JP2014500864A5 - - Google Patents
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- Publication number
- JP2014500864A5 JP2014500864A5 JP2013536866A JP2013536866A JP2014500864A5 JP 2014500864 A5 JP2014500864 A5 JP 2014500864A5 JP 2013536866 A JP2013536866 A JP 2013536866A JP 2013536866 A JP2013536866 A JP 2013536866A JP 2014500864 A5 JP2014500864 A5 JP 2014500864A5
- Authority
- JP
- Japan
- Prior art keywords
- disease
- compound
- optionally substituted
- agent
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 24
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 11
- 201000010099 disease Diseases 0.000 claims 8
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 239000003795 chemical substances by application Substances 0.000 claims 5
- 210000003169 central nervous system Anatomy 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 125000001624 naphthyl group Chemical group 0.000 claims 4
- 125000003107 substituted aryl group Chemical group 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 239000003098 androgen Substances 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 208000035475 disorder Diseases 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- 125000000547 substituted alkyl group Chemical group 0.000 claims 3
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 208000018522 Gastrointestinal disease Diseases 0.000 claims 2
- 208000012931 Urologic disease Diseases 0.000 claims 2
- 206010046798 Uterine leiomyoma Diseases 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 239000002246 antineoplastic agent Substances 0.000 claims 2
- 229940127089 cytotoxic agent Drugs 0.000 claims 2
- 230000001419 dependent effect Effects 0.000 claims 2
- 208000010643 digestive system disease Diseases 0.000 claims 2
- 208000016097 disease of metabolism Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 208000018685 gastrointestinal system disease Diseases 0.000 claims 2
- 150000004677 hydrates Chemical class 0.000 claims 2
- 201000010066 hyperandrogenism Diseases 0.000 claims 2
- 208000030159 metabolic disease Diseases 0.000 claims 2
- 239000000651 prodrug Substances 0.000 claims 2
- 229940002612 prodrug Drugs 0.000 claims 2
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- 208000014001 urinary system disease Diseases 0.000 claims 2
- RBYAUFGMTNJMOR-UHFFFAOYSA-N 1-(6,7-dimethoxynaphthalen-2-yl)-2-methyl-1-pyrimidin-4-ylpropan-1-ol Chemical compound C1=C2C=C(OC)C(OC)=CC2=CC=C1C(O)(C(C)C)C1=CC=NC=N1 RBYAUFGMTNJMOR-UHFFFAOYSA-N 0.000 claims 1
- KQHINUMYUSHNFQ-UHFFFAOYSA-N 1-[6-(difluoromethoxy)-5-(trifluoromethyl)quinolin-2-yl]-2-methyl-1-pyrimidin-4-ylpropan-1-ol Chemical compound C=1C=C2C(C(F)(F)F)=C(OC(F)F)C=CC2=NC=1C(O)(C(C)C)C1=CC=NC=N1 KQHINUMYUSHNFQ-UHFFFAOYSA-N 0.000 claims 1
- DPDJCBFXTGUXDE-UHFFFAOYSA-N 1-[6-(difluoromethoxy)-5-thiophen-2-ylquinolin-2-yl]-2-methyl-1-pyrimidin-4-ylpropan-1-ol Chemical compound C=1C=C2C(C=3SC=CC=3)=C(OC(F)F)C=CC2=NC=1C(O)(C(C)C)C1=CC=NC=N1 DPDJCBFXTGUXDE-UHFFFAOYSA-N 0.000 claims 1
- DZZCPVWGUSOPGH-UHFFFAOYSA-N 1-[6-(difluoromethoxy)quinolin-2-yl]-2-methyl-1-pyrimidin-4-ylpropan-1-ol Chemical compound C=1C=C2C=C(OC(F)F)C=CC2=NC=1C(O)(C(C)C)C1=CC=NC=N1 DZZCPVWGUSOPGH-UHFFFAOYSA-N 0.000 claims 1
- XFYFDUFRMKIUBX-UHFFFAOYSA-N 1-[6-chloro-5-(trifluoromethyl)quinolin-2-yl]-2-methyl-1-pyrimidin-4-ylpropan-1-ol Chemical compound C=1C=C2C(C(F)(F)F)=C(Cl)C=CC2=NC=1C(O)(C(C)C)C1=CC=NC=N1 XFYFDUFRMKIUBX-UHFFFAOYSA-N 0.000 claims 1
- QOJFKGAOIAZZGS-UHFFFAOYSA-N 2-methyl-1-(6-methylsulfanylquinolin-2-yl)-1-pyrimidin-4-ylpropan-1-ol Chemical compound C1=CC2=CC(SC)=CC=C2N=C1C(O)(C(C)C)C1=CC=NC=N1 QOJFKGAOIAZZGS-UHFFFAOYSA-N 0.000 claims 1
