CA2708364A1 - Carboxamide compounds and their use as chemokine receptor agonists - Google Patents

Carboxamide compounds and their use as chemokine receptor agonists Download PDF

Info

Publication number
CA2708364A1
CA2708364A1 CA2708364A CA2708364A CA2708364A1 CA 2708364 A1 CA2708364 A1 CA 2708364A1 CA 2708364 A CA2708364 A CA 2708364A CA 2708364 A CA2708364 A CA 2708364A CA 2708364 A1 CA2708364 A1 CA 2708364A1
Authority
CA
Canada
Prior art keywords
trifluoromethyl
pyrrolidin
methyl
alkyl
carbonyl
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.)
Abandoned
Application number
CA2708364A
Other languages
English (en)
French (fr)
Inventor
Efrat Ben-Zeev
Dongli Chen
Merav Fichman
Shomir Ghosh
Steffi Koerner
Jian Lin
Yael Marantz
Rosa Melendez
Pradyumna Mohanty
Sharon Shacham
Zhaoda Zhang
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
CytoPathfinder Inc
Original Assignee
Individual
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 Individual filed Critical Individual
Publication of CA2708364A1 publication Critical patent/CA2708364A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P3/04—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
    • A61P3/08—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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Immunology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Obesity (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Communicable Diseases (AREA)
  • Hospice & Palliative Care (AREA)
  • Child & Adolescent Psychology (AREA)
  • Transplantation (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Reproductive Health (AREA)
  • Emergency Medicine (AREA)
CA2708364A 2007-12-11 2008-12-11 Carboxamide compounds and their use as chemokine receptor agonists Abandoned CA2708364A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US1281907P 2007-12-11 2007-12-11
US61/012,819 2007-12-11
US3667508P 2008-03-14 2008-03-14
US61/036,675 2008-03-14
PCT/US2008/086388 WO2009076512A1 (en) 2007-12-11 2008-12-11 Carboxamidξ compounds and their use as chemokine receptor agonists

Publications (1)

Publication Number Publication Date
CA2708364A1 true CA2708364A1 (en) 2009-06-18

Family

ID=40352365

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2708364A Abandoned CA2708364A1 (en) 2007-12-11 2008-12-11 Carboxamide compounds and their use as chemokine receptor agonists

Country Status (10)

Country Link
US (1) US8569282B2 (enExample)
EP (1) EP2280766A1 (enExample)
JP (1) JP2011506466A (enExample)
KR (1) KR20100102646A (enExample)
CN (1) CN101925383A (enExample)
AU (1) AU2008335135A1 (enExample)
BR (1) BRPI0820701A2 (enExample)
CA (1) CA2708364A1 (enExample)
RU (1) RU2010128543A (enExample)
WO (1) WO2009076512A1 (enExample)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2604599A1 (en) 2007-04-27 2013-06-19 Purdue Pharma LP TRPV1 antagonists and uses thereof
KR20100102646A (ko) 2007-12-11 2010-09-24 가부시키가이샤 사이토파스파인더 카르복스아미드 화합물 및 케모카인 수용체 길항제로서의 이의 용도
MX2011010919A (es) * 2009-04-16 2011-11-02 Janssen Pharmaceutica Nv Antagonistas del receptor 2 de citocina quimioatrayente de 4-azetidinil-1-heteroaril-ciclohexano.
KR20120006051A (ko) * 2009-04-17 2012-01-17 얀센 파마슈티카 엔.브이. Ｃｃｒ2의 4-아제티디닐-1-헤테로원자 연결된 사이클로헥산 길항제
NZ595432A (en) * 2009-04-17 2013-12-20 Janssen Pharmaceutica Nv 4-azetidinyl-1-phenyl-cyclohexane antagonists of ccr2
US9273043B2 (en) 2011-06-22 2016-03-01 Purdue Pharma L.P. TRPV1 antagonists including dihydroxy substituent and uses thereof
GB201115633D0 (en) * 2011-09-09 2011-10-26 Univ Liverpool Compositions of efavirenz
JO3407B1 (ar) * 2012-05-31 2019-10-20 Eisai R&D Man Co Ltd مركبات رباعي هيدرو بيرازولو بيريميدين
CR20240144A (es) 2021-10-01 2024-05-24 Xinthera Inc Inhibidores de parp1 de azetidina y pirrolidina y usos de estos
AU2023209820B2 (en) 2022-01-21 2024-10-10 Xinthera, Inc. Parp1 inhibitors and uses thereof
KR20240161147A (ko) 2022-03-14 2024-11-12 슬랩 파마슈티컬스 엘엘씨 다중 사이클릭 화합물
CA3250945A1 (en) 2022-04-28 2023-11-02 Xinthera, Inc. TRICYCLIC PARP1 INHIBITORS AND THEIR USES
WO2025055965A1 (zh) * 2023-09-13 2025-03-20 中国药科大学 氮杂环丁烷衍生物、其制备方法及其医药用途
TW202542150A (zh) * 2023-12-21 2025-11-01 大陸商翼思生物醫藥（蘇州）有限公司 二氫吡咯並吡啶衍生物及其用途

