JP2009521483A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2009521483A5 JP2009521483A5 JP2008547641A JP2008547641A JP2009521483A5 JP 2009521483 A5 JP2009521483 A5 JP 2009521483A5 JP 2008547641 A JP2008547641 A JP 2008547641A JP 2008547641 A JP2008547641 A JP 2008547641A JP 2009521483 A5 JP2009521483 A5 JP 2009521483A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally
- compound
- halo
- optionally substituted
- alkyl
- 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.)
- Pending
Links
- 150000001875 compounds Chemical class 0.000 claims description 36
- 125000005843 halogen group Chemical group 0.000 claims description 29
- 125000000217 alkyl group Chemical group 0.000 claims description 23
- -1 cycloaliphatic Chemical group 0.000 claims description 22
- 125000001424 substituent group Chemical group 0.000 claims description 22
- 125000003118 aryl group Chemical group 0.000 claims description 21
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 17
- 125000001072 heteroaryl group Chemical group 0.000 claims description 17
- 125000001931 aliphatic group Chemical group 0.000 claims description 16
- 125000003545 alkoxy group Chemical group 0.000 claims description 14
- 125000004043 oxo group Chemical group O=* 0.000 claims description 11
- 229910052739 hydrogen Inorganic materials 0.000 claims description 9
- 239000001257 hydrogen Substances 0.000 claims description 9
- 125000002619 bicyclic group Chemical group 0.000 claims description 8
- 125000006168 tricyclic group Chemical group 0.000 claims description 8
- 102000014415 Muscarinic acetylcholine receptor Human genes 0.000 claims description 7
- 108050003473 Muscarinic acetylcholine receptor Proteins 0.000 claims description 7
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 7
- 125000005073 adamantyl group Chemical group C12(CC3CC(CC(C1)C3)C2)* 0.000 claims description 6
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 6
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 5
- 125000000623 heterocyclic group Chemical group 0.000 claims description 5
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 4
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 claims description 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 3
- 229910052757 nitrogen Inorganic materials 0.000 claims description 3
- 102000005962 receptors Human genes 0.000 claims description 3
- 108020003175 receptors Proteins 0.000 claims description 3
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims 6
- 150000002431 hydrogen Chemical class 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 125000005093 alkyl carbonyl alkyl group Chemical group 0.000 claims 4
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 2
- 125000004171 alkoxy aryl group Chemical group 0.000 claims 2
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 2
- 125000004466 alkoxycarbonylamino group Chemical group 0.000 claims 2
- 125000002877 alkyl aryl group Chemical group 0.000 claims 2
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 2
- 125000004656 alkyl sulfonylamino group Chemical group 0.000 claims 2
- 125000005225 alkynyloxycarbonyl group Chemical group 0.000 claims 2
- 125000005001 aminoaryl group Chemical group 0.000 claims 2
- 125000005100 aryl amino carbonyl group Chemical group 0.000 claims 2
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 125000004993 haloalkoxycarbonyl group Chemical group 0.000 claims 2
- 125000004475 heteroaralkyl group Chemical group 0.000 claims 2
- 125000005223 heteroarylcarbonyl group Chemical group 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000006413 ring segment Chemical group 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 201000000980 schizophrenia Diseases 0.000 claims 2
