Abstract: One embodiment of the present invention is a compound represented by the Structural Formula (I): Y is a covalent bond of a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C═Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R7R8)—. R1 is an aliphatic group, a substituted aliphatic group, a non-aromatic heterocyclic group, or a substituted non-aromatic heterocyclic group, R2-R4 are independently —H, an aliphatic group, a substituted aliphatic group, a non-aromatic heterocyclic group, a substituted non-aromatic heterocyclic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring.

Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.

Abstract: A method for the inhibition of high affinity glycine transporters, compounds that inhibit these transporters; pharmaceutically active compositions comprising such compounds; and the use of such compounds either as above, or in formulations for the control or prevention of disease states in which glycine is involved are disclosed.

Abstract: Disclosed is a compound represented by the Structural Formula (I): 1

Abstract: The novel compounds of formula (I), wherein R1, R2, R2′, R2″, R3, R4, R5, R5′, R5″, R5′″, R″″, X, Y, U, V and W have the meanings given in patent claim no. 1, are inhibitors of the coagulation factors Xa and VIIa and can be used for treating thromboses, myocardial infarction, arteriosclerosis, inflammations, apoplexy, angina pectoris, restenosis following angioplasty, intermittent claudication, tumours, tumour diseases and/or tumour metastases.

Abstract: Process for producing a nitroetheneamine derivative or its stereoisomer, its tautomer or a salt thereof comprising reacting a compound of the formula with a compound of the formula R6—CH2NO2 to obtain a compound of the formula and reacting the resulting compound with a compound of the formula

Abstract: The present invention is directed to carbocyclic hydrazino compounds that function as inhibitors of copper-containg amine oxidases commonly known as semicarbazide-sensitive amine oxidases (SSAO), including the human SSAO known as Vascular Adhesion Protein-I (VAP-1). These SSAO inhibitors have therapeutic utility as drugs to treat conditions and diseases including, but not limited to, a number of inflammatory conditions and diseases (in particular chronic inflammatory conditions such as chronic arthritis, inflammatory bowel diseases, and chronic skin dermatoses), diseases related to carbohydrate metabolism and to aberrations in adipocyte differentiation or function and smooth muscle cell function, and vascular diseases.

Abstract: Disclosed is a compound represented by the Structural Formula (I): 1

Abstract: Novel derivatives of 1-aminoindan and their salts are described. Optically active 1-aminoindan derivatives are prepared by reacting a N-benzyl analog of the desired compound with an enantiomer of mandelic acid.

Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.

Abstract: Novel anthranilic acid derivatives having an inhibiting activity of cGMP-PDE are represented by the formula I where A is a lower alkylene group: 1

Abstract: The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.

Abstract: Salicylohydrazide derivatives of the formula I in which the index and the substituents have the following meanings: X is halogen, NO2, cyano, alkyl or alkoxy; m is 0, 1, 2 or 3, it being possible for the substituents X to differ from each other if n is greater than 1; R1 is NO2, NH2 or NH—CO—A; A is hydrogen, alkyl, alkoxy, NH2, NHCH3 or N(CH3)2; R2 is hydrogen, cyano, alkyl, alkenyl, alkynyl, haloalkyl, alkoxy or alkylthio; it being possible for the hydrocarbon radicals to be unsubstituted or substituted, R3 is phenyl, naphthyl, cycloalkyl, 5-membered or 6-membered hetaryl or 5-membered or 6-membered heterocyclyl containing one to three N atoms and/or one O or S atom or one or two O and/or S atoms, the ring systems being unsubstituted or substituted; the preparation of these compounds, compositions comprising them, and their use for controlling harmful fungi.

Abstract: A medical composition containing, as an active constituent, a nitroetheneamine derivative represented by the formula (I): wherein the substituents are as defined in the disclosure, its stereoisomers, its tautomers or a salt thereof.

