JP2013510859A5 - - Google Patents
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- Publication number
- JP2013510859A5 JP2013510859A5 JP2012538935A JP2012538935A JP2013510859A5 JP 2013510859 A5 JP2013510859 A5 JP 2013510859A5 JP 2012538935 A JP2012538935 A JP 2012538935A JP 2012538935 A JP2012538935 A JP 2012538935A JP 2013510859 A5 JP2013510859 A5 JP 2013510859A5
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- pharmaceutically acceptable
- acceptable salt
- pyrazol
- fluoro
- 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
- -1 chloro, cyano, cyanomethyl Chemical group 0.000 claims 19
- 150000003839 salts Chemical class 0.000 claims 11
- 150000001875 compounds Chemical class 0.000 claims 10
- 125000001153 fluoro group Chemical group F* 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 239000001257 hydrogen Substances 0.000 claims 5
- OKKJLVBELUTLKV-UHFFFAOYSA-N methanol Natural products OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000004849 alkoxymethyl group Chemical group 0.000 claims 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- 125000001607 1,2,3-triazol-1-yl group Chemical group [*]N1N=NC([H])=C1[H] 0.000 claims 1
- 125000003626 1,2,4-triazol-1-yl group Chemical group [*]N1N=C([H])N=C1[H] 0.000 claims 1
- XTVMMUUMUBGOPK-UHFFFAOYSA-N 2-chloro-4,4-difluoro-1'-[[3-methyl-1-[3-(pyrazol-1-ylmethyl)pyridin-2-yl]pyrazol-4-yl]methyl]spiro[5h-thieno[2,3-c]pyran-7,4'-piperidine] Chemical compound C1=C(CN2CCC3(CC2)C=2SC(Cl)=CC=2C(F)(F)CO3)C(C)=NN1C1=NC=CC=C1CN1C=CC=N1 XTVMMUUMUBGOPK-UHFFFAOYSA-N 0.000 claims 1
- TVSCFMXJYNZEER-UHFFFAOYSA-N 7-methoxy-11a-methyl-1,9b,10,11-tetrahydronaphtho[1,2-g]indole Chemical compound C1CC2(C)CC=NC2=C2C=CC3=CC(OC)=CC=C3C21 TVSCFMXJYNZEER-UHFFFAOYSA-N 0.000 claims 1
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical group CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 1
- 208000019695 Migraine disease Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 206010033307 Overweight Diseases 0.000 claims 1
- NKQHBJNRBKHUQR-UHFFFAOYSA-N [2-[4-[(2-chloro-4,4-difluorospiro[5h-thieno[2,3-c]pyran-7,4'-piperidine]-1'-yl)methyl]-3-methylpyrazol-1-yl]pyridin-3-yl]methanol Chemical compound C1=C(CN2CCC3(CC2)C=2SC(Cl)=CC=2C(F)(F)CO3)C(C)=NN1C1=NC=CC=C1CO NKQHBJNRBKHUQR-UHFFFAOYSA-N 0.000 claims 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 125000004859 cyclopropyloxymethyl group Chemical group C1(CC1)OC* 0.000 claims 1
- 125000004284 isoxazol-3-yl group Chemical group [H]C1=C([H])C(*)=NO1 0.000 claims 1
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 claims 1
- 206010027599 migraine Diseases 0.000 claims 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 125000004304 oxazol-5-yl group Chemical group O1C=NC=C1* 0.000 claims 1
- 125000004353 pyrazol-1-yl group Chemical group [H]C1=NN(*)C([H])=C1[H] 0.000 claims 1
