CN103764641B - 部分饱和的三环化合物及其制备和使用方法 - Google Patents
部分饱和的三环化合物及其制备和使用方法 Download PDFInfo
- Publication number
- CN103764641B CN103764641B CN201280033359.8A CN201280033359A CN103764641B CN 103764641 B CN103764641 B CN 103764641B CN 201280033359 A CN201280033359 A CN 201280033359A CN 103764641 B CN103764641 B CN 103764641B
- Authority
- CN
- China
- Prior art keywords
- chromene
- carboxylic acid
- 7bsr
- 1ars
- tetrahydrocyclopropane
- 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.)
- Expired - Fee Related
Links
- 0 CC1(*)C=COCC1(*)* Chemical compound CC1(*)C=COCC1(*)* 0.000 description 11
- XISZPNMGFHMQON-UHFFFAOYSA-N CC(C)(C)OC(N(C(OC(C)(C)C)=O)c1c(C(OC)=O)c(OSc2ccc(C)cc2)ccc1)=O Chemical compound CC(C)(C)OC(N(C(OC(C)(C)C)=O)c1c(C(OC)=O)c(OSc2ccc(C)cc2)ccc1)=O XISZPNMGFHMQON-UHFFFAOYSA-N 0.000 description 1
- YQWJXKXYDUNPGP-UHFFFAOYSA-N CC(C)(C)OC(N(C1)CC1c1cccc(F)c1)=O Chemical compound CC(C)(C)OC(N(C1)CC1c1cccc(F)c1)=O YQWJXKXYDUNPGP-UHFFFAOYSA-N 0.000 description 1
- XNDNBWFUKMQQCX-UHFFFAOYSA-N CC(C)(C)OC(N(CC1)CC1OCC(C(C=C1)S(Cl)(=O)=O)C=C1F)=O Chemical compound CC(C)(C)OC(N(CC1)CC1OCC(C(C=C1)S(Cl)(=O)=O)C=C1F)=O XNDNBWFUKMQQCX-UHFFFAOYSA-N 0.000 description 1
- MJIKMYJGZCZECP-KHSQXAGFSA-N CC(C)(C)O[IH](N(CC1)C[C@@H]1OCc(cc(cc1)F)c1S(N(C)c1c(C(OC)=O)c(OC[C@H]2[C@@H]3C2)c3cc1)=O)=O Chemical compound CC(C)(C)O[IH](N(CC1)C[C@@H]1OCc(cc(cc1)F)c1S(N(C)c1c(C(OC)=O)c(OC[C@H]2[C@@H]3C2)c3cc1)=O)=O MJIKMYJGZCZECP-KHSQXAGFSA-N 0.000 description 1
- NLVOJIKOULHWIP-UHFFFAOYSA-N CC1CC(F)=CC(CN(C)C(C(F)(F)F)=O)=C(C)C1 Chemical compound CC1CC(F)=CC(CN(C)C(C(F)(F)F)=O)=C(C)C1 NLVOJIKOULHWIP-UHFFFAOYSA-N 0.000 description 1
- OFPPJOSAYFDRFK-CLFYSBASSA-M CCN(C)C/C=C\c(cccc1)c1S([N-]c1ccc(C(C2)C2CO2)c2c1C(OC)=O)(=O)=O Chemical compound CCN(C)C/C=C\c(cccc1)c1S([N-]c1ccc(C(C2)C2CO2)c2c1C(OC)=O)(=O)=O OFPPJOSAYFDRFK-CLFYSBASSA-M 0.000 description 1
- ZTMVHLCRBRHLGA-WAYWQWQTSA-N CCN(CC)C/C=C\c1c(CNC2=CCC(C(C3CO4)C3(F)F)C4=C2C(O)=O)ccc(F)c1 Chemical compound CCN(CC)C/C=C\c1c(CNC2=CCC(C(C3CO4)C3(F)F)C4=C2C(O)=O)ccc(F)c1 ZTMVHLCRBRHLGA-WAYWQWQTSA-N 0.000 description 1
- YTPCLGSFCBHDBZ-GYWYDZQHSA-N CCN(CC1)CC1C(C)CCC(C/C(/C=C(\C)/F)=C(/C)\S(CNc1c(C2=[O][C@H]2O)c(OCC2C3C2)c3cc1)=N)=O Chemical compound CCN(CC1)CC1C(C)CCC(C/C(/C=C(\C)/F)=C(/C)\S(CNc1c(C2=[O][C@H]2O)c(OCC2C3C2)c3cc1)=N)=O YTPCLGSFCBHDBZ-GYWYDZQHSA-N 0.000 description 1
- GOLVGZOPWLLUSF-LURJTMIESA-N CCN(CC1)C[C@H]1N Chemical compound CCN(CC1)C[C@H]1N GOLVGZOPWLLUSF-LURJTMIESA-N 0.000 description 1
- PKJXIIULUVRYOL-UHFFFAOYSA-N CCN1CC(CN(C(O)OC(C)C(C)C)C(OC(C)(C)C)=O)C1 Chemical compound CCN1CC(CN(C(O)OC(C)C(C)C)C(OC(C)(C)C)=O)C1 PKJXIIULUVRYOL-UHFFFAOYSA-N 0.000 description 1
- QKMYEKUXLYPHBG-MRVPVSSYSA-N CCN1C[C@H](CC#N)CC1 Chemical compound CCN1C[C@H](CC#N)CC1 QKMYEKUXLYPHBG-MRVPVSSYSA-N 0.000 description 1
- OSDOHDPAFPNPCV-WAYWQWQTSA-N CCNC/C=C\c(cc(cc1)F)c1S(NC(C1C(OC)=O)=CC=C2C1(C)OCC1C2C1)(=O)=O Chemical compound CCNC/C=C\c(cc(cc1)F)c1S(NC(C1C(OC)=O)=CC=C2C1(C)OCC1C2C1)(=O)=O OSDOHDPAFPNPCV-WAYWQWQTSA-N 0.000 description 1
