CN103180318B - 雄性避孕组合物以及使用方法 - Google Patents
雄性避孕组合物以及使用方法 Download PDFInfo
- Publication number
- CN103180318B CN103180318B CN201180033583.2A CN201180033583A CN103180318B CN 103180318 B CN103180318 B CN 103180318B CN 201180033583 A CN201180033583 A CN 201180033583A CN 103180318 B CN103180318 B CN 103180318B
- Authority
- CN
- China
- Prior art keywords
- compound
- pharmaceutically acceptable
- pharmaceutical composition
- acceptable salt
- compounds
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
Links
- 0 Cc1c(C)[s]c-2c1C(c1cccnc1)=N[C@@](C*)c1nnc(*)[n]-21 Chemical compound Cc1c(C)[s]c-2c1C(c1cccnc1)=N[C@@](C*)c1nnc(*)[n]-21 0.000 description 6
- DNVXATUJJDPFDM-KRWDZBQOSA-N CC(C)(C)OC(C[C@@H](c1nnc(C)[n]1-c1c2c(C)c(C)[s]1)N=C2c(cc1)ccc1Cl)=O Chemical compound CC(C)(C)OC(C[C@@H](c1nnc(C)[n]1-c1c2c(C)c(C)[s]1)N=C2c(cc1)ccc1Cl)=O DNVXATUJJDPFDM-KRWDZBQOSA-N 0.000 description 2
- DRAFCSAJESYJHV-INIZCTEOSA-N CC(C)(C)OC(C[C@@H](c1nnc(C)[n]1-c1c2c(C)c(C)[s]1)N=C2c1cnccc1)=O Chemical compound CC(C)(C)OC(C[C@@H](c1nnc(C)[n]1-c1c2c(C)c(C)[s]1)N=C2c1cnccc1)=O DRAFCSAJESYJHV-INIZCTEOSA-N 0.000 description 1
- ZJAASZGGNFOQNT-SFHVURJKSA-N CC(C)(C)OC(C[C@@H]1N=C(c2ccccc2)c(cccc2)c2-[n]2c1nnc2C)=O Chemical compound CC(C)(C)OC(C[C@@H]1N=C(c2ccccc2)c(cccc2)c2-[n]2c1nnc2C)=O ZJAASZGGNFOQNT-SFHVURJKSA-N 0.000 description 1
- UMIBLDRMWPTDSJ-VVESCEMWSA-N CC(C)(C)OC1OC1C[C@@H](c1nnc(C)[n]1-c1c2c(C)c(C)[s]1)N=C2c(cc1)ccc1F Chemical compound CC(C)(C)OC1OC1C[C@@H](c1nnc(C)[n]1-c1c2c(C)c(C)[s]1)N=C2c(cc1)ccc1F UMIBLDRMWPTDSJ-VVESCEMWSA-N 0.000 description 1
- RWQUFNCPGPFPTO-LWNRLHBOSA-N C[C@]1(C=CC1(C)I)C1=N[C@@H](CN)c2nnc(C)[n]2-c2c1c(C)c(C)[s]2 Chemical compound C[C@]1(C=CC1(C)I)C1=N[C@@H](CN)c2nnc(C)[n]2-c2c1c(C)c(C)[s]2 RWQUFNCPGPFPTO-LWNRLHBOSA-N 0.000 description 1
- UZTOHVPWBXIIOR-UHFFFAOYSA-N Cc1c(C)[s]c(N)c1C(c(cc1)ccc1F)=O Chemical compound Cc1c(C)[s]c(N)c1C(c(cc1)ccc1F)=O UZTOHVPWBXIIOR-UHFFFAOYSA-N 0.000 description 1
- WOAUDLIUVRNRNI-UHFFFAOYSA-N Cc1c(C)[s]c(N)c1C(c1cccnc1)=O Chemical compound Cc1c(C)[s]c(N)c1C(c1cccnc1)=O WOAUDLIUVRNRNI-UHFFFAOYSA-N 0.000 description 1
- LJOSBOOJFIRCSO-AWEZNQCLSA-N Cc1c(C)[s]c-2c1C(c(cc1)ccc1Cl)=N[C@@H](CC(O)=O)c1nnc(C)[n]-21 Chemical compound Cc1c(C)[s]c-2c1C(c(cc1)ccc1Cl)=N[C@@H](CC(O)=O)c1nnc(C)[n]-21 LJOSBOOJFIRCSO-AWEZNQCLSA-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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
- A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
- A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
-
- 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
- A61P15/16—Masculine contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D495/14—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Reproductive Health (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicinal Preparation (AREA)
- Peptides Or Proteins (AREA)
Applications Claiming Priority (11)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US33499110P | 2010-05-14 | 2010-05-14 | |
| US61/334,991 | 2010-05-14 | ||
| US37074510P | 2010-08-04 | 2010-08-04 | |
| US61/370,745 | 2010-08-04 | ||
| US37586310P | 2010-08-22 | 2010-08-22 | |
| US61/375,863 | 2010-08-22 | ||
| US201161467376P | 2011-03-24 | 2011-03-24 | |
| US201161467299P | 2011-03-24 | 2011-03-24 | |
| US61/467,299 | 2011-03-24 | ||
| US61/467,376 | 2011-03-24 | ||
| PCT/US2011/036667 WO2011143657A1 (en) | 2010-05-14 | 2011-05-16 | Male contraceptive compositions and methods of use |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103180318A CN103180318A (zh) | 2013-06-26 |