- 125000004289 pyrazol-3-yl group Chemical group [H]N1N=C(*)C([H])=C1[H] 0.000 claims 1
- 125000004192 tetrahydrofuran-2-yl group Chemical group [H]C1([H])OC([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 0 *C(*)(COC12CCN(Cc3c[n](-c4c(*)cccn4)nc3*)CC1)c1c2[s]c(*)c1 Chemical compound *C(*)(COC12CCN(Cc3c[n](-c4c(*)cccn4)nc3*)CC1)c1c2[s]c(*)c1 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09382246.8 | 2009-11-16 | ||
| EP09382246 | 2009-11-16 | ||
| US29862910P | 2010-01-27 | 2010-01-27 | |
| US61/298,629 | 2010-01-27 | ||
| PCT/US2010/056180 WO2011060035A1 (en) | 2009-11-16 | 2010-11-10 | Spiropiperidine compounds as orl-1 receptor antagonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013510859A JP2013510859A (ja) | 2013-03-28 |
| JP2013510859A5 true JP2013510859A5 (enExample) | 2013-11-14 |
| JP5680101B2 JP5680101B2 (ja) | 2015-03-04 |
Family
ID=41728051
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012538935A Expired - Fee Related JP5680101B2 (ja) | 2009-11-16 | 2010-11-10 | Ｏｒｌ−１受容体アンタゴニストとしてのスピロピペリジン化合物 |
Country Status (34)
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104193761B (zh) | 2009-12-04 | 2017-10-17 | 桑诺维恩药品公司 | 多环化合物及其使用方法 |
| JP2013540145A (ja) * | 2010-10-21 | 2013-10-31 | ウニベルシテート デス ザールランデス | コルチゾール依存性疾患の治療用の選択的ｃｙｐ１１ｂ１阻害剤 |
| TWI582096B (zh) * | 2011-12-06 | 2017-05-11 | 美國禮來大藥廠 | 用於酒精依賴及濫用處理之４',５'－二氫螺［哌啶－４,７'－噻吩并[２，３－c]哌喃］化合物 |
| TW201416370A (zh) | 2012-07-31 | 2014-05-01 | Lilly Co Eli | 用於治療焦慮之ｏｒｌ－１受體拮抗劑 |
| DK2903440T3 (en) | 2012-10-02 | 2017-12-11 | Bayer Cropscience Ag | THETEROCYCLIC COMPOUNDS AS PESTICIDES |
| US10154988B2 (en) | 2012-11-14 | 2018-12-18 | The Johns Hopkins University | Methods and compositions for treating schizophrenia |
| TW201607923A (zh) | 2014-07-15 | 2016-03-01 | 歌林達有限公司 | 被取代之氮螺環（４．５）癸烷衍生物 |
| JO3638B1 (ar) * | 2015-09-09 | 2020-08-27 | Lilly Co Eli | مركبات مفيدة في تثبيط ror - جاما- t |
| BR112019001407A2 (pt) | 2016-07-29 | 2019-07-09 | Sunovion Pharmaceuticals Inc. | compostos e composições e usos dos mesmos |
| SG10202100724UA (en) | 2016-07-29 | 2021-03-30 | Sunovion Pharmaceuticals Inc | Compounds and compositions and uses thereof |
| EP3582815A1 (en) | 2017-02-16 | 2019-12-25 | Sunovion Pharmaceuticals Inc. | Methods of treating schizophrenia |
| LT3589638T (lt) | 2017-03-02 | 2021-06-10 | Eli Lilly And Company | Junginiai, naudingi ror-gama-t slopinimui |
| DK3589637T3 (da) * | 2017-03-02 | 2021-06-14 | Lilly Co Eli | Forbindelser, der er anvendelige til inhibering af ROR-GAMMA-T |
| MX2020000523A (es) | 2017-08-02 | 2020-08-20 | Sunovion Pharmaceuticals Inc | Compuestos de isocromano y usos de los mismos. |
| SG11202007823PA (en) | 2018-02-16 | 2020-09-29 | Sunovion Pharmaceuticals Inc | Salts, crystal forms, and production methods thereof |