Abstract: The present invention relates to novel, non-peptidic small organic compounds having an affinity for cyclophilin (CyP)-type immunophilin proteins. In the compounds of this invention, at least two carbo- or heterocyclic groups are attached to a central saturated, partially saturated, or aromatic 5-6 membered carbocyclic ring by a combination of straight or branched linker chains. The invention further relates to pharmaceutical compositions comprising one or more of the said compounds, and to the uses of these compounds and compositions for binding CyP-type proteins, inhibiting their peptidyl-prolyl isomerase activity, and for research, development, and therapeutic applications in a variety of medical disorders, such as neurological disorders, hair loss disorders, ischemic disorders, and disorders caused by viral or protozoan infection.

Abstract: Process for the preparation of symmetrical diacylhydrazines having general formula (I): R1—CO—NH—NH—CO—R1 wherein R1 represents a linear or branched C1-C18 alkyl group; a linear or branched C2-C8 alkoxyalkyl group; a C2-C8 cyanoalkyl group; a C5-C8 cycloalkyl group, said cycloalkyl group optionally containing a heteroatom selected from oxygen, nitrogen and sulfur; a C6-C18 aryl group; a C7C20 arylalkyl group or alkylaryl group, said arylalkyl or alkylaryl groups optionally substituted with one or more hydroxyl groups, or with one or more linear or branched C1-C8 alkoxyl groups; comprising: (a) reacting an ester of a carboxylic acid having general formula (II): R1—CO—OR2 wherein R1 has the same meanings defined above and R2 represents a linear or branched C1-C18 alkyl group, with hydrazine, in its pure or hydrated state, obtaining a monoacylhydrazine having general formula (III): R1—CO—NH—NH2; (b) reacting the monoacylhydrazine having general formula

Abstract: A method for the inhibition of high affinity glycine transporters, compounds that inhibit these transporters; pharmaceutically active compositions comprising such compounds; and the use of such compounds either as above, or in formulations for the control or prevention of disease states in which glycine is involved are disclosed.

Abstract: The present invention provides a method for producing a hydrazine derivative of the formula [2]: wherein R1 is alkyl group having 1-12 carbon atoms and the like, R2 is alkyl group having 1-12 carbon atoms and the like, and Ar is phenylene group and the like, from a hydrazone derivative of the formula [1] wherein R1, R2 and Ar are as defined above, in the presence of at least one base selected from the group consisting of an organic base and an inorganic base, and a metal hydrogenating catalyst. By this method, reduction proceeds selectively and a hydrogenolysis reaction (side reaction) can be suppressed.

Abstract: Salicylic acid derivatives of the formula I, 1

Abstract: The present invention relates to a hydrazine oxoacetamide derivative or its salt which exhibits an excellent insecticidal effect even at a low concentration.

Abstract: There is disclosed a complex and a combination of the glycosylated polypeptide fetuin and a therapeutically active small molecule compound having a net positive charge at physiological pH. The presence of fetuin as a drug complex or in combination with the therapeutically active small molecule compound enhances therapeutic activity of the small molecule compound. The present invention further provides a means for screening for therapeutically active small molecule compounds by means of binding to fetuin.

Abstract: A method is provided for the transition metal-catalyzed arylation, or vinylation, of hydrazines, hydrazones, and the like. Additionally, the invention provides a conceptually novel strategy, the cornerstone of which is the transition metal-catalyzed arylation or vinylation method, for the synthesis of indoles, carbazoles, and the like. The methods and strategies of the invention may be utilized in standard, parallel, and combinatorial synthetic protocols.

Abstract: Novel derivatives of 1-aminoindan and their salts are described. Optically active 1-aminoindan derivatives are prepared by reacting a N-benzyl analog of the desired compound with an enantiomer of mandelic acid.

