BR9916733A - Derivados de arilalcanoìla, processos para sua preparação, seu uso e composições farmacêuticas que os contêm - Google Patents

Derivados de arilalcanoìla, processos para sua preparação, seu uso e composições farmacêuticas que os contêm

Info

Publication number
BR9916733A
BR9916733A BR9916733-6A BR9916733A BR9916733A BR 9916733 A BR9916733 A BR 9916733A BR 9916733 A BR9916733 A BR 9916733A BR 9916733 A BR9916733 A BR 9916733A
Authority
BR
Brazil
Prior art keywords
formula
preparation
compounds
processes
derivatives
Prior art date
Application number
BR9916733-6A
Other languages
English (en)
Inventor
Elisabeth Defossa
Uwe Heinelt
Otmar Klingler
Gerhard Zoller
Hans Matter
Fahad D Al-Obeidi
Armin Walser
Peter Wildgoose
Original Assignee
Aventis Pharma Gmbh
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
Priority claimed from EP99100001A external-priority patent/EP1022268A1/en
Application filed by Aventis Pharma Gmbh filed Critical Aventis Pharma Gmbh
Publication of BR9916733A publication Critical patent/BR9916733A/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C279/04—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton
    • C07C279/10—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton being further substituted by doubly-bound oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/40—Acylated substituent nitrogen atom
    • 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
    • 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
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C257/00—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines
    • C07C257/10—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines
    • C07C257/18—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines having carbon atoms of amidino groups bound to carbon atoms of six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C279/04—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton
    • C07C279/14—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton being further substituted by carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D211/08—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/26—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/56—Amides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/20—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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
    • C07D233/72—Two oxygen atoms, e.g. hydantoin
    • C07D233/74—Two oxygen atoms, e.g. hydantoin with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to other ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
    • C07D271/07—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
    • 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
    • C07D413/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0205—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)3-C(=0)-, e.g. statine or derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

Abstract

Patente de Invenção: <B>"DERIVADOS DE ARILALCANOìLA, PROCESSOS PARA SUA PREPARAçãO, SEU USO E COMPOSIçõES FARMACêUTICAS QUE OS CONTêM"<D>. A presente invenção refere-se a novos compostos para a inibição das proteínas de coágulo do sangue e, mais particularmente, a derivados de arilalcanoíla da fórmula (I) em que R(1), R(2), R(3) ,R(4), R(5), R(6a) e R(6b) têm os significados indicados nas reivindicações. Os compostos da fórmula (I) são inibidores do fator Xa da enzima de coágulo do sangue. A invenção também refere-se a processos para a preparação dos compostos da fórmula (I), a métodos de inibição da atividade do fator Xa e de inibição do coágulo do sangue, ao uso dos compostos da fórmula (I) no tratamento e profilaxia de doenças, que podem ser tratadas ou prevenidas pela inibição da atividade do fator Xa tal como doenças tromboembólicas, e ao uso dos compostos da fórmula (I) na preparação de medicamentos a ser aplicados nessas doenças. A invenção adicionalmente refere-se a composições que contêm um composto da fórmula (I) em mistura ou, de outro modo, em associação com um veículo inerte, em particular, composições farmacêuticas que contêm um composto da fórmula (I) com substâncias de veículo farmaceuticamente aceitáveis e substâncias auxiliares.
BR9916733-6A 1999-01-02 1999-12-23 Derivados de arilalcanoìla, processos para sua preparação, seu uso e composições farmacêuticas que os contêm BR9916733A (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP99100001A EP1022268A1 (en) 1999-01-02 1999-01-02 Arylalkanoyl derivatives, processes for their preparation, their use and pharmaceutical compositions containing them
EP99119538 1999-10-01
PCT/EP1999/010341 WO2000040548A1 (en) 1999-01-02 1999-12-23 Arylalkanoyl derivatives, processes for their preparation, their use and pharmaceutical compositions containing them

Publications (1)

Publication Number Publication Date
BR9916733A true BR9916733A (pt) 2001-09-25

Family

ID=26152842

Family Applications (1)

Application Number Title Priority Date Filing Date
BR9916733-6A BR9916733A (pt) 1999-01-02 1999-12-23 Derivados de arilalcanoìla, processos para sua preparação, seu uso e composições farmacêuticas que os contêm

Country Status (20)