Family Cites Families (111)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB860303A (en) 1958-06-20 1961-02-01 Ici Ltd Pharmaceutical compositions comprising ª‡-aryloxy-aliphatic carboxylic acids and/or ª
US3383281A (en) 1961-09-22 1968-05-14 Merck & Co Inc Method for binding bile acids in vivo
SE353319B (enExample) 1964-08-15 1973-01-29 Sumitomo Chemical Co
US3674836A (en) 1968-05-21 1972-07-04 Parke Davis & Co 2,2-dimethyl-{11 -aryloxy-alkanoic acids and salts and esters thereof
US4058552A (en) 1969-01-31 1977-11-15 Orchimed Sa Esters of p-carbonylphenoxy-isobutyric acids
US3803237A (en) 1969-11-03 1974-04-09 Upjohn Co Reaction products of polyethylenepolyamines and chlorohydrins or epoxy containing compounds
US3692895A (en) 1970-09-08 1972-09-19 Norman A Nelson Method of reducing hypercholesteremia in humans employing a copolymer of polyethylenepolyamine and a bifunctional substance, such as epichlorohydria
DE2230383C3 (de) 1971-10-01 1981-12-03 Boehringer Mannheim Gmbh, 6800 Mannheim Phenoxyalkylcarbonsäurederivate und Verfahren zur Herstellung derselben
DE2708913A1 (de) 1976-03-04 1977-09-08 Hoechst Ag Benzoylpiperidyalkyl-indole und verwandte verbindungen
FR2350341A1 (fr) 1976-05-07 1977-12-02 Synthelabo Nouveaux derives de piperidine et leur methode de preparation
GB2021108B (en) 1978-05-18 1982-07-21 Pfizer Ltd 6,7 - di - 4 - amino - 2 - quinazolines
DK159079A (da) * 1978-05-18 1979-11-19 Pfizer Fremgangsmaade til fremstilling af derivater af 4-amino-2-piperidinoquinazolin eller syreadditionssalte deraf
DE2928485A1 (de) 1979-07-14 1981-01-29 Bayer Ag Verwendung von harnstoffderivaten als arzneimittel bei der behandlung von fettstoffwechselstoerungen
US4452813A (en) 1981-05-22 1984-06-05 Taiho Pharmaceutical Company Limited Sulfonate derivatives, process for preparing same and antilipemic compositions containing the derivative
CA1247547A (en) 1983-06-22 1988-12-28 Paul Hadvary Leucine derivatives
US4847271A (en) 1986-01-27 1989-07-11 Merck & Co., Inc. Antihypercholesterolemic β-lactones
US5041432A (en) 1987-01-30 1991-08-20 E. I. Du Pont De Nemours And Company Steroid derivatives useful as hypocholesterolemics
US4716175A (en) 1987-02-24 1987-12-29 Warner-Lambert Company Saturated fatty acid amides as inhibitors of acyl-CoA:cholesterol acyltransferase
US5015644A (en) 1987-06-02 1991-05-14 Warner-Lambert Company Antihyperlipidemic and antiatherosclerotic urea and carbamate compounds
EP0306375A1 (fr) * 1987-08-07 1989-03-08 Synthelabo Dérivés de[(pipéridinyl-4)méthyl]-2 tétrahydro-1,2,3,4 isoquinoléine, leur préparation et leur application en thérapeutique
WO1990005132A1 (fr) 1988-11-11 1990-05-17 Banyu Pharmaceutical Co., Ltd. Derives d'allylamine substitues, procede de preparation et utilisation
US5064856A (en) 1989-07-31 1991-11-12 Merck & Co., Inc. Novel hmg-coa synthase inhibitors
