 drug Drugs 0.000 title 1
- 239000000328 estrogen antagonist Substances 0.000 title 1
- 238000000034 method Methods 0.000 claims 16
- 150000001875 compounds Chemical class 0.000 claims 11
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 206010006187 Breast cancer Diseases 0.000 claims 3
- 208000026310 Breast neoplasm Diseases 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 238000001356 surgical procedure Methods 0.000 claims 3
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 238000002560 therapeutic procedure Methods 0.000 claims 2
- 229940122815 Aromatase inhibitor Drugs 0.000 claims 1
- 206010005949 Bone cancer Diseases 0.000 claims 1
- 208000018084 Bone neoplasm Diseases 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 201000009273 Endometriosis Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 1
- 239000003886 aromatase inhibitor Substances 0.000 claims 1
- 238000002512 chemotherapy Methods 0.000 claims 1
- 238000009261 endocrine therapy Methods 0.000 claims 1
- 229940034984 endocrine therapy antineoplastic and immunomodulating agent Drugs 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 230000005855 radiation Effects 0.000 claims 1
- 206010046766 uterine cancer Diseases 0.000 claims 1
- 206010046885 vaginal cancer Diseases 0.000 claims 1
- 208000013139 vaginal neoplasm Diseases 0.000 claims 1
Classifications
-
- 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
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non 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
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/475—Quinolines; Isoquinolines having an indole ring, e.g. yohimbine, reserpine, strychnine, vinblastine
-
- 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
- A61K31/495—Heterocyclic 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric 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
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
-
- 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
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/32—Antioestrogens
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Physical Education & Sports Medicine (AREA)
- Reproductive Health (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Diabetes (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (39)
1. Способ предотвращения рецидива рака у пациента, включающий введение пациенту соединения Формулы I:
I
или его фармацевтически приемлемой соли,
где
X является -O-;
каждый R1 и R2 является водородом;
каждый R3 и R4 независимо выбран из водорода и галогена, и когда один из R3 или R4 является галогеном, другой из R3 или R4 является водородом;
R5 является C1-C6алкилом или C1-C6галогеналкилом;
R6 является C1-C6галогеналкилом; и
каждый R7 и R8 независимо выбран из водорода и C1-C6алкила.
2. Способ по п. 1, где рак выбран из рака молочной железы, рака яичника, рака эндометрия, рака влагалища, рака легкого, рака кости, рака матки и эндометриоза.
3. Способ по п. 1, где соединение вводят в качестве вспомогательной терапии после или вместо химиотерапии, радиации или хирургии.
4. Способ по п. 3, где соединение вводят после хирургии.
5. Способ по п. 1, где соединение вводят до хирургии.
6. Способ по п. 2, где раком является рак молочной железы.
7. Способ по п. 6, где рак молочной железы прогрессировал в присутствии эндокринной терапии или терапии ингибитором ароматазы.
10. Способ по п. 1, где соединение является соединением Формулы I(a):
I(a)
или его фармацевтически приемлемой солью.
11. Способ по п. 10, где каждый R1, R2, R3 и R4 является водородом.
12. Способ по п. 1, где соединение является соединением Формулы I(c):
I(c)
или его фармацевтически приемлемой солью.
13. Способ по п. 12, где каждый R1, R2, R3 и R4 является водородом.
14. Способ по п. 1, где соединение представляет собой:
или его фармацевтически приемлемую соль.
15. Способ по п. 1, где соединение представляет собой:
или его фармацевтически приемлемую соль.
16. Способ по п. 1, где соединение представляет собой:
или его фармацевтически приемлемую соль.
Applications Claiming Priority (2)
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US201562235900P | 2015-10-01 | 2015-10-01 | |
US62/235,900 | 2015-10-01 |
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RU2018115696A Division RU2745742C1 (ru) | 2015-10-01 | 2016-09-29 | ТЕТРАГИДРО-1Н-ПИРИДО[3,4-b]ИНДОЛЬНЫЕ АНТИЭСТРОГЕННЫЕ ЛЕКАРСТВЕННЫЕ СРЕДСТВА |
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RU2021107754A true RU2021107754A (ru) | 2021-04-01 |
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RU2018115696A RU2745742C1 (ru) | 2015-10-01 | 2016-09-29 | ТЕТРАГИДРО-1Н-ПИРИДО[3,4-b]ИНДОЛЬНЫЕ АНТИЭСТРОГЕННЫЕ ЛЕКАРСТВЕННЫЕ СРЕДСТВА |
RU2021107754A RU2021107754A (ru) | 2015-10-01 | 2016-09-29 | ТЕТРАГИДРО-1H-ПИРИДО[3,4-b]ИНДОЛЬНЫЕ АНТИЭСТРОГЕННЫЕ ЛЕКАРСТВЕННЫЕ СРЕДСТВА |
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RU2018115696A RU2745742C1 (ru) | 2015-10-01 | 2016-09-29 | ТЕТРАГИДРО-1Н-ПИРИДО[3,4-b]ИНДОЛЬНЫЕ АНТИЭСТРОГЕННЫЕ ЛЕКАРСТВЕННЫЕ СРЕДСТВА |
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US (5) | US10292971B2 (ru) |
EP (2) | EP3912680A1 (ru) |
JP (3) | JP6776348B2 (ru) |
KR (1) | KR20180071274A (ru) |
CN (2) | CN108366996B (ru) |
AU (3) | AU2016331065B2 (ru) |
BR (2) | BR122023020677A2 (ru) |
CA (1) | CA3000410A1 (ru) |
CL (1) | CL2018000827A1 (ru) |
CY (1) | CY1124669T1 (ru) |
DK (1) | DK3355884T3 (ru) |
ES (1) | ES2881398T3 (ru) |
HR (1) | HRP20211124T1 (ru) |
HU (1) | HUE055321T2 (ru) |
IL (3) | IL286518B1 (ru) |
LT (1) | LT3355884T (ru) |
MX (2) | MX2018003929A (ru) |
PL (1) | PL3355884T3 (ru) |
PT (1) | PT3355884T (ru) |
RS (1) | RS62133B1 (ru) |
RU (2) | RU2745742C1 (ru) |
SI (1) | SI3355884T1 (ru) |
UA (1) | UA122346C2 (ru) |
WO (1) | WO2017059139A1 (ru) |
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CN111770924B (zh) * | 2018-04-04 | 2023-05-09 | 深圳福沃药业有限公司 | 用于治疗乳腺癌的***受体降解剂 |
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