KR102603199B1 - Ｓ1ｐ1 수용체-관련 장애에서의 사용을 위한 (ｒ)-2-(7-(4-시클로펜틸-3-(트리플루오로메틸)벤질옥시)-1,2,3,4-테트라히드로시클로-펜타[ｂ]인돌-3-일)아세트산 (화합물 1)의 결정성 ｌ-아르기닌 염 - Google Patents

Ｓ1ｐ1 수용체-관련 장애에서의 사용을 위한 (ｒ)-2-(7-(4-시클로펜틸-3-(트리플루오로메틸)벤질옥시)-1,2,3,4-테트라히드로시클로-펜타[ｂ]인돌-3-일)아세트산 (화합물 1)의 결정성 ｌ-아르기닌 염 Download PDF

Info

Publication number
KR102603199B1
KR102603199B1 KR1020187001785A KR20187001785A KR102603199B1 KR 102603199 B1 KR102603199 B1 KR 102603199B1 KR 1020187001785 A KR1020187001785 A KR 1020187001785A KR 20187001785 A KR20187001785 A KR 20187001785A KR 102603199 B1 KR102603199 B1 KR 102603199B1
Authority
KR
South Korea
Prior art keywords
delete delete
cyclopentyl
benzyloxy
acetic acid
trifluoromethyl
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
KR1020187001785A
Other languages
English (en)
Korean (ko)
Other versions
KR20180015259A (ko
Inventor
안토니 씨. 블랙번
리안 오. 카스트로
마크 에이. 하드
유-안 마
안토니오 개리도 몬탈반
제이미 카린 류터
리 알라니 셀비
사가 라지 샤카
말런 카를로스
Original Assignee
아레나 파마슈티칼스, 인크.
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=56322311&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=KR102603199(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by 아레나 파마슈티칼스, 인크. filed Critical 아레나 파마슈티칼스, 인크.
Priority to KR1020237039088A priority Critical patent/KR102883123B1/ko
Publication of KR20180015259A publication Critical patent/KR20180015259A/ko
Application granted granted Critical
Publication of KR102603199B1 publication Critical patent/KR102603199B1/ko
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • 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
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/80—[b, c]- or [b, d]-condensed
    • C07D209/94—[b, c]- or [b, d]-condensed containing carbocyclic rings other than six-membered
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P3/08—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C279/04—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton
    • C07C279/12—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton being further substituted by nitrogen atoms not being part of nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C279/04—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton
    • C07C279/14—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton being further substituted by carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Epidemiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurosurgery (AREA)
  • Emergency Medicine (AREA)
  • Neurology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Immobilizing And Processing Of Enzymes And Microorganisms (AREA)
  • Enzymes And Modification Thereof (AREA)
KR1020187001785A 2015-06-22 2016-06-21 Ｓ1ｐ1 수용체-관련 장애에서의 사용을 위한 (ｒ)-2-(7-(4-시클로펜틸-3-(트리플루오로메틸)벤질옥시)-1,2,3,4-테트라히드로시클로-펜타[ｂ]인돌-3-일)아세트산 (화합물 1)의 결정성 ｌ-아르기닌 염 Active KR102603199B1 (ko)

Priority Applications (1)

Application Number Priority Date Filing Date Title
KR1020237039088A KR102883123B1 (ko) 2015-06-22 2016-06-21 Ｓ1ｐ1 수용체-관련 장애에서의 사용을 위한 (ｒ)-2-(7-(4-시클로펜틸-3-(트리플루오로메틸)벤질옥시)-1,2,3,4-테트라히드로시클로-펜타[ｂ]인돌-3-일)아세트산 (화합물 1)의 결정성 ｌ-아르기닌 염

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201562182841P 2015-06-22 2015-06-22
US62/182,841 2015-06-22
US201562207531P 2015-08-20 2015-08-20
US62/207,531 2015-08-20
PCT/US2016/038506 WO2016209809A1 (en) 2015-06-22 2016-06-21 Crystalline l-arginine salt of (r)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid(compound1) for use in sipi receptor-associated disorders

Related Child Applications (1)

Application Number Title Priority Date Filing Date
KR1020237039088A Division KR102883123B1 (ko) 2015-06-22 2016-06-21 Ｓ1ｐ1 수용체-관련 장애에서의 사용을 위한 (ｒ)-2-(7-(4-시클로펜틸-3-(트리플루오로메틸)벤질옥시)-1,2,3,4-테트라히드로시클로-펜타[ｂ]인돌-3-일)아세트산 (화합물 1)의 결정성 ｌ-아르기닌 염

Publications (2)

Publication Number Publication Date
KR20180015259A KR20180015259A (ko) 2018-02-12
KR102603199B1 true KR102603199B1 (ko) 2023-11-16

Family

ID=56322311

Family Applications (2)

Application Number Title Priority Date Filing Date
KR1020187001785A Active KR102603199B1 (ko) 2015-06-22 2016-06-21 Ｓ1ｐ1 수용체-관련 장애에서의 사용을 위한 (ｒ)-2-(7-(4-시클로펜틸-3-(트리플루오로메틸)벤질옥시)-1,2,3,4-테트라히드로시클로-펜타[ｂ]인돌-3-일)아세트산 (화합물 1)의 결정성 ｌ-아르기닌 염
KR1020237039088A Active KR102883123B1 (ko) 2015-06-22 2016-06-21 Ｓ1ｐ1 수용체-관련 장애에서의 사용을 위한 (ｒ)-2-(7-(4-시클로펜틸-3-(트리플루오로메틸)벤질옥시)-1,2,3,4-테트라히드로시클로-펜타[ｂ]인돌-3-일)아세트산 (화합물 1)의 결정성 ｌ-아르기닌 염

Family Applications After (1)

Application Number Title Priority Date Filing Date
KR1020237039088A Active KR102883123B1 (ko) 2015-06-22 2016-06-21 Ｓ1ｐ1 수용체-관련 장애에서의 사용을 위한 (ｒ)-2-(7-(4-시클로펜틸-3-(트리플루오로메틸)벤질옥시)-1,2,3,4-테트라히드로시클로-펜타[ｂ]인돌-3-일)아세트산 (화합물 1)의 결정성 ｌ-아르기닌 염

Country Status (20)

Country Link
US (6) US10301262B2 (enExample)
EP (2) EP3939965A1 (enExample)
JP (3) JP6838744B2 (enExample)
KR (2) KR102603199B1 (enExample)
CN (1) CN108349891B (enExample)
AU (4) AU2016284162A1 (enExample)
BR (1) BR112017027656B1 (enExample)
CA (1) CA3002551A1 (enExample)
CY (1) CY1125778T1 (enExample)
DK (1) DK3310760T3 (enExample)
EA (1) EA201890096A1 (enExample)
ES (1) ES2929526T3 (enExample)
HU (1) HUE060476T2 (enExample)
IL (2) IL285890B (enExample)
MA (1) MA42807A (enExample)
MX (2) MX383854B (enExample)
PL (1) PL3310760T3 (enExample)
PT (1) PT3310760T (enExample)
SI (1) SI3310760T1 (enExample)
WO (1) WO2016209809A1 (enExample)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG10201500639TA (en) 2010-01-27 2015-03-30 Arena Pharm Inc Processes for the preparation of (r)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid and salts thereof
ES2995737T3 (en) 2015-01-06 2025-02-11 Arena Pharm Inc Compound for use in treating conditions related to the s1p1 receptor
MA42807A (fr) 2015-06-22 2018-07-25 Arena Pharm Inc Sel l-arginine cristallin d'acide (r)-2-(7-(4-cyclopentyl-3-(trifluorométhyl)benzyloxy)-1,2,3,4-tétrahydrocyclo-penta[b]indol-3-yl)acétique (composé 1) pour une utilisation dans des troubles associés au récepteur de s1p1
CA3053416A1 (en) 2017-02-16 2018-08-23 Arena Pharmaceuticals, Inc. Compounds and methods for treatment of inflammatory bowel disease with extra-intestinal manifestations
WO2018151873A1 (en) 2017-02-16 2018-08-23 Arena Pharmaceuticals, Inc. Compounds and methods for treatment of primary biliary cholangitis
IL271149B2 (en) * 2017-06-14 2024-05-01 Trevena Inc Compounds for modulating s1p1 activity and methods of using the same
EP3801459B1 (en) 2018-06-06 2024-08-07 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the s1p1 receptor
WO2020051378A1 (en) * 2018-09-06 2020-03-12 Arena Pharmaceuticals, Inc. Compounds useful in the treatment of autoimmune and inflammatory disorders
US20210386706A1 (en) * 2018-10-03 2021-12-16 Arena Pharmaceuticals, Inc. Methods for the treatment of scleroderma
CN109678715B (zh) * 2018-11-28 2019-11-12 中国药科大学 2-(1-酰氧正戊基)苯甲酸与碱性氨基酸或氨基胍形成的盐、其制备方法及用途
MX2022003982A (es) * 2019-10-01 2022-07-12 Arena Pharm Inc Metodos de tratamiento de enfermedades relacionadas con el receptor s1p1.
PH12022551043A1 (en) 2019-10-31 2023-05-03 Idorsia Pharmaceuticals Ltd Combination of a cxcr7 antagonist with an s1p1 receptor modulator
JP2023502123A (ja) 2019-11-19 2023-01-20 トレベナ・インコーポレイテッド Ｓ１ｐ１モジュレーター化合物及び化合物を調製する方法
WO2025177319A2 (en) * 2024-02-22 2025-08-28 Msn Laboratories Private Limited, R&D Center Solid state forms of L-Arginine, (3R)-7-[[4-cyclopentyl-3-(trifluoromethyl)phenyl]methoxy]-1,2,3,4-tetrahydrocyclopent[b]indole-3-acetate and processes for preparation thereof

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010011316A1 (en) 2008-07-23 2010-01-28 Arena Pharmaceuticals, Inc. SUBSTITUTED 1,2,3,4- TETRAHYDROCYCLOPENTA[b]INDOL-3-YL) ACETIC ACID DERIVATIVES USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS
WO2011094008A1 (en) 2010-01-27 2011-08-04 Arena Pharmaceuticals, Inc. Processes for the preparation of (r)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid and salts thereof

