JP2006511486A5 - - Google Patents
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- Publication number
- JP2006511486A5 JP2006511486A5 JP2004544591A JP2004544591A JP2006511486A5 JP 2006511486 A5 JP2006511486 A5 JP 2006511486A5 JP 2004544591 A JP2004544591 A JP 2004544591A JP 2004544591 A JP2004544591 A JP 2004544591A JP 2006511486 A5 JP2006511486 A5 JP 2006511486A5
- Authority
- JP
- Japan
- Prior art keywords
- use according
- sarm
- nhcor
- conhr
- snr
- 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.)
- Abandoned
Links
- 239000000849 selective androgen receptor modulator Substances 0.000 claims 88
- 229940083324 Selective androgen receptor modulator Drugs 0.000 claims 86
- 125000000217 alkyl group Chemical group 0.000 claims 52
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 48
- 150000001875 compounds Chemical class 0.000 claims 40
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 28
- 239000000126 substance Substances 0.000 claims 28
- 101100149678 Caenorhabditis elegans snr-3 gene Proteins 0.000 claims 24
- 125000004122 cyclic group Chemical group 0.000 claims 24
- 239000003814 drug Substances 0.000 claims 24
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims 20
- 125000003342 alkenyl group Chemical group 0.000 claims 20
- 125000004982 dihaloalkyl group Chemical group 0.000 claims 20
- 125000001188 haloalkyl group Chemical group 0.000 claims 20
- 125000004385 trihaloalkyl group Chemical group 0.000 claims 20
- 230000000694 effects Effects 0.000 claims 16
- 229910052760 oxygen Inorganic materials 0.000 claims 16
- 210000002307 prostate Anatomy 0.000 claims 14
- 230000003042 antagnostic effect Effects 0.000 claims 12
- 230000008878 coupling Effects 0.000 claims 12
- 238000010168 coupling process Methods 0.000 claims 12
- 238000005859 coupling reaction Methods 0.000 claims 12
- 229940079593 drug Drugs 0.000 claims 12
- 210000003205 muscle Anatomy 0.000 claims 12
- 229910052717 sulfur Inorganic materials 0.000 claims 12
- 102000007399 Nuclear hormone receptor Human genes 0.000 claims 8
- 108020005497 Nuclear hormone receptor Proteins 0.000 claims 8
- 239000003098 androgen Substances 0.000 claims 8
- 125000003710 aryl alkyl group Chemical group 0.000 claims 8
- 210000000988 bone and bone Anatomy 0.000 claims 8
- 210000003169 central nervous system Anatomy 0.000 claims 8
- 239000013078 crystal Substances 0.000 claims 8
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 8
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 8
- 239000007788 liquid Substances 0.000 claims 8
- 239000002207 metabolite Substances 0.000 claims 8
- 239000008188 pellet Substances 0.000 claims 8
- -1 polymorphs Substances 0.000 claims 8
- 229940002612 prodrug Drugs 0.000 claims 8
- 239000000651 prodrug Substances 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 239000007787 solid Substances 0.000 claims 8
- 201000004384 Alopecia Diseases 0.000 claims 6
- 208000010228 Erectile Dysfunction Diseases 0.000 claims 6
- 206010058359 Hypogonadism Diseases 0.000 claims 6