| LT3897833T (lt) | 2018-12-17 | 2026-04-27 | Vertex Pharmaceuticals Incorporated | Apol1 inhibitoriai ir jų panaudojimo būdai |
| JP7703449B2 (ja) | 2019-03-14 | 2025-07-07 | スミトモ・ファーマ・アメリカ・インコーポレイテッド | イソクロマニル化合物の塩およびその結晶体、ならびにそれらの製造方法、治療用途および医薬組成物 |
| KR20230003503A (ko) | 2020-04-14 | 2023-01-06 | 선오비온 파마슈티컬스 인코포레이티드 | 신경학적 및 정신의학적 장애의 치료를 위한 (S)-(4,5-디히드로-7H-티에노[2,3-c]피란-7-일)-N-메틸메탄아민 |
| CN115867543A (zh) | 2020-06-12 | 2023-03-28 | 弗特克斯药品有限公司 | Apol1抑制剂的固体形式及其使用方法 |
| BR112023003423A2 (pt) | 2020-08-26 | 2023-03-21 | Vertex Pharma | Inibidores de apol1 e métodos de uso destes |
| CN119343353A (zh) * | 2022-02-08 | 2025-01-21 | 弗特克斯药品有限公司 | 作为APOL1抑制剂的2-甲基-4',5'-二氢螺[哌啶-4,7'-噻吩并[2,3-c]吡喃]衍生物和其使用方法 |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL96507A0 (en) | 1989-12-08 | 1991-08-16 | Merck & Co Inc | Nitrogen-containing spirocycles and pharmaceutical compositions containing them |
| JP3989247B2 (ja) | 1999-12-06 | 2007-10-10 | ユーロ−セルティーク エス．エイ． | ノシセプチン受容体親和性を有するトリアゾスピロ化合物 |
| CN1516584A (zh) | 2001-04-18 | 2004-07-28 | ŷ�����ǹɷ�����˾ | 螺吡唑化合物 |
| WO2002088089A1 (en) | 2001-04-19 | 2002-11-07 | Banyu Pharmaceutical Co., Ltd. | Spiropiperidine derivatives, nociceptin receptor antagonists containing the same as the active ingredient and medicinal compositions |
| CA2454785C (en) | 2001-07-23 | 2010-09-07 | Banyu Pharmaceutical Co., Ltd. | 4-oxoimidazolidine-2-spiropiperidine derivatives |
| EP1470126A1 (en) * | 2002-01-28 | 2004-10-27 | Pfizer Inc. | N-substituted spiropiperidine compounds as ligands for orl-1 receptor |
| WO2003095427A1 (en) | 2002-05-10 | 2003-11-20 | Taisho Pharmaceutical Co.,Ltd. | Spiro-ring compound |
| US6995168B2 (en) | 2002-05-31 | 2006-02-07 | Euro-Celtique S.A. | Triazaspiro compounds useful for treating or preventing pain |
| AU2003268512A1 (en) | 2002-09-09 | 2004-03-29 | Janssen Pharmaceutica N.V. | Hydroxy alkyl substituted 1,3,8-triazaspiro[4.5]decan-4-one derivatives useful for the treatment of ORL-1 receptor mediated disorders |
| WO2005016913A1 (en) * | 2003-08-19 | 2005-02-24 | Pfizer Japan, Inc. | Tetrahydroisoquinoline or isochroman compounds as orl-1 receptor ligands for the treatment of pain and cns disorders |
| DE10360792A1 (de) * | 2003-12-23 | 2005-07-28 | Grünenthal GmbH | Spirocyclische Cyclohexan-Derivate |
| WO2005092858A2 (en) * | 2004-03-29 | 2005-10-06 | Pfizer Japan Inc. | Alpha aryl or heteroaryl methyl beta piperidino propanamide compounds as orl1-receptor antagonist |
| DE102004039382A1 (de) * | 2004-08-13 | 2006-02-23 | Grünenthal GmbH | Spirocyclische Cyclohexan-Derivate |
| EP2020414A1 (en) | 2007-06-20 | 2009-02-04 | Laboratorios del Dr. Esteve S.A. | spiro[piperidine-4,4'-thieno[3,2-c]pyran] derivatives and related compounds as inhibitors of the sigma receptor for the treatment of psychosis |