Family Cites Families (516)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH389134A (de) 1960-03-15 1965-03-15 Ciba Geigy Verfahren zur Herstellung neuer Anthrachinonküpenfarbstoffe
NL293572A (enExample) 1962-06-07
CH478819A (de) 1965-10-22 1969-09-30 Ciba Geigy Verfahren zur Herstellung neuer N,N'-Di-(pyrimidyl-(4)-aminoalkyl)-diazacycloalkanen
CH480410A (de) 1967-01-09 1969-10-31 Geigy Ag J R Verfahren zur Herstellung von wasserlöslichen Azopyrimidinfarbstoffen
CA961052A (en) 1967-01-12 1975-01-14 Max Schellenbaum N-2-ethylhexyl-n'-aryl ureas and preparation containing them
FR1593586A (enExample) 1967-10-17 1970-06-01
US3608087A (en) 1968-06-21 1971-09-21 Merck & Co Inc Feed compositions
US3887329A (en) 1969-05-05 1975-06-03 Ciba Geigy Ag Hexamethyl phosphotriamide-dye compositions
BE756953A (fr) 1969-10-02 1971-04-01 Merck & Co Inc Potentialisation d'antibiotiques
US3686238A (en) 1970-01-19 1972-08-22 Syntex Corp Glycerol esterified with 2-naphthyl-acetic acids and fatty acids
US3852434A (en) 1970-09-11 1974-12-03 Merck & Co Inc Potentiation of ({31 ) cis-1,2-epoxypropyl)phosphonic acid and analogues thereof
US3690834A (en) 1971-01-11 1972-09-12 Syva Co Ligand determination with spin labeled compounds by receptor displacement
US3966744A (en) 1971-01-11 1976-06-29 Syva Company Spin labeled compounds
DE2106585A1 (de) 1971-02-11 1972-08-24 Farbenfabriken Bayer Ag, 5090 Leverkusen Aminothiodiazole und Thiodiazol-Azofarbstoffe
CH560197A5 (en) 1971-05-17 1975-03-27 Ciba Geigy Ag 2-alkylthio-4,6-bis (subst amino)-5-nitropyrimidines - - herbicides
CH558137A (de) 1971-05-17 1975-01-31 Ciba Geigy Ag Mittel zur beeinflussung des pflanzenwachstums.
DE2226703A1 (de) 1972-05-25 1973-12-13 Schering Ag Neue tetrahydrocarbazolderivate und verfahren zu ihrer herstellung
US3966764A (en) 1972-07-10 1976-06-29 Syva Company Ligand determination of spin labeled compounds by receptor displacement-amphetamine analogs
US3849420A (en) 1972-10-20 1974-11-19 Dow Chemical Co Bis-(alkylthio-and alkylsulfonyl)-pentachloroquinolines
CH574206A5 (enExample) 1972-11-16 1976-04-15 Ciba Geigy Ag
DE2340569C2 (de) 1973-08-10 1982-12-02 Bayer Ag, 5090 Leverkusen Azofarbstoffe
AT340933B (de) 1973-08-20 1978-01-10 Thomae Gmbh Dr K Verfahren zur herstellung neuer pyrimidinderivate und ihrer saureadditionssalze
DE2341925A1 (de) 1973-08-20 1975-03-06 Thomae Gmbh Dr K Neue pyrimidinderivate und verfahren zu ihrer herstellung
US4057559A (en) 1973-10-01 1977-11-08 American Home Products Corporation Carbazole acetic acid derivatives
CH584739A5 (enExample) 1973-12-21 1977-02-15 Ciba Geigy Ag
US4101541A (en) 1973-12-21 1978-07-18 Ciba-Geigy Corporation 3-Cyano-1,2,4-thiadiazolyl-5-czo dyestuffs
FR2258841B1 (enExample) 1974-01-29 1977-11-04 Ugine Kuhlmann
AT327605B (de) 1974-05-06 1976-02-10 Ciba Geigy Ag Mittel zur hemmung des pflanzenwachstums
AU492126B2 (en) 1974-05-14 1975-11-20 Ciba-Geigy Ag Nitropyrimidine derivatives
FR2306697A1 (fr) 1975-04-10 1976-11-05 Sogeras Nouvelles pyrimidines utilisables comme medicaments antidiabetiques et hypocholesterolemiants
US4139705A (en) 1977-05-20 1979-02-13 The Dow Chemical Company Pyrazolopyrimidines
US4189579A (en) 1977-05-20 1980-02-19 The Dow Chemical Company Aminoalkylthiopurines
DE2731264A1 (de) 1977-07-11 1979-02-01 Boehringer Mannheim Gmbh Neue 1-acyl-2-cyanaziridine, verfahren zu deren herstellung und diese verbindungen enthaltende pharmazeutische zubereitungen
JPS6038696B2 (ja) 1977-12-09 1985-09-02 コニカ株式会社 ハロゲン化銀カラ−写真感光材料
US4242507A (en) 1978-02-23 1980-12-30 Fujisawa Pharmaceutical Co., Ltd. Sulfonic acid esters
DE2831580C2 (de) 1978-07-18 1980-09-18 Boehringer Mannheim Gmbh, 6800 Mannheim Verfahren und Reagens zur Bestimmung von Glycerin
DE2831850A1 (de) 1978-07-20 1980-02-07 Basf Ag N-arylsulfonylpyrrole, ihre herstellung und diese enthaltende therapeutische mittel
DE2906603A1 (de) 1979-02-21 1980-09-04 Boehringer Mannheim Gmbh N-substituierte aziridin-2-carbonsaeurederivate, verfahren zu deren herstellung sowie diese substanzen enthaltende arzneimittel
US4343804A (en) 1979-03-26 1982-08-10 A. H. Robins Company, Inc. 4-Amino-3-quinolinecarboxylic acids and esters-antisecretory anti-ulcer compounds
DE3070304D1 (en) 1980-04-28 1985-04-25 Teijin Ltd Thiazolo(3,2-a)pyrimidine derivatives, process for preparing same, and drug containing same
EP0053678A1 (de) 1980-12-05 1982-06-16 BASF Aktiengesellschaft 5-Amino-1-phenyl-4-cyanpyrazole, diese enthaltende herbizide Mittel, Verfahren zu ihrer Herstellung und ihre Anwendung als Herbizide
RU938559C (ru) 1980-12-12 1993-11-30 Всесоюзный научно-исследовательский химико-фармацевтический институт им.Серго Орджоникидзе S-Производные 5-амино-6-меркаптопиримидина, обладающие противоопухолевым и цитостатическим действием
DOP1981004033A (es) 1980-12-23 1990-12-29 Ciba Geigy Ag Procedimiento para proteger plantas de cultivo de la accion fitotoxica de herbicidas.
US4476248A (en) 1983-02-28 1984-10-09 The Upjohn Company Crystallization of ibuprofen
DE3334455A1 (de) 1983-03-04 1984-09-06 Bayer Ag, 5090 Leverkusen Guanidin - derivate
US4612376A (en) 1983-03-25 1986-09-16 Fujisawa Pharmaceutical Co., Ltd. Substituted-3,4-dihydro-4-(2,4,6-trimethoxyphenylimino)-2(1H)-pyrimidones useful as cardiotonic, antihypertensive, cerebrovascular vasodilator and anti-platelet agent
ZA848275B (en) 1983-12-28 1985-08-28 Degussa New piridine-2-ethers or pyridine-2-thioethers having a nitrogen-containing cycloaliphatic ring
DE3406329A1 (de) 1984-02-22 1985-08-22 Merck Patent Gmbh, 6100 Darmstadt Pyridone
JPS6157587A (ja) 1984-08-29 1986-03-24 Shionogi & Co Ltd 縮合複素環誘導体および抗潰瘍剤
PH22302A (en) 1985-02-11 1988-07-22 Fujisawa Pharmaceutical Co Piperidine compounds
AU601145B2 (en) 1985-03-01 1990-09-06 Duphar International Research B.V. Benzoyl urea derivatives having anti-tumor activity
DE3601196A1 (de) 1986-01-17 1987-07-23 Merck Patent Gmbh 1,4-dihydropyridine
US4810699A (en) 1987-02-20 1989-03-07 American Home Products Corporation Substituted 1,3,4,9-tetrahydropyrano[3,4,-b]indole-1-acetic acids, pharmaceutical compositions containing them, and methods for treating inflammatory conditions and for analgesic purposes using them
CA1340284C (en) 1987-03-19 1998-12-22 Zeneca Inc. Herbicidal substituted cyclic diones
DE68926687T2 (de) 1988-01-11 1997-03-06 Fuji Photo Film Co Ltd Verfahren zur Erzeugung von extrem hochkontrastreichen negativen Bildern
US4782076A (en) 1988-03-01 1988-11-01 American Home Products Corporation Substituted 2,3,4,9-tetrahydro-1H-carbazole-1-acetic acid derivatives, composition and use
PT95692A (pt) 1989-10-27 1991-09-13 American Home Prod Processo para a preparacao de derivados de acidos indole-,indeno-,piranoindole- e tetra-hidrocarbazole-alcanoicos, ou quais sao uteis como inibidores de pla2 e da lipoxigenase
NZ238863A (en) 1990-07-19 1993-03-26 Janssen Pharmaceutica Nv Substituted thiazolyl and pyridinyl derivatives
US5221678A (en) 1990-07-26 1993-06-22 Merck Frosst Canada, Inc. (quinolin-2-ylmethoxy)tetrahydrocarbazoles as inhibitors of the biosynthesis of leukotrienes
EP0567643A4 (en) 1991-01-16 1995-07-19 Yoshitomi Pharmaceutical PYRIDINE COMPOUND USED AS A SELECTIVE DRUG AND NEW PYRIDINE COMPOUND.
CA2070978A1 (en) 1991-06-11 1992-12-12 William J. Greenlee Cyclic renin inhibitors
GB9114760D0 (en) 1991-07-09 1991-08-28 Pfizer Ltd Therapeutic agents
JPH0533359A (ja) 1991-08-02 1993-02-09 Kubota Corp 全旋回型の小型バツクホウ
EP0556889A1 (en) 1992-02-18 1993-08-25 Duphar International Research B.V Method of preparing aryl(homo)piperazines
DE4208254A1 (de) 1992-03-14 1993-09-16 Hoechst Ag Substituierte pyrimidine, verfahren zu ihrer herstellung und ihre verwendung als schaedlingsbekaempfungsmittel und fungizid
TW237456B (enExample) 1992-04-09 1995-01-01 Ciba Geigy
FR2692575B1 (fr) 1992-06-23 1995-06-30 Sanofi Elf Nouveaux derives du pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant.
NZ314207A (en) 1992-09-28 2000-12-22 Vertex Pharma 1-(2-Oxoacetyl)-piperidine-2-carboxylic acid derivatives as multi drug resistant cancer cell sensitizers
DE4241632A1 (de) 1992-12-10 1994-06-16 Thomae Gmbh Dr K Carbonsäurederivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
TW370529B (en) 1992-12-17 1999-09-21 Pfizer Pyrazolopyrimidines
US5998499A (en) 1994-03-25 1999-12-07 Dentsply G.M.B.H. Liquid crystalline (meth)acrylate compounds, composition and method
JPH0753546A (ja) 1993-08-09 1995-02-28 Kuraray Co Ltd ジアリール置換複素環化合物およびその医薬用途
NZ274978A (en) 1993-10-12 1998-04-27 Du Pont Merck Pharma 1n-alkyl-n-aryl pyrimidinamine derivatives and pharmaceutical compositions thereof
GB9400889D0 (en) 1994-01-18 1994-03-16 Sandoz Ltd Novel compounds
TW530047B (en) 1994-06-08 2003-05-01 Pfizer Corticotropin releasing factor antagonists
CN1118454C (zh) 1994-09-09 2003-08-20 日本新药株式会社 杂环衍生物和医药
SK281865B6 (sk) 1994-11-29 2001-08-06 Dainippon Pharmaceutical Co., Ltd. Indolový derivát a jeho optický izomér, spôsob jeho prípravy a farmaceutický prostriedok
CA2214685C (en) 1995-03-10 2008-05-20 Berlex Laboratories, Inc. Benzamidine derivatives their preparation and their use as anti-coagulants
US5691364A (en) 1995-03-10 1997-11-25 Berlex Laboratories, Inc. Benzamidine derivatives and their use as anti-coagulants
IL117659A (en) 1995-04-13 2000-12-06 Dainippon Pharmaceutical Co Substituted 2-phenyl pyrimidino amino acetamide derivative process for preparing the same and a pharmaceutical composition containing same
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
WO1996033994A1 (en) 1995-04-28 1996-10-31 Nippon Soda Co., Ltd. Amino-substituted derivatives, process for the preparation thereof, and herbicide
US6020492A (en) 1995-05-12 2000-02-01 Neurogen Corporation Deazapurine derivatives; a new class of CRF1 specific ligands
WO1996036613A1 (en) 1995-05-19 1996-11-21 Nippon Soda Co., Ltd. Substituted benzoic acid derivatives, process for the production thereof, and herbicides
US6956047B1 (en) 1995-06-06 2005-10-18 Pfizer Inc. Corticotropin releasing factor antagonists
US6403599B1 (en) 1995-11-08 2002-06-11 Pfizer Inc Corticotropin releasing factor antagonists
TWI238064B (en) 1995-06-20 2005-08-21 Takeda Chemical Industries Ltd A pharmaceutical composition for prophylaxis and treatment of diabetes
KR0169813B1 (ko) 1995-07-12 1999-01-15 김종인 4-아미노-3-아실나프티리딘 유도체
ATE197150T1 (de) 1995-08-31 2000-11-15 Lonza Ag Verfahren zur herstellung von dihydroxypyrimidin- derivaten