- DFQBLAFVPCPNRJ-YBUBMKCBSA-N CC[N-](CCC1)[C@H]1C(N(C)Cc(cc(cc1)F)c1S([C@@H](C)c1c(C(O)=O)c(OCC2C3C2)c3cc1)(=C)=O)=O Chemical compound CC[N-](CCC1)[C@H]1C(N(C)Cc(cc(cc1)F)c1S([C@@H](C)c1c(C(O)=O)c(OCC2C3C2)c3cc1)(=C)=O)=O DFQBLAFVPCPNRJ-YBUBMKCBSA-N 0.000 description 1
- URAOWNSMLORSRE-UHFFFAOYSA-N Cc1c(C2C(CO)C2)ccc(N)c1C(OC)=O Chemical compound Cc1c(C2C(CO)C2)ccc(N)c1C(OC)=O URAOWNSMLORSRE-UHFFFAOYSA-N 0.000 description 1
- ZXAPMANOWGBURM-UHFFFAOYSA-N Fc1cc(CC2CCNCC2)ccc1 Chemical compound Fc1cc(CC2CCNCC2)ccc1 ZXAPMANOWGBURM-UHFFFAOYSA-N 0.000 description 1
- FQVVJFIHGLIEBJ-UHFFFAOYSA-N O=C(c1ccccc1S(Cl)(=O)=O)Cl Chemical compound O=C(c1ccccc1S(Cl)(=O)=O)Cl FQVVJFIHGLIEBJ-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
- C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D311/94—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems condensed with rings other than six-membered or with ring systems containing such rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4355—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having oxygen as a ring hetero atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
- C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
- C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/04—Ortho-condensed systems
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Cardiology (AREA)
- Child & Adolescent Psychology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Pyrane Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161483257P | 2011-05-06 | 2011-05-06 | |
| US61/483,257 | 2011-05-06 | ||
| US201161559856P | 2011-11-15 | 2011-11-15 | |
| US61/559,856 | 2011-11-15 | ||
| PCT/US2012/036789 WO2012154676A1 (en) | 2011-05-06 | 2012-05-07 | Partially saturated tricyclic compounds and methods of making and using same |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103764641A CN103764641A (zh) | 2014-04-30 |
| CN103764641B true CN103764641B (zh) | 2016-10-26 |
Family
ID=46147038
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201280033359.8A Expired - Fee Related CN103764641B (zh) | 2011-05-06 | 2012-05-07 | 部分饱和的三环化合物及其制备和使用方法 |
Country Status (14)
| Country | Link |
|---|---|
| US (3) | US9290472B2 (enExample) |
| EP (1) | EP2705030B1 (enExample) |
| JP (1) | JP6062423B2 (enExample) |
| KR (1) | KR101979039B1 (enExample) |
| CN (1) | CN103764641B (enExample) |
| AU (1) | AU2012253757B2 (enExample) |
| BR (1) | BR112013028534A2 (enExample) |
| CA (1) | CA2835261C (enExample) |
| EA (1) | EA025526B1 (enExample) |
| IL (1) | IL229246A (enExample) |
| MX (1) | MX345535B (enExample) |
| PH (1) | PH12013502261A1 (enExample) |
| SG (1) | SG194812A1 (enExample) |
| WO (1) | WO2012154676A1 (enExample) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010065877A2 (en) | 2008-12-04 | 2010-06-10 | Zafgen Corporation | Methods of treating an overweight or obese subject |
| WO2010065883A2 (en) | 2008-12-04 | 2010-06-10 | Zafgen Corporation | Method of treating an overweight or obese subject |
| MX337575B (es) | 2009-10-09 | 2016-03-10 | Zafgen Corp | Compuestos de sulfona y métodos para lafabricación y uso de éstos. |
| US8772333B2 (en) | 2010-01-08 | 2014-07-08 | Zafgen, Inc. | Fumigillol type compounds and methods of making and using same |
