ME02729B - Indolski i indazolski spojevi koji aktiviraju ampk - Google Patents

Indolski i indazolski spojevi koji aktiviraju ampk

Info

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
Application number
MEP-2017-137A
Other languages
German (de)
English (en)
French (fr)
Inventor
Kevin James Filipski
Daniel Wei-Shung Kung
Esther Cheng Yin Lee
Aaron Christopher Smith
Meihua Mike Tu
Original Assignee
Pfizer
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Pfizer filed Critical Pfizer
Publication of ME02729B publication Critical patent/ME02729B/me

Links

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)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Cosmetics (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (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.
MEP-2017-137A 2012-04-10 2013-04-01 Indolski i indazolski spojevi koji aktiviraju ampk ME02729B (me)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261622129P 2012-04-10 2012-04-10
EP13720084.6A EP2836490B1 (en) 2012-04-10 2013-04-01 Indole and indazole compounds that activate ampk
PCT/IB2013/052604 WO2013153479A2 (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)

Country Link
US (2) US8889730B2 (me)
EP (1) EP2836490B1 (me)
JP (1) JP6026642B2 (me)
KR (1) KR20150002782A (me)
CN (1) CN104245688A (me)
AP (1) AP2014007983A0 (me)
AR (1) AR090633A1 (me)
AU (1) AU2013246552A1 (me)
CA (1) CA2869692C (me)
CO (1) CO7091185A2 (me)
CR (1) CR20140411A (me)
CU (1) CU20140118A7 (me)
CY (1) CY1119194T1 (me)
DK (1) DK2836490T3 (me)
DO (1) DOP2014000228A (me)
EA (1) EA028564B1 (me)
EC (2) ECSP14020545A (me)
ES (1) ES2637238T3 (me)
GT (1) GT201400215A (me)
HK (1) HK1202547A1 (me)
HR (1) HRP20171028T1 (me)
HU (1) HUE033096T2 (me)
IL (1) IL234860A0 (me)
IN (1) IN2014DN09200A (me)
LT (1) LT2836490T (me)
MD (1) MD20140109A2 (me)
ME (1) ME02729B (me)
MX (1) MX2014012330A (me)
NI (1) NI201400121A (me)
NZ (1) NZ630700A (me)
PE (1) PE20142294A1 (me)
PH (1) PH12014502280A1 (me)
PL (1) PL2836490T3 (me)
PT (1) PT2836490T (me)
RS (1) RS56290B1 (me)
SG (1) SG11201405571SA (me)
SI (1) SI2836490T1 (me)
TN (1) TN2014000420A1 (me)
TW (1) TWI465431B (me)
UY (1) UY34736A (me)
WO (2) WO2013153479A2 (me)
ZA (1) ZA201406792B (me)

Families Citing this family (45)

* Cited by examiner, † Cited by third party
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
EP2951170B1 (en) 2013-02-04 2018-10-24 Janssen Pharmaceutica NV Flap modulators
EP2963013A4 (en) 2013-02-27 2016-09-14 Shionogi & Co INDOLE AND AZAINDOLE DERIVATIVES HAVING AMPK ACTIVATION ACTIVITY EACH
JP6064062B2 (ja) * 2013-03-15 2017-01-18 ファイザー・インク Ａｍｐｋを活性化させるインダゾール化合物
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
US9980948B2 (en) 2014-08-27 2018-05-29 Shionogi & Co., Ltd. Azaindole derivative having AMPK-activating activity
MA41051B1 (fr) 2014-10-06 2020-11-30 Vertex Pharma Modulateurs du régulateur de conductance transmembranaire de la mucoviscidose
WO2016092413A1 (en) * 2014-12-10 2016-06-16 Pfizer Inc. Indole and indazole compounds that activate ampk
HK1244792B (en) 2014-12-24 2019-07-12 北京生命科学研究所 Necrosis inhibitors
ES2849951T3 (es) 2015-06-18 2021-08-24 89Bio Ltd Derivados de piperidina 4-bencil y 4-benzoil sustituidos
EA201890086A1 (ru) * 2015-06-18 2018-06-29 Сефалон, Инк. 1,4-замещенные производные пиперидина
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
CA3019380A1 (en) 2016-03-31 2017-10-05 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
DK3442980T3 (da) 2016-04-15 2021-08-30 Cancer Research Tech Ltd Heterocykliske forbindelser som ret-kinase-hæmmere
LT3442535T (lt) 2016-04-15 2022-10-25 Cancer Research Technology Limited Heterocikliniai junginiai kaip ret kinazės inhibitoriai