- 125000000547 substituted alkyl group Chemical group 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims 1
- 208000020925 Bipolar disease Diseases 0.000 claims 1
- 208000028698 Cognitive impairment Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 201000010374 Down Syndrome Diseases 0.000 claims 1
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims 1
- 206010013774 Dry eye Diseases 0.000 claims 1
- 201000011240 Frontotemporal dementia Diseases 0.000 claims 1
- 201000004311 Gilles de la Tourette syndrome Diseases 0.000 claims 1
- 208000010412 Glaucoma Diseases 0.000 claims 1
- 206010018612 Gonorrhoea Diseases 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- 241000699670 Mus sp. Species 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 208000000609 Pick Disease of the Brain Diseases 0.000 claims 1
- 208000028017 Psychotic disease Diseases 0.000 claims 1
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 1
- 208000000323 Tourette Syndrome Diseases 0.000 claims 1
- 208000016620 Tourette disease Diseases 0.000 claims 1
- 201000004810 Vascular dementia Diseases 0.000 claims 1
- 206010052428 Wound Diseases 0.000 claims 1
- 208000027418 Wounds and injury Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 208000006218 bradycardia Diseases 0.000 claims 1
- 230000036471 bradycardia Effects 0.000 claims 1
- 208000015114 central nervous system disease Diseases 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 230000027119 gastric acid secretion Effects 0.000 claims 1
- 208000001786 gonorrhea Diseases 0.000 claims 1
- 230000035876 healing Effects 0.000 claims 1
- 230000004410 intraocular pressure Effects 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 230000002093 peripheral effect Effects 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 0 *C(CC1)CCN1c1cnccn1 Chemical compound *C(CC1)CCN1c1cnccn1 0.000 description 13
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical compound CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 description 3
- 125000003368 amide group Chemical group 0.000 description 3
- 238000006243 chemical reaction Methods 0.000 description 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 230000003551 muscarinic effect Effects 0.000 description 2
- QCHFTSOMWOSFHM-WPRPVWTQSA-N (+)-Pilocarpine Chemical compound C1OC(=O)[C@@H](CC)[C@H]1CC1=CN=CN1C QCHFTSOMWOSFHM-WPRPVWTQSA-N 0.000 description 1
- 229930003347 Atropine Natural products 0.000 description 1
- WLVPJAPBRZNIRL-UHFFFAOYSA-N CC(CC1)CCN1C1=NCC(c2ccncc2)N=C1 Chemical compound CC(CC1)CCN1C1=NCC(c2ccncc2)N=C1 WLVPJAPBRZNIRL-UHFFFAOYSA-N 0.000 description 1
- NZXTTZCHGXRFGF-UHFFFAOYSA-N CC(CC1)CCN1c1cc(OC)ccc1 Chemical compound CC(CC1)CCN1c1cc(OC)ccc1 NZXTTZCHGXRFGF-UHFFFAOYSA-N 0.000 description 1
- PTMCNXVROIQJSS-UHFFFAOYSA-N CCC(CC1)CCN1c1cncnc1 Chemical compound CCC(CC1)CCN1c1cncnc1 PTMCNXVROIQJSS-UHFFFAOYSA-N 0.000 description 1
- KUHCKJQBOIUHMR-UHFFFAOYSA-N CCc(nc1)cnc1N1CCC(C)CC1 Chemical compound CCc(nc1)cnc1N1CCC(C)CC1 KUHCKJQBOIUHMR-UHFFFAOYSA-N 0.000 description 1
- SFLYLCSGHCILEF-UHFFFAOYSA-N CN(C1)C1C(CC1)CCN1c1ccccn1 Chemical compound CN(C1)C1C(CC1)CCN1c1ccccn1 SFLYLCSGHCILEF-UHFFFAOYSA-N 0.000 description 1
- QEFQAVCBWZDGPE-UHFFFAOYSA-N Cc(nc1)cnc1N(CC1)CCC1N Chemical compound Cc(nc1)cnc1N(CC1)CCC1N QEFQAVCBWZDGPE-UHFFFAOYSA-N 0.000 description 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 1
- RKUNBYITZUJHSG-UHFFFAOYSA-N Hyosciamin-hydrochlorid Natural products CN1C(C2)CCC1CC2OC(=O)C(CO)C1=CC=CC=C1 RKUNBYITZUJHSG-UHFFFAOYSA-N 0.000 description 1
