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
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- -1 chloro, cyano, cyanomethyl Chemical group 0.000 claims 18
- 150000003839 salts Chemical class 0.000 claims 11
- 239000011780 sodium chloride Substances 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
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- OKKJLVBELUTLKV-UHFFFAOYSA-N methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 4
- 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
- 206010027599 Migraine Diseases 0.000 claims 1
- 208000008085 Migraine Disorders 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
- 125000000217 alkyl group Chemical group 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
- KFZMGEQAYNKOFK-UHFFFAOYSA-N iso-propanol Chemical group CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 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
- RHICUTFVLMIIRN-UHFFFAOYSA-N methyl carbamate Chemical group [CH2]OC(N)=O RHICUTFVLMIIRN-UHFFFAOYSA-N 0.000 claims 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 235000020825 overweight 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
Claims (11)
- 下記式の化合物:
R1は、フルオロまたはクロロであり、
R2aおよびR2bは、各々水素であるか、または各々フルオロであり、
R3は、水素、メチル、ヒドロキシメチル、または(C1−C3)アルコキシメチルであり、
R4は、フルオロ、クロロ、シアノ、シアノメチル、(C1−C3)アルキル、シクロプロピル、ヒドロキシメチル、メトキシ、シクロプロピルメトキシ、アミノカルボニルメトキシ、(C1−C3)アルコキシメチル、シクロプロピルオキシメチル、シクロプロピルメトキシメチル、1−ヒドロキシ−1−メチルエチル、アミノカルボニルオキシメチル、メチルアミノカルボニルオキシメチル、ジメチルアミノカルボニルオキシメチル、アミノカルボニル、アミノカルボニルメチル、−CH2−NR5R6、ヒドロキシイミン、メトキシイミン、モルホリン−4−イル、モルホリン−4−イルメチル、Ar1、−CH2Ar1、テトラヒドロフラン−2−イル、3−オキソモルホリン−4−イルメチル、2−オキソピロリジン−1−イルメチル、および2−オキソピペリジン−1−イルメチルからなる群より選択され、
R5は、水素、C1−C3アルキル、シアノメチル、−C(O)CH3、またはアミノカルボニルメチルであり、
R6は、水素またはメチルであり、
Ar1は、イミジゾール−1−イル、イミジゾール−2−イル、2−メチルイミジゾール−1−イル、ピラゾール−1−イル、1,2,3−トリアゾール−1−イル、1,2,3−トリアゾール−2−イル、1,2,4−トリアゾール−1−イル、イソオキサゾール−3−イル、オキサゾール−5−イル、および3−メチル−1,2,4−オキサジアゾール−5−イルからなる群より選択される部分である)
またはその医薬的に許容可能な塩。 - R1がクロロである、請求項1に記載の化合物、またはその医薬的に許容可能な塩。
- R2aおよびR2bが各々フルオロである、請求項1または2に記載の化合物、またはその医薬的に許容可能な塩。
- R1がフルオロであり、R2aおよびR2bが各々水素である、請求項1に記載の化合物、またはその医薬的に許容可能な塩。
- R3がメチルである、請求項1〜4のいずれか一項に記載の化合物、またはその医薬的に許容可能な塩。
- R4がフルオロ、ヒドロキシメチル、メトキシメチル、またはピラゾール−1−イルメチルである、請求項1〜5のいずれか一項に記載の化合物、またはその医薬的に許容可能な塩。
- [2−[4−[(2−クロロ−4,4−ジフルオロ−スピロ[5H−チエノ[2,3−c]ピラン−7,4’−ピペリジン]−1’−イル)メチル]−3−メチル−ピラゾール−1−イル]−3−ピリジル]メタノール、
2−クロロ−4,4−ジフルオロ−1’−[[3−メチル−1−[3−(ピラゾール−1−イルメチル)−2−ピリジル]ピラゾール−4−イル]メチル]スピロ[5H−チエノ[2,3−c]ピラン−7,4’−ピペリジン]、または
[4−[(2−クロロ−4,4−ジフルオロ−スピロ[5H−チエノ[2,3−c]ピラン−7,4’―ピペリジン]−1’−イル)メチル]−1−(3−フルオロ−2−ピリジル)ピラゾール−3−イル]メタノール
である、請求項1に記載の化合物、またはその医薬的に許容可能な塩。 - [2−[4−[(2−クロロ−4,4−ジフルオロ−スピロ[5H−チエノ[2,3−c]ピラン−7,4’−ピペリジン]−1’−イル)メチル]−3−メチル−ピラゾール−1−イル]−3−ピリジル]メタノールである、請求項1に記載の化合物、またはその医薬的に許容可能な塩。
- 請求項1〜8のいずれか一項に記載の化合物、またはその医薬的に許容可能な塩を含む、肥満または過体重を治療するための医薬組成物。
- 請求項1〜8のいずれか一項に記載の化合物、またはその医薬的に許容可能な塩を含む、片頭痛を治療するための医薬組成物。
- 請求項1〜8のいずれか一項に記載の化合物、またはその医薬的に許容可能な塩を含む、鬱病を治療するための医薬組成物。
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 (ja) | 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)
Country | Link |
