Arylmethylamine derivatives for use as tryptase inhibitors and pharmaceutical compositions containing them
Patent Information
- Application Number
- HU2003002485
- Authority / Receiving Office
- HU · HU
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2001-04-27
- Filing Date
- 2001-04-27
- Publication Date
- 2007-09-28
- Estimated Expiration
- Not applicable · inactive patent
AI Technical Summary
There is a need for new compounds with tryptase inhibitory properties to treat mast cell-mediated inflammatory conditions such as asthma, chronic asthma, hay fever, inflammatory bowel disease, psoriasis, atopic dermatitis, rheumatoid arthritis, osteoarthritis, rheumatic arthritis, rheumatic spondylitis, fibrosis, pulmonary fibrosis, interstitial lung diseases, heart attacks, atherosclerotic plaque rupture, peptic ulcers, viral infections, and other inflammatory disorders.
Development of arylmethylamine derivatives that act as tryptase inhibitors, which can be administered alone or in combination with beta-adrenergic agonists, anticholinergics, and anti-inflammatory corticosteroids to treat various inflammatory and fibrotic conditions.
The arylmethylamine derivatives effectively inhibit tryptase activity, providing therapeutic benefits in treating a wide range of inflammatory and fibrotic conditions, including asthma, arthritis, psoriasis, and other inflammatory disorders, by reducing inflammation and preventing tissue damage.
Description
BASIC VERSION ARYLMETHYLAMLN DERIVATIVES FOR USE AS TRXPTASE INHIBITORS AND E2WET WM^ The invention relates to substituted arylmethylamines, the preparation of the compounds, medicinal preparations containing such compounds and their therapeutic use in the treatment of modulable disease states by inhibiting tryptase. The IMÉáb ákh i tA kJ did / . h / HA'tTF z. eh Trlptase is in the secretory granules of mast cells. stored and human mast cells, main excretory protease. Tryptase has been found to be involved in various biological processes, including the degradation of vasodilator and broncho-relaxant neuropeptides [Caaghey et al., J. Fharnaool, Exp. Ther., 244, 133-137 (1938); Franco! et al., Jk PJia«aeoL Sxp. Ther. , 24 8, 947-951 (1988); and Tam et al., Am. J. Respir. Coll Moi. Szol., 3, 27-32 (1990)] and participates in bronchial responsiveness to histamine (Sekizawa et al., J, Cián, levest., 83, 175-179 (1989)1. As a result, trlptase inhibitors can presumably be used as an anti-inflammatory agent (K. Rica, P. A. Sprengrel, Cvrrenz ppirion in Drug Piscovery and Dev&lopaientf2(3), 463-474 (1999)1, especially in the treatment of chronic asthma [M, Q. Fhang, H. Timmerman, Aedlators Jnfianm., 112, 311-317 (1997)}, and hay fever [S. Klisén et al., Cian. Exp., A2lergy, 28, 220-227 (1998)1, inflammatory bowel disease (S.C. Risohoff et al., Mistopachology, 28, 113 {1996}], psoriasis (A, Naukkarlnen et al., Arob. Pernatol. őea,, 233, 341-346 (1993}], conjunctival inflammation (A, A, Irani et al,, d. Aliergy Ciin, Immunoi., 8 6, 34-40 (1990}], atopic der 979?0- 7500-SBE * * ♦ matitis [A. Jarvikallio et al., Br harmatod., 136, 871--87 / / · (1997) í, rheumatic arthritis (L, C. Tetlow efc í Bheum, dia., 54 , 549-555 (1998)], osteoarthritis SEE G. Buckiey et al., J, Pathol., 186, 67-74 (1998)1, rheumatoid arthritis, rheumatic spondylitis and the they can also be used in the treatment and prevention of cartilaginous joint diseases, In addition to the above, tryptase has been shown to be an effective mitogen for fibroblasts, which suggests its involvement in pulmonary fibrosis in asthma and interstitial lung diseases (Ruoss et al., u« Clín. levest., 88, 493-499 (1991)]. Therefore, tryptase inhibitors are effective in fibrotic conditions [J.A. Cairns and A.f. Walls, dl Clin. Invest., 99, 1313-1321 (1997)] such as fibrosis, scleroderma, puimonal fibrosis, liver cirrhosis, myocardial fibrosis, neurofibromas and hypertrophy. can be used to treat scars. In addition, tryptase inhibitors can also be used in the treatment or prevention of heart attacks, filters, angina and other consequences of atherosclerotic plaque rupture]M. Jeziorska. et al., u. Patkói., 182., 115-122 (1997)]. Tryptase has been recognized to activate prostrome, which in turn activates collagen, thereby causing the breakdown of cartilage and periodontal connective tissue. Therefore, tryptase inhibitors may be useful in the treatment or prevention of arthritis, periodontal disease, diabetic retinopathy and tumor growth [W. J. Bell et al., Exp. Bematol., 2 6, 158-169 (1998)]. Amaphylaxis of tryptase inhibitors (L, 8. Schwarz efc al., <7. f ..you '? f'í. Invest., 96, 2782-2710 (1995)], multiple sclerosis IM. Steinhoff et al., op. Afed, (N. ¥.} .§(2), 151-158 (2000)·}, They can also be used in the treatment and prevention of peptic ulcers and viral infections. Mast cell-mediated inflammatory conditions, especially asthma, are a growing public health problem. Asthma is often characterized by the progressive development of hypersensitivity of the trachea and bronchi. immune-specific allergens, as well as general chemical and physical stimuli, leads to the development of chronic inflammation. Eukocytes containing IgE receptors, namely mast cells and foosophiles, are present in the epicalium and are located beneath the smooth muscle tissues of the bronchi. These leukocytes are initially activated by the binding of specific inhaled antigens to IgE receptors and then release a number of chemical mediators. The degranulation of mast cells leads to the release of, for example, proteoglycans, peroxidase, arylsulfatase B, tryptase and chymase, which results in contraction of the small bronchi. Accordingly, there is a need for new and useful compounds possessing valuable medicinal properties and in particular tryptase inhibitory properties. Such compounds are readily useful in the treatment of patients suffering from pseudo-Lapotto's disease that can be ameliorated by the administration of a tryptase inhibitor, such as mast cell-mediated inflammatory conditions, inflammation, and diseases or disorders associated with the degradation of vasodilator and bronchodilator neuropeptides. Specific examples of such states are mentioned later. The description does not contain references to any literary sources ο can be considered as your knowledge that such a reference belongs to the state of the art in relation to this application. The present invention has a broad meaning; for a compound of the general formula, and for the compound's b-oxide, ester prodrug, pharmaceutically acceptable salt, solvate j price. and refers to the compound hydrate, in the formula Ar is an aryl or heteroaryl group, and the (aj) group on the product group is connected in the beta position relative to the (fcj) group; where —- means a single or double bond; Ft and R': means, independently of each other, a hydrogen atom or an alkyl group with 1~4 carbon atoms; td means ári swept down; (d is a hydrogen atom, nitrogen atom, alkyl, alkyl, alkyloxycarbonyl, carboxyl, cyano, hydroxyl group, -Ck;;Oj.....A group of the general formula ΝΥ3·ΥΛ or an alkyl group, which is optionally substituted by an alkoxy-, alkylcarbonitamino-, alkylsultonylamino-, hydroxyisoport or a group of the general formula -S (O).m-alkyl or ~NY*Y ; Y Y is independently hydrogen, alkyl, alkyl, aryl, arylalkyl, cycloalkyl, heteroaryl, heteroarylalkyl or heterocycloalkyl; or the group of general formula ~NY;d' can form a ring amine; m nose wedge is 0 or an integer that is 1 or 2; and the value of n is 2. The present invention covers the compound of the general formula (oil), the corresponding oxide of the compound, its salt, its pharmaceutically acceptable salt, solvate, and the compound also for hours, in the formula it means single or garden binding; and R is independently a hydrogen atom or a C1-C4 alkyl group; means an aryl group, means a hydrogen atom, a halogen atom, a steel, alkoxy-, alkyloxycarbonyl-, carboxy-, oiano-, hydroxyl group, a group of the general formula -C (-0} NY:Y~ or an alkyl group, which is optionally alkoxy-, alkylcarbonylamino Substituted by -, alkylsultonylamino-, hydroxyl group, -53 (0; ".-alkyl or -HY:YÓ group of general formula; means hydrogen atom:, halogen atom, acyl~, alkoxy·-, alkyloxycarbonyl-, aryl·-·, carboxy-, oiano-, heteroaryl-, heteroaryloxy-, heterocycloalkyl-, hetsrocycloalkyloxy-, heterocycloalkylalkyloxy-, heteroarylalkyloxyhydroxyl-, trlflnormethyl group, —C) -NY' Y'g -NYAYZ, - / 1-(C2-6 alkylene-Pl general formula group or alkyl group, which optionally is alkoxy-, alkylcarbonylamino-, alkylisopropylamino-, aryl-, heteroaryl-, heterocycloalkyl··, hydroxyl -, areidocsopert, ~C {===0) -sits, -Ytg-hY'Yg -3(0:..,slicks or -ΙΡΓΎ4 substituted with a group of general formula; means a hydroxyl-, alkoxy-, nreido group, -ü (-0) -ΝΥ'Ύ2, SCy-hY'Y'n -S (0;--alkyl or ~üY:Yi: group of the general formula; means a hydrogen atom or 1- C4-alkylated; and Y" is independently a hydrogen atom, alkyl, alkyl, aryl, arylalkyl, cycloalkyl, heteroaryl, hexaroanialkyl or heterocycloalkyl; or by -ΥόΥ- an ionic group can form a cyclic amine; 2 means an oxygen atom, “S(G)m~ or a group with the general formula -ΝΡΛ-; and m is 0 or an integer equal to 1 or 2; 2. In another embodiment, the invention relates to a compound of the general formula (Ibi) and the corresponding d-oxide of the compound, its esterification drug, its gemologically acceptable salt, and its soy product, in the formula, R4 means a hydrogen atom, if an ion atom, acyl~, alkom.!···, acylosicarbonyl-, carboxyl-, cyano-, hydroxyl swept, -C(-0; :~Νϊ*ϊ4 group or alkyl group, which is optionally substituted with an akoxy-, alkylcarbonylaraino-, alkylsulfonylamino-, hydrocylsulfide, ~S(0)^-alkyl or ηΥΌ general formula group; and R" is a hydrogen atom if an ion atom, aryl-, alkyloxy-, alkyloxycarbonyl-, aryl-, carboxyl-, cyano-, heteroaryl-, heteroaryloxy-, heterocycloalkyloxy-, heterocycloalkyloxy-, heterocycloalkylalkyloxy-, heteroarylalkyloxy-, hydroxy-, trifluoromethylisosporin, -C (=0) -Μϊ:kp, -ΚΥ'Ύρ -o'-ız-ü carbon atom alkyl group -Fi general formula f group or alkyl group, which is optionally akoxy-, akyl.arboniiamino-, a 1. k z 1 s z n . 11 ο η. í i a m i η o -, arii-,, h e t e r oa r i, h er e r ο ο i k 1 o a .1 k i .1 -, hydroxyi-, with nreidoosoport, -ü Y -űtcdn -SCg-Nállö, -3(0}; Substituted with a group of the general formula -;aikii or -ϊηΓΥ-. Examples of such compounds are described later. The present invention further extends to the pharmaceutical composition according to the present invention containing the compound described above and a medically usable carrier material. Several examples of pharmaceutical carriers that may be used in the present invention are described below. In addition, the present application presents a method for the treatment of patients suffering from a condition that can be improved by administering tryptase inhibitors, during the method an effective amount of a compound according to the present invention is administered. The conditions that can be treated with the compound according to the present invention include, but are not limited to, inflammatory diseases such as arthritis, synovitis, rheumatoid arthritis, rheumatoid arthritis, gouty arthritis, traumatic arthritis, rubella arthritis, psoriatic arthritis and other chronic inflammatory joint diseases, conditions that can be treated by the method of the present invention other examples are degenerative diseases of the joints, conjunctivitis, spring conjunctivitis, inflammatory skin disease, asthma, hay fever, interstitial lung diseases, fibrosis, scleroderma, puimonal fibrosis, cirrhosis of the liver, myocardial fibrosis, neurofibromas, hypertrophic scars , various dermatological conditions such as atopic dermatitis and psoriasis, heart attack, stroke, angina and other consequences of atherosclerotic plaque rupture, as well as periodontal disease, diabetic retinopathy, tumor growth, anaphyxia, solerosis multiplex, peptic ulcers and synovial infections are also viral infections, to name but a few. In the present application, we also present a method suitable for the treatment of an individual suffering from asthma, during which the individual is administered an effective amount of the