- YZCKVEUIGOORGS-IGMARMGPSA-N Protium Chemical compound [1H] YZCKVEUIGOORGS-IGMARMGPSA-N 0.000 description 1
- QCHFTSOMWOSFHM-UHFFFAOYSA-N SJ000285536 Natural products C1OC(=O)C(CC)C1CC1=CN=CN1C QCHFTSOMWOSFHM-UHFFFAOYSA-N 0.000 description 1
- 239000005557 antagonist Substances 0.000 description 1
- 125000004429 atom Chemical group 0.000 description 1
- RKUNBYITZUJHSG-SPUOUPEWSA-N atropine Chemical compound O([C@H]1C[C@H]2CC[C@@H](C1)N2C)C(=O)C(CO)C1=CC=CC=C1 RKUNBYITZUJHSG-SPUOUPEWSA-N 0.000 description 1
- 229960000396 atropine Drugs 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 125000004432 carbon atom Chemical group C* 0.000 description 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 description 1
- 210000003169 central nervous system Anatomy 0.000 description 1
- 238000012512 characterization method Methods 0.000 description 1
- 230000008878 coupling Effects 0.000 description 1
- 238000010168 coupling process Methods 0.000 description 1
- 238000005859 coupling reaction Methods 0.000 description 1
- 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 1
- 125000000596 cyclohexenyl group Chemical group C1(=CCCCC1)* 0.000 description 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 1
- 125000000640 cyclooctyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 description 1
- 125000002433 cyclopentenyl group Chemical group C1(=CCCC1)* 0.000 description 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 1
- 229910052731 fluorine Inorganic materials 0.000 description 1
- 239000011737 fluorine Substances 0.000 description 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 description 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 description 1
- 239000000472 muscarinic agonist Substances 0.000 description 1
- 229960001416 pilocarpine Drugs 0.000 description 1
- 239000011541 reaction mixture Substances 0.000 description 1
- 238000004007 reversed phase HPLC Methods 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- 239000006228 supernatant Substances 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US75318705P | 2005-12-22 | 2005-12-22 | |
| PCT/US2006/049141 WO2007076070A2 (en) | 2005-12-22 | 2006-12-22 | Modulators of muscarinic receptors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2009521483A JP2009521483A (ja) | 2009-06-04 |
| JP2009521483A5 true JP2009521483A5 (https=) | 2010-02-18 |
Family
ID=38138812
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008547641A Pending JP2009521483A (ja) | 2005-12-22 | 2006-12-22 | ムスカリン受容体のモジュレーター |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US7858635B2 (https=) |
| EP (1) | EP1973543A2 (https=) |
| JP (1) | JP2009521483A (https=) |
| KR (1) | KR20080087841A (https=) |
| CN (1) | CN101374519A (https=) |
| AU (1) | AU2006330866A1 (https=) |
| CA (1) | CA2634456A1 (https=) |
| IL (1) | IL192327A0 (https=) |
| NO (1) | NO20083011L (https=) |
| RU (1) | RU2008130094A (https=) |
| WO (1) | WO2007076070A2 (https=) |
| ZA (1) | ZA200806028B (https=) |
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2290731A1 (en) * | 1999-11-26 | 2001-05-26 | D. Jed Harrison | Apparatus and method for trapping bead based reagents within microfluidic analysis system |
| JP2003294742A (ja) | 2002-03-29 | 2003-10-15 | Inst Of Physical & Chemical Res | ハイブリダイゼーション用基板及びその使用方法 |
| US7786141B2 (en) * | 2004-08-19 | 2010-08-31 | Vertex Pharmaceuticals Incorporated | Dihydrospiroindene modulators of muscarinic receptors |
| NZ570497A (en) * | 2006-02-22 | 2011-09-30 | Vertex Pharma | Spiro condensed 4,4'-quinilino-piperidines derivatives as modulators of muscarinic receptors |
