JP2014520886A5 - - Google Patents
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- JP2014520886A5 JP2014520886A5 JP2014521705A JP2014521705A JP2014520886A5 JP 2014520886 A5 JP2014520886 A5 JP 2014520886A5 JP 2014521705 A JP2014521705 A JP 2014521705A JP 2014521705 A JP2014521705 A JP 2014521705A JP 2014520886 A5 JP2014520886 A5 JP 2014520886A5
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- Prior art keywords
- het
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- physiologically acceptable
- compound according
- hal
- 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.)
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- 150000003839 salts Chemical class 0.000 claims 6
- 239000011780 sodium chloride Substances 0.000 claims 6
- 125000004432 carbon atoms Chemical group C* 0.000 claims 5
- 150000001875 compounds Chemical class 0.000 claims 5
- 239000003814 drug Substances 0.000 claims 4
- 102000008175 FSH Receptors Human genes 0.000 claims 3
- 108010060374 FSH Receptors Proteins 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- 208000000509 Infertility Diseases 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- 210000004681 Ovum Anatomy 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 125000004435 hydrogen atoms Chemical group [H]* 0.000 claims 2
- 238000000338 in vitro Methods 0.000 claims 2
- 230000036512 infertility Effects 0.000 claims 2
- 231100000535 infertility Toxicity 0.000 claims 2
- 230000000051 modifying Effects 0.000 claims 2
- 125000004434 sulfur atoms Chemical group 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 230000000240 adjuvant Effects 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 229940079593 drugs Drugs 0.000 claims 1
- 235000013601 eggs Nutrition 0.000 claims 1
- 230000004720 fertilization Effects 0.000 claims 1
- 125000002911 monocyclic heterocycle group Chemical group 0.000 claims 1
- 125000004433 nitrogen atoms Chemical group N* 0.000 claims 1
- 125000004430 oxygen atoms Chemical group O* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 230000003449 preventive Effects 0.000 claims 1
- 230000001225 therapeutic Effects 0.000 claims 1
- 0 CCCS(CCCc(cc1)c(*C(c2ccc[o]2)=O)cc1C(CCC*(C(CC1)=O)C1=O)=O)c1ccccc1C Chemical compound CCCS(CCCc(cc1)c(*C(c2ccc[o]2)=O)cc1C(CCC*(C(CC1)=O)C1=O)=O)c1ccccc1C 0.000 description 1
Claims (8)
- 下記部分式（Ｉ−Ｂ）：
Ｙは、Ｈ又はＡを示し；
Ａは、１〜６個のＣ原子を有する枝なし又は分枝アルキルを示し、ここで１〜４個のＨ原子は互いに独立して、Ｈａｌ及び／又はＯＨにより置換され得；
Ｃｙｃは、３〜６個のＣ原子を有するシクロアルキルを示し、ここで１〜４個のＨ原子はＯＨにより置換され得；
Ａｒは、Ａ、Ｈａｌ、ＯＹ、ＣＯＮＨ2、−（ＣＨ2）n−ＮＡ2，ＳＯ2ＮＨ2及びＨｅｔ2の群から選択される少なくとも１つの置換基により一又は二置換され得る、６〜８個のＣ原子を有する芳香族単環式炭素環を示し；
Ｈｅｔ1は、Ｈａｌ、Ａ、 Ｃｙｃ及び−(ＣＨ2)n−ＮＡ2の群から選択される少なくとも１つの置換基により一又は二置換され得る、１〜６個のＣ原子及び１〜３個のＮ、Ｏ及び／又はＳ原子を有する、不飽和又は芳香族単環式複素環を示し；
Ｈｅｔ2は、テトラジルを示し；
Ｈｅｔ3は、＝Ｏ、Ａ及びＯＹの群から選択される少なくとも１つの置換基により一、二又は三置換され得る、３〜６個のＣ原子及び１〜３個のＮ、Ｏ及び／又はＳ原子を有する、飽和単環式複素環を示し；
Ｈａｌは、Ｆ、Ｃｌ又はＢｒを示し；そして
ｎは、０、１、２、又は３を示す］を有する化合物、及び／又は生理学的に許容できるその塩。 - 下記式：
- 少なくとも１つの請求項１又は２に記載の化合物及び／又は生理学的に許容できるその塩を含んで成る薬剤。
- 活性成分として、少なくとも１つの請求項１又は２に記載の化合物及び／又は生理学的に許容できるその塩、及び経口投与のための医薬的耐容性のアジュバント、並びに任意には、少なくとも別の活性医薬剤を含んでなる医薬組成物。
- 不妊障害の予防又は治療処置及び／又はモニターリングにおける使用のための請求項３に記載の薬剤。
- 不妊障害の治療方法であって、少なくとも１つの請求項１又は２に記載の化合物及び／又は生理学的に許容できるその塩を、そのような治療の必要なヒト以外の哺乳類に投与する方法。
- 下記段階：
（ａ）請求項６に記載の方法に従ってヒト以外の哺乳類を処理する段階、
（ｂ）前記哺乳類から卵子を採取する段階、
（ｃ）前記卵子を受精する段階、及び
（ｄ）前記受精された卵子を、ヒト以外の宿主哺乳類中に移植する段階、
を含んで成るインビトロ受精方法。 - ＦＳＨ受容体の調節方法であって、ＦＳＨ受容体を発現する系と、少なくとも１つの請求項１又は２に記載の化合物及び／又は生理学的に許容できるその塩とを、ＦＳＨの存在下で、前記ＦＳＨ受容体が調節されるような条件下で接触せしめるインビトロ方法。
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161508861P | 2011-07-18 | 2011-07-18 | |
| US61/508,861 | 2011-07-18 | ||
| US201161526342P | 2011-08-23 | 2011-08-23 | |