compound according to the present invention. In the present application, we also present a method suitable for the treatment of a patient suffering from arthritis, during which the patient is administered an effective amount of a compound according to the present invention. The invention covers a pharmaceutical composition that contains a compound according to the present invention and a second compound selected by hand as a beta-adrenergic agonist, anticholinergic, anti-inflammatory corticosteroid and anti-inflammatory agent, and a medically applicable carrier. A specific inflammatory disease or disorder that can be treated with such a pharmaceutical composition includes, but is not limited to, asthma, In addition, the present report also presents a method suitable for the treatment of a patient suffering from an inflammatory disorder, during which the patient is given a compound according to the present invention and a beta a-adrenergic agonist, anticholinergic, anti-inflammatory corticosteroid and gyal. lenes: a second compound selected from the agent is administered. In this method, a compound according to the present invention can be administered before a second compound, a second compound before a compound according to the present invention, or a compound according to the present invention and a second compound can be administered simultaneously. Adrenergic agonists, anticholinergics, anti-inflammatory corticosteroids, and others that can be used in such a procedure. for drugs with sedation examples are given in the following chapters. According to the above, the main goal is to prescribe compounds against tryptase activity. Such compounds can easily be used to treat conditions that can be improved by administration of a tryptase inhibitor, A. another goal of the present invention is to provide pharmaceutical preparations for the treatment of conditions that can be improved by the administration of an eryptase inhibitor. A further aim of the present invention is to provide pharmaceutical preparations containing the compound according to the present invention. These and other aspects of the present invention will be better understood from the following detailed description. DETAILED DESCRIPTION In a method according to the deficiency, a compound according to the present invention is placed before a second compound, a second compound is placed before a compound according to the present invention, or a compound according to the present invention and a second compound; can be administered simultaneously. Adrenergic agonists, anticholinergics, anti-inflammatory corticosteroids and anti-inflammatory drugs can be used in the method according to the present invention. examples of these will be given later < According to the above, the main aim is to provide compounds against tryptase activation. Such compounds can easily be used to treat conditions that respond to tryptase inhibitor administration. another purpose is medicinal preparations The present talc is provided for the treatment of conditions that can be improved by tryptase inhibition / administration. / A further purpose of the present invention is to prescribe / prescribe medicinal preparations containing the compound of the present invention. release of e. / These and other aspects of the present invention can be better understood / by referring to the following detailed description,........... ...................... the following terms, as used above and in the present description and appended claims, unless otherwise indicated, have the following meanings. As used herein, compounds of the present invention and equivalent terms refer to compounds of formula (I), (Ia) or (Ibj) as described above, the term includes prodrugs, pharmaceutically acceptable salts and solvents such as hydrates, X* where as connections allow est. Likewise, where reference is made to intermediates, whether or not they are claimed themselves, the term includes salts and solvates of the compounds where the context so permits. To make it clearer, we sometimes refer to some cases in the text when the context allows, but these cases are only illustrative and do not exclude other cases if the context so requires. In the description, treatment' includes preventive therapy as well as treatment of an established condition. Patient includes humans and other mammals. The effective amount describes the amount of the compound according to the present invention that is effective in inhibiting cryptase and thus results in the desired therapeutic effect. Acylisoport means a group with the formula H-CO- or alkyl-CO-, where the meaning of alkylisoport is as described here. "Acylamino group" is a group of the formula acyl-NH-, in which the meaning of steel is as defined herein. The alkyl group is an aliphatic hydrocarbon group containing a carbon bond in a chain of approx. 2 - approx. - approx. and which contains straight or branched Ián15 carbon atoms; and contains 4 carbon atoms. In this way, it means that an alkyl group with one carbon atom can have two carbons, the longest in the chain is approx. the term "branched chain" is attached to the present straight chain by one or more, for example, methyl, ethyl or prepa swept; the straight 4 .-¾ chain here is a straight alkenyl chain The low-carbon alkene ÍR nyl group” contains a carbon atom in the chain, which can be straight or branched. Examples of alkenyl groups include ethenyl, propanyl, n-butenyl, isobutenyl, 3-methylbut-2-enyl, η-pentyl, heptenyl, octenyl and deoenyl. "Alkoxy group" means a group of the formula alk.yl~O-, where the meaning of the alkyl group is as described herein. Examples of .alkoxy groups include methoxy, ethoxy, η-propoxy, isopropoxy, n-butoxy and hepoxy. The "alkyl oxycarbonyl group" means a group with the formula alkyl-0-C (-0) -, in which the meaning of the alkyl sweep is as described here. Alkoxycarbonyl groups include ethoxy and ethoxycarbonyl groups. "Alkyl-swept", unless otherwise defined, is an aliphatic carbon bridging group, which can be straight or branched, and in the chain approx. 1 - contains about 15 carbon atoms; the chain is optionally substituted with an alkoxy group or one or more halogen atoms 7-d. Is the lower alkyl group f-d as a group? or a low-carbon aikoxy-, low-carbon a.l ki.lt io-, -(-b Part of a C10 alkylsuitinyl or lower C10 alkylsulfonyl group, unless otherwise specified, is an aliphatic hydrocarbon group that can be straight or branched and contains kba-b~ carbon atoms in the chain. For alkyl groups. examples include metal-, ethyl-, n-propyl-, isopropyl-, n-butyl, sec-butyl, tert-butyl, n-pentyl, 3-pentyl, heptyl, octyl-, non.yl-, decyl- and dodecyl-swept. Alkylcarbonylaminoisoport means a group of the formula alkyl-C<>O>-NH-, in which the meaning of the alkyl group is as described herein. Examples of the alkylcarbonylamino group include acetamido and propionamido isoport. «X glaze "Alkylene group" means an aliphatic divalent group derived from a straight or branched chain alkyl group, where the meaning of the alkyl group is as described herein. An alkylene group is, for example, methylene, ethylene and trimethylene. "Alkylenedioxy group" means a group of the formula -O-alkyl-O-, in which the meaning of the alkyl group is as defined above. Alkyleneyloxy groups include methylenedioxy and ethylenedioxy groups. "Alkyl sultinyl-esoport" means a group of the formula alkyl-SO-, in which the meaning of the alkyl group is as previously described. Those alkylsulfinyl groups in which the alkyl group has 1 to 4 carbon atoms are preferred. The "alkylsulfonyl group" means a group of the formula alkyl-SO>-, in which the meaning of the alkyl group is as described above. Preference is given to alkylsulfonyl groups in which the alkyl group has 1 to 4 carbon atoms. The alkylsulfonyl amino ester means a group of the formula alkyl-SOa-NH-, in which the meaning of the alkyl group is as described herein. Alkylsulfonylamino groups include methanesulfonamido and ethanesulfonamido. "Alkythioesoport" means a group with the formula alkyl-S-, in which the meaning of the alkyl group is as described above. Examples of alkyl thioisophores include methylthio, ethylthio, isopropylthio and heptylthio. "Alkynyl-swept" means an aliphatic hydrocarbon group containing a carbon-carbon triple bond and which can be straight or branched, with a chain length of approx. 2 - approx. You have 15 carbon atoms... Carbon atoms between 2 and about 12 in the chain are preferred * groups containing φ; and· are preferable in the chain approx. 2 and approx. containing between 5 carbon atoms. Examples of alkynyl groups include ethynyl, propynyl, n-butynyl, 2-butynyl, 3-methylbut-2-ynyl and n-pentynyl. Aroylisoport"' means a group of the formula aryl-CO-, in which the meaning of arylisoport is as described herein. For example, benzene and 1- and 2-naphthoyl groups are aroyl-swept. "Aroylamino group" is a group with the formula aroyl-NH-, in which the meaning of aroyl is defined above. "Arylisoport" as a group or part of a group (i) is an optionally substituted one-ring or multi-ring aromatic carboxyl molecule, which is approx. 6 and approx. contains between 14 carbon atoms, such as phenyl or naphthyl; or (ii) an optionally substituted partially saturated polycyclic aromatic carboxyl moiety in which an aryl is fused to a cycloalkyl or cycloalkylene ring to form a ring structure such as tetrahydronaphthyl, indenyl or indanyl. The aryl substituents can be substituted by one or more aryl group~ substituents, which can be the same or different, where the "aryl substituent" means, for example, a halogen atom, acyl, acylamino, alkoxy, alkyloxylcarbonyl, alkylenedioxy, alkylsulfinyl, alkylsulfonyl, alkylthio, aroyl, aroylamino, aryl, arylalkenal, arylalkynyl, aralkyloxy, arylalkyloxycarbonyl, arylalkylthio, aryloxy, aryloxyalkyl- . Κ * * · Λ Λ ** * . *♦·♦ * ϊ : * «ϊ*. - — *«♦ F The symbol A' is an oxygen atom, w x? .L t jr -NY1- (OO) -alki i, / given . e s e t, the group with the formula 1kox1-, άηοχϊΐ- or -NY1?'* oáta-kenyl- is the swept meaning of 1. keni .iaí keni . 1 -· group o k tzent. At the Aryans- hydroxyl-, nitro-, trifluoromethyl-, -NY'A, -CONY;Y, -SChNY'Yy -2^-(2-6- carbon atom alkyl'j^-NY^Y2 (where -NR:;:~ or -S 105 ",- esc -NY^SOs-alkyl or swept alkyl, which is substituted by a group of the formula aro.yl-, aryl~, arxyloxy-, beteroaryl 1- . The arylalkenyl group*' means arylalc in which the aryl is swept and as described above. Examples of preferred groups containing carbon alkenyl groups are styryl and phenylallyl. "Arylalkyl-swept" means a group of the formula arylalkyl, in which the meaning of the aryl and alkyl groups is as described above. Preferred arylalkyl groups contain alkyl groups having 1 to 4 carbon atoms. Examples of arylalkyl groups are benzyl, 2-phenethyl, and naphthylmethylisoport. "Aryl.Alkoxy group" means a group of the formula arylalkyl-O-, in which the meaning of the arylalkyl groups is as described above. Examples of arylalkyloxy groups include benzyloxy and 1- or 2-naphthalenemethoxy. group" of the formula arylalkyl-O-CO- *' represents an aryl I:iloxycarbon group. in which he described above. The arylaic zyloxycarbon1-group powder.. The ” ar ϊ 1 ak i.l. t i o—cs ooo r anlaí zir-n-kepietu means a group in which the meaning of the aryl alkyl group is as described above. An example of an arylalkylthio-ceopor is the benzylthio group. £ The meaning of the arylalkynyl group is a group of the formula aryl~a.l, in which the meanings of the aryl-·· and the alkynyl group are as described above. Examples of arylalkyl groups include phenylethyl and 3-phenylbutylene chloroport. The aryloxy group means a group of the formula aryl-O-, in which the meaning of arylisoport is as described above. Examples of aryl groups include optionally substituted phen1.1oxy and naphthoxolospor. "Aryloxyalkyl group" means a group of the formula aryl-O-alkyl, in which the meanings of the aryl and alkyl groups are as described above. Examples of aryloxyalkyl radicals include phenoxymethyl and 1- or 2-naphtholoxymethyl radicals. Arlloxycarbon! swept*' means a group of the formula arii-O-C(~0)-, in which, ariiesoport has the meaning described above. Examples of the aryloxycarbonyl group are phenoxycarbonyl- and naph t ο x i car bon i I.c s opo r t. "Arylsulfinyl group" means a group of the formula aryl-SO-, in which the meaning of arylisoport is as described above. The arylsulfonyl group means a group of the formula aryl-Stb-, in which the meaning of arylisoport is as described above. Azí!ari Itlogroup means a group of formula arii-5-, in which the meaning of ariiesoport is described above. Examples of arylthio groups are phenylthio and naphthylthio. "Azaheteroari 1-group"' means an aromatic carbocyclic molecular part, which has approx. 