Country Link
US (1) US6759420B1 (pt)
EP (1) EP1150946B1 (pt)
JP (1) JP2002534408A (pt)
KR (1) KR20010089753A (pt)
CN (1) CN1332723A (pt)
AR (1) AR022130A1 (pt)
AT (1) ATE292114T1 (pt)
AU (1) AU2285700A (pt)
BR (1) BR9916733A (pt)
CA (1) CA2358581C (pt)
CZ (1) CZ20012378A3 (pt)
DE (1) DE69924527T2 (pt)
ES (1) ES2239478T3 (pt)
HK (1) HK1041687A1 (pt)
HU (1) HUP0202647A3 (pt)
IL (1) IL144095A0 (pt)
NO (1) NO20013141L (pt)
NZ (1) NZ512669A (pt)
TR (1) TR200101980T2 (pt)
WO (1) WO2000040548A1 (pt)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1127884A1 (en) 2000-02-26 2001-08-29 Aventis Pharma Deutschland GmbH Novel malonic acid derivatives, processes for their preparation, their use as inhibitor of factor XA activity and pharmaceutical compositions containing them
WO2002014262A1 (fr) * 2000-08-11 2002-02-21 Kaken Pharmaceutical Co.,Ltd. Derives de l'acide 2,3-diphenylpropionique ou leurs sels, medicaments ou inhibiteurs d'adhesion cellulaire en contenant, et leur utilisation
EP1569912B1 (en) 2002-12-03 2015-04-29 Pharmacyclics, Inc. 2-(2-hydroxybiphenyl-3-yl)-1h-benzoimidazole-5-carboxamidine derivatives as factor viia inhibitors
DE10204072A1 (de) * 2002-01-31 2003-08-14 Morphochem Ag Komb Chemie Neue Verbindungen, die Faktor Xa-Aktivität inhibieren
US7682782B2 (en) * 2004-10-29 2010-03-23 Affymetrix, Inc. System, method, and product for multiple wavelength detection using single source excitation
EP1828109B1 (en) 2004-11-12 2013-06-05 UCL Business PLC Guanidine derivatives as inhibitors of ddah
KR20100037600A (ko) * 2007-06-13 2010-04-09 브리스톨-마이어스 스큅 컴퍼니 응고 인자 억제제로서의 디펩티드 유사체

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2593812B1 (fr) * 1986-01-24 1988-08-26 Sanofi Sa Derives na-substitues des na-arylsulfonylaminoacyl p-amidinophenylalaninamides, leur procede de preparation, leur application comme medicaments et les compositions les renfermant
PT84170B (pt) * 1986-01-24 1989-03-30 Sanofi Sa Processo para a preparacao de derivados n alfa-substituidos das n alfa-aril-sulfonilaminoacil d-amidinofenil-alaninamidas
US5424334A (en) * 1991-12-19 1995-06-13 G. D. Searle & Co. Peptide mimetic compounds useful as platelet aggregation inhibitors
DE69333639D1 (en) * 1992-01-30 2004-11-04 Dendreon Corp Trypsininhibitoren
US5576342A (en) * 1992-03-13 1996-11-19 Bayer Aktiengesellschaft Phenylglycinamides of heterocyclically substitued phenylacetic acid derivatives
SK286094B6 (sk) * 1994-04-26 2008-03-05 Aventis Pharmaceuticals Inc. Zlúčenina špecificky inhibujúca aktivitu faktora Xa, farmaceutická kompozícia s jej obsahom a jej použitie
US6025472A (en) * 1994-12-21 2000-02-15 Corvas International, Inc. N-substituted glycine derivatives as enzyme inhibitors
CZ297544B6 (cs) * 1996-01-02 2007-02-07 Aventis Pharmaceuticals Inc. Substituované N-[(aminoiminomethyl)-fenyl]propylamidy nebo N-[(aminomethyl)fenyl]propylamidy
SI1042287T1 (en) 1997-12-24 2005-10-31 Aventis Pharma Deutschland Gmbh Indole derivatives as inhibitors of factor xa
CA2358578A1 (en) 1999-01-02 2000-07-13 Aventis Pharma Deutschland Gmbh Novel malonic acid derivatives, processes for their preparation, their use and pharmaceutical compositions containing them (inhibition of factor xa activity)

Also Published As

Publication number Publication date
CA2358581A1 (en) 2000-07-13
CN1332723A (zh) 2002-01-23
EP1150946A1 (en) 2001-11-07
KR20010089753A (ko) 2001-10-08
AU2285700A (en) 2000-07-24
NO20013141D0 (no) 2001-06-22
DE69924527T2 (de) 2006-02-09
AR022130A1 (es) 2002-09-04
ATE292114T1 (de) 2005-04-15
IL144095A0 (en) 2002-05-23
NZ512669A (en) 2003-11-28
ES2239478T3 (es) 2005-09-16
US6759420B1 (en) 2004-07-06
TR200101980T2 (tr) 2002-04-22
HUP0202647A2 (hu) 2002-11-28
EP1150946B1 (en) 2005-03-30
JP2002534408A (ja) 2002-10-15
HK1041687A1 (zh) 2002-07-19
CZ20012378A3 (cs) 2001-09-12
WO2000040548A1 (en) 2000-07-13
NO20013141L (no) 2001-08-03
HUP0202647A3 (en) 2003-12-29
DE69924527D1 (de) 2005-05-04
CA2358581C (en) 2010-02-02

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Legal Events

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B25D Requested change of name of applicant approved

Owner name: SANOFI-AVENTIS DEUTSCHLAND GMBH (DE)

Free format text: ALTERADO DE: AVENTIS PHARMA DEUTSCHLAND GMBH

B06A Patent application procedure suspended [chapter 6.1 patent gazette]
B06A Patent application procedure suspended [chapter 6.1 patent gazette]
B09B Patent application refused [chapter 9.2 patent gazette]
B09B Patent application refused [chapter 9.2 patent gazette]

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