| WO2011085198A1 (en) | 2010-01-08 | 2011-07-14 | Zafgen Corporation | Metap-2 inhibitor for use in treating benign prostatic hypertrophy (bph) |
| WO2011127304A2 (en) | 2010-04-07 | 2011-10-13 | Zafgen Corporation | Methods of treating an overweight subject |
| WO2012012642A1 (en) | 2010-07-22 | 2012-01-26 | Zafgen Corporation | Tricyclic compounds and methds of making and using same |
| WO2012051318A1 (en) | 2010-10-12 | 2012-04-19 | Zafgen Corporation | Sulphonamide compounds and methods of making and using same |
| BR112013013411A2 (pt) | 2010-11-29 | 2016-09-13 | Zafgen Inc | tratamento de obesidade usando administração não diária de 6-0-(4-dimetilaminoetxi) cinamoil fumagilol |
| CN103402989B (zh) | 2011-01-26 | 2016-04-06 | 扎夫根股份有限公司 | 四唑化合物及其制备和使用方法 |
| EP2683706B1 (en) | 2011-03-08 | 2018-02-21 | Zafgen, Inc. | Oxaspiro [2.5]octane derivatives and analogs |
| KR20140040739A (ko) | 2011-05-06 | 2014-04-03 | 자프겐 인크. | 삼환식 피라졸 설폰아마이드 화합물 그리고 그의 제조방법 및 그를 이용하는 방법 |
| BR112013028665A2 (pt) | 2011-05-06 | 2016-09-06 | Zafgen Inc | compostos de sulfonamida tricíclicos e métodos para fazer e usar os mesmos |
| WO2012154676A1 (en) | 2011-05-06 | 2012-11-15 | Zafgen Corporation | Partially saturated tricyclic compounds and methods of making and using same |
| EP2763671A2 (en) | 2011-10-03 | 2014-08-13 | Zafgen, Inc. | Methods of treating age related disorders |
| MX2014008706A (es) | 2012-01-18 | 2015-03-05 | Zafgen Inc | Compuestos tricíclicos de sulfonamida y métodos para elaborarlos y usarlos. |
| BR112014017780A8 (pt) * | 2012-01-18 | 2017-07-11 | Zafgen Inc | Compostos de sulfona tricíclicos e métodos para fazer e usar os mesmos |
| EP2846792B1 (en) | 2012-05-08 | 2018-08-15 | Zafgen, Inc. | Treating hypothalamic obesity with metap2 inhibitors |
| JP6177888B2 (ja) | 2012-05-09 | 2017-08-09 | ザフゲン,インコーポレイテッド | フマギロール型化合物ならびにその製造および使用方法 |
| US9868717B2 (en) | 2012-11-05 | 2018-01-16 | Zafgen, Inc. | Tricyclic sulphonamide compounds and methods of making and using same |
| JP6169716B2 (ja) * | 2012-11-05 | 2017-07-26 | ザフゲン,インコーポレイテッド | 肝疾患を治療する方法 |
| WO2014071363A1 (en) * | 2012-11-05 | 2014-05-08 | Zafgen, Inc. | Tricyclic compounds and methods of making and using same |
| US9597309B2 (en) | 2013-03-14 | 2017-03-21 | Zafgen, Inc. | Methods of treating renal disease and other disorders |
| CN106432255A (zh) | 2015-08-11 | 2017-02-22 | 扎夫根公司 | 烟曲霉素醇螺环化合物和制备和使用其的方法 |
| AR105671A1 (es) | 2015-08-11 | 2017-10-25 | Zafgen Inc | Compuestos heterocíclicos de fumagillol y sus métodos de elaboración y uso |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010065883A2 (en) * | 2008-12-04 | 2010-06-10 | Zafgen Corporation | Method of treating an overweight or obese subject |
Family Cites Families (100)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5164410A (en) | 1988-01-09 | 1992-11-17 | Takeda Chemical Industries, Ltd. | Fumagillol derivatives and pharmaceutical compositions thereof |
| PH26256A (en) | 1988-08-12 | 1992-04-01 | Fujisawa Pharmaceutical Co | Oxaspiro [2,5] octane derivative |
