Abstract: The present invention provides modified amino acids for delivering active agents, and particularly biologically or chemically active agents. The preferred modified amino acids of the present invention include N-acylated or sulfonated amino acids. These modified amino acids are used as carriers to facilitate the delivery of a cargo to a target. Such modified amino acids are well suited to form non-covalent mixtures with biologically-active agents for oral administration to animals. Methods for the preparation and administration of the modified amino acids and compositions including the same are also provided.

Abstract: A sulfur-containing amino acid compound having a high inhibitory activity on LTA.sub.4 hydrolase which is represented by the following formula: ##STR1## wherein R.sup.1 represents H, alkyl, optionally substituted phenyl alkyl, alkanoyl or optionally substituted benzoyl; R.sup.2 represents ester, amide or carboxyl; R.sup.3 represents hydroxyl, alkyl, halogenoalkyl, alkoxy, halogenoalkoxy, alkylthio, optionally substituted phenyl, optionally substituted phenoxy, optionally substituted phenylthio, halogen atom, alkylsulfonyl, halogenoalkylsulfonyl, nitro or cyano; R.sup.4 represents alkyl; A.sup.1 represents alkylene; and A.sup.2 represents alkylene.

Abstract: Compounds of formula (I) ##STR1## and their pharmaceutically acceptable salts inhibit matrix metalloproteases, such as stromelysin, gelatinase, matrilysin and collagenase, and are useful in the treatment of mammals having disease-states alleviated by the inhibition of such matrix metalloproteases.

Abstract: Molecular mimetics of unique epitopes of Neisseria meningitidis serogroup B ("MenB") are disclosed. Compositions containing such molecular mimetics can be used to prevent MenB or E. coli K1 disease without the risk of evoking autoantibody responses.

Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are .alpha.v.beta.3 antagonists, .alpha.v.beta.5 antagonists or dual .alpha.v.beta.3/.alpha.v.beta.5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, viral disease, and tumor growth.

Abstract: The phenylalkan(en)oic acids of the formula: ##STR1## as defined herein, posses an antagonistic activity on leukotriene B.sub.4.

Abstract: The present invention has as subject compounds of formula: ##STR1## in which Y is C.sub.2 H.sub.5, (CH.sub.3).sub.2 CH or (R) CH(OH)CH.sub.3, and R" is (S) CH(C.sub.2 H.sub.5)C.sub.6 H.sub.5, (S) CH(CH.sub.3)C.sub.6 H.sub.5 or (R) CH(CH.sub.2 OCH.sub.3)C.sub.6 H.sub.5. These compounds are useful as sweetening agents.

Abstract: A compound represented by general formula (I) or a pharmaceutically acceptable salt or ester thereof: [wherein each of Ar.sup.1, Ar.sup.2, Ar.sup.3 and Ar.sup.4 is an aryl group or an aromatic heterocyclic group; A.sup.1 is a C.sub.2-6 chain hydrocarbon group or a group represented by --A.sup.1a --W.sup.1 --A.sup.1b -- (wherein W.sup.1 is an oxygen atom, a sulfur atom, an ethynylene group, a cyclopropylene group or a group represented by --NR.sup.W --; A.sup.2 is a C.sub.2-8 chain hydrocarbon group; each of X and Y is an oxygen atom, a sulfur atom, a carbonyl group or a group represented by --CHR.sup.a -- or by --NR.sup.b --, or X and Y together represent a vinylene group or an ethynylene group; each of R.sup.1, R.sup.2, R.sup.3, R.sup.7 and R.sup.8 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group, a lower alkenyl group or a lower alkoxy group; each of R.sup.4 and R.sup.

Abstract: Novel dipeptide derivatives, such as N-3,3-dimethylbutyl-.alpha.-L-aspartyl-.alpha.-methyl-L-phenylalanine methyl ester and N-3,3-dimethylbutyl-.alpha.-L-aspartyl-.alpha.-methyl-L-tyrosine methyl ester, and sweetening agents comprising, as the active ingredient, anyone of the derivatives and their salts, being low-calorie sweetening agents which are excellent in stability, safety and degree of sweetness, are provided. The products to have been sweetened, comprising such above sweetening agents are also provided.

