HRP20110408T1 - Inhibitori nukleozidnih fosforilaza i hidrolaza acikličkog amina - Google Patents
Inhibitori nukleozidnih fosforilaza i hidrolaza acikličkog amina Download PDFInfo
- Publication number
- HRP20110408T1 HRP20110408T1 HR20110408T HRP20110408T HRP20110408T1 HR P20110408 T1 HRP20110408 T1 HR P20110408T1 HR 20110408 T HR20110408 T HR 20110408T HR P20110408 T HRP20110408 T HR P20110408T HR P20110408 T1 HRP20110408 T1 HR P20110408T1
- Authority
- HR
- Croatia
- Prior art keywords
- compound according
- pyrrolo
- pyrimidin
- hydroxy
- methyl
- Prior art date
Links
- -1 Acyclic amine Chemical class 0.000 title claims 6
- 108010063372 N-Glycosyl Hydrolases Proteins 0.000 title abstract 3
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 102000004157 Hydrolases Human genes 0.000 title 1
- 102100036286 Purine nucleoside phosphorylase Human genes 0.000 title 1
- 108010009099 nucleoside phosphorylase Proteins 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 18
- 201000010099 disease Diseases 0.000 claims abstract 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract 6
- 102000030764 Purine-nucleoside phosphorylase Human genes 0.000 claims abstract 5
- 102000010722 N-Glycosyl Hydrolases Human genes 0.000 claims abstract 4
- 208000035143 Bacterial infection Diseases 0.000 claims abstract 2
- 206010028980 Neoplasm Diseases 0.000 claims abstract 2
- 210000001744 T-lymphocyte Anatomy 0.000 claims abstract 2
- 208000022362 bacterial infectious disease Diseases 0.000 claims abstract 2
- 201000011510 cancer Diseases 0.000 claims abstract 2
- 230000001404 mediated effect Effects 0.000 claims abstract 2
- 101710101148 Probable 6-oxopurine nucleoside phosphorylase Proteins 0.000 claims 3
- ARXKVVRQIIOZGF-UHFFFAOYSA-N 1,2,4-butanetriol Chemical compound OCCC(O)CO ARXKVVRQIIOZGF-UHFFFAOYSA-N 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 108010060908 purine nucleosidase Proteins 0.000 claims 2
- BGLYJTBLQSNABJ-UHFFFAOYSA-N 2-amino-7-[(2,4-dihydroxybutylamino)methyl]-1,5-dihydropyrrolo[3,2-d]pyrimidin-4-one Chemical compound O=C1NC(N)=NC2=C1NC=C2CNCC(O)CCO BGLYJTBLQSNABJ-UHFFFAOYSA-N 0.000 claims 1
- YKCZORHAJYWZPI-UHFFFAOYSA-N 2-amino-7-[[[3,4-dihydroxy-2-(hydroxymethyl)butyl]amino]methyl]-1,5-dihydropyrrolo[3,2-d]pyrimidin-4-one Chemical compound O=C1NC(N)=NC2=C1NC=C2CNCC(CO)C(O)CO YKCZORHAJYWZPI-UHFFFAOYSA-N 0.000 claims 1
- MUGWLXRKUGUISI-UHFFFAOYSA-N 2-amino-7-[[[3-hydroxy-2-(hydroxymethyl)propyl]amino]methyl]-1,5-dihydropyrrolo[3,2-d]pyrimidin-4-one Chemical compound O=C1NC(N)=NC2=C1NC=C2CNCC(CO)CO MUGWLXRKUGUISI-UHFFFAOYSA-N 0.000 claims 1
- CBYPUSIRVAYVNK-UHFFFAOYSA-N 7-[(2,4-dihydroxybutylamino)methyl]-1,5-dihydropyrrolo[3,2-d]pyrimidin-4-one Chemical compound N1=CNC(=O)C2=C1C(CNCC(O)CCO)=CN2 CBYPUSIRVAYVNK-UHFFFAOYSA-N 0.000 claims 1