DE69628051T2 (de) 1995-10-26 2004-02-26 Mitsubishi Pharma Corp. Phenylethanolamin-verbindungen und ihre anwendung als beta3 agonisten, verfahren zu ihrer herstellung und zwischenprodukte ihrer herstellung
US5849759A (en) 1995-12-08 1998-12-15 Berlex Laboratories, Inc. Naphthyl-substituted benzimidazole derivatives as anti-coagulants
USH2007H1 (en) 1996-01-19 2001-12-04 Fmc Corporation Insecticidal N-heterocyclylalkyl-or N-[(polycyclyl)alkyl]-N′substituted piperazines
DE19602095A1 (de) 1996-01-22 1997-07-24 Bayer Ag Halogenpyrimidine
WO1997028137A1 (en) 1996-02-02 1997-08-07 Merck & Co., Inc. Heterocyclic derivatives as antidiabetic and antiobesity agents
CZ244598A3 (cs) 1996-02-07 1998-10-14 Janssen Pharmaceutica N.V. Pyrazolopyrimidiny jako antagonisty CRF receptoru
US5948786A (en) 1996-04-12 1999-09-07 Sumitomo Pharmaceuticals Company, Limited Piperidinylpyrimidine derivatives
DE122010000020I1 (de) 1996-04-25 2010-07-08 Prosidion Ltd Verfahren zur Senkung des Blutglukosespiegels in Säugern
DE19624659A1 (de) 1996-06-20 1998-01-08 Klinge Co Chem Pharm Fab Neue Pyridylalken- und Pyridylalkinsäureamide
WO1997049706A1 (en) 1996-06-25 1997-12-31 Novartis Ag SUBSTITUTED 7-AMINO-PYRROLO[3,2-d]PYRIMIDINES AND THE USE THEREOF
US6060478A (en) 1996-07-24 2000-05-09 Dupont Pharmaceuticals Azolo triazines and pyrimidines
US5776967A (en) 1996-07-26 1998-07-07 American Home Products Corporation Pyranoindole inhibitors of COX--2
AR008789A1 (es) 1996-07-31 2000-02-23 Bayer Corp Piridinas y bifenilos substituidos
US5830911A (en) 1996-08-14 1998-11-03 American Home Products Corporation Pyranoindole and tetrahydrocarbazole inhibitors of COX-2
TW477787B (en) 1996-08-27 2002-03-01 Pfizer Pyrido six-membered nitrogen-containing cyclic ring derivatives having corticotropin releasing factor antagonist activity and pharmaceutical composition containing same
CZ68199A3 (cs) 1996-08-28 1999-11-17 Pfizer Inc. 6,5-Heterobicyklické deriváty, farmaceutická kompozice na jejich bázi a způsob léčení chorob
US6008234A (en) 1996-09-12 1999-12-28 Berlex Laboratories, Inc. Benzamidine derivatives substituted by cyclic amino acid and cyclic hydroxy acid derivatives and their use as anti-coagulants
DK0929547T3 (da) 1996-09-12 2003-03-10 Schering Ag Benzamidinderivater substitueret af cykliske aminosyrederivater eller cykliske hydroxysyrederivater og deres anvendelse som antikoagulantia
GB9718972D0 (en) 1996-09-25 1997-11-12 Zeneca Ltd Chemical compounds
TW492957B (en) 1996-11-07 2002-07-01 Novartis Ag N-substituted 2-cyanopyrrolidnes
DZ2376A1 (fr) 1996-12-19 2002-12-28 Smithkline Beecham Plc Dérivés de sulfonamides nouveaux procédé pour leurpréparation et compositions pharmaceutiques les c ontenant.
IL123232A0 (en) 1997-02-11 1999-11-30 Lilly Co Eli Medicament for inhibiting glucose metabolism deterioration
WO1998035967A2 (en) 1997-02-18 1998-08-20 Neurocrine Biosciences, Inc. Biazacyclic crf antagonists
US6211195B1 (en) 1997-04-22 2001-04-03 Neurocrine Biosciences, Inc. CRF antagonistic thiophenopyridines
PT977737E (pt) 1997-04-22 2004-02-27 Janssen Pharmaceutica Nv Quino- e quinazolinas antagonistas de crf
JPH11193277A (ja) 1997-05-14 1999-07-21 Nippon Soda Co Ltd ピリミジン誘導体、その製法および有害生物防除剤
DE19737723A1 (de) 1997-08-14 1999-02-18 Bayer Ag Methoximinomethyloxadiazine
JP2001515076A (ja) 1997-08-14 2001-09-18 バイエル・アクチエンゲゼルシヤフト 有害生物防除剤として使用されるメトキシイミノメチルオキサジアジン
NL1010018C2 (nl) 1997-09-09 1999-03-10 Duphar Int Res Chinoline en chinazoline derivaten met corticotropine releasing factor (CRF) antagonistische werking.
US6861448B2 (en) 1998-01-14 2005-03-01 Virtual Drug Development, Inc. NAD synthetase inhibitors and uses thereof
US6187777B1 (en) 1998-02-06 2001-02-13 Amgen Inc. Compounds and methods which modulate feeding behavior and related diseases
JP2002510687A (ja) 1998-04-02 2002-04-09 ニューロゲン コーポレイション アミノアルキル置換ピロロ［２，３−ｂ］ピリジンおよびピロロ［２，３−ｄ］ピリミジン誘導体：ｃｒｆ１レセプタのモジュレータ
JP2000038350A (ja) 1998-05-18 2000-02-08 Yoshitomi Pharmaceut Ind Ltd 糖尿病治療薬
EP1105394A1 (en) 1998-08-21 2001-06-13 Du Pont Pharmaceuticals Company ISOXAZOLO 4,5-d]PYRIMIDINES AS CRF ANTAGONISTS
AU762523C (en) 1998-11-10 2004-02-12 Janssen Pharmaceutica N.V. HIV replication inhibiting pyrimidines
US6262088B1 (en) 1998-11-19 2001-07-17 Berlex Laboratories, Inc. Polyhydroxylated monocyclic N-heterocyclic derivatives as anti-coagulants
ES2308759T3 (es) 1998-11-20 2008-12-01 Arena Pharmaceuticals, Inc. Receptores acoplados a proteina g humanos huerfanos.
CO5150173A1 (es) 1998-12-10 2002-04-29 Novartis Ag Compuestos n-(glicilo sustituido)-2-cianopirrolidinas inhibidores de peptidasa de dipeptidilo-iv (dpp-iv) los cuales son efectivos en el tratamiento de condiciones mediadas por la inhibicion de dpp-iv
US6239126B1 (en) 1998-12-17 2001-05-29 American Home Products Corporation Arylpiperidine and aryl-1,2,5,6-tetra-hydropyridine urea derivatives
JP2002532472A (ja) 1998-12-17 2002-10-02 アメリカン・ホーム・プロダクツ・コーポレイション ５−ｈｔ１ａ受容体活性を有するアリールピペリジンおよびアリール−１，２，５，６−テトラヒドロピリジン尿素誘導体
JP2002532479A (ja) 1998-12-18 2002-10-02 アクシス・ファーマシューティカルズ・インコーポレイテッド プロテアーゼインヒビター
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
US6267985B1 (en) 1999-06-30 2001-07-31 Lipocine Inc. Clear oil-containing pharmaceutical compositions
HUP0105114A3 (en) 1999-03-17 2002-09-30 Astrazeneca Ab Quinazolinone derivatives, pharmaceutical compositions containing them, their use and process for their preparation
EP1040831A3 (en) 1999-04-02 2003-05-02 Pfizer Products Inc. Use of corticotropin releasing factor (CRF) antagonists to prevent sudden death
RU2267484C2 (ru) 1999-04-28 2006-01-10 Авентис Фарма Дойчланд Гмбх Производные диариловой кислоты и фармацевтическая композиция на их основе
KR20020027463A (ko) 1999-07-12 2002-04-13 우에노 도시오 스핀고신-1-인산 수용체 아고니스트 또는스핀고신-1-인산을 유효 성분으로서 함유하는 선유화 억제제
EP1074549B1 (en) 1999-08-06 2003-11-19 F. Hoffmann-La Roche Ag Tetrahydro-benzo(d)azepines and their use as antagonists at metabotropic glutamate receptors
DE60004685T2 (de) 1999-09-17 2004-07-29 Abbott Gmbh & Co. Kg Pyrazolopyrimidine als arzneimittel
US6921763B2 (en) 1999-09-17 2005-07-26 Abbott Laboratories Pyrazolopyrimidines as therapeutic agents
US6414002B1 (en) 1999-09-22 2002-07-02 Bristol-Myers Squibb Company Substituted acid derivatives useful as antidiabetic and antiobesity agents and method
JP2001089452A (ja) 1999-09-22 2001-04-03 Sankyo Co Ltd ピリミジン誘導体
DE60025837T2 (de) 1999-09-24 2006-11-02 Janssen Pharmaceutica N.V. Antivirale feste dispersionen
PL354982A1 (en) 1999-09-30 2004-03-22 Neurogen Corporation Amino substituted pyrazolo[1,5,-a]-1,5-pyrimidines and pyrazolo[1,5-a]-1,3,5-triazines
OA12050A (en) 1999-09-30 2006-05-02 Neurogen Corp Certain alkylene diamine-substituted heterocycles.
HUP0202678A3 (en) 1999-09-30 2004-06-28 Pfizer Certain alkylene diamine-substituted pyrazolo[1,5,-a]-1,5-pyrimidines and pyrazolo[1,5-a]-1,3,5-triazines, pharmaceutical compositions containing them and their use
DE19947154A1 (de) 1999-10-01 2001-10-04 Bayer Ag Substituierte 2-Thio-3,5-dicyano-4-aryl-6-aminopyridine und ihre Verwendung
US6887870B1 (en) 1999-10-12 2005-05-03 Bristol-Myers Squibb Company Heterocyclic sodium/proton exchange inhibitors and method
CO5271670A1 (es) 1999-10-29 2003-04-30 Pfizer Prod Inc Antagonistas del factor de liberacion de corticitropina y composiciones relacionadas
GR990100388A (el) 1999-11-09 2001-07-31 Φαρμακευτικος συνδυασμος αποτελουμενος απο χωριστες δοσολογικες μορφες σε συσκευασια συμμορφωσης (compliance package) ενος αναστολεα της αναγωγασης του υδροξυ-μεθυλο-γλουταρυλο συνενζυμου α (στατινης, statin) και ενος παραγωγου του φιμπρικου οξεος....
WO2001046204A1 (en) 1999-12-22 2001-06-28 Merck Frosst Canada & Co. Aromatic phosphonates as protein tyrosine phosphatase 1b (ptp-1b) inhibitors
DE19962936A1 (de) 1999-12-24 2001-06-28 Bayer Ag Neue beta-Aminosäureverbindungen als Integrinantagonisten
TR200201684T2 (tr) 1999-12-30 2002-10-21 H. Lundbeck A/S Fenilpiperazinil türevleri
MXPA02007047A (es) 2000-01-18 2002-12-13 Pfizer Prod Inc Antagonista del factor liberador de corticotropina.
SK11202002A3 (sk) 2000-02-09 2003-03-04 Hokuriku Seiyaku Co., Ltd. Deriváty 1H-imidazopyridínu
JP2003523418A (ja) 2000-02-15 2003-08-05 フオスター・ミラー・インコーポレイテツド 揮発性有機成分を含まない放射硬化性樹脂組成物
US6569879B2 (en) 2000-02-18 2003-05-27 Merck & Co., Inc. Aryloxyacetic acids for diabetes and lipid disorders
CA2400021A1 (en) 2000-02-18 2001-08-23 Merck & Co., Inc. Aryloxyacetic acids for diabetes and lipid disorders
CA2398274C (en) 2000-02-25 2009-09-22 F. Hoffmann-La Roche Ag Adenosine receptor modulators
PE20020229A1 (es) 2000-04-12 2002-04-11 Novartis Ag COMBINACION DE UN ANTAGONISTA DEL RECEPTOR AT1; UN INHBIDOR DE HMG-CoA REDUCTASA Y UN INHIBIDOR DE ACE
EP1282607B1 (en) 2000-05-08 2015-11-11 Janssen Pharmaceutica NV Prodrugs of hiv replication inhibiting pyrimidines
DE10024319A1 (de) 2000-05-17 2001-11-22 Merck Patent Gmbh Bisacylguanidine
AU2001263288A1 (en) 2000-05-18 2001-11-26 Neurocrine Biosciences, Inc. Crf receptor antagonists
EP1287133B1 (en) 2000-05-18 2006-12-13 Bayer HealthCare AG Regulation of human dopamine-like g protein-coupled receptor
CN1187342C (zh) 2000-05-25 2005-02-02 弗·哈夫曼-拉罗切有限公司 取代的1－氨基烷基内酰胺化合物及其作为毒蕈碱受体拮抗剂的用途
US6620821B2 (en) 2000-06-15 2003-09-16 Bristol-Myers Squibb Company HMG-CoA reductase inhibitors and method
HRP20030027A2 (en) 2000-06-28 2004-02-29 Teva Pharma Carvedilol
AU2001268718B2 (en) 2000-06-29 2006-01-05 Abbott Laboratories Aryl phenylheterocyclyl sulfide derivatives and their use as cell adhesion-inhibiting anti-inflammatory and immune-suppressive agents
AR028782A1 (es) 2000-07-05 2003-05-21 Taisho Pharmaceutical Co Ltd Derivados heterociclicos tetrahidropiridino o piperidino
US6444685B1 (en) 2000-07-17 2002-09-03 Wyeth N-(4-sulfonylaryl)Cyclylamine 2-hydroxyethylamines as beta-3 adrenergic receptor agonists
PL359416A1 (en) 2000-07-18 2004-08-23 Yamanouchi Pharmaceutical Co, Ltd. Medicine comprising dicyanopyridine derivative
AU7705601A (en) 2000-07-25 2002-02-05 Merck & Co Inc N-substituted indoles useful in the treatment of diabetes
US6410583B1 (en) 2000-07-25 2002-06-25 Merck Frosst Canada & Co. Cyclopentanoindoles, compositions containing such compounds and methods of treatment
WO2002019975A1 (fr) 2000-09-05 2002-03-14 Taisho Pharmaceutical Co., Ltd. Stimulants de la croissance des cheveux
EP1322289B1 (en) 2000-09-20 2007-07-25 Jagotec AG Spray drying process of compositions containing fenofibrate