| US5180738A (en) | 1988-09-01 | 1993-01-19 | Takeda Chemical Industries | Fumagillol derivatives and pharmaceutical compositions thereof |
| KR0138530B1 (ko) | 1988-09-01 | 1998-05-15 | 우메모또 요시마사 | 푸마길롤 유도체 |
| US5166172A (en) | 1988-09-01 | 1992-11-24 | Takeda Chemical Industries, Ltd. | Fumagillol derivatives and pharmaceutical compositions thereof |
| DE69001187T2 (de) | 1989-03-06 | 1993-07-08 | Takeda Chemical Industries Ltd | 6-epifumagillole, ihre herstellung und ihre verwendung. |
| US5288722A (en) | 1989-03-06 | 1994-02-22 | Takeda Chemical Industries, Ltd. | 6-amino-6-desoxyfumagillols, production and use thereof |
| US5290807A (en) | 1989-08-10 | 1994-03-01 | Children's Medical Center Corporation | Method for regressing angiogenesis using o-substituted fumagillol derivatives |
| US6017954A (en) | 1989-08-10 | 2000-01-25 | Children's Medical Center Corp. | Method of treating tumors using O-substituted fumagillol derivatives |
| EP0415294A3 (en) | 1989-08-31 | 1991-06-12 | Takeda Chemical Industries, Ltd. | Cyclohexanol derivatives, production and use thereof |
| TW282399B (enExample) | 1990-05-25 | 1996-08-01 | Takeda Pharm Industry Co Ltd | |
| US5238950A (en) | 1991-12-17 | 1993-08-24 | Schering Corporation | Inhibitors of platelet-derived growth factor |
| DE69330690T2 (de) | 1992-01-30 | 2002-06-20 | Takeda Chemical Industries, Ltd. | Verfahren zur Herstellung hoch-wasserlöslicher Zyklodextrinkomplexe |
| DE69311278T2 (de) | 1992-12-16 | 1997-10-30 | Takeda Chemical Industries Ltd | Stabile pharmazeutische Zubereitung mit Fumagillolderivaten |
| HU224028B1 (hu) | 1995-03-27 | 2005-05-30 | Assistance Publique-Hopitaux De Paris | Fumagillol és származékai alkalmazása bélfertőzések kezelésére szolgáló gyógyszerek előállítására |
| WO1997013509A1 (en) | 1995-10-11 | 1997-04-17 | Fujisawa Pharmaceutical Co., Ltd. | Vascular permeation inhibitor |
| EP0799616A1 (en) | 1996-04-01 | 1997-10-08 | Takeda Chemical Industries, Ltd. | Oral composition comprising a fumagillol derivative |
| WO1998005293A2 (en) | 1996-08-02 | 1998-02-12 | The Children's Medical Center Corporation | Method of regulating the female reproductive system through angiogenesis inhibitors |
| US6281245B1 (en) | 1996-10-28 | 2001-08-28 | Versicor, Inc. | Methods for solid-phase synthesis of hydroxylamine compounds and derivatives, and combinatorial libraries thereof |
| DK0973392T3 (da) | 1997-03-04 | 2004-03-29 | Monsanto Co | Divalente sulfonyl-aryl eller heteroarylhydroxamsyreforbindelser |
| US7115632B1 (en) | 1999-05-12 | 2006-10-03 | G. D. Searle & Co. | Sulfonyl aryl or heteroaryl hydroxamic acid compounds |
| US6207704B1 (en) | 1997-06-09 | 2001-03-27 | Massachusetts Institute Of Technology | Type 2 methionine aminopeptidase [MetAP2] inhibitors and uses thereof |
| JP2002502814A (ja) | 1997-10-31 | 2002-01-29 | チルドレンズ・メディカル・センター・コーポレイション | 血管化した正常組織の大きさおよび増殖の調節のための方法 |
| WO1999032433A1 (en) | 1997-12-23 | 1999-07-01 | Warner-Lambert Company | Thiourea and benzamide compounds, compositions and methods of treating or preventing inflammatory diseases and atherosclerosis |