EA202092441A1 (ru) 2016-06-07 2021-05-21 Джакобио Фармасьютикалс Ко., Лтд. Новые гетероциклические производные, применимые в качестве ингибиторов shp2
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
CN109803962B (zh) 2016-09-30 2022-04-29 弗特克斯药品有限公司 囊性纤维化跨膜传导调控蛋白的调节剂、以及药物组合物
MD3551622T2 (ro) 2016-12-09 2021-03-31 Vertex Pharma Modulator al regulatorului conductanței transmembranare în fibroză chistică, compoziții farmaceutice, metode de tratament și procedeu pentru fabricarea modulatorului
KR20240026521A (ko) 2017-03-23 2024-02-28 자코바이오 파마슈티칼스 컴퍼니 리미티드 Shp2 억제제로서 유용한 신규한 헤테로환형 유도체
GB201705971D0 (en) 2017-04-13 2017-05-31 Cancer Res Tech Ltd Inhibitor compounds
US11253509B2 (en) 2017-06-08 2022-02-22 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
MA49631A (fr) 2017-07-17 2020-05-27 Vertex Pharma Méthodes de traitement de la fibrose kystique
JP7121794B2 (ja) 2017-08-02 2022-08-18 バーテックス ファーマシューティカルズ インコーポレイテッド ピロリジン化合物を調製するためのプロセス
WO2019079760A1 (en) 2017-10-19 2019-04-25 Vertex Pharmaceuticals Incorporated CRYSTALLINE FORMS AND COMPOSITIONS OF CFTR MODULATORS
EP3720849A2 (en) 2017-12-08 2020-10-14 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
WO2019168874A1 (en) * 2018-02-27 2019-09-06 The Research Foundation For The State University Of New York 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
EP3774825A1 (en) 2018-04-13 2021-02-17 Vertex Pharmaceuticals Incorporated 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.
CN112839935A (zh) 2018-09-26 2021-05-25 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
CA3124838A1 (en) * 2018-12-31 2020-07-09 The Board Of Trustees Of The Leland Stanford Junior University Methods and formulations to treat 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
WO2021236617A1 (en) 2020-05-19 2021-11-25 Kallyope, Inc. Ampk activators
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
CA3183575A1 (en) 2020-06-26 2021-12-30 Iyassu Sebhat Ampk activators
EP4221700A1 (en) 2020-09-30 2023-08-09 Bioverativ Therapeutics Inc. Ampk activators and methods of use thereof
AU2024249981A1 (en) * 2023-04-06 2025-10-16 Pfizer Inc. Substituted indazole propionic acid derivative compounds and uses thereof as ampk activators
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
CN121752550A (zh) 2023-08-31 2026-03-27 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)

* Cited by examiner, † Cited by third party
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
US5215994A (en) 1990-09-25 1993-06-01 Fujisawa Pharmaceutical Co., Ltd. Angiotenin II antagonizing heterocyclic derivatives
US5210092A (en) 1990-09-25 1993-05-11 Fujisawa Pharmaceutical Co., Ltd. Angiotensin 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
EP0548553A1 (en) 1991-11-25 1993-06-30 Takeda Chemical Industries, Ltd. Optically active azole compounds, their production and use
EP0545478A1 (en) 1991-12-03 1993-06-09 MERCK SHARP & DOHME LTD. Heterocyclic compounds as tachykinin antagonists
CA2109931A1 (en) 1992-03-27 1993-10-14 Hiroshi Matsui 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
US5616537A (en) 1992-07-03 1997-04-01 Kumiai Chemical Industry Co., Ltd. Condensed heterocyclic derivatives and herbicides
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
JP2829788B2 (ja) 1994-02-10 1998-12-02 ファイザー インク． ベンゾジアゼピン受容体部位アゴニスト及びアンタゴニストとしての５−ヘテロアリールインドール誘導体
MX9700696A (es) 1994-07-27 1997-04-30 Sankyo Co Compuestos heterociclicos, utiles como productores de efecto aloesterico en receptores muscarinicos.
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
ES2175079T3 (es) 1995-04-10 2002-11-16 Fujisawa Pharmaceutical Co Derivados de indol utiles como inhibidores de cgmp-pde.