- 208000029725 Metabolic bone disease Diseases 0.000 claims 6
- 206010027940 Mood altered Diseases 0.000 claims 6
- 208000008589 Obesity Diseases 0.000 claims 6
- 206010049088 Osteopenia Diseases 0.000 claims 6
- 208000001132 Osteoporosis Diseases 0.000 claims 6
- 206010060862 Prostate cancer Diseases 0.000 claims 6
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 6
- 201000001880 Sexual dysfunction Diseases 0.000 claims 6
- 231100000360 alopecia Toxicity 0.000 claims 6
- 208000007502 anemia Diseases 0.000 claims 6
- 230000001149 cognitive effect Effects 0.000 claims 6
- 230000003247 decreasing effect Effects 0.000 claims 6
- 201000001881 impotence Diseases 0.000 claims 6
- 230000007510 mood change Effects 0.000 claims 6
- 235000020824 obesity Nutrition 0.000 claims 6
- 231100000872 sexual dysfunction Toxicity 0.000 claims 6
- 229940124011 Androgen receptor agonist Drugs 0.000 claims 4
- 229940123407 Androgen receptor antagonist Drugs 0.000 claims 4
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims 4
- 150000001204 N-oxides Chemical class 0.000 claims 4
- 208000004403 Prostatic Hyperplasia Diseases 0.000 claims 4
- 230000001270 agonistic effect Effects 0.000 claims 4
- 239000003936 androgen receptor antagonist Substances 0.000 claims 4
- 239000002775 capsule Substances 0.000 claims 4
- 239000006071 cream Substances 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 239000003937 drug carrier Substances 0.000 claims 4
- 239000000839 emulsion Substances 0.000 claims 4
- 239000012530 fluid Substances 0.000 claims 4
- 238000009472 formulation Methods 0.000 claims 4
- 239000000499 gel Substances 0.000 claims 4
- 150000004677 hydrates Chemical class 0.000 claims 4
- 238000004519 manufacturing process Methods 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 239000000243 solution Substances 0.000 claims 4
- 239000000829 suppository Substances 0.000 claims 4
- 239000000725 suspension Substances 0.000 claims 4
- 208000024891 symptom Diseases 0.000 claims 4
- 239000003826 tablet Substances 0.000 claims 4
- WSNMPAVSZJSIMT-UHFFFAOYSA-N COc1c(C)c2COC(=O)c2c(O)c1CC(O)C1(C)CCC(=O)O1 Chemical compound COc1c(C)c2COC(=O)c2c(O)c1CC(O)C1(C)CCC(=O)O1 WSNMPAVSZJSIMT-UHFFFAOYSA-N 0.000 claims 3
- 230000002401 inhibitory effect Effects 0.000 claims 3
- 206010020880 Hypertrophy Diseases 0.000 claims 2
- 230000005764 inhibitory process Effects 0.000 claims 2
- 230000003405 preventing effect Effects 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 230000001603 reducing effect Effects 0.000 claims 2
- 230000009467 reduction Effects 0.000 claims 2
- 208000001076 sarcopenia Diseases 0.000 claims 2
- 230000001629 suppression Effects 0.000 claims 2
- 101000685982 Homo sapiens NAD(+) hydrolase SARM1 Proteins 0.000 claims 1
- 102100023356 NAD(+) hydrolase SARM1 Human genes 0.000 claims 1
- 230000007423 decrease Effects 0.000 claims 1
- 0 C*C1C=CC(NC([C@](C)(C*c2ccc(*C)cc2)O)=O)=CC1* Chemical compound C*C1C=CC(NC([C@](C)(C*c2ccc(*C)cc2)O)=O)=CC1* 0.000 description 4
