BR112012014860A2 - pró-fármacos de [4 [4-(5-aminometil-2-flúor-fenil)-piperidin-1-il]-(1h-pirrolo-piridin-il)-metanonas e sua síntese - Google Patents

pró-fármacos de [4 [4-(5-aminometil-2-flúor-fenil)-piperidin-1-il]-(1h-pirrolo-piridin-il)-metanonas e sua síntese

Info

Publication number
BR112012014860A2
BR112012014860A2 BR112012014860A BR112012014860A BR112012014860A2 BR 112012014860 A2 BR112012014860 A2 BR 112012014860A2 BR 112012014860 A BR112012014860 A BR 112012014860A BR 112012014860 A BR112012014860 A BR 112012014860A BR 112012014860 A2 BR112012014860 A2 BR 112012014860A2
Authority
BR
Brazil
Prior art keywords
methanones
pyrrolo
piperidin
aminomethyl
prodrugs
Prior art date
Application number
BR112012014860A
Other languages
English (en)
Inventor
Gregory B Poli
Yong Mi Choi-Sledeski
Original Assignee
Sanofi Sa
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 Sanofi Sa filed Critical Sanofi Sa
Publication of BR112012014860A2 publication Critical patent/BR112012014860A2/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • 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
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Abstract

pró-fármacos de [4 [4-(5-aminometil-2-flúor-fenil)-piperidin-1-il]-(1h-pirrolo-piridin-il)-metanonas e sua síntese. a presente invenção refere-se a compostos e composições para o tratamento e melhora de doenças inflamatórias. especificamente, a presente invenção refere-se a compostos que têm atividade de inibição de triptase e seus intermediários, composições farmacêuticas que compreendem tais compostos, e um método para tratar indivíduos que sofrem de uma condição, doença ou distúrbio que pode ser melhorado pela administração de um inibidor de triptase, incluindo, porém sem limitações , por exemplo, asma e outras doenças inflamatórias, incluindo degeneração macular aguda.
BR112012014860A 2009-12-23 2010-12-21 pró-fármacos de [4 [4-(5-aminometil-2-flúor-fenil)-piperidin-1-il]-(1h-pirrolo-piridin-il)-metanonas e sua síntese BR112012014860A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US28953709P 2009-12-23 2009-12-23
FR1057197 2010-09-10
PCT/US2010/061434 WO2011079095A1 (en) 2009-12-23 2010-12-21 Prodrugs of [4[4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-(1h-pyrrolo-pyridin-yl)-methanones and synthesis thereof

Publications (1)

Publication Number Publication Date
BR112012014860A2 true BR112012014860A2 (pt) 2016-03-29

Family

ID=44246892

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112012014860A BR112012014860A2 (pt) 2009-12-23 2010-12-21 pró-fármacos de [4 [4-(5-aminometil-2-flúor-fenil)-piperidin-1-il]-(1h-pirrolo-piridin-il)-metanonas e sua síntese

Country Status (26)

Country Link
US (1) US8710080B2 (pt)
EP (1) EP2516418B1 (pt)
JP (1) JP2013515732A (pt)
KR (1) KR20120106824A (pt)
CN (1) CN102791702A (pt)
AR (1) AR079661A1 (pt)
AU (1) AU2010333772B2 (pt)
BR (1) BR112012014860A2 (pt)
CA (1) CA2784891A1 (pt)
CY (1) CY1115445T1 (pt)
DK (1) DK2516418T3 (pt)
ES (1) ES2481790T3 (pt)
HK (1) HK1178517A1 (pt)
HR (1) HRP20140607T1 (pt)
IL (1) IL220380A0 (pt)
MX (1) MX2012006739A (pt)
MY (1) MY155980A (pt)
PL (1) PL2516418T3 (pt)
PT (1) PT2516418E (pt)
RS (1) RS53456B (pt)
RU (1) RU2012131146A (pt)
SG (1) SG181501A1 (pt)
SI (1) SI2516418T1 (pt)
TW (1) TW201125860A (pt)
UY (1) UY33134A (pt)
WO (1) WO2011079095A1 (pt)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL2516418T3 (pl) 2009-12-23 2014-10-31 Sanofi Sa Proleki [4-[4-(5-aminometylo-2-fluoro-fenylo)-piperydyn-1-ylo]-(1H-pirolo-pirydynylo)-metanonów oraz ich synteza
CN102770425A (zh) * 2009-12-23 2012-11-07 赛诺菲 用作β-类胰蛋白酶抑制剂的吲哚基-哌啶基苄胺类化合物