---|---|
US (1) | US8232289B2 (ja) |
EP (1) | EP2501703B1 (ja) |
JP (1) | JP5680101B2 (ja) |
KR (1) | KR101363830B1 (ja) |
CN (1) | CN102612520B (ja) |
AR (1) | AR078863A1 (ja) |
AU (1) | AU2010319581C1 (ja) |
CA (1) | CA2796161C (ja) |
CO (1) | CO6541545A2 (ja) |
CR (1) | CR20130087A (ja) |
DK (1) | DK2501703T3 (ja) |
DO (1) | DOP2012000135A (ja) |
EA (1) | EA020848B1 (ja) |
EC (1) | ECSP12011902A (ja) |
ES (1) | ES2435814T3 (ja) |
HK (1) | HK1169988A1 (ja) |
HN (1) | HN2012001011A (ja) |
HR (1) | HRP20130967T1 (ja) |
IL (1) | IL219370A (ja) |
JO (1) | JO2887B1 (ja) |
MA (1) | MA33751B1 (ja) |
ME (1) | ME01537B (ja) |
MX (1) | MX2012005691A (ja) |
MY (1) | MY160665A (ja) |
NZ (1) | NZ600006A (ja) |
PE (1) | PE20121430A1 (ja) |
PL (1) | PL2501703T3 (ja) |
PT (1) | PT2501703E (ja) |
RS (1) | RS53018B (ja) |
SI (1) | SI2501703T1 (ja) |
TW (1) | TWI465453B (ja) |
UA (1) | UA107943C2 (ja) |
WO (1) | WO2011060035A1 (ja) |
ZA (1) | ZA201202967B (ja) |
Families Citing this family (20)
Publication number | Priority date | Publication date | Assignee | Title |
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KR102074089B1 (ko) | 2009-12-04 | 2020-02-05 | 선오비온 파마슈티컬스 인코포레이티드 | 다환형 화합물 및 이의 사용 방법 |
US9394290B2 (en) * | 2010-10-21 | 2016-07-19 | Universitaet Des Saarlandes Campus Saarbruecken | Selective CYP11B1 inhibitors for the treatment of cortisol dependent diseases |
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 |
AU2013326600B2 (en) | 2012-10-02 | 2017-03-30 | Bayer Cropscience Ag | Heterocyclic compounds as pesticides |
EP2919788A4 (en) | 2012-11-14 | 2016-05-25 | Univ Johns Hopkins | METHODS AND COMPOSITIONS FOR THE TREATMENT OF 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 |
EA201990400A1 (ru) | 2016-07-29 | 2019-07-31 | Суновион Фармасьютикалз, Инк. | Соединения и композиции и их применение |
MA45795A (fr) | 2016-07-29 | 2019-06-05 | Sunovion Pharmaceuticals Inc | Composés et compositions, et utilisations associées |
KR102605854B1 (ko) | 2017-02-16 | 2023-11-23 | 선오비온 파마슈티컬스 인코포레이티드 | 조현병의 치료방법 |
DK3589638T3 (da) | 2017-03-02 | 2021-06-07 | Lilly Co Eli | Forbindelser, der er anvendelige til inhibering af ROR-Gamma-T |
SI3589637T1 (sl) * | 2017-03-02 | 2021-08-31 | Eli Lilly And Company | Spojine uporabne pri inhibiciji ROR-GAMMA-T |
EP3661929B1 (en) | 2017-08-02 | 2021-07-14 | Sunovion Pharmaceuticals Inc. | Isochroman compounds and uses thereof |
MX2020008537A (es) | 2018-02-16 | 2021-01-08 | Sunovion Pharmaceuticals Inc | Sales, formas cristalinas y metodos de produccion de las mismas. |
SG11202105769XA (en) | 2018-12-17 | 2021-07-29 | Vertex Pharma | Inhibitors of apol1 and methods of using same |
US11136304B2 (en) | 2019-03-14 | 2021-10-05 | Sunovion Pharmaceuticals Inc. | Salts of a heterocyclic compound and crystalline forms, processes for preparing, therapeutic uses, and pharmaceutical compositions thereof |
CN115734785A (zh) | 2020-04-14 | 2023-03-03 | 桑诺维恩药品公司 | (S)-(4,5-二氢-7H-噻吩并[2,3-c]吡喃-7-基)-N-甲基甲胺用于治疗神经和精神方面的病症 |
