BR0010607A - Derivados de piperidina úteis como antagonistas de ccr5 - Google Patents

Derivados de piperidina úteis como antagonistas de ccr5

Info

Publication number
BR0010607A
BR0010607A BR0010607-0A BR0010607A BR0010607A BR 0010607 A BR0010607 A BR 0010607A BR 0010607 A BR0010607 A BR 0010607A BR 0010607 A BR0010607 A BR 0010607A
Authority
BR
Brazil
Prior art keywords
alkyl
naphthyl
optionally substituted
substituted phenyl
ccr5 antagonists
Prior art date
Application number
BR0010607-0A
Other languages
English (en)
Inventor
Bahige M Baroudy
John W Clader
Hubert B Josien
Stuart W Mccombie
Brian A Mckittrick
Michael W Miller
Bernard R Neustadt
Anandan Palani
Ruo Steensma
Jayaram R Tagat
Susan F Vice
Mark A Aughlinl
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
Application filed by Schering Corp filed Critical Schering Corp
Publication of BR0010607A publication Critical patent/BR0010607A/pt

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P17/04—Antipruritics
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • A61P31/12—Antivirals
    • 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
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic 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
    • C07D211/36—Heterocyclic 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
    • C07D211/56—Nitrogen atoms
    • C07D211/58—Nitrogen atoms attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • AIDS & HIV (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Patente de Invenção: "DERIVADOS DE PIPERIDINA úTEIS COMO ANTAGONISTAS DE CCR5". Esta invenção refere-se ao uso de antagonistas de CCR5 de fórmula (I) ou de um sal dos mesmos farmaceuticamente aceitável, onde X é -C(R^ 13^)2-, -C(R^ 13^)(R^ 19^)-, -C(O)-, -O-, -NH-, -N(alquila)-, (a), (b), (c), (d), (e), (f), (g), (h), (i), (j), (k), (l), (m) ou (n); R é fenila, piridila, tiofenila ou naftila opcionalmente substituídas; R^ 1^ é H, alquila ou alquenila; R^ 2^ é fenila, fenilalquila, heteroarila ou heteroarilalquila, naftila, fluorenila ou difenilmetila opcionalmente substituídas; R^ 3^ é fenila, heteroarila ou naftila opeionalmente substituídas; R^ 4^ é H, alquila, flúor-alquila, ciclopropilmetila, -CH~ 2~CH~ 2~OH, -CH~ 2~CH~ 2~-O-alquila, -CH~ 2~C(O)-O-alquila, -CH~ 2~C(O)NH~ 2~, -CH~ 2~C(O)-NHalquila ou -CH~ 2~C(O)-N(alquila)~ 2~; R^ 19^ é fenila, heteroarila ou naftila, cicloalquila, cicloalquilalquila ou alcoxialquila opcionalmente substituídas; e R^ 5^, R^ 13^, R^ 14^, R^ 15^ e R^ 16^ são hidrogênio ou alquila para o tratamento de HIV, rejeição de transplante de órgãos sólidos, enxerto versus doença do hospedeiro, artrite, artrite reumatóide, doença inflamatória dos intestinos, dermatite atópica, psoríase, asma, alergias ou esclerose múltipla, bem como se refere a novos compostos, composições farmacêuticas que os compreendem e à combinação de antagonistas de CCR5 da invenção em combinação com agentes antivirais úteis no tratamento de HIV ou agentes úteis no tratamento de doenças inflamatórias.
BR0010607-0A 1999-05-04 2000-05-01 Derivados de piperidina úteis como antagonistas de ccr5 BR0010607A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US30518799A 1999-05-04 1999-05-04
PCT/US2000/011633 WO2000066559A1 (en) 1999-05-04 2000-05-01 Piperidine derivatives useful as ccr5 antagonists

Publications (1)