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5087240A (en) 1983-08-18 1992-02-11 Drug Delivery Systems Inc. Transdermal drug patch with conductive fibers
US4921475A (en) 1983-08-18 1990-05-01 Drug Delivery Systems Inc. Transdermal drug patch with microtubes
US4879119A (en) 1984-02-21 1989-11-07 Yamanouchi Pharmaceutical Co., Ltd. Patch
NL8720442A (nl) 1986-08-18 1989-04-03 Clinical Technologies Ass Afgeefsystemen voor farmacologische agentia.
US5163899A (en) 1987-03-20 1992-11-17 Drug Delivery Systems Inc. Transdermal drug delivery system
US5312325A (en) 1987-05-28 1994-05-17 Drug Delivery Systems Inc Pulsating transdermal drug delivery system
GB8804164D0 (en) 1988-02-23 1988-03-23 Tucker J M Bandage for administering physiologically active compound
US5008110A (en) 1988-11-10 1991-04-16 The Procter & Gamble Company Storage-stable transdermal patch
US5088977A (en) 1988-12-21 1992-02-18 Drug Delivery Systems Inc. Electrical transdermal drug applicator with counteractor and method of drug delivery
US5013556A (en) 1989-10-20 1991-05-07 Liposome Technology, Inc. Liposomes with enhanced circulation time
EP0431519B1 (en) 1989-12-04 1994-06-15 G.D. Searle & Co. System for transdermal albuterol administration
NZ241954A (en) 1991-03-15 1994-01-26 Amgen Inc Compositions of g-csf for pulmonary administration.
US5352456A (en) 1991-10-10 1994-10-04 Cygnus Therapeutic Systems Device for administering drug transdermally which provides an initial pulse of drug
JPH07502219A (ja) 1991-12-18 1995-03-09 ミネソタ　マイニング　アンド　マニュファクチャリング　カンパニー 多重層型バリアー構造体
ATE132381T1 (de) 1992-01-29 1996-01-15 Voelkl Franz Ski Ballspielschläger, insbesondere tennisschläger
US5451569A (en) 1994-04-19 1995-09-19 Hong Kong University Of Science And Technology R & D Corporation Limited Pulmonary drug delivery system
GB0012362D0 (en) 2000-05-22 2000-07-12 Aventis Pharma Ltd Chemical compounds
CA2409827C (en) * 2000-05-22 2010-06-01 Aventis Pharmaceuticals Products Inc. Arylmethylamine derivatives for use as tryptase inhibitors
PT2367812E (pt) * 2008-08-22 2016-01-20 Sanofi Sa [4-(5-aminometil-2-fluoro-fenil)-piperidin-1-il]-[7-fluoro-1-(2-metoxi-etil)-4-trifluorometoxi-1h-indol-3-il]metanona como um inibidor da triptase de mastócitos
PL2516418T3 (pl) 2009-12-23 2014-10-31 Sanofi Sa Proleki [4-[4-(5-aminometylo-2-fluoro-fenylo)-piperydyn-1-ylo]-(1H-pirolo-pirydynylo)-metanonów oraz ich synteza