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP20020292606 EP1413306A1 (en) | 2002-10-21 | 2002-10-21 | Tetrahydroquinoline derivatives as CRTH2 antagonists |
| US43489602P | 2002-12-19 | 2002-12-19 | |
| PCT/IB2003/004505 WO2004035543A1 (en) | 2002-10-21 | 2003-10-10 | Tetrahydroquinoline derivatives as crth2 antagonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2006511486A JP2006511486A (ja) | 2006-04-06 |
| JP2006511486A5 true JP2006511486A5 (enExample) | 2006-08-17 |
Family
ID=32109153
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2004544591A Abandoned JP2006511486A (ja) | 2002-10-21 | 2003-10-10 | Ｃｒｔｈ２拮抗剤としてのテトラヒドロキノリン誘導体 |
Country Status (11)
| Country | Link |
|---|---|
| US (2) | US7220760B2 (enExample) |
| EP (1) | EP1556356B1 (enExample) |
| JP (1) | JP2006511486A (enExample) |
| AT (1) | ATE327977T1 (enExample) |
| AU (1) | AU2003269327A1 (enExample) |
| BR (1) | BR0315547A (enExample) |
| CA (1) | CA2500083A1 (enExample) |
| DE (1) | DE60305724T2 (enExample) |
| ES (1) | ES2263015T3 (enExample) |
| MX (1) | MXPA05003660A (enExample) |
| WO (1) | WO2004035543A1 (enExample) |
Families Citing this family (55)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA011385B1 (ru) * | 2002-10-04 | 2009-02-27 | Миллениум Фармасьютикалз, Инк. | Антагонисты рецептора pgd2 для лечения воспалительных заболеваний |
| US7504508B2 (en) | 2002-10-04 | 2009-03-17 | Millennium Pharmaceuticals, Inc. | PGD2 receptor antagonists for the treatment of inflammatory diseases |
| WO2004035543A1 (en) * | 2002-10-21 | 2004-04-29 | Warner-Lambert Company Llc | Tetrahydroquinoline derivatives as crth2 antagonists |
| EP1435356A1 (en) * | 2003-01-06 | 2004-07-07 | Warner-Lambert Company LLC | Quinoline derivatives as CRTH2 antagonists |
| AU2004253967B2 (en) | 2003-07-03 | 2010-02-18 | Cytovia, Inc. | 4-arylamino-quinazolines as activators of caspases and inducers of apoptosis |
| US8309562B2 (en) | 2003-07-03 | 2012-11-13 | Myrexis, Inc. | Compounds and therapeutical use thereof |
| US20050038070A1 (en) * | 2003-07-09 | 2005-02-17 | Amgen Inc. | Asthma and allergic inflammation modulators |
| AU2005229356B2 (en) | 2004-03-11 | 2011-06-09 | Idorsia Pharmaceuticals Ltd | Tetrahydropyridoindole derivatives |
| KR20070002085A (ko) * | 2004-04-07 | 2007-01-04 | 밀레니엄 파머슈티컬스 인코퍼레이티드 | 염증 질병을 치료하기 위한 ｐｇｄ２ 수용체 길항제 |
| WO2005102338A1 (en) * | 2004-04-20 | 2005-11-03 | Pfizer Limited | Method of treating neuropathic pain using a crth2 receptor antagonist |
| WO2006030826A1 (ja) | 2004-09-17 | 2006-03-23 | Eisai R & D Management Co., Ltd. | 医薬組成物 |
| US20060063803A1 (en) * | 2004-09-23 | 2006-03-23 | Pfizer Inc | 4-Amino substituted-2-substituted-1,2,3,4-tetrahydroquinoline compounds |
| EP1833482A4 (en) | 2005-01-03 | 2011-02-16 | Myriad Genetics Inc | COMPOUNDS AND ITS THERAPEUTIC USE |
| US8258145B2 (en) | 2005-01-03 | 2012-09-04 | Myrexis, Inc. | Method of treating brain cancer |
| ATE447572T1 (de) * | 2005-01-26 | 2009-11-15 | Hoffmann La Roche | Phenylmethanonderivate und ihre verwendung als glycin-transporter-1-hemmer |