Publication Number Publication Date
BR0010607A true BR0010607A (pt) 2002-02-13

Family

ID=23179704

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0010607-0A BR0010607A (pt) 1999-05-04 2000-05-01 Derivados de piperidina úteis como antagonistas de ccr5

Country Status (32)

Country Link
EP (2) EP1175402B1 (pt)
JP (3) JP3894729B2 (pt)
KR (1) KR100439357B1 (pt)
CN (2) CN1524527A (pt)
AR (1) AR023939A1 (pt)
AT (1) ATE299866T1 (pt)
AU (2) AU780983B2 (pt)
BR (1) BR0010607A (pt)
CA (1) CA2371587C (pt)
CO (1) CO5170522A1 (pt)
CZ (1) CZ301161B6 (pt)
DE (1) DE60021371T2 (pt)
DK (1) DK1175402T3 (pt)
EG (1) EG24533A (pt)
ES (1) ES2246233T3 (pt)
HK (1) HK1039330B (pt)
HU (1) HUP0203528A3 (pt)
IL (1) IL145742A0 (pt)
MY (1) MY141473A (pt)
NO (1) NO322044B1 (pt)
NZ (1) NZ514675A (pt)
PE (1) PE20010113A1 (pt)
PL (1) PL203117B1 (pt)
PT (1) PT1175402E (pt)
RU (2) RU2266281C2 (pt)
SA (1) SA00210270B1 (pt)
SI (1) SI1175402T1 (pt)
SK (1) SK286968B6 (pt)
TR (2) TR200103213T2 (pt)
TW (1) TWI283666B (pt)
WO (1) WO2000066559A1 (pt)
ZA (1) ZA200108867B (pt)