5 - approx. It has 10 ring members, where one of the ring atoms is a nitrogen atom, and the other ring members are chosen from carbon, oxygen, sulfur and nitrogen atoms. The azahetero··4* Examples of aryl groups include benzimidazolyl, imidazolyl, isoquinoyl, isoxazolyl, pyraziopyrimidine, pyridyl, pyrimidine, quinazolinyl, quinazolinyl and thiazolyl. Cyclic amine means a 3-8-membered monocyclic cycloalkyl ring system, where one of the ring carbon atoms is replaced by a nitrogen atom, and the ring (i) is optionally an additional heteroatom selected from oxygen, sulfur and the group of the general formula -ΜΥ·5-- contains (where Y5 is a hydrogen atom, alkyl-, arylalkyl or arylisoport) and (ii.) can condense with an additional aryl or heteroaryl ring to form a two-ring ring system. Examples of cyclic amines include pyrrolidine-, piperidine-, morloline-, piperazine-, indolin- and pyrindoline ringfc is mentioned, Cycloalkenyl refers to a cycloalkenyl group that is at least one carbon-carbon. contains a double bond. Examples of single-ring cycloalkenyl rings include cyclopentenyl, cyclohexyl, and cycloheptenyl. "Cycloalkyl ester" means a saturated one-ring or two-ring ring system, which is approx. 3 - approx. It contains 10 carbon atoms and is optionally substituted with a group of the general formula oxo-, alkyl-, aryl- or -C(--0-)-NY1Y2. Examples of the single-ring cycloalkyl group include cycloalkyl rings with 3-8 carbon atoms, such as cyclopropyl-, cyclopentyl-, cyclohexyl- and a. cycloheptyl rings are mentioned. Cycloalkyl-alkyl-esoport means a cycloalkyl-alkyl group, in which the meanings of the cycloalkyl and alkyl groups are as described above. Examples of monocyclic cycloalkylalkyl groups include cyclopropylmethyl, cyclopentylmethyl, cyclohexylmethyl and cycloheptylmethyl. The halogen atom. means fluorine, chlorine, or iodine. A fluorine or chlorine atom is preferred. "Heteroaryl-swept" means a heteroaryl-C(--O)-compound group, in which the meaning of the heteroaryl group is as described herein. As an example, we mention the pyryldylcarbonyl group. The "heteroaroylamino group" means a group of the formula heteroaroyl-NH-, in which the meaning of the heteroaryl group is as described above. "Heteroaryl" as a group or part of a group (i) means an optionally substituted aromatic monocyclic or polycyclic organic moiety having approx. S - approx. contains 10 ring members, where one or more of the ring members have different carbon atoms, for example nitrogen, oxygen or sulfur atoms (examples of such groups are benzimiazolyl, benzthiazolyl, benzthiophenyl, phenyl, imidazolyl, indolyl, indolizinyl, isoxazolyl -, isoquinolinyl-, isothiazolyl-, oxadiazolyl-, pyrazinyl-, pyridazinyl-, pyrazolyl-, pyridinium-, pyrimidinyl-, pyrrolyl-, quinazolinyl-, quinolinyl-, 1,3,4-thiadiazolyl-, thi.azolyl- , thienyl and triazolium groups, which are optionally substituted by the substituents of one or more aryl groups, as defined above); í is a substituted, partially saturated polycyclic heteroheteroaryl and a carbocyclic molecular moiety in which a cycloalkyl or cycloalkenyl group is substituted in the given case. condensed into a ring structure (such a group is, for example, the pyrindanyl group; optionally, the substituent present is one or more aryl substituents), as defined above. ϊ *» .ί .** ·»» » * * »·*« "Aryldiyl group" means a divalent group derived from a commodity group, substituted where appropriate. Examples of aryl groups include the optionally substituted phenylene, naphthaene and indanylene groups. Suitable substituents include, but are not limited to, one or more "aryl-swept substituents" as defined above, especially halogen, methyl, or methoxy. The "heteroaryldiyl" group means a divalent group derived from a heteroaryl group as defined above. "Heteroarylalkenyl 1-group" means a group of the formula heteroaryl-alkenyl-, in which the meaning of the heteroaryl- and the elkenyl group is as described above. Preferred hetero4g arylalkenyl groups contain low carbon alkenyl groups. Examples of heteroarylalkenyl esters include pyridyl ethenyl and polyridylallyl. "Heteroarylalkyl" refers to a group with the formula heteroarylalkyl, in which the meanings of the heteroaryl and planar alkyl parts are as described above. Preferred heteroarylalkyl groups contain alkyl groups having 1 to 4 carbon atoms. An example of a heteroarylalkyl group is pyridylmethyl. Heteroarylalkyloxyisoport means a group with the formula heteroarylalkyl-O-, in which the meaning of heteroarylalkyl 1-c. group is described above. Examples of heteroaryloxy groups include optionally substituted pyridylmethoxyisoport. The heteroarylalkynyl group means a group of the formula heteroarylalkynyl, in which the heteroaryl group and the alkynyl group have the meanings described above. HeteroarlIsiken!1~group Ί among others, pyridyletin 1- and 3-pyriöylbut~2~inylswept. The "heteroaryloxy group" means a group of the formula heteroaryl.11.-0-, in which the meaning of the heteroaryl group is as described above. A heteroaromatic group includes, among others, the optionally substituted pyridyloxy group. "Heteroaryloxyalkyl" means a group of the formula heteroaryl-O-alkyl, in which the meanings of heteroaryl and alkyl are as described above. Examples of heteroaryloxyalkyl groups include pyridinium 1- and 2-, 3-, or 4-quinolinyloxymetal groups. The meaning of "heterocycloarkenii-ceoporfc" is approx. A 3-7 ring-membered cycloalkenyl group containing one or more hete atoms selected from oxygen and sulfur or -NY4- (in the formula Y is a hydrogen atom, alkyl-, aryl-, arylalkyl- or alkyloxycarbonyl- group). An example of a heterocycloalkenyl sweep is the 1,2,3,ε-tetrahydropyridine group. The heterocycloalkyl group" (i) means an approximately 3-7 membered cycloalkyl group containing one or more heteroatoms selected from oxygen and sulfur or -NY4- (where Y* is a hydrogen atom, alkyl-, an aryl, arylalkyl or alkoxycarbon group, and which can optionally be substituted with an oxo group (such a group is, for example, piperianyl, pyrrolidine, morphoyl, tetrahydropyranyl and tetrahydrotrophenyl); (ii) optionally partially substituted means a saturated multi-ring heterocarbocyclic molecular moiety in which one or more aryl rings (or heteroaryl rings) and a cycloalkyl with approximately 3-7 rings21 ** »♦ «*** »'* »♦«} * ΐ · »»« * «Ktt -A - * * * 4 * **» 4»* * group, which contains one or more oxygen and sulfur atoms and a neteroatom selected from the group with the formula -NY4áitaian, and which may optionally be substituted by oxo groups, forms a condensed ring structure (such group including the Cromani l", the dichlorobenzofaranyl-·, the indolinyl··· and the pyrindolinyl~ group. "Heterocycloalkylalkyl group" means a group of the formula heterocycloalkylalkyl, in which the heterocycloalkyl group and the alkyl group have the meanings described above. The meaning of the heterocycloalkylalkyloxy group is a group of the formula "heterocycloalkylalkyl-0", in which the meanings of the heterocycloalkyl and the alkyl group are as described above. "Heterocycloalkyloxy" means a group of the formula heterocycloalkyl, wherein heterocycloalkylisoporfc has the meaning previously described. "Ingestive medicine" means a compound that can be administered to a patient without causing any particular toxicity, irritation, or allergic response, and can be converted in vivo metabolically (for example, by hydrolysis) into a compound according to the present invention, including its N~oxide. A thorough study was prepared by T. Híguchí and V. Stella in *'Pro~drugs as heat Delivery Systems ” císsael (A. C. S.· Symposinm. Series vol. 14) and edited by Edward B. Roch entitled af?Bioreversible Carríers in Drug Design”. work {American Pharmaceutical Association and Pergamen Press, 1987), both of which are incorporated herein by reference. For example, the ester of a compound according to the present invention containing a hydroxy group can be converted into the original molecule by hydrolysis, in some cases, a compound according to the present invention. Ester of a compound containing carboxylates with a tying zis. also, it can be converted into the original molecule. Suitable esters of the hydroxyl scavenger-containing compounds according to the present invention are acetates, cyphrates, lactates, tartrates, malonates, oxalates, salicylates, propionates, succinates, fumarates, maisates, methylene bls(P-hydroxynaphthoeth)oc, gentisates, isethienates, di(p -toluenesulfonates, methanesol braids, ethanesulfonates, benzenesulfonates,· p-toluenesulfonates, cyclohexylsulfamates and quinates. A particularly useful group of esters of compounds containing hydroxyl groups according to the present invention can be formed by Sundgaard et al. in J. ófed. üdém,, 32, 2503-2507 (1989·) esters formed with selected acids, including substituted (aminomethyl? benzoates, for example dialkylaminomethyl benzoates, in which two alkyl groups can be connected and / or with an oxygen atom or in a specific case substituted nitrogen atoms, for example interrupted by an alkylated nitrogen atom, more specifically (morphoinomethyl)benzoates, for example 3- or 4-(morphoinomethyl)benzoates, and (4-alkylpiperazine-1-yl)benzoates, for example 3- or 4- -capsicum-l-ildobenzoates. Suitable esters of compounds containing a carboxyl group according to the present invention are, for example, F. <7. According to Leinweber, P. rug is old foam. Aes.z18, 379 (1987). described in the literature. The compounds according to the present invention are basic, and as such compounds can be used in the form of the free base or their pharmaceutically acceptable acid addition salts, Acid addition salts are more suitable for application; In practical hydroliϊ « *»«», the use of salt corresponds to the use of the free base form. The acids that can be used to prepare the acid addition salts preferably include those that combine with the free base to form pharmaceutically acceptable salts, i.e., whose anion is not toxic to the patient at a pharmaceutical dose of the salt, so that the beneficial inhibitory effects of the base are not impaired at the expense of the anion. writeable side effects, although pharmaceutically acceptable salts of basic compounds are preferred, any acid addition salt is useful as a source of the free base form, even if the salt itself is only desirable as an intermediate, such as when the salt is formed only for purification and identification purposes, or when used as an intermediate in the preparation of a pharmaceutically acceptable salt by an ion exchange process. Pharmaceutically acceptable salts within the scope of the invention include salts formed with mineral acids and organic acids, including hydrogen halides, such as hydrochlorides and hydroformides, sulfates, phosphates, nitrates, sulfates, acetates, citrates, lactates, tartrates, malonates, oxalates, salicylates, propionates, succinates, fumarates, mateates, methylene bis(β-hydroxynaphthoate), gentisates, isethionates, di(p-toluoyl;farcarates, methanesulfonates, ethanesulfonates, benzosulfonates, p-toluenesulfonates, cyclohexylsulfamates and .Nats. The salts of the compounds according to the invention can be used by themselves as effective compounds, and they can also be used to purify the compounds, for example by exploiting the differences in the solubility of the salts and the original compounds, the by-product and / or the starting materials, using techniques well known to those skilled in the art.