Abstract: Novel aspartyldipeptidoamides and salts thereof. The apartyldipeptides are useful as a low-calorie sweetener for food and beverage products and have excellent taste and chemical stability.

Abstract: The present invention provides the compound having the structure: ##STR1## wherein each of R.sub.1 and R.sub.2 are independently the same as or different from each other; when R.sub.1 and R.sub.2 are the same, each is a substituted or unsubstituted arylamino, cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine, or thiozoleamino group; when R.sub.1 and R.sub.2 are different, R.sub.1 =R.sub.3 --N--R.sub.4, wherein each of R.sub.3 and R.sub.4 are independently the same as or different from each other and are a hydrogen atom, a hydroxyl group, a substituted or unsubstituted, branched or unbranched alkyl, alkenyl, cycloalkyl, aryl, alkyloxy, aryloxy, arylalkyloxy, or pyridine group, or R.sub.3 and R.sub.4 bond together to form a piperidine group and R.sub.2 is a hydroxylamino, hydroxyl, amino, alkylamino, dialkylamino or alkyloxy group; and n is an integer from about 4 to about 8.

Abstract: The present invention relates to a compound of the formula (I): ##STR1## wherein Ar.sup.1, Ar.sup.2, Ar.sup.3 and Ar.sup.4 represent an aryl group or a heteroaromatic ring group; A represents a hydrocarbon group which may be substituted; X and Y represent an oxygen atom, a sulfur atom, a carbonyl group or a group of the formula --CHR.sup.a -- (wherein R.sup.a is a hydrogen atom or a lower alkyl group) or --NR.sup.b -- (wherein R.sup.b is a hydrogen atom or a lower alkyl group), or X and Y together represent a vinylene group or an ethynylene group; R.sup.1, R.sup.2, R.sup.3, R.sup.8 and R.sup.9 represent a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a lower alkoxy group; R.sup.4 and R.sup.

Abstract: The present invention relates to pyrrolidine derivatives, and more particularly to the compound (S)-1-?(S)-2-(4-methoxybenzamido)-3-methylbutyryl!-N-?(S)-2-methyl-1-(trif luoroacetyl)propyl!pyrrolidine-2-carboxamide, shown by formula I, and solvates thereof. The present invention also provides pharmaceutical compositions, intermediates and methods of preparation of the compound. The compound of formula I is an inhibitor of human neutrophil elastase and is useful in the treatment of diseases in which the enzyme is implicated, such as, for example, emphysema and acute respiratory distress syndrome (ARDS).

Abstract: A new type of yellow dyes with general formula Q-CO--CO--X is disclosed. They can be used in photographic materials as antihalation dyes, acutance dyes or filter dyes. Preferably they are incorporated in UV sensitive contact materials for pre-press applications.

Abstract: Mesogens are provided based on substituted unsaturated carboxylic acids such as acrylic and methacrylic acid. Substitution of a variety of hydrophobic tails onto the carboxylic acid or acid derivative via the vinyl carbon proximal to the carbonyl of the carboxylic acid results in mesogens that are capable of forming thermotropic and single-phase lyotropic mesophases over a broad range of compositions. The mesophases can be polymerized to lock in the ordered phases.

Abstract: A process for the preparation of disodium Z-L-aspartate from fumaric acid, in whicha) fumaric acid is reacted with ammonia in an inert diluent in the presence of aspartase or aspartase-producing microorganisms to give ammonium L-aspartate thenb) the ammonium L-aspartate-containing solution is treated with sodium hydroxide, forming, depending on the amount of sodium hydroxide used, the mono- or disodium L-aspartate or a mixture thereof, andc) the eliminated ammonia is returned to a fumaric acid suspension, which is used as starting solution for further enzymatic reactions, and thend) the residual mono and/or disodium L-aspartate-containing solution is reacted with benzyloxycarbonyl chloride at a pH of between 9 and 14, with the simultaneous addition of sodium hydroxide, to form disodium Z-L-aspartate.

