HUP0202867A2 - CCR5 antagonistákként alkalmazható piperazinszármazékok és ezeket tartalmazó gyógyszerkészítmények - Google Patents

CCR5 antagonistákként alkalmazható piperazinszármazékok és ezeket tartalmazó gyógyszerkészítmények

Info

Publication number
HUP0202867A2
HUP0202867A2 HU0202867A HUP0202867A HUP0202867A2 HU P0202867 A2 HUP0202867 A2 HU P0202867A2 HU 0202867 A HU0202867 A HU 0202867A HU P0202867 A HUP0202867 A HU P0202867A HU P0202867 A2 HUP0202867 A2 HU P0202867A2
Authority
HU
Hungary
Prior art keywords
alkyl
active ingredients
substituted phenyl
optionally substituted
pharmaceutical compositions
Prior art date
Application number
HU0202867A
Other languages
English (en)
Inventor
Bahige M. Baroudy
John W. Clader
Eric Gilbert
Hubert B. Josien
Marc A. Labroli
Mark A. Laughlin
Stuart W. Mccombie
Brian A. Mckittrick
Michael W. Miller
Bernard R. Neustadt
Anandan Palani
Elizabeth M. Smith
Ruo Steensma
Jayaram R. Tagat
Susan F. Vice
Original Assignee
Schering Corp.
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=23179892&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HUP0202867(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Schering Corp. filed Critical Schering Corp.
Publication of HUP0202867A2 publication Critical patent/HUP0202867A2/hu
Publication of HUP0202867A3 publication Critical patent/HUP0202867A3/hu

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/56Nitrogen atoms
    • C07D211/58Nitrogen atoms attached in position 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Abstract

A találmány tárgyát az általános képletű vegyületek - ahol R adottesetben szubsztituált fenil-, piridil-, tienil- vagy naftilcsoport; R1hidrogénatom vagy alkilcsoport; R2 szubsztituált fenil-, szubsztituáltheteroaril-, naftil-, fluorenil-, difenil-metil- vagy adott esetbenszubsztituált fenil- vagy heteroaril-alkil-csoport; R3 hidrogénatom,alkil-, alkoxi-alkil-, cikloalkil-, cikloalkil-alkil- vagy adottesetben szubsztituált fenil-, fenil-alkil-, naftil-alkil-, heteroaril-vagy heteroaril-alkil-csoport; R4, R5 és R7 hidrogénatom vagyalkilcsoport; és R6 hidrogénatom, alkil- vagy alkenilcsoport - vagygyógyszerészetileg elfogadható sóik és hatóanyagként ezeket avegyületeket egyedül vagy más hatóanyagokkal, például a HIVkezelésében alkalmazott vírusellenes hatóanyagokkal vagy a gyulladásosbetegségek kezelésében alkalmazott hatóanyagokkal kombinációbantartalmazó gyógyszerkészítmények képezik. Ó
HU0202867A 1999-05-04 2000-05-01 Piperazine derivatives useful as ccr5 antagonists and pharmaceutical compositions containing them HUP0202867A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US30522699A 1999-05-04 1999-05-04
PCT/US2000/011632 WO2000066558A1 (en) 1999-05-04 2000-05-01 Piperazine derivatives useful as ccr5 antagonists

Publications (2)

Publication Number Publication Date
HUP0202867A2 true HUP0202867A2 (hu) 2003-01-28
HUP0202867A3 HUP0202867A3 (en) 2004-01-28

Family

ID=23179892

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0202867A HUP0202867A3 (en) 1999-05-04 2000-05-01 Piperazine derivatives useful as ccr5 antagonists and pharmaceutical compositions containing them

Country Status (31)