US20030224058A1 (en) 2002-05-24 2003-12-04 Elan Pharma International, Ltd. Nanoparticulate fibrate formulations
US7276249B2 (en) 2002-05-24 2007-10-02 Elan Pharma International, Ltd. Nanoparticulate fibrate formulations
PE20020507A1 (es) 2000-10-17 2002-06-25 Schering Corp Compuestos no-imidazoles como antagonistas del receptor histamina h3
AU2002223626A1 (en) 2000-10-20 2002-04-29 Novartis Ag Combinations of a thyromimetic compound and a statin
EP2404603A1 (en) 2000-10-23 2012-01-11 Glaxosmithkline LLC Novel trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds for the treatment of CSBP/p38 kinase mediated diseases
EP1347755A2 (en) 2000-10-31 2003-10-01 Merck & Co., Inc. Benzopyrancarboxylic acid derivatives for the treatment of diabetes and lipid disorders
ES2279835T3 (es) 2000-11-03 2007-09-01 Neurocrine Biosciences, Inc. Antagonistas del receptor de crf y metodos relacionados.
US20020058026A1 (en) 2000-11-13 2002-05-16 Milton Hammerly HMG CoA reductase inhibitor medications combined wih CoEnzyme Q-10
AU2002223492A1 (en) 2000-11-14 2002-05-27 Neurosearch A/S Use of malaria parasite anion channel blockers for treating malaria
UA77165C2 (en) 2000-11-17 2006-11-15 Lilly Co Eli (n)-((s)-2-hydroxy-3-methyl-butyryl)-1-(l-alaninyl)-(s)-1-amino-3-methyl-4,5,6,7-tetrahydro-2h-3-benzazepin-2-one dihydrate, processes for manufacturing and pharmaceutical composition
CA2429426A1 (en) 2000-11-17 2002-05-23 Takeda Chemical Industries, Ltd. Isoxazole derivatives
KR100846339B1 (ko) 2000-11-20 2008-07-15 바이오비트럼 에이비(피유비엘) 세로토닌 5ｈｔ-2 수용체의 아고니스트 또는안타고니스트로서의 피페라지닐피라진 화합물
AU2002218509A1 (en) 2000-12-01 2002-06-11 Yamanouchi Pharmaceutical Co..Ltd. Method of screening remedy for diabetes
US20020137755A1 (en) 2000-12-04 2002-09-26 Bilodeau Mark T. Tyrosine kinase inhibitors
US20020107262A1 (en) 2000-12-08 2002-08-08 3M Innovative Properties Company Substituted imidazopyridines
US6545017B1 (en) 2000-12-08 2003-04-08 3M Innovative Properties Company Urea substituted imidazopyridines
US6525064B1 (en) 2000-12-08 2003-02-25 3M Innovative Properties Company Sulfonamido substituted imidazopyridines
US6545016B1 (en) 2000-12-08 2003-04-08 3M Innovative Properties Company Amide substituted imidazopyridines
DK1347971T3 (da) 2000-12-21 2006-05-15 Bristol Myers Squibb Co Thiazolylinhibitorer af tyrosinkinaser fra Tec-familien
HU230435B1 (hu) 2001-01-26 2016-06-28 Merck Sharp & Dohme Corp Szubsztituált azetidinon vegyületek alkalmazása szitoszterinémia kezelésére
AU2002237988B2 (en) 2001-01-30 2008-01-03 University Of Virginia Patent Foundation Agonists and antagonists of sphingosine-1-phosphate receptors
US6852738B2 (en) 2001-01-30 2005-02-08 Merck & Co., Inc. Acyl sulfamides for treatment of obesity, diabetes and lipid disorders
US7342021B2 (en) 2001-02-08 2008-03-11 Memory Pharmaceuticals Corp. Phosphodiesterase 4 inhibitors
AU2002251978B2 (en) 2001-02-09 2007-07-19 Merck & Co., Inc. 2-aryloxy-2-arylalkanoic acids for diabetes and lipid disorders
DE10110754A1 (de) 2001-03-07 2002-09-19 Bayer Ag Substituierte 2-Thio-3,5-dicyano-4-aryl-6-aminopyridine und ihre Verwendung
WO2002072101A1 (en) 2001-03-13 2002-09-19 Bristol-Myers Squibb Pharma Company A corticotropin releasing factor receptor ligand, its enantiomer and pharmaceutically acceptable salts
WO2002079131A1 (en) 2001-03-29 2002-10-10 Kansai Research Institute, Inc. Optically active compound and photosensitive resin composition
WO2002081454A1 (en) 2001-04-09 2002-10-17 Dr. Reddy's Laboratories Ltd. Derivatives of aryl acids, their use in medicine, process for their preparation and pharmaceutical compositions containing them
US6815456B2 (en) 2001-04-20 2004-11-09 Wyeth Heterocyclyloxy-, -thioxy- and -aminobenzazole derivatives as 5-hydroxytryptamine-6 ligands
EP1391199B1 (en) 2001-05-10 2008-12-10 Ono Pharmaceutical Co., Ltd. Carboxylic acid derivatives and drugs containing the same as the active ingredient
ATE448210T1 (de) 2001-06-01 2009-11-15 Hoffmann La Roche Pyrimidin, triazin und pyrazinderivate als glutamatrezeptoren
HUP0402352A2 (hu) 2001-06-19 2005-02-28 Bristol-Myers Squibb Co. Foszfodiészteráz (PDE) 7 inhibitorként alkalmazható pirimidinszármazékok és ezeket tartalmazó gyógyszerkészítmények
US6825198B2 (en) 2001-06-21 2004-11-30 Pfizer Inc 5-HT receptor ligands and uses thereof
EP1406875B1 (en) 2001-06-26 2013-07-31 Bristol-Myers Squibb Company N-heterocyclic inhibitors of tnf-alpha expression
UA74912C2 (en) 2001-07-06 2006-02-15 Merck & Co Inc Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes
GB0117899D0 (en) 2001-07-23 2001-09-12 Astrazeneca Ab Chemical compounds
WO2003026661A1 (fr) 2001-09-14 2003-04-03 Yamanouchi Pharmaceutical Co., Ltd. Accelerateur de secretion de l'insuline et nouveau derive de pyrimidine
CA2461212C (en) 2001-09-27 2010-08-17 Kyorin Pharmaceutical Co., Ltd. Diaryl sulfide derivatives, salts thereof and immunosuppressive agents using the same
EP1438048A1 (en) 2001-10-18 2004-07-21 Boehringer Ingelheim Pharmaceuticals Inc. 1,4-disubstituted benzo-fused urea compounds as cytokine inhibitors
GB0229931D0 (en) 2002-12-21 2003-01-29 Astrazeneca Ab Therapeutic agents
SE0104334D0 (sv) 2001-12-19 2001-12-19 Astrazeneca Ab Therapeutic agents
AU2002351752A1 (en) 2001-12-29 2003-07-30 Novo Nordisk A/S Combined use of a glp-1 compound and another drug for treating dyslipidemia
WO2003057689A1 (en) 2002-01-02 2003-07-17 Fujisawa Pharmaceutical Co., Ltd. Aminopyrimidine compounds, processes for their preparation and pharmaceutical compositions containing them
US20070225351A1 (en) 2002-01-11 2007-09-27 Lippa Arnold S Methods and compositions for controlling body weight and appetite
WO2003061567A2 (en) 2002-01-18 2003-07-31 Merck & Co., Inc. Selective s1p1/edg1 receptor agonists
EP1467729A1 (en) 2002-01-18 2004-10-20 The Genetics Company Inc. Beta-secretase inhibitors
WO2003062252A1 (en) 2002-01-18 2003-07-31 Merck & Co., Inc. Edg receptor agonists
GB0201850D0 (en) 2002-01-26 2002-03-13 Astrazeneca Ab Therapeutic treatment
EP1482895A4 (en) 2002-03-01 2005-04-27 Merck & Co Inc AMINO ALKYL PHOSPHONATES AND RELATED COMPOUNDS AS EDG RECEPTOR AGONISTS
AU2003218056A1 (en) 2002-03-01 2003-09-16 Merck & Co., Inc. Aminoalkylphosphonates and related compounds as edg receptor agonists
AU2003228283A1 (en) 2002-03-07 2003-09-22 X-Ceptor Therapeutics, Inc. Quinazolinone modulators of nuclear receptors
US7731985B2 (en) 2002-03-15 2010-06-08 Ciba Specialty Chemicals Corporation 4-aminopyrimidines and their use for the antimicrobial treatment of surfaces
TW200810743A (en) 2002-03-22 2008-03-01 Novartis Ag Combination of organic compounds
AU2003225027A1 (en) 2002-04-16 2003-11-03 Merck And Co., Inc. Combination therapy using a ppar alpha/gamma agonist
EP1499598A1 (en) 2002-04-18 2005-01-26 Ucb, S.A. Chemical compounds with dual activity, processes for their preparation and pharmaceutical compositions
DE10219435A1 (de) 2002-05-02 2003-11-13 Bayer Cropscience Ag Substituierte Pyrazolo-pyrimidin-4-one
WO2003094845A2 (en) 2002-05-08 2003-11-20 Bristol-Myers Squibb Company Pyridine-based thyroid receptor ligands
US7057046B2 (en) 2002-05-20 2006-06-06 Bristol-Myers Squibb Company Lactam glycogen phosphorylase inhibitors and method of use
AR040241A1 (es) 2002-06-10 2005-03-23 Merck & Co Inc Inhibidores de la 11-beta-hidroxiesteroide deshidrogrenasa 1 para el tratamiento de la diabetes obesidad y dislipidemia
JP2005531606A (ja) 2002-06-10 2005-10-20 エラン ファーマ インターナショナル，リミティド ナノ粒子ステロール製剤およびステロールの組合せ
EP1511467A1 (en) 2002-06-10 2005-03-09 Elan Pharma International Limited Nanoparticulate polycosanol formulations and novel polycosanol combinations
CA2488499C (en) 2002-06-10 2013-03-19 Elan Pharma International Ltd. Nanoparticulate formulations comprising hmg coa reductase inhibitor derivatives ("statins"),combinations thereof as well as manufacturing of these pharmaceutical compositions
EP1549336B1 (en) 2002-06-14 2011-01-05 Amylin Pharmaceuticals, Inc. Prevention and/or treatment of ulcerative colitis using pyy or pyy[3-36]
DE10226943A1 (de) 2002-06-17 2004-01-08 Bayer Ag Phenylaminopyrimidine und ihre Verwendung
AU2003276043A1 (en) 2002-06-17 2003-12-31 Merck & Co., Inc. 1-((5-aryl-1,2,4-oxadiazol-3-yl)benzyl)azetidine-3-carboxylates and 1-((5-aryl-1,2,4-oxadiazol-3-yl)benzyl)pyrrolidine-3-carboxylates as edg receptor agonists
GB0214254D0 (en) 2002-06-20 2002-07-31 Glaxo Group Ltd Chemical compounds
SE0201976D0 (sv) 2002-06-24 2002-06-24 Astrazeneca Ab Novel compounds
SE0201980D0 (sv) 2002-06-24 2002-06-24 Astrazeneca Ab Novel compounds
EP1531832B1 (en) 2002-06-28 2009-04-15 Glykos Finland Oy Therapeutic compositions for use in prophylaxis or treatment of diarrheas
US7071210B2 (en) 2002-07-02 2006-07-04 Pfizer Inc. CETP inhibitors in combination with antihypertensive agents and uses thereof
US20040053842A1 (en) 2002-07-02 2004-03-18 Pfizer Inc. Methods of treatment with CETP inhibitors and antihypertensive agents
EP1541563A4 (en) 2002-07-10 2007-11-07 Ono Pharmaceutical Co ANTAGONIST OF CCR4 AND CORRESPONDING MEDICINAL USE
EP1534389A2 (en) 2002-07-23 2005-06-01 SmithKline Beecham Corporation Pyrazolopyrimidines as kinase inhibitors
WO2004009602A1 (en) 2002-07-23 2004-01-29 Smithkline Beecham Corporation Pyrazolopyrimidines as kinase inhibitors
EP1523314A2 (en) 2002-07-23 2005-04-20 SmithKline Beecham Corporation Pyrazolopyrimidines as protein kinase inhibitors
AU2003258542A1 (en) 2002-07-29 2004-02-23 Axxima Pharmaceuticals Ag Method for isolating atp binding proteins by means of immobolized protein inhibitors
AU2003259296A1 (en) 2002-07-30 2004-02-16 University Of Virginia Patent Foundation Compounds active in spinigosine 1-phosphate signaling
CA2491733A1 (en) 2002-07-30 2004-02-05 Merck & Co., Inc. Ppar alpha selective compounds for the treatment of dyslipidemia and other lipid disorders
US7297715B2 (en) 2002-07-30 2007-11-20 Merck & Co., Inc. PPAR alpha selective compounds for the treatment of dyslipidemia and other lipid disorders
JP2004067575A (ja) 2002-08-06 2004-03-04 Yaizu Suisankagaku Industry Co Ltd 糖尿病治療薬効果促進剤
AR041191A1 (es) 2002-08-08 2005-05-04 Amgen Inc Ligandos del receptor vanilloide y su uso en tratamientos
DE10237722A1 (de) 2002-08-17 2004-08-19 Aventis Pharma Deutschland Gmbh Indol- oder Benzimidazolderivate zur Modulation der IKappaB-Kinase
US20060167045A1 (en) 2002-08-21 2006-07-27 Joanne Waldstreicher Combination therapy using a dual ppar alpha/gamma agonist and an angiotensin II type I receptor antagonist
