CN102612520B - 作为orl-1受体拮抗剂的螺哌啶化合物 - Google Patents
作为orl-1受体拮抗剂的螺哌啶化合物 Download PDFInfo
- Publication number
- CN102612520B CN102612520B CN201080051850.4A CN201080051850A CN102612520B CN 102612520 B CN102612520 B CN 102612520B CN 201080051850 A CN201080051850 A CN 201080051850A CN 102612520 B CN102612520 B CN 102612520B
- Authority
- CN
- China
- Prior art keywords
- methyl
- mmol
- compound
- pyran
- thieno
- 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
- YTKQMHFKNFYQRF-UHFFFAOYSA-N Brc1c(C[n]2cncc2)cccn1 Chemical compound Brc1c(C[n]2cncc2)cccn1 YTKQMHFKNFYQRF-UHFFFAOYSA-N 0.000 description 1
- OTLRGEXZCYWXIC-UHFFFAOYSA-N C/C=S(\C)/OCc(cccn1)c1Br Chemical compound C/C=S(\C)/OCc(cccn1)c1Br OTLRGEXZCYWXIC-UHFFFAOYSA-N 0.000 description 1
- OWSWJACVANVMFR-UHFFFAOYSA-N CC(C)(c1c(-[n]2nc(C)c(CN(CC3)CCC3(c([s]3)c4cc3Cl)OCC4(F)F)c2)nccc1)O Chemical compound CC(C)(c1c(-[n]2nc(C)c(CN(CC3)CCC3(c([s]3)c4cc3Cl)OCC4(F)F)c2)nccc1)O OWSWJACVANVMFR-UHFFFAOYSA-N 0.000 description 1
- YKRHONDKLRQMQM-UHFFFAOYSA-N CCOC(c(c(CN(CC1)CCC1(c([s]1)c2cc1Cl)OCC2(F)F)c1)n[n]1-c(nccc1)c1F)=O Chemical compound CCOC(c(c(CN(CC1)CCC1(c([s]1)c2cc1Cl)OCC2(F)F)c1)n[n]1-c(nccc1)c1F)=O YKRHONDKLRQMQM-UHFFFAOYSA-N 0.000 description 1
- DAZCWNVSEHDRFI-UHFFFAOYSA-N Cc(c(C=O)c1)n[n]1-c(nccc1)c1C(OC)=O Chemical compound Cc(c(C=O)c1)n[n]1-c(nccc1)c1C(OC)=O DAZCWNVSEHDRFI-UHFFFAOYSA-N 0.000 description 1
- PVYRNDVFVMPPFM-UHFFFAOYSA-N Cc(c(C=O)c1)n[n]1-c1c(COC)cccn1 Chemical compound Cc(c(C=O)c1)n[n]1-c1c(COC)cccn1 PVYRNDVFVMPPFM-UHFFFAOYSA-N 0.000 description 1
- ATEIVTLSBQMKSQ-UHFFFAOYSA-N O=C1N(Cc(cccn2)c2Br)CCOC1 Chemical compound O=C1N(Cc(cccn2)c2Br)CCOC1 ATEIVTLSBQMKSQ-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
- C07D495/20—Spiro-condensed systems
-
- 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
- A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
- A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4436—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/06—Antimigraine agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Child & Adolescent Psychology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Hydrogenated Pyridines (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09382246 | 2009-11-16 | ||
| EP09382246.8 | 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 (2)
| Publication Number | Publication Date |
|---|---|
| CN102612520A CN102612520A (zh) | 2012-07-25 |
| CN102612520B true CN102612520B (zh) | 2015-04-08 |
Family
ID=41728051
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201080051850.4A Expired - Fee Related CN102612520B (zh) | 2009-11-16 | 2010-11-10 | 作为orl-1受体拮抗剂的螺哌啶化合物 |
Country Status (34)
| Country | Link |
|---|---|
| US (1) | US8232289B2 (https=) |
| EP (1) | EP2501703B1 (https=) |
| JP (1) | JP5680101B2 (https=) |
| KR (1) | KR101363830B1 (https=) |
| CN (1) | CN102612520B (https=) |
| AR (1) | AR078863A1 (https=) |
| AU (1) | AU2010319581C1 (https=) |
| CA (1) | CA2796161C (https=) |
| CO (1) | CO6541545A2 (https=) |
| CR (1) | CR20130087A (https=) |
| DK (1) | DK2501703T3 (https=) |
| DO (1) | DOP2012000135A (https=) |
| EA (1) | EA020848B1 (https=) |
| EC (1) | ECSP12011902A (https=) |
| ES (1) | ES2435814T3 (https=) |
| HN (1) | HN2012001011A (https=) |