MX2023002269A (es) | 2020-08-26 | 2023-05-16 | Vertex Pharma | Inhibidores de apol1 y metodos para usar los mismos. |
AU2023218994A1 (en) * | 2022-02-08 | 2024-08-22 | Vertex Pharmaceuticals Incorporated | 2-methyl-4',5'-dihydrospiro[piperidine-4,7'-thieno[2,3-c]pyran] derivatives as inhibitors of apol1 and methods of using same |
Family Cites Families (15)
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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 |
RU2299883C2 (ru) | 2001-04-18 | 2007-05-27 | Эро-Селтик, С.А. | Соединения спиропиразола, содержащая их фармацевтическая композиция, способ модуляции опиоидного рецептора и способ лечения с применением таких соединений |
WO2002088089A1 (fr) | 2001-04-19 | 2002-11-07 | Banyu Pharmaceutical Co., Ltd. | Derives de spiropiperidine, antagonistes du recepteur de nociceptine les contenant en tant qu'ingredient actif et compositions medicinales |
US7192964B2 (en) | 2001-07-23 | 2007-03-20 | 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 (fr) | 2002-05-10 | 2003-11-20 | Taisho Pharmaceutical Co.,Ltd. | Compose a noyau spiranique |
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 |
CN102046633B (zh) | 2008-03-27 | 2015-03-25 | 格吕伦塔尔有限公司 | 取代的螺环状环己烷衍生物 |
-
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 PE PE2012000659A patent/PE20121430A1/es active IP Right Grant
- 2010-11-10 MY MYPI2012002117A patent/MY160665A/en unknown
- 2010-11-10 ES ES10782482T patent/ES2435814T3/es active Active
- 2010-11-10 PL PL10782482T patent/PL2501703T3/pl unknown
- 2010-11-10 PT PT107824823T patent/PT2501703E/pt unknown
- 2010-11-10 US US12/943,187 patent/US8232289B2/en not_active Expired - Fee Related
- 2010-11-10 CN CN201080051850.4A patent/CN102612520B/zh not_active Expired - Fee Related
- 2010-11-10 EP EP10782482.3A patent/EP2501703B1/en active Active
- 2010-11-10 NZ NZ600006A patent/NZ600006A/en not_active IP Right Cessation
- 2010-11-10 CA CA2796161A patent/CA2796161C/en not_active Expired - Fee Related
- 2010-11-10 WO PCT/US2010/056180 patent/WO2011060035A1/en active Application Filing
- 2010-11-10 AU AU2010319581A patent/AU2010319581C1/en not_active Ceased
- 2010-11-10 RS RS20130485A patent/RS53018B/en unknown
- 2010-11-10 JP JP2012538935A patent/JP5680101B2/ja not_active Expired - Fee Related
- 2010-11-10 EA EA201290352A patent/EA020848B1/ru not_active IP Right Cessation
- 2010-11-10 SI SI201030388T patent/SI2501703T1/sl unknown
- 2010-11-10 ME MEP-2013-118A patent/ME01537B/me unknown
- 2010-11-10 MX MX2012005691A patent/MX2012005691A/es active IP Right Grant
- 2010-11-10 KR KR1020127012498A patent/KR101363830B1/ko active IP Right Grant
- 2010-11-10 DK DK10782482.3T patent/DK2501703T3/da active
-
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
- 2012-10-26 HK HK12110735.5A patent/HK1169988A1/xx not_active IP Right Cessation
-
2013
- 2013-02-26 CR CR20130087A patent/CR20130087A/es unknown
- 2013-10-11 HR HRP20130967AT patent/HRP20130967T1/hr unknown
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