LV11547B - O-aryl, o-alkyl, o-alkenyl and o-alkynyl- macrolides having immunosuppressive activity - Google Patents
O-aryl, o-alkyl, o-alkenyl and o-alkynyl- macrolides having immunosuppressive activity Download PDFInfo
- Publication number
- LV11547B LV11547B LVP-96-112A LV960112A LV11547B LV 11547 B LV11547 B LV 11547B LV 960112 A LV960112 A LV 960112A LV 11547 B LV11547 B LV 11547B
- Authority
- LV
- Latvia
- Prior art keywords
- quot
- dimethoxy
- tetraone
- dioxa
- ethyl
- Prior art date
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- 239000003120 macrolide antibiotic agent Substances 0.000 title description 42
- 230000001506 immunosuppresive effect Effects 0.000 title description 9
- 229940041033 macrolides Drugs 0.000 title description 4
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- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 337
- 150000001875 compounds Chemical class 0.000 claims description 218
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- 239000000203 mixture Substances 0.000 claims description 162
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims description 107
- RTZKZFJDLAIYFH-UHFFFAOYSA-N diethyl ether Substances CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims description 79
- -1 allyl 4-NO Chemical compound 0.000 claims description 75
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 74
- 229910052739 hydrogen Inorganic materials 0.000 claims description 74
- 239000001257 hydrogen Substances 0.000 claims description 73
- 125000001424 substituent group Chemical group 0.000 claims description 72
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 69
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 62
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 45
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 27
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- 125000004180 3-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(F)=C1[H] 0.000 claims 1
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- BDIIUPVXKMUQOG-UHFFFAOYSA-N tris(4-methylsulfanylphenyl)bismuthane Chemical compound C1=CC(SC)=CC=C1[Bi](C=1C=CC(SC)=CC=1)C1=CC=C(SC)C=C1 BDIIUPVXKMUQOG-UHFFFAOYSA-N 0.000 description 1
- QZURPDZAEABPID-UHFFFAOYSA-N tris(6-methoxynaphthalen-2-yl)bismuthane Chemical compound C1=C(OC)C=CC2=CC([Bi](C=3C=C4C=CC(OC)=CC4=CC=3)C3=CC4=CC=C(C=C4C=C3)OC)=CC=C21 QZURPDZAEABPID-UHFFFAOYSA-N 0.000 description 1
- NOVPTUJIGKLOEX-UHFFFAOYSA-N tris[4-[tert-butyl(dimethyl)silyl]oxyphenyl]bismuthane Chemical compound C1=CC(O[Si](C)(C)C(C)(C)C)=CC=C1[Bi](C=1C=CC(O[Si](C)(C)C(C)(C)C)=CC=1)C1=CC=C(O[Si](C)(C)C(C)(C)C)C=C1 NOVPTUJIGKLOEX-UHFFFAOYSA-N 0.000 description 1
- ZDPHROOEEOARMN-UHFFFAOYSA-N undecanoic acid Chemical compound CCCCCCCCCCC(O)=O ZDPHROOEEOARMN-UHFFFAOYSA-N 0.000 description 1
- 238000002255 vaccination Methods 0.000 description 1
- 230000003966 vascular damage Effects 0.000 description 1
- 239000003981 vehicle Substances 0.000 description 1
- 230000003442 weekly effect Effects 0.000 description 1
- 230000029663 wound healing Effects 0.000 description 1
- 238000002689 xenotransplantation Methods 0.000 description 1
Classifications
-
- 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
- C07D491/12—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 three hetero rings
- C07D491/16—Peri-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/18—Bridged systems