Country Link
EP (2) EP1175401B1 (hu)
JP (2) JP3722700B2 (hu)
KR (1) KR100439358B1 (hu)
AR (5) AR023823A1 (hu)
AT (2) ATE299865T1 (hu)
AU (2) AU780888B2 (hu)
BR (1) BR0010304A (hu)
CA (1) CA2371583C (hu)
CH (1) CH1175401H9 (hu)
CL (1) CL2008002737A1 (hu)
CO (1) CO5170523A1 (hu)
CZ (1) CZ20013940A3 (hu)
DE (2) DE60045528D1 (hu)
DK (1) DK1175401T3 (hu)
EG (1) EG24136A (hu)
ES (1) ES2244437T3 (hu)
HK (1) HK1039930B (hu)
HU (1) HUP0202867A3 (hu)
IL (1) IL145741A0 (hu)
MY (1) MY128367A (hu)
NO (1) NO322045B1 (hu)
PE (1) PE20010150A1 (hu)
PL (1) PL203116B1 (hu)
RU (1) RU2299206C9 (hu)
SA (2) SA06270096B1 (hu)
SI (1) SI1175401T1 (hu)
SK (2) SK286641B6 (hu)
TR (1) TR200103214T2 (hu)
TW (1) TWI285200B (hu)
WO (1) WO2000066558A1 (hu)
ZA (1) ZA200108868B (hu)