| HR (1) | HRP20130967T1 (https=) |
| IL (1) | IL219370A (https=) |
| JO (1) | JO2887B1 (https=) |
| MA (1) | MA33751B1 (https=) |
| ME (1) | ME01537B (https=) |
| MX (1) | MX2012005691A (https=) |
| MY (1) | MY160665A (https=) |
| NZ (1) | NZ600006A (https=) |
| PE (1) | PE20121430A1 (https=) |
| PH (1) | PH12012500969A1 (https=) |
| PL (1) | PL2501703T3 (https=) |
| PT (1) | PT2501703E (https=) |
| RS (1) | RS53018B (https=) |
| SI (1) | SI2501703T1 (https=) |
| TW (1) | TWI465453B (https=) |
| UA (1) | UA107943C2 (https=) |
| WO (1) | WO2011060035A1 (https=) |
| ZA (1) | ZA201202967B (https=) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG10201510665WA (en) | 2009-12-04 | 2016-01-28 | Sunovion Pharmaceuticals Inc | Multicycle Compounds And Pharmaceutical Compositions Useful For The Treatment Of Neurological Disorders |
| 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 |
| DK2903440T3 (en) | 2012-10-02 | 2017-12-11 | Bayer Cropscience Ag | THETEROCYCLIC COMPOUNDS AS PESTICIDES |
| US20140206667A1 (en) | 2012-11-14 | 2014-07-24 | Michela Gallagher | 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 |
| MA45795A (fr) | 2016-07-29 | 2019-06-05 | Sunovion Pharmaceuticals Inc | Composés et compositions, et utilisations associées |
| PT3494119T (pt) | 2016-07-29 | 2024-12-10 | Pgi Drug Discovery Llc | Compostos e composições e seus usos |
| MX390141B (es) | 2017-02-16 | 2025-03-20 | Sunovion Pharmaceuticals Inc | Metodos para tratar esquizofrenia |
| HUE054483T2 (hu) | 2017-03-02 | 2021-09-28 | Lilly Co Eli | ROR-gamma-T gátlására alkalmas vegyületek |
| US10603320B2 (en) * | 2017-03-02 | 2020-03-31 | Eli Lilly And Company | Compounds useful for inhibiting ROR-gamma-t |
| CA3070993C (en) | 2017-08-02 | 2025-05-20 | Sunovion Pharmaceuticals Inc. | ISOCHROMANE COMPOUNDS AND THEIR USES |
| UA130249C2 (uk) | 2018-02-16 | 2025-12-31 | Сумітомо Фарма Америка, Інк. | Солі, кристалічні форми і способи їх отримання |
| US11618746B2 (en) | 2018-12-17 | 2023-04-04 | Vertex Pharmaceuticals Incorporated | Inhibitors of APOL1 and methods of using same |
| EP3938045A1 (en) | 2019-03-14 | 2022-01-19 | Sunovion Pharmaceuticals Inc. | Salts of a isochromanyl compound and crystalline forms, processes for preparing, therapeutic uses, and pharmaceutical compositions thereof |
| CA3180115A1 (en) | 2020-04-14 | 2021-10-21 | Sunovion Pharmaceuticals Inc. | (s)-(4,5-dihydro-7h-thieno[2,3-c]pyran-7-yl)-n-methylmethanamine for treating neurological and psychiatric disorders |
| 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 |
| CN116547287B (zh) | 2020-08-26 | 2025-09-26 | 弗特克斯药品有限公司 | Apol1的抑制剂及其使用方法 |
| CA3251050A1 (en) * | 2022-02-08 | 2023-08-17 | Vertex Pharmaceuticals Incorporated | 2-METHYL-4',5'-DIHYDROSPIRO[PIPERIDINE-4,7'-THIENO[2,3-C]PYRAN] DERIVATIVES USED AS APOL1 INHIBITORS AND THEIR METHODS OF USE |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1922189A (zh) * | 2003-12-23 | 2007-02-28 | 格吕伦塔尔有限公司 | 对orl1受体具有亲合力的螺环环己烷衍生物 |
Family Cites Families (14)
| 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 |
| US6686370B2 (en) * | 1999-12-06 | 2004-02-03 | Euro-Celtique S.A. | Triazospiro compounds having nociceptin receptor affinity |