- KUQJLVZYIKHFMX-OGFXRTJISA-N 7-[[[(2r)-2,3-dihydroxypropyl]amino]methyl]-1,5-dihydropyrrolo[3,2-d]pyrimidin-4-one;hydrochloride Chemical compound Cl.N1=CN=C2C(CNC[C@@H](O)CO)=CNC2=C1O KUQJLVZYIKHFMX-OGFXRTJISA-N 0.000 claims 1
- QZLAGQIKRPVUTO-WLYNEOFISA-N 7-[[[(2r,3r)-1,3,4-trihydroxybutan-2-yl]amino]methyl]-1,5-dihydropyrrolo[3,2-d]pyrimidin-4-one;hydrochloride Chemical compound Cl.N1=CN=C2C(CN[C@H](CO)[C@@H](O)CO)=CNC2=C1O QZLAGQIKRPVUTO-WLYNEOFISA-N 0.000 claims 1
- MXMZHPBJYLDKFX-UHFFFAOYSA-N 7-[[[3,4-dihydroxy-2-(hydroxymethyl)butyl]amino]methyl]-1,5-dihydropyrrolo[3,2-d]pyrimidin-4-one Chemical compound N1=CNC(=O)C2=C1C(CNCC(CO)C(O)CO)=CN2 MXMZHPBJYLDKFX-UHFFFAOYSA-N 0.000 claims 1
- AZMNDLXJAAHUEZ-UHFFFAOYSA-N 7-[[[3-hydroxy-2-(hydroxymethyl)propyl]amino]methyl]-1,5-dihydropyrrolo[3,2-d]pyrimidin-4-one Chemical compound N1=CNC(=O)C2=C1C(CNCC(CO)CO)=CN2 AZMNDLXJAAHUEZ-UHFFFAOYSA-N 0.000 claims 1
- YSGRJXDMEAXCIA-HTQZYQBOSA-N 7-[methyl-[(2r,3s)-1,3,4-trihydroxybutan-2-yl]amino]-1,5-dihydropyrrolo[3,2-d]pyrimidin-4-one Chemical compound N1=CN=C2C(N([C@H](CO)[C@H](O)CO)C)=CNC2=C1O YSGRJXDMEAXCIA-HTQZYQBOSA-N 0.000 claims 1
- 101000594820 Homo sapiens Purine nucleoside phosphorylase Proteins 0.000 claims 1
- 101900329439 Plasmodium falciparum Purine nucleoside phosphorylase Proteins 0.000 claims 1
- 208000010362 Protozoan Infections Diseases 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 230000003287 optical effect Effects 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- 229940002612 prodrug Drugs 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 108700006317 Purine-nucleoside phosphorylases Proteins 0.000 abstract 2
- 206010037075 Protozoal infections Diseases 0.000 abstract 1
- 208000015181 infectious disease Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
-
- 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
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
- A61P33/06—Antimalarials
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- 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
-
- 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
-
- 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
-
- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Dermatology (AREA)
- Transplantation (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Enzymes And Modification Thereof (AREA)
Abstract
Spoj formule (I): naznačen time da: R4 je dihidroksipropil, dihidroksibutil, trihidroksibutil, dihidroksipentil ilitrihidroksipentil; A je N ili CH; B je OH ili alkoksi; iD je H, OH, NH2, ili SCH3;ili njegov tautomer ili njegova farmaceutski prihvatljiva sol ili njegov ester oblika prolijeka. Patent sadrži još 14 patentnih zahtjeva.
Claims (15)
1. Spoj formule (I):
[image]
naznačen time da:
R4 je dihidroksipropil, dihidroksibutil, trihidroksibutil, dihidroksipentil ili
trihidroksipentil;
A je N ili CH;
B je OH ili alkoksi; i
D je H, OH, NH2, ili SCH3;
ili njegov tautomer ili njegova farmaceutski prihvatljiva sol ili njegov ester oblika prolijeka.