AU6944696A (en) 1995-09-14 1997-04-01 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
WO1998028292A1 (en) 1996-12-23 1998-07-02 Smithkline Beecham Corporation Novel piperidine containing compounds
EP0973767A1 (en) 1997-03-31 2000-01-26 Dupont Pharmaceuticals Company Indazoles of cyclic ureas useful as hiv protease inhibitors
ATE364374T1 (de) 1997-08-11 2007-07-15 Pfizer Prod Inc Feste pharmazeutische dispersionen mit erhöhter bioverfügbarkeit
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
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
EE200000488A (et) * 1998-02-25 2002-02-15 Genetics Institute, Inc. Fosfolipaasensüümide inhibiitorid ja farmatseutilised kompositsioonid
JP2002515488A (ja) 1998-05-15 2002-05-28 ギルフォード 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、組成物、及びｐａｒｐ活性の抑制方法
AU4981199A (en) 1998-07-08 2000-02-01 Gregory N. Beatch Compositions and methods for modulating sexual activity
AU758789B2 (en) 1998-07-15 2003-03-27 Teijin Limited Thiobenzimidazole derivatives
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
AU2001275537A1 (en) 2000-06-20 2002-01-02 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
US20040063733A1 (en) 2000-10-25 2004-04-01 Lambert Christine Marie Paul Quinazoline derivatives
HUP0302718A3 (en) 2000-11-01 2011-03-28 Merck Patent Gmbh Methods and compositions for the treatment of diseases of the eye
WO2002040481A2 (en) 2000-11-20 2002-05-23 Millennium Pharmaceuticals, 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
EP1359139A1 (en) 2001-01-18 2003-11-05 Shionogi & Co., Ltd. Terphenyl compounds bearing substituted amino groups
WO2002057237A1 (en) 2001-01-22 2002-07-25 Shionogi & Co., Ltd. Hetero-tricyclic compounds having substituted amino groups
RU2003126913A (ru) 2001-02-02 2005-03-10 Шеринг Корпорейшн (US) 3,4-дизамещенные циклобутен-1,2-дионы, как антагонисты хемокинового рецептора схс
IL157253A0 (en) 2001-02-28 2004-02-19 Merck & Co Inc Acylated piperidine derivatives as melanocortin-4 receptor agonists
US6951848B2 (en) 2001-03-12 2005-10-04 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
PL208928B1 (pl) 2001-04-16 2011-06-30 Pharmacopeia 3, 4-di-podstawione cyklobuten-1, 2-diony jako ligandy receptora CXC chemokiny
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)
EP1411942A4 (en) 2001-07-05 2005-01-26 Synaptic Pharma Corp SUBSTITUTED ANILINPIPERIDINES AS MCH-SELECTIVE ANTAGONISTS
PL207175B1 (pl) 2001-08-01 2010-11-30 Merck Patent Gmbh Zastosowanie inhibitorów integryny do wytwarzania kompozycji farmaceutycznych do zapobiegania i/lub terapii chorób oczu
WO2003020719A1 (en) 2001-09-03 2003-03-13 Takeda Chemical Industries, Ltd. 1,3-benzothiazinone derivatives and use thereof
JP2005505595A (ja) 2001-10-12 2005-02-24 シェーリング　コーポレイション Ｃｘｃ−ケモカインレセプターアンタゴニストとしての３，４−二置換マレイミド化合物
CA2464333C (en) 2001-10-26 2011-07-26 University Of Connecticut Heteroindanes: a new class of potent cannabimimetic ligands
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
JP5039268B2 (ja) 2001-10-26 2012-10-03 アベンティス・ファーマスーティカルズ・インコーポレイテツド ベンゾイミダゾールおよび類縁体および蛋白キナーゼ阻害剤としてのその使用
US20030187026A1 (en) 2001-12-13 2003-10-02 Qun Li Kinase inhibitors
TWI317634B (en) 2001-12-13 2009-12-01 Nat Health Research Institutes Aroyl indoles 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
JP4390563B2 (ja) 2002-02-21 2009-12-24 旭化成ファーマ株式会社 置換フェニルアルカン酸誘導体及びその用途
NZ534582A (en) 2002-02-27 2006-03-31 Pfizer Prod Inc ACC inhibitors
WO2003082271A2 (en) 2002-04-03 2003-10-09 Astrazeneca Ab Indole derivatives having anti-angiogenetic activity
US7019017B2 (en) 2002-05-14 2006-03-28 Baylor College Of Medicine Small molecule inhibitors of HER2 expression