| US6242494B1 (en) | 1998-05-01 | 2001-06-05 | Abbott Laboratories | Substituted β-amino acid inhibitors of methionine aminopeptidase-2 |
| KR100357542B1 (ko) | 1998-05-15 | 2002-10-18 | 주식회사종근당 | 푸마질롤 유도체 및 그 제조방법 |
| KR100357541B1 (ko) | 1998-05-15 | 2002-10-18 | 주식회사종근당 | 5-데메톡시 푸마질롤 유도체 및 그 제조방법 |
| JP2000116337A (ja) | 1998-10-09 | 2000-04-25 | Nippon Shokuhin Kako Co Ltd | ペットフード |
| US6383471B1 (en) | 1999-04-06 | 2002-05-07 | Lipocine, Inc. | Compositions and methods for improved delivery of ionizable hydrophobic therapeutic agents |
| EE200100558A (et) | 1999-04-28 | 2002-12-16 | Aventis Pharma Deutschland Gmbh | Triarüülhappe derivaat, seda sisaldav farmatseutiline kompositsioon ja ühendi raviotstarbeline kasutamine |
| EP1223932A4 (en) | 1999-10-01 | 2003-01-15 | Smithkline Beecham Corp | COMPOUNDS AND METHODS |
| US20020002152A1 (en) | 2000-04-14 | 2002-01-03 | Craig Richard A. | Hydrazide and alkoxyamide angiogenesis inhibitors |
| US6323228B1 (en) | 2000-09-15 | 2001-11-27 | Abbott Laboratories | 3-substituted indole angiogenesis inhibitors |
| AR030631A1 (es) | 2000-09-29 | 2003-08-27 | Abbott Lab | Polipeptidos antiangiogenicos y metodos para inhibir la angiogenesis |
| US6548477B1 (en) | 2000-11-01 | 2003-04-15 | Praecis Pharmaceuticals Inc. | Therapeutic agents and methods of use thereof for the modulation of angiogenesis |
| AU2002239479B2 (en) | 2000-11-01 | 2006-11-09 | Praecis Pharmaceuticals Incorporated | Peptides as Met-AP2 inhibitors |
| WO2002059124A2 (en) | 2000-12-20 | 2002-08-01 | Bristol-Myers Squibb Company | Substituted pyrroloquinolines and pyridoquinolines as serotonin agonists and antagonists |
| WO2002078699A1 (en) | 2001-03-29 | 2002-10-10 | Smithkline Beecham Corporation | Compounds and methods |
| US20020183242A1 (en) | 2001-04-11 | 2002-12-05 | Jack Henkin | Peptide antiangiogenic drugs |
| DE60233420D1 (de) | 2001-09-27 | 2009-10-01 | Equispharm Co Ltd | Fumagillolderivate und verfahren zu deren herstellung |
| US6803382B2 (en) | 2001-11-09 | 2004-10-12 | Galderma Research & Development, S.N.C. | Angiogenesis inhibitors and pharmaceutical and cosmetic use thereof |
| US7119120B2 (en) | 2001-12-26 | 2006-10-10 | Genzyme Corporation | Phosphate transport inhibitors |
| KR100451485B1 (ko) | 2002-03-28 | 2004-10-06 | 주식회사종근당 | 푸마질롤 유도체 또는 그 염의 포접 화합물, 및 이를포함하는 약제학적 조성물 |
| US6989392B2 (en) | 2002-06-18 | 2006-01-24 | Abbott Laboratories | 2-Aminoquinolines as melanin concentrating hormone receptor antagonists |
| US7030262B2 (en) | 2002-08-06 | 2006-04-18 | Abbott Laboratories | 3-Amino-2-hydroxyalkanoic acids and their prodrugs |
| US20040067266A1 (en) | 2002-10-07 | 2004-04-08 | Toppo Frank R. | Weight loss compound |
| US7491718B2 (en) * | 2002-10-08 | 2009-02-17 | Abbott Laboratories | Sulfonamides having antiangiogenic and anticancer activity |
| US20040157836A1 (en) | 2002-10-08 | 2004-08-12 | Comess Kenneth M. | Sulfonamides having antiangiogenic and anticancer activity |
| US20040068012A1 (en) * | 2002-10-08 | 2004-04-08 | Comess Kenneth M. | Sulfonamides having antiangiogenic and anticancer activity |