2. Spoj prema zahtjevu 1 naznačen time da A je CH.
3. Spoj prema zahtjevu 1 ili zahtjevu 2 naznačen time da B je OH.
4. Spoj prema bilo kojem od zahtjeva 1 do 3 naznačen time da D je H ili NH2.
5. Spoj prema bilo kojem od zahtjeva 1 do 4 naznačen time da D je H.
6. Spoj prema zahtjevu 1, naznačen time da ima formulu:
[image]
7. Spoj prema zahtjevu 1 naznačen time da je:
(2R*,3S*)-3-((4-hidroksi-5H-pirolo[3,2-d]pirimidin-7-il)metilamino)butan-1,2,4-triol;
(R)-3-((4-hidroksi-5H-pirolo[3,2-d]pirimidin-7-il)metilamino)-propan-1,2-diol hidroklorid;
(2R,3R)-3-((4-hidroksi-5H-pirolo[3,2-d]pirimidin-7-il)metilamino)butan-1,2,4-triol hidroklorid;
2-amino-7-((2,4-dihidroksibutilamino)metil)-3H-pirolo[3,2-d]pirimidin-4(5H)-on;
7-((2,4-dihidroksibutilamino)metil)-3H-pirolo[3,2-d]pirimidin-4(5H)-on;
2-amino-7-((3,4-dihidroksi-2-(hidroksimetil)butilamino)metil)-3H-pirolo[3,2-d]pirimidin-4(5H)-on;
7-((3,4-dihidroksi-2-(hidroksimetil)butilamino)metil)-3H-pirolo[3,2-d]pirimidin-4(5H)-on;
2-amino-7-((3-hidroksi-2-(hidroksimetil)propilamino)metil)-3H-pirolo[3,2-d]pirimidin-4(5H)-on;
7-((3-hidroksi-2-(hidroksimetil)propilamino)metil)-3H-pirolo[3,2-d]pirimidin-4(5H)-on.
8. Optički izomer ili stereoizomer spoja prema bilo kojem od zahtjeva 1-7.
9. Spoj prema zahtjevu 1 naznačen time da je (2S,3R)-3-((4-hidroksi-5H-pirolo[3,2-d]pirimidin-7-il)-metilamino)butan-1,2,4-triol koji ima formulu:
[image]
10. Farmaceutski pripravak naznačen time da sadrži farmaceutski učinkovitu količinu spoja prema bilo kojem od zahtjeva 1 do 9.
11. Spoj prema bilo kojem od zahtjeva 1 do 9 naznačen time da je za upotrebu kao lijek.
12. Spoj prema bilo kojem od zahtjeva 1 do 9 naznačen time da je za upotrebu kod liječenja bolesti ili stanja kod kojeg je poželjno inhibirati purinsku nukleozidnu fosforilazu ili nukleozidnu hidrolazu.
13. Upotreba spoja prema bilo kojem od zahtjeva 1 do 9 naznačena time da je za proizvodnju lijeka za liječenje bolesti ili stanja kod kojeg je poželjno inhibirati purinsku nukleozidnu fosforilazu ili nukleozidnu hidrolazu.
14. Spoj prema zahtjevu 12 ili upotreba prema zahtjevu 13 naznačen time da bolest ili stanje je rak, bakterijska infekcija, protozoa infekcija, ili bolest ili stanje posredovano T-stanicama.
15. Upotreba spoja prema bilo kojem od zahtjeva 12 do 14 naznačena time da purinska nukleozidna fosforilaza je humana purinska nukleozidna fosforilaza (Hs PNP) ili Plasmodium falciparum purinska nukleozidna fosforilaza (Pf PNP).