AU2003239508A1 (en) 2002-05-21 2003-12-12 Bristol-Myers Squibb Company Indole compounds useful as impdh inhibitors
AU2003281205A1 (en) 2002-07-09 2004-01-23 Fujisawa Pharmaceutical Co., Ltd. Remedy for urinary frequency and urinary incontinence
US6972336B2 (en) 2002-07-18 2005-12-06 Novartis Ag N-alkylation of indole derivatives
US20060135516A1 (en) 2002-08-10 2006-06-22 Astex Technology, Ltd. 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
BRPI0315959C1 (pt) 2002-11-28 2021-05-25 Suven Life Sciences Ltd composto, composição farmacêutica, uso do composto, método para o tratamento, método para reduzir a morbidez e a mortalidade associadas com o excesso de peso e processo para a preparação do composto
JP2006516254A (ja) 2003-01-06 2006-06-29 イーライ・リリー・アンド・カンパニー Ｐｐａｒモジュレータとしての縮合ヘテロ環誘導体
AU2003303681A1 (en) 2003-01-06 2004-08-10 Eli Lilly And Company Fused heterocyclic derivates 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
ATE409176T1 (de) 2003-02-21 2008-10-15 Chiesi Farma Spa 1-phenylalkancarbonsäurederivate zur behandlung neurodegenerativer erkrankungen
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
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
WO2004089471A2 (en) 2003-04-11 2004-10-21 Novo Nordisk A/S NEW PYRAZOLO[1,5-a] PYRIMIDINES DERIVATIVES AND PHARMACEUTICAL USE THEREOF
DE602004025220D1 (de) 2003-04-11 2010-03-11 High Point Pharmaceuticals Llc Pharmazeutische verwendungen von kondensierten 1,2,4-triazolen
WO2004089367A1 (en) 2003-04-11 2004-10-21 Novo Nordisk A/S Pharmaceutical use of substituted 1,2,4-triazoles
EP1615667A2 (en) 2003-04-11 2006-01-18 Novo Nordisk A/S Combinations of an 11-beta-hydroxysteroid dehydrogenase type 1 inhibitor and a glucocorticoid receptor agonist
ATE467616T1 (de) 2003-04-11 2010-05-15 High Point Pharmaceuticals Llc Verbindungen mit aktivität an der 11beta- hydroxasteroiddehydrogenase
MXPA05011539A (es) 2003-04-30 2006-01-23 Inst For Pharm Discovery Inc Acidos carboxilicos sustituidos con heterociclo como inhibidores de la proteina tirosina-fosfatasa-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
WO2005005411A1 (en) 2003-07-04 2005-01-20 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
US7470807B2 (en) 2003-08-14 2008-12-30 Asahi Kasei Pharma Corporation Substituted arylalkanoic acid derivatives and use thereof
EP2468729B1 (en) 2003-10-15 2013-12-25 Ube Industries, Ltd. Novel indazole derivative
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
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
DE602004010299T2 (de) 2003-12-22 2008-09-18 Memory Pharmaceuticals Corp. Indole, 1h-indazole, 1,2-benzisoxazole und 1,2-benzisothiazole und deren herstellung und anwendungen
NZ550534A (en) 2004-03-25 2009-07-31 Memory Pharm Corp Indazoles, benzothiazoles, benzoisothiazoles, benzisoxazoles, and preparation and uses thereof
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
JP2007538011A (ja) 2004-05-07 2007-12-27 メモリー・ファーマシューティカルズ・コーポレイション １ｈ−インダゾール、ベンゾチアゾール、１，２−ベンゾイソキサゾール、１，２−ベンゾイソチアゾール、およびクロモン、ならびにそれらの調製および使用
KR100869616B1 (ko) 2004-05-12 2008-11-21 화이자 프로덕츠 인코포레이티드 프롤린 유도체 및 그의 다이펩티딜 펩티다제－ｉｖ저해제로서의 용도
UA84208C2 (en) 2004-05-25 2008-09-25 Пфайзер Продактс Инк. Tetraazabenzo(e)azulene derivatives and analogs thereof
JP2008501689A (ja) 2004-06-03 2008-01-24 ブランデイス ユニヴァーシティー シンコナアルカロイドを基本構造とする二官能触媒を用いた不斉マイケル付加およびアルドール付加反応
DE602005014233D1 (de) 2004-06-18 2009-06-10 Biolipox Ab Zur behandlung von entzündungen geeignete indole
MXPA06014535A (es) 2004-06-18 2007-06-05 Biolipox Ab Indoles utiles en el tratamiento de la inflamacion.
