RU2012106657A - Изоформы избирательного ингибитора фосфолипазы d - Google Patents
Изоформы избирательного ингибитора фосфолипазы d Download PDFInfo
- Publication number
- RU2012106657A RU2012106657A RU2012106657/04A RU2012106657A RU2012106657A RU 2012106657 A RU2012106657 A RU 2012106657A RU 2012106657/04 A RU2012106657/04 A RU 2012106657/04A RU 2012106657 A RU2012106657 A RU 2012106657A RU 2012106657 A RU2012106657 A RU 2012106657A
- Authority
- RU
- Russia
- Prior art keywords
- optionally substituted
- cycloalkyl
- hydrogen
- alkylsulfonyl
- azide
- Prior art date
Links
- 108090000553 Phospholipase D Proteins 0.000 title claims 3
- 102000011420 Phospholipase D Human genes 0.000 title 1
- 102000001708 Protein Isoforms Human genes 0.000 title 1
- 108010029485 Protein Isoforms Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 28
- 239000001257 hydrogen Substances 0.000 claims abstract 28
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims abstract 21
- 125000003545 alkoxy group Chemical group 0.000 claims abstract 20
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims abstract 20
- 150000004820 halides Chemical class 0.000 claims abstract 20
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims abstract 20
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims abstract 20
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims abstract 20
- 125000005518 carboxamido group Chemical group 0.000 claims abstract 19
- 150000001875 compounds Chemical class 0.000 claims abstract 19
- 125000004093 cyano group Chemical group *C#N 0.000 claims abstract 19
- DYMRYCZRMAHYKE-UHFFFAOYSA-N n-diazonitramide Chemical compound [O-][N+](=O)N=[N+]=[N-] DYMRYCZRMAHYKE-UHFFFAOYSA-N 0.000 claims abstract 19
- 125000000547 substituted alkyl group Chemical group 0.000 claims abstract 14
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract 9
- 125000003118 aryl group Chemical group 0.000 claims abstract 8
- 229910052799 carbon Inorganic materials 0.000 claims abstract 8
- 125000004432 carbon atom Chemical group C* 0.000 claims abstract 8
- 125000000753 cycloalkyl group Chemical group 0.000 claims abstract 8
- -1 cyano- Chemical class 0.000 claims abstract 7
- 125000000392 cycloalkenyl group Chemical group 0.000 claims abstract 7
- 125000004366 heterocycloalkenyl group Chemical group 0.000 claims abstract 7
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims abstract 7
- 125000001424 substituent group Chemical group 0.000 claims abstract 7
- 150000002431 hydrogen Chemical class 0.000 claims 20
- 125000003396 thiol group Chemical class [H]S* 0.000 claims 16
- 238000000034 method Methods 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 241000124008 Mammalia Species 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- FCEHBMOGCRZNNI-UHFFFAOYSA-N 1-benzothiophene Chemical compound C1=CC=C2SC=CC2=C1 FCEHBMOGCRZNNI-UHFFFAOYSA-N 0.000 claims 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000001041 indolyl group Chemical group 0.000 claims 2
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 2
- 125000004491 isohexyl group Chemical group C(CCC(C)C)* 0.000 claims 2
- 125000001972 isopentyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])C([H])([H])* 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 2
- 125000001280 n-hexyl group Chemical group C(CCCCC)* 0.000 claims 2
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 2
- 125000001624 naphthyl group Chemical group 0.000 claims 2
- 125000001971 neopentyl group Chemical group [H]C([*])([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 125000003548 sec-pentyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- BAXOFTOLAUCFNW-UHFFFAOYSA-N 1H-indazole Chemical compound C1=CC=C2C=NNC2=C1 BAXOFTOLAUCFNW-UHFFFAOYSA-N 0.000 claims 1