· In the case of compounds of general formula (la) above, the special and preferred groups are a. R1 may in particular represent a hydrogen atom. R2 may in particular represent a hydrogen atom. R'· may in particular represent a commodity group, such as optionally substituted phenyl or optionally substituted naphtha, especially substituted phenyl. The optionally present substituent includes, inter alia, alkyl substituted with one or more halogen atoms or sryl groups, alkyl substituted with aryloxy groups, alkyl substituted with aroyl, alkyl substituted with a heteroaryl group, arylalkynyl, hetero arylalkynyl, aryl, heteroaryl, arylalkene .yl or arylalkyloxy group, in which the aryl or heteroaryl substituents may be further substituted with one or more aryl group substituents. R3 can represent a heteroaryl group, such as optionally substituted pyridine, optionally substituted quinolinyl, optionally substituted thienyl, optionally substituted furanyl or optionally substituted indolyl, especially substituted thienyl, substituted parayl or indolyl isoport . The optionally present substituents include, inter alia, alkyl substituted with aryl groups, alkyl substituted with aryloxy groups, alkyl substituted with aroyl groups, alkyl substituted with heteroaryl groups, arylalkynyl, heteroarylalkynyl, heteroaryl, arylalkenyl, or arylalkyloxy, where aryl or heteroaryl groups can be further substituted by ί« « « with one or more aryl group substituents. R4 in particular can represent a hydrogen atom, R4 can also be a cyano group in particular, especially when it is attached to the tertiary ring carbon atom. Rr may in particular be a hydrogen atom. R? can also mean an alkyl group with particularly few carbon atoms (for example, a metyl group) or a halogen atom (for example, a fluorine atom). Z'\ ---- in particular can mean a / a-e-type j^&small intestine ligature. The value of n can be 2 in particular. Of course, the present invention covers all suitable combinations of the specific and preferred groups mentioned herein. A special group of compounds according to the invention is made up of the compounds of general formula (Ib): in the formula, R3, R4 and R5 mean the above and the corresponding N-oxides and their prodrugs; and pharmaceutically acceptable salts and solvates (eg, hydrates) and oxides and prodrugs of such compounds. : substituting aryl isosporin, so if appropriate, a substituted naphth11 group; yes The preferred group is an alkyl group substituted with one or more aryl groups or heteroaryl groups, where the aryl or heteroaryl groups can be further substituted with one or more aryl group substituents. The meaning of Pb in particular The (lb) general picture; in which R'1 means ari) sited fenii- or given especially the substituted hel present in any case; halogen atom or ary sweeper * * * e < »· * * · * » «- A A · ♦ Λ « «Α ** * dichlorophenyl group (for example, 3,i-dichlorophenylisoport), C1-alkyl)phenyl group (for example, phenethyl), hydroxyphenyl(1-3-carbon alkyl)phenyl group (for example, 4-hydroxyphenylethyl.lphen.yl group) and andanopyridine (C1-3 alkyl)phenyl group [for example (aminopyrid-3-yl)ethylphenyl group], Those compounds of general formula (Ib)· are preferred, in which R3 is heteroaryl, optionally substituted pyridyl-, optionally substituted quinolinyl-, optionally substituted thienyl-, optionally substituted turanic 1- or optionally substituted indol.yl-, in particular substituted thienyl, substituted pyridyl or indodium. Preferred optionally present substituents include, inter alia, alkylisospor substituted with an aryl group and alkylisospor substituted with a heteroaryl group, where the aryl or heteroaryl radicals themselves can be further substituted with one or more arylisospor substituents. R3 is especially phenyl. (C1-3 alkylpyridiisoport (e.g. 5-phenylethyl-pyrid-3-yl), phenyl (C1-3 alkyl)thienyl (e.g. S-phenylethylthien-2) and indoyl (e.g. indol-<6-1 ). Those preferred compounds of general formula (Ib) in which R' is a hydrogen atom. Compounds of formula (ίο) in which Pr is a cyano group are also preferred. P? preferably a. is attached at the 4-position of the piperidine ring. Compounds of formula (Ib) in which R3 is a hydrogen atom are preferred. Those compounds of general formula (ib) in which <-h are also preferred. The meaning of R is an alkyl group with a carbon atom (for example, a methyl group) or a halogen atom (for example, a fluorine atom). R5 is preferably attached to the phenyl ring in relation to the -CHüib group. A preferred group of the compounds of the general formula (Ibi) according to the invention are those compounds in which the meaning of ib is substituted phenyl [especially 3, 4-diphenyl-·, phenethyl-, 4-hydroxyphenylethylphenyl·- and (4-aminopyrid-3-yl) ethylphenylene} or an optionally substituted heteroaryl group (in particular 5-phenylethyl~pyri~3~yl~, S-phenylene.n-2-.yl~ or indoyl-S-yl group}; R4 is a hydrogen atom or a cyano group attached at the 4-position of the piperidine ring ; R" is a hydrogen atom or a lower alkyl group (for example, methyl-swept) or a halogen atom (for example, a fluorine atom) attached to the phenyl ring in the para position relative to the group; and the corresponding N-oxides and their prodrugs; and- pharmaceutically acceptable salts and solvates of such compounds ( for example its hydrates) and their N-oxides and derivatives. Special compounds according to the invention are those which are formed in such a way that the fragments A1-A10 shown in Table I are added via the C* carbon atom to a. It is connected to the C* carbon atom of fragments Β1-ΒΊ2 shown in Table 2, and the N* nitrogen atom of fragments 81-312 is connected to the C* carbon atom of one of the acidic fragments Cl-Cl03 shown in Table 3. * * Taoism # X * * figure •3 Table 3 * * ♦ * > * ♦ * <β* '3 « « * Χ-* « V » X M * 6 «f* * 4 κ w «·« Ω **· * » * * « * * r 9 9 *9 * > φ * * X φ * 9 * *1 «Φ 4^ · Table 4 AI-B1-C1 AÍ-BI-C2 A1-B1-C3 A1-BI-C4 ' A1-B1-C5 A1-B1-C6 AI-B1-C7 AÍ-8I-C8 AÍ-BÍ-C9 AI-B1- CÍ0 Aí-Bí-Cn A1-B1-C12 ai-bi-cb A1-B1-CI4 Al-Bl-Cl 5 A1-B1-C16 Al-Bl-Cl 7 Al-Bl -Cl 8 A1-B1-C19 A1 -B1-C2O AÍ-S1-C2I A1-BÍ-C22 A1-.81-C23 Al-Bl~C24 A1-B1-C25 A1-B1-C26 A t-B 1-027 A1-B1-C28 A1.-B 1 -C29 Al-Bl -C30 AI-B1-C3I A1-BI-C32 A1-B1-C33 AI-B1-C34 A1-BS-C35 A1-B1-C36 A1-BIC37 A.1-B1-C38 AI-B1 -C39 A1-BI-C40 AI-B1-C41 A1-B1-C42 A1-B1-C43 A1-B1-C44 A1-B1-C45 AI-B1-C46 A1-B1-C47 A1-BI-C48 A1-SI -C49 AI-B1-C50 ABB1-C51 A1-B1-C52 A i-31-053 A3-B1-C54 A1-BI-C3S Al-Bl-PIPE Al-Bl-C57 AI-BI-C5S A1-B1- C59 A1-B1-C60 A..1-BI-C61 A1-B1-CŐ2 AI-BI-C63 A1-B1-C64 A1-BI-C65 A;-81-066 A1-BI-C6? A1-B1-C6S A1-B1-CŐ9 A1-B1-C70 A1-B1-C71 Al-Bl-C72 AI-B1--C73 A1-B1-C74 ABBBC75 AI-B.I-C76 Al-Bl--C77 A1- B1-C78 ÁI-B1-C79 Al-Bl-CSö A1-B1-C81 A1-B1--C82 Á1-BI-C83 A1-B1-C84 Ai-m-css A1-B1-C86 A1-B1-C87 AÍ -B1-C88 A1-B1-CS9 AÍ-B1-C90 A1-S3-C91 AI-BI-C92 A1-B1-C93 A1-B1-C94 A1-B1-C95 A1-B1-C96 AI-81--C97 A1-BI-C9S A1-B1-C99 Al-Bl-ClOO Al-Bl-Cl 01 A1-BI-C102 A1-BI-C103 A1B1-C104 A1-B1-C1Ö5 Al-Bl-Cl 06 A1-B1-C107 Al-Bl-ClöS Al-BMC 109 AI-B1-C11Ö Al-Bl-Cili Al-Bl-Cl 12 Al-Bl -Cl 13 Al-Bl-Cl 14 Á1-BI-CH5 Ál-B1-0i horse A1-B1-CU7 A1-BLC118 ALB1-CH9 A1-81-Cl 20 A LB1-0121 A1-B1-O122 Ál-Bt-Cl23 A1-B1-C124 A1-BI -C125 A1-BJ-C126 Al-81-0127 Al-81-0128 A1-81-0129 A1-BLC130 AI-B1-CT3I A1-8LC132 ALS1-0133 A !~B 1-C134 A1-81-C135 A1- B1-C136 A1-B1-C137 . A1-BJ-C13S 5 Ál-B1-0139 AI-81-CI4Ö BLANK. BLANK BLANK BLaNK A1-B2-CI A1-82-02. A1-82-03 A1-82-C4 A1-B2-C5 ALB2-C6 A1-B2-C7 A1-82-08 AL82-C9 A1-B2-CÍÖ ÁJ-82-0 Π A1-B2-C12 A1-B2 -C13 A1-.B2-C14 A1-82-0 IS AÍ-B2-C16 A1-82-017 A1-B2-C1S A1-B2-C19 A1-82-020 A1-82-021 Ál-82-022 A1 -B2-C23 Ál-82-024 10 A1-B2-C2S A1-82-026 A1-82-027 Á1-B2-C2S Ál-82-029 A1-82-030 A1-B2-C31. A1-82-032 A1-B2-C33 A1-B2-C34 AI-B2-C35 AI-82-035 A1-82-C37 AI-B2-C38 A1-82-039 AI-B2-C40 A1-82-041 A;-82-042 A1-B2-C43 AI-82-C44 AI-82-C4S A1-B2-C46 A1-82-047 AI-82-048 Á1-82-049 ALB2-C50 Al-82-051 ΑΧ -82-052 A1-B2-C53 A5-B2-CS4 15 A.1-B2-C55 AI-B2-C56 A1-B2-C57 A1-B2-C5S A1-82-O59 Á1-B2-C60 Á1-B2 -C61 A1-B2-OŐ2 Á1-S2-CŐ3 A1-82-064 A1-82-065 A :-.82-006 A1-82-067 A. 1-82-068 A1-B2-C69 A1-B2- C70 A1-82-071 A1-B2-C72 A1-B2-C73 A1-82-074 A1-B2-C75 A1-B2-C76 A1,82-077 A1-82-078 A.I-B2.-C79 A1-B2 -C80 A1-82-081 A1-B2-C82 * A1-B2-C&3 AI-B2-CS4 20 A 1-82-085 A1-B2-CS6 A1-B2-CS7 A1-82-038 A1-B2-C&9 A1-82-090 AAB2-C91 A1-B2-C92 A1-B2-C93 A1-B2-O94 Λ1-82-095 ALB2-C96 AL-B2-C97 AI-B2-C98 A1-82-C99 A1-B2- CI00 A1-.82-CICH A1-B2-C102 A1-B2-C103 A. 1-82-0104 A1-82-0105 AI-B2-C1G6 A1-B2-C107 A1-82-0108 A1-B2-O109 A1 -B2-C110 A1-82-0111 A1~B2-CU2 A1-B2-C113 A1-B2-CÍ14 25 A1-B2-O15 A1-82-0116 Al-82-0117 Α1~Β2~ΟΠ8 A1-82-0119 AI-B2-CJ2Ö AÍ-B2-C121 Ál-82-0122 A1-82-0123 A1-B2-C124 A.1-82-C125 A1-B2-C426 A1-.B2 -C127 ANB2-C128 Á1-S2-CI29 A1-B2-C130 A1-B2-C131 Al-82-0132 A 1-.8:2-0133 A1-62-0134 A1-82-0135 Al-82-0156 AI -B2-C137 A1-B2-CJ38 A1-B2-C139 A1-82-0140 BLANK B.LANK BLANK BLANK 30 A1-B3-C1 A1-B3-C2 A1-83-03 A1-83-04 False-83- 05 ÁNB3-C6 A1-B3-C? A1-B3-C8 A1-83-09 At-83-010 Α1-Β3-ΟΠ A1-B3-C12 A 1-.83-013 A1-83-014 A1-83-C1S A1-B3-C16 A1 -83 -Cl 7 A1-B3-C18 Pseudo-83-019 A1-B3-C20 A1-83-C21 A1-B3-O22 A1-83-023 A1-83-024 Pseudo-83-025 Pseudo-83-026 A1- B3-C27 Al-83-028 A1-83-029 A1-83-030 35 A1-83-031 A1-B3-C32 A.I-B3-C33 AI-B3-C34 A1-B3-C35 A.l-83-036 A1 -B3-C37 A1-83-03 8 A1-B3-C39 A1-B3-C4O Al-83-041 A1-B3-C42 ,4.1-.83-043 A1-B3-C44 A.1-B3-C4S A1 -B3-C46 A1-83-047 A1-B3-C43 λ « χ. V (S « a Á1-B3-C49 A1-B3-C5Ö A1-B3-C51 A1-B3-C52 A1-B3-C53 A1-B3--C54 A1-B3-C55 A1-B3-C56 A1-B3- C57 A1-B3-C58 A1-B3-C59 A1-83-060 ANB3-C61 Á1-B3-C62 A1-B3-CŐ3 A1-.B3-CŐ4 AI-B3-C65 A1-83-066 ÁÍ~B3-Cő AI~S3~C6§ A1-B3-C69 Á.I-B3-C7Ö Á1-B3-C71 A1-83-C72 5 ÁI-B3-C73 A1-B3-C74 ÁÍ-B3-C75 A1-B3-C76 A1~83~C77 A1-B3-C78 Á1--B3-C79 A1-B3-C80 A1-B3-C8I A1-B3-C82 ÁI-B3-C83 A1-83-084 ABB3-C85 A!~B3-C86 A1-B3-C87 Al~B3~C88 A1-B3-C89 A1-B3-C90 A1-B3-C91 A1-B3-C92 Ai~B3~C93 A1-B3-C94 A1-B3-C95 ÁÍ-B3-C96 A1-B3-C97 A1-B3-C98 A1-B3-C99 Á1-B3-C1ÖÖ A1-B3-C1ÖI Ai~B3~C102 lö A1-B3-C1Ö3 AI-B3-GI04 A1-B3-C1G5 AÍ-B3- C1Ö6 A1~83~C.1O? A1-B3-C116 AJ--.83--0117 A1-83-0118 ABB3-C119 A 1-83-0120 Α1--Β3~€12ϊ A1-B3-C122 AI~B3~C123 A1-B3-CÍ24 A1 -B3-C125 A1-B3-C126 A1-B3-C127 AI-B3-CI28 A1-B3-CI29 A1-B3-CÍ3Ö AI-B3-CB1 A1-33-C132 15 AI-B3-CÍ33 A1-B3-C134 A1-B3-C135 ALB3-C136 A!~B3~CB7 A1-B3-C138 A1-Ö3-C139 AÍ-B3-CM& BCANJG BLANK BLANK BL ANK A1-B4-Ü1 AI-B4-C2 - A1-B4-C3 A1-B4-C4 Ai~B4~C5 A1-B4-CŐ Á1-B4-C7 A1-B4-C8 AI-B4-C9 Á1-B4 -C10 Al-B4-Cri A1-B4-C12 Al~B4~C13 A1-B4-C14 A1-B4--C15 A1-B4-C16 ' ABB4-C17 AI-B4-C1S 20 Á1~B4~€19 Á1 -B4-C20 AI-B4-C2I A1-S4-C22 A1-B4-C23 A.1-S4-C24 A1~B4~C25 Al -B4~C26 A1-B4-C27 A1-B4-C28 AÍ-84- C29 A1-B4-C30 A1-B4-C31 A1-B4-C32 Á1-B4-C33 AI-B4-C34 A1-B4-C35 A1-B4-C36 A1-B4-C37 A1-B4-C38 A1-B4- C39 ABB4-C40 A.Í~134~C4i A2-B4-C42 AL-B4-C43 A1-B4-C44 ANB4-C4S A1-B4-C46 A1-B4-C47 Á1-B4-C48 25 AI-B4-C49 A.1-B4-C58 A1-B4-C51 A1-B4-C52 A1-B4-C53 A1-B4-C54 A1-B4-C55 A1-B4-CS6 AI-B4-C57 A1-B4-C58 A1-B4 -C59 A1-B4-C6Ö A1--B4-C61 A1-B4-C62 A1-B4-C63 A1-B4-C64 A1-B4-C65 A Ϊ -B4-C66 ANB4-C67 AI-B4-C68 A1-B4 -C69 A.1-B4-C7Ö ÁI-B4-C71 A1-B4--C72 A1-B4-C73 AI-B4-C74 A1-B4-C75 A1-B4-C76 A1-B4-C77 A2-B4-C7S 30 AI-B4-C79 Al-B4~C8Ö A 1--.84-(381 A1-B4-CS2 Á1-B4-C83 Al-84--084 ABB4-CS5 A1-B4-C86 AI-B4-C87 AI ~B4~CSS Á2-84-C89 A1-84-090 ÁIB4-C9! AI-B4-C92 Á1-B4-C93 A1-B4-C94 A1-B4-C95 A1-B4-C96 A1B4~C97 A1-B4-C98 A1-B4-C99 AI-B4-C100 A1-B4-CIQI A1- B4-C1Ö2 A1-B4-C103 A1-B4-C104 A1-B4-C1Ö5 A1-B4-C1Ö6 A1-B4-C107 A1-84-008 •χ ·; Α1~Β4~€1Θ9 A1-B4-C110 Al -B4-CI11 A1-B4-C112 A1-B4-CH3 A1-.84-C114 A1-B4~C.il 5 Al--B4-.Ü11 δ Al- B4~€n? A1-B4-C1I8 A.1-B4-C119 Ai~34~Ci20 Ai-B4~Ci2i A1-B4-C122 Α1·-Β4~€123 A1-B4-CI24 A1-B4-CJ25 ΑΙ-Β4Ό26 * ¢. THE J » « Á1-B4-C127 A1-B4-C128 Ai~B4-Ci29 A1-B4-C130 A1-BGC131 A1-B4-C132 A1-04-033 A1-B4-C134 A1-B4-CI35 AI-B4-C136 A1- B4-C137 A1-B4-C138 Al~34~CB$ A1-B4-C140 8LANK BEÁNK BEÁNK BEÁNK A1-B5-CI A1-B5-C2 AI-BS-C3 A1-B5-C4 A.1-B5-C5 AEB5-C6 AI-B5-C7 AE.B5-CS A1-B5-C9 AI-B5-CW A1-B5-C11 A1-B5-C12 A3-B5-CI3 A1-B5-C14 AI-B5-C15 A1- B3-C16 A1-B5-C17 A1-B5-C18 A1-B5-C19 AI-B5-C20 A1-B5-C21 AGBS-C22 A1-B5-C2.3 A1-B5-C24 A1-B5-C25 A1- B5-C26 A.1-B5-C27 A1-B5-C28 A.1-BS-C29 A1-B5-C30 A1-B5-C31 A1-B5-C32 A1-B5-C33 A1-B5-C34 Á1-B5 -C3S AI.-BS-C36' A1-B5-C37 A1-B5-C38 A1~B5-Ü.3.9 A1-B.5-C4O A1-B5-C4Í AÍ-B5-C42 AGBŐ-C43 A1-B5- C44 A.I-B5-C4S AI-B5-C4Ó A1-B5-C47 A1-135-C48 AÍ-S5-C49 A1-B5-C5Ö AE.B5-C5Í A1-B5-C52 A1-B5-C53 Al -B5- C54 A1-B5-CS5 A.1-B5-C56 A1-B5-C57 A1-BS-C58 A1-B5-C59 AI-B5-C6Ö AI-B5-C61 A1-B5-C62 A.1-B5-C63 A1-BS-C64 A1-B5-C65 AGB5-C64 AG85-C6? 