EP1773771A2 (en) 2004-07-23 2007-04-18 Daiamed, Inc. Compounds and methods for treatment of thrombosis
US8193205B2 (en) 2004-07-28 2012-06-05 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
EP1802303B1 (en) 2004-09-17 2011-11-02 Whitehead Institute For Biomedical Research Compounds, compositions and methods of inhibiting a-synuclein toxicity
TW200616613A (en) 2004-10-05 2006-06-01 Shionogi & Co Biaryl derivatives
EP1804801A2 (en) 2004-10-15 2007-07-11 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
RU2418797C2 (ru) 2004-12-22 2011-05-20 Мемори Фармасьютиклз Корпорейшн Лиганды никотинового рецептора альфа-7, их получение и применение
JP2008526734A (ja) 2004-12-31 2008-07-24 エスケー ケミカルズ カンパニー リミテッド 糖尿及び肥満治療予防に有効なキナゾリン誘導体
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
EP1871766A4 (en) 2005-03-30 2010-07-21 Dae Woong Pharma TRIAZONE DERIVATIVES WITH ANTIPILY EFFECT
WO2006110516A1 (en) 2005-04-11 2006-10-19 Abbott Laboratories Acylhydrazide p2x7 antagonists and uses thereof
CN101203512A (zh) 2005-04-22 2008-06-18 第一三共株式会社 杂环化合物
DK2444079T3 (en) 2005-05-17 2017-01-30 Sarcode Bioscience Inc Compositions and Methods for the Treatment of Eye Diseases
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
EP1893562A4 (en) 2005-06-14 2010-04-28 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
RS50821B (sr) 2005-06-27 2010-08-31 Sanofi-Aventis Derivati pirazolopiridina kao inhibitori beta-adrenergičnog receptora kinaze 1
JP2009500351A (ja) 2005-07-04 2009-01-08 ドクター レディズ ラボラトリーズ リミテッド Ａｍｐｋアクチベータとしてのチアゾール誘導体
JP2007015952A (ja) 2005-07-06 2007-01-25 Shionogi & Co Ltd ナフタレン誘導体
EP1931632A4 (en) 2005-08-18 2011-05-11 Microbia Inc USEFUL INDOOR CONNECTIONS
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
AU2006311851A1 (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
MX2008005661A (es) 2005-11-03 2008-12-15 Ilypsa Inc Inhibidores de fosfolipasa, que incluyen inhibidores de fosfolipasa multivalente, y uso de los mismos, que incluyen como inhibidores de fosfolipasa localizadas en el lumen.
WO2007056582A1 (en) 2005-11-09 2007-05-18 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
AU2006325746A1 (en) 2005-12-14 2007-06-21 Bristol-Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
EP1981854B1 (en) 2005-12-14 2011-06-01 Bristol-Myers Squibb Company Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor xia inhibitors
WO2007079173A2 (en) 2005-12-30 2007-07-12 Emergent Biosolutions Inc. Novel 2-heteroaryloxy-phenol derivatives as antibacterial agents
CA2640476A1 (en) 2006-02-03 2007-08-16 Eli Lilly And Company Compounds and methods for modulating fx-receptors
GB0603041D0 (en) 2006-02-15 2006-03-29 Angeletti P Ist Richerche Bio Therapeutic compounds
EP2006271A4 (en) 2006-03-30 2011-08-10 Asahi Kasei Pharma Corp SUBSTITUTED BICYCLIC CYCLIC DERIVATIVE AND USE THEREOF
JP5255559B2 (ja) 2006-03-31 2013-08-07 アボット・ラボラトリーズ インダゾール化合物
JP2009534399A (ja) 2006-04-18 2009-09-24 アボット・ラボラトリーズ バニロイド受容体サブタイプ１型（ｖｒ１）の拮抗薬およびその使用
JP5190448B2 (ja) 2006-04-20 2013-04-24 ファイザー・プロダクツ・インク グルコキナーゼ仲介疾患を予防および治療するための縮合フェニルアミド複素環化合物
UA92083C2 (ru) 2006-05-19 2010-09-27 Эбботт Леборетриз Азабициклические алкановые производные, замещенные конденсированным бициклогетероциклом
CN101448791B (zh) 2006-05-24 2011-11-16 伊莱利利公司 Fxr激动剂
WO2007142323A1 (ja) 2006-06-08 2007-12-13 Ube Industries, Ltd. 側鎖にスピロ環構造を有する新規インダゾール誘導体
EP2046741B1 (en) 2006-07-03 2012-10-31 Proximagen Ltd. Indoles as 5-ht6 modulators