HRP20050181A2 (en) 2002-08-29 2006-03-31 Merck & Co. Inc. Indoles having anti-diabetic activity
US7393960B2 (en) 2002-08-29 2008-07-01 Merck & Co., Inc. Indoles having anti-diabetic activity
WO2004024943A1 (ja) 2002-09-11 2004-03-25 Yamanouchi Pharmaceutical Co., Ltd. インスリン含量増加剤スクリーニング方法
JP2006510597A (ja) 2002-09-27 2006-03-30 メルク　エンド　カムパニー　インコーポレーテッド 置換ピリミジン類
US7067658B2 (en) 2002-09-30 2006-06-27 Bristol-Myers Squibb Company Pyridino and pyrimidino pyrazinones
AU2003282679A1 (en) 2002-10-04 2004-05-04 Arena Pharmaceuticals, Inc. Hydroxypyrazoles for use against metabolic-related disorders
AU2003284111A1 (en) 2002-10-09 2004-05-04 Genaissance Pharmaceuticals, Inc. Itgb3 gene haplotypes and atorvastatin dose effects on hdl cholesterol
JP2006504755A (ja) 2002-10-15 2006-02-09 スミスクライン ビーチャム コーポレーション Ｇｓｋ−３阻害薬としてのピリダジン化合物
US7129239B2 (en) 2002-10-28 2006-10-31 Pfizer Inc. Purine compounds and uses thereof
WO2004041164A2 (en) 2002-10-30 2004-05-21 Merck & Co., Inc. Kinase inhibitors
US7960369B2 (en) 2002-11-08 2011-06-14 Takeda Pharmaceutical Company Limited Receptor function regulator
US7098235B2 (en) 2002-11-14 2006-08-29 Bristol-Myers Squibb Co. Triglyceride and triglyceride-like prodrugs of glycogen phosphorylase inhibiting compounds
US20040110241A1 (en) 2002-12-06 2004-06-10 Segal Mark S. Materials and methods for monitoring vascular endothelial function
EP1581509B1 (en) 2002-12-20 2011-01-19 Merck Sharp & Dohme Corp. 1-(amino)indanes as edg receptor agonists
WO2004058727A1 (en) 2002-12-20 2004-07-15 Bayer Pharmaceuticals Corporation Substituted 3,5-dihydro-4h-imidazol-4-ones for the treatment of obesity
CA2510793A1 (en) 2002-12-20 2004-07-15 Bayer Pharmaceuticals Corporation Indane acetic acid derivatives and their use as pharmaceutical agents, intermediates, and method of preparation
JO2397B1 (en) 2002-12-20 2007-06-17 ميرك شارب اند دوم كوربوريشن Terazol derivatives as beta-hydroxy steroid dihydrogenase-1 inhibitors
GB0230021D0 (en) 2002-12-23 2003-01-29 Syngenta Ltd Fungicides
GB0230020D0 (en) 2002-12-23 2003-01-29 Syngenta Ltd Fungicides
DE602004009295T2 (de) 2003-01-14 2008-07-03 Arena Pharmaceuticals, Inc., San Diego 1,2,3-trisubstituierte aryl- und heteroarylderivate als modulatoren des metabolismus zur vorbeugung und behandlung von metabolismus-bedingten krankheiten wie diabetes oder hyperglykämie
ATE359782T1 (de) 2003-01-16 2007-05-15 Sb Pharmco Inc Heteroaryl-substituierte pyrrol(2, 3- b)pyridin- derivate als crf-rezeptor-antagonisten
CA2512879A1 (en) 2003-01-17 2004-08-12 Soumya P. Sahoo N-cyclohexylaminocarbonyl benzenesulfonamide derivatives
GB0301259D0 (en) 2003-01-20 2003-02-19 Novartis Ag Organic compounds
US7256206B2 (en) 2003-02-11 2007-08-14 Irm Llc Bicyclic compounds and compositions
TW200418829A (en) 2003-02-14 2004-10-01 Avanir Pharmaceutics Inhibitors of macrophage migration inhibitory factor and methods for identifying the same
CN100344638C (zh) 2003-02-18 2007-10-24 杏林制药株式会社 氨基膦酸衍生物、其加成盐以及s1p受体调节剂
JP2006518763A (ja) 2003-02-24 2006-08-17 アリーナ ファーマシューティカルズ， インコーポレイテッド グルコース代謝のモジュレーターとしてのフェニル−およびピリジルピペリジン誘導体
JP2004269468A (ja) 2003-03-12 2004-09-30 Yamanouchi Pharmaceut Co Ltd ピリミジン誘導体又はその塩
JP2004269469A (ja) 2003-03-12 2004-09-30 Yamanouchi Pharmaceut Co Ltd ピリミジン誘導体又はその塩
OA13153A (en) 2003-03-28 2006-12-13 Pfizer Prod Inc 1,2,4-substituted 1,2,3,4-tetrahydro-and 1,2 dihydro-quinoline and 1,2,3,4-tetrahydroquinoxaline derivatives as CETP inhibitors for the treatment of atherosclerosis and obesity.
CA2523677A1 (en) 2003-04-30 2004-11-11 Novartis Ag Aminopropanol derivatives as sphingosine-1-phosphate receptor modulators
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
ATE547395T1 (de) 2003-04-30 2012-03-15 Novartis Pharma Gmbh Aminopropanol-derivate als modulatoren des sphingosin-1-phosphat-rezeptors
TWI494102B (zh) 2003-05-02 2015-08-01 Japan Tobacco Inc 包含ｓ-〔２（〔〔１-（２-乙基丁基）環己基〕羰基〕胺基）苯基〕２-甲基丙烷硫酯及ｈｍｇ輔酶ａ還原酶抑制劑之組合
DE60333546D1 (de) 2003-05-06 2010-09-09 Univ Palackeho PyrazoloÄ4,3-DÜpyrimidines, verfahren zur ihre herstellung und deren verwendung
US7083933B1 (en) 2003-05-09 2006-08-01 Prosidion Limited Methods for identification of modulators of OSGPR116 activity
SE0301368D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Chemical compounds
US20060252741A1 (en) 2003-05-15 2006-11-09 Colandrea Vincent J 3-(2-amino-1-azacyclyl)-5-aryl-1,2,4-oxadiazoles as s1p receptor agonists
WO2004104205A2 (en) 2003-05-16 2004-12-02 Merck & Co., Inc. Enzymatic preparation of chiral indole esters
BRPI0410454A (pt) 2003-05-19 2006-06-13 Irm Llc composições e compostos imunossupressores
JP4728962B2 (ja) 2003-05-19 2011-07-20 アイアールエム・リミテッド・ライアビリティ・カンパニー 免疫抑制化合物および組成物
MY150088A (en) 2003-05-19 2013-11-29 Irm Llc Immunosuppressant compounds and compositions
PE20050158A1 (es) 2003-05-19 2005-05-12 Irm Llc Compuestos inmunosupresores y composiciones
US6987118B2 (en) 2003-05-21 2006-01-17 Pfizer Inc. Tetrahydroisoquinoline derivatives as PPAR-alpha activators
US20060160834A1 (en) 2003-06-06 2006-07-20 Fong Tung M Combination therapy for the treatment of hypertension
AU2003902882A0 (en) 2003-06-10 2003-06-26 Fujisawa Pharmaceutical Co., Ltd. Piperidyl derivatives
GB0313612D0 (en) 2003-06-12 2003-07-16 Novartis Ag Organic compounds
AR045047A1 (es) 2003-07-11 2005-10-12 Arena Pharm Inc Derivados arilo y heteroarilo trisustituidos como moduladores del metabolismo y de la profilaxis y tratamiento de desordenes relacionados con los mismos
EP2292620A3 (en) 2003-07-14 2011-06-22 Arena Pharmaceuticals, Inc. Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prohylaxis and treatment of disorders related thereto
WO2005012221A1 (ja) 2003-08-04 2005-02-10 Ono Pharmaceutical Co., Ltd. ジフェニルエーテル化合物、その製造方法および用途
DK2287156T3 (da) 2003-08-15 2013-08-26 Novartis Ag 2,4-Di(phenylamino)-pyrimidiner egnede i behandling af neoplastiske sygdomme, inflammatoriske lidelser og lidelser i immunsystemet
ATE449069T1 (de) 2003-08-28 2009-12-15 Novartis Pharma Gmbh Aminopropanolderivate
CN101407471A (zh) 2003-08-29 2009-04-15 小野药品工业株式会社 能够结合s1p受体的化合物及其药物用途
JP2007504230A (ja) 2003-09-02 2007-03-01 メルク　エンド　カムパニー　インコーポレーテッド ジペプチジルペプチダーゼ−ｉｖ阻害剤のリン酸塩の新規結晶性形態
WO2005023762A1 (en) 2003-09-04 2005-03-17 Abbott Laboratories Pyrrolidine-2-carbonitrile derivatives and their use as inhibitors of dipeptidyl peptidase-iv (dpp-iv)
PE20050374A1 (es) 2003-09-05 2005-05-30 Vertex Pharma Inhibidores de proteasas de serina, en particular proteasa ns3-ns4a del vhc
EP1661889A4 (en) 2003-09-05 2009-08-05 Ono Pharmaceutical Co ANTAGONIST OF THE CHEMOKINE RECEPTOR AND ITS USE FOR MEDICAL PURPOSES
US7790734B2 (en) 2003-09-08 2010-09-07 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
EP1697342A2 (en) 2003-09-08 2006-09-06 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
AR046330A1 (es) 2003-09-09 2005-12-07 Japan Tobacco Inc Inhibidor de dipeptidilpeptidasa iv
EP1667524A4 (en) 2003-09-23 2009-01-14 Merck & Co Inc NEW CRYSTALLINE FORM OF A PHOSPHORIC ACID SALT OF A DIPEPTIDYLPEPTIDASE IV INHIBITOR
US7692017B2 (en) 2003-09-23 2010-04-06 Merck Sharp & Dohme Corp. Quinoline potassium channel inhibitors
CN1859908A (zh) 2003-10-01 2006-11-08 默克公司 作为s1p受体激动剂的3,5－芳基、杂芳基或环烷基取代的－1,2,4－噁二唑类化合物
WO2005033099A2 (en) 2003-10-03 2005-04-14 Glenmark Pharmaceuticals Ltd. Novel dipeptidyl peptidase iv inhibitors; processes for their preparation and compositions thereof
US20060089335A1 (en) 2003-10-14 2006-04-27 Guosong Liu Compositions and methods for enhancing cognitive function and synaptic plasticity
GB0324236D0 (en) 2003-10-16 2003-11-19 Astrazeneca Ab Chemical compounds
TW200523252A (en) 2003-10-31 2005-07-16 Takeda Pharmaceutical Pyridine compounds
WO2005041899A2 (en) 2003-11-03 2005-05-12 University Of Virginia Patent Foundation Orally available sphingosine 1-phosphate receptor agonists and antagonists
WO2005044780A1 (ja) 2003-11-10 2005-05-19 Kyorin Pharmaceutical Co., Ltd. アミノカルボン酸誘導体とその付加塩及びｓ１ｐ受容体調節剤
WO2005046603A2 (en) 2003-11-10 2005-05-26 Synta Pharmaceuticals, Corp. Pyridine compounds
AR046778A1 (es) 2003-11-12 2005-12-21 Phenomix Corp Compuestos heterociclicos de acido boronico. metodos de obtencion y composiciones farmaceuticas.
MY141220A (en) 2003-11-17 2010-03-31 Astrazeneca Ab Pyrazole derivatives as inhibitors of receptor tyrosine kinases
WO2005058315A1 (en) 2003-12-12 2005-06-30 Ribapharm, Inc. Novel heterocyclic compounds as ikk2 inhibitors with anti-hbv activity
WO2005058849A1 (en) 2003-12-15 2005-06-30 Glenmark Pharmaceuticals Ltd. New dipeptidyl peptidase in inhibitors; process for their preparation and compositions containing them
CA2547198A1 (en) 2003-12-17 2005-06-30 Merck & Co., Inc. (3,4-disubstituted)propanoic carboxylates as s1p (edg) receptor agonists
ATE528276T1 (de) 2003-12-19 2011-10-15 Ono Pharmaceutical Co Lysophosphatidylsäurerezeptor-antagonistische verbindungen und ihre anwendungen
GB0329498D0 (en) 2003-12-19 2004-01-28 Novartis Ag Organic compounds
DE10360835A1 (de) 2003-12-23 2005-07-21 Boehringer Ingelheim Pharma Gmbh & Co. Kg Bicyclische Imidazolverbindungen, deren Herstellung und deren Verwendung als Arzneimittel
CN1898235A (zh) 2003-12-24 2007-01-17 普罗西迪恩有限公司 作为gpcr受体激动剂的杂环衍生物
WO2005072530A1 (en) 2004-01-16 2005-08-11 Merck & Co., Inc. Novel crystalline salts of a dipeptidyl peptidase-iv inhibitor
GB0401332D0 (en) 2004-01-21 2004-02-25 Novartis Ag Organic compounds
WO2005075426A1 (en) 2004-02-03 2005-08-18 Glenmark Pharmaceuticals Ltd. Novel dipeptidyl peptidase iv inhibitors; processes for their preparation and compositions thereof
US7534798B2 (en) 2004-02-11 2009-05-19 Amgen Inc. Vanilloid receptor ligands and their use in treatments
TW200530236A (en) 2004-02-23 2005-09-16 Chugai Pharmaceutical Co Ltd Heteroaryl phenylurea
EP1718604A4 (en) 2004-02-24 2008-02-13 Irm Llc COMPOUNDS AND COMPOSITIONS OF IMMUNOSUPPRESSANTS
TW200538433A (en) 2004-02-24 2005-12-01 Irm Llc Immunosuppressant compounds and compositiions
JP2005272453A (ja) 2004-02-24 2005-10-06 Sankyo Co Ltd アミノアルコール化合物
CN1934094A (zh) 2004-03-05 2007-03-21 万有制药株式会社 二芳基取代杂环5元环衍生物
GB0405289D0 (en) 2004-03-09 2004-04-21 Novartis Ag Organic compounds
GB0405933D0 (en) 2004-03-16 2004-04-21 Glaxo Group Ltd Compounds
AU2005230897B2 (en) 2004-04-02 2011-03-03 Merck Sharp & Dohme Corp. Asymmetric hydrogenation process useful for the preparation of cycloalkanoindole derivatives