US5391571A (en) 1989-11-15 1995-02-21 American Home Products Corporation Cholesterol ester hydrolase inhibitors
SE8904298D0 (sv) 1989-12-21 1989-12-21 Astra Ab New compounds
US5051534A (en) 1990-03-22 1991-09-24 Merrell Dow Pharmaceuticals Inc. Novel cyclopropyl squalene derivatives and their use as inhibitors of cholesterol synthesis
US5102915A (en) 1990-03-22 1992-04-07 Merrell Dow Pharmaceuticals Inc. Cyclopropyl squalene derivatives and their use as inhibitors of cholesterol synthesis
US5011859A (en) 1990-03-30 1991-04-30 Merrell Dow Pharmaceuticals Inc. Di- and tetra-fluoro analogs of squalene as inhibitors of squalene epoxidase
US5064864A (en) 1990-03-30 1991-11-12 Merrell Dow Pharmaceuticals Inc. Di- and tetra-fluoro analogs of squalene as inhibitors of squalene epoxidase
US5120729A (en) 1990-06-20 1992-06-09 Merck & Co., Inc. Beta-lactams as antihypercholesterolemics
CA2047375C (en) 1990-07-25 2003-04-15 Charlotte L. Barney Piperidyl ethers and thioethers as inhibitors of cholesterol biosynthesis
US5026554A (en) 1990-09-13 1991-06-25 Merck & Co., Inc. Method of inhibiting fungal growth using squalene synthetase inhibitors
US5084461A (en) 1991-03-27 1992-01-28 Merrell Dow Pharmaceuticals Inc. Azadecalin amides and thioamides as inhibitors of cholesterol biosynthesis
US5274143A (en) 1991-07-23 1993-12-28 Hoffmann-La Roche Inc. Process for the preparation of (R)-3-hexyl-5,6-dihydro-4-hydroxy-6-undecyl-2H-pyran-2-one and (R)-5,6-dihydro-6-undecyl-2H-pyran-2,4(3H)-dione
EP0618803A4 (en) 1991-12-19 1995-03-22 Southwest Found Biomed Res POLYPEPTIDE INHIBITING PROTEIN TRANSFER TO CHOLESTERYL ESTERS, ANTIBODIES AGAINST SYNTHETIC POLYPEPTIDE AND ANTI-ATHEROSCLEROSIS PROPHYLACTIC AND THERAPEUTIC TREATMENTS.
CA2098167C (en) 1992-06-24 2006-12-19 Dorothea Isler Foodstuffs and feedstuffs containing a lipase inhibitor
FR2697252B1 (fr) 1992-10-28 1994-12-09 Fournier Ind & Sante Dérivés de 1,2,3,5,6,7,8,8a-octahydro-5,5,8a-triméthyl-(8abeta)-6-isoquinolineamine, leur procédé de préparation et leur utilisation en thérapeutique.
US5364867A (en) 1992-11-30 1994-11-15 Sterling Winthrop Inc. 4-phenylpiperdine agents for treating cns disorders
US5635510A (en) 1993-05-06 1997-06-03 Merrell Pharmaceuticals Inc. Substituted pyrrolidin-3-yl-alkyl-piperidines
US5824690A (en) 1993-05-06 1998-10-20 Hoechst Marion Roussel Inc. Substituted pyrrolidin-3-yl-alkyl-piperidines
TW381025B (en) 1993-08-05 2000-02-01 Hoffmann La Roche Pharmaceutical composition containing a glucosidase inhibitor and a lipase inhibitor
SE9400447D0 (sv) 1994-02-11 1994-02-11 Astra Ab New compounds
US5576313A (en) 1994-08-29 1996-11-19 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5475109A (en) 1994-10-17 1995-12-12 Merck & Co., Inc. Dioxobutanoic acid derivatives as inhibitors of influenza endonuclease