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
US8884020B2 (en) 2006-08-07 2014-11-11 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
EA200900613A1 (ru) 2006-11-29 2009-10-30 Пфайзер Продактс Инк. Спирокетоновые ингибиторы ацетил-коа-карбоксилаз
AU2007329480A1 (en) 2006-12-05 2008-06-12 National Chio Tung University Indazole compounds
WO2008072850A1 (en) 2006-12-11 2008-06-19 Amorepacific Corporation Triazine derivatives having inhibitory activity against acetyl-coa carboxylase
ES2396160T3 (es) 2006-12-14 2013-02-19 Bayer Intellectual Property Gmbh Derivados de DIHIDROPIRIDINA que utiliza como inhibidores de la proteina quinasa
EP2079687A1 (en) 2006-12-18 2009-07-22 Ambrx, Inc. Compositions containing, methods involving, and uses of non-natural amino acids and polypeptides
JP2010514688A (ja) 2006-12-22 2010-05-06 ノバルティス アーゲー インドール−４−イルピリミジニル−２−イル−アミン誘導体およびサイクリン依存性キナーゼ阻害剤としてのその使用
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
CN101687789A (zh) 2007-02-12 2010-03-31 因特蒙公司 C型肝炎病毒复制的新颖抑制剂
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
EP2132208A1 (en) 2007-03-28 2009-12-16 NeuroSearch AS 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
AR067769A1 (es) 2007-08-03 2009-10-21 Betagenon Ab Derivado de ditiazol para el tratamiento del cancer
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
WO2009032116A1 (en) 2007-08-29 2009-03-12 Schering Corporation 2, 3-substituted indole derivatives for treating viral infections
TW200924780A (en) 2007-08-29 2009-06-16 Schering Corp 2-carboxy substituted indole derivatives and methods of use thereof
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
CA2705587A1 (en) 2007-11-16 2009-05-22 Schering Corporation 3-aminosulfonyl substituted indole derivatives and methods of use thereof
BRPI0820171B8 (pt) 2007-11-16 2021-05-25 Rigel Pharmaceuticals Inc compostos de carboxamida, sulfonamida e amina para distúrbios metabólicos, composição farmacêutica, e, uso dos mesmos
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
MX2010008376A (es) * 2008-02-04 2011-02-22 Mercury Therapeutics Inc Moduladores ampk.
WO2009115874A2 (en) 2008-03-17 2009-09-24 Matrix Laboratories Ltd. Novel heterocyclic compounds, pharmaceutical compositions containing them and processes for their preparation
WO2009115427A1 (en) 2008-03-20 2009-09-24 F. Hoffmann-La Roche Ag Pyrrolidinyl derivatives and uses thereof
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
MY155836A (en) 2008-04-11 2015-12-15 Merck Patent Gmbh Thienopyridone derivatives as amp-activated protein kinase (ampk) activators
MX2010011288A (es) 2008-04-23 2010-11-09 Rigel Pharmaceuticals Inc Compuestos de carboxamida para el tratamiento de trastornos metabolicos.
DK2280952T3 (da) 2008-05-05 2012-07-23 Merck Patent Gmbh Thienopyridinonderivater som amp-aktiverede proteinkinase(ampk)aktivatorer
GB0808282D0 (en) 2008-05-07 2008-06-11 Medical Res Council Compounds for use in stabilizing p53 mutants
US20110009443A1 (en) 2008-05-28 2011-01-13 Kevin Daniel Freeman-Cook Pyrazolospiroketone Acetyl-Coa Carboxylase Inhibitors
WO2009144554A1 (en) 2008-05-28 2009-12-03 Pfizer, Inc. Pyrazolospiroketone acetyl-c0a carboxylase inhibitors
PL2285786T3 (pl) 2008-06-16 2014-01-31 Merck Patent Gmbh Pochodne chinoksalinodionowe
UY31922A (es) 2008-06-20 2010-01-05 Glaxo Group Ltd Compuestos
DE102008031480A1 (de) 2008-07-03 2010-01-07 Merck Patent Gmbh Salze enthaltend ein Pyrimidincarbonsäure-Derivat