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A2-BS-C88 A2-BS-C89 A2-B8-C90 A2~B8~C9I A2-B8-C92 A2-B8-C93 A2-88-C94 Á2-B8-C95 A2-B8-C96 A2-B8-C97 A2-B8-C98 A2-B8-C99 A2-B8-C10Ö A2-B8-C101 A2-B8-C102 35 A2-B8-C103 A2-B8-CKM A2-B8-CW5 Á2-B8-C106 A2-B8- C1Ö7 A2-B8-C1Ö8 A2-B§~C109 A2-B8-C11Ö Á2-B8-C11Í A2-B8-CH2 Á2-B8-C! 13 A2-B8-C.H4 A2-S8-CI55 A2-B8-C116 A2-B8-C117 A2-B8-CH8 A2-BS-CU9 A2-BS-C12Ö A2-B8-C121 A2-B8-CI22 A2-B8-CI23 A2-BS-ÜI24 A2-B8-C125 A2-B8-C126 Α2-438-027 A2-B8-C128 A2-B8-O29 Á2-B8-CÍ30 A2~B8~C!3í A2-B8-O.32 A2-B8-CN3 Á2-B8-CÍ34 A2-B8-C135 A2-B8-C136 A2-B8-C137 A2-B8-CI38 A2-B8-C. 139 A2-BS-C140 BLANK BLANK BLANK BLANK A2-B9-C1 Á2-B9-C2 A2-B9-C3 A2-B9-C4 A2-B9-C5 A2-B9-C6 A2-B9-C7 A2-B9-C8 A2-B9-C9. A2-B9-CW A2-B9-C! 1 A2-S9-CÍ2 A2-B9-Ü13 A2-B9-C14 A2-B9-C15 A2-B9-C16 A2-B9-C17 A2-B9-C18 A2-B9-O9 A2-B9-C2Ö A2-B9- C21 A2-B9-C22 A2-B9-C23 A2-B9-C24 A2-B9-C25 A2-B9-C26 A2-B9-C27 A2-B9-C28 A2-89-C29 A2-B.9-C30 A2- B9-C31 A2-B9-C32 A2-B9-C33 A2-B9-C34 A2-B9-C35 A2-B9-C36 A2-B9-C37 A2-B9-C38 A2-B9-C39 A2-B9-C.40 A2-B9-C4I A2-B9-C42 Á2-B9-C43 A2-B9-C44 A2-B9-C45 A2-B9-C46 A2-B9-C47 A2-B9-C48 A2-B9-C49 A2-B9-C5Ö A2-B9-C51 A2-B9-C52 A2-B9-C53 A2-B9-C54 A2-B9-C55 A2-B9-C56 A2-B9-C57 A2-B9-C58 A2-B9-C59 A2-B9-C60 A2-B9-C6! A2-B9-C62 A2-B9-CŐ3 A2-B9-C64 A2-B9-C65 A2-B9-C66 A2-B9-C67 A2-B9-C68 A2-B9-C69 Á2-B9-C70 A2-B9-C71 A2-S9-C7.2. A2-B9-C73 A2-B9-C74 A2-B9-C75 A2-B9-C76 A2-B9-C77 A2-B9-C78 A2-B9-C79 A2-B9-C8G A2-B9-C81 A2-B9-C82 Α2-Β9·ΌΜ A2-B9-C84 A2~.B9-C8.5 A2-B9-C8Ó' A2-B9-C87 A2-B9-C88 4 A2-B9-C89 A2-B9-C90 A2--B9- C91 A2-B9-C92 A2-B9-C93 A2-B9-C94 A2-B9-C95 A2-B9-C9Ð A2-B9-C97 A2-B9-C9S A2-B9-C99 A2-B9-C10O A2-B9- C10I A2-B9-C102 A2-B9-C103 A2-B9-C104 A2-B9-C1C5 A2-B9-C106 A2-B9-C10? A2-B9-C1Ö8 A2-B9-C109 A2-B9-CÍ1G A2~B9-C)I1 A2-B9-C112 A2-B9-CH3 A2-B9-C114 A2-B9-CK5 A2-B9-CII6 A2-B9 -C117 A2-B9-C118 A2-B9-C119 A2-.B9-C120 A2-B9-CI21 A.2-B9-Ü.I22 A2-B9-C123 A2~B9~C124 A2-B9-C125 Á2-B9 - ADDRESS 2Ð A2-B9-C12? A2-B9-C128 A2-B9-C129 A2-B9-C130 A2-B9-O31 A2-B9-C132 A2-B9-O33 A2-B9-C134 A2-B9-CD5 A2--B9-CI36 A2-B9- C137 A2-.B9-C138 A2-B9-CÍ39 Λ2-Β9-Ο40 BLANK BLANK. BLANK BLANK A2-B10-CI A2-B1Ö-C2 A2-810-C3 A2-B1Ö-C4 A3-BIÖ-C5 A2-B10-C6 A2--.5.10-0 7 A2-B10-C8 A2-B10-C9 A2-B10-C1O A2-B10~Cii A2-B1Ö-C12 A2-BW-CI3 A2-BÍ0-CM A.2-BW-C15 A2-BW-C1Ó A2-810-C17 A2-B10-08 A2-BI .0-CJ9 A2-B1Ö-C20 A2-B10-C21 A2-BIÖ-C22 A2-BW-C23 A2-B10-C24 A2-B10-C25 A2~.B ÍÖ-C26 A2-B1G-C27 A2-BI0- C28 A2-BÍÖ-C29 A2-B16-C30 Á2-B1Ö-C31 A2.-B10-C32 A2-BK4C33 A2-B10-C34 A2-BÍ0-C35 A2-B10-C36 A2-B1Ö-C37 A2-B1Ö-C38 A2-B19-C39 A2-BW-C49 A2-B10-C4! A2-B10-C42 A2-B10-C43 A2-BIÖ-C44 Á2-B10-C45 A2-B10-C46 A2-BÍ0-C47 A2-B1Ö-C48 A2-B10-C49 A2-B1 ö-CSö A2-B1Ö- C5I A2-BI0-C52 A2-B10-C53 A2-B1Ö-C54 A2-B1O-C55 A2-B10-C56 Á2-B10-CS7 A2-BI0-C58 A2-S.IÖ-C59 A2-B10-C60 A2-BI0-CSI .A2-B1Ö-C62 Á2-B10-CŐ3 A2- B10-C64 Á2-8Í0-CŐ5 A2-BI0-C66 A2-B1Ö~C6? A2-310-C6S A2-B10-C69 A2-B1O-C7Ö A2-B10-C71 A2-BW-C72 A2-31Ö-C73 A2-BJÖ-C74 A2-BÍ0-C75 A2-B10-C76 A2-B10-C77 A2-B1Ö-C78 5 A2-3IÖ-C79 A2-BÍÖ-C8Ö A2-8IÖ-C81 A2-R1Ö-C82 A2-3W-C83 A2-B10-C84 A2-B10-C85 Á2-810-CSő Á2-B1Ö- C87 A2-B1Ö-C8S A2-B10-CB9 A2-810-C90 A2-B1Ö-C9I A2-B10-C92 A2-BI0-C93 A2-B18-C94 A2-B10-C95 A2-BKLC9Ő A2-B10-C97 A2 -B10-C9S A2-B10-C99 A2-B10-000 A2-B10-001 A2-B10-C102 A2-BW-CI03 A2-BÍO-O04 A2-BI0-CT05 Á2-B1Ö-C106 .Ά2-Β10-007 A2-BÍ0-C108 ΙΘ A.2-B1Ö-CI09 A2-B10-C1ÍO A2-810-CÜ1 A2-B10-C112 A2-B10-O13 A2-S1Ö-CH4 A2-B10-C1Í5 A2-BÍÖ-CJ1Ő A2~ B1Ö-C117 A2-B1Ö-C118 A2-B10-0 19 A2-B10-C120 Α2-Β10-C i 2 · Α2-.Β10Ό22 A2-B10-CÍ23 Á2-BIÖ-O.24 A2-810-025 A2- 810-CI2Ö A2-B10-C127 A2-B10-028 A2-B10-029 A2-B10-O3O A2-B1G-C131 A2-B10-032 A2-BIÖ-C133 A2-S1Q-CI34 Á2-B10-CB5 A2- B10-C13Ó A2-B10-C137 A2-BI0--C138 15 A2-B10-C139 A2-BI0-C140 3ÍANS BLANK BLANK BLANK A2-BÍ.I-C1 A2-81Í-C2 A2-B11-C3 A2-B11- C4 A2-B.11-C5 A2-B11-C6 Á2-BIÍ-C7 A2-BJ1-C8 A2-BI1-C9 A2-B11-00 A2-BÍÍ-C1Í A2-B11-C12 A2-BH-C13 A2 -S11-04 A2-B11-05 Á2-B11-C 16 A2-B11-O7 A2-B1I-CJ8 Α2-ΒΠ-Ο9 A2-B11-C20 A2-B1Í-C21 A2-B11-C22 ' A2-BU- C23 A2-BU-C24 20 A2-fö 1Í-C25 A2-BH-C2Ő A2-B11-C27' A2-B11-C28 A2-B11-C29 A2-B11-C30 A2-B1 Í-C3.1 A2-BH -C32 A2-B11-C33 A2-B1I-C34 A2-B1NC35 A2-BIBC36 A2-S11-C37 A2-BU-C38 A2-BU-C39 A2-B11-C40 A2-ÖL1-C41 A2-B11-C42 Α2- ΒΠ~€43 A2-BI1-C44 A2-B11-C45 A2-B11-C4Ő A2-B11-C47 A2-B11-C48 A2-B11-C49 A2-B11-C50 A2-B11-C51 A2-BU-C52 A2 -Ö11-C53 A2~B1I-CS4 25 A2-B11-C55 A2-BU-C56 A2-B11-C57 A2-B11-C58 A2-B11-C59 A2-B11-C6Ö A2-BU-C61 A2-BH-C62 A2-B11-C63 A2-B1.1-CŐ4 A2-ÖI1-C65 A2-B11-C66 A2-BÖ-CÖ7 A2-BH-CŐ8 A2~Bn-C69 A2-BU-C70 A2-B11-C71 A2-BM -C72 A2-B1Í-C73 A2-BU-C74 A2-Ö11-C75 A2-BÍ1-C7Ő A2-BI1-C77 A2-B11-C7S A2-B11-C79 Α2-ΒΪ 1-CSÖ A2-ÖI1-C81 A2~ B11~C82 A2-B1LC83 A2-B11-C84 30 A2-B1I-C85 A2-B11-C86 A2-BH-C87 A2-B11-C88 A2-B11-C89 A2-811-C90 A2-BM-C91 A2-B11 -C92 A2-BH-C93 A2-B11-C94 A2-BH-C9S Á2-BU-C96 Α2-Β 11-C97 A2-BÍ 1-098 Á2-BH-C99 ,42-Bll-ClöQ A2-BH-C101 A2-B11-002 Α2-ΒΠ-Ο03 A2-B11-C104 Α2-ΒΠ-Ο.0 5 Α2-8Π-Ο06 A2-B11-007 A2-B1I-C3O8 Λ2-ΒΠ~α09 A2-B11-O10 A2-BI1-C1Í1 A2-B11-C 112 Α2-ΒΠ-Ο13 A2-BN-C114 35 Α2- ΒΠ~€115 A2~Bli-CU6 A2-B11-C.1.17 A2-B11-CH8 Α2-ΒΠ-Ο19 A2-B11-C12Ö Α2-ΒΠ-Ο21 Α2-ΒΠΌ22 A2-S11-C123 A2~B 11-024 A2-B11-CI25 Α2-ΒΠ-Ο20 Α2-Β Π-Cl 27 A2-B11-028 A2-B11-C129 ZÍ2-B11-C130 A2-BH-C131 A2-B11-032 Α2-Β s1 -CDi í A2-B11-C134 a2-bu~cb: 5 A2-B11-CB6 A2-BU-C13' 7 Á2-B11-038 Α2~ΒΠ~Ο35 » A2.-B11~C!4Ö BLANK BLANK BLANK A2-B12-C1 A2-B.12-C2 A2-B12-C3 A2-B12-C4 A2-B1.2-C5 A2-B12-C6 A2-BI2-C7 A2-BI2-C8 A2- B12-C9 A2-B12-C10 A2-B12-OÍ A2-BI2-O2 Á2-B12-CI3 A2-BI2-CH A2-BI2-CI5 A2-.B12-CÍ6 Á2-812-O7 Á2-BI2-C1S A2 -B12-C19 A2-BX2-C20 A2-B12-C21 A2-B12-C22 A2-B12-C23 A2-B12-C24 A2-B12-C25 A2-B12-C26 A2-B12-C27 A2-B12-C28 Á2 -B12-C29 A2-B12-C30 A2-B12-C3I A2-BI2-C32 A2-B12-C33 A2-B12-C34 A2-B12-C35 A2-S12-C36 A2-BI2-C3? A2-B12-C38 A2-B12-C39 A2-B12-C40 A2-812-C41 A2-B12-C42 Á.2-B12-C43 A2-BÍ2-C44 A2-B12-C45 A2-B12-C4Ð A2-B12 -C47 A2-BÍ2-C48 Á2-B12-C49 A2-B12-C5G A2-SI2-C51 A2-B12-C52 Á2-312-C53 A2-B12-C54 A2-.812-C55 A2-B12-C5Ó A2- BI2-C57 A2-B12-C58 A2-B12-C59 A2-B12-CÓ0 A2-Ö.Í2-CŐI A2-B22C62 A2-B12-CŐ3 A2-B12-C64 A2-B.Í2-C65 A2-B 1.2- CŐó A2-B12--CŐ? Á2-BI2-C68 A2-B12C69 A2-B12-C70 A2-B12-C71 A2-B12-C72 A2-B12-C73 A2-B12-C74 Á2-B12-C75 A2-B12-C7Ð A2-B12-C77 A2- B12-C78 A2~B12~C79 A.2-BÍ 2-C80 A2-B12-CS1 A2-B12-C82 A2-B12-C83 A2-B12-C84 A2-B12-C85 A2-B12-C86 A2-B12- C87 A2-B12-CS8 A2-B12-CS9 A2-BI2-C9G A2-BI2-C9.1 A.2-BI2-C92 A2-SI2-C93 A2-B12-G94 A2-S22-C95 A2-B12-C96 A2-BÍ2-C97 A2-B12-C98 A2-B12-C99 A2-B12-CI07 A2-B12-OOÍ A2-B12-CI02 A2-.B12~C.1Ö3 A2-BI2-CW4 A2-B12-C105 A2- B12-006 Λ2-Β12-007 A2-BÍ2-CÍ08 A2-B12.-C1Ö9 A2-B12-C110 A2-8.12-CNJ. A2-B12A112 Α2-ΒΙ2Ό13 A2-BI2-O14 A2-B12-C1.15 A2-B12-C11Ő A2-B12.C117 A2-BI2-C118 A2-B12-019 A2-B12-C12O A2-B12-C121 A2-B12-C121 BÍ2-C122 A2-B12-O23 A2-B12-C.124 A2-B12-O25 A2-B12-026 A2-BI2-C12.7 A2-B12-C12S A2-B12-O29 A2-B12-C13Ö A2-B12 -O31 Á2-B12-O32 A2-B12-C133 A2-B12-034 A2-B12-O35 A2-R12-CB6 A2-B12-037 A2-B12-O38 Á2-B 12-03.9 A2-B 12-0.40 BEÁNK BLANK BEANS BLANK. A2-B13-O A2-B13-C2 A2-B13-C3 A2-BI3-C4 A2-B13-C5 A2-BB-C6 A2-BI3-C7 A2-B13-CS A2-B13-C9 A2-B13-00 A2-B13-01 A2-B13-02 A2-B13-CI3 A2-B13-C14 A2-B13-CÍ5 A2-B13-C16 A2-B13-C17 A2-B13-O8 A2-B13-O9 A2-B13-C20 A2-B13-C2; A2-B13-C22 A2-BI3-C23 A2-BI3-C24 A2-B13-C25 A2-BI3-C26 A2-B13-C2? A2-B13-C28 A2-B13-C29 A2-B13-C30 AABI3-C31 A2-B13-C32 A2-B13-C33 A2-SI3-C34 A2-B13-C3S A2-B13-C36 A2-B13-C37 A2- BI3-C38 A2-BJ3-C39 A2-B13-C40 A2-B13-C41 Á2-S13-C42 A2-B13-C43 A2-B13-C44 A2-BI3-Ü45 A2-B13-C4Ó A2-B13-C47 Á2- BI3-C48 A2-BB-C49 A2-B13-C59 Á2-BJ.3-C51 A2-BI3-C52 A2-BI3-C53 A2-BI3-C54 A2-B13-C55 A2-B13-C56 A2-B13-C57 A2-B13-C58 A2-B13-C59 Á2-B13-C6Ö A2~B13-Có'I A2-BI3-C62 A2-B13-CŐ3 A2-B13-CÖ4 A2-B13-C65 A2-B13-CS6 ". »» »· ϊ * ? .. «>κ<* **<*Λ— bb A2-BÍ3-C6? 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A12-B9-C8 A12-B9-C9 A12-B9-C.1Ö A12-B9-O1 A12-B9-C12 A22-B9-O3 A.12-B9-C14 A.12439-0 5 AI2439-C16* A12 -B9-O7 A12439-08 20 A12-S9-C19 AÍ2-B9-C20 A12-B9-C21 A12-B9-G22 AI2-89-G23 A12-B9-C24 A12-B9-C25 A12-B9-C26 A. 12-B9-C27 A12-B9-C2S A12-B9-C29 AÍ2-B9-C3Ö A12-B9-C31 AÍ2-B9-C32 A12-B9-C33 Á12-B9-C34 A12-B9-C35 A12-B9-C36 A12-B9-C37 A12-B9-C38 A12-B9-C30 A12-B9-C40 A12-B9-C4I A12-B9-C42 A12-B9-C43 A12-B9-C44 A12-B9-C45 A12-B9-C46 AI2-S9-C47 A.12-B9-C48 25 Á12-B9-C49 A12-S9-C5Ö A12-39-C5Í AI2-B9-C52 A12-S9-C53 A12-B9-C54 AJ2-B9-C5S A12- B9--C56 A12-894357 A12-B9-C58 A12-B9-C59 AI2-B9-C60 Á12-B9-C61 A12439-02 A12-B9-C63 A12-B9-CŐ4 ÁI2-B9-C65 AI2-B9-C66 A12-B9-C67 A12-B9-C68 A12-89-C69 ÁI2-B9-C7Ö A12-B9-C71 A12-B9-C72 Á12-B9-C73 A12-B9-C74 A12--B9-C75 A12-B9- C7Ő A12-B9-C77 A12-B9-C7S 30 A12-B9-C79 A12-B9-C8Ö Α12-Β9Ό! A.12-B9-C82 A12-B9-C83 A12439-CS4 AI2-B9-C85 A12-B9-C86 A12-89-CS7 A12-B9-C88 A12-B9-C89 A12-B9-C.9Ö A12-B9 -C91 A12-B9-C92 Á12-B9-C93 A12-B9-C94 AI2-B9-C95 A12-B9-C96 AI2-B9-C97 A12-B9-C9S A.I2-B9-C99 A12439-0 00 A. I2-B9-O91 AI2-B9-CI02 A12-.B9-O03 A12-B9-C1Ö4 A12-B9-OOS A12439-0 Üó A12-B9-O07 A12-B9-C108 35 A12-B9-O09 A12-B9- CU0 Á12-B9-C11.1 A12-B9-CII2 A12-S9-O13 A12-B9-O14 A12-B9-CU5 A12-B9-CH6 AI 2-139-01? AI2-B9-OI8 A12-S9-O19 A12-89-0 20 AI2-B9-O21 A12-B9-C122 ÁI2-B9-O23 A12-B9-C124 A12439-O25 A12439-026 A12-B9-C127 Α12-Β9Ό28 AI2-B9-O29 - AL2-B9-O30 Á12-B9-O31 A12-B9-O32 A.Í2-B9-CO3 A12-B9-O34 A12-B9-O35 A.12- B9-O3Ő A12-B9-O37 A12-B9-C138 Α12-Β9-Ο39 AI2-B9-O40 BLANK BLANK ΒΙ.,ΑΝΚ. BLANK Α12-Β10-Ο A12-S10-C2 A12-B10-C3 A12-B10-C4 A12-B10-C5 A12-B10-C6 5 A12-B10-C7 Dummy 2-B 10-C8 A12-B10-C9 A 12-B 10-00 Á12-810-CN A12-B10-O2 A12-BI0-CB A12-B10-O4 A12-B 10-0 5 AI2-BJ0-CI6 A 12-B 10-07 A12-B10-Clg AÍ2-B10-CI9 AI2-BW-C20 A12-B1.0-C21 Á12-B10-C22 A12-B10-C23 AÍ2-B10-C24 A12-B10-C25 A12-BI0-C26 A12-B10-C27 A12-B10 -C28 AI2-B10-C29 A12-B10-C30 A12-B10-C3I A12-B 3 0-C32 A12-B10-C33 A12-B10-C34 AI2-BIÖ-C35 A12-B1Ö-C36 10 Á12-BIÖ-C37 A12-B10-C38 A12-B1Ö-C39 A12-B10-C40 A12-BIÖ-C41 A12-B1Ö-C42 A12-B1Ö~O3 A12-B1Ö-C44 A12-B1Ö-C45 A12-B10-C46 Á12-B10-C4 ? AÍ2-B1Ö-C48 A12-B10-C49 AI2-B1O-C50 Á12-B10-C5Í A22-B1Ö-C52 A12-B1O-C53 A12-B10-C54 ÁI2-BIÖ-C55 A 12-B 10-CSö A12-B1Ö -C57 A12-B10-C58 A12-BÍÖ-C59 A12-B10-C60 AI2~B!Ö~Cói AÍ2~B1Ö~C62 A12-B10-C63 Λ12-Β10364 A12-B10-C65 A12-B10-C66 35 A12- B1Ö-C67 A12-B1Ö-C68 ÁÍ2-B10-OŐ9 AI2-BI0-C70 A12-B10-C71 A12-B10-C72 Á12-B10-C73 AI2-BIÖ-C74 ÁI2-B.10-C75 A12-B10-C7Ő Α12-δί0-€77 AI2-B1Ö-C78 A12-B1Ö-C79 AI2-B1Q-C80 A12-B1O-C81 A12-B10-CS2 A12-B1Ö-C83 AÍ2-BÍ0-C84 A120104385 A12-B10-C86 Á.12 -B30-CS7 AÍ2-B1.0-C88 A12-B1Ö-C89 A12-B10-C9O A12-B.10-C9I A12-B10-C92 A 12-B 10-033 AI2-B.10-C94 A12-BI0 -C95 A12-B10-C96 20 AÍ2-B10-C97 A12-B10-C98 A12-B10-C99 A12-B10-C100 A12-B 10-0 01 A 12-B 10-0 02 A12-B10-OO3 A12- B10-OO4 Á12-B10-C105 A12-B 1Ö~C 106 A12-B1O-O07 A 12-B 10-008 AÍ2-BI0-C109 AI2-S1O--CÍ10 A n-Blö-C ni AI2-B1Ö-C112 A12-BW-OB A I2-B10-C.114 A12-B10-C115 A 12-B 10-016 Á.12-B10-C117 A12-B1Ö-OI8 A12-B 10-0 19 A12-B1Ö-C120 A12 -B1Ö-O21 A 12-B 10-0 22 Á 12-B 1.0-0 23 A12-B10-C124 A12-B1Ö-O25 A 12-B .10-0 26 2 5 Á32-B10-CI27 A12-B 10-0 28 Al 2-B 10-029 Á.12-B.1Ö-C130 Á12-810-O3I AI2-B10-032 A12-BI0-O33 . A 12-B 10-0 34 Α12-Β1Θ-Ο35 A12-B10-C136 A12-BI0-C137 Á12-B10-038 A12-B10-C139 A12-BI0-C14Ö BLANK. BLANK BLANK BLANK AI2-B11-O A12-B1LC2 Á12-B1I-C3 A12-BI1-C4 A12-B11-C5 A12-B11-C6 A12-BU-C7 A12-B U-Cg A12-B11-C9 A12-BN -C10 A.12-B11-O1 A12-BL1-CI2 30 A.12-B 11-03 Α12-ΒΠ-Ο4 AI2-B1I-O5 A12-B11-O6 A12-BN-O7 Á12-B11-C1S Α12- ΒΠ-Ο9 Á12-BN--C20 A12-BH-C21 A12-BU-C22 A 12-B Π-03 Á12-B11-C24 A12-B.Í1-C25 AI2-811-Ü26 A12-BH~C2? A12-B11-C28 A12-B11-C29 A12-B1I-C30 A12-B1LC3Í A12-BH-C32 ÁI2~BI1~C33 A12-B11-C34 A12-B11-C35 Á12-B11-C36 AI2-BH-C37 A12- B11-C38 Á12-BH-C39 A12-BÍ1-C40 A12-BN-C41 Á12-B11-C42 35 A12-B1LC43 Á12--B.11-C44 Á12-B.U-C4S AÍ2-BN-C46 AI2-B.11 -C47 A12-B11-C48 AI2-B1I-C49 A12-B11-C50 Ái2~sn-esi A12-B11-C52 A 12-B 11-C53 A12-BN-C54 A12-B11-C55 A12-B 11-C56 AMI 1-C57 Al2-BlI~C5g Α12-Β1.1-C50 A 12-B 1I.