| WO2008121066A1 (en) * | 2007-03-30 | 2008-10-09 | Astrazeneca Ab | Novel tricyclic spiropiperidines or spiropyrrolidines and their use as modulators of chemokine receptors |
| TW201322983A (zh) * | 2007-08-31 | 2013-06-16 | Purdue Pharma Lp | 經取代之喹□啉型哌啶化合物及其用途 |
| HRP20120968T1 (hr) * | 2008-02-06 | 2013-01-31 | Astrazeneca Ab | Spojevi |
| CA2794153C (en) | 2010-03-25 | 2018-01-02 | Glaxosmithkline Llc | Substituted indoline derivatives as perk inhibitors |
| TW201643169A (zh) * | 2010-07-09 | 2016-12-16 | 艾伯維股份有限公司 | 作為s1p調節劑的螺-哌啶衍生物 |
| AU2012338581B2 (en) | 2011-11-18 | 2016-12-08 | Nxera Pharma Uk Limited | Muscarinic M1 receptor agonists |
| BR112015006029B1 (pt) | 2012-09-18 | 2022-01-25 | Heptares Therapeutics Limited | Compostos aza bicíclicos como agonistas de receptor m1 muscarínicos, composição farmacêutica compreendendo ditos compostos e uso dos mesmos para tratar um distúrbio cognitivo ou distúrbio psicótico ou para tratar ou reduzir a gravidade de dores agudas, crônicas, neuropáticas ou inflamatórias |
| GB2519470A (en) * | 2013-09-18 | 2015-04-22 | Heptares Therapeutics Ltd | Bicyclic aza compounds as muscarinic M1 receptor agonists |
| KR102352388B1 (ko) | 2014-02-06 | 2022-01-17 | 헵테얼즈 테라퓨틱스 리미티드 | 무스카린성 m1 수용체 및/또는 m4 수용체 작용제로서 바이사이클릭 아자 화합물 |
| GB201404922D0 (en) * | 2014-03-19 | 2014-04-30 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
| US10118890B2 (en) | 2014-10-10 | 2018-11-06 | The Research Foundation For The State University Of New York | Trifluoromethoxylation of arenes via intramolecular trifluoromethoxy group migration |
| US9745253B2 (en) | 2015-03-13 | 2017-08-29 | Forma Therapeutics, Inc. | Alpha-cinnamide compounds and compositions as HDAC8 inhibitors |
| GB201504675D0 (en) * | 2015-03-19 | 2015-05-06 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
| GB201513743D0 (en) | 2015-08-03 | 2015-09-16 | Heptares Therapeutics Ltd | Muscarinic agonists |
| AR105911A1 (es) | 2015-09-03 | 2017-11-22 | Forma Therapeutics Inc | Inhibidores de hdac8 bicíclicos fusionados [6,6] |
| GB201519352D0 (en) | 2015-11-02 | 2015-12-16 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
| WO2017107089A1 (en) | 2015-12-23 | 2017-06-29 | Merck Sharp & Dohme Corp. | 3- (1h-pyrazol-4-yl) pyridineallosteric modulators of the m4 muscarinic acetylcholine receptor |
| US10329289B2 (en) | 2015-12-23 | 2019-06-25 | Merck Sharp & Dohme Corp. | 6,7-dihydro-5H-pyrrolo[3,4-B]pyridin-5-one allosteric modulators of the M4 muscarinic acetylcholine receptor |
| GB201617454D0 (en) | 2016-10-14 | 2016-11-30 | Heptares Therapeutics Limited | Pharmaceutical compounds |
| WO2018112842A1 (en) | 2016-12-22 | 2018-06-28 | Merck Sharp & Dohme Corp. | 6,6-fused heteroaryl piperidine ether allosteric modulators of m4 muscarinic acetylcholine receptor |
| WO2018112843A1 (en) | 2016-12-22 | 2018-06-28 | Merck Sharp & Dohme Corp. | Heteroaryl piperidine ether allosteric modulators of the m4 muscarinic acetylcholine receptor |
| WO2018112840A1 (en) | 2016-12-22 | 2018-06-28 | Merck Sharp & Dohme Corp. | 6, 5-fused heteroaryl piperidine ether allosteric modulators of the m4 muscarinic acetylcholine receptor |
| WO2019000236A1 (en) | 2017-06-27 | 2019-01-03 | Merck Sharp & Dohme Corp. | ALLOSTERIC MODULATORS OF 3- (1H-PYRAZOL-4-YL) PYRIDINE FROM THE M4 ACETYLCHOLINE MUSCARINIC RECEPTOR |
| WO2019000238A1 (en) | 2017-06-27 | 2019-01-03 | Merck Sharp & Dohme Corp. | 5- (PYRIDIN-3-YL) OXAZOLE ALLOSTERIC MODULATORS OF M4 ACETYLCHOLINE MUSCARINIC RECEPTOR |
| WO2019000237A1 (en) | 2017-06-27 | 2019-01-03 | Merck Sharp & Dohme Corp. | ALLOSTERIC MODULATORS OF 3- (1H-PYRAZOL-4-YL) PYRIDINE FROM THE M4 ACETYLCHOLINE MUSCARINIC RECEPTOR |