Abstract: Hydrazine derivatives of the formula wherein Y is CO or SO2; R1 is lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl or aryl-lower alkyl; R2 is lower alkyl, halo-lower alkyl, aryl-lower alkyl, aryl-lower alkenyl or aryl when Y is SO2 and is lower alkyl, halo-lower alkyl, lower alkoxy, lower alkoxycarbonyl, acyl, lower cycloalkyl, aryl, aryl-lower alkyl, aryl-lower alkoxy or NR5R6 when Y is CO; and R3 is hydrogen, lower alkyl optionally substituted by cyano, amino, hydroxy, lower alkoxy, lower alkoxycarbonyl, heterocyclyl or heterocyclylcarbonyl, lower alkenyl, lower alkynyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl-lower alkyl, aryl-lower alkenyl, aryl or heterocyclyl; or R2 and R3 together form the residue of a 5-, 6- or 7-membered cyclic amide, cyclic imide, cyclic sulphonamide or cyclic urethane group; R4 is lower alkyl, hydroxy-lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl or a group of the formula X-aryl, X-heteroar

Abstract: Benzamides of the formula I: wherein R1 and R2 independently of one another are each alkyl having 1-6 C atoms, or R1 and R2 together are alkylene, and their salts, are suitable as intermediates in the synthesis of drugs.

Abstract: Compounds of formula (I): R—NH—A—CO—NH—NH—(W)n—Z  (I) wherein: n is 0 or 1, W represents —CO— or S(O)r wherein r is 0, 1 or 2, Z represents a group selected from aryl, arylalkyl, heteroaryl and heteroarylalkyl, each optionally substituted, R represents a grouping selected from: Z1—T—CO—, Z1—O—T—CO—, Z1—T—O—CO—, Z1—T—S(O)q— wherein Z1, T and q are as defined in the description, A represents alkylene, alkenylene or alkynylene each having from 3 to 8 carbon atoms, alkylenecycloalkylene, cycloalkylenealkylene, alkylenecycloalkylenealkylene, alkylenearylene, arylenealkylene, alkylenearylenealkylene a grouping wherein B1 is as defined in the description, or A forms with the adjacent nitrogen atom a grouping as defined in the description, and medicinal products containing the same which are useful as Neuropeptide Y receptor

Abstract: This invention provides a convenient process for the preparation of monoacylhydrazines from carboxylic acids or their salts and hydrazine or substituted hydrazine in the presence of a 1,3,5-triazine substituted with at least one chloro or fluoro. The resulting monoacylhydrazine can further be converted to a diacylhydrazine by effectively either repeating the reaction or through reaction with a carboxylic acid chloride.

Abstract: Neuroprotective drugs are disclosed with at least 3 branches extending outwardly from a center atom or group, each branch having a guanidino group at its terminus. All branches preferably should be identical, and distributed around the center atom or group in a radial manner. Three branches can be bonded to a nitrogen atom, or four branches can be coupled to a carbon atom; other center groups include stable aromatic, cycloalkyl, heterocyclic, or bicyclic structures. Starting reagents are disclosed with a center atom or group, and with reactive groups (such as primary amines or hydroxyl groups) at the ends of short "spacer chains" bonded to the center atom or group. Reagents derived from arginine (an amino acid having a terminal guanidino group) can be bonded to these center components, using protective groups on the arginyl reagents to ensure desired final products with accessible guanidino groups at the ends of spacer chains.

Abstract: This invention provides novel reagents for the preparation of radiopharmaceuticals useful as imaging agents for the diagnosis of cardiovascular disorders, infection, inflammation and cancer, diagnostic kits comprising said reagents and intermediate compounds useful for the preparation of said reagents. The reagents are comprised of stable hydrazone modified biologically active molecules that react with gamma emitting radioisotopes to form radiopharmaceuticals that selectively localize at sites of disease and thus allow an image to be obtained of the loci using gamma scintigraphy.

Abstract: A silver halide photographic material is disclosed containing a new type of hydrazide compound represented by following general formula I, the different symbols of which are defined in the description. ##STR1## In a preferred embodiment Q is pyridinium, substituted with a propargyllic group or butynyl group.The photographic material is preferably a graphic arts recording material. High gradation and excellent hard dot quality are obtained.