- YZOPOQGEOGOYFX-UHFFFAOYSA-N 2-methyl-1-pyrimidin-4-yl-1-[6-(trifluoromethoxy)quinolin-2-yl]propan-1-ol Chemical compound C=1C=C2C=C(OC(F)(F)F)C=CC2=NC=1C(O)(C(C)C)C1=CC=NC=N1 YZOPOQGEOGOYFX-UHFFFAOYSA-N 0.000 claims 1
- SYDJCZOYFHFFNO-UHFFFAOYSA-N 2-methyl-1-pyrimidin-4-yl-1-[6-thiophen-2-yl-5-(trifluoromethyl)quinolin-2-yl]propan-1-ol Chemical compound C=1C=C2C(C(F)(F)F)=C(C=3SC=CC=3)C=CC2=NC=1C(O)(C(C)C)C1=CC=NC=N1 SYDJCZOYFHFFNO-UHFFFAOYSA-N 0.000 claims 1
- 208000002874 Acne Vulgaris Diseases 0.000 claims 1
- 201000004384 Alopecia Diseases 0.000 claims 1
- 201000005670 Anovulation Diseases 0.000 claims 1
- 206010002659 Anovulatory cycle Diseases 0.000 claims 1
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 208000008448 Congenital adrenal hyperplasia Diseases 0.000 claims 1
- 208000017701 Endocrine disease Diseases 0.000 claims 1
- 201000009273 Endometriosis Diseases 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- 206010017533 Fungal infection Diseases 0.000 claims 1
- 206010020112 Hirsutism Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000031888 Mycoses Diseases 0.000 claims 1
- 208000010195 Onychomycosis Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000004403 Prostatic Hyperplasia Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 1
- 206010000496 acne Diseases 0.000 claims 1
- 230000001919 adrenal effect Effects 0.000 claims 1
- 210000004100 adrenal gland Anatomy 0.000 claims 1
- 239000000556 agonist Substances 0.000 claims 1
- 206010068168 androgenetic alopecia Diseases 0.000 claims 1
- 201000002996 androgenic alopecia Diseases 0.000 claims 1
- 239000004037 angiogenesis inhibitor Substances 0.000 claims 1
- 231100000552 anovulation Toxicity 0.000 claims 1
- 239000002260 anti-inflammatory agent Substances 0.000 claims 1
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 1
- 239000003429 antifungal agent Substances 0.000 claims 1
- 229940121375 antifungal agent Drugs 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- 208000030270 breast disease Diseases 0.000 claims 1
- YDVJBLJCSLVMSY-UHFFFAOYSA-N carbamoyl cyanide Chemical compound NC(=O)C#N YDVJBLJCSLVMSY-UHFFFAOYSA-N 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 230000001054 cortical effect Effects 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 239000002254 cytotoxic agent Substances 0.000 claims 1
- 231100000599 cytotoxic agent Toxicity 0.000 claims 1
- 125000004663 dialkyl amino group Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000002526 effect on cardiovascular system Effects 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 208000030172 endocrine system disease Diseases 0.000 claims 1
- 239000000262 estrogen Substances 0.000 claims 1
- 229940011871 estrogen Drugs 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 125000004428 fluoroalkoxy group Chemical group 0.000 claims 1
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 1
- 230000002538 fungal effect Effects 0.000 claims 1
- 125000004438 haloalkoxy group Chemical group 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 208000000509 infertility Diseases 0.000 claims 1
- 231100000535 infertility Toxicity 0.000 claims 1
- 230000036512 infertility Effects 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 201000010260 leiomyoma Diseases 0.000 claims 1
- -1 monoalkylamino Chemical group 0.000 claims 1
- 230000002611 ovarian Effects 0.000 claims 1
- 201000010065 polycystic ovary syndrome Diseases 0.000 claims 1
- 208000006155 precocious puberty Diseases 0.000 claims 1
