ME02729B - Indolski i indazolski spojevi koji aktiviraju ampk - Google Patents
Indolski i indazolski spojevi koji aktiviraju ampkInfo
- Publication number
- ME02729B ME02729B MEP-2017-137A MEP2017137A ME02729B ME 02729 B ME02729 B ME 02729B ME P2017137 A MEP2017137 A ME P2017137A ME 02729 B ME02729 B ME 02729B
- Authority
- ME
- Montenegro
- Prior art keywords
- hydroxycyclobutyl
- indole
- carboxylic acid
- phenyl
- chloro
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title claims 7
- 102100036009 5'-AMP-activated protein kinase catalytic subunit alpha-2 Human genes 0.000 title 1
- 101000783681 Homo sapiens 5'-AMP-activated protein kinase catalytic subunit alpha-2 Proteins 0.000 title 1
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical compound C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 title 1
- 239000012190 activator Substances 0.000 title 1
- 150000003839 salts Chemical class 0.000 claims 3
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- VPUNMIRZXILGLE-UHFFFAOYSA-N 4,6-difluoro-5-[4-(1-hydroxycyclobutyl)phenyl]-1h-indole-3-carboxylic acid Chemical compound FC1=C2C(C(=O)O)=CNC2=CC(F)=C1C(C=C1)=CC=C1C1(O)CCC1 VPUNMIRZXILGLE-UHFFFAOYSA-N 0.000 claims 1
- HFTSUSPGKRQUGS-UHFFFAOYSA-N 6-chloro-5-[2-fluoro-4-(1-hydroxycyclobutyl)phenyl]-1h-indole-3-carboxylic acid Chemical compound C1=C2C(C(=O)O)=CNC2=CC(Cl)=C1C(C(=C1)F)=CC=C1C1(O)CCC1 HFTSUSPGKRQUGS-UHFFFAOYSA-N 0.000 claims 1
- VJRMUMYLSWYBNV-UHFFFAOYSA-N 6-chloro-5-[3-fluoro-4-(1-hydroxycyclobutyl)phenyl]-1h-indole-3-carboxylic acid Chemical compound C1=C2C(C(=O)O)=CNC2=CC(Cl)=C1C(C=C1F)=CC=C1C1(O)CCC1 VJRMUMYLSWYBNV-UHFFFAOYSA-N 0.000 claims 1
- KMRDDGOECBQZPA-UHFFFAOYSA-N 6-chloro-5-[4-(1-hydroxycyclobutyl)-3-methoxyphenyl]-1h-indole-3-carboxylic acid Chemical compound COC1=CC(C=2C(=CC=3NC=C(C=3C=2)C(O)=O)Cl)=CC=C1C1(O)CCC1 KMRDDGOECBQZPA-UHFFFAOYSA-N 0.000 claims 1
- FHQXLWCFSUSXBF-UHFFFAOYSA-N 6-chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1h-indole-3-carboxylic acid Chemical group C1=C2C(C(=O)O)=CNC2=CC(Cl)=C1C(C=C1)=CC=C1C1(O)CCC1 FHQXLWCFSUSXBF-UHFFFAOYSA-N 0.000 claims 1
- RQZSOXIQLVNMAF-UHFFFAOYSA-N 6-chloro-5-[4-(3-hydroxycyclobutyl)phenyl]-1h-indole-3-carboxylic acid Chemical compound C1C(O)CC1C1=CC=C(C=2C(=CC=3NC=C(C=3C=2)C(O)=O)Cl)C=C1 RQZSOXIQLVNMAF-UHFFFAOYSA-N 0.000 claims 1
- JCVIFVYRMKVCDU-UHFFFAOYSA-N 6-fluoro-5-[4-(1-hydroxycyclobutyl)phenyl]-1h-indole-3-carboxylic acid Chemical compound C1=C2C(C(=O)O)=CNC2=CC(F)=C1C(C=C1)=CC=C1C1(O)CCC1 JCVIFVYRMKVCDU-UHFFFAOYSA-N 0.000 claims 1
- 208000009304 Acute Kidney Injury Diseases 0.000 claims 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 1
- 208000032928 Dyslipidaemia Diseases 0.000 claims 1
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 208000033626 Renal failure acute Diseases 0.000 claims 1
- 201000011040 acute kidney failure Diseases 0.000 claims 1
- 239000002585 base Substances 0.000 claims 1
- 208000020832 chronic kidney disease Diseases 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 208000033679 diabetic kidney disease Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 208000030761 polycystic kidney disease Diseases 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
Classifications
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic 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
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- 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
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
- C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
- C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D405/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D405/10—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 carbon chain containing aromatic 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
- 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
- C07D405/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Diabetes (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Child & Adolescent Psychology (AREA)
- Urology & Nephrology (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Indole Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Cosmetics (AREA)
Claims (6)
1. Spoj Formule (II) , naznačen time što X je CH; L je veza; R1 je -C(O)ORA; RA je H; R2 je H ili F; R3 je Cl, F ili CN; R4 i R5 su H; R6 i R7 su neovisno H, F ili metoksi; R9 i R10 su H; i R8 je (C3-C8)cikloalkil, gdje je (C3-C8)cikloalkil ciklobutil supstituiran s hidroksilom; ili njegova farmaceutski prihvatljiva sol.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je 6-klor-5-(4-(1-hidroksiciklobutil)fenil)-1H-indol-3-karboksilna kiselina; 6-fluor-5-(4-(1-hidroksiciklobutil)fenil)-1H-indol-3-karboksilna kiselina; 4,6-difluor-5-(4-(1-hidroksiciklobutil)fenil)-1H-indol-3-karboksilna kiselina; 6-klor-5-[2-fluor-4-(1-hidroksiciklobutil)fenil]-1H-indol-3-karboksilna kiselina; 6-klor-5-[3-fluor-4-(1-hidroksiciklobutil)fenil]-1H-indol-3-karboksilna kiselina; 6-klor-5-[4-(1-hidroksiciklobutil)-3-metoksifenil]-1H-indol-3-karboksilna kiselina; ili 6-klor-5-[4-(trans-3-hidroksiciklobutil)fenil]-1H-indol-3-karboksilna kiselina; ili njihove farmaceutski prihvatljive soli.
3. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima strukturu , ili njegova farmaceutski prihvatljiva sol.
4. Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s patentnim zahtjevom 1, kao i najmanje jednu farmaceutski prihvatljivu pomoćnu tvar, razrjeđivač ili podlogu.
5. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je namijenjen upotrebi u liječenju ili sprječavanju kronične bolesti bubrega, dijabetične nefropatije, akutne ozljede bubreg ili bolesti policističnog bubrega kod sisavca, osobito čovjeka.
6. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je namijenjen upotrebi u liječenju ili sprječavanju dijabetesa tip II, dislipidemije ili pretilosti kod sisavca, osobito čovjeka.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261622129P | 2012-04-10 | 2012-04-10 | |
| PCT/IB2013/052604 WO2013153479A2 (en) | 2012-04-10 | 2013-04-01 | Indole and indazole compounds that activate ampk |
| EP13720084.6A EP2836490B1 (en) | 2012-04-10 | 2013-04-01 | Indole and indazole compounds that activate ampk |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ME02729B true ME02729B (me) | 2017-10-20 |
Family
ID=48237173
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MEP-2017-137A ME02729B (me) | 2012-04-10 | 2013-04-01 | Indolski i indazolski spojevi koji aktiviraju ampk |
Country Status (42)
Families Citing this family (44)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI644899B (zh) | 2013-02-04 | 2018-12-21 | 健生藥品公司 | Flap調節劑 |
| EP3070085B1 (en) * | 2013-02-04 | 2019-01-09 | Janssen Pharmaceutica NV | Flap modulators |
| CA2903657A1 (en) | 2013-02-27 | 2014-09-04 | Shionogi & Co., Ltd. | Indole and azaindole derivatives each having ampk-activating activity |
| CA2905242C (en) * | 2013-03-15 | 2016-11-29 | Pfizer Inc. | Indole compounds that activate ampk |
| JP6435923B2 (ja) * | 2014-03-07 | 2018-12-12 | Jnc株式会社 | ジヒドロピラン化合物、液晶組成物および液晶表示素子 |
| AU2015309863B2 (en) | 2014-08-27 | 2019-12-05 | Shionogi & Co., Ltd. | Azaindole derivative having AMPK-activating effect |
| IL313498A (en) | 2014-10-06 | 2024-08-01 | Vertex Pharma | Modulators of the cystic fibrosis transmembrane conductance regulator |
| WO2016092413A1 (en) * | 2014-12-10 | 2016-06-16 | Pfizer Inc. | Indole and indazole compounds that activate ampk |
| JP6683712B2 (ja) | 2014-12-24 | 2020-04-22 | ナショナル・インスティチュート・オブ・バイオロジカル・サイエンシズ,ベイジン | ネクローシス阻害薬 |
| US10919875B2 (en) | 2015-06-18 | 2021-02-16 | 89Bio Ltd | Substituted 4-benzyl and 4-benzoyl piperidine derivatives |
| ES2821049T3 (es) * | 2015-06-18 | 2021-04-23 | 89Bio Ltd | Derivados de piperidina 1,4 sustituidos |
| WO2017011917A1 (en) * | 2015-07-23 | 2017-01-26 | Thrasos Therapeutics Inc. | Methods for treating and preventing polycystic kidney diseases (pkd) using amp-activated protein kinase (ampk) modulators and activators |
| JPWO2017146186A1 (ja) | 2016-02-26 | 2018-12-20 | 塩野義製薬株式会社 | Ampk活性化作用を有する5−フェニルアザインドール誘導体 |
| EP3436446B1 (en) | 2016-03-31 | 2023-06-07 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| PT3442535T (pt) * | 2016-04-15 | 2022-09-05 | Cancer Research Tech Ltd | Compostos heterocíclicos como inibidores da ret quinase |
| RS62322B1 (sr) | 2016-04-15 | 2021-10-29 | Cancer Research Tech Ltd | Heterociklična jedinjenja kao inhibitori ret kinaze |
| CN114539273A (zh) | 2016-06-07 | 2022-05-27 | 北京加科思新药研发有限公司 | 可用作shp2抑制剂的新型杂环衍生物 |
| WO2018002215A1 (en) | 2016-06-30 | 2018-01-04 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and pharmaceutical compositions for the treatment of cardiomyopathies |
| HRP20211683T1 (hr) | 2016-09-30 | 2022-03-04 | Vertex Pharmaceuticals Incorporated | Modulator transmembranskog regulatora provodljivosti cistične fibroze, farmaceutski pripravci, postupci liječenja, i postupak za pripravu modulatora |
| MX2021013639A (es) | 2016-12-09 | 2022-09-30 | Vertex Pharma | Forma cristalina del compuesto 1, un modulador del regulador de conductancia transmembrana de fibrosis quística, procesos para su preparación, composiciones farmacéuticas del compuesto 1, y su uso en el tratamiento de fibrosis quística. |
| HRP20241239T1 (hr) | 2017-03-23 | 2024-12-06 | Jacobio Pharmaceuticals Co., Ltd. | Novi heterociklički derivati korisni kao shp2 inhibitori |
| GB201705971D0 (en) | 2017-04-13 | 2017-05-31 | Cancer Res Tech Ltd | Inhibitor compounds |
| AU2018279646B2 (en) | 2017-06-08 | 2023-04-06 | Vertex Pharmaceuticals Incorporated | Methods of treatment for cystic fibrosis |
| AU2018304168B2 (en) | 2017-07-17 | 2023-05-04 | Vertex Pharmaceuticals Incorporated | Methods of treatment for cystic fibrosis |
| TWI799435B (zh) | 2017-08-02 | 2023-04-21 | 美商維泰克斯製藥公司 | 製備化合物之製程 |
| WO2019079760A1 (en) | 2017-10-19 | 2019-04-25 | Vertex Pharmaceuticals Incorporated | CRYSTALLINE FORMS AND COMPOSITIONS OF CFTR MODULATORS |
| US11465985B2 (en) | 2017-12-08 | 2022-10-11 | Vertex Pharmaceuticals Incorporated | Processes for making modulators of cystic fibrosis transmembrane conductance regulator |
| TWI810243B (zh) | 2018-02-05 | 2023-08-01 | 美商維泰克斯製藥公司 | 用於治療囊腫纖化症之醫藥組合物 |
| US11760701B2 (en) | 2018-02-27 | 2023-09-19 | The Research Foundation For The State University Of New Yrok | Difluoromethoxylation and trifluoromethoxylation compositions and methods for synthesizing same |
| KR102224550B1 (ko) * | 2018-04-02 | 2021-03-09 | 울산대학교 산학협력단 | 신규한 에테르 화합물, 및 광 산화환원 촉매를 이용하여 활성화된 알켄 화합물로부터 에테르 화합물을 제조하는 방법 |
| WO2019200246A1 (en) | 2018-04-13 | 2019-10-17 | Alexander Russell Abela | Modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator |
| CN108572223B (zh) * | 2018-04-23 | 2021-01-26 | 南京明捷生物医药检测有限公司 | 一种测定多肽中活性诱导物质的方法 |
| MX2021003156A (es) | 2018-09-18 | 2021-05-14 | 1 Globe Biomedical Co Ltd | Tratamiento para la enfermedad del higado graso no alcoholico. |
| WO2020063760A1 (en) | 2018-09-26 | 2020-04-02 | Jacobio Pharmaceuticals Co., Ltd. | Novel heterocyclic derivatives useful as shp2 inhibitors |
| EP3906027A4 (en) * | 2018-12-31 | 2022-09-21 | The Board of Trustees of the Leland Stanford Junior University | METHODS AND FORMULATIONS FOR THE TREATMENT OF MITOCHONDRIAL DYSFUNCTION |
| WO2020201263A1 (en) | 2019-04-01 | 2020-10-08 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and pharmaceutical compositions for the treatment and prevention of cardiac remodeling |
| CN112441900B (zh) * | 2019-09-05 | 2024-07-23 | 浙江中科创越药业有限公司 | 4-联苯乙酸的制备方法 |
| CN111333486A (zh) * | 2020-04-08 | 2020-06-26 | 南京优氟医药科技有限公司 | 一种2-甲基-2-(4-氯苯基)-1,3-丙二醇的生产工艺 |
| JP2023526625A (ja) | 2020-05-19 | 2023-06-22 | キャリーオペ,インク. | Ampkアクチベーター |
| CN111423379B (zh) * | 2020-05-21 | 2021-08-03 | 湖南科技大学 | 取代3-吲唑类Mcl-1蛋白抑制剂及制备方法和应用 |
| CN116390925A (zh) | 2020-06-26 | 2023-07-04 | 卡尔优普公司 | Ampk活化剂 |
| EP4221700A1 (en) * | 2020-09-30 | 2023-08-09 | Bioverativ Therapeutics Inc. | Ampk activators and methods of use thereof |
| WO2025021039A1 (zh) * | 2023-07-21 | 2025-01-30 | 深圳众格生物科技有限公司 | Ampk激动剂及其用途 |
| WO2025045185A1 (zh) * | 2023-08-31 | 2025-03-06 | 深圳众格生物科技有限公司 | 芳基或杂芳基取代的氨基甲酸酯类化合物及其衍生物和用途 |
Family Cites Families (281)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0010061B1 (en) | 1978-09-25 | 1983-07-13 | Stuart John Mc Farlane | Pharmaceutical preparations containing a mollusc extract |
| JP2602037B2 (ja) | 1987-10-31 | 1997-04-23 | 持田製薬株式会社 | 1−アシル−2,3−ジヒドロ−4(1h)−キノリノン−4−オキシム誘導体、その製法およびそれらを主成分とする利尿、降圧、抗浮腫および腹水除去用医薬組成物 |
| GB8814277D0 (en) | 1988-06-16 | 1988-07-20 | Glaxo Group Ltd | Chemical compounds |