Abstract: Methods of use for compounds of formula (I) are described wherein R represent a --CONHOH, carboxyl (--CO.sub.2 H) or esterified carboxyl group; R.sup.1 represents a hydrogen atom or an optionally substituted alkyl, alkenyl, aryl, aralkyl, heteroaralkyl or heteroarylthioalkyl group; R.sup.2 represents an optionally substituted phenylethyl, phenylpropyl or phenylbutyl group; R.sup.3 represents a hydrogen atom or an alkyl group; R.sup.4 represents a hydrogen atom or an alkyl group; R.sup.5 represents an optionally substituted alkyl or alkenyl group optionally interrupted by one or more --O-- or --S-- atoms or --N(R.sup.7)-- groups (where R.sup.7 is a hydrogen atom or a C.sub.1-6 alkyl group); X represents an amino (--NH.sub.2), or substituted amino, hydroxyl or substituted hydroxyl group; and the salts, solvates and hydrates thereof.

Abstract: A process and intermediates for preparing .alpha.

Abstract: The present invention provides a compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof, which are useful for inhibiting protein farnesyltransferase and the farnesylation of the oncogene protein Ras or inhibiting de novo squalene production resulting in the inhibition of cholesterol biosynthesis, processes for the preparation of the compounds of the invention in addition to intermediates useful in these processes, a pharmaceutical composition, and to methods of using such compounds.

Abstract: A compound according to the formula: ##STR1## and conjugates thereof.

Abstract: Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have the generalized formula: ##STR1## wherein T is a substituent and R.sup.24 is a substituted amide moiety. These compounds are useful for inhibiting matrix metalloproteases and, therefore, combating conditions to which MMP's contribute, such as osteoarthritis, rheumatoid arthritis, septic arthritis, periodontal disease, corneal ulceration, proteinuria, aneurysmal aortic disease, dystrophobic epidermolysis, bullosa, conditions leading to inflammatory responses, osteopenias mediated by MMP activity, tempera mandibular joint disease, demyelating diseases of the nervous system, tumor metastasis or degenerative cartilage loss following traumatic joint injury, and coronary thrombosis from athrosclerotic plaque rupture. The present invention also provides pharmaceutical compositions and methods for treating such conditions.

Abstract: Novel aspartyldipeptideamide derivatives of formula (I):L--Asp--X--NH--C*HR.sub.1 R.sub.2and salts thereof, wherein X is a D-.alpha.-amino acid residue or a DL-.alpha.-amino acid residue selected from the group consisting of D-alanine, D-.alpha.-aminobutyric acid, D-norvaline, D-valine, D-norleucine, D-leucine, D-isoleucine, D-alloisoleucine, D-t-leucine, D-serine, D-O-methylserine, D-threonine, D-O-methylthreonine, D-allothreonine, D-O-methylallothreonine, D-phenyl glycine and D- or DL furyl glycine, or X is a cyclic or non-cyclic .alpha., .alpha.-dialkyl amino acid residue having 3 to 6 carbon atoms; R.sub.1 is a linear or branched alkyl group having 1 to 6 carbon atoms or an alkoxymethyl group having 2 to 7 carbon atoms in the alkoxy portion; R.sub.

Abstract: A process for preparing polymeric amides is disclosed. The process comprises sequentially reacting a hydrocarbon polymer functionalized (e.g., via the Koch reaction) to contain acid, ester, thioacid and/or thioester groups with a heavy polyamine to form a partially derivatized product in which at least about 85% of the functional groups are converted to heavy (thio)amide groups, and then reacting the partially derivatized product with an excess of light amine to complete the derivatization by converting substantially all of the remaining functional groups to light (thio)amide groups. Products of the foregoing process are also disclosed, which products are useful as additives in fuels and in lubricants.

Abstract: The present invention has as subject compounds of formula: ##STR1## in which Y is C.sub.2 H.sub.5, (CH.sub.3).sub.2 CH or (R) CH(OH)CH.sub.3, and R" is (S) CH(C.sub.2 H.sub.5)C.sub.6 H.sub.5, (S) CH(CH.sub.3)C.sub.6 H.sub.5 or (R) CH(CH.sub.2 OCH.sub.3)C.sub.6 H.sub.5. These compounds are useful as sweetening agents.