-C60 141 Α12-812-061 Α12-ΒΠ-Ο62 A12-811-063 A12-B11-064 Α12-ΒΠ-Ο65 A12--B11-066 A12-B1I-C67 A 12-B 11-063 A12-811-069 A 12 -B 11-070 ΑΙ2-ΒΠ-Ο7Ι AI2-B11-072 A12-Β11-073 A 12-B 11-074 A 12-B 11-075 A12-BH-C76 ΑΙ2-ΒΠ--Ο77 A12-811-078 Á12-BU-C79 A Ϊ 2-818080 A12-BU-C8? A12-BU-C82 A12-B11-083 A 12-B 11-CS4 5 Α13-ΒΠ-Ο85 A12-B11-CS6 A 12-B 11-047 Α12-ΒΠ-Ο8Κ AI2-BJ1-089 A12-8 Π- 090 AI2-BI.1-C9I A 12-B 11-092 Al 2-811-093 A 12-B 11-094 A12-B1I-C95 A 12-B 11-096 Α12-Β11-097 Á12-BII-C9S A12-BI1-099 A! 2-BI1-010C f A12-BÍI-C101 i AI2-BILCI02 A 12-B Π-C l 03 - A12-BÍ1-0104 • A S2-BI1-0105 A12-B1.1-0106 í A12-311-C10 ? A12-B11-0108 A12-BI1-0109 A 12-B 11 -Cl 10 ΑΙ2-ΒΝ-0Π1 Α12-Β11~ΟΠ2 Á12-B1I-C113 ; ΑΙ2-ΒΠ-Ο114 ΙΟ Λ12-ΒΠ-ΟΠ5 A12-BI I-Cl horse A12-811-00? Α12-Β1Ι-ΟΠ8 Α12-ΒΠ-€Π9 A12-8I1-0120 AÍ2-BI 1-012.2 A 12-B 11-0122 A12-811-0123 A12-B1Í-CÍ24 A12-8II-Cl 25 A 12-B 11 -0126 ÁM Π-Cl27 Al 2-811-0128 Α12-ΒΠ-Ο129 A12-B11-0130 A12-BII-C13J A 12-B 11-0232 A12-811-0133 A12-811-0134 A12-811-0135 A 12-B 11-036 Ά12-ΒΙ1-0137 A12-81I-C138 A 12-B 11-0139 A 12-B 11-Cl 40 BLANK BLANK BLANK BLANK 15 Á12-BJ2-C1 A 12-B 12-02 A 12 -B 12-03 Á12-B12-C4 A12-B12-05 A12 822-C6 Α12-Β12-07 A 12-B 12-04 Al 2-8 3 2-09 AI2-B12-C10 Aí 2-812-01 A12-B12-C12 A12-B12-C13 A12-B12-C14 A 12-B 12-015 A 12-B 12-016 A12-B12-C17 A 12-B 12-018 Á12-B12-C19 A 12-B 12-020 A12-8Í2-C21 Á12-B12-C22 A12-B12-C23 A.12-B 12-024 AÍ2-B12-025 A 12-B 12-026 A 12-B 12-02? Al 2-812-028 A12-8I2-C29 A12-B12-C3Ö 20 A12-812-031 A 12-B 12-03 2 Al 2-812-033 A 12-B 12-034 A12-.B 12-035 A 12-B 12-036 A12-BI2-C37 A 12-B 12-038 A12-BI2-C39 A12-812-040 A12-B12-041 A 12-B 12-042 A12-B12-C43 A12-B12- O44 A12-812-045 ÁI2-BI2-C46 A12-B12-C4? A12-812-048 A Π-Β12-049 A 12-B 12-050 A12-B12-C51 A12-812-C52 A12-BI2-C53 A32-BI2-CS4 A 12-8.12-05 5 A12-B12-C56 A12-B12-C5? A 12-B 12-058 AI2-B12-C59 Al 2-812-060 25 A12-B12-C61 Al 2-812-062 A 12-B 12-063 A12-812-064 A12-812-065 A12-8 22-066 A12-B12-C67 A12-BÍ2-C68 A12-B12-C69 A12-B12-C70 A12-B12-O71 A 12-B 12-072 Α22-Β12-073 A 12-B 12-074 A12-B12 -C75 A12-B12-C7Ő A 12-B 12-077 Á1.2-B12-C78 A 12-B 12-079 A 12-B 12-080 A 12-B 12-081 A12-B12-082 A12-B12 -CS3 A 12-B 12-C 84 A12-812-085 Al 2-812-046 A 12-B 12-OS? A 12-B 12-088 A12-812-089 A 12-B 12-090 3D False 2-812-091 A12-812-092 A12-B12-C93 AÍ2-B12-C94 A12-8I2-C95 A12-B12- C96 AU-B12-097 A12-B12-C9S A12-B12-C99 A12-B12-C1ÖÖ A12-BI2-C10I A12-812-0102 False 2-BI2-0103 A 12-B 12-0104 AI2-B12-C105 A12 -B12-OI06 A 12-B 12-CI07 Aí 2-82 2-01Ö8 A.Í2-BI2-C1Ö9 Al 2-812-0 NO A12-B12-C111 AI2-B12-C112 Al 2-812-0113 A12- B12-C114 A12-812-C1 IS A12-B12-C116 A12-B12-C117 A12-812-CI18 A12-B12-0119 A 12-B 12-0120 35 A12-812-0121 Al 24312-0122 Aí 2-812 -0123 A12-B12-C124 A12-812-0125 A 12-B 12-0126 A12-B12-C127 A12-B12-Cl 28 A12-B12-0129 AI2-812-CI30 A12-B12-0131 A12-B12-C132 A. 12-B12-0133 A12-B12-G134 A12-B12-0135 Al 2-812-C136 A12-B12-C137 Á12-BÍ2-C13S A12-812-03' 9 Α12-ΒΓ2-Ο41 ) BLANK A.12-B13-C1 A12-813-02 A12-B13-C3 Á12-B13-C7 A12-813-0 A 12-B 13-09 ΑΙ2- Β 1.3-03 AÍ2-BÍ3-O4 A12-B13-O5 5 Α12-Β13-ΟΓ9 A12-B13-C2Ö A12-B13-C2I Á12-BI3-C25 False 2-813-026 A 12-B 13-027 A12- BI3-C31 Á12-B13-032 A.12-S13 -033 Α12-Β13-037 Át 2-813-033 AMI 3-039 A12-B13-C43 A12-B13-044 A12-B13-C45 10 Α.12- Β .13-049 A12-8Í3-C50 A12-B13-C51 ΑΙ2-Β13-055 A12-BÍ3-C56 A :2-813-057 Α12-Β13-Ο61 A12-B13-C62 A 12-B 13-063 A12 -B13-CÖ7 AI2-B13-O6S A12-813-C69 ' A12-B13-C73 A 12-B 13-074 A12-B13-075 15 A12-B13-C79 A12-813-PIPE AI2-B13-C81 AI2- B13-CS5 A.12-B13-CS6 AI2-BJ3-CS? A12-B13-C91 Al 2-813-092 A 12-B 13-093 A12-BI3-C97 A 12-B 13-098 Á12-813-099 Α12-.Β 13-003 A12-B i 3-004 A12 -B13-OOS 2© A12-BÍ3-O09 Ά12-813-010 Al 2-813-0 Here Α22-Β13-015 A12-B13-C116 Α12-ΒΙ3-ΟΠ7 Al 2-.813-021 Α12-Β13-Ο22 A 12-B 13-0 23 A12-B13-C127 Á12-B .13-028 A12-B13-O29 Α12-Β13-Ο33 Á12-8I3-O34 A12-BD-C135 25 A 12-Β 13-039 A 12 -Β .13-040 BLANK * ♦« X 12 ♦ « * * * ♦ * « X Φ ♦ * « w v ** ** ♦♦'«X * * * X * « 4> « « » write * ♦ V * * «♦ . X BLANK BLANK BLANK A.12-B13-C4 A12-B13-C5 A 12-B .13-06 A12-013-00 ÁI2-B13-CU ÁÍ2-B13-02 A 12-B 13-06 Ά12-813- 07 A 12-B 13-08 A 12-B 13-022 A12-BI3-C23 A12-.B 13-024 A12-B13-C2S Á12-S13-029 A12-B13-C30 A 12-B 13-034 A 12-B 13-035 A12-B13-C36 A 12-B 13-C4Ö A12-B13-C4Í A 12-B 13-042 AI2-BX3-C46 A12-BB-C4? A 12-B 13-048 A12-B'13-052 A12-813-053 A12-B13-C54 A12-BI3-C5S A 12-B 13-059 A 12-B 13-060 Al 2-B13-C64 A12 -B13-C65 A 12-B 13-066 A12-B13-C70 A12-B.13-C71 A 12-B 13-072 A12-BB-C76 A12-B13-C77 A 12-B 13-078 A12-B13 -C82 A12-B13-O83 AI2-813-C84 A12-B13-C88 A12-B13-CS9 A 12-B 1.3-0.90 ΑΓ2-Β13-094 A 12-B 13-095 AÍ2-B13-C96 A12- BH-OOÖ A12-BÍ3-OOÍ AÍ2-B13-002 A 12-B 13-0196 Á.I2-B13-007 A 12-B 13-0 OS A12-B13-O12 A 12-B 1.3-013 A 12- B 13-0:4 A O-B13-018 A I2.-B13-C.lt 9 A12-B13-O20 Α12-ΒΓ3-Ο24 A 12-B Í3-O25 A 12-B 13-Cl 26 A12-B13 -O3Ö A.12-813-031 Á.12-B 13-0 32 A 12-B 13-036 A12-B13-C137 Al 2-813-038 BLANK. BLANK BLANK. for example, & in the list above with the letters A1-E1-C1 is the combination of Ibit compound no. . Preferred compounds according to the invention are: 3-[1-(5-Phenylethynylpyrain-3-carbonyl)-piperidine-1-11>-benzeneamine; 8-[1-(3-Phenylethyl-1-benzoyl)-piperidine-4-yl]-benzylamine; 3-{1-13-H-Hydroxyphenyl}-yl-benzyl]-piperidine-«-ii t-benzylamine; 3-(1-(3-(6-Ansino-pyridin-3-yl)ethyl-benzoyl).-piperidine-4-11}-benzylamine; 3-(1-(S-phenylthiophene-2-carbonyl)-piperidin-4-yl)-henzylamine; 4 - f 1 u o r - 3 -11 - (5 - f s n i 1 e 111 - pi r í d i n - 3 - k a r b ο n i 1) - p i per ídin-4-ii]ben.zí iamin; - n?s t ί 1 - 3 - (' 1 - (5 - f e η ί 1 e t i 1 -pi r i dl. n - 3 - k a r b ο n i 1) - p í p a r i d i n - 4 - i 1 ] -benziiamine; 3-[1-(1ndo1-6 -carbοη11;-p ípe r í d in-4 -11}ben z iIamί n; - (3 - ami neme t i 1 - phen i 15 -1 - (5 - phen ethyl -pyr i d. i n - 3- car bon i 1 ? ~pipe r i din-4-carbonitri1; [4-(3-aminomethylphenyl)piperidine-1-yl-1-(3,1-dicyclophenyl)methanone; ] -methano.il}-3-metii~ s z u 1 f an.il -6,7-dióid r o- 5 H- ben z o (c ] tio f e n - 4 ~ οn-1 r 1 f 1 a o r a c e t á t ; 1-(4-(3-Aminomethylphenyl)-piperidin-1-yl-1-(3-methylsulfonyl-3,7-dihydro-benzo[c]thiophen-yl)-methanone-trifineracetate; i-(1-H~ (3-Aminomethyl-phenyl)-piperidine-1.-ii]-methanoyl? benzo(ej thiophen-4-one trifluoroacetate; i i-{1 - fi- ; 3-ohmometer; - ion! 1) -piperidine--1--.yl 3-mianoii í -3-propylsu I f a n i i - 6,7 - dihydro - 5 H ~b e η. z o f c) t i o f e n - 4 - ο n - t r i £ I uo r a c e t á t; i—) 1—(4-(3-Aminomethyl-phenyl)-piperidin-1-yl]-methanoyl}-3-isopropyl Isulfanyl-6,1-dihydro-SH-benzo [ej t ioien-4 -on---trifluoroacetate; 1- (4- (3-aminomethyl--phenyl)-piper Iden.-1-11 3 ~1-benzol}thiophen-2-yl-1-ethanone-trifluoroacetate; 1-- [4- <3~aminomethyl~phenyl)-4-b.hydroxy-piperidin-1-yl]-1-(o-phenet 1 1 -p lridin ~ 3 -11)- ~metha non- d1 (t r 1 f 1 no r a ce t át); - f 4 - (3-aroinomethyl-phenyl}-piperedene~1-yl}~l-(I-met 11-1H-indcl-3i i)-roe t a non --1 r i f 1 u o r a ce t á t ; 1-[4-(3-Aminomethyl-phenyl)-pyridin-1-yl]-1-[3-(2-chlorophenylethyl-ynyl-phenyl-methanone-trifluoroacetate; i~ (4 ~ C3~ara.inoroethyl-phenyl.yl)-piperid in-1 - yl ] -1- {3- [2- ? 2-Fluoro-phenyl-ethyl]-phenyl-methanone trifluoroacetate; 1-{4-f 3-Arsinomethyl-phenyl}-piperidin-yl-1-[3-(2-(n-amino-pyridin-3-yl)-ethyl]-phenyl}-methanonetri - trifluorocetate; 1-[4-C3-Aminomethylphenyl)piperidin-1-yl]-1-(6-Chloro-thieno{3,2-b11iophen-2-11}-methanone-1-fluoroacetate; • 39,iS) and (3S;4R)-4- C3--aminomethyl-phenyl.>-i-(5-phenethyl-pyridine-3-carboni1)-piperi di n-3-ka rbο n.sa v-e ti1- e s zte r-di hydrochloride; 3-[(5-phenylethylene-furan-2-carbonyl)-piperider-4-yl]-benzylamine trifluoroacetate; 1-1 4 -13-Aminomethylphenyl)piperidene-1-113-1-(2f3-dihydrobenzenetri1-S-11)-methanone; I- f 4 - {3~aroinometí I-phenéi} -püperidin-I~yl 1-1- t 3,6-d.ikiör-pyridine3" 11)··methanone; 1-ί 4 -(3-Aminometh11-phenyl;-piperidin-1-yl-1~{3-bromo-4-fluoro-phenyl)-methanone? 1- [ 4- (3-afflinoroethí 1-phenyl)-piperidine-l-ylj ---1- (3-bromo~5-iodo-pheny 11 ---methanone ? eá-,-— *·;, mtbÁ···'.···-and the corresponding N~oxides and their* prodrugs; and that. the medicinally acceptable salts and solvates of such compounds (for example, h 1 d r á t j a 1.) 6-o / U.v mituprjT^nigyog.. As mentioned above, the compounds of the present invention have valuable pharmacology! have an effect and are accordingly included in medicinal preparations and used in the treatment of patients suffering from certain medical disorders. In accordance with a further aspect of the present invention, compounds according to the invention and pharmaceutical preparations containing compounds according to the invention are provided for use in medicine, where the pharmaceutical preparation according to the present invention contains a compound according to the present invention and a pharmaceutically acceptable carrier. As used herein, the term "medically acceptable" is preferably defined as approved by a regulatory authority of a government, particularly the Federal Government or a state government, or δ. 1. Means what is listed in the pharmacopoeia or other generally recognized pharmacopoeia in the field, especially in humans. Suitable pharmaceutical carriers in S. éh Martin: Remingtons's Pharmaceuticai Sciences' handbook They write it off. The medicinal preparation according to the present invention can be prepared by the usual methods, using one or more pharmaceutically acceptable adjuvants or auxiliary substances. Adjuvants include, but are not limited to, diluents, sterile aqueous media, and various non-toxic organic solvents. .The preparations can be tablets, pills, granules, powders, aqueous solutions or suspensions, injectable: solutions, elixirs or syrups, and can contain one or more agents from the excipients, flavoring agents, coloring agents or stabilizers in order to obtain medicinally acceptable preparations. The choice of the carrier and the content of the active ingredient in the carrier is usually determined by the solubility and chemical properties of the active compound, the given method of administration and the conditions to be taken into account in pharmaceutical practice. For the production of tablets, for example, lactated sodium citrate, calcium carbonate, dicalcium phosphate and disintegrants such as starch, alginic acids and certain complex silicates can be used in combination with lubricants such as magnesium stearate, sodium lauryl sulfate and possibly talc. In the production of capsules, it is advantageous to use lactose and high molecular weight polyethylene glycols. When aqueous suspensions are used, they may contain emulsifiers or agents that promote 3ζυΞζροπ0ό100ήηί. Whereas substances such as sucrose, ethanol, polyethylene glycol, propylene glycol, glycerin and chloroform are mixtures of these! can also be used·. Such gemologically acceptable carriers can be sterile water and oil, including, but not limited to, mineral oil, oil of animal, vegetable or synthetic origin, such as peanut oil, soybean oil, mineral oil, sesame oil and the like. Water is a preferred carrier when the pharmaceutical composition is administered intravenously. Saline and aqueous dextrose and glycerin solutions can also be used as liquid carriers, especially for injectable solutions. Suitable pharmaceutical excipients include mennit, human serum albuman (HSA), starch, glucose, lactose, sucrose, gelatin, malt, rice, flour, chalk, silica, magnesium -carbonate, magnesium stearate, sodium stearate, glyceryl monostearate, taifcum, sodium chloride, skimmed milk powder, glycerin, propylene glycol, water and ethanol. These preparations can be solutions, suspensions, tablets, pills, capsules, powders or sustained-release preparations. A pharmaceutical composition according to the present invention naturally contains an effective diagnostic or therapeutic amount of the active compound with a suitable amount of carrier material to obtain a perfect dosage form for the patient. Although intravenous injection is a very effective form of administration, other routes may be used, such that administration may be by injection or by oral, nasal or parenteral administration, as detailed below. ’y.v > e long j m p. The A' d.