JP2011528363A (ja) 2008-07-16 2011-11-17 キング・ファーマシューティカルズ・リサーチ・アンド・デベロプメント・インコーポレイティッド アテローム性動脈硬化症の治療
WO2010010186A1 (en) 2008-07-25 2010-01-28 Galapagos Nv Novel compounds useful for the treatment of degenerative and inflammatory diseases
EP2318370A1 (en) 2008-07-29 2011-05-11 Pfizer Inc. Fluorinated heteroaryls
MY155418A (en) 2008-08-28 2015-10-15 Pfizer Dioxa-bicyclo[3.2.1]octane-2,3,4-triol derivatives
CN102164909A (zh) 2008-09-26 2011-08-24 弗·哈夫曼-拉罗切有限公司 用于治疗hcv的吡啶或吡嗪衍生物
WO2010036910A1 (en) 2008-09-26 2010-04-01 Yoshikazu Ohta Heart protection by administering an amp-activated protein kinase activator
WO2010047982A1 (en) 2008-10-22 2010-04-29 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
WO2010051176A1 (en) 2008-10-29 2010-05-06 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
JP5557845B2 (ja) 2008-10-31 2014-07-23 メルク・シャープ・アンド・ドーム・コーポレーション 糖尿病用剤として有用な新規環状ベンゾイミダゾール誘導体
KR20100054098A (ko) 2008-11-13 2010-05-24 주식회사 머젠스 허혈 또는 허혈 재관류에 의해 유발되는 심장질환의 치료 및 예방을 위한 약제 조성물
WO2010058858A1 (ja) 2008-11-21 2010-05-27 ラクオリア創薬株式会社 ５－ｈｔ２ｂ受容体拮抗活性を有する新規ピラゾール－３－カルボキサミド誘導体
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
WO2010069949A1 (en) 2008-12-18 2010-06-24 Merck Serono S.A. 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
CA2772760A1 (en) 2008-12-23 2010-07-01 President And Fellows Of Harvard College Small molecule inhibitors of necroptosis
CN102365275B (zh) 2009-01-28 2014-09-24 里格尔药品股份有限公司 羧酰胺化合物及其使用方法
WO2010086613A1 (en) 2009-01-30 2010-08-05 Betagenon Ab Compounds useful as inhibitors as ampk
WO2010086820A1 (en) 2009-02-02 2010-08-05 Pfizer Inc. 4-amino-5-oxo-7, 8-dihydropyrimido [5,4-f] [1,4] oxazepin-6 (5h) -yl) phenyl derivatives, pharmaceutical compositions and uses thereof
US20100210682A1 (en) 2009-02-19 2010-08-19 Abbott Laboratories Repeated Dosing of TRPV1 Antagonists
US20110319379A1 (en) 2009-03-11 2011-12-29 Corbett Jeffrey W Substituted Indazole Amides And Their Use As Glucokinase Activators
MY151246A (en) 2009-03-11 2014-04-30 Pfizer Benzofuranyl derivatives
WO2010106457A2 (en) 2009-03-20 2010-09-23 Pfizer Inc. 3-oxa-7-azabicyclo[3.3.1]nonanes
CN102361878A (zh) 2009-03-24 2012-02-22 住友化学株式会社 用于制备硼酸酯化合物的方法
CA2757615C (en) 2009-03-31 2018-07-17 Renascience Co., Ltd. Plasminogen activator inhibitor-1 inhibitor
WO2010118009A1 (en) 2009-04-06 2010-10-14 Ptc Therapeutics, 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
AU2010270030B2 (en) 2009-07-08 2015-12-24 Baltic Bio Ab 1, 2, 4-thiazolidin-3-one derivatives and their use in the treatment of cancer
WO2011005611A1 (en) 2009-07-09 2011-01-13 Merck Sharp & Dohme Corp. Neuromedin u receptor agonists and uses thereof
CN102574787B (zh) 2009-07-30 2014-12-31 新加坡国立大学 具有潜在的抗癌活性的小分子异戊二烯基半胱氨酸羧基甲基转移酶抑制剂
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
CA2784553C (en) 2009-12-29 2014-08-19 Poxel Thieno [2,3-b] pyridinedione activators of ampk and therapeutic uses thereof
US8895596B2 (en) 2010-02-25 2014-11-25 Merck Sharp & Dohme Corp Cyclic benzimidazole derivatives useful as anti-diabetic agents
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
EP2566868A1 (en) 2010-05-05 2013-03-13 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
BR112013002112B1 (pt) 2010-07-29 2021-04-06 Rigel Pharmaceuticals, Inc. Composto, composição farmacêutica, e, uso de um composto, ou de um respectivo sal farmaceuticamente aceitável, ou de uma composição
KR101190141B1 (ko) 2010-08-24 2012-10-12 서울대학교산학협력단 Ａｍｐｋ를 활성화시키는 화합물을 함유하는 약학조성물
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