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Transplantation (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Color Printing (AREA)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US08/132,072 US5565560A (en) | 1991-05-13 | 1993-10-04 | O-Aryl,O-alkyl,O-alkenyl and O-alkynylmacrolides having immunosuppressive activity |
PCT/US1994/011114 WO1995009857A1 (en) | 1993-10-04 | 1994-09-30 | O-aryl, o-alkyl, o-alkenyl and o-alkynyl-macrolides having immunosuppressive activity |
Publications (2)
Publication Number | Publication Date |
---|---|
LV11547A LV11547A (lv) | 1996-10-20 |
LV11547B true LV11547B (en) | 1997-02-20 |
Family
ID=22452330
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
LVP-96-112A LV11547B (en) | 1993-10-04 | 1996-04-15 | O-aryl, o-alkyl, o-alkenyl and o-alkynyl- macrolides having immunosuppressive activity |
Country Status (18)
Country | Link |
---|---|
US (2) | US5565560A (pt) |
EP (1) | EP0722448A4 (pt) |
JP (1) | JPH09503507A (pt) |
KR (1) | KR960704896A (pt) |
CN (1) | CN1137275A (pt) |
AU (1) | AU690157B2 (pt) |
BG (1) | BG100474A (pt) |
BR (1) | BR9407720A (pt) |
CA (1) | CA2172124A1 (pt) |
CZ (1) | CZ99396A3 (pt) |
FI (1) | FI961496A (pt) |
HU (1) | HUT74591A (pt) |
LV (1) | LV11547B (pt) |
NO (1) | NO961345L (pt) |
NZ (1) | NZ275203A (pt) |
PL (1) | PL313870A1 (pt) |
SK (1) | SK43096A3 (pt) |
WO (1) | WO1995009857A1 (pt) |
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US5693648A (en) * | 1994-09-30 | 1997-12-02 | Merck & Co., Inc. | O-aryl, O-alkyl, O-alkenyl and O-alkynyl-macrolides having immunosuppressive activity |
US6413967B1 (en) * | 1995-03-30 | 2002-07-02 | The University Of Virginia Patents Foundation | Inhibition of novel calcium entry pathway in electrically non-excitable cells acting as an anti-proliferative therapy |
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US6271244B1 (en) | 1998-06-03 | 2001-08-07 | Gpi Nil Holdings, Inc. | N-linked urea or carbamate of heterocyclic thioester hair growth compositions and uses |
US5945441A (en) * | 1997-06-04 | 1999-08-31 | Gpi Nil Holdings, Inc. | Pyrrolidine carboxylate hair revitalizing agents |
US6187796B1 (en) | 1998-06-03 | 2001-02-13 | Gpi Nil Holdings, Inc. | Sulfone hair growth compositions and uses |
US6274602B1 (en) | 1998-06-03 | 2001-08-14 | Gpi Nil Holdings, Inc. | Heterocyclic thioester and ketone hair growth compositions and uses |
US20010049381A1 (en) * | 1997-06-04 | 2001-12-06 | Gpl Nil Holdings, Inc., | Pyrrolidine derivative hair growth compositions and uses |
US6274617B1 (en) | 1998-06-03 | 2001-08-14 | Gpi Nil Holdings, Inc. | Heterocyclic ester and amide hair growth compositions and uses |
US6172087B1 (en) | 1998-06-03 | 2001-01-09 | Gpi Nil Holding, Inc. | N-oxide of heterocyclic ester, amide, thioester, or ketone hair growth compositions and uses |
US6429215B1 (en) | 1998-06-03 | 2002-08-06 | Gpi Nil Holdings, Inc. | N-oxide of heterocyclic ester, amide, thioester, or ketone hair growth compositions and uses |
US6506788B1 (en) | 1998-08-14 | 2003-01-14 | Gpi Nil Holdings, Inc. | N-linked urea or carbamate of heterocyclic thioesters for vision and memory disorders |
US6335348B1 (en) | 1998-08-14 | 2002-01-01 | Gpi Nil Holdings, Inc. | Nitrogen-containing linear and azepinyl/ compositions and uses for vision and memory disorders |
US6339101B1 (en) | 1998-08-14 | 2002-01-15 | Gpi Nil Holdings, Inc. | N-linked sulfonamides of N-heterocyclic carboxylic acids or isosteres for vision and memory disorders |