| GB201810239D0 (en) | 2018-06-22 | 2018-08-08 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
| GB201810245D0 (en) | 2018-06-22 | 2018-08-08 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
| GB201819960D0 (en) | 2018-12-07 | 2019-01-23 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
| GB201819961D0 (en) | 2018-12-07 | 2019-01-23 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
| GB202020191D0 (en) | 2020-12-18 | 2021-02-03 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
| EP4077307B1 (en) | 2019-12-18 | 2025-03-12 | Crinetics Pharmaceuticals, Inc. | Gem-disubstituted piperidine melanocortin subtype-2 receptor (mc2r) antagonists and uses thereof |
| WO2021133563A1 (en) | 2019-12-23 | 2021-07-01 | Crinetics Pharmaceuticals, Inc. | Spirocyclic piperidine melanocortin subtype-2 receptor (mc2r) antagonists and uses thereof |
| AU2021275233A1 (en) * | 2020-05-22 | 2022-12-08 | Vanderbilt University | Competitive and noncompetitive inhibitors of the muscarinic acetylcholine receptor M5 |
| WO2022032073A2 (en) * | 2020-08-07 | 2022-02-10 | Casma Therapeutics, Inc. | Trpml modulators |
Family Cites Families (86)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3666764A (en) * | 1970-08-26 | 1972-05-30 | Mead Johnson & Co | Spiroindenylpiperidines |
| US3654287A (en) * | 1970-08-26 | 1972-04-04 | Mead Johnson & Co | Spiroindanylpiperidines |
| DK145949C (da) | 1973-09-28 | 1983-09-26 | Ciba Geigy Ag | Analogifremgangsmaade til fremstilling af i 3-stillingen substituerede rifamycin s-forbindelser eller sv-forbindelser eller syreadditionssalte eller kvaternaere ammoniumsalte deraf |
| US3962259A (en) * | 1973-12-12 | 1976-06-08 | American Hoechst Corporation | 1,3-Dihydrospiro[isobenzofuran]s and derivatives thereof |
| US3959475A (en) * | 1973-12-12 | 1976-05-25 | American Hoechst Corporation | Substituted 1,3-dihydrospiro(isobenzofuran)s |
| JPS54109983A (en) * | 1978-02-13 | 1979-08-29 | Sumitomo Chem Co Ltd | Novel spiroamine derivative and its preparation |
| GB1575800A (en) | 1978-05-16 | 1980-10-01 | Sumitomo Chemical Co | Spiro amines their production and compositions containing them |
| US4349549A (en) | 1981-05-18 | 1982-09-14 | Syntex (U.S.A.) Inc. | Anti-hypertensive 1-substituted spiro(piperidine-oxobenzoxazine)s |
| JPS5815979A (ja) | 1981-07-11 | 1983-01-29 | Kyowa Hakko Kogyo Co Ltd | 新規なピペリジン誘導体およびその製造法 |
| JPS5959685A (ja) | 1982-09-28 | 1984-04-05 | Kyowa Hakko Kogyo Co Ltd | 新規なピペリジン誘導体 |
| US4558049A (en) * | 1982-11-24 | 1985-12-10 | Farmitalia Carlo Erba S.P.A. | Antipsycotic benzoxazines |
| GB2131021B (en) | 1982-11-24 | 1985-12-18 | Erba Farmitalia | Antipsychotic benzoxazines |
| SE445649B (sv) | 1983-06-08 | 1986-07-07 | Jorgen Hermansson | Anvendning av en fast berare med immobiliserad orosomucoid for separation, forfarande for framstellning av separationsmaterial, separationsanordning samt separationsmaterial |
| GB8917069D0 (en) | 1989-07-26 | 1989-09-13 | Merck Sharp & Dohme | Therapeutic agents |
| US5091387A (en) * | 1990-03-02 | 1992-02-25 | Merck & Co., Inc. | Spirocyclic oxytocin antagonists |
| EP0444945A3 (en) | 1990-03-02 | 1992-05-13 | Merck & Co. Inc. | Use of spirocyclic compounds as oxytocin antagonists |
| EP0445974A3 (en) * | 1990-03-05 | 1992-04-29 | Merck Sharp & Dohme Ltd. | Spirocyclic antipsychotic agents |
| IL99957A0 (en) | 1990-11-13 | 1992-08-18 | Merck & Co Inc | Piperidinylcamphorsulfonyl oxytocin antagonists and pharmaceutical compositions containing them |