| EP1861372A1 (en) | 2005-02-24 | 2007-12-05 | Millennium Pharmaceuticals, Inc. | Pgd2 receptor antagonists for the treatment of inflammatory diseases |
| ATE524182T1 (de) | 2005-04-21 | 2011-09-15 | Merck Serono Sa | 2,3-substituierte pyrazinsulfonamide als crth2- hemmer |
| MX2007014256A (es) | 2005-05-24 | 2008-03-26 | Serono Lab | Derivados espiro triciclicos como moduladores crth2. |
| DK2037967T3 (en) | 2006-06-16 | 2017-03-13 | Univ Pennsylvania | PROSTAGLANDIN-D2 RECEPTOR ANTAGONISTS FOR TREATMENT OF ANDROGENETIC ALOPECI |
| TW200831085A (en) * | 2006-12-13 | 2008-08-01 | Merck & Co Inc | Non-nucleoside reverse transcriptase inhibitors |
| JP5466507B2 (ja) | 2007-09-27 | 2014-04-09 | 興和株式会社 | テトラヒドロキノリン化合物を有効成分とする貧血の予防及び／又は治療剤 |
| DK2327693T3 (da) | 2007-12-14 | 2012-08-13 | Pulmagen Therapeutics Asthma Ltd | Indoler og terapeutisk anvendelse deraf |
| ES2566739T3 (es) | 2008-02-01 | 2016-04-15 | Brickell Biotech, Inc. | Aminoalquilbifenilo N,N-disustituidos antagonistas de receptores de prostaglandina D2 |
| WO2009108720A2 (en) | 2008-02-25 | 2009-09-03 | Amira Pharmaceuticals, Inc. | Antagonists of prostaglandin d2 receptors |
| AU2009224418B2 (en) * | 2008-03-11 | 2014-12-11 | Aska Pharmaceutical Co., Ltd. | Solid dispersion, pharmaceutical compositions containing the same, and processes for the production of both |
| GB2463788B (en) | 2008-09-29 | 2010-12-15 | Amira Pharmaceuticals Inc | Heteroaryl antagonists of prostaglandin D2 receptors |
| WO2010039977A2 (en) | 2008-10-01 | 2010-04-08 | Amira Pharmaceuticals, Inc. | Heteroaryl antagonists of prostaglandin d2 receptors |
| US8524748B2 (en) | 2008-10-08 | 2013-09-03 | Panmira Pharmaceuticals, Llc | Heteroalkyl biphenyl antagonists of prostaglandin D2 receptors |
| GB2465062B (en) | 2008-11-06 | 2011-04-13 | Amira Pharmaceuticals Inc | Cycloalkane(B)azaindole antagonists of prostaglandin D2 receptors |
| BRPI0921254A2 (pt) * | 2008-11-17 | 2018-10-23 | Hoffmann La Roche | acidos naftilacéticos |
| US8273769B2 (en) | 2009-02-12 | 2012-09-25 | Merck Serono Sa | Phenoxy acetic acid derivatives |
| US8791090B2 (en) | 2009-03-31 | 2014-07-29 | Kowa Company, Ltd. | Prophylactic and/or therapeutic agent for anemia comprising tetrahydroquinoline compound as active ingredient |
| WO2011014587A2 (en) | 2009-07-31 | 2011-02-03 | Amira Pharmaceuticals, Inc. | Ophthalmic pharmaceutical compositions of dp2 receptor antagonists |
| CA2768587A1 (en) | 2009-08-05 | 2011-02-10 | Panmira Pharmaceuticals, Llc | Dp2 antagonist and uses thereof |
| US20120077842A1 (en) * | 2009-08-19 | 2012-03-29 | Eisai R&D Management Co., Ltd. | Quinoline derivative-containing pharmaceutical composition |
| EP2590944B1 (en) | 2010-07-05 | 2015-09-30 | Actelion Pharmaceuticals Ltd. | 1-phenyl-substituted heterocyclyl derivatives and their use as prostaglandin d2 receptor modulators |
| CN103702985B (zh) * | 2010-12-23 | 2016-02-17 | 默沙东公司 | 作为crth2受体调节剂的喹喔啉和氮杂喹喔啉 |
