RU2014111060A - Лиганды рецептора эстрогена и способы их применения - Google Patents
Лиганды рецептора эстрогена и способы их применения Download PDFInfo
- Publication number
- RU2014111060A RU2014111060A RU2014111060/15A RU2014111060A RU2014111060A RU 2014111060 A RU2014111060 A RU 2014111060A RU 2014111060/15 A RU2014111060/15 A RU 2014111060/15A RU 2014111060 A RU2014111060 A RU 2014111060A RU 2014111060 A RU2014111060 A RU 2014111060A
- Authority
- RU
- Russia
- Prior art keywords
- alkyl
- compound
- aryl
- membered
- haloalkyl
- Prior art date
Links
- 239000003446 ligand Substances 0.000 title claims 2
- 102000015694 estrogen receptors Human genes 0.000 title 1
- 108010038795 estrogen receptors Proteins 0.000 title 1
- 238000000034 method Methods 0.000 claims abstract 42
- 125000000217 alkyl group Chemical group 0.000 claims abstract 30
- 125000003118 aryl group Chemical group 0.000 claims abstract 25
- 150000001875 compounds Chemical class 0.000 claims abstract 23
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract 19
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 19
- 239000001257 hydrogen Substances 0.000 claims abstract 19
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims abstract 19
- 125000001188 haloalkyl group Chemical group 0.000 claims abstract 15
- 229910052736 halogen Inorganic materials 0.000 claims abstract 14
- 150000002367 halogens Chemical class 0.000 claims abstract 14
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims abstract 14
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims abstract 13
- 229910052799 carbon Inorganic materials 0.000 claims abstract 13
- 206010060862 Prostate cancer Diseases 0.000 claims abstract 11
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims abstract 11
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract 10
- 229940124530 sulfonamide Drugs 0.000 claims abstract 10
- 150000003456 sulfonamides Chemical class 0.000 claims abstract 10
- 125000003545 alkoxy group Chemical group 0.000 claims abstract 9
- 125000004093 cyano group Chemical group *C#N 0.000 claims abstract 9
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims abstract 9
- 239000000825 pharmaceutical preparation Substances 0.000 claims abstract 9
- 229940127557 pharmaceutical product Drugs 0.000 claims abstract 9
- 150000003839 salts Chemical class 0.000 claims abstract 9
- 125000003342 alkenyl group Chemical group 0.000 claims abstract 5
- 125000000753 cycloalkyl group Chemical group 0.000 claims abstract 5
- 125000004982 dihaloalkyl group Chemical group 0.000 claims abstract 5
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims abstract 5
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract 5
- 125000004433 nitrogen atom Chemical group N* 0.000 claims abstract 5
- 125000004385 trihaloalkyl group Chemical group 0.000 claims abstract 5
- 230000002401 inhibitory effect Effects 0.000 claims abstract 2
- 230000004083 survival effect Effects 0.000 claims abstract 2
- 208000024891 symptom Diseases 0.000 claims abstract 2
- MUMGGOZAMZWBJJ-DYKIIFRCSA-N Testostosterone Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 MUMGGOZAMZWBJJ-DYKIIFRCSA-N 0.000 claims 14
- 210000002966 serum Anatomy 0.000 claims 9