ú:i cd. The compounds within the scope of the present invention have tryptase inhibitory properties in the in vitro tests described in the literature and described later, and from these test results we believe that they are related to the pharmacology in rats and other mammals! with activity. In this way, in accordance with a further embodiment, compounds according to the present invention and compositions containing the compounds according to the invention are provided for use in the treatment of patients suffering from or exposed to conditions that can be improved by administration of triplet inhibitors. For example, the compounds of the present invention are suitable for inflammatory diseases such as arthritis, including arthritis, inflammation, rheumatoid arthritis and other joint conditions, such as rheumatic spondylitis, gouty arthritis, traumatic arthritis, rubella arthritis. inflammation, psoriatic arthritis, bony joint inflammation and other chronic inflammatory joint diseases, or porclebomiasis of the joint, psoriatic arthritis, spring conjunctivitis, inflammatory bowel disease, asthma, hay fever, interstitial lung diseases, fibrosis, calluses, pulmonary fibrosis , liver cirrhosis, myocardial fibrosis, neurofibromas, hypertrophic scars, various dermatological conditions, such as atopic dermatitis and psoriasis, heart attack, stroke, angina and other consequences of atherosclerotic plaque rupture, as well as periodontal disease, diabetic retinopathy, tumor growth, anaphyxia, multiple sclerosis , for the treatment of digestive ulcers and sinusoidal viral infections. A special embodiment of the therapeutic methods according to the present invention is the treatment of asthma. The therapeutic methods according to the present invention are another special way of strengthening the treatment of joint inflammations. 1 ΙΟ Another special embodiment of the therapeutic methods according to the present invention is the treatment of inflammatory bowel disease. him > ebsvd 4 According to an additional feature of the Á-aikádaeény', the procedure b«-ti «sáXuak.....for the treatment of a human or animal patient suffering from or exposed to a condition that can be improved by the administration of a trlptase inhibitor, for example, such as the above-described áiíapots. during the process, an effective amount of a chemical according to the invention or a preparation containing a compound according to the invention is administered to the patient. A. effective amount is an amount of the compound according to the present invention that is effective in inhibiting tryptax and thus results in the desired therapeutic effect. KOdÚJA rí n d TFŐáW A As already mentioned above, other medicinally effective agents can be used in combination with the compound according to the invention, depending on the disease to be treated. In the case of asthma treatment, for example, beta-adrenergic agonists, such as albenterol, terbutaline, formoterol, fenoterol or prenalin, as well as anticholinergic agents, such as ipratropium bromide, inflammation and cortical steroids, such as ο n - d. i p r o r 1 o n á t o, triamoinion-acetonide, iinizol time or denamet azent, and anti-inflammatory agents., for example sodium cromogicate and nedocromil sodium can also be included in the preparation, in this way the present invention also covers medicinal preparations , which are a compound according to the present invention and a second compound selected from a beta-adrenergic agonist, an anticholinergic agent, an anti-inflammatory corticosteroid, and an anti-inflammatory agent; and medicine i. contains iag acceptable carrier material *·». The special pharmaceutical carriers that can be used in this medicinal product are listed in the present described below. procedure suitable for the treatment of patients with diabetes, during which the patient is given a compound according to the present invention and a beta-adrenergic agonist, anticholinergic compound, anti-inflammatory agent. We add a second compound chosen from dirt floor solvent or flame retardant. In...
Claims
Patent claims 1. A compound of general formula (I), in which Ar represents an aryl or heteroaryl group, and the group of general formula (a) is attached to the group of general formula (b) in the beta position relative to the group of general formula; --- represents a single or double bond? R1 and Pb represent independently of each other a hydrogen atom or an alkyl group having 1-4 carbon atoms; Pb represents an aryl or heteroaryl group; a represents a hydrogen atom, a halogen atom, an acyl, alkoxy, alkyloxycarbonyl, carboxyl, cyano, hydroxyl group, a group of general formula -C í-Oj -NY1!'2 or an alkyl group, which may optionally be alkoxy, al.wherein Y1 and Y2 are independently hydrogen, alkenyl, alkyl, aryl, arylalkyl, cycloalkyl, heteroaryl, heteroarylalkyl or heterocycloalkyl; or the group of the formula -HYJ / M may form a cyclic amine; r0 is 0 or an integer that is 1 or 2; and n is 2; the y-oxide of the compound, the ester prodrug of the compound, the pharmaceutically acceptable salt of the compound, the solvate of the compound and the hydrate of the compound.
2. The compound of claim 1, wherein Pb and / or ab are hydrogen. ·ί ZÍ < U Ö - 326π m V' 5:
3. The compound of claim 2, wherein R3 is arylsulfur phenyl or naphthyl.
4. The compound of claim 2, wherein Rt is aryl substituted with at least one substituent.
5. The compound of claim 4, wherein the substituent is selected from halogen, aryl-substituted alkyl, aryloxy-substituted alkyl, aryl-substituted alkyl, heteroaryl-substituted alkyl, arylalkynyl, heteroaryl-, arylalkenyl-1- and arylalkyloxy.
6. The compound of claim 5, wherein the aryl group or heteroaryl group of the substituent is further substituted with at least one aryl group substituent selected from acyl, acylamino, alkoxy, alkyloxycarbonyl, alkylenedioxy, alkylsulfinyl, alkylsulfonyl, alkylthio, aro.yl-, aroylamino-, aryl-, arylalkynyl-, arylalkyloxy-, arylalkyloxycarbonyl-, arylalkylthio-, aryloxy-, aryloxyalkyl-, aryloxycarbonyl-, arylsulfonyl-, arylthio-, carboxyl-, cyano group, halogen atom, heteroaroyl-, heteroaryl-, heteroarylalkenal-, heteroarylalkynyl-, heteroarylalkyloxy-, heteroaroylamino-, heteroaryloxy-, heteroaryloxyalkyl-, hydroxyl-, nitro-, trifluoromethyl group, -HÜY'g -CONYÜ2, -SO'zNY'1 Y2, -20-(2-6 carbon alkylene}-NY^Y', ~RY'~(€-0) alkyl, -NYx~SÜ2-alkyl or an alkyl group optionally substituted with alkoxy, aroyl, aryl, aryloxy, heteroaryl, hydroxyl or ~NYÜ2, wherein - 327 2U3J 2* represents an oxygen atom or a group of the general formula S{O)W; Ry represents a hydrogen atom or a C1-C2 alkyl group and m is 0 or an integer that is 1 or 2, 7 . A. The compound of claim 2. wherein the heteroaryl .1 cs ο ρ ort pyridyl-, quinoline-, thienyl-, turaniyl- or indolyl-sweep.
8. The compound of claim 7, wherein the heteroaryl-sweep is substituted with at least one substituent.
9. The compound of claim 8, wherein the substituent is alkyl, aryl-substituted alkyl, aryloxy-substituted alkyl, phenyl-substituted alkyl, heteroaryl-substituted alkyl, arylalkynyl, heteroaryl-, arylalkenyl or arylalkyloxy;.
10. The compound of claim 9, wherein the aryl group of the substituent is further substituted with at least one aryl group substituent selected from the group consisting of acyl, acylamino, alkoxy, alkyloxycarbonyl, alkylenedioxy, alkylsulfinthialalkylsulfonyl, alkylthio, aryl, aroylamino, aryl, arylalkenyl, arylalkynyl, arylalkyloxy, arylalkyloxycarbonyl, arylalkylthio, aryloxy, aryloxyalkyl, aryloxycarbonyl, arylsulfinyl, arylsulfonyl.1-, arylthio-, carboxyl-, cyano group, halogen atom, heteroaroyl-, heteroaryl-, heteroaryl-alkenyl-, heteroarylalkynyl-, heteroarylalkyloxy-, heteroaroylamino-, heteroaryloxy·-, heteroaryl loxyalkyl-, hydroxy.l-, nitro-, trifluoromethyl-swept, -NY1' / 2, -CQNY*Y2, -SCyNY' Y2, -Ά- {2~6 carbon a.'llylene)-·ΝΥχϊ2, ~NY:~ (C=0) alkyl, -NYA-SO2~alkyl 1 group or optionally substituted with alkoxy-, aroyl-, aryl-, aryloxy-, heteroaryl-, hydroxyl group or -NYT group, where 22 is an oxygen atom, NRS or S(0>.m tube.X.·' O- ö / Rt? represents a hydrogen atom or an alkyl group of 1-4 carbon atoms and m is 0 or an integer that is 1 or 2. ü.. The compound of claim 1, wherein represents a single bond.
12. A compound according to claim 1, wherein Ar is phenyl; R3 and Rh' are both hydrogen; R* is hydrogen or cyano; and ~~~ is a bond.
13. The compound of claim 12, wherein Rt is an aryl group substituted with at least one halogen atom, an aryl-substituted alkyl group, an aryloxy-substituted alkyl group, an aryl-substituted alkyl group, an aryloxy-substituted alkyl group, an aryl-substituted alkyl group, an aryl-substituted alkyl group, an aryl-substituted alkyl group, an aryl-substituted alkyl group, an aryl-substituted alkyl group, an arylalkynyl, aryl-, heteroaryl-, arylalkenyl or arylalkyloxy group.
14. The compound of claim 13, wherein the aryl or heteroaryl group in the substituent is further substituted with at least one aryl group substituent selected from the group consisting of acyl, acyl-, aren-, alkoxy, alkyloxycarbonyl, alkylenedioxy, alkylsulfinyl, alkylsulfonyl, alkylthio, aroyl, aroylaroino, aryl, arylalkenyl, arylalkynyl, arylalkyloxy, arylalkyloxycarbonyl, arylalkylthio, aryloxy, aryloxyalkyl, aryloxycarbonyl, arylsulfinyl, arylsulfonyl, arylthio, carboxyl, cyano, halogen atom, heteroaroyl, heteroaryl, heteroarylalkenyl, heteroarylalkynyl, heteroarylalkyloxy, heteroaroyl.a group of the general formula selected from phenyl, heteroaryloxy, heteroaryloxyalkyl, hydroxyl, nitro, trifluoromethyl, -NY1YZ, -CONY'Y'y -SCnNY^Ya -Z2-(C2-6 alkylene) -ΝΥλΥζ, -NY1-(C~ö) alkyl, -NY^-SO-z-alkyl or an alkyl group optionally substituted with an alkoxy, aroyl~, aryl, aryloxy, heteroaryl, hydroxyl group or a group of the general formula -NY1!2, where Zr represents an oxygen atom, a group of the general formula NR or S(0)w; R a represents a hydrogen atom or a C1-4 alkyl group and m is 0 or an integer which is 1 or 2.
15. A compound according to claim 14, wherein the heteroaryl group in R5 is substituted with at least one pyridyl, phenyl, thienyl, furanyl or indolyl group.
16. The compound of claim 15, wherein the heteroaryl group is substituted with at least one aryl-substituted alkyl, aryloxy-substituted alkyl, aryl-swept alkyl, heteroaryl-substituted alkyl, aryl-alkynyl, heteroaryl-alkynyl, heteroaryl-, arylalkenyl, or arylalkyloxy group.
17. A compound according to claim 16, wherein the aryl group of the substituent is further substituted with at least one aryl group substituent selected from the group consisting of aryl, arylamino, alkoxy, alkyloxycarbonyl, alkylenedioxy, alkylsulfonyl, alkylthio, aryl, arylamino, aryl, arylalkenyl, arylalkynyl, arylalkyloxy, arylalkyloxycarbonyl, arylalkylthio, aryloxy, aryloxyalkyl, aryloxycarbonyl, arylsulfonyl, arylthio, carboxyl, chloro, halogen, heteroaroyl, heteroaryl, heteroarylalkenyl, heteroarylalkynyl, heteroarylalkyloxy, heteroaroylamino, heteroaryloxy, heteroaryloxyalkyl, hydroxyl, nitro, trifluoromethyl, -NHYi, -CONY^Y2, -SOsN'HY^, ~íh~ (2-6 carbon alkylene)--ΝΥΛΥώ, ~dY:~ (005 alkyl, -ΝΥΑ-§·ο2•“.alkyl.or an alkyl group optionally substituted with alkoxy, aroyl, aryl, aryloxy, heteroaryl, hydroxylisopropanyl or -NY*Y2, wherein Z2 is an oxygen atom, Nh5 or a group of the general formula 3(0)β; is a hydrogen atom or an alkyl group having 1-4 carbon atoms and m is 0 or an integer which is 1 or 2.
18. a compound according to claim 1, which corresponds to the general formula (la), in which the formula represents a hydrogen atom, a halogen atom, an acyl, an alkoxy, an alkyloxycarbonyl, an aryl, an carboxyl, a cyano, an heteroaryl, an heteroaryloxy, a heterocycloalkyl, a heterocycloalkyl, a heterocycloalkyl, a heterocycloalkyl, a heterocycloalkyl, a heterocycloalkyl, a heterocycloalkyl, a heterocycloalkyl, a hydroxy, a trifluoromethyl group, a ~C(-O;~NYd, -NY'Yy ~2d2~6 carbon alkylene)-R? a group of the general formula or an alkyl group, optionally having the general formula alkoxy, alkylcarbonylamino, alkylsulfonylamine, aryl, heteroaryl, heterocycloalkyl, hydroxyl, ursido, -C(~O)-NYXY2, -SOj-ldYd -S (O1®-alkyl or -idd.substituted with a group; R' is a hydroxyl, alkoxy, nrddoosoport, ddd'Yy -SCdNY'Yy -S;O}„-alkyl or -dd group, Rá is a hydrogen atom or a C 1-4 alkyl group; Y1 and Yz are independently a hydrogen atom, an alkynyl, alkyl, aryl, arylaky!-, cycloalkyl, heteroaryl, heteroarylalkyl or heterocycloalkyl.yl group or the group of the general formula -NYd may form a cyclic amine; d is an oxygen atom, a SCO;- or I4R'° group and m is 0 or an integer that is 1 or 2, or the corresponding N-oxide of the compound, an ester prodrug of the compound, a pharmaceutically acceptable salt of the compound, a solvate of the compound.