| JPH02264757A (ja) | 1989-04-06 | 1990-10-29 | Nippon Steel Chem Co Ltd | ニトロインドール類の製造方法 |
| US5210092A (en) | 1990-09-25 | 1993-05-11 | Fujisawa Pharmaceutical Co., Ltd. | Angiotensin ii antagonizing heterocyclic derivatives |
| US5215994A (en) | 1990-09-25 | 1993-06-01 | Fujisawa Pharmaceutical Co., Ltd. | Angiotenin II antagonizing heterocyclic derivatives |
| US5354759A (en) | 1991-09-12 | 1994-10-11 | Fujisawa Pharmaceutical Co., Ltd. | Angiotenin II antagonizing heterocyclic compounds |
| WO1993006082A1 (en) | 1991-09-13 | 1993-04-01 | Merck & Co., Inc. | Process for the preparation of 4-substituted-1,4-dihydropyridines |
| DE4136489A1 (de) | 1991-11-06 | 1993-05-13 | Bayer Ag | Neue diethylentriamin-derivate und deren verwendung zu diagnostischen und therapeutischen zwecken |
| TW212798B (me) | 1991-11-25 | 1993-09-11 | Takeda Pharm Industry Co Ltd | |
| CA2083891A1 (en) | 1991-12-03 | 1993-06-04 | Angus Murray Macleod | Heterocyclic compounds, compositions containing them and their use in therapy |
| EP0597112A4 (en) | 1992-03-27 | 1994-06-22 | Kyoto Pharma Ind | Novel imidazole derivative, pharmaceutical use thereof, and intermediate therefor. |
| JP3229654B2 (ja) | 1992-06-05 | 2001-11-19 | ティーディーケイ株式会社 | 有機el素子用化合物および有機el素子 |
| BR9305569A (pt) | 1992-07-03 | 1995-12-26 | Kumiai Chemical Industry Co | Derivados heterocíclicos condensados e herbicidas |
| GB2271991A (en) | 1992-11-02 | 1994-05-04 | Merck Sharp & Dohme | N-(2-oxo-1H-1,4-benzodiazepin-3-yl)-ureas |
| EP0639573A1 (de) | 1993-08-03 | 1995-02-22 | Hoechst Aktiengesellschaft | Benzokondensierte 5-Ringheterocyclen, Verfahren zu ihrer Herstellung, ihre Verwendung als Medikament, ihre Verwendung als Diagnostikum, sowie sie enthaltendes Medikament |
| US5354763A (en) | 1993-11-17 | 1994-10-11 | American Home Products Corporation | Substituted N-heteroaryl and N-aryl-1,2-diaminocyclobutene-3,4-diones |
| WO1995021836A1 (en) | 1994-02-10 | 1995-08-17 | Pfizer Inc. | 5-heteroarylindole derivatives as benzodiazepine receptor site agonists and antagonists |
| CN1166169A (zh) | 1994-07-27 | 1997-11-26 | 三共株式会社 | 用作毒蕈碱性受体别构效应物的杂环化合物 |
| FR2723739B1 (fr) | 1994-08-19 | 1997-02-14 | Sanofi Sa | Derives de glycinamide, procedes pour leur preparation et medicaments les contenant. |
| JPH08225535A (ja) | 1994-11-15 | 1996-09-03 | Dai Ichi Seiyaku Co Ltd | インダゾール誘導体 |
| EP0717143A1 (de) | 1994-12-16 | 1996-06-19 | Lignozym GmbH | Mehrkomponentensystem zum Verändern, Abbau oder Bleichen von Lignin, ligninhaltigen Materialien oder ähnlichen Stoffen sowie Verfahren zu seiner Anwendung |
| US6069156A (en) | 1995-04-10 | 2000-05-30 | Fujisawa Pharmaceutical Co., Ltd. | Indole derivatives as cGMP-PDE inhibitors |
| WO1997010214A1 (en) | 1995-09-14 | 1997-03-20 | Shionogi & Co., Ltd. | Novel phenylacetic acid derivatives and medicinal composition containing the same |
| EP0914322A1 (en) | 1996-05-27 | 1999-05-12 | Fujisawa Pharmaceutical Co., Ltd. | New indolyl and benzofuranyl carboxamides as inhibitors of nitric oxide production |
| US5629325A (en) | 1996-06-06 | 1997-05-13 | Abbott Laboratories | 3-pyridyloxymethyl heterocyclic ether compounds useful in controlling chemical synaptic transmission |
| US5861398A (en) | 1996-08-26 | 1999-01-19 | Alanex Corporation | Benzoperimidine-carboxylic acids and derivatives thereof |
| EP0973767A1 (en) | 1997-03-31 | 2000-01-26 | Dupont Pharmaceuticals Company | Indazoles of cyclic ureas useful as hiv protease inhibitors |
| PT901786E (pt) | 1997-08-11 | 2007-08-07 | Pfizer Prod Inc | Disperções farmacêuticas sólidas com biodisponibilidade melhorada |
| SE9704544D0 (sv) | 1997-12-05 | 1997-12-05 | Astra Pharma Prod | Novel compounds |
| SE9704545D0 (sv) | 1997-12-05 | 1997-12-05 | Astra Pharma Prod | Novel compounds |
| JP2002515891A (ja) | 1997-12-19 | 2002-05-28 | スミスクライン・ビーチャム・コーポレイション | 新規なピペリジン含有化合物 |
| WO1999036422A1 (en) | 1998-01-14 | 1999-07-22 | The Uab Research Foundation | Methods of synthesizing and screening inhibitors of bacterial nad synthetase enzyme, compounds thereof, and methods of treating bacterial and microbial infections with inhibitors of bacterial nad synthetase enzyme |
| CA2260499A1 (en) | 1998-01-29 | 1999-07-29 | Sumitomo Pharmaceuticals Company Limited | Pharmaceutical compositions for the treatment of ischemic brain damage |
| JP2002504541A (ja) * | 1998-02-25 | 2002-02-12 | ジェネティックス・インスチチュート・インコーポレーテッド | ホスホリパーゼ酵素阻害剤 |
| CA2332279A1 (en) | 1998-05-15 | 1999-11-25 | Jia-He Li | Carboxamide compounds, compositions, and methods for inhibiting parp activity |
| AU4981199A (en) | 1998-07-08 | 2000-02-01 | Gregory N. Beatch | Compositions and methods for modulating sexual activity |
| EE04904B1 (et) | 1998-07-15 | 2007-10-15 | Teijin Limited | Tiobensimidasooli derivaadid ja farmatseutiline kompositsioon |
| DE19842354A1 (de) | 1998-09-16 | 2000-03-23 | Bayer Ag | Isothiazolcarbonsäureamide |
| FR2783520B1 (fr) | 1998-09-21 | 2000-11-10 | Oreal | Nouveaux 4-hydroxyindoles cationiques, leur utilisation pour la teinture d'oxydation des fibres keratiniques, compositions tinctoriales et procede de teinture |
| AU1738900A (en) | 1998-11-19 | 2000-06-05 | Nortran Pharmaceuticals Inc. | Serotonin ligands as pro-erectile compounds |
| AR021509A1 (es) | 1998-12-08 | 2002-07-24 | Lundbeck & Co As H | Derivados de benzofurano, su preparacion y uso |
| CZ27399A3 (cs) | 1999-01-26 | 2000-08-16 | Ústav Experimentální Botaniky Av Čr | Substituované dusíkaté heterocyklické deriváty, způsob jejich přípravy, tyto deriváty pro použití jako léčiva, farmaceutická kompozice a kombinovaný farmaceutický přípravek tyto deriváty obsahující a použití těchto derivátů pro výrobu léčiv |
| AU7962200A (en) | 1999-10-29 | 2001-05-14 | Wakunaga Pharmaceutical Co., Ltd | Novel indole derivatives and drugs containing the same as the active ingredient |
| CN1105722C (zh) | 1999-11-12 | 2003-04-16 | 中国科学院上海药物研究所 | 含氮杂环基的青蒿素衍生物及其制备方法 |
| AU2001260081B2 (en) | 2000-05-22 | 2005-07-28 | Leo Pharma A/S | Benzophenones as inhibitors of il-1beta and tnf-alpha |
| US6995268B2 (en) | 2000-06-20 | 2006-02-07 | Wayne State University | N- and O-substituted 4-[2-(diphenylmethoxy)-ethyl]-1- (phenyl) methyl) piperidine analogs and methods of treating CNS disorders therewith |
| JP2002017387A (ja) | 2000-07-06 | 2002-01-22 | Mitsubishi Rayon Co Ltd | インドール誘導体の製造法 |
| JP2002017386A (ja) | 2000-07-06 | 2002-01-22 | Mitsubishi Rayon Co Ltd | インドール−3−カルボン酸誘導体の製造法 |
| WO2002018363A2 (en) | 2000-08-29 | 2002-03-07 | Abbott Laboratories | 3-phenyl-propanoic acid derivatives as protein tyrosine phosphatase inhibitors |
| DE10046934A1 (de) | 2000-09-21 | 2002-04-18 | Consortium Elektrochem Ind | Verfahren zur fermentativen Herstellung von nicht-proteinogenen L-Aminosäuren |
| EP1332141A1 (en) | 2000-10-25 | 2003-08-06 | AstraZeneca AB | Quinazoline derivatives |
| PT1381382E (pt) | 2000-11-01 | 2009-03-03 | Merck Patent Gmbh | Métodos e composições para o tratamento de doenças oculares |