| CL2009000731A1 (es) | 2008-03-27 | 2009-05-15 | Gruenenthal Gmbh | Compuestos derivados de ciclohexano espirociclicos sustituidos, composicion farmaceutica que contiene a dicho compuesto y su uso como moduladores del receptor de opioides µ y el receptor orl-1 para tratar el dolor, ansiedad, depresion, epilepsia, alzheimer, abuso de alcohol, hipertension, anorexia, obesidad y diarrea. |
-
2010
- 2010-10-11 UA UAA201205367A patent/UA107943C2/uk unknown
- 2010-11-02 AR ARP100104035A patent/AR078863A1/es active IP Right Grant
- 2010-11-03 JO JO2010386A patent/JO2887B1/en active
- 2010-11-05 TW TW099138241A patent/TWI465453B/zh not_active IP Right Cessation
- 2010-11-10 PT PT107824823T patent/PT2501703E/pt unknown
- 2010-11-10 MX MX2012005691A patent/MX2012005691A/es active IP Right Grant
- 2010-11-10 DK DK10782482.3T patent/DK2501703T3/da active
- 2010-11-10 NZ NZ600006A patent/NZ600006A/en not_active IP Right Cessation
- 2010-11-10 PL PL10782482T patent/PL2501703T3/pl unknown
- 2010-11-10 EA EA201290352A patent/EA020848B1/ru not_active IP Right Cessation
- 2010-11-10 RS RS20130485A patent/RS53018B/sr unknown
- 2010-11-10 HR HRP20130967AT patent/HRP20130967T1/hr unknown
- 2010-11-10 AU AU2010319581A patent/AU2010319581C1/en not_active Ceased
- 2010-11-10 US US12/943,187 patent/US8232289B2/en not_active Expired - Fee Related
- 2010-11-10 CA CA2796161A patent/CA2796161C/en not_active Expired - Fee Related
- 2010-11-10 SI SI201030388T patent/SI2501703T1/sl unknown
- 2010-11-10 PE PE2012000659A patent/PE20121430A1/es active IP Right Grant
- 2010-11-10 ME MEP-2013-118A patent/ME01537B/me unknown
- 2010-11-10 WO PCT/US2010/056180 patent/WO2011060035A1/en not_active Ceased
- 2010-11-10 EP EP10782482.3A patent/EP2501703B1/en active Active
- 2010-11-10 MY MYPI2012002117A patent/MY160665A/en unknown
- 2010-11-10 JP JP2012538935A patent/JP5680101B2/ja not_active Expired - Fee Related
- 2010-11-10 CN CN201080051850.4A patent/CN102612520B/zh not_active Expired - Fee Related
- 2010-11-10 ES ES10782482T patent/ES2435814T3/es active Active
- 2010-11-10 PH PH1/2012/500969A patent/PH12012500969A1/en unknown
- 2010-11-10 KR KR1020127012498A patent/KR101363830B1/ko not_active Expired - Fee Related
-
2012
- 2012-04-23 IL IL219370A patent/IL219370A/en not_active IP Right Cessation
- 2012-04-23 ZA ZA2012/02967A patent/ZA201202967B/en unknown
- 2012-05-04 CO CO12073055A patent/CO6541545A2/es active IP Right Grant
- 2012-05-11 HN HN2012001011A patent/HN2012001011A/es unknown
- 2012-05-11 DO DO2012000135A patent/DOP2012000135A/es unknown
- 2012-05-14 MA MA34869A patent/MA33751B1/fr unknown
- 2012-05-16 EC ECSP12011902 patent/ECSP12011902A/es unknown
-
2013
- 2013-02-26 CR CR20130087A patent/CR20130087A/es unknown
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