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US84286706P | 2006-09-07 | 2006-09-07 | |
PCT/NZ2007/000261 WO2008030119A1 (en) | 2006-09-07 | 2007-09-07 | Acyclic amine inhibitors of nucleoside phosphorylases and hydrolases |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20110408T1 true HRP20110408T1 (hr) | 2011-06-30 |
Family
ID=39157466
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HR20110408T HRP20110408T1 (hr) | 2006-09-07 | 2011-05-31 | Inhibitori nukleozidnih fosforilaza i hidrolaza acikličkog amina |
Country Status (20)
Country | Link |
---|---|
US (1) | US8853224B2 (hr) |
EP (2) | EP2395005A1 (hr) |
JP (1) | JP5388067B2 (hr) |
KR (1) | KR101433621B1 (hr) |
CN (1) | CN101528749B (hr) |
AT (1) | ATE502038T1 (hr) |
AU (1) | AU2007293774C1 (hr) |
CA (1) | CA2662628C (hr) |
CY (1) | CY1111507T1 (hr) |
DE (1) | DE602007013252D1 (hr) |
DK (1) | DK2057165T3 (hr) |
ES (1) | ES2362805T3 (hr) |
HK (1) | HK1131612A1 (hr) |
HR (1) | HRP20110408T1 (hr) |
NZ (1) | NZ575365A (hr) |
PL (1) | PL2057165T3 (hr) |
PT (1) | PT2057165E (hr) |
RS (1) | RS51864B (hr) |
SI (1) | SI2057165T1 (hr) |
WO (1) | WO2008030119A1 (hr) |
Families Citing this family (37)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DK1539783T3 (da) | 2002-08-21 | 2011-06-20 | Einstein Coll Med | Inhibitorer af nucleosidphosphorylaser og nucleosidaser |
NZ533360A (en) | 2004-06-04 | 2007-02-23 | Ind Res Ltd | Improved method for preparing 3-hydroxy-4-hydroxymethyl-pyrrolidine compounds |
WO2007016291A2 (en) * | 2005-07-27 | 2007-02-08 | Albert Einstein College Of Medicine Of Yeshiva University | Transition state structure of 5'-methylthioadenosine/s-adenosylhomocysteine nucleosidases |
US8394950B2 (en) * | 2006-02-22 | 2013-03-12 | Industrial Research Limited | Analogues of coformycin and their use for treating protozoan parasite infections |
WO2007097647A1 (en) | 2006-02-24 | 2007-08-30 | Albert Einstein College Of Medicine Of Yeshiva University | Methods of treating cancer |
CA2662626C (en) * | 2006-09-07 | 2016-07-26 | Industrial Research Limited | Acyclic amine inhibitors of 5'-methylthioadenosine phosphorylase and nucleosidase |
CN101600711A (zh) | 2006-12-22 | 2009-12-09 | 工业研究有限公司 | 核苷酶和磷酸化酶抑制剂的氮杂环丁烷类似物 |
US20090247750A1 (en) * | 2008-03-28 | 2009-10-01 | Biocryst Pharmaceuticals, Inc. | Process for preparing nucleoside analogs |
US20110190265A1 (en) * | 2008-09-22 | 2011-08-04 | Schramm Vern L | Methods and compositions for treating bacterial infections by inhibiting quorum sensing |
CA2768291C (en) | 2009-07-17 | 2018-03-27 | Albert Einstein College Of Medicine Of Yeshiva University | 3-hydroxypyrrolidine inhibitors of 5'-methylthioadenosine phosphorylase and nucleosidase |
AR077898A1 (es) | 2009-08-26 | 2011-09-28 | Nycomed Gmbh | Metilpirrolopirimidincarboxamidas |
MX2012004340A (es) | 2009-10-16 | 2012-11-23 | Rib X Pharmaceuticals Inc | Compuestos antimicrobianos y metodos para fabricar y utilizar los mismos. |
CN102712657A (zh) | 2009-10-16 | 2012-10-03 | Rib-X制药公司 | 抗微生物化合物和其制备和使用方法 |
CA2777741A1 (en) | 2009-10-16 | 2011-04-21 | Rib-X Pharmaceuticals, Inc. | Antimicrobial compounds and methods of making and using the same |
