JP2007530577A5 - - Google Patents
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- Publication number
- JP2007530577A5 JP2007530577A5 JP2007505172A JP2007505172A JP2007530577A5 JP 2007530577 A5 JP2007530577 A5 JP 2007530577A5 JP 2007505172 A JP2007505172 A JP 2007505172A JP 2007505172 A JP2007505172 A JP 2007505172A JP 2007530577 A5 JP2007530577 A5 JP 2007530577A5
- Authority
- JP
- Japan
- Prior art keywords
- hydroxy
- aryl
- halogen
- optionally substituted
- alkylene
- 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
- 125000000217 alkyl group Chemical group 0.000 claims 36
- 229910052736 halogen Inorganic materials 0.000 claims 34
- 150000002367 halogens Chemical class 0.000 claims 34
- 125000003545 alkoxy group Chemical group 0.000 claims 33
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 32
- 125000003118 aryl group Chemical group 0.000 claims 25
- 150000001875 compounds Chemical class 0.000 claims 23
- 125000002947 alkylene group Chemical group 0.000 claims 21
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 17
- 125000000623 heterocyclic group Chemical group 0.000 claims 14
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 12
- 125000000753 cycloalkyl group Chemical group 0.000 claims 12
- 229910052739 hydrogen Inorganic materials 0.000 claims 11
- 239000001257 hydrogen Substances 0.000 claims 11
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 9
- 125000002102 aryl alkyloxo group Chemical group 0.000 claims 8
- 239000008194 pharmaceutical composition Substances 0.000 claims 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 125000004104 aryloxy group Chemical group 0.000 claims 5
- 239000003433 contraceptive agent Substances 0.000 claims 5
- 230000002254 contraceptive effect Effects 0.000 claims 5
- -1 hydroxy-alkylene- Chemical group 0.000 claims 5
- 208000035475 disorder Diseases 0.000 claims 4
- 239000000825 pharmaceutical preparation Substances 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 102000009132 CB1 Cannabinoid Receptor Human genes 0.000 claims 3
- 108010073366 CB1 Cannabinoid Receptor Proteins 0.000 claims 3
- 239000004480 active ingredient Substances 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000011580 syndromic disease Diseases 0.000 claims 3
- 101100240516 Caenorhabditis elegans nhr-10 gene Proteins 0.000 claims 2
- 102000018208 Cannabinoid Receptor Human genes 0.000 claims 2
- 108050007331 Cannabinoid receptor Proteins 0.000 claims 2
- UGJMXCAKCUNAIE-UHFFFAOYSA-N Gabapentin Chemical compound OC(=O)CC1(CN)CCCCC1 UGJMXCAKCUNAIE-UHFFFAOYSA-N 0.000 claims 2
- RJKFOVLPORLFTN-LEKSSAKUSA-N Progesterone Chemical class C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)C)[C@@]1(C)CC2 RJKFOVLPORLFTN-LEKSSAKUSA-N 0.000 claims 2
- KJADKKWYZYXHBB-XBWDGYHZSA-N Topiramic acid Chemical group C1O[C@@]2(COS(N)(=O)=O)OC(C)(C)O[C@H]2[C@@H]2OC(C)(C)O[C@@H]21 KJADKKWYZYXHBB-XBWDGYHZSA-N 0.000 claims 2
- 239000000556 agonist Substances 0.000 claims 2
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims 2
- 125000001118 alkylidene group Chemical group 0.000 claims 2
- 230000036528 appetite Effects 0.000 claims 2
- 235000019789 appetite Nutrition 0.000 claims 2
- 125000005098 aryl alkoxy carbonyl group Chemical group 0.000 claims 2