Abstract: A hydrazine compound represented by the following formula (I):Ar.sub.1 --NH--NH--G.sub.1 --R.sub.1 (I)wherein Ar.sub.1 represents an aromatic group; G.sub.1 represents a carbonyl group, a sulfonyl group, a sulfoxy group, a phosphoryl group, an oxalyl group or an iminomethylene group; R.sub.1 represents a hydrogen atom or a block group; and at least one of Ar.sub.1 and R.sub.1 has a group represented by the following formula (II): ##STR1## wherein * represents a bond for connecting directly or through a liking group to Ar.sub.1 or R.sub.1 ; Z represents a nonmetallic atom group capable of forming a 5- or 6-membered unsaturated heterocyclic ring having a conjugated positive charge; and X.sup.- represents --O.sup.-, --S.sup.- or --N.sup.- --R.sub.2, wherein R.sub.2 represents an alkyl group, an alkenyl group, an alkynyl group, an aryl group or a heterocyclic group. Also disclosed is a silver halide photographic light-sensitive material containing the hydrazine compound.

Abstract: An .alpha.-hydrazino acid derivative of general formula (I) is described, wherein R.sub.1, R.sub.2, R.sub.3 are hydrogen or a carbon radical, such that when R.sub.2 and R.sub.3 are different, C* is an asymmetric carbon of L, D or DL configuration, and R.sub.4 and R.sub.5 are a protecting group, characterized in that R.sub.4 is a benzyl ArCH.sub.2 radical of formula (a), wherein Ar is a phenyl radical or phenyl substituted by one or more X groups; X being hydrogen, halogen, a nitro or alkyl radical; and in that R.sub.5 is a Y--O--CO group, where Y is a carbon radical different from R.sub.4.

Abstract: The disclosure describes new compositions of matter useful for the preparation of optically-active vicinal aminoalcohols. The compositions are chiral .beta.-hydroxycarboxamides, .beta.-hydroxyhydraxides, and .beta.-hydroxyhydroxamic acids.

Abstract: A heterocyclic aromatic halide or an aryl halide is reacted with an amine compound in the presence of a base to give a heterocyclic aromatic amine or an arylamine, respectively. In this reaction, a catalyst comprising a palladium compound and a tertiary phosphine is used for the preparation of a heterocyclic aromatic amine, and a catalyst comprising a palladium compound and a trialkylphosphine is used for the preparation of an arylamine.

Abstract: The invention relates to a novel process for the preparation of compounds of formula I ##STR1## wherein R.sub.1 is hydrogen or a suitable amino-protecting group,R.sub.2 is unsubstituted or substituted alkyl,R.sub.3 is hydrogen, aryl, heterocyclyl, unsubstituted or substituted alkyl or unsubstituted or substituted cycloalkyl,R.sub.4, independently of R.sub.1, is hydrogen or a suitable amino-protecting group andm is a number from 1 to 7; and wherein further suitable protecting groups for functional groups may be present; which compounds are antivirally active or can be used as starting materials for pharmaceutically active, especially antiviral compounds.

Abstract: Novel monoamine oxidase B inhibitors of formula (I), wherein R.sub.1 .dbd.H, an optionally substituted benzyloxy or phenylethoxy group; p=0-3; R.sub.3 .dbd.H, a CN, OH, CCH group, a C.sub.1 -C.sub.3 alkoxy-carbonyl group, or a C.sub.1 -C.sub.3 alkylated cyanomethyl group; R.sub.2 .dbd.H or a C.sub.1 -C.sub.3 alkyl group; n=0 or 1; if n=0, R.sub.4 is a C.sub.1 -C.sub.3 alkyl group or a C.sub.1 -C.sub.3 alkoxy group, while if n=1, y=1 and R.sub.4 is a C.sub.1 -C.sub.3 alkyl group, a C.sub.1 -C.sub.3 alkoxy group or a phenyl group. The invention also concerns processes for the preparation of said novel inhibitors and the therapeutic use thereof.