Abstract: Compounds of the formula A--B--C--D(--E).sub.p are used to stimulate the release of growth hormone from the pituitary.

Abstract: Amine compound derivatives enhancing the transdermal delivery (skin penetration) of pharmacologically active substances (drugs). In order to pass through the skin more effectively, the present invention provides derivatives that are soluble or miscible, or compatible with both lipids and water. These derivatives are formed by combining a drug of the amine class (to which most drugs belong) with a lipid-soluble long-chain acid such as oleic, linoleic, stearic, myristic, or palmitic acid.

Abstract: This invention relates to a method of stereoselective preparation of a derivative of .beta.-phenylisoserine of formula (I) by the action of an N-carbonyl-benzylimine of formula (II) on an optically active amide of a protected hydroxyacetic acid of formula (III), followed by hydrolysis of the product obtained. In formula (I), (II) or (III), R is an optionally substituted phenyl radical or R.sub.1 --O, Ar is an optionally substituted aryl radical and G.sub.1 is a hydroxy function protection grouping. The product of formula (I) is particularly useful in preparing taxol and Taxotere which have remarkable antitumor properties.

Abstract: Aspartyldipeptide compounds of the formula (I)L-Asp-X-NH-C*R.sub.1 R.sub.2 (I)where R.sub.1 is alkyl or alkoxymethyl, R.sub.2 is phenyl, benzyl, cyclohexyl or cyclohexylmethyl, C* has an (S) configuration when R.sub.1 is alkyl and an (R) configuration when R.sub.1 is alkoxymethyl and X is a residue of a D-.alpha.-amino acid, a DL-.alpha.-amino acid or a residue of a cyclic or acyclic .alpha.,.alpha.-diallylamino acid and the bond between L-Asp and X is an .alpha.-bond; and their use as active ingredients in sweetener compositions.

Abstract: Novel trienoic compounds having activity for retinoic acid receptors and retinoid X receptors are provided. Also provided are pharmaceutical compositions incorporating such compounds and methods for their use.

Abstract: A compound of the formula ##STR1## wherein Q is an organic group of at least two carbon atoms having at least m substituents,m is 1, 2, 3, 4, 5 or 6, andn is 0 or 1.R.sup.3 is H or methyl,R.sup.8 and R.sup.9 are independently hydrogen, alkyl group or aryl,R.sup.12 and R.sup.13 are independently selected from the group consisting of an alkyl group or a cation, andR.sup.10 is independently selected from the group consisting of hydrogen, an alkyl group, aryl group, and highly-fluorinated alkyl group,R.sup.4 may be hydrogen or alkyl group, andR.sup.7 may be hydrogen or lower alkyl group, provides excellent stability to dispersions.

Abstract: This invention is directed to compounds having the structure: ##STR1## wherein R.sub.1 and R.sub.2 are independently the same as or different from each other; when R.sub.1 and R.sub.2 are the same, each is a substituted or unsubstituted arylamino, cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine or thiazoleamino group; when R.sub.1 and R.sub.2 are different, R.sub.1 =R.sub.3 --N--R.sub.4, and n is an integer from about 4 to about 8. This invention also provides a method of selectively inducing terminal differentiation of neoplastic cells and thereby inhibiting proliferation of such cells. The invention further provides pharmaceutical compositions comprising a therapeutically effective amount of the compounds of the present invention and a pharmaceutically acceptable carrier.

Abstract: Diethylenetriaminepentaacetic acid monoamide derivatives, their complexes and complex salts, containing an element of atomic numbers 21-29, 31, 32, 39, 42-44, 49 or 57-83, pharmaceutical agents containing these compounds, their use as contrast media and process for their production.

Abstract: Stilbene compounds of the following formula (I) or their pharmaceutically acceptable salts are effective as carcinostatics and of low toxicity: ##STR1## wherein X represents a hydrogen atom or a nitrile group, and Y represents an amino acid acyl group.