Also Published As

Publication number Publication date
RU2012131146A (ru) 2014-02-10
EP2516418A1 (en) 2012-10-31
SI2516418T1 (sl) 2014-08-29
US20120238573A1 (en) 2012-09-20
ES2481790T3 (es) 2014-07-31
HK1178517A1 (en) 2013-09-13
CA2784891A1 (en) 2011-06-30
AR079661A1 (es) 2012-02-08
MX2012006739A (es) 2012-06-28
DK2516418T3 (da) 2014-08-11
KR20120106824A (ko) 2012-09-26
AU2010333772B2 (en) 2016-07-14
MY155980A (en) 2015-12-31
IL220380A0 (en) 2012-08-30
US8710080B2 (en) 2014-04-29
AU2010333772A1 (en) 2012-07-05
HRP20140607T1 (hr) 2014-09-26
EP2516418B1 (en) 2014-05-14
JP2013515732A (ja) 2013-05-09
WO2011079095A1 (en) 2011-06-30
SG181501A1 (en) 2012-07-30
RS53456B (en) 2014-12-31
CN102791702A (zh) 2012-11-21
TW201125860A (en) 2011-08-01
PT2516418E (pt) 2014-07-18
UY33134A (es) 2011-07-29
CY1115445T1 (el) 2017-01-04
PL2516418T3 (pl) 2014-10-31

Similar Documents

Publication Publication Date Title
MA32393B1 (fr) Composés et compositions servant d'inhibiteurs de kinases
TN2012000081A1 (en) Compounds and compositions as protein kinase inhibitors
MA33838B1 (fr) Forme amorphe et cristalline de l'hémitartrate de genz 112638 au titre d'inhibiteur de la glucosylcéramide synthétase
MX2009007944A (es) Compuestos y composiciones de purina como inhibidores de quinasa para el tratamiento de enfermedades relacionadas con plasmodium.
NZ598694A (en) Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
MX2009013990A (es) Metodos para tratar enfermedades y trastornos mediados por serotonina.
HK1136283A1 (en) Compounds for the prevention and treatment of cardiovascular diseases
EA201690787A1 (ru) Соединения и их применение в качестве ингибиторов фермента расщепления бета-сайта app (bace)
CR9347A (es) Derivados de pirimidina para el tratamiento de trastornos hiperproliferativos
CO6150162A2 (es) Pirrolopirimidinas para composiciones farmaceuticas
UA103915C2 (ru) Твердая лекарственная форма, которая содержит линаглиптин и ингибитор sglt2, и ее применение
EA201100138A1 (ru) 4-феноксиметилпиперидины в качестве модуляторов активности gpr119
EA200901032A1 (ru) Соединения и композиции в качестве модуляторов активности gpr119
MX2012006730A (es) Tiazolidinadionas moderadoras de receptores activados por proliferador de peroxizoma (ppar) y combinaciones para tratamiento de enfermedades neurodegenerativas y otras enfermedades metabolicas.
UA103930C2 (ru) Соединения и композиция для лечения паразитарных болезней
TR201901114T4 (tr) Özgün immünomodülatör ve anti inflamatuvar bileşikler.
EA201100391A1 (ru) Соединения, ингибирующие активность семикарбазид-чувствительной аминооксидазы
IN2012DN02471A (pt)
IL193252A0 (en) N-hydroxyacrylamide compounds
MX2011013032A (es) Inhibidores de fosfatidilinositol 3-cinasa.
MX337849B (es) Composiciones y metodos para inhibicion de la via jak.
EP2257161A4 (en) AHCY HYDROLASE INHIBITORS FOR THE TREATMENT OF HYPER-HOMOCYSEINEMIA
BR112013027241A2 (pt) "composto inibidor de rock, composição que o compreende e seus usos"
MX2011008645A (es) Inhibidores de tetrahidrotiazolopiridina de fosfatidilinositol 3 cinasa.
BRPI0801239A2 (pt) uso de um ou mais benzopiranonas, composição farmacêutica e método de prevenção ou tratamento de doenças, disfunções e distúrbios associados a monoamino oxidase

Legal Events

Date Code Title Description
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 6A ANUIDADE.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]