19. A compound according to claim 18, which corresponds to the compound of general formula (Ifo). X / / X / V-|:
20. A compound according to claim 10 or 15, wherein the aryl group in Ra is phenyl or naphthyl.
21. The compound of claim 20, wherein the aryl group is substituted with at least one halogen atom, an alkyl group substituted with aryl group, or an alkyl group substituted with a heteroaryl group.
22. The compound of Claim 21, wherein the aryl or heteroaryl substituent of the substituent is further substituted with at least one aryl group substituent selected from the group consisting of acyl, acylamino, alkoxy, alkyloxycarbonyl, alkylenedioxy, alkylsulfinyl, alkylsulfonyl, alkylthio, arylamino, aryl, arylalkenyl, arylalkyl, arylalkyloxy, arylalkyloxy, arylalkyl, arylalkyloxy, arylsulfinyl, arylsulfonyl, arylthio, carboxyl, cyano, halogen, heteroaroyl, heteroaryl, heteroarylalkenyl, heteroarylalkynyl, heteroarylalkyloxy, heteroaroylamino, heteroaryloxy, heteroaryloxyalkyl, hydroxyl, nitro, trifluoromethyl., -ΝϊΑΎζ, -CONY'Y, ~SO?NYY;, ~5h~ (2-6 carbon alkylene) ~xY:Y2, -NY1-(6=0) alkyl, -N'YA~S'02-alkyl group of general formula or optionally substituted by alkoxy, aroil, aryl, aryloxy, heteroaryl, hydroxyl groups or -NY1' / 2 group of general formula selected from the group; where Z2 represents an oxygen atom, NPh or SCO),, group of general formula; represents a hydrogen atom or a 1-4 alkyl group and m is 0 or an integer which is 1 or 2. 33;.
23. A compound according to claim 18 or 19, wherein P is a heteroaryl group selected from pyridyl, quinolinyl, thienyl, furanyl or indyl.
24. The compound of claim 23, wherein the heteroaryl group is substituted with at least one alkyl group substituted with aryl group or an aryl group substituted with a heteroaryl group.
25. The compound of claim 24, wherein the aryl group and the heteroaryl group of the above substituent are further substituted with at least one aryl group substituent selected from acyl, acylamino, alkoxy, alkyloxycarbonyl, alkylenedioxy, alkylene, alkylthio, aroyl, aroylamino, aryl, arylalkenyl, arylalkynyl, arylalkyloxy, arylalkyl, arylalkylthio, aryloxyalkyl, aryloxycarbonyl, arylsulfonyl, arylsulfonyl, arylthio, carboxyl, cyano, halogen, heteroaroyl, heteroaryl, heteroarylalkenyl, heteroariiaikin.il-, heteroar.yl-alkyloxy-, heteroaroylamino-, heteroaryloxy-, heteroaryloxy~ alkyl-, hydroxyl-, nitro-, trifluoro-, -NYXYZ, ~CONY2Y2, -SO>NY:Y2, ~22~(2~6 carbon alkylene)-NY1!'2, -NY1-íC-ö)alkyl, -NYi~SG2-alkyl1 group or optionally substituted by alkoxy-, aroyl-, aryl-, arylcxí-, heteroaryl, hydroxyl- or <0 group selected from alkyl group, where 2r represents an oxygen atom, or a group of the general formula S(Ojr.; 3S represents a hydrogen atom or a C1-4 alkyl group and b / m is 0 or an integer that is 1 or 2.
26. A compound according to claim 18 or 1.9, wherein is phenyl(C1-C3 alkyl)pyridyl, phenyl(C1-C3 alkyl)thienyl or indole.
27. A compound according to any one of claims 1, 18, or 19, wherein Rb is hydrogen or cyano.
28. A compound according to claim 18 or 19, wherein Pb is hydrogen, C1-C4 alkyl or halogen.
29. The compound of claim 28, wherein R5' is methyl or fluorine.
30. The compound of claim 28, wherein Pb is attached to the phenyl ring in the para-position relative to the -CH2KH2 group, 31. A compound according to claim 18 or 19, wherein Pb is a phenyl group; a naphthyl group; a heteroaryl group selected from pyridyl, quinolinyl, thienyl, furanyl or indole group; a phenyl group substituted with at least one substituent, a naphthyl group substituted with at least one substituent; or a heteroaryl group selected from pyridyl, quinolinyl, thienyl, furanyl or indole group substituted with at least one substituent, wherein the substituent is a halogen atom, an aryl-substituted alkyl group, an heteroaryl-substituted alkyl group, wherein the aryl or heteroaryl group is substituted with one or more aryl group substituents; Ia represents an oxygen atom, RRS or a group of the general formula S(GjK); Rd represents a hydrogen atom or an alkyl group having 1-4 carbon atoms and m is 0 or an integer which is 1 or 2. Pl represents a hydrogen atom or a cyano group; and c, R represents a hydrogen atom, an alkyl group having 1-4 carbon atoms or a halogen atom, 32. The compound of claim 31, wherein R5 is selected from the group consisting of (1-3 C alkyl) pyridyl, phenyl (1-3 C alkyl) thienyl or indole; R4 is hydrogen or cyano; and P4 is methyl or fluorine, and is attached to the phenyl ring in the para-position with respect to the -C1-bNH2 group. 331 The compound of claim 26, wherein the phenyl (1-3 C alkyl) pyridyl is o-phenylethyl pyrid-3-yl, the phenyl (1-3 C alkyl) thienyl is 5-phenylethyl thien-2-yl and the indole is ei nd ο I - 6 - i 1 - c ε o po r t.
34. Az 1. igénypont szerinti vegyűlet, applied 3-{1- (C-phenietinii-pyridin-é-carbonyl) -piperidin-4-yl]:-benz.ilamine; 3 - (1- (3-phenylethyl 1-phoenzoyl í -piperidin-4-yl'j; -benzylaraine; 3~{I~[3- (4-hydroxy phenyl.) ethyl-benzol 1 ] -piperidin-4-iI} -benzylaraine; ethyl1-benzoylj -piperidin-4-yl} - -benzylamine 3- (1 — (5~phenylethyl-thiophene-2~carbon.íi) -piperidin-4-yl} -benzylamib; 4-met.i 1-3- (1- (5-phenylethyl-pyridine-3~carboniI; -piper.idin-4-iI ] -be nz.yl amine; 3- [1- (indo-6-carbon.yl) -piper.idin~4-yl ] ~benz.ylamine; pheneti 1 - pyridine ~ 3 - car bon i 1 ? -raetanoil}-3—.raetils zu 1 fan 1 - 6, 7 - d í hydro - 5 H - be η zo [ c ] thiophene - 4 - on -trifluoroacetate? 1 - f 4 -- (3-aroinome of 1 - feni 1) -piper idin~Ii 1) -1 - [3 -metii s zni fant 1-6, 7-dihydro-benzo[ejthiofen-l~yl)-methanene-trifluoroacetate; 1-f 1- [4 - (3-aminemethyl-phenyl / -piperidin-l-yl] -methanol 1) -3—et.ylsulfanyl-6, 6-diraet.yl-6, 7-dinihydro-5H-benzene[cj thiophene-4-on-trifIuoracetate; 1-{1- [4- (3-aminomethyl-phenyl / -piperidin-i-yl] -methanoyl )-3-propyl z η 1 fan 11 - 6,7 - d ih i dr o-~ 5 H - benze· fc 31 iofen --- 4 - ο n -1 rif I uoracet á t; 1-f1-[4-(3-aminomethyl-phenyl}-piperidine-i-ylj-methanoyl}-3-isopropylsulfanyl-6, 7-dihydro-SH-benzo [ej thiophene-4-on-trifluoroacetate; 11 -1 - be η zo [ b ] tio .phen-2-yl methanone erythrioacetate; 1-[4-[3-aminomethylphenyl)-1-hydronipiperidin-1-yl]-1-(5-phenethylpyridin-3-yl)-methanone di(trifluoroacetate); 1-H~(3-Aminomethyl-phenyl}-piperidin-1-yl]-i-(1-methyl-1H-indol-3yl}-methanone trifluoroacetate; 337 1- (4~ (3-AminoBethyl-phenyl)-piperidin-1-yl)-1- (3- (2-fluoro-phenyl-ethynyl)-phenyl]-methanone-trifluoroacetate; 1- [4-(3-Aminomethyl~.phenyl)-piperidin-1-yl]-1-(3-(2-(2-fluorophenyl)-ethyl]-phenyl}-methanone-trifluoroacetate,* I"H~ (3-aminomethyl-phenyl)-piperidin-yl]-1- { 3-(2- (6-Amino-pyridin-3-yl)-ethyl]-phenyl}-methanone-tri-trifluoroacetate; 1-[4-(3-aminomethylphenyl)-piperidin-1-yl]-1-(6-chlorothieno[3,2-b]thiophene-2-yl)-methionine trifluoroacetate; <3R, 4S) and (3S, 4R)-4-(3-aminomethylphenyl)-1-(5-phenethylpyridine-3-carbonyl)-piperidine-3-carboxylic acid ethyl ester dihydrochloride; 3-(1-{5-phenylethynylfuran-2-chlorophenyl)-piperidin-4-yl]-benzylamine trifluoroacetate; 1-[4-(3-aminomethylphenyl)-piperidin-1-yl]-1-(2,3-di.hydrobenzonitrile-5-yl)methanone; 1-(4-(3-a.minorofcii~f.eniX)-piperidin-1-yl]-1-(5,β-dichloropyridine3-ii)-methanone; -piperidln-1-ii]-1-(3-bromo-5~iodo--phenyl.)-methanone.
35. A pharmaceutical composition comprising a compound according to claim 1 or 34 and a pharmaceutically acceptable carrier. 36 < A 35. igénypont szerinti gyógyaszati készítmény, ahol. a vegulet 3 - (1 - (5 - í eni 1 etini 1 -p i. r í d in- 3 - carbon 1} -piperid n - 4 -· £ 1} -benzoyl 1 amine; 3- [1- (3-phenii-benzoyl) -piperioin-4-yl] -benz [1-3-3-I; (4-hi.droxiphenii) ethyl-foenzoíl] -piperid.in-4-yl}-phoenzylamine 3“ (1- (3- .(.6~amino~pic.idin~.3-yl jetyl-benzoyl}~piperidín-4“yl} -benzylamine; a. 1) - piperid ί n - 4 - i 1] - fo e η z 11 arai n; 4-raetiI-3-[1-(5-pheniiietii~pyridin-3-carbcnyl}~piperidin-4-yl]ne nziz ama.n; 3- [i~ (indole-6-carbonyl}-piperidin-4-yl] -benzylaraine; 4- (3-arainaraethyl-phenyl) -1- (5~phenethii-pyridine~3~carboraii) -piperidine-4-carbonitrium; (4-(3 -arainoraethyphenyl-3)-pyridine; 4-dichlorophenyl)methanone; -piperi.din-I-ii] -1- í3-methylsulfanyl-6, 7-dihydro-benzo pho]thiophene-I-ii; ssulfanyl-6,6-dimethyl~€,7-diphohydro-SH-benzo(c)thiophene-4-on-tri.f Iuoracetate l-{ 1 — (4- ( 3~aminomethy.I-phen.í;l)-piperidin-l-yl] -methenoy}-3'-propyl~ szültani 1-6,7-dinidro-5H~benzo[o]thiophene-4~en-trifIuoracetate; 1-(1-(4 -(3-arainometii-pheni1)-piperidin-l-yl]-raetanoyl}-3~isopropylszuifani 1-6, l-dihydro-SH-benzo[c] thiof en-4-on-t rif iuoracetáte ; -l-bsnzc(b] thiofen-2~.ilrae ta η ο n -1 ri £ 1 uoracet át ; luoracetát) ; -(3-aminometii-pheni!)-piperidin-l-yl]-1-[3-(2-fluor-phenylethynyl)-phenyl1-methane-trifluoracetáte; 1™[i~(3-aminomethyl-phenyl)-piperidin-i-il]~I~{3-[2-(2-fInor-phenyi)-ethylj-phenyl}-methenon-trifluoracetáte 1—(4 — (3-am;inomethyl-phenyl)-piperidin-1-yl]-1-(3-[3-{6-amino-pyridin-3-yl)-ethyl]-phenyl}-methanone-tri-trifluoroacetate; 1-[4-(3-aminomethyl-phenyl)-piperidin-1-yl]-1-(6-chloro-thieno[3,2-b]thiophen-z-yl)-methanone-trifluoroacetate; (32,43) and (3S,4R)-4·· (3-aminomethyl-phenyl)-1-(5-phenethyl-pyridine-3-carbonyl}-piperidine-3-carboxylic acid ethyl ester dihydrochloride; 3-[1-(5-phenylethynyl-furan-2-carbonyl)-piperidin-d-yl]-benzylamine trifluoroacetate; 4-(3-aminomethyl-phenyl)-piperidine-1-carboxylic acid (3,4-dichloro-phenyl)-amide trifluoroacetate; 1-[4-(3-aminomethyl-phenyl)-piperidin-1-yl]-1-(2,3-dihydro-benzonitrile-5-yl)-methanone; 1-(4-(3-aminomethyl-phenyl}-piperidin-1-yl)-1-(5, 6-dichloro-pyridin-3-yl)-methanone; 1- (4-(3-aminomethyl-phenyl'-piperidin-1-yl)-1-(3-bromo-4-fluoro-phenyl}-methanone; 1- [4-yl-aminomethyl-phenyl)-piperidin-1-yl]-1-(3-bromo-5-iodo-phenyl)-methanone.
37. A pharmaceutical composition comprising a compound according to claim 18 or 13 and a pharmaceutically acceptable carrier. '1') ύ ο r\ S 38. Use of the compounds of any one of Claims 1, 18, 19 or 34 for the preparation of pharmaceutical compositions for the treatment of conditions ameliorated by the administration of tryptase inhibitors.
39. The use of claim 38, wherein the condition is an inflammatory disease, a degenerative joint disease, conjunctivitis, vernal conjunctivitis, inflammatory bowel disease, asthma, hay fever, interstitial lung disease, fibrosis, sclerosis, pulmonary fibrosis, liver cirrhosis, myocardial fibrosis, neurofibroma, hypertrophic scar, dermatological condition, arteriosclerotic plaque-related condition, periodontal disease, diadema retinopathy, turbidity, anaphylaxis, multiple sclerosis, peptic ulcer or sinusitis viral infection. 45 A 39.The use according to claim 1, wherein the inflammatory disease is arthritis, arthrosis, rheumatoid arthritis, rheumatoid spondylitis, gouty arthritis, traumatic arthritis, rubella arthritis, psoriatic arthritis or osteoarthrosis, the dermatological condition is atopic dermatitis or psoriasis; and the condition associated with atherosclerotic plaque rupture is myocardial infarction, stroke or angina.
41. A pharmaceutical composition comprising a compound according to any one of claims 1, 18, 19 or 34 and a second compound selected from a beta-adrenergic agonist, an anticholinergic, an anti-inflammatory corticosteroid and an anti-inflammatory agent, and a pharmaceutically acceptable carrier.
42. The pharmaceutical composition of claim 41, wherein the beta-adrenergic agonist is albuterol, terbutaline, tormoterol, fenoterol, or prenaline; the anticholinergic agent is ipratropium bromide; the anti-inflammatory corticosteroid is beclometasone dipropionate, triamcinolone acetonide, flunisolide, or dexamethasone; and the anti-inflammatory agent is sodium cromoglicate or nedocromil sodium.
43. Use of a compound according to any one of claims 1, 18, 19 or 34 and a second compound selected from a beta-adrenergic agonist, an anticholinergic, an anti-inflammatory corticosteroid and an anti-inflammatory agent for the preparation of a pharmaceutical composition for the treatment of asthma.