Abstract: Novel Carboxy-peptidyl compounds of Formula I are found to be useful inhibitors of matrix metalloendoproteinase-mediated diseases including osteoarthritis, rheumatoid arthritis, septic arthritis, tumor invasion in certain cancers, periodontal disease, corneal ulceration, proteinuria, dystrophobic epidermolysis bullosa, coronary thrombosis associated with atherosclerotic plaque rupture, and aneurysmal aortic disease. The matrix metalloendoproteinases are a family of zinc-containing proteinases including but not limited to stromelysin, collagenase, and gelatinase, that are capable of degrading the major components of articular cartilage and basement membranes. The inhibitors claimed herein may also be useful in preventing the pathological sequelae following a traumatic injury that could lead to a permanent disability. These compounds may also have utility as a means for birth control by preventing ovulation or implantation.

Abstract: The present invention relates to compounds containing an oxamic acid group, which show high reactivity and have stability for water and are used as paints, adhesives, and plastic materials etc. in the form of a reaction material or a resin. Since into these compounds an oxamic acid group is introduced in a part of the molecule and the oxamic acid group is an ionic functional group, the compounds show superior solubility and dispersing character in water and also, since the oxamic acid group is a group of a disappearing type with heating, the compounds do not remain, after hardening, in the hardened product. Accordingly, the hardened products obtained from these compounds are superior in water-resistant and anticorrosion properties and in durability.

Abstract: Modified amino acid compounds useful for the delivery of active agents are provided. The amino acids, non-alpha-amino acids, have been modified by acylation on the amino group particularly with phenyl or cyclohexyl groups. These groups have a variety of substituents including but not limited to hydroxy, methyl, fluoro, chloro, and the like. The compounds of the invention can be combined with numerous active agents including but not limited to heparin, peptides, and parathyroid hormone, and can then be used for effective administration of the active agent. Administration can be, for example, oral or parenteral.

Abstract: The present invention relates to a compound of the formula (I): ##STR1## wherein Ar.sup.1, Ar.sup.2 and Ar.sup.3 represent an aryl group or a heteroaromatic ring group; A represents a hydrocarbon group which may be substituted; Q represents a group of the formula --(CH.sub.2).sub.m -- (m is an integer of from 1 to 6) or --(CH.sub.2).sub.n --W--(CH.sub.2).sub.p -- (W is an oxygen atom, a sulfur atom, a vinylene group or an ethynylene group; n and p are a integer of from 0 to 3); R.sup.1 represents a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group, a lower alkoxy group, an aryl or heteroaromatic ring group which may be substituted; R.sup.2, R.sup.7 and R.sup.8 represent a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a lower alkoxy group; R.sup.3 and R.sup.

Abstract: Modified amino acid compounds useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.

Abstract: Novel organic compounds and metal ion-containing amino acid chelates are described which are useful in solid phase synthesis of polypeptides and as magnetic resonance imaging (MRI) enhancing agents. The present invention also relates to a convenient and straightforward method to synthesize a metal-ligating amino acid suitable as MRI enhancing agents or for introducing a strong metal binding site at any chosen position in a peptide. Some compounds are designed to be compatible with N-.alpha.-Fmoc peptide synthesis strategy, and can easily be prepared on large scale. Thus, flexible linkers of different lengths and containing various structures can be placed between the .alpha.-carbon backbone of peptides and metal binding moieties. These peptides will provide a variety of affinity cleaving reagents which can be directed against protein or nucleic acid targets. Therefore, these molecules can serve as an important tool to study protein folding, protein-protein and protein-nucleic acid interactions.

Abstract: The present invention provides a method of preparing L-aspartyl-D-.alpha.-aminoalkane carboxylic acid-(S)-N-.alpha.-alkylbenzylamide which is less expensive and more efficient than previous methods using N-protected-L-aspartic anhydride.

Abstract: Amino acid derivatives of formula (Ia) and (Ib) and prodrugs thereof containing a group responsible for chelating the zinc atom of enkephalinase and angiotensin convertase enzymes are disclosed as inhibitors of these enzymes.