| AU2002239277A1 (en) | 2000-11-20 | 2002-05-27 | Cor Therapeutics, Inc. | Adenine based inhibitors of adenylyl cyclase, pharmaceutical compositions and method of use thereof |
| US6387992B1 (en) | 2000-11-27 | 2002-05-14 | Ciba Specialty Chemicals Corporation | Substituted 5-heteroaryl-2-(2-hydroxyphenyl)-2h-benzotriazole UV absorbers, a process for preparation thereof and compositions stabilized therewith |
| GB0031315D0 (en) | 2000-12-21 | 2001-02-07 | Glaxo Group Ltd | Indole derivatives |
| JP4094955B2 (ja) | 2001-01-18 | 2008-06-04 | 塩野義製薬株式会社 | 置換アミノ基を有するテルフェニル化合物 |
| US20040087604A1 (en) | 2001-01-22 | 2004-05-06 | Tatsuo Tsuri | Hetero-tricyclic compounds having substituted amino groups |
| IL156793A0 (en) | 2001-02-02 | 2004-02-08 | Schering Corp | 3,4-di-substituted cyclobutene-1,2-diones as cxc chemokine receptor antagonists |
| EA200300944A1 (ru) | 2001-02-28 | 2004-04-29 | Мерк Энд Ко., Инк. | Ацилированные пиперидиновые производные в качестве агонистов рецептора-4 меланокортина |
| EP1377549A1 (en) | 2001-03-12 | 2004-01-07 | Millennium Pharmaceuticals, Inc. | Functionalized heterocycles as modulators of chemokine receptor function and methods of use therefor |
| GB0106586D0 (en) | 2001-03-16 | 2001-05-09 | Smithkline Beecham Plc | Novel compounds |
| CA2444031C (en) | 2001-04-16 | 2012-02-21 | Schering Corporation | 3,4-di-substituted cyclobutene-1,2-diones as cxc-chemokine receptor ligands |
| JPWO2002100833A1 (ja) | 2001-06-12 | 2004-09-24 | 住友製薬株式会社 | Rhoキナーゼ阻害剤 |
| EP1844771A3 (en) | 2001-06-20 | 2007-11-07 | Wyeth | Substituted indole acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1) |
| KR20040027870A (ko) | 2001-07-05 | 2004-04-01 | 시냅틱 파마세틱칼 코포레이션 | Mch 선택적인 안타고니스트로서의 치환 아닐린 피페리딘 |
| ES2243744T3 (es) | 2001-08-01 | 2005-12-01 | Merck Patent Gmbh | Inhibidores de integrina para el tratamiento de enfermedades de los ojos. |
| EP1424336A4 (en) | 2001-09-03 | 2004-11-10 | Takeda Chemical Industries Ltd | 1,3-BENZOTHIAZINE DERIVATIVES AND THEIR USE |
| CN1599734A (zh) | 2001-10-12 | 2005-03-23 | 先灵公司 | 作为cxc趋化因子受体拮抗剂的3,4-二取代的马来酰亚胺化合物 |
| FR2831536A1 (fr) | 2001-10-26 | 2003-05-02 | Aventis Pharma Sa | Nouveaux derives de benzimidazoles, leur procede de preparation, leur application a titre de medicament, compositions pharmaceutiques et nouvelle utilisation notamment comme inhibiteurs de kdr |
| EP1441725A1 (en) | 2001-10-26 | 2004-08-04 | Aventis Pharmaceuticals Inc. | Benzimidazoles and analogues and their use as protein kinases inhibitors |
| US7666867B2 (en) | 2001-10-26 | 2010-02-23 | University Of Connecticut | Heteroindanes: a new class of potent cannabimimetic ligands |
| US20030187026A1 (en) | 2001-12-13 | 2003-10-02 | Qun Li | Kinase inhibitors |
| US6933316B2 (en) | 2001-12-13 | 2005-08-23 | National Health Research Institutes | Indole compounds |
| SE0104331D0 (sv) | 2001-12-19 | 2001-12-19 | Astrazeneca Ab | Novel compounds |
| JP2003192716A (ja) | 2001-12-27 | 2003-07-09 | Mitsui Chemicals Inc | オレフィン重合用触媒および該触媒を用いたオレフィンの重合方法 |
| ATE420847T1 (de) | 2002-02-21 | 2009-01-15 | Asahi Kasei Pharma Corp | Substituiertes phenylalkansäurederivat und dessen verwendung |
| HRP20040716A2 (en) | 2002-02-27 | 2005-02-28 | Pfizer Products Inc. | Acc inhibitors |
| US7125906B2 (en) | 2002-04-03 | 2006-10-24 | Astrazeneca Ab | Indole derivatives having anti-angiogenetic activity |
| WO2003097855A2 (en) | 2002-05-14 | 2003-11-27 | Baylor College Of Medicine | Small molecule inhibitors of her2 expression |
| US7008958B2 (en) | 2002-05-21 | 2006-03-07 | Bristol-Myers Squibb Company | 2-substituted 5-oxazolyl indole compounds useful as IMPDH inhibitors and pharmaceutical compositions comprising same |
| JPWO2004004701A1 (ja) | 2002-07-09 | 2005-11-04 | アステラス製薬株式会社 | 頻尿および尿失禁治療剤 |
| US6972336B2 (en) | 2002-07-18 | 2005-12-06 | Novartis Ag | N-alkylation of indole derivatives |
| WO2004014922A1 (en) | 2002-08-10 | 2004-02-19 | Astex Technology Limited | 3-(carbonyl) 1h-indazole compounds as cyclin dependent kinases (cdk) inhibitors |
| FR2845382A1 (fr) | 2002-10-02 | 2004-04-09 | Sanofi Synthelabo | Derives d'indazolecarboxamides, leur preparation et leur utilisation en therapeutique |
| FR2846656B1 (fr) | 2002-11-05 | 2004-12-24 | Servier Lab | Nouveaux derives d'imidazopyridine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| US7423148B2 (en) | 2002-11-21 | 2008-09-09 | Chiron Corporation | Small molecule PI 3-kinase inhibitors and methods of their use |
| IS7839A (is) | 2002-11-22 | 2004-05-23 | Merck Frosst Canada Ltd. | 4-oxó-1-(3-setið fenýl-1,4-díhýdró-1,8-naftýridín-3-karboxamíð fosfódíesterasa-4 hindrar |
| AU2003237599B2 (en) | 2002-11-28 | 2009-06-18 | Suven Life Sciences Limited | N-arylsulfonyl-3-substituted indoles having serotonin receptor affinity, process for their preparation and pharmaceutical composition containing them |
| AU2003296405A1 (en) | 2003-01-06 | 2004-08-10 | Eli Lilly And Company | Fused heterocyclic derivatives as ppar modulators |
| EP1581491A1 (en) | 2003-01-06 | 2005-10-05 | Eli Lilly And Company | Indole derivatives as ppar modulators |
| CL2004000234A1 (es) | 2003-02-12 | 2005-04-15 | Biogen Idec Inc | Compuestos derivados 3-(piridin-2-il)-4-heteroaril-pirazol sustituidos, antagonistas de aik5 y/o aik4; composicion farmaceutica y uso del compuesto en el tratamiento de desordenes fibroticos como esclerodermia, lupus nefritico, cicatrizacion de herid |
| ITMI20030287A1 (it) | 2003-02-18 | 2004-08-19 | Acraf | Indazolammidi dotate di attivita' analgesica metodo, per |
| KR101152448B1 (ko) | 2003-02-21 | 2012-07-02 | 키에시 파르마슈티시 엣스. 피. 에이. | 신경 퇴행성 질환의 치료를 위한 1-페닐알캔카복실산 추출물의 제조방법 |
| JP2004284997A (ja) | 2003-03-24 | 2004-10-14 | Taoka Chem Co Ltd | 高純度インドールカルボン酸類の製造方法 |
| JP2004284998A (ja) | 2003-03-24 | 2004-10-14 | Taoka Chem Co Ltd | 1−アルキルインドール類の製造方法 |
| EP1618090A1 (en) | 2003-04-11 | 2006-01-25 | Novo Nordisk A/S | 11ß-HYDROXYSTEROID DEHYDROGENASE TYPE 1 ACTIVE COMPOUNDS |
| WO2004089415A2 (en) | 2003-04-11 | 2004-10-21 | Novo Nordisk A/S | COMBINATIONS OF AN 11β-HYDROXYSTEROID DEHYDROGENASE TYPE 1 INHIBITOR AND A GLUCOCORTICOID RECEPTOR AGONIST |
| EP1615697A2 (en) | 2003-04-11 | 2006-01-18 | Novo Nordisk A/S | New pyrazolo[1,5-a] pyrimidine derivatives and pharmaceutical use thereof |
| JP2006522750A (ja) | 2003-04-11 | 2006-10-05 | ノボ ノルディスク アクティーゼルスカブ | 代謝性症候群ならびに関連の疾患および障害を治療するために、11β−ヒドロキシステロイドデヒドロゲナーゼ1型阻害剤および抗高血圧剤を使用する併用療法 |
| WO2004089367A1 (en) | 2003-04-11 | 2004-10-21 | Novo Nordisk A/S | Pharmaceutical use of substituted 1,2,4-triazoles |
| ES2338656T3 (es) | 2003-04-11 | 2010-05-11 | High Point Pharmaceuticals, Llc | Uso farmaceutico de 1,2,4-triazoles fusionados. |
| CA2523743A1 (en) | 2003-04-30 | 2004-11-18 | The Institutes For Pharmaceutical Discovery, Llc | Heterocycle substituted carboxylic acids as inhibitors of protein tyrosine phosphatase-1b |