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000005872 benzooxazolyl group Chemical group 0.000 claims 1
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- 125000003354 benzotriazolyl group Chemical group N1N=NC2=C1C=CC=C2* 0.000 claims 1
- 230000004663 cell proliferation Effects 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 230000004064 dysfunction Effects 0.000 claims 1
- 125000001207 fluorophenyl group Chemical group 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000000740 n-pentyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000004593 naphthyridinyl group Chemical group N1=C(C=CC2=CC=CN=C12)* 0.000 claims 1
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 125000004309 pyranyl group Chemical group O1C(C=CC=C1)* 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000002098 pyridazinyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 238000000926 separation method Methods 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
- 125000005247 tetrazinyl group Chemical group N1=NN=NC(=C1)* 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 125000004306 triazinyl group Chemical group 0.000 claims 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 5
- 150000003573 thiols Chemical class 0.000 abstract 4
- 150000001540 azides Chemical class 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/10—Spiro-condensed 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
- A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US22849209P | 2009-07-24 | 2009-07-24 | |
| US61/228,492 | 2009-07-24 | ||
| PCT/US2010/043045 WO2011011680A1 (en) | 2009-07-24 | 2010-07-23 | Isoform selective phospholipase d inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2012106657A true RU2012106657A (ru) | 2013-08-27 |
Family
ID=43499428
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2012106657/04A RU2012106657A (ru) | 2009-07-24 | 2010-07-23 | Изоформы избирательного ингибитора фосфолипазы d |
Country Status (14)
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9127005B2 (en) | 2009-07-24 | 2015-09-08 | Vanderbilt University | Isoform selective phospholipase D inhibitors |
| US9453017B2 (en) | 2011-09-30 | 2016-09-27 | Vanderbilt University | Antiviral therapies with phospholipase D inhibitors |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20140378524A1 (en) * | 2012-12-11 | 2014-12-25 | Vanderbilt University | Methods and compositions comprising akt inhibitors and/or phospholipase d inhibitors |
| BR112015013744A2 (pt) * | 2012-12-11 | 2017-07-11 | Univ Vanderbilt | método para tratar um sujeito contra infecção por hiv, composição farmacêutica, e, kit |
| CN114778844A (zh) * | 2022-03-07 | 2022-07-22 | 天津市肿瘤医院（天津医科大学肿瘤医院） | Pld1作为评估肿瘤患者对于化疗药物敏感性的分子标志物的用途 |
| IL317147A (en) * | 2022-06-16 | 2025-01-01 | Japan Tobacco Inc | Dihydroxyoxadiazinone compound and its pharmaceutical use |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IT1281502B1 (it) | 1995-06-13 | 1998-02-18 | Sardinian Antiviral Research C | Impiego di un inibitore non nucleosidico della trascrittasi inversa in associazione con inibitori nucleosidici per il trattamento della |
| US6187559B1 (en) | 1997-08-28 | 2001-02-13 | Novartis Ag | Phospholipase D gene |
| EP1313498A4 (en) | 2000-05-25 | 2004-04-21 | Ben-Tsion Williger | PHOSPHOLIPASE D EFFECTORS FOR THERAPY AND SCREENING |
| US6482829B2 (en) * | 2000-06-08 | 2002-11-19 | Hoffmann-La Roche Inc. | Substituted heterocyclic siprodecane compound active as an antagonist of neurokinin 1 receptor |
| WO2004026898A1 (en) | 2002-09-18 | 2004-04-01 | Postech Foundation | Peptide complexes containing phospholipase d |
