JP2015529229A5 - - Google Patents
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- Publication number
- JP2015529229A5 JP2015529229A5 JP2015532318A JP2015532318A JP2015529229A5 JP 2015529229 A5 JP2015529229 A5 JP 2015529229A5 JP 2015532318 A JP2015532318 A JP 2015532318A JP 2015532318 A JP2015532318 A JP 2015532318A JP 2015529229 A5 JP2015529229 A5 JP 2015529229A5
- Authority
- JP
- Japan
- Prior art keywords
- atoms
- pharmaceutically acceptable
- tautomer
- stereoisomer
- acceptable salt
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 12
- 150000003839 salts Chemical class 0.000 claims 12
- 239000000203 mixture Substances 0.000 claims 10
- 125000004432 carbon atom Chemical group C* 0.000 claims 7
- -1 benzo-1,3-dioxolyl Chemical group 0.000 claims 6
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 3
- 125000005874 benzothiadiazolyl group Chemical group 0.000 claims 3
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 3
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 3
- 125000001041 indolyl group Chemical group 0.000 claims 3
- 125000005956 isoquinolyl group Chemical group 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- 125000004430 oxygen atom Chemical group O* 0.000 claims 3
- 125000005493 quinolyl group Chemical group 0.000 claims 3
- 125000004434 sulfur atom Chemical group 0.000 claims 3
- 210000004369 blood Anatomy 0.000 claims 2
- 239000008280 blood Substances 0.000 claims 2
- 210000000038 chest Anatomy 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000002541 furyl group Chemical group 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 125000001786 isothiazolyl group Chemical group 0.000 claims 2
- 125000000842 isoxazolyl group Chemical group 0.000 claims 2
- 125000002950 monocyclic group Chemical group 0.000 claims 2
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 2
- 125000002971 oxazolyl group Chemical group 0.000 claims 2
- 210000003800 pharynx Anatomy 0.000 claims 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims 2
- 125000003831 tetrazolyl group Chemical group 0.000 claims 2
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 2
- 125000000335 thiazolyl group Chemical group 0.000 claims 2
- 125000001544 thienyl group Chemical group 0.000 claims 2
- 125000001425 triazolyl group Chemical group 0.000 claims 2
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000001738 Nervous System Trauma Diseases 0.000 claims 1
- 238000006069 Suzuki reaction reaction Methods 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 239000011149 active material Substances 0.000 claims 1
- 125000003354 benzotriazolyl group Chemical group N1N=NC2=C1C=CC=C2* 0.000 claims 1
- 125000002619 bicyclic group Chemical group 0.000 claims 1
- 210000000988 bone and bone Anatomy 0.000 claims 1
- ZADPBFCGQRWHPN-UHFFFAOYSA-N boronic acid Chemical compound OBO ZADPBFCGQRWHPN-UHFFFAOYSA-N 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 210000000621 bronchi Anatomy 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 201000007455 central nervous system cancer Diseases 0.000 claims 1
- 210000003679 cervix uteri Anatomy 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 230000006806 disease prevention Effects 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 210000003238 esophagus Anatomy 0.000 claims 1
- 125000004185 ester group Chemical group 0.000 claims 1
- 210000001508 eye Anatomy 0.000 claims 1
- 210000004392 genitalia Anatomy 0.000 claims 1
- 210000003128 head Anatomy 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 210000000867 larynx Anatomy 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 210000001165 lymph node Anatomy 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 210000000214 mouth Anatomy 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 210000003739 neck Anatomy 0.000 claims 1
