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 (enExample) | 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 (enExample) |
| EP (1) | EP2632903A4 (enExample) |
| JP (1) | JP5921560B2 (enExample) |
| AU (1) | AU2011320565A1 (enExample) |
| CA (1) | CA2816088A1 (enExample) |
| WO (1) | WO2012058529A2 (enExample) |
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 |
| AU2013209516A1 (en) | 2012-01-20 | 2014-08-28 | Viamet Pharmaceuticals (NC), Inc. | Metalloenzyme inhibitor compounds |
| WO2014043376A1 (en) * | 2012-09-12 | 2014-03-20 | Dow Agrosciences Llc | Metalloenzyme inhibitor compounds |
| US20160022606A1 (en) * | 2013-03-14 | 2016-01-28 | Pellficure Pharmaceuticals Inc. | Novel therapy for prostate carcinoma |
| WO2015160664A1 (en) * | 2014-04-15 | 2015-10-22 | Dow Agrosciences Llc | Metalloenzyme inhibitor compounds as fungicides |
| JP2017513848A (ja) * | 2014-04-15 | 2017-06-01 | 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 |
| ES2970715T3 (es) | 2016-12-22 | 2024-05-30 | Prec Pharmaceuticals Inc | Composiciones y métodos para inhibir la actividad de la arginasa |
| 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 |
|---|---|---|---|---|
| US4921475A (en) | 1983-08-18 | 1990-05-01 | Drug Delivery Systems Inc. | Transdermal drug patch with microtubes |
| US5087240A (en) | 1983-08-18 | 1992-02-11 | Drug Delivery Systems Inc. | Transdermal drug patch with conductive fibers |
| 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 |
| ATE107176T1 (de) | 1989-12-04 | 1994-07-15 | Searle & Co | System zur transdermalen albuterol applikation. |
| US5077033A (en) | 1990-08-07 | 1991-12-31 | Mediventures Inc. | Ophthalmic drug delivery with thermo-irreversible gels of polxoxyalkylene polymer and ionic polysaccharide |
| EP0495421B1 (en) | 1991-01-15 | 1996-08-21 | Alcon Laboratories, Inc. | Use of carrageenans in topical ophthalmic compositions |
| US5352456A (en) | 1991-10-10 | 1994-10-04 | Cygnus Therapeutic Systems | Device for administering drug transdermally which provides an initial pulse of drug |
| JPH07502219A (ja) | 1991-12-18 | 1995-03-09 | ミネソタ マイニング アンド マニュファクチャリング カンパニー | 多重層型バリアー構造体 |
| ATE132381T1 (de) | 1992-01-29 | 1996-01-15 | Voelkl Franz Ski | 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 |
| WO2003027095A1 (en) * | 2001-09-26 | 2003-04-03 | Bayer Pharmaceuticals Corporation | Substituted 3-pyridyl tetrazoles as steroid c17,20 lyase inhibitors |
| GB0127557D0 (en) | 2001-11-16 | 2002-01-09 | Syngenta Participations Ag | Organic compounds |
| DE602004019193D1 (de) * | 2003-03-11 | 2009-03-12 | 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 |
| KR101391900B1 (ko) | 2005-12-13 | 2014-05-02 | 인사이트 코포레이션 | 야누스 키나아제 억제제로서의 헤테로아릴 치환된 피롤로［2,3-ｂ］피리딘 및 피롤로［2,3-ｂ］피리미딘 |
| HRP20151398T1 (hr) * | 2006-12-22 | 2016-02-12 | Astex Therapeutics Limited | Tricikliäśni derivati amina kao inhibitori protein tirozin kinaze |
| JP5492075B2 (ja) * | 2007-05-23 | 2014-05-14 | アラーガン インコーポレイテッド | アドレナリンレセプター作用薬としての（（二環式ヘテロアリール）イミダゾリル）メチルヘテロアリール化合物 |
| US8143280B2 (en) | 2007-09-27 | 2012-03-27 | Hoffmann-La Roche Inc. | Glucocorticoid receptor antagonists |
| US20110015158A1 (en) | 2007-12-11 | 2011-01-20 | Viamet Pharmaceuticals, Inc. | Metalloenzyme inhibitors using metal binding moieties in combination with targeting moieties |
| WO2010127177A1 (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 AU AU2011320565A patent/AU2011320565A1/en not_active Abandoned
- 2011-10-28 EP EP11837150.9A patent/EP2632903A4/en not_active Withdrawn
- 2011-10-28 US US13/882,443 patent/US9056855B2/en not_active Expired - Fee Related
- 2011-10-28 WO PCT/US2011/058274 patent/WO2012058529A2/en not_active Ceased
- 2011-10-28 CA CA2816088A patent/CA2816088A1/en not_active Abandoned
- 2011-10-28 JP JP2013536866A patent/JP5921560B2/ja not_active Expired - Fee Related
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