US6384056B1 (en) | 1998-08-14 | 2002-05-07 | Gpi Nil Holdings, Inc. | Heterocyclic thioesters or ketones for vision and memory disorders |
US6337340B1 (en) | 1998-08-14 | 2002-01-08 | Gpi Nil Holdings, Inc. | Carboxylic acids and isosteres of heterocyclic ring compounds having multiple heteroatoms for vision and memory disorders |
US6333340B1 (en) | 1998-08-14 | 2001-12-25 | Gpi Nil Holdings, Inc. | Small molecule sulfonamides for vision and memory disorders |
US6218423B1 (en) | 1998-08-14 | 2001-04-17 | Gpi Nil Holdings, Inc. | Pyrrolidine derivatives for vision and memory disorders |
US7410995B1 (en) | 1998-08-14 | 2008-08-12 | Gpi Nil Holdings Inc. | N-linked sulfonamide of heterocyclic thioesters for vision and memory disorders |
US6399648B1 (en) | 1998-08-14 | 2002-06-04 | Gpi Nil Holdings, Inc. | N-oxides of heterocyclic ester, amide, thioester, or ketone for vision and memory disorders |
US6376517B1 (en) | 1998-08-14 | 2002-04-23 | Gpi Nil Holdings, Inc. | Pipecolic acid derivatives for vision and memory disorders |
US7338976B1 (en) | 1998-08-14 | 2008-03-04 | Gpi Nil Holdings, Inc. | Heterocyclic esters or amides for vision and memory disorders |
US7265150B1 (en) | 1998-08-14 | 2007-09-04 | Gpi Nil Holdings Inc. | Carboxylic acids and carboxylic acid isosteres of N-heterocyclic compounds for vision and memory disorders |
ATE445838T1 (de) | 2001-07-25 | 2009-10-15 | Raptor Pharmaceutical Inc | Zusammensetzungen und verfahren zur modulation des transports durch die blut-hirn-schranke |
AU2007237187B2 (en) * | 2002-07-16 | 2010-08-05 | Biotica Technology Limited | Production of polyketides |
EP1539157B1 (en) | 2002-09-18 | 2013-08-21 | Trustees Of The University Of Pennsylvania | Rapamycin for use in inhibiting or preventing choroidal neovascularization |
DE10250870A1 (de) * | 2002-10-31 | 2004-05-13 | Switch Biotech Ag | Zusammensetzung enthaltend Aktivatoren von IK-Kaliumkanälen und Calcineurin-Antagonisten und deren Verwendung |
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AU2005326322B2 (en) * | 2004-07-01 | 2009-02-05 | Yale University | Targeted and high density drug loaded polymeric materials |
JP2008528491A (ja) | 2005-01-20 | 2008-07-31 | アレイ バイオファーマ、インコーポレイテッド | 免疫調節性障害および呼吸器の疾患の処置のための大環状アナログ |
BRPI0608152A2 (pt) | 2005-02-09 | 2009-11-10 | Macusight Inc | formulações para tratamento ocular |
US8663639B2 (en) | 2005-02-09 | 2014-03-04 | Santen Pharmaceutical Co., Ltd. | Formulations for treating ocular diseases and conditions |
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US10265407B2 (en) | 2007-02-15 | 2019-04-23 | Yale University | Modular nanodevices for smart adaptable vaccines |
US20100151436A1 (en) * | 2007-03-02 | 2010-06-17 | Fong Peter M | Methods for Ex Vivo Administration of Drugs to Grafts Using Polymeric Nanoparticles |
US20080265343A1 (en) * | 2007-04-26 | 2008-10-30 | International Business Machines Corporation | Field effect transistor with inverted t shaped gate electrode and methods for fabrication thereof |
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US20120077778A1 (en) | 2010-09-29 | 2012-03-29 | Andrea Bourdelais | Ladder-Frame Polyether Conjugates |
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US9814703B2 (en) | 2013-11-14 | 2017-11-14 | The Board Of Trustees Of The Leland Stanford Junior University | Methods for treating cancer by activation of BMP signaling |
US10981951B2 (en) | 2014-01-31 | 2021-04-20 | Mayo Foundation For Medical Education And Research | Therapeutics for the treatment of glaucoma |