| NZ243065A (en) | 1991-06-13 | 1995-07-26 | Lundbeck & Co As H | Piperidine derivatives and pharmaceutical compositions |
| DE69223573D1 (de) | 1991-09-16 | 1998-01-29 | Merck & Co Inc | Hydantoin und Succinimid-substituierte Spiroindanylcamphorsulfonyl als Oxytocin-Antagonisten |
| DK78692D0 (da) * | 1992-06-12 | 1992-06-12 | Lundbeck & Co As H | Dimere piperidin- og piperazinderivater |
| NZ258412A (en) | 1992-12-11 | 1997-01-29 | Merck & Co Inc | Spiro-fused piperidine derivatives and pharmaceutical compositions |
| US5536716A (en) | 1992-12-11 | 1996-07-16 | Merck & Co., Inc. | Spiro piperidines and homologs which promote release of growth hormone |
| WO1994022846A1 (en) | 1993-03-30 | 1994-10-13 | Pfizer Inc. | Compounds enhancing antitumor activity of other cytotoxic agents |
| US5817679A (en) * | 1993-04-01 | 1998-10-06 | University Of Virginia | 7-Azabicyclo 2.2.1!-heptane and -heptene derivatives as cholinergic receptor ligands |
| US5457207A (en) | 1993-10-05 | 1995-10-10 | Regents Of The University Of Minnesota | Spirovesamicols |
| HUT75224A (en) | 1993-10-19 | 1997-04-28 | Merck & Co Inc | Combination of bisphosphonates and growth hormone secretagogues |
| AU687953B2 (en) | 1993-11-16 | 1998-03-05 | Merck & Co., Inc. | Piperidinylcamphorsulfonyl oxytocin antagonists |
| AU2223495A (en) | 1994-04-15 | 1995-11-10 | Yamanouchi Pharmaceutical Co., Ltd. | Spiro compound and medicinal composition thereof |
| US5789402A (en) * | 1995-01-17 | 1998-08-04 | Eli Lilly Company | Compounds having effects on serotonin-related systems |
| US5627196A (en) * | 1995-01-17 | 1997-05-06 | Eli Lilly And Company | Compounds having effects on serotonin-related systems |
| US5614523A (en) * | 1995-01-17 | 1997-03-25 | Eli Lilly And Company | Compounds having effects on serotonin-related systems |
| US5576321A (en) * | 1995-01-17 | 1996-11-19 | Eli Lilly And Company | Compounds having effects on serotonin-related systems |
| US5741789A (en) * | 1995-01-17 | 1998-04-21 | Eli Lilly And Company | Compounds having effects on serotonin-related systems |
| US6130217A (en) * | 1995-09-20 | 2000-10-10 | Pfizer Inc | Compounds enhancing antitumor activity of other cytotoxic agents |
| GB2308064A (en) | 1995-10-31 | 1997-06-18 | Merck & Co Inc | Treatment of congestive heart failure with a growth hormone secretagogue |
| GB9601724D0 (en) * | 1996-01-29 | 1996-03-27 | Merck Sharp & Dohme | Therapeutic agents |
| AU711884B2 (en) | 1996-05-07 | 1999-10-21 | Merck & Co., Inc. | Enhancement of sleep with a growth hormone secretagogue |
| WO1997041878A1 (en) | 1996-05-07 | 1997-11-13 | Merck & Co., Inc. | Treatment of mood disorders with a growth hormone secretagogue |
| BR9812118A (pt) | 1997-07-31 | 2000-07-18 | Elan Pharm Inc | Compostos do tipo 4-amino-fenilalanina que inibem adesão de leucócito mediada por vla-4 |
| EP1009405A4 (en) * | 1997-08-28 | 2001-05-09 | Merck & Co Inc | PAYRROLIDINE AND PIPERIDINE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY |
| US6013652A (en) * | 1997-12-04 | 2000-01-11 | Merck & Co., Inc. | Spiro-substituted azacycles as neurokinin antagonists |
| AU2206699A (en) * | 1997-12-23 | 1999-07-12 | Alcon Laboratories, Inc. | Muscarinic agents and use thereof to treat glaucoma, myopia and various other conditions |
| GB9810886D0 (en) * | 1998-05-13 | 1998-07-22 | Lilly Industries Ltd | Pharmaceutical compounds |
| AU742425B2 (en) | 1998-06-11 | 2002-01-03 | Merck & Co., Inc. | Spiropiperidine derivatives as melanocortin receptor agonists |
| ID29137A (id) | 1998-07-27 | 2001-08-02 | Schering Corp | Ligan-ligan afinitas tinggi untuk reseptor nosiseptin orl-1 |