| US61/526,342 | 2011-08-23 | ||
| PCT/US2012/047038 WO2013012848A1 (en) | 2011-07-18 | 2012-07-17 | Benzamides |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017043934A Division JP6254730B2 (ja) | 2011-07-18 | 2017-03-08 | ベンズアミド類 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014520886A JP2014520886A (ja) | 2014-08-25 |
| JP2014520886A5 true JP2014520886A5 (ja) | 2017-06-15 |
| JP6162694B2 JP6162694B2 (ja) | 2017-07-12 |
Family
ID=46551951
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014521705A Active JP6162694B2 (ja) | 2011-07-18 | 2012-07-17 | ベンズアミド類 |
| JP2017043934A Active JP6254730B2 (ja) | 2011-07-18 | 2017-03-08 | ベンズアミド類 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017043934A Active JP6254730B2 (ja) | 2011-07-18 | 2017-03-08 | ベンズアミド類 |
Country Status (10)
| Country | Link |
|---|---|
| US (3) | US9181226B2 (ja) |
| EP (2) | EP2734517B1 (ja) |
| JP (2) | JP6162694B2 (ja) |
| CN (1) | CN103702993B (ja) |
| AU (2) | AU2012284184B2 (ja) |
| CA (1) | CA2834199C (ja) |
| ES (2) | ES2649995T3 (ja) |
| HK (1) | HK1195557A1 (ja) |
| IL (1) | IL230463A (ja) |
| WO (1) | WO2013012848A1 (ja) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
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| EP2734517B1 (en) * | 2011-07-18 | 2017-08-30 | Merck Patent GmbH | Benzamides |
| WO2013106409A1 (en) * | 2012-01-10 | 2013-07-18 | Merck Patent Gmbh | Benzamide derivatives as modulators of the follicle stimulating hormone |
| CA2914178C (en) | 2013-01-07 | 2023-06-13 | University Of Southern California | Deoxyuridine triphosphatase inhibitors |
| SG11201505999VA (en) | 2013-03-11 | 2015-08-28 | Merck Patent Gmbh | 6-[4-(1 h-imidazol-2-yl)piperidin-1 -yl]pyrimidin-4-amine derivatives as modulators of kinase activity |
| CN104717415B (zh) * | 2013-12-12 | 2019-03-01 | 华为技术有限公司 | 一种摄像装置 |
| WO2015196335A1 (en) | 2014-06-23 | 2015-12-30 | Tocopherx, Inc. | Pyrazole compounds as modulators of fshr and uses thereof |
| WO2016087878A1 (en) * | 2014-12-05 | 2016-06-09 | Pulmocide Limited | Antimycotic compound |
| US10577321B2 (en) | 2015-07-08 | 2020-03-03 | University Of Southern California | Deoxyuridine triphosphatase inhibitors |
| US10570100B2 (en) | 2015-07-08 | 2020-02-25 | University Of Southern California | Deoxyuridine triphosphatase inhibitors containing amino sulfonyl linkage |
| WO2017006283A1 (en) | 2015-07-08 | 2017-01-12 | Cv6 Therapeutics (Ni) Limited | Deoxyuridine triphosphatase inhibitors containing cyclopropano linkage |
| EP3319939A1 (en) | 2015-07-08 | 2018-05-16 | CV6 Therapeutics (NI) Limited | Hydantoin containing deoxyuridine triphosphatase inhibitors |
| MX2018004814A (es) | 2015-10-22 | 2019-04-01 | Procter & Gamble | Sintesis de derivados de ciclohexano carboxamida utiles como agentes de percepcion en productos de consumo. |
| US11168059B2 (en) | 2016-11-23 | 2021-11-09 | Cv6 Therapeutics (Ni) Limited | Amino sulfonyl compounds |
| WO2018098208A1 (en) | 2016-11-23 | 2018-05-31 | Cv6 Therapeutics (Ni) Limited | Nitrogen ring linked deoxyuridine triphosphatase inhibitors |
| US11174271B2 (en) | 2016-11-23 | 2021-11-16 | Cv6 Therapeutics (Ni) Limited | 6-membered uracil isosteres |
| WO2018128720A1 (en) | 2017-01-05 | 2018-07-12 | Cv6 Therapeutics (Ni) Limited | Uracil containing compounds |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH07258224A (ja) * | 1994-03-24 | 1995-10-09 | Dai Ichi Seiyaku Co Ltd | 二環性化合物 |
| JPH0959236A (ja) * | 1995-08-23 | 1997-03-04 | Dai Ichi Seiyaku Co Ltd | ベンズアミド化合物 |
| WO1997029079A1 (fr) * | 1996-02-06 | 1997-08-14 | Japan Tobacco Inc. | Composes chimiques et utilisation pharmaceutique |