Families Citing this family (122)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR033517A1 (es) 2000-04-08 2003-12-26 Astrazeneca Ab Derivados de piperidina, proceso para su preparacion y uso de estos derivados en la fabricacion de medicamentos
US20050065319A1 (en) * 2000-12-19 2005-03-24 Baroudy Bahige M. Combination method for treating viral infections
WO2002079194A1 (en) 2001-03-29 2002-10-10 Schering Corporation Ccr5 antagonists useful for treating aids
GB0108876D0 (en) * 2001-04-09 2001-05-30 Novartis Ag Organic Compounds
DK1404667T3 (da) * 2001-07-02 2006-07-10 Astrazeneca Ab Piperidinderivater, der er anvendelige som modulatorer af chemokinreceptoraktivitet
GB0120461D0 (en) 2001-08-22 2001-10-17 Astrazeneca Ab Novel compounds
AR036366A1 (es) * 2001-08-29 2004-09-01 Schering Corp Derivados de piperidina utiles como antagonistas de ccr5, composiciones farmaceuticas, el uso de dichos derivados para la fabricación de un medicamento y un kit
GB0122503D0 (en) 2001-09-18 2001-11-07 Astrazeneca Ab Chemical compounds
US6818773B2 (en) 2001-10-15 2004-11-16 Schering Corporation Synthesis of 4-[(Z)-4-bromophenyl)(ethoxyimino) methyl]-1'-[(2,4-dimethyl-1-oxido-3-pyridinyl)carbony)]-4'-methyl-1,4-′bipiperidine
US6914142B2 (en) 2001-10-15 2005-07-05 Schering Corporation Synthesis of (4-bromopnenyl)(4-piperidyl)methanone-(Z)-O-ethyloxime and salts
WO2003066593A2 (en) * 2001-11-29 2003-08-14 Schering Corporation Preparation of pharmaceutical salts of 4 ( (z) - (4-bromophenyl) (ethoxyimino) methyl )-1'-( (2,4-dimethyl-1-oxido-3-pyridinyl) carbonyl) -4'-methyl-1,4' bipiperidine as ccr5-antagonists for the treatment of aids and related hiv infections
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
SE0200843D0 (sv) * 2002-03-19 2002-03-19 Astrazeneca Ab Chemical compounds
SE0200844D0 (sv) 2002-03-19 2002-03-19 Astrazeneca Ab Chemical compounds
CN101139343A (zh) * 2002-03-29 2008-03-12 先灵公司 作为ccr5拮抗药的哌啶和哌嗪化合物的合成
WO2003090748A1 (fr) * 2002-04-24 2003-11-06 Takeda Pharmaceutical Compay Limited. Utilisation de composes a antagonisme anti-ccr
WO2004026833A1 (ja) * 2002-09-20 2004-04-01 Takeda Pharmaceutical Company Limited 環状アミン化合物、その製造法および用途
JP2004107298A (ja) * 2002-09-20 2004-04-08 Takeda Chem Ind Ltd ウレア化合物およびその用途
GB0223223D0 (en) * 2002-10-07 2002-11-13 Novartis Ag Organic compounds
KR20050087832A (ko) * 2002-12-13 2005-08-31 스미스클라인 비참 코포레이션 Ｃｃｒ5 길항제로서 피페리딘 유도체
PE20040769A1 (es) * 2002-12-18 2004-11-06 Schering Corp Derivados de piperidina utiles como antagonisas ccr5
TW201018661A (en) 2003-03-14 2010-05-16 Ono Pharmaceutical Co Heterocyclic rinf having nitrogen atom derivatives and medicament containing the derivatives as active ingredient
SE0300957D0 (sv) 2003-04-01 2003-04-01 Astrazeneca Ab Chemical compounds
EP1619193A4 (en) 2003-04-18 2010-08-11 Ono Pharmaceutical Co SPIROPIPERIDINE COMPOUND 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
AR044519A1 (es) 2003-05-02 2005-09-14 Novartis Ag Derivados de piridin-tiazol amina y de pirimidin-tiazol amina
KR20060009390A (ko) * 2003-06-13 2006-01-31 쉐링 악티엔게젤샤프트 Ｃｃｒ-５ 길항제로서의 퀴놀릴 아미드 유도체
MXPA06000369A (es) 2003-07-10 2006-03-28 Schering Corp Procedimiento para la preparacion y purificacion de esteres del acido 2-(alcoxialquiliden)-3-cetoalcanoico a partir de esteres del acido 3-cetoalcanoico.