| BR9912406A (pt) | 1998-07-28 | 2001-04-24 | Smithkline Beecham Corp | Compostos de anilida substituida e métodos |
| CA2338804A1 (en) | 1998-07-28 | 2000-02-10 | Smithkline Beecham Corporation | Propenamides as ccr5 modulators |
| EP1142587A1 (en) | 1998-12-24 | 2001-10-10 | Meiji Seika Kaisha Ltd. | Remedies for pain |
| US6303593B1 (en) * | 1999-03-02 | 2001-10-16 | Merck & Co., Inc. | 3-thienyl and 3-furanyl pyrrolidine modulators of chemokine receptor activity |
| ITMI991452A1 (it) | 1999-07-01 | 2001-01-01 | Mediolanum Farmaceutici Srl | Antagonisti selettivi per i recettori m2 con struttura 5h-dibenzo b,fazepinica |
| US6803372B2 (en) * | 1999-08-20 | 2004-10-12 | Banyu Pharmaceutical Co., Ltd. | Spiro compounds |
| TWI279402B (en) * | 1999-08-20 | 2007-04-21 | Banyu Pharma Co Ltd | Spiro compounds having NPY antagonistic activities and agents containing the same |
| GB2355264A (en) | 1999-09-30 | 2001-04-18 | Merck & Co Inc | Spirohydantoin derivatives useful as alpha 1a adrenoceptor antagonists |
| WO2001022919A2 (en) | 1999-09-30 | 2001-04-05 | Merck & Co., Inc. | Spiro[bicyclic -azacycloalkyl and -cycloalkyl] derivatives and uses thereof |
| GB2355456A (en) * | 1999-09-30 | 2001-04-25 | Merck & Co Inc | Novel arylhydantoin derivatives useful as alpha 1a adrenoceptor antagonists |
| AU7952800A (en) | 1999-10-22 | 2001-04-30 | Sankyo Company Limited | 2-alkoxybenzene derivatives |
| JP2001278886A (ja) | 2000-03-28 | 2001-10-10 | Dai Ichi Seiyaku Co Ltd | ベンゾオキサジン誘導体及びこれを含有する医薬 |
| US6720324B2 (en) * | 2000-07-05 | 2004-04-13 | Synaptic Pharmaceutical Corporation | Selective melanin concentrating hormone-1 (MCH1) receptor antagonists and uses thereof |
| BR0116113A (pt) * | 2000-12-12 | 2004-08-03 | Neurogen Corp | Espiro[isobenzofuran-1,4'-piperidin]-3-onas e 3h-espiroisoben-zofuran-1,4'-piperidinas |
| PT1385514E (pt) * | 2001-04-18 | 2009-02-04 | Euro Celtique Sa | Compostos espiroindeno e espiroindano |
| JP2002316987A (ja) | 2001-04-20 | 2002-10-31 | Sankyo Co Ltd | ２−アルコキシベンゼン誘導体を含有する医薬 |
| ATE427935T1 (de) | 2001-08-07 | 2009-04-15 | Banyu Pharma Co Ltd | Spiro isobenzofurane als neuropeptid y rezeptor antagonisten |
| AU2002363236A1 (en) * | 2001-10-30 | 2003-05-12 | Millennium Pharmaceuticals, Inc. | Compounds, pharmaceutical compositions and methods of use therefor |
| WO2003064425A1 (en) * | 2002-01-28 | 2003-08-07 | Pfizer Japan Inc. | N-substituted spiropiperidine compounds as ligands for orl-1 receptor |
| US7220862B2 (en) * | 2002-06-05 | 2007-05-22 | Bristol-Myers Squibb Company | Calcitonin gene related peptide receptor antagonists |
| GB0213715D0 (en) * | 2002-06-14 | 2002-07-24 | Syngenta Ltd | Chemical compounds |
| US7105526B2 (en) * | 2002-06-28 | 2006-09-12 | Banyu Pharmaceuticals Co., Ltd. | Benzimidazole derivatives |
| UA77814C2 (en) * | 2002-07-03 | 2007-01-15 | Lundbeck & Co As H | Spirocyclic piperidines as antagonists of mch1 and use thereof |
| KR101025633B1 (ko) * | 2002-09-19 | 2011-03-30 | 일라이 릴리 앤드 캄파니 | 오피오이드 수용체 안타고니스트로서의 디아릴 에테르 |
| US7045527B2 (en) * | 2002-09-24 | 2006-05-16 | Amgen Inc. | Piperidine derivatives |
| DE60328035D1 (de) * | 2002-11-29 | 2009-07-30 | Banyu Pharma Co Ltd | Neue azolderivate |
| US7247628B2 (en) * | 2002-12-12 | 2007-07-24 | Pfizer, Inc. | Cannabinoid receptor ligands and uses thereof |
| WO2004082682A1 (en) * | 2003-03-18 | 2004-09-30 | Merck & Co. Inc. | Amino cyclobutylamide modulators of chemokine receptor activity |
| JP3856815B2 (ja) * | 2003-04-04 | 2006-12-13 | メルク エンド カムパニー インコーポレーテッド | メラノコルチン−４受容体アゴニストとしてのアシル化スピロピペリジン誘導体 |
| CN1297557C (zh) | 2003-04-10 | 2007-01-31 | 上海药明康德新药开发有限公司 | 螺环类模板化合物的制备 |