Abstract: A process for selectively monoacylating monoalkylhydrazines by reacting such with trichloromethyl aryl ketones.

Abstract: This invention concerns new methods and compositions that are useful in preventing and ameliorating cachexia, the clinical syndrome of poor nutritional status and bodily wasting associated with cancer and other chronic diseases. More particularly, the invention relates to aromatic guanylhydrazone (more properly termed amidinohydrazone) compositions and their use to inhibit the uptake of arginine by macrophages and/or its conversion to urea. These compositions and methods are also useful in preventing the generation of nitric oxide (NO) by cells, and so to prevent NO-mediated inflammation and other responses in persons in need of same. In another embodiment, the compounds can be used to inhibit arginine uptake in arginine-dependent tumors and infections.

Abstract: A process for producing a hydrazide of the formula: ##STR1## is disclosed. The process comprises reacting a hydrazone of the formula: ##STR2## wherein said hydrazone is in toluene, with a mixture of Grignard reagents, wherein said Grignard reagents are in a suitable organic solvent; wherein: (A) Z is a suitable carbonyl protecting group; (B) R is a suitable --OH protecting group; (C) R.sup.1 is selected from: H, a non-enolizable alkyl, a non-enolizable substituted alkyl, aryl, substituted aryl, --S-aryl, --S-(substituted aryl), --S-alkyl, --S-(substituted alkyl), alkoxy, substituted alkoxy, aryloxy, or substituted aryloxy; (D) said mixture of Grignard reagents comprises R.sup.2 MgX in admixture with R.sup.3 MgX; (E) R.sup.2 is a suitable alkyl, substituted alkyl, alkenyl, alkynyl, aryl, substituted aryl, or aralkyl group capable of adding to the --C.dbd.N group of the hydrazone to produce the hydrazide; (F) R.sup.

Abstract: This application relates to a process for selectively monoacylating hydrazines by reacting unsubstituted or monoalkylhydrazines with trichloromethyl aryl ketones.

Abstract: The present invention can provide a process for the preparation of an 1-acyl-2-substituted hydrazine compound from a mixture containing the 1-acyl-2-substituted hydrazine and an 1-acyl-1-substituted hydrazine by selective hydrolysis or alcoholysis of the 1-acyl-yl-1-substituted hydrazine in the presence of an acid catalyst, and by separation of the resulting carboxylic acid and derivative thereof.The 1-acyl-2-alkyl hydrazine obtained has a high purity.

Abstract: This invention concerns new methods and compositions that are useful in preventing and ameliorating cachexia, the clinical syndrome of poor nutritional status and bodily wasting associated with cancer and other chronic diseases. More particularly, the invention relates to aromatic guanylhydrazone (more properly termed amidinohydrazone) compositions and their use to inhibit the uptake of arginine by macrophages and/or its conversion to urea. These compositions and methods are also useful in preventing the generation of nitric oxide (NO) by cells, and so to prevent NO-mediated inflammation and other responses in persons in need of same. In another embodiment, the compounds can be used to inhibit arginine uptake in arginine-dependent tumors and infections.

Abstract: Compounds having the structural formula ##STR1## wherein R is C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkyl; R.sup.1 is fluorenyl, thienyl, pyridyl or thiazolyl, unsubstituted or substituted by one or more substituents selected from C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkylthio, halogen, C.sub.1 -C.sub.4 haloalkyl and nitro; and R.sup.2 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.1 -C.sub.6 haloalkyl, C.sub.2 -C.sub.6 alkenyl, or C.sub.2 -C.sub.6 alkoxyalkyl. The compounds of this invention are effective for controlling mites and nematodes.

Abstract: A process for the asymmetric hydrogenation of N-acylhydrazones to optically active N-acylhydrazines in the presence of a chiral phospholane catalyst complex, a process for the reductive N--N bond cleavage of N-acylhydrazine to amines with samarium diiodide, and a multistep process for converting keto group-bearing compounds to the corresponding optically active amino group-bearing compounds are disclosed.