| BRPI0517423A (pt) * | 2004-12-27 | 2008-10-07 | Astrazeneca Ab | composto, composição farmacêutica, método para o tratamento ou prevenção de distúrbios neurológicos e psiquiátricos associados com disfunção do glutamato em um animal, e, uso em um composto |
| CN101223120A (zh) | 2005-02-23 | 2008-07-16 | 杰克·L·阿比瑟 | 用于治疗增殖障碍的和厚朴酚衍生物 |
| CN101448844B (zh) * | 2006-05-18 | 2012-07-25 | 霍夫曼-拉罗奇有限公司 | 作为腺苷a2b受体拮抗剂的噻唑并嘧啶/吡啶脲衍生物 |
| US20100009970A1 (en) | 2008-03-19 | 2010-01-14 | Combinatorx (Singapore) Pte. Ltd. | Compositions and methods for treatment of viral diseases |
| WO2010037081A1 (en) | 2008-09-29 | 2010-04-01 | Palatin Technologies, Inc. | Melanocortin receptor-specific spiro-piperidine compounds |
| CA2756141A1 (en) | 2009-03-31 | 2010-10-07 | Sanofi-Aventis Deutschland Gmbh | Drug delivery device body |
| EP2435563A4 (en) | 2009-05-29 | 2013-10-02 | Univ Columbia | MODULATION OF PHOSPHOLIPASE D FOR THE TREATMENT OF NEURODEEGENERATIVE DISEASES |
| US9127005B2 (en) | 2009-07-24 | 2015-09-08 | Vanderbilt University | Isoform selective phospholipase D inhibitors |
| WO2011019498A1 (en) | 2009-07-27 | 2011-02-17 | The Trustees Of Princeton University | Inhibition of glycerol-3-phosphate acyltransferase (gpat) and associated enzymes for treatment of viral infections |
| CA2850597A1 (en) | 2011-09-30 | 2013-04-04 | Vanderbilt University | Antiviral therapies with phospholipase d inhibitors |
| US20140378524A1 (en) | 2012-12-11 | 2014-12-25 | Vanderbilt University | Methods and compositions comprising akt inhibitors and/or phospholipase d inhibitors |
| BR112015013744A2 (pt) | 2012-12-11 | 2017-07-11 | Univ Vanderbilt | método para tratar um sujeito contra infecção por hiv, composição farmacêutica, e, kit |
-
2010
- 2010-07-23 US US13/386,397 patent/US9127005B2/en not_active Expired - Fee Related
- 2010-07-23 RU RU2012106657/04A patent/RU2012106657A/ru not_active Application Discontinuation
- 2010-07-23 MX MX2012001064A patent/MX2012001064A/es not_active Application Discontinuation
- 2010-07-23 EP EP10802947.1A patent/EP2456307B1/en not_active Not-in-force
- 2010-07-23 AU AU2010275526A patent/AU2010275526A1/en not_active Abandoned
- 2010-07-23 BR BRBR112012001586-9A patent/BR112012001586A2/pt not_active IP Right Cessation
- 2010-07-23 CA CA2768940A patent/CA2768940C/en not_active Expired - Fee Related
- 2010-07-23 JP JP2012521826A patent/JP2013500260A/ja active Pending
- 2010-07-23 IN IN1661DEN2012 patent/IN2012DN01661A/en unknown
- 2010-07-23 SG SG2012005252A patent/SG178102A1/en unknown
- 2010-07-23 WO PCT/US2010/043045 patent/WO2011011680A1/en not_active Ceased
- 2010-07-23 KR KR1020127004698A patent/KR20120090034A/ko not_active Withdrawn
- 2010-07-23 CN CN2010800423044A patent/CN102573474A/zh active Pending
-
2012
- 2012-01-24 IL IL217720A patent/IL217720A0/en unknown
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9127005B2 (en) | 2009-07-24 | 2015-09-08 | Vanderbilt University | Isoform selective phospholipase D inhibitors |
| US9453017B2 (en) | 2011-09-30 | 2016-09-27 | Vanderbilt University | Antiviral therapies with phospholipase D inhibitors |
Also Published As
| Publication number | Publication date |
|---|---|
| IN2012DN01661A (cg-RX-API-DMAC10.html) | 2015-06-05 |
| US20120214832A1 (en) | 2012-08-23 |
| US9127005B2 (en) | 2015-09-08 |
| KR20120090034A (ko) | 2012-08-16 |
| EP2456307A4 (en) | 2013-01-16 |
| JP2013500260A (ja) | 2013-01-07 |
| AU2010275526A1 (en) | 2012-03-15 |
| EP2456307B1 (en) | 2016-11-02 |
| BR112012001586A2 (pt) | 2015-09-01 |
| IL217720A0 (en) | 2012-03-29 |
| CN102573474A (zh) | 2012-07-11 |
| WO2011011680A1 (en) | 2011-01-27 |
| EP2456307A1 (en) | 2012-05-30 |
| SG178102A1 (en) | 2012-03-29 |
| CA2768940A1 (en) | 2011-01-27 |
| CA2768940C (en) | 2018-03-13 |
| MX2012001064A (es) | 2012-07-17 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20141110 |