Families Citing this family (129)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7825121B2 (en) 1999-05-04 2010-11-02 Schering Corporation Piperazine derivatives useful as CCR5 antagonists
KR100613528B1 (ko) * 2001-03-29 2006-08-16 쉐링 코포레이션 Ccr5 길항제, 및 이를 포함하는 약제학적 조성물 및 키트
ATE418542T1 (de) 2001-03-29 2009-01-15 Schering Corp Als ccr5-antagonisten verwendbare aryloxim- piperazine
WO2003048153A1 (en) * 2001-11-29 2003-06-12 Schering Corporation Process for the preparation of compositions having an increased amount of pharmaceutically active salts of rotamers
EP2311818B1 (en) 2002-02-28 2013-01-16 Novartis AG Combination of a 5-phenylthiazole compound as PI3 kinase inhibitor with an antiinflammatory, bronchodilatory or antihistamine drug
JP4671091B2 (ja) * 2002-03-18 2011-04-13 東レ・ファインケミカル株式会社 1−置換−2−メチルピペラジンの製造方法
EP1490352A1 (en) * 2002-03-29 2004-12-29 Schering Corporation Synthesis of piperidine and piperazine compounds as ccr5 antagonists
WO2003084942A2 (en) 2002-03-29 2003-10-16 Schering Corporation Stereoselective alkylation of chiral 2-methyl-4-protected piperazines
US20050245537A1 (en) * 2002-04-24 2005-11-03 Noboru Tsuchimori Use of compounds having ccr antagonism
JP2003335737A (ja) 2002-05-21 2003-11-28 Central Glass Co Ltd 光学活性(r)−1−(4−トリフルオロメチルフェニル)エチルアミン
US7132539B2 (en) 2002-10-23 2006-11-07 The Procter & Gamble Company Melanocortin receptor ligands
US20060251651A1 (en) * 2002-12-13 2006-11-09 Ono Pharmaceutical Co., Ltd. Antagonist and agonist which bind to a strong binding site of chemokine receptor
PE20040769A1 (es) * 2002-12-18 2004-11-06 Schering Corp Derivados de piperidina utiles como antagonisas ccr5
BRPI0408332A (pt) 2003-03-14 2006-03-21 Ono Pharmaceutical Co derivados heterocìclicos contendo nitrogênio e medicamentos contendo os mesmos como ingrediente ativo
US7498323B2 (en) 2003-04-18 2009-03-03 Ono Pharmaceuticals Co., Ltd. Spiro-piperidine compounds and medicinal use thereof
WO2004092136A1 (ja) * 2003-04-18 2004-10-28 Ono Pharmaceutical Co., Ltd. 含窒素複素環化合物およびその用途
TW200519106A (en) 2003-05-02 2005-06-16 Novartis Ag Organic compounds
WO2004113323A1 (en) * 2003-06-13 2004-12-29 Schering Aktiengesellschaft Quinolyl amide derivatives as ccr-5 antagonists
GB0313661D0 (en) * 2003-06-13 2003-07-16 Avecia Ltd Process
US7345042B2 (en) 2003-06-30 2008-03-18 Schering Corporation MCH antagonists for the treatment of obesity
US7652142B2 (en) 2003-11-03 2010-01-26 Schering Corporation Bipiperidinyl derivatives useful as inhibitors of chemokine receptors
GB0329284D0 (en) * 2003-12-18 2004-01-21 Avecia Ltd Process
GB0401334D0 (en) 2004-01-21 2004-02-25 Novartis Ag Organic compounds
ATE428422T1 (de) * 2004-02-05 2009-05-15 Schering Corp Piperidin-derivate als ccr3-antagonisten
WO2005075484A2 (en) * 2004-02-10 2005-08-18 F. Hoffmann-La Roche Ag Chemokine ccr5 receptor modulators
ES2526614T3 (es) 2004-03-05 2015-01-13 Nissan Chemical Industries, Ltd. Compuesto de benzamida sustituida con isoxazolina y agente de control de organismos nocivos
JP4948395B2 (ja) 2004-04-13 2012-06-06 インサイト・コーポレイション ケモカインレセプターアンタゴニストとしてのピペラジニルピペリジン誘導体
ES2297727T3 (es) 2004-06-09 2008-05-01 F. Hoffmann-La Roche Ag Derivados de octahidropirrolo(3,4-c)pirrol y su empleo como agentes antiviricos.
GB0417804D0 (en) * 2004-08-10 2004-09-15 Novartis Ag Organic compounds
CN101775013A (zh) 2004-09-13 2010-07-14 小野药品工业株式会社 含氮杂环衍生物及含有其作为活性成分的药物
GT200500281A (es) 2004-10-22 2006-04-24 Novartis Ag Compuestos organicos.
GB0426164D0 (en) 2004-11-29 2004-12-29 Novartis Ag Organic compounds
NZ555320A (en) 2004-12-03 2010-11-26 Schering Corp Substituted piperazines as CB1 antagonists