Abstract: A process for the asymmetric hydrogenation of N-acylhydrazones to optically active N-acylhydrazines in the presence of a chiral phospholane catalyst complex, a process for the reductive N--N bond cleavage of N-acylhydrazine to amines with samarium diiodide, and a multistep process for converting keto group-bearing compounds to the corresponding optically active amino group-bearing compounds are disclosed.

Abstract: Oxalyl hydrazide-hydroxamic acid derivatives of the formula I ##STR1## where the substituents have the following meanings: R, R.sup.1, R.sup.2 and R.sup.3 independently of one another arehydrogen, substituted or unsubstituted alkyl, alkenyl or alkynyl orsubstituted or unsubstituted cycloalkyl or cycloalkylmethyl,substituted or unsubstituted cycloalkenyl or cycloalkenylmethyl,substituted or unsubstituted phenyl, phenylalkyl, phenylalkenyl, hetaryl- or hetarylalkyl radicals, where R.sup.2 and R.sup.3 may also. together with the nitrogen atom whose substituents they are, form a 5- or 6-membered ring, orR.sup.2 together with R.sup.3 is the group ##STR2## where R.sup.4 and R.sup.5 are one of the radicals R, R.sup.1, R.sup.2 or R.sup.3, or R.sup.4 together with R.sup.5 and the carbon atom whose substituents they are, are monocyclic or polycyclic cycloalkyl, orR.sup.4 together with R.sup.5 and the carbon atom whose substituents they are, form a 5- or 6-membered, saturated heterocycle containing O, S or --N(R.sup.

Abstract: Disclosed are a novel azide compound represented, for example, by the formula, ##STR1## wherein R.sub.f represents a fluoroalkyl or fluoroalkylpolyether group, ##STR2## wherein R represents a divalent organic group having an ester bond, and R.sub.f ' represents a fluoroalkylpolyether group, and a novel diacylhydrazine compound having a fluoroalkylpolyether group in the side chain and lubricants containing them. When this lubricant is coated onto the carbonaceous protective film of magnetic recording media and reacted by the action of light or heat, it strongly bonds or adheres to the protective film. Thus, the durability of the lubricant improves, as a result of which a high-density magnetic recording medium having a high reliability and long life can be obtained.

Abstract: The present invention relates to compounds exhibiting central nervous system (CNS) activity which are useful in the treatment of epilepsy and other CNS disorders. The compounds of this invention have the following general formula: ##STR1## and pharmaceutically acceptable salts thereof.

Abstract: Compounds having the structural formula ##STR1## where X, Y, R and Z are defined in the specification are disclosed. The compounds of this invention are effective for controlling mites, nematodes, rice planthopper, tobacco budworm, and southern corn rootworm. Methods for making these compounds are also set forth.

Abstract: Bifunctional chemicals useful for linking aldehyde containing moieties to moieties containing functionalities which are or can be reactive with sulfhydryl are claimed and have the formula:L--S--(CH.sub.2).sub.n1 --CONH--SPACER--NH--XwhereinL is a leaving group selected from --H or --S--Ar, wherein Ar represents optionally substituted phenyl or pyridyl;n.sub.1 =2-4;X is selected from: ##STR1## wherein Y is alkylene or oxaalkylene and Z is alkylene or a polypeptide residue briding the N-terminal amino group and C-terminal carboxy group thereof;the SPACER is oxaalkylene or oxaalkylene substituted with hydroxyl and specifically includes residues having formulas selected from--(CH.sub.2).sub.n2 --O--(CH.sub.2).sub.n2 --O--(CH.sub.2).sub.n2 --a)wherein each n2 is independently 2-4 and ##STR2## wherein n3 is 2-6. Also claimed are hydrazides, semicarbazides, and thiosemicarbazides of .omega.-mercaptocarboxylic acids which lack SPACER diamine.