CN1968954A (zh) 2004-04-12 2007-05-23 三共株式会社 噻吩并吡啶衍生物
JP5213229B2 (ja) 2004-04-23 2013-06-19 エグゼリクシス， インコーポレイテッド キナーゼ調節因子および使用方法
ATE415397T1 (de) 2004-06-04 2008-12-15 Arena Pharm Inc Substituierte aryl- und heteroarylderivate als modulatoren des stoffwechsels und für die prophylaxe und behandlung von damit in zusammenhang stehenden erkrankungen
WO2005123677A1 (en) 2004-06-16 2005-12-29 Actelion Pharmaceuticals Ltd 4-carbonyl substituted 1,1,2-trimethyl-1a,4,5,5a-tetrahydro-1h-4-aza-cyclopropa'a!pentalene derivatives as agonists for the g-protein-coupled receptor s1p1/edg1 and immunosuppressive agents
EP1760071A4 (en) 2004-06-23 2008-03-05 Ono Pharmaceutical Co COMPOUND WITH S1P RECEPTOR BINDING ABILITY AND USE THEREOF
EP1772145B1 (en) 2004-07-16 2011-03-23 Kyorin Pharmaceutical Co., Ltd. Method of effectively using medicine and method concerning prevention of side effect
JP2007284350A (ja) 2004-07-27 2007-11-01 Takeda Chem Ind Ltd 糖尿病治療剤
TW200611687A (en) 2004-07-29 2006-04-16 Sankyo Co Pharmaceutical compositions used for immunosuppressant
WO2006010379A1 (en) 2004-07-29 2006-02-02 Actelion Pharmaceuticals Ltd. Novel thiophene derivatives as immunosuppressive agents
EP1798226A4 (en) 2004-08-04 2009-06-17 Taisho Pharmaceutical Co Ltd TRAIZOL DERIVATIVE
US20060223866A1 (en) 2004-08-13 2006-10-05 Praecis Pharmaceuticals, Inc. Methods and compositions for modulating sphingosine-1-phosphate (S1P) receptor activity
JP2008509931A (ja) 2004-08-13 2008-04-03 プレーシス ファーマスーティカルズ インコーポレイテッド スフィンゴシン−１−ホスフェート（ｓ１ｐ）レセプター活性を調節するための方法および組成物
CN101090724A (zh) 2004-09-20 2007-12-19 泽农医药公司 用于抑制人硬脂酰CoA去饱和酶的吡啶衍生物
US7250441B2 (en) 2004-09-23 2007-07-31 Wyeth Carbazole and cyclopentaindole derivatives to treat infection with Hepatitis C virus
US7884104B2 (en) 2004-10-01 2011-02-08 Merck Sharp & Dohme Corp. Aminopiperidines as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
EP1806347A4 (en) 2004-10-08 2009-07-01 Astellas Pharma Inc PYRIMIDINE DERIVATIVES FUSED WITH AN AROMATIC RING
BRPI0515992A (pt) 2004-10-12 2008-08-19 Forbes Medi Tech Res Inc compostos e métodos para o tratamento de resistência à insulina e cardiomiopatia
TW200621257A (en) 2004-10-20 2006-07-01 Astellas Pharma Inc Pyrimidine derivative fused with nonaromatic ring
WO2006047195A2 (en) 2004-10-22 2006-05-04 Merck & Co., Inc. 2-(aryl)azacyclylmethyl carboxylates, sulfonates, phosphonates, phosphinates and heterocycles as s1p receptor agonists
DE602004014277D1 (de) 2004-10-22 2008-07-17 Bioprojet Soc Civ Neue Dicarbonsäurederivate
AR051596A1 (es) 2004-10-26 2007-01-24 Irm Llc Compuestos heterociclicos condensados nitrogenados como inhibidores de la actividad del receptor canabinoide 1; composiciones farmaceuticas que los contienen y su empleo en la preparacion de medicamentos para el tratamiento de trastornos alimentarios
JP5785354B2 (ja) 2004-11-03 2015-09-30 アリーナ ファーマシューティカルズ， インコーポレイテッド インスリン関連障害の処置のためのｇｐｒ４１およびその調節因子
GB0425035D0 (en) 2004-11-12 2004-12-15 Novartis Ag Organic compounds
AU2005307718A1 (en) 2004-11-18 2006-05-26 The Institutes For Pharmaceutical Discovery, Llc Heterocycle substituted carboxylic acids for the treatment of diabetes
WO2006057448A1 (ja) 2004-11-26 2006-06-01 Takeda Pharmaceutical Company Limited アリールアルカン酸誘導体
US20060160785A1 (en) 2004-12-03 2006-07-20 Judith Aronhime Ezetimibe polymorphs
JP2008522977A (ja) 2004-12-06 2008-07-03 ユニバーシティ オブ バージニア パテント ファンデーション スフィンゴシン＝１−リン酸のアリールアミドアナログ
TW200633720A (en) 2004-12-13 2006-10-01 Sankyo Co Medicinal composition for diabetic
EP2371811B1 (en) 2004-12-13 2014-10-08 Ono Pharmaceutical Co., Ltd. Azetidinecarboxylic acid derivative and medicinal use thereof
BRPI0516407A (pt) 2004-12-24 2008-09-02 Prosidion Ltd agonistas de receptor acoplado à proteìna g (gpr116) e uso destes para o tratamento de obesidade e diabetes
EP1838706A1 (en) 2004-12-24 2007-10-03 Prosidion Limited G-protein coupled receptor agonists
GB0428514D0 (en) 2004-12-31 2005-02-09 Prosidion Ltd Compounds
DOP2006000008A (es) 2005-01-10 2006-08-31 Arena Pharm Inc Terapia combinada para el tratamiento de la diabetes y afecciones relacionadas y para el tratamiento de afecciones que mejoran mediante un incremento de la concentración sanguínea de glp-1
DOP2006000010A (es) 2005-01-10 2006-07-31 Arena Pharm Inc Procedimiento para preparar eteres aromáticos
MY148521A (en) 2005-01-10 2013-04-30 Arena Pharm Inc Substituted pyridinyl and pyrimidinyl derivatives as modulators of metabolism and the treatment of disorders related thereto
DOP2006000009A (es) 2005-01-13 2006-08-15 Arena Pharm Inc Procedimiento para preparar eteres de pirazolo [3,4-d] pirimidina
CA2595205A1 (en) 2005-01-19 2006-07-27 Neurogen Corporation Heteroaryl substituted piperazinyl-pyridine analogues
JP5798282B2 (ja) 2005-01-25 2015-10-21 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ メソゲン性化合物、液晶媒体および液晶ディスプレイ
EP1685841A1 (en) 2005-01-31 2006-08-02 Bayer Health Care Aktiengesellschaft Prevention and treatment of thromboembolic disorders
US7754703B2 (en) 2005-02-14 2010-07-13 University Of Virginia Patent Foundation Cycloalkane-containing sphingosine 1-phosphate agonists
CN101146529B (zh) 2005-03-23 2012-08-29 埃科特莱茵药品有限公司 新颖噻吩衍生物作为鞘氨醇-1-磷酸酯-1受体激动剂
EP1863787B1 (en) 2005-03-23 2011-05-25 Actelion Pharmaceuticals Ltd. Hydogrenated benzo[c]thiophene derivatives as immunomodulators
US7846964B2 (en) 2005-03-23 2010-12-07 Actelion Pharmaceuticals Ltd. Thiophene derivatives as spingosine-1-phosphate-1 receptor agonists
EP1893591A1 (en) 2005-06-08 2008-03-05 Novartis AG POLYCYCLIC OXADIAZOLES OR I SOXAZOLES AND THEIR USE AS SlP RECEPTOR LIGANDS
CA2611446A1 (en) 2005-06-09 2006-12-14 Banyu Pharmaceutical Co., Ltd. Npy y2 agonist for use as therapeutic agent for disease accompanied by diarrhea
CA2612661A1 (en) 2005-06-24 2006-12-28 Actelion Pharmaceuticals Ltd. Novel thiophene derivatives
TWI418350B (zh) 2005-06-24 2013-12-11 Sankyo Co 含有ｐｐａｒ調節劑之醫藥組成物的用途
JP2008545010A (ja) 2005-06-30 2008-12-11 プロシディオン・リミテッド Ｇタンパク質共役受容体アゴニスト
MX2007016066A (es) 2005-07-01 2008-03-10 Irm Llc Derivados de bencimidazol sustituidos por pirimidina como inhibidores de cinasa de proteina.
US20070060573A1 (en) 2005-08-10 2007-03-15 Lars Wortmann Acyltryptophanols
WO2007024922A1 (en) 2005-08-23 2007-03-01 Irm Llc Immunosuppressant compounds and compositions
DE602006006461D1 (de) 2005-09-16 2009-06-04 Arena Pharm Inc Stoffwechselmodulatoren und behandlung damit verbundener erkrankungen
TW200745055A (en) 2005-09-23 2007-12-16 Organon Nv 4-Phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives
WO2007037196A1 (ja) 2005-09-29 2007-04-05 Yamamoto Chemicals, Inc. インドリン系化合物及びその製造方法
KR101297302B1 (ko) 2005-10-07 2013-08-19 교린 세이야꾸 가부시키 가이샤 2-아미노-1,3-프로판디올 유도체를 유효성분으로 하는간장질환 치료제 및 간장질환 치료방법
JP2009520688A (ja) 2005-11-23 2009-05-28 エピックス デラウェア， インコーポレイテッド Ｓ１ｐ受容体調節化合物およびそれらの使用
AR057894A1 (es) 2005-11-23 2007-12-26 Actelion Pharmaceuticals Ltd Derivados de tiofeno
WO2007089335A2 (en) 2005-12-29 2007-08-09 Lexicon Pharmaceutical Inc. Multicyclic amino acid derivatives and methods of their use
TWI404706B (zh) 2006-01-11 2013-08-11 Actelion Pharmaceuticals Ltd 新穎噻吩衍生物
TW200736234A (en) 2006-01-17 2007-10-01 Astrazeneca Ab Chemical compounds
AU2006335967B2 (en) 2006-01-19 2012-01-19 Orchid Chemicals & Pharmaceuticals Limited Novel heterocycles
JP5063615B2 (ja) 2006-01-24 2012-10-31 アクテリオン ファーマシューティカルズ リミテッド 新規ピリジン誘導体
GB0601744D0 (en) 2006-01-27 2006-03-08 Novartis Ag Organic compounds
TWI389683B (zh) 2006-02-06 2013-03-21 Kyorin Seiyaku Kk A therapeutic agent for an inflammatory bowel disease or an inflammatory bowel disease treatment using a 2-amino-1,3-propanediol derivative as an active ingredient
WO2007092638A1 (en) 2006-02-09 2007-08-16 University Of Virginia Patent Foundation Bicyclic sphingosine 1-phosphate analogs
TW200806611A (en) 2006-02-09 2008-02-01 Daiichi Seiyaku Co Novel amidopropionic acid derivatives and medicine containing the same
US20070191371A1 (en) 2006-02-14 2007-08-16 Kalypsys, Inc. Heterocyclic modulators of ppar
CN101460458A (zh) 2006-02-15 2009-06-17 阿勒根公司 具有1－磷酸－鞘氨醇(s1p)受体拮抗剂生物活性的带芳基或者杂芳基基团的吲哚－3－羧酸的酰胺、酯、硫代酰胺和硫羟酸酯化合物
AU2007214434B2 (en) 2006-02-15 2012-06-14 Allergan, Inc. Indole-3-carboxylic acid amide, ester, thioamide and thiol ester compounds bearing aryl or heteroaryl groups having sphingosine-1-phosphate (S1P) receptor antagonist biological activity
CN101384566A (zh) 2006-02-21 2009-03-11 弗吉尼亚大学专利基金会 作为s1p受体激动剂的苯基-环烷基和苯基-杂环衍生物
US7649098B2 (en) 2006-02-24 2010-01-19 Lexicon Pharmaceuticals, Inc. Imidazole-based compounds, compositions comprising them and methods of their use
JP2009530281A (ja) 2006-03-14 2009-08-27 アムジエン・インコーポレーテツド 代謝障害の治療に有用である二環式カルボン酸誘導体
TW200806633A (en) 2006-03-21 2008-02-01 Epix Pharm Inc S1P receptor modulating compounds and use thereof
JP2007262009A (ja) 2006-03-29 2007-10-11 Dai Ichi Seiyaku Co Ltd ヘテロアリール低級カルボン酸誘導体
EP2003132B1 (en) 2006-04-03 2014-03-05 Astellas Pharma Inc. Oxadiazole derivatives as S1P1 agonists
AU2007238805B2 (en) 2006-04-11 2012-04-05 Arena Pharmaceuticals, Inc. Methods of using GPR119 receptor to identify compounds useful for increasing bone mass in an individual
PE20071221A1 (es) 2006-04-11 2007-12-14 Arena Pharm Inc Agonistas del receptor gpr119 en metodos para aumentar la masa osea y para tratar la osteoporosis y otras afecciones caracterizadas por masa osea baja, y la terapia combinada relacionada a estos agonistas
GB0607389D0 (en) 2006-04-12 2006-05-24 Novartis Ag Organic compounds
WO2007129473A1 (ja) 2006-05-09 2007-11-15 Daiichi Sankyo Company, Limited 二環性アリール誘導体
BRPI0711358A2 (pt) 2006-05-09 2011-09-27 Pfizer Prod Inc derivados do ácido cicloalquilamino e suas composições farmacêuticas
US20090324581A1 (en) 2006-05-09 2009-12-31 Daiichi Sankyo Company Limited Heteroarylamide lower carboxylic acid derivative
TW200811140A (en) 2006-07-06 2008-03-01 Arena Pharm Inc Modulators of metabolism and the treatment of disorders related thereto
TW200811147A (en) 2006-07-06 2008-03-01 Arena Pharm Inc Modulators of metabolism and the treatment of disorders related thereto
WO2008008887A2 (en) 2006-07-13 2008-01-17 Smithkline Beecham Corporation Gpr119 agonists for treating metabolic disorders
AR062156A1 (es) 2006-08-01 2008-10-22 Praecis Pharm Inc Compuestos agonistas y selectivos del receptor s1p-1
US20080070866A1 (en) 2006-08-01 2008-03-20 Praecis Pharmaceuticals Incorporated Chemical compounds