- 239000000812 cholinergic antagonist Substances 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- OVBPIULPVIDEAO-LBPRGKRZSA-N folic acid Chemical compound C=1N=C2NC(N)=NC(=O)C2=NC=1CNC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 OVBPIULPVIDEAO-LBPRGKRZSA-N 0.000 claims 2
- 125000002541 furyl group Chemical group 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 230000004060 metabolic process Effects 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 239000000583 progesterone congener Substances 0.000 claims 2
- 239000002464 receptor antagonist Substances 0.000 claims 2
- 239000002469 receptor inverse agonist Substances 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- 125000001544 thienyl group Chemical group 0.000 claims 2
- 229960004394 topiramate Drugs 0.000 claims 2
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 1
- 102000009135 CB2 Cannabinoid Receptor Human genes 0.000 claims 1
- 108010073376 CB2 Cannabinoid Receptor Proteins 0.000 claims 1
- 102100033868 Cannabinoid receptor 1 Human genes 0.000 claims 1
- 206010010904 Convulsion Diseases 0.000 claims 1
- 208000010412 Glaucoma Diseases 0.000 claims 1
- 208000019022 Mood disease Diseases 0.000 claims 1
- 208000008238 Muscle Spasticity Diseases 0.000 claims 1
- OVBPIULPVIDEAO-UHFFFAOYSA-N N-Pteroyl-L-glutaminsaeure Natural products C=1N=C2NC(N)=NC(=O)C2=NC=1CNC1=CC=C(C(=O)NC(CCC(O)=O)C(O)=O)C=C1 OVBPIULPVIDEAO-UHFFFAOYSA-N 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- CXOFVDLJLONNDW-UHFFFAOYSA-N Phenytoin Chemical compound N1C(=O)NC(=O)C1(C=1C=CC=CC=1)C1=CC=CC=C1 CXOFVDLJLONNDW-UHFFFAOYSA-N 0.000 claims 1
- 230000002921 anti-spasmodic effect Effects 0.000 claims 1
- 229940124575 antispasmodic agent Drugs 0.000 claims 1
- 125000005161 aryl oxy carbonyl group Chemical group 0.000 claims 1
- 229960000623 carbamazepine Drugs 0.000 claims 1
- FFGPTBGBLSHEPO-UHFFFAOYSA-N carbamazepine Chemical compound C1=CC2=CC=CC=C2N(C(=O)N)C2=CC=CC=C21 FFGPTBGBLSHEPO-UHFFFAOYSA-N 0.000 claims 1
- 230000004663 cell proliferation Effects 0.000 claims 1
- 230000019771 cognition Effects 0.000 claims 1
- 230000008602 contraction Effects 0.000 claims 1
- 230000006735 deficit Effects 0.000 claims 1
- NIJJYAXOARWZEE-UHFFFAOYSA-N di-n-propyl-acetic acid Natural products CCCC(C(O)=O)CCC NIJJYAXOARWZEE-UHFFFAOYSA-N 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000000262 estrogen Substances 0.000 claims 1
- 229940011871 estrogen Drugs 0.000 claims 1
- 229960000304 folic acid Drugs 0.000 claims 1
- 235000019152 folic acid Nutrition 0.000 claims 1
- 239000011724 folic acid Substances 0.000 claims 1
- 229960002870 gabapentin Drugs 0.000 claims 1
- 230000036039 immunity Effects 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000004410 intraocular pressure Effects 0.000 claims 1
- 229940125425 inverse agonist Drugs 0.000 claims 1
- 229960001848 lamotrigine Drugs 0.000 claims 1
- PYZRQGJRPPTADH-UHFFFAOYSA-N lamotrigine Chemical compound NC1=NC(N)=NN=C1C1=CC=CC(Cl)=C1Cl PYZRQGJRPPTADH-UHFFFAOYSA-N 0.000 claims 1
- 239000002207 metabolite Substances 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 230000037023 motor activity Effects 0.000 claims 1
- 230000004112 neuroprotection Effects 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 229940127234 oral contraceptive Drugs 0.000 claims 1
- 239000003539 oral contraceptive agent Substances 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 229960002036 phenytoin Drugs 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- 229940002612 prodrug Drugs 0.000 claims 1