- 208000028412 nervous system injury Diseases 0.000 claims 1
- 210000001672 ovary Anatomy 0.000 claims 1
- 210000000496 pancreas Anatomy 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 210000000664 rectum Anatomy 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 210000003491 skin Anatomy 0.000 claims 1
- 210000002784 stomach Anatomy 0.000 claims 1
- 210000001550 testis Anatomy 0.000 claims 1
- 210000001685 thyroid gland Anatomy 0.000 claims 1
- 210000003932 urinary bladder Anatomy 0.000 claims 1
- 210000004291 uterus Anatomy 0.000 claims 1
- 239000003981 vehicle Substances 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP12006668.3 | 2012-09-24 | ||
| EP12006668 | 2012-09-24 | ||
| PCT/EP2013/002606 WO2014044356A1 (en) | 2012-09-24 | 2013-08-30 | Hydropyrrolopyrrole derivatives for use as fatty acid synthase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015529229A JP2015529229A (ja) | 2015-10-05 |
| JP2015529229A5 true JP2015529229A5 (enExample) | 2016-10-20 |
| JP6259460B2 JP6259460B2 (ja) | 2018-01-10 |
Family
ID=47088611
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015532318A Expired - Fee Related JP6259460B2 (ja) | 2012-09-24 | 2013-08-30 | 脂肪酸シンターゼ阻害剤として使用するためのヒドロピロロピロール誘導体 |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US9416133B2 (enExample) |
| EP (1) | EP2897958B1 (enExample) |
| JP (1) | JP6259460B2 (enExample) |
| KR (1) | KR20150061644A (enExample) |
| CN (1) | CN104640866B (enExample) |
| AR (1) | AR092211A1 (enExample) |
| AU (1) | AU2013320636A1 (enExample) |
| BR (1) | BR112015005862A2 (enExample) |
| CA (1) | CA2885673A1 (enExample) |
| ES (1) | ES2608040T3 (enExample) |
| HK (1) | HK1210470A1 (enExample) |
| IL (1) | IL237839A0 (enExample) |
| MX (1) | MX2015003542A (enExample) |
| RU (1) | RU2015115278A (enExample) |
| SG (1) | SG11201502014XA (enExample) |
| WO (1) | WO2014044356A1 (enExample) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2822656B1 (en) | 2012-03-07 | 2016-10-19 | Institute of Cancer Research: Royal Cancer Hospital (The) | 3-aryl-5-substituted-isoquinolin-1-one compounds and their therapeutic use |
| AR095079A1 (es) | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
| EP3587406B1 (en) | 2013-03-13 | 2021-01-27 | Forma Therapeutics, Inc. | 2-hydroxy-1-{4-[(4-phenylphenyl)carbonyl]piperazin-1-yl}ethan-1-one derivatives and related compounds as fatty acid synthase (fasn) inhibitors for the treatment of cancer |
| US9611223B2 (en) | 2013-09-11 | 2017-04-04 | Institute Of Cancer Research: Royal Cancer Hospital (The) | 3-aryl-5-substituted-isoquinolin-1-one compounds and their therapeutic use |
| KR20160087900A (ko) | 2013-11-26 | 2016-07-22 | 에프. 호프만-라 로슈 아게 | 신규한 옥타하이드로-사이클로부타[1,2-c；3,4-c'']다이피롤-2-일 |
| SI3122750T1 (sl) | 2014-03-26 | 2019-12-31 | F. Hoffmann-La Roche Ag | Biciklične spojine kot zaviralci proizvodnje avtotaksina (ATX) in lizofosfatidne kisline (LPA) |
| BR112017027339A2 (pt) | 2015-06-18 | 2018-09-04 | Cephalon, Inc. | derivados de piperidina 1,4-substituída |
| US10919875B2 (en) | 2015-06-18 | 2021-02-16 | 89Bio Ltd | Substituted 4-benzyl and 4-benzoyl piperidine derivatives |
| JP6886967B2 (ja) | 2015-09-04 | 2021-06-16 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | フェノキシメチル誘導体 |
| CN107635995B (zh) | 2015-09-24 | 2022-08-19 | 豪夫迈·罗氏有限公司 | 作为atx抑制剂的二环化合物 |
| RU2018112230A (ru) | 2015-09-24 | 2019-10-30 | Ф. Хоффманн-Ля Рош Аг | Бициклические соединения в качестве ингибиторов atx |
| AU2016328365B2 (en) * | 2015-09-24 | 2020-04-23 | F. Hoffmann-La Roche Ag | New bicyclic compounds as dual ATX/CA inhibitors |
| WO2017156350A1 (en) | 2016-03-09 | 2017-09-14 | K-Gen, Inc. | Methods of cancer treatment |