CA3166579A1 (en) * | 2020-02-07 | 2021-08-12 | Qlaris Bio, Inc. | Improved methods and compositions for cromakalim prodrug therapy |
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US5250678A (en) * | 1991-05-13 | 1993-10-05 | Merck & Co., Inc. | O-aryl, O-alkyl, O-alkenyl and O-alkynylmacrolides having immunosuppressive activity |
US5162334A (en) * | 1991-05-13 | 1992-11-10 | Merck & Co., Inc. | Amino O-alkyl, O-alkenyl and O-alkynlmacrolides having immunosuppressive activity |
US5262533A (en) * | 1991-05-13 | 1993-11-16 | Merck & Co., Inc. | Amino O-aryl macrolides having immunosuppressive activity |
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US5189042A (en) * | 1991-08-22 | 1993-02-23 | Merck & Co. Inc. | Fluoromacrolides having immunosuppressive activity |
US5247076A (en) * | 1991-09-09 | 1993-09-21 | Merck & Co., Inc. | Imidazolidyl macrolides having immunosuppressive activity |
US5252732A (en) * | 1991-09-09 | 1993-10-12 | Merck & Co., Inc. | D-heteroaryl, O-alkylheteroaryl, O-alkenylheteroaryl and O-alkynylheteroarylmacrolides having immunosuppressive activity |
US5208241A (en) * | 1991-09-09 | 1993-05-04 | Merck & Co., Inc. | N-heteroaryl, n-alkylheteroaryl, n-alkenylheteroaryl and n-alkynylheteroarylmacrolides having immunosuppressive activity |
-
1993
- 1993-10-04 US US08/132,072 patent/US5565560A/en not_active Expired - Fee Related
-
1994
- 1994-09-30 CA CA002172124A patent/CA2172124A1/en not_active Abandoned
- 1994-09-30 PL PL94313870A patent/PL313870A1/xx unknown
- 1994-09-30 JP JP7510920A patent/JPH09503507A/ja active Pending
- 1994-09-30 BR BR9407720A patent/BR9407720A/pt not_active Application Discontinuation
- 1994-09-30 NZ NZ275203A patent/NZ275203A/en unknown
- 1994-09-30 SK SK430-96A patent/SK43096A3/sk unknown
- 1994-09-30 CZ CZ96993A patent/CZ99396A3/cs unknown
- 1994-09-30 AU AU80737/94A patent/AU690157B2/en not_active Ceased
- 1994-09-30 HU HU9600870A patent/HUT74591A/hu unknown
- 1994-09-30 CN CN94194139A patent/CN1137275A/zh active Pending
- 1994-09-30 EP EP94931789A patent/EP0722448A4/en not_active Withdrawn
- 1994-09-30 WO PCT/US1994/011114 patent/WO1995009857A1/en not_active Application Discontinuation
-
1995
- 1995-05-12 US US08/440,180 patent/US5532248A/en not_active Expired - Fee Related
-
1996
- 1996-04-02 NO NO961345A patent/NO961345L/no unknown
- 1996-04-03 BG BG100474A patent/BG100474A/xx unknown
- 1996-04-03 FI FI961496A patent/FI961496A/fi unknown
- 1996-04-04 KR KR1019960701760A patent/KR960704896A/ko not_active Application Discontinuation
- 1996-04-15 LV LVP-96-112A patent/LV11547B/en unknown
Also Published As
Publication number | Publication date |
---|---|
CA2172124A1 (en) | 1995-04-13 |
AU8073794A (en) | 1995-05-01 |
PL313870A1 (en) | 1996-07-22 |
US5532248A (en) | 1996-07-02 |
US5565560A (en) | 1996-10-15 |
FI961496A0 (fi) | 1996-04-03 |
BR9407720A (pt) | 1997-03-04 |
BG100474A (en) | 1996-12-31 |
NO961345L (no) | 1996-06-03 |
HUT74591A (en) | 1997-01-28 |
HU9600870D0 (en) | 1996-06-28 |
NZ275203A (en) | 1998-01-26 |
AU690157B2 (en) | 1998-04-23 |
NO961345D0 (no) | 1996-04-02 |
FI961496A (fi) | 1996-04-03 |
SK43096A3 (en) | 1996-10-02 |
JPH09503507A (ja) | 1997-04-08 |
KR960704896A (ko) | 1996-10-09 |
EP0722448A4 (en) | 1998-04-29 |
CZ99396A3 (en) | 1996-09-11 |
LV11547A (lv) | 1996-10-20 |
WO1995009857A1 (en) | 1995-04-13 |
EP0722448A1 (en) | 1996-07-24 |
CN1137275A (zh) | 1996-12-04 |
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