| FR2765221B1 (fr) * | 1997-06-25 | 1999-07-30 | Synthelabo | Derives de 4-[(1h-imidazol-4-yl)piperidin-1-yl]anilide, leur preparation et leur application en therapeutique |
| AR013693A1 (es) * | 1997-10-23 | 2001-01-10 | Uriach & Cia Sa J | Nuevas piperidinas y piperazinas como inhibidores de la agregacion plaquetaria |
| CA2339018A1 (en) | 1998-08-07 | 2000-02-17 | Applied Research Systems Ars Holding N.V. | Fsh mimetics for the treatment of infertility |
| US7101878B1 (en) * | 1998-08-20 | 2006-09-05 | Agouron Pharmaceuticals, Inc. | Non-peptide GNRH agents, methods and intermediates for their preparation |
| MXPA01009307A (es) * | 1999-03-17 | 2002-07-30 | Astrazeneca Ab | Derivados de amida. |
| SE9904652D0 (sv) * | 1999-12-17 | 1999-12-17 | Astra Pharma Prod | Novel Compounds |
| JP2004505051A (ja) | 2000-07-27 | 2004-02-19 | スミスクライン ビーチャム コーポレーション | 卵胞刺激ホルモン活性のアゴニスト |
| US20040010033A1 (en) * | 2001-02-20 | 2004-01-15 | Pfizer Inc. | Non-peptide GnRH agents, methods and intermediates for their preparation |
| SE0101387D0 (sv) * | 2001-04-20 | 2001-04-20 | Astrazeneca Ab | Novel compounds |
| AU2003202115A1 (en) * | 2002-02-12 | 2003-09-04 | Pfizer Inc. | Non-peptide compounds affecting the action of gonadotropin-releasing hormone (gnrh) |
| JP2005538064A (ja) * | 2002-06-13 | 2005-12-15 | ファイザー・インク | 非ペプチドＧｎＲＨ剤、医薬組成物、およびそれらの使用方法 |
| US7754722B2 (en) * | 2002-09-20 | 2010-07-13 | Merck Serono Sa | Piperazine derivatives and methods of use |
| SE0203070D0 (en) * | 2002-10-16 | 2002-10-16 | Astrazeneca Ab | Novel compounds |
| FR2851563B1 (fr) * | 2003-02-26 | 2005-04-22 | Sod Conseils Rech Applic | Nouveaux derives de benzimidazole et d'imidazo-pyridine et leur utilisation en tant que medicament |
| US7700583B2 (en) * | 2003-04-11 | 2010-04-20 | High Point Pharmaceuticals, Llc | 11β-hydroxysteroid dehydrogenase type 1 active compounds |
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| TWI461426B (zh) | 2009-05-27 | 2014-11-21 | Merck Sharp & Dohme | （二氫）咪唑並異〔５，１－ａ〕喹啉類 |
| ES2796774T3 (es) * | 2011-07-01 | 2020-11-30 | Merck Patent Gmbh | Dihidropirazoles, composiciones farmacéuticas de los mismos y su uso para el tratamiento de trastornos de fertilidad |
| EP2734517B1 (en) * | 2011-07-18 | 2017-08-30 | Merck Patent GmbH | Benzamides |
| WO2013106409A1 (en) * | 2012-01-10 | 2013-07-18 | Merck Patent Gmbh | Benzamide derivatives as modulators of the follicle stimulating hormone |
-
2012
- 2012-07-17 EP EP12738368.5A patent/EP2734517B1/en active Active
- 2012-07-17 EP EP17187673.3A patent/EP3263568B1/en active Active
- 2012-07-17 WO PCT/US2012/047038 patent/WO2013012848A1/en active Application Filing
- 2012-07-17 US US13/551,072 patent/US9181226B2/en active Active
- 2012-07-17 ES ES12738368.5T patent/ES2649995T3/es active Active
- 2012-07-17 AU AU2012284184A patent/AU2012284184B2/en active Active
- 2012-07-17 JP JP2014521705A patent/JP6162694B2/ja active Active
- 2012-07-17 CN CN201280035159.6A patent/CN103702993B/zh active Active
- 2012-07-17 ES ES17187673T patent/ES2899000T3/es active Active
- 2012-07-17 CA CA2834199A patent/CA2834199C/en active Active
-
2014
- 2014-01-15 IL IL230463A patent/IL230463A/en active IP Right Grant
- 2014-09-04 HK HK14109011.0A patent/HK1195557A1/zh not_active IP Right Cessation
-
2015
- 2015-09-24 US US14/863,865 patent/US9498475B2/en active Active
-
2016
- 2016-10-03 US US15/283,938 patent/US9938262B2/en active Active
-
2017
- 2017-02-14 AU AU2017200985A patent/AU2017200985A1/en not_active Abandoned
- 2017-03-08 JP JP2017043934A patent/JP6254730B2/ja active Active
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