| WO2004078113A2 (en) | 2003-03-04 | 2004-09-16 | Pharmacia Corporation | Treatment and prevention of obesity with cox-2 inhibitors alone or in combination with weight-loss agents |
| EA200600203A1 (ru) | 2003-08-08 | 2006-08-25 | Янссен Фармацевтика, Н. В. | Производные 2-(хиноксалин-5-илсульфониламино)бензамида в качестве модуляторов сск2 |
| PE20050948A1 (es) | 2003-09-09 | 2005-12-16 | Japan Tobacco Inc | Compuestos de carbamoil-amina como inhibidores de la dipeptidil peptidasa iv |
| PL1697378T3 (pl) | 2003-12-22 | 2008-04-30 | Memory Pharm Corp | Indole, 1h-indazole, 1,2-benzoizoksazole i 1,2-benzoizotiazole oraz ich wytwarzanie i zastosowania |
| US20050239878A1 (en) | 2003-12-29 | 2005-10-27 | Praecis Pharmaceuticals, Inc. | Inhibitors of methionine aminopeptidase-2 and uses thereof |
| KR100552043B1 (ko) | 2004-02-28 | 2006-02-20 | 주식회사종근당 | 푸마질롤 유도체를 포함하는 비만치료용 조성물 |
| AU2005245401A1 (en) | 2004-05-12 | 2005-12-01 | Chemocentryx | Aryl sulfonamides |
| CA2571683A1 (en) | 2004-06-30 | 2006-01-12 | Combinatorx, Incorporated | Methods and reagents for the treatment of metabolic disorders |
| US20060045865A1 (en) | 2004-08-27 | 2006-03-02 | Spherics, Inc. | Controlled regional oral delivery |
| MX2007003623A (es) | 2004-09-24 | 2007-09-11 | Johnson & Johnson | Compuestos sulfonamida. |
| EP1809598B1 (en) * | 2004-10-14 | 2011-03-16 | Abbott GmbH & Co. KG | Aminomethyl substituted bicyclic aromatic compounds suitable for treating disorders that respond to modulation of the dopamine d3 receptor |
| JP2008528574A (ja) | 2005-01-26 | 2008-07-31 | チョン クン ダン ファーマシューティカル コープ. | フマギロール誘導体またはフマギロール誘導体の製造方法およびこれを含む医薬用組成物 |
| FR2886855B1 (fr) | 2005-06-08 | 2009-07-17 | Agronomique Inst Nat Rech | Utilisation de la fumagilline et de ses derives pour augmenter la biodisponibilite des lactones macrocyliques |
| WO2006138475A2 (en) | 2005-06-16 | 2006-12-28 | Jenrin Discovery | Mao-b inhibitors useful for treating obesity |
| WO2007076348A2 (en) | 2005-12-23 | 2007-07-05 | Smithkline Beecham Corporation | Azaindole inhibitors of aurora kinases |
| TW200815405A (en) | 2006-06-09 | 2008-04-01 | Astrazeneca Ab | Novel compounds |
| WO2008008374A2 (en) | 2006-07-14 | 2008-01-17 | Chemocentryx, Inc. | Ccr2 inhibitors and methods of use thereof |
| DE102007020492A1 (de) | 2007-04-30 | 2008-11-06 | Grünenthal GmbH | Substituierte Sulfonamid-Derivate |
| EP2155719A1 (en) | 2007-05-24 | 2010-02-24 | Wyeth LLC | Azacyclylbenzamide derivatives as histamine-3 antagonists |
| CA2690244C (en) | 2007-06-26 | 2016-08-09 | Ofra Benny-Ratsaby | Metap-2 inhibitor polymersomes for therapeutic administration |
| US20090011994A1 (en) | 2007-07-06 | 2009-01-08 | Bristol-Myers Squibb Company | Non-basic melanin concentrating hormone receptor-1 antagonists and methods |
| BRPI0820229A2 (pt) | 2007-11-28 | 2017-05-09 | A Stevenson Cheri | conjugados de análogos de fumagilina biodegradáveis biocompatíveis |
| ATE506359T1 (de) | 2007-11-30 | 2011-05-15 | Bayer Schering Pharma Ag | Heteroaryl-substituierte piperidine |
| WO2010009374A1 (en) | 2008-07-18 | 2010-01-21 | Zafgen, Inc. | Methods of treating an overweight or obese subject |