WO2006071875A1 (en) 2004-12-29 2006-07-06 Millennium Pharmaceuticals, Inc. Compounds useful as chemokine receptor antagonists
WO2006071958A1 (en) 2004-12-29 2006-07-06 Millennium Pharmaceuticals, Inc. Compounds useful as chemokine receptor antagonists
MX2007008281A (es) 2005-01-06 2007-09-07 Schering Corp Preparacion de sales farmaceuticas de compuestos de piperazina.
EP1853583B1 (en) * 2005-02-16 2011-09-07 Schering Corporation Amine-linked pyridyl and phenyl substituted piperazine-piperidines with cxcr3 antagonist activity
CN101146793A (zh) 2005-02-16 2008-03-19 先灵公司 具有cxcr3拮抗剂活性的新的杂环取代了的吡啶或苯基化合物
CA2598489A1 (en) 2005-02-16 2006-08-24 Schering Corporation Piperazine-piperidines with cxcr3 antagonist activity
EP1856097B1 (en) * 2005-02-16 2012-07-11 Schering Corporation Pyridyl and phenyl substituted piperazine-piperidines with cxcr3 antagonist activity
EP1856098B1 (en) * 2005-02-16 2012-08-01 Schering Corporation Pyrazinyl substituted piperazine-piperidines with cxcr3 antagonist activity
BRPI0609251A2 (pt) * 2005-02-23 2010-03-09 Schering Corp derivados de piperidinil piperazina úteis como inibidores de receptores de quimiocinas
GB0507577D0 (en) 2005-04-14 2005-05-18 Novartis Ag Organic compounds
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
WO2006129679A1 (ja) 2005-05-31 2006-12-07 Ono Pharmaceutical Co., Ltd. スピロピペリジン化合物およびその医薬用途
EP1893603B1 (en) 2005-06-02 2009-10-14 F. Hoffmann-La Roche AG Piperidin-4-yl-amide derivatives and their use as sst receptor subtype 5 antagonists
US7665658B2 (en) 2005-06-07 2010-02-23 First Data Corporation Dynamic aggregation of payment transactions
KR20080056220A (ko) 2005-10-19 2008-06-20 에프. 호프만-라 로슈 아게 페닐-아세트아마이드 nnrt 저해제
EP2532678A1 (en) 2005-10-21 2012-12-12 Novartis AG Human antibodies against il13 and therapeutic uses
PL1942108T3 (pl) 2005-10-28 2014-03-31 Ono Pharmaceutical Co Związek zawierający grupę zasadową i jego zastosowanie
ES2407115T3 (es) 2005-11-18 2013-06-11 Ono Pharmaceutical Co., Ltd. Compuesto que contiene un grupo básico y uso del mismo
US20070123538A1 (en) * 2005-11-30 2007-05-31 Schering Corporation Compositions comprising a combination of CCR5 and CXCR4 antagonists
GB0525671D0 (en) 2005-12-16 2006-01-25 Novartis Ag Organic compounds
GB0526244D0 (en) 2005-12-22 2006-02-01 Novartis Ag Organic compounds
JP2009528266A (ja) 2006-01-18 2009-08-06 シェーリング コーポレイション カンナビノイド受容体修飾因子
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
WO2007105637A1 (ja) 2006-03-10 2007-09-20 Ono Pharmaceutical Co., Ltd. 含窒素複素環誘導体およびそれらを有効成分とする薬剤
PT2013211E (pt) 2006-04-21 2012-06-21 Novartis Ag Derivados de purina para utilização como agonistas de receptores a2a de adenosina
JP5257068B2 (ja) 2006-05-16 2013-08-07 小野薬品工業株式会社 保護されていてもよい酸性基を含有する化合物およびその用途
EP2055705A4 (en) 2006-07-31 2014-08-20 Ono Pharmaceutical Co COMPOUND WITH A CYCLIC GROUP BOUND BY A SPIRO BINDING THEREOF AND APPLY THEREOF
AU2007286345B2 (en) 2006-08-16 2012-03-08 F. Hoffmann-La Roche Ag Non-nucleoside reverse transcriptase inhibitors
ATE502943T1 (de) 2006-09-29 2011-04-15 Novartis Ag Pyrazolopyrimidine als pi3k-lipidkinasehemmer
CA2671478C (en) 2006-12-13 2015-02-17 F. Hoffmann-La Roche Ag Non-nucleoside reverse transcriptase inhibitors
GB0625523D0 (en) * 2006-12-21 2007-01-31 Ge Healthcare Ltd In vivo imaging agents
WO2008085608A1 (en) 2007-01-10 2008-07-17 Irm Llc Compounds and compositions as channel activating protease inhibitors
DK2137162T3 (en) * 2007-03-15 2018-11-26 Novartis Ag Organic compounds and their applications
MX2009010503A (es) 2007-03-29 2009-10-19 Hoffmann La Roche Compuestos heterociclicos antiviricos.
PL2155721T3 (pl) 2007-05-07 2011-07-29 Novartis Ag Związki organiczne