JP3200070B2 (ja) 1994-11-16 2001-08-20 シナプティック・ファーマスーティカル・コーポレーション ジヒドロピリミジン類およびその使用
US6268369B1 (en) 1994-11-16 2001-07-31 Synaptic Pharmaceutical Corporation 5-(heterocyclic alkyl)-6-aryl-dihydropyrimidines
US5510379A (en) 1994-12-19 1996-04-23 Warner-Lambert Company Sulfonate ACAT inhibitors
US5688960A (en) 1995-05-02 1997-11-18 Schering Corporation Substituted oximes, hydrazones and olefins useful as neurokinin antagonists
US5696267A (en) 1995-05-02 1997-12-09 Schering Corporation Substituted oximes, hydrazones and olefins as neurokinin antagonists
US6369116B1 (en) 1995-06-02 2002-04-09 Oculex Pharmaceuticals, Inc. Composition and method for treating glaucoma
DK0832069T3 (da) 1995-06-07 2003-04-22 Pfizer Biphenyl-2-carboxylsyre-tetrahydroisoquinolin-6-ylamidderivater, deres fremstilling og deres anvendelse som inhibitorer af sekretion af mikrosomalt triglyceridoverførselsprotein og/eller apolipoprotein B (Apo B)
FR2735129B1 (fr) 1995-06-07 1997-07-11 Adir Nouveaux derives de l'indole, de l'indazole et du benzisoxazole, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US6228861B1 (en) 1995-11-16 2001-05-08 Synaptic Pharmaceutical Corporation Dihydropyrimidines and uses thereof
US6245773B1 (en) 1996-05-16 2001-06-12 Synaptic Pharmaceutical Corporation 5-(heterocyclic alkyl)-6-aryl-dihydropyrimidines
TR199901180T2 (xx) 1996-11-27 1999-08-23 Pfizer Inc. Apo B-Salg�lama/MTP inhibit�r amidler.
US5977139A (en) 1996-12-15 1999-11-02 Hoechst Marion Roussel, Inc. Carboxysubstituted cyclic carboxamide derivatives
US5861417A (en) 1996-12-19 1999-01-19 Hoechst Marion Roussel, Inc. Heterocyclic substituted pyrrolidine amide derivatives
US6136827A (en) 1997-07-25 2000-10-24 Merck & Co., Inc. Cyclic amine modulations of chemokine receptor activity
DE69827138T2 (de) 1997-08-11 2006-02-23 Allergan, Inc., Irvine Steriles Retinoid enthaltendes biodegradierbares Implantat mit verbesserter Biokompatibilität und Verfahren zu dessen Herstellung
US6020347A (en) 1997-11-18 2000-02-01 Merck & Co., Inc. 4-substituted-4-piperidine carboxamide derivatives
US6303620B1 (en) 1998-05-11 2001-10-16 Novo Nordisk A/S Compounds with growth hormone releasing properties
US6316445B1 (en) 1998-05-15 2001-11-13 Aventis Pharmaceuticals Inc. Carboxy substituted acylic carboxamide derivatives
GT199900147A (es) 1998-09-17 1999-09-06 1, 2, 3, 4- tetrahidroquinolinas 2-sustituidas 4-amino sustituidas.
US6133291A (en) 1998-10-16 2000-10-17 Schering Corporation N-(imidazolylalkyl)substituted cyclic amines as histamine-H3 agonists or antagonists
EP1186601B1 (en) 1999-06-03 2004-03-24 Yamanouchi Pharmaceutical Co. Ltd. Novel isoquinoline derivatives or salts thereof
US6331313B1 (en) 1999-10-22 2001-12-18 Oculex Pharmaceticals, Inc. Controlled-release biocompatible ocular drug delivery implant devices and methods