| CN103180318B true CN103180318B (zh) | 2017-05-10 |
Family
ID=44914744
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201180033583.2A Expired - Fee Related CN103180318B (zh) | 2010-05-14 | 2011-05-16 | 雄性避孕组合物以及使用方法 |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US9301962B2 (enExample) |
| EP (1) | EP2571875A4 (enExample) |
| JP (1) | JP6022442B2 (enExample) |
| CN (1) | CN103180318B (enExample) |
| CA (1) | CA2799381A1 (enExample) |
| WO (1) | WO2011143657A1 (enExample) |
Families Citing this family (44)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5913292B2 (ja) * | 2010-05-14 | 2016-04-27 | ダナ−ファーバー キャンサー インスティテュート, インコーポレイテッド | 代謝を調節する組成物および方法 |
| US8981083B2 (en) * | 2010-05-14 | 2015-03-17 | Dana Farber Cancer Institute, Inc. | Compositions and methods for treating neoplasia, inflammatory disease and other disorders |
| CA2799381A1 (en) | 2010-05-14 | 2011-11-17 | Dana-Farber Cancer Institute, Inc. | Male contraceptive compositions and methods of use |
| MX373121B (es) | 2010-05-14 | 2020-04-30 | Dana Farber Cancer Inst Inc | Composiciones y metodos para el tratamiento de leucemia. |
| US9249161B2 (en) | 2010-12-02 | 2016-02-02 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| AR084070A1 (es) | 2010-12-02 | 2013-04-17 | Constellation Pharmaceuticals Inc | Inhibidores del bromodominio y usos de los mismos |
| WO2012151512A2 (en) | 2011-05-04 | 2012-11-08 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| US9328117B2 (en) | 2011-06-17 | 2016-05-03 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| TWI602820B (zh) | 2012-06-06 | 2017-10-21 | 星宿藥物公司 | 溴域抑制劑及其用途 |
| US9624244B2 (en) | 2012-06-06 | 2017-04-18 | Constellation Pharmaceuticals, Inc. | Benzo [B] isoxazoloazepine bromodomain inhibitors and uses thereof |
| US9714946B2 (en) * | 2013-03-14 | 2017-07-25 | Dana-Farber Cancer Institute, Inc. | Bromodomain binding reagents and uses thereof |
| MX366703B (es) | 2013-03-15 | 2019-07-22 | Incyte Holdings Corp | Heterociclos tricíclicos como inhibidores de la proteína bet. |
| CA2901083A1 (en) | 2013-04-26 | 2014-10-30 | Beigene, Ltd. | Substituted 5-(3,5-dimethylisoxazol-4-yl)indoline-2-ones |
| WO2015006193A1 (en) | 2013-07-08 | 2015-01-15 | Incyte Corporation | Tricyclic heterocycles as bet protein inhibitors |
| BR112016001457A2 (pt) | 2013-07-25 | 2017-08-29 | Dana Farber Cancer Inst Inc | Inibidores de fatores de transcrição e usos dos mesmos |
| CN103694253A (zh) * | 2013-11-04 | 2014-04-02 | 湖南华腾制药有限公司 | 一种噻吩并三唑并[4,3-a][1,4]二氮杂卓类化合物的制备方法 |
| KR20160072261A (ko) | 2013-11-08 | 2016-06-22 | 다나-파버 캔서 인스티튜트 인크. | 브로모도메인 및 엑스트라-말단 (bet) 단백질 저해제를 이용한 암 치료를 위한 조합 요법 |
| US9315501B2 (en) | 2013-11-26 | 2016-04-19 | Incyte Corporation | Bicyclic heterocycles as BET protein inhibitors |
| WO2015081203A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| US9309246B2 (en) | 2013-12-19 | 2016-04-12 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| MX2016009974A (es) | 2014-01-31 | 2016-10-31 | Dana Farber Cancer Inst Inc | Derivados de diaminopirimidina bencensulfona y sus usos. |
| WO2015117087A1 (en) | 2014-01-31 | 2015-08-06 | Dana-Farber Cancer Institute, Inc. | Uses of diazepane derivatives |
| RU2722179C2 (ru) | 2014-02-28 | 2020-05-28 | Тэнша Терапеутикс, Инк. | Лечение состояний, ассоциированных с гиперинсулинемией |
| ES2827253T3 (es) | 2014-04-14 | 2021-05-20 | Hayashibara Co | Preparación cutánea externa antienvejecimiento |