| EP2350012B1 (en) | 2008-10-06 | 2017-06-28 | The Johns Hopkins University | Quinoline compounds as inhibitors of angiogenesis, human methionine aminopeptidase, and sirt1, and methods of treating disorders |
| WO2010048499A1 (en) | 2008-10-24 | 2010-04-29 | Wake Forest University | Platinum acridine anti-cancer compounds and methods thereof |
| US20120010290A1 (en) | 2008-12-04 | 2012-01-12 | Vath James E | Methods of Treating an Overweight or Obese Subject |
| WO2010065881A2 (en) | 2008-12-04 | 2010-06-10 | Zafgen Corporation | Methods of treating an overweight or obese subject |
| WO2010065877A2 (en) | 2008-12-04 | 2010-06-10 | Zafgen Corporation | Methods of treating an overweight or obese subject |
| MX337575B (es) * | 2009-10-09 | 2016-03-10 | Zafgen Corp | Compuestos de sulfona y métodos para lafabricación y uso de éstos. |
| WO2011085198A1 (en) | 2010-01-08 | 2011-07-14 | Zafgen Corporation | Metap-2 inhibitor for use in treating benign prostatic hypertrophy (bph) |
| WO2011088055A2 (en) | 2010-01-12 | 2011-07-21 | Zafgen Corporation | Methods and compositions for treating cardiovascular disorders |
| WO2011127304A2 (en) | 2010-04-07 | 2011-10-13 | Zafgen Corporation | Methods of treating an overweight subject |
| WO2011150338A1 (en) | 2010-05-27 | 2011-12-01 | Zafgen Corporation | Methods of treating obesity |
| WO2012012642A1 (en) * | 2010-07-22 | 2012-01-26 | Zafgen Corporation | Tricyclic compounds and methds of making and using same |
| WO2012051318A1 (en) | 2010-10-12 | 2012-04-19 | Zafgen Corporation | Sulphonamide compounds and methods of making and using same |
| PH12013500934A1 (en) | 2010-11-09 | 2022-10-24 | Zafgen Inc | Crystalline solids of a metap-2 inhibitor and methods of making and using same |
| US20140073691A1 (en) | 2010-11-10 | 2014-03-13 | Zafgen, Inc. | Methods and composition for Treating Thyroid Hormone Related Disorders |
| US20140011870A1 (en) | 2010-11-29 | 2014-01-09 | Zafgen, Inc. | Methods of Treating Obesity Using an Effective Dose of a METAP-2 Inhibitor |
| BR112013013411A2 (pt) | 2010-11-29 | 2016-09-13 | Zafgen Inc | tratamento de obesidade usando administração não diária de 6-0-(4-dimetilaminoetxi) cinamoil fumagilol |
| WO2012074968A1 (en) | 2010-11-29 | 2012-06-07 | Zafgen Corporation | Methods of reducing risk of hepatobiliary dysfunction during rapid weight loss with metap-2 inhibitors |
| CN103402989B (zh) | 2011-01-26 | 2016-04-06 | 扎夫根股份有限公司 | 四唑化合物及其制备和使用方法 |
| WO2012154676A1 (en) | 2011-05-06 | 2012-11-15 | Zafgen Corporation | Partially saturated tricyclic compounds and methods of making and using same |
| KR20140040739A (ko) | 2011-05-06 | 2014-04-03 | 자프겐 인크. | 삼환식 피라졸 설폰아마이드 화합물 그리고 그의 제조방법 및 그를 이용하는 방법 |
| BR112013028665A2 (pt) * | 2011-05-06 | 2016-09-06 | Zafgen Inc | compostos de sulfonamida tricíclicos e métodos para fazer e usar os mesmos |
| US9090640B2 (en) | 2011-09-02 | 2015-07-28 | Ulrich Bierbach | Targeted delivery and prodrug designs for platinum-acridine anti-cancer compounds and methods thereof |
| BR112014017780A8 (pt) * | 2012-01-18 | 2017-07-11 | Zafgen Inc | Compostos de sulfona tricíclicos e métodos para fazer e usar os mesmos |