| US9945862B2 (en) | 2011-06-03 | 2018-04-17 | Eisai R&D Management Co., Ltd. | Biomarkers for predicting and assessing responsiveness of thyroid and kidney cancer subjects to lenvatinib compounds |
| AR086931A1 (es) * | 2011-06-17 | 2014-01-29 | Merck Sharp & Dohme | Tetrahidroquinolinas condensadas con cicloalquilo como moduladores de receptores de crth |
| CN104114169A (zh) | 2011-12-16 | 2014-10-22 | 阿托佩斯治疗有限公司 | 用于治疗嗜酸细胞性食管炎的crth2拮抗剂和质子泵抑制剂的组合物 |
| US9255090B2 (en) | 2011-12-21 | 2016-02-09 | Actelion Pharmaceuticals Ltd. | Heterocyclyl derivatives and their use as prostaglandin D2 receptor modulators |
| CN108938441A (zh) | 2012-03-21 | 2018-12-07 | 宾夕法尼亚大学理事会 | 用于调节毛发生长的组合物和方法 |
| US9169270B2 (en) | 2012-07-05 | 2015-10-27 | Actelion Pharmaceuticals Ltd. | 1-phenyl-substituted heterocyclyl derivatives and their use as prostaglandin D2 receptor modulators |
| MX2015004979A (es) | 2012-12-21 | 2015-07-17 | Eisai R&D Man Co Ltd | Forma amorfa de derivado de quinolina y metodo para su produccion. |
| SG11201509278XA (en) | 2013-05-14 | 2015-12-30 | Eisai R&D Man Co Ltd | Biomarkers for predicting and assessing responsiveness of endometrial cancer subjects to lenvatinib compounds |
| IL302218B2 (en) | 2014-08-28 | 2024-10-01 | Eisai R&D Man Co Ltd | Methods for manufacturing high-purity lenvatinib and its derivatives |
| EP3256121B1 (en) | 2015-02-13 | 2024-08-07 | INSERM - Institut National de la Santé et de la Recherche Médicale | Ptgdr-1 and/or ptgdr-2 antagonists for preventing and/or treating systemic lupus erythematosus |
| JP6792546B2 (ja) | 2015-02-25 | 2020-11-25 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | キノリン誘導体の苦味抑制方法 |
| AU2015384801B2 (en) | 2015-03-04 | 2022-01-06 | Eisai R&D Management Co., Ltd. | Combination of a PD-1 antagonist and a VEGFR/FGFR/RET tyrosine kinase inhibitor for treating cancer |
| EP3311841B1 (en) | 2015-06-16 | 2021-07-28 | PRISM BioLab Co., Ltd. | Anticancer agent |
| US12201625B2 (en) | 2015-07-30 | 2025-01-21 | The Trustees Of The University Of Pennsylvania | Single nucleotide polymorphic alleles of human DP-2 gene for detection of susceptibility to hair growth inhibition by PGD2 |
| CN108135894B (zh) | 2015-08-20 | 2021-02-19 | 卫材R&D管理有限公司 | 肿瘤治疗剂 |
| RU2750539C2 (ru) | 2017-02-08 | 2021-06-29 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Фармацевтическая композиция для лечения опухоли |
| AU2018269996A1 (en) | 2017-05-16 | 2019-11-21 | Eisai R&D Management Co., Ltd. | Treatment of hepatocellular carcinoma |
| CN115947683B (zh) * | 2022-12-29 | 2025-08-05 | 湖南工程学院 | 一种四氢喹啉及其衍生物的合成方法 |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4521607A (en) * | 1981-02-27 | 1985-06-04 | Takeda Chemical Industries, Ltd. | Chromanyl glycines |
| DE69026708T2 (de) | 1989-10-20 | 1997-04-03 | Otsuka Pharma Co Ltd | Benzoheterozyklische verbindungen |
| US5753677A (en) * | 1989-10-20 | 1998-05-19 | Otsuka Pharmaceutical Co., Ltd. | Benzoheterocyclic compounds |
| US6168784B1 (en) * | 1997-09-03 | 2001-01-02 | Gryphon Sciences | N-terminal modifications of RANTES and methods of use |