SE0302956D0 (sv) * 2003-11-07 2003-11-07 Astrazeneca Ab Chemical compounds
US7498346B2 (en) * 2003-12-11 2009-03-03 Genzyme Corporation Chemokine receptor binding compounds
GB0401334D0 (en) 2004-01-21 2004-02-25 Novartis Ag Organic compounds
EP1716156A2 (en) 2004-02-10 2006-11-02 F.Hoffmann-La Roche Ag Chemokine ccr5 receptor modulators
SE0400925D0 (sv) * 2004-04-06 2004-04-06 Astrazeneca Ab Chemical compounds
RU2369604C2 (ru) 2004-04-13 2009-10-10 Инсайт Корпорейшн Производные пиперазинилпиперидина в качестве антагонистов хемокинового рецептора
PL1761542T3 (pl) 2004-06-09 2008-06-30 Hoffmann La Roche Pochodne oktahydropirolo[3,4-c]pirolu i ich zastosowanie jako środków przeciwwirusowych
NZ553696A (en) * 2004-09-13 2010-02-26 Ono Pharmaceutical Co Nitrogenous heterocyclic derivative and medicine containing the same as an active ingredient
GT200500281A (es) 2004-10-22 2006-04-24 Novartis Ag Compuestos organicos.
GB0426164D0 (en) 2004-11-29 2004-12-29 Novartis Ag Organic compounds
JP2008528477A (ja) * 2005-01-20 2008-07-31 ファイザー・リミテッド 化合物
US7868006B2 (en) * 2005-02-16 2011-01-11 Schering Corporation Heterocyclic substituted piperazines with CXCR3 antagonist activity
PE20061074A1 (es) * 2005-02-23 2006-11-08 Schering Corp Derivados de piperidinil piperidina como inhibidores de receptores de quimioquinas
GB0507577D0 (en) 2005-04-14 2005-05-18 Novartis Ag Organic compounds
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
US20110052612A1 (en) 2005-05-31 2011-03-03 Ono Pharmaceutical Co., Ltd. Spiropiperidine compound and medicinal use thereof
US7665658B2 (en) 2005-06-07 2010-02-23 First Data Corporation Dynamic aggregation of payment transactions
CA2615650A1 (en) 2005-07-21 2007-01-25 Astrazeneca Ab Novel piperidine derivatives
EP1940781A1 (en) 2005-10-19 2008-07-09 F.Hoffmann-La Roche Ag Phenyl-acetamide nnrt inhibitors
WO2007045477A2 (en) 2005-10-21 2007-04-26 Novartis Ag Human antibodies against il-13 and therapeutic uses
EP1942108B1 (en) 2005-10-28 2013-09-04 Ono Pharmaceutical Co., Ltd. Compound containing basic group and use thereof
WO2007058322A1 (ja) 2005-11-18 2007-05-24 Ono Pharmaceutical Co., Ltd. 塩基性基を含有する化合物およびその用途
GB0525671D0 (en) 2005-12-16 2006-01-25 Novartis Ag Organic compounds
GB0526244D0 (en) 2005-12-22 2006-02-01 Novartis Ag Organic compounds
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
EA200870344A1 (ru) 2006-03-10 2009-04-28 Оно Фармасьютикал Ко., Лтд. Азотсодержащее гетероциклическое производное и фармацевтическое средство, включающее такое производное в качестве активного ингредиента
US20090124636A1 (en) * 2006-04-12 2009-05-14 Pfizer Inc. Chemical compounds
US8258141B2 (en) 2006-04-21 2012-09-04 Novartis Ag Organic compounds
WO2007132846A1 (ja) 2006-05-16 2007-11-22 Ono Pharmaceutical Co., Ltd. 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
PL2057125T3 (pl) 2006-08-16 2011-09-30 Hoffmann La Roche Nienukleozydowe inhibitory odwrotnej transkryptazy
MX2009003185A (es) 2006-09-29 2009-04-03 Novartis Ag Pirazolopirimidinas como inhibidores de lipido cinasa pi3k.
AU2007332654B2 (en) 2006-12-13 2013-06-20 F. Hoffmann-La Roche Ag 2-(piperidin-4-yl)-4-phenoxy- or phenylamino-pyrimidine derivatives as non-nucleoside reverse transcriptase inhibitors