CA2687931C (en) 2007-05-31 2016-05-24 Boehringer Ingelheim International Gmbh Ccr2 receptor antagonists and uses thereof
JP2010540584A (ja) 2007-10-01 2010-12-24 エフ.ホフマン−ラ ロシュ アーゲー Ccr受容体アンタゴニストとしてのn−複素環ビアリールカルボキサミド類
CL2008003651A1 (es) 2007-12-10 2009-06-19 Novartis Ag Compuestos derivados de 3,5-diamino-6-cloropirazinamida sustituida; composicion farmaceutica; combinacion farmaceutica; y uso en el tratamiento de una condición inflamatoria o alergica, en particular una enfermedad inflamatoria u obstructiva de las vias respiratorias.
US20110059154A1 (en) * 2008-02-29 2011-03-10 Strizki Julie M Ccr5 antagonists as prophylactics for preventing hiv infection and methods of inhibiting transmission of same
US8268834B2 (en) 2008-03-19 2012-09-18 Novartis Ag Pyrazine derivatives that inhibit phosphatidylinositol 3-kinase enzyme
WO2009128947A1 (en) * 2008-04-17 2009-10-22 Concert Pharmaceuticals, Inc. Piperazine derivatives
BRPI0915018A2 (pt) 2008-06-10 2015-10-27 Novartis Ag compostos orgânicos
US20100041663A1 (en) 2008-07-18 2010-02-18 Novartis Ag Organic Compounds as Smo Inhibitors
PE20120061A1 (es) 2008-12-19 2012-02-19 Boehringer Ingelheim Int Derivados de pirimidina como antagonistas del receptor ccr2
US20110281917A1 (en) 2009-01-29 2011-11-17 Darrin Stuart Substituted Benzimidazoles for the Treatment of Astrocytomas
WO2010129351A1 (en) 2009-04-28 2010-11-11 Schepens Eye Research Institute Method to identify and treat age-related macular degeneration
US8389526B2 (en) 2009-08-07 2013-03-05 Novartis Ag 3-heteroarylmethyl-imidazo[1,2-b]pyridazin-6-yl derivatives
EA201200260A1 (ru) 2009-08-12 2012-09-28 Новартис Аг Гетероциклические гидразоны и их применение для лечения рака и воспаления
MX2012002066A (es) 2009-08-17 2012-03-29 Intellikine Inc Compuestos heterociclicos y usos de los mismos.
EA201200318A1 (ru) 2009-08-20 2012-09-28 Новартис Аг Гетероциклические оксимы
AU2010310449A1 (en) 2009-10-22 2012-05-03 Vertex Pharmaceuticals Incorporated Compositions for treatment of cystic fibrosis and other chronic diseases
PT3091012T (pt) 2009-12-17 2018-06-27 Centrexion Therapeutics Corp Antagonistas do receptor ccr2 e suas utilizações
JP5658272B2 (ja) * 2009-12-17 2015-01-21 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ccr2の新規アンタゴニスト及びこれらの使用
US8247436B2 (en) 2010-03-19 2012-08-21 Novartis Ag Pyridine and pyrazine derivative for the treatment of CF
US8946218B2 (en) 2010-05-12 2015-02-03 Boehringer Ingelheim International Gmbh CCR2 receptor antagonists, method for producing the same, and use thereof as medicaments
JP2013526507A (ja) 2010-05-12 2013-06-24 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規ccr2受容体アンタゴニスト、その製造方法及び薬物としてのその使用
US8841313B2 (en) 2010-05-17 2014-09-23 Boehringer Ingelheim International Gmbh CCR2 antagonists and uses thereof
JP5636094B2 (ja) 2010-05-25 2014-12-03 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ccr2受容体アンタゴニスト
EP2576538B1 (en) 2010-06-01 2015-10-28 Boehringer Ingelheim International GmbH New CCR2 antagonists
ES2622519T3 (es) 2010-07-14 2017-07-06 Novartis Ag Componentes heterocíclicos agonistas del receptor IP
US8372845B2 (en) 2010-09-17 2013-02-12 Novartis Ag Pyrazine derivatives as enac blockers
WO2012107500A1 (en) 2011-02-10 2012-08-16 Novartis Ag [1, 2, 4] triazolo [4, 3 -b] pyridazine compounds as inhibitors of the c-met tyrosine kinase
US9127000B2 (en) 2011-02-23 2015-09-08 Intellikine, LLC. Heterocyclic compounds and uses thereof
JP5786258B2 (ja) 2011-07-15 2015-09-30 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規かつ選択的なccr2拮抗薬
EP2741777B1 (en) 2011-08-12 2017-01-18 INSERM - Institut National de la Santé et de la Recherche Médicale Methods and pharmaceutical compositions for treatment of pulmonary hypertension