| 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 |
| US20070254903A1 (en) * | 2003-12-23 | 2007-11-01 | Arena Pharmaceuticals, Inc. | Novel Spiroindoline or Spiroisoquinoline Compounds, Methods of Use and Compositions Thereof |
| KR100863854B1 (ko) * | 2004-02-10 | 2008-10-15 | 에프. 호프만-라 로슈 아게 | 케모카인 ｃｃｒ5 수용체 조절제 |
| TW200533398A (en) * | 2004-03-29 | 2005-10-16 | Bristol Myers Squibb Co | Novel therapeutic agents for the treatment of migraine |
| CA2561801A1 (en) * | 2004-04-02 | 2005-10-20 | Elixir Pharmaceuticals, Inc. | Sulfonamides and uses thereof |
| US7279471B2 (en) * | 2004-04-15 | 2007-10-09 | Boehringer Ingelheim International Gmbh | Selected CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions |
| AU2005249494A1 (en) * | 2004-05-28 | 2005-12-15 | Vertex Pharmaceuticals Incorporated | Modulators of muscarinic receptors |
| TW200621244A (en) * | 2004-08-19 | 2006-07-01 | Vertex Pharma | Modulators of muscarinic receptors |
| US7786141B2 (en) * | 2004-08-19 | 2010-08-31 | Vertex Pharmaceuticals Incorporated | Dihydrospiroindene modulators of muscarinic receptors |
| US7351706B2 (en) * | 2006-01-05 | 2008-04-01 | Hoffmann-La Roche Inc. | Indol-3-yl-carbonyl-spiro-piperidine derivatives |
-
2006
- 2006-12-22 US US11/644,124 patent/US7858635B2/en not_active Expired - Fee Related
- 2006-12-22 RU RU2008130094/14A patent/RU2008130094A/ru not_active Application Discontinuation
- 2006-12-22 CN CNA2006800529466A patent/CN101374519A/zh active Pending
- 2006-12-22 EP EP06848092A patent/EP1973543A2/en not_active Withdrawn
- 2006-12-22 JP JP2008547641A patent/JP2009521483A/ja active Pending
- 2006-12-22 AU AU2006330866A patent/AU2006330866A1/en not_active Abandoned
- 2006-12-22 CA CA002634456A patent/CA2634456A1/en not_active Abandoned
- 2006-12-22 KR KR1020087017741A patent/KR20080087841A/ko not_active Withdrawn
- 2006-12-22 WO PCT/US2006/049141 patent/WO2007076070A2/en not_active Ceased
-
2008
- 2008-06-19 IL IL192327A patent/IL192327A0/en unknown
- 2008-07-03 NO NO20083011A patent/NO20083011L/no not_active Application Discontinuation
- 2008-07-10 ZA ZA200806028A patent/ZA200806028B/xx unknown
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2009521483A5 (https=) | ||
| JP6236067B2 (ja) | ＲＯＲγ活性を阻害し疾患を治療するための二環式スルホン化合物 | |
| RU2008130094A (ru) | Модуляторы мускариновых рецепторов | |
| JP6309519B2 (ja) | Ｎ置換ベンズアミド及びその使用方法 | |
| JP7279758B2 (ja) | テトラヒドロナフタレン誘導体 | |
| JPWO2005047286A1 (ja) | スピロ複素環化合物 | |
| EP3440081A1 (en) | Pyrrolo[1,2-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders | |
| KR20170081204A (ko) | 제약 화합물 | |
| JP2023554282A (ja) | 置換ピペリジノ化合物及び関連する治療方法 | |
| JP6380777B2 (ja) | ＰＩ３Ｋ、ｍＴＯＲ阻害薬としての縮合キノリン化合物 | |
| WO2003099765A1 (en) | β-ALANINE DERIVATIVE AND USE THEREOF | |
| TW201623310A (zh) | 用於誘發軟骨生成之化合物及組合物 | |
| JP2008510728A5 (https=) | ||
| JP6673218B2 (ja) | ジヒドロナフタレン誘導体 | |
| JP6569661B2 (ja) | 選択的ｅｐ２アゴニスト活性を有する化合物 | |
| RU2006105782A (ru) | Производные 1-сульфонилиндола, их получение и их применение в качестве лигандов 5-нт-6 | |
| CN1795176A (zh) | 作为毒蕈碱受体拮抗剂的氮杂双环衍生物 | |
| JP6197971B1 (ja) | Ｋｃｎｑ２〜５チャネル関連疾患の予防および／または治療剤 | |
| KR20210065944A (ko) | Dp 길항제 | |
| CN1318053A (zh) | 用作钾通道开放剂的环戊酮二氢吡啶化合物 | |
| AU2014297144B2 (en) | Novel biphenyl derivative and method for preparing same | |
| JP6242811B2 (ja) | 新規なオクタヒドロピリドキナゾリン誘導体、それを含有する医薬組成物およびそれらの用途 | |
| EP3327018B1 (en) | 2-(octahydrocyclopenta[b]pyran-2-yl)1,3-thiazole-4-carboxylic acid derivatives and related compounds as ep2 agonists with intraocular pressure lowering activity | |
| JP2016011291A (ja) | 新規なドパミンｄ２受容体アゴニスト | |
| KR20250125490A (ko) | Glp-1 수용체 작용제 및 이의 용도 |