LT2898885T (lt) | 2010-10-15 | 2018-02-26 | Biocryst Pharmaceuticals, Inc. | Pirolopirimidino dariniai, skirti naudoti virusinių infekcijų gydymui |
US9290501B2 (en) | 2010-11-29 | 2016-03-22 | Albert Einstein College Of Medicine, Inc. | Methods, assays and compounds for treating bacterial infections by inhibiting methylthioinosine phosphorylase |
WO2012071896A1 (en) * | 2010-11-30 | 2012-06-07 | Wuxi Adessonanotech Co., Limited | Novel agents for reworkable epoxy resins |
PT2697229T (pt) * | 2011-04-15 | 2018-04-13 | Melinta Therapeutics Inc | Compostos antimicrobianos e seus métodos de fabrico e de utilização |
WO2012150866A1 (en) * | 2011-05-03 | 2012-11-08 | Industrial Research Limited | Phosphoribosyltransferase inhibitors and uses thereof |
EP2741765B9 (fr) | 2011-08-10 | 2016-09-28 | Adocia | Solution injectable d'au moins une insuline basale |
BR112014016889A8 (pt) | 2012-01-09 | 2017-07-04 | Adocia | composição sob a forma de uma solução aquosa injetável, sujo ph está compreendido entre 6,0 e 8,0 e, formulação de dose unitária com ph compreendido entre 7 e 7,8 |
US11186575B2 (en) | 2012-08-07 | 2021-11-30 | Alber Einslein College of Medicine | Treatment of helicobacter pylori infections |
US20150314003A2 (en) | 2012-08-09 | 2015-11-05 | Adocia | Injectable solution at ph 7 comprising at least one basal insulin the isoelectric point of which is between 5.8 and 8.5 and a hydrophobized anionic polymer |
FR3001895B1 (fr) | 2013-02-12 | 2015-07-03 | Adocia | Solution injectable a ph7 comprenant au moins une insuline basale dont le point isoelectrique est compris en 5,8 et 8,5 et un compose anionique porteur de charges carboxylates et de radicaux hydrophobes |
US9452217B2 (en) | 2013-06-22 | 2016-09-27 | Nitor Therapeutics | Methods for potentiating immune response for the treatment of infectious diseases and cancer |
PT3252058T (pt) | 2013-07-12 | 2021-03-09 | Gilead Sciences Inc | Compostos policíclicos-carbamoílpiridona e seu uso para o tratamento de infecções por hiv |
NO2865735T3 (hr) | 2013-07-12 | 2018-07-21 | ||
JP2016536338A (ja) | 2013-09-09 | 2016-11-24 | メリンタ セラピューティクス,インコーポレイテッド | 抗微生物化合物ならびにそれの製造方法および使用方法 |
JP2016529325A (ja) | 2013-09-09 | 2016-09-23 | メリンタ セラピューティクス,インコーポレイテッド | 抗微生物化合物ならびにそれの製造方法および使用方法 |
NZ724103A (en) | 2014-02-12 | 2020-07-31 | Albert Einstein College Medicine Inc | Treatment of h. pylori infections using mtan inhibitors |
CA2979342A1 (en) | 2015-03-11 | 2016-09-15 | Melinta Therapeutics, Inc. | Antimicrobial compounds and methods of making and using the same |
EP3426659A4 (en) | 2016-03-06 | 2019-12-25 | Biocryst Pharmaceuticals, Inc. | METHODS AND COMPOSITIONS FOR THE TREATMENT OF ZIKA VIRUS INFECTION |
BR112018017117B1 (pt) * | 2016-03-15 | 2021-11-16 | Shionogi & Co., Ltd. | Metodo de produqao para derivados de fenoxietanol |
CA3023317A1 (en) | 2016-05-06 | 2017-11-09 | Melinta Therapeutics, Inc. | Antimicrobials and methods of making and using same |
CN113045484B (zh) * | 2019-12-27 | 2024-01-26 | 南京药石科技股份有限公司 | 一种2-氨基-2-(1-甲基-4-哌啶基)丙烷-1-醇的制备方法 |