- 239000000018 receptor agonist Substances 0.000 claims 1
- 229940044601 receptor agonist Drugs 0.000 claims 1
- 229940044551 receptor antagonist Drugs 0.000 claims 1
- 230000000241 respiratory effect Effects 0.000 claims 1
- 239000000779 smoke Substances 0.000 claims 1
- 201000009032 substance abuse Diseases 0.000 claims 1
- 231100000736 substance abuse Toxicity 0.000 claims 1
- 208000011117 substance-related disease Diseases 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
- MSRILKIQRXUYCT-UHFFFAOYSA-M valproate semisodium Chemical compound [Na+].CCCC(C(O)=O)CCC.CCCC(C([O-])=O)CCC MSRILKIQRXUYCT-UHFFFAOYSA-M 0.000 claims 1
- 229960000604 valproic acid Drugs 0.000 claims 1
- 230000004580 weight loss Effects 0.000 claims 1
- ZSDQUVCCRVSHNN-UHFFFAOYSA-O CCOC(C(CC1)CC(C(C(NC2C(C)(CC3)CC3C2(C)C)=O)=[NH2+])=C1NC1CCCCC1)=O Chemical compound CCOC(C(CC1)CC(C(C(NC2C(C)(CC3)CC3C2(C)C)=O)=[NH2+])=C1NC1CCCCC1)=O ZSDQUVCCRVSHNN-UHFFFAOYSA-O 0.000 description 1
- SVSATFKHXUZCDS-UHFFFAOYSA-N O=C(c1n[n](C2CCCCC2)c2c1CCCC2Cl)NC1C2C34C1CC3CC4C2 Chemical compound O=C(c1n[n](C2CCCCC2)c2c1CCCC2Cl)NC1C2C34C1CC3CC4C2 SVSATFKHXUZCDS-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US55589004P | 2004-03-24 | 2004-03-24 | |
| US60/555,890 | 2004-03-24 | ||
| PCT/US2005/009819 WO2005095353A1 (en) | 2004-03-24 | 2005-03-23 | Tetrahydro-indazole cannabinoid modulators |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2007530577A JP2007530577A (ja) | 2007-11-01 |
| JP2007530577A5 true JP2007530577A5 (https=) | 2008-04-24 |
| JP4825792B2 JP4825792B2 (ja) | 2011-11-30 |
Family
ID=34965110
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007505172A Expired - Fee Related JP4825792B2 (ja) | 2004-03-24 | 2005-03-23 | テトラヒドロ−インダゾールカンナビノイドモジュレーター |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US7452997B2 (https=) |
| EP (1) | EP1735286B1 (https=) |
| JP (1) | JP4825792B2 (https=) |
| CN (1) | CN1956964B (https=) |
| AR (1) | AR048341A1 (https=) |
| AT (1) | ATE540027T1 (https=) |
| AU (1) | AU2005228868B2 (https=) |
| BR (1) | BRPI0509207A (https=) |
| CA (1) | CA2561305C (https=) |
| CR (1) | CR8701A (https=) |
| DK (1) | DK1735286T3 (https=) |
| EA (1) | EA010887B1 (https=) |
| EC (1) | ECSP066877A (https=) |
| ES (1) | ES2378071T3 (https=) |
| IL (1) | IL178290A0 (https=) |
| MX (1) | MXPA06011017A (https=) |
| NO (1) | NO20064810L (https=) |
| PL (1) | PL1735286T3 (https=) |
| PT (1) | PT1735286E (https=) |
| TW (1) | TW200602324A (https=) |
| WO (1) | WO2005095353A1 (https=) |
| ZA (1) | ZA200608808B (https=) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2875230A1 (fr) * | 2004-09-13 | 2006-03-17 | Sanofi Aventis Sa | Derives de pyrazole condense, leur preparation et leur application en therapeutique |
| US7888381B2 (en) | 2005-06-14 | 2011-02-15 | Bristol-Myers Squibb Company | Modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity, and use thereof |
| US8378096B2 (en) | 2005-09-23 | 2013-02-19 | Janssen Pharmaceutica N.V. | Hexahydro-cycloheptapyrazole cannabinoid modulators |
| BRPI0616401A2 (pt) * | 2005-09-23 | 2011-06-21 | Janssen Pharmaceutica Nv | moduladores de hexa-hidro-ciclo-otil pirazol canabinoide e uso dos mesmos |