US20090318389A1 (en) 2006-08-04 2009-12-24 Praecis Pharmaceuticals Incorporated Agonists of the sphingosine-1 phosphate receptor
PL2058317T3 (pl) 2006-08-08 2014-03-31 Kyorin Seiyaku Kk Aminowa pochodna estru kwasu fosforowego i modulator receptora S1P zawierający ją jako składnik aktywny
WO2008024196A1 (en) 2006-08-24 2008-02-28 Praecis Pharmaceuticals Incorporated Chemical compounds
JP2009269819A (ja) 2006-08-25 2009-11-19 Asahi Kasei Pharma Kk アミン化合物
EP2059516A1 (en) 2006-08-30 2009-05-20 BIOVITRUM AB (publ) Pyridine compounds for treating gpr119 related disorders
TWI408139B (zh) 2006-09-07 2013-09-11 Actelion Pharmaceuticals Ltd 新穎噻吩衍生物
MY149853A (en) 2006-09-07 2013-10-31 Actelion Pharmaceuticals Ltd Pyridin-4-yl derivatives as immunomodulating agents
CA2662852A1 (en) 2006-09-07 2008-03-13 Allergan, Inc. Heteroaromatic compounds having sphingosine-1-phosphate (s1p) receptor agonist and/or antagonist biological activity
CA2662091A1 (en) 2006-09-08 2008-03-13 Novartis Ag N-biaryl (hetero) arylsulphonamide derivatives useful in the treatment of diseases mediated by lymphocytes interactions
KR20090051774A (ko) 2006-09-21 2009-05-22 액테리온 파마슈티칼 리미티드 페닐 유도체 및 면역조절제로서 이들의 용도
WO2008070692A2 (en) 2006-12-06 2008-06-12 Smithkline Beecham Corporation Bicyclic compounds and use as antidiabetics
CA2672059A1 (en) 2006-12-14 2008-06-26 Merck & Co., Inc. Acyl bipiperidinyl compounds, compositions containing such compounds and methods of treatment
EP2109364A4 (en) 2006-12-15 2010-04-14 Abbott Lab NOVEL OXADIAZONE COMPOUNDS
JO2701B1 (en) 2006-12-21 2013-03-03 جلاكسو جروب ليميتد Vehicles
GB0625648D0 (en) 2006-12-21 2007-01-31 Glaxo Group Ltd Compounds
UY30829A1 (es) 2006-12-21 2008-07-31 Abbott Lab Compuestos agonistas y antagonistas del receptor de esfinfosina-1-fosfato
CA2674946A1 (en) 2007-01-11 2008-07-24 Allergan, Inc. 6-substituted indole-3-carboxylic acid amide compounds having sphingosine-1-phosphate (s1p) receptor antagonist biological activity
WO2008091967A1 (en) 2007-01-26 2008-07-31 Smithkline Beecham Corporation Chemical compounds
WO2008097819A2 (en) 2007-02-05 2008-08-14 Smithkline Beecham Corporation Chemical compounds
DK2125797T3 (da) 2007-03-16 2014-02-10 Actelion Pharmaceuticals Ltd Aminopyridinderivater som s1p1/edg1-receptoragonister
MX2009010060A (es) 2007-03-21 2010-01-20 Epix Pharm Inc Compuestos moduladores del receptor de esfingosin-1-fosfato y uso de los mismos.
WO2008128832A1 (en) 2007-04-18 2008-10-30 Nicox S.A. Nitroderivatives of non-peptidic renin inhibitors for the treatment of cardiovascular, renal and chronic liver disease, inflammations and metabolic syndrome
CA2684385A1 (en) 2007-04-19 2008-10-30 Glaxo Group Limited Oxadiazole substituted indazole derivatives for use as sphingosine 1-phosphate (s1p) agonists
PE20090222A1 (es) 2007-05-04 2009-03-27 Bristol Myers Squibb Co Compuestos [6,6] y [6,7]-biciclicos como agonistas del receptor acoplado a la proteina g gpr119
EP2014653A1 (en) 2007-06-15 2009-01-14 Bioprojet Novel dicarboxylic acid derivatives as S1P1 receptor agonists
WO2009011850A2 (en) 2007-07-16 2009-01-22 Abbott Laboratories Novel therapeutic compounds
WO2009019506A1 (en) 2007-08-03 2009-02-12 Astrazeneca Ab Heterocyclyc sulfonamides having edg-1 antagonistic activity
WO2009019167A1 (en) 2007-08-08 2009-02-12 Merck Serono S.A. 6-amino-pyrimidine-4-carboxamide derivatives and related compounds which bind to the sphingosine 1-phosphate (s1p) receptor for the treatment of multiple sclerosis
EP2197873B1 (en) 2007-09-20 2014-07-16 Irm Llc Compounds and compositions as modulators of gpr119 activity
TW200930368A (en) 2007-11-15 2009-07-16 Astrazeneca Ab Bis-(sulfonylamino) derivatives in therapy
EP2225201A2 (en) 2007-11-28 2010-09-08 Synta Pharmaceuticals Corp. Polymorphs of n-malonyl-bis(n'-methyl-n'-thiobenzoylhydrazide)
ATE531711T1 (de) 2007-12-18 2011-11-15 Arena Pharm Inc Für die behandlung von autoimmunerkrankungen und entzündlichen erkrankungen geeignete tetrahydrocyclopentaäbüindol-3- ylcarbonsäurederivate
US20100292233A1 (en) 2008-01-25 2010-11-18 Arena Pharmaceuticals, Inc. Dihydro-1h-pyrrolo[1,2-a]indol-1-yl carboxylic acid derivatives which act as s1p1 agonists
AR070398A1 (es) 2008-02-22 2010-03-31 Gruenenthal Chemie Derivados sustituidos de indol
WO2009108924A2 (en) 2008-02-28 2009-09-03 Solar Roofing Systems, Inc. Photovoltaic roofing tile with fire suppression
KR101718639B1 (ko) 2008-03-17 2017-03-21 액테리온 파마슈티칼 리미티드 선별적 ｓ1ｐ₁ 수용체 작동약에 대한 투약 섭생
WO2009125434A2 (en) 2008-04-07 2009-10-15 Cadila Healthcare Limited Oxime derivatives
EP2271619A1 (en) 2008-04-07 2011-01-12 Irm Llc Compounds and compositions as modulators of gpr119 activity
EP2108960A1 (en) 2008-04-07 2009-10-14 Arena Pharmaceuticals, Inc. Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditons modulated by PYY
DK2291080T3 (en) 2008-05-14 2015-12-07 Scripps Research Inst Novel modulator of sphingosinphosphatreceptorer
WO2009151621A1 (en) 2008-06-13 2009-12-17 Arena Pharmaceuticals, Inc. Substituted (1, 2, 4-0xadiaz0l-3-yl) indolin-1-yl carboxylic acid derivatives useful as s1p1 agonists
WO2009151626A1 (en) 2008-06-13 2009-12-17 Arena Pharmaceuticals, Inc. Substituted (1, 2, 4-0xadiaz0l-3-yl) indolin-1-yl carboxylic acid derivatives useful as s1p1 agonists
US8415484B2 (en) * 2008-08-27 2013-04-09 Arena Pharmaceuticals, Inc. Substituted tricyclic acid derivatives as S1P1 receptor agonists useful in the treatment of autoimmune and inflammatory disorders
JP5657565B2 (ja) 2008-12-22 2015-01-21 ノバルティス アーゲー Ｓ１ｐ受容体アゴニストの投与レジメン
HRP20151190T1 (hr) 2008-12-22 2016-01-01 Novartis Ag Režim doziranja za fingolimod u lijeäśenju multiple skleroze
WO2010075273A1 (en) 2008-12-23 2010-07-01 Schering Corporation Bicyclic heterocycle derivatives and methods of use thereof
US8410122B2 (en) 2008-12-23 2013-04-02 Merck Sharp & Dohme Corp. Bicyclic heterocycle derivatives and methods of use thereof
WO2010074271A1 (ja) 2008-12-26 2010-07-01 武田薬品工業株式会社 糖尿病治療剤
WO2010084944A1 (ja) 2009-01-22 2010-07-29 田辺三菱製薬株式会社 新規ピロロ［２，３－ｄ］ピリミジン化合物
PE20120578A1 (es) 2009-02-10 2012-06-17 Abbott Lab Agonistas y antagonistas del receptor de s1p5, y metodos de uso de los mismos
WO2011005290A1 (en) 2009-06-23 2011-01-13 Arena Pharmaceuticals, Inc. Disubstituted oxadiazole derivatives useful in the treatment of autoimmune and inflammatory disorders
WO2011005295A1 (en) 2009-06-24 2011-01-13 Arena Pharmaceuticals, Inc. Modulators of the sphingosine-1-phosphate (s1p) receptor useful for the treatment of disorders related thereto
AR077642A1 (es) 2009-07-09 2011-09-14 Arena Pharm Inc Moduladores del metabolismo y el tratamiento de trastornos relacionados con el mismo
AR077638A1 (es) 2009-07-15 2011-09-14 Lilly Co Eli Compuesto de (metanosulfonil -piperidin )-( alcoxi-aril) -tetrahidro- piridina , composicion farmaceutica que lo comprende y su uso para preparar un medicamento util para el tratamiento de diabetes u obesidad
WO2011030139A1 (en) 2009-09-11 2011-03-17 Astrazeneca Ab 4- (pyrimidin-2-yl) -piperazine and 4- (pyrimidin-2-yl) -piperidine derivatives as gpr119 modulators
ES2759949T3 (es) 2009-10-29 2020-05-12 Bristol Myers Squibb Co Compuestos heterocíclicos tricíclicos
US8299059B2 (en) 2009-10-30 2012-10-30 Eli Lilly And Company Crystalline compound and a process for its preparation
US8440693B2 (en) 2009-12-22 2013-05-14 Novartis Ag Substituted isoquinolinones and quinazolinones
MTP4285B (en) 2009-12-30 2011-07-04 Medichem Sa A 1-(1h-1,2,3-triazol-1-yl)butan-2-ol derivative for pharmaceutical use, and the use of a 1-(1h-1, 2, 4- triazol-1yl) butan-2-ol derivative with substially undefined crystal shap for preparing said 1-(1h-1, 2, 4-triazol-1-yl0 butan-2-ol derivative
EP2542554B1 (en) 2010-03-03 2015-11-04 Arena Pharmaceuticals, Inc. Processes for the preparation of s1p1 receptor modulators and crystalline forms thereof
JP2013523819A (ja) 2010-04-06 2013-06-17 アリーナ ファーマシューティカルズ， インコーポレイテッド Ｇｐｒ１１９レセプターのモジュレーターおよびそれに関連する障害の処置
WO2012015758A2 (en) 2010-07-30 2012-02-02 Saint Louis University Methods of treating pain
PH12013500547A1 (en) 2010-09-22 2013-06-10 Arena Pharm Inc Modulators of the gpr119 receptor and the treatment of disorders related thereto
PT2672823T (pt) 2011-02-07 2016-11-21 Biogen Ma Inc Agentes que modulam s1p
US20140018371A1 (en) 2011-04-01 2014-01-16 Arena Pharmaceuticals, Inc. Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
WO2012145361A1 (en) 2011-04-19 2012-10-26 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2012145603A1 (en) 2011-04-22 2012-10-26 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2012145604A1 (en) 2011-04-22 2012-10-26 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2012170702A1 (en) 2011-06-08 2012-12-13 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2013055910A1 (en) 2011-10-12 2013-04-18 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
JP2015505564A (ja) 2012-02-03 2015-02-23 テバ ファーマシューティカル インダストリーズ リミティド 第一選択の抗ＴＮＥα療法に失敗したクローン病患者を治療するためのラキニモドの使用
US20160038506A1 (en) 2012-02-14 2016-02-11 Repros Therapeutics Inc. Selective Estrogen Receptor Modulators With Short Half-Lives and Uses Thereof
US8962888B2 (en) 2012-12-03 2015-02-24 Physical Sciences, Inc. Forming spherical crystal habit
JP5589110B1 (ja) 2013-03-08 2014-09-10 株式会社ポーラファルマ 晶癖を有する結晶及び該結晶を有効成分として含有する医薬組成物
ES2995737T3 (en) 2015-01-06 2025-02-11 Arena Pharm Inc Compound for use in treating conditions related to the s1p1 receptor
MA42807A (fr) 2015-06-22 2018-07-25 Arena Pharm Inc Sel l-arginine cristallin d'acide (r)-2-(7-(4-cyclopentyl-3-(trifluorométhyl)benzyloxy)-1,2,3,4-tétrahydrocyclo-penta[b]indol-3-yl)acétique (composé 1) pour une utilisation dans des troubles associés au récepteur de s1p1
WO2018151873A1 (en) 2017-02-16 2018-08-23 Arena Pharmaceuticals, Inc. Compounds and methods for treatment of primary biliary cholangitis
CA3053416A1 (en) 2017-02-16 2018-08-23 Arena Pharmaceuticals, Inc. Compounds and methods for treatment of inflammatory bowel disease with extra-intestinal manifestations
EP3801459B1 (en) 2018-06-06 2024-08-07 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the s1p1 receptor
US20210386706A1 (en) 2018-10-03 2021-12-16 Arena Pharmaceuticals, Inc. Methods for the treatment of scleroderma
KR102824401B1 (ko) 2018-11-30 2025-06-25 아레나 파마슈티칼스, 인크. S1p1 수용체와 관련된 병태의 치료 방법
WO2020146529A1 (en) 2019-01-08 2020-07-16 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the s1p1 receptor