CN111320634A (zh) * | 2020-04-14 | 2020-06-23 | 浙江工业大学 | 一种乙酰氧取代的吡咯并[2,3-d]嘧啶衍生物的制备方法 |
GB202218782D0 (en) | 2022-12-13 | 2023-01-25 | Mehrling Thomas | Purine nucleoside phosphorylase inhibitor for metabolic syndrome |
Family Cites Families (28)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH0920777A (ja) * | 1995-06-30 | 1997-01-21 | Nippon Paper Ind Co Ltd | 新規なプリンヌクレオシド誘導体、その製造方法及びその誘導体を有効成分とする酵素阻害剤 |
WO1997031008A1 (en) | 1996-02-23 | 1997-08-28 | Industrial Research Limited | Enzyme detection/assay method and substrates |
US5985848A (en) | 1997-10-14 | 1999-11-16 | Albert Einstein College Of Medicine Of Yeshiva University | Inhibitors of nucleoside metabolism |
US6228741B1 (en) | 1998-01-13 | 2001-05-08 | Texas Instruments Incorporated | Method for trench isolation of semiconductor devices |
JP4430247B2 (ja) | 1999-04-08 | 2010-03-10 | インダストリアル リサーチ リミテッド | ヌクレオシド代謝インヒビターの製造方法 |
US6448799B1 (en) * | 1999-09-30 | 2002-09-10 | Hitachi Electronics Engineering Co., Ltd. | Timing adjustment method and apparatus for semiconductor IC tester |
WO2002018371A1 (en) | 2000-08-29 | 2002-03-07 | Industrial Research Limited | Nucleoside metabolism inhibitors |
US6458799B1 (en) | 2000-08-31 | 2002-10-01 | Biocryst Pharmaceuticals, Inc. | Deazaguanine analog, preparation thereof and use thereof |
JP2002296365A (ja) * | 2001-03-29 | 2002-10-09 | Seiko Epson Corp | 電子機器、電子制御式機械時計、電子機器の制御方法 |
TW200306191A (en) | 2002-02-22 | 2003-11-16 | Teijin Ltd | Pyrrolopyrimidine derivatives |
US7098334B2 (en) | 2002-03-25 | 2006-08-29 | Industrial Research Limited | 4-amino-5H-pyrrolo[3,2-d]pyrimidine inhibitors of nucleoside phosphorylases and nucleosidases |
DK1539783T3 (da) | 2002-08-21 | 2011-06-20 | Einstein Coll Med | Inhibitorer af nucleosidphosphorylaser og nucleosidaser |
GB0301736D0 (en) | 2003-01-24 | 2003-02-26 | Xenova Ltd | Pharmaceutical compounds |
NZ523970A (en) | 2003-02-04 | 2005-02-25 | Ind Res Ltd | Process for preparing inhibitors of nucleoside phoshorylases and nucleosidases |
NZ533360A (en) | 2004-06-04 | 2007-02-23 | Ind Res Ltd | Improved method for preparing 3-hydroxy-4-hydroxymethyl-pyrrolidine compounds |
EP1771452A4 (en) | 2004-07-27 | 2009-07-15 | Biocryst Pharm Inc | 5'-METHYLTHIOADENOSINE PHOSPHORYLASE AND 5'METHYL THIOADENOSINE / S-ADENOSYLHOMOCYSTEIN NUCLEOSIDASE HEMMER |
NZ540160A (en) | 2005-05-20 | 2008-03-28 | Einstein Coll Med | Inhibitors of nucleoside phosphorylases |
WO2007016291A2 (en) | 2005-07-27 | 2007-02-08 | Albert Einstein College Of Medicine Of Yeshiva University | Transition state structure of 5'-methylthioadenosine/s-adenosylhomocysteine nucleosidases |
NZ544187A (en) | 2005-12-15 | 2008-07-31 | Ind Res Ltd | Deazapurine analogs of 1'-aza-l-nucleosides |
CN101384594A (zh) | 2005-12-23 | 2009-03-11 | 诺瓦提斯公司 | 用作dpp-iv抑制剂的稠合杂环化合物 |
US20110092521A1 (en) | 2006-02-24 | 2011-04-21 | Richard Hubert Furneaux | Methods of Treating Diseases Using Inhibitors of Nucleoside Phosphorylases and Nucleosidases |
WO2007097647A1 (en) | 2006-02-24 | 2007-08-30 | Albert Einstein College Of Medicine Of Yeshiva University | Methods of treating cancer |