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
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
BR112013021236B1 (pt) 2011-02-25 2021-05-25 Merck Sharp & Dohme Corp composto derivado de benzimidazol, e, composição
US20130345243A1 (en) 2011-03-07 2013-12-26 Glaxosmithkline Llc 1h-pyrollo[3,2-d]pyrimidinedione derivatives
CA2830706A1 (en) 2011-03-07 2012-09-13 Glaxosmithkline Llc Quinolinone derivatives
CN103889976A (zh) 2011-08-12 2014-06-25 弗·哈夫曼-拉罗切有限公司 吲唑化合物、组合物及使用方法
CA2860250C (en) 2012-02-21 2020-11-10 Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.P.A. 1h-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta inhibitors

Also Published As

Publication number Publication date
CA2869692A1 (en) 2013-10-17
EP2836490B1 (en) 2017-06-14
HRP20171028T1 (hr) 2017-10-06
TN2014000420A1 (fr) 2016-03-30
LT2836490T (lt) 2017-08-10
NI201400121A (es) 2015-03-05
US20150038484A1 (en) 2015-02-05
CO7091185A2 (es) 2014-10-21
ES2637238T3 (es) 2017-10-11
JP2015512931A (ja) 2015-04-30
PL2836490T3 (pl) 2017-10-31
PH12014502280B1 (en) 2014-12-15
JP6026642B2 (ja) 2016-11-16
AP2014007983A0 (en) 2014-10-31
SI2836490T1 (sl) 2017-08-31
MX2014012330A (es) 2015-01-12
CA2869692C (en) 2016-08-02
ZA201406792B (en) 2016-01-27
WO2014140704A1 (en) 2014-09-18
HK1202547A1 (en) 2015-10-02
AR090633A1 (es) 2014-11-26
CU20140118A7 (es) 2014-11-27
GT201400215A (es) 2015-10-15
CY1119194T1 (el) 2018-02-14
WO2013153479A2 (en) 2013-10-17
KR20150002782A (ko) 2015-01-07
PH12014502280A1 (en) 2014-12-15
ECSP14026271A (es) 2015-11-30
NZ630700A (en) 2015-11-27
PT2836490T (pt) 2017-08-23
RS56290B1 (sr) 2017-12-29
CN104245688A (zh) 2014-12-24
US8889730B2 (en) 2014-11-18
IN2014DN09200A (me) 2015-07-10
IL234860A0 (en) 2014-12-31
EA028564B1 (ru) 2017-12-29
EA201491592A1 (ru) 2015-03-31
SG11201405571SA (en) 2014-10-30
EP2836490A2 (en) 2015-02-18
CR20140411A (es) 2014-10-14
TWI465431B (zh) 2014-12-21
ECSP14020545A (es) 2017-07-31
US20130267493A1 (en) 2013-10-10
UY34736A (es) 2013-11-29
AU2013246552A1 (en) 2014-09-25
TW201402547A (zh) 2014-01-16
WO2013153479A3 (en) 2013-12-05
DK2836490T3 (en) 2017-07-31
MD20140109A2 (ro) 2015-02-28
DOP2014000228A (es) 2014-11-30
PE20142294A1 (es) 2014-12-27
HUE033096T2 (en) 2017-11-28

Similar Documents

Publication Publication Date Title
ME02729B (me) Indolski i indazolski spojevi koji aktiviraju ampk
JP2015512931A5 (me)
HRP20210255T1 (hr) Postupak priprave derivata karbamoilpiridona i međuprodukata
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
JP2016506960A5 (me)
JP2016505614A5 (me)
ME01421B (me) 5-supstituisani derivati kinazolinona kao protivtumorska sredstva
JP2013537203A5 (me)
JP2013544860A5 (me)
ME03723B (me) 2-amin0-6-(difluorometil)- 5,5-difluoro-6-fenil-3,4,5,6-tetrahidropiridini kао васе1 inhibiтori
JP2011519854A5 (me)
EP2288260A4 (en) TRIAZOLOPYRIDINE-JAK HEMMER COMPOUNDS AND METHOD
WO2014068402A3 (en) Pharmaceutical formulation containing thienotriazolodiazepine compounds
AR089134A1 (es) Arilos y heteroarilos biciclicos inhibidores de los canales de sodio
JP2014508811A5 (me)
JP2014507464A5 (me)
MX344276B (es) Compuesto de piperidina novedoso o sal del mismo.
SI2895174T1 (en) The prodrugs of the amino quinazoline kinase inhibitor
AR082620A1 (es) Compuesto de quinolil amina, composicion farmaceutica que lo comprende y su uso para preparar un medicamento util para tratar una enfermedad mediada por la inhibicion de la quinasa rip2
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