| MX2014008706A (es) * | 2012-01-18 | 2015-03-05 | Zafgen Inc | Compuestos tricíclicos de sulfonamida y métodos para elaborarlos y usarlos. |
| WO2014071363A1 (en) | 2012-11-05 | 2014-05-08 | Zafgen, Inc. | Tricyclic compounds and methods of making and using same |
| US9868717B2 (en) | 2012-11-05 | 2018-01-16 | Zafgen, Inc. | Tricyclic sulphonamide compounds and methods of making and using same |
| JP6169716B2 (ja) | 2012-11-05 | 2017-07-26 | ザフゲン,インコーポレイテッド | 肝疾患を治療する方法 |
-
2012
- 2012-05-07 WO PCT/US2012/036789 patent/WO2012154676A1/en not_active Ceased
- 2012-05-07 MX MX2013012921A patent/MX345535B/es active IP Right Grant
- 2012-05-07 KR KR1020137032337A patent/KR101979039B1/ko not_active Ceased
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- 2012-05-07 SG SG2013082219A patent/SG194812A1/en unknown
- 2012-05-07 EP EP12722591.0A patent/EP2705030B1/en active Active
- 2012-05-07 JP JP2014509510A patent/JP6062423B2/ja not_active Expired - Fee Related
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- 2012-05-07 BR BR112013028534A patent/BR112013028534A2/pt not_active Application Discontinuation
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- 2013-11-04 IL IL229246A patent/IL229246A/en active IP Right Grant
-
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- 2016-02-03 US US15/014,524 patent/US9617237B2/en not_active Expired - Fee Related
-
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- 2017-02-15 US US15/433,452 patent/US20180002307A1/en not_active Abandoned
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010065883A2 (en) * | 2008-12-04 | 2010-06-10 | Zafgen Corporation | Method of treating an overweight or obese subject |
Non-Patent Citations (1)
| Title |
|---|
| Lead optimization of methionine aminopeptidase-2 (MetAP2) inhibitors containing sulfonamides of 5,6-disubstituted anthranilic acids;Gary T. Wang et al.;《Bioorg. Med. Chem. Lett.》;20070225;第17卷(第10期);第2817-2822页 * |
Also Published As
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| AU2012253757A8 (en) | 2015-10-22 |
| JP2014514349A (ja) | 2014-06-19 |
| CA2835261A1 (en) | 2012-11-15 |
| US20140088078A1 (en) | 2014-03-27 |
| EP2705030A1 (en) | 2014-03-12 |
| KR20140047611A (ko) | 2014-04-22 |
| EP2705030B1 (en) | 2016-07-27 |
| EA201391644A1 (ru) | 2014-11-28 |
| CN103764641A (zh) | 2014-04-30 |
| JP6062423B2 (ja) | 2017-01-18 |
| US20180002307A1 (en) | 2018-01-04 |
| US20170001973A1 (en) | 2017-01-05 |
| AU2012253757B2 (en) | 2017-04-13 |
| MX2013012921A (es) | 2014-02-27 |
| SG194812A1 (en) | 2013-12-30 |
| US9617237B2 (en) | 2017-04-11 |
| AU2012253757A1 (en) | 2013-11-21 |
| KR101979039B1 (ko) | 2019-05-15 |
| WO2012154676A1 (en) | 2012-11-15 |
| EA025526B1 (ru) | 2017-01-30 |
| MX345535B (es) | 2017-02-03 |
| CA2835261C (en) | 2019-06-04 |
| IL229246A0 (en) | 2014-01-30 |
| US9290472B2 (en) | 2016-03-22 |
| BR112013028534A2 (pt) | 2016-09-06 |
| IL229246A (en) | 2017-05-29 |
| NZ617388A (en) | 2015-11-27 |
| WO2012154676A9 (en) | 2014-03-27 |
| PH12013502261A1 (en) | 2022-10-26 |
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