KR101084787B1 (ko) 2007-01-10 2011-11-21 아이알엠 엘엘씨 채널 활성화 프로테아제 억제제로서의 화합물 및 조성물
KR20090127298A (ko) 2007-03-29 2009-12-10 에프. 호프만-라 로슈 아게 헤테로사이클릭 항바이러스 화합물
CA2685546A1 (en) 2007-05-07 2008-11-13 Novartis Ag Organic compounds
WO2009074575A2 (en) 2007-12-10 2009-06-18 Novartis Ag Organic compounds
JP2011513317A (ja) * 2008-02-29 2011-04-28 シェーリング コーポレイション Ｈｉｖ感染を防止するための予防薬としてのｃｃｒ５アンタゴニストおよびｈｉｖの伝播を抑制する方法
US8268834B2 (en) 2008-03-19 2012-09-18 Novartis Ag Pyrazine derivatives that inhibit phosphatidylinositol 3-kinase enzyme
JP2011522860A (ja) 2008-06-10 2011-08-04 ノバルティス アーゲー 上皮性ナトリウムチャネルブロッカーとしてのピラジン誘導体
ES2396023T3 (es) 2009-01-29 2013-02-18 Novartis Ag Bencimidazoles sustituidos para el tratamiento de astrocitomas
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
AU2010283806A1 (en) 2009-08-12 2012-03-01 Novartis Ag Heterocyclic hydrazone compounds and their uses to treat cancer and inflammation
MX2012002066A (es) 2009-08-17 2012-03-29 Intellikine Inc Compuestos heterociclicos y usos de los mismos.
EP2467383A1 (en) 2009-08-20 2012-06-27 Novartis AG Heterocyclic oxime compounds
EP2490687A1 (en) 2009-10-22 2012-08-29 Vertex Pharmaceuticals Incorporated Compositions for treatment of cystic fibrosis and other chronic diseases
US8247436B2 (en) 2010-03-19 2012-08-21 Novartis Ag Pyridine and pyrazine derivative for the treatment of CF
CU24147B1 (es) 2010-07-14 2016-02-29 Novartis Ag Compuestos heterociclícos agonistas del receptor ip
US8372845B2 (en) 2010-09-17 2013-02-12 Novartis Ag Pyrazine derivatives as enac blockers
US20130324526A1 (en) 2011-02-10 2013-12-05 Novartis Ag [1,2,4] triazolo [4,3-b] pyridazine compounds as inhibitors of the c-met tyrosine kinase
WO2012116237A2 (en) 2011-02-23 2012-08-30 Intellikine, Llc Heterocyclic compounds and uses thereof
WO2013024022A1 (en) 2011-08-12 2013-02-21 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
EA026655B1 (ru) 2011-09-15 2017-05-31 Новартис Аг 6-ЗАМЕЩЕННЫЕ 3-(ХИНОЛИН-6-ИЛТИО)[1,2,4]ТРИАЗОЛО[4,3-a]ПИРИДИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ c-MET ТИРОЗИНКИНАЗЫ
JP6165733B2 (ja) 2011-09-16 2017-07-19 ノバルティス アーゲー Ｎ−置換ヘテロシクリルカルボキサミド類
WO2013038378A1 (en) 2011-09-16 2013-03-21 Novartis Ag Pyridine amide derivatives
WO2013038373A1 (en) 2011-09-16 2013-03-21 Novartis Ag Pyridine amide derivatives
WO2013038381A1 (en) 2011-09-16 2013-03-21 Novartis Ag Pyridine/pyrazine amide derivatives
WO2013038386A1 (en) 2011-09-16 2013-03-21 Novartis Ag Heterocyclic compounds for the treatment of cystic fibrosis
CN104039321B (zh) 2011-11-18 2017-02-22 赫普泰雅治疗有限公司 药物化合物
WO2013078440A2 (en) 2011-11-23 2013-05-30 Intellikine, Llc Enhanced treatment regimens using mtor inhibitors
WO2013105065A1 (en) 2012-01-13 2013-07-18 Novartis Ag Fused piperidines as ip receptor agonists for the treatment of pah and related disorders
CN104169282B (zh) 2012-01-13 2016-04-20 诺华股份有限公司 Ip受体激动剂的盐
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
EP2802581A1 (en) 2012-01-13 2014-11-19 Novartis AG 7,8- dihydropyrido [3, 4 - b]pyrazines as ip receptor agonists for the treatment of pulmonary arterial hypertension (pah) and related disorders
EP2802583A1 (en) 2012-01-13 2014-11-19 Novartis AG Fused piperidines as ip receptor agonists for the treatment of pulmonary arterial hypertension (pah) and related disorders