UY34305A (es) 2011-09-01 2013-04-30 Novartis Ag Derivados de heterociclos bicíclicos para el tratamiento de la hipertensión arterial pulmonar
MX339302B (es) 2011-09-15 2016-05-19 Novartis Ag 3-(quinolin-6-il-tio)-[1,2,4]-triazolo-[4,3-a]-piridinas 6-sustituidas como cinasas de tirosina.
WO2013038386A1 (en) 2011-09-16 2013-03-21 Novartis Ag Heterocyclic compounds for the treatment of cystic fibrosis
WO2013038373A1 (en) 2011-09-16 2013-03-21 Novartis Ag Pyridine amide derivatives
WO2013038378A1 (en) 2011-09-16 2013-03-21 Novartis Ag Pyridine amide derivatives
WO2013038390A1 (en) 2011-09-16 2013-03-21 Novartis Ag N-substituted heterocyclyl carboxamides
WO2013038381A1 (en) 2011-09-16 2013-03-21 Novartis Ag Pyridine/pyrazine amide derivatives
WO2013078440A2 (en) 2011-11-23 2013-05-30 Intellikine, Llc Enhanced treatment regimens using mtor inhibitors
WO2013105063A1 (en) 2012-01-13 2013-07-18 Novartis Ag Fused piperidines as ip receptor agonists for the treatment of pulmonary arterial hypertension (pah) and related disorders
US9115129B2 (en) 2012-01-13 2015-08-25 Novartis Ag Substituted pyrido[2,3-B]pyrazines as IP receptor agonists
EP2802582A1 (en) 2012-01-13 2014-11-19 Novartis AG Fused dihydropyrido [2,3 -b]pyrazines as ip receptor agonists for the treatment of pulmonary arterial hypertension (pah) and related disorders
US20140378463A1 (en) 2012-01-13 2014-12-25 Novartis Ag IP receptor agonist heterocyclic compounds
ES2565826T3 (es) 2012-01-13 2016-04-07 Novartis Ag Pirroles fusionados como agonistas del receptor IP para el tratamiento de hipertensión arterial pulmonar (PAH) y trastornos relacionados
WO2013105066A1 (en) 2012-01-13 2013-07-18 Novartis Ag Salts of an ip receptor agonist
US8809340B2 (en) 2012-03-19 2014-08-19 Novartis Ag Crystalline form
WO2013149581A1 (en) 2012-04-03 2013-10-10 Novartis Ag Combination products with tyrosine kinase inhibitors and their use
US9227990B2 (en) 2012-10-29 2016-01-05 Cipla Limited Antiviral phosphonate analogues and process for preparation thereof
US9604981B2 (en) 2013-02-13 2017-03-28 Novartis Ag IP receptor agonist heterocyclic compounds
US9073921B2 (en) 2013-03-01 2015-07-07 Novartis Ag Salt forms of bicyclic heterocyclic derivatives
WO2014151147A1 (en) 2013-03-15 2014-09-25 Intellikine, Llc Combination of kinase inhibitors and uses thereof
WO2015084804A1 (en) 2013-12-03 2015-06-11 Novartis Ag Combination of mdm2 inhibitor and braf inhibitor and their use
BR112016024484A2 (pt) 2014-04-24 2017-08-15 Novartis Ag derivados de aminopiridina como inibidores de fosfatidilinositol 3-quinase
CA2945257A1 (en) 2014-04-24 2015-10-29 Novartis Ag Pyrazine derivatives as phosphatidylinositol 3-kinase inhibitors
EA032075B1 (ru) 2014-04-24 2019-04-30 Новартис Аг Производные аминопиразина в качестве ингибиторов фосфатидилинозитол-3-киназы
WO2016011658A1 (en) 2014-07-25 2016-01-28 Novartis Ag Combination therapy
RU2695230C2 (ru) 2014-07-31 2019-07-22 Новартис Аг Сочетанная терапия
CN107108581B (zh) * 2014-08-21 2020-06-23 百时美施贵宝公司 作为强效rock抑制剂的回接苯甲酰胺衍生物
MX2017017177A (es) 2015-07-02 2018-11-09 Centrexion Therapeutics Corp Citrato de (4-((3r,4r)-3-metoxitetrahidro-piran-4-ilamino)piperidi n-1-il)(5-metil-6-(((2r,6s)-6-(p-tolil)tetrahidro-2h-piran-2-il)m etilamino)pirimidin-4il) metanona.
CN113891744A (zh) 2019-06-10 2022-01-04 诺华股份有限公司 用于治疗cf、copd和支气管扩张的吡啶和吡嗪衍生物
EP4021572A1 (en) 2019-08-28 2022-07-06 Novartis AG Substituted 1,3-phenyl heteroaryl derivatives and their use in the treatment of disease
TW202140550A (zh) 2020-01-29 2021-11-01 瑞士商諾華公司 使用抗tslp抗體治療炎性或阻塞性氣道疾病之方法