| KR100628292B1 (ko) * | 2001-04-18 | 2006-09-27 | 유로-셀티크 소시에떼 아노뉨 | 스파이로파이라졸 화합물 |
| 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 |
| ATE396995T1 (de) * | 2001-07-23 | 2008-06-15 | Banyu Pharma Co Ltd | 4-oxoimidazolidin-2-spiro piperidin derivat |
| BR0307268A (pt) * | 2002-01-28 | 2004-12-14 | Pfizer | Compostos de espiropiperidina n-substituìda como ligantes para o receptor orl-1 |
| 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 |
| JP4712384B2 (ja) * | 2002-09-09 | 2011-06-29 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | Ｏｒｌ−１受容体介在障害の治療に有用なヒドロキシアルキル置換１，３，８−トリアザスピロ［４．５］デカン−４−オン誘導体 |
| 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 |
| US7354925B2 (en) * | 2004-03-29 | 2008-04-08 | Pfizer Inc. | Alpha aryl or heteroaryl methyl beta piperidino propanamide compounds as ORL1-receptor antagonists |
| 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 |
| PT2260042E (pt) * | 2008-03-27 | 2011-12-06 | Gruenenthal Gmbh | Derivados de ciclo-hexano espirocíclicos substituídos |
-
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 NZ NZ600006A patent/NZ600006A/en not_active IP Right Cessation
- 2010-11-10 ME MEP-2013-118A patent/ME01537B/me unknown
- 2010-11-10 JP JP2012538935A patent/JP5680101B2/ja not_active Expired - Fee Related
- 2010-11-10 KR KR1020127012498A patent/KR101363830B1/ko not_active Expired - Fee Related
- 2010-11-10 MX MX2012005691A patent/MX2012005691A/es active IP Right Grant
- 2010-11-10 WO PCT/US2010/056180 patent/WO2011060035A1/en not_active Ceased
- 2010-11-10 PT PT107824823T patent/PT2501703E/pt unknown
- 2010-11-10 MY MYPI2012002117A patent/MY160665A/en unknown
- 2010-11-10 RS RS20130485A patent/RS53018B/sr unknown
- 2010-11-10 CA CA2796161A patent/CA2796161C/en not_active Expired - Fee Related
- 2010-11-10 PH PH1/2012/500969A patent/PH12012500969A1/en unknown
- 2010-11-10 SI SI201030388T patent/SI2501703T1/sl unknown
- 2010-11-10 US US12/943,187 patent/US8232289B2/en not_active Expired - Fee Related
- 2010-11-10 ES ES10782482T patent/ES2435814T3/es active Active
- 2010-11-10 AU AU2010319581A patent/AU2010319581C1/en not_active Ceased
- 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 EA EA201290352A patent/EA020848B1/ru not_active IP Right Cessation
- 2010-11-10 DK DK10782482.3T patent/DK2501703T3/da active
- 2010-11-10 PL PL10782482T patent/PL2501703T3/pl unknown
- 2010-11-10 PE PE2012000659A patent/PE20121430A1/es active IP Right Grant
- 2010-11-10 HR HRP20130967AT patent/HRP20130967T1/hr unknown
-
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 DO DO2012000135A patent/DOP2012000135A/es unknown
- 2012-05-11 HN HN2012001011A patent/HN2012001011A/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
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1922189A (zh) * | 2003-12-23 | 2007-02-28 | 格吕伦塔尔有限公司 | 对orl1受体具有亲合力的螺环环己烷衍生物 |
Non-Patent Citations (2)
| Title |
|---|
| Design, synthesis, and structure–activity relationship study of a novel class of ORL1 receptor antagonists based on N-biarylmethyl spiropiperidine;Takashi Yoshizumi，等;《Bioorganic & Medicinal Chemistry Letters》;20080516;第18卷(第13期);第3778-3782页 * |
| 孤啡肽及其受体的研究进展;史淑红，等;《山东医药》;20071231;第47卷(第21期);第117-118页 * |
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