Abstract: The present invention relates to substantially pure piperidine derivative compounds of the formulae: ##STR1## wherein R.sub.1 is hydrogen or hydroxy;R.sub.2 is hydrogen;or R.sub.2 and R.sub.2 taken together form a second bond between the carbon atoms bearing R.sub.1 and R.sub.2 ;R.sub.3 is --COOH or --COOR.sub.4 ;R.sub.4 has 1 to 6 carbon atoms;A, B, and D are the substituents of their respective rings each of which may be different or the same and are hydrogen, halogens, alkyl, hydroxy, alkoxy, or other substituents.A process of preparing such piperidine derivative compounds in substantially pure form is also disclosed.

Abstract: Novel antagonists of endothelin are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, acute and chronic renal failure, hypertension, myocardial infarction, metabolic, endocrinological, neurological disorders especially cerebral vasospasm, stroke, and head injury, congestive heart failure, endotoxic shock, subarachnoid hemorrhage, arrhythmias, asthma, preeclampsia, atherosclerotic disorders including Raynaud's disease, restenosis, angina, cancer, pulmonary hypertension, ischemic disease, gastric mucosal damage, hemorrhagic shock, ischemic bowel disease, and diabetes.

Abstract: The present invention relates to compounds that can maintain, increase, or restore sensitivity of cells to therapeutic or prophylactic agents. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well-suited for treatment of multi-drug resistant cells, for prevention of the development of multi-drug resistance, and for use in multi-drug resistant cancer therapy.

Abstract: Disclosed are compounds of Formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof, wherein: R.sup.3 is alkyl, alkenyl, alkynyl, aryl, alkaryl, aralkyl, cycloalkyl, acyloxymethyl, alkoxy, alkoxymethyl, or alkyl substituted with cycloalkyl;R.sup.4 is H, alkyl, alkenyl, alkoxy, or --OH.Also disclosed are pharmaceutical compositions containing compounds of Formula I, methods for inhibiting tumor necrosis factor-.alpha. and methods for treating septic shock, inflammation, or allergic disease by administering a compound of Formula I.

Abstract: This disclosure relates to a novel class of hydroxamic and carboxylic acid based matrix metalloproteinase inhibitor derivatives. The disclosure further relates to pharmaceutical compositions containing such compounds and to the use of such compounds and compositions in the treatment of matrix metalloproteinase induced diseases.

Abstract: A process and catalyst composition are provided for the highly efficient enantioselective hydrogenation of dehydroamino acid derivatives. The catalyst composition comprises rhodium or iridium and a diphosphinite carbohydrate ligand, wherein the phosphorous atoms are attached to aromatic groups substituted with electron-donating substituents. Also provided is a means to selectively produce .alpha. amino acids in either the L or the D form, based upon use of a sugar in the ligand with phosphinites attached in an absolute Right-Left or Left-Right configuration, respectively.

Abstract: An N-acylamino acid compound represented by the general formula (1):R--CO--(NH--X--CO).sub.n --OR.sup.1 (1)wherein (NH--X--CO) is an amino acid residue, X in (NX--X--CO) is variable with the kind of amino acid to be used, R--CO is a saturated or an unsaturated fatty acid residue having 6 to 24 carbon atoms, R.sup.1 is hydrogen atom, sodium atom, potassium atom, or methyl group and n is an integer in the range of from 1 to 3, indicating that at least one histidine is contained as a component amino acid is disclosed, which is obtained by causing an N-hydroxysuccinimide ester to react with an amino acid or a peptide.The compound excels in antioxidizing power, emulsifying power, antibacterial power, chelating power, infrared absorbing power, and humidity-retaining power.

Abstract: A compound of the formula (I) or its pharmaceutically acceptable salt or ester: ##STR1## wherein each of the substituents are herein defined.

Abstract: Stable crystals of N-(trans-4-isopropylcyclohexylcarbonyl)-D-phenylalanine may be produced by treating this compound with a solvent at a temperature of at least 10.degree. C. and forming crystals in the solvent at a temperature of at least 10.degree. C. For example, crystals may be formed by crystallization out of solution, or may be formed from solid particles of the compound suspended in a solvent. Crystals formed in this way have different melting point, infra red spectrum and X-ray diffraction patterns from previously known forms of the compound and have enhanced processability, eg. stability to grinding.