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL117149A0 (en) 1995-02-23 1996-06-18 Schering Corp Muscarinic antagonists
US5889006A (en) * 1995-02-23 1999-03-30 Schering Corporation Muscarinic antagonists
WO1999004794A1 (en) * 1997-07-25 1999-02-04 Merck & Co., Inc. Cyclic amine modulators of chemokine receptor activity
TW474933B (en) * 1998-06-30 2002-02-01 Schering Corp Muscarinic antagonists

Also Published As

Publication number Publication date
HUP0202867A3 (en) 2004-01-28
KR100439358B1 (ko) 2004-07-07
EP1632479B1 (en) 2011-01-12
CZ20013940A3 (cs) 2002-04-17
ES2244437T3 (es) 2005-12-16
MY128367A (en) 2007-01-31
SK286641B6 (sk) 2009-03-05
RU2299206C9 (ru) 2007-11-20
PL351388A1 (en) 2003-04-07
DE60021370T2 (de) 2006-04-27
SI1175401T1 (en) 2005-10-31
TWI285200B (en) 2007-08-11
KR20020019907A (ko) 2002-03-13
EP1632479A3 (en) 2007-05-09
DK1175401T3 (da) 2005-11-14
DE60021370D1 (de) 2005-08-25
EP1175401A1 (en) 2002-01-30
EP1632479A2 (en) 2006-03-08
TR200103214T2 (tr) 2002-03-21
AU780888B2 (en) 2005-04-21
DE60045528D1 (de) 2011-02-24
HK1039930A1 (en) 2002-05-17
IL145741A0 (en) 2002-07-25
AR023823A1 (es) 2002-09-04
DE60021370C5 (de) 2007-11-08
JP3722700B2 (ja) 2005-11-30
CH1175401H1 (de) 2007-02-15
NO20015366L (no) 2002-01-03
NO322045B1 (no) 2006-08-07
CA2371583A1 (en) 2000-11-09
ATE495154T1 (de) 2011-01-15
ZA200108868B (en) 2003-01-27
PL203116B1 (pl) 2009-08-31
EG24136A (en) 2008-08-06
JP2006052225A (ja) 2006-02-23
SA06270096B1 (ar) 2009-02-25
AU2005202357B2 (en) 2009-04-02
JP2002543185A (ja) 2002-12-17
SK287418B6 (sk) 2010-09-07
SA00210271B1 (ar) 2006-07-30
AU2005202357A1 (en) 2005-06-23
AR057107A2 (es) 2007-11-14
EP1175401B1 (en) 2005-07-20
HK1039930B (zh) 2005-12-09
CH1175401H9 (de) 2007-03-30
AU4500900A (en) 2000-11-17
SK15692001A3 (sk) 2002-07-02
AR057873A2 (es) 2007-12-26
AR057786A2 (es) 2007-12-19
WO2000066558A1 (en) 2000-11-09
CA2371583C (en) 2005-09-13
CL2008002737A1 (es) 2009-01-16
ATE299865T1 (de) 2005-08-15
NO20015366D0 (no) 2001-11-02
RU2299206C2 (ru) 2007-05-20
CO5170523A1 (es) 2002-06-27
BR0010304A (pt) 2002-02-13
PE20010150A1 (es) 2001-02-09
AR057106A2 (es) 2007-11-14