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010011316A1 (en) 2008-07-23 2010-01-28 Arena Pharmaceuticals, Inc. SUBSTITUTED 1,2,3,4- TETRAHYDROCYCLOPENTA[b]INDOL-3-YL) ACETIC ACID DERIVATIVES USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS
WO2011094008A1 (en) 2010-01-27 2011-08-04 Arena Pharmaceuticals, Inc. Processes for the preparation of (r)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid and salts thereof

Also Published As

Publication number Publication date
IL285890B (en) 2022-07-01
EA201890096A1 (ru) 2018-08-31
AU2020204164A1 (en) 2020-07-09
AU2021249972B2 (en) 2022-12-15
EP3310760B1 (en) 2022-09-14
US20240140911A1 (en) 2024-05-02
KR20180015259A (ko) 2018-02-12
DK3310760T3 (da) 2022-10-24
AU2023200978A1 (en) 2023-03-23
ES2929526T3 (es) 2022-11-29
CA3002551A1 (en) 2016-12-29
WO2016209809A1 (en) 2016-12-29
EP3310760A1 (en) 2018-04-25
AU2020204164B2 (en) 2021-11-04
PL3310760T3 (pl) 2023-03-06
US20220002244A1 (en) 2022-01-06
AU2021249972A1 (en) 2021-11-04
AU2016284162A1 (en) 2018-02-01
NZ738862A (en) 2023-12-22
BR112017027656A2 (pt) 2018-08-28
HUE060476T2 (hu) 2023-03-28
PT3310760T (pt) 2022-11-10
JP6838744B2 (ja) 2021-03-03
CN108349891A (zh) 2018-07-31
EP3310760B8 (en) 2022-10-19
CN108349891B (zh) 2022-04-05
MX383854B (es) 2025-03-14
MX2021007666A (es) 2021-08-05
MX2017016530A (es) 2018-03-12
US20200361869A1 (en) 2020-11-19
BR112017027656B1 (pt) 2023-12-05
US20180186738A1 (en) 2018-07-05
EP3939965A1 (en) 2022-01-19
US20190330153A1 (en) 2019-10-31
JP2020196756A (ja) 2020-12-10
US10301262B2 (en) 2019-05-28
KR102883123B1 (ko) 2025-11-10
AU2023200978B2 (en) 2024-07-25
US20250346560A1 (en) 2025-11-13
IL285890A (en) 2021-09-30
US11091435B2 (en) 2021-08-17
SI3310760T1 (sl) 2023-02-28
US12378198B2 (en) 2025-08-05
HK1253714A1 (en) 2019-06-28
KR20230160955A (ko) 2023-11-24
MA42807A (fr) 2018-07-25
JP2018525336A (ja) 2018-09-06
JP2023022155A (ja) 2023-02-14
IL256084B (en) 2021-10-31
IL256084A (en) 2018-02-28
US10676435B2 (en) 2020-06-09
US11884626B2 (en) 2024-01-30
CY1125778T1 (el) 2024-09-20

Similar Documents

Publication Publication Date Title
KR102603199B1 (ko) Ｓ1ｐ1 수용체-관련 장애에서의 사용을 위한 (ｒ)-2-(7-(4-시클로펜틸-3-(트리플루오로메틸)벤질옥시)-1,2,3,4-테트라히드로시클로-펜타[ｂ]인돌-3-일)아세트산 (화합물 1)의 결정성 ｌ-아르기닌 염
JP2015516425A (ja) ６−ｏ−（４−ジメチルアミノエトキシ）シンナモイルフマギロールのシュウ酸塩の多形塩ならびにその製造および使用方法
RU2537847C2 (ru) Новые фумаратные соли антагониста гистаминового рецептора н3
CN115093416B (zh) Ttk抑制剂的固体形式
HK40067541A (en) Crystalline l-arginine salt of (r)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid for use in sipi receptor-associated disorders
HK1253714B (en) Crystalline l-arginine salt of (r)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl) acetic acid for use in s1p1 receptor-associated disorders
EA040427B1 (ru) КРИСТАЛЛИЧЕСКАЯ L-АРГИНИНОВАЯ СОЛЬ (R)-2-(7-(4-ЦИКЛОПЕНТИЛ-3-(ТРИФТОРМЕТИЛ)БЕНЗИЛОКСИ)-1,2,3,4-ТЕТРАГИДРОЦИКЛОПЕНТА[b]ИНДОЛ-3-ИЛ)УКСУСНОЙ КИСЛОТЫ (СОЕДИНЕНИЯ 1) ДЛЯ ПРИМЕНЕНИЯ ПРИ РАССТРОЙСТВАХ, СВЯЗАННЫХ С S1P1-РЕЦЕПТОРОМ
EA045975B1 (ru) Кристаллическая l-аргининовая соль (r)-2-(7-(4-циклопентил-3-(трифторметил)бензилокси)-1,2,3,4-тетрагидроциклопента[b]индол-3-ил)уксусной кислоты (соединения 1) для применения при расстройствах, связанных с s1p1-рецептором
KR20240158969A (ko) 새로운 s1p1 수용체 작용제, 결정질 염, 제조 방법, 및 이에 관한 용도
CN118922405A (zh) 新的s1p1受体激动剂、结晶盐、制备方法及其相关用途
WO2017120532A1 (en) Polymorphs of a phosphate salt of quinuclidin-4-ylmethyl 4-methyl-1h-indole-3-carboxylate and uses thereof

Legal Events

Date Code Title Description
PA0105 International application

Patent event date: 20180119

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application
PA0201 Request for examination

Patent event code: PA02012R01D

Patent event date: 20210616

Comment text: Request for Examination of Application

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

Comment text: Notification of reason for refusal

Patent event date: 20230525

Patent event code: PE09021S01D

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

Patent event code: PE07011S01D

Comment text: Decision to Grant Registration

Patent event date: 20231005

GRNT Written decision to grant
PR0701 Registration of establishment

Comment text: Registration of Establishment

Patent event date: 20231113

Patent event code: PR07011E01D

PR1002 Payment of registration fee

Payment date: 20231114

End annual number: 3

Start annual number: 1

PG1601 Publication of registration