- 230000002028 premature Effects 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 201000004240 prostatic hypertrophy Diseases 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 230000009885 systemic effect Effects 0.000 claims 1
- 201000005882 tinea unguium Diseases 0.000 claims 1
- 206010046766 uterine cancer Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US40778010P | 2010-10-28 | 2010-10-28 | |
| US61/407,780 | 2010-10-28 | ||
| PCT/US2011/058274 WO2012058529A2 (en) | 2010-10-28 | 2011-10-28 | Metalloenzyme inhibitor compounds |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014500864A JP2014500864A (ja) | 2014-01-16 |
| JP2014500864A5 true JP2014500864A5 (https=) | 2014-12-18 |
| JP5921560B2 JP5921560B2 (ja) | 2016-05-24 |
Family
ID=45994792
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013536866A Expired - Fee Related JP5921560B2 (ja) | 2010-10-28 | 2011-10-28 | 金属酵素阻害化合物 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US9056855B2 (https=) |
| EP (1) | EP2632903A4 (https=) |
| JP (1) | JP5921560B2 (https=) |
| AU (1) | AU2011320565A1 (https=) |
| CA (1) | CA2816088A1 (https=) |
| WO (1) | WO2012058529A2 (https=) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101823275B1 (ko) | 2010-08-04 | 2018-03-08 | 펠피큐어 파마슈티걸즈 아이엔씨 | 전립선 암종의 치료를 위한 병용 요법 |
| ES2774267T3 (es) * | 2012-01-20 | 2020-07-20 | Mycovia Pharmaceuticals Inc | Compuestos inhibidores de metaloenzimas |
| US20150246898A1 (en) * | 2012-09-12 | 2015-09-03 | Dow Agrosciences Llc | Metalloenzyme inhibitor compounds |
| EP2968219B1 (en) * | 2013-03-14 | 2019-04-24 | Pellficure Pharmaceuticals, Inc. | Novel therapy for prostate carcinoma |
| US9944664B2 (en) * | 2014-04-15 | 2018-04-17 | Dow Agrosciences Llc | Metalloenzyme inhibitor compounds as fungicides |
| JP6532480B2 (ja) * | 2014-04-15 | 2019-06-19 | ダウ アグロサイエンシィズ エルエルシー | 殺真菌剤としての金属酵素阻害剤化合物 |
| SMT202100573T1 (it) | 2016-12-22 | 2021-11-12 | Calithera Biosciences Inc | Composizioni e metodi per l'inibizione dell'attivita' dell'arginasi |
| CN110256342B (zh) * | 2019-07-16 | 2022-06-07 | 河南省科学院化学研究所有限公司 | 一种2-氰基喹啉衍生物的合成方法 |
Family Cites Families (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5087240A (en) | 1983-08-18 | 1992-02-11 | Drug Delivery Systems Inc. | Transdermal drug patch with conductive fibers |
| US4921475A (en) | 1983-08-18 | 1990-05-01 | Drug Delivery Systems Inc. | Transdermal drug patch with microtubes |
| US4738851A (en) | 1985-09-27 | 1988-04-19 | University Of Iowa Research Foundation, Inc. | Controlled release ophthalmic gel formulation |
| US5163899A (en) | 1987-03-20 | 1992-11-17 | Drug Delivery Systems Inc. | Transdermal drug delivery system |
| US5312325A (en) | 1987-05-28 | 1994-05-17 | Drug Delivery Systems Inc | Pulsating transdermal drug delivery system |
| GB8804164D0 (en) | 1988-02-23 | 1988-03-23 | Tucker J M | Bandage for administering physiologically active compound |
| US4882150A (en) | 1988-06-03 | 1989-11-21 | Kaufman Herbert E | Drug delivery system |
| GB8819308D0 (en) | 1988-08-13 | 1988-09-14 | Pfizer Ltd | Triazole antifungal agents |
| US5008110A (en) | 1988-11-10 | 1991-04-16 | The Procter & Gamble Company | Storage-stable transdermal patch |
| US5088977A (en) | 1988-12-21 | 1992-02-18 | Drug Delivery Systems Inc. | Electrical transdermal drug applicator with counteractor and method of drug delivery |
| US5521222A (en) | 1989-09-28 | 1996-05-28 | Alcon Laboratories, Inc. | Topical ophthalmic pharmaceutical vehicles |
| EP0431519B1 (en) | 1989-12-04 | 1994-06-15 | G.D. Searle & Co. | System for transdermal albuterol administration |
| US5077033A (en) | 1990-08-07 | 1991-12-31 | Mediventures Inc. | Ophthalmic drug delivery with thermo-irreversible gels of polxoxyalkylene polymer and ionic polysaccharide |