| US7119205B2 (en) | 2003-05-16 | 2006-10-10 | Abbott Laboratories | Thienopyridones as AMPK activators for the treatment of diabetes and obesity |
| US7429596B2 (en) | 2003-06-20 | 2008-09-30 | The Regents Of The University Of California | 1H-pyrrolo [2,3-D] pyrimidine derivatives and methods of use thereof |
| EP1648881A1 (en) | 2003-07-04 | 2006-04-26 | GlaxoSmithKline S.p.A. | Substituted indole ligands for the orl-1 receptor |
| WO2005014554A1 (en) | 2003-08-08 | 2005-02-17 | Astex Therapeutics Limited | 1h-indazole-3-carboxamide compounds as mapkap kinase modulators |
| WO2005016862A1 (en) | 2003-08-14 | 2005-02-24 | Asahi Kasei Pharma Corporation | Substituted arylalkanoic acid derivative and use thereof |
| EP2468729B1 (en) | 2003-10-15 | 2013-12-25 | Ube Industries, Ltd. | Novel indazole derivative |
| JP2005145859A (ja) | 2003-11-13 | 2005-06-09 | Nippon Steel Chem Co Ltd | 脱水素化方法及び芳香族複素環化合物の製造方法 |
| JP4458819B2 (ja) | 2003-11-13 | 2010-04-28 | 株式会社リコー | アゾ置換インドール化合物及びこれを用いた光記録媒体 |
| JP4824578B2 (ja) | 2003-12-22 | 2011-11-30 | メモリー・ファーマシューティカルズ・コーポレイション | インドール類、1,2−ベンズイソオキサゾール類、および1,2−ベンゾイソチアゾール類、ならびにそれらの製造と使用 |
| MXPA06010852A (es) | 2004-03-25 | 2007-01-16 | Memory Pharm Corp | Indazoles, benzotiazoles, benzoisotiazoles, bencisoxazoles y preparacion y usos de los mismos. |
| WO2005097203A2 (en) | 2004-04-01 | 2005-10-20 | Cardiome Pharma Corp. | Serum protein conjugates of ion channel modulating compounds and uses thereof |
| JP4510500B2 (ja) | 2004-04-15 | 2010-07-21 | 株式会社リコー | アゾ置換インドール化合物及びアゾ金属キレート化合物、並びに光記録媒体 |
| KR20070015607A (ko) | 2004-05-07 | 2007-02-05 | 메모리 파마슈티칼스 코포레이션 | 1h-인다졸, 벤조티아졸, 1,2-벤조이속사졸,1,2-벤조이소티아졸, 및 크로몬 및 그의 제조법 및 용도 |
| HRP20090471T1 (hr) | 2004-05-12 | 2009-10-31 | Pfizer Products Inc. | Derivati prolina i njihova upotreba kao inhibitori dipeptidil-peptidaze iv |
| JP4069159B2 (ja) | 2004-05-25 | 2008-04-02 | ファイザー・プロダクツ・インク | テトラアザベンゾ[e]アズレン誘導体及びそれらのアナログ |
| KR20070024667A (ko) | 2004-06-03 | 2007-03-02 | 브랜데이스 유니버시티 | 이작용성 신코나-알칼로이드 기재 촉매를 사용하는 비대칭마이클 및 알돌 부가반응 |
| WO2005123675A1 (en) | 2004-06-18 | 2005-12-29 | Biolipox Ab | Indoles useful in the treatment of inflammation |
| WO2005123673A1 (en) | 2004-06-18 | 2005-12-29 | Biolipox Ab | Indoles useful in the treatment of inflammation |
| US20080146811A1 (en) | 2004-07-23 | 2008-06-19 | Hongfeng Deng | Compounds and Methods For Treatment of Thrombosis |
| AU2005266312C1 (en) | 2004-07-28 | 2011-06-16 | Janssen Pharmaceutica N.V. | Substituted indolyl alkyl amino derivatives as novel inhibitors of histone deacetylase |
| US20070015771A1 (en) | 2004-07-29 | 2007-01-18 | Threshold Pharmaceuticals, Inc. | Lonidamine analogs |
| JP2006045119A (ja) | 2004-08-04 | 2006-02-16 | Toray Ind Inc | ピラジン誘導体及びそれを有効成分とする腎炎治療薬 |
| US20060035893A1 (en) | 2004-08-07 | 2006-02-16 | Boehringer Ingelheim International Gmbh | Pharmaceutical compositions for treatment of respiratory and gastrointestinal disorders |
| NZ588431A (en) | 2004-09-17 | 2012-02-24 | Whitehead Biomedical Inst | Using Benzimidazole or Indole compounds with a 1,2-diazole group to Inhibit Alpha-Synuclein Toxicity |
| US20070299114A1 (en) | 2004-10-05 | 2007-12-27 | Shionogi & Co., Ltd. | Biaryl Derivatives |
| WO2006044509A2 (en) | 2004-10-15 | 2006-04-27 | Biogen Idec Ma Inc. | Methods of treating vascular injuries |
| JP2006131519A (ja) | 2004-11-04 | 2006-05-25 | Idemitsu Kosan Co Ltd | 縮合環含有化合物及びそれを用いた有機エレクトロルミネッセンス素子 |
| DE102004054666A1 (de) | 2004-11-12 | 2006-05-18 | Bayer Cropscience Gmbh | Substituierte Pyrazol-3-carboxamide, Verfahren zur Herstellung und Verwendung als Herbizide und Pflanzenwachstumsregulatoren |
| JPWO2006051937A1 (ja) | 2004-11-15 | 2008-05-29 | 塩野義製薬株式会社 | ヘテロ5員環誘導体 |
| CA2591817A1 (en) | 2004-12-22 | 2006-06-29 | Memory Pharmaceuticals Corporation | Nicotinic alpha-7 receptor ligands and preparation and uses thereof |
| WO2006071095A1 (en) | 2004-12-31 | 2006-07-06 | Sk Chemicals Co., Ltd. | Quinazoline derivatives for the treatment and prevention of diabetes and obesity |
| PA8660701A1 (es) | 2005-02-04 | 2006-09-22 | Pfizer Prod Inc | Agonistas de pyy y sus usos |
| FR2882054B1 (fr) | 2005-02-17 | 2007-04-13 | Sanofi Aventis Sa | Derives de 1,5-diarylpyrrole, leur preparation et leur application en therapeutique |
| JP5055263B2 (ja) | 2005-03-30 | 2012-10-24 | ダエウン ファーマシューティカル カンパニー リミテッド | 抗真菌性トリアゾール誘導体 |
| WO2006110516A1 (en) | 2005-04-11 | 2006-10-19 | Abbott Laboratories | Acylhydrazide p2x7 antagonists and uses thereof |
| KR20070121013A (ko) | 2005-04-22 | 2007-12-26 | 다이이찌 산쿄 가부시키가이샤 | 헤테로 고리 화합물 |
| EP2444079B1 (en) | 2005-05-17 | 2016-11-30 | SARcode Bioscience Inc. | Compositions and Methods for Treatment of Eye Disorders |
| WO2006130453A1 (en) | 2005-05-27 | 2006-12-07 | Brandeis University | Asymmetric aldol additions using bifunctional cinchona-alkaloid-based catalysts |
| WO2006130437A2 (en) | 2005-05-27 | 2006-12-07 | Brandeis University | Asymmetric carbon-carbon-bond-forming reactions catalyzed by bifunctional cinchona alkaloids |
| US7553964B2 (en) | 2005-06-03 | 2009-06-30 | Abbott Laboratories | Cyclobutyl amine derivatives |
| CA2610659A1 (en) | 2005-06-14 | 2006-12-21 | Merck Frosst Canada Ltd. | Reversible inhibitors of monoamine oxidase a and b |
| US20080221088A1 (en) | 2005-06-23 | 2008-09-11 | Vijay Kumar Potluri | 3,4-Substituted Thiazoles as Ampk Activators |
| EP1899333B1 (en) | 2005-06-27 | 2009-02-18 | Sanofi-Aventis | Pyrazolopyridine derivatives as inhibitors of beta-adrenergic receptor kinase 1 |
| EP1907369A4 (en) | 2005-07-04 | 2009-07-22 | Reddys Lab Ltd Dr | THIAZOLE DERIVATIVES USEFUL AS AMPK ACTIVATORS |
| JP2007015952A (ja) | 2005-07-06 | 2007-01-25 | Shionogi & Co Ltd | ナフタレン誘導体 |
| WO2007022501A2 (en) | 2005-08-18 | 2007-02-22 | Microbia, Inc. | Useful indole compounds |
| EP1754483A1 (en) | 2005-08-18 | 2007-02-21 | Merck Sante | Use of thienopyridone derivatives as AMPK activators and pharmaceutical compositions containing them |
| US8106066B2 (en) | 2005-09-23 | 2012-01-31 | Memory Pharmaceuticals Corporation | Indazoles, benzothiazoles, benzoisothiazoles, benzisoxazoles, pyrazolopyridines, isothiazolopyridines, and preparation and uses thereof |
| CA2627349A1 (en) | 2005-11-03 | 2007-05-18 | Ilypsa, Inc. | Azaindole compounds and use thereof as phospholipase-a2 inhibitors |
| US7666898B2 (en) | 2005-11-03 | 2010-02-23 | Ilypsa, Inc. | Multivalent indole compounds and use thereof as phospholipase-A2 inhibitors |
| AU2006311765A1 (en) | 2005-11-03 | 2007-05-18 | Ilypsa, Inc. | Phospholipase inhibitors, including multi-valent phospholipase inhibitors, and use thereof, including as lumen-localized phospholipase inhibitors |
| EP1963332A1 (en) | 2005-11-09 | 2008-09-03 | Memory Pharmaceuticals Corporation | 1 h-indazoles, benzothiazoles, 1,2-benzoisoxazoles, 1,2-benzoisothiazoles, and chromones and preparation and uses thereof |