- 230000002280 anti-androgenic effect Effects 0.000 claims 8
- 239000000051 antiandrogen Substances 0.000 claims 8
- 210000000988 bone and bone Anatomy 0.000 claims 8
- 230000000694 effects Effects 0.000 claims 8
- 238000002560 therapeutic procedure Methods 0.000 claims 8
- 229960003604 testosterone Drugs 0.000 claims 7
- 102000007066 Prostate-Specific Antigen Human genes 0.000 claims 5
- 108010072866 Prostate-Specific Antigen Proteins 0.000 claims 5
- 208000010392 Bone Fractures Diseases 0.000 claims 4
- 101100341863 Canis lupus familiaris KCNH2 gene Proteins 0.000 claims 4
- FKLJPTJMIBLJAV-UHFFFAOYSA-N Compound IV Chemical compound O1N=C(C)C=C1CCCCCCCOC1=CC=C(C=2OCCN=2)C=C1 FKLJPTJMIBLJAV-UHFFFAOYSA-N 0.000 claims 4
- 208000033830 Hot Flashes Diseases 0.000 claims 4
- 206010060800 Hot flush Diseases 0.000 claims 4
- 210000000577 adipose tissue Anatomy 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 201000000079 gynecomastia Diseases 0.000 claims 4
- 229910052500 inorganic mineral Inorganic materials 0.000 claims 4
- 230000001394 metastastic effect Effects 0.000 claims 4
- 206010061289 metastatic neoplasm Diseases 0.000 claims 4
- 239000011707 mineral Substances 0.000 claims 4
- 230000003247 decreasing effect Effects 0.000 claims 3
- 102000006395 Globulins Human genes 0.000 claims 1
- 108010044091 Globulins Proteins 0.000 claims 1
- 239000003163 gonadal steroid hormone Substances 0.000 claims 1
- 238000011474 orchiectomy Methods 0.000 claims 1
- 229940095743 selective estrogen receptor modulator Drugs 0.000 claims 1
- 239000000333 selective estrogen receptor modulator Substances 0.000 claims 1
- 239000003270 steroid hormone Substances 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- LKDRXBCSQODPBY-AMVSKUEXSA-N L-(-)-Sorbose Chemical compound OCC1(O)OC[C@H](O)[C@@H](O)[C@@H]1O LKDRXBCSQODPBY-AMVSKUEXSA-N 0.000 abstract 2
- YUCFVHQCAFKDQG-UHFFFAOYSA-N fluoromethane Chemical group F[CH] YUCFVHQCAFKDQG-UHFFFAOYSA-N 0.000 abstract 2
- 125000004429 atom Chemical group 0.000 abstract 1
- LJMYQSJCZOBGHG-UHFFFAOYSA-N CCCc(cc1)ccc1C(N(c(cc1)ccc1O)c(cc1)ccc1O)=O Chemical compound CCCc(cc1)ccc1C(N(c(cc1)ccc1O)c(cc1)ccc1O)=O LJMYQSJCZOBGHG-UHFFFAOYSA-N 0.000 description 1
- NJUCPSQPZWRTIE-UHFFFAOYSA-N Cc1c(C)c(C(N(c(cc2)ccc2O)c(cc2)ccc2O)=O)ccc1 Chemical compound Cc1c(C)c(C(N(c(cc2)ccc2O)c(cc2)ccc2O)=O)ccc1 NJUCPSQPZWRTIE-UHFFFAOYSA-N 0.000 description 1
- FYJHZJIZNLBYPB-UHFFFAOYSA-N Cc1cccc(CN(c(cc2)ccc2O)c(cc2)ccc2O)c1C Chemical compound Cc1cccc(CN(c(cc2)ccc2O)c(cc2)ccc2O)c1C FYJHZJIZNLBYPB-UHFFFAOYSA-N 0.000 description 1
- FBCQEUMZZNVQKD-UHFFFAOYSA-N Oc(cc1)ccc1N(C(c(cc1)cc(F)c1O)=O)c(cc1)ccc1F Chemical compound Oc(cc1)ccc1N(C(c(cc1)cc(F)c1O)=O)c(cc1)ccc1F FBCQEUMZZNVQKD-UHFFFAOYSA-N 0.000 description 1
- VLJZTJRWPPMWCP-UHFFFAOYSA-N Oc(cc1)ccc1N(C(c(cc1F)ccc1O)=O)c(cc1)ccc1O Chemical compound Oc(cc1)ccc1N(C(c(cc1F)ccc1O)=O)c(cc1)ccc1O VLJZTJRWPPMWCP-UHFFFAOYSA-N 0.000 description 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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
-
- 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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
-
- 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
- A61K31/4453—Non condensed piperidines, e.g. piperocaine only substituted in position 1, e.g. propipocaine, diperodon