CN104053659B (zh) 2012-01-13 2016-11-09 诺华股份有限公司 用于治疗肺动脉高压(pah)及相关病症的作为ip 受体激动剂的稠合的吡咯类
US8809340B2 (en) 2012-03-19 2014-08-19 Novartis Ag Crystalline form
EP2834246B1 (en) 2012-04-03 2021-07-28 Novartis AG Combination products with tyrosine kinase inhibitors and their use
WO2014122474A1 (en) 2013-02-07 2014-08-14 Takeda Pharmaceutical Company Limited Piperidin-1 -yl and azepin-1 -yl carboxylates as muscarinic m4 receptor agonists
ES2637719T3 (es) 2013-02-13 2017-10-16 Novartis Ag Compuestos heterocíclicos agonistas del receptor IP
US9073921B2 (en) 2013-03-01 2015-07-07 Novartis Ag Salt forms of bicyclic heterocyclic derivatives
EP2968340A4 (en) 2013-03-15 2016-08-10 Intellikine Llc COMBINING 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
JOP20200052A1 (ar) 2013-12-19 2017-06-16 Bayer Pharma AG بيبريدينيل تتراهيدرو كوينولينات مستبدلة واستخدامها كمعضدات مستقبل أدريني ألفا- 2c
CN106029657A (zh) 2013-12-19 2016-10-12 拜耳制药股份公司 作为肾上腺素能受体α2C拮抗剂的取代的联哌啶基衍生物
EP3083594A1 (de) 2013-12-19 2016-10-26 Bayer Pharma Aktiengesellschaft Substituierte bipiperidinyl-derivate als adrenorezeptor alpha 2c antagonisten
CR20160277A (es) 2013-12-19 2016-10-14 Bayer Pharma AG Piperidinil tetrahidroquinolinas sustituidas
EA033571B1 (ru) 2014-04-24 2019-11-06 Novartis Ag Производные пиразина в качестве ингибиторов фосфатидилинозитол 3-киназы
JP6454727B2 (ja) 2014-04-24 2019-01-16 ノバルティス アーゲー ホスファチジルイノシトール３−キナーゼ阻害薬としてのアミノピリジン誘導体
KR20160141855A (ko) 2014-04-24 2016-12-09 노파르티스 아게 포스파티딜이노시톨 3-키나제 억제제로서의 아미노 피라진 유도체
WO2016011658A1 (en) 2014-07-25 2016-01-28 Novartis Ag Combination therapy
BR112017001695A2 (pt) 2014-07-31 2017-11-21 Novartis Ag terapia de combinação
GB201513743D0 (en) 2015-08-03 2015-09-16 Heptares Therapeutics Ltd Muscarinic agonists
GB201519352D0 (en) 2015-11-02 2015-12-16 Heptares Therapeutics Ltd Pharmaceutical compounds
GB201617454D0 (en) 2016-10-14 2016-11-30 Heptares Therapeutics Limited Pharmaceutical compounds
GB201810239D0 (en) 2018-06-22 2018-08-08 Heptares Therapeutics Ltd Pharmaceutical compounds
GB201819960D0 (en) 2018-12-07 2019-01-23 Heptares Therapeutics Ltd Pharmaceutical compounds
GB202020191D0 (en) 2020-12-18 2021-02-03 Heptares Therapeutics Ltd Pharmaceutical compounds
EP3980121A1 (en) 2019-06-10 2022-04-13 Novartis AG Pyridine and pyrazine derivative for the treatment of cf, copd, and bronchiectasis
AU2020338971B2 (en) 2019-08-28 2023-11-23 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
US11629196B2 (en) 2020-04-27 2023-04-18 Incelldx, Inc. Method of treating SARS-CoV-2-associated hypercytokinemia by administering a human monoclonal antibody (PRO-140) that inhibits CCR5/CCL5 binding interactions

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5889006A (en) * 1995-02-23 1999-03-30 Schering Corporation Muscarinic antagonists
HUP9904622A3 (en) * 1996-07-10 2001-07-30 Schering Corp 1,4-di-sustituted piperidines as muscarinic antagonists
AU6623796A (en) * 1996-07-25 1998-02-20 Terence George Mackay Improvements in or relating to fishing
ES2241053T3 (es) * 1996-08-15 2005-10-16 Schering Corporation Eteres antagonistas muscarinicos.
EP1003514A4 (en) * 1997-07-25 2000-10-11 Merck & Co Inc CYCLIC AMINE MODULATORS OF CHEMOKIN RECEPTORS

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