| WO2007058504A1 (en) | 2005-11-21 | 2007-05-24 | Lg Life Sciences, Ltd. | Novel compounds as agonist for ppar gamma and ppar alpha, method for preparation of the same, and pharmaceutical composition containing the same |
| CN1978445B (zh) | 2005-12-02 | 2010-09-01 | 中国科学院上海药物研究所 | 一种可用作人源腺苷单核苷酸激活蛋白激酶激活剂的化合物及其制备方法和应用 |
| JP2009519966A (ja) | 2005-12-14 | 2009-05-21 | ブリストル−マイヤーズ スクイブ カンパニー | セリンプロテアーゼ阻害剤として有用な6員ヘテロ環 |
| AR058379A1 (es) | 2005-12-14 | 2008-01-30 | Bristol Myers Squibb Co | Derivados de arilpropionamida arilacrilamida arilpropinamida o arilmetilurea como inhibidores del factor xia. proceso de obtencion y composiciones farmaceuticas. |
| WO2007079173A2 (en) | 2005-12-30 | 2007-07-12 | Emergent Biosolutions Inc. | Novel 2-heteroaryloxy-phenol derivatives as antibacterial agents |
| CN101374834B (zh) | 2006-02-03 | 2011-12-14 | 伊莱利利公司 | 用于调节fxr的化合物和方法 |
| GB0603041D0 (en) | 2006-02-15 | 2006-03-29 | Angeletti P Ist Richerche Bio | Therapeutic compounds |
| MX2008012529A (es) | 2006-03-30 | 2008-10-14 | Asahi Kasei Pharma Corp | Derivado biciclico substituido y uso del mismo. |
| MX2008012482A (es) | 2006-03-31 | 2008-10-10 | Abbott Lab | Compuestos de indazol. |
| CN101426498A (zh) | 2006-04-18 | 2009-05-06 | 艾博特公司 | 香草素受体亚型1(vr1)的拮抗剂及其用途 |
| EP2463283B1 (en) | 2006-04-20 | 2014-06-11 | Pfizer Products Inc. | Fused phenyl Amido heterocyclic compounds for the prevention and treatment of glucokinase-mediated diseases |
| HRP20110917T1 (hr) | 2006-05-19 | 2012-03-31 | Abbott Laboratories | Derivati azabicikličkih alkana supstituirani fuzioniranim bicikloheterociklima aktivni u središnjem živčanom sustavu |
| DK2029547T3 (da) | 2006-05-24 | 2010-07-26 | Lilly Co Eli | FXR-agonister |
| EP2025676A4 (en) | 2006-06-08 | 2011-06-15 | Ube Industries | NEW INDAZONE DERIVATIVE WITH SPIRING STRUCTURE IN SIDE CHAIN |
| ES2398299T3 (es) | 2006-07-03 | 2013-03-15 | Proximagen Ltd. | Indoles como moduladores de 5-HT6 |
| FR2903695B1 (fr) | 2006-07-13 | 2008-10-24 | Merck Sante Soc Par Actions Si | Utilisation de derives d'imidazole activateurs de l'ampk, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| KR100826108B1 (ko) | 2006-08-04 | 2008-04-29 | 한국화학연구원 | 퓨란-2-카복실산 유도체 및 그의 제조 방법 |
| SG176477A1 (en) | 2006-08-07 | 2011-12-29 | Ironwood Pharmaceuticals Inc | Indole compounds |
| JP2008063278A (ja) | 2006-09-07 | 2008-03-21 | Fujifilm Finechemicals Co Ltd | 1−ピリジン−4−イル−インドール類の製造方法 |
| JP2008106037A (ja) | 2006-09-29 | 2008-05-08 | Osaka Prefecture Univ | インドール化合物の製造方法およびインドール化合物 |
| WO2008054748A2 (en) | 2006-10-31 | 2008-05-08 | Arena Pharmaceuticals, Inc. | Indazole derivatives as modulators of the 5-ht2a serotonin receptor useful for the treatment of disorders related thereto |
| CN101541809A (zh) | 2006-11-29 | 2009-09-23 | 辉瑞产品公司 | 螺环酮乙酰基-CoA羧化酶抑制剂 |
| US7825261B2 (en) | 2006-12-05 | 2010-11-02 | National Taiwan University | Indazole compounds |
| WO2008072850A1 (en) | 2006-12-11 | 2008-06-19 | Amorepacific Corporation | Triazine derivatives having inhibitory activity against acetyl-coa carboxylase |
| CN101558040B (zh) | 2006-12-14 | 2013-03-27 | 拜耳先灵医药股份有限公司 | 用作蛋白激酶抑制剂的二氢吡啶衍生物 |
| MX2009006617A (es) | 2006-12-18 | 2009-07-24 | Ambrx Inc | Composiciones que contienen, metodos que involucran y usos de aminoacidos y polipeptidos no naturales. |
| MX2009006535A (es) | 2006-12-22 | 2009-06-26 | Novartis Ag | Derivados de indol-4-il-pirimidinil-2-il-amina y su uso como inhibidores de cinasa dependiente de ciclina. |
| CA2674237C (en) | 2006-12-28 | 2015-11-24 | Rigel Pharmaceuticals, Inc. | N-substituted-heterocycloalkyloxybenzamide compounds and methods of use |
| PE20081559A1 (es) | 2007-01-12 | 2008-11-20 | Merck & Co Inc | DERIVADOS DE ESPIROCROMANONA SUSTITUIDOS COMO INHIBIDORES DE ACETIL CoA CARBOXILASA |
| US7999001B2 (en) | 2007-01-15 | 2011-08-16 | The United States Of America As Represented By The Secretary Of The Army | Antiviral compounds and methods of using thereof |
| DE102007002717A1 (de) | 2007-01-18 | 2008-07-24 | Merck Patent Gmbh | Heterocyclische Indazolderivate |
| JP2008179567A (ja) | 2007-01-25 | 2008-08-07 | Toray Ind Inc | ピラジン誘導体を有効成分とする抗がん剤 |
| AR065093A1 (es) | 2007-02-05 | 2009-05-13 | Merck Frosst Canada Ltd | Compuestos farmacéuticos inhibidores de la biosintesis de leucotrienos |
| MX2009008439A (es) | 2007-02-12 | 2009-08-13 | Intermune Inc | Nuevos inhibidores de la replicacion del virus de hepatitis c. |
| JP5107589B2 (ja) | 2007-02-13 | 2012-12-26 | 旭化成株式会社 | インドール誘導体 |
| JP2008208074A (ja) | 2007-02-27 | 2008-09-11 | Toray Ind Inc | ピラジン誘導体を有効成分とする抗がん剤 |
| JP2008222576A (ja) | 2007-03-09 | 2008-09-25 | Japan Enviro Chemicals Ltd | インドール化合物の製造方法 |
| WO2008110863A1 (en) | 2007-03-15 | 2008-09-18 | Glenmark Pharmaceuticals S.A. | Indazole derivatives and their use as vanilloid receptor ligands |
| US7947698B2 (en) | 2007-03-23 | 2011-05-24 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the JAK pathway |
| EP2142545A1 (en) | 2007-03-28 | 2010-01-13 | NeuroSearch A/S | Purinyl derivatives and their use as potassium channel modulators |
| KR20080099174A (ko) | 2007-05-07 | 2008-11-12 | 주식회사 머젠스 | 비만, 당뇨, 대사성 질환, 퇴행성 질환 및 미토콘드리아이상 질환의 치료 또는 예방을 위한 나프토퀴논계 약제조성물 |
| WO2008150899A1 (en) | 2007-05-29 | 2008-12-11 | Emory University | Combination therapies for treatment of cancer and inflammatory diseases |
| FR2917735B1 (fr) | 2007-06-21 | 2009-09-04 | Sanofi Aventis Sa | Nouveaux indazoles substitutes, leur preparation et leur utilisation en therapeutique |
| TW200906823A (en) | 2007-07-16 | 2009-02-16 | Lilly Co Eli | Compounds and methods for modulating FXR |
| US20090036425A1 (en) | 2007-08-02 | 2009-02-05 | Pfizer Inc | Substituted bicyclolactam compounds |
| WO2009019446A1 (en) | 2007-08-03 | 2009-02-12 | Betagenon Ab | Compounds useful as medicaments |
| KR20090016804A (ko) | 2007-08-13 | 2009-02-18 | 주식회사 티지 바이오텍 | 신규 벤질에스테르계 화합물 및 이를 유효성분으로함유하는 비만, 당뇨 및 고지혈증의 예방 및 치료용 조성물 |
| WO2009026107A1 (en) | 2007-08-17 | 2009-02-26 | Portola Pharmaceuticals, Inc. | Protein kinase inhibitors |
| AR068106A1 (es) | 2007-08-29 | 2009-11-04 | Schering Corp | Derivados de indol 2-carboxi sustituidos y una composicion farmaceutica |
| AR068107A1 (es) | 2007-08-29 | 2009-11-04 | Schering Corp | Derivados indolicos 2,3 sustituidos y una composicion farmaceutica |
| WO2009037247A1 (en) | 2007-09-17 | 2009-03-26 | Neurosearch A/S | Pyrazine derivatives and their use as potassium channel modulators |
| US8404713B2 (en) | 2007-10-26 | 2013-03-26 | Janssen Pharmaceutica Nv | Quinolinone derivatives as PARP inhibitors |
| US20090124680A1 (en) | 2007-10-31 | 2009-05-14 | Mazence Inc. | Use of prodrug composition containing naphthoquinone-based compound for manufacture of medicament for treatment or prevention of diseases involving metabolic syndrome |
| CN102317285A (zh) | 2007-11-16 | 2012-01-11 | 先灵公司 | 3-氨基磺酰基取代的吲哚衍生物及其使用方法 |
| ES2552733T3 (es) | 2007-11-16 | 2015-12-01 | Rigel Pharmaceuticals, Inc. | Compuestos de carboxamida, sulfonamida y amina para trastornos metabólicos |