DE60005545D1 (de) 1999-10-27 2003-10-30 Millennium Pharm Inc Pyridyl enthaltende spirocyclische verbindungen als inhibitoren der fibrinogen-abhängigen blutplättchen aggregation
US6258833B1 (en) 1999-12-23 2001-07-10 Icos Corporation Cyclic AMP-specific phosphodiesterase inhibitors
CA2419310A1 (en) 2000-08-23 2002-02-28 Merck & Co., Inc. Substituted piperidines as melanocortin receptor agonists
US6608054B2 (en) 2001-03-20 2003-08-19 Boehringer Ingelheim Pharma Kg Pharmaceutical compositions based on anticholinergics and endothelin antagonists
US6620438B2 (en) 2001-03-08 2003-09-16 Boehringer Ingelheim Pharma Kg Pharmaceutical compositions based on anticholinergics and NK1-receptor antagonists
US7776315B2 (en) 2000-10-31 2010-08-17 Boehringer Ingelheim Pharma Gmbh & Co. Kg Pharmaceutical compositions based on anticholinergics and additional active ingredients
US20020137764A1 (en) 2000-10-31 2002-09-26 Karin Drechsel Inhalable formulation of a solution containing a tiotropium salt
AU2002236495B2 (en) 2000-11-29 2006-05-11 Allergan, Inc. Intraocular implants for preventing transplant rejection in the eye
MXPA03008356A (es) 2001-03-13 2003-12-11 Schering Corp Compuestos del tipo no imidazol como antagonistas de histamina h3.
GB0118238D0 (en) 2001-07-26 2001-09-19 Smithkline Beecham Plc Medicaments
WO2003028650A2 (en) 2001-10-02 2003-04-10 Acadia Pharmaceuticals, Inc. Benzimidazolidinone derivatives as muscarinic agents
MXPA04010172A (es) 2002-04-18 2005-02-03 Schering Corp 1-(4-piperidinil)benzimidazolonas como antagonistas de histamina h3).
US7105505B2 (en) 2002-04-18 2006-09-12 Schering Corporation Benzimidazole derivatives useful as histamine H3 antagonists
TW200403058A (en) * 2002-04-19 2004-03-01 Bristol Myers Squibb Co Heterocyclo inhibitors of potassium channel function
US7230008B2 (en) 2002-04-29 2007-06-12 Merck & Co, Inc. Tetrahydropyranyl cyclopentyl tetrahydropyridopyridine modulators of chemokine receptor activity
JP2006503008A (ja) 2002-08-13 2006-01-26 ワーナー−ランバート カンパニー リミティド ライアビリティー カンパニー マトリクスメタロプロテイナーゼ阻害物質としての４−ヒドロキシキノリン誘導体
WO2004024720A1 (en) 2002-09-11 2004-03-25 Merck & Co., Inc. Piperazine urea derivatives as melanocortin-4 receptor agonists
KR20050051691A (ko) 2002-10-11 2005-06-01 아스트라제네카 아베 1,4-이치환 피페리딘 유도체 및 11-베타ｈｓｄ1억제제로서의 이들의 용도
AU2004220321B2 (en) * 2003-03-12 2010-02-25 Kudos Pharmaceuticals Ltd Phthalazinone derivatives
US7393844B2 (en) * 2003-03-18 2008-07-01 Merck & Co., Inc. Tetrahydropyranyl cyclopentyl heterocyclic amide modulators of chemokine receptor activity
EP1468999A1 (en) 2003-03-20 2004-10-20 MyoContract Ltd. Substituted piperidine and piperazine derivatives as melanocortin-4 receptor modulators
CN1764458A (zh) 2003-03-26 2006-04-26 麦克公司 作为黑皮质素－4受体激动剂的双环哌啶衍生物