| BRPI0616263A2 (pt) * | 2005-09-23 | 2011-06-14 | Janssen Pharmaceutica Nv | moduladores canabinàides do tipo tetrahidro-ciclopentil pirazol |
| US7825151B2 (en) * | 2005-09-23 | 2010-11-02 | Janssen Pharmaceutica Nv | Hexahydro-cyclooctyl pyrazole cannabinoid modulators |
| JP2009508954A (ja) * | 2005-09-23 | 2009-03-05 | 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 | 置換３−アミド−テトラヒドロ−インダゾリル系カンナビノイドモジュレーター |
| BRPI0616402A2 (pt) * | 2005-09-23 | 2011-06-21 | Janssen Pharmaceutica Nv | moduladores de canabinóide de hexaidro-cicloeptapirazol |
| US8378117B2 (en) | 2005-09-23 | 2013-02-19 | Janssen Pharmaceutica N.V. | Hexahydro-cycloheptapyrazole cannabinoid modulators |
| US7795294B2 (en) | 2006-02-14 | 2010-09-14 | Janssen Pharmaceutica N.V. | Tetrahydro-2H-indazole pyrazole cannabinoid modulators |
| US20070254911A1 (en) * | 2006-03-27 | 2007-11-01 | Mingde Xia | Tetrahydro-Pyrazolo[3,4-c]Pyridine Cannabinoid Modulators |
| US8012957B2 (en) | 2006-03-27 | 2011-09-06 | Janssen Pharmaceutica Nv | Tetrahydro-1H-1,2,6-triaza-azulene cannabinoid modulators |
| WO2008054508A2 (en) * | 2006-04-13 | 2008-05-08 | Alza Corporation | Stable nanosized amorphous drug |
| EP2091921A2 (en) * | 2006-11-03 | 2009-08-26 | Glenmark Pharmaceuticals S.A. | Bridged bicyclic indazoles as cannabinoid receptor ligands |
| EP1935420A1 (en) * | 2006-12-21 | 2008-06-25 | Merck Sante | 2-Adamantyl-butyramide derivatives as selective 11beta-HSD1 inhibitors |
| CN101677556A (zh) * | 2007-03-21 | 2010-03-24 | 詹森药业有限公司 | 治疗cb2受体介导的疼痛的方法 |
| AU2008229265A1 (en) * | 2007-03-21 | 2008-09-25 | Janssen Pharmaceutica N.V. | Method for treating CB2 receptor mediated pain |
| UA100120C2 (en) * | 2007-04-03 | 2012-11-26 | Анадис Фармасьютикалз, Инк. | 5,6-dihydro-1h-pyridin-2-one compounds |
| US8338623B2 (en) * | 2007-07-09 | 2012-12-25 | Abbvie Inc. | Compounds as cannabinoid receptor ligands |
| US7943653B2 (en) * | 2007-08-13 | 2011-05-17 | Janssen Pharmaceutica N.V. | Substituted 5-vinylphenyl-1-phenyl-pyrazole cannabinoid modulators |
| AU2009203549B2 (en) * | 2008-01-08 | 2013-03-07 | Purdue Pharma L.P. | Proline Analogs as ligands for cannabinoid receptors for the treatment of pain |
| US20090215850A1 (en) * | 2008-02-27 | 2009-08-27 | Mingde Xia | Method for treating cb2 receptor mediated pain |
| CA2735886A1 (en) * | 2008-09-25 | 2010-04-01 | F. Hoffmann-La Roche Ag | Indazole or 4,5,6,7-tetrahydro-indazole derivatives |
| US8652527B1 (en) | 2013-03-13 | 2014-02-18 | Upsher-Smith Laboratories, Inc | Extended-release topiramate capsules |
| US9101545B2 (en) | 2013-03-15 | 2015-08-11 | Upsher-Smith Laboratories, Inc. | Extended-release topiramate capsules |
| WO2016179349A1 (en) | 2015-05-05 | 2016-11-10 | Northwestern University | Cxcr4 chemokine receptor modulators |
| US9682940B2 (en) | 2015-08-25 | 2017-06-20 | Janssen Pharmaceutica Nv | Indazole derivatives useful as CB-1 inverse agonists |
| CN105367498B (zh) * | 2015-11-11 | 2019-05-17 | 中国农业大学 | 吡唑并环-3-甲酰胺类似物及其制备和应用 |
| CN106397218A (zh) * | 2016-09-04 | 2017-02-15 | 王际菊 | S‑α‑环己基苯甲胺 |
| WO2020008317A1 (en) * | 2018-07-03 | 2020-01-09 | Janssen Pharmaceutica Nv | Acylsufonamide compounds useful as ep3 receptor antagonists |
| WO2021047583A1 (zh) * | 2019-09-12 | 2021-03-18 | 四川海思科制药有限公司 | 一种三环吡唑衍生物及其制备 |
| WO2021047581A1 (zh) * | 2019-09-12 | 2021-03-18 | 四川海思科制药有限公司 | 一种六氢化苯并吡唑衍生物及其制备 |