| WO2009084695A1 (ja) | 2007-12-28 | 2009-07-09 | Carna Biosciences Inc. | 2-アミノキナゾリン誘導体 |
| US8469654B2 (en) | 2008-01-31 | 2013-06-25 | National University Corporation Yokohama National University | Fluid machine |
| MY158994A (en) | 2008-02-04 | 2016-11-30 | Mercury Therapeutics Inc | Ampk modulators |
| WO2009115874A2 (en) | 2008-03-17 | 2009-09-24 | Matrix Laboratories Ltd. | Novel heterocyclic compounds, pharmaceutical compositions containing them and processes for their preparation |
| MX2010009147A (es) | 2008-03-20 | 2010-09-07 | Hoffmann La Roche | Derivados de pirrolidinilo y usos de los mismos. |
| WO2009120783A1 (en) | 2008-03-25 | 2009-10-01 | The Johns Hopkins University | High affinity inhibitors of hepatitis c virus ns3/4a protease |
| AU2009228931B2 (en) | 2008-03-27 | 2013-05-23 | Janssen Pharmaceutica Nv | Aza-bicyclohexyl substituted indolyl alkyl amino derivatives as novel inhibitors of histone deacetylase |
| MX2010011047A (es) | 2008-04-11 | 2010-10-26 | Merck Patent Gmbh | Derivados de tienopiridonas como activadores de proteina cinasa activada por amp (ampk). |
| BRPI0911681B8 (pt) | 2008-04-23 | 2021-05-25 | Rigel Pharmaceuticals Inc | composto, composição farmacêutica, e, método para ativar a via de proteína quinase ativada por 5'-amp em uma célula in vitro |
| MY160357A (en) | 2008-05-05 | 2017-02-28 | Merck Patent Gmbh | Thienopyridone derivatives as amp-activated protein kinase (ampk) activators |
| GB0808282D0 (en) | 2008-05-07 | 2008-06-11 | Medical Res Council | Compounds for use in stabilizing p53 mutants |
| ES2545231T3 (es) | 2008-05-28 | 2015-09-09 | Pfizer Inc. | Inhibidores de pirazoloespirocetona acetil-CoA carboxilasa |
| EP2297164A1 (en) | 2008-05-28 | 2011-03-23 | Pfizer Inc. | Pyrazolospiroketone acetyl-coa carboxylase inhibitors |
| BRPI0915064B8 (pt) | 2008-06-16 | 2021-05-25 | Merck Patent Gmbh | derivados de quinoxalinadiona, seus usos, e medicamentos |
| AR072184A1 (es) | 2008-06-20 | 2010-08-11 | Glaxo Group Ltd | Derivados de oxadiazol como agonistas del receptor s1p1 |
| DE102008031480A1 (de) | 2008-07-03 | 2010-01-07 | Merck Patent Gmbh | Salze enthaltend ein Pyrimidincarbonsäure-Derivat |
| EP2300496A4 (en) | 2008-07-16 | 2012-04-25 | King Pharmaceuticals Res & Dev | ATHEROSCLEROSIS TREATMENT METHODS |
| WO2010010186A1 (en) | 2008-07-25 | 2010-01-28 | Galapagos Nv | Novel compounds useful for the treatment of degenerative and inflammatory diseases |
| JP2011529483A (ja) | 2008-07-29 | 2011-12-08 | ファイザー・インク | フッ素化ヘテロアリール |
| MX2011002166A (es) | 2008-08-28 | 2011-04-07 | Pfizer | Derivados de dioxa-biciclo[3.2.1]octano-2,3,1-triol. |
| WO2010036910A1 (en) | 2008-09-26 | 2010-04-01 | Yoshikazu Ohta | Heart protection by administering an amp-activated protein kinase activator |
| MX2011002846A (es) | 2008-09-26 | 2011-04-07 | Hoffmann La Roche | Derivados de pirina o pirazina para tratar el virus de la hepatitis c. |
| US8410284B2 (en) | 2008-10-22 | 2013-04-02 | Merck Sharp & Dohme Corp | Cyclic benzimidazole derivatives useful as anti-diabetic agents |
| US8563746B2 (en) | 2008-10-29 | 2013-10-22 | Merck Sharp & Dohme Corp | Cyclic benzimidazole derivatives useful as anti-diabetic agents |
| US8329914B2 (en) | 2008-10-31 | 2012-12-11 | Merck Sharp & Dohme Corp | Cyclic benzimidazole derivatives useful as anti-diabetic agents |
| WO2010056041A2 (ko) | 2008-11-13 | 2010-05-20 | 주식회사 머젠스 | 허혈 또는 허혈 재관류에 의해 유발되는 심장질환의 치료 및 예방을 위한 약제 조성물 |
| EP2386546B1 (en) | 2008-11-21 | 2015-08-19 | RaQualia Pharma Inc | Novel pyrazole-3-carboxamide derivate having 5-ht2b receptor antagonist activity |
| KR101061599B1 (ko) | 2008-12-05 | 2011-09-02 | 한국과학기술연구원 | 비정상 세포 성장 질환의 치료를 위한 단백질 키나아제 저해제인 신규 인다졸 유도체, 이의 약학적으로 허용가능한염 및 이를 유효성분으로 함유하는 약학적 조성물 |
| WO2010068287A2 (en) | 2008-12-11 | 2010-06-17 | Angion Biomedica Corp. | Small molecule modulators of hepatocyte growth factor (scatter factor) activity |
| US8741923B2 (en) | 2008-12-18 | 2014-06-03 | Merck Serono Sa | Oxadiazole fused heterocyclic derivatives useful for the treatment of multiple sclerosis |
| WO2010073011A2 (en) | 2008-12-23 | 2010-07-01 | Betagenon Ab | Compounds useful as medicaments |
| EP3000468A1 (en) | 2008-12-23 | 2016-03-30 | President and Fellows of Harvard College | Small molecule inhibitors of necroptosis |
| JP5658688B2 (ja) | 2009-01-28 | 2015-01-28 | ライジェル ファーマシューティカルズ, インコーポレイテッド | カルボキサミド化合物およびその使用方法 |
| WO2010086613A1 (en) | 2009-01-30 | 2010-08-05 | Betagenon Ab | Compounds useful as inhibitors as ampk |
| TW201038580A (en) | 2009-02-02 | 2010-11-01 | Pfizer | 4-amino-5-oxo-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-6(5H)-yl)phenyl derivatives |
| US20100210682A1 (en) | 2009-02-19 | 2010-08-19 | Abbott Laboratories | Repeated Dosing of TRPV1 Antagonists |
| JP5086480B2 (ja) | 2009-03-11 | 2012-11-28 | ファイザー・インク | グルコキナーゼ活性化剤として使用されるベンゾフラニル誘導体 |
| CA2754685A1 (en) | 2009-03-11 | 2010-09-16 | Pfizer Inc. | Substituted indazole amides |
| US20120095028A1 (en) | 2009-03-20 | 2012-04-19 | Pfizer Inc. | 3-oxa-7-azabicyclo[3.3.1]nonanes |
| JP5462932B2 (ja) | 2009-03-24 | 2014-04-02 | 住友化学株式会社 | ボロン酸エステル化合物の製造方法 |
| JP5730190B2 (ja) | 2009-03-31 | 2015-06-03 | 株式会社レナサイエンス | プラスミノーゲンアクチベーターインヒビター−1阻害剤 |
| US8927576B2 (en) | 2009-04-06 | 2015-01-06 | PTC Therpeutics, Inc. | HCV inhibitor and therapeutic agent combinations |
| CA2759843A1 (en) | 2009-05-08 | 2010-11-10 | Pfizer Inc. | Gpr 119 modulators |
| WO2010128414A1 (en) | 2009-05-08 | 2010-11-11 | Pfizer Inc. | Gpr 119 modulators |
| NZ596467A (en) | 2009-06-05 | 2014-01-31 | Pfizer | L- ( piperidin-4-yl) -pyrazole derivatives as gpr 119 modulators |
| WO2011004162A2 (en) | 2009-07-08 | 2011-01-13 | Betagenon Ab | Compounds useful as medicaments |
| WO2011005611A1 (en) | 2009-07-09 | 2011-01-13 | Merck Sharp & Dohme Corp. | Neuromedin u receptor agonists and uses thereof |
| WO2011014128A1 (en) | 2009-07-30 | 2011-02-03 | National University Of Singapore | Small molecule inhibitors of isoprenylcysteine carboxyl methyltransferase with potential anticancer activity |
| GB0915892D0 (en) | 2009-09-10 | 2009-10-14 | Smithkline Beecham Corp | Compounds |
| WO2011032320A1 (en) | 2009-09-21 | 2011-03-24 | F. Hoffmann-La Roche Ag | Novel alkene oxindole derivatives |
| WO2011069298A1 (en) | 2009-12-11 | 2011-06-16 | F. Hoffmann-La Roche Ag | Novel cyclopropane indolinone derivatives |
| JP2013047189A (ja) | 2009-12-25 | 2013-03-07 | Kyorin Pharmaceutical Co Ltd | 新規パラバン酸誘導体及びそれらを有効成分とする医薬 |
| EA020588B1 (ru) | 2009-12-29 | 2014-12-30 | Поксел | ТИЕНО[2,3-b]ПИРИДИНДИОНОВЫЕ АКТИВАТОРЫ АМФК И ИХ ТЕРАПЕВТИЧЕСКОЕ ПРИМЕНЕНИЕ |
| JP2013520502A (ja) | 2010-02-25 | 2013-06-06 | メルク・シャープ・エンド・ドーム・コーポレイション | 有用な抗糖尿病薬である新規な環状ベンズイミダゾール誘導体 |
| WO2011123681A1 (en) | 2010-03-31 | 2011-10-06 | Rigel Pharmaceuticals, Inc. | Methods for using carboxamide, sulfonamide and amine compounds |