US7268133B2 (en) 2003-04-23 2007-09-11 Pfizer, Inc. Patent Department Cannabinoid receptor ligands and uses thereof
US20040259887A1 (en) 2003-06-18 2004-12-23 Pfizer Inc Cannabinoid receptor ligands and uses thereof
CA2540196C (en) 2003-09-26 2012-03-20 Actelion Pharmaceuticals Ltd Pyridine derivatives and use thereof as urotensin ii antagonists
GB0325745D0 (en) 2003-11-05 2003-12-10 Astrazeneca Ab Chemical compounds
CN1918145A (zh) * 2004-02-12 2007-02-21 默克公司 作为趋化因子受体活性调节剂的氨基杂环类化合物
JP2007532582A (ja) 2004-04-09 2007-11-15 ミレニアム・ファーマシューティカルズ・インコーポレイテッド 炎症性疾患の処置に有用なβ−カルボリン
US20070059336A1 (en) 2004-04-30 2007-03-15 Allergan, Inc. Anti-angiogenic sustained release intraocular implants and related methods
US20060182783A1 (en) 2004-04-30 2006-08-17 Allergan, Inc. Sustained release intraocular drug delivery systems
US7115601B2 (en) 2004-05-18 2006-10-03 Bristol-Myers Squibb Company HIV integrase inhibitors
AU2005247906B2 (en) 2004-05-18 2011-08-25 Merck Sharp & Dohme Corp. Substituted 2-quinolyl-oxazoles useful as PDE4 inhibitors
WO2005121090A1 (en) 2004-06-02 2005-12-22 Abbott Laboratories Substituted piperidines that have antiangiogenic activity
EP1778646A1 (en) 2004-08-11 2007-05-02 Janssen Pharmaceutica N.V. Mercaptoimidazoles as ccr2 receptor antagonists
EP1802602A1 (en) 2004-09-28 2007-07-04 Janssen Pharmaceutica N.V. Substituted dipiperdine ccr2 antagonists
US8138342B2 (en) 2004-10-12 2012-03-20 High Point Pharmacueticals, LLC 11β-hydroxysteroid dehydrogenase type 1 active spiro compounds
FR2876692B1 (fr) 2004-10-19 2007-02-23 Sanofi Aventis Sa Derives de 2-amido-4-phenylthiazole, leur preparation et leur application en therapeutique
CA2588449A1 (en) 2004-11-24 2006-06-01 Therakine Corporation An implant for intraocular drug delivery
JP2008540575A (ja) 2005-05-13 2008-11-20 レキシコン・ファーマシューティカルズ・インコーポレーテッド 多環系化合物とその使用の方法
US7425633B2 (en) 2005-08-26 2008-09-16 National Health Research Institutes Pyrrolidine compounds
WO2007053499A2 (en) * 2005-11-01 2007-05-10 Millennium Pharmaceuticals, Inc. Compounds useful as antagonists of ccr2
WO2008045558A2 (en) 2006-10-12 2008-04-17 Epix Delaware, Inc. Benzothiadiazine compounds and their use
CL2007002958A1 (es) 2006-10-12 2008-05-09 Epix Delaware Inc Compuestos derivados de heteroaril-carboxamida, antagonistas del receptor de quimioquina; composicion farmaceutica; y uso para el tratamiento o prevencion de enfermedades tales como rechazo de transplante de organos, artritis reumatoidea, lupus, entr
US20100331298A1 (en) 2007-12-10 2010-12-30 Cytopathfinder, Inc. Carboxamide Compounds and Their Use
KR20100102646A (ko) 2007-12-11 2010-09-24 가부시키가이샤 사이토파스파인더 카르복스아미드 화합물 및 케모카인 수용체 길항제로서의 이의 용도
TW201105667A (en) 2009-05-08 2011-02-16 Cytopathfinder Inc Dihydronaphthyridinyl and related compounds for use in treating ophthalmological disorders