CA2662626C (en) | 2006-09-07 | 2016-07-26 | Industrial Research Limited | Acyclic amine inhibitors of 5'-methylthioadenosine phosphorylase and nucleosidase |
WO2008039324A1 (en) | 2006-09-26 | 2008-04-03 | Albert Einstein College Of Medicine Of Yeshiva University | Transition state structure of human 5'-methylthioadenosine phosphorylase |
CN101600711A (zh) | 2006-12-22 | 2009-12-09 | 工业研究有限公司 | 核苷酶和磷酸化酶抑制剂的氮杂环丁烷类似物 |
WO2009082247A1 (en) | 2007-12-21 | 2009-07-02 | Industrial Research Limited | Process for preparing immucillins having a methylene link |
US20110190265A1 (en) | 2008-09-22 | 2011-08-04 | Schramm Vern L | Methods and compositions for treating bacterial infections by inhibiting quorum sensing |
CA2768291C (en) | 2009-07-17 | 2018-03-27 | Albert Einstein College Of Medicine Of Yeshiva University | 3-hydroxypyrrolidine inhibitors of 5'-methylthioadenosine phosphorylase and nucleosidase |
-
2007
- 2007-09-07 AT AT07834863T patent/ATE502038T1/de active
- 2007-09-07 US US12/310,708 patent/US8853224B2/en active Active
- 2007-09-07 PT PT07834863T patent/PT2057165E/pt unknown
- 2007-09-07 CN CN2007800402949A patent/CN101528749B/zh active Active
- 2007-09-07 SI SI200730602T patent/SI2057165T1/sl unknown
- 2007-09-07 NZ NZ575365A patent/NZ575365A/en unknown
- 2007-09-07 ES ES07834863T patent/ES2362805T3/es active Active
- 2007-09-07 KR KR1020097006628A patent/KR101433621B1/ko active IP Right Grant
- 2007-09-07 CA CA2662628A patent/CA2662628C/en active Active
- 2007-09-07 EP EP11158228A patent/EP2395005A1/en not_active Withdrawn
- 2007-09-07 DE DE602007013252T patent/DE602007013252D1/de active Active
- 2007-09-07 AU AU2007293774A patent/AU2007293774C1/en active Active
- 2007-09-07 RS RS20110192A patent/RS51864B/en unknown
- 2007-09-07 EP EP07834863A patent/EP2057165B1/en active Active
- 2007-09-07 JP JP2009527314A patent/JP5388067B2/ja active Active
- 2007-09-07 WO PCT/NZ2007/000261 patent/WO2008030119A1/en active Application Filing
- 2007-09-07 DK DK07834863.8T patent/DK2057165T3/da active
- 2007-09-07 PL PL07834863T patent/PL2057165T3/pl unknown
-
2009
- 2009-11-10 HK HK09110497.8A patent/HK1131612A1/xx unknown
-
2011
- 2011-05-31 CY CY20111100525T patent/CY1111507T1/el unknown
- 2011-05-31 HR HR20110408T patent/HRP20110408T1/hr unknown
Also Published As
Publication number | Publication date |
---|---|
CA2662628A1 (en) | 2008-03-13 |
PL2057165T3 (pl) | 2011-08-31 |
WO2008030119A1 (en) | 2008-03-13 |
CN101528749A (zh) | 2009-09-09 |
PT2057165E (pt) | 2011-05-12 |
NZ575365A (en) | 2012-02-24 |
AU2007293774A1 (en) | 2008-03-13 |
EP2395005A1 (en) | 2011-12-14 |
ES2362805T3 (es) | 2011-07-13 |
JP2010502696A (ja) | 2010-01-28 |
EP2057165B1 (en) | 2011-03-16 |
EP2057165A1 (en) | 2009-05-13 |
CN101528749B (zh) | 2013-07-31 |
JP5388067B2 (ja) | 2014-01-15 |
DE602007013252D1 (de) | 2011-04-28 |
WO2008030119A9 (en) | 2009-09-24 |
ATE502038T1 (de) | 2011-04-15 |
EP2057165A4 (en) | 2009-09-02 |
AU2007293774C1 (en) | 2014-12-18 |
SI2057165T1 (sl) | 2011-07-29 |
KR101433621B1 (ko) | 2014-08-27 |
US20110130412A1 (en) | 2011-06-02 |
DK2057165T3 (da) | 2011-06-27 |