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Emergency Medicine (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Steroid Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US13/215,679 US9427418B2 (en) | 2009-02-23 | 2011-08-23 | Estrogen receptor ligands and methods of use thereof |
| US13/215,679 | 2011-08-23 | ||
| PCT/US2012/052141 WO2013043304A1 (en) | 2009-02-23 | 2012-08-23 | Estrogen receptor ligands and methods of use thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2014111060A true RU2014111060A (ru) | 2015-09-27 |
Family
ID=48444651
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2014111060/15A RU2014111060A (ru) | 2011-08-23 | 2012-08-23 | Лиганды рецептора эстрогена и способы их применения |
Country Status (10)
| Country | Link |
|---|---|
| EP (1) | EP2747562A4 (enExample) |
| JP (1) | JP2014524479A (enExample) |
| KR (1) | KR20140064906A (enExample) |
| CN (1) | CN103957706A (enExample) |
| AU (1) | AU2012312902B2 (enExample) |
| CA (1) | CA2845890A1 (enExample) |
| IL (1) | IL231070A0 (enExample) |
| IN (1) | IN2014DN01959A (enExample) |
| MX (1) | MX2014002105A (enExample) |
| RU (1) | RU2014111060A (enExample) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111164093A (zh) * | 2017-09-27 | 2020-05-15 | 塔尔格免疫治疗有限公司 | 去势抵抗性前列腺癌 |
| JP2022523094A (ja) * | 2019-01-30 | 2022-04-21 | アラゴン ファーマシューティカルズ，インコーポレイテッド | 転移性去勢感受性前立腺癌の治療のための抗アンドロゲン剤 |
| CN113853216A (zh) * | 2019-02-01 | 2021-12-28 | 肿瘤学研究所基金会(Ior) | 治疗去势抵抗性前列腺癌的方法 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8546451B2 (en) * | 2005-11-28 | 2013-10-01 | Gtx, Inc. | Estrogen receptor ligands and methods of use thereof |
| EA023472B1 (ru) * | 2005-11-28 | 2016-06-30 | Джи Ти Икс, ИНК. | Агенты, связывающиеся с ядерными рецепторами |
| US8158828B2 (en) * | 2005-11-28 | 2012-04-17 | Gtx, Inc. | Nuclear receptor binding agents |
| WO2010096801A1 (en) * | 2009-02-23 | 2010-08-26 | Gtx, Inc. | Estrogen receptor ligands and methods of use thereof |
-
2012
- 2012-08-23 KR KR1020147007549A patent/KR20140064906A/ko not_active Withdrawn
- 2012-08-23 AU AU2012312902A patent/AU2012312902B2/en not_active Ceased
- 2012-08-23 IN IN1959DEN2014 patent/IN2014DN01959A/en unknown
- 2012-08-23 JP JP2014527312A patent/JP2014524479A/ja active Pending
- 2012-08-23 MX MX2014002105A patent/MX2014002105A/es unknown
- 2012-08-23 CA CA2845890A patent/CA2845890A1/en not_active Abandoned
- 2012-08-23 CN CN201280051979.4A patent/CN103957706A/zh active Pending
- 2012-08-23 EP EP12834287.0A patent/EP2747562A4/en not_active Withdrawn
- 2012-08-23 RU RU2014111060/15A patent/RU2014111060A/ru not_active Application Discontinuation
-
2014
- 2014-02-20 IL IL231070A patent/IL231070A0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AU2012312902B2 (en) | 2016-03-17 |
| JP2014524479A (ja) | 2014-09-22 |
| MX2014002105A (es) | 2014-09-25 |
| KR20140064906A (ko) | 2014-05-28 |
| CN103957706A (zh) | 2014-07-30 |
| CA2845890A1 (en) | 2013-03-28 |
| IN2014DN01959A (enExample) | 2015-05-15 |
| EP2747562A4 (en) | 2015-05-06 |
| IL231070A0 (en) | 2014-03-31 |
| EP2747562A1 (en) | 2014-07-02 |
| AU2012312902A1 (en) | 2013-05-23 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20161024 |