| US8344137B2 (en) | 2010-04-14 | 2013-01-01 | Hoffman-La Roche Inc. | 3,3-dimethyl tetrahydroquinoline derivatives |
| WO2011138307A1 (en) | 2010-05-05 | 2011-11-10 | Glaxosmithkline Llc | Pyrrolo [3, 2 -d] pyrimidin-3 -yl derivatives used as activators of ampk |
| US8592594B2 (en) | 2010-07-02 | 2013-11-26 | Hoffmann-La Roche Inc. | Tetrahydro-quinoline derivatives |
| AU2011283684B2 (en) | 2010-07-29 | 2015-08-27 | Rigel Pharmaceuticals, Inc. | AMPK-activating heterocyclic compounds and methods for using the same |
| KR101190141B1 (ko) | 2010-08-24 | 2012-10-12 | 서울대학교산학협력단 | Ampk를 활성화시키는 화합물을 함유하는 약학조성물 |
| WO2012027548A1 (en) | 2010-08-25 | 2012-03-01 | The Feinstein Institute For Medical Research | Compounds and methods for prevention and treatment of alzheimer's and other diseases |
| JP2013230986A (ja) | 2010-08-25 | 2013-11-14 | Kyorin Pharmaceutical Co Ltd | 新規ヒダントイン誘導体及びそれらを有効成分とする医薬 |
| WO2012033149A1 (ja) | 2010-09-10 | 2012-03-15 | 塩野義製薬株式会社 | Ampk活性化作用を有するヘテロ環縮合イミダゾール誘導体 |
| WO2012040499A2 (en) | 2010-09-22 | 2012-03-29 | Surface Logix, Inc. | Metabolic inhibitors |
| US8546427B2 (en) | 2010-10-20 | 2013-10-01 | Hoffmann-La Roche Inc. | Tetrahydroquinoline derivatives |
| US8809369B2 (en) | 2011-01-26 | 2014-08-19 | Hoffmann-La Roche Inc. | Tetrahydroquinoline derivatives |
| PH12013501686A1 (en) | 2011-02-25 | 2017-10-25 | Merck Sharp & Dohme | Novel cyclic azabenzimidazole derivatives useful as anti-diabetic agents |
| US20130345243A1 (en) | 2011-03-07 | 2013-12-26 | Glaxosmithkline Llc | 1h-pyrollo[3,2-d]pyrimidinedione derivatives |
| KR101624020B1 (ko) | 2011-03-07 | 2016-05-24 | 글락소스미스클라인 엘엘씨 | 퀴놀리논 유도체 |
| HK1199255A1 (en) | 2011-08-12 | 2015-06-26 | F. Hoffmann-La Roche Ag | Indazole compounds, compositions and methods of use |
| ES2564961T3 (es) | 2012-02-21 | 2016-03-30 | Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.P.A. | Compuestos de 1H-indazol-3-carboxamida como inhibidores de la glucógeno sintasa cinasa 3 beta |
-
2013
- 2013-03-15 US US13/831,588 patent/US8889730B2/en active Active
- 2013-04-01 HR HRP20171028TT patent/HRP20171028T1/hr unknown
- 2013-04-01 PL PL13720084T patent/PL2836490T3/pl unknown
- 2013-04-01 MD MDA20140109A patent/MD20140109A2/ro not_active Application Discontinuation
- 2013-04-01 CN CN201380019226.XA patent/CN104245688A/zh active Pending
- 2013-04-01 IN IN9200DEN2014 patent/IN2014DN09200A/en unknown
- 2013-04-01 SG SG11201405571SA patent/SG11201405571SA/en unknown
- 2013-04-01 JP JP2015505038A patent/JP6026642B2/ja not_active Expired - Fee Related
- 2013-04-01 KR KR20147031394A patent/KR20150002782A/ko not_active Ceased
- 2013-04-01 RS RS20170792A patent/RS56290B1/sr unknown
- 2013-04-01 DK DK13720084.6T patent/DK2836490T3/en active
- 2013-04-01 CA CA2869692A patent/CA2869692C/en not_active Expired - Fee Related
- 2013-04-01 HU HUE13720084A patent/HUE033096T2/en unknown
- 2013-04-01 AU AU2013246552A patent/AU2013246552A1/en not_active Abandoned
- 2013-04-01 EA EA201491592A patent/EA028564B1/ru not_active IP Right Cessation
- 2013-04-01 NZ NZ630700A patent/NZ630700A/en not_active IP Right Cessation
- 2013-04-01 PE PE2014001610A patent/PE20142294A1/es not_active Application Discontinuation
- 2013-04-01 AP AP2014007983A patent/AP2014007983A0/xx unknown
- 2013-04-01 SI SI201330694T patent/SI2836490T1/sl unknown
- 2013-04-01 LT LTEP13720084.6T patent/LT2836490T/lt unknown
- 2013-04-01 MX MX2014012330A patent/MX2014012330A/es active IP Right Grant
- 2013-04-01 HK HK15103224.5A patent/HK1202547A1/xx unknown
- 2013-04-01 WO PCT/IB2013/052604 patent/WO2013153479A2/en not_active Ceased
- 2013-04-01 EP EP13720084.6A patent/EP2836490B1/en active Active
- 2013-04-01 ME MEP-2017-137A patent/ME02729B/me unknown
- 2013-04-01 PT PT137200846T patent/PT2836490T/pt unknown
- 2013-04-01 ES ES13720084.6T patent/ES2637238T3/es active Active
- 2013-04-08 TW TW102112379A patent/TWI465431B/zh not_active IP Right Cessation
- 2013-04-09 AR ARP130101147A patent/AR090633A1/es unknown
- 2013-04-10 UY UY0001034736A patent/UY34736A/es not_active Application Discontinuation
- 2013-09-24 WO PCT/IB2013/058819 patent/WO2014140704A1/en not_active Ceased
-
2014
- 2014-09-05 CR CR20140411A patent/CR20140411A/es unknown
- 2014-09-16 ZA ZA2014/06792A patent/ZA201406792B/en unknown
- 2014-09-26 EC ECIEPI201420545A patent/ECSP14020545A/es unknown
- 2014-09-28 IL IL234860A patent/IL234860A0/en unknown
- 2014-09-30 CU CU2014000118A patent/CU20140118A7/es unknown
- 2014-10-02 TN TN2014000420A patent/TN2014000420A1/fr unknown
- 2014-10-09 NI NI201400121A patent/NI201400121A/es unknown
- 2014-10-09 DO DO2014000228A patent/DOP2014000228A/es unknown
- 2014-10-09 PH PH12014502280A patent/PH12014502280A1/en unknown
- 2014-10-10 CO CO14225646A patent/CO7091185A2/es active IP Right Grant
- 2014-10-10 GT GT201400215A patent/GT201400215A/es unknown
- 2014-10-20 US US14/518,165 patent/US20150038484A1/en not_active Abandoned
- 2014-12-01 EC ECIEPI201426271A patent/ECSP14026271A/es unknown
-
2017
- 2017-08-07 CY CY20171100844T patent/CY1119194T1/el unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ME02729B (me) | Indolski i indazolski spojevi koji aktiviraju ampk | |
| JP2015512931A5 (me) | ||
| ME02892B (me) | Hemijska jedinjenja | |
| JP2013505969A5 (me) | ||
| ME02766B (me) | Derivati arilmetoksi izoindolina i kompozicije koje ih obuhvataju i postupci njihove primene | |
| HRP20150941T1 (hr) | Derivati aminodihidrotiazina kao inhibitori bace u lijeäśenju alzheimerove bolesti | |
| AR057109A1 (es) | Benzimidazoles sustituidos y metodos para usarlos como inhibidores de las quinasas asociadas con la tumorigenesis | |
| ME01421B (me) | 5-supstituisani derivati kinazolinona kao protivtumorska sredstva | |
| JP2016505614A5 (me) | ||
| JP2013537203A5 (me) | ||
| JP2013544860A5 (me) | ||
| JP2011519854A5 (me) | ||
| AR089134A1 (es) | Arilos y heteroarilos biciclicos inhibidores de los canales de sodio | |
| JP2014508811A5 (me) | ||
| JP2013540755A5 (me) | ||
| AR092045A1 (es) | Combinaciones farmaceuticas | |
| JP2014507464A5 (me) | ||
| UA112317C2 (uk) | Похідні 2-(1,2,3-триазол-2-іл)бензаміду та 3-(1,2,3-триазол-2-іл)піколінаміду як антагоністи рецептора орексину | |
| MX344276B (es) | Compuesto de piperidina novedoso o sal del mismo. | |
| SI2895174T1 (en) | The prodrugs of the amino quinazoline kinase inhibitor | |
| RU2018131440A (ru) | Антагонисты FimH, являющиеся производными маннозы, пригодные для лечения заболевания | |
| EA201390476A1 (ru) | Новые пиперазиновые аналоги с замещенными гетероарильными группами в качестве противовирусных средств широкого применения против гриппа | |
| JP2016503403A5 (me) | ||
| MX2013008161A (es) | Formas solidas del inhibidor de girasa (r)-1-etil-3-[6-fluoro-5-[2 -(1-hidroxi-1-metil-etil) pirimidin-5-il]-7-(tetrahidrofuran-2-il) -1h-benzimidazol-2-il]urea. | |
| ME02167B (me) | Piridinil- i pirazinil-metiloksi-aril derivati korisni kao inhibitori tirozin kinaze slezine (syk) |