US8853224B2 (en) | 2014-10-07 |
RS51864B (en) | 2012-02-29 |
HK1131612A1 (en) | 2010-01-29 |
AU2007293774B2 (en) | 2013-07-04 |
KR20090069281A (ko) | 2009-06-30 |
CA2662628C (en) | 2016-02-09 |
CY1111507T1 (el) | 2015-08-05 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
HRP20110408T1 (hr) | Inhibitori nukleozidnih fosforilaza i hidrolaza acikličkog amina | |
MY150059A (en) | Pyrrolo [2,3-d] pyrimidin derivatives as protein kinase b inhibitors | |
UY30408A1 (es) | Derivados sustituidos del acetato de 8-(4-metoxifenil)-2,3,4,8-tetrahidroimidazo-[1,5-a]-pirimidin-6-amina, composiciones farmacéuticas y aplicaciones | |
MA33670B1 (fr) | Derives de pyrrolo[2,3-d]pyrimidine | |
MA30226B1 (fr) | Agents cytotoxiques comprenant de nouveaux derives de tomaymycine et leur utilisation therapeutique. | |
EA201070841A1 (ru) | НОВЫЕ ПИРАЗОЛО[3,4-d]ПИРИМИДИНОВЫЕ ПРОИЗВОДНЫЕ В КАЧЕСТВЕ ПРОТИВОРАКОВЫХ ЛЕКАРСТВЕННЫХ СРЕДСТВ | |
EA200600973A1 (ru) | ПИРИДО[2,3-d] ПИРИМИДИН-2,4-ДИАМИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ PDE 2 | |
HK1136489A1 (en) | Imidazotriazines and imidazopyrimidines as kinase inhibitors | |
BRPI0509369A (pt) | azaindóis úteis como inibidores de jak e outras proteìna cinases | |
EA201001017A1 (ru) | 3h-[1,2,3]триазоло[4,5-d]пиримидиновые соединения, их применение в качестве ингибиторов киназы mtor и киназы pi3 и их синтезы | |
MEP13408A (en) | Cdk inhibiting pyrimidines, production thereof and their use as medicaments | |
BR122013028005B8 (pt) | compostos de ciclopentanos de pirimidila hidroxilados e metoxilados, composição farmacêutica, kit e forma de dosagem oral compreendendo os referidos compostos, uso das referidas composições, bem como processo de preparação dos referidos compostos | |
EA200970287A1 (ru) | Способы, соединения, композиции и носители, подходящие для доставки 3-амино-1-пропансульфоновой кислоты | |
EA200801998A1 (ru) | ПИРИДИН[3,4-b]ПИРАЗИНОНЫ | |
NZ701440A (en) | Pyrazole derivatives as jak inhibitors | |
MX2012007273A (es) | Pteridinonas como inhibidores de la quinasa tipo polo. | |
EA201101395A1 (ru) | Производные 1-гетероциклил-1,5-дигидропиразоло[3,4d]пиримидин-4-oha и их применение в качестве модуляторов pde9a | |
MY135902A (en) | SUBSTITUTED HEXAHYDROPYRAZINO [1, 2-a] PYRIMIDINE-4, 7-DIONE DERIVATIVES, PROCESSES FOR THEIR PREPARATION AND THEIR USE AS MEDICAMENTS | |
EA201000614A1 (ru) | Производные пурина как лиганды аденозинового рецептора а | |
ES2939004T3 (es) | Derivados de pirimidina para la prevención y tratamiento de infecciones bacterianas | |
BRPI0414864A (pt) | composição farmacêutica multiparticulada compreendendo ácido micofenólico ou micofenolato de sódio e combinação com rapamicida | |
BRPI0516626A (pt) | pteridinas substituìdas e uso das mesmas | |
CO5690567A2 (es) | Formulaciones de tableta de liberacion extendida de venlafaxina | |
HRP20161529T1 (hr) | Spoj benzazepina | |
MA31630B1 (fr) | Dérivés de 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine-6-carboxamides et de 2,3,4,5-tetrahydropyrrolo[1,2-a][1,4]-diazépine-7-carboxamides, leur préparation et leur application en thérapeutique |