| UA119870C2 (uk) | 2014-04-23 | 2019-08-27 | Інсайт Корпорейшн | 1H-ПІРОЛО[2,3-c]ПІРИДИН-7(6H)-ОНИ ТА ПІРАЗОЛО[3,4-c]ПІРИДИН-7(6H)-ОНИ ЯК ІНГІБІТОРИ БІЛКІВ BET |
| CN106687463B (zh) | 2014-06-20 | 2019-04-09 | 星座制药公司 | 一种乙酰胺类化合物的晶型 |
| WO2016022970A1 (en) | 2014-08-08 | 2016-02-11 | Dana-Farber Cancer Institute, Inc. | Dihydropteridinone derivatives and uses thereof |
| EP3177626A4 (en) | 2014-08-08 | 2017-12-27 | Dana Farber Cancer Institute, Inc. | Diazepane derivatives and uses thereof |
| ES2855225T3 (es) | 2014-09-15 | 2021-09-23 | Incyte Corp | Heterociclos tricíclicos para su uso como inhibidores de proteínas BET |
| UA122130C2 (uk) * | 2014-10-27 | 2020-09-25 | Тенша Терапеутікс, Інк. | Інгібітори бромодомену |
| US20180163180A1 (en) * | 2015-05-01 | 2018-06-14 | The UAB Research Foundation Inc. | Method of enhancing somatic cell reprogramming with the acetyllysine reader brd3r |
| US10702527B2 (en) | 2015-06-12 | 2020-07-07 | Dana-Farber Cancer Institute, Inc. | Combination therapy of transcription inhibitors and kinase inhibitors |
| JP2018526424A (ja) * | 2015-09-11 | 2018-09-13 | ダナ−ファーバー キャンサー インスティテュート, インコーポレイテッド | アセトアミドチエノトリアゾロジアゼピンおよびこれらの使用 |
| US11306105B2 (en) | 2015-09-11 | 2022-04-19 | Dana-Farber Cancer Institute, Inc. | Cyano thienotriazolodiazepines and uses thereof |
| PE20181068A1 (es) * | 2015-10-02 | 2018-07-04 | Dana Farber Cancer Inst Inc | Terapia de combinacion de inhibidores de bromodominios y bloqueo de puntos de control |
| TW201722966A (zh) | 2015-10-29 | 2017-07-01 | 英塞特公司 | Bet蛋白質抑制劑之非晶固體形式 |
| CR20180336A (es) | 2015-11-25 | 2018-08-06 | Dana Farber Cancer Inst Inc | Inhibidores de bromodominio bivalentes y usos de los mismos |
| WO2017172914A1 (en) | 2016-03-30 | 2017-10-05 | Wisconsin Alumni Research Foundation | Methods and compositions for modulating frataxin expression |
| AU2017281286B2 (en) | 2016-06-20 | 2021-05-20 | Incyte Corporation | Crystalline solid forms of a bet inhibitor |
| EP3555059A1 (en) * | 2016-12-16 | 2019-10-23 | H. Hoffnabb-La Roche Ag | Process for the manufacture of diazepine derivatives |
| WO2018183679A1 (en) | 2017-03-29 | 2018-10-04 | Wisconsin Alumni Research Foundation | Methods and compositions for modulating gene expression |
| WO2020027225A1 (ja) | 2018-07-31 | 2020-02-06 | ファイメクス株式会社 | 複素環化合物 |
| US11548875B2 (en) | 2018-12-12 | 2023-01-10 | University Of Washington | Inhibitor compounds for male contraception |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20060142257A1 (en) * | 2001-01-19 | 2006-06-29 | Eberhard Nieschlag | Male contraceptive formulation comprising norethisterone |
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- 2011-05-16 EP EP11781410.3A patent/EP2571875A4/en not_active Ceased
- 2011-05-16 CN CN201180033583.2A patent/CN103180318B/zh not_active Expired - Fee Related
- 2011-05-16 US US13/698,006 patent/US9301962B2/en not_active Expired - Fee Related
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2015
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Also Published As
| Publication number | Publication date |
|---|---|
| CN103180318A (zh) | 2013-06-26 |
| CA2799381A1 (en) | 2011-11-17 |
| WO2011143657A1 (en) | 2011-11-17 |
| US20130210813A1 (en) | 2013-08-15 |
| JP6022442B2 (ja) | 2016-11-09 |
| EP2571875A1 (en) | 2013-03-27 |
| US20160317547A1 (en) | 2016-11-03 |
| EP2571875A4 (en) | 2013-10-30 |
| JP2013528600A (ja) | 2013-07-11 |
| US9789120B2 (en) | 2017-10-17 |
| US9301962B2 (en) | 2016-04-05 |
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