| ATE141502T1 (de) | 1991-01-15 | 1996-09-15 | Alcon Lab Inc | Verwendung von karrageenan in topischen ophthalmologischen zusammensetzungen |
| US5352456A (en) | 1991-10-10 | 1994-10-04 | Cygnus Therapeutic Systems | Device for administering drug transdermally which provides an initial pulse of drug |
| DE69228827T2 (de) | 1991-12-18 | 1999-10-21 | Minnesota Mining And Mfg. Co., Saint Paul | Mehrschichtige sperrstrukturen |
| EP0553769B1 (de) | 1992-01-29 | 1996-01-03 | FRANZ VÖLKL GmbH & CO. SKI UND TENNIS SPORTARTIKELFABRIK KG | Ballspielschläger, insbesondere Tennisschläger |
| IL114193A (en) | 1994-06-20 | 2000-02-29 | Teva Pharma | Ophthalmic pharmaceutical compositions based on sodium alginate |
| ES2094688B1 (es) | 1994-08-08 | 1997-08-01 | Cusi Lab | Manoemulsion del tipo de aceite en agua, util como vehiculo oftalmico y procedimiento para su preparacion. |
| EP0823423B1 (en) * | 1995-04-28 | 2004-06-16 | Banyu Pharmaceutical Co., Ltd. | 1,4-disubstituted piperidine derivatives |
| US5837719A (en) | 1995-08-10 | 1998-11-17 | Merck & Co., Inc. | 2,5-substituted aryl pyrroles, compositions containing such compounds and methods of use |
| IT1283911B1 (it) | 1996-02-05 | 1998-05-07 | Farmigea Spa | Soluzioni oftalmiche viscosizzate con polisaccaridi della gomma di tamarindo |
| US5800807A (en) | 1997-01-29 | 1998-09-01 | Bausch & Lomb Incorporated | Ophthalmic compositions including glycerin and propylene glycol |
| US6261547B1 (en) | 1998-04-07 | 2001-07-17 | Alcon Manufacturing, Ltd. | Gelling ophthalmic compositions containing xanthan gum |
| US6197934B1 (en) | 1998-05-22 | 2001-03-06 | Collagenesis, Inc. | Compound delivery using rapidly dissolving collagen film |
| CA2461363A1 (en) * | 2001-09-26 | 2003-04-03 | Bayer Pharmaceuticals Corporation | Substituted 3-pyridyl indoles and indazoles as c17,20 lyase inhibitors |
| GB0127557D0 (en) | 2001-11-16 | 2002-01-09 | Syngenta Participations Ag | Organic compounds |
| ATE421324T1 (de) * | 2003-03-11 | 2009-02-15 | Novartis Ag | Verwendung von isochinolin-derivaten zur behandlung von krebs und erkrankungen im zusammenhang mit map kinase |
| CN1993348A (zh) * | 2004-07-29 | 2007-07-04 | 默克公司 | 钾通道抑制剂 |
| EP2455382B1 (en) | 2005-12-13 | 2016-10-26 | Incyte Holdings Corporation | Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors |
| CN101679409B (zh) * | 2006-12-22 | 2014-11-26 | Astex治疗学有限公司 | 双环杂环衍生化合物、其医药组合物和其用途 |
| WO2008147786A1 (en) * | 2007-05-23 | 2008-12-04 | Allergan, Inc. | ((bicylicheteroaryl) imidazolyl) methylheteroaryl compounds as adrenergic receptor agonists |
| US8143280B2 (en) * | 2007-09-27 | 2012-03-27 | Hoffmann-La Roche Inc. | Glucocorticoid receptor antagonists |
| JP2011517313A (ja) | 2007-12-11 | 2011-06-02 | ビアメト ファーマシューティカルズ，インク． | 金属結合部分を標的化部分と組み合わせて使用する金属酵素阻害剤 |
| CA2760541A1 (en) * | 2009-04-29 | 2010-11-04 | Medivation Technologies, Inc. | Pyrido[4,3-b] indoles and methods of use |
| DE102009060174A1 (de) * | 2009-12-23 | 2011-06-30 | Merck Patent GmbH, 64293 | Pyrrolopyridinyl-pyrimidin-2-yl-amin-derivate |
-
2011
- 2011-10-28 US US13/882,443 patent/US9056855B2/en not_active Expired - Fee Related
- 2011-10-28 JP JP2013536866A patent/JP5921560B2/ja not_active Expired - Fee Related
- 2011-10-28 EP EP11837150.9A patent/EP2632903A4/en not_active Withdrawn
- 2011-10-28 WO PCT/US2011/058274 patent/WO2012058529A2/en not_active Ceased
- 2011-10-28 AU AU2011320565A patent/AU2011320565A1/en not_active Abandoned
- 2011-10-28 CA CA2816088A patent/CA2816088A1/en not_active Abandoned
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