Also Published As

Publication number Publication date
US20100324035A1 (en) 2010-12-23
BRPI0820701A2 (pt) 2015-06-16
JP2011506466A (ja) 2011-03-03
WO2009076512A1 (en) 2009-06-18
KR20100102646A (ko) 2010-09-24
US8569282B2 (en) 2013-10-29
RU2010128543A (ru) 2012-01-20
CN101925383A (zh) 2010-12-22
EP2280766A1 (en) 2011-02-09
AU2008335135A1 (en) 2009-06-18

Similar Documents

Publication Publication Date Title
US8569282B2 (en) Carboxamide compounds and their use
US20100331298A1 (en) Carboxamide Compounds and Their Use
US20100210633A1 (en) Carboxamide compounds and their use
US8067457B2 (en) Compounds useful as antagonists of CCR2
US7902199B2 (en) Heterocyclic substituted piperazine compounds with CXCR3 antagonist activity
CN100415716C (zh) 1－(1，2－双取代哌啶基)－4－取代哌嗪衍生物
US20100286136A1 (en) Dihydronaphthyridinyl and related compounds for use in treating ophthalmological disorders
AU2001283345B2 (en) Cyclopentyl modulators of chemokine receptor activity
US20090022670A1 (en) Novel compounds
US20050119482A1 (en) Hydroxynaphthyridinone carboxamides useful as hiv integrase inhibitors
US20030191143A1 (en) Fused heterocyclic compounds and use thereof
EP1856098A2 (en) Pyrazinyl substituted piperazine-piperidines with cxcr3 antagonist activity
KR20180067599A (ko) Apj 효능제로서의 2,4-디히드록시-니코틴아미드
KR20100072077A (ko) 치환된 ｎ­페닐­비피롤리딘 카복스아미드 및 이의 치료적 용도
WO2004052286A2 (en) Tyrosine kinase inhibitors
US20100184749A1 (en) Benzothiadiazine compounds and their use
EP1615699A2 (en) Benzoxazinyl-amidocyclopentyl-heterocyclic modulators of chemokine receptors
WO2008100620A2 (en) Bicyclic aminopropyl tetrahydro-pyrazolo-pyridine modulators of cathepsin s
PL184489B1 (pl) Nowa N acylo podstawiona benzimidazolilo lub imidazopirydynylo podstawiona piperydyna kompozycja farmaceutyczna sposób wytwarzania kompozycji farmaceutycznej i sposób wytwarzania N acylo podstawionej benzimidazolilo lub imidazopiperydynylo podstawionej piperydyny
US20100016289A1 (en) Compounds Useful as Antagonists of CCR2
AU2005214319A1 (en) Amino heterocyclic modulators of chemokine receptor activity
AU2012309556A1 (en) Pyrrolidine-3-ylacetic acid derivative
US7091211B2 (en) Cyclopentyl modulators of chemokine receptor activity
US8476301B2 (en) Pyrrolidin-3-ylacetic acid derivative
WO2008100635A1 (en) 1- [3- (monocyclic amino) propyl] - 4, 5, 6, 7-tetrahydro-1h-pyrazolo [4, 3-c] -pyridines as modulators of cathepsin s

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20131128

FZDE Discontinued

Effective date: 20151211