| GT199900147A (es) * | 1998-09-17 | 1999-09-06 | 1, 2, 3, 4- tetrahidroquinolinas 2-sustituidas 4-amino sustituidas. | |
| US6197786B1 (en) * | 1998-09-17 | 2001-03-06 | Pfizer Inc | 4-Carboxyamino-2-substituted-1,2,3,4-tetrahydroquinolines |
| US6140342A (en) * | 1998-09-17 | 2000-10-31 | Pfizer Inc. | Oxy substituted 4-carboxyamino-2-methyl-1,2,3,4-tetrahydroquinolines |
| US6147090A (en) * | 1998-09-17 | 2000-11-14 | Pfizer Inc. | 4-carboxyamino-2-methyl-1,2,3,4,-tetrahydroquinolines |
| US6147089A (en) * | 1998-09-17 | 2000-11-14 | Pfizer Inc. | Annulated 4-carboxyamino-2-methyl-1,2,3,4,-tetrahydroquinolines |
| US6878522B2 (en) * | 2000-07-07 | 2005-04-12 | Baiyong Li | Methods for the identification of compounds useful for the treatment of disease states mediated by prostaglandin D2 |
| JP2002053557A (ja) | 2000-08-14 | 2002-02-19 | Japan Tobacco Inc | アポリポ蛋白ａ−ｉ産生促進薬 |
| SE0101161D0 (sv) | 2001-03-30 | 2001-03-30 | Astrazeneca Ab | New compounds |
| US20050228016A1 (en) | 2002-06-13 | 2005-10-13 | Enrique Michelotti | Tetrahydroquinolines for modulating the expression of exogenous genes via an ecdysone receptor complex |
| EA011385B1 (ru) * | 2002-10-04 | 2009-02-27 | Миллениум Фармасьютикалз, Инк. | Антагонисты рецептора pgd2 для лечения воспалительных заболеваний |
| WO2004035543A1 (en) * | 2002-10-21 | 2004-04-29 | Warner-Lambert Company Llc | Tetrahydroquinoline derivatives as crth2 antagonists |
| AU2003289207A1 (en) | 2002-12-06 | 2004-06-30 | Kyowa Hakko Kogyo Co., Ltd. | Anti-inflammatory agent |
| US20040204450A1 (en) * | 2003-03-28 | 2004-10-14 | Pfizer Inc | Quinoline and quinoxaline compounds |
| US20050038070A1 (en) * | 2003-07-09 | 2005-02-17 | Amgen Inc. | Asthma and allergic inflammation modulators |
| US20070149567A1 (en) * | 2004-09-23 | 2007-06-28 | Pfizer Inc | Quinoline compounds |
| US20060063803A1 (en) * | 2004-09-23 | 2006-03-23 | Pfizer Inc | 4-Amino substituted-2-substituted-1,2,3,4-tetrahydroquinoline compounds |
-
2003
- 2003-10-10 WO PCT/IB2003/004505 patent/WO2004035543A1/en not_active Ceased
- 2003-10-10 DE DE60305724T patent/DE60305724T2/de not_active Expired - Fee Related
- 2003-10-10 BR BR0315547-1A patent/BR0315547A/pt not_active IP Right Cessation
- 2003-10-10 AU AU2003269327A patent/AU2003269327A1/en not_active Abandoned
- 2003-10-10 MX MXPA05003660A patent/MXPA05003660A/es unknown
- 2003-10-10 ES ES03751107T patent/ES2263015T3/es not_active Expired - Lifetime
- 2003-10-10 JP JP2004544591A patent/JP2006511486A/ja not_active Abandoned
- 2003-10-10 EP EP03751107A patent/EP1556356B1/en not_active Expired - Lifetime
- 2003-10-10 AT AT03751107T patent/ATE327977T1/de not_active IP Right Cessation
- 2003-10-10 CA CA002500083A patent/CA2500083A1/en not_active Abandoned
- 2003-10-17 US US10/688,566 patent/US7220760B2/en not_active Expired - Fee Related
-
2007
- 2007-04-16 US US11/735,686 patent/US20070197587A1/en not_active Abandoned
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