Similar Documents

Publication Publication Date Title
HUP0202867A2 (hu) CCR5 antagonistákként alkalmazható piperazinszármazékok és ezeket tartalmazó gyógyszerkészítmények
RS101304A (sr) Indolni, azaindolni i srodni heterociklični 4-alkenil piperidinski amidi
HUP0103460A2 (hu) Vírusellenes hatású indolszármazékok és a vegyületeket tartalmazó gyógyszerkészítmények
HUP0300641A2 (hu) Triazaspiro[5.5]undekán-származékok és hatóanyagként ezeket tartalmazó gyógyszerkészítmények
HUP0101530A2 (hu) Daganatellenes hatású indol-3-il-glioxilsav-származékokat tartalmazó gyógyszerkészítmények
HUP0401740A2 (hu) N-szubsztituált hidroxipirimidinon-karboxamid HIV-integráz inhibitorok és ezeket tartalmazó gyógyszerkészítmények
CA2443918A1 (en) Visual function disorder improving agents containing rho kinase inhibitors
HUP0300721A2 (hu) Antibakteriális hatású (amino-piperidino)-kinolinok és aza-izoszter analógjaik, eljárás előállításukra, az ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk
NO20020180D0 (no) Nye kinuklidinderivater og medisinske sammensetninger inneholdende det samme
EP1201239A4 (en) CYCLIC AMINES AS CCR3 ANTAGONISTS
HUP0202795A2 (hu) Pirimidin- és pirazinszármazékok, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk
RU2000115577A (ru) Новые производные пиридазина и лекарственные средства, содержащие их в качестве эффективных ингредиентов
HUP0004559A1 (hu) Ciklinfüggő kinázok aminotiazol inhibitorai, az ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk
NO175259C (no) Analogifremgangsmåte for fremstilling av terapeutisk aktive triazolo-1,4-diazepinforbindelser
HUP0401777A2 (hu) 3H-[1,2,4]Triazolo[5,1-i]purin-5-il-aminok mint adenozin A2a receptor antagonisták és a vegyületeket tartalmazó gyógyszerkészítmények
HUP0402019A2 (hu) CCR5 antagonistaként alkalmazható piperidinszármazékok és ezeket tartalmazó gyógyszerkészítmények
HUP9901820A2 (hu) 4-Amino-pirimidin-származékok, ezeket tartalmazó gyógyszerkészítmények, alkalmazásuk és eljárás előállításukra
HUP0301005A2 (hu) Pirrolotriazin kináz inhibitorok, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk
HUP0401488A2 (hu) Fungicid hatású 7-amino-triazolopirimidinek, előállításuk, alkalmazásuk és ilyeneket tartalmazó készítmények
NO20060147L (no) Benzimidazolderivater, sammensetninger som inneholder slike, fremstilling derav og anvendelse derav
AP1789A (en) Tropane derivatives useful in therapy.
NO20060146L (no) Benzimidazolderivater, sammensetninger som inneholder slike, fremstilling derav og anvendelse derav
CA2369560A1 (en) Agent for prophylaxis and treatment of liver disease
HUP0103063A2 (hu) Új 2H-piridazin-származékok, alkalmazásuk, ilyen hatóanyagot tartalmazó gyógyászati készítmények, és eljárás a hatóanyag előállítására
HUP0100684A2 (hu) Szubsztituált krománszármazékok, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények

Legal Events

Date Code Title Description
FD9A Lapse of provisional protection due to non-payment of fees