| WO2018167113A1 (en) | 2017-03-16 | 2018-09-20 | F. Hoffmann-La Roche Ag | New bicyclic compounds as atx inhibitors |
| EP3596059B1 (en) | 2017-03-16 | 2024-04-24 | F. Hoffmann-La Roche AG | Heterocyclic compounds useful as dual atx/ca inhibitors |
| PT3448859T (pt) | 2017-03-20 | 2019-10-25 | Forma Therapeutics Inc | Composições de pirrolopirrole como ativadores de piruvato quinase (pkr). |
| ES2989438T3 (es) | 2018-09-19 | 2024-11-26 | Novo Nordisk Healthcare Ag | Activación de la piruvato cinasa R |
| US12053458B2 (en) | 2018-09-19 | 2024-08-06 | Novo Nordisk Health Care Ag | Treating sickle cell disease with a pyruvate kinase R activating compound |
| TWI767148B (zh) | 2018-10-10 | 2022-06-11 | 美商弗瑪治療公司 | 抑制脂肪酸合成酶(fasn) |
| CN113382633A (zh) | 2018-10-29 | 2021-09-10 | 福马治疗股份有限公司 | (4-(2-氟-4-(1-甲基-1H-苯并[d]咪唑-5-基)苯甲酰基)哌嗪-1-基)(1-羟基环丙基)甲酮的固体形式 |
| CN114615977B (zh) | 2019-09-19 | 2025-01-14 | 诺沃挪第克健康护理股份公司 | 丙酮酸激酶r(pkr)活化组合物 |
| US12128035B2 (en) | 2021-03-19 | 2024-10-29 | Novo Nordisk Health Care Ag | Activating pyruvate kinase R |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0710474A2 (pt) * | 2006-02-15 | 2011-08-16 | Hoffmann La Roche | compostos antivirais hetero bicìclicos |
| US7544698B2 (en) * | 2006-04-07 | 2009-06-09 | Janssen Pharmaceutica, N.V. | Indoles and benzoimidazoles as modulators of the histamine H4 receptor |
| WO2008059214A1 (en) * | 2006-11-13 | 2008-05-22 | Astrazeneca Ab | Bisamlde derivatives and use thereof as fatty acid synthase inhibitors |
| BRPI0808525A2 (pt) * | 2007-03-01 | 2014-08-19 | Janssen Pharmaceutica Nv | Compostos de tetraidroisoquinolina como moduladors do receptor de histamina h3 |
| WO2009002770A1 (en) * | 2007-06-22 | 2008-12-31 | Merck & Co., Inc. | 6.5-pyrrolopiperidine tachykinin receptor antagonists |
| JP5744886B2 (ja) | 2009-10-19 | 2015-07-08 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | シクロペンタンカルボキサミド誘導体、このような化合物を含む薬物及びそれらの使用 |
| WO2011056635A1 (en) | 2009-10-27 | 2011-05-12 | Glaxosmithkline Llc | Benzimidazoles as fatty acid synthase inhibitors |
| US8633183B2 (en) * | 2010-01-26 | 2014-01-21 | Boehringer Ingelheim International Gmbh | 5-alkynyl-pyrimidines |
| US20130237535A1 (en) | 2010-11-08 | 2013-09-12 | Nicholas D. Adams | Fatty acid synthase inhibitors |
| WO2012122391A1 (en) * | 2011-03-08 | 2012-09-13 | 3-V Biosciences, Inc. | Heterocyclic modulators of lipid synthesis |
| WO2013028445A1 (en) * | 2011-08-19 | 2013-02-28 | Glaxosmithkline Llc | Fatty acid synthase inhibitors |
-
2013
- 2013-08-23 AR ARP130102988A patent/AR092211A1/es unknown
- 2013-08-30 RU RU2015115278A patent/RU2015115278A/ru unknown
- 2013-08-30 CA CA 2885673 patent/CA2885673A1/en not_active Abandoned
- 2013-08-30 MX MX2015003542A patent/MX2015003542A/es unknown
- 2013-08-30 HK HK15111265.8A patent/HK1210470A1/xx unknown
- 2013-08-30 US US14/430,630 patent/US9416133B2/en not_active Expired - Fee Related
- 2013-08-30 ES ES13758748.1T patent/ES2608040T3/es active Active
- 2013-08-30 JP JP2015532318A patent/JP6259460B2/ja not_active Expired - Fee Related
- 2013-08-30 CN CN201380049347.9A patent/CN104640866B/zh not_active Expired - Fee Related
- 2013-08-30 KR KR1020157010529A patent/KR20150061644A/ko not_active Ceased
- 2013-08-30 EP EP13758748.1A patent/EP2897958B1/en not_active Not-in-force
- 2013-08-30 AU AU2013320636A patent/AU2013320636A1/en not_active Abandoned
- 2013-08-30 WO PCT/EP2013/002606 patent/WO2014044356A1/en not_active Ceased
- 2013-08-30 SG SG11201502014XA patent/SG11201502014XA/en unknown
- 2013-08-30 BR BR112015005862A patent/BR112015005862A2/pt not_active IP Right Cessation
-
2015
- 2015-03-19 IL IL237839A patent/IL237839A0/en unknown
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