| CA3186769A1 (en) * | 2020-06-11 | 2021-12-16 | Betta Pharmaceuticals Co., Ltd | Bicyclic compounds and use thereof |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IT1052111B (it) * | 1972-02-29 | 1981-06-20 | Acraf | Acidi i benzil i h indazol 3 carbossilici sostituiti e loro derivati |
| US3895025A (en) * | 1973-03-29 | 1975-07-15 | Du Pont | 2-Benzimidazolethiol preparation |
| EP0226624A1 (en) * | 1985-06-14 | 1987-07-01 | The Upjohn Company | Cyclopentapyrazole and tetrahydroindazole compounds |
| US4861777A (en) * | 1987-09-11 | 1989-08-29 | Mitsubishi Kasei Corporation | Pyrazole derivative and insecticidal and miticidal composition containing the derivative as active ingredient |
| JPH06306053A (ja) | 1993-01-29 | 1994-11-01 | Sagami Chem Res Center | ３−アゾールカルボン酸誘導体の製造方法及びその中間体 |
| US5532237A (en) * | 1995-02-15 | 1996-07-02 | Merck Frosst Canada, Inc. | Indole derivatives with affinity for the cannabinoid receptor |
| US6410533B1 (en) * | 2000-02-10 | 2002-06-25 | Genzyme Corporation | Antibacterial compounds |
| WO2001058869A2 (en) * | 2000-02-11 | 2001-08-16 | Bristol-Myers Squibb Company | Cannabinoid receptor modulators, their processes of preparation, and use of cannabinoid receptor modulators in treating respiratory and non-respiratory diseases |
| US7666867B2 (en) | 2001-10-26 | 2010-02-23 | University Of Connecticut | Heteroindanes: a new class of potent cannabimimetic ligands |
| US20050154202A1 (en) * | 2002-04-05 | 2005-07-14 | Hagmann William K. | Substituted aryl amides |
| US7145012B2 (en) * | 2003-04-23 | 2006-12-05 | Pfizer Inc. | Cannabinoid receptor ligands and uses thereof |
-
2005
- 2005-03-23 EP EP05732229A patent/EP1735286B1/en not_active Expired - Lifetime
- 2005-03-23 CA CA2561305A patent/CA2561305C/en not_active Expired - Fee Related
- 2005-03-23 MX MXPA06011017A patent/MXPA06011017A/es unknown
- 2005-03-23 AT AT05732229T patent/ATE540027T1/de active
- 2005-03-23 WO PCT/US2005/009819 patent/WO2005095353A1/en not_active Ceased
- 2005-03-23 TW TW094108873A patent/TW200602324A/zh unknown
- 2005-03-23 PL PL05732229T patent/PL1735286T3/pl unknown
- 2005-03-23 CN CN2005800160828A patent/CN1956964B/zh not_active Expired - Fee Related
- 2005-03-23 AU AU2005228868A patent/AU2005228868B2/en not_active Ceased
- 2005-03-23 DK DK05732229.9T patent/DK1735286T3/da active
- 2005-03-23 BR BRPI0509207-8A patent/BRPI0509207A/pt not_active IP Right Cessation
- 2005-03-23 PT PT05732229T patent/PT1735286E/pt unknown
- 2005-03-23 EA EA200601760A patent/EA010887B1/ru not_active IP Right Cessation
- 2005-03-23 US US11/087,943 patent/US7452997B2/en not_active Expired - Fee Related
- 2005-03-23 ES ES05732229T patent/ES2378071T3/es not_active Expired - Lifetime
- 2005-03-23 JP JP2007505172A patent/JP4825792B2/ja not_active Expired - Fee Related
- 2005-03-28 AR ARP050101196A patent/AR048341A1/es not_active Application Discontinuation
-
2006
- 2006-09-22 EC EC2006006877A patent/ECSP066877A/es unknown
- 2006-09-25 IL IL178290A patent/IL178290A0/en unknown
- 2006-10-20 CR CR8701A patent/CR8701A/es unknown
- 2006-10-23 ZA ZA200608808A patent/ZA200608808B/en unknown
- 2006-10-23 NO NO20064810A patent/NO20064810L/no not_active Application Discontinuation
-
2008
- 2008-10-08